WO2003035622A1 - 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists - Google Patents

3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists Download PDF

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Publication number
WO2003035622A1
WO2003035622A1 PCT/IB2002/003668 IB0203668W WO03035622A1 WO 2003035622 A1 WO2003035622 A1 WO 2003035622A1 IB 0203668 W IB0203668 W IB 0203668W WO 03035622 A1 WO03035622 A1 WO 03035622A1
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WO
WIPO (PCT)
Prior art keywords
alkyl
exo
aza
ethyl
phenyl
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.)
Ceased
Application number
PCT/IB2002/003668
Other languages
English (en)
French (fr)
Inventor
Stanton Furst Mchardy
Spiros Liras
Steven Donald Heck
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.)
Pfizer Products Inc
Original Assignee
Pfizer Products 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
Priority to KR1020047006011A priority Critical patent/KR100621292B1/ko
Priority to NZ531807A priority patent/NZ531807A/xx
Priority to IL16115702A priority patent/IL161157A0/xx
Priority to APAP/P/2004/003007A priority patent/AP1816A/en
Priority to SI200230688T priority patent/SI1440059T1/sl
Priority to HK05104840.9A priority patent/HK1072052B/xx
Priority to JP2003538138A priority patent/JP4155522B2/ja
Priority to EP02765197A priority patent/EP1440059B1/en
Priority to BR0213464-0A priority patent/BR0213464A/pt
Priority to YUP-251/04A priority patent/RS25104A/sr
Priority to HU0401884A priority patent/HUP0401884A2/hu
Priority to UA20040402979A priority patent/UA75714C2/uk
Priority to CA002463264A priority patent/CA2463264C/en
Priority to EA200400467A priority patent/EA006708B1/ru
Priority to DE60226161T priority patent/DE60226161T2/de
Priority to DK02765197T priority patent/DK1440059T3/da
Priority to MXPA04003730A priority patent/MXPA04003730A/es
Priority to HRP20040288 priority patent/HRP20040288A2/hr
Priority to AU2002329557A priority patent/AU2002329557B2/en
Application filed by Pfizer Products Inc filed Critical Pfizer Products Inc
Publication of WO2003035622A1 publication Critical patent/WO2003035622A1/en
Priority to IS7187A priority patent/IS7187A/is
Priority to IL161157A priority patent/IL161157A/en
Priority to NO20041626A priority patent/NO329092B1/no
Priority to TNP2004000071A priority patent/TNSN04071A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/36—Opioid-abuse
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/04—Compounds containing oxirane rings containing only hydrogen and carbon atoms in addition to the ring oxygen atoms

Definitions

  • X is H, halogen, -OH, -CN, -C C alkyl substituted with from one to three halogen atoms, or -0(CrC 4 alkyl), wherein the alkyl of -0(C C 4 alkyl) is optionally substituted with from one to three halogen atoms;
  • Preferred compounds of formula I of the invention are:
  • isotopically labeled compounds of formula I of this invention can generally be prepared by carrying out the procedures disclosed in the Schemes and/or in the Examples below, by substituting a readily
  • the subject invention also provides a pharmaceutical composition for treating in a mammal, including a human, in need thereof a disorder or condition selected from irritable bowel syndrome; constipation; nausea; vomiting; pruritic dermatoses, including allergic dermatitis and contact dermatitis; psoriasis; eczema; an insect bite; an eating disorder, including anorexia, bulimia, and obesity; depression, smoking addiction; drug addiction, including alcohol addiction, amphetamine addiction, cocaine addiction and addiction to an opiate, for example morphine, opium, or heroine; an opiate overdose; a sexual dysfunction, including erectile dysfunction and impotence; stroke; head trauma; traumatic brain injury; spinal damage; Parkinson's disease; Alzheimer's disease, age-related cognitive decline; and Attention Deficit and Hyperactivity Disorder; which composition comprises an amount of a compound of formula I effective in treating said disorder or condition and a pharmaceutically acceptable carrier.
  • a disorder or condition selected from irritable bowel syndrome; cons
  • an aniline of formula (XI) with an appropriately substituted sulfonyl chloride, such as methanesulfonyl chloride, in the presence of a suitable base, such as pyridine or triethyl amine, in a solvent such as ethyl acetate, at temperatures ranging from 0 °C to room temperature, preferably at about room temperature, produces the desired sulfonamide of formula (VIII).
  • a suitable base such as pyridine or triethyl amine
  • the binding is initiated with the addition of a crude membrane preparation of rat forebrain tissue to 96-well polypropylene plates containing the radioligand I ⁇ HJ-DAMGO and test compound, and are incubated for about 90 minutes at about 25 °C.
  • the assay is terminated by rapid filtration with 50mM Tris HCI pH 7.4 onto Wallac Filtermat B and counted on a Betaplate reader (Wallac).
  • the data generated can be analyzed using IC 50 analysis software in Graphpad Prism.

