Ayerst, Mckenna & Harrison, Inc.

American Home Products Corporation

Jehan F Bagli

Tibor Bogri

Nedumparambil A Abraham

Bozidar Palameta

Eckhardt Ferdinandi

Katherine Voith

Wilbur Lippmann

Sumanas Rakhit

Francesco Bellini

Adi Treasurywala

Luis E Borella

Disclosed herein are antisecretory agents represented by the formula ##STR1## wherein R.sup.1 is hydrogen and R.sup.2 is lower alkylthio, (2-thienylmethyl)thio or SCH.sub.2 -- COOR.sup.5 wherein R.sup.5 is hydrogen or lower alkyl, or R.sup.1 and R.sup.2 are independently a lower alkylthio or (2-thienylmethyl)thio, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a 2-imidazolidinylidene; and R.sup.3 and R.sup.4 are each the same lower alkyl, or R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached form a cyclohexane wherein said carbon atom is a spiro atom in common with the cyclohexane ring and the adjoining dioxane ring.

Antisecretory agents derived from meldrum's acid

.alpha.-Cyanoacrylic acid lower alkyl esters, and their corresponding amides, characterized by having a heterocyclic containing mercapto radical as one .beta.-substituent and an alkylthio, alkenylthio or a heterocyclic containing mercapto radical as another .beta.-substituent are useful for treating ulcers and for suppressing gastric acid secretion.

Pyridinyl substituted ketenemercaptal derivatives

Herein is disclosed a method of using 6-amino-5-pyrimidinecarbonitrile derivatives, therapeutically acceptable addition salts thereof, for increasing cardiac contractility in a mammal.

Use of 6-amino-5-pyrimidinecarbonitrile derivatives as cardiotonic agents

Herein is disclosed amino-pyrimidine derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for increasing cardiac contractility in a mammal.

Amino-pyrimidine derivatives, compositions and use

2-(1-Piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.

2-(1-Piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives

2-(4-Hydroxyalkyl-1-piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.

2-(4-Hydroxyalkyl-1-piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives

2-(4-Substituted alkyl-1-piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.

2-(4-Substituted alkyl-1-piperazinyl)-2,4,6-cycloheptatrien-1-one

Aldose reductase inhibitors of the formula ##STR1## in which R.sup.1 is CH.sub.2 COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl; R.sup.2 is COOR.sup.5 wherein R.sup.5 is hydrogen or lower alkyl; and R.sup.3 is lower alkoxy, benzyloxy or CH.sub.2 COOR.sup.6 wherein R.sup.6 is hydrogen or lower alkyl; with the provisos that when R.sup.4 is hydrogen then R.sup.5 and R.sup.6 is hydrogen; and that when R.sup.4 is lower alkyl then R.sup.5 and R.sup.6 are lower alkyl with R.sup.4 and R.sup.6 being the same lower alkyl; are useful for treating diabetic complications.

4,7-Dihydro-4,7-dioxi-1H-cyclohepta[b]pyridine derivatives

Aldose reductase inhibitors of the formula ##STR1## in which R.sup.1 is COOH and R.sup.2 is hydrogen, 8-halo or 6-hydroxy, or R.sup.1 is CON(R.sup.3)-CH.sub.2 COOH wherein R.sup.3 is lower alkyl and R.sup.2 is hydrogen or 8-halo are useful for treating diabetic complications.

4,9-Dihydro-4,9-dioxo-1H-cyclohepta[b]pyridine derivatives

2-(1-Piperazinyl)-cycloheptimidazole derivatives are disclosed. The foregoing compounds are useful antihypertensive agents.

2(1-Piperazinyl)-cycloheptimidazole antihypertensive composition and

Herein is disclosed 2-(1-piperazinyl)-4-pyrimidinamine derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are distinguished most readily by having novel substituents at position 4 of the piperazinyl radical, the substituents being selected from the group consisting of 2-thiazoylyl, oxazolo(4,5-b)pyridin-2-yl and optionally substituted 1-(lower alkyl)-1H-benzimidazol-2-yl. The derivatives are useful for treating hypertension in a mammal.

2-(Piperazinyl)-4-pyrimidinamines

Disclosed herein are 1,2-dihydro-2-oxo(or 2-thioxo)cyclohepta[b]-pyrrole-1-acetic acid derivatives having optional substitution at positions 3, on the cycloheptatriene ring and on the acetic acid side chain. The compounds are aldose reductase inhibitors and thus are useful for treating diabetic complications.

Cyclohepta[b]pyrrole derivatives

Herein is disclosed 2-(1-piperazinyl)-4-pyrimidinamine derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are distinguished most readily by having novel substituents at position 4 of the piperazinyl radical, the substituents being selected from the group consisting of optionally substituted 2-cycloheptimidazolyl, 1,4,5,6,7,8-hexahydrocycloheptimidazol-2-yl, 2-benzoxazolyl, benzthiazol-2-yl, 1H-2-benzimidazolyl and 1-oxo-2,4,6-cycloheptarien-2-yl. The derivatives are useful for treating hypertension in a mammal.

2-(Piperazinyl)-4-pyrimioinamines

2-(1-Piperazinyl)-cycloheptimidazole derivatives

Tropone derivatives characterized by having a derivative of oxamic acid at positions 2 and or 5 are disclosed. In addition, the tropone nucleus can be optionally further substituted. The foregoing compounds are useful for preventing or treating allergic conditions in a mammal. Methods for the preparation and use of said compounds are disclosed.

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Kirkland, Canada

Jehan F Bagli