ES2335698T3 - Derivados de piperidina sustituida por heteroarilo como inhibidores de l-cpt1. - Google Patents
Derivados de piperidina sustituida por heteroarilo como inhibidores de l-cpt1. Download PDFInfo
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- ES2335698T3 ES2335698T3 ES06819660T ES06819660T ES2335698T3 ES 2335698 T3 ES2335698 T3 ES 2335698T3 ES 06819660 T ES06819660 T ES 06819660T ES 06819660 T ES06819660 T ES 06819660T ES 2335698 T3 ES2335698 T3 ES 2335698T3
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- lower alkyl
- alkoxy
- optionally substituted
- carbonyl
- dihydro
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- 102100027943 Carnitine O-palmitoyltransferase 1, liver isoform Human genes 0.000 title 1
- 101000859570 Homo sapiens Carnitine O-palmitoyltransferase 1, liver isoform Proteins 0.000 title 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical class C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 36
- 125000003545 alkoxy group Chemical group 0.000 abstract 13
- 229910052739 hydrogen Inorganic materials 0.000 abstract 9
- 239000001257 hydrogen Substances 0.000 abstract 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 9
- -1 pyridinyl-2-one Chemical group 0.000 abstract 8
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical group 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 6
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 4
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000002757 morpholinyl group Chemical group 0.000 abstract 3
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 3
- 125000001425 triazolyl group Chemical group 0.000 abstract 3
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- WJRBRSLFGCUECM-UHFFFAOYSA-N hydantoin Chemical compound O=C1CNC(=O)N1 WJRBRSLFGCUECM-UHFFFAOYSA-N 0.000 abstract 2
- 125000002883 imidazolyl group Chemical group 0.000 abstract 2
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 2
- IWELDVXSEVIIGI-UHFFFAOYSA-N piperazin-2-one Chemical compound O=C1CNCCN1 IWELDVXSEVIIGI-UHFFFAOYSA-N 0.000 abstract 2
- 125000004193 piperazinyl group Chemical group 0.000 abstract 2
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical compound O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical compound O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 2
- 125000005988 1,1-dioxo-thiomorpholinyl group Chemical group 0.000 abstract 1
- LZTSCEYDCZBRCJ-UHFFFAOYSA-N 1,2-dihydro-1,2,4-triazol-3-one Chemical compound OC=1N=CNN=1 LZTSCEYDCZBRCJ-UHFFFAOYSA-N 0.000 abstract 1
- SWEICGMKXPNXNU-UHFFFAOYSA-N 1,2-dihydroindazol-3-one Chemical compound C1=CC=C2C(O)=NNC2=C1 SWEICGMKXPNXNU-UHFFFAOYSA-N 0.000 abstract 1
- AICIYIDUYNFPRY-UHFFFAOYSA-N 1,3-dihydro-2H-imidazol-2-one Chemical compound O=C1NC=CN1 AICIYIDUYNFPRY-UHFFFAOYSA-N 0.000 abstract 1
- SILNNFMWIMZVEQ-UHFFFAOYSA-N 1,3-dihydrobenzimidazol-2-one Chemical group C1=CC=C2NC(O)=NC2=C1 SILNNFMWIMZVEQ-UHFFFAOYSA-N 0.000 abstract 1
- ABJFBJGGLJVMAQ-UHFFFAOYSA-N 1,4-dihydroquinoxaline-2,3-dione Chemical compound C1=CC=C2NC(=O)C(=O)NC2=C1 ABJFBJGGLJVMAQ-UHFFFAOYSA-N 0.000 abstract 1
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 abstract 1
- HRSWSISJJJDBOQ-UHFFFAOYSA-N 2-oxo-1,3-diaza-8-azoniaspiro[4.5]dec-3-en-4-olate Chemical compound N1C(=O)NC(=O)C11CCNCC1 HRSWSISJJJDBOQ-UHFFFAOYSA-N 0.000 abstract 1
- VXTHXGKVRHXATD-UHFFFAOYSA-N 3,4-dihydroquinazolin-2-one Chemical compound C1=CC=C2CNC(=O)[N]C2=C1 VXTHXGKVRHXATD-UHFFFAOYSA-N 0.000 abstract 1
- HQQTZCPKNZVLFF-UHFFFAOYSA-N 4h-1,2-benzoxazin-3-one Chemical compound C1=CC=C2ONC(=O)CC2=C1 HQQTZCPKNZVLFF-UHFFFAOYSA-N 0.000 abstract 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- MNFORVFSTILPAW-UHFFFAOYSA-N azetidin-2-one Chemical compound O=C1CCN1 MNFORVFSTILPAW-UHFFFAOYSA-N 0.000 abstract 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 abstract 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 abstract 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 abstract 1
