JP2005511545A5 - - Google Patents
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- Publication number
- JP2005511545A5 JP2005511545A5 JP2003538138A JP2003538138A JP2005511545A5 JP 2005511545 A5 JP2005511545 A5 JP 2005511545A5 JP 2003538138 A JP2003538138 A JP 2003538138A JP 2003538138 A JP2003538138 A JP 2003538138A JP 2005511545 A5 JP2005511545 A5 JP 2005511545A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- exo
- aza
- bicyclo
- hex
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims description 17
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 229910052736 halogen Inorganic materials 0.000 claims description 11
- 150000002367 halogens Chemical class 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 9
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 229910052717 sulfur Inorganic materials 0.000 claims description 8
- 125000005842 heteroatom Chemical group 0.000 claims description 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 5
- 125000005843 halogen group Chemical group 0.000 claims description 5
- MCTWTZJPVLRJOU-UHFFFAOYSA-N 1-methyl-1H-imidazole Chemical compound CN1C=CN=C1 MCTWTZJPVLRJOU-UHFFFAOYSA-N 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 150000001721 carbon Chemical group 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 2
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims description 2
- 125000002619 bicyclic group Chemical group 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 16
- -1 2-hydroxy-1,2,3,4-tetrahydro-naphthalen-2-ylmethyl Chemical group 0.000 claims 8
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 6
- DDLNRZAJSKPWSP-UHFFFAOYSA-N 2-[[6-(3-aminophenyl)-6-ethyl-3-azabicyclo[3.1.0]hexan-3-yl]methyl]-1,3-dihydroinden-2-ol Chemical compound C12CN(CC3(O)CC4=CC=CC=C4C3)CC2C1(CC)C1=CC=CC(N)=C1 DDLNRZAJSKPWSP-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 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 1
- PACFFBCNNSRDCR-UHFFFAOYSA-N 1-[3-[6-(3-aminophenyl)-6-propan-2-yl-3-azabicyclo[3.1.0]hexan-3-yl]propyl]cyclohexan-1-ol Chemical compound C1C2C(C(C)C)(C=3C=C(N)C=CC=3)C2CN1CCCC1(O)CCCCC1 PACFFBCNNSRDCR-UHFFFAOYSA-N 0.000 claims 1
- LWPCAAAKAPPOFX-UHFFFAOYSA-N 2-[[6-(3-aminophenyl)-6-ethyl-3-azabicyclo[3.1.0]hexan-3-yl]methyl]-3,4-dihydro-1H-naphthalen-2-ol Chemical compound C12CN(CC3(O)CC4=CC=CC=C4CC3)CC2C1(CC)C1=CC=CC(N)=C1 LWPCAAAKAPPOFX-UHFFFAOYSA-N 0.000 claims 1
- DBGVUCQKUIZWQG-UHFFFAOYSA-N 2-[[6-(3-aminophenyl)-6-propyl-3-azabicyclo[3.1.0]hexan-3-yl]methyl]-1,3-dihydroinden-2-ol Chemical compound C12CN(CC3(O)CC4=CC=CC=C4C3)CC2C1(CCC)C1=CC=CC(N)=C1 DBGVUCQKUIZWQG-UHFFFAOYSA-N 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 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 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 0 CCC*(C)c1cccc(*)c1CC Chemical compound CCC*(C)c1cccc(*)c1CC 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007272602A Division JP2008069169A (ja) | 2001-10-22 | 2007-10-19 | オピオイド受容体アンタゴニストとしての３−アザビシクロ（３．１．０）ヘキサン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005511545A JP2005511545A (ja) | 2005-04-28 |
| JP2005511545A5 true JP2005511545A5 (https=) | 2007-12-13 |
| JP4155522B2 JP4155522B2 (ja) | 2008-09-24 |
Family
ID=23325099
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003538138A Expired - Fee Related JP4155522B2 (ja) | 2001-10-22 | 2002-09-09 | オピオイド受容体アンタゴニストとしての３−アザビシクロ（３．１．０）ヘキサン誘導体 |
