Abstract: This invention provides novel PDE11 genes and polypeptides, and variants, homologues, fragments, and derivatives thereof. This invention also provides vectors and host cells comprising the disclosed nucleotide sequences. This invention further provides antibodies that bind to the PDE11 polypeptides. This invention further yet provides methods for identifying agents that affect the expression or activity of the PDE11 genes and polypeptides. This invention also provides pharmaceutical compositions comprising the PDE11 genes or polypeptides, or inhibitors thereof. This invention additionally provides methods for treating diseases and conditions related to PDE11 activity, or the inhibition thereof.

Abstract: This invention relates to dihydroxyhexanoic acid derivatives and their intermediates, as well as to methods of preparing such compounds. Additionally, present invention relates to removing a protecting group from a protected amine wherein the method comprises reacting the protected amine with phosphoric acid.

Abstract: A process for producing substantially optically pure sertraline utilizes chromatographic separation on a solid stationary chiral phase of spherical clay particles having an interlayer containing an optically pure metal-organic complex, and a liquid mobile phase preferably containing at least methyl acetate. The liquid mobile phase is preferably free of acetonitrile. The process is operable at temperatures above 40° C.

Abstract: The present invention provides 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)quinazoline mesylate of the formula together with processes for preparing, and compositions containing it. The invention also relates to substantially pure anhydrous crystalline polymorphic forms of the free base. The compounds are particularly useful in the treatment of benign prostatic hyperplasia.

Abstract: In accordance with the present invention, there are provided fully human monoclonal antibodies against human cytotoxic T-lymphocyte antigen 4 (CTLA-4). Nucelotide sequences encoding and amino acid sequences comprising heavy and light chain immunoglobulin molecules, particularly contiguous heavy and light chain sequences spanning the complementarity determining regions (CDRs), specifically from within FR1 and/or CDR1 through CDR3 and/or within FR4, are provided. Further provided are antibodies having similar binding properties and antibodies (or other antagonists) having similar functionality as antibodies disclosed herein.

Abstract: Use of vardenafil or a pharmaceutical composition thereof in the preparation of a medicament for the curative, palliative or prophylactic treatment of type 2 diabetes mellitus.

Abstract: The instant invention provides crystal forms of 5-chloro-N-[(1S,2R)-3-[3R,4S]-3,4-dihydroxy-1-pyrrolidinyl]-2-hydroxy-3-oxo-1-(phenyl) methyl)propyl]-1H-indole-2-carboxamide (I) processes for the production of such crystal forms; pharmaceutical compositions comprising such crystal forms; and methods of treating glycogen phosphorylase dependent diseases, or conditions with such crystal forms, or such pharmaceutical compositions.

Abstract: The present invention relates to compounds of the formula I 1

Abstract: An apparatus, system, method, and computer readable medium containing computer-executable code for implementing image analysis uses multivariate statistical analysis of sample images, and allows segmentation of the image into different groups or classes, depending on a correlation to one or more sample textures, or sample surface features. In one embodiment, the invention performs multivariate statistical analysis of ultrasound images, wherein a tumor may be characterized by segmenting viable tissue from necrotic tissue, allowing for more detailed in vivo analysis of tumor growth beyond simple dimensional measurements or univariate statistical analysis. Application of the apparatus and method may also be used for characterizing other types of samples having textured features including, for example, tumor angiogenesis biomarkers from Power Doppler.

Abstract: A composition comprises a solid dispersion comprising a low-solubility drug and at least one polymer. At least a major portion of the drug in the dispersion is amorphous. The polymer has a glass transition temperature of at least 100° C. measured at a relative humidity of fifty percent. Another aspect of the invention comprises the same composition except that the dispersion has a glass transition temperature of at least 50° C. at a relative humidity of fifty percent. In another aspect of the invention, a composition comprises a solid dispersion comprising a low-solubility drug and a stabilizing polymer. At least a major portion of the drug in the dispersion is amorphous. The composition also includes a concentration-enhancing polymer that increases the concentration of the drug in a use environment. The stabilizing polymer has a glass transition temperature that is greater than the glass transition temperature of the concentration-enhancing polymer at a relative humidity of 50%.

Abstract: The present invention provides compounds of formula (I) 1

Abstract: The invention relates to methods for identifying agents, which bind to and/or modulate exopeptidases or endopeptidases, preferably human soluble secreted endopeptidase (SEP), oxytocinase, neutral endopeptidase (NEP), or non-human SEP, preferably comprising contacting said agents with a polypeptide comprising: SEQ ID NO: 2, an amino acid sequence encoded by the polynucleotide sequence of SEQ ID NO: 1 or SEQ ID NO: 5; or a polypeptide encoded by the cDNA of NCIMB 41110, and determining whether binding and/or modulation occurs. Preferably, said method is carried out in the presence of a substrate peptide labelled with at least one fluorescent donor dye and at least one fluorescence acceptor dye, with the method used to detect said agents being a competitive binding Fluorescence Resonance Energy Transfer (FRET) assay.

Abstract: The present invention relates to amlodipine free base in a crystalline form, to pharmaceutical formulations comprising such material, processes of manufacture and its use in therapy.

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

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 1

Abstract: The present invention relates to polynucleotide molecules comprising nucleotide sequences encoding an aveC gene product, which polynucleotide molecules can be used to alter the ratio or amount of class 2:1 avermectins produced in fermentation cultures of S. avermitilis. The present invention further relates to vectors, host cells, and mutant strains of S. 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: This invention relates to a process for controlling the hydrate mix of a compound, or a composition comprising the compound, the compound being capable of forming a plurality of hydration forms of differing stability and also of dissolution to give a solution that, when frozen below the eutectic point, is a eutectic mixture. This invention further relates to disodium salt of fosfluconazole in the form of its trihydrate, its hexahydrate, or as a mixture of tri- and hexahydrates.

Abstract: The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1

Abstract: A macrolide antibiotic of the formula 1

Abstract: The invention provides non-human, genetically-modified mammals and genetically modified animals cells having a functionally disrupted P2×7 receptor gene. Also provided are methods for producing genetically modified mice in which one or both P2×7R alleles have been functionally inactivated.