Abstract: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.

Abstract: Reaction products of guanidine compounds or salts thereof, polyepoxide compounds and polyhalogen compounds may be used as levelers in metal electroplating baths, such as copper electroplating baths, to provide good throwing power. Such reaction products may plate with good surface properties of the metal deposits and good physical reliability.

Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Abstract: Compounds of formula (I) or salts thereof, in which R1, R2, R3, R4, R5, R6, X and Y are defined as in claim 1, can be prepared by a process characterized in that a compound of the formula (II) or a salt thereof, is reacted to a compound of the formula (III) or a salt thereof, and an aluminium(III) source, optionally, in the presence of a protic additive or solvent selected from the group consisting of alcohols or amines. The compounds (I) are suitable to be used for the preparation of heterocyclic compounds corresponding to (I) where the group Al(X)(Y) is replaced with an optionally substituted carbon atom, or s-triazine derivatives thereof.

Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Abstract: A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK? and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

Abstract: Provided are novel organic electroluminescent compounds, and organic electroluminescent devices and organic solar cells employing the same. Specifically, the organic electroluminescent compounds according to the invention are characterized in that they are represented by Chemical Formula (1): wherein, A, B, C and D independently represent CR5 or N, provided that A, B, C and D cannot represent CR5 all at the same time. Since the organic electroluminescent compounds according to the invention have good luminous efficiency and excellent color purity and life property of material, OLED's having very good operation life can be manufactured therefrom.

Abstract: This invention relates to methods of preserving the integrity of peptides in the gut. In particular it concerns the use of certain compounds as inhibitors of gut proteases. Compounds identified as having gut protease inhibitory activity are biguanides, certain bile acids and pharmaceutically acceptable salts of these compounds. This activity makes these compounds useful for co-administration with prophylactic or therapeutic peptides. This invention relates to methods of inhibiting gut proteases and peptide formulations comprising these gut protease inhibitor.

Abstract: Disclosed herein is the process for the preparation of 1-(4-chlorophenyl)-5-isopropyl-biguanide hydrochloride (Proguanil hydrochloride), Formula-I, an antimalarial agent.

Abstract: The invention provides methods, PCR primers and sequence determination oligonucleotides for determining a human's capacity to metabolise a substrate of the CYP2C19 enzyme using genetic analysis.

Abstract: A compound represented by formula (1), a tautomer thereof, or a salt of the compound or tautomer, which is useful as a bactericide/disinfectant. In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like, R2 represents a hydrogen atom or an optionally substituted alkyl group, or alternatively R1 and R2 may combine together with an adjacent nitrogen atom to form an optionally substituted nitrogen-containing heterocyclic group; R4 represents a hydrogen atom or an optionally substituted alkyl group; R3 represents an optionally substituted alkyl group; and R5 and R6 each represents a hydrogen atom or a methyl group, excluding a compound wherein both R2 and R4 represent a hydrogen atom and a compound wherein both R1 and R4 represent a hydrogen atom are excluded.

Abstract: The present invention provides a process for producing 1-(3,4-dichlorobenzyl)-5-octylbiguanide or a salt thereof, the process comprising reacting 1-cyano-3-octylguanidine or a salt thereof, with 3,4-dichlorobenzylamine or a salt thereof, in an ester-based organic solvent. According to the present invention, the reaction can be carried out at a low temperature using general-purpose equipment, and 1-(3,4-dichlorobenzyl)-5-octylbiguanide or a salt thereof can be produced in a high yield by a safe and easy process.

Abstract: The invention provides a novel apparatus and method for preparing a solution of a shear sensitive material.

Abstract: The present invention provides a process for producing 1-(3,4-dichlorobenzyl)-5-octylbiguanide or a salt thereof, the process comprising reacting 1-cyano-3-octylguanidine or a salt thereof, with 3,4-dichlorobenzylamine or a salt thereof, in an ester-based organic solvent. According to the present invention, the reaction can be carried out at a low temperature using general-purpose equipment, and 1-(3,4-dichlorobenzyl)-5-octylbiguanide or a salt thereof can be produced in a high yield by a safe and easy process.

Abstract: Biguanide/quaternary ammonium compounds and the use of same as antimicrobial agents in pharmaceutical compositions are described. The biguanide/quaternary ammonium compounds are useful in the preservation of pharmaceutical compositions, particularly ophthalmic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting contact lenses.

Abstract: The present invention relates to novel benzylideneamino guanidines of general formula and to the use of these benzylideneamino guanidines as melanocortin receptor agonists or antagonists. The invention further relates to benzylideneamino guanidines which show selectivity to the MC1 and MC4 melanocortin receptors as agonists and/or antagonists.

Abstract: Compounds of the formulae are disclosed. A method of protecting subjects from infections caused by an organism of the group: Plasmodium sp. Mycobacterium sp., P. falciparum, and Pneumocystis carinii by administering to the subjects liable to infections, a prophylactically effective amount of a compound of the foregoing formulae; and a method of reducing the level of infection in subjects caused by the above-listed organism by administering to the subjects an infection reductively effective amount of a compound of the foregoing formulae are also disclosed.

Abstract: The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.

Abstract: A compound of formula (I) or (II), wherein X is hydrogen, halogen, alkyl, aralkyl,aryloxy, arylalkoxy or alkoxy, Y is hydrogen, halogen, alkyl, aralkyl, aryloxy, arylalkoxy or alkoxy, or formula (a) wherein A and B are different and one of A and B is CH2 and the other is O, NH, or S or A and B are both CH2 or CH═, and Ra, Rb, and Rc are the same or different and are hydrogen, halogen, alkyl, alkoxy, aryloxy, aralkyl or arylalkoxy. R1 is hydrogen, and R2 is hydrogen, C1-C6 alkyl or aryl which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkyl, which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkoxy, aralkyl, aryloxy or aryl, C1-C6 alkoxy, aralkyl, arylalkoxy, aryloxy or aryl, which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkyl or C1-C6 alkoxy; and pharmaceutically acceptable salts thereof; with the proviso that when R2 is phenyl and Y is hydrogen, X is not chlorine.

