Parke-davis Company

Warner-lambert Company

Warner Lambert LLC

Alfred Campbell

Francis John Tinney

Ernest D Nicolaides

John C Hodges

Gary Louis Bolton

Daniele Marie Leonard

Donald John Hupe

Eugene Leroy Wittle

Tomi Sawyer

Mildred Catherine Rebstock

Judith Sebolt-Leopold

Richard Gowan

Inhibitors of protein:farnesyl transferase enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue proliferative diseases, including cancer and restenosis.

Substituted tetra- and pentapeptide inhibitors of protein: farnesyl

New octapeptides having the formula Prot Grp-R-Trp-Ser-Tyr-R.sub.2 -Leu-Arg-Pro-R.sub.3 ; salts thereof; wherein R is Gln, Gln (bzl), His (bzl), Ser (bzl), Pro, Leu, Tyr (bzl), Ile, Cys (bzl) or Phe, R.sub.2 is D-Phe, D-Ala, D-Leu, D-Trp, D-Tyr, D-Tyr (Me), D-Ser, D-Met, D-Arg, D-Val, D-His, D-Gln, D-Phs, D-Thr, D-Pro, D-Me.sub.5 Phe or D-Asn and R.sub.3 is NH.sub.2, NH(lower alkyl), N-(lower alkyl).sub.2, NH-benzyl, NHCH.sub.2 CH.sub.2 N-(lower alkyl).sub.2 or NH-CH.sub.2 CH.sub.2 SO.sub.2 NH-benzyl; methods for their production; certain peptide intermediates and their salts used in the production thereof; and the use of said octapeptides as luteinizing hormone releasing factor antagonists.

Octapeptides and methods for their production

New nonapeptides having the formula R-Gln-Trp-Ser-Tyr-Trp-Pro-Pro-Tyr(benzyl)-Ser(benzyl)-Y wherein R is a protective group and Y is amino, lower alkylamino or di(lower alkyl)amino.

Nonapeptides and methods for their production

New pentapeptides having the formula X-R-Tyr-(benzyl)-Ser(benzyl)-R.sup.1 -Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl, R is a single amino acid fragment, a dipeptide fragment or tripeptide fragment utilizing amino acids selected from the group consisting of Pro, Aze, His-(benzyl) and Trp; R.sup.1 is a single bond or a single amino acid fragment or a dipeptide fragment utilizing amino acids selected from the group consisting of Ala, Trp and His and Y is lower alkoxy, hydrazino, amino, lower alkylamino or di(lower alkyl)amino with the proviso that the total number of amino acid units when R and R.sup.1 are combined is three.

New pentapeptides and methods for their production

New tetrapeptides having the formula A-Pro-Pro-Tyr(benzyl)-Ser(benzyl)-R.sub.1 wherein A is t-butoxycarbonyl, cyclohexylcarbonyl, benzyloxycarbonyl and p-nitrobenzyloxycarbonyl; Pro is D-Pro or L-Pro; Tyr(benzyl) is D-Tyr(benzyl) or L-Tyr(benzyl); Ser(benzyl) is D-Ser(benzyl) or L-Ser(benzyl) and R.sub.1 is lower alkoxy, hydrazino, amino, lower alkylamino or di(lower alkyl)amino.

Tetrapeptides

New tripeptides having the formula A-R.sub.1 -Tyr(benzyl)-Ser(benzyl)-R.sub.2 wherein A is t-butoxycarbonyl or cyclohexylcarbonyl, R.sub.1 is Trp, His(benzyl), Cys(benzyl) or Pro and R.sub.2 is lower alkoxy, hydrazino, amino, lower alkylamino, di(lower alkyl)amino, benzylamino, allylamino, (diethoxyphosphinyl)methylamino, 2-(diethoxyphosphinyl)ethylamino or 2-[[(phenylmethyl)amino]sulfonyl]ethylamino, methods for their production, and the use of said tripeptides as luteinizing hormone releasing factor antagonists.

Growing community of inventors

Ann Arbor, MI, United States of America

Alfred Campbell