EP0214743A2
Expired / Lapsed
EP
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Use of quinoline derivatives in the manufacture of medicaments for the treatment of cerebrovascular disorders and cerebral senility
Assignee: Beecham Wuelfing GmbH and Co KG
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Filing: 1986-07-29
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Granted: —
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Expires: 2006-07-29
Abstract
Abstract A method for the treatment and/or prophylaxis of cerebrovascular disorders and/or disorders associated with cerebral senility in mammals, such as humans, which comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of a compound of formula (I): wherein: n is 1 or 2; R₁ is chloro, bromo, C 1-6 alkylcarbonyl or cyano; one of R₃ and R₄ is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl or R₃ and R₄ together are C 2-5 polymethylene; and either R₅ is hydroxy, C 1-3 alkoxy or C 1-8 acyloxy; and R₂ is hydrogen and the cyclic amide moiety and R₅ are trans ; or R₅ and R₂ together form a bond, novel compounds within formula (I), processes for their preparation.
Inventors
- 👤 Geoffrey c/o Beecham Pharmaceuticals Stemp
- 👤 John Morris c/o Beecham Pharmaceuticals Evans
- 👤 Charles David Nicholson
- 👤 Dieter Angersbach
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-28 17:29
CPC Classifications
C; C07; C07D; C07D401/00; C07D401/02; C07D401/04; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
104 words
The use of a compound of formula (I): wherein: n is 1 or 2; R₁ is chloro, bromo, C 1-6 alkylcarbonyl or cyano; one of R₃ and R₄ is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl or R₃ and R₄ together are C 2-5 polymethylene; and either R₅ is hdyroxy, C 1-3 alkoxy or C 1-8 acyloxy; and R₂ is hydrogen and the cyclic amide moiety and R₅ are trans ; or R₅ and R₂ together form a bond, for the manufacture of a medicament for the treatment and/or prophylaxis of cerebrovascular disorders and/or disorders associated with cerebral senility.
Claim 2
Dependent Claim
104 words
The use of a compound of formula (I): wherein: n is 1 or 2; R₁ is chloro, bromo, C 1-6 alkylcarbonyl or cyano; one of R₃ and R₄ is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl or R₃ and R₄ together are C 2-5 polymethylene; and either R₅ is hdyroxy, C 1-3 alkoxy or C 1-8 acyloxy; and R₂ is hydrogen and the cyclic amide moiety and R₅ are trans ; or R₅ and R₂ together form a bond, for the manufacture of a medicament for the treatment and/or prophylaxis of cerebrovascular disorders and/or disorders associated with cerebral senility.
Claim 3
Dependent Claim
10 words
A use according to claim 1, wherein n is 1.
Claim 4
Dependent Claim
15 words
A use according to claim 1 or 2, wherein R₁ is chloro, bromo or cyano.
Claim 5
Dependent Claim
14 words
A use according to any preceding claim, wherein R₃ and R₄ are both methyl.
Claim 6
Dependent Claim
15 words
A use according to any preceding claim, wherein R₂ and R₃ together form a bond.
Claim 7
Dependent Claim
18 words
A use according to any of claims 1 to 4, wherein R₂ is hydrogen and R₅ is hydroxy.
Claim 8
Dependent Claim
22 words
A use according to claim 1 wherein the compound of formula (I) is 6-bromo-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline, 6-cyano-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline, trans-2,2-dimethyl-6-cyano-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydro- quinolin-3-ol, trans-2,2-dimethyl-6-chloro-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydro- quinolin-3-ol, 6-chloro-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline or trans-2,2-dimethyl-6-bromo-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydro-quinolin-3-ol.
Claim 9
Dependent Claim
3 words
6-Bromo-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline or 6-cyano-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline.
Claim 10
Dependent Claim
3 words
6-Bromo-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline or 6-cyano-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline.
Claim 11
Dependent Claim
15 words
A pharmaceutical composition comprising a compound according to claim 8 and a pharmaceutically acceptable carrier.
Claim 12
Dependent Claim
13 words
A compound according to claim 8 for use as an active therapeutic substance.
Claim 13
Dependent Claim
22 words
A compound according to claim 8 for use in the treatment and/or prophylaxis of cerebrovascular disorders and/or disorders associated with cerebral senility.
Claim 14
Dependent Claim
53 words
A process for the preparation of compounds according to claim 8 of formula (IIa): in which R₁₀ is bromo or cyano, which process comprises dehydrating a compound of formula (IV): in which R₆ is hydrogen or an N-protecting group, and thereafter, if necessary, converting R₁₀ to other R₁₀ and converting R₆ to hydrogen.
Claim 15
Dependent Claim
2 words
cis -2,2-Dimethyl-6-bromo-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydroquinolin-3-ol.
Claim 16
Dependent Claim
2 words
cis -2,2-Dimethyl-6-bromo-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydroquinolin-3-ol.
References Cited (Backward Citations)
No citation records indexed.
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