Abstract: This invention provides certain N-[(phenyl)amino]carbonyl-bicyclicsulfonamide sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.

Abstract: The present invention relates to new heteroaromatic amine derivatives of general formula ##STR1## wherein the substituents are defined hereinbelow, which have valuable pharmacological properties, particularly a heart rate lowering activity and a positive inotropic activity.

Abstract: New isoindolone derivatives of general formula (I) are ##STR1## disclosed in which the radicals R represent hydrogen atoms or, together, form a bond, the symbol R' represents a hydrogen atom or a readily removable radical and the symbols R" are identical and represent phenyl radicals which can be substituted with a halogen atom or a methyl radical at the ortho or meta position, in the (3aR, 7aR) form or in the form of a mixture of the (3aRS, 7aRS) forms, as well as their salts.These derivatives are useful as intermediates for the preparation of therapeutically active products.

Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.

Abstract: The invention relates to a process for the enantiomer-selective preparation of .gamma.-keto-.delta.-amino acid derivatives of the formula I ##STR1## characterized in that a compound of the formula II ##STR2## is converted, using a trialkylchlorosilane, into a compound of the formula III ##STR3## this compound is then reacted with a diazoacetate of the formula N.sub.2 CH.sub.2 COOR.sup.4 (R.sup.4 .noteq.H) to give a cyclopropane compound of the formula IV ##STR4## and then the compound IV is converted, by ring-opening and removal of the silyl groups, and where appropriate saponification, into the compound of the formula I, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 having the meanings indicated in claim 1.

Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n denotes a number from 1 to 19, andB denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.

Abstract: Asymmetric hydrogenation of prochiral N-aliphatic ketimines to give optically active secondary amines at a temperature from -20.degree. to 80.degree. C., a hydrogen pressure of 10.sup.5 to 10.sup.7 Pa, with the addition of catalytic amounts of an iridium compound of the formula III or IIIa[XIrYZ] (III)or[XIrY].sup..sym. A.sup..crclbar. (IIIa)in which X is two olefin ligands or a diene ligand, Y is a chiral diphosphine the secondary phosphine group of which are attached through 2-4 C atoms and which, together with the Ir atom, forms a 5-membered, 6-membered or 7-membered ring, or Y is a chiral diphosphinite the phosphinite groups of which are attached via 2 C atoms and which, together with the Ir atom, forms a 7-membered ring, Z is Cl, Br or I and A.sup.- is the anion of an oxygen acid or complex acid, and, if appropriate, with the addition of an ammonium chloride, bromide or iodide or an alkali metal chloride, bromide or iodide.

Abstract: The invention relates to new optically active .alpha.-amino aldehydes of the formulae ##STR1## in which R.sub.1 represents an optionally substituted alkyl, alkenyl, aralkyl or aryl radical, andR.sub.2 and R.sub.3, independently of one another, denote an optionally substituted alkyl, alkenyl, cycloalkyl or aralkyl group, together form an optionally substituted phenylene-(1,2)-bis-methylene radical, or R.sub.2 is an optionally substituted, alkyl, cycloalkyl or aralkyl radical, and R.sub.3 forms together with R.sub.1 a 1,3-propylene radical.a process for the preparation thereof, and the use thereof for the stereoselective preparation of optically active .beta.-amino alcohols.

Abstract: Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.

Abstract: The invention concerns novel phenoxyacetic acid amide derivatives of the formula I (and pharmaceutically acceptable salts thereof) in which R.sup.1 is hydrogen or fluoro, R.sup.2 is phenyl, cycloalkyl, alkyl or alkenyl as defined herein, and R.sup.3 is hydrogen, methyl or ethyl, or R.sup.2 and R.sup.3 together form polymethylene as defined herein. The invention also includes pharmaceutical compositions containing the amide derivatives, means for the manufacture of the said derivatives and for their use in the treatment of obesity and related conditions and/or in the manufacture of novel medicaments.

Abstract: A thermal imaging method is provided which comprises heating imagewise a di- or triarylmethane compound possessing within its di- or triarylmethane structure an aryl group substituted in the ortho position to the meso carbon atom with a moiety ring-closed on the meso carbon atom directly through a nitrogen atom, which nitrogen atom is also bound to a group with a masked acyl substituent that undergoes fragmentation upon heating to liberate the acyl group for effecting intramolecular acylation of said nitrogen atom to form a new group in the ortho position whereby the di- or triarylmethane compound is rendered colored in an imagewise pattern corresponding to said imagewise heating.

Abstract: This invention relates to aryloxy dihydrobenzofuran, oxoindole or benzofuranone derivatives having herbicidal activity and to the use of such compounds to control the growth of noxious plants, i.e., weeds.

Abstract: There is provided a fluorescent adduct which is amenable to detection by fluorometric and electrochemical techniques. The adduct is of the formula: ##STR1## wherein X is a radical derived from a primary amine of the formula X--NH.sub.2 and where R.sub.1 --R.sub.6 are selected from various organic or inorganic substituents.

Abstract: The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S-- is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m --(m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychoromatic disease and anxiety neurosis.

Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.

Abstract: A novel compound of the formula, ##STR1## wherein R denotes a lower perfluoroalkyl group, l is an integer of 3 or 4, n+m is an integer of 2 or 3, provided that n may be zero, and at least one of ring A and ring B may be substituted by a lower perfluoroalkyl group, prepared by reacting the corresponding perhydro compound with fluorine is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.

Abstract: Novel and known functionally substituted phenoxyalkyl-, thiophenoxyalkyl- and pyridyloxyalkylsilanes are prepared by reacting substantially equimolar amounts of an alkali- or alkaline earth metal phenoxide, thiophenoxide or pyridyloxide with a haloalkylsilane under anhydrous conditions using a dipolar, aprotic solvent in combination with a liquid hydrocarbon.

Abstract: (Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.

Abstract: Compounds of the formula ##STR1## wherein X is various imino or amino acids or esters are disclosed. These compounds possess angiotensin converting enzyme inhibition activity and depending upon the definition of X also possess enkephalinase inhibition activity.

Abstract: Compounds of the formula ##STR1## wherein A is a cycloalkyl ring, a substituted cycloalkyl ring, a phenyl ring, or a substituted phenyl ring and ##STR2## are various dipeptide groups are disclosed. The compounds possess angiotensin converting enzyme inhibition activity and depending upon the terminal amino acid may also possess enkephalinase inhibition activity.

Abstract: Substituted acyl derivatives of octahydro-1H-isoindole-1-carboxylic acid compounds and the pharmaceutically acceptable salts thereof are produced by acylating a suitably substituted octahydro-1H-isoindole with a suitably activated substituted carboxylic acid and when desired hydrolyzing the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.

Abstract: Amino thiol substituted dipeptides of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: Isoindoledione compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.3 each separately is phenyl, substituted phenyl, alkyl of 1 to 4 carbons, --CHO, --CH.sub.2 OR.sub.6, --CO.sub.2 R.sub.6, --COR.sub.6, hydrogen, or together with R.sub.2 is a divalent alkyl or alkenyl group of 3 to 5 carbons which form a cyclic ring;R.sub.2 is phenyl, substituted phenyl, --CH.sub.2 OR.sub.6, --CH.sub.2 CH.sub.2 OR.sub.6, alkyl of 1 to 4 carbons or with either R.sub.1 or R.sub.3 is a divalent alkyl or alkenyl group of 3 to 5 carbons which form a cyclic ring;R.sub.4 and R.sub.5 which may be the same or different each separately is hydrogen, alkyl of 1 to 4 carbons, --OR.sub.6, --CO.sub.2 R.sub.6, --COR.sub.6, --CHO, --CH.sub.2 OR.sub.6 or together R.sub.4 and R.sub.5 is a butadiene radical which forms a benzene ring;R.sub.6 is hydrogen or alkyl of 1 to 4 carbons; provided that R.sub.1 and R.sub.3 are not both phenyl and that when R.sub.4 and R.sub.5 are both hydrogen, R.sub.1, R.sub.2 and R.sub.3 are not all methyl.

