Abstract: The present invention describes the identification of novel non-ribosomal peptide synthetases and associated biosynthetic genes from Streptomyces hygroscopicus. The present invention further provides methods for generating novel compounds, such as antibiotics, from these synthetases and associated genes.

Abstract: Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.

Abstract: The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.

Abstract: The present invention provides a method for the non-sedative treatment of noise phobia in a companion animal, particularly a dog, which comprises providing said animal with a therapeutically effective amount of N-methyl-N-[3-(3-methyl-1,2,4-triazolo-[4,3-b]pyridazin-6-yl)phenyl]acetamide or 7-(3-pyridyl)pyrazolo[1,5-a]pyrimidine-3-carbonitrile.

Abstract: The present disclosure is directed to combination therapies of tigecycline and warfarin and methods of administration of tigecycline and warfarin.

Abstract: Compounds of Formula 1, or pharmaceutically acceptable salts thereof, are provided: which are inhibitors of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis.

Abstract: Methods for determining if test compounds are able to modulate the interaction between androgen receptor and ?-catenin are disclosed. Methods for the determining whether a test compound selectively modulates an androgen receptor signaling pathway over a ?-catenin-Wnt signaling pathway or a ?-catenin-Wnt signaling pathway over an androgen receptor signaling pathway are also disclosed.

Abstract: High load concentrate compositions comprising metaflumizone, an optional bridging agent, a surfactant, and a suitable carrier solvent. These compositions may be topically administered to animals, and are useful for preventing or treating ectoparasitic infestations in warm-blooded animals for prolonged periods of time. Additionally, they may be further diluted to provide other types of formulations useable for both topical and oral administration.

Abstract: The invention is directed to methods of making substituted 3-cyanoquinolines, including compounds according to the following formula: The methods are amenable to large scale manufacture, avoid the use of chromatographic separations, and provide stable, high purity product more efficiently than in the prior art.

Abstract: This invention provides an isolated mixture of higher molecular weight primary aliphatic alcohols having 20, 22, 24, 26, 27, 28, 30, 32 and 34 carbon atoms and having enhanced purity. This invention also provides a process for obtaining the alcohol mixture by extracting a natural product with organic solvents with or without saponification of the natural product. The alcohol mixture is useful in pharmaceutical compositions, foodstuffs and dietary supplements and is effective for lowering total cholesterol and LDL-cholesterol and increasing HDL-cholesterol levels and therefore is effective in treating hypercholesterolemia. The composition may be used to reduce the risk of coronary heart disease, to inhibit the atherosclerotic process (platelet hyperaggregability, ischemia and thrombosis), and can be used as an anti-inflammatory and anti-thrombotic agent. The composition also possesses neurotrophic properties and is useful for improving male sexual activity.

Abstract: This invention provides processes for preparing compounds formula: wherein R is H, alkyl, acyl, aryl, aroyl or —C(O)R?; R? is alkyl or aryl; R1, R2, R4 and R5 are H, —OH, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl or alkoxy, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, acyl, aryl or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, as well as novel compounds useful in the synthesis of these compounds.

Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: The present invention relates generally to substituted oxadiazolidinediones and methods of using them.

Abstract: The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.

Abstract: The present invention provides compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, m and n are defined as described herein. The invention also provides methods of making the compounds of formula (I), and methods of treating inflammatory diseases, such as rheumatoid arthritis, in a mammal comprising administering a therapeutically effective amount of a compound of formula (I) to the mammal.

Abstract: Novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical formulations containing such compounds which are useful as anti-aquaretic agents in the treatment of nocturnal urinary enuresis, nocturnal urinary urgency, and/or similar conditions.

Abstract: Truncated aggrecanase proteins and nucleotides sequences encoding them as well as processes for producing them are disclosed. Additionally, aggrecanases with amino acid mutations that lead to increased stability and expression levels in comparison with wild-type or native aggrecanases are also disclosed. Aggrecanases of the invention are especially useful for development of compositions for treatment of diseases such as osteoarthritis. Methods for developing inhibitors of the aggrecanase enzymes and antibodies to the enzymes for treatment of conditions characterized by the degradation of aggrecan are also disclosed.

Abstract: The invention provides compounds of formula or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, and B are as defined in the accompanying specification. Methods of making such compounds are also provided.

Abstract: The invention provides compounds of formula or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, A, and B are as defined in the accompanying specification. Methods of making such compounds are also provided.

Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.