Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents

Patent metadata

Field	Value
Publication number	US-9512125-B2
Application number	US-71972205-A
Country	US
Kind code	B2
Filing date	Nov 21, 2005
Priority date	Nov 19, 2004
Publication date	Dec 6, 2016
Grant date	Dec 6, 2016

Abstract

The present invention provides anti-inflammatory compounds useful in the treatment of diseases and conditions in which inflammation is involved in disease progression or the manifestation of symptoms of the disease or condition.

First claim

What is claimed is:

1. A compound having the formula:

wherein
R 1 is R 15 -substituted or unsubstituted fused ring heteroaryl;
R 2 , R 3 , and R 4 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted aryl, or substituted or unsubstituted heteroaryl;
R 15 is —OH, halogen, —CF 3 , —NH 2 , substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl;
and
L 1 is a bond or unsubstituted alkylene.

2. A compound according to claim 1 , wherein
R 2 is R 10 -substituted C 1 -C 20 alkyl, 2 to 20 membered substituted or unsubstituted heteroalkyl, R 11 -substituted C 3 -C 8 cycloalkyl, R 11 -substituted C 3 -C 8 heterocycloalkyl, R 12 -substituted heteroaryl, or R 13 -substituted aryl, wherein
R 10 is oxo, —OH, halogen, —CF 3 , —NH 2 , 2 to 20 membered substituted or unsubstituted heteroalkyl, 3 to 7 membered substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroaryl, or R 13 -substituted aryl,
R 11 is oxo, —OH, halogen, —CF 3 , —NH 2 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl,
R 12 is —OH, halogen, —CF 3 , —NH 2 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, and
R 13 is —OH, —NH 2 , substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted aryl.

3. The compound of claim 1 , wherein R 3 and R 4 are hydrogen.

4. The compound of claim 1 , wherein R 1 is a fused-ring heteroaryl substituted with one R 15 substituent.

5. The compound of claim 4 , wherein R 15 is —OH, halogen, —CF 3 , or —NH 2 .

6. The compound of claim 1 , wherein R 2 is substituted or unsubstituted alkyl.

Assignees

• Shokat Kevan M
• Sepetov Nikolai
• Zhang Chao
• Gschwend Heinz W
• Kunkel Eric J
• Univ California

Inventors

• Shokat Kevan M
• Sepetov Nikolai
• Zhang Chao
• Gschwend Heinz W
• Kunkel Eric J

Classifications

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P7/06

  Antianaemics · CPC title

• A61P9/04

  Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P9/14

  Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers · CPC title