JP2009528371A5 - - Google Patents
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- Publication number
- JP2009528371A5 JP2009528371A5 JP2008557405A JP2008557405A JP2009528371A5 JP 2009528371 A5 JP2009528371 A5 JP 2009528371A5 JP 2008557405 A JP2008557405 A JP 2008557405A JP 2008557405 A JP2008557405 A JP 2008557405A JP 2009528371 A5 JP2009528371 A5 JP 2009528371A5
- Authority
- JP
- Japan
- Prior art keywords
- azabicyclo
- benzamide
- endo
- oct
- ethyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 27
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 11
- 125000005843 halogen group Chemical group 0.000 claims 10
- 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 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- XKTYXVDYIKIYJP-UHFFFAOYSA-N 3h-dioxole Chemical compound C1OOC=C1 XKTYXVDYIKIYJP-UHFFFAOYSA-N 0.000 claims 2
- -1 4,4-difluoro-cyclohexyl Chemical group 0.000 claims 2
- GWRSATNRNFYMDI-UHFFFAOYSA-N 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-n-(1-methylpiperidin-4-yl)benzamide Chemical compound FC=1C=C(NC=2N=C3N(C4CCCC4)CC(F)(F)C(=O)N(C)C3=CN=2)C(OC)=CC=1C(=O)NC1CCN(C)CC1 GWRSATNRNFYMDI-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000005466 alkylenyl group Chemical group 0.000 claims 2
- 125000005605 benzo group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 102000051367 mu Opioid Receptors Human genes 0.000 claims 2
- 108020001612 μ-opioid receptors Proteins 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- JQJMOQDSYKZKJS-UHFFFAOYSA-N C1(CCCC1)CN(CCN1C2CC(CC1CC2)C1=C(C(=O)N)C=CC=C1)C(CO)=O Chemical compound C1(CCCC1)CN(CCN1C2CC(CC1CC2)C1=C(C(=O)N)C=CC=C1)C(CO)=O JQJMOQDSYKZKJS-UHFFFAOYSA-N 0.000 claims 1
- 208000030053 Opioid-Induced Constipation Diseases 0.000 claims 1
- 206010054048 Postoperative ileus Diseases 0.000 claims 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229940124636 opioid drug Drugs 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US77796206P | 2006-03-01 | 2006-03-01 | |
| US60/777,962 | 2006-03-01 | ||
| US84102806P | 2006-08-30 | 2006-08-30 | |
| US60/841,028 | 2006-08-30 | ||
| PCT/US2007/005388 WO2007103187A2 (en) | 2006-03-01 | 2007-02-28 | 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012171119A Division JP2012211193A (ja) | 2006-03-01 | 2012-08-01 | ミューオピオイド受容体拮抗剤としての８−アザビシクロ［３．２．１］オクタン化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009528371A JP2009528371A (ja) | 2009-08-06 |
| JP2009528371A5 true JP2009528371A5 (enExample) | 2010-04-08 |
| JP5086280B2 JP5086280B2 (ja) | 2012-11-28 |
Family
ID=38436795
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008557405A Active JP5086280B2 (ja) | 2006-03-01 | 2007-02-28 | ミューオピオイド受容体拮抗剤としての８−アザビシクロ［３．２．１］オクタン化合物 |
| JP2012171119A Withdrawn JP2012211193A (ja) | 2006-03-01 | 2012-08-01 | ミューオピオイド受容体拮抗剤としての８−アザビシクロ［３．２．１］オクタン化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012171119A Withdrawn JP2012211193A (ja) | 2006-03-01 | 2012-08-01 | ミューオピオイド受容体拮抗剤としての８−アザビシクロ［３．２．１］オクタン化合物 |
Country Status (24)
| Country | Link |
|---|---|
| US (11) | US7622508B2 (enExample) |
| EP (1) | EP2001876B1 (enExample) |
| JP (2) | JP5086280B2 (enExample) |
| KR (1) | KR101376479B1 (enExample) |
| AR (1) | AR059690A1 (enExample) |
| AT (1) | ATE509928T1 (enExample) |
| AU (1) | AU2007224213B2 (enExample) |
| BR (1) | BRPI0708490B8 (enExample) |
| CA (1) | CA2646409C (enExample) |
| CY (1) | CY1111747T1 (enExample) |
| DK (1) | DK2001876T3 (enExample) |
| HR (1) | HRP20110590T1 (enExample) |
| IL (1) | IL193690A (enExample) |
| MA (1) | MA30284B1 (enExample) |
| MX (1) | MX2008011165A (enExample) |
| MY (1) | MY145633A (enExample) |
| NZ (1) | NZ570764A (enExample) |
| PE (1) | PE20071311A1 (enExample) |
| PL (1) | PL2001876T3 (enExample) |
| PT (1) | PT2001876E (enExample) |
| RU (1) | RU2423362C2 (enExample) |
| SI (1) | SI2001876T1 (enExample) |
| TW (1) | TWI379832B (enExample) |
| WO (1) | WO2007103187A2 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY145633A (en) * | 2006-03-01 | 2012-03-15 | Theravance Inc | 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| 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 |
