RU2011116111A - Сульфонилсодержащие соединения, которые селективно модулируют рецептор св2 - Google Patents
Сульфонилсодержащие соединения, которые селективно модулируют рецептор св2 Download PDFInfo
- Publication number
- RU2011116111A RU2011116111A RU2011116111/04A RU2011116111A RU2011116111A RU 2011116111 A RU2011116111 A RU 2011116111A RU 2011116111/04 A RU2011116111/04 A RU 2011116111/04A RU 2011116111 A RU2011116111 A RU 2011116111A RU 2011116111 A RU2011116111 A RU 2011116111A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- hydrogen
- cycloalkyl
- group
- ring
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract 14
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical class O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 20
- 239000001257 hydrogen Substances 0.000 claims abstract 20
- 229910052736 halogen Inorganic materials 0.000 claims abstract 12
- 150000002367 halogens Chemical class 0.000 claims abstract 12
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 10
- -1 C1-C4-acyl Chemical group 0.000 claims abstract 9
- 125000001424 substituent group Chemical group 0.000 claims abstract 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 8
- 229910052799 carbon Inorganic materials 0.000 claims abstract 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 8
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims abstract 7
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 7
- 125000003118 aryl group Chemical group 0.000 claims abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 6
- 125000004043 oxo group Chemical group O=* 0.000 claims abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 3
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims abstract 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims abstract 2
- 125000002950 monocyclic group Chemical group 0.000 claims abstract 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 8
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 8
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 7
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000002393 azetidinyl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004276 dioxalanyl group Chemical group 0.000 claims 2
- 125000000532 dioxanyl group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 208000004998 Abdominal Pain Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 206010058019 Cancer Pain Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000002881 Colic Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 208000023178 Musculoskeletal disease Diseases 0.000 claims 1
- 206010051606 Necrotising colitis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000001294 Nociceptive Pain Diseases 0.000 claims 1
- 206010037660 Pyrexia Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 208000025747 Rheumatic disease Diseases 0.000 claims 1
- 208000005392 Spasm Diseases 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 208000030961 allergic reaction Diseases 0.000 claims 1
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 208000010643 digestive system disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000030172 endocrine system disease Diseases 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 230000027950 fever generation Effects 0.000 claims 1
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 208000007565 gingivitis Diseases 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 210000003714 granulocyte Anatomy 0.000 claims 1
- 238000001631 haemodialysis Methods 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 230000000322 hemodialysis Effects 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 208000017445 musculoskeletal system disease Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000004995 necrotizing enterocolitis Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000000626 neurodegenerative effect Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 230000008816 organ damage Effects 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 201000006195 perinatal necrotizing enterocolitis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 230000035939 shock Effects 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000003685 thermal hair damage Effects 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 5
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 0 CC(C)(COC(C(C)(C)S(CCCC(*)(*)*)(=O)=O)=O)c1n[o]c(NC(C)=O)c1 Chemical compound CC(C)(COC(C(C)(C)S(CCCC(*)(*)*)(=O)=O)=O)c1n[o]c(NC(C)=O)c1 0.000 description 4
- MQKSLQXGEPJSNF-UHFFFAOYSA-N CC(C(C)(C)c1cc(NC(C(C)(C)SCC2CCOCC2)=O)n[o]1)O Chemical compound CC(C(C)(C)c1cc(NC(C(C)(C)SCC2CCOCC2)=O)n[o]1)O MQKSLQXGEPJSNF-UHFFFAOYSA-N 0.000 description 1
- VYIFDHJKQMISLP-UHFFFAOYSA-N CC(C(C)(C)c1n[o]c(NC(C)=O)c1)O Chemical compound CC(C(C)(C)c1n[o]c(NC(C)=O)c1)O VYIFDHJKQMISLP-UHFFFAOYSA-N 0.000 description 1
- SFJQFVZDSPCNRI-UHFFFAOYSA-N CC(C)(C(Nc1cc(CCCCO)n[o]1)=O)S(C1CCOCC1)(=O)=O Chemical compound CC(C)(C(Nc1cc(CCCCO)n[o]1)=O)S(C1CCOCC1)(=O)=O SFJQFVZDSPCNRI-UHFFFAOYSA-N 0.000 description 1
- RZMKLFLXXZBKFM-UHFFFAOYSA-N CC(C)(C)Cc1nc(cc(cc2)S(C(C)(C)C(Nc3cc(C(C)(C)CO)n[o]3)=O)(=O)=O)c2[n]1CC1CC1 Chemical compound CC(C)(C)Cc1nc(cc(cc2)S(C(C)(C)C(Nc3cc(C(C)(C)CO)n[o]3)=O)(=O)=O)c2[n]1CC1CC1 RZMKLFLXXZBKFM-UHFFFAOYSA-N 0.000 description 1
- XJWCJJBZNUACLA-UHFFFAOYSA-N CC(C)(CO)c1n[o]c(NC(C)=O)c1 Chemical compound CC(C)(CO)c1n[o]c(NC(C)=O)c1 XJWCJJBZNUACLA-UHFFFAOYSA-N 0.000 description 1
