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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (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
DE602008005771D1 (de) * 2007-08-27 2011-05-05 Theravance Inc Disubstituierte alkyl-8-azabicycloä3.2.1üoktan-verbindungen als mu-opioid-rezeptorantagonisten
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
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
JP5797655B2 (ja) * 2009-09-18 2015-10-21 アドラー・コーポレーション 消化管障害のためのオピオイド受容体アンタゴニストの使用
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
EP2632922B1 (de) 2010-10-27 2019-02-27 Bayer CropScience Aktiengesellschaft Heteroarylpiperidin und -piperazinderivate als fungizide
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
CN104987330B (zh) 2011-02-01 2019-04-05 拜耳知识产权有限责任公司 作为杀真菌剂的杂芳基哌啶和杂芳基哌嗪衍生物
IN2014CN01862A (zh) 2011-09-15 2015-05-29 Bayer Ip Gmbh
MX388852B (es) 2011-12-27 2025-03-20 Bayer Cropscience Ag Derivados de heteroarilpiperidina y de heteroarilpiperazina como fungicidas.
WO2015095644A1 (en) 2013-12-20 2015-06-25 AntiOP, Inc. Intranasal naloxone compositions and methods of making and using same
US20160287573A1 (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
MA51738A (fr) 2018-02-05 2021-05-12 Alkermes Inc Composés pour le traitement de la douleur
CA3196642A1 (en) * 2020-11-06 2022-05-12 Christian GRUGEL 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
IL151550A0 (en) 2000-03-03 2003-04-10 Ortho Mcneil Pharm Inc 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
DE60230437D1 (de) 2001-10-09 2009-01-29 Nisshin Pharma Inc Neue 4-(2-furoyl)-amino-piperidine, zwischenprodukte für deren synthese, verfahren zu deren herstellung und deren medizinische verwendung
OA12711A (en) 2001-10-22 2006-06-27 Pfizer Prod Inc 3-AzabicycloÄ3.1.0Ühexane derivatives as opoioid receptor antagonists.
US7381721B2 (en) 2003-03-17 2008-06-03 Adolor Corporation Substituted piperidine compounds
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
US20040204453A1 (en) 2003-04-14 2004-10-14 Pfizer Inc 4-Phenyl-piperidine compounds and their use as modulators of opioid receptors
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
EA201100544A1 (ru) 2006-11-07 2012-01-30 Нектар Терапьютикс Применение комбинации опиоидного агониста и конъюгата полимер-опиоидный антагонист для изготовления лекарственного средства для лечения и предупреждения боли
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
DE602008005771D1 (de) * 2007-08-27 2011-05-05 Theravance Inc Disubstituierte alkyl-8-azabicycloä3.2.1üoktan-verbindungen als mu-opioid-rezeptorantagonisten
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
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

Also Published As

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

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