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical group C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002071 phenylalkoxy group Chemical group 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003003 spiro group Chemical group 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract 1
- 125000001984 thiazolidinyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/4192—1,2,3-Triazoles
-
- 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
- A61K31/4196—1,2,4-Triazoles
-
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
- 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
- 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
-
- 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
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Compuestos de la fórmula (I) **(Ver fórmula)** en la que X es C(R8R9), NR10, O, S, S(O), S(O2); R1 es fenilo opcionalmente sustituido por de 1 a 3 sustituyentes elegidos entre el grupo formado por halógeno, hidroxi, alquilo inferior, hidroxialquilo inferior, fluoralquilo inferior, alcoxi inferior y CN; R2 es hidrógeno o alquilo inferior; R3 y R4 con independencia entre sí son hidrógeno, halógeno, alquilo inferior o alcoxi inferior, o R3 y R4 juntos son =O para formar un grupo carbonilo junto con el átomo de carbono al que están unidos; R5 y R6 con independencia entre sí son hidrógeno, halógeno, alquilo inferior o alcoxi inferior, o R5 y R6 juntos son =O para formar un grupo carbonilo junto con el átomo de carbono al que están unidos; R7 es un oxadiazolilo o triazolilo, dichos oxadiazolilo o triazolilo están sustituidos por R11 y opcionalmente sustituidos por R12; R8 y R9 con independencia entre sí son hidrógeno, halógeno, hidroxi, alquilo inferior, alcoxi inferior; o R8 y R9 están unidos entre sí y -R8-R9- es -(CH2)2-7- para formar un anillo junto con el átomo de carbono al que están unidos; R10 es hidrógeno, alquilo inferior, (alquilo inferior)-carbonilo o alquilsulfonilo inferior; R11 es arilo o heteroarilo elegido entre el grupo formado por piridinilo, pirazinilo, pirimidinilo, piridinil-2-ona, oxadiazolilo, indazolilo, 1,3-dihidro-bencimidazol-2-ona, 1,3-dihidro-indol-2-ona, benzotriazolilo, imidazopiridinilo, triazolpiridinilo, tetrazolpiridinilo, bencimidazolilo, 2-oxo-2,3-dihidro-1H-indol-5-ilo, pirimidin-4-ona, furanilo, tiadiazolilo, pirazolilo, isoxazolilo, pirimidina-2,4-diona, benzooxazin-3-ona, 1,4-dihidro-benzooxazin-2-ona, indolilo, tiofenilo, oxazolilo, benzooxazin-2-ona, 3,4-dihidro-quinazolin-2-ona, piridazinilo, quinoxalinilo, benzotiazolilo, benzotiadiazolilo, naftiridinilo, cinolinilo, 1,4-dihidro-quinoxalina-2,3-diona y 1,2-dihidro-indazol-3-ona, dicho arilo o heteroarilo está opcionalmente sustituido por de 1 a 3 sustituyentes elegidos entre el grupo formado por alquilo inferior, hidroxi, B(OH)2, carboxi-alcoxi inferior, carbamoil-alcoxi inferior, ciano, hidroxialquilo inferior, fluoralquilo inferior, alcoxi inferior, halógeno, S(O2)R13, C(O)R14, NO2, NR15R16, imidazolilo, pirazolilo, tetrazolilo, pirrolilo, fenil-alcoxi inferior, [1,3,4]oxadiazol-2-ona, oxadiazolilo, triazolilo e isoxazolilo, dicho imidazolilo está opcionalmente sustituido por alquilo inferior y dicho fenil-alcoxi inferior está opcionalmente sustituido por hidroxi, halógeno, alquilo inferior, alcoxi inferior o fluoralquilo inferior y dicho pirazolilo está opcionalmente sustituido por alquilo inferior y dicho isoxazolilo está opcionalmente sustituido por alquilo inferior; R12 es hidrógeno o alquilo inferior; R13 es alquilo inferior, NR17R18 o fluoralquilo inferior; R14 es OH, NR19R20, alcoxi inferior, alqueniloxi inferior o alquilo inferior; R15 y R16 con independencia entre sí son hidrógeno, alquilo inferior, (alquilo inferior)-carbonilo, alquilo inferior-SO2, (alqueniloxi inferior)-carbonilo, NH2-carbonilo, (alquilo inferior)-NH-carbonilo, (alquilo inferior)2N-carbonilo o fenil-alquilo inferior, dicho fenil-alquilo inferior está opcionalmente sustituido por hidroxi, halógeno, alquilo inferior, alcoxi inferior o fluoralquilo inferior; o NR15R16 es un heterociclilo elegido entre el grupo formado por morfolinilo, tiomorfolinilo, 1,1-dioxo-tiomorfolinilo, piperidinilo, piperidin-2-ona, piperazin-2-ona, 8-oxa-3-aza-biciclo[3.2.1]octilo, piperazinilo, pirrolidinilo, 1,1-dioxo-isotiazolidinilo, pirrolidin-2-ona, imidazolidina-2,4-diona, 2,4-dihidro[1,2,4]triazol-3-ona, pirrolidina-2,5-diona, azetidin-2-ona y 1,3-dihidro-imidazol-2-ona, dicho heterociclilo está opcionalmente sustituido por hidroxialquilo inferior o (alquilo inferior)-carbonilo; R17 y R18 con independencia entre sí son hidrógeno, alquilo inferior, hidroxialquilo inferior, alcoxi inferior-alquilo inferior; o NR17R18 es morfolinilo; R19 y R20 con independencia entre sí son hidrógeno, alquilo inferior, cicloalquilo, hidroxialquilo inferior, alcoxi inferior-alquilo inferior, (alquilo inferior)2N-alquilo inferior, piridinil-alquilo inferior o ciano-alquilo inferior; o NR19R20 es un heterociclilo elegido entre el grupo formado por morfolinilo, pirrolidinilo, 8-oxa-3-aza-biciclo[3.2.1]octilo, piperidinilo, piperazinilo, piperazin-2-ona, tiazolidinilo, tiomorfolinilo, 1,3,8-triaza-espiro[4,5]decano-2,4-diona y espiro(1-ftalano)-piperidin-4-ilo, dicho heterociclilo está opcionalmente sustituido por hidroxi, (alquilo inferior)-S(O2), alquilo inferior, (alquilo inferior)-carbonilo, carboxi, carbamoílo, alcoxi inferior-carbonilo, ciano, fenilo, piridinilo o alcoxi inferior; y las sales y ésteres farmacéuticamente aceptables de los mismos, en donde el término "alquilo inferior ", solo o en combinación con otros grupos, se refiere a un radical de alquilo monovalente de cadena lineal o ramificada de uno a siete átomos de carbono; el término "alcoxi inferior ", solo o en combinación con otros grupos, se refiere al grupo R''-O-, en donde R'' es un alquilo inferior; y el termino "alquenilo inferior ", solo o en combinación con otros grupos, se refiere a un resto hidrocarburo de cadena lineal o ramificada que comprende un enlace olefínico y hasta 7 átomos de carbono.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05111560 | 2005-12-01 | ||
| EP05111560 | 2005-12-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2335698T3 true ES2335698T3 (es) | 2010-03-31 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES06819660T Active ES2335698T3 (es) | 2005-12-01 | 2006-11-22 | Derivados de piperidina sustituida por heteroarilo como inhibidores de l-cpt1. |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7645776B2 (es) |
| EP (1) | EP1959951B1 (es) |
| JP (1) | JP4855478B2 (es) |
| KR (1) | KR101135310B1 (es) |
| CN (1) | CN101321525B (es) |
| AR (1) | AR056821A1 (es) |
| AT (1) | ATE452635T1 (es) |
| AU (1) | AU2006319247B2 (es) |
| BR (1) | BRPI0619086A2 (es) |
| CA (1) | CA2630460C (es) |
| DE (1) | DE602006011363D1 (es) |
| DK (1) | DK1959951T3 (es) |
| ES (1) | ES2335698T3 (es) |
| NO (1) | NO20082388L (es) |
| PL (1) | PL1959951T3 (es) |
| PT (1) | PT1959951E (es) |
| RU (1) | RU2396269C2 (es) |
| TW (1) | TWI358409B (es) |
| WO (1) | WO2007063012A1 (es) |
| ZA (1) | ZA200804393B (es) |
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| CA2689383C (en) * | 2007-06-01 | 2013-10-08 | F. Hoffmann-La Roche Ag | Piperidine-amide derivatives |
