DE60207744T2 - Verfahren zur herstellung von 1,5,6,7-tetrahydropyrrolo[3,2-c]derivaten zur behandlung der fettleibigkeit - Google Patents
Verfahren zur herstellung von 1,5,6,7-tetrahydropyrrolo[3,2-c]derivaten zur behandlung der fettleibigkeit Download PDFInfo
- Publication number
- DE60207744T2 DE60207744T2 DE60207744T DE60207744T DE60207744T2 DE 60207744 T2 DE60207744 T2 DE 60207744T2 DE 60207744 T DE60207744 T DE 60207744T DE 60207744 T DE60207744 T DE 60207744T DE 60207744 T2 DE60207744 T2 DE 60207744T2
- Authority
- DE
- Germany
- Prior art keywords
- alkyl
- alkoxy
- optionally substituted
- trifluoromethyl
- phenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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- 125000000217 alkyl group Chemical group 0.000 claims description 212
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 145
- -1 trifluoromethoxy, carboxyl Chemical group 0.000 claims description 138
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 119
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 119
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- 125000000449 nitro group Chemical class [O-][N+](*)=O 0.000 claims description 50
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- VMNFCTDOMRUEJN-UHFFFAOYSA-N 1-(2-chlorophenyl)-2-(4-methoxyphenyl)-3-methyl-5-piperidin-1-yl-6,7-dihydropyrrolo[3,2-c]pyridin-4-one;hydrochloride Chemical compound Cl.C1=CC(OC)=CC=C1C(N1C=2C(=CC=CC=2)Cl)=C(C)C(C2=O)=C1CCN2N1CCCCC1 VMNFCTDOMRUEJN-UHFFFAOYSA-N 0.000 claims description 3
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
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- A61P3/04—Anorexiants; Antiobesity agents
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- 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
- A61P9/10—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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- Engineering & Computer Science (AREA)
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- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
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- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32444301P | 2001-09-24 | 2001-09-24 | |
| US324443P | 2001-09-24 | ||
| PCT/US2002/030541 WO2003027114A1 (en) | 2001-09-24 | 2002-09-24 | Preparation and use of 1,5,6,7-tetrahydropyrrolo[3,2-c]pyridine derivatives for treatment of obesity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60207744D1 DE60207744D1 (de) | 2006-01-05 |
| DE60207744T2 true DE60207744T2 (de) | 2006-08-03 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60207744T Expired - Fee Related DE60207744T2 (de) | 2001-09-24 | 2002-09-24 | Verfahren zur herstellung von 1,5,6,7-tetrahydropyrrolo[3,2-c]derivaten zur behandlung der fettleibigkeit |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US7071207B2 (https=) |
| EP (1) | EP1432708B1 (https=) |
| JP (1) | JP2005504100A (https=) |
| AT (1) | ATE311386T1 (https=) |
| CA (1) | CA2461142A1 (https=) |
| DE (1) | DE60207744T2 (https=) |
| ES (1) | ES2252524T3 (https=) |
| MX (1) | MXPA04002249A (https=) |
| WO (1) | WO2003027114A1 (https=) |
Families Citing this family (49)
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| JP3813152B2 (ja) | 2002-03-12 | 2006-08-23 | メルク エンド カムパニー インコーポレーテッド | 置換アミド類 |
| EP1558252B1 (en) | 2002-08-02 | 2007-10-10 | Merck & Co., Inc. | Substituted furo [2,3-b]pyridine derivatives |
| US7129239B2 (en) | 2002-10-28 | 2006-10-31 | Pfizer Inc. | Purine compounds and uses thereof |
| US7247628B2 (en) | 2002-12-12 | 2007-07-24 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| CN101012193A (zh) | 2003-01-02 | 2007-08-08 | 霍夫曼-拉罗奇有限公司 | 新cb 1受体反激动剂 |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| US7329658B2 (en) | 2003-02-06 | 2008-02-12 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| US7176210B2 (en) | 2003-02-10 | 2007-02-13 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7141669B2 (en) | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod receptor ligands and uses thereof |
| US7268133B2 (en) | 2003-04-23 | 2007-09-11 | Pfizer, Inc. Patent Department | Cannabinoid receptor ligands and uses thereof |
| US7232823B2 (en) | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| WO2005007628A1 (en) | 2003-07-11 | 2005-01-27 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives as cannabinoid receptor modulators |
| JP2007501827A (ja) * | 2003-08-08 | 2007-02-01 | ファルマシア・イタリア・エス・ピー・エー | キナーゼ阻害剤として活性なピリミジルピロール誘導体 |
| US20050043346A1 (en) * | 2003-08-08 | 2005-02-24 | Pharmacia Italia S.P.A. | Pyridylpyrrole derivatives active as kinase inhibitors |
| US7326706B2 (en) | 2003-08-15 | 2008-02-05 | Bristol-Myers Squibb Company | Pyrazine modulators of cannabinoid receptors |
| US7151097B2 (en) | 2003-11-07 | 2006-12-19 | Pfizer Inc. | Bicyclic pyrazolyl and imidazolyl compounds and uses thereof |
| EP1734963A4 (en) | 2004-04-02 | 2008-06-18 | Merck & Co Inc | METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER |
| TW200602314A (en) | 2004-05-28 | 2006-01-16 | Tanabe Seiyaku Co | A novel pyrrolidine compound and a process for preparing the same |
| CA2613678A1 (en) | 2005-06-02 | 2006-12-07 | Glenmark Pharmaceuticals S.A. | Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
| US7923465B2 (en) | 2005-06-02 | 2011-04-12 | Glenmark Pharmaceuticals S.A. | Cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
| AR056560A1 (es) | 2005-10-06 | 2007-10-10 | Astrazeneca Ab | Pirrolopiridinonas como moduladores cb1 |
| US7618982B2 (en) | 2005-12-19 | 2009-11-17 | Nerviano Medical Sciences S.R.L. | Heteroarylpyrrolopyridinones active as kinase inhibitors |
| CN101007815B (zh) * | 2006-01-27 | 2010-06-23 | 江苏恒瑞医药股份有限公司 | 吡咯并六元杂环化合物及其在医药上的用途 |
| DK1973910T3 (da) | 2006-01-27 | 2013-08-12 | Shanghai Hengrui Pharm Co Ltd | Pyrrolo[3,2-c]pyridin-4-on-2-indolinon-proteinkinaseinhibitorer |
| ES2546816T3 (es) | 2007-02-27 | 2015-09-28 | Nerviano Medical Sciences S.R.L. | Isoquinolinpirrolopiridinonas activas como inhibidores de cinasa |
| AR065909A1 (es) * | 2007-04-03 | 2009-07-08 | Astrazeneca Ab | Agentes terapeuticos 685 |
| AR066207A1 (es) * | 2007-04-03 | 2009-08-05 | Astrazeneca Ab | Agentes terapeuticos 684 |
| WO2008134354A1 (en) * | 2007-04-27 | 2008-11-06 | Array Biopharma, Inc. | TNF-α PRODUCTION INHIBITOR |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
| MX354786B (es) | 2007-06-04 | 2018-03-21 | Synergy Pharmaceuticals Inc | Agonistas de guanilato ciclasa utiles para el tratamiento de trastornos gastrointestinales, inflamacion, cancer y otros trastornos. |
| EP2003129B1 (en) | 2007-06-11 | 2017-08-09 | Nerviano Medical Sciences S.r.l. | 1H-Pyrido[3,4-B]indol-1-one and 2,3,4,9-Tetrahydro-1H-Beta-Carbolin-1-one Derivatives |
| ES2522968T3 (es) | 2008-06-04 | 2014-11-19 | Synergy Pharmaceuticals Inc. | Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos |
| AU2009270833B2 (en) | 2008-07-16 | 2015-02-19 | Bausch Health Ireland Limited | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
| EP2348857B1 (en) | 2008-10-22 | 2016-02-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| US8329914B2 (en) | 2008-10-31 | 2012-12-11 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| JP2013520502A (ja) | 2010-02-25 | 2013-06-06 | メルク・シャープ・エンド・ドーム・コーポレイション | 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体 |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| SG192941A1 (en) | 2011-02-25 | 2013-09-30 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| RU2015106909A (ru) | 2012-08-02 | 2016-09-27 | Мерк Шарп И Доум Корп. | Антидиабетические трициклические соединения |
| KR20150118158A (ko) | 2013-02-22 | 2015-10-21 | 머크 샤프 앤드 돔 코포레이션 | 항당뇨병 비시클릭 화합물 |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| AU2014235215A1 (en) | 2013-03-15 | 2015-10-01 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
| AU2014235209B2 (en) | 2013-03-15 | 2018-06-14 | Bausch Health Ireland Limited | Guanylate cyclase receptor agonists combined with other drugs |
| BR112015030326A2 (pt) | 2013-06-05 | 2017-08-29 | Synergy Pharmaceuticals Inc | Agonistas ultrapuros de guanilato ciclase c, método de fabricar e usar os mesmos |
| EP3033342A1 (en) * | 2013-08-13 | 2016-06-22 | Grünenthal GmbH | Annelated pyrroles and their use as crac inhibitors |
| JO3442B1 (ar) | 2013-10-07 | 2019-10-20 | Takeda Pharmaceuticals Co | مضادات ذات نوع فرعي من مستقبل سوماتوستاتين 5 (sstr5) |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1484140A (en) | 1974-04-24 | 1977-08-24 | Wyeth John & Brother Ltd | Pyrrolopyridine derivatives |
| US4897390A (en) * | 1987-07-21 | 1990-01-30 | Ruhe Rodney C | Novel anti-obesity compounds and method of use |
| KR960705824A (ko) * | 1993-10-20 | 1996-11-08 | 아사이 이페이 | 인돌 유도체(Indole Derivative) |
| KR100251522B1 (ko) * | 1997-08-13 | 2000-08-01 | 김충섭 | 할로알콕시기를 함유하는 피롤[3,2-c]퀴놀린 유도체 및 약학적으로 허용되는 그의 염 |
| ATE328887T1 (de) | 1999-01-19 | 2006-06-15 | Neurosearch As | Kondensierte heterocyclische verbindungen und ihre verwendung zur behandlung von neurodegenerativen erkrankungen |
| CA2376158C (en) | 1999-07-06 | 2011-03-15 | Endorecherche, Inc. | Use of selective estrogen receptor modulators in the manufacture of medicaments for treating and/or suppressing weight gain |
-
2002
- 2002-09-24 MX MXPA04002249A patent/MXPA04002249A/es active IP Right Grant
- 2002-09-24 CA CA002461142A patent/CA2461142A1/en not_active Abandoned
- 2002-09-24 AT AT02780364T patent/ATE311386T1/de not_active IP Right Cessation
- 2002-09-24 ES ES02780364T patent/ES2252524T3/es not_active Expired - Lifetime
- 2002-09-24 US US10/487,976 patent/US7071207B2/en not_active Expired - Fee Related
- 2002-09-24 DE DE60207744T patent/DE60207744T2/de not_active Expired - Fee Related
- 2002-09-24 EP EP02780364A patent/EP1432708B1/en not_active Expired - Lifetime
- 2002-09-24 JP JP2003530702A patent/JP2005504100A/ja not_active Withdrawn
- 2002-09-24 WO PCT/US2002/030541 patent/WO2003027114A1/en not_active Ceased
-
2006
- 2006-01-18 US US11/335,349 patent/US20060122215A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2005504100A (ja) | 2005-02-10 |
| EP1432708B1 (en) | 2005-11-30 |
| US20040224970A1 (en) | 2004-11-11 |
| ES2252524T3 (es) | 2006-05-16 |
| DE60207744D1 (de) | 2006-01-05 |
| CA2461142A1 (en) | 2003-04-03 |
| US20060122215A1 (en) | 2006-06-08 |
| ATE311386T1 (de) | 2005-12-15 |
| WO2003027114A1 (en) | 2003-04-03 |
| US7071207B2 (en) | 2006-07-04 |
| EP1432708A1 (en) | 2004-06-30 |
| MXPA04002249A (es) | 2004-06-29 |
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