Syntex (u.s.a.) Inc.

Other

Tsung-tee Li

Michael Marx

Colin C Beard

Gary F Cooper

Douglas L Wren

Albert R Van Horn

Joseph M Muchowski

Jurg R Pfister

Robert J Greenhouse

Jack Ackrell

Lewis J Throop

This invention relates to a process for making an enantiomer or racemic mixture of a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta.; novel intermediates useful for preparing these compounds; and processes for making the intermediates.

Processes and intermediates for making 16-phenoxy and 16-substituted

This invention relates to a process for making a compound of formula I ##STR1## in the form of a stereoisomer or mixture thereof, wherein R is hydrogen, lower alkyl; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta., or a pharmaceutically acceptable, non-toxic salt of the compound wherein R is hydrogen; novel intermediates useful for preparing these compounds; processes for making the intermediates; and a stereoisomer of the compound of formula I wherein R is methyl and X is hydrogen and a process for making same.

This invention relates to a process for making an enantiomer or racemic mixture of a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is a .alpha. the other is .beta.; novel intermediates useful for preparing these compounds; and processes for making the intermediates.

Compounds useful in treating cardiovascular disorders are the carboxylic acids depicted in formulas (1) and (2) ##STR1## as well as their pharmaceutically acceptable, non-toxic salts and esters, wherein:

[3.2.0]Bicycloheptanone oxime ethers with valuable therapeutic properties

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

(3.2.0) Bicycloheptanone oxime ethers with therapeutic properties

Novel, topically-active anti-inflammatory steroids are represented by the formula ##STR1## wherein X is fluoro, chloro or hydrogen; X.sup.1 is fluoro, chloro, bromo, or hydrogen; X.sup.2 is hydroxy or may be chloro when X.sup.1 is chloro; and X.sup.3 and X.sup.4 are independently fluoro, chloro or bromo. These steroids are prepared by formylating at the 21-position a 16.alpha.,17.beta.-isopropylidenedioxypregna-1,4,9(11)-triene-3,20-dione or the corresponding 21-fluoro compound, halogenating at the 21 position, deformylating, then reacting to add the desired components at the 9.alpha. and 11.beta. positions.

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Los Altos Hills, CA, United States of America

Tsung-tee Li