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| EP3941475A4 (en) * | 2019-03-20 | 2023-01-25 | Goldfinch Bio, Inc. | PYRIDAZINONES AND METHODS OF USE THEREOF |
| EP4334313A1 (en) | 2021-05-04 | 2024-03-13 | 2N Pharma ApS | Diazepane derivatives, processes for their preparation, and uses thereof for the amelioration, prevention and/or treatment of mental and neurological diseases |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5196418A (en) * | 1992-02-14 | 1993-03-23 | Board Of Supervisors, Louisiana State University Agricultural & Mechanical College | Hemicholinium lipids and use thereof |
| CZ287268B6 (en) * | 1995-11-09 | 2000-10-11 | Sanofi Synthelabo | Derivatives of 5-phenyl-3-(piperidin-4-yl)-1,3,4-oxadiazol-2(3H)-one, process of their preparation and pharmaceutical preparation in which they are comprised |
| US6030993A (en) * | 1996-07-02 | 2000-02-29 | Sang Sup Jew | 2-hydroxypropionic acid derivative and its manufacturing method |
| US6207665B1 (en) * | 1997-06-12 | 2001-03-27 | Schering Aktiengesellschaft | Piperazine derivatives and their use as anti-inflammatory agents |
| WO1999065881A1 (en) * | 1998-06-19 | 1999-12-23 | Nissan Chemical Industries, Ltd. | Heterocyclic compounds as hypoglycemic agents |
| JP2001031652A (ja) * | 1998-06-19 | 2001-02-06 | Nissan Chem Ind Ltd | 六員環複素環類 |
| WO2001034594A1 (en) * | 1999-11-12 | 2001-05-17 | Guilford Pharmaceuticals, Inc. | Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors |
| US20050256159A1 (en) * | 2002-10-11 | 2005-11-17 | Astrazeneca Ab | 1,4-disubstituted piperidine derivatives and their use as 11,betahsd1 inhibitors |
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- 2006-11-22 EP EP06819660A patent/EP1959951B1/en not_active Not-in-force
- 2006-11-22 CA CA2630460A patent/CA2630460C/en not_active Expired - Fee Related
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- 2006-11-22 AT AT06819660T patent/ATE452635T1/de active
- 2006-11-22 BR BRPI0619086-3A patent/BRPI0619086A2/pt not_active IP Right Cessation
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- 2006-11-22 ES ES06819660T patent/ES2335698T3/es active Active
- 2006-11-22 RU RU2008126398/04A patent/RU2396269C2/ru not_active IP Right Cessation
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- 2006-11-22 CN CN2006800453448A patent/CN101321525B/zh not_active Expired - Fee Related
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- 2006-11-22 PT PT06819660T patent/PT1959951E/pt unknown
- 2006-11-22 KR KR1020087015998A patent/KR101135310B1/ko not_active Expired - Fee Related
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2008
- 2008-05-21 ZA ZA200804393A patent/ZA200804393B/xx unknown
- 2008-05-26 NO NO20082388A patent/NO20082388L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TWI358409B (en) | 2012-02-21 |
| AR056821A1 (es) | 2007-10-24 |
| US7645776B2 (en) | 2010-01-12 |
| ATE452635T1 (de) | 2010-01-15 |
| JP4855478B2 (ja) | 2012-01-18 |
| DE602006011363D1 (de) | 2010-02-04 |
| CN101321525B (zh) | 2013-01-30 |
| PT1959951E (pt) | 2010-03-02 |
| KR101135310B1 (ko) | 2012-04-12 |
| CA2630460C (en) | 2013-01-08 |
| AU2006319247B2 (en) | 2010-03-11 |
| AU2006319247A1 (en) | 2007-06-07 |
| DK1959951T3 (da) | 2010-03-01 |
| JP2009517438A (ja) | 2009-04-30 |
| AU2006319247A8 (en) | 2008-07-17 |
| WO2007063012A1 (en) | 2007-06-07 |
| PL1959951T3 (pl) | 2010-06-30 |
| RU2008126398A (ru) | 2010-01-10 |
| RU2396269C2 (ru) | 2010-08-10 |
| ZA200804393B (en) | 2009-04-29 |
| EP1959951A1 (en) | 2008-08-27 |
| KR20080072097A (ko) | 2008-08-05 |
| US20070129544A1 (en) | 2007-06-07 |
| NO20082388L (no) | 2008-08-26 |
| TW200804357A (en) | 2008-01-16 |
| BRPI0619086A2 (pt) | 2011-09-20 |
| CA2630460A1 (en) | 2007-06-07 |
| CN101321525A (zh) | 2008-12-10 |
| EP1959951B1 (en) | 2009-12-23 |
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