Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel 2-substituted bicyclic benzoheterocyclic compounds of Formula I: 1

Abstract: This invention provides compounds of Formula I 1

Abstract: This invention relates to 3H-quinazolin-4-one derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as selective monoamine oxidase B inhibitors.

Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented.

Abstract: The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH2, hydroxy and alkoxy; R2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R6 is H, or C1-C8 alkyl; R19 is optionally substituted aryl; and m is 0-6.

Abstract: This invention provides methods for controlling invertebrate pests comprising contacting the pests or their environment with an arthropodicidally effective amount of a compound of Formula (I), its N-oxides or agriculturally suitable salts wherein B, J, K, R3 and R4 and n are as defined in the disclosure.This invention also pertains to certain compounds of Formula (I) and compositions for controlling invertebrate pests comprising a biologically effective amount of a compound of Formula I and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents.

Abstract: The invention relates to compounds of formula (I) 1

Abstract: Pyrimidone compounds of formula (I): 1

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

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

Abstract: This invention comprises the novel compounds of formula (I): 1

Abstract: The present invention provides intermediates, synthetic methods and novel quinazolinone compositions of matter.

Abstract: The present invention relates to quinazolinone compounds of formula (I): 1

Abstract: The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.

Abstract: It is the object of this invention to discover and study new chemical substances of non-proteinogenic structure which have a matrix metalloproteinase (MMP)-inhibitory effect.

Abstract: The invention provides novel compounds represented by the general formula 5 compound represented by the formula: 1

Abstract: The present invention describes a therapeutic method useful for treating or preventing a condition of platelet aggregation in a subject including administering a pharmaceutically effective amount of a compound or composition that inhibits JAK-3 and/or tyrosine phosphorylation of STAT-3 and inhibits thrombin induced platelet aggregation. The condition of platelet aggregation includes hematopoietic and cerbrovascular diseases.

Abstract: This invention relates to compounds that are efflux pump inhibitors and therefore are useful as potentiators of anti-fungal agents for the treatment of infections caused by fungi that employ an efflux pump resistance mechanism.

Abstract: Quinazolinones of formulae (a, b, c and d) are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.

Abstract: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.

Abstract: This invention relates to the modulation and/or inhibition of cell signaling, cell proliferation, cell inflammatory response, the control of abnormal cell growth and cell reproduction. More specifically, this invention relates to the use of mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in inhibiting cell proliferation, including compounds which are useful protein tyrosine kinase (PTK) inhibitors. The method of treating cell proliferation and/or differentiation or mediator release using said quinazoline compounds and their use in pharmaceutical compositions is described.

Abstract: A chymase inhibitor for the prevention or treatment of diseases involving an increase of eosinophils, as the effective ingredient, is disclosed, suppress the progress of the disease and to prevent progression of complications, wherein the chymase inhibitor is a quinazoline derivative having the formula (I): wherein X, R1, R2 and R3 are herein defined, or a pharmaceutically acceptable salt thereof.

Abstract: Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.

Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K&dgr;) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K&dgr; plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K&dgr;, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K&dgr; activity, including compounds that selectively inhibit PI3K&dgr; activity. Methods of using PI3K&dgr; inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K&dgr; inhibitory compounds to inhibit PI3K&dgr;-mediated processes in vitro and in vivo.

Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.

Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors.

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.

Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.

Abstract: A compound selected from those of formula (I): 1

Abstract: This invention describes novel pyrazole compounds of formula IIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.

Abstract: A compound given by general formula (1): [wherein T represents oxygen or sulfur atom, Y represents alkyl, cycloalkyl group, etc., ring W represents benzene ring, etc., R1 and R2 represent independently hydrogen atom, lower alkyl group, etc., and R3 represents hydrogen atom, alkyl group, etc. Z represents a group given by formula: {wherein A1 and A2 represent independently hydrogen atom, alkyl group, etc. and G represents straight chain alkylene having 1-6 of the carbon number, etc.} or a group given by formula: {wherein n represents 0, 1 or 2, ring E represents 4-8 membered saturated heterocyclic ring containing nitrogen atom(s), and A3 represents hydrogen atom, alkyl group, etc.}], its prodrug or pharmaceutically acceptable salt thereof is an antagonist against muscarinic receptor that is useful as anticholinergic medicaments, and therefore it is useful as pollakiuria or urinary incontinence remedy.

Abstract: Disclosed are therapeutic compounds having the formula:

Abstract: The present invention describes a therapeutic method useful for treating or preventing a condition of platelet aggregation in a subject including administering a pharmaceutically effective amount of a compound or composition that inhibits JAK-3 and/or tyrosine phosphorylation of STAT-3 and inhibits thrombin induced platelet aggregation. The condition of platelet aggregation includes hematopoietic and cerbrovascular diseases.

Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.

Abstract: Novel compounds of formula I: 1

Abstract: The present invention relates to novel quinazolin-4-one derivatives of the formula wherein A is a benzo or thieno fused aromatic ring; B is phenyl, pyridyl or pyrimidyl; X is N or CH; and Y-Z is —CH2NH— or —NHCH2—; and to pharmaceutical compositions containing such compounds, and the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

Abstract: Compounds of formula 1 modulate the activity of Rho C: 1

Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and/or epileptogenesis. Methods for preparing the compounds of the invention are also described.

Abstract: The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The present invention provides an oil preparation comprising a high lipophilic medicament such as a compound of the formula (I): 1

Abstract: The invention is directed to novel quinazoline and quinazoline-like derivatives of Formula (I): 1

Abstract: A compound selected from those of formula (I): 1

Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.

Abstract: The present invention relates to pharmacologically active compounds which are capable of binding to nuclear hormone receptors and are useful for the stimulation of osteoblast proliferation and ultimately bone growth. This invention also relates to the use of such compounds for the treatment or prevention of diseases and/or disorders associated with nuclear hormone receptor families.

Abstract: Compounds and compositions are provided that bind to the CXCR3 chemokine receptor and which are useful for treating diseases associated with CXCR3 activity, such as multiple sclerosis.

Abstract: The present invention generally relates to compositions useful in the treatment or prevention of cancer, in some cases by limiting or preventing angiogenesis. Other compositions useful for the treatment or prevention of cancer or angiogenesis include homologs, analogs, derivatives, enantiomers or functionally equivalent compositions of the present invention. The present compositions can be packaged in kits. The present invention also relates to the use of compositions useful for the treatment of patients susceptible to or exhibiting symptoms characteristic of cancer, for example, patients with solid tumors.

Abstract: Compounds, compositions containing compounds, methods of sing compounds, and processes of making compounds, of formula I containing at least one ring nitrogen: 1

Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: 1