Abstract: Nitroarylacetic acid esters are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base so that the ester undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their esters are useful intermediates for the synthesis of pharmaceuticals.

Abstract: Substituted peptide compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: This invention relates to compounds and methods of using said compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkyl, alkenyl or alkoxycarbonylalkyl; Y is O or S; m is an integer of 1 to 3 and n is an integer of 0 to 1 which compounds are insect repellents.

Abstract: A series of organic diamine base compounds derived from either an aromatic, alicyclic or heterocyclic ring and possessing, for the most part, an intervening methylene group between the ring and the aforesaid basic moiety have been prepared, including their pharmaceutically acceptable acid addition salts as well as oral pharmaceutical compositions containing same. These particular compounds are found to be useful in therapy as oral hypoglycemic agents. Preferred member compounds include 1,1'-[1,2-phenylenebis(methylene)]bispiperidine, 2,3-dihydro-2-[2-(1-piperidinomethyl)phenylmethyl]-1H-isoindole and 2,3-dihydro-2-[2-(4-morpholinomethyl)phenylmethyl]-1H-isoindole. Alternate methods of preparation are provided and the two principal synthetic routes leading to these compounds are described in some detail.

Abstract: Bicyclic imino acids, particularly 2-carboxylic acid derivatives of azabicycloalkanes and process for preparing them.These compounds have therapeutical activity and may be used as medicines, particularly as cardiovascular and antihypertensive drugs in human or veterinary medicine.

Abstract: Novel dyes of the formula ##STR1## where A is cyano, carbo-C.sub.1 -C.sub.4 -alkoxy, carbamyl, N-C.sub.1 -C.sub.4 -alkylcarbamyl, N-phenylcarbamyl, acetyl, benzoyl, 4-nitrophenyl or 4-cyanophenyl,X is hydrogen, chlorine, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, and if n is 2 the substituents may be identical or different,n is 1 or 2,R.sup.1 is hydrogen, methyl, ethyl or 2-hydroxyethyl andR.sup.2 is phenyl or cyclohexyl, orR.sup.1 is hydrogen andR.sup.2 is C.sub.1 -C.sub.4 -alkyl, orR.sup.1 and R.sup.2 are C.sub.1 -C.sub.6 -alkyl, allyl or phenyl-C.sub.1 -C.sub.4 -alkyl orthe group ##STR2## is a saturated heterocyclic five-membered or six-membered ring which may additionally contain an oxygen or a further nitrogen as ring members,Y is hydrogen, hydroxyl, methyl or ethyl; ##STR3## where R.sup.3 is linear or branched C.sub.1 -C.sub.12 -alkyl, or is phenyl; ##STR4## where R.sup.4 is hydrogen or C.sub.1 -C.sub.4 -alkyl and R.sup.5 is hydrogen, linear or branched C.sub.1 -C.sub.

Abstract: Compounds of the general formula: ##STR1## in which A is a benzene ring or a carbocyclic aromatic group consisting of two or three fused benzene rings, the group A being linked to the nitrogen containing ring at two adjacent carbon atoms and the benzene ring or each benzene ring optionally carrying one or more substituents which may be the same or different, and may be alkyl, aryl, halo, hydroxy, acyloxy or alkoxy, or two adjacent positions in a ring may be substituted so as to form a methylene dioxy group (--O--CH.sub.2 --O--);R.sub.1 and R.sub.2 which may be the same or different, each represent hydrogen; an alkyl group which contains 1 to 6 carbon atoms and which may be substituted; a hydroxycarbonyl or an alkoxycarbonyl group; andone of R.sub.3 and R.sub.4 represents hydrogen, an alkyl group which contains 1 to 6 carbon atoms and which may be substituted, or a hydroxy, alkoxy, hydroxycarbonyl or alkoxycarbonyl group and the other of R.sub.3 and R.sub.