Abstract: Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl.Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position.Furthermore, the compounds have remarkable antitumor activities and therefore can provide novel antitumor agents.

Abstract: There are disclosed substituted imidazole derivatives of Formula I which are useful as angiotensin II antagonists.

Abstract: A process for the preparation of a 2-chloro-5-chloromethyl-pyridine, of the formula (I) ##STR1## comprising reacting a 2-alkoxy-5-alkoxymethylpyridine derivative of the formula (II) ##STR2## in which R.sup.1 represents alkyl,with a chlorinating agent, is appropriate, in the presence of a diluent and if appropriate, in the presence of a reaction auxiliary, at a temperature between 0.degree. C. and 200.degree. C.

Abstract: Certain novel imidazole derivatives N-substituted by a vinyl group itself carrying a mevalonic acid derivative or corresponding lactone are inhibitors of HMG-CoA reductase and are useful for lowering blood plasma cholesterol levels.The compounds are of general formula (I): ##STR1## in which one of the groups R.sup.1 and R.sup.2 represents a C.sub.1-6 alkyl group optionally substituted by one to three halogen atoms and the other represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, S(O).sub.n C.sub.1-3 alkyl, (CH.sub.2).sub.m NR.sup.a R.sup.b, (CH.sub.2).sub.m NR.sup.c COR.sup.d and trifluoromethyl groups;R.sup.3 represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, S(O).sub.n C.sub.1-3 alkyl, (CH.sub.2).sub.m NR.sup.a R.sup.b, (CH.sub.2).sub.m NR.sup.c COR.sup.

Abstract: The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective inhibitors of cyclooxygenase and 5-lipoxygenase.

Abstract: A method of retouching a dye image comprises selective removal with an aqueous acidic organic solvent solution, as described in the application, of a portion of a dye image from an exposed and processed photographic silver halide element comprising a support bearing a dye image from a dye-forming coupler and a primary amine photographic color developing agent, wherein the dye-forming coupler: (a) contains so ionizable group that is retained as part of a dye formed upon oxidative coupling, (b) has a structure such that the Log P of the coupler is greater than 4 and is derived from a four-equivalent coupler that has a Log P less than 8, and (c) has a coupling reactivity that enables formation of maximum image density of at least 0.6. The method comprises the step of contacting the dye image with an aqueous acidic organic solvent solution, as described in the application, for a time and at a temperature sufficient to selectively dissolve and remove a portion of the dye image from the photographic element.

Abstract: Described herein is a process for preparation of substituted pyridine dicarboxylate compounds.

Abstract: The econazole and miconazole sulfosolicylic acid addition salts show, in vitro, a relevant anti-fungal activity with wide spectrum and, if locally applied, are well tolerated and more effective than the corresponding nitrates for the control, in vivo and clinically, of the mycosis as induced from dermatophytes and from Candida albicans.

Abstract: Imidazole derivatives of the formula: ##STR1## are described wherein R.sup.1 represents halogen, alkyl or alkoxy, n is 0 to 5, R.sup.2 represents hydrogen or alkyl, R.sup.3 represents hydrogen or alkyl optionally substituted by halogen, hydroxy, acyloxy, alkoxy, hydroxyalkoxy, acyloxyalkoxy, or by optionally substituted phenyl, or the groups R.sup.3 and the carbon atom to which they are attached together form a cycloalkane or cycloalkene group. They are pharmaceutically useful as antiatherosclerotic agents.

Abstract: Acetylenic imidazole compounds having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of the parasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.

Abstract: A process for the preparation of N-substituted pyrrolidin-2-ones of the general formula I ##STR1## where R.sup.1 is C.sub.1 - to C.sub.20 -alkyl, C.sub.6 - to C.sub.10 aryl or C.sub.7 - to C.sub.12 -aralkyl comprises hydrogenolytically cleaving 5-iminopyrrolidin-2-ones of the general formula II ##STR2## in which the R.sup.1 radicals are identical or different C.sub.1 - to C.sub.20 -alkyl, C.sub.6 - to C.sub.10 -aryl or C.sub.7 - to C.sub.12 -aralkyl, at super-atmospheric pressure and elevated temperature in the presence of a hydrogenation catalyst to give the pyrrolidin-2-ones I; specifically, the 5-iminopyrrolidin-2-ones of the formula II are obtained by reacting .beta.-cyanopropionic acid esters of the general formula III ##STR3## where R.sup.2 is C.sub.1 - to C.sub.20 -alkyl, C.sub.7 - to C.sub.12 -aralkyl or C.sub.6 - to C.sub.10 -aryl, with an amine of the general formula IVR.sup.1 --NH.sub.2 IVwhere R.sup.1 is as defined above.

Abstract: Imidazole derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, R'.sub.1 and R'.sub.2 which can be the same or different, are H, CH.sub.3, C.sub.2 H.sub.5, OCH.sub.3, OH, CH.sub.2 OH, NH.sub.2 or halogen; R' if H or ##STR2## where R.sub.3 is H, CH.sub.3, or halogen; R.sub.4 is H and R.sub.5 is H or OH and R.sub.6 is H or OH or one of R.sub.5 and R.sub.6 is H and the other, together with R.sub.4, forms a bond and X and Y, which can be the same or different, are a bond, a straight C.sub.1-2 -alkyl or the corresponding alkenyl, and pharmaceutically acceptable salts thereof exhibit valuable pharmacological properties, especially aromatase inhibiting effects and are useful in the treatment of estrogen dependent diseases, e.g. breast cancer. Anti-mycotic and antifungal properties have also been found.

Abstract: A charge generating compound for use in electrophotographic devices of the formula: ##STR1## wherein: A and A.sup.1 are each independently selected from phenyl, substituted phenyl, quinolino, naphthyl and substituted naphthyl wherein the substituents are independently selected from halo, alkyl, alkoxy, alkylthio, phenyl, phenoxy, phenylthio, CF.sub.3, CH.sub.2 OH, CO.sub.2 R.sup.1, NHCOR.sup.1, COR.sup.1, NO.sub.2 and NR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 are each independently H or C.sub.1-6 -alkyl.

Abstract: D-(+)-biotin can be prepared from optically active hydantoins of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in Patent claim 1, in a simple, stereospecific manner. Furthermore bicyclic nitriles of the formula XI ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given represent precious intermediate products and educts of a multitude of possibilities to synthesize optically active D-(+)-biotin.

Abstract: Substituted indolyl compounds of the formula ##STR1## are potent inhibitors of the lipoxygenase enzymes and are useful as agents for the treatment of allergies and inflammatory disease states.

Abstract: A series of novel 1-(phenethyl) and 1-(1-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone. The most preferred compound is (3R)-diphenylmethoxy-1-(3,4-methylenedioxyphenethyl)piperidine. Methods for preparing these compounds from known starting materials are provided.

Abstract: A class of N-substituted imidazol-2-one compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R.sup.0 is selected from hydrido, methyl, fluoro, chloro, monofluoromethyl, difluoromethyl, trifluoromethyl, formyl, carboxyl and dimethoxymethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sub.7, R.sup.8, R.

Abstract: Compounds of the Formula VII: ##STR1## wherein; X.sup.1 and X.sup.2 are each independently selected from H, cyano, alkyl, alkoxy, aryl, carbamoyl, sulphamoyl, COOH and carboxylic acid ester;Z.sup.1 and Z.sup.2 are both --O--;R.sup.1 and R.sup.2 are each independently selected from H, or an optionally substituted alkyl, alkenyl, cycloalkyl, aryl and aralkyl group; orR.sup.1 and R.sup.2 together with the N atom to which they are attached, form a heterocycle;R.sup.4, R.sup.5, R.sup.7 and R.sup.8 are each independently selected from E, halogen, or an optionally substituted alkyl, alkenyl and alkoxy group orR.sup.1 and R.sup.4 or R.sup.2 and R.sup.5 together with the N atom and the two carbon atoms in Ring B to which they are attached form a heterocycle fused to Ring B; orR.sup.1 and R.sup.7 or R.sup.2 and R.sup.8 together with the N atom and the two carbon atoms in Ring A to which they are attached form a heterocycle fused to Ring A; orR.sup.

Abstract: 2-Benzimidazole terephthalic acid, 4,4'-dicarboxy-2,2'-bisbenzimidazole benyl and 4,4"-dicarboxy-2'-phenyl-3'-[2-(4-phenylbenzthiazole)]-6'-[2-(3-phenylbenz imidazole]-p-terphenyl are provided.Also provided are methods for preparing these dicarboxylic acids. 2-benzimidazole terephthalic acid is prepared by reacting trimellitic anhydride with o-phenylenediamine in a suitable solvent. 4,4'-dicarboxy-2,2'-bisbenzimidazole biphenyl is prepared by diazotizing 2-amino-5-bromobenzoic acid to prepare 4,4'-dibromodiphenic acid, reacting the 4,4'-dibromodiphenic acid with o-phenylenediamine in trimethylsilyl polyphosphate solution to prepare 4,4'-dibromo-2,2'-bisbenzimidazolyl biphenyl, reacting the 4,4'-dibromo-2,2'-bisbenzimidazolyl biphenyl with cuprous cyanide to prepare the corresponding dicyano compound, and hydrolyzing the dicyano compound.

Abstract: 1,4-dihydropyridines of formula I ##STR1## wherein X is --CO.sub.2 R.sub.1, cyano, nitro, --COCH.sub.3 ; each of R and R.sub.1, which are the same or different, is a primary, secondary or tertiary, saturated or unsaturated, linear or branched C.sub.1 -C.sub.6 alkyl group optionally substituted by one or more hydroxy, C.sub.1 -C.sub.7 -monoalkylamino, di-C.sub.1 -C.sub.7 -alkylamino, benzylamino, C.sub.1 -C.sub.6 -alkoxy, phenoxy groups which are optionally substituted; R.sub.2 is hydrogen; R.sub.3 is hydrogen or hydroxy, --OCOR.sub.5, OSO.sub.2 R.sub.6, azide, amino, --NHPO(OR.sub.7).sub.2, --NHCOR.sub.5, C.sub.1 -C.sub.4 -alkoxy or fluorine, chlorine, bromine or iodine, SH, SCOR.sub.6 or C.sub.1 -C.sub.6 -alkylthio, phenylthio or benzylthio; R.sub.4 is an optionally substituted aromatic or an optionally substituted 5- or 6-membered heteroaromatic group; Y is one or more substituents, which may be the same or different, selected from C.sub.1 -C.sub.4 -alkoxy, halogen, nitro, cyano, C.sub.1 -C.sub.