Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, and use for treating cancer thereof are disclosed, wherein, the definitions of X, Y, R1, R2 and n are described in description.

Abstract: The present invention relates to novel thiourea derivatives as a modulator for vanilloid receptor (VR) and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

Abstract: The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT2B and 5-HT7 receptors having selective binding affinities for 5-HT2B and 5-HT7 receptors. The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT2B receptor antagonist having selective binding affinity for 5-HT2B receptor or a 5-HT7 receptor antagonist having selective binding affinity for 5-HT7 receptor.

Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes. The compounds of this invention have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1-5 are as defined herein. The methods of this invention are directed to administering to a warm-blooded animal in need thereof an effective amount of a compound of structure (I), typically in the form of a pharmaceutical composition.

Abstract: A process is described for preparing sodium dicyanamide, in which cyanamide is reacted simultaneously with sodium hydroxide solution and cyanogen chloride in aqueous solution at temperatures of 20 to 100° and a pH of 7.0 to 10.0. By means of the inventive process it is possible, starting from raw materials which are available in technical-grade quality, to prepare sodium dicyanamide in good yields of 75 to 95% and very high purities of up to 100% in a very environmentally friendly manner, for which reason this process is particularly highly suitable for the industrial scale.

Abstract: The present invention relates to novel substituted imide derivatives of the general formula (I) in which R1 represents optionally substituted cycloalkyl, R2 represents optionally substituted alkyl or optionally substituted cycloalkyl, R3 represents alkyl, alkoxy, alkylthio, amino, alkylamino or dialkylamino and R4 represents cyano or nitro, and to processes for their preparation and to their use for controlling animal pests and as herbicides.

Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes.

Abstract: A compound selected from the group consisting of a compound of formula I 1

Abstract: There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting on a nociceptin receptor.

Abstract: Benzoic acid derivatives of the formula I 1

Abstract: The (R)-enantiomer of 4-[[(cyanoimino)-[(1,2,2-trimethylpropyl)amino]methyl]amino]-benzonitrile as well as the corresponding (S)-enantiomer are useful for promoting hair growth such as in male pattern baldness.

Abstract: Guanidine and diaminonitroethene derivatives represented by the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined in the description, compositions thereof and methods for preparing the compounds are described. The se compounds are useful in the treatment of diseases of the central nervous system, cardiovascular system, pulmonary system, gastrointestinal system and endocrinologic system.

Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.

Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1--6 alkyl; R.sup.2 is hydrogen or C.sub.1- 6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl--S--, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.

Abstract: Disclosed are novel cyanoguanidine derivatives which are usable as an epoxy resin curing agent and are represented by the following general formula (1). A thermosetting resin composition and a photocurable and thermosetting resin composition containing the following cyanoguanidine derivatives and other derivatives as the epoxy resin curing agent are also disclosed. ##STR1## wherein R.sup.1 represents a substituent selected from the group consisting of the following substituents (a) through (k).

Abstract: Compounds of the formula: ##STR1## useful as regulators of nitric oxide synthase that indirectly modulate cyclic guanosine monophosphate (cGMP), pharmaceutical compositions thereof, for treating disorders of vascular smooth muscles, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, sickle cell anemia and diabetes.

Abstract: A butenoic acid compound of the following formula: ##STR1## in which Z is O, S, vinylene or azomethyne, A is an alkylene group and J is phenyl group, is a useful in treating heart disease.

Abstract: Oligomeric cyanoguanidines of formula I ##STR1## wherein, for example, R.sup.1 and R.sup.2 are each phenyl, R is 1,4-phenylene and n is an integer from 1 to 20, are suitable latent hardeners for epoxy resins. They are readily soluble in solvents suitable for the application of epoxy resins, and the cured products obtained therewith have a high glass transition temperature.

Abstract: A curing agent for epoxy resins having improved solubility characteristics has the formula ##STR1## where R is --CH.sub.2 C.sub.6 H.sub.4 X or --CH.sub.2 CH.sub.2 C.sub.6 H.sub.4 X,and X is either --H, --CH.sub.3, --OCH.sub.3, --OH, or --NY,and where Y is --H or CH.sub.3.Such substituted cyanoguanidines are soluble in various solvents and do not require the use of undesirable solvents necessary with cyanoguanidine (dicyanodiamide) itself.

Abstract: Compounds of the formula: ##STR1## useful as regulators of nitric oxide synthase that indirectly modulate cyclic guanosine monophosphate (cGMP), pharmaceutical compositions thereof, for treating disorders of vascular smooth muscles, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, sickle cell anemia and diabetes.

Abstract: Oligomeric cyanoguanidines of formula I ##STR1## wherein, for example, R.sup.1 and R.sup.2 are each phenyl, R is 1,4-phenylene and n is an integer from 1 to 20, are suitable latent hardeners for epoxy resins. They are readily soluble in solvents suitable for the application of epoxy resins, and the cured products obtained therewith have a high glass transition temperature.

Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.

Abstract: An improved method of preparing 1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane from alkali dicyanamide and a hexamethylene diammonium salt in alcoholic solution or suspension. The reaction is carried out in the presence of a limited amount of water and of a catalytic amount of a base, preferably a tertiary amine. The pH of the reaction mixture at the start of the reaction is 8 to 10. After the reaction is over, the reaction mixture is compounded with water at a temperature above 80.degree. C. and the coarse product which crystallizes out is separated from the liquid phase.Preferably, sodium dicyanamide and hexamethylene diamine dihydrochloride, preferably formed in situ from aqueous 1,6-diaminohexane and aqueous hydrochloric acid, are reacted at pH 9-9.5 in n-butanol in the presence of 0.1 to 20% by wt. water in relation to the solvent including water.1,6-di(N.sup.3 -cyano-N.sup.

Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-assocated hypertension, hyperaldosteronism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.

Abstract: Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.

Abstract: Disclosed are alpha-acyloxyketone derivatives which are useful as intermediates for production of N-cyano-N'-methyl-N"-[2-{(5-methyl-1H-imidazol-4-yl)methylthio}ethyl]guani dine (common name: Cimetidine; Cimetidine applies hereinafter) and Cimetidine-related compounds which have an action of controlling secretion of gastric acid and are useful as a drug for treating gastric ulcer.

Abstract: A novel cyanoguanidine derivative represented by the following general formula (I): ##STR1## wherein X stands for a hydrogen atom, a chlorine atom or a bromine atom, and R stands for a lower alkyl group, is an effective precursor for the synthesis of N-cyano-N'-methyl-N"-(2-(5-methyl-4-imidazolylmethylthio(ethyl)-guanidine (Cimetidine) which has an action of controlling secretion of gastric acid and is valuable as an agent for the remedy of a gastric ulcer.This cyanoguanidine derivative is prepared by reacting a methylvinylketone derivative with a mercaptoguanidine derivative or by reacting an amidinoketone derivative with a halogenating agent.

Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.

Abstract: Novel substituted phenyl and benzyl nitroguanidine and phenyl and benzyl cyanoguanidine compounds. Methods for increasing crop yield, inhibiting lodging of graminaceous crops, and inducing cytokinin-like responses in crop plants with said novel guanidine compounds and derivatives thereof, as well as methods for inhibiting deterioration and/or extending the shelf life of harvested fruit, vegetables, and ornamentals are disclosed.

Abstract: This invention relates to novel cyanoguanidine compounds and the intermediate N'-cyano-N-(1,2,3,4-tetrahydro-1-naphthyl)-S-methylisothiourea. These novel compounds are useful as animal growth promoting agents.

Abstract: This invention relates to a novel cyanoguanidine compound, N'-cyano-N-(1,2,3,4-tetrahydro-1-naphthyl)guanidine, which is useful as an animal growth promoting agent.

Abstract: Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.

