Abstract: The present invention provides novel 8-heteroaryltetrahydrobenzopyrans and analogs thereof. These novel compounds are useful as inhibitors of endoperoxide cyclooxygenase which prevents the conversion of unsaturated fatty acids to endoperoxides. Because of this pharmacological activity, these compounds represent potent platelet aggregation inhibitors.
Abstract: Phenacyl-type esters of PGF.sub.2.alpha., 15(S)-15-methyl-PGF.sub.2.alpha., and 15(R)-15-methyl-PGF.sub.2.alpha. are disclosed, represented by the formula ##STR1## wherein M is ##STR2## wherein R.sub.1 is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl; and wherein R.sub.2 is hydrogen or benzoyl. The products are useful for the same pharmacological and medical purposes as the corresponding prostaglandin and analogs, and are also useful as a means for obtaining highly purified products.
Abstract: The present invention provides novel 7-methyl-6-methylthiomethylsulfinyl-, and methylsulfonylmethylfurochromones, which are useful as antiatherosclerotic agents.
Abstract: Phenacyl-type esters of PGE.sub.2, PGE.sub.1, and 13,14-dihydro-PGE.sub.1 and their 15-methyl, 16,16-dimethyl, and 17-phenyl analogs, including the respective 15(R)epimers, are disclosed, represented by the formula ##STR1## wherein M is ##STR2## wherein R.sub.3 is hydrogen or methyl; wherein Q is ##STR3## wherein each of R.sub.4 and R.sub.5 is hydrogen or methyl, being the same or different, or ##STR4## wherein the moiety--C.sub.t H.sub.2t -- represents a valence bond or alkylene of one to 10 carbon atoms, inclusive, with one to 7 carbon atoms, inclusive, between ##STR5## and the phenyl ring; wherein R.sub.1 is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl; wherein R.sub.2 is hydrogen or benzoyl; and wherein (a) X is --CH.sub.2 CH.sub.2 -- or trans--CH.dbd.CH-- and Y is --CH.sub.2 CH.sub.2 --, or (b) X is trans--CH.dbd.CH-- and Y is cis--CH.dbd.CH--.
Abstract: This invention relates to certain structural and pharmacological analogs of prostacyclin (PGI.sub.2) wherein the C-5 to C-6 double bond is isomerized to the C-4 to C-5 position. These novel trans-4,5-didehydro-5,6-dihydro prostacyclin-type compounds are useful as smooth muscle stimulators.
Abstract: PGE-type compounds are stabilized in a composition comprising a mixture of triacetin and ethanol. This composition surprisingly and unexpectedly retains virtually all of the stability of triacetin compounds and additionally provides the superior water miscibility of ethanol.
Abstract: The present invention relates to novel amido and sulfonamido derivatives of 2-decarboxy-2-amino-methyl-PG-type compounds. These analogs are useful as nasal decongestants, antifertility agents, and as cytoprotection agents.
Abstract: 5-Oxa-17-phenyl-18,19,20-trinor-PGF.sub.1 .alpha. alkyl esters and 5-oxa-17-phenyl-18,19,20-trinor PGF.sub.1 .alpha. amide are combined with certain other prostaglandins in synergistic combinations to induce menses in female primates, preferably humans. These synergistic prostaglandin compositions have improved efficacy and safety.
Abstract: This invention provides a method for inducing menses and interrupting early pregnancy in female primate mammals, especially humans, which comprises the concomitant administration of a 5-oxa-17-phenyl-18,19,20-trinor-PGF.sub.1 .alpha., alkyl ester and an estrogenic compound. This invention further provides a pharmaceutical composition having these compounds as active ingredients. This method provides greater efficacy and safety as compared with the prior art.
Abstract: The present invention relates to certain 6-alkyl-1,2-dihydro-2-oxo-3-substituted pyridine derivatives, their preparation and antihyperglycemic use.
Abstract: The present invention provides novel substituted sulfooxy-pyrimidinium, -pyridinium, and -triazinium hydroxide inner salts. These compounds are useful for the treatment of hypertension and peripheral vascular diseases. They are formed by reacting the corresponding aminopyrimidine, aminotriazine, and aminopyridine N-oxides with a latent sulfate source such as pyridinium-sulfur trioxide complex, triethylamine-sulfur trioxide complex, chlorosulfonic acid or chlorosulfuryl chloride.
Abstract: The present invention provides novel 19,20-didehydro-PG.sub.2 compounds, methods for their preparation and pharmacological use for the induction of prostaglandin-like effect.
Abstract: The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.
Abstract: The present invention provides novel 2-decarboxy-2-hydroxymethyl-19,20-didehydro-13,14-dihydro-PG.sub.1 compounds methods for their preparation and pharmacological use for the induction of prostaglandin-like effect.
Abstract: The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic 6-halofurochromones.
Abstract: The present invention provides novel isoxazolyl derivatives prepared from 9.alpha.,11.alpha.-epoxyimino-9,11,15-trideoxy-PGF-type compounds. These novel compounds are useful as anti-inflammatory agents, anti-asthma agents, and platelet aggregation inhibitors in mammals and especially in humans.
Abstract: Phospholipase A.sub.2 inhibition the present invention relates to a method for treating or preventing a phospholipase A.sub.2 mediated condition (PMC) in a mammal suffering from or susceptible to such a condition. The method involves administering to such a mammal an amount effective to treat the condition of a compound selected from a certain group of butyrophenones.
Abstract: The compound of the formula ##STR1## wherein R' and R" are alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2 is phenyl, o-chlorophenyl, o-fluorophenyl, or 2,6-difluorophenyl, is prepared by reacting a 1-halomethyl-6-phenyl-4H-s-triazo[4,3-a][1,4]-benzodiazepine with N,N-dimethylhydroxylamine and a strong base. The compound II and its pharmacologically acceptable acid addition salts have sedative and tranquilizing activity.