Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.

Abstract: Aqueous antibiotic compositions comprising a mixture of an azalide compound, propylene glycol, and one or more acids, and methods for preparing such compositions, are disclosed.

Abstract: The present invention relates to novel triazolo-pyridines of the formula I 1

Abstract: This invention relates to pharmaceutical combinations of amlodipine or a pharmaceutically acceptable acid addition salt thereof and statins or pharmaceutically acceptable salts thereof, kits containing such combinations and methods of using such combinations to treat subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and to treat subjects presenting with symptoms of cardiac risk, including humans. This invention also relates to additive and synergistic combinations of amlodipine or a pharmaceutically acceptable acid addition salt thereof and statins or pharmaceutically acceptable salts thereof whereby those additive and synergistic combinations are useful in treating subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and those subjects presenting with symptoms of cardiac risk, including humans.

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 relates to novel screening methods which enable the selection of neurokinin-1 (NK-1) receptor antagonist compounds which do not possess significant inhibitory potency towards cytochrome P450 enzymes, in particular, CYP2D6. The present invention also relates to a method of generating a pharmacophore model for the CYP2D6 inhibitory activity of NK-1 receptor antagonist compounds; to methods for the discovery of molecules that are potential NK-1 receptor antagonist compounds which do not possess significant inhibitory potency towards the CYP2D6 enzyme; to methods of modeling the features of the CYP2D6 pharmacophore useful in selecting NK-1 receptor antagonist molecules which do not possess significant potency towards CYP2D6.

Abstract: The present invention relates to a method for inhibiting a neurogenic inflammation caused or potentiated by an administration of viral vectors in gene therapy by administering to said mammal an antagonist that binds to a NK-1 receptor in an amount that is effective to inhibit said neurogenic inflammation.

Abstract: Compounds of the formula (I): wherein A, Y, R, X, R1, R2, R3 and R4 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 or other disorders involving nerve damage.

Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X, Y, V, W1, W2, Z1 and Z2 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods of treating bacterial and protozoal infections in mammals by administering the above compounds.

Abstract: The present invention relates to a novel process for the preparation of a compound of formula I: 1

Abstract: The subject invention provides a compound of the formula 1, 1

Abstract: The present invention relates to the compounds 6-[4-(N-methyl-3-azetidinoxy)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, 6-[4-(N,N-dimethylaminomethyl)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, 6-[4-(N-methylaminomethyl)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine and 6-[4-(3-azetidinoxy)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds and to the use of such compounds in the treatment and prevention of central nervous system and other disorders.

Abstract: This application is directed to 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: where Y is ═C(R1a)— or —[N□(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted bi

Abstract: This invention provides a method of conducting a simultaneous chemical reaction and controlled crystallization of the product employing impinging fluid jet streams containing reactants capable of producing the product with desired particle size characteristics.

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, 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, maintanence of skin thickness, metabolic homeostasis or renal homeostasis.

Abstract: The invention relates to a process for preparing (1&agr;,3&agr;,5&agr;)(3-aminomethyl-bicyclo[3.2.0]hept-3-yl)-acetic acid, or an acid addition salt thereof.

Abstract: The present invention relates to method for the preparation of dialkylpyridylboranes by reacting a pyridine Grignard reagent with an alkoxydialkylborane or a trialkylborane. The reaction can be conducted at a temperature ranging from about 0° C. to about 40° C. The pyridine Grignard reagent is preferably prepared in situ by the reaction of a Grignard reagent (RMgX) and a halopyridine in a suitable solvent, such as tetrahydrofuran, followed by the addition of an alkoxydialkylborane or a trialkylborane to form a dialkylpyridylborane.

Abstract: The invention provides a method for synthesis of compounds of formula 1

Abstract: The invention provides a novel cytochrome P450 2D6 gene variant. Also provided, are primers, vectors, host cells, antibodies, agonists, antagonists, gene chips, methods for detecting susceptibility to drug sensitivity, and methods of treatment.

Abstract: The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or R3 is the radical  wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R9 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group; R4 is hydrogen, halogen, trifluorom