TW200800981A - 8-azabicyclo[3.2.1]octane compounds as MU opioid receptor antagonists - Google Patents

8-azabicyclo[3.2.1]octane compounds as MU opioid receptor antagonists

Info

Publication number
TW200800981A
TW200800981A TW096106339A TW96106339A TW200800981A TW 200800981 A TW200800981 A TW 200800981A TW 096106339 A TW096106339 A TW 096106339A TW 96106339 A TW96106339 A TW 96106339A TW 200800981 A TW200800981 A TW 200800981A
Authority
TW
Taiwan
Prior art keywords
opioid receptor
compounds
azabicyclo
receptor antagonists
octane compounds
Prior art date
Application number
TW096106339A
Other languages
English (en)
Other versions
TWI379832B (en
Inventor
Daniel D Long
Lan Jiang
Timothy J Church
John R Jacobsen
Daisuke Roland Saito
Ioanna Stergiades
Dyke Priscilla M Van
Original Assignee
Theravance Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38436795&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TW200800981(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Theravance Inc filed Critical Theravance Inc
Publication of TW200800981A publication Critical patent/TW200800981A/zh
Application granted granted Critical
Publication of TWI379832B publication Critical patent/TWI379832B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P1/10—Laxatives
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW096106339A 2006-03-01 2007-02-26 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists TWI379832B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US77796206P 2006-03-01 2006-03-01
US84102806P 2006-08-30 2006-08-30

Publications (2)

Publication Number Publication Date
TW200800981A true TW200800981A (en) 2008-01-01
TWI379832B TWI379832B (en) 2012-12-21

Family

ID=38436795

Family Applications (1)

Application Number Title Priority Date Filing Date
TW096106339A TWI379832B (en) 2006-03-01 2007-02-26 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

Country Status (24)

Country Link
US (11) US7622508B2 (zh)
EP (1) EP2001876B1 (zh)
JP (2) JP5086280B2 (zh)
KR (1) KR101376479B1 (zh)
AR (1) AR059690A1 (zh)
AT (1) ATE509928T1 (zh)
AU (1) AU2007224213B2 (zh)
BR (1) BRPI0708490B8 (zh)
CA (1) CA2646409C (zh)
CY (1) CY1111747T1 (zh)
DK (1) DK2001876T3 (zh)
HR (1) HRP20110590T1 (zh)
IL (1) IL193690A (zh)
MA (1) MA30284B1 (zh)
MX (1) MX2008011165A (zh)
MY (1) MY145633A (zh)
NZ (1) NZ570764A (zh)
PE (1) PE20071311A1 (zh)
PL (1) PL2001876T3 (zh)
PT (1) PT2001876E (zh)
RU (1) RU2423362C2 (zh)
SI (1) SI2001876T1 (zh)
TW (1) TWI379832B (zh)
WO (1) WO2007103187A2 (zh)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
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
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
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
WO2009029257A1 (en) * 2007-08-27 2009-03-05 Theravance, Inc. Disubstituted alkyl-8-azabicyclo [3.2.1.] octane compounds as mu opioid receptor antagonists
BR112012006069A8 (pt) * 2009-09-18 2017-10-10 Adolor Corp Método para tratar ou prevenir constipação induzida e disfunção intestinal induzida por opióide em um humano, e, uso de uma quantidade terapeuticamente efetiva de composto
US20120122928A1 (en) 2010-08-11 2012-05-17 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
US8759527B2 (en) 2010-08-25 2014-06-24 Bayer Cropscience Ag Heteroarylpiperidine and -piperazine derivatives as fungicides
BR112013010497B1 (pt) 2010-10-27 2018-07-17 Bayer Intellectual Property Gmbh derivados de heteroaril - piperidina e - piperazina enquanto fungicidas, composição os compreendendo, bem como processo para a produção de composições para controle de fungos fitopatogênicos nocivos e método para controle de fungos fitopatogênicos nocivos
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
MX352307B (es) 2011-02-01 2017-11-17 Bayer Ip Gmbh Derivados de heteroarilpiperidina y -piperazina como fungicidas.
IN2014CN01862A (zh) 2011-09-15 2015-05-29 Bayer Ip Gmbh
DK2921493T3 (da) 2011-12-27 2017-11-27 Bayer Ip Gmbh Heteroarylpiperidin og ¿piperazinderivater
US9192570B2 (en) 2013-12-20 2015-11-24 AntiOP, Inc. Intranasal naloxone compositions and methods of making and using same
RU2017134794A (ru) 2015-04-02 2019-04-04 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Комбинированная лекарственная форма антагониста мю-опиоидного рецептора и опиоидного средства
EP3749667A1 (en) 2018-02-05 2020-12-16 Alkermes, Inc. Compounds for the treatment of pain
US20230416243A1 (en) * 2020-11-06 2023-12-28 Actinogen Medical Limited Process for Preparing Heterocyclic Methanone Compounds and AZA-Bicyclo Intermediates Thereof

