CA2646409C - 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 Download PDF

Info

Publication number
CA2646409C
CA2646409C CA2646409A CA2646409A CA2646409C CA 2646409 C CA2646409 C CA 2646409C CA 2646409 A CA2646409 A CA 2646409A CA 2646409 A CA2646409 A CA 2646409A CA 2646409 C CA2646409 C CA 2646409C
Authority
CA
Canada
Prior art keywords
endo
oct
benzamide
ethyl
azabicyclo
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.)
Active
Application number
CA2646409A
Other languages
English (en)
French (fr)
Other versions
CA2646409A1 (en
Inventor
Daniel Long
Timothy J. Church
John R. Jacobsen
Lan Jiang
Daisuke Roland Saito
Ioanna Stergiades
Priscilla Van Dyke
Sean Dalziel
Leticia Preza
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Theravance Biopharma R&D IP LLC
Original Assignee
Theravance Biopharma R&D IP LLC
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=CA2646409(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Theravance Biopharma R&D IP LLC filed Critical Theravance Biopharma R&D IP LLC
Publication of CA2646409A1 publication Critical patent/CA2646409A1/en
Application granted granted Critical
Publication of CA2646409C publication Critical patent/CA2646409C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2646409A 2006-03-01 2007-02-28 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists Active CA2646409C (en)

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

Publications (2)

Publication Number Publication Date
CA2646409A1 CA2646409A1 (en) 2007-09-13
CA2646409C true CA2646409C (en) 2015-11-10

Family

ID=38436795

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2646409A Active CA2646409C (en) 2006-03-01 2007-02-28 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

Country Status (24)

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

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
ATE502939T1 (de) * 2007-08-27 2011-04-15 Theravance Inc Disubstituierte alkyl-8-azabicycloä3.2.1üoktan- verbindungen als mu-opioid-rezeptorantagonisten
EP2195313B1 (en) * 2007-08-27 2014-04-02 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
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
CA2774021A1 (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
PE20141002A1 (es) 2010-10-27 2014-08-17 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
ES2661849T3 (es) 2011-09-15 2018-04-04 Bayer Intellectual Property Gmbh Piperidinpirazoles como fungicidas
DK2921493T3 (da) 2011-12-27 2017-11-27 Bayer Ip Gmbh Heteroarylpiperidin og ¿piperazinderivater
CA2875384A1 (en) 2013-12-20 2015-06-20 AntiOP, Inc. Intranasal naloxone compositions and methods of making and using same
HK1247105A1 (zh) 2015-04-02 2018-09-21 Theravance Biopharma R&D Ip, Llc Mu类鸦片受体拮抗剂与类鸦片药剂的组合剂型
SG11202007422QA (en) 2018-02-05 2020-09-29 Alkermes Inc Compounds for the treatment of pain
KR20230154789A (ko) * 2020-11-06 2023-11-09 액티노젠 메디컬 리미티드 헤테로고리 메탄온 화합물 및 그의 아자-비시클로 중간체의 제조 공정

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
EP1443046B1 (en) 2001-10-09 2008-12-17 Kyorin Pharmaceutical Co., Ltd. Novel 4-(2furoyl)aminopiperidines, intermediates in synthesizing the same, process for producing the same and medicinal use of the same
EA006708B1 (ru) 2001-10-22 2006-02-24 Пфайзер Продактс Инк. Производные 3-азабицикло (3.1.0) гексана в качестве антагонистов опиоидного рецептора
US7381721B2 (en) 2003-03-17 2008-06-03 Adolor Corporation Substituted piperidine compounds
US7056930B2 (en) * 2003-04-14 2006-06-06 Pfizer Inc. 2-Azabicyclo[3.3.1]nonane derivatives
EP1615894A2 (en) * 2003-04-14 2006-01-18 Pfizer Products Inc. 3-azabicyclo 3.2.1 octane derivatives
US20040204453A1 (en) 2003-04-14 2004-10-14 Pfizer Inc 4-Phenyl-piperidine compounds and their use as modulators of opioid receptors
JP2006523673A (ja) 2003-04-15 2006-10-19 ファイザー・プロダクツ・インク オピオイド受容体活性を有する３−ベンズヒドリリデン−８−アザ−ビシクロ［３．２．１］オクタン誘導体
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
AU2007317788B2 (en) 2006-11-07 2013-05-02 Nektar Therapeutics Dosage forms and co-administration of an opioid agonist and an opioid antagonist
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
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
ATE502939T1 (de) * 2007-08-27 2011-04-15 Theravance Inc Disubstituierte alkyl-8-azabicycloä3.2.1üoktan- verbindungen als mu-opioid-rezeptorantagonisten

Also Published As

Publication number Publication date
AR059690A1 (es) 2008-04-23
WO2007103187A3 (en) 2007-11-01
US8927573B2 (en) 2015-01-06
EP2001876B1 (en) 2011-05-18
US20070219278A1 (en) 2007-09-20
DK2001876T3 (da) 2011-08-29
NZ570764A (en) 2011-08-26
US20190308966A1 (en) 2019-10-10
JP5086280B2 (ja) 2012-11-28
PL2001876T3 (pl) 2011-10-31
BRPI0708490B1 (pt) 2019-07-30
RU2008138875A (ru) 2010-04-10
US8263618B2 (en) 2012-09-11
JP2009528371A (ja) 2009-08-06
US20100035921A1 (en) 2010-02-11
AU2007224213B2 (en) 2012-06-14
US10745394B2 (en) 2020-08-18
US20230183232A1 (en) 2023-06-15
US20150291579A1 (en) 2015-10-15
HRP20110590T1 (hr) 2011-09-30
EP2001876A2 (en) 2008-12-17
IL193690A (en) 2013-02-28
IL193690A0 (en) 2009-08-03
US20160176863A1 (en) 2016-06-23
US7622508B2 (en) 2009-11-24
CA2646409A1 (en) 2007-09-13
ATE509928T1 (de) 2011-06-15
US10081626B2 (en) 2018-09-25
BRPI0708490A2 (pt) 2011-05-31
US10377751B2 (en) 2019-08-13
KR20080100282A (ko) 2008-11-14
PT2001876E (pt) 2011-08-18
HK1125935A1 (en) 2009-08-21
TWI379832B (en) 2012-12-21
TW200800981A (en) 2008-01-01
MY145633A (en) 2012-03-15
US9206172B2 (en) 2015-12-08
US11548887B2 (en) 2023-01-10
US8664242B2 (en) 2014-03-04
US20190119267A1 (en) 2019-04-25
JP2012211193A (ja) 2012-11-01
MA30284B1 (fr) 2009-03-02
WO2007103187A2 (en) 2007-09-13
SI2001876T1 (sl) 2011-09-30
BRPI0708490B8 (pt) 2021-05-25
US20130158060A1 (en) 2013-06-20
RU2423362C2 (ru) 2011-07-10
US20210024515A1 (en) 2021-01-28
US20140288112A1 (en) 2014-09-25
US20170349578A1 (en) 2017-12-07
AU2007224213A1 (en) 2007-09-13
US9663509B2 (en) 2017-05-30
KR101376479B1 (ko) 2014-03-27
PE20071311A1 (es) 2007-12-29
CY1111747T1 (el) 2015-10-07
MX2008011165A (es) 2008-09-15

Similar Documents

Publication Publication Date Title
US20230183232A1 (en) 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
US7947710B2 (en) Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
US7902221B2 (en) Amidoalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
ES2366058T3 (es) Compuestos de 8-azabiciclo[3.2.1]octano como antagonistas de los receptores opioides mu.
HK1125935B (en) 8-azabicyclo [3.2.1] octane compounds as mu opioid receptor antagonists

Legal Events

Date Code Title Description
EEER Examination request
MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 18TH ANNIV.) - STANDARD

Year of fee payment: 18

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250221

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20250224