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CA2297889A1 - Antagoniste de recepteur adrenergique alpha 1a - Google Patents

Antagoniste de recepteur adrenergique alpha 1a Download PDF

Info

Publication number
CA2297889A1
CA2297889A1 CA002297889A CA2297889A CA2297889A1 CA 2297889 A1 CA2297889 A1 CA 2297889A1 CA 002297889 A CA002297889 A CA 002297889A CA 2297889 A CA2297889 A CA 2297889A CA 2297889 A1 CA2297889 A1 CA 2297889A1
Authority
CA
Canada
Prior art keywords
alkyl
halogen
alkoxy
compound
substituted
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.)
Abandoned
Application number
CA002297889A
Other languages
English (en)
Inventor
Norihiro Ikemoto
Robert D. Larsen
Michel Chartrain
Daniel R. Sidler
Gerald F. Bills
Colleen S. Taylor
Wenjie Li
Christopher M. Roberge
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.)
Merck and Co Inc
Original Assignee
Individual
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 claimed from GBGB9719708.1A external-priority patent/GB9719708D0/en
Priority claimed from GBGB9719706.5A external-priority patent/GB9719706D0/en
Priority claimed from US09/122,301 external-priority patent/US6207444B1/en
Application filed by Individual filed Critical Individual
Publication of CA2297889A1 publication Critical patent/CA2297889A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention a trait à des sels cristallins pharmaceutiquement acceptables d'un antagoniste de récepteur adrénergique alpha 1a, le composé A, qui sont utiles dans le traitement d'hyperplasie prostatique bénigne. L'invention a également trait à des compositions pharmaceutiques employant les sels cristallins, et à des procédés de fabrication et d'utilisation des sels cristallins et des compositions pharmaceutiques du composé A. L'invention se réfère en outre à un procédé permettant d'obtenir un produit intermédiaire pur du point de vue des énantiomères, qui est utile en vue de la synthèse du produit final que constituent les antagonistes de récepteur adrénergique alpha 1a. Les composés obtenus comme produit final sont utiles pour traiter l'hyperplasie prostatique bénigne, et pour obtenir un relâchement de tissus des voies urinaires inférieures. L'invention concerne également un procédé utile pour la préparation d'une classe de composés dihydropyrimidinone dont le composé A fait partie; le procédé comporte les étapes consistant à effectuer une déprotonation d'un composé dihydropyrimidinone, et ensuite coupler le dérivé déprotonaté à une amine primaire.
CA002297889A 1997-08-05 1998-07-31 Antagoniste de recepteur adrenergique alpha 1a Abandoned CA2297889A1 (fr)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US5490297P 1997-08-05 1997-08-05
US5481597P 1997-08-05 1997-08-05
GB9719706.5 1997-09-16
GB9719708.1 1997-09-16
GBGB9719708.1A GB9719708D0 (en) 1997-09-16 1997-09-16 Enzymatic resolution of a dihydropyrimidinone
GBGB9719706.5A GB9719706D0 (en) 1997-09-16 1997-09-16 Alpha 1a adrenergic receptor antagonist
US60/054,902 1998-07-24
US60/054,815 1998-07-24
US09/122,301 1998-07-24
US09/122,301 US6207444B1 (en) 1997-08-05 1998-07-24 Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease
PCT/US1998/016011 WO1999007695A2 (fr) 1997-08-05 1998-07-31 ANTAGONISTE DE RECEPTEUR ADRENERGIQUE ALPHA 1a

Publications (1)

Publication Number Publication Date
CA2297889A1 true CA2297889A1 (fr) 1999-02-18

Family

ID=27517427

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002297889A Abandoned CA2297889A1 (fr) 1997-08-05 1998-07-31 Antagoniste de recepteur adrenergique alpha 1a

Country Status (5)

Country Link
EP (1) EP1003734A2 (fr)
JP (1) JP2001512724A (fr)
AU (1) AU8680598A (fr)
CA (1) CA2297889A1 (fr)
WO (1) WO1999007695A2 (fr)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6268369B1 (en) 1994-11-16 2001-07-31 Synaptic Pharmaceutical Corporation 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
JP3200070B2 (ja) 1994-11-16 2001-08-20 シナプティック・ファーマスーティカル・コーポレーション ジヒドロピリミジン類およびその使用
US6228861B1 (en) 1995-11-16 2001-05-08 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
US6469065B1 (en) 1996-02-02 2002-10-22 Nitromed, Inc. Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
US6172066B1 (en) 1996-05-16 2001-01-09 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
US6245773B1 (en) 1996-05-16 2001-06-12 Synaptic Pharmaceutical Corporation 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
JP2002532525A (ja) * 1998-12-23 2002-10-02 シナプティック・ファーマスーティカル・コーポレーション ジヒドロピリミジンおよびその使用
US6680323B2 (en) 1998-12-23 2004-01-20 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
US6274585B1 (en) * 1998-12-23 2001-08-14 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
US6720324B2 (en) 2000-07-05 2004-04-13 Synaptic Pharmaceutical Corporation Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
CN1301977C (zh) 2001-07-13 2007-02-28 阿斯特拉曾尼卡英国有限公司 氨基嘧啶化合物的制备方法
JP4579821B2 (ja) 2002-12-16 2010-11-10 アストラゼネカ・ユーケイ・リミテッド ピリミジン化合物を製造するための方法
EP2426120A1 (fr) 2003-08-18 2012-03-07 Fujifilm Finechemicals Co., Ltd. Pyridyl-tétrahydropyridines et pyridyl-pipéridines et procédé de leur fabrication
GB0428328D0 (en) 2004-12-24 2005-02-02 Astrazeneca Uk Ltd Chemical process

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3200070B2 (ja) * 1994-11-16 2001-08-20 シナプティック・ファーマスーティカル・コーポレーション ジヒドロピリミジン類およびその使用
CZ184098A3 (cs) * 1995-12-14 1998-11-11 Merck And Co., Inc. Způsob výroby dihydropyrimidinonů

Also Published As

Publication number Publication date
WO1999007695A3 (fr) 1999-06-17
WO1999007695A2 (fr) 1999-02-18
AU8680598A (en) 1999-03-01
EP1003734A2 (fr) 2000-05-31
JP2001512724A (ja) 2001-08-28

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