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EP0076072A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Sulphonamides

Assignee: Beecham Wuelfing GmbH and Co KG
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Filing: 1982-09-20
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Granted: —
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Expires: 2002-09-20
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Abstract

Abstract Compounds of the formula (I) and salts thereof: wnerem: A is a bond, -CH 2 - or -CH=CH-; R 2 is hydrogen and R 1 is selected from C 1-4 alkyl, hydroxyl, C 1-4 alkoxy, C 1-4 alkanoyloxy, hydrogen, halogen, nitro, cyano, and amino optionally substituted by one or two C 1-4 alkyl groups or by C 1-4 alkanoyl; R 4 is C 1-4 alkyl, hydroxy, C 1-4 alkoxy, C 1-4 alkanoyloxy or n i trato; R 2 N is 1-piperidyl, morpholino or 4-methyl-1-piperazyl, optionally substituted by one or two methyl groups in the 2-, 4- or 6- positions as apt, or 1-pyrrolidyl substituted by one or two methyl groups. m is 0 or 1; and n is 0 to 3 a process for their preparation and compositions containing them.

Inventors

  • 👤 Ljerka Jozic

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-23 18:13
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/12; C07D295/125; C07D295/13; A; A61; A61P; A61P9/00; A61P9/06

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 123 words
A compound of the formula (I) or a pharmaceutically acceptable salt thereof: wherein: A is a bond, -CH 2 - or -CH=CH=; R 2 is hydrogen and R 1 is selected from C 1-4 alkyl, hydroxyl, C 1-4 alkoxy, C 1-4 alkanoyloxy, hydrogen, haloge nitro, cyano, and amino optionally substituted by one or two C 1-4 alkyl groups or by C 1-4 alkanoyl; R 4 is C 1-4 alkyl, hydroxy, C 1-4 alkoxy, C 1-4 alkanoyloxy or nitrato; R 2 N is 1-piperidyl, morpholino or 4-methyl-l-piperazyl, optionally substituted by one or two methyl groups in the 2-, 4- or 6- positions as apt or 1-pyrrolidyl substituted by one or two methyl groups. m is 0 or 1; and n is 0 to 3
Claim 2
Dependent Claim 123 words
A compound of the formula (I) or a pharmaceutically acceptable salt thereof: wherein: A is a bond, -CH 2 - or -CH=CH=; R 2 is hydrogen and R 1 is selected from C 1-4 alkyl, hydroxyl, C 1-4 alkoxy, C 1-4 alkanoyloxy, hydrogen, haloge nitro, cyano, and amino optionally substituted by one or two C 1-4 alkyl groups or by C 1-4 alkanoyl; R 4 is C 1-4 alkyl, hydroxy, C 1-4 alkoxy, C 1-4 alkanoyloxy or nitrato; R 2 N is 1-piperidyl, morpholino or 4-methyl-l-piperazyl, optionally substituted by one or two methyl groups in the 2-, 4- or 6- positions as apt or 1-pyrrolidyl substituted by one or two methyl groups. m is 0 or 1; and n is 0 to 3
Claim 3
Dependent Claim 44 words
A compound according to claim 1 wherein: R 2 is hydrogen and R 1 is selected from C 1-4 alkoxy, C 1-4 alkanoyloxy, hydrogen, halogen, nitro, cyano and amino optionally substituted by one or two C 1-4 alkyl groups or by C 1-4 alkanoyl.
Claim 4
Dependent Claim 19 words
A compound according to claim 2 wherein R 2 N is 1-pyrrolidyl substituted by one or two methyl groups.
Claim 5
Dependent Claim 12 words
A compound according to claim 2 wherein R 2 N is 1-piperidyl.
Claim 6
Dependent Claim 19 words
A compound according to claim 2 wherein R 2 N is 1-piperidyl substituted by one or two methyl groups.
Claim 7
Dependent Claim 29 words
A compound according to any one of claims 2 to 5 wherein R 2 is selected from C 1-4 alkoxy, hydrogen, nitro, cyano and optionally substituted amino as defined.
Claim 8
Dependent Claim 23 words
A compound according to claim 1, of formula (VII): wherein: is hydrogen or C 1-4 alkoxy; and n 1 is 1 or 2.
Claim 9
Dependent Claim 11 words
1-[2-(4-methoxy-1-naphthalenesulphonamido) propyl]-2-methylpiperidine, 1-[4-(1-naphthalenesulphonamdio) pentyl]-2-methyl piperidine or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim 11 words
1-[2-(4-methoxy-1-naphthalenesulphonamido) propyl]-2-methylpiperidine, 1-[4-(1-naphthalenesulphonamdio) pentyl]-2-methyl piperidine or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim 75 words
A process for the preparation of a compound according to claim 1 comprising the reaction of a compound of the formula (VIII): wherein the variables are as defined in relation to formula (I) and a compound of the formula (IX): wherein Z is a group readily displaceable by a nucleophile, such as chlorine or bromine and A, and are as hereinbefore defined; and optionally forming a salt of the resultant compound of the formula (I).
Claim 12
Dependent Claim 22 words
A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.
Claim 13
Independent Claim 37 words
A method of treatment or prophylaxis of cardiac arrhythmia in mammals including humans, comprising the administration to a sufferer of a therapeutically effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof.
Claim 14
Independent Claim 37 words
A method of treatment or prophylaxis of cardiac arrhythmia in mammals including humans, comprising the administration to a sufferer of a therapeutically effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim 18 words
A compound according to claim 1 wherein R 2 is hydrogen and R 1 is C 1-4 alkyl.
Claim 16
Dependent Claim 19 words
A compound according to claim 12 wherein R 2 N is 1-pyrrolidyl substituted by one or two methyl groups.
Claim 17
Dependent Claim 31 words
A compound according to claim 1 of formula (IV) : wherein R 1 1 is C 1-4 alkox y , C 1-4 alkyl or hydrogen, and n is 1 or 3.
Claim 18
Dependent Claim 9 words
1- [4-(4-methoxy-1-naphthalenesulponamido) pentyl]-2,3-dimethylpyrrolidine or a pharmaceutically acceptable salt thereof.
Claim 19
Dependent Claim 9 words
1- [4-(4-methoxy-1-naphthalenesulponamido) pentyl]-2,3-dimethylpyrrolidine or a pharmaceutically acceptable salt thereof.

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