Abstract: Compounds of the formulae 1

Abstract: The invention relates to novel substituted 2-amino-4-alkylamino-1,3,5-triazines of the formula (I) in which R1 represents in each case optionally substituted alkyl having 2 to 6 carbon atoms or cycloalkyl having 3 to 6 carbon atoms, R2 represents hydrogen or represents alkyl having 1 to 4 carbon atoms, A represents oxygen or methylene, Ar represents in each case optionally substituted phenyl, naphthyl or heterocyclyl, and Z represents hydrogen, represents halogen or represents in each case optionally substituted alkyl, alkoxy, alkylcarboxyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenyl or alkinyl, to processes and to novel intermediates for their preparation and to their use as herbicides.

Abstract: The present invention provides a process for preparing a compound of the general formula (I): wherein R1 to R5 are independently selected from hydrogen, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6 alkoxy, all optionally substituted by one or more of halogen, hydroxy and aryl groups, as well as being independently selected from amino, mono- or disubstituted amino, alkenyloxy, acyl, acyloxy, cyano, nitro, aryl and alkylthio groups, which process comprises reacting a compound of the general formula (II): wherein R1 to R5 are as defined in formula (I), with aminoguanidine bicarbonate in a mixture of a water-soluble solvent and polyphosphoric acid.

Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.

Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.

Abstract: There is disclosed compound according to the formula: ##STR1## wherein A, independently,=CH.sub.3 or CH.sub.2 CH.sub.3, P=1 or 2; and ##STR2## wherein X=NH.sub.2, CH.sub.3 or CH.sub.2 CH.sub.3 ; X'=CH.sub.3 or CH.sub.2 CH.sub.3 ; Y=NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 ; and Z=H, CH.sub.3 or CH.sub.2 CH.sub.3 ; or ##STR3## wherein Y' and Z', independently,=H, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 or N.sup.+ (CH.sub.3).sub.3 ; Q is N or CH; and salts thereof.

Abstract: A method for removing biguanide from aqueous sources, such as swimming pools, is disclosed. The method includes the steps of bringing at least one polymeric metaphosphate into contact with the aqueous source in a sufficient concentration to form particles containing the biguanide. The particles containing at least a portion of the biguanide can then be removed by various means, including filtration or vacuuming.

Abstract: The present invention encompasses the use of the compounds of formula as given below to detect certain specific protein structures which are present in nuclear localization sequences ##STR1## wherein A is, independently CH.sub.3 or CH.sub.2 CH.sub.3 and R is ##STR2## and salts thereof.

Abstract: The invention presents a biguanide derivative or its salt expressed by a formula: ##STR1## (where R.sup.1 and R.sup.2 are as defined in Specification), or formula: ##STR2## (where A and R.sup.3 is as defined in specification). This biguanide derivative or its salt is preferably used as the effective amount of a disinfectant for humans, animals, medical appliances, etc.

Abstract: There are provided compounds of the formula ##STR1## wherein R.sup.1 is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, aryl and arlkyl, R.sup.3 is selected from the group consisting of same group of values as R.sup.5, R.sup.5 is selected from the group consisting of substituted and unsubstituted alkyl of 1-10 carbon atoms, aryl, cycloalkyl and heterocycloalkyl of 3-8 carbon atoms, wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, cycloalkyl of 3-8 carbon atoms, lower alkenyl, lower alkynyl, nitro, lower alkoxy, lower alkoxycarbonyl, phenyl loweralkyl, phenyl, mono and polyhalophenyl, phenoxy, mono and polyhalophenoxy, R.sup.6 and R.sup.7 may be the same or different and are hydrogen, alkanoyl or alkoxyalkanoyl, R.sup.7 may also have the same value as R.sup.

Abstract: The present invention relates to a process for the production of a biguanide derivative useful as an intermediate for triazine-type herbicides, in which the biguanide derivative can be produced at high yields by reacting a phenoxyalkylamine salt with dicyandiamide in a solvent containing a paraffinic hydrocarbon having 8 to 15 carbon atoms, or by reacting a free phenoxylakylamine with a hydrogen halide in a solvent containing a paraffinic hydrocarbon having 8 to 15 carbon atoms and reacting the resultant a phenoxyalkylamine salt with dicyandiamide in the same solvent without isolating the phenoxyalkylamine salt.

Abstract: The present invention relates to bisguanidine derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, alkyl, alkenyl, alkenyl, alkoxyalkyl, haloalkenyl; or cycloalkyl which has 5-12 carbon atoms in the ring and may be substituted, or benzyl which may be substituted, with the proviso that only one of R.sup.1 and R.sup.2 can be hydrogen; orR.sup.1 and R.sup.2 are, together with the atoms which they substitute, a heterocyclic ring which may be substituted;X is CH.sub.2, O, a single bond, NH, N-alkyl or N-benzyl whose phenyl ring may be substituted,n is 5 to 8,and their plant-compatible acid addition salts and their metal complexes and fungicides containing these compounds.

Abstract: A bisbiguanide compound of the formula:R.sup.1 R.sup.2 N.C(:NR.sup.6)NH.C(:NH)NH.CH.sub.2 X-- --(CH.sub.2).sub.3 NH.C(:NH)NH.C(:NR.sup.7)NR.sup.3 R.sup.4 Vor a tautomer thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 2-16C alkoxyalkyl radical, a 3-12C cycloalkyl radical, