Abstract: The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diones, pharmaceutically acceptable salts thereof and physiologically functional derivatives.

Abstract: A cell population expressing folate receptors is selectively targeted with a folate mimetic. The folate mimetic is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.

Abstract: The present invention relates to imidazo[2,1-f]triazin-4-one analogues which are substituted in the 7-position by a substituted phenyl ring, being ligands for GABAA receptors and accordingly of benefit in the therapy of deleterious neurological disorders.

Abstract: The present invention provides substituted 2-aminopyridines of formula I, wherein R1, A1, W, X, and Y are as defined in the specification, useful in treating cell proliferative disorders.

Abstract: An object of the present invention is to provide compounds having potent antitumor activity. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein X and Z represent CH or N; Y represents O or S; R1, R2, and R3 represent H, alkoxy or the like; R4 represents H; R5, R6, R7, and R8 represent H, halogen, alkoxy or the like; R9 and R10 represent H, alkyl or the like; and R11 represents optionally substituted azolyl.

Abstract: Methods of treating one or more conditions associated with p38 kinase activity are disclosed comprising administering to a patient in need thereof at least one compound having the formula (I): 1

Abstract: Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C1-C3 alkyl; or A and E can be taken together to form —CH2—, —CH2CH2—, —O—, —S—, —S(O)—, —S(O)2—, —NR8—, —OCH2—, —SCH2—, —N(R8)CH2—, substituted —CH2— and substituted —CH2CH2—, the substituents independently selected from 1-2 halogen and 1-2 methyl; W is N or CR4; X is CR5R6, O, S, NR7 or a direct bond, provided that when W is N, then X is other than a direct bond; Y is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, C3-C6 cycloalkylalkyl, NR9R10, N═CR11R12, OR7, COR13, CO2R14 or C1-C6 alkyl substituted by at least one group selected from halogen, C1-C3 alkoxy, CN, NO2, S(O)rR15, COR13, CO2R14 and optionally substituted phenyl; Z is O or S; and R2, R3, R4, R5, R6, R7, R8, R

Abstract: A compound represented by the formula I: 1

Abstract: A compound of the formula 1

Abstract: An object of the present invention is to provide compounds which have antitumor activity and do not change cytomorphosis. Disclosed are compounds represented by formula (I) and a pharmaceutically acceptable salts and solvates thereof and pharmaceutical compositions comprising said compounds: wherein X and Z each independently represent CH or N; R1 to R3 represent H, substituted alkoxy, unsubstituted alkoxy or the like; R4 represents H; R5 to R8 represent H, halogen, alkyl, alkoxy, alkylthio, nitro, or amino, provided that R5 to R8 do not simultaneously represent H; R9 and R10 represent H, alkyl, or alkylcarbonyl; and R11 represents alkyl, alkenyl, alkynyl, or aralkyl.

Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.

Abstract: The invention relates to 3,5-diamino-1,2,4-triazoles as kinase inhibitors, the production thereof and the use of the same as a medicament for treating cancer, for example solid tumours and leukaemia, auto-immune diseases such as psoriasis, alopecia and multiple sclerosis, alopecia induced by chemotherapeutic agents and mucositis, cardiovascular diseases such as stenoses, arterioscleroses, and restenoses, infectious diseases such as those caused by unicellular parasites such as trypanosome, toxoplasma or plasmodium, or by fungi, nephrological diseases such as glomerulonephritis, chronic neurodegenerative diseases such as Huntington's disease, amyotropic lateral sclerosis, Parkinson's disease, AIDS dementia and Alzheimer's disease, acute neurodegenerative diseases such as cerebral ischemia and neurotrauma, and viral infections such as cytomegalovirus infections, herpes, hepatitis B and C, and HIV diseases.

Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is a hydrogen atom or a group containing 1 to 4 non-hydrogen atoms; RA is —COCONH2 or the like; R3 is -(L2)-(acidic group) wherein L2 is a group connecting with an acid group; R4 is a hydrogen atom or the like, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF).

Abstract: An improved process for the preparation of certain pyrrolotriazine compounds is disclosed. The compounds exhibit utility as kinase inhibitors.

Abstract: The present invention provides compounds of formula I 1

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

Abstract: This application relates to matrix metalloprotease inhibitors having the generalized formula in which r is 0-2, T is selected from and R40 is a mono-or bi-heterocyclic structure. More particularly, the present application claims the various stereoisomeric forms of 4-(4′-choloro-biphenyl-4-yl)-4-oxo-2-[2-(4-oxo-4H-benzo[d][1,2,3]triazin-3-yl)ethyl]butyric acid, as well as their pharmaceutically acceptable salts. Pharmaceutical compositions containing these compounds, and methods for inhibiting matrix metalloprotease activity in mammals such as humans and for treating various conditions by administering such compounds are also claimed.

Abstract: There are provided compounds which can be used in the treatment of diseases mediated by the autophosphorylation of a PDGF receptor, specifically, compounds which can inhibit neointima formation hypertrophy.

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

Abstract: This invention relates to a novel class of heterocyclic compounds that bind chemokine receptors, inhibiting the binding of their natural ligands thereby. These compounds result in protective effects against infection by HIV through binding to chemokine receptors, including CXCR4 and CCR5, thus inhibiting the subsequent binding by these chemokines.

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formulae I and V: 1

Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain  in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the salt

Abstract: Compounds having the formula (I), 1

Abstract: The present invention relates to a process for preparing certain pyrrolotriazine compounds of the formula 1

Abstract: Disclosed are heterocyclic compounds and methods for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoids. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.

Abstract: The present invention provides compounds of formula I, 1

Abstract: Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

Abstract: The present invention provides compounds of formula I, 1

Abstract: The present invention provides compounds of formula I, 1

Abstract: This invention provides compounds defined by Formula I 1

Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: The present invention relates to compounds of the general formula (I), 1

Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, being selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: Methods of treating one or more conditions associated with p38 kinase activity are disclosed comprising administering to a patient in need thereof at least one compound having the formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, or NH2, preferably methyl, and X, R1 through R6, and Z are as described in the specification. Advantageously the groups —ZR4R5 taken together comprise an —NH-substituted aryl.

Abstract: Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

Abstract: Compounds having the formula (I), 1

Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of PDGF receptor to hinder abnormal cell growth and cell wandering and thus are useful for the prevention or treatment of cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

Abstract: A compound is provided having the formula: 1

Abstract: We have synthesized a series of new derivatives of (2-azinylamino) quinone, that have the general formula shown below. Several compounds of this new series of derivatives have been shown to be inhibitors of 5-lipoxygenase, with minimal or no effect on cycloxygenase-1 and 2-(COX-1 and COX-2) activity. where: A is N, CH, or, CCl; B is N, CH, CCH3, or Cph; X is H, Cl, Br, or I; Y is H, or CH3; R1 is H, CH3, OCH3, or Ph; and R2 is H, CH3, OCH3, or Ph; or R1—R2 is (CH═CH)2; and R3 is H or CH3.

Abstract: Compounds of the formula 1

Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.

Abstract: The present invention provides a compound of formula I 1

Abstract: The present invention relates to a compound of the general formula (I): 1

Abstract: The present invention relates to tyrosyl derivatives and their pharmaceutically acceptable salts; compositions thereof and methods of preparing the compounds are also described. The compounds are useful in the treatment of diseases in mammals that are mediated by the action of the P2X7 receptor.

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs)), and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compounds are useful for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; and the like.

Abstract: The present invention relates to biphenyl derivatives of general formula wherein Ra to Rg and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.

Abstract: The invention relates to novel 3-substituted 1,2,4-benzotriazines of general formula I. The invention is also directed to a method of producing said 3-substituted 1,2,4-benzotriazines and to the use thereof in the treatment and prophylaxis of tumor-related diseases.

Abstract: Fused bicyclic amines of formula (1) are described wherein Ar is an aryl or heteroaryl group; Y is a —S(O2)— or —C(O)— group; R1 is a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy or cyano group; X is a nitrogen atom or a C(R1a) group where R1a is as defined for R1 and may be the same or different; W and Z are each a carbon atom and together with U form an optionally substituted five- or six-membered monocyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the activity of Class I receptor tyrosine kinases and are of use in the prophylaxis and treatment of hyperproliferative disorders such as cancer, psoriasis, restenosis, atherosclerosis and fibrosis.