Abstract: Compounds of the formula ##STR1## wherein m is the integer 1, 2 or 3; R is independently selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, halo, trifluoromethyl and hydroxy when m is the integer 1, 2 or 3 and methylenedioxy when m is the integer 2; Z is hydroxymethylene, esterified hydroxymethylene, alkoxymethylene, alkylthiomethylene, carbonyl, or ketal-, thioketal- or hemithioketal-protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsants, anti-secretory agents and spermatocides.
Abstract: Psoriasis in mammals is relieved by topically administering substituted naphthoquinone of the formula: ##STR1## wherein: R.sup.3 is halo, linear or branched alkoxy of one to eighteen carbon atoms or --S(O).sub.n R wherein:n is 0, 1 or 2; andR is a alkyl of one to eighteen carbon atoms, alkoxycarbonylalkyl, optionally substituted phenyl, optionally substituted phenylalkyl or optionally substituted heterocyclic aryl and the pharmaceutically acceptable salts of said heterocyclic aryl.
Abstract: Racemic mixtures of d,1-2-(6-methoxy-2-naphthyl)propanal are resolved by forming a condensation product with N-R-D-glucamine or a salt thereof where R is hydrogen, alkyl of 1 to 36 carbon atoms or cycloalkyl of 3 to 8 carbon atoms, from which a product substantially enriched in d-2-(6-methoxy-2-naphthyl)propanal can be obtained and then can be selectively oxidized to d-2-(6-methoxy-2-naphthyl)propionic acid.
Abstract: Compounds useful as antifungal, antibacterial and antiprotozoal agents are represented by the formula: ##STR1## wherein: Z is oxygen or sulfur;R.sup.1 is phenyl optionally substituted with one or more substituents selected from the group consisting of halo, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms and trifluoromethyl;R.sup.2 is phenyl or benzyl wherein the phenyl ring of R.sup.2 is optionally substituted by one or more substituents selected from the group consisting of halo, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms and trifluoromethyl; or by a phenyl optionally substituted by halo, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms or trifluoromethyl; andthe antimicrobial acid addition salts thereof.
Abstract: A gel formulation, which is inherently spermicidal and which provides an efficient delivery system for spermicidal and other contraceptively effective compounds intravaginally is disclosed. Said formulation is useful in methods of intravaginal contraception.
Type:
Grant
Filed:
May 7, 1981
Date of Patent:
January 11, 1983
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Brian H. Vickery, Shabbir Anik, Richard E. Jones
Abstract: Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula: ##STR1## wherein:R.sup.1 is ##STR2##R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen or lower alkyl of one to four carbon atoms;X is hydrogen, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms or halo;m is 1 or 2; andn is 1, 2 or 3; andthe pharmaceutically acceptable acid addition salts thereof.
Abstract: Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula ##STR1## wherein: R.sup.1 is ##STR2## wherein X is hydrogen, lower alkyl, lower alkoxy, halo, carboxamido or hydroxy; m is 1, 2 or 3; and n is 1, 2 or 3;R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl; andthe pharmaceutically acceptable acid addition salts thereof.
Abstract: Novel compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo;R is hydrogen or lower alkyl; andA is selected from the group consisting of:2-(benzodioxan-2-yl)-2-hydroxyethyl;.omega.-(benzodioxan-2-yl)-alkyl (1-4);3-(aryloxy)-2-hydroxypropyl, wherein aryloxy is phenyloxy optionally substituted by 1-3 moieties selected from the group consisting of lower alkyl, lower alkoxy, halo, alkylsulfamido, lower alkoxycarbonyl, cyano and trifluoromethyl;.omega.-arylalkyl (1-4), wherein aryl is phenyl optionally substituted by 1-3 moieties selected from the group consisting of lower alkyl, lower alkoxy, halo, alkylsulfamido, lower alkoxycarbonyl, cyano and trifluoromethyl;.omega.-aryl-.omega.-oxoalkyl (1-4), wherein aryl is as herein defined;.omega.-aryl-.omega.-hydroxyalkyl (1-4), wherein aryl is as herein defined; and.omega.
Type:
Grant
Filed:
May 18, 1981
Date of Patent:
September 14, 1982
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Adolph P. Roszkowski, Robin D. Clark, Arthur F. Kluge
Abstract: Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula ##STR1## wherein: R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen or lower alkyl of one to four carbon atoms; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl of one to four carbon atoms or lower alkoxy of one to four carbon atoms; andthe pharmaceutically acceptable acid addition salts thereof.
Abstract: Compounds useful as anticonvulsant agents, antifungals and antibacterials are represented by the formula ##STR1## wherein R.sup.1 is phenyl optionally substituted by one or more substituents selected from the group consisting of halo, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms and trifluoromethyl; Z is ethylene or propylene optionally substituted by one or more lower alkyl groups of one to four carbon atoms; m is 1, 2, 3 or 4 and n is 0, 1, 2 or 3 with the proviso that the sum of m and n is 2, 3 or 4; and the pharmaceutically acceptable acid addition salts thereof.The ketone intermediates useful in preparing compounds of formula (I) also have anticonvulsant activity.
Abstract: Compounds of the formula ##STR1## wherein Z is C.sub.1 and C.sub.4 alkoxymethylene, hydroxymethylene, esterified hydroxymethylene, carbonyl, or ketal-protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsant and anti-secretory agents.
Abstract: Compounds of the formula ##STR1## wherein m is the integer 1, 2 or 3; R is independently selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, halo, trifluoromethyl and hydroxy when m is the integer 1, 2 or 3 and methylenedioxy when m is the integer 2; Z is hydroxymethylene, esterified hydroxymethylene, alkoxymethylene, alkylthiomethylene, carbonyl, or ketal-, thioketal- or hemithioketal- protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsants, anti-secretory agents and spermatocides.
Abstract: The compounds of the present invention are represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are optionally substituted furyl or thienyl the substituents independently selected from the group halo, C.sub.1 to C.sub.6 alkyl and C.sub.1 to C.sub.6 alkoxy or optionally substituted phenyl the substituents independently selected from the group halo, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy and trifluoromethyl; X is oxygen or sulfur; m is the integer 0; and n is the integer 2 or 3; and the antimicrobial acid addition salts thereof, with the proviso that when either R.sup.1 or R.sup.2 is said optionally substituted phenyl the other R.sup.1 or R.sup.2 is said optionally substituted furyl or thienyl.The compounds are useful for combatting fungi, bacteria and protozoa. They also have spermatocidal and spermatostatic activity.