Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.

Abstract: Fluorinated alkene compounds useful for controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the formula BrCF.sub.2 CFClCH.sub.2 CO--R where R is R.sub.1 or R.sub.2. R.sub.1 is --SR.sub.5, halogen, --NHOH or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are independently H; an aliphatic or aromatic group; an aliphatic amine group; an aliphatic carboxylic acid group; or R.sub.5 and R.sub.6 when taken with the N of R.sub.1 are an amino acid or a cyclic group or R.sub.1 is --OR.sub.5, where R.sub.5 is an aliphatic or aromatic group; an aliphatic amine group; or an aliphatic carboxylic acid group. R.sub.2 is --SR.sub.5 or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are independently H; an aliphatic, aromatic or heterocyclic group; an aliphatic amine group; an aliphatic carboxylic acid group; R.sub.5 and R.sub.6 when taken with the N of R.sub.2 are an amino acid or a cyclic group; R.sub.5 and R.sub.6 when taken with the N of R.sub.

Abstract: The present invention comprises methods and compositions for reducing or eliminating multidrug resistance in cancers or certain infections by drug resistant microorganisms in patients. According to the method and composition of the present invention, a non-ionic amphipathic diester of fatty acids or a reverse poloxmer is administered to a patient in which a cancer or microorganism exhibits multidrug resistance to the chemotherapeutic agent. The method and composition of the present invention may be employed with particular efficacy where multidrug resistance to any chemotherapeutic agent has been conferred upon a cancer.

Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.

Abstract: Certain tetralinyl- and indanyl-ethylamides are useful central nervous system agents.

Abstract: The present invention deals with the certain novel esters which are prepared by the reaction of an alpha methyl alcohol and a fatty acid. These materials are useful as conditioning agents for skin.

Abstract: Pharmaceutical compositions in topical or parenteral form containing organic nitrites are effective in treating male impotence and erectile dysfunction through topical or intracavernosal administration to the penis. Methods of treatment utilizing the nitrite-containing compositions are also disclosed, as are certain novel organic nitrite compounds.

Abstract: The present invention provides novel hydrogel-forming, self-solvating, absorbable polyester copolymers capable of selective, segmental association into compliant hydrogels upon contacting an aqueous environment. Methods of using the novel polyester copolymers of the invention in humans are also disclosed for providing a protective barrier to prevent post-surgical adhesion, treatment of defects in conduits such as blood vessels, and controlled release of a biologically active agent for modulating cellular events such as wound healing and tissue regeneration or therapeutic treatment of diseases such as infection of the periodontium, dry socket, bone, skin, vaginal, and nail infections.

Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.

Abstract: The present invention comprises methods and compositions for reducing or eliminating multidrug resistance in cancers or certain infections by drug resistant microorganisms in patients. According to the method and composition of the present invention, a non-ionic amphipathic diester of fatty acids or a reverse poloxmer is administered to a patient in which a cancer or microorganism exhibits multidrug resistance to the chemotherapeutic agent. The method and composition of the present invention may be employed with particular efficacy where multidrug resistance to any chemotherapeutic agent has been conferred upon a cancer.

Abstract: The present invention provides an agricultural or horticultural fungicide including an effective amount of an amino-acid derivative represented by the formula: ##STR1## wherein R.sup.1 represents a lower alkyl group (optionally having at least one same or different substituent of a halogen atom, an alkoxy group, and a cyano group), R.sup.2 represents an ethyl group, or an n-propyl group, R.sup.3 represents a hydrogen atom or a lower alkyl group, R.sup.4 represents a hydrogen atom, R.sup.5, R.sup.6, and R.sup.7 independently represent a hydrogen atom or a lower alkyl group, R.sup.8 represents a hydrogen atom, or a lower alkyl group, Z.sup.1 and Z.sup.2 independently represent an oxygen atom or a sulfur atom, Z.sup.3 represents an oxygen atom, or a sulfur atom, Q represents a phenyl group, m represents an integer from 0 to 2, and n represents 0 or 1.

Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.

Abstract: There are disclosed compositions which, when administered to a warm-blooded animal, are capable of regulating blood sugar levels. The compositions contain inulin, one or more metal complexes, and, optionally, one or more medium chain triglycerides. Also disclosed is a method for regulating blood sugar levels by administration of the compositions of this invention.

Abstract: A compound of formula (I), in which each of R.sub.1 and R.sub.2 is independently hydrogen, alkyi or, together with the carbon atom to which it is bonded, a cycloalkyl; and each of R.sub.3 and R.sub.4 is independently hydrogen, alkyl or substituted alkyl. The compounds are useful intermediates and prodrugs.

Abstract: A method of treating a patient suffering from a condition requiring vasodilator therapy, comprising long term, continuous adminstration of an organic nitrite to the patient in a dosage form capable of delivering a sufficient therapeutic amount of nitrite to the bloodstream of the patient thereby providing effective vasodilator therapy for at least 24 hours without the development of tolerance in the patient. The method of the invention is useful in treating conditions such as angina, particularly chronic, stable angina pectoris, ischemic diseases and congestive heart failure, and for controlling hypertension and/or impotence in male patients.

Abstract: A Legionella specific antibiotic AL072 is disclosed. In addition the antibiotic is produced by the microorganism Streptomyces sp. AL91KCCM 10055. Further, the antibiotic compound has a specified formula.

Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract wherein ##STR2## Z=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene, lower-alkoxy-carbonyloxy;n=1-5;y=0-4; andw=1-4in an aqueous pharmaceutically acceptable carrier.

Abstract: Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I ##STR1## in which A--B, R.sup.3, R.sup.4, R.sup.5, Y and Z have the meanings indicated, for use as inhibitors of the glucose-6-phosphatase system of the liver in mammals are described. The compounds are suitable for the production of pharmaceutical preparations.

Abstract: There are described new 2-cyclohexan-1-yl-amine derivatives of formula (I) ##STR1## in which A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meaning given in the description, and processes for their preparation.The compounds of the formula (I) are used as anti-microbial agents.

Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.

Abstract: A solvent for producing emulsifiable concentrates from agriculturally active chemicals which are insoluble in water comprises an alkoxyalkyl lactam such as butoxy propyl pyrrolidone. An agriculturally active chemical and the alkoxyalkyl lactam are admixed optionally with co-solvents, emulsifiers and surfactants to produce a stable emulsifiable concentrate. The concentrate is dilutable with water at the point of use to produce either macro or micro emulsions which are themselves stable to assure even application.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinX= ##STR2## Z=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy,n is 1-5;y is 0-4; andw is 1-4.

Abstract: Disclosed herein is an infection protectant which is excellent in infection protective effects and is also safe. .kappa.-Casein, a sialic-acid-conjugated protein derived from cow milk, and a glycomacropeptide derived from .kappa.-casein, each of which is useful as an active ingredient in this invention, have been found to be effective for the prevention of adhesion of E. coli on cells and also for the inhibition of transformation of lymphocytes by EBV and also to have strong HI activity against virus. The infection protectant of this invention is hence believed to exhibit marked effects for the prevention of occurrence of infectious diarrhea, for mass protection against spreading of influenza, and also against canceration of lymphocytes. Since the active ingredient of the infection protectant is a substance derived from cow milk, it is free of any problem from the viewpoint of safety. Moreover, it is absolutely tasteless and odorless. It can therefore be added to foods for its application.

Abstract: A wood preservative composition which comprises a wood preservative in an amount of 0.01-10% by weight and a diphenylalkane compound represented by the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or an alkyl, in an amount of not less than 1% by weight and in an amount of 1-1000 parts by weight in relation to one part by weight of the wood preservative.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.

Abstract: Mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein Y is a specified small group or single atom and R.sup.1 and R.sup.2 are selected from a wide range of specified substituents.

Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.

Abstract: Mazindol and other nonreinforcing dopamine uptake inhibitors are effective to lessen craving for abused substances.

Abstract: Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.

Abstract: Fungicidal substituted amino acid amides of the formula ##STR1## in which Ar and Ar' are identical or different and represent unsubstituted or substituted aryl, unsubstituted or substituted aralkyl, unsubstituted or substituted heteroaryl and unsubstituted or substituted heteroarylalkyl, andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are identical or different and represent hydrogen or alkyl orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring.

Abstract: The hair setting shampoo composition of the invention comprises a resin provided by about 1-15% by weight of about a 20-50% resin active alcoholic solution of the alkyl half-ester of a C.sub.1 -C.sub.5 alkyl vinyl ether-maleic anhydride copolymer having a molecular weight of at least one million, which is about 5-90% neutralized, preferably with about 0.01-1% by weight of 2-amino-2-methyl-1-propanol, about 5-60% by weight of a surfactant, optionally 0-10% by weight of added ethanol, and about 30-90% by weight of water. The composition provides a subtle temporary set on hair of the user without the use of auxiliary fixatives in the composition.

Abstract: Formamidine compounds of general formula I ##STR1## in which: R.sub.1 represents H or C.sub.1-4 alkyl,R.sub.2 represents benzoyl, benzyl, or alpha-hydroxybenzyl, the aromatic ring being optionally substituted by a halogen atom,R.sub.3 and R.sub.4, which are identical or different, represent hydrogen, lower-alkyl, or lower-alkenyl, or form between them with the formamidine function a heterocycle,R.sub.5 represents hydrogen or C.sub.1-4 lower-alkyl or forms with R.sub.4 a double bond (--N.dbd.R.sub.4) in the case of pseudoaromatic heterocycles,n equals 0 or 1,A represents a linear or branched C.sub.1-4 alkylene chain,X represents hydrogen, halogen, C.sub.1-4 lower-alkyl, C.sub.1-4 lower-alkoxy, or nitro, and pharmaceutically-acceptable salts thereof, are disclosed.The compounds and pharmaceutical compositions thereof are used, optionally in combination with other active principles, as drugs for the treatment of gastrointestinal ailments, especially as gastric antisecretory and antiulcer agents.

