US2003114480A1PendingUtilityA1
Anellated dihydropyridines for the treatment of chronic pain
Assignee: BOEHRINGER INGELHEIM PHARMAPriority: Jul 25, 2000Filed: Sep 11, 2002Published: Jun 19, 2003
Est. expiryJul 25, 2020(expired)· nominal 20-yr term from priority
A61K 31/4747C07D 217/16C07D 495/04A61K 31/4743A61K 31/47A61K 31/4365
53
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Claims
Abstract
The invention relates to the use of anellated dihydropyridines according to the following formula I, and the salts thereof with physiologically acceptable acids, for the treatment of chronic pain, wherein A is benzo or thieno and Z, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are defined as in the specification: The inventions also relates to novel compounds of formula I and pharmaceutical compositions thereof.
Claims
exact text as granted — not AI-modifiedWe claim:
1 ) A method of treating chronic pain comprising administering to a host in need of such treatment a compound of the following formula I or a salt thereof with a physiologically acceptable acid:
wherein A is benzo or thieno,
and if A is benzo
R 1 , R 2 and R 3 independently of one another denote
H, OH,C 1 -C 5 alkyl, C 1 -C 5 alkoxy, or —O—(CH 2 ) 1-5 —OCH 3 ,
or R 2 and R 3 together form the group
—O—CH 2 —O—, and
if A is thieno, R 1 , R 2 and R 3 denote hydrogen;
R 4 and R 5 independently of one another denote
H, or C 1 -C 5 alkyl or together with the atom to which they are bonded form a C 3 -C 7 ring;
R 6 denotes C 1 -C 12 alkyl, or denotes a phenyl or benzyl group each substituted by the groups R 7 and R 8 ,
wherein R 7 and R 8 independently of one another denote hydrogen, halogen, C 1 -C 5 alkyl, C 1 -C 5 alkoxy or C 1 -C 5 fluoroalkyl group;
Z denotes O, S or an NHCO— group or, if at least one of the groups R 4 and R 5 is other than hydrogen, Z may also denote a single bond.
2 ) A method according to claim 1 , wherein the compound of formula I is a compound of Formula IA,
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and Z are as defined in claim 1 .
3 ) A method according to claim 1 , wherein R 1 , R 2 and R 3 independently of each other denote hydrogen, methyl or methoxy.
4 ) A method according to claim 2 , wherein R 1 , R 2 and R 3 independently of each other denote hydrogen, methyl or methoxy.
5 ) A method according to claim 3 , wherein R 2 and R 3 denote methoxy and R 1 is methoxy or hydrogen.
6 ) A method according to claim 4 , wherein R 2 and R 3 denote methoxy and R 1 is methoxy or hydrogen.
7 ) A method according to any one of claims 1 to 6 , wherein R 4 and R 5 independently of each other denote hydrogen or a methyl group.
8 ) A method according to any one of claims 1 to 6 , wherein Z-R 6 denotes a group of formula II, III or IV:
9 ) A method according to claim 7 , wherein Z-R 6 denotes a group of formula II, III or IV:
10 ) A method according to any one of claims 1 to 6 , wherein R 6 denotes C 6 -C 10 alkyl.
11 ) A method according to claim 7 , wherein R 6 denotes C 6 -C 10 alkyl.
12 ) A method according to claim 8 , wherein Z-R 6 denotes a phenoxy group of formula II in the ortho or para-position.
13 ) A method according to claim 9 , wherein Z-R 6 denotes a phenoxy group of formula II in the ortho or para-position.
14 ) A method according to any one of claims 1 to 6 , wherein at least one of the groups R 7 and R 8 denotes a CF 3 group or an F atom.
15 ) A method according to claim 7 , wherein at least one of the groups R 7 and R 8 denotes a CF 3 group or an F atom.
16 ) A method according to claim 8 , wherein at least one of the groups R 7 and R 8 denotes a CF 3 group or an F atom.
17 ) A method according to claim 9 , wherein at least one of the groups R 7 and R 8 denotes a CF 3 group or an F atom.
18 ) A method according to claim 12 , wherein at least one of the groups R 7 and R 8 denotes a CF 3 group or an F atom.
19 ) A method according to claim 13 , wherein at least one of the groups R 7 and R 8 denotes a CF 3 group or an F atom.
20 ) A method according to claim 1 wherein the compound of formula I is a compound of the following formula:
wherein R 4 and R 5 simultaneously denote hydrogen or methyl, and R 6 denotes a group of formula V, VI or VII:
21 ) A method according to claim 1 wherein the compound of formula I is a compound of the following formula:
wherein R 1 denotes methyl or methoxy, R 4 and R 5 simultaneously denote hydrogen or methyl, and R 6 denotes a group of formula V or VII:
22 ) A method according to claim 1 wherein the compound of formula I is a compound of the following formula:
23 ) A method according to claim 1 , wherein the chronic pain is selected from the group consisting of: migraine, neuralgia, muscle pain, inflammatory pain, postoperative pain, shingles, phantom pain, diabetic neuropathy, pain after chronic nerve compression, and pain associated with AIDS or cancer in their final stages.Cited by (0)
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