Merck + Co., Inc.

Merek & Co., Inc.

David B Johnston

Burton G Christensen

Susan M Schmitt

Arthur A Patchett

Malcolm MacCoss

Lihu Yang

Ravi P Nargund

James R Tata

Ravindra N Guthikonda

William J Greenlee

Meng-Hsin Chen

Thomas F Walsh

Prasun K Chakravarty

Gary H Rasmusson

Nathan B Mantlo

John Hannah

Thomas R Beattie

Glen E Arth, Deceased

Richard L Tolman

Alexander Pasternak

Raymond A Firestone

Liangqin Guo

Kevin Tyler Chapman

Stephen Marburg

Ronald B Jobson

Meng Hsin Chen

Scott C Berk

Laura C Meurer

Donald F Reinhold

Torleif Utne

F Aileen Bouffard

Michael W Fordice

This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. Compounds of the formula: ##STR1## including pharmaceutically acceptable salts and hydrates thereof are disclosed. These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome, pain and diabetic retinopathy. Many of the compounds are also orally active.

Somatostatin agonists

There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.

Method of using spiro piperidines to promote the release of growth

Spiro piperidines and homologs promote release of growth hormone

Spiro piperidines and homologs which promote release of growth hormone

There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists. These compounds have the general formula: ##STR1##

Substituted imidazo-fused 5-membered ring heterocycles as angiotensin II

Substituted imidazo-fused 5-membered ring heterocycles and their use as

Substituted quinolines of the formula (I), are angiotensin II antagonists, ##STR1## and useful in the treatment of hypertension, ocular hypertension and certain CNS disorders.

Substituted quinolines as angiotensin II antagonists

There are disclosed certain 6-piperazinopurines and heteroaromatic derivatives thereof which have oral hypoglycemic acitivity and with such ability to lower blood sugar are useful in the treatment of type II diabetes and/or obesity with associated insulin resistance. Processes for the preparation of such compounds and compositions containing such compounds as the active ingredient thereof are also disclosed.

Piperazinyl derivatives of purines and isosteres thereof as hypoglycemic

Disclosed are 2- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R.sup.6, and R.sup.7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acyclic connecting group selected, inter alia, from alkyl, cyclalkyl, aryl, heteroaryl, heteroalkyl; R.sup.1 and R.sup.2 inter alia, independently selected from hydrogen, alkyl, aryl; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, 'carbamimidiums' are disclosed by quarternization of one of the nitrogen atoms of said carbammidoyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharamaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

2-carbamimidoyl-6-substituted-1-carbadethiapen-2-em-3-carboxylic acids

Disclosed are 2- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R.sup.6, R.sup.7 and R.sup.8 are inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

2-substituted-6-carbadethiapen-2-em-3-carboxylic acids

Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; and

2-Amino-3-cyano-5-halo-6-(substituted)pyrazine

Antimicrobial compounds of the formula: ##STR1## wherein: R is mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted lower alkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl; are useful in various agricultural and industrial areas.

2-Amino-3,5-dicyano-6-(substituted)pyrazine antimicrobial compounds

Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine;

3-Acyl-2-amino-5-halo-6-(substituted)pyrazine antimicrobial compounds

N-[2-amino-5-halo-6-(substituted)-3-pyrazinyl)-methylene]amine

2-Amino-3-carboxylate-5-halo-6-(substituted)pyrazine antimicrobial

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Warren, NJ, United States of America

David B Johnston