Abstract: Compounds of the formula: ##STR1## wherein A is CH.sub.2 ; n is 0 or 1; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, aralkyl and cycloalkyl; Z is the residue from a non-steroidal anti-inflammatory carboxylic acid compound; and M is a pharmaceutically acceptable cation or a metabolically cleavable group; and the pharmaceutically acceptable salts thereof; and a non toxic pharmaceutically acceptable carrier.These compounds are useful as inhibitors of 5-lipoxygenase.

Abstract: Compounds such as 1-(4-bromoacetamidobenzyl)-5-methoxy-2-methylindole-3-acetic acid, N-(4-bromoacetamidophenyl) anthranilic acid and N-(3-bromoacetamidophenyl) anthranilic acid function as irreversible ligands for nonsteroidal antiinflammatory drug (NSAID) and prostaglandin binding sites. It is therefore expected that these compounds, and analogs thereof, will have utility as anti-inflammatory drugs, as affinity labeling agents and as ligands for use in affinity chromatography.

Abstract: A cosmetic preparation consists essentially of a mixture of a stable oil/water emulsion of cosmetically acceptable ingredients and a stable water/oil emulsion of cosmetically acceptable ingredients. The new preparation is prepared by mixing the two original emulsions such that a superfinely dispersed product is obtained. The particle size of the inner phases of the emulsions is 2-50 .mu.m. The preparation provides needed ingredients such as fats or moisture to skin of varying types. An example of the cosmetic preparation is a cream containing jojoba oil.

Abstract: The present invention relates to the use of the sulphenic acid amides of the general formula (I) ##STR1## in which X represents identical or different halogen atoms, Y.sup.1 and Y.sup.2 are identical or different and represent hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or NO.sub.2 andZ represents halogen, --OH, --NHOH or the group --OR.sup.1,in whichR.sup.1 denotes optionally substituted radicals from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aryl, aralkyl and heterocyclyl, orZ represents the group ##STR2## in which R.sup.2 and R.sup.3 are identical or different and denote hydrogen or a heterocyclic radical, orZ represents the group --OMin whichM denotes ammonium or the equivalent of an alkali metal, alkaline earth metal or heavy metal cation,for prolonging the duration of a high activity in agents for combating soil pests.

Abstract: Novel film-forming gel compositions are described comprising from 10-40% by weight of a water dissipatable polymer, from 10 to 40% by weight of humectants and 20-60% by weight of water. The gel compositions may also be in the form of an emulsion comprising from 15-30% by weight of a water dissipatable polymer, from 15 to 35% by weight of humectants, up to 40% by weight of emollients, from 15 to 35% by weight water and a small amount of emulsifier. Additionally the gels of the present invention may contain optional agents such as, for example, coloring agents, pigments, preservatives, medical agents, cosmetic agents or agents to modify the refractive index of the gel.

Abstract: Novel bis-S-alkylbenzene derivatives capable of inhibiting lipoxygenase, inparticular, 5-lipoxygenase are disclosed. It is expected that the compounds, which are hardly metabolized in vivo, are highly useful in the treatment and/or prevention of various diseases, including allergic diseases such as asthma, inflammation, myocardial infarction, nephritis, scabies and gout.

Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.

Abstract: The present invention relates to 1-substituted derivatives of 4-methoxy-2,3,6-trimethylbenzene which are useful in cosmetic or pharmaceutical preparations for use in the treamtnet of dermatological complaints connected with a keratinisation disorder, dermatological complaints having an inflammatory and/or immuno-alleric component or ophthalmological complaints.

Abstract: Cosmetic comprising a diglyceride which is liquid at room temperature, and a polyol type humectant. It may take any form such as an oily cosmetic, emulsion cosmetic, aqueous cosmetic and can suitably be applied to roughened skin, or hair requiring a humectant effect. They can provide a high, long-lasting moisturizing effect, and at the same time preserve the moisturizing function of the skin or hair after a lapse of time or even after the portion to which it was applied has been washed. These effects are further promoted by formulating to the cosmetics a specific type hydrophilic humectant.

Abstract: Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.

Abstract: Cosmetic Base composition exhibiting therapeutic properties includes an acyl fatty acid lactylate ester or alkali metal salt thereof, a sucrose fatty acid ester, and a solvent.

Abstract: Complete dissolution of a wide range of drugs in chlorofluorocarbon aerosol propellents is achieved by the presence of glycerol phosphatides, preferably phosphatidylcholine.

Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic peptides useful for treating hypertension are disclosed.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.

Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.

Abstract: The invention relates to topical antiinflammatory medicament formulations which also have analgesic activity and contain 2-(2-hydroxyethoxy)-ethyl N-(.alpha.,.alpha.,.alpha.,-trifluoro-m-tolyl) anthranilate as the active ingredient and an adjuvant which is preferably a triglyceride.