| JP2007272602A Pending JP2008069169A (ja) | 2001-10-22 | 2007-10-19 | オピオイド受容体アンタゴニストとしての３−アザビシクロ（３．１．０）ヘキサン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007272602A Pending JP2008069169A (ja) | 2001-10-22 | 2007-10-19 | オピオイド受容体アンタゴニストとしての３−アザビシクロ（３．１．０）ヘキサン誘導体 |
Country Status (42)
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ551453A (en) | 2001-04-18 | 2008-02-29 | Euro Celtique Sa | Nociceptin analogs for the treatment of pain |
| EP1440059B1 (en) * | 2001-10-22 | 2008-04-16 | Pfizer Products Inc. | 3-azabicyclo(3.1.0)hexane derivatives as opioid receptor antagonists |
| BRPI0409307A (pt) * | 2003-04-14 | 2006-04-25 | Pfizer Prod Inc | derivados de 3-azabiciclo[3.2.1]octano |
| 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 |
| KR20060095865A (ko) * | 2003-10-14 | 2006-09-04 | 화이자 프로덕츠 인크. | 글리신 수송 억제제로서의 비시클릭 [3.1.0] 유도체 |
| RU2006112576A (ru) * | 2003-10-16 | 2006-08-27 | Пфайзер Продактс Инк. (Us) | Получение производных 3-азабицикло [3.1.0] гексана |
| PE20051173A1 (es) | 2004-02-23 | 2006-02-14 | Glaxo Group Ltd | Compuestos azabiciclico (3.1.0) hexanos como moduladores de receptores de dopamina d3 |
| JPWO2005085228A1 (ja) * | 2004-03-05 | 2008-01-17 | 萬有製薬株式会社 | シクロアルカノピリジン誘導体 |
| US20080227803A1 (en) * | 2004-12-14 | 2008-09-18 | Shioonogi & Co., Ltd., A Legal Entity Of Japan | Indolomorphinan Derivative Having Carboxy in 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 |
| US7947710B2 (en) * | 2007-08-27 | 2011-05-24 | Theravance, Inc. | Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| 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 |
| US7691878B2 (en) * | 2007-08-27 | 2010-04-06 | 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 |
| JP2013542929A (ja) | 2010-09-28 | 2013-11-28 | パナセア バイオテック リミテッド | 新規ビシクロ環化合物 |
| US9663463B2 (en) * | 2013-11-20 | 2017-05-30 | Sanwa Kagaku Kenkyusho Co., Ltd. | 3-azabicyclo[3.1.0]hexane derivative and use thereof for medical purpose |
| KR20180004734A (ko) * | 2015-05-20 | 2018-01-12 | 가부시키가이샤산와카가쿠켄큐쇼 | 신규 3-아자비시클로［3.1.0］헥산 유도체의 염의 결정 및 그의 의약 용도 |
| CN110352055A (zh) | 2017-03-02 | 2019-10-18 | 株式会社三和化学研究所 | 酒精使用障碍的治疗药物 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CA1321792C (en) | 1987-04-16 | 1993-08-31 | Eli Lilly And Company | 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 |
| NZ242117A (en) | 1991-03-29 | 1994-11-25 | Lilly Co Eli | 4-phenylpiperidine derivatives and medicaments containing them |
| 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 |
| GB9912413D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds 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 |
| 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 |
| GB0015562D0 (en) * | 2000-06-23 | 2000-08-16 | Pfizer Ltd | Heterocycles |
| US20030207876A1 (en) * | 2000-06-23 | 2003-11-06 | Banks Bernard Joseph | 3-Azabicyclo[3.1.0]hexane derivatives useful in therapy |
| DE10042885A1 (de) * | 2000-08-31 | 2002-03-14 | Heidelberger Druckmasch Ag | Bogentransportzylinder |
| EP1440059B1 (en) | 2001-10-22 | 2008-04-16 | Pfizer Products Inc. | 3-azabicyclo(3.1.0)hexane derivatives as opioid receptor antagonists |
| US20050222204A1 (en) | 2002-05-30 | 2005-10-06 | Mitch Charles H | Opioid receptor antagonists |
| US7056930B2 (en) * | 2003-04-14 | 2006-06-06 | Pfizer Inc. | 2-Azabicyclo[3.3.1]nonane derivatives |
| US20040204453A1 (en) * | 2003-04-14 | 2004-10-14 | Pfizer Inc | 4-Phenyl-piperidine compounds and their use as modulators of opioid receptors |
