Carbon substituted aminothiazole inhibitors of cyclin...

Details Carbon substituted aminothiazole inhibitors of cyclin... Carbon substituted aminothiazole inhibitors of cyclin...

1999-06-10

2002-06-18

Stockton, Laura L. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S371000, C546S270700, C548S195000

Reexamination Certificate

active

06407124

ABSTRACT:

BRIEF DESCRIPTION OF THE INVENTION
The present invention is directed to compounds of the formula
and pharmaceutically acceptable salts thereof. As used in formula I, and throughout the specification, the symbols have the following meanings:
R
1
=R
2
, COR
3
, CONH
2
, CONR
2
R
3
, COOR
2
, or SO
2
R
2
;
R
2
=alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl;
R
3
=H, alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl;
R
4
=alkyl with two or more carbon atoms, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, or R
9
, with the proviso that when R
1
is acetyl or propionyl and
Y=alkene, then R
4
cannot be nitrofuryl or 2-quinolinyl;
R
5
, R
6
, R
7
, R
8
=independently H, alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, halo, or
hydroxy, alkoxy, amino, NR
12
R
13
, thio, or alkylthio, with the proviso that only one such heteroatom group is bonded to any one carbon atom;
R
10
, R
11
=independently H, alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, halo, hydroxy, alkoxy, alkylcarbonyloxy, carboxy, alkyloxycarbonyl, amino, NR
5
R
16
, carbamoyl, ureido, thio, or alkylthio;
R
12
, R
13
, R
14
, R
15
, R
16
=independently H, alkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl.
The compounds of formula I are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, and cardiovascular disease.


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Goro, A. et al, “Nitroheterocyclic Antimicrobial Agents. I. Nitrothiazolecarboxaldehyde Derivaties”, J. Med. Chem., 1969, 12, 374-379.
Pazzi, P.V. et al, “H2-Antagonists: Synthesis and Activity of 2-Amino-5-Thiazolyl Derivatives”, I1 Farmaco, 44(11), 1011-1030, 1989.

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