- NTPWVCZBXWZNIJ-UHFFFAOYSA-N CC(C)(COC(C)=O)c1n[o]c(NC(C(C)(C)S(C2CCOCC2)(=O)=O)=O)c1 Chemical compound CC(C)(COC(C)=O)c1n[o]c(NC(C(C)(C)S(C2CCOCC2)(=O)=O)=O)c1 NTPWVCZBXWZNIJ-UHFFFAOYSA-N 0.000 description 1
- FVJUJAFOBDEYDE-UHFFFAOYSA-N CC(C)(COC(C)=O)c1n[o]c(NC(C(C)(C)SC2CCOCC2)=O)c1 Chemical compound CC(C)(COC(C)=O)c1n[o]c(NC(C(C)(C)SC2CCOCC2)=O)c1 FVJUJAFOBDEYDE-UHFFFAOYSA-N 0.000 description 1
- JRUWIZDZHRGRLW-UHFFFAOYSA-N CC(C)C(Nc1cc(C(C)(C)COC(C)=O)n[o]1)=O Chemical compound CC(C)C(Nc1cc(C(C)(C)COC(C)=O)n[o]1)=O JRUWIZDZHRGRLW-UHFFFAOYSA-N 0.000 description 1
- UIGQZFWDSKZUCL-UHFFFAOYSA-N CC1(c2n[o]c(NC(C)=O)c2)OCCC1 Chemical compound CC1(c2n[o]c(NC(C)=O)c2)OCCC1 UIGQZFWDSKZUCL-UHFFFAOYSA-N 0.000 description 1
- FFEDFQSEXJCCFG-UHFFFAOYSA-N CCCC(C)(C)c1n[o]c(NC(C(C)(C)SC2CCOCC2)=O)c1 Chemical compound CCCC(C)(C)c1n[o]c(NC(C(C)(C)SC2CCOCC2)=O)c1 FFEDFQSEXJCCFG-UHFFFAOYSA-N 0.000 description 1
- WHBKOWSSGOJYPP-UHFFFAOYSA-N CC[n]1nc(NC(C(C)(C)S(C2CCOCC2)(=O)=O)=O)nc1-c(cc1)ccc1OC Chemical compound CC[n]1nc(NC(C(C)(C)S(C2CCOCC2)(=O)=O)=O)nc1-c(cc1)ccc1OC WHBKOWSSGOJYPP-UHFFFAOYSA-N 0.000 description 1
- JMDMOXQXKMYZJX-PXYINDEMSA-N C[C@@H](C(C)(C)c1n[o]c(NC(C(C)(C)SCC2OCCOC2)=O)c1)O Chemical compound C[C@@H](C(C)(C)c1n[o]c(NC(C(C)(C)SCC2OCCOC2)=O)c1)O JMDMOXQXKMYZJX-PXYINDEMSA-N 0.000 description 1
- FICAQKBMCKEFDI-UHFFFAOYSA-N Cc1n[o]c(C)c1 Chemical compound Cc1n[o]c(C)c1 FICAQKBMCKEFDI-UHFFFAOYSA-N 0.000 description 1
- MPBPVACPFBSAFW-UHFFFAOYSA-N Cc1n[s]c(C)n1 Chemical compound Cc1n[s]c(C)n1 MPBPVACPFBSAFW-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D249/14—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/14—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
Abstract
1. Соединение формулы (I) !! в которой: ! Het обозначает 5-членное гетероарильное кольцо, необязательно замещенное С1-С5-алкилом; ! R1 обозначает C1-С10-алкил, C1-C10-алкоксигруппу, С3-С10-циклоалкил, 3-10-членное насыщенное гетероциклическое кольцо, 5-10-членное моно- или бициклическое гетероарильное кольцо или фенил, каждый независимо необязательно содержащий 1-3 заместителя, выбранных из группы, включающей C1-C8-алкил, С1-С4-алкоксигруппу, С3-С10-циклоалкил, С3-С10-циклоалкил-С1-С5-алкил, С1-С4-алкилсульфонил, С1-С4-ацил, оксогруппу, цианогруппу, фенил, гидроксигруппу и галоген; ! R2 и R3 обозначают С1-С4-алкил или водород при условии, что оба R2 и R3 не могут обозначать водород; или R2 и R3 вместе с атомом углерода, к которому они присоединены, образуют 3-6-членное циклоалкильное или гетероциклическое кольцо; ! R4 обозначает водород или метил; !R5 выбран из ! , , , , , , , , , , , и ! или R5 обозначает 3-10-членное насыщенное гетероциклическое кольцо, необязательно замещенное 1-3 C1-C4-алкилами; ! m равно 0, 1, 2 или 3; ! каждый R6 независимо обозначает водород, C1-С6-алкил, 3-10-членное насыщенное гетероциклическое кольцо, арил, бензил или -(CH2)1-3-O-(CH2)0-1-X, где X обозначает арил или СН3, каждое гетероциклическое, бензильное или арильное кольцо необязательно замещено одним или более С1-С4-алкилом, C1-С4-алкоксигруппой или галогеном; !где R7 и R8 каждый независимо обозначает водород или С1-С4-алкил при условии, что оба R7 и R8 не могут обозначать водород, и где R7 и R8 необязательно могут циклизоваться с образованием С3-С7-циклоалкильного кольца; ! R9 обозначает С1-С4-алкил, который заменяет метиленовый атом водорода в -(СН2)n- или отсутствует; ! n равно 0, 1 или 2; ! где любой атом углерода в формуле (I) или л�
Claims (12)
1. Соединение формулы (I)
в которой:
Het обозначает 5-членное гетероарильное кольцо, необязательно замещенное С1-С5-алкилом;
R1 обозначает C1-С10-алкил, C1-C10-алкоксигруппу, С3-С10-циклоалкил, 3-10-членное насыщенное гетероциклическое кольцо, 5-10-членное моно- или бициклическое гетероарильное кольцо или фенил, каждый независимо необязательно содержащий 1-3 заместителя, выбранных из группы, включающей C1-C8-алкил, С1-С4-алкоксигруппу, С3-С10-циклоалкил, С3-С10-циклоалкил-С1-С5-алкил, С1-С4-алкилсульфонил, С1-С4-ацил, оксогруппу, цианогруппу, фенил, гидроксигруппу и галоген;
R2 и R3 обозначают С1-С4-алкил или водород при условии, что оба R2 и R3 не могут обозначать водород; или R2 и R3 вместе с атомом углерода, к которому они присоединены, образуют 3-6-членное циклоалкильное или гетероциклическое кольцо;
R4 обозначает водород или метил;
R5 выбран из
или R5 обозначает 3-10-членное насыщенное гетероциклическое кольцо, необязательно замещенное 1-3 C1-C4-алкилами;
m равно 0, 1, 2 или 3;
каждый R6 независимо обозначает водород, C1-С6-алкил, 3-10-членное насыщенное гетероциклическое кольцо, арил, бензил или -(CH2)1-3-O-(CH2)0-1-X, где X обозначает арил или СН3, каждое гетероциклическое, бензильное или арильное кольцо необязательно замещено одним или более С1-С4-алкилом, C1-С4-алкоксигруппой или галогеном;
где R7 и R8 каждый независимо обозначает водород или С1-С4-алкил при условии, что оба R7 и R8 не могут обозначать водород, и где R7 и R8 необязательно могут циклизоваться с образованием С3-С7-циклоалкильного кольца;
R9 обозначает С1-С4-алкил, который заменяет метиленовый атом водорода в -(СН2)n- или отсутствует;
n равно 0, 1 или 2;
где любой атом углерода в формуле (I) или любой указанный выше заместитель R, если это возможно, необязательно частично или полностью галогенирован;
или его фармацевтически приемлемая соль.