Family Cites Families (30)

* Cited by examiner, † Cited by third party
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
US20030181447A1 (en) 2001-02-22 2003-09-25 Boyd Robert E. 3-(Diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives
KR20030009376A (ko) 2000-03-03 2003-01-29 오르토-맥네일 파마슈티칼, 인코퍼레이티드 3-(디아릴메틸렌)-8-아자비사이클로[3.2.1]옥탄 유도체
US20020025948A1 (en) 2000-06-23 2002-02-28 Banks Bernard Joseph 3-azabicyclo[3.1.0]hexane derivatives useful in therapy
ES2319879T3 (es) 2001-10-09 2009-05-14 Kyorin Pharmaceutical Co., Ltd. 4-(2-furoil)aminopiperidinas novedosas, productos intermedios en la sintesis de las mismas, procedimiento para producir las mismas y uso medico de las mismas.
IL161157A0 (en) 2001-10-22 2004-08-31 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
CA2522323C (en) 2003-04-14 2009-09-15 Pfizer Products Inc. 3-azabicyclo[3.2.1]octane derivatives as opioid receptor ligands
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
EP1615920A1 (en) 2003-04-15 2006-01-18 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
WO2005075472A1 (en) 2004-02-03 2005-08-18 Janssen Pharmaceutica, N.V. 3-(diheteroarylnethylene)-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
WO2009029257A1 (en) 2007-08-27 2009-03-05 Theravance, Inc. Disubstituted alkyl-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
US7691878B2 (en) * 2007-08-27 2010-04-06 Theravance, Inc. Heteroarylalkyl-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

Also Published As

Publication number Publication date
US20130158060A1 (en) 2013-06-20
CY1111747T1 (el) 2015-10-07
US9663509B2 (en) 2017-05-30
US8664242B2 (en) 2014-03-04
AR059690A1 (es) 2008-04-23
AU2007224213A1 (en) 2007-09-13
US8263618B2 (en) 2012-09-11
US20210024515A1 (en) 2021-01-28
PE20071311A1 (es) 2007-12-29
ATE509928T1 (de) 2011-06-15
US10081626B2 (en) 2018-09-25
JP5086280B2 (ja) 2012-11-28
SI2001876T1 (sl) 2011-09-30
BRPI0708490B1 (pt) 2019-07-30
NZ570764A (en) 2011-08-26
US10745394B2 (en) 2020-08-18
EP2001876A2 (en) 2008-12-17
JP2012211193A (ja) 2012-11-01
BRPI0708490B8 (pt) 2021-05-25
US20190119267A1 (en) 2019-04-25
AU2007224213B2 (en) 2012-06-14
PL2001876T3 (pl) 2011-10-31
HK1125935A1 (zh) 2009-08-21
CA2646409A1 (en) 2007-09-13
TWI379832B (en) 2012-12-21
MY145633A (en) 2012-03-15
MX2008011165A (es) 2008-09-15
US20170349578A1 (en) 2017-12-07
US9206172B2 (en) 2015-12-08
JP2009528371A (ja) 2009-08-06
RU2423362C2 (ru) 2011-07-10
MA30284B1 (fr) 2009-03-02
RU2008138875A (ru) 2010-04-10
BRPI0708490A2 (pt) 2011-05-31
US10377751B2 (en) 2019-08-13
KR101376479B1 (ko) 2014-03-27
US8927573B2 (en) 2015-01-06
DK2001876T3 (da) 2011-08-29
HRP20110590T1 (hr) 2011-09-30
IL193690A0 (en) 2009-08-03
US20100035921A1 (en) 2010-02-11
US20190308966A1 (en) 2019-10-10
IL193690A (en) 2013-02-28
US20160176863A1 (en) 2016-06-23
KR20080100282A (ko) 2008-11-14
PT2001876E (pt) 2011-08-18
US20070219278A1 (en) 2007-09-20
EP2001876B1 (en) 2011-05-18
US20230183232A1 (en) 2023-06-15
US20150291579A1 (en) 2015-10-15
US11548887B2 (en) 2023-01-10
US20140288112A1 (en) 2014-09-25
US7622508B2 (en) 2009-11-24
WO2007103187A2 (en) 2007-09-13
CA2646409C (en) 2015-11-10
WO2007103187A3 (en) 2007-11-01

