US 2004/0171630 A1Published application

Tyrosine kinase inhibitors

OwnerYuntae Kim, Barbara Hanneyinventors

Life of this patent

Estimating the term…

Abstract

The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

Claims34

Dependent claims

A compound of Formula I

25
wherein
W is selected from:
26
X and Y are independently selected from C or N, provided that when X is N, then Y is C and when X is C, then Y is N;
V is C or N;
R1 is selected from unsubstituted or substituted aryl or unsubstituted or substituted heterocycle, where the substituted group may have from 1 to 3 substituents selected from:
1) unsubstituted or substituted C1-C6 alkyl,
2) unsubstituted or substituted C3-C10 cycloalkyl,
3) unsubstituted or substituted aryl,
4) unsubstituted or substituted aralkyl,
5) CF3,
6) OR4,
7) halo,
8) CN,
9) —(CH2)tR9C(O)R4,
10) —(CH2)tOR4,
11) —(CH2)tR9C(O)NR7R4, where R4 and R7 may be taken together with the nitrogen to which they are attached to form a 5-7 membered heterocycle containing, in addition to the nitrogen, one or two additional heteroatoms selected from N, O and S, said heterocycle being optionally substituted with one to three substituents selected from R2;and
12) —C(O)R4;
R2 is selected from:
1) H,
2) halo,
3) unsubstituted or substituted C1-C6 alkyl,
4) unsubstituted or substituted aryl,
5) unsubstituted or substituted C2-C6 alkenyl,
6) unsubstituted or substituted C2-C6 alkynyl,
7) OR4,
8) CN, and
9) N(R4)2;
R3 is independently selected from:
1) H,
2) unsubstituted or substituted C1-C6 alkyl,
3) unsubstituted or substituted aryl,
4) unsubstituted or substituted heterocycle,
5) CN,
6) Halo,
7) OR4, and
8) N(R4)2;
R4 is selected from:
1) H,
2) unsubstituted or substituted C1-C6 alkyl,
3) unsubstituted or substituted aryl,
4) unsubstituted or substituted aralkyl, and
5) unsubstituted or substituted heterocycle;
R7 is selected from:
1) H,
2) unsubstituted or substituted C1-C6 alkyl,
3) unsubstituted or substituted aryl,
4) unsubstituted or substituted aralkyl, and
5) unsubstituted or substituted heterocycle;
R9 is selected from unsubstituted or substituted heterocycle;
m is 0, 1 or 2;
n is 0, 1, 2, 3, 4 or 5;
and
t is 0, 1, 2, 3, 4 or 5;
or a pharmaceutically acceptable salt, hydrate or stereoisomer thereof.

53 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/481,370Filed 19 Dec 2003
Priority: 19 Jun 2001
Published: 2 Sep 2004
Term ends: Not estimatedThe source records don’t support an estimate.

Classification11 codes

C07D 239/42
One oxygen, sulfur or nitrogen atom: one nitrogen atom
A61K 31/506
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim: not condensed and containing further heterocyclic rings
A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…
A61P 19/00
Drugs for skeletal disorders

Family

Application60/299,343Us provisional application · filed 19 Jun 2001
US 2004/0171630 A1This patent

From the US filing history. Foreign family members aren’t listed.

Timeline

Citations

Open elsewhere

patentgrep

Loading patent…

Abstract

A compound of Formula I

25
wherein
W is selected from:
26
X and Y are independently selected from C or N, provided that when X is N, then Y is C and when X is C, then Y is N;
V is C or N;
R1 is selected from unsubstituted or substituted aryl or unsubstituted or substituted heterocycle, where the substituted group may have from 1 to 3 substituents selected from:
1) unsubstituted or substituted C1-C6 alkyl,
2) unsubstituted or substituted C3-C10 cycloalkyl,
3) unsubstituted or substituted aryl,
4) unsubstituted or substituted aralkyl,
5) CF3,
6) OR4,
7) halo,
8) CN,
9) —(CH2)tR9C(O)R4,
10) —(CH2)tOR4,
11) —(CH2)tR9C(O)NR7R4, where R4 and R7 may be taken together with the nitrogen to which they are attached to form a 5-7 membered heterocycle containing, in addition to the nitrogen, one or two additional heteroatoms selected from N, O and S, said heterocycle being optionally substituted with one to three substituents selected from R2;and
12) —C(O)R4;
R2 is selected from:
1) H,
2) halo,
3) unsubstituted or substituted C1-C6 alkyl,
4) unsubstituted or substituted aryl,
5) unsubstituted or substituted C2-C6 alkenyl,
6) unsubstituted or substituted C2-C6 alkynyl,
7) OR4,
8) CN, and
9) N(R4)2;
R3 is independently selected from:
1) H,
2) unsubstituted or substituted C1-C6 alkyl,
3) unsubstituted or substituted aryl,
4) unsubstituted or substituted heterocycle,
5) CN,
6) Halo,
7) OR4, and
8) N(R4)2;
R4 is selected from:
1) H,
2) unsubstituted or substituted C1-C6 alkyl,
3) unsubstituted or substituted aryl,
4) unsubstituted or substituted aralkyl, and
5) unsubstituted or substituted heterocycle;
R7 is selected from:
1) H,
2) unsubstituted or substituted C1-C6 alkyl,
3) unsubstituted or substituted aryl,
4) unsubstituted or substituted aralkyl, and
5) unsubstituted or substituted heterocycle;
R9 is selected from unsubstituted or substituted heterocycle;
m is 0, 1 or 2;
n is 0, 1, 2, 3, 4 or 5;
and
t is 0, 1, 2, 3, 4 or 5;
or a pharmaceutically acceptable salt, hydrate or stereoisomer thereof.

53 more elements

Facts

Application

10/481,370Filed 19 Dec 2003

Priority

19 Jun 2001

Published

2 Sep 2004

Term ends

Not estimatedThe source records don’t support an estimate.

Classification11 codes

C07D 239/42
One oxygen, sulfur or nitrogen atom: one nitrogen atom
A61K 31/506
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim: not condensed and containing further heterocyclic rings
A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…
A61P 19/00
Drugs for skeletal disorders