Abstract: The invention relates to compounds of the formula 1, 2, and 3 and to pharmaceutically acceptable salts and prodrugs thereof, wherein the groups are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I, methods of using said compounds of formula 1, 2, and 3 the treatment of infections, and methods of preparing said compounds of formula 1, 2, and 3.

Abstract: Compounds of the formula wherein R1 R2, R7, R8, X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from. dementia and Alzheimer's disease.

Abstract: Compounds according formula (I) A—G—Z—W and pharmaceutically acceptable salts, solvates or hydrates thereof; wherein, A is (C6-C10)aryl, (C6-C10)aryl-SO2, (C6-C10)aryl-CH2—, (C6-C10)arylcarbonyl, (C1-C9)heteroaryl, (C1-C9)heteroaryl-SO2—, (C1-C9)heteroaryl-CH2—; or (C1-C9)heteroarylcarbonyl; G is selected from the group consisting of:  where B is (C6-C10)aryl or (C1-C9)heteroaryl, and X is CH2, SO2, or carbonyl;  where X is CH2, SO2, or carbonyl; and R1 and R1′ are each independently selected from H, CN, (C1-C8)alkyl-, and phenyl(CH2)—, wherein said alkyl and phenyl groups are optionally substituted; and  where Z and W are as defined in the present Specificiation; and pharmaceutical compositions and methods useful to increase secretion of growth hormone(GH) from the anterior pituitary of mammals, including on a sustained release basis.

Abstract: The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are as defined herein. The above compounds of formula 1 are useful in the treatment of hyperproliferative disorders, such as cancer, in mammals. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to a mammal requiring such treatment.

Abstract: Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors.

Abstract: This invention relates to compounds of formula (I), wherein A, B, D, E, K, G, Z, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. Compounds (I) are corticotropin releasing factor (hormone) CRF (CRH) antagonists.

Abstract: The invention relates to compounds of the formulas 1 and 2 and to pharmaceutically acceptable salts and hydrates thereof, wherein X1, R1, R2 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1 and 2 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formulas 1 and 2.

Abstract: A method and device for the automated large scale preparation for testing of drug-drug interactions, particularly with determination of IC50 and Ki, as a screening tool enhancement for determining viability of large numbers of compounds as drug candidates. Small samples of specific probe substrates and new compound inhibitors are automatically dispensed en masse into multi-welled reaction plates which are prefilled with thawed human microsomes, buffer and cofactor. The reaction plates are incubated and the reaction products are tested within degradation time limits, for initial biological determinations of relevant interaction effects of the compounds.

Abstract: The present invention relates to a novel process for the preparation of a diastereomeric mixture of piperidinylaminomethyl trifluoromethyl cyclic ether compounds of formulae Ia and Ib: and pharmaceutically acceptable salts thereof, wherein R1 is C1-C6 alkyl; R2 is C1-C6 alkyl, halo C1-C6 alkyl or phenyl or substituted phenyl; R3 is hydrogen or halo; m is zero, one or two, and wherein said mixture is highly enriched in the compound of formula Ia, and to novel processes for the preparation and purification of intermediate compounds useful in the preparation of compounds of formulae Ia and Ib.

Abstract: Four antigenic preparations are provided, each of which contains a different protein from Leptospira which can be used immunologically in vaccines for leptospirosis caused by this organism. Also provided in the invention are polynucleotides encoding these four proteins and antibodies which bind the proteins for use in the diagnosis of leptospirosis.

Abstract: The invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof, wherein R1 and R2 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 compounds of formula 1.

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

Abstract: The present invention relates to the compound (+)-6-[amino-(6-chloro-pyridin-3-yl)-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-cyclopropylmethyl-1H-quinolin-2-one, pharmaceutically acceptable salts and solvates thereof, prodrugs thereof, and to the use of said compound for inhibiting abnormal cell growth, including cancer, in mammals. The invention also relates to methods useful in synthesizing the aforementioned compound.

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 invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3 and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.

Abstract: The present invention relates to a compound of the formula wherein R1, R2, R3 and R4 are as defined above, and pharmaceutically acceptable salts and solvates thereof, that are useful, for example, as matrix metalloproteinase inhibitors. The present invention is also directed to pharmaceutical compositions comprising such compounds and methods of treatment for diseases such as osteoarthritis, rheumatoid arthritis, cancer, osteoporosis, tissue ulceration, restinosis, periodontal disease, inflammation, epidermolysis bullosa, scleritis, stroke, Alzheimer's disease, and the like, characterized by inappropriate matrix metalloproteinase activity. Processes for the synthesis of compounds of formula (I) are also disclosed.

Abstract: This invention relates to the use of a compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined in the disclosure, for treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.

Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives. wherein R, R1 and R2 are as defined herein.

Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.