EP0059983A1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Substituted biphenyl compounds for use as a medicament
Assignee: Wellcome Foundation Ltd
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Filing: 1982-03-10
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Granted: —
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Expires: 2002-03-10
Abstract
Abstract 2-(4-Substitutedphenyl)-2-benzoic acid derivatives, methods for their preparation, pharmaceutical formulations containing the compounds and the use thereof in the reduction or control of blood lipids in animals, including man, are disclosed. The preferred compound is 2-(4-trifluoromethylphenyl)-benzoic acid, which may be administered to man in a dose of about 4 mg/kg bodyweight per day.
Inventors
- 👤 Lawrence Nathaniel Bell
- 👤 Michael Thomas Burke
- 👤 Gordon Lewis Hodgson, Jr.
- 👤 Thomas Kevin Shumaker
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-25 21:58
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/185; A61K31/19; C; C07; C07D; C07D263/00; C07D263/02; C07D263/08; C07D263/10; A61K31/01; A61K31/015; A61P; A61P3/00; A61P3/06; C07C; C07C43/00; C07C43/30; C07C43/307; C07C45/00; C07C45/004; C07C63/00; C07C63/33; C07C63/331; C07C63/337; C07C63/34; C07C63/36; C07C63/68; C07C63/72; C07C65/00; C07C65/21; C07C65/24; C07F; C07F15/00; C07F15/0006; C07F15/006
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
58 words
A compound of the formula (I) wherein:-Ar 1 is selected from Ar 2 is selected from and R is selected from C 1-5 alkyl, halogen, perhalo-C 1-4 alkyl, C 1-4 alkoxy, phenyl, C 1-4 acyl, C 1-6 alkoxycarbonyl, amino or hydroxy, and pharmaceutically acceptable salts thereof for use in the treatment of a mammal, including man, by therapy.
Claim 2
Dependent Claim
58 words
A compound of the formula (I) wherein:-Ar 1 is selected from Ar 2 is selected from and R is selected from C 1-5 alkyl, halogen, perhalo-C 1-4 alkyl, C 1-4 alkoxy, phenyl, C 1-4 acyl, C 1-6 alkoxycarbonyl, amino or hydroxy, and pharmaceutically acceptable salts thereof for use in the treatment of a mammal, including man, by therapy.
Claim 3
Dependent Claim
30 words
A compound of formula (I) as claimed in claim 1 for use in the therapy of a condition in which the underlying atielogy is associated with elevated blood lipid levels.
Claim 4
Dependent Claim
28 words
A compound of formula (I) as claimed in claim 1 or claim 2 which has the formula (IA) or (IB) wherein R is as defined in claim 1.
Claim 5
Dependent Claim
30 words
A compound of formula (I) as claimed in anyone of claims 1 to 3 wherein R is selected from C l-5 alkyl, halogen, C l-4 , alkoxy, phenyl or trihalomethyl.
Claim 6
Dependent Claim
20 words
A compound of formula (I) as claimed in claim 1 wherein R is selected from C 2-5 alkyl or trihalomethyl.
Claim 7
Dependent Claim
23 words
A compound of formula (I) as claimed in anyone of claims 1 to 5 wherein the compound of formula (I) is 2-(4-trifluoromethylphenyl)-benzoic acid.
Claim 8
Dependent Claim
31 words
A pharmaceutical formulation comprising a compound of formula (I) as defined in anyone of claims 1 to 6 or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier therefor.
Claim 9
Dependent Claim
35 words
A compound of the formula (II) in which Ar 7 is selected from Ar 8 is selected from and R 1 is C 2-5 alkyl, perfluoro C 1-4 alkyl, phenyl; and pharmaceutically acceptable salts thereof.
Claim 10
Dependent Claim
35 words
A compound of the formula (II) in which Ar 7 is selected from Ar 8 is selected from and R 1 is C 2-5 alkyl, perfluoro C 1-4 alkyl, phenyl; and pharmaceutically acceptable salts thereof.
Claim 11
Dependent Claim
27 words
A compound of formula (II) as claimed in claim 8, which compound has the formula (IIA) or (IIB) wherein R 1 is as defined in claim 8.
Claim 12
Dependent Claim
18 words
2-(4-Trifluoromethylphenyl)-benzoic acid; 2-(4-Ethylphenyl)-benzoic acid; 2-(4-isoPropylphenyl)-benzoic acid; 2-(4-n-Butylphenyl)-benzoic acid; 2-(4-t-Butylphenyl)-benzoic acid; 2-(4-Biphenyl)-benzoic acid; 1-(4-Trifluoromethylphenyl)-2-naphthoic acid; 1-(4-Ethylphenyl)-2-naphthoic acid; 2-(2-Naphthyl)-benzoic acid.
Claim 13
Dependent Claim
18 words
2-(4-Trifluoromethylphenyl)-benzoic acid; 2-(4-Ethylphenyl)-benzoic acid; 2-(4-isoPropylphenyl)-benzoic acid; 2-(4-n-Butylphenyl)-benzoic acid; 2-(4-t-Butylphenyl)-benzoic acid; 2-(4-Biphenyl)-benzoic acid; 1-(4-Trifluoromethylphenyl)-2-naphthoic acid; 1-(4-Ethylphenyl)-2-naphthoic acid; 2-(2-Naphthyl)-benzoic acid.
Claim 14
Dependent Claim
146 words
A method for the preparation of a compound of formula (I) as defined in claim 1 which method comporises:- a) conversion, to a compound of formula (I), of a compound of formula (III) wherein Ar is as defined in claim 1; Ar 3 is and Z is a protected carboxylic acid group or a carboxylic acid group precursor; b) reduction of a compound of formula (IIII) wherein Ar 2 is as defined in claim 1; Ar 4 is Y is and R is as defined in claim 1; c) Selective oxidation of a compound of formula (IX) wherein Ar 1 is as defined in claim 1; and R is C 1-4 alkyl or hydrogen; or d) Reaction of a compound of formula (XI) in which Ar 1 is as defined above and Ar 9 is A is -Mg X were X is halogen with carbon dioxide.
Claim 15
Dependent Claim
29 words
12) A method as claimed in claim 11 where the compound of formula (I) is a compound of formula (II) as defined in anyone of claims 8 to 10.
References Cited (Backward Citations)
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