Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).

Abstract: A compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2 or NR10 where R10 is hydrogen or C1-6 alkyl, and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are various specified organic groups. These compounds are inhibitors of aurora 2 kinase, and are useful in the treatment of cancer.

Abstract: Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein which are useful in treating leukocyte activation-associated disorders.

Abstract: 5-Halogen-6-phenyl-7-fluoroalkylamino-triazolopyrimidines of formula I: (I) in which R1 is hydrogen, fluoro, alkyl, alkenyl, alkynyl, alkadienyl, where the carbon chains of these radicals may be unsubstituted or substituted as defined in the description; R2 is hydrogen, alkyl, alkenyl, alkynyl, alkadienyl, where these radicals may be unsubstituted or substituted; R3 is fluoroalkyl or fluoroalkenyl; X is halogen; n is 0 or an integer from 1 to 4; L each independently is halogen, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy. Processes for their preparation, compositions containing them and to their use for combating phytopathogenic fungi.

Abstract: The invention provides a compound of the formula: wherein A is selected from N, CH and CR; R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH2, NHR1, NR1R2 and SR3; R1, R2 and R3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from NH2 and NHR4; R4 is an optionally substituted alkyl, aralkyl or aryl group; X is selected from H, OH and halogen; Z is selected from H, Q, SQ and OQ; Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer, a pharmaceutically acceptable salt, an ester, or a prodrug thereof; with the proviso that the stereochemistry of the aza-sugar moiety is D-ribo or 2?-deoxy-D-erythro-; pharmaceutical compositions comprising said compound; and methods of treatment using said compound.

Abstract: The invention provides 5,8-dihydro-6H-pyrido[2,3-d]pyrimidin-7-one compounds that are selective inhibitors of KDR and FGFR kinases, and are useful in the treatment of cancers. The compounds have the generic structure I where Ar, Ar?, and R1 are as set forth in the present specification. The invention also provides pharmaceutical compositions containing these compounds and methods for their use.

Abstract: Use of a compound of the formula (I) wherein R1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR7R8, NR6COR7, NR6CO2R9 and NR6SO2R9; R2 is selected from aryl attached via an unsaturated carbon; R3 and R4 are independently selected from H, alkyl, halogen, alkoxy, alkylthio, CN and NR7R8; R5 is selected from H, acyclic alkyl, COR6, CONR7R8, CONR6NR7R8, CO2R9 and SO2R9; R6, R7 and R8 are independently selected from H, alkyl and aryl or where R7 and R8 are in an NR7R8 group R7 and R8 may be linked to form a hererocyclic group, or where R6, R7 and R8 are in a (CONR6NR7R8) group, R6 and R7 may be linked to form a hererocyclic group; and R9 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the manufacture of a medicament for the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder

Abstract: This invention describes novel pyrazole compounds of formula III: 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, 5–8 membered carbocyclo ring; 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: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are independently hydrogen, C1–C4 alkyl, C1–C4 substituted alkyl, C1–C4 alkoxy, C1–C4 substituted alkoxy, C1–C4 acyl, halogen, cyano, nitro, amino, alkylamino, or dialkylamino; R3, R4, R5, R6, R7, and R8 are independently CH or nitrogen; R9 is hydrogen or methyl; R10 is C?O or (CH2)n; where n is 0, 1, 2, 3, or 4; R11 and R12 are independently nitrogen or CH; X1 and X2 are independently hydrogen, deuterium, tritium or halogen; and X3 is N; and their pharmaceutically acceptable salts; compositions thereof. 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: Disclosed are a method for producing fungicidal triazolopyrimidine compounds, agents containing said compounds, and the use thereof for controlling harmful fungi. Also disclosed are triazolopyrimidines of formula (I), in which the substituents have the following meaning: L1 represents alkyl; L2 represents halogen; L3represents hydrogen or halogen; X represents halogen, cyano, alkyl, alkoxy, or haloalkoxy; R1, R2 represent hydrogen, alkyl, haloalkyl, cycloalkyl, alkenyl, alkadienyl, alkinyl, or cycloalkinyl, phenyl, naphthyl, or a five-unit to ten-unit saturated, partially unsaturated, or aromatic heterocycle containing one to four heteroatoms from the group O, N, or S, R1 and R2 can also form a five-unit or six-unit ring along with the nitrogen atom to which they are linked. Said ring can be interrupted and/or substituted by an atom from the group O, N, and S while R1 and/or R2 can be substituted according to the description.

Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.

Abstract: Compounds of formula I are described. These compounds are protein kinase inhibitors, in particular they inhibit the src family tyrosine kinases. Thus, these compounds are useful for the treatment of diseases mediated by src tyrosine kinases, including cell proliferative disorders such as cancer. Also described are methods of making and using compounds of formula I as well as pharmaceutical compositions containing these compounds.

Abstract: The present invention discloses compounds corresponding to formula wherein A, R, X, Y, R, R1 and R2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: A method of monotherapy for a subject suffering from abnormal cell growth expressing the epidermal growth factor receptor (EGFR) which comprises orally administering to the subject a therapeutically effective amount of a crystalline polymorph of the hydrochloride salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine so as to treat the subject.

Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.

Abstract: Use of a compound of formula (I): wherein R1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5COR6, NR5CONR6R7, NR5CO2R8 and NR5SO2R8; R2 is selected from heteroaryl attached via an unsaturated carbon; R3 is selected from H, alkyl, halogen, OR5, SR5 and NR6R7; R4 is selected from H, acyclic alkyl, CONR6R7, CONR5NR6R7, COR6, CO2R8 and SO2R; R5, R6 and R7 are independently selected from H, alkyl and aryl, or where R6 and R7 are in an NR6R7 group, R6 and R7 may be linked to form a heterocyclic group, or where R5, R6 and R7 are in a (CONR5NR6R7) group, R5 and R6 may be linked to form a heterocyclic group; and R8 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or s

Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) —(CH2)jO(CH2)nR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —(CH2)jCON(R10)2; g) —(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; R8, R9a, R9b, and R10 are each independently hydrogen, C1–C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; j is an index from 0 to 5,

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: A device for supplying air or medical gases in a conditioned, particularly a moistened and/or heated state to a patient, through an air pipe. The device includes at least one component to be connected to said air pipe, the component being formed by a cylinder-shaped element with an inner tube through which the moistened air flows, which cylinder-shaped element is fitted with self-regulating heating resistors which heat the air flowing through the tube, while the cylinder-shaped tube from one element at least is filled with a material which adsorbs or absorbs the water supplied by a water-supply line from a container, and has a good air-permeability.