Abstract: Sulfohydroxamic acid diarylamines and derivatives thereof; compositions made from them; and methods of using them.

Abstract: This invention relates to compounds of the formula wherein a, R1, R2, R3, R4, R5, R6 and X are each as defined above, and to pharmaceutically acceptable salts thereof, useful as potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating bacterial and protozoal infections by administering the compounds of formula I.

Abstract: Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated.

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: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

Abstract: This invention relates to compounds of the formula 1: and to pharmaceutically acceptable salts and solvates thereof wherein X1, X2, R2, R8, R9, R10 and R11 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract: The invention relates to hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salt forms of 3-(4-bromo-2,6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4-carboxylic acid amide having the following formula: The invention also relates to pharmaceutical compositions containing the hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salts of formula I. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above salts and to methods of preparing the crystal forms of the above salts.

Abstract: This invention provides a high throughput method for identifying drug candidates which produce reactive metabolites that contribute to toxicity of the drug product.

Abstract: The present invention provides a compound of formula (I): where Q is a group of formula: These compounds inhibit cyclic guanosine 3′,5′-monophosphate phosphodiesterases (cGMP PDEs). More notably, the compounds are potent and selective inhibitors of the type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterases and have utility therefore in a variety of therapeutic areas. In particular, the present compounds are of value for the curative or prophylactic treatment of mammalian sexual disorders.

Abstract: The invention provides genetically-modified non-human mammals and genetically-modified animal cells containing a functionally disrupted PDE11A gene. Also provided by the invention are methods of screening for agents that modulate PDE11A to modulate spermatogenesis, methods of treating mammals to modulate spermatogenesis, and methods of modulating cAMP and cGMP signal transduction in cells that express PDE11A.

Abstract: This invention relates to compounds of Formula I or stereoisomers, pharmaceutically acceptable salts or prod rugs thereof or a pharmaceutically acceptable salts of the prodrugs. This invention also relates to pharmaceutical compositions comprising a compound of Formula I, and to methods of treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, or tissue ischemia.

Abstract: The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives.

Abstract: The present invention relates to a process for preparing 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen-2-ol compounds useful as an estrogen agonist.

Abstract: This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t is 0, 1, or 2; Y is ═C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1-C4) alkyl; —(C2-C4) alkynyl; fluorinated-(C1-C3) alkyl; fluorinated-(C1-C3) alkoxy; —OR16; and —C(═O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1-C4) alkyl; —(C3-C7) cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that one

Abstract: Compounds of Formula (IA) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described herein.

Abstract: The present invention is directed to a polymorph of the citrate salt of 4-(3,4-dichlorophenyl)-2-[2-(4-methylpiperazin-1-yl)-benzylidene]-thiomorpholin-3-one: and pharmaceutical compositions thereof.

Abstract: The invention relates to processes for preparing compounds of formula 1 wherein R3 is as defined herein, and to pharmaceutically acceptable salts thereof, as well as intermediates useful in such processes. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing compounds prepared by the processes of the invention and to methods of treating bacterial protozoa infections by administering such compounds.

Abstract: The invention relates to novel erythromycin derivatives, particularly ones with novel C-13 R13 substitutents, and to pharmaceutically acceptable salts thereof. The compounds of this invention are useful as antibacterial agents and antiprotozoa agents and for other applications (e.g., anticancer, atherosclerosis, gastric motility reduction, etc.) in mammals, including man, as well as in fish and. 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: A compound of the formula whereon R1 is: R5 is: and n, m, Z, R8, R9, R10 and R11 are as defined herein, useful in the treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia, particularly myocardial ischemia.