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Nutrition Science (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
PCT/IB2002/003668 2001-10-22 2002-09-09 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists Ceased WO2003035622A1 (en)

Priority Applications (23)

Application Number Priority Date Filing Date Title
CA002463264A CA2463264C (en) 2001-10-22 2002-09-09 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists
IL16115702A IL161157A0 (en) 2001-10-22 2002-09-09 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists
APAP/P/2004/003007A AP1816A (en) 2001-10-22 2002-09-09 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists.
SI200230688T SI1440059T1 (sl) 2001-10-22 2002-09-09 Derivati 3-azabiciklo(3.1.0)heksana kot antagonisti opioidnega receptorja
HK05104840.9A HK1072052B (en) 2001-10-22 2002-09-09 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists
JP2003538138A JP4155522B2 (ja) 2001-10-22 2002-09-09 オピオイド受容体アンタゴニストとしての３−アザビシクロ（３．１．０）ヘキサン誘導体
EP02765197A EP1440059B1 (en) 2001-10-22 2002-09-09 3-azabicyclo(3.1.0)hexane derivatives as opioid receptor antagonists
BR0213464-0A BR0213464A (pt) 2001-10-22 2002-09-09 Derivados de 3-azabiciclo[3.1.0]hexano como antagonistas receptores de opióide
YUP-251/04A RS25104A (sr) 2001-10-22 2002-09-09 Derivati 3-azabiciklo (3.1.0)heksana kao antagonisti opijatnih receptora
HU0401884A HUP0401884A2 (hu) 2001-10-22 2002-09-09 Opioid receptor antagonista hatású 3-azabiciklo[3.1.0]hexán-származékok és ezeket tartalmazó gyógyszerkészítmények
DE60226161T DE60226161T2 (de) 2001-10-22 2002-09-09 3-azabicyclo[3.1.0]hexan derivative als antagonisten der opioid rezeptoren
KR1020047006011A KR100621292B1 (ko) 2001-10-22 2002-09-09 오피오이드 수용체 길항제로서의3-아자비사이클로[3.1.0]헥산 유도체
EA200400467A EA006708B1 (ru) 2001-10-22 2002-09-09 Производные 3-азабицикло (3.1.0) гексана в качестве антагонистов опиоидного рецептора
UA20040402979A UA75714C2 (en) 2001-10-22 2002-09-09 3-azabicyclo [3.1.0] hexane derivatives as opioid receptor antagonists and pharmaceutical composition based thereon
DK02765197T DK1440059T3 (da) 2001-10-22 2002-09-09 3-azabicyclo(3.1.0)hexanderivater som opioidreceptorantagonister
MXPA04003730A MXPA04003730A (es) 2001-10-22 2002-09-09 Derivados del 3-azabiciclo[3.1.0]hexano.
HRP20040288 HRP20040288A2 (en) 2001-10-22 2002-09-09 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists
AU2002329557A AU2002329557B2 (en) 2001-10-22 2002-09-09 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists
NZ531807A NZ531807A (en) 2001-10-22 2002-09-09 3-Azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists
IS7187A IS7187A (is) 2001-10-22 2004-03-18 3-asabísýkló (3.1.0) hexanafleiður sem ópíóíðviðtaka mótlyf
IL161157A IL161157A (en) 2001-10-22 2004-03-29 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists
NO20041626A NO329092B1 (no) 2001-10-22 2004-04-21 3-azabicyklo (3.1.0) heksanderivater som opioidreseptorantagonister samt farmasoytisk sammensetning
TNP2004000071A TNSN04071A1 (fr) 2001-10-22 2004-04-21 Derives de 3-azabicyclo [3.1.0] hexane servant d'antagonistes des recepteurs d'opioides

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33851101P 2001-10-22 2001-10-22
US60/338,511 2001-10-22

Publications (1)

Publication Number Publication Date
WO2003035622A1 true WO2003035622A1 (en) 2003-05-01

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ID=23325099

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Application Number Title Priority Date Filing Date
PCT/IB2002/003668 Ceased WO2003035622A1 (en) 2001-10-22 2002-09-09 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists

Country Status (41)

