CA2294591A1 - Antagonistes des adrenorecepteurs alpha 1a - Google Patents

Antagonistes des adrenorecepteurs alpha 1a Download PDF

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Publication number
CA2294591A1
CA2294591A1 CA002294591A CA2294591A CA2294591A1 CA 2294591 A1 CA2294591 A1 CA 2294591A1 CA 002294591 A CA002294591 A CA 002294591A CA 2294591 A CA2294591 A CA 2294591A CA 2294591 A1 CA2294591 A1 CA 2294591A1
Authority
CA
Canada
Prior art keywords
phenyl
alkyl
cyano
independently selected
cycloalkyl
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
CA002294591A
Other languages
English (en)
Inventor
Michael A. Patane
Mark G. Bock
Dhanapalan Nagarathnam
Bharat Lagu
Wai C. Wong
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.)
Lundbeck Research USA Inc
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 GBGB9800219.9A external-priority patent/GB9800219D0/en
Application filed by Individual filed Critical Individual
Publication of CA2294591A1 publication Critical patent/CA2294591A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/45—Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C255/46—Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of non-condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/26—Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Cette invention se rapporte à certains nouveaux composés et dérivés de ces composés, à leur synthèse et à leur utilisation en tant qu'antagonistes des adrénorécepteurs alpha 1a. L'une des applications de ces composés se fait dans le traitement de l'hyperplasie prostatique bénigne. Ces composés sont sélectifs du point de vue de leur capacité à provoquer la détente de tissus des muscles lisses enrichis par un récepteur du sous-type alpha 1a et ce, sans entraîner d'hypotension. L'un de ces tissus entoure la tunique urétrale. Par conséquent, les composés selon l'invention peuvent être utilisés pour induire un soulagement prononcé chez les hommes souffrant de l'hyperplasie prostatique bégnigne du fait qu'ils permettent un écoulement de l'urine plus facile. Les composés selon la présente invention peuvent également être utilisés en combinaison avec un composé inhibiteur de la réductase 5-alpha humaine et ce, de manière à induire un soulagement prononcé et chronique concernant les effets de l'hyperplasie prostatique bénigne.
CA002294591A 1997-06-18 1998-06-17 Antagonistes des adrenorecepteurs alpha 1a Abandoned CA2294591A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US5013697P 1997-06-18 1997-06-18
US60/050,136 1997-06-18
GBGB9800219.9A GB9800219D0 (fr) 1998-01-07 1998-01-07
GB9800219.9 1998-01-07
PCT/US1998/012573 WO1998057632A1 (fr) 1997-06-18 1998-06-17 ANTAGONISTES DES ADRENORECEPTEURS ALPHA 1a

Publications (1)

Publication Number Publication Date
CA2294591A1 true CA2294591A1 (fr) 1998-12-23

Family

ID=26312897

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002294591A Abandoned CA2294591A1 (fr) 1997-06-18 1998-06-17 Antagonistes des adrenorecepteurs alpha 1a

Country Status (5)

Country Link
EP (1) EP1014973A4 (fr)
JP (1) JP2002511086A (fr)
AU (1) AU8147498A (fr)
CA (1) CA2294591A1 (fr)
WO (1) WO1998057632A1 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6207444B1 (en) 1997-08-05 2001-03-27 Merck & Co., Inc. Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease
AU5234899A (en) 1998-07-30 2000-02-21 Merck & Co., Inc. Alpha 1a adrenergic receptor antagonists
US6319932B1 (en) 1998-11-10 2001-11-20 Merck & Co., Inc. Oxazolidinones useful as alpha 1A adrenoceptor antagonists
US6228870B1 (en) 1998-11-10 2001-05-08 Merck & Co., Inc. Oxazolidinones useful as alpha 1a adrenoceptor antagonists
US6358959B1 (en) 1999-01-26 2002-03-19 Merck & Co., Inc. Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists
GB2355456A (en) 1999-09-30 2001-04-25 Merck & Co Inc Novel arylhydantoin derivatives useful as alpha 1a adrenoceptor antagonists
GB2355264A (en) 1999-09-30 2001-04-18 Merck & Co Inc Spirohydantoin derivatives useful as alpha 1a adrenoceptor antagonists
GB2355457A (en) 1999-09-30 2001-04-25 Merck & Co Inc Novel spirotricyclic substituted azacycloalkane derivatives useful as alpha 1a adrenoceptor antagonists
GB2355263A (en) 1999-09-30 2001-04-18 Merck & Co Inc Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4593024A (en) * 1985-08-15 1986-06-03 International Minerals & Chemical Corp. Dihydroisoxazole compounds and anthelmintic use
US5231179A (en) * 1986-01-27 1993-07-27 Sumitomo Pharmaceuticals Company, Limited Heterocyclic compounds and their production
US5380737A (en) * 1989-05-04 1995-01-10 Sterling Winthrop Inc. Saccharin derivative proteolytic enzyme inhibitors
US5620993A (en) * 1995-06-07 1997-04-15 Merck & Co., Inc. Alpha-1a adrenergic receptor antagonists
WO1997018209A1 (fr) * 1995-11-15 1997-05-22 Merck & Co., Inc. ANTAGONISTES DE RECEPTEURS ADRENERGIQUES ALPHA 1a
WO1997017969A1 (fr) * 1995-11-16 1997-05-22 Synaptic Pharmaceutical Corporation Dihydropirimidines et leurs emplois

Also Published As

Publication number Publication date
WO1998057632A1 (fr) 1998-12-23
EP1014973A4 (fr) 2000-09-20
AU8147498A (en) 1999-01-04
JP2002511086A (ja) 2002-04-09
EP1014973A1 (fr) 2000-07-05

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