EA006708B1 - Производные 3-азабицикло (3.1.0) гексана в качестве антагонистов опиоидного рецептора - Google Patents
Производные 3-азабицикло (3.1.0) гексана в качестве антагонистов опиоидного рецептора Download PDFInfo
- Publication number
- EA006708B1 EA006708B1 EA200400467A EA200400467A EA006708B1 EA 006708 B1 EA006708 B1 EA 006708B1 EA 200400467 A EA200400467 A EA 200400467A EA 200400467 A EA200400467 A EA 200400467A EA 006708 B1 EA006708 B1 EA 006708B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- azabicyclo
- exo
- hex
- ethyl
- propyl
- Prior art date
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- 229940123257 Opioid receptor antagonist Drugs 0.000 title abstract description 3
- 150000005228 3‐azabicyclo[3.1.0]hexanes Chemical class 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 161
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 10
- -1 (3- {3- [3- ( 1 -hydroxymethylcyclopentyl) propyl] -6-isopropyl-3-azabicyclo [3.1.0] hex-6-yl} phenyl) methanesulfonamide Chemical compound 0.000 claims description 60
- 150000003839 salts Chemical class 0.000 claims description 38
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 33
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- 229910052736 halogen Inorganic materials 0.000 claims description 24
- 150000002367 halogens Chemical class 0.000 claims description 24
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- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 18
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- QFGRKFNEKRHKDU-UHFFFAOYSA-N 1-[3-[6-(3-aminophenyl)-6-ethyl-3-azabicyclo[3.1.0]hexan-3-yl]propyl]cyclohexan-1-ol Chemical compound C1C2C(CC)(C=3C=C(N)C=CC=3)C2CN1CCCC1(O)CCCCC1 QFGRKFNEKRHKDU-UHFFFAOYSA-N 0.000 claims description 13
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Classifications
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/04—Compounds containing oxirane rings containing only hydrogen and carbon atoms in addition to the ring oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
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- General Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
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- Neurology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
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- Psychology (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Nutrition Science (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
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|---|---|---|---|
| US33851101P | 2001-10-22 | 2001-10-22 | |
| PCT/IB2002/003668 WO2003035622A1 (en) | 2001-10-22 | 2002-09-09 | 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists |
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| EA200400467A1 EA200400467A1 (ru) | 2004-08-26 |
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| ATE434607T1 (de) | 2001-04-18 | 2009-07-15 | Euro Celtique Sa | 1-(4-amino-cyclohexyl)-1,3-dihydro-2h- benzimidazole-2-on derivate und verwandte verbindungen als nociceptin analoge und orl1 liganden zur behandlung von schmerz |
| SI1440059T1 (sl) * | 2001-10-22 | 2008-08-31 | Pfizer Prod Inc | Derivati 3-azabiciklo(3.1.0)heksana kot antagonisti opioidnega receptorja |
| CA2522323C (en) * | 2003-04-14 | 2009-09-15 | Pfizer Products Inc. | 3-azabicyclo[3.2.1]octane derivatives as opioid receptor ligands |
| US20050043327A1 (en) * | 2003-08-21 | 2005-02-24 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of addiction in a mammal |
| US7153976B2 (en) * | 2003-10-06 | 2006-12-26 | Pfizer Inc. | Purification process for an azabicyclo[3.1.0]hexane compound |
| AU2004281794B2 (en) * | 2003-10-14 | 2010-04-22 | Pfizer Products Inc. | Bicyclic [3.1.0] derivatives as glycine transporter inhibitors |
| KR20060096038A (ko) * | 2003-10-16 | 2006-09-05 | 화이자 프로덕츠 인크. | 3-아자비시클로〔3.1.0〕헥산 유도체의 제조법 |
| CA2557115C (en) | 2004-02-23 | 2012-10-02 | Glaxo Group Limited | Azabicyclo (3.1.0) hexane derivatives useful as modulators of dopamine d3 receptors |
| EP1726590A4 (en) * | 2004-03-05 | 2009-07-15 | Banyu Pharma Co Ltd | CYCLOALKANOPYRIDINDERIVAT |
| CA2590182A1 (en) * | 2004-12-14 | 2006-06-22 | Shionogi & Co., Ltd. | Indolomorphinan derivatives having carboxy at the 6'-position |
| GB0512099D0 (en) * | 2005-06-14 | 2005-07-20 | Glaxo Group Ltd | Compounds |
| GB0517191D0 (en) * | 2005-08-22 | 2005-09-28 | Glaxo Group Ltd | Compounds |
| US7592461B2 (en) * | 2005-12-21 | 2009-09-22 | Bristol-Myers Squibb Company | Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof |
| MY145633A (en) | 2006-03-01 | 2012-03-15 | Theravance Inc | 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| WO2008075162A2 (en) * | 2006-12-15 | 2008-06-26 | Pfizer Limited | Selective mu opioid receptor antagonists for the treatment of female sexual dysfunction |
| TWI409067B (zh) * | 2007-02-28 | 2013-09-21 | Theravance Inc | 8-氮雜雙環〔3.2.1〕辛烷化合物之結晶型 |
| WO2009029253A1 (en) * | 2007-08-27 | 2009-03-05 | Theravance, Inc. | Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| WO2009029252A1 (en) * | 2007-08-27 | 2009-03-05 | Theravance, Inc. | Amidoalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| ATE502939T1 (de) * | 2007-08-27 | 2011-04-15 | Theravance Inc | Disubstituierte alkyl-8-azabicycloä3.2.1üoktan- verbindungen als mu-opioid-rezeptorantagonisten |
| TWI423801B (zh) * | 2007-08-27 | 2014-01-21 | Theravance Inc | 作為μ類鴉片受體拮抗劑之8-氮雜雙環〔3.2.1〕辛基-2-羥基苯甲醯胺化合物 |
| US9133116B2 (en) | 2010-09-28 | 2015-09-15 | Panacea Biotec Ltd. | Bicyclic compounds |
| WO2015076310A1 (ja) | 2013-11-20 | 2015-05-28 | 株式会社 三和化学研究所 | 新規3-アザビシクロ[3.1.0]ヘキサン誘導体及びその医薬用途 |
| WO2016186184A1 (ja) * | 2015-05-20 | 2016-11-24 | 株式会社 三和化学研究所 | 新規3-アザビシクロ[3.1.0]ヘキサン誘導体の塩の結晶及びその医薬用途 |
| AU2018229062A1 (en) | 2017-03-02 | 2019-09-26 | Ube Industries, Ltd. | Therapeutic agent for alcohol use disorders |
Family Cites Families (26)
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| US2099214A (en) * | 1937-11-16 | Process fob forming the sulphuric | ||
| US2099216A (en) * | 1934-05-04 | 1937-11-16 | Frederick H Nass | Metal testing machine |
| US3004340A (en) * | 1959-09-24 | 1961-10-17 | Bernice L Collins | Kitchen utensil |
| US3078282A (en) * | 1960-01-02 | 1963-02-19 | Bayer Ag | Anthraquinone dyestuffs |
| PH24752A (en) | 1987-04-16 | 1990-10-01 | Lilly Co Eli | Piperidine opioid antagonists |
| JPH04155522A (ja) * | 1990-10-19 | 1992-05-28 | Nec Corp | ファースト・イン・ランダム・アウト回路 |
| ZA922180B (en) | 1991-03-29 | 1993-09-27 | Lilly Co Eli | Piperidine derivatives |
| US5159081A (en) | 1991-03-29 | 1992-10-27 | Eli Lilly And Company | Intermediates of peripherally selective n-carbonyl-3,4,4-trisubstituted piperidine opioid antagonists |
| GB9725114D0 (en) * | 1997-11-28 | 1998-01-28 | Pfizer Ltd | Treatment of pruritus |
| GB9810671D0 (en) | 1998-05-18 | 1998-07-15 | Pfizer Ltd | Anti-pruritic agents |
| TWI244481B (en) * | 1998-12-23 | 2005-12-01 | Pfizer | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| GB9912410D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912411D0 (en) | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912415D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912413D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| US20020064825A1 (en) | 2000-05-19 | 2002-05-30 | Lewis Marilyn Evelyn | Novel polypeptide |
| US20020025948A1 (en) * | 2000-06-23 | 2002-02-28 | Banks Bernard Joseph | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| US20030207876A1 (en) * | 2000-06-23 | 2003-11-06 | Banks Bernard Joseph | 3-Azabicyclo[3.1.0]hexane derivatives useful in therapy |
| GB0015562D0 (en) * | 2000-06-23 | 2000-08-16 | Pfizer Ltd | Heterocycles |
| DE10042885A1 (de) * | 2000-08-31 | 2002-03-14 | Heidelberger Druckmasch Ag | Bogentransportzylinder |
| SI1440059T1 (sl) | 2001-10-22 | 2008-08-31 | Pfizer Prod Inc | Derivati 3-azabiciklo(3.1.0)heksana kot antagonisti opioidnega receptorja |
| WO2003101963A1 (en) | 2002-05-30 | 2003-12-11 | Eli Lilly And Company | Opioid receptor antagonists |
| US20040204453A1 (en) | 2003-04-14 | 2004-10-14 | Pfizer Inc | 4-Phenyl-piperidine compounds and their use as modulators of opioid receptors |
| US7056930B2 (en) | 2003-04-14 | 2006-06-06 | Pfizer Inc. | 2-Azabicyclo[3.3.1]nonane derivatives |
| US20050043327A1 (en) | 2003-08-21 | 2005-02-24 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of addiction in a mammal |
| US7153976B2 (en) | 2003-10-06 | 2006-12-26 | Pfizer Inc. | Purification process for an azabicyclo[3.1.0]hexane compound |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |