Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

Abstract: Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.

Abstract: Methods and pharmaceutical compositions relating to selective antagonists of the 5-HT6 receptor and 5-HT2A receptor useful for the treatment of cognitive disorders are presented.

Abstract: A method of associating a phenotype with one or more candidate chromosomal regions in a genome of an organism includes the step of deriving a phenotypic data structure that represents differences in phenotypes between different strains of the organism. Further, a genotypic data structure is established. The genotypic data structure corresponds to a locus selected from a plurality of loci in the genome of the organism. The genotypic data structure represents variations of at least one component of the locus between different strains of the organism. The phenotypic data structure is compared to the genotypic data structure to form a correlation value. The process of establishing a genotypic data structure and comparing it to the phenotypic data structure is repeated for each locus in the plurality of loci, thereby identifying one or more genotypic data structures that form a high correlation value relative to all other compared genotypic data structures.

Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.

Abstract: The present invention relates to assays that can measure the activity of enzymes that catalyze phosphate modifications, such as kinases, phosphatases, cyclases and phosphodiesterases. The assays can also be used to identify and screen for substances that modulate the activity of kinases, phosphatases, cyclases and phosphodiesterases.

Abstract: Compounds having the formula i wherein m, R1, R2, R4 and X1 are herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, processes for making the compounds and synthetic intermediates used in the process.

Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.

Abstract: The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficiency virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficiency virus containing a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3, and R4 are as defined herein.

Abstract: Compounds of formula I: wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds, pharmaceutical compositions, methods of using the compounds for treatment of p38 MAP kinase-mediated diseases, and methods of using the compounds for treatment of Raf kinase-mediated diseases.

Abstract: Compounds having the formula I wherein R1 is as herein defined are Hepatitis C virus NS5b polymerase inhibitors.

Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.

Abstract: The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-1,5-diol (2), which is useful for the preparation of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one (1) a MAP-kinase inhibitor useful in the treatment of rheumatoid arthritis.

Abstract: The invention relates to a novel process for the preparation of 4?-azido-cytidine (I) or a pharmaceutically accepted salt thereof. The compound of formula I is useful for treating virus mediated diseases, particularly for treating HCV mediated diseases.

Abstract: This invention relates to piperidine derivatives of formula I wherein R1, R2, R3 and R4 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPD.

Abstract: The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein.

Abstract: The present invention provides compounds of formula I where R1 to R4 are as defined herein which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides for methods of treating or preventing HIV infection with compounds according to formula I and compositions containing the same. The invention still further provides process for the preparation of compounds of formula I wherein R4 is A1 and X1 is NH or O.

Abstract: Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R1-R3 and Ar are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.

Abstract: Compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ar, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, methods of preparing the compounds, and method of using the compounds for treatment of monoamine reuptake inhibitor-mediated diseases.