Abstract: A process for producing optically active succinimide derivatives as key intermediates of (3R)-2?-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4?(1?H)-pyrrolo[1,2-a]pyrazine}-1?,2,3?,5(2?H)-tetraone, which comprises the following reaction steps.

Abstract: This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.

Abstract: A process for producing optically active succinimide derivatives as key intermediates of (3R)-2?-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4?(1H)-pyrrolo[1,2-a]pyrazine}-1?,2,3?,5(2?H)-tetraone, which comprises the following reaction steps.

Abstract: The present invention provides a method for producing N-substituted carbamic acid-O-aryl ester derived from a compound having an ureido group, the method comprising the step of carrying out esterification or esterification and transesterification from the compound having the ureido group and a hydroxy composition containing one type or a plurality of types of hydroxy compounds.

Abstract: Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Inhibition of histone deacetylase can lead to the histone deacetylase-mediated transcriptional repression of tumor suppressor genes. For example, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, such as hematopoiesis, and genetic related metabolic disorders, such as, cystic fibrosis and adrenoleukodystrophy.

Abstract: The present invention provides a process for making N-alkoxy(or aryloxy)carbonyl isothiocyanate derivatives by reacting a chloroformate with a thiocyanate, in the presence of an aqueous solvent and a catalytic amount of a N,N-dialkylarylamine, to produce a N-alkoxy(or aryloxy)carbonyl isothiocyanate intermediate product, wherein the intermediate product is converted to a N-alkoxy(or aryloxy)carbonyl isothiocyanate derivative in high yield and purity.

Abstract: An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxamide, an intermediate for an HIV protease inhibitor.

Abstract: A process for producing an aryl carbamate of a high purity at a high yield by reacting a diaryl carbonate with an amine compound having one or more hydrogen atoms bonded to the N position in the presence of carboxylic acid(s) of the following general formulae (I): R.sup.1 --COOH and/or (II): R.sup.2 --COOH (wherein R.sup.1 represents an alkyl or cycloalkyl group having an .alpha.-positioned carbon atom bonded to only one hydrogen atom, an alkyl group having an .alpha.-positioned carbon atom bonded to no hydrogen atom, or an aryl or heterocyclic group, and R.sup.2 represents an alkyl group having an .alpha.-positioned carbon atom bonded to two or more hydrogen atoms).

Abstract: The present invention provides a process for making N-alkoxy(or aryloxy)carbonyl isothiocyanate derivatives by reacting a chloroformate with a thiocyanate, in the presence of an organic solvent and a catalytic amount of a N,N-dialkylarylamine, to produce a N-alkoxy(or aryloxy)carbonyl isothiocyanate intermediate product, wherein the intermediate product is converted to a N-alkoxy(or aryloxy)carbonyl isothiocyanate derivative in high yield and purity.

Abstract: An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxaimide, an intermediate for an HIV protease inhibitor.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalyzed reactions.

Abstract: The present invention relates to a novel process for preparing triazolinones of the general formula (I) ##STR1## in which R.sup.1 represents halogenoalkyl, andR.sup.2 represents hydrogen, hydroxyl or amino, or represents alkyl, alkenyl, alkinyl, alkoxy, alkylamino, dialkylamino, cycloalkyl, cycloalkylalkyl, phenyl or phenylalkyl which are in each case optionally substituted,and also to novel intermediates for preparing these triazolinones and to processes for preparing the intermediates themselves.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT).

Abstract: A process for the manufacture of N-protected .alpha.-aminoketones and N-protected .alpha.-aminoalcohols of the formula ##STR1## wherein X is halogen, one of Q.sup.1 and Q.sup.2 is hydrogen and the other is hydroxy or Q.sup.1 and Q.sup.2 together are oxo, R.sup.1 is an amino protecting group and R.sup.2 is hydrogen or the characterizing group of an .alpha.-aminocarboxylic acid,starting from the corresponding lower alkyl N-protected .alpha.-aminocarboxylates via corresponding lower alkyl N-silyl protected .alpha.-aminocarboxylates.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalyzed reactions.