| TWI415850B (zh) * | 2007-07-20 | 2013-11-21 | Theravance Inc | 製備ｍｕ類鴉片受體拮抗劑之中間物的方法 |
| 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 |
| US7947710B2 (en) * | 2007-08-27 | 2011-05-24 | Theravance, Inc. | Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| EP2195313B1 (en) * | 2007-08-27 | 2014-04-02 | Theravance, Inc. | Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| ES2390195T3 (es) * | 2007-08-27 | 2012-11-07 | Theravance, Inc. | Compuestos de amidoalquil-8-azabiciclo(3,2,1)octano, como antagonistas del receptor opioide mu |
| WO2011035142A1 (en) * | 2009-09-18 | 2011-03-24 | Adolor Corporation | Use of opioid receptor antagonist for gastrointestinal tract disorders |
| US20120122928A1 (en) | 2010-08-11 | 2012-05-17 | Bayer Cropscience Ag | Heteroarylpiperidine and -Piperazine Derivatives as Fungicides |
| US8759527B2 (en) | 2010-08-25 | 2014-06-24 | Bayer Cropscience Ag | Heteroarylpiperidine and -piperazine derivatives as fungicides |
| EP2423210A1 (de) | 2010-08-25 | 2012-02-29 | Bayer CropScience AG | Heteroarylpiperidin- und -piperazinderivate als Fungizide |
| MX352731B (es) | 2010-10-27 | 2017-12-06 | Bayer Ip Gmbh | Derivados de heteroarilpiperidina y -piperazina como fungicidas. |
| JP5703009B2 (ja) * | 2010-12-16 | 2015-04-15 | 住友精化株式会社 | スルホン化合物、スルホン化合物の製造方法、および電気化学デバイス用電解液 |
| KR101848116B1 (ko) | 2011-02-01 | 2018-04-11 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 살진균제로서의 헤테로아릴 피페리딘 및 헤테로아릴 피페라진 유도체 |
| IN2014CN01862A (enExample) | 2011-09-15 | 2015-05-29 | Bayer Ip Gmbh | |
| EP2921492B1 (de) | 2011-12-27 | 2017-09-06 | Bayer Intellectual Property GmbH | Heteroarylpiperidin- und -heteroarylpiperazinderivate |
| US9192570B2 (en) | 2013-12-20 | 2015-11-24 | AntiOP, Inc. | Intranasal naloxone compositions and methods of making and using same |
| PT3277278T (pt) | 2015-04-02 | 2020-04-16 | Theravance Biopharma R&D Ip Llc | Forma farmacêutica de combinação de um antagonista do recetor opioide mu e um agente opioide |
| SG11202007422QA (en) | 2018-02-05 | 2020-09-29 | Alkermes Inc | Compounds for the treatment of pain |
| EP4240740A4 (en) * | 2020-11-06 | 2024-12-11 | Actinogen Medical Limited | PROCESS FOR PREPARING HETEROCYCLIC METHANONE COMPOUNDS AND AZABICYCLO INTERMEDIATES THEREOF |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1067824B (de) * | 1954-10-20 | 1959-10-29 | Sandoz Ag | Verfahren zur Herstellung saeureamidartiger Tropanabkoemmlinge |
| 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 |
| UA58476C2 (uk) * | 1997-10-09 | 2003-08-15 | Санофі-Сентелябо | Похідні 8-азабіцикло[3.2.1]октан-3-метанаміну, фармацевтична композиція та лікарський засіб |
| US6900228B1 (en) | 1998-03-10 | 2005-05-31 | Research Triangle Institute | Opiate compounds, methods of making and methods of use |
| 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 |
| US6469030B2 (en) | 1999-11-29 | 2002-10-22 | Adolor Corporation | Methods for the treatment and prevention of ileus |
| KR20030009376A (ko) | 2000-03-03 | 2003-01-29 | 오르토-맥네일 파마슈티칼, 인코퍼레이티드 | 3-(디아릴메틸렌)-8-아자비사이클로[3.2.1]옥탄 유도체 |
| US20030181447A1 (en) * | 2001-02-22 | 2003-09-25 | Boyd Robert E. | 3-(Diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives |
| US20020025948A1 (en) | 2000-06-23 | 2002-02-28 | Banks Bernard Joseph | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| JP4009251B2 (ja) | 2001-10-09 | 2007-11-14 | 杏林製薬株式会社 | 新規な４−（２−フロイル）アミノピペリジン、その合成中間体、その製造方法および医薬としてのその用途 |
| GEP20084300B (en) | 2001-10-22 | 2008-02-11 | Pfizer Prod Inc | 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists |
| US7381721B2 (en) | 2003-03-17 | 2008-06-03 | Adolor Corporation | Substituted piperidine compounds |
| US20040204453A1 (en) | 2003-04-14 | 2004-10-14 | Pfizer Inc | 4-Phenyl-piperidine compounds and their use as modulators of opioid receptors |
| JP3984281B2 (ja) * | 2003-04-14 | 2007-10-03 | ファイザー・プロダクツ・インク | ３−アザビシクロ〔３，２，１〕オクタン誘導体 |
