Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

Abstract: The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine .beta.-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-4-yl and 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.

Abstract: Nucleosides compounds of Formula I: ##STR1## wherein B is a purine or a pyrimidine;X and X' are H;Y is H;Y' is OH, F or H;or Y' and X' together makes a bond;Z is ##STR2## where n is zero, one, two or three; or Y' and Z together form a cyclic phosphate ester; Z' is --CN, --CH.sub.3, CH.sub.2 N.sub.3 or --CH.sub.2 J,where J is a halogen atom;or Z' and Y' together are --CH.sub.2 O--; and pharmaceutically acceptable esters, ethers, amides, N-acyl moieties and salts thereof.

Abstract: Compounds useful in treating or preventing gastrointestinal ulcers and in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): ##STR1## wherein: A is --C.tbd.C--, trans --HC.dbd.CH--, trans --CH.dbd.CHCH.sub.2 -- or --CH.sub.2 CH.sub.2 --;X is lower alkyl of 1-6 carbon atoms;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);n is an integer from 2-4;R.sub.1 is --CH.sub.2 OH, --CHO, --CO.sub.2 R or --CO.sub.2 H, and the olefin formed by the R.sub.1 (CH.sub.2).sub.n CH.dbd. moiety is either (E) or (Z);R.sub.2 is hydrogen or methyl, or optionally --CH.dbd.CH.sub.2 when A is trans --CH.dbd.CHCH.sub.2 --; andR.sub.3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, ##STR2## --(CH.sub.2).sub.m -phenyl or CH.sub.2 O-phenyl; in which each phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen.

Abstract: A process for preparing compounds represented by the formula ##STR1## wherein: X is hydrogen or lower alkoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);n is an integer from 2-4;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl, ##STR2## --(CH.sub.2).sub.m -phenyl or --CH.sub.2 O-phenyl; in which any phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, anda is an integer of 0, 1 or 2;b is an integer of 3-7;m is an integer of 0, 1 or 2,as a mixture or separately in a sequence starting from an epoxide represented by the formula ##STR3## and processes for making the novel intermediates.

Abstract: The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.

Abstract: The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.

Abstract: New compounds of the formula ##STR1## wherein: R.sup.1 is cycloalkyl of five to seven carbon atoms optionally substituted with one or more lower alkyl groups;R.sup.2 is alkyl of two to twelve carbon atoms, cycloalkyl of five to seven carbon atoms, or cycloalkylalkyl of six to ten carbon atoms wherein the cycloalkyl group may be optionally substituted with one or more lower alkyl groups;R.sup.3 is hydrogen or lower alkyl;a is 0, 1, 2 or 3; andb is 1, 2 or 3;and the pharmaceutically acceptable acid addition salts thereof are useful as spermicidal and spermatostatic agents.

Abstract: A compound useful as antifungal, antibacterial and antiprotozoal agents and as spermicides have the formula ##STR1## and the acid addition salts thereof wherein Z is oxygen or sulfur;m is 0, 1, 2 or 3;n is 1, 2 or 3;R.sup.1 is hydrogen; alkyl; cycloalkyl; cycloalkyl-lower-alkyl; optionally substituted phenyl; phenyl-lower-alkyl; monocyclic heteroaromatic ring; monocyclic heteroaromatic-lower-alkyl; naphthyl; or naphthyl-lower-alkyl.A and B are independently hydrogen, halo, lower alkyl or lower alkoxy and either one of A or B may be nitro, amino or alkanoylamino;Q is (a) NR.sup.2 R.sup.3 or (b) NR.sup.4 C(X)YR.sup.5 whereinX is oxygen or sulfur;Y is oxygen, sulfur, NR.sup.6 or a bond;R.sup.2 is hydrogen; alkyl; cycloalkyl; cycloalkyl-lower-alkyl; optionally substituted phenyl or optionally substituted phenyl-lower-alkyl;R.sup.3 is hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together with N is a five or six membered optionally substituted ring;R.sup.4 and R.sup.6 are independently hydrogen or lower alkyl;R.

Abstract: Compounds of the formula: ##STR1## wherein R is alkyl of 1 to 12 carbon atoms, cyclopentyl, cyclohexyl, cyclopentylloweralkyl or cyclohexylloweralkyl;Z is ethylene or propylene, optionally substituted with a single substituent which is lower alkyl;A is the integer 1, 2, or 3; andthe pharmaceutically acceptable acid addition salts thereof, said compounds being useful as spermicidal, antimicrobial and anticonvulsant agents and thromboxane synthetase inhibitors.

Abstract: 1-Substituted imidazole derivatives exhibit spermatostatic and spermatocidal activity and are useful for contraceptive purposes both in male and female mammals.

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: 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: Compounds of the formula: ##STR1## wherein R.sub.1 is phenyl optionally substituted with one or more substituents independently selected from the group consisting of lower alkyl, lower alkoxy, halo, or trifluoromethyl;Z is ethylene or propylene, optionally substituted with a single substituent which is lower alkyl;A is the integer 0, 1, 2, or 3;B is the integer 1, 2, or 3; andwherein the sum of A and B is 1, 2, 3 or 4; andthe pharmaceutically acceptable acid addition salts thereof, said compounds being useful as spermicidal, antimicrobial and anticonvulsant agents.

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.

Abstract: 1-Substituted imidazole derivatives exhibit spermatostatic and spermatocidal activity and are useful for contraceptive purposes both in male and female mammals.