| 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 |
-
2002
- 2002-09-09 EP EP02765197A patent/EP1440059B1/en not_active Expired - Lifetime
- 2002-09-09 AP APAP/P/2004/003007A patent/AP1816A/en active
- 2002-09-09 PL PL02368919A patent/PL368919A1/xx not_active Application Discontinuation
- 2002-09-09 JP JP2003538138A patent/JP4155522B2/ja not_active Expired - Fee Related
- 2002-09-09 HR HRP20040288 patent/HRP20040288A2/hr not_active Application Discontinuation
- 2002-09-09 RS YUP-251/04A patent/RS25104A/sr unknown
- 2002-09-09 EA EA200400467A patent/EA006708B1/ru not_active IP Right Cessation
- 2002-09-09 IL IL16115702A patent/IL161157A0/xx unknown
- 2002-09-09 AT AT02765197T patent/ATE392415T1/de not_active IP Right Cessation
- 2002-09-09 DK DK02765197T patent/DK1440059T3/da active
- 2002-09-09 BR BR0213464-0A patent/BR0213464A/pt not_active IP Right Cessation
- 2002-09-09 SI SI200230688T patent/SI1440059T1/sl unknown
- 2002-09-09 HU HU0401884A patent/HUP0401884A2/hu unknown
- 2002-09-09 OA OA1200400109A patent/OA12711A/en unknown
- 2002-09-09 AU AU2002329557A patent/AU2002329557B2/en not_active Ceased
- 2002-09-09 DE DE60226161T patent/DE60226161T2/de not_active Expired - Lifetime
- 2002-09-09 KR KR1020047006011A patent/KR100621292B1/ko not_active Expired - Fee Related
- 2002-09-09 UA UA20040402979A patent/UA75714C2/uk unknown
- 2002-09-09 MX MXPA04003730A patent/MXPA04003730A/es active IP Right Grant
- 2002-09-09 CA CA002463264A patent/CA2463264C/en not_active Expired - Fee Related
- 2002-09-09 ES ES02765197T patent/ES2302839T3/es not_active Expired - Lifetime
- 2002-09-09 WO PCT/IB2002/003668 patent/WO2003035622A1/en not_active Ceased
- 2002-09-09 NZ NZ531807A patent/NZ531807A/xx unknown
- 2002-09-09 PT PT02765197T patent/PT1440059E/pt unknown
- 2002-09-09 GE GEAP20028173A patent/GEP20084300B/en unknown
- 2002-09-09 CN CNB028208854A patent/CN100368398C/zh not_active Expired - Fee Related
- 2002-10-16 PY PY200200225353A patent/PY0225353A/es unknown
- 2002-10-17 MY MYPI20023878A patent/MY136580A/en unknown
- 2002-10-17 PA PA20028556701A patent/PA8556701A1/es unknown
- 2002-10-18 HN HN2002000299A patent/HN2002000299A/es unknown
- 2002-10-18 PE PE2002001032A patent/PE20030610A1/es not_active Application Discontinuation
- 2002-10-21 AR ARP020103960A patent/AR036905A1/es unknown
- 2002-10-21 SV SV2002001363A patent/SV2004001363A/es not_active Application Discontinuation
- 2002-10-22 US US10/278,142 patent/US7049335B2/en not_active Expired - Fee Related
- 2002-10-22 GT GT200200216A patent/GT200200216A/es unknown
-
2004
- 2004-03-18 IS IS7187A patent/IS7187A/is unknown
- 2004-03-18 ZA ZA200402172A patent/ZA200402172B/en unknown
- 2004-03-29 IL IL161157A patent/IL161157A/en not_active IP Right Cessation
- 2004-04-15 MA MA27630A patent/MA27141A1/fr unknown
- 2004-04-20 CR CR7317A patent/CR7317A/es unknown
- 2004-04-21 NO NO20041626A patent/NO329092B1/no not_active IP Right Cessation
- 2004-04-21 TN TNP2004000071A patent/TNSN04071A1/fr unknown
- 2004-04-22 EC EC2004005077A patent/ECSP045077A/es unknown
-
2005
- 2005-02-24 US US11/066,095 patent/US20050171178A1/en not_active Abandoned
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2006
- 2006-03-01 US US11/366,903 patent/US20070054950A1/en not_active Abandoned
-
2007
- 2007-10-19 JP JP2007272602A patent/JP2008069169A/ja active Pending