Abbott Laboratories Corporation

University of Pittsburgh

Tap Holdings, LLC

Other

Tap Pharmaceuticals, Inc.

Tap Holding Inc.

Rolf E Swenson

Fortuna Haviv

Nicholas A Mort

Timothy D Fitzpatrick

Jonathan Greer

Charles J Nichols

Said M Sebti

Daniel W Norbeck

Andrew Stewart Tasker

Le Wang

Wang Shen

Kenneth Jay Barr

Gerard M Sullivan

David John Augeri

Andrew D Hamilton

Thomas J Sowin

Saul H Rosenberg

Stephen J O'Connor

Douglas M Kalvin

Kenneth J Henry

Jill E Hochlowski

James T Wasicak

Stephen A Fakhoury

David A Janowick

Lissa T J Nelson

Anne-Laure Marie Grillot

Gang Liu

Milan Bruncko

Bryan K Sorensen

Wesley J Dwight

Indrani W Gunawardana

Michele A Kaminski

Lisa Marie Frey

John A DeMattei

Daryl R Sauer

Bradley W Crawford

Bryan K Sorenson

Bruce G Szczepankiewicz

James I Wasick

Bernard G Donner

John J Larsen

Stephen J O'CONNOR

The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.

Attached tags for use in combinatorial chemistry synthesis

Inhibitors of protein isoprenyl transferases

Tetrahydroisoquinoline derivatives of the formula: ##STR1## or a pharmaceutically acceptable salt, ester, or prodrug thereof, having activity as an LHRH antagonist, as well as pharmaceutical compositions containing the same, and methods for their use and preparation.

Tetrahydroisoquinoline derivatives as LHRH antagonists

6-position modified decapeptide LHRH antagonists

Peptides possessing LHRH antagonistic activity, and useful for the controlling the release of LHRH in mammals are decapeptide analogues of LHRH having a lactam group at the N-terminus of the formula ##STR1## where n is 1, 2, or 3 and R.sup.1 is selected from the group consisting of hydrogen, benzyl, 4-chlorobenzyl, 2-methylnaphth-1-yl, 1-methylnaphth-2-yl, and quinolin-3-ylmethyl.

LHRH antagonists having lactam groups at the N-terminus

Decapaptide and undecapaptides substituted on the N-terminal nitrogen atom by acyl groups which include furo-2-yl, isonicotinyl, nicotinyl, 2-, 3-, and 4-quinolinecarbonyl, shikimyl, dihydroshikimyl, and tetrahydrofur-2-oyl are potent antagonists of LHRH and are useful for suppressing the levels of sex hormones in mammals.

N-terminus modified analogs of LHRH

A class of potent LHRH decapeptide antagonists possess N-alkylated aminoacyl residues where the side-chain portion of the residue is a 4-(substimtedamino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or .OMEGA.-(substitutedamino)alkyl group, and additionally the aminoacyl residues at position 5 are N-alkylated on the nitrogen atom of the peptide backbone.

LHRH antagonists having modified aminoacyl residues at positions 5 and 6

The present invention provides a process for the preparation of peptides which have or side-chains containing an alkyl- or dialkyl-substituted guanidinyl group or a imidazinylamino or tetrahydropyrimidinylamino group. The process provides higher overall yields of peptide product by permitting the synthesis of the entire peptide chain prior to modification of the side-chain to introduce the groups.

Process for producing peptides with side chains containing

Decapaptides substituted on the N-terminal nitrogen atom by acyl groups are potent antagonists of LHRH and are useful for suppressing the levels of sex hormones in mammals.

Growing community of inventors

Grayslake, IL, United States of America

Rolf E Swenson