Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano; M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymethylene; L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine; J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine; W is selected from the group consisting of --CH.sub.2 --CH-- or trans --CH.dbd.C--; T.sub.1 and T.sub.2 are attached to adjacent carbon atoms; T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl; T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl; Or T.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 or 6 carbon atoms. Also disclosed are methods for preparing such prostaglandin analogues.
The present invention relates to novel not naturally occurring 10,11-dihydro-derivatives of prostaglandins of the A-series as well as a process for their preparation. The compounds of the invention have an antiprostaglandin effect and may be used as medicaments for the inhibition or suppression pharmacological properties of the prostaglandins.
The invention concerns novel [(4-phenyl-1,3-dioxan-cis-5-yl)alkyl]phenylalkanoic acids of the formula I wherein Ra and Rb are a variety of substituents including alkyl, alkenyl, halogenoalkyl, phenyl and benzyl, or together form polymethylene; Rc is hydroxy, alkoxy or alkanesulphonamido; A.sup.1 and A.sup.2 are polymethylene; X is oxygen, sulphur or a direct bond; and benzene ring A bears a variety of substituents; and, when Rc is hydroxy, the physiologically acceptable salts thereof. The compounds of formula I are thromboxane antagonists of value in treating a variety of disease conditions. The invention also provides processes for the manufacture of, and pharmaceutical compositions of, the compounds of formula I.
Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano; M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymethylene; L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine; J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine; W is selected from the group consisting of ##STR2## T.sub.1 and T.sub.2 are attached to adjacent carbon atoms; T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl; T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl; or T.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 or 6 carbon atoms. Also disclosed are methods for preparing such prostaglandin analogues.
Cyclohexanone-5,6-benzo analogues of prostaglandin
申请人:Miles Laboratories, Inc.
公开号:US04100352A1
公开(公告)日:1978-07-11
Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano; M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymethylene; L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine; J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine; W is selected from the group consisting of ##STR2## T.sub.1 and T.sub.2 are attached to adjacent carbon atoms; T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl; T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl; Or T.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 or 6 carbon atoms. Also disclosed are methods for preparing such prostaglandin analogues.