Abstract: The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, or enantiomeric and diasteriomeric forms or pharmaceutically acceptable salts thereof, have the formula: wherein R is an ether or amino unit, R1 is substituted phenyl, each R2 and R3 unit is independently selected from the group consisting of: a) hydrogen; and b) substituted or unsubstituted C1-C10 hydrocarbyl selected from the group consisting of: i) C1-C10 linear, branched or cyclic alkyl; ii) C1-C10 aryl; iii) C1-C10 heterocyclic; iv) C1-C10 heteroaryl.

Abstract: An aromatic carboxylic acid bicyclic sulfur compound of the formula (II): wherein X1 is a C1 to C4 alkyl, a halogen, a C1 to C4 haloalkyl, a C2 to C4 alkoxyalkyl, a C1 to C4 alkoxy or a C1 to C4 haloalkoxy; X2 is a hydrogen, a C1 to C4 alkyl or a C1 to C4 haloalkyl, or X2 forms a bond with X5; X3 is a hydrogen, a C1 to C4 alkyl or a C1 to C4 haloalkyl; X4 is a hydrogen, a halogen, a C1 to C4 alkyl, a C1 to C4 haloalkyl or a C1 to C4 alkoxy; X5 forms a bond with X2 or X5 forms a bond with X7; each of X6 and X8 is independently a hydrogen or a C1 to C4 alkyl or forms a bond with X5; p is 1; and n is 0, 1 or 2; or a salt thereof.

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R represents hydrogen, C1-10alkyl, haloC1-10alkyl or aryl; which are useful intermediates in the preparation of morpholine derivatives of formula (A). Compounds of formula (A) are useful as therapeutic agents.

Abstract: The present invention provides pyrazole and pyrazolone derivatives. Preferred compounds of the invention are useful as RNA polymerase inhibitors. Further preferred compounds of the invention are useful as antimicrobial agents.

Abstract: The present invention provides a series of compounds having structural formulas wherein n1 is 1 to 5, n2 is 1 to 4 and m is 1 to 3; X is O or NH; Y is CH2, O, S, NH, NR; R is selected from the group consisting a straight-chain aliphatic group, a branched-chain aliphatic group and an alicyclic group; wherein R′ is selected from the group consisting of hydrogen, methyl and ethyl; when Y is O, n1 is not 1; and wherein X and R′ are independently optionally substituted at C2, C3 or C4 in compounds of Fomula IV or a pharmaceutically acceptable salt thereof. Also provided is a method of inactivating antigen-specific T cells in an individual.

Abstract: The invention concerns a one-pot reaction for the preparation of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitroquinazolin-4-yl]-amine (I) or of (3-chloro-4-fluorophenyl)-[7-(3-morpholino-4-yl-propoxy)-6-aminoquinazolin-4-yl]-amine (VII)

Abstract: An object of the present invention is to provide a material having spectroscopic properties, light resistance, solubility and thermal decomposition properties suitable for recording for DVD-R. More specifically, the present invention provides squarylium compounds in a state of a metal complex represented by the general formula (I): wherein, R1 and R2 are the same or different, and represent an alkyl group optionally having a substituent, an aralkyl group optionally;,having a substituent, an aryl group optionally having a substituent, or a heterocyclic group optionally having a substituent; Q represents a metal atom with a coordination ability; q represents 2 or 3; and A represents an aryl group optionally having a substituent, a heterocyclic group optionally having a substituent, or Y═CH— wherein Y represents an aryl group optionally having a substituent or a heterocyclic group optionally having a substituent.

Abstract: The present invention is directed to a benzoxazole compound represented by the following formula (1): (wherein R1 represents an alkyl group, a C6-10 aryl-C1-8 alkyl group, etc.; each of R2 and R3, which are identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; and n represents a number of 1 to 3) or a salt thereof and to a pharmaceutical compound containing the same. These compounds electively activate PPAR&agr;.

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

Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

Abstract: Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.

Abstract: Compounds represented by the following formula (I): wherein R1 represents a lower alkenyl group or a phenyl group which may be substituted, R2 and R3 independently represent a phenyl group which may be substituted or salts thereof, and a plant growth regulator which comprises said compound or a salt thereof as an active ingredient.

Abstract: A compound of general formula (I) and physiologically acceptable salts wherein R represents phthalidyl, (2-oxo-5-methyl-1,3-diox-olen-4-yl)methyl or the group CHR4 OCO(O)pR5 wherein R4 is hydrogen or C1-4 alcyl, p is zero or I, R5 is C1-6 alkly, C5-8 cycloalyl (optionally substituted by C1-3 alkyl or carboxyl), C1-4 alkyl substituted by C1-3 alkoxy or carboxy), C1-4 alkyl substituted by one or more groups selected from amino, (C1-4 alkylamino di(C1-4 alkyl)amino or carboxyl, phenyl (optionally substituted by carboxyl or aminoalkyl, C1-4 alkylaminoalkyl or di(C1-4 alkyl)aminoalcyl, or R5 is a 5-8 membered heterocyclic group containing 1 or 2 heteroatoms selected from oxygen or nitrogen, processes for their preparation, pharmaceutical compositions containing them and their use in medicine.

Abstract: 3-(4,5-Dihydroisoxazol-5-yl)benzoylcyclohexenones of the formula I in which the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl or C1-C6-haloalkylsulfonyl; R3 is hydrogen, halogen or alkyl; R4 is hydrogen or alkyl; R5, R6 are hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl, benzyl or carbonyl, it being possible for the 7 last-mentioned radicals to be substituted; R11 is unsubstituted or substituted cyclohexenone which is linked in position 2 and has attached to it in position 1 a hydroxyl radical or derivatives thereof; and their agriculturally useful salts, processes for the preparation of the 3-(4,5-dihydroisoxazol-5-yl)benzoylcyclohexenones, compositions comprising them, and the use of these derivatives or of compositions comprising them for controlling undesired plants.

Abstract: A class of 3-phenylimidazo(1,2-a)pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, CO2Ra, —CONRaRb or —CRa═NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group.

Abstract: The present invention relates to certain 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives that inhibit kinases, in particular VEGFR and/or PDGFR kinases. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.

Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may be, for example, iso-butyl, wherein X and Y, same or different, may be, for example, NH2 and F, and wherein R2 and R3 are as defined herein.

Abstract: A method of controlling parasites in or on an animal comprising orally administering to the animal a parasiticidally effective, substantially non-emetic 1-arylpyrazole.

Abstract: A photochromic naphthopyran of formula (I) wherein R1 through R15, which may be the same or different, are independently selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen, C1-C4 alkylcarbonyloxy, benzoyloxy, C3-C6 cycloalkyl, phenyl, and NR16R17, wherein R16 and R17 are each C1-C4 alkyl or together with the N atom form a 5-12 membered monocyclic or polycyclic ring having, optionally, one or more further heteroatoms; R is hydrogen, alkyl or alkoxy; and >C(CnH2n=1) (CmH2m=1) is a tert-alkylene grup, wherein n and m are integers from 1 to 5.

Abstract: The present invention relates to 5-heterocyclo-pyrazoles of the formula I: wherein ring W, m, n, and R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.