Denis R Patrick

US Patent:

59944129, Nov 30, 1999

Filed:

Jul 2, 1998

Appl. No.:

9/110006

Inventors:

Seok H. Lee - Seoul, KR
Maria T. Diez - Madrid, ES
Fernando Pelaez - Madrid, ES
Marina Mojena Sanchez - Madrid, ES
M. Dolores Vilella Amils - Madrid, ES
Hans E. Huber - Lansdale PA
Denis R. Patrick - Chalfont PA
Otto D. Hensens - Red Bank NJ
Rosalind G. Jenkins - Somerset NJ
Leeyuan Huang - Watchung NJ
Annie Z. Zhao - Edison NJ
Deborah L. Zink - Manalapan NJ
Anne Dombrowski - East Brunswick NJ
Gerald F. Bills - Clark NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A01N 3114

US Classification:

514721

Abstract:

A compound represented by the formula I is disclosed: ##STR1## or a pharmaceutically acceptable salt or hydrate thereof. The compound has inhibitory activity against the oncoprotein Raf. Also included are pharmaceutical compositions, methods of treating cancer, cultures of the producing fungal microorganism and methods of fermentative production of the compound.

US Patent:

61034878, Aug 15, 2000

Filed:

Aug 26, 1998

Appl. No.:

9/140557

Inventors:

Stanley F. Barnett - North Wales PA
David C. Heimbrook - Fleetwood PA
Hans E. Huber - Lansdale PA
Denis R. Patrick - Chalfont PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C12Q 148

US Classification:

435 15

Abstract:

The instant invention provides for a method of inhibiting prenyl-protein transferases and treating cancer which comprises administering to a mammal a prenyl-protein transferase inhibitor which is efficacious in vivo as an inhibitor of geranylgeranyl-protein transferase type I (GGTase-I). The invention also provides for a method of inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I by administering a compound that is a dual inhibitor of both of those prenyl-protein transferases. The invention also provides for a method of identifying such a compound, the method comprising a modified inhibitory assay that incorporates a modulator anion that alters the in vitro potency of prenyl-protein transferase inhibitors in a way that predicts their potency in vivo, thus providing convenient identification of compounds that possess such in vivo activity.