2. Соединение по п.1 и в котором
Het обозначает
R1 обозначает C1-С6-алкил, фенил, циклопропил, циклобутил, циклопентил, циклогексил, циклогептил, циклооктил, тетрагидрофуранил, тетрагидропиранил, азетидинил, пиперидинил; бензоксазолил, бензотиазолил, бензимидазолил, диоксаланил, диоксанил, оксазолил, изоксазолил, тиазолил, пиразолил, пирролил, имидазолил, тиенил, тиоморфолинил, 1,1-диоксо-1λ6-тиоморфолинил, морфолинил, пиридинил, пиримидинил, пиридазинил, пиразинил, триазинил, пирролидинил, пиперазинил, пуринил, хинолинил, дигидро-2Н-хинолинил, изохинолинил, хиназолинил, индазолил, индолил, бензофуранил, бензопиранил или бензодиоксолил, каждый необязательно содержащий 1-2 заместителя, выбранных из группы, включающей галоген, C1-С6-алкил, гидроксигруппу, C1-С4-алкоксигруппу, С1-С4-алкилсульфонил, С3-С10-циклоалкил-С1-С5-алкил или эксогруппу;
R2 и R3 независимо обозначают метил, этил, н-пропил, изопропил или водород при условии, что оба R2 и R3 не могут обозначать водород; или R2 и R3 вместе с атомом углерода, к которому они присоединены, образуют циклопропильное, циклобутильное или циклопентильное кольцо;
R5 выбран из
где Ar обозначает тетрагидропиранил или тетрагидрофуранил, каждый необязательно замещенный C1-С3-алкилом,
где R10 обозначает водород или метил, или R5 обозначает тетрагидропиранил или тетрагидрофуранил, каждый необязательно замещенный C1-С3-алкилом;
R6 обозначает водород, бензил, фенил или C1-С4-алкил, каждое бензильное или фенильное кольцо необязательно замещено одним или более C1-С4-алкилом, C1-С4-алкоксигруппой или галогеном;
R7 и R8 каждый обозначает C1-С3-алкил или C3-С6-циклоалкил, где R7 и R8 необязательно могут циклизоваться с образованием C3-С6-циклоалкильного кольца.
3. Соединение по п.2 и в котором
R1 обозначает C1-С5-алкил, фенил, циклопропил, циклобутил, циклопентил, циклогексил, циклогептил, тетрагидрофуранил, тетрагидропиранил, диоксаланил, диоксанил, азетидинил, пиперидинил, бензимидазолил, пирролил, пиридинил, пиримидинил, пиридазинил, пиразинил, пирролидинил или пиперазинил, каждый необязательно содержащий 1-2 заместителя, выбранных из группы, включающей галоген, C1-С6-алкил, C1-С4-алкилсульфонил, C3-С10-циклоалкил-C1-С5-алкил, гидроксигруппу, C1-С4-алкоксигруппу и оксогруппу;
R2 и R3 независимо обозначают метил, этил, н-пропил, изопропил или водород при условии, что оба R2 и R3 не могут обозначать водород; или R2 и R3 вместе с атомом углерода, к которому они присоединены, образуют циклопропильное, циклобутильное или циклопентильное кольцо;
n равно 0 или 1;
R5 выбран из
где Ar обозначает тетрагидропиранил или тетрагидрофуранил, каждый необязательно замещенный C1-С3-алкилом,
где R10 обозначает водород или метил, или R5 обозначает тетрагидропиранил или тетрагидрофуранил, каждый необязательно замещенный C1-С3-алкилом;
R6 обозначает водород, бензил, фенил или C1-С4-алкил, каждое бензильное или фенильное кольцо необязательно замещено одним или более C1-С4-алкилом, C1-С4-алкоксигруппой или галогеном;
R7 и R8 все обозначают C1-С3-алкил или C3-С6-циклоалкил, где R7 и R8 необязательно могут циклизоваться с образованием C3-С6-циклоалкильного кольца.
4. Соединение по п.3 и в котором
Het обозначает
R1 обозначает фенил или бензимидазолил, каждый необязательно содержащий 1-2 заместителя, выбранных из группы, включающей галоген, С1-С6-алкил, C1-С4-алкилсульфонил, C3-С6-циклоалкил-C1-С3-алкил, или оксогруппу;
или R1 обозначает C1-С5-алкил, циклопропил, циклобутил, циклопентил, циклогексил, тетрагидропиранил, тетрагидрофуранил, азетидинил, пирролидинил или пиперидинил, каждый необязательно содержащий заместитель, выбранный из группы, включающей галоген, C1-С4-алкил, C1-С4-алкоксигруппу, C1-С4-алкилсульфонил или оксогруппу;
R2 и R3 независимо обозначают метил или R2 и R3 вместе с атомом углерода, к которому они присоединены, образуют циклопропильное или циклобутильное кольцо;
R7 и R8 каждый обозначает C1-С2-алкил, где R7 и R8 необязательно могут циклизоваться с образованием C3-С6-циклоалкильного кольца.
6. Соединение по п.5 и в котором
R1 обозначает фенил или бензимидазолил, каждый необязательно содержащий 1-2 заместителя, выбранных из группы, включающей галоген, C1-С6-алкил или C3-С5-циклоалкил-C1-С3-алкил;
или R1 обозначает C1-С5-алкил, циклопропил, циклобутил, циклопентил, циклогексил, тетрагидропиранил, тетрагидрофуранил или пиперидинил, каждый необязательно содержащий заместитель, выбранный из группы, включающей галоген, C1-С4-алкил, C1-С4-алкоксигруппу или C1-С4-алкилсульфонил.
7. Соединение формулы (II)
в котором
формулы (I) выбран из столбца А1-А11 таблицы I и
формулы (I) выбран из столбца В1-В36 таблицы I,
или его фармацевтически приемлемая соль.
10. Фармацевтическая композиция, содержащая соединение по любому из пп.1-9 в терапевтически эффективном количестве и один или большее количество фармацевтически приемлемых носителей и/или вспомогательных веществ.
11. Способ лечения боли, включающий введение соединения по любому из пп.1-10 в терапевтически эффективном количестве.
