Abstract: A compound represented by formula (I): (wherein the symbols are the same as defined in the description), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medicinal use thereof. The compound represented by formula (I) has CXCR4 antagonistic activity. It is hence useful as, e.g., a preventive and/or therapeutic agent for CXCR4-mediated diseases such as inflammatory/immunologic diseases (e.g., rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, and rejection reactions of transplanted organs), allergic diseases, infections diseases (e.g., human immunodeficiency virus infection and acquired immunologic deficiency syndrome), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease, metabolic diseases, cancer diseases (e.g., cancer, cancer metastasis) or as an agent for regeneration therapy.

Abstract: The present invention provides a compound of pyrazolo[3,4-d]pyrimidine having the formula wherein: X=N; R=H, alkylthio, or aminoalkylthio; R1=NHcyclopropyl, NHC3H7, NHC4H9, N(CH2CH3)2, NHCH2CH2OC2H5, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, NHcyclohexyl, 1-hexahydroazepinyl, NHCH2C6H5, or NHCH2CH2C6H5; wherein R3=H, halogen, or alkyl and R5=Cl, Br or OH.

Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.

Abstract: The invention relates to methods of screening for binding partners, especially binding partners essential for the biological activity of erastin (e.g. VDACs such as VDAC3). The invention also provides reagents and methods for effective killing of cancer cells with erastin and related compounds or derivatives.

Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C7 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.

Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C6 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.

Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C4 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.

Abstract: The present invention encompasses compounds of general Formula (I) wherein X and R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.

Abstract: The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.

Abstract: Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.

Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.

Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: This invention relates to a method for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, or tissue injuries. The method includes administering to a subject in need thereof an effective amount of one or more compounds of formula (I). Each variable in this formula is defined in the specification.

Abstract: This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N?-substituted-N?-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.

Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.

Abstract: Fungicidal mixtures comprising, as active components 1) the strobilurin derivative of the formula I, and 2) at least one active compound II selected from the group of heterocyclic compounds in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compound I with active compounds II, the use of the compound I with active compounds II for preparing such mixtures and compositions comprising these mixtures.

Abstract: Compounds represented by Formula (I): and/or pharmaceutically acceptable salts, individual enantiomers and stereoisomers thereof, are effective as NMDA/NR2B antagonists useful for treating conditions such as pain, Parkinson's disease, Alzheimer's disease, epilepsy, depression, anxiety, ischemic brain injury including stroke.

Abstract: The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.

Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

Abstract: The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc. Q is single bond, a methylene group or a group of the formula: —N(RQ)—, RQ is an alkyl group, Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), R3 and R4 are the same or different and a hydrogen atom, a cyano group etc. E is one of the following groups (i) to (v): R00 is an alkyl group, Q1 is a single bond etc., Q2 is a single bond or an alkylene group, one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., one of R50 and R60 is a hydrogen atom or an alkyl group and the other is a hydrogen atom, an alkyl group etc., R51 is an alkyl group or an optionally substituted arylsulfonyl group, R61 is an alkylamino group or an azido group, or a pharmaceutically acceptable salt thereof.

Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl m

Abstract: The present invention relates to naphthylpyrimidine analogs, methods of making naphthylpyrimidine analogs, compositions comprising a naphthylpyrimidine analog, and methods for treating canonical Wnt-?-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analog.

Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable-salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.

Abstract: The present invention relates to an agent for pancreas protection which contains a combination of a blood glucose lowering drug that does not stimulate insulin secretion and a compound represented by the formula (I) wherein each symbol is defined as in the description, or a salt thereof, or a compound represented by the formula (II) wherein each symbol is defined as in the description, or a salt thereof.

Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.

Abstract: The present invention relates to amino-substituted quinazoline derivatives as inhibitors of ?-catenin/tcf-4 pathway, which can be useful in the treatment of cancer; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.

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

Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4).

Abstract: The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors.

Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2?, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2? are optionally taken together with their intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.

Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N?N—. —NR7—, —CR7?CR8—, —CR7?N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.

Abstract: The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds.

Abstract: A compound of formula (I): wherein: R1, R2, R3, R4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful as kinase modulators.

Abstract: The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3/R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; and R, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof.

Abstract: The invention concerns amide derivatives of Formula (Ia) wherein X is —NHCO— or —CONH—; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino and carboxy; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino and N-(1-6C)alkyl-arylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines

Abstract: The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof-alone or in combination with one or more other pharmaceutically active compounds-for the treatment of a disease, especially a proliferative disease, such as a tumour disease, a method for the treatment of such diseases in mammals, especially in humans, and the use of such a compound-alone or in combination with one or more other pharmaceutically active compounds-for the preparation of a pharmaceutical composition (medicament) for the treatment especially of a proliferative disease, such as a tumour.

Abstract: Certain TRPV1-modulating thiazolopyrimidine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.

Abstract: The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein formula I is: wherein X, Y, Z, R1 and R2 are as defined in the description and claims. The compounds of the present invention act as antagonists and/or inverse agonists at the histamine 3 receptor and are useful for the treatment and/or prevention of diseases such as obesity, metabolic syndrome (syndrome X), and other eating disorders.

Abstract: The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- represents a saturated or an unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical -{circle around (A)}- is substituted with R2 being hydrogen, hydroxy, C1-4alkyl, or C1-4alkyloxy; -a1=a2-a3=a4- represents an optionally substituted bivalent radical; R1 is hydrogen, C1-6alkyl, aryl1, C1-6alkyl substituted with aryl1, C1-4alkyloxycarbonyl, aryl1carbonyl, aryl1C1-6alkylarbonyl C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR3, wherein R3 is hydrogen, C1-6alkyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl substituted with aryl2 and optionally with hydroxy, C1-4alkylcarbonylC1-4alkyl su

Abstract: A compound of the formula (I) or a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, an optically active compound thereof, a racemate thereof or a diastereomer mixture thereof has a superior tyrosine-specific protein kinase inhibitory activity and is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of various cancers, psoriasis or diseases caused by arteriosclerosis, and the like.

Abstract: A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are provided

Abstract: The present invention relates to dihydropyrazolo[1,5-a]pyrimidine and dihydroimidazo[1,5-a]pyrimidine derivatives, compositions comprising an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative and methods for treating or preventing cancer, comprising administering to a subject in need thereof an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative.

Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.