Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.

Abstract: N-substituted perhydro-2,3-diazines of the formula I in which the variables Z, R, m and RA are as defined in claim 1, a process for their preparation and the use of the compounds of the formula I as starting materials for preparing herbicides of the formula V in which R, RA, Z and m are as defined above, X is O or S and Q is a C6-C14-aromatic radical are described.

Abstract: Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.

Abstract: A process for the preparation of 6-(2,3-dichlorophenyl)-1,2,4-triazine-3-5-diamine (lamotrigine) of the formula I: 2,3-Dichloronitrobenzene in C1-C6 aliphatic alkanol is hydrogenated at 55-90 psi gas pressure using metal catalyst at 27-35° C. 2,3-Dichloroaniline is diazotised and cyano-de-diazonised with metal cyanide at 65-80° C. 2,3-Dichlorobenzonitrile is hydrolysed and 2,3-dichlorobenzoic acid is chlorinated at 55-130° C. Cyano-de-halogenation of 2,3-dichlorobenzoyl chloride is carried out with a metal cyanide and alkali metal iodide by refluxing in an aprotic solvent under an inert atmosphere. 2,3-Dichlorobenzoyl cyanide is condensed with aminoguanidine bicarbonate in an organic solvent in acidic conditions using catalyst at 90-125° C. followed by insitu cyclisation of the Schiff's base by refluxing in an aliphatic alkanol with base. Crude lamotrigine is purified.

Abstract: Compound of formula (I): wherein: R1 represents hydroxy, RCO—O— or RCO—NRa—, R2 represents hydrogen, halogen, or hydroxy, R′CO—O or R′CO—NR′a—, R and R′, which may be identical or different, represent linear or branched (C1-C6)alkyl optionally substituted by aryl, linear or branched (C2-C6)alkenyl optionally substituted by aryl, linear or branched (C1-C6)perhaloalkyl, (C3-C7)cycloalkyl, adamantyl, aryl or heteroaryl, Ra and R′a, which may be identical or different, represent hydrogen or linear or branched (C1-C6)alkyl, linear or branched (C1-C6)perhaloalkyl, linear or branched (C1-C6)acyl, aryl or heteroaryl, its isomer and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as AMPA modulators.

Abstract: This invention relates to the use as catalyst for the cyclotrimerization reaction of isocyanates of a hydrogencarbonate of a cation which either as it is or in the form complexed with a complexing agent has an average molecular or ionic radius of more than 1 Å, preferably greater than 1.5 Å, and which is at least partially soluble in the reaction medium. The invention also relates to a method of preparing (poly)isocyanurate polyisocyanates by catalytic cyclotrimerization of isocyanates, in which a catalytic system is used which comprises a cyclotrimerization catalyst based on a quaternary ammonium salt as catalyst and imidazole as cocatalyst.

Abstract: Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or tri-alkyl-silyl, formyl or alkoxycarbonyl, wherein R1 groups are unsubstituted or substituted as defined in the specification; R2 represents phenyl, cycloalkyl or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which are unsubstituted or substituted; R3 represents hydrogen, halogen or alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; which are unsubstituted or substituted; R4 represents hydrogen or alkyl, alkenyl or alkynyl; which are unsubstituted or substituted; and X represents O, S, NR5 or a single bond, wherein R5 represents hydrogen or alkyl; or R1 and R5 together with the interjacent nitrogen ato

Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted  m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—,  phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinso

Abstract: Amino-pyrimidine and amino-triazine derivatives having 5-HT7 antagonist activity for the treatment of sleeping disorders, depression, schizophrenia, anxiety, obsessive compulsive disorders, circadian rhythm disorders, ocular disorders and/or centrally and peripherally mediated hypertension are provided.

Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which m, n, Q, R1, R2, R3, R4, R5, X and Y are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides.

Abstract: A [5-chloro-6-phenyl-2-(4-trifluoromethylphenyl)-4-pyrimidinyl-amino]acetamide derivative of the formula (I): wherein R1 is a methyl group or a cyclopropyl group, and a pharmaceutical composition containing the same. Said compounds exhibit a potent anti-rheumatoid activity and show low toxicity, and hence, they are useful as an agent for prophylaxis or treatment of immuno inflammatory diseases such as rheumatoid diseases (e.g., rheumatoid arthritis, Behcet disease, ankylosing spondylitis, etc.) and autoimmune diseases (e.g., multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, etc.).

Abstract: There is disclosed a process for continuously producing an aromatic carboxylic acid comprising the steps of (A) subjecting a poly-alkyl aromatic hydrocarbon to a liquid-phase oxidation by continuously supplying an oxidation reactor with said hydrocarbon, a catalyst, a reaction accelerator, acetic acid containing water and a gas containing molecular oxygen; (B) continuously taking out from the oxidation reactor, the reaction products containing aromatic carboxylic acids, and separating the same into crude aromatic carboxylic acids and acetic acid containing water; and (C) continuously taking out from the oxidation reactor, the oxidative reaction exhaust gas containing evaporated acetic acid containing water, introducing the above gas in a condenser, and condensing the above evaporated acid, wherein acetic acid containing water is supplied to an oxidative reaction exhaust gas inlet line leading to the condenser.

Abstract: Novel 2-alkoxy-5-methoxypyrimidines and tautomeric forms thereof and also processes for preparing them are described. The 2-alkoxy-5-methoxypyrimidines according to the invention can be synthesized in few reaction steps and in high yields from simple precursors.

Abstract: A process for producing 3-phenyl-2,4(1H,3H)-pyrimidinediones having the general formula I and their salts which comprises reacting the isocyanates represented by the general formula (II) and the substituted hydrazono esters represented by the general formula (III) in the presence of a base. These compounds are useful as herbicides, defoliants and desiccants.

Abstract: The invention relates to new substituted acylaminophenyl-uracils of the general formula (I) in which n, A, Ar, Q1, R1, R2, R3, R4, R5 and R6 have the meanings given in the description, and to a process for their preparation, and to their use as herbicides.

Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by a (cyano)(fluoro)phenyl moiety, being selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.

Abstract: Compounds of the formula where the symbols are as defined in the specification, have retinoid agonist, antagonist or negative hormone-like biological activity.

Abstract: Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.

Abstract: The present invention concerns a new general process for asymetric hemisynthesis of harringtonines and their analogs, that are alcaloids used in chimiotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and fonctionalization are entirely preformed.