12. Способ лечения заболевания или патологического состояния, выбранного из группы, включающей заболевание легких, ревматическое заболевание, аутоиммунное заболевание, скелетно-мышечное заболевание, аллергическое заболевание, аллергическую реакцию, сосудистое заболевание, кожное заболевание, заболевание почек, заболевание печени, желудочно-кишечное заболевание, нейродегенеративное заболевание глаз, заболевания уха, носа и горла, неврологическое заболевание, заболевание крови, опухоли, эндокринные заболевания, заболевания, связанные с трансплантацией органов и тканей и заболевания "трансплантат против хозяина", состояния тяжелого шока, острую боль, висцеральную боль, спазм желудочно-кишечного тракта или матки, колики, невропатическую боль, воспалительную и ноцицептивную боль, боль при раке, головную боль, рестеноз, атеросклероз, реперфузионное поражение, застойную сердечную недостаточность, инфаркт миокарда, термическое повреждение, множественное поражение органов после травмы, некротизирующий энтероколит и синдромы, связанные с гемодиализом, лейкофорезом и трансфузией гранулоцитов, саркоидоз, гингивит и гипертермию, включающий введение соединения по любому из пп.1-10 в терапевтически эффективном количестве.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10007708P | 2008-09-25 | 2008-09-25 | |
| US61/100,077 | 2008-09-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2011116111A true RU2011116111A (ru) | 2012-10-27 |
Family
ID=41698020
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2011116111/04A RU2011116111A (ru) | 2008-09-25 | 2009-09-22 | Сульфонилсодержащие соединения, которые селективно модулируют рецептор св2 |
Country Status (24)
| Country | Link |
|---|---|
| US (4) | US8372874B2 (ru) |
| EP (2) | EP2342200B1 (ru) |
| JP (2) | JP4928650B2 (ru) |
| KR (2) | KR20110063485A (ru) |
| CN (2) | CN102164916A (ru) |
| AP (1) | AP2011005674A0 (ru) |
| AR (2) | AR073687A1 (ru) |
| AU (2) | AU2009296838A1 (ru) |
| BR (2) | BRPI0919172A2 (ru) |
| CA (2) | CA2737645A1 (ru) |
| CL (2) | CL2011000663A1 (ru) |
| CO (1) | CO6361912A2 (ru) |
| EA (1) | EA201100523A1 (ru) |
| EC (1) | ECSP11010931A (ru) |
| IL (2) | IL210433A0 (ru) |
| MA (1) | MA32654B1 (ru) |
| MX (1) | MX2011002904A (ru) |
| NZ (1) | NZ591111A (ru) |
| PE (1) | PE20110397A1 (ru) |
| RU (1) | RU2011116111A (ru) |
| TW (2) | TW201018677A (ru) |
| UY (1) | UY32139A (ru) |
| WO (2) | WO2010036630A2 (ru) |
| ZA (1) | ZA201100483B (ru) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2657247A1 (en) | 2006-07-28 | 2008-01-31 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| EP2074084B1 (en) | 2006-09-25 | 2013-08-28 | Boehringer Ingelheim International GmbH | Compounds which modulate the cb2 receptor |
| WO2008048914A1 (en) | 2006-10-17 | 2008-04-24 | Boehringer Ingelheim International Gmbh | Polycyclic compounds which modulate the cb2 receptor |
| US8173638B2 (en) * | 2006-11-21 | 2012-05-08 | Boehringer Ingelheim International Gmbh | Compounds which modulate the CB2 receptor |
| JP2011500820A (ja) * | 2007-10-25 | 2011-01-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を制御するジアゼパン化合物 |
| CA2704684A1 (en) * | 2007-11-07 | 2009-05-14 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| WO2009105509A1 (en) * | 2008-02-21 | 2009-08-27 | Boehringer Ingelheim International Gmbh | Amine and ether compounds which modulate the cb2 receptor |
| WO2010005782A1 (en) | 2008-07-10 | 2010-01-14 | Boehringer Ingelheim International Gmbh | Sulfone compounds which modulate the cb2 receptor |
| CN102164916A (zh) * | 2008-09-25 | 2011-08-24 | 贝林格尔.英格海姆国际有限公司 | 选择性调节cb2受体的磺酰基化合物 |
| JP5583694B2 (ja) | 2009-01-05 | 2014-09-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を調節するピロリジン化合物 |
| WO2010096371A2 (en) | 2009-02-18 | 2010-08-26 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds which modulate the cb2 receptor |
| US8299103B2 (en) * | 2009-06-15 | 2012-10-30 | Boehringer Ingelheim International Gmbh | Compounds which selectively modulate the CB2 receptor |
| EP2443107B1 (en) | 2009-06-16 | 2018-08-08 | Boehringer Ingelheim International GmbH | Azetidine 2 -carboxamide derivatives which modulate the cb2 receptor |
| JP2013505295A (ja) * | 2009-09-22 | 2013-02-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を選択的に調節する化合物 |
| MX346393B (es) | 2009-12-17 | 2017-03-17 | Centrexion Therapeutics Corp | Nuevos antagonistas del receptor ccr2 y usos de los mismo. |
| EP2523936A1 (en) | 2010-01-15 | 2012-11-21 | Boehringer Ingelheim International GmbH | Compounds which modulate the cb2 receptor |
| JP5746228B2 (ja) * | 2010-03-05 | 2015-07-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を選択的に調節するテトラゾール化合物 |
| US8846936B2 (en) | 2010-07-22 | 2014-09-30 | Boehringer Ingelheim International Gmbh | Sulfonyl compounds which modulate the CB2 receptor |
| WO2012061926A1 (en) * | 2010-11-08 | 2012-05-18 | Zalicus Pharmaceuticals Ltd. | Bisarylsulfone and dialkylarylsulfone compounds as calcium channel blockers |
| UA114657C2 (uk) * | 2012-12-07 | 2017-07-10 | Ф. Хоффманн-Ля Рош Аг | Піридин-2-аміди, придатні як агоністи канабіноїдного рецептора 2 |
| EP2803668A1 (en) | 2013-05-17 | 2014-11-19 | Boehringer Ingelheim International Gmbh | Novel (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles |
| BR112017028492B1 (pt) | 2015-07-02 | 2023-12-26 | Centrexion Therapeutics Corporation | Citrato de (4-((3r,4r)-3-metoxitetra-hidro-piran-4- ilamino)piperidin-1-il) (5- metil-6-(((2r, 6s)-6-(p-tolil) tetra-hidro-2h-piran-2-il)metilamino)pirimidin-4-il) metanona, seu uso e seu método de preparação, e composição farmacêutica |
| AU2021280893A1 (en) | 2020-05-08 | 2023-01-05 | Halia Therapeutics, Inc. | Inhibitors of NEK7 kinase |
| WO2023111996A1 (en) | 2021-12-17 | 2023-06-22 | Reglagene Holding, Inc. | Compositions and methods of making and using small molecules in the treatment of cancer |
| KR102584607B1 (ko) * | 2023-01-19 | 2023-10-04 | 아주대학교산학협력단 | 1h-피라졸-3-아마이드계 화합물 유도체를 포함하는 염증성 피부질환 예방 또는 치료용 조성물 |
| US12215102B2 (en) | 2023-02-28 | 2025-02-04 | Reglagene, Inc. | Compositions and methods for making and using small molecules for tubulin-targeted therapy in the treatment of cancers and related conditions |
| CN116947716B (zh) * | 2023-08-11 | 2025-10-28 | 绍兴贝斯美化工股份有限公司 | 一种2,3-二甲基-4-甲磺酰基苯甲酸甲酯的制备方法 |
| CN116947775B (zh) * | 2023-08-11 | 2025-10-28 | 绍兴贝斯美化工股份有限公司 | 一种3-(4,5-二氢-3-异噁唑基)-2-甲基-4-甲砜基苯甲酸甲酯的制备方法 |
Family Cites Families (126)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3117128A (en) | 1964-01-07 | Certificate of correction | ||
| US3116284A (en) | 1963-12-31 | Chs chj | ||
| CH312963A (de) | 1953-03-10 | 1956-03-15 | Sandoz Ag | Verfahren zur Herstellung von Azofarbstoffen |
| GB853799A (en) | 1957-11-21 | 1960-11-09 | Pfizer & Co C | Diquaternary compounds and process of preparing same |
| GB884258A (en) | 1958-11-06 | 1961-12-13 | Ciba Ltd | A new quinone derivative |
| GB1237126A (en) | 1968-04-10 | 1971-06-30 | Agfa Gevaert Nv | 3-acyl-amino-pyrazolin-5-ones |
| US3577462A (en) | 1968-08-08 | 1971-05-04 | American Home Prod | N-arylalkyl-beta-hydroxy-beta-phenyl-ethylamines and the salts thereof |
| US3966809A (en) | 1973-11-19 | 1976-06-29 | Stauffer Chemical Company | Insect repellent compounds |
| US4257954A (en) | 1978-08-08 | 1981-03-24 | Sterling Drug Inc. | Novel compounds, processes and marking systems |
| US4535087A (en) | 1982-11-19 | 1985-08-13 | Chevron Research Company | N-Substituted phenoxyacetamide fungicides |
| US4672065A (en) | 1982-11-19 | 1987-06-09 | Chevron Research Company | N-substituted phenoxyacetamide fungicides |
| US4859707A (en) | 1983-08-23 | 1989-08-22 | Key Pharmaceuticals, Inc. | Sulfur-substituted phenylacetamides |
| JPS6127955A (ja) | 1984-07-18 | 1986-02-07 | Hokko Chem Ind Co Ltd | アリ−ルスルホニル脂肪酸アミド誘導体、その製造法および除草剤 |
| JPS6127905U (ja) | 1984-07-25 | 1986-02-19 | 本田技研工業株式会社 | Ohc型内燃機関 |
| JPS61126071A (ja) | 1984-11-22 | 1986-06-13 | Hokko Chem Ind Co Ltd | 農園芸用殺菌剤 |
| DE3600950A1 (de) | 1986-01-15 | 1987-07-16 | Bayer Ag | 5-acylamido-1-aryl-pyrazole |
| WO1991009594A1 (en) | 1989-12-28 | 1991-07-11 | Virginia Commonwealth University | Sigma receptor ligands and the use thereof |
| DK0559898T3 (da) | 1990-11-26 | 1996-08-19 | Taisho Pharmaceutical Co Ltd | Anilidderivater |
| US5362878A (en) | 1991-03-21 | 1994-11-08 | Pfizer Inc. | Intermediates for making N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT) |
| CA2077252C (en) | 1992-08-31 | 2001-04-10 | Khashayar Karimian | Methods of making ureas and guanidines, and intermediates therefor |
| IL107120A (en) | 1992-09-29 | 1997-09-30 | Boehringer Ingelheim Int | Atomising nozzle and filter and spray generating device |
| US5256658A (en) | 1993-01-15 | 1993-10-26 | Ortho Pharmaceutical Corporation | Angiotensin II inhibitors |
| US5428037A (en) | 1993-04-09 | 1995-06-27 | Syntex Pharmaceuticals, Ltd. | Heterocyclic derivatives in the treatment of Ischaemia and related diseases |
| DE4319039A1 (de) | 1993-06-08 | 1994-12-15 | Bayer Ag | Substituierte (2-Oxo-1-benzimidazolinyl)-piperidine, Verfahren zu ihrer Herstellung und Verwendung als anti-retrovirale Mittel |
| WO1995003286A1 (en) | 1993-07-23 | 1995-02-02 | The Green Cross Corporation | Triazole derivative and pharmaceutical use thereof |
| US5583147A (en) | 1994-03-23 | 1996-12-10 | The Dupont Merck Pharmaceutical Company | Amides for the treatment of atherosclerosis |
| WO1996026925A1 (en) | 1995-03-01 | 1996-09-06 | Banyu Pharmaceutical Co., Ltd. | Arylthioacetamide derivatives |
| DE19536903C2 (de) | 1995-10-04 | 1998-09-10 | Boehringer Ingelheim Int | Vorrichtung zum Haltern eines fluidischen Bauteils |
| DE19536902A1 (de) | 1995-10-04 | 1997-04-10 | Boehringer Ingelheim Int | Vorrichtung zur Hochdruckerzeugung in einem Fluid in Miniaturausführung |
| DE19545226C1 (de) | 1995-12-05 | 1997-06-19 | Boehringer Ingelheim Int | Sperrspannwerk für einen federbetätigten Abtrieb |
| EP0906310A4 (en) | 1996-06-07 | 1999-09-01 | Merck & Co Inc | OXADIAZOLE-BENZOSULFONAMIDES AS SELECTIVE BETA-3 ADRENERGIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETIS AND OBESITY |
| US5808453A (en) | 1996-08-21 | 1998-09-15 | Siliconix Incorporated | Synchronous current sharing pulse width modulator |
| CN1104428C (zh) | 1996-09-13 | 2003-04-02 | 先灵公司 | 用作法呢基-蛋白转移酶抑制剂的取代的苯并芳庚并吡啶 |
| ES2236829T3 (es) | 1996-09-27 | 2005-07-16 | PHARMACIA & UPJOHN COMPANY LLC | Acidos beta-sulfonil hidroxamicos como inhibidores de las metaloproteinas de la matriz. |
