Abstract: The present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2?-methyl-2?,3?-dihydro-1?H-spiro[cyclopropane-1,4?-isoquinolin]-7?-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.

Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.

Abstract: The present invention is directed to novel 3-oxo-2,3-dihydropyrazolo[4,3-c]quinolizine derived compounds of generic formula (I) or a pharmaceutically acceptable salt thereof, which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: Nucleic acids encoding a new family of small cysteine rich soluble proteins, from a mammal, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.

Abstract: In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.

Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.

Abstract: The present invention relates to methods useful for treating and/or preventing mucositis using an active vitamin D compound.

Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

Abstract: Compounds of Formula (I) are disclosed; wherein XA, k, A, B, R3A, R3B, R4 and R5 are defined herein. The compounds of Formula (I) are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: The present invention is directed to alkoxy tetrahydro-pyridopyrimidine compounds of formula I, which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Abstract: The present invention relates to spiroazaindole compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

Abstract: Purified genes encoding interleukin-B30 from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this molecule are provided. Methods of using said reagents and diagnostic kits are also provided.

Abstract: Substituted bicyclic beta-lactams of Formula I: (I), are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).

Abstract: A liquid formulation for oral administration of the CETP inhibitor of formula (I) has improved bioavailability compared with conventional solid formulations. The formulation comprises the CETP inhibitor, or a pharmaceutically acceptable salt thereof; an oil; and one or more nonionic surfactants having a hydrophilic lipophilic balance (HLB)>10.

Abstract: The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: The invention relates to the identification and use of gene expression profiles, or patterns, with clinical relevance to the treatment of cellular proliferative disorders, especially those mediated by aberrant Notch signaling using a Notch signaling inhibitor. In particular, the invention provides the identities of genes, whose individual or cumulative expression patterns may be useful in various assays. The gene expression profiles, whether embodied in nucleic acid expression, protein expression, or other expression formats, may be used to select subjects afflicted with a Notch mediated cancer who will likely respond to treatment with a gamma-secretase inhibitor or another Notch inhibiting agent. It is to be understood and will be appreciated that the same markers may be used in the classification of patients being treated with other Notch inhibitors. The methods may further comprise providing diagnostic, prognostic, or predictive information based on the classifying step.

Abstract: Disclosed herein is a drug delivery system consisting of one or more compartments and comprising a progestogenic compound dissolved in a thermoplastic polyethylene vinylacetate copolymer. Also disclosed are a contraceptive kit or hormone-replacement therapy kit comprising the drug delivery system, and a combination preparation that simultaneously provides contraception and treatment of a sexually transmitted disease comprising the drug delivery system.