US2007004758A1PendingUtilityA1
Compositions and treatments for inhibiting kinase and/or hmg-coa reductase
Est. expiryApr 29, 2024(expired)· nominal 20-yr term from priority
C07D 405/14C07D 401/04A61K 31/4439C07D 403/04Y02A50/30A61K 31/4178A61K 31/506A61K 31/4172
55
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Claims
Abstract
The present invention provides compositions of matter, kits and methods for their use in the treatment of MAP kinase-related conditions and/or HMG-CoA reductase-related conditions. In particular, the invention provides compositions for treating inflammatory and/or cardiovascular conditions in an animal subject by inhibiting p38α MAP kinase and/or HMG-CoA reductase, as well as providing formulations and modes of administering such compositions. The invention further provides methods for the rational design of inhibitors of MAP kinase, HMG-CoA reductase, or both for use in the practice of the present invention.
Claims
exact text as granted — not AI-modified1 . A method of inhibiting a MAP kinase comprising administering an effective amount of at least one compound comprising formula V:
wherein R 1 is
n being 0 or any integer;
R 2 is optionally substituted alkyl, aryl, or heteroaryl;
R 4 is optionally substituted
and R 5 is optionally substituted aryl or heteroaryl, or a salt thereof.
2 . The method as recited in claim 1 wherein said R 1 has the following stereochemistry:
3 . The method as recited in claim 1 wherein said inhibited MAP kinase is p38 MAP kinase.
4 . The method as recited in claim 1 , further comprising inhibiting an HMG CoA reductase.
5 . The method as recited in claim 1 wherein said administering treats a MAP kinase-related condition.
6 . The method as recited in claim 1 wherein said administering treats a MAP kinase-related condition and an HMG CoA reductase-related condition.
7 . The method as recited in claim 1 wherein said administering treats an inflammatory condition.
8 . A compound comprising formula V:
wherein R 1 is
being 0 or any integer;
R 2 is optionally substituted alkyl, aryl, or heteroaryl;
R 4 is optionally substituted
and R 5 is optionally substituted aryl or heteroaryl, or a salt thereof,
with the proviso that when R 4 is the pyridinyl ring optionally substituted with one or more substituents selected from halogen atoms and hydroxyl, C 1-3 alkyl, C 1-3 alkoxy and trifluoromethyl groups, then the bridging group of R 1 is —CH 2 —CH 2 —.
9 . The compound as recited in claim 8 wherein R 2 is a C 3-4 branched alkyl group.
10 . The compound as recited in claim 8 wherein R 2 is isopropyl.
11 . The compound as recited in claim 8 wherein R 2 is t-butyl.
12 . The compound as recited in claim 8 wherein R 2 is —CF 3 .
13 . The compound as recited in claim 8 wherein R 2 is phenyl.
14 . The compound as recited in claim 8 wherein R 2 is
15 . The compound as recited in claim 8 wherein R 2 is
16 . The compound as recited in claim 8 wherein R 4 is
17 . The compound as recited in claim 8 wherein R 4 is
18 . The compound as recited in claim 8 wherein R 4 is
19 . The compound as recited in claim 8 wherein R 4 is
20 . The compound as recited in claim 8 wherein R 4 is
21 . The compound as recited in claim 8 wherein R 4 is
22 . The compound as recited in claim 8 wherein R 4 is
23 . The compound as recited in claim 8 wherein R 4 is
24 . The compound as recited in claim 8 wherein R 4 is
25 . The compound as recited in claim 8 wherein R 4 is
26 . The compound as recited in claim 8 wherein R 5 is an optionally substituted phenyl group.
27 . The compound as recited in claim 8 wherein R 5 is 4-fluorophenyl.
28 . The compound as recited in claim 8 wherein R 5 is 3-trifluoromethylphenyl.
29 - 32 . (canceled)
33 . A compound comprising formula V:
wherein R 1 is
or any integer;
R 2 is optionally substituted alkyl, aryl, or heteroaryl;
R 4 is optionally substituted
and R 5 is optionally substituted aryl or heteroaryl, or a salt thereof,
with the proviso that when R 4 is the pyridinyl ring, said pyridinyl ring is substituted with one or more optionally substituted amino groups.
34 . A compound comprising formula Va:
wherein R 1 is
being 0 or any integer;
R 2 is optionally substituted alkyl, aryl, or heteroaryl;
the pyrimidinyl ring is optionally substituted;
and R 5 is optionally substituted aryl or heteroaryl, or a salt thereof.
35 . A compound comprising formula Vb:
wherein R 1 is
being 0 or any integer;
R 2 is optionally substituted alkyl, aryl, or heteroaryl;
the pyridinyl ring is optionally substituted, with the proviso that when the pyridinyl ring is unsubstituted or substituted with one or more substituents selected from halogen atoms and hydroxyl, C 1-3 alkyl, C 1-3 alkoxy and trifluoromethyl groups, then the bridging group of R 1 is —CH 2 —CH 2 —; and R 5 is optionally substituted aryl or heteroaryl, or a salt thereof.
36 . A pharmaceutical composition comprising an effective amount of at least one compound as recited in claim 8 with a pharmaceutically acceptable carrier.
37 . A method of treating a condition in a subject in need thereof comprising administering to said subject an effective amount of at least one compound comprising formula V:
wherein R 1 is
n being 0 or any integer;
R 2 is optionally substituted alkyl, aryl, or heteroaryl;
R 4 is optionally substituted
and R 5 is optionally substituted aryl or heteroaryl, or a salt thereof,
with the proviso that when R 4 is the pyridinyl ring optionally substituted with one or more substituents selected from halogen atoms and hydroxyl, C 1-3 alkyl, C 1-3 alkoxy and trifluoromethyl groups, then the bridging group of R 1 is —CH 2 —CH 2 —.
38 . The method as recited in claim 37 wherein said condition is a MAP kinase and/or an HMG-CoA reductase related condition.Cited by (0)
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