Abstract: An N-hydroxycarbamate compound of the formula ROCONHOH in which R is C.sub.1-8 alkyl, C.sub.3-12 cycloalkyl, aryl or aralkyl group, is produced by reacting a carbonic acid diester of the formula ROCOOR in which R is as defined above, with hydroxylamine in the presence of a basic substance, for example, an alkali metal hydroxide or alkoxide.

Abstract: A compound of the following general formula which is useful in treating hypocholesterolemia and atherosclerosis: ##STR1## wherein X is oxygen or sulfur; R is hydrogen, alkyl having from 1 to 8 carbon atoms, or benzyl; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, a heterocyclic group, or a hydrocarbon chain of from 1 to 20 carbon atoms which is saturated or contains 1 to 3 double bonds and each of R.sub.2 and R.sub.3 is selected from hydrogen, provided both are not hydrogen, an aralkyl group, a hydrocarbon chain of from 1 to 20 carbon atoms which is saturated or contains 1 to 3 double bonds, an w-substituted alkylC.sub.1-6, a heterocyclic group, phenyl, substituted phenyl or NR.sub.2 R.sub.3 taken together form a monocyclic heterocyclic group.

Abstract: Antimicrobial compounds of the formula ##STR1## wherein R.sup.1 is selected from the group consisting of H, lower (C.sub.1 -C.sub.4)alkyl, alkyl aryl, CH.sub.2 OR, CH.sub.2 SR, and CH(CH.sub.3)OR; andR, R.sup.2, and R.sup.3 are independently selected from H, (C.sub.1 -C.sub.4)alkyl, aryl, arylalkyl, alkaryl, and halopropargyl.

Abstract: The ethylenically unsaturated organic compounds are of the general formula ##STR1## where R is alkyl, aryl or a radical R.sup.1, and R.sup.1 is a radical ##STR2## where R.sup.2 to R.sup.6 are each H, alkyl, OH, Oalkyl, SH, Salkyl, halogen, N(alkyl).sub.2 or N(alkyl)(aryl), and not less than one but not more than three of the radicals R.sup.2 to R.sup.6 are each a radical ##STR3## where X is alkylene or oxaalkylene, each of 2 to 10 carbon atoms, and Y is H or CH.sub.3. These compounds have particularly high photochemical reactivity in the medium-wavelength to relatively long-wavelength UV range.

Abstract: Alkoxy and aryloxy isothiocyanates are produced by the reaction of a haloformate and an alkali or alkaline earth metal thiocyanate in the presence of water and (i) a catalyst comprising a six membered mononuclear or ten membered fused polynuclear aromatic, heterocyclic compound having 1 or 2 nitrogen atoms as the only hetero atoms in the ring and (ii) a co-catalyst comprising an alkali metal or alkaline earth metal salt of an acid having a pKa of about 10.sup.-3 or below. The co-catalyst accelerates the reaction rate, increases product purity and reduces the adverse effects of impurities in certain grades of the thiocyanate reactants.

Abstract: The compounds of the present invention have the formula ##STR1## wherein each of X and Y is oxygen or sulfur, R is hydrogen or lower alkyl, and each of R.sub.1 and R.sub.2 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, aralkyl, a hydrocarbon chain, a hetero group, or a heteroalkyl group, and the compounds are useful in treating atherosclerosis.

Abstract: Disclosed is a novel route to diamines and triamines comprising reacting nitroalcohols with isocyanates to prepare di- and trinitro compounds which are subsequently reduced over a metal hydrogenation catalyst to the corresponding polyamino compound.

