Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof, wherein X is a direct link or C1-C4 alkylene; and R is C3-C7 cycloalkyl optionally substituted by 1 or 2 substituents each independently selected from fluoro and C3-C7 cycloalkyl: with the proviso that X is not methylene when R is cyclopropyl, together with processes for the preparation of, intermediates used in the preparation of, compositions containing and uses of, such compounds. These compounds are useful as tachykinin antagonists.

Abstract: The invention relates to the compounds of the formula 1 and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X and Y are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of using said compounds of formula 1 in the treatment of infections, and methods of preparing said the compounds of formula 1.

Abstract: Compounds of the formula (I): where X1, A, Ar1, X and R are as defined in the specification, and pharmaceutically-acceptable salts thereof, are new, and are useful as tachykinin inhibitors which act at the NK1, NK2 and NK3 receptors or a combination of two or more thereof.

Abstract: Two crystalline polymorphic forms of (2-Benzhydryl-1-azo-bicyclo(2.2.2]Octyl-3-yl)-(5-iso-propyl-2-methoxybenzyl)amine dihydrochloride dihydrate are Form I and Form II. The pharmaceutical composition containing at least are of these polymorphs has advantageous stability for formulation to treat emesis in patients receiving chemotherapy. The administration of this pharmaceutical composition is conventional oral by preferably tablet or capsule or intravenous. A method of making Forms I and II is also disclosed.

Abstract: A method for preparing pyrrole-carboxyamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloakane-diones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.

Abstract: This invention relates to a mutual salt of amlodipine and atorvastatin, pharmaceutical compositions thereof and methods of treating angina pectoris, atherosclerosis and combined hypertension and hyperlipidemia in mammals with such a mutual salt and compositions. This invention also relates to methods of managing cardiac risk in a mammal presenting with symptoms of cardiac risk, including humans by administering such a mutual salt and compositions.

Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R1, and R2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula (I), or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal. The invention also relates to intermediates that are useful in the preparation of the compounds of formula (I).

Abstract: This invention relates to a method of treating Parkinson's Disease whereby a mammal suffering from Parkinson's Disease is treated with a combination of a forebrain selective NMDA antagonist and a compound which is capable of increasing the excitatory feedback from the ventral lateral nucleus of the thalamus into the cortex. This invention also relates to pharmaceutical compositions containing the synergistic combination.

Abstract: The present invention relates to compounds of formula 1 and pharmaceutically acceptable salts and solvates thereof wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and Z are as defined herein. The invention also relates to pharmaceutical compositions comprising compounds of formula 1 and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering compounds of formula 1 to the mammal. The invention also relates to intermediates and methods useful in synthesizing compounds of formula 1.

Abstract: Compounds of the formula wherein R1, R2, R3, R4, R5 and X are defined as in the specification. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists.

Abstract: The invention relates to crystalline 9-E-(O-methyl)oxime of 11,12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-O-methyl-&agr;-L-ribohexopyranosyloxy)-6-O-methyl-12,11-(iminocarbonyl-(2-(3-(4-(3-pyridinyl)-1H-imidazol-1-yl)propyl)hydrazono))-3-oxoerythromycin wherein said crystalline compound is as the free base of said compound, the hemihydrate of said compound or the mesylate (methanesufonic acid) salt of said compound. The invention also relates to pharmaceutical compositions containing the foregoing crystalline compound and to methods of treating bacterial and protozoa infections by administering said crystalline compound.

Abstract: This invention provides a process for preparing a compound of the formula (I): wherein R1 is H or a hydroxyimino-protecting group; R2 is H, C1-4 alkyl or C1-4 alkoxy; R3 is C1-8 alkyl, C2-8 alkenyl or C3-8 cycloalkyl, and R4 is H, halo, C1-4 alkyl or C1-4 alkoxy, which process comprises the steps of (a) reacting an avermectin B2 derivative with an oxidizing agent to form a 5-oxo compound; (b) allowing the 5-oxo compound to react with a compound of formula R1—O—NH2 wherein R1 is H or a hydroxyimino-protecting group, to form a 5-imino compound; (c) reacting the 5-imino compound with a thionocarbonizing agent to form a 4″, 23-bisthionocarbonyl ester; (d) reacting the 4″, 23-bisthionocarbonyl ester with a deoxygenation agent to form a 4″, 23-dideoxy compound; and (e) reacting the R″, 23-dideoxy compound with an acid to form a compound of the formula (I).

Abstract: A single crystalline polymorphic form (2S,3S)-N-(methoxy-5-t-butylphenylmethyl-2-diphenylmethyl-1-azobicyclo[2,2,2] octan-3-amine citrate(citrate monohydrate) and its pharmaceutical composition. The pharmaceutical composition of the polymorphic form if the citrate monohydrate has advantageous stability for formulation to treat emesis. The administration of this pharmaceutical composition is immediate release, oral dosage form preferably by tablet or capsule or intravenous.

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, and particularly eletriptan, in combination with metoclopramide. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5HT1 receptor agonist and metoclopramide.

Abstract: Parasiticidal pyrazole derivatives of formula (I) wherein: R1 represents CN, C1-6 alkoxycarbonyl, NO2, CHO, C1-6 alkanoyl, phenyl optionally substituted by one or more halogen, or C1-6 alkyl optionally substituted by one or more halogen; R2 represents a group of formula (II), (III) or (IV) in which: R7 represents H, halogen, carbamoyl, cyano, tri(C1-6 alkyl)silyl, C1-6 alkyl (optionally substituted by one or more halogen, OH or C1-6 alkoxy), C1-6 alkoxycarbonyl, phenyl, or a 5- or 6-membered ring heterocycle which is saturated or partially or fully unsaturated and contains up to 4 hetero-atoms independently selected from up to 4 N atoms, up to 2 O atoms and up to 2 S atoms and which is attached to the alkynyl moiety by an available C, S or N atom where the valence allows; and R8, R9 and R10 each independently represents H, halogen, phenyl optionally substituted by one or more halogen, CN or C1-6 alkyl optionally substituted by one or more halogen; R3 represents H, C1-6 alkyl, halogen, NH2, NH(C1-6 alkanoyl),

Abstract: A series of 2-(4-hydroxypiperidino)-1-alkanol derivatives are useful as medicaments for the treatment of traumatic injuries to the brain and spinal cord and neuronal degenerative diseases including senile dementias, in mammals, especially humans.

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 the formulae (IA) and (IB): wherein R1 is C1 to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from C1 to C4 alkoxy; halo; CN; CF3; OCF3 or C1 to C4 alkyl wherein said C1 to C4 alkyl group is optionally substituted by C1 to C4 haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2 is C1 to C6 alkyl and R13 is OR3 or NR5R6, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

Abstract: Compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is H and the other is N═C(NH2)2 or NHC(═NH)NH2, and the other substituents are as defined herein, are urokinase (uPA) inhibitors.