Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, wherein R1 represents C1-4 alkyl; R2 represents halo, C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyloxy, —SO2(C1-4 alkyl), optionally substituted C1-4 alkyloxy, Het or —OHet; R3 represents a bicyclic group of the formula ?wherein X and Y are selected from C and N, provided that at least one is C; Ring A together with X and Y represents a 5- or 6-membered aromatic ring containing 0, 1, 2 or 3 nitrogen atoms in the ring; n is), 1 or 2 L represents a direct link, C1-4 alkylene or C1-4 alkoxyalkylene; R4 represents H, —NR5R6, C3-6 cycloalkyl, —OR7, Het1 or Het4; R5 and R6 are independently selected from H, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-4 alkylene, —SO2(C1-4 alkyl) and optionally substituted C1-4 alkyl R7 is selected from H, C1-4 alkyl, C1-4 alkoxyalkyl, C3-6cycloalkyl, Het2 and C1-4alkyl-Het3; R8 is H or C1-4 alkyl; Het, Het1, Het2 and Het3 independently represent an optionally substituted 4 to 7 membered saturat

Abstract: The invention provides genetically-modified non-human mammals and genetically-modified animal cells containing a disrupted RAMP1, RAMP2, or RAMP3 gene. Also provided by the invention are methods of screening for agents that modulate the activity or expression of a RAMP and methods of treating mammals to modulate liver function and/or muscle metabolism.

Abstract: The invention relates to 6- or 7-bicyclic-substituted 4-amino-subsituted pyridopyrimidines and to pharmaceutically acceptable salts, prodrugs and hydrates thereof. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating hyperproliferative disorders abnormal cell growth in a mammal by administering the compounds.

Abstract: The invention relates to substituted tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid trans: protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease.

Abstract: The present invention relates to compounds of the formula Orosco wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.

Abstract: The present invention relates to novel quinazolin-4-one derivatives of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

Abstract: The invention provides compounds of Formula I: Azabicyclo-N(R1)—C(?X)—W??Formula I These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.

Abstract: The present invention provides processes useful in the preparation of certain ?3-adrenergic receptor agonists of the structural formula the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.

Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

Abstract: The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of a matrix metalloproteinase inhibitor and an antineoplastic agent.

Abstract: Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or a N-linked heterocyclic group; (CH2)nHet or (CH2)nAr, R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are each independently selected from H and C1 to C4 alkyl optionally substituted with C1 to C4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R7 and R8, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; Het is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of,

Abstract: This invention relates to compounds of formula (I)

Abstract: This invention relates to novel nucleic acid sequences encoding three novel human phosphodiesterase (hPDE IV) isozymes. It also relates to polypeptides encoded by such sequences. This invention also relates to an assay method for detecting the presence of such novel isozymes in human cells, and to a method of identifying compounds or other substances that inhibit or modify the activity of such isozymes.

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 wherein the variables A, B, Y, D, Z1, G and e are as described herein.

Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.

Abstract: This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of Formula 1 and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of Formula 1 and to methods of their use for the treatment and/or prevention of diseases such as, but not limited to, cancer.

Abstract: A method for removing impurities from racemic cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol and purified cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol useful as an estrogen agonist/antagonist.

Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.

Abstract: This invention relates to compounds of the formula wherein A, B, D, E, K, T, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.