| US5968929A (en) | 1996-10-30 | 1999-10-19 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US6048900A (en) | 1998-02-13 | 2000-04-11 | Bayer Corporation | Amide derivatives and methods for using the same as selective neuropeptide Y receptor antagonists |
| CA2281929C (en) | 1997-02-21 | 2007-07-10 | Bayer Aktiengesellschaft | Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases |
| KR20000075808A (ko) | 1997-02-27 | 2000-12-26 | 윌리암 에이취 캘넌, 에곤 이 버그 | 매트릭스 메탈로프로테이나제 억제제로서의 n-하이드록시-2-(알킬, 아릴, 또는 헤테로아릴 설파닐, 설피닐 또는 설포닐)-3-치환된 알킬, 아릴 또는 헤테로아릴아미드 |
| US5958940A (en) | 1997-09-11 | 1999-09-28 | Schering Corporation | Tricyclic compounds useful as inhibitors of farnesyl-protein transferase |
| US20030166687A1 (en) | 1997-11-21 | 2003-09-04 | Warpehoski Martha A. | Alpha-hydroxy,-amino and -fluoro derivatives of beta-sulphonyl hydroxamic acids as matrix metalloproteinases inhibitors |
| US6528529B1 (en) | 1998-03-31 | 2003-03-04 | Acadia Pharmaceuticals Inc. | Compounds with activity on muscarinic receptors |
| US6359009B1 (en) | 1998-04-08 | 2002-03-19 | Basf Aktiengesellschaft | Substituted anilide insecticidal agents |
| GB9810671D0 (en) | 1998-05-18 | 1998-07-15 | Pfizer Ltd | Anti-pruritic agents |
| US6235755B1 (en) | 1998-08-07 | 2001-05-22 | Applied Research Systems Ars Holding N.A. | FSH mimetics for the treatment of infertility |
| CN1353605A (zh) | 1999-03-26 | 2002-06-12 | 欧洲凯尔特股份有限公司 | 芳基取代的吡唑、咪唑、噁唑、噻唑和吡咯及其应用 |
| DE19929076A1 (de) | 1999-06-25 | 2000-12-28 | Aventis Pharma Gmbh | Indanylsubstituierte Benzolcarbonamide, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen |
| US6355653B1 (en) | 1999-09-06 | 2002-03-12 | Hoffmann-La Roche Inc. | Amino-triazolopyridine derivatives |
| WO2001029007A1 (en) | 1999-10-18 | 2001-04-26 | University Of Connecticut | Pyrazole derivatives as cannabinoid receptor antagonists |
| CO5221057A1 (es) | 2000-03-02 | 2002-11-28 | Aventis Cropscience Sa | Componentes y composiciones plagicidas |
| BR0116388A (pt) | 2000-12-22 | 2003-09-30 | Astrazeneca Ab | Composto, processo para preparar um composto, composição farmacêutica e método para tratar, em um animal de sangue quente, distúrbios de alimentação e uso de um composto |
| US20020099035A1 (en) | 2001-01-24 | 2002-07-25 | Sandanayaka Vincent P. | Method for preparing alpha-sulfonyl hydroxamic acid derivatives |
| US7507767B2 (en) | 2001-02-08 | 2009-03-24 | Schering Corporation | Cannabinoid receptor ligands |
| US7067539B2 (en) | 2001-02-08 | 2006-06-27 | Schering Corporation | Cannabinoid receptor ligands |
| WO2002088089A1 (en) | 2001-04-19 | 2002-11-07 | Banyu Pharmaceutical Co., Ltd. | Spiropiperidine derivatives, nociceptin receptor antagonists containing the same as the active ingredient and medicinal compositions |
| DE10129899A1 (de) | 2001-06-21 | 2003-01-09 | Basf Coatings Ag | Physikalisch, thermisch oder thermisch und mit aktinischer Strahlung härtbarer wäßriger Beschichtungsstoff und seine Verwendung |
| CA2458446A1 (en) | 2001-10-04 | 2003-04-17 | Novartis Ag | Cyanoacetyl compounds |
| AU2002363250A1 (en) | 2001-11-01 | 2003-05-12 | Icagen, Inc. | Pyrazole-amides and-sulfonamides |
| JP2003155285A (ja) | 2001-11-19 | 2003-05-27 | Toray Ind Inc | 環状含窒素誘導体 |
| EP2305648A1 (en) | 2001-12-21 | 2011-04-06 | Novo Nordisk A/S | Amide derivatives useful as glucokinase activators |
| EP1539693B9 (en) | 2002-06-19 | 2008-10-08 | Schering Corporation | Cannabinoid receptor agonists |
| JP2006502134A (ja) | 2002-08-09 | 2006-01-19 | アストラゼネカ アクチボラグ | 代謝調節型グルタミン酸受容体において活性を有する化合物 |
| US20040132726A1 (en) | 2002-08-09 | 2004-07-08 | Astrazeneca Ab And Nps Pharmaceuticals, Inc. | New compounds |
| UY27939A1 (es) | 2002-08-21 | 2004-03-31 | Glaxo Group Ltd | Compuestos |
| HRP20050053A2 (en) | 2002-09-19 | 2005-04-30 | Solvay Pharmaceuticals B.V. | 1 h-1,2,4-triazole-3-carboxamide derivatives as cannabinoid-cb1 receptor ligands |
| GB0222495D0 (en) | 2002-09-27 | 2002-11-06 | Glaxo Group Ltd | Compounds |
| EP1558253A4 (en) | 2002-10-30 | 2007-07-25 | Merck & Co Inc | PIPERIDINYL ALPHA AMINOAMIDE MODULATORS DERCHEMOKIN RECEPTOR ACTIVITY |
| US7642277B2 (en) | 2002-12-04 | 2010-01-05 | Boehringer Ingelheim International Gmbh | Non-nucleoside reverse transcriptase inhibitors |
| SE0300010D0 (sv) | 2003-01-07 | 2003-01-07 | Astrazeneca Ab | Novel Compounds |
| US7718692B2 (en) | 2004-02-13 | 2010-05-18 | Carson John R | Hetero-substituted acetanilide derivatives as analgesic agents |
| US7449464B2 (en) | 2003-03-12 | 2008-11-11 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| SE0301372D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
| WO2004099200A1 (en) | 2003-05-12 | 2004-11-18 | Pfizer Products Inc. | Isoxazole and isothiazole compounds for the treatment of neurodegenerative disorders |
| JP2004337701A (ja) | 2003-05-14 | 2004-12-02 | Seiko Epson Corp | 液滴吐出方法、及び液滴吐出装置 |
| AU2004273865A1 (en) | 2003-09-18 | 2005-03-31 | Merck & Co., Inc. | Substituted sulfonamides |
| US20070021430A1 (en) | 2003-09-23 | 2007-01-25 | Chen Alex M | Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor |
| WO2005040355A2 (en) | 2003-10-24 | 2005-05-06 | Exelixis, Inc. | Tao kinase modulators and methods of use |
| CA2550012A1 (en) | 2003-12-17 | 2005-06-30 | Takeda Pharmaceutical Company Limited | Urea derivative, process for producing the same and use |
