EA200801536A1 - Новые тиенопирсульфоновые производные - Google Patents
Новые тиенопирсульфоновые производныеInfo
- Publication number
- EA200801536A1 EA200801536A1 EA200801536A EA200801536A EA200801536A1 EA 200801536 A1 EA200801536 A1 EA 200801536A1 EA 200801536 A EA200801536 A EA 200801536A EA 200801536 A EA200801536 A EA 200801536A EA 200801536 A1 EA200801536 A1 EA 200801536A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- optionally substituted
- group
- heterocyclyl
- substituted alkyl
- heteroatoms
- Prior art date
Links
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 102000005962 receptors Human genes 0.000 abstract 2
- 108020003175 receptors Proteins 0.000 abstract 2
- 208000000094 Chronic Pain Diseases 0.000 abstract 1
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 abstract 1
- 102100036834 Metabotropic glutamate receptor 1 Human genes 0.000 abstract 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 208000005298 acute pain Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 abstract 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 abstract 1
- 235000010290 biphenyl Nutrition 0.000 abstract 1
- 239000004305 biphenyl Substances 0.000 abstract 1
- -1 cyano, amino Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 208000028774 intestinal disease Diseases 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 108010014719 metabotropic glutamate receptor type 1 Proteins 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000002232 neuromuscular Effects 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 210000001635 urinary tract Anatomy 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
-
- 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
- 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
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P27/02—Ophthalmic agents
-
- 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
- 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
- A61P9/10—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pyridine Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Настоящее изобретение касается новых, имеющих предпочтение к рецепторам подтипов mGluR1 и mGluR5 лигандов формулы I, где Х означает группу, выбранную из SO, SO; Y означает группу, выбранную из (СН), NH, NHCH; n - целое число от 0 до 1; Z означает Н или замещающий его алкил, нитро, галоген, алкокси, трифторметил, циано, амино, алкиламино, диалкиламино, аминометил, алкиламинометил, диалкиламинометил, гидроксил, алкилсульфониламино; Rозначает необязательно замещенный алкил, циклоалкил, фенил, бифенил или гетероциклил; Rозначает необязательно замещенный фенил, гетероциклил или группу NRR, где Rи Rвыбраны независимо из группы: водород и необязательно замещенный алкил, либо Rи Rвместе с атомом N, с которым они соединены, образуют необязательно замещенный С-гетероциклил, содержащий один или несколько гетероатомов; либо группу NH-CO-NRR, где Rи Rвыбраны независимо из группы: водород и необязательно замещенный алкил, либо Rи Rвместе с атомом N, с которым они соединены, образуют необязательно замещенный Cгетероциклил, содержащий один или несколько гетероатомов; и/или их гидратов, и/или сольватов, и/или фармацевтически приемлемых солей, образованных с кислотами или основаниями; способов их получения, содержащих их фармацевтических композиций и их применения в терапии и/или профилактике таких патологических состояний, требующих модулирования рецепторов mGluRl и mG1uR5, как неврологические заболевания, психиатрические заболевания, острые и хронические боли, нервно-мышечные дисфункции нижнего отдела мочевыводящих путей и желудочно-кишечные заболевания.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU0501171A HU0501171D0 (en) | 2005-12-20 | 2005-12-20 | New compounds |
| HU0600920A HUP0600920A3 (en) | 2006-12-18 | 2006-12-18 | Substituted thieno[2,3-b]pyridines, process for their preparation, their use and pharmaceutical compositions containing them |
| PCT/HU2006/000123 WO2007072095A1 (en) | 2005-12-20 | 2006-12-19 | New compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA200801536A1 true EA200801536A1 (ru) | 2008-12-30 |
Family
ID=89987203
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200801536A EA200801536A1 (ru) | 2005-12-20 | 2006-12-19 | Новые тиенопирсульфоновые производные |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20100022521A1 (ru) |
| EP (1) | EP1963337B1 (ru) |
| JP (1) | JP2009520016A (ru) |
| KR (1) | KR20080087099A (ru) |
| AT (1) | ATE479690T1 (ru) |
| AU (1) | AU2006327899A1 (ru) |
| BR (1) | BRPI0620205A2 (ru) |
| CA (1) | CA2630739A1 (ru) |
| DE (1) | DE602006016643D1 (ru) |
| EA (1) | EA200801536A1 (ru) |
| EC (1) | ECSP088572A (ru) |
| MA (1) | MA30167B1 (ru) |
| WO (1) | WO2007072095A1 (ru) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8263773B2 (en) | 2008-06-26 | 2012-09-11 | Richter Gedeon Nyrt. | Thieno [2,3-b] pyridine compounds with mGluR activity |
| HUP0800407A2 (en) * | 2008-06-30 | 2010-03-01 | Richter Gedeon Nyrt | Thieno [2,3-b] pyridine compounds as metalotropic glutamate receptor (mglur) ligands |
| US9801863B2 (en) | 2012-04-16 | 2017-10-31 | Case Western Reserve University | Inhibitors of short-chain dehydrogenase activity for modulating hematopoietic stem cells and hematopoiesis |
| WO2013158649A1 (en) | 2012-04-16 | 2013-10-24 | Case Western Reserve University | Compositions and methods of modulating 15-pgdh activity |
| EP3057973B1 (en) * | 2013-10-15 | 2019-09-04 | Case Western Reserve University | Compositions comprising a 15-pgdh inhibitor for the healing of wounds |
| CN107921025A (zh) | 2015-03-08 | 2018-04-17 | 卡斯西部储备大学 | 用于治疗纤维症的短链脱氢酶活性的抑制剂 |
| JP7139308B2 (ja) * | 2016-07-18 | 2022-09-20 | ケース ウエスタン リザーブ ユニバーシティ | 神経新生の促進及びニュ－ロン細胞死の阻害のための短鎖脱水素酵素活性の阻害剤 |
| EP3548035A4 (en) | 2016-11-30 | 2020-07-22 | Case Western Reserve University | COMBINATIONS OF 15-PGDH INHIBITORS WITH CORCOSTEROIDS AND / OR TNF INHIBITORS AND THEIR USES |
| CN110573154A (zh) | 2017-02-06 | 2019-12-13 | 卡斯西部储备大学 | 调节短链脱氢酶活性的组合物和方法 |
| AU2018249956B2 (en) | 2017-04-07 | 2024-05-23 | Board Of Regents Of The Univeristy Of Texas | Inhibitors of short-chain dehydrogenase activity for treating coronary disorders |
| SG11202105345TA (en) | 2018-11-21 | 2021-06-29 | Univ Case Western Reserve | Compositions and methods of modulating short-chain dehydrogenase activity |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5656638A (en) * | 1995-04-18 | 1997-08-12 | Geron Corporation | Telomerase inhibitors |
| WO2001032632A2 (en) * | 1999-11-01 | 2001-05-10 | Eli Lilly And Company | Pharmaceutically active 4-substituted pyrimidine derivatives |
| US6369222B1 (en) * | 2000-07-18 | 2002-04-09 | Hoffmann-La Roche Inc. | mGluR antagonists and a method for their synthesis |
| JP2008507518A (ja) * | 2004-07-22 | 2008-03-13 | ピーティーシー セラピューティクス，インコーポレーテッド | Ｃ型肝炎を治療するためのチエノピリジン |
| US20090149495A1 (en) * | 2005-12-20 | 2009-06-11 | Katalin Nogradi | Compounds |
| HUP0501168A3 (en) * | 2005-12-20 | 2007-10-29 | Richter Gedeon Nyrt | 2-(acyl, oxycarbonyl or aminocarbonyl)-3-phenyl-thieno[2,3-b]pyridines, process for their preparation, their use and pharmaceutical composition containing them |
| HUP0501170A2 (en) * | 2005-12-20 | 2007-09-28 | Richter Gedeon Nyrt | 2-heteroaryl-3-phenyl-thieno[2,3-b]pyridines, process for their preparation, their use and pharmaceutical compositions containing them |
| US8263773B2 (en) * | 2008-06-26 | 2012-09-11 | Richter Gedeon Nyrt. | Thieno [2,3-b] pyridine compounds with mGluR activity |
-
2006
- 2006-12-19 CA CA002630739A patent/CA2630739A1/en not_active Abandoned
- 2006-12-19 JP JP2008546651A patent/JP2009520016A/ja active Pending
- 2006-12-19 US US12/158,568 patent/US20100022521A1/en not_active Abandoned
- 2006-12-19 EP EP06831522A patent/EP1963337B1/en active Active
- 2006-12-19 AU AU2006327899A patent/AU2006327899A1/en not_active Abandoned
- 2006-12-19 KR KR1020087015458A patent/KR20080087099A/ko not_active Withdrawn
- 2006-12-19 AT AT06831522T patent/ATE479690T1/de not_active IP Right Cessation
- 2006-12-19 EA EA200801536A patent/EA200801536A1/ru unknown
- 2006-12-19 WO PCT/HU2006/000123 patent/WO2007072095A1/en not_active Ceased
- 2006-12-19 BR BRPI0620205-5A patent/BRPI0620205A2/pt not_active IP Right Cessation
- 2006-12-19 DE DE602006016643T patent/DE602006016643D1/de active Active
-
2008
- 2008-06-20 EC EC2008008572A patent/ECSP088572A/es unknown
- 2008-07-18 MA MA31130A patent/MA30167B1/fr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2009520016A (ja) | 2009-05-21 |
| US20100022521A1 (en) | 2010-01-28 |
| EP1963337A1 (en) | 2008-09-03 |
| ATE479690T1 (de) | 2010-09-15 |
| KR20080087099A (ko) | 2008-09-30 |
| ECSP088572A (es) | 2008-07-30 |
| CA2630739A1 (en) | 2007-06-28 |
| BRPI0620205A2 (pt) | 2011-11-01 |
| DE602006016643D1 (de) | 2010-10-14 |
| MA30167B1 (fr) | 2009-01-02 |
| WO2007072095A1 (en) | 2007-06-28 |
| AU2006327899A1 (en) | 2007-06-28 |
| EP1963337B1 (en) | 2010-09-01 |
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