Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ and methods of preparing pharmaceutical compositions comprising such NHE-1 inhibitors.

Abstract: Compounds of the formula: wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.

Abstract: The present invention relates to a novel process for the preparation of a compound of formula I: wherein R1 is defined herein and compounds of formula II: wherein R1 and R2 are defined herein. Said compound of formula I is useful in the treatment of various central nervous system disorders including depression.

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: A compound of the formula wherein X, Y, Z, R2 and R3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1, agonist or antagonist is indicated.

Abstract: The present invention relates to compounds of formula I: and to their pharmaceutically acceptable salts. Compounds of formula I exhibit activity as serotonin, norepinephrine, and dopamine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.

Abstract: A composition comprising eletriptan and a p-glycoprotein (p-gp) inhibitor useful for the treatment of migraine. The bioavailability of eletriptan can be increased by co-administering eletriptan with a p-gp inhibitor. The eletriptan and p-gp inhibitor can be administered together in a composition or as separate components. If administered separately, they can be embodied as a kit. Also provided is a method of treating migraine using said composition or sequential administration of components.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: The present invention is directed to a compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, Y, U, W, k, A, E, V, R4 and R5 are as defined herein, pharmaceutical compositions thereof, and methods of use thereof in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of compounds of formula (I) and intermediates useful therefor.

Abstract: The present invention provides a method of treating or preventing a novelty-seeking disorder, such as pathological gambling, attention deficit disorder with hyperactivity disorder and sex addiction, comprising administering a compound which is a dopamine D4 receptor ligand, or a pharmaceutically acceptable salt thereof.

Abstract: A method is provided for treating or preventing a disorder or condition selected from hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress syndrome, avoidant personality disorder, premature ejaculation, eating disorders, obesity, cluster headache, migraine, pain, obsessive-compulsive disorder, panic disorder, endocrine disorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, premenstrual syndrome, fibromyalgia syndrome, stress incontinence, chronic paroxysmal hemicrania and headache in a mammal, comprising administering to a mammal in need of such treatment or prevention an amount of a compound of the formula (I) or the pharmaceutically acceptable salt thereof; wherein X, Y, Z, R2 and R3 are as defined herein.

Abstract: The present invention relates to compounds of the formula These compounds are useful as psychotherapeutic agents.

Abstract: The present invention relates to compounds of formula 1, wherein R1, R2, R3 and R4 are defined as in the specification. These compounds are useful as psychotherapeutic agents.

Abstract: The present invention relates to tetrahydroquinazoline-2,4-diones derivatives of the formula (I): pharmaceutically acceptable salts thereof, wherein A is (CH2)n where n is equal to 0, 1 or 2; U is CH2, NH, or NR3, R1 and R2 are selected independently from H, (C1-C6)alkyl, Cl, F, CN, nitro, CF3, —NHC(O)R6 and —OR7, or R1 and R2, together with the atoms to which they are attached, form a carbocyclic or heterocyclic five- or six-membered ring, R3 is selected from the group consisting of H, (C1-C6)malkyl, C(═O)—(C1-C6)alkyl, where m=1 or 2; R4 and R5 are selected from H, (C1-C6)alkyl, Cl, F, —CF3, —CN, —NHC(═O)R6, —OR7, a 5-to 7-membered aryl or heteroaryl ring, where m, R6 and R7 are as defined above; and R6 and R7 are selected independently from H, (C1-C6)alkyl or a 5- to 7-membered aryl or heteroaryl ring; V is CH, CR3, or N; W is CH2, C(O), or S(O)2; X is C or N; and Y is CH, CR1,CR2, or N.

Abstract: There is provided a compound of formula I, wherein R1, R2, R3 and R4 have meanings given in the description, which are useful in the prophylaxis and in the treatment of pruritus.

Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: The present invention relates to a method of treating migraine in a mammal, including a human, by administering to the mammal a 5HT1 receptor agonist in combination with caffeine and a cyclooxygenase-2 (COX-2) inhibitor. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5HT1 receptor agonist with caffeine and a cyclooxygenase-2 (COX-2) inhibitor.

Abstract: A compound of formula: R1 and R2 are independently C1-C4 alkyl; or R1 and R2, taken together with the carbon atom to which they are attached, form a mono-, bi-, tri- or spiro-cyclic group having 3 to 13 carbon atoms, wherein the cyclic group is optionally substituted by one to five substituents; A is (C1-C3)alkyl, phenyl, benzyl or the like; R is hydrogen, (C1-C3)alkyl, amino-(C1-C6)alkyl, heterocyclic-(C1-C3)alkyl wherein the heterocyclic is optionally substituted by amino, ((C1-C4)alkyl)-Z—(C1-C6)alkyl wherein Z is OC(═O) or the like; and X is (C1-C3)alkyl, phenyl or the like. These compounds are useful as ORL1-receptor agonists, and useful as analgesics or the like in mammalian subjects.

Abstract: Compounds of the formula where W is n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is —O—, —S—, —NH, or —CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or —Q—R4; R2 and R3 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, —COR3, —CO2R8, —CONR9R10, —OR3, —SO2NR9R10, or —S(O)4R9; R9 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three- to seven-membered alkyl ring or a three- to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 to C3 alkyl; R11 is hydrogen, —OR12, or —NHCOR12; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alk