Abstract: The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.

Abstract: Disclosed is a process for forming an N-acylamino pyrazole comprising contacting a N-acyl-3-oxo-imino ether compound either with a salt of hydrazine in the presence of a base or with hydrazine.

Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

Abstract: A benzimidazole compound or a salt thereof which has an inhibitory action of forming of macrophages and is useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of arteriosclerosis, which is represented by the formula (I): wherein, R1 represents a functional group on the benzene ring selected from the group consisting of hydrogen atom, a halogen atom, a lower alkyl group and a lower alkoxy group; R2 represents hydrogen atom, an alkyl group or an acyl group; R3 represents a functional group on the ring containing the nitrogen atom and Z; Z represents a divalent group which forms a 5- or 6-membered ring; L represents a C4-C8 alkylene group or an ethyleneoxy linking group represented by (CH2CH2O)nCH2CH2 wherein n represents 1 or 2; and X represents O or S.

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract: The present invention relates to compounds of the formulae (Ia) and (Ib) wherein R1 represents C1-10 alkyl which may be unsubstituted or substituted with halogen, or represents C2-4 alkoxyalkyl, C2-4 hydroxyalkyl, C3-6 cycloalkyl, hydroxy, C1-9 alkoxy which may be unsubstituted or substituted with halogen, or represents C3-6 cycloalkoxy, C2-4 alkoxyalkoxy or C3-4 alkynyloxy, and R2 represents hydrogen, C1-4 alkoxycarbonyl, C1-3 alkylcarbonyl or C2-4 alkoxyalkyl, to processes for their preparation and to their use for controlling animal pests.

Abstract: The invention relates to novel 3-oxo-2,1-benzisomazol-1(3H)-carboxamides (I), where R1, R2 are the same or different and independently=H, halogen, C1 C6 alkyl C1 C6 alkoxy, C1 C3 perfluoroalkyl, or a group NR5R6; R3, R4 are the same or different and independently=C1 C8 alkyl, whose carbon chain is optionally interrupted by an O, S or NR7 and is optionally singly or severally substituted by C3 C6 cycloalkyl, C1 C4 alkoxy, OH, halogen or NR8R9; C3 C8 cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR10 and is optionally singly or severally substituted by C1 C4 alkoxy, OH, halogen or NR11R12, or R3 and R4 together with a nitrogen atom form a saturated or partially unsaturated 3- to 10-membered mono- or bi-cyclic heteocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C1 C4 alkyl, C1 C4 alkoxy, OH, halogen, COOR13 or NR14R15 and X=O or S.

Abstract: The invention relates to novel pyrazolyl benzyl ethers, to a plurality of processes for their preparation and to their use for controlling harmful organisms.

Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders.

Abstract: The invention relates to hetaryl-substituted benzyl phenyl ethers of formula (I) in which the substituents have the following meanings: (Q): C(═CHOCH3)—COOCH3, C(═CHCH3)—COOCH3, C(═NOCH3)—COOCH3, C(═NOCH3)—CONHCH3, N(—OCH3)—COOCH3 or a group F, G, H or J, whereby # characterizes the bond with the phenyl ring, and (X) five-linked heteroaryl which is optionally substituted by a group Y2p and which contains one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom. The invention also relates to the salts of the inventive hetaryl-substituted benzyl phenyl ethers, to the production of compounds (I), and to the use of compounds (I) for combating harmful fungi and animal pests.

Abstract: Provided are processes for the preparation of the compound of the formula wherein R1, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, hydroxyl, nitro, lower alkyl, lower alkoxy, carboxy, C1-C6 trihaloalkyl, and cyano; and R2 is amino or lower alkyl. Also provided are synthetic intermediates that are useful as intermediates in the preparation of the compound of the formula 1.

Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioaryl-alkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is sele

Abstract: A new series of derivatives of 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid and their synthesis have been discovered. Surprisingly, by modifying the substituent of the 3-carboxylic acid group, new compounds were produced with high activity as PAF receptor antagonists. These compounds were shown to protect neurons from brain damage that normally occurs in response to stroke and other cerebrovascular diseases. These compounds are also protective against edema generation resulting from traumatic breakdown of the blood-brain barrier. Moreover, these compounds were found to be non-toxic and cytoprotective of cells undergoing oxidative stress that would normally trigger apoptotic cell death; and to have activity as (a) antagonists of an intracellular platelet activating factor (“PAF”)-binding site, (b) inhibitors of PAF- and cytokine-mediated c-aminoterminal jun kinase (JNK) and extracellular regulated kinase (ERK), and (c) transcriptional inhibitors of COX-2 expression.

Abstract: Pyrazoles of the formula I where: R1 is hydrogen, nitro, halogen, cyano, thiocyanato or an aliphatic radical; R2 is a substituted sulfur, nitrogen or phosphorus atom; R3 is hydrogen, halogen or an aliphatic radical; R4, R5 are hydrogen, nitro, halogen, cyano, thiocyanato, or an aliphatic radical; R6 is hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C3-C8-cycloalkyl; R7, R8, R9 are hydrogen, C1-C6-alkyl, but at most one of the radicals R7, R8 and R9 is hydrogen; and their tautomers and agriculturally useful salts are described. Moreover, the invention relates to processes for preparing compounds of the formula I, to compositions comprising them and to the use of the compounds of the formula I and of the compositions comprising them for controlling harmful plants.

Abstract: The present invention relates to intermediate thiazole compounds and a process for preparing 2-chloro-5-chloromethylthiazole which is a known compound useful for the preparation of insecticides.

Abstract: The invention provides compounds of Formula I: compounds of the Formula I: wherein R1, R2, R4, R6, X, and W are defined herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which &agr;7 is known to be involved.

Abstract: A carbazole wherein R1, R2, R3, and R4 are independently a hydrocarbyl, and wherein Ar is an aryl.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA) X2—CH2—C*H(OH)—CH2—NH—CO—RN  (VIIIA) and processes for production of pharmacologically useful oxazolidinones.

Abstract: The invention relates to novel pyrazolyl benzyl ethers, to a process for their preparation and to their use for controlling harmful organisms.

Abstract: A method treating or preventing inflammatory and immune cell-mediated diseases by the administration of certain novel and known small molecules.