Abstract: Novel isothiazole and isoxazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.

Abstract: The present invention relates to polynucleotide molecules comprising sequences encoding avec gene products, which polynucleotide molecules can be used to alter the ratio or amount of class 2:1 avermectins produced in fermentation cultures of Streptomyces avermitilis. AveC genes, homologs and partial homologs thereof are described for S. avermitilis, S. hygroscopicus, and S. griseochromogenes, respectively. The present invention further relates to vectors, host cells, and mutant strains of Streptomyces avermitilis in which the avec gene has been inactivated, or mutated so as to change the ratio or amount of class 2:1 avermectins produced.

Abstract: The present invention relates to chiral N-acetyl-alpha-amino acid salts of optically active ?-amino alkylnitriles, and also to a process for preparing optically active ?-amino alkylnitriles by resolving racemic ?-amino alkylnitriles using chiral N-acetyl-alpha-amino acids as resolving agent.

Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.

Abstract: The invention described herein relates to: the use of an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase in the manufacture of a composition for the treatment of rumen acidosis; a method of treatment of rumen acidosis which comprises administration of an effective amount of an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase to a ruminant; a formulation suitable for the treatment of rumen acidosis in an animal which comprises an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase in admixture with a suitable excipient, diluent or carrier selected with regard to the intended route of administration and standard pharmaceutical/veterinary/farming practice; screening methods useful in the identification of a suitable inhibitor of a bacterial ?-amylase and/or ?-glucosidase for the treatment of acidosis in a ruminant; a process for improving ruminant milk quality and/or quantity which comprises treatment of a ruminant with an effective amount of an inhibitor of bacte

Abstract: The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R7, R8, R9, R10, and R11 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, 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 invention relates to a method of vaccinating a domesticated bird against coccidiosis comprising administering in ovo an effective immnunizing dose of live Eimeria sporozoites or merozoites, or a mixture thereof. In a preferred embodiment, the domesticated bird that is vaccinated is a chicken or turkey.

Abstract: A process for preparing acyl derivatives as prodrugs of 5-(2-(4-(1,2 benzisothiazole-3-yl)-1-piperazinyl)ethyl-6-chloro-1,3-dihydro-2H-indol-2-one and pharmaceutically acceptable acid addition salts and methods of use as an antipsychotic.

Abstract: A process for preparing a naphthyridone carboxylic acid and its derivatives makes use of side chain intermediates of formulae I and IV herein.

Abstract: The invention provides new methods for treating certain disorders resulting from neurodegeneration and for treating depression which comprise administration of NR2B subunit selective NMDA antagonists. The disorders that can be treating by the invention include hearing loss, vision loss, neurodegeneration caused by epileptic seizures, neurotoxin poisoning, Restless Leg Syndrome, multi-system atrophy, non-vascular headache, and depression.

Abstract: The invention presents compounds of formula (I), where R represents H or a suitable carboxylic acid protecting group, which are intermediates in the preparation of therapeutic fused bicyclic amino acids.

Abstract: The invention relates to novel erythromycin analogs and azalides, particularly ones with novel C-13 substituents, and to pharmaceutically acceptable salts thereof. The compounds of this invention are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial protozoa infections by administering such compounds. The invention also relates to methods of preparing such compounds and to intermediates useful in such preparation.

Abstract: This invention relates to substituted pyrimidinone and pyrimidithione derivatives that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety disorders, and depression and stress related disorders.

Abstract: There is provided a compound of formula I, wherein R1, R2, R3 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 2-aminopyridine derivatives of the formula wherein G, R1 and R2 are defined as in the specification, 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 and other disorders.

Abstract: This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a methyl group or an ethyl group; R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group of R3 is substituted by said alkoxy group, said alkyl group is a branched alkyl group. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract: The present invention is drawn to set of formulations of at least one compound selected from tolterodine, salts thereof, prodrugs thereof and/or metabolites thereof, wherein in the set of formulations contains at least one device for transdermal administration and at least one formulation for oral, sublingual, buccal, nasal, pulmonary, rectal and/or other transmucosal administration, in order to achieve an effect against overactive bladder and/or symptoms associated with this condition. The present invention is further drawn to methods of treating an overactive bladder with the formulations.

Abstract: A method for preparing indan-1,3-dicarboxylic acid compounds which are useful intermediates in the syntheses of aryl fused azapolycyclic compounds as agents for the treatment of neurological and psychological disorders.

Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, X and Y are defined as in the specification. Those compounds are 5HT7 partial agonists and are useful in the treatment of several disorders of the central nervous system.

Abstract: There is provided a process for the production a compound of general formula I: wherein A, R1, R2, R3 and R4 have meanings given in the description, which process comprises the reaction of a compound of formula II, wherein Rx is a group substitutable by an aminopyrazole, with a compound of general formula III