Abstract: There are provided novel nitroguanidine and cyanoguanidine compounds. A method of dessicating and defoliating plants by applying to the foliage thereof certain nitroguanidine or cyanoguanidine compounds and a method for the selective preemergence control of undesirable broadleaf weeds and grasses in the presence of graminaceous crops are disclosed.

Abstract: Process for preparing diphenylazomethines of formula (II) ##STR1## by decarboxylation of diphenylazomethines of formula (I) ##STR2## in which X.sub.1 and X.sub.2 each denote, independently of each other, a hydrogen atom or a halogen atom or a methyl radical,R.sub.1 is H or linear or branched (C.sub.1-4) alkyl radical,R.sub.2 is the radical COOH, a linear or branched (C.sub.1-4) alkyl radical, the radical CONH.sub.2 or a linear or branched COO(C.sub.1-4) alkyl radical, andR.sub.3 denotes a hydrogen atom or the methyl radical.

Abstract: Novel substituted phenyl and benzyl nitroguanidine and phenyl and benzyl cyanoguanidine compounds. Methods for increasing crop yield, inhibiting lodging of graminaceous crops, and inducing cytokinin-like responses in crop plants with said novel guanidine compounds and derivatives thereof, as well as methods for inhibiting deterioration and/or extending the shelf life of harvested fruit, vegetables, and ornamentals are disclosed.

Abstract: Cystamine derivatives of the formula: ##STR1## [wherein n represents 2 or 3, R.sup.1 and R.sup.2 each represents a hydrogen atom, or an alkyl group optionally substituted by a hydroxy, amino, alkylamino or dialkylamino group, or represents a cycloalkyl or aryl group, and X.sup.1 represents a group selected from the formulae .dbd.N--CN, .dbd.N--NO.sub.2, .dbd.N--COR.sup.3, .dbd.N--COOR.sup.3, .dbd.N--NH--CONH.sub.2, .dbd.N--SO.sub.2 R.sup.3, .dbd.CH--NO.sub.2, .dbd.CH--SO.sub.2 R.sup.3, .dbd.C(CN).sub.2, .dbd.C(CN)COOR.sup.3 and .dbd.C(CN)CONH.sub.2 (wherein R.sup.3 represents an alkyl or aryl group), or R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl group optionally substituted by a hydroxy, amino, alkylamino or dialkylamino group, or represents a cycloalkyl or aryl group and X.sup.1 represents an oxygen or sulphur atom] have been found to be useful in the promotion of the growth of non-human animals including birds.

Abstract: The present invention provides a process for the modification of the crystal form of dicyandiamide, wherein dicyandiamide is crystallized from aqueous solution in the presence of 0.001 to 10% by weight of polyvinyl alcohol and/or of a water-soluble cellulose ether derivative, referred to the amount of dicyandiamide. The crystalline dicyandiamide obtained in this manner has outstanding flow and storage properties and its mechanical strength is substantially improved.

Abstract: A class of naphthalene aminoalkylene ether and thioether compounds exhibiting pharmacological activity including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.

Abstract: 1-Cyano-3-(fluoroalkyl)guanidines of the formula: ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 are the same or different members of the class of hydrogen, fluorine, lower alkyl or lower alkenyl provided that at least one member is fluorine or fluoro-substituted alkyl or alkenyl. These compounds are useful for their biological properties, e.g. in treating elevated blood pressure and Parkinson's disease.

Abstract: Trisubstituted cyanoguanidines of the formula ##STR1## in which R.sup.1 represents an optionally substituted phenyl or phenylalkyl radical, an alkyl radical with more than 1 carbon atom, a substituted alkyl radical, an alkenyl or alkinyl radical or an optionally substituted cycloalkyl radical,R.sup.2 represents an optionally substituted alkyl radical or an alkenyl or alkinyl radical andR.sup.3 represents an optionally substituted alkyl radical, an alkenyl or alkinyl radical, an optionally substituted cycloalkyl radical or an optionally substituted phenyl or phenylalkyl radical, orR.sup.2 and R.sup.3, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical, which optionally contains an oxygen atom as a further hetero-atom,or a physiologically acceptable acid addition salt thereof, which possess fungicidal properties. Processes for their preparation are also taught.

