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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic 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
    • C07D451/02Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Addiction (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
WO2009029257A1 (en) * 2007-08-27 2009-03-05 Theravance, Inc. Disubstituted alkyl-8-azabicyclo [3.2.1.] octane compounds as mu opioid receptor antagonists
US7902221B2 (en) * 2007-08-27 2011-03-08 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
WO2009029253A1 (en) * 2007-08-27 2009-03-05 Theravance, Inc. Heteroarylalkyl-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
BR112013019667B1 (pt) 2011-02-01 2019-07-02 Bayer Intellectual Property Gmbh Compostos derivados de heteroaril-piperidina e -piperazina, seus usos, composição, processos de produção de compostos e de composições, método para o controle de fungos fitopatogênicos prejudiciais
ES2661849T3 (es) 2011-09-15 2018-04-04 Bayer Intellectual Property Gmbh Piperidinpirazoles como fungicidas
ES2647442T3 (es) 2011-12-27 2017-12-21 Bayer Intellectual Property Gmbh Compuestos intermedios para la preparación de derivados de heteroarilpiperidina y de heteroarilpiperazina como fungicidas
EP3082816B1 (en) 2013-12-20 2019-03-20 Indivior UK Limited Intranasal naloxone compositions and methods of making and using same
WO2016161069A1 (en) 2015-04-02 2016-10-06 Theravance Biopharma R&D Ip, Llc Combination dosage form of a mu opioid receptor antagonist and an opioid agent
JP2021512952A (ja) 2018-02-05 2021-05-20 アルカームス・インコーポレイテッド 疼痛の処置のための化合物
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
IL151550A0 (en) 2000-03-03 2003-04-10 Ortho Mcneil Pharm Inc 3-(diarylmethylene)-8-azabicyclo [3.2.1] octane derivatives
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
PT1443046E (pt) 2001-10-09 2009-02-26 Nisshin Pharma Inc Novas 4-(2-furoil)aminopiperidinas, produtos intermédios para a sua síntese, processos para a sua produção e utilização das mesmas em medicina
PL368919A1 (en) 2001-10-22 2005-04-04 Pfizer Products 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
US7056930B2 (en) * 2003-04-14 2006-06-06 Pfizer Inc. 2-Azabicyclo[3.3.1]nonane derivatives
MXPA05011070A (es) 2003-04-14 2005-12-12 Pfizer Prod Inc Derivados de 3-azabiciclo [3.2.1] octano.
MXPA05011163A (es) 2003-04-15 2005-12-14 Pfizer Prod Inc Derivados de 3-benzhidriliden-8-azabiciclo[3.2.1]octano con actividad de receptores opioides.
US6992090B2 (en) 2003-06-16 2006-01-31 Adolor Corporation Substituted piperidine compounds and methods of their use
US7435822B2 (en) 2004-02-03 2008-10-14 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
JP2010509227A (ja) 2006-11-07 2010-03-25 ネクター セラピューティックス エイエル,コーポレイション オピオイド作動薬およびオピオイド拮抗薬の用量形態および同時投与
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
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
WO2009029253A1 (en) 2007-08-27 2009-03-05 Theravance, Inc. Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
US7902221B2 (en) * 2007-08-27 2011-03-08 Theravance, Inc. Amidoalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

Also Published As

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

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