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EP0308956A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Leukotriene LTD4 and LTB4 antagonists

Assignee: GD Searle LLC
•
Filing: 1988-09-23
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Granted: —
•
Expires: 2008-09-23
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Abstract

Abstract This invention encompasses compounds of Formula I and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein: X, Y, and Z are each independently O or S with S optionally oxidized to S = O; Alk is straight or branched chain alkylene or hydroxyalkylene containing 1-6 carbon atoms; R₁ is hydrogen or lower alkyl; n is 0 to 5; R₂ is hydrogen, lower alkyl, cycloalkyl, -(CH₂) n -CO₂R₁, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; and Ar is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl. This invention is in the field of pharmaceutical agents which act as leukotriene D₄ (LTD₄) antagonists and includes embodiments which act as leukotriene B₄ (LTD₄) antagonists.

Inventors

  • 👤 James Ronald Deason
  • 👤 Michael Allan Stealey
  • 👤 Richard Mathias Weier

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-08 16:02
CPC Classifications
C; C07; C07D; C07D327/00; C07D327/02; C07D327/04; A; A61; A61P; A61P29/00; A61P37/00; A61P37/08; C07D339/00; C07D339/02; C07D339/06

Claims Analysis

Total Claims: 3
Claim 1
Independent Claim 133 words
Process for preparing compounds of Formula I and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein: X, Y, and Z are each independently O or S with S optionally oxidized to S = O; Alk is straight or branched chain alkylene or hydroxyalkylene containing 1-6 carbon atoms; R₁ is hydrogen or lower alkyl; n is 0 to 5; R₂ is hydrogen, lower alkyl, cycloalkyl, -(CH₂) n -CO₂R₁, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; and Ar is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl; by reacting compounds of the formula with in the presence of BF₃ and by reacting the obtained compound with ArO Alk Br wherein Ar, X, Y, Z, n, Alk, R₁ and R₂ are as defined above.
Claim 2
Dependent Claim 133 words
Process for preparing compounds of Formula I and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein: X, Y, and Z are each independently O or S with S optionally oxidized to S = O; Alk is straight or branched chain alkylene or hydroxyalkylene containing 1-6 carbon atoms; R₁ is hydrogen or lower alkyl; n is 0 to 5; R₂ is hydrogen, lower alkyl, cycloalkyl, -(CH₂) n -CO₂R₁, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; and Ar is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl; by reacting compounds of the formula with in the presence of BF₃ and by reacting the obtained compound with ArO Alk Br wherein Ar, X, Y, Z, n, Alk, R₁ and R₂ are as defined above.
Claim 3
Dependent Claim 14 words
Use of compounds prepared according to claim 1 for preparing medicaments for treating allergy.

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