Abstract: The invention relates to rhodium complexes of the formula[A--O--(CH.sub.2 CH.sub.2 O).sub.n --A].sup.2+ 2X.sup.- (Ia)and[A--O--(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3 ].sup.+ X.sup.-(Ib)in whichn=5-1,000,m=5-250,X.sup.- denotes a tetrafluoroborate, hexafluorophosphate or per-chlorate anion,A denotes a radical of the formula ##STR1## (en).sub.2 denotes two molecules of a monoolefin or one molecule of a diolefinAr denotes phenyl or phenyl which is substituted by one or two alkyl groups having 1 or 2 carbon atoms andR.sup.1 denotes an arylene or alkylene bridge,and their use for the preparation of L-phosphinothricin and its derivatives by enantioselective catalytic hydrogenation of 2,3-dehydrophosphinothricin (derivatives).

Abstract: Poly(alkylene carbonate) monoahls and polyahls useful as nonionic surfactants and having a poly(alkylene carbonate) backbone are prepared by reacting an oligomeric poly(alkylene carbonate) polyahl with a compound having mono- or difunctional active hydrogen moieties, such as alcohols, carboxylic acids, mercaptans, amides, primary or secondary amines, or substituted phenols, optionally in the presence of a catalyst, under transesterification conditions.

Abstract: Polyunsaturated compounds useful in radiation curable compositions are made by reacting p-vinylphenol and a polyisocyanate in the ratio of one mole of p-vinylphenol for each isocyanate group of the polyisocyanate.

Abstract: A physical property-improving reagent which comprises an alkenoylcarbamate compound of the formula: ##STR1## wherein R is a hydrogen atom or a lower alkyl group, X is an oxygen atom (--O--), a sulfur atom (--S--) or a substituted or unsubstituted imino group (--NR'--), R' being a hydrogen atom or a lower alkyl group, and Y is the residue of an active hydrogen atom-containing compound excluding --X-H therefrom dissolved in an organic solvent having a solubility parameter of not less than 8, which can impact excellent physical properties to a polymer produced with the same.

Abstract: Compounds having the formula: ##STR1## wherein R.sup.1 is --NH(C.dbd.O)OR.sup.5, --NH(C.dbd.NH)NH.sub.2 or --NH(C.dbd.N--NO.sub.2)HN.sub.2 ; R.sup.2 is hydrogen, C.sub.1-8 alkyl or C.sub.6-8 aryl; n is 2 to 6; and R.sup.5 is hydrogen,C.sub.1-8 alkyl, C.sub.6-8 aryl, or C.sub.7-8 alkaryl; are disclosed in addition to methods to employ such compounds to induce migration of endothelial cells into denuded areas of vessel lining and to treat malignant hypercalcemia.

Abstract: A method for producing aliphatic O-arylurethanes by the reaction of an aliphatic primary amine with an aromatic hydroxyl compound and urea. Ammonia produced as a by-product in the reaction is removed during the reaction so that the ammonia concentration of the reaction solution is maintained at 2 wt % or less.

Abstract: The present invention relates to isocyanto-acylurethanes corresponding to Formula I ##STR1## wherein R has a valency of m+n and is a hydrocarbon group,R' is a hydrocarbon group andm and n may be identical or different, and each have a value of 1 or 2.The present invention also relates to a process for preparation of these isocyanato-acylurethanes which comprises reacting isocyanato-carboxylic acid chlorides with carbamic acid esters. Finally, the present invention is directed to the use of these isocyanato-acylurethanes as intermediate products for the production of thermally cross-linkable synthetic resins or synthetic resin precursors and also as intermediate products for the preparation of cross-linking agents for synthetic resins.

Abstract: A method of combating endoparasites which comprises applying thereto or to an endoparasite habitat an endoparasiticidally effective amount of an N-organooxycarbamic acid ester of the formula ##STR1## in which R.sup.1 represents alkyl, cycloalkyl, alkenyl, alkinyl or aryl, which can optionally be substituted,R.sup.2 represents alkyl, alkenyl or alkinyl, which can optionally be substituted, andR.sup.3 represents alkyl, alkenyl or alkinyl, which can optionally be substituted.Those compounds wherein one of R.sup.2 and R.sup.3 is alkinyl are new.

