Abstract: The present invention relates to epothilon derivatives and to their use.

Abstract: A hair-treating composition containing a diester or polyester of a naphthalene dicarboxylic acid having compound formula (I) or (II), or mixtures; for imparting gloss and/or hair color stabilization: wherein each R1, same or different, is an alkyl group having 1 to 22 carbon atoms, a diol having the structure HO—R2—OH, or a polyglycol having the structure HO—R3—(—O—R2—)m—OH, wherein R2 and R3, same or different, are each an alkylene group, sight chain or branched, having 1 to 6 carbon atoms, and wherein m and n are each 1 to about 100, or a mixture thereof. These diesters and polyesters of formula (I) or (II) are quite effective in stabilizing the dibenzoylmethane derivative UV-A filter compounds making them more effective, and effective for longer periods of time.

Abstract: Compounds characterized generally as amino acyl amino propargyl diol derivatives are useful as renin inhibitors for the treatment of a renin-mediated disease Compounds of particular interest are those of Formula I wherein A is selected from CO and SO2; wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, &bgr;,&bgr;&bgr;-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R5 is selected from hydrido, alkyl, pyrazolealkyl, pyridylalkyl, thiazolylalkyl, imidazolealkyl, thienylalkyl, furanylalkyl, oxazolylalkyl, isoxazolylalkyl, pyrimidinylalkyl, pyridazinylalkyl and pyrazi

Abstract: The present invention relates to a new crystalline aminothiazole derivative represented by the following formula (I) which is very useful for the preparation of cephalosporin antibiotics, including ceftazidime and cefixime, etc: wherein R1 and R2 are the same or different and independently represent H, an alkyl group of 1 to 4 carbon atoms, or a cycloalkyl group of 3 to 5 carbon atoms, X represents chlorine or bromine, and the acid in the acid addition salt represents an inorganic acid, such as hydrochloric acid, hydrobromic acid, sulfuric acid, or perchloric acid, or an organic acid, such as formic acid, acetic acid, trifluoroacetic acid, propionic acid, methanesulfonic acid, or benzenesulfonic acid.

Abstract: There are disclosed an industrially favorable process for producing a tetrazole compound of general formula (1): characterized in that a nitrile of general formula (2): R1CN  (2) is reacted with hydrazine or a salt thereof in the presence of a catalyst, followed by reaction with a nitrous acid compound of general formula (3): ANO2  (3) or a nitrile of general formula (2) is reacted with hydrogen sulfide, followed by reaction with an alkyl halide of general formula (4): R4J  (4) with hydrazine or a salt thereof, and then with a nitrous acid compound of general formula (3); and an intermediate of general formula (5): R1C(═R5)R6  (5) which is useful for the production of the tetrazole compound (in which R1 to R6, A and J in the above formulas are as defined in the specification).

Abstract: The invention relates to oxadiazole derivatives of general formula (I) wherein X, Y, Z and R1 are defined as described in the specification and claims, processes for preparing them and their use as pharmaceutical compositions.

Abstract: Disclosed are novel compounds of formula I wherein R1, R2, R3, L, X and Y are as defined in the specification. These compounds are useful in the treatment of conditions mediated by nuclear receptors, in particular the Retinoid X Receptor (RXR) and the Peroxisome Proliferator-Activated Receptor (PPAR) families. Such conditions include diabetes and obesity.

Abstract: The invention relates to novel oxime derivatives of formula (I), in which A stands for alkadiyl, Ar for optionally substituted aryls or heteroaryls respectively, G for a single bond, optionally an alkandiyl interrupted by heteroatoms (in which nonetheless the carbon atom is bound to R1, and is always bound to a carbon atom of the alkandiyl chain) or a grouping, R3—O—N═C═ wherein R3 stands for alkyl, R1 respectively for hydrogen, cyano or substituted alkyl, alkoxy, alkylthio, alkylamino or cycloalkyl, R2 stands for hydrogen or alkyl, Y stands for oxygen, sulfur or NH, and Z stands respectively for optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, aryl or heterocyclyl, to a method for their production and their use as fungicides, as well as to new intermediate products and multiple methods for their production.

Abstract: A process for the preparation of a compound of formula (I), wherein X is a leaving group; which process comprises, a) for the preparation of a compound of formula (I) wherein X is —OS(═O)2A and A is as defined in the specification, reacting a compound of formula (II) with a sulfonylating agent; or, b) for the preparation of a compound of formula (I) wherein X is iodine, reacting a compound of formula (III) with an iodinating agent, preferably sodium iodide; or, c) for the preparation of a compound of formula (I) whrein X is bromine, reacting a compound of formula (IV) with a brominating agent; or, d) for the preparation of a compound (I) wherein X is chlorine or bromine, reacting a compound (V), wherein R and X are as defined in the specification, with a chlorinating agent, a compound of formula (Ib), the use thereof and a process for the preparation of a compound of formula (II) and a compound of formula (A) are described.

Abstract: The novel 13,14-dihydro-15-keto prostaglandins E of the invention have remarkable preventive effects against ulcers. Further, the novel 13,14-dihydro-15-keto-prostaglandins E of the invention have an advantage that they have none of side effects which prostaglandin E intrinsically has, or can remarkably reduce such effects of the prostaglandin E. Therefore, the novel 13,14-dihydro-15-keto prostaglandins E of the invention are effective for animal and human use for treatment and prevention of ulcers, such as duodenal ulcer and gastric ulcer.

Abstract: &ohgr;-Cycloalkyl-prostaglandin E2 derivatives of formula (I) (wherein all symbols are as defined in the description); and non-toxic salts thereof, prodrugs thereof and cyclodextrin clathrates thereof. Compounds of formula (I) strongly bind on the EP2 subtype receptor. Therefore, they are useful for prevention and/or treatment of immunological diseases (autoimmune diseases, organ transplantation etc.), asthma, abnornmal bone formation, neuronal cell death, liver damage, abortion, premature birth or retina neuropathy of glaucoma etc.

Abstract: The invention is concerned with epothilones in which the thiazole substituent has been modified, with methods for their preparation and with antifungal or therapeutic agents which contain these epothilones.

Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof. R1 and R2 are independently hydrogen, fluorine or alkyl; R3 is aryl or heteroaryl R4 is alkyl, cycloalkyl, aryl, cycloalkylalkyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl; m is an integer of 0 to 2; and n is an integer of 1 to 3. The compounds of formula I are protein kinase inhibitors and are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.

Abstract: The present invention provides calixpyrrole, calixpyridinopyrrole, and calixpyridine macrocycles, having 4, 5, 6, 7, or 8 heterocyclic rings, as well as syntheses, derivatives, conjugates, multimers, and solid supports thereof. Such macrocycles have proved to be effective and selective ion- and neutral molecule-binding agents forming supramolecular ensembles, and ion- and neutral molecule-separation agents. The macrocycles are fully meso-non-hydrogen-substituted porphyrinogens, a few molecules of which were previously known but not recognized as possessing anion- or molecule-binding properties. The binding mode is noncovalent, primarily that of hydrogen-bonding, thereby providing a new mode for liquid chromatography, that of Hydrogen Bonding Liquid Chromatography. Further useful applications of the macrocycles provided herein include environmental remediation by removal of undesired ions or neutral molecules, and removal of phosphate for kidney dialysis.

Abstract: The invention concerns the therapeutic use of tricyclic salts and their pharmaceutically acceptable salts having the general formula: in which: A is either a sulfur atom, an oxygen atom, or an R3N radical where R3 is a hydrogen atom, a C1-C5 alkyl radical, or a substituted or unsubstituted aromatic ring, or a substituted or unsubstituted heteroaromatic ring. R1 is either a C1-C5 alkyl radical, or an R4NH radical where R4 is a hydrogen atom, a C1-C5 alkyl radical, or a substituted or unsubstituted aromatic ring, or a substituted or unsubstituted heteroaromatic ring, or an aromatic ring that may or may not be substituted by one or more acceptor or donor groups, or a heteroaromatic ring having one or more heteroatoms, which may or may not be substituted by acceptor or donor groups.

Abstract: Novel amidinophenol derivatives of formula (IB) and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of leukotine B4 and inhibitors of phospholipase A2 and/or trypsin; methods for preventing or treating diseases induced by phospholipase A2 and/or trypsin comprising administering to a patient a compound of formula (IB); and methods for treating diseases induced by leukotine B4 comprising administering to a patient a compound of formula (IB) or a known amidinophenol derivative of formula (IA)

Abstract: The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I) wherein A, X and the groups R1, R2, R3, R4 and R5 are defined as in the claims, processes for preparing them and their use as pharmaceutical compositions.

Abstract: Suitable lubricant additives are the compounds of formulae wherein the substituents and groups have the following preferred meanings: R1=H; R2=methyl or tert-butyl; R3=tert-butyl; s=0, 1 or 2; R4=—A—[(C6H2)(methyl or tert-butyl)(OH)(tert-butyl)]; A=—CH2CH2O—(C═O)—CH2CH2— or —CH2CH(CH3)—O—(C═O)—CH2CH2—.

Abstract: The invention relates to novel substituted thiazolines of the formula (I) in which Ar1 and Ar2 each represent independently of one another optionally substituted phenyl, processes for their preparation, and their use for controlling animal pests.

Abstract: An efficient method is proposed for the stabilization of a sex pheromone compound of insect pest, which is a long-chain aliphatic unsaturated ester, alcohol, ketone or hydrocarbon compound having at least ten carbon atoms and at least one double bond in a molecule, used in pest control. The method comprises admixing the compound with 2-(2′-hydroxy-5′-methylphenyl) benzotriazole and an antioxidant which is preferably a hydroquinone compound such as tert-butyl hydroquinone, 2,5-di-tert-butyl hydroquinone and 2,5-di-tert-amyl hydroquinone.