E. R. Squibb Sons, Inc.

Bristol-myers Squibb Compnay

Koster, William H.

Ermann, Peter H.

Sundeen, Joseph E.

Treuner, Uwe D.

Straub, Henner

Joseph E Sundeen

Frederic P Hauck

Bang-Chi Chen

Tamara Dejneka

Christopher M Cimarusti

Joyce Reid

Rulin Zhao

Rudiger D Haugwitz

Robert Zahler

Kyoung S Kim

Raj N Misra

William H Koster

Venkatachala L Narayanan

S David Kimball

Peter H Ermann

Uwe D Treuner

Mark E Salvati

Sailesh A Varia

Henner Straub

Kent Amsberry

Michael Fakes

Hai-Yun Xiao

Frederick Peter Hauck

Stefan Jendrzejewski

Katerina Leftheris

Sundeep Dugar

Karnail S Atwal

Saleem Ahmad

Stephen T Wrobleski

John T Hynes

Peter W Sprague

Shung C Wu

David M Floyd

Jeffrey T North

Annie J Pullockaran

Peng Guo

Hai-Yun Xia

Ving G Lee

An improved process for the preparation of certain pyrrolotriazine compounds is disclosed. The compounds exhibit utility as kinase inhibitors.

Process for preparing pyrrolotriazine kinase inhibitors

The present invention relates to new, efficient processes for the preparation of 5-(-2-oxyazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula Ior a pharmaceutically acceptable salt thereof, wherein:

Process for preparing azacycloalkanoylaminothiazoles (LD 137e)

Process for preparing azacycloalkanoylaminothiazoles

Process for preparing arylacetylaminothiazoles

The present invention provides an improved process for the preparation of N-(substituted phenyl)-3-alkyl-, aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds of formula I that exhibit antiandrogenic activity and are useful in the treatment of malignant or benign prostatic disease or of androgen dependent disease conditions such as acne, hirsutism or seborrhea.

Process for the preparation of N-(substituted phenyl)-3-alkyl-,aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds

A process is provided for preparing chiral cyclopropane carboxylic acids, preferably of the structure ##STR1## which are intermediates used in preparing acyl guanidine sodium/proton exchange (NHE) inhibitors.

Process for preparing chiral cyclopropane carboxylic acids and acyl

A novel process for the production of tertiary amines by reductive alkylation of second amine using hydrosilane and a Lewis acid is disclosed. The novel process has applications in the preparation of imidazole-containing benzodiazepines, inhibitors of farnesyl protein transferase.

Reductive alkylation of secondary amines with hydrosilane

Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring.

Hereroaryl derivatives of monocyclic beta-lactam antibiotics

Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring. Also described are various intermediates for the preparation of compounds of formula 1.

Intermediates for the preparation of heteroaryl derivatives of

Heteroaryl derivatives of monocyclic beta-lactam antibiotics

The compound [3S(Z)]-3-[[(2-amino-4-thiazolyl)[[2-(hydroxyamino)-2-oxoethoxy]imino]acet yl]amino]-2,2-dimethyl-4-oxo-1-azetidinyl sulfate has gram-positive and gram-negative activity and good oral absorption.

[3S(Z)]-3-[[(2-amino-4-

Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen or alkyl or R.sub.3 and R.sub.4 taken together with the nitrogen atoms to which they are attached form a 1,2-diazacyclobutane, 1,2-diazacyclopentane, 1,2-diazacyclohexane, or 1,2-diazacycloheptane ring and Y, and Y.sub.2 are either hydrogen or hydroxy but are not the same; are useful chemical intermediates for the preparation of .beta.-lactam antibiotics.

Monobactam hydrazides containing catechol sulfonic acid groups

Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof and possessing antibacterial activiy, and intermediates to compounds of formula I having the formula ##STR2##

6,7-dihydroxyquinoxalines as intermediates to beta-lactam antibiotics

Growing community of inventors

Yardley, PA, United States of America

Joseph E Sundeen