Abstract: At least one of a Rh catalyst, a Pd catalyst or a Ru catalyst is used as a catalyst in preparing the salt of &ggr;-(piperidyl)-butyric acid (2) by hydrogenating the salt of &ggr;-(pyridyl)butyric acid (1) [preferably the salt of &ggr;-(pyridyl)butyric acid (1) obtained in the undermentioned steps (a) and (b) and containing not more than 3% by weight of salt of bis(pyridylethyl)acetic acid (3)] in a solvent in the presence of a catalyst: (a) reacting the vinylpyridine (4) with the diester of malonic acid (5) in the presence of a base to give the 2-(pyridylethyl)malonic acid diester (6), and (b) hydrolyzing and decarboxylating the 2-(pyridylethyl)malonic acid diester (6) obtained in the step (a) in an acidic aqueous solution to give the salt of &ggr;-(pyridyl)butyric acid (1).

Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3

Abstract: Sulfonamide-substituted chromans, processes for their preparation, their use as a medicament or a diagnostic, and medicament comprising them Chromans of the formula I and of the formula 1a having the meanings R(A), R(B), R(C) and R(1) to R(8) indicated in the claims are outstandingly suitable for preparing a medicament for blocking the K+ channel which is opened by cyclic adenosine monophosphate (cAMP); and further for preparing a medicament for inhibiting gastric acid secretion; for the treatment of ulcers of the stomach and of the intestinal region, in particular of the duodenum, for the treatment of reflux esophagitis, for the treatment of diarrheal illnesses, for the treatment and prevention of all types of arrhythmias including ventricular and supraventricular arrhythmias, and for the control of reentry arrhythmias and for the prevention of sudden heart death as a result of ventricular fibrillation.

Abstract: An erythromycin A derivative represented by Formula wherein R1 is a group represented by the formula: a group represented by the formula: (c) pyridylacetyl, (d) cycloalkylmethyl or (e) 1,2 bis-(ethoxycarbonyl)vinyl, R2 is the same group as defined for R1, hydrogen, alkyl, alkanoyl, alkoxycarbonyl, R1 and R2 together may form ═CH—R14, or R1 and R2 together with the nitrogen atom to which they are attached may form: R3 is hydrogen, alkyl or cinnamyl, R4 is hydrogen, acetyl, ethylsuccinyl or nicotinoyl, A is —OC(═O)—R17, —OC(═O)—CH2—R17, —OC(═O)—NH—R17, —O—R17 or —OC(═O)—O—R17, and R5 and R6 are each hydrogen or alkyl.

Abstract: The present invention is directed to compounds of the formula: and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same, where R1, R2, R3, R4, R5, R6, R7 and X are defined herein.

Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: Novel morphinan derivatives and pharmaceutically acceptable acid addition salts thereof as compounds having abilities to bind to opioid &egr;-receptor, which have agonist or antagonist activities, are disclosed. The morphinan derivatives according to the present invention are represented by the formula (I).

Abstract: Compounds of the formula I having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal illnesses.

Abstract: The present invention is directed to a method for selecting compounds for use in treating sickle cell disease in a patient. The method comprises the steps of selecting a first set of HbS ligands from a first group of chemical compounds, selecting from the first set of HbS ligands a seconds set that exhibit inhibition of HbS polymerization, and selecting from the second set a third set that display anti-sickling activity of red blood cells when in the presence thereof. The method may include the step of performing a methemoglobin S proteolysis assay measuring a percent protease protection for each compound. The method may additionally include the steps of measuring HbS aggregation, inhibition of protease, deoxy-HbS gelation inhibition activity, O2 affinity of HbS, and cytotoxic effect to cell activity. The method may further include assessing red blood cell morphology, and eliminating compounds that contain moieties that bind to heme.

Abstract: A process for preparing a naphthyridone carboxylic acid and its derivatives makes use of side chain intermediates of formulae I and IV herein.

Abstract: An N-hydroxyurea derivative having an antiallergic action or anti-inflammatory action having the formula wherein, either one of R1, R3, and R4 represents A, either one of the other groups of R1, R3, and R4 and R2 represents a 3-pyridyl group or 3-pyridylalkyl group, the remaining groups of R1, R2, R3, and R4 independently represent a hydrogen atom, halogen atom, or a substituted or unsubstituted C1 to C8 alkyl group, R5 represents a hydrogen atom or lower alkyl group, R6 represents a hydrogen atom, lower alkyl group, C3 to C7 cycloalkyl group, or a substituted or unsubstituted phenyl group, where the substituent represents a halogen atom, lower alkyl group, or lower alkoxy group, B represents a bond, C1 to C20 alkylene group, C2 to C8 alkenylene group, or C2 to C8 alkynylene group or B—C(R5) represents a C2 to C6 alkylene group having a benzene ring in the middle thereof or its pharmacologically acceptable salt or the hydrate or solvate thereof.

Abstract: A working solution for producing hydrogen peroxide, containing an alkylanthraguinone working compound dissolved in a solvent, is regenerated by contacting the working solution with a catalyst containing from 5% to 100% boehmite at a temperature of 25° C. to 150° C. At least a portion of the tetrahydro-alkylanthraquinone epoxide present in the working solution is converted to working compound to maintain the composition of the working solution within specified limits.

Abstract: The present invention intends to provide a method for producing 3-isochromanones represented by formula (II) useful as a synthetic starting material of medicals or agricultural chemicals and the cyano compound represented by formula (I) by an industrially advantageous method in a high yield. Disclosed herein is a method for manufacturing a 3-isochromanone represented by the following formula (II): (wherein R2, R3, R4 and R5 each independently represents a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group), said method is characterized by comprising the steps of: hydrolyzing a cyano compound represented by formula (I): (wherein R1 represents a hydrogen atom, an alkyl group or an aryl group, and R2, R3, R4 and R5 have the same meanings as defined above) and subjecting the hydrolyzate to intra-molecular cyclization.

Abstract: The present invention provides acetone complexes of sulfoxide compounds, useful as medicines such as inhibitors of gastric acid secretion and anti-ulcer agents or as intermediates for production of medicines, a process for producing the same and a purification method of using the same. Namely, it is the acetone complexes of sulfoxide compounds or of pharmaceutically acceptable salts thereof represented by the following formula: (wherein R1 represents a hydrogen atom, a methoxy group or a difluoromethoxy group, R2 represents a methyl group or a methoxy group, R3 represents a 3-methoxypropoxy group, a methoxy group or a 2,2,2-trifluoroethoxy group, R4 represents a hydrogen atom or a methyl group, n and m independently represent an integer of 1 to 4, and B represents a hydrogen atom, an alkali metal atom or ½ alkaline earth metal atom), which are obtained by treating the sulfoxide compounds or pharmaceutically acceptable salts thereof with acetone.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: Compounds and methods of preparing compounds represented by structural formula (I): wherein X represents any suitable counter-anion; R1 and R2 independently represent hydrogen, C1-6 alkoxy or nitro; R3, R4, R5 and R6 each independently represents hydrogen, hydroxy, halo, C1-6 alkyl, C2-6 alkenyl or C1-6 alkoxy; and R7, R8, R9 and R10 each independently represents hydrogen, hydroxy, halo, C1-6 alkyl, C2-6 alkenyl or C1-6 alkoxy. Compounds represented by structural formula (I) are useful in treating or preventing free radical-associated diseases or conditions in mammals.

Abstract: A process for preparing compounds of the formula: and intermediates for use in the process.

Abstract: Compounds of the formula I having the meanings of the substituents indicated in the claims are outstandingly efficacious substances for producing medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.

Abstract: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.

Abstract: The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein Z, R, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to said mammal.