Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturat

Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated

Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1–C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, halogen or (C1–C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, or (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturat

Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) hete

Abstract: This invention relates to new compounds selected from those of the general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof: wherein D, E and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.

Abstract: A compound of the formulae (I) or (II): 1

Abstract: The present invention provides compounds of the general formulas: 1

Abstract: N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&agr;]-pyrimidin-7-yl}phenyl)acetamide, and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Compositions containing N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&agr;]-pyrimidin-7-yl}phenyl)acetamide, as well as pharmaceutically acceptable salts thereof, are also disclosed.

Abstract: N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&agr;]-pyrimidin-7-yl}phenyl)acetamide, and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Compositions containing N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&agr;]-pyrimidin-7-yl}phenyl)acetamide, as well as pharmaceutically acceptable salts thereof, are also disclosed.

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: Disclosed are 3-substituted-7-[3-(imidazol-1-yl)phenyl]-pyrazolo[1,5-a]pyrimidines of the formula: ##STR1## wherein R.sup.1, R.sup.3 and R.sup.4 are defined in the specification which compounds have anxiolytic, anti-convulsant, sedative-hypnotic and skeletal muscle relaxant activity.

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: Novel N-((dialkylamino)methylene)-substituted-pyrazolo(1,5-a)pyrimidine-3-carbox amide and N-((dialkylamino)methylene)-substituted-4,5-dihydropyrazolo-(1,5-a)-pyrimi dine-3-carboxamide compounds are disclosed which are useful as neurotropic and/or anxiolytic and/or anti-hypertensive agents in mammals.

Abstract: A novel process for producing .alpha.-[(dialkylamino)substituted-methylene].beta.-oxo-(substituted) propanenitriles of the formula: ##STR1## where R, R.sub.1 and R.sub.2 are defined in the specification by reacting a substituted isoxazole with a diaklyamide dimethylacetal is provided.

Abstract: Novel N-((dialkylamino)methylene)-substituted- pyrazolo(1,5-a)pyrimidine-3-carboxamide and N-((dialkylamino) )methylene-substituted-4,5-dihydropyrazolo-(1,5-a)-pyrimidine-3-carboxamid e compounds are disclosed which are useful as neurotropic and/or anxiolytic and/or anti-hypertensive agents in mammals.

Abstract: A novel process for producing .alpha.-[(dialkylamino) substituted-methylene].beta.-oxo-(substituted) propanenitriles of the formula: ##STR1## where R, R.sub.1 and R .sub.2 are defined in the specification by reacting a substituted isoxazole with a diaklylamide dimethylacetal is provided.