Joseph I Degraw

US Patent:

60280719, Feb 22, 2000

Filed:

Mar 8, 1999

Appl. No.:

9/214984

Inventors:

Francis M. Sirotnak - New York NY
James R. Piper - Birmingham AL
Joseph I. DeGraw - Missoula MT
William T. Colwell - Menlo Park CA

Assignee:

Sloan-Kettering Institute for Cancer Research - New York NY
SRI International - Menlo Park CA
Southern Research Institute - Birmingham AL

International Classification:

A61K 31505
C07D47508

US Classification:

514249

Abstract:

Highly purified 10-propargyl-10-deazaaminopterin (10-propargyl-10dAM) compositions tested in xenograft models for their efficacy against human tumors are shown to be far superior to methotrexate ("MTX") and are even superior to the newer clinical candidate edatrexate ("EDX"). Moreover, 10-propragyl-10dAM showed a surprising ability to cure tumors such that there was no evidence of tumor growth several weeks after the cessation of therapy. Thus, highly purified compositions containing 10-propargyl-10dAM can be used to treat human tumors, particularly human mammary tumors and human lung cancer.

US Patent:

50774042, Dec 31, 1991

Filed:

Aug 29, 1989

Appl. No.:

7/399840

Inventors:

James R. Piper - Birmingham AL
John A. Montgomery - Birmingham AL
Francis M. Sirotnak - New York NY
Joseph I. DeGraw - Sunnyvale CA

International Classification:

C07D23970

US Classification:

544250

Abstract:

5,10-Dialkyl substituted 5,10-dideazaaminopterins and a cyclized derivative thereof are disclosed as potent antineoplastic agents. Also disclosed is an improved process for the preparation of 10-ethyl-10-deazaaminopterin using the intermediate methyl 4-[[2-(2,4-diamino-6-pteridinyl)-1-ethyl]ethenyl]benzoate.

US Patent:

63232057, Nov 27, 2001

Filed:

Feb 17, 2000

Appl. No.:

9/505571

Inventors:

Francis M. Sirotnak - New York NY
James R. Piper - Birmingham AL
Joseph I. DeGraw - Missoula MT
William T. Colwell - Menlo Park CA

Assignee:

Sloan-Kettering Institute for Cancer Research - New York NY
SRI International - Menlo Park CA
Southern Research Institute - Birmingham AL

International Classification:

A61K 31505

US Classification:

514249

Abstract:

Preliminary clinical studies in humans have now been done which show both the efficacy of 10-propargyl-10dAM and a preferred dosage schedule for such treatments. In addition, it has now been determined that combinations of 10-propargyl-10-deazaaminopterin (preferably highly purified forms, substantially free of 10-deazaaminopterin) with taxols exhibit synergistic effectiveness in the treatment of tumors. 10-propargyl-10-deazaaminopterin and a taxol in therapeutically effective amounts can be administered concurrently, one right after the other, or with a period of time in between.