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US4622319A Expired / Lapsed US ⏱️ 0.0 years remaining

Methods of using PAF-antagonistic diazepines

Assignee: Boehringer Ingelheim GmbH
•
Filing: 1985-10-01
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Granted: 1986-11-11
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Expires: 2005-10-01
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Abstract

Abstract The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II <IMAGE> (I) or <IMAGE> (II) wherein A is an anellated and optionally substituted benzene or 5- or 6-membered heterocyclic ring; R5 and Z are each independently hydrogen or an optionally substituted C1-C8 alkyl, alkenyl or alkynyl; R6 is an optionally substituted phenyl, or is thienyl or is alpha -pyridyl; Y is CO, CS or CH2; and nontoxic, pharmaceutically acceptable acid addition salts thereof.

Inventors

  • 👤 Jorge Casals-Stenzel
  • 👤 Karl-Heinz Weber
  • 👤 Gerhard Walther
  • 👤 Albrecht Harreus
  • 👤 Gojko Muacevic

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-06 05:01
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/55; A61P; A61P11/00; A61P11/08; A61P43/00; A61P7/00; A61P7/02

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 225 words
A method of treating an individual having a disorder responsive to PAF-antagonist activity, which method comprises treating said individual with a therapeutically effective amount of a compound of formulae ##STR58## wherein A is an anellated ring of formula ##STR59## B is an anellated ring of formula ##STR60## R 1 and R 2 , are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl or an acid amide group; cycloalkyl; a saturated carbocyclic or heterocyclic ring condensed on, which may contain oxygen, sulphur or nitrogen as a heteroatom while the nitrogen-containing ring can carry an alkyl group at the nitrogen atom; halogen, trifluoromethyl, nitro, cyano, optionally substituted amino, alkylmercapto, alkylcarbonyl, alkoxy, alkyloxycarbonyl or an acid amide group; R 3 , R 4 R 5 and Z are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl, or an acid amide group; R 6 is phenyl, which can optionally be substituted, preferably in the 2 position, by methyl, methoxy, halogen, nitro or trifluoromethyl, or R 6 can be thienyl or α-pyridyl; Y is <CO, <CS or <CH 2 ; and non-toxic, pharmaceutically acceptable acid addition salts thereof.
Claim 2
Independent Claim 225 words
A method of treating an individual having a disorder responsive to PAF-antagonist activity, which method comprises treating said individual with a therapeutically effective amount of a compound of formulae ##STR58## wherein A is an anellated ring of formula ##STR59## B is an anellated ring of formula ##STR60## R 1 and R 2 , are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl or an acid amide group; cycloalkyl; a saturated carbocyclic or heterocyclic ring condensed on, which may contain oxygen, sulphur or nitrogen as a heteroatom while the nitrogen-containing ring can carry an alkyl group at the nitrogen atom; halogen, trifluoromethyl, nitro, cyano, optionally substituted amino, alkylmercapto, alkylcarbonyl, alkoxy, alkyloxycarbonyl or an acid amide group; R 3 , R 4 R 5 and Z are each independently hydrogen, a C 1 -C 8 straight-chained or branched alkyl, alkenyl or alkynyl optionally mono- or polysubstituted by halogen, hydroxy, alkoxy, alkylmercapto, amino, alkylamino, dialkylamino, alkylcarbonyl, alkyloxycarbonyl, or an acid amide group; R 6 is phenyl, which can optionally be substituted, preferably in the 2 position, by methyl, methoxy, halogen, nitro or trifluoromethyl, or R 6 can be thienyl or α-pyridyl; Y is <CO, <CS or <CH 2 ; and non-toxic, pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim 14 words
The method of claim 1 which comprises treating with compounds of the formula ##STR61##
Claim 4
Dependent Claim 10 words
The method of claim 2 wherein Y is <CH 2
Claim 5
Dependent Claim 9 words
The method of claim 3 wherein Y is <CO
Claim 6
Dependent Claim 27 words
The method of claim 4 wherein A is ##STR62## Z is C 2 H 5 R 5 is hydrogen; and Y is <CO R 6 is ##STR63##
Claim 7
Dependent Claim 31 words
The method of claim 4 which comprises treating with compounds of the formula A is ##STR64## Z is CH 3 R 5 is hydrogen; Y is <CO R 6 is ##STR65##
Claim 8
Dependent Claim 25 words
The method of claim 4 wherein A is ##STR66## Z is CH 3 R 5 is H Y is <CO and R 6 is ##STR67##
Claim 9
Dependent Claim 24 words
A method of claim 4 wherein H is ##STR68## Z is CH 3 R 5 is H Y is <CO R 6 is ##STR69##
Claim 10
Dependent Claim 14 words
The method of claim 1 which comprises treating with compounds of the formula ##STR70##
Claim 11
Dependent Claim 9 words
The method of claim 9 wherein A is ##STR71##
Claim 12
Dependent Claim 17 words
The method of claim 10 wherein B is ##STR72## R 5 is H R 6 is ##STR73##
Claim 13
Dependent Claim 10 words
B is ##STR74## R 5 is H R 6 ##STR75##
Claim 14
Dependent Claim 10 words
B is ##STR74## R 5 is H R 6 ##STR75##
Claim 15
Dependent Claim 17 words
The method of claim 10 wherein B is ##STR76## R 5 is H R 6 is ##STR77##

References Cited (Backward Citations)

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Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-11-10 1990-05-12 1990-11-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-11-10 1994-05-12 1994-11-11 $3760.00 Window Closed / Lapsed
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