Syntex (u.s.a.) Inc.

Other

Jack Ackrell

Joseph M Muchowski

Jurg R Pfister

Robert J Greenhouse

Anthony Prince

Tsung-tee Li

Tsung-Tee Li

Otto Halpern

A compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof are potent antihypertensive agents and are therefore useful as cardiovascular system regulators. These compounds are also useful as bronchodilators.

+2-[(3,4-Methylenedioxy)phenethyl]-5-[(3-carboxamido-4-hy

Compounds of the formula ##STR1## and the pharmaceutically acceptable, nontoxic, acid addition salts thereof, wherein

Hypotensive benzoxathiole pyrrolidines

A compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof are potent antihypertensive agents and are therefore useful as cardiovascular system regulators.

.+-.2-[Phenethyl]-5-[(3,4-methylenedioxy)-.alpha.-hydroxybenzyl]py

This invention relates to novel 4-(8X-6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-yl)-4-oxobutyric acids and their derivatives, wherein X is hydrogen, methoxy or chloro, methods of preparation, compositions and uses thereof.

Novel 4-(8X-6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-yl)-4-oxobutyric

Novel dibenzo[b.f]thiepin and oxepin compounds of the formula and the pharmaceutically acceptable esters and salts thereof, wherein R is hydrogen or methyl; X is oxygen or S(O).sub.n in which n is the integer 0, 1 or 2 and Z is a single or double bond, provided that when Z is a double bond X is not SO, and when R is methyl the compounds are (dl) mixtures, and methods for the production thereof.

Dibenzo [b.f]thiepin and dibenzo[b.f]oxepin derivatives

The novel compounds 6,11-dihydrodibenzo[b.e.]-thiepin-11-one-3-acetaldehyde and (dl) 2(6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-yl)propionaldehyde, certain dialkyl- and cyclic acetals thereof, and processes and novel intermediates for making same.

6,11-Dihydrodibenzo-[b. e.]-thiepin-11-one-3-aldehyde and 3-acetal

Esters of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-ones of the formula: ##STR1## wherein R is hydrogen or methyl and R.sup.1 is --CH.sub.2 --CH(OH)--CH.sub.2 OH, ##STR2## where Y is either O or S, or ##STR3## where R.sup.2 and R.sup.3 are independently hydrogen, alkyl having 1 to 6 carbon atoms, phenyl or benzyl or together R.sup.2 and R.sup.3 form an alkylene bridge having 4, 5 or 6 carbon atoms, and processes for the production thereof.

Novel esters of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-alkanoic

Novel thioesters of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid, (dl) 2-(6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-yl)propionic acid and the individual (d) isomers of the latter, and processes for making the same.

6,11-Dihydrodibenzo-[b.e.]-thiepin-11-one-3-thioacetates

6,11-Dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid is prepared from 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetonitrile, a novel intermediate, by strong acid or base hydrolysis.

6,11-Dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetonitrile

This invention relates to a novel method for the preparation of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid and the novel intermediate 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-carboxaldehyde used in the preparation thereof.

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Palo Alto, CA, United States of America

Jack Ackrell