Abstract: .alpha.,.beta.-Diaminoacrylonitriles of the general formula IR.sup.3 R.sup.2 NC(R.sup.1).dbd.C(NR.sup.2 R.sup.3)CN Iwhere R.sup.1, R.sup.2 and R.sup.3 are identical or different and independently of one another are each hydrogen, alkyl, cycloalkyl, aralkyl, aryl or a heterocyclic radical, and the organic radicals R.sup.2 may furthermore be bonded to one another to form a 6-membered or 7-membered ring, or R.sup.2 and R.sup.3 may be bonded to one another to form a 5-membered or 6-membered ring, are prepared by reacting an .alpha.-dicarbonyl compound R.sup.1 COCHO, or a reactive derivative of this with (a) a salt of sulfurous acid or sulfur dioxide, (b) an amine HNR.sup.2 R.sup.3 or an aliphatic diamine R.sup.3 HN-(CH.sub.2).sub.n NHR.sub.3 where n is 2 or 3 and (c) hydrocyanic acid or a hydrocyanic acid donor in any sequence.

Abstract: Disclosed herein are a cephalosporin derivative represented by the formula (I): ##STR1## wherein R.sup.1 represents a halogenoalkyl group, a salt and ester thereof, a process for producing the same, and a pharmaceutical composition and an antibacterial agent comprising the same.

Abstract: This invention relates to intermediates of Mannich-alkynyl aminothiadiazole oxides having histamine H.sub.2 -antagonist activity. A particular final product of this invention is 3-amino-4-[7-piperidinohept-5-ynylamino]-1,2,5-thiadiazole-1-oxide.

Abstract: In one of its embodiments the present invention provides a smoking composition which contains a novel type of acylpyrazine ether flavorant additive as exemplified by 1-(3-methoxy-2-pyrazinyl)-2-methyl-1-propanone.

Abstract: There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is ##STR2## R.sup.2 and R.sup.3 are each individually hydrogen, lower alkyl, carboxy, lower alkoxycarbonyl, cyano, nitro, trifluoromethyl, phenyl or naphthyl; or R.sup.2 and R.sup.3 taken together represent ##STR3## or a 5- or 6- membered unsaturated aza-, diaza-, triaza-, tetraza-, thia-, thiaza-, oxathia-, oxathiaza-, oxa-, dioxa-, oxaza- or oxadiazacyclic moiety; and the dotted line denotes an optional double bond; andR.sup.4 is hydrogen, lower alkyl, phenyl or naphthyl.

Abstract: There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is ##STR2## R.sup.2 and R.sup.

Abstract: There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is ##STR2## R.sup.2 and R.sup.

Abstract: Nitriles of fused ring pyridine compounds such as 5,6,7,8-tetrahydroquinolines are prepared from metal derivatives of the starting compounds such as 8-litho-5,6,7,8-tetrahydroquinolines which have been prepared by treating a 5,6,7,8-tetrahydroquinoline with a metal amide prepared in situ from a metal alkyl and an N-benzylidine-N-alkylamine.

Abstract: The invention relates to a process for preparing carbamic acid derivatives of formula: ##STR1## in which R.sup.1 or R.sup.2 denotes a hydrogen atom or a substituted or unsubstituted, saturated or unsaturated aliphatic, cycloaliphatic or heterocyclic radical, or R.sup.1 and R.sup.2 together form a ring, and Y denotes OR, SR, ##STR2## groups, R being a substituted or unsubstituted, saturated or unsaturated aliphatic or cycloaliphatic radical, or a substituted or unsubstituted aromatic radical, R.sup.3 and R.sup.4 denote a hydrogen atom or an aliphatic, cycloaliphatic, araliphatic, aromatic or heterocyclic radical or together form a ring, and R.sup.6 and R.sup.7 denote a saturated or unsaturated, substituted or unsubstituted aliphatic or cycloaliphatic radical, a hydrogen atom, an alkylthio radical or an alkyloxy radical.According to the process, a compound of formula ##STR3## is reacted with an .alpha.-halogenated derivative of formula ##STR4## at a temperature of -5.degree. to 150.degree. C.

Abstract: A novel perylene-3,4,9,10-tetracarboxylic acid diimide of the formula ##STR1## is very useful as a black dye or, together with white pigments, as a gray dye.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently hydrogen, alkyl of 1 to 4 carbon atoms, hydroxyl, alkoxy of 1 to 4 carbon atoms, alkanoyloxy of 1 to 4 carbon atoms, halogen, trihalomethyl, di(lower alkyl of 1 to 4 carbon atoms)amino, (alkoxy of 1 to 4 carbon atoms)carbonyl, nitro, cyano or alkanoyl of 1 to 3 carbon atoms;R.sub.7 and R.sub.8 are independently hydrogen, methyl, hydroxyl, carboxyl, (alkoxy of 1 to 4 carbon atoms)carbonyl, hydroxymethyl, phenyl, or p-chlorophenyl;R.sub.9 and R.sub.10 are independently hydrogen or methyl;j and k are independently 0, 1, 2, or 3, their sum being no more than 4;m and n are independently 0, 1, 2, or 3, their sum being no more than 4;A is --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --;R.sub.7 and R.sub.9 together are oxo, provided k is other than o;R.sub.8 and R.sub.10 together are oxo, provided m is other than o;R.sub.11 and R.sub.

Abstract: New semicarbazide derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sup.2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl,R.sup.3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, orR.sup.2 and R.sup.3 are taken together to form (C.sub.2 -C.sub.6)alkylidene group optionally substituted with aryl or taken together with the adjacent nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl; orR.sup.1 and R.sup.2 are taken together with the adjacent nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group,R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl;R.sup.4 is aryl which may have substituent(s) selected from lower alkyl, halogen, lower alkoxy, lower alkylamino, halo(lower)alkyl, hydroxy, lower alkanoyl, esterified carboxy and carboxy,R.sup.

Abstract: 2-Amino-3-cyano-5-dialkoxymethylpyrazine derivatives of the general formula III ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or a protective group usually employed for amino groups and R.sup.5 and R.sup.6 are each alkyl of 1 to 4 carbon atoms, or together form an ethylene or propylene radical which is unsubstituted or substituted by methyl, are prepared starting from a novel 3-halomethyl-5-dihalomethyl-2-aminopyrazine derivative of the formula IV ##STR2## where X is Cl or Br, via a novel intermediate of the general formula I ##STR3## where R.sup.3 is --CH.sub.2 --O--CO--CH.sub.3 (a), --CH.sub.2 OH (b), ##STR4## or --C.tbd.N (d) and R.sup.4 is --CHCl.sub.2 or --CHBr.sub.2 or, where R.sup.1 and R.sup.2 are each a protective group, R.sup.4 may furthermore be ##STR5##The compounds according to the invention are useful intermediates for the preparation of folic acid and active compounds derived from this.

Abstract: A compound of the formula: ##STR1## wherein R.sub.1 stands for n-propyl or isopropyl; and R.sub.2 stands for n-butyl, isobutyl, n-pentyl, n-hexyl or 2-ethylbutyl, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.

Abstract: Novel 2-substituted-aminomethyl-1,4-benzodiazepines which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.

Abstract: The invention relates to novel 2-phenyl-imidazoles of the formula ##STR1## and the tautomers and acid addition salts thereof, particularly the pharmacologically acceptable acid addition salts, which exhibit valuable pharmacological properties, particularly an effect on the contractility of the heart muscle. The compounds of Formula I may be prepared by methods conventionally used for similar compounds.

Abstract: The novel ester, N-benzylazetidine-3-carboxylic acid methyl ester and its use in the preparation of the corresponding free acid by a process which comprises reacting N-benzyl-3-cyanozetidine with methanol and hydrolyzing the resulting methyl ester with hot water.

Abstract: This invention relates to novel chemical compounds, methods and compositions for inhibiting the production of human perspiration, especially axillary perspiration. More particularly, the practice of the invention comprises the topical application to the axiallary area or other perspiration-producing portion of the body of an anticholinergic eucatropine ester having reduced mydriatic activity and distributed in a suitable dermatologically acceptable carrier.

Abstract: The present invention relates to a process for the dimerization of 4,4'-diisocyanatodiphenylmethane from emulsion in apolar solvents with the formation of complexes and to the complexes obtainable for the first time by this process. The complexes consist of one mol of low molecular weight 4,4'-diisocyanato-diphenylmethane-uretdione or its low oligomers corresponding to the idealized formula (I) ##STR1## (n=0 to 0.5, where n is the average degree of oligomerization of the dimer) and 2 to 3 mol of 4,4'-diisocyanatodiphenylmethane (MDI) ##STR2## In the process according to the invention, 4,4'-diisocyanatodiphenylmethane (II) in the molten form is emulsified in apolar solvents. Dimerization is started in the presence of conventional dimerization catalysts at temperatures above the melting point of MDI, preferably up to an upper temperature limit of 50.degree. to 60.degree. C. The temperature is then lowered to <40.degree. C. If desired, dimerization can be stopped when an isocyanate content of from 22.4 to 26.

Abstract: This invention relates to novel compositions, their preparation and the use thereof as anticholinergic agents in the treatment or prophylaxis of organophosphate or nerve gas poisoning in animals. These compositions and pharmaceutical preparations containing them in their free base form and acid addition salts thereof are represented by the formula ##STR1## wherein R represents lower alkyl groups containing 1 to 7 carbon atoms; R.sup.1 represents hydrogen, phenyl, cyclohexyl, and cyclopentyl; and R.sup.2 represents lower alkyl groups containing 1 to 7 carbon atoms, hydroxymethyl, and hydroxyl.