Abstract: The subject of the invention is a novel procedure for the preparation of the compounds of formula I: ##STR1## in which n varies in particular from 2 to 5 and R represents Cl, Br or FZ represents in particular hydrogen, characterized in that the halogenoformate of formula II: ##STR2## R and n having the meanings indicated above, Y representing a halogen, is made to react with NH.sub.2 CH.sub.2 CH.sub.2 Cl to form the compound of formula Ia: ##STR3## in which R has the meanings indicated above, and in that the compound Ia is treated directly with nitrosylsulfuric acid.

Abstract: Prepare .alpha., .beta.-saturated geminal biscarbamates by contacting an .alpha.,.beta.-unsaturated ether with a carbamate under reaction conditions, optionally in the presence of a catalyst.

Abstract: The molecule of the new urethanes contains an aliphatic fluoroalcohol, an isocyanate and an aromatic dihydroxy, diamino, aminohydroxy, aminocarboxy or hydroxycarboxy compound. They are prepared by reacting an aliphatic fluoroalcohol with a diisocyanate or triisocyanate to give the fluoroalcohol/isocyanate adduct and by reacting this adduct with said aromatic compound to give the desired urethanes composed of an aliphatic fluoroalcohol, an isocyanate and the bifunctional aromatic compound mentioned, and also be reacting a urethane of this type which also carries an active hydrogen atom on the bifunctional aromatic compound, with an isocyanate compound containing one or more isocyanate groups. The new urethanes are preferably used for imparting an oleophobic and hydrophobic finish to textiles and leather.

Abstract: Alkoxy and aryloxy isothiocyanates are produced by the reaction of a haloformate and an alkali or alkaline earth metal thiocyanate in the presence of water and a catalyst comprising a six membered mononuclear or ten membered fused polynuclear aromatic, heterocyclic compound having 1 or 2 nitrogen atoms as the only hetero atoms in the ring.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 denote alkyl, OH, CF.sub.3 or cyanoethyl, A preferably denotes --COOH, R.sub.3 denotes inter alia alkoxycarbonylalkoxy, fairly high-molecular (>C.sub.12) alkoxy, alkylcarbonylalkoxy or nitrobenzyloxy, are valuable herbicides and growth regulators.

Abstract: An addition polymerizable antioxidant is prepared by reacting an isocyanatoalkyl ester of an addition polymerizable carboxylic acid (2-isocyanatoethyl methacrylate) with an antioxidant functionality bearing an active hydrogen moiety which is reactive with the isocyanate.

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, halogen, C.sub.1-6 alkyl, or haloalkyl; R.sub.4 is hydrogen; C.sub.1-4 alkyl, alkenyl, alkoxy, haloalkyl; C.sub.1-2 alkylamino, C.sub.1-2 alkylthio, C.sub.2-4 cycloalkyl, C.sub.2-6 alkoxyalkyl, C.sub.2-6 alkylthiomethyl, amino, phenoxy, phenamino, or furan; and R.sub.5 is hydrogen or C.sub.1-4 alkyl, are useful to retard the growth of turf grass.

Abstract: A stable copolymer dispersion is prepared by addition copolymerization of (1) a monomeric adduct of an active hydrogen compound, e.g., a polyether polyol or polyether monool, and an ethylenically unsaturated N-chlorosulfonyl carbamyl compound such as acryloxyethylchlorosulfonylcarbamate or an unsaturated N-chlorocarbonyl carbamyl compound with (2) ethylenically unsaturated monomer(s), e.g., styrene or a mixture thereof with acrylonitrile, while (1) and (2) are dispersed or dissolved in an excess of an active hydrogen polyfunctional compound such as a polyether polyol. The molar ratio of carbamyl moiety to active hydrogen compound is preferably less than about 0.1:1. The resulting dispersion has a controlled particle size and a viscosity such that it is suitably employed in the production of polyurethane foams.

