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: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.

Abstract: Compounds of formula (I) wherein the substituents are as defined herein, are antiparasitic agents.

Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-4 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted; R4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent,  or represents a cyclic group of formula Ia,  or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.

Abstract: The invention described herein relates to the use of calcium channel blockers such as amlodipine in the treatment of renal disease in normotensive animals. Also described are new unit doses of amlodipine suitable for the treatment of renal disease in normotensive cats.

Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.

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: The invention relates to crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxy butanedioate salts having the formula shown below: 1

Abstract: The invention provides a method for treating certain neurologic and psychiatric disorders in mammals, including humans, comprising administration of a selective PDE10 inhbitor. In particular, the invention relates to treatment of mood, movement, and anxiety disorders; psychosis; drug, for example alcohol, addiction; disorders having as a symptom deficient cognition; and neurodegenerative disorders and conditions. The invention furthermore provides the use of papaverine as a selective inhibitor of PDE10. The invention also provides assays for identifying chemical compounds that have activity as selective PDE10 inhibitors.

Abstract: Sustained release dosage forms of sertraline which release sertraline at a rate between 1 mgA/hr and 40 mgA/hr. The dosage forms may exhibit an initial delay period during which sertraline is released at a rate less than 1 mgA/hr.

Abstract: The invention relates to compounds of Formula 1 and to pharmaceutically acceptable salts, solvates, and prodrugs thereof, wherein X, Y, Z, R1, R2, R3, R4, and R5 are defined herein. The invention further relates to methods of making compounds of Formula 1 and to pharmaceutical compositions comprising compounds of Formula 1. The invention is also related to methods of treating diseases and disorders such as, but not limited to, bacterial and protozoal infections which comprise the administration of a compound of Formula 1, or a pharmaceutically acceptable salt, solvate, or prodrug thereof.

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: A process for preparing a compound of the formula wherein n, R1, R2, R3 and X are as defined above, used as an intermediate in the synthesis of &bgr;-adrenergic receptor agonists.

Abstract: Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A′ is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, especially irritable bowel syndrome.

Abstract: The present invention relates to lactam derivatives of the formula 1

Abstract: The present invention relates to the identification of diarylsulfonylurea binding proteins (DBPs) as therapeutic targets for agents that suppress the release of inflammatory mediators such as interleukin IL-1 and IL-1&bgr;.

Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: 1

Abstract: This invention relates to tetrazoles and their pharmaceutically acceptable salts which are selective agonists for the delta opioid receptor, particularly useful in the treatment of inflammatory diseases such as arthritis, psoriasis, asthma, inflammatory bowel disease, disorders or respiratory function, gastrointestinal disorders such as functional bowel disease and functional GI disorders, of formula (I) wherein R1 is H, C2-C6 alkanoyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (C3-C7 cycloalkyl)-(C1-C4 alkyl), (C1-C4 alkoxy)-(C1-C4 alkyl), carboxy-(C1-C4 alkyl), aryl-(C1-C4 alkyl) or heteroaryl-(C1-C4 alkyl); R2 and R3 are each independently H or C1-C4 alkyl; R4 is selected from (i) H, (ii) a group of the formula R6—(CH2)m—Z—(CH2)n—, where m is 0, 1, 2 or 3, n is 1, 2 or 3, Z is a direct link or O, and R6 is —CO2H or —CO2(C1-C4 alkyl), and (iii) a group of formula (a) where R7 is H or C1-C4 alkyl; and R5 is hydroxy, C1-C4 alkoxy or &mda

Abstract: NPY antagonists, methods of using such NPY antagonists and pharmaceutical compositions containing such NPY antagonists. The NPY antagonists are useful for the treatment of NPY mediated disease/conditions including obesity.

Abstract: Certain diaryl imidazoles act as partial agonists or antagonists for NPY receptors, in particular NPY 5 receptors. They are of use, for example in treating loss of appetite. Such compounds bear aryl groups in the 2 position. Many of the compounds are novel.