4-aminopyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors

• US 5,639,757 A
• Filed: 05/23/1995
• Issued: 06/17/1997
• Est. Priority Date: 05/23/1995
• Status: Expired due to Fees

• Current Assignee: Pfizer Inc.
• Original Assignee: Pfizer Inc.
• Inventors: Koch, Kevin, Dow, Robert L.
• Primary Examiner(s): KRASS, FREDERICK F
• Application Number:
  US08/448,248
• Time in Patent Office: 756 Days
• Field of Search: 514/261, 514/258, 514/260, 514/259
• US Class Current: 514/265.1
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings

Abstract

Certain 4-aminopyrrolo[2,3-d]pyrimidine compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and are useful for immunoregulation and for the treatment of cancer, angiogenesis and atherosclerosis.

Claims

1. A method of treating tyrosine kinase dependent diseases which comprises administering to a mammal suffering from cancer, atherosclerosis, angiogenesis, graft rejection, rheumatoid arthritis or psoriasis a cancer, atherosclerosis, angiogenesis, graft rejection, rheumatoid arthritis or psoriasis treating amount of a tyrosine kinase inhibitor compound of Formula I:

##STR2## or a pharmaceutically-acceptable anionic salt thereof wherein R₁ and R₂ are each independently H, halo, alkyl (C₁ -C₄), or alkyloxy (C₁ -C₄) and inhibiting cancer, atherosclerosis, angiogenesis, graft rejection, rheumatoid arthritis or psoriasis dependent tyrosine kinases.

2. The method as recited in claim 1 wherein R₁ and R₂ are each independently H, halo, alkyl (C₁ -C₄), or alkyloxy (C₁ -C₄) and the tyrosine kinase is pp60src.

3. The method as recited in claim 1 where R₁ and R₂ are each in the para position.

4. The method as recited in claim 2 wherein R₁ and R₂ are each in the para position.

5. The method as recited in claim 2 wherein the amount is from about 0.1% to 20 mg/kg of body weight daily.

6. The method as recited in claim 5 wherein the tyrosine kinase dependent disease/ is graft rejection, atherosclerosis, angiogenesis or psoriasis.

7. The method as recited in claim 5 wherein the tyrosine kinase dependent disease is cancer or rheumatoid arthritis.