Similar Documents

Publication Publication Date Title
TW200800981A (en) 8-azabicyclo[3.2.1]octane compounds as MU opioid receptor antagonists
ATE502939T1 (de) Disubstituierte alkyl-8-azabicycloä3.2.1üoktan- verbindungen als mu-opioid-rezeptorantagonisten
MX2010002171A (es) Compuestos 8-azabiciclo[3.2.1] octil-2 hidroxibenzamida como antagonistas de los receptores opioides mu.
IL184932A0 (en) Glucagon receptor antagonists, preperation and therapeutic uses
MX2009005461A (es) N-oxidos de analogos de 4,5-epoxi-morfinano.
NZ590650A (en) Buprenorphine analogs
UA92670C2 (ru) Пиразолиновые соединения и их фармацевтическое применение, композиция на их основе
MY143581A (en) Carboxamide derivatives as muscarinic receptor antagonists
MX2011011156A (es) COMPUESTOS DIAMIDA QUE TIENE ACTIVIDAD COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS Y COMO AGONISTAS DE LOS RECEPTORES ANDRENERGICOS ß2.
PH12012501800A1 (en) 2,3 dihydro- 1h - inden- 1 - yl -2,7 -diazaspirol [ 3.5 ] nonane derivatives and their use as antagonists or inverse agonists of the ghrelin receptor
MX2009006018A (es) Derivados de quinuclidinol como antagonistas de receptores muscarinicos.
SG171681A1 (en) Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-ht2a serotonin receptor
SI1957484T1 (sl) Antagonisti glukagonskega receptorja, priprava in terapevtske uporabe
ATE446089T1 (de) 2-benzoyl-imidazopyridin-derivate, herstellungsverfahren und ihre verwendung für therapeutika
MY148318A (en) Crystalline forms of an 8-azabicyclo [3.2.1] octane compound
MY149973A (en) 3-carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists
MX2010004498A (es) Derivados de ciclohexenoamida y su uso como antagonistas de trpv1.
DE602007012313D1 (de) Als a2b-adenosinrezeptorantagonisten geeignete 5-phenyl-6-pyridin-4-yl-1,3-dihydro-2h-imidazoä4,5-büpyridin-2-onderivate
TW200714587A (en) Biphenyl compounds useful as muscarinic receptor antagonists
WO2009076399A3 (en) Aminotetralin compounds as mu opioid receptor antagonists
DE602006018713D1 (de) Als agonisten für den nikotinischen acetylcholinrezeptor geeignete azabicycloalkanderivate
MY147756A (en) Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists
GB0513886D0 (en) Novel compounds
MY179041A (en) Crystalline forms of a 3-carboxypropyl-aminotetralin compound
SI1861360T1 (sl) Derivati pirolidina kot antagonisti histaminskega h3 receptorja