Abstract: Compounds according to the formula: and pharmaceutically acceptable salts, solvates or hydrates thereof; wherein group Ar is optionally substituted (C6-C10)aryl or (C1-C9)heteroaryl; X is a direct link, —CH2—, —SO2—, —CO—, —CHR1— where R1 is (C1-C6) alkyl, or —CR1′R1″— where both R1′ and R1″ are, independently, (C1-C6)alkyl; Y is N or CH; and Z and W are as herein defined, and pharmaceutical compositions thereof, and methods useful to facilitate secretion of growth hormone(GH) in mammals.

Abstract: The invention provides transgenic, non-human animals and transgenic non-human mammalian cells harboring a transgene encoding a p25 (activator of the protein kinase cdk 5) polypeptide. The two neuropathological lesions associated with Alzheimer's disease (AD) are amyloid plaques and neurofibrillary tangles (NFTs), composed predominantly of amyloid &bgr; peptides and hyperphosphorylated tau, respectvely. While animal models for plaque formation exist, there is no animal model that recapitulates the formation of NFTs. This invention provides transgenic mice that overexpress human p25, an activator of cdk5, resulting in tau that is hyperphosphorylated at AD-relevant epitopes. Deposition of tau is detected in the amygdala, thalamus and cortex. Increased phosphorylated neurofilament, silver-positive neurons and neuronal death are also observed in these regions. We conclude that the overexpression of p25, an activator of cdk5, is sufficient to produce hyperphosphorylation of tau and neuronal death.

Abstract: The present invention provides the amino acid and nucleotide sequences of a CCV spike gene, and compositions containing one or more fragments of the spike gene and encoded polypeptide for prophylaxis, diagnostic purposes and treatment of CCV infections.

Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.

Abstract: The present invention is directed to a novel process for the preparation of the mesylate trihydrate of the compound of formula (I), (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol: The present invention is further directed to a process for the preparation of a (2S)-(+)-compound of formula (II): wherein R1 is a protecting group. In addition, the present invention relates to intermediates useful in said processes.

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 I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.

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 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: 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: The present invention relates to compounds of the formula and the pharmaceutically acceptable salts and solvates thereof wherein X1, X2, X3, R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods of treating shizophrenic and shizo-affective disorders, and related disorders which may be treated by administering compounds having dopaminergic activity such as the above compounds of formula 1.

Abstract: The present invention provides the amino acid and nucleotide sequences of a CCV spike gene, and compositions containing one or more fragments of the spike gene and encoded polypeptide for prophylaxis, diagnostic purposes and treatment of CCV infections.

Abstract: The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula wherein R1, R2, R3 and R4 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: The present invention relates to a process for preparing hydroxamic acids from hydroxylic acid intermediates wherein the carboxylic acid intermediate does not possess reactive substituents such as hydroxy or amino groups.

Abstract: The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I

Abstract: Compounds of formula (I) or pharmaceutically, veterinarily or agriculturally acceptable salts thereof, or pharmaceutically, veterinarily or agriculturally acceptable solvates of either entity, wherein R1 is 2,4,6-trisubsituted phenyl or 3,5-disubstituted pyridin-2-yl; R3 is C1-C4 alkyl optionally substituted with hydroxy or with one or more halo; cyano, C1 to C5 alkanoyl or phenyl R5 is hydrogen, C1 to C4 alkyl, amino or halo; R2 and R4 are each independently selected from hydrogen, C1 to C4 alkyl, fluoro, chloro and bromo or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group; R6 and R8 are each independently selected from hydrogen, C1 to C4 alkyl, fluoro, chloro and bromo; or; when R2 and R4 do not form part of a cycloalkyl group, R2 and R6, together with the carbon atoms to which they are attached, may form a C5 to C7 cycloalkyl group; and R7 is hydrogen, C1 to C4 alkyl optionally substituted with one or more halo; or C1 to C4 alkoxy; are parasitici

Abstract: The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein Z, R, R3 and R4 are as defined herein. 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 said mammal.

Abstract: This invention relates to novel azabicyclic compounds of the formula ##STR1## wherein R.sup.1, Q and Z are defined as in the specification, pharmaceutical compositions containing them, and the use of such compounds for the treatment of neurodegenerative diseases and other disorders involving nerve damage.

Abstract: A process for preparing phenoxyphenylsulfonyl halides, which are useful intermediates for the preparation of matrix metalloproteinase inhibitors.

Abstract: The present invention relates to a process for alkylating hindered sulfonamides useful as intermediates in the preparation of matrix metalloproteinase inhibitors.