| US7056930B2 (en) | 2003-04-14 | 2006-06-06 | Pfizer Inc. | 2-Azabicyclo[3.3.1]nonane derivatives |
| CA2522199A1 (en) | 2003-04-15 | 2004-10-28 | Pfizer Products Inc. | 3-benzhydrylidene-8-aza-bicyclo¬3.2.1|octane derivatives with opioid receptor activity |
| US6992090B2 (en) | 2003-06-16 | 2006-01-31 | Adolor Corporation | Substituted piperidine compounds and methods of their use |
| EP1737853A1 (en) | 2004-02-03 | 2007-01-03 | Janssen Pharmaceutica N.V. | 3-(diheteroarylmethylene)-8-azabicyclo¬3.2.1|octane and 3-((aryl)(heteroaryl)methylene)-8-azabicyclo¬3.2.1|octane derivatives |
| US7087749B2 (en) | 2004-03-11 | 2006-08-08 | Adolor Corporation | Substituted piperidine compounds and methods of their use |
| US7538110B2 (en) | 2005-10-27 | 2009-05-26 | Adolor Corporation | Opioid antagonists |
| MY145633A (en) | 2006-03-01 | 2012-03-15 | Theravance Inc | 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| MX2009004965A (es) | 2006-11-07 | 2009-06-05 | Nektar Therapeutics Al Corp | Formas de dosificacion y co-administracion de un agonista de opioides y un antagonista de opioides. |
| 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 |
| TWI415850B (zh) * | 2007-07-20 | 2013-11-21 | Theravance Inc | 製備ｍｕ類鴉片受體拮抗劑之中間物的方法 |
| EP2195313B1 (en) * | 2007-08-27 | 2014-04-02 | Theravance, Inc. | Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| 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 |
| ES2390195T3 (es) | 2007-08-27 | 2012-11-07 | Theravance, Inc. | Compuestos de amidoalquil-8-azabiciclo(3,2,1)octano, como antagonistas del receptor opioide mu |
-
2007
- 2007-02-07 MY MYPI20070176A patent/MY145633A/en unknown
- 2007-02-26 TW TW096106339A patent/TWI379832B/zh active
- 2007-02-28 BR BRPI0708490A patent/BRPI0708490B8/pt not_active IP Right Cessation
- 2007-02-28 EP EP07752111A patent/EP2001876B1/en active Active
- 2007-02-28 SI SI200730691T patent/SI2001876T1/sl unknown
- 2007-02-28 AT AT07752111T patent/ATE509928T1/de active
- 2007-02-28 PL PL07752111T patent/PL2001876T3/pl unknown
- 2007-02-28 KR KR1020087024027A patent/KR101376479B1/ko active Active
- 2007-02-28 AR ARP070100835A patent/AR059690A1/es active IP Right Grant
- 2007-02-28 US US11/711,961 patent/US7622508B2/en active Active
- 2007-02-28 WO PCT/US2007/005388 patent/WO2007103187A2/en not_active Ceased
- 2007-02-28 RU RU2008138875/04A patent/RU2423362C2/ru active
- 2007-02-28 JP JP2008557405A patent/JP5086280B2/ja active Active
- 2007-02-28 CA CA2646409A patent/CA2646409C/en active Active
- 2007-02-28 NZ NZ570764A patent/NZ570764A/en not_active IP Right Cessation
- 2007-02-28 DK DK07752111.0T patent/DK2001876T3/da active
- 2007-02-28 MX MX2008011165A patent/MX2008011165A/es active IP Right Grant
- 2007-02-28 AU AU2007224213A patent/AU2007224213B2/en active Active
- 2007-02-28 HR HR20110590T patent/HRP20110590T1/hr unknown
- 2007-02-28 PE PE2007000212A patent/PE20071311A1/es active IP Right Grant
- 2007-02-28 PT PT07752111T patent/PT2001876E/pt unknown
-
2008
- 2008-08-26 IL IL193690A patent/IL193690A/en active IP Right Grant
- 2008-09-17 MA MA31246A patent/MA30284B1/fr unknown
-
2009
- 2009-10-14 US US12/578,715 patent/US8263618B2/en active Active
-
2011
- 2011-08-09 CY CY20111100762T patent/CY1111747T1/el unknown
-
2012
- 2012-06-20 US US13/527,942 patent/US8664242B2/en active Active
- 2012-08-01 JP JP2012171119A patent/JP2012211193A/ja not_active Withdrawn
-
2014
- 2014-01-15 US US14/156,014 patent/US8927573B2/en active Active
- 2014-11-06 US US14/534,798 patent/US9206172B2/en active Active
-
2015
- 2015-10-29 US US14/926,225 patent/US9663509B2/en active Active
-
2017
- 2017-04-25 US US15/496,269 patent/US10081626B2/en active Active
-
2018
- 2018-08-16 US US15/998,823 patent/US10377751B2/en active Active
-
2019
- 2019-06-24 US US16/449,857 patent/US10745394B2/en active Active
-
2020
- 2020-07-07 US US16/922,414 patent/US11548887B2/en active Active
-
2022
- 2022-12-09 US US18/078,891 patent/US20230183232A1/en not_active Abandoned
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