Abstract: A process for preparing insecticidal N-acyl-tetrahydro-2-nitromethylene-2H-1,3-thiazines, intermediates involved therein and certain of the products.

Abstract: The invention concerns new 1-tert.-alkyl-thiohydrazine-1,2-dicarboxylic a derivatives, their production, and their use as reagents for the transfer of a 1-tert.-alkylthio residue, particularly of a 1-tert.-butylthio residue as a protective group for thiols.

Abstract: Carbamate-sulfenyl-carbamoyl fluoride compounds are valuable insecticidal compositions and are also useful intermediates in the production of bis-carbamate compounds.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 denote alkyl, CF.sub.3, benzyl cyclohexyl, cyanoethyl, phenyl or OH and A denotes, inter alia, the groups --CO--, CHOH or CH--NH.sub.2 and --COR.sub.3 denotes a carboxyl, carboxylic ester or carboxamido group, are active herbicides.

Abstract: Unsymmetrical N-substituted bis-carbamoyl sulfide compounds exhibit exceptional broad spectrum pesticidal activity coupled with extremely low mammalian toxicity and phytotoxicity.

Abstract: The present invention relates to a process for the preparation of N-substituted imido-dicarboxylic acid diaryl ester compound of the formulaR.sup.1 --N(CO--OR.sup.2).sub.2 (I)whereinR.sup.1 is an optionally substituted aliphatic, cycloaliphatic, araliphatic, aromatic or heterocyclic radical; andR.sup.2 is an optionally substituted aryl radical, which are useful as intermediates for the production of known herbicides, which process comprises reacting a primary amine of the formulaR.sup.1 --NH.sub.2 (II)with a carbonic acid aryl ester halide of the formulaX--CO--OR.sup.2 (III)wherein X is a halogen atom, at a temperature between 100.degree. and 300.degree. C.

Abstract: Bis-sulfenylated bis-carbamate compounds exhibit activity against insect and mite pests.

Abstract: N-substituted N-isocyanatocarbonyl-carbamates, some of which are new, of the general formula ##STR1## are prepared by reacting an N-substituted carbamic acid ester of the general formulaR--NH--COOR.sup.1 (II)with chlorocarbonyl isocyanate of the formulaCl--CO--NCO (III)in a diluent, at a temperature between 50.degree. and 200.degree. C. The compounds (I) can be used as intermediate products for the preparation of new pest-combating agents.

Abstract: N-Sulphenylated biuret-N"-carboxylic acid esters of the general formula ##STR1## in which R.sup.1 and R.sup.2 can be identical or different and represent an optionally substituted aliphatic, cycloaliphatic, aromatic or araliphatic radical,R.sup.3 represents a hydrogen atom or an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical andR.sup.4 represents a trihalogenomethyl radical,are obtained by the reaction of an acyl isocyanate of the general formula ##STR2## with a sulphenamide of the general formula ##STR3## if appropriate in the presence of a diluent. The compounds of the formula (I) are new. They can be used as pest-combating agents which are microbicides, especially fungicides or bactericides.

Abstract: Novel N-substituted imido-dicarboxylic acid diaryl ester compounds of the general formula ##STR1## in which R.sup.1 represents an optionally substituted aliphatic, cycloaliphatic, araliphatic, aromatic, heterocyclic radical andR.sup.2 and R.sup.3 can be identical or different and represent an optionally substituted aryl radical,and a process for their preparation characterized in that a carbamic acid aryl ester of the general formula:R.sup.1 --NH--CO--OR.sup.2 (II)in which R.sup.1 and R.sup.2 have the abovementioned meanings, is reacted with a carbonic acid aryl ester halide of the general formulaX--CO--OR.sup.3 (III)in whichR.sup.3 has the abovementioned meaning andX represents a halogen atom, optionally in the presence of a diluent, optionally at a temperature between 100.degree. and 300.degree. C.The new compounds (I) can be used as intermediate products for the preparation of known herbicidal active compounds from the 1,3,5-triazine,2,4-(1H,3H)-dione series.