AU2008219615B2 - Crystalline forms of an 8-azabicyclo[3.2.1]octane compound - Google Patents

Crystalline forms of an 8-azabicyclo[3.2.1]octane compound Download PDF

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Publication number
AU2008219615B2
AU2008219615B2 AU2008219615A AU2008219615A AU2008219615B2 AU 2008219615 B2 AU2008219615 B2 AU 2008219615B2 AU 2008219615 A AU2008219615 A AU 2008219615A AU 2008219615 A AU2008219615 A AU 2008219615A AU 2008219615 B2 AU2008219615 B2 AU 2008219615B2
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AU
Australia
Prior art keywords
crystalline
salt form
crystalline salt
cyclohexylmethyl
endo
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Ceased
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AU2008219615A
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English (en)
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AU2008219615A1 (en
Inventor
Pierre-Jean Colson
Sean Dalziel
Leticia M. Preza
Miroslav Rapta
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Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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Assigned to THERAVANCE BIOPHARMA R&D IP, LLC reassignment THERAVANCE BIOPHARMA R&D IP, LLC Request for Assignment Assignors: THERAVANCE, INC.
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Classifications

    • 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)
AU2008219615A 2007-02-28 2008-02-27 Crystalline forms of an 8-azabicyclo[3.2.1]octane compound Ceased AU2008219615B2 (en)

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
AU2008219615A1 AU2008219615A1 (en) 2008-09-04
AU2008219615B2 true AU2008219615B2 (en) 2013-05-09

Family

ID=39620376

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2008219615A Ceased AU2008219615B2 (en) 2007-02-28 2008-02-27 Crystalline forms of an 8-azabicyclo[3.2.1]octane compound

Country Status (26)

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)

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* 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 (3)

* Cited by examiner, † Cited by third party
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
WO2004089908A2 (en) * 2003-04-14 2004-10-21 Pfizer Products Inc. 3-azabicyclo[3.2.1]octane derivatives
WO2007103187A2 (en) * 2006-03-01 2007-09-13 Theravance, Inc. 8-azabicyclo[3.2.1]octane compounds as mu 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
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
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 (3)

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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
WO2004089908A2 (en) * 2003-04-14 2004-10-21 Pfizer Products Inc. 3-azabicyclo[3.2.1]octane derivatives
WO2007103187A2 (en) * 2006-03-01 2007-09-13 Theravance, Inc. 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

Also Published As

Publication number Publication date
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
CN101616916B (zh) 2011-10-12
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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Owner name: THERAVANCE BIOPHARMA R&D IP, LLC

Free format text: FORMER OWNER WAS: THERAVANCE, INC.

MK14 Patent ceased section 143(a) (annual fees not paid) or expired