| WO2005077345A1 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Compounds for the treatment of gastro-esophageal reflux disease |
| WO2005077368A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| WO2005077373A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| US7585881B2 (en) | 2004-02-18 | 2009-09-08 | Astrazeneca Ab | Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| FR2866885B1 (fr) | 2004-02-26 | 2007-08-31 | Sanofi Synthelabo | Derives de piperidinylalkylcarbamates, leur prepation et leur application en therapeutique |
| JP2007526324A (ja) | 2004-03-02 | 2007-09-13 | スミスクライン・ビーチャム・コーポレイション | Akt活性のある阻害剤 |
| CA2568976A1 (en) | 2004-06-03 | 2005-12-22 | Ciphergen Biosystems, Inc. | Biomarkers for peripheral artery disease |
| WO2006012227A2 (en) | 2004-06-24 | 2006-02-02 | Incyte Corporation | Amido compounds and their use as pharmaceuticals |
| FR2872813B1 (fr) | 2004-07-09 | 2007-01-19 | Sanofi Synthelabo | Derives de 2-carbamide-4-phenylthiazole, leur preparation et leur application en therapeutique |
| WO2006030805A1 (ja) | 2004-09-16 | 2006-03-23 | Astellas Pharma Inc. | トリアゾール誘導体またはその塩 |
| WO2006044645A2 (en) | 2004-10-13 | 2006-04-27 | Adolor Corporation | Sulfamoyl benzamides and methods of their use |
| AU2005311930B9 (en) | 2004-12-03 | 2009-09-10 | Merck Sharp & Dohme Corp. | Substituted piperazines as CB1 antagonists |
| JP2008526887A (ja) * | 2005-01-10 | 2008-07-24 | ユニバーシティ オブ コネチカット | カンナビノイド受容体に作用する新規なヘテロピロール類似体 |
| WO2006080040A1 (en) | 2005-01-25 | 2006-08-03 | Università Degli Studi Di Siena | New potent and selective ligands of cannabinoid receptors |
| GB0504753D0 (en) | 2005-03-08 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| GB0506133D0 (en) | 2005-03-24 | 2005-05-04 | Sterix Ltd | Compound |
| FR2885364B1 (fr) | 2005-05-03 | 2007-06-29 | Sanofi Aventis Sa | Derives d'alkyl-, alkenyl-et alkynylcarbamates, leur preparation et leur application en therapeutique |
| WO2007020502A2 (en) | 2005-08-16 | 2007-02-22 | Pharmacia & Upjohn Company Llc | Cannabinoid receptor ligands and uses thereof |
| CA2628844C (en) | 2005-11-08 | 2011-12-06 | Pfizer Limited | Pyrazole derivatives and their medical use |
| WO2007070760A2 (en) | 2005-12-15 | 2007-06-21 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| BRPI0706395A2 (pt) | 2006-01-11 | 2011-03-22 | Astrazeneca Ab | composto, uso do mesmo, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente e para tratar doença, composição farmacêutica, e, processo para preparar um composto |
| US20070213311A1 (en) | 2006-03-02 | 2007-09-13 | Yun-Long Li | Modulators of 11-beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same |
| WO2007102059A1 (en) | 2006-03-06 | 2007-09-13 | Pfizer Japan Inc. | Sulfonyl benzimidazole derivatives |
| WO2007118041A1 (en) | 2006-04-07 | 2007-10-18 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| BRPI0712720A2 (pt) * | 2006-05-31 | 2012-11-20 | Abbott Lab | compostos tiazàis como ligantes do receptor canabinàide e usos dos mesmos |
| CA2657247A1 (en) | 2006-07-28 | 2008-01-31 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| EP2057140B1 (en) | 2006-08-24 | 2012-08-08 | AstraZeneca AB | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| EP2074084B1 (en) | 2006-09-25 | 2013-08-28 | Boehringer Ingelheim International GmbH | Compounds which modulate the cb2 receptor |
| WO2008048914A1 (en) | 2006-10-17 | 2008-04-24 | Boehringer Ingelheim International Gmbh | Polycyclic compounds which modulate the cb2 receptor |
| US8173638B2 (en) | 2006-11-21 | 2012-05-08 | Boehringer Ingelheim International Gmbh | Compounds which modulate the CB2 receptor |
| WO2008098025A1 (en) | 2007-02-08 | 2008-08-14 | Boehringer Ingelheim International Gmbh | Arylsulfonamide compounds which modulate the cb2 receptor |
| CA2679185A1 (en) | 2007-02-28 | 2008-09-04 | Advinus Therapeutics Private Limited | 2,2,2-tri-substituted acetamide derivatives as glucokinase activators, their process and pharmaceutical application |
| CA2682639A1 (en) | 2007-03-29 | 2008-10-09 | F. Hoffmann-La Roche Ag | Heterocyclic antiviral compounds |
| JP2011500820A (ja) | 2007-10-25 | 2011-01-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を制御するジアゼパン化合物 |
| CA2704684A1 (en) | 2007-11-07 | 2009-05-14 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| EP2234984B1 (en) | 2007-12-17 | 2016-03-16 | Janssen Pharmaceutica, N.V. | Fluoroalkyl substituted benzimidazole cannabinoid agonists |
| EP2219646A4 (en) | 2007-12-21 | 2010-12-22 | Univ Rochester | PROCESS FOR EXTENDING THE LIFE OF EUKARYOTIC ORGANISMS |
| WO2009105509A1 (en) | 2008-02-21 | 2009-08-27 | Boehringer Ingelheim International Gmbh | Amine and ether compounds which modulate the cb2 receptor |
| EP2418207A1 (en) | 2008-05-13 | 2012-02-15 | Boehringer Ingelheim International GmbH | Sulfone compounds which modulate the CB2 receptor |
| WO2010005782A1 (en) | 2008-07-10 | 2010-01-14 | Boehringer Ingelheim International Gmbh | Sulfone compounds which modulate the cb2 receptor |
| CN102164916A (zh) | 2008-09-25 | 2011-08-24 | 贝林格尔.英格海姆国际有限公司 | 选择性调节cb2受体的磺酰基化合物 |
| JP5583694B2 (ja) | 2009-01-05 | 2014-09-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を調節するピロリジン化合物 |
| WO2010096371A2 (en) | 2009-02-18 | 2010-08-26 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds which modulate the cb2 receptor |
| US8299103B2 (en) | 2009-06-15 | 2012-10-30 | Boehringer Ingelheim International Gmbh | Compounds which selectively modulate the CB2 receptor |
| EP2443107B1 (en) | 2009-06-16 | 2018-08-08 | Boehringer Ingelheim International GmbH | Azetidine 2 -carboxamide derivatives which modulate the cb2 receptor |
| JP2013505295A (ja) | 2009-09-22 | 2013-02-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を選択的に調節する化合物 |
| EP2523936A1 (en) | 2010-01-15 | 2012-11-21 | Boehringer Ingelheim International GmbH | Compounds which modulate the cb2 receptor |
| JP5746228B2 (ja) | 2010-03-05 | 2015-07-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を選択的に調節するテトラゾール化合物 |
| US8846936B2 (en) | 2010-07-22 | 2014-09-30 | Boehringer Ingelheim International Gmbh | Sulfonyl compounds which modulate the CB2 receptor |
-
2009
- 2009-09-22 CN CN2009801374019A patent/CN102164916A/zh active Pending
- 2009-09-22 CA CA2737645A patent/CA2737645A1/en not_active Abandoned
- 2009-09-22 BR BRPI0919172A patent/BRPI0919172A2/pt not_active IP Right Cessation
- 2009-09-22 BR BRPI0919024A patent/BRPI0919024A2/pt not_active IP Right Cessation
- 2009-09-22 JP JP2011529152A patent/JP4928650B2/ja active Active
- 2009-09-22 EP EP09792816A patent/EP2342200B1/en active Active
- 2009-09-22 MX MX2011002904A patent/MX2011002904A/es active IP Right Grant
- 2009-09-22 NZ NZ591111A patent/NZ591111A/xx not_active IP Right Cessation
- 2009-09-22 WO PCT/US2009/057776 patent/WO2010036630A2/en not_active Ceased
- 2009-09-22 AU AU2009296838A patent/AU2009296838A1/en not_active Abandoned
- 2009-09-22 EP EP09792817.0A patent/EP2342199B1/en active Active
- 2009-09-22 EA EA201100523A patent/EA201100523A1/ru unknown
- 2009-09-22 KR KR1020117006824A patent/KR20110063485A/ko not_active Withdrawn
- 2009-09-22 WO PCT/US2009/057777 patent/WO2010036631A2/en not_active Ceased
- 2009-09-22 PE PE2011000669A patent/PE20110397A1/es not_active Application Discontinuation
- 2009-09-22 AP AP2011005674A patent/AP2011005674A0/xx unknown
- 2009-09-22 RU RU2011116111/04A patent/RU2011116111A/ru not_active Application Discontinuation
- 2009-09-22 KR KR1020117004615A patent/KR20110063438A/ko not_active Withdrawn
- 2009-09-22 US US12/564,133 patent/US8372874B2/en active Active
- 2009-09-22 CA CA2737639A patent/CA2737639A1/en not_active Abandoned
- 2009-09-22 AU AU2009296837A patent/AU2009296837A1/en not_active Abandoned
- 2009-09-22 US US12/564,132 patent/US8048899B2/en active Active
- 2009-09-22 JP JP2011529153A patent/JP5453437B2/ja active Active
- 2009-09-22 CN CN2009801376048A patent/CN102164917A/zh active Pending
- 2009-09-24 UY UY0001032139A patent/UY32139A/es not_active Application Discontinuation
- 2009-09-25 TW TW098132529A patent/TW201018677A/zh unknown
- 2009-09-25 AR ARP090103707A patent/AR073687A1/es unknown
- 2009-09-25 AR ARP090103708A patent/AR073688A1/es unknown
- 2009-09-25 TW TW098132577A patent/TW201016690A/zh unknown
-
2011
- 2011-01-02 IL IL210433A patent/IL210433A0/en unknown
- 2011-01-19 ZA ZA2011/00483A patent/ZA201100483B/en unknown
- 2011-01-25 IL IL210853A patent/IL210853A0/en unknown
- 2011-03-17 CO CO11033548A patent/CO6361912A2/es not_active Application Discontinuation
- 2011-03-24 MA MA33723A patent/MA32654B1/fr unknown
- 2011-03-25 CL CL2011000663A patent/CL2011000663A1/es unknown
- 2011-03-25 CL CL2011000662A patent/CL2011000662A1/es unknown
- 2011-03-29 EC EC2011010931A patent/ECSP11010931A/es unknown
- 2011-08-25 US US13/217,480 patent/US8362039B2/en active Active
- 2011-09-21 US US13/238,054 patent/US8349871B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2011116111A (ru) | Сульфонилсодержащие соединения, которые селективно модулируют рецептор св2 | |
| KR102204748B1 (ko) | 신규 비페닐 화합물 또는 그의 염 | |
| US10604526B2 (en) | Chemokine receptor modulators and uses thereof | |
| CN103497188B (zh) | 调节c‑fms和/或c‑kit活性的化合物及其应用 | |
| ES2733946T3 (es) | Derivados de pirimido[4,5-b]indol y su uso en la expansión de células madre hematopoyéticas | |
| US10080743B2 (en) | Isoxazole derivatives as FXR agonists and methods of use thereof | |
| TWI727172B (zh) | 新穎聯苯化合物或其鹽 | |
| CN101952281B (zh) | 具有细胞、组织及器官保存效果的吲哚及吲唑衍生物 | |
| ES2710491T3 (es) | Moduladores de la vía del complemento y sus usos | |
| TWI383980B (zh) | C型肝炎病毒之大環抑制劑 | |
| RU2013123275A (ru) | Пиперидин-4-илазетидиндиамиды как ингибиторы моноацилглицеринлипазы | |
| CA2990234C (en) | 3-tetrazolyl-benzene-1,2-disulfonamide derivatives as metallo-beta-lactamase inhibitors | |
| CN104507928B (zh) | 脂质合成的杂环调节剂 | |
| RU2009125614A (ru) | Глюкокортикоидные миметики, способы их получения, фармацевтические композиции и их применения | |
| KR20140027090A (ko) | 연령-관련 황반 변성 (amd)의 치료에 유용한 인돌 화합물 또는 그의 유사체 | |
| JP2009511498A5 (ru) | ||
| JP2006504658A5 (ru) | ||
| RU2013114771A (ru) | Диамиды азетидинила как ингибиторы моноацилглицерол липазы | |
| EA014293B1 (ru) | Макроциклические ингибиторы вируса гепатита с | |
| JP2013521291A5 (ru) | ||
| CN111434655A (zh) | 溶血磷脂酸受体拮抗剂及其制备方法 | |
| US20220388955A1 (en) | Ep2 antagonist | |
| SG171781A1 (en) | Monocarbams | |
| JPWO2023064857A5 (ru) | ||
| TW202137979A (zh) | 使用有新穎聯苯化合物之抗腫瘤效果增強劑 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20140110 |