Abstract: Novel phosphonic acid salts produced from ethane- or methanephosphonic acid, dicyandiamide and/or guanidine and optionally ammonia and corresponding to the formula ##STR1## wherein n, p, q, t and y are each 1 or 2, are particularly suitable for fireproofing organic fibre materials. Synthetic and/or cellulose-containing fibre materials are treated with an aqueous solution of the phosphonic acid salts and are then dried preferably at 60.degree. to 200.degree. C. The applied phosphonic acid salts impair only negligibly the textile-mechanical properties of the treated fibre materials, especially of the cellulose-containing fibre materials dried at 120.degree. to 150.degree. C.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: a is 1 to 3;b is 0 to 2;c is 2 to 4;d is 1 to 5;X is sulphur, oxygen or --CH.sub.2 --;Y is oxygen, sulphur, NR.sub.4 or CHR.sub.5 wherein R.sub.4 is hydrogen, C.sub.1-4 alkyl, NO.sub.2 or CN, C.sub.1-4 alkylsulphonyl or phenylsulphonyl optionally substituted in the phenyl moiety by one or two substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, fluorine, chlorine or bromine, and R.sub.5 is NO.sub.2, C.sub.1-4 alkylsulphonyl or optionally substituted phenylsulphonyl as defined for R.sub.4 ;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-4 alkyl, or C.sub.3-6 cycloalkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached represent a pyrrolidino or piperidino ring;R.sub.6 and R.sub.7 are independently hydrogen or C.sub.

Abstract: Novel cyanoguanidine derivatives, and acid addition salts thereof useful as medicines which have pharmacological actions such as anti-secretory effect, local anesthesia action and the like; and process for the preparation thereof.

Abstract: Novel cyanoguanidine derivatives, and acid addition salts thereof useful as medicines which have pharmacological actions such as anti-secretory effect, local anesthesia action and the like; and process for the preparation thereof.

Abstract: Novel cyanoguanidine derivatives having the formula ##STR1## wherein Ar is a phenyl or pyrrol-1-yl group substituted by one or more substituents selected from halogen, trifluoromethyl, lower alkyl, lower alkoxy and nitro and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen or lower alkyl or R.sub.1 and R.sub.2 taken together form dimethylene or trimethylene, lower blood pressure and, in some cases are also anti-ulcer agents.

Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.

Abstract: Propenimidates are provided having the formula: ##STR1## wherein X and Y are independently O or S; andR.sup.1 and R.sup.2 are independently C.sub.1 -C.sub.4 alkyl, (CH.sub.2).sub.n OR.sup.3 where R.sup.3 is C.sub.1 -C.sub.4 alkyl and n is 1 or 2, CH.sub.2 CH.sub.2 Cl, or CH.sub.2 CF.sub.3, provided that when R or R.sup.2 is CH.sub.2 CH.sub.2 Cl or CH.sub.2 CF.sub.3, then the respective X or Y is O.Preferred propenimidates have X and Y as O and R.sup.1 and R.sup.2 as methyl or ethyl.The propenimidates are made by preparing a monohydrohalide salt from a dihydrohalide salt of the formula: ##STR2## and then contacting the monohydrohalide salt with cyanamide. The propenimidates upon heating ring close to pyrimidines which are useful in preparing herbicidal compounds.

Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl; R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.

Abstract: Hexamethylene.bis-dicyandiamide is safely prepared in good yield and desired purity by a novel method which comprises reacting N-cyano-O (or S)-alkyl-iso (or isothio) urea with hexamethylenediamine. The desired product is useful as an intermediate of chlorhexidine which is an antibacterial agent.