Country Link
US (3) US7049335B2 (enExample)
EP (1) EP1440059B1 (enExample)
JP (2) JP4155522B2 (enExample)
KR (1) KR100621292B1 (enExample)
CN (1) CN100368398C (enExample)
AP (1) AP1816A (enExample)
AR (1) AR036905A1 (enExample)
AT (1) ATE392415T1 (enExample)
AU (1) AU2002329557B2 (enExample)
BR (1) BR0213464A (enExample)
CA (1) CA2463264C (enExample)
CR (1) CR7317A (enExample)
DE (1) DE60226161T2 (enExample)
DK (1) DK1440059T3 (enExample)
EA (1) EA006708B1 (enExample)
EC (1) ECSP045077A (enExample)
ES (1) ES2302839T3 (enExample)
GE (1) GEP20084300B (enExample)
GT (1) GT200200216A (enExample)
HN (1) HN2002000299A (enExample)
HR (1) HRP20040288A2 (enExample)
HU (1) HUP0401884A2 (enExample)
IL (2) IL161157A0 (enExample)
IS (1) IS7187A (enExample)
MA (1) MA27141A1 (enExample)
MX (1) MXPA04003730A (enExample)
MY (1) MY136580A (enExample)
NO (1) NO329092B1 (enExample)
NZ (1) NZ531807A (enExample)
OA (1) OA12711A (enExample)
PA (1) PA8556701A1 (enExample)
PE (1) PE20030610A1 (enExample)
PL (1) PL368919A1 (enExample)
PT (1) PT1440059E (enExample)
RS (1) RS25104A (enExample)
SI (1) SI1440059T1 (enExample)
SV (1) SV2004001363A (enExample)
TN (1) TNSN04071A1 (enExample)
UA (1) UA75714C2 (enExample)
WO (1) WO2003035622A1 (enExample)
ZA (1) ZA200402172B (enExample)

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005018645A1 (en) * 2003-08-21 2005-03-03 Pfizer Products Inc. A pharmaceutical composition for the prevention and treatment of addiction in a mammal
US6867222B2 (en) 2001-04-18 2005-03-15 Euro-Celtique, S.A. Nociceptin analogs
WO2005080382A1 (en) * 2004-02-23 2005-09-01 Glaxo Group Limited Azabicyclo (3.1.0) hexane derivatives useful as modulators of dopamine d3 receptors
US7049335B2 (en) 2001-10-22 2006-05-23 Pfizer Inc. 3-azabicyclo[3.1.0]hexane derivatives
WO2006133946A1 (en) * 2005-06-14 2006-12-21 Glaxo Group Limited Azab i cyclo [3 . 1 . 0] hexane derivatives as dopamin d3 receptor modulators
WO2007022934A3 (en) * 2005-08-22 2007-05-10 Glaxo Group Ltd Azabicyclo (3, 1, 0) hexan derivatives useful as modulators of dopamine d3 receptors
WO2007073503A3 (en) * 2005-12-21 2007-11-08 Bristol Myers Squibb Co Indane modulators of glucocorticoid receptor, ap-1, and/or nf-kb activity and use thereof
JPWO2005085228A1 (ja) * 2004-03-05 2008-01-17 萬有製薬株式会社 シクロアルカノピリジン誘導体
WO2008075162A3 (en) * 2006-12-15 2008-10-23 Pfizer Ltd Selective mu opioid receptor antagonists for the treatment of female sexual dysfunction
EP1837022A4 (en) * 2004-12-14 2009-12-16 Toray Industries INDOLOMORPHINANE DERIVATIVE WITH CARBOXY IN 6 'POSITION
WO2015076310A1 (ja) 2013-11-20 2015-05-28 株式会社 三和化学研究所 新規３－アザビシクロ［３．１．０］ヘキサン誘導体及びその医薬用途
US9133116B2 (en) 2010-09-28 2015-09-15 Panacea Biotec Ltd. Bicyclic compounds
WO2018159716A1 (ja) 2017-03-02 2018-09-07 株式会社 三和化学研究所 アルコール使用障害の治療薬
US10392345B2 (en) 2015-05-20 2019-08-27 Sanwa Kagaku Kenkyusho Co., Ltd. Crystal of salt of novel 3-azabicyclo[3.1.0]hexane derivative and pharmaceutical use thereof

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US7153976B2 (en) * 2003-10-06 2006-12-26 Pfizer Inc. Purification process for an azabicyclo[3.1.0]hexane compound
ES2634841T3 (es) * 2003-10-14 2017-09-29 Pfizer Products Inc. Derivados bicíclicos [3.1.0] como inhibidores del transportador de glicina
KR20060096038A (ko) * 2003-10-16 2006-09-05 화이자 프로덕츠 인크. 3-아자비시클로〔3.1.0〕헥산 유도체의 제조법
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
EP2195314B1 (en) * 2007-08-27 2011-03-23 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
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