CN101616916B - 8-氮杂双环[3.2.1]辛烷化合物的晶型 - Google Patents

8-氮杂双环[3.2.1]辛烷化合物的晶型 Download PDF

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Publication number
CN101616916B
CN101616916B CN2008800059690A CN200880005969A CN101616916B CN 101616916 B CN101616916 B CN 101616916B CN 2008800059690 A CN2008800059690 A CN 2008800059690A CN 200880005969 A CN200880005969 A CN 200880005969A CN 101616916 B CN101616916 B CN 101616916B
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salt
ethyl
oct
reaction mixture
aza
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CN101616916A (zh
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肖恩·达尔齐尔
莱蒂西亚·M·普雷萨
米罗斯拉夫·拉普塔
皮埃尔-让·科尔松
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Theravance Biopharma R&D IP LLC
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Shiwan Pharmaceutical
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    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN2008800059690A 2007-02-28 2008-02-27 8-氮杂双环[3.2.1]辛烷化合物的晶型 Active CN101616916B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US90409007P 2007-02-28 2007-02-28
US60/904,090 2007-02-28
PCT/US2008/002583 WO2008106159A1 (en) 2007-02-28 2008-02-27 Crystalline forms of an 8-azabicyclo[3.2.1]octane compound

Publications (2)

Publication Number Publication Date
CN101616916A CN101616916A (zh) 2009-12-30
CN101616916B true CN101616916B (zh) 2011-10-12

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CN2008800059690A Active CN101616916B (zh) 2007-02-28 2008-02-27 8-氮杂双环[3.2.1]辛烷化合物的晶型

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Country Link
US (7) US7943772B2 (enExample)
EP (1) EP2132204B1 (enExample)
JP (2) JP5512289B2 (enExample)
KR (1) KR101480530B1 (enExample)
CN (1) CN101616916B (enExample)
AR (2) AR065554A1 (enExample)
AU (1) AU2008219615B2 (enExample)
BR (1) BRPI0807974B8 (enExample)
CA (1) CA2678073C (enExample)
CL (1) CL2008000573A1 (enExample)
CO (1) CO6220856A2 (enExample)
CY (1) CY1115077T1 (enExample)
DK (1) DK2132204T3 (enExample)
ES (1) ES2402031T3 (enExample)
HR (1) HRP20130193T1 (enExample)
IL (1) IL200131A (enExample)
MX (1) MX2009009141A (enExample)
MY (1) MY148318A (enExample)
NZ (1) NZ578871A (enExample)
PL (1) PL2132204T3 (enExample)
PT (1) PT2132204E (enExample)
RU (1) RU2458061C2 (enExample)
SI (1) SI2132204T1 (enExample)
TW (1) TWI409067B (enExample)
WO (1) WO2008106159A1 (enExample)
ZA (1) ZA200905832B (enExample)

Families Citing this family (9)

* 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
WO2009029253A1 (en) * 2007-08-27 2009-03-05 Theravance, Inc. Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
DE602008005771D1 (de) * 2007-08-27 2011-05-05 Theravance Inc Disubstituierte alkyl-8-azabicycloä3.2.1üoktan-verbindungen als mu-opioid-rezeptorantagonisten
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
EP2185553B1 (en) * 2007-08-27 2012-06-27 Theravance, Inc. Amidoalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
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
HRP20200432T1 (hr) 2015-04-02 2020-06-12 Theravance Biopharma R&D Ip, Llc Oblik za kombinacijsko doziranje antagonista mu opioidnog receptora i opioidnog sredstva

Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2004089909A1 (en) * 2003-04-14 2004-10-21 Pfizer Products Inc. 2-azabicyclo[3.3.1]nonane derivatives as opioid receptor antagonists

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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
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
US6467084B1 (en) * 1999-12-16 2002-10-15 Emware, Inc. Systems and methods for reprogramming an embedded device with program code using relocatable program code
US6552036B2 (en) 2000-03-03 2003-04-22 Ortho-Mcneil Pharmaceutical, 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
AP1816A (en) 2001-10-22 2008-01-04 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
MXPA05011070A (es) 2003-04-14 2005-12-12 Pfizer Prod Inc Derivados de 3-azabiciclo [3.2.1] octano.
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
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
MY145633A (en) 2006-03-01 2012-03-15 Theravance Inc 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
CN101534827A (zh) 2006-11-07 2009-09-16 尼克塔治疗亚拉巴马公司 阿片样物质激动剂和阿片样物质拮抗剂的剂型和联合给药
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

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2004089909A1 (en) * 2003-04-14 2004-10-21 Pfizer Products Inc. 2-azabicyclo[3.3.1]nonane derivatives as opioid receptor antagonists

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Publication number Publication date
AU2008219615B2 (en) 2013-05-09
JP2013151564A (ja) 2013-08-08
US20160287572A1 (en) 2016-10-06
US8247555B2 (en) 2012-08-21
US20130072515A1 (en) 2013-03-21
PL2132204T3 (pl) 2013-06-28
US20150073014A1 (en) 2015-03-12
US9949963B2 (en) 2018-04-24
MX2009009141A (es) 2009-09-03
US20110184008A1 (en) 2011-07-28
SI2132204T1 (sl) 2013-05-31
US20140080856A1 (en) 2014-03-20
PT2132204E (pt) 2013-03-25
KR20090115767A (ko) 2009-11-05
CA2678073A1 (en) 2008-09-04
IL200131A0 (en) 2010-04-15
BRPI0807974A2 (pt) 2014-09-16
US8536335B2 (en) 2013-09-17
HRP20130193T1 (hr) 2013-03-31
NZ578871A (en) 2012-01-12
WO2008106159A1 (en) 2008-09-04
US8816091B2 (en) 2014-08-26
CL2008000573A1 (es) 2008-05-16
KR101480530B1 (ko) 2015-01-08
MY148318A (en) 2013-03-29
JP5512289B2 (ja) 2014-06-04
TW200845984A (en) 2008-12-01
AR109224A2 (es) 2018-11-07
US9290491B2 (en) 2016-03-22
EP2132204B1 (en) 2013-01-23
IL200131A (en) 2013-03-24
US20180200246A1 (en) 2018-07-19
RU2458061C2 (ru) 2012-08-10
US7943772B2 (en) 2011-05-17
BRPI0807974B1 (pt) 2020-11-24
DK2132204T3 (da) 2013-04-29
ZA200905832B (en) 2010-05-26
TWI409067B (zh) 2013-09-21
RU2009135834A (ru) 2011-04-10
ES2402031T3 (es) 2013-04-26
HK1139399A1 (en) 2010-09-17
CY1115077T1 (el) 2016-12-14
CO6220856A2 (es) 2010-11-19
JP2010520198A (ja) 2010-06-10
US10426766B2 (en) 2019-10-01
EP2132204A1 (en) 2009-12-16
US20080207676A1 (en) 2008-08-28
BRPI0807974B8 (pt) 2021-05-25
AR065554A1 (es) 2009-06-17
AU2008219615A1 (en) 2008-09-04
CA2678073C (en) 2016-01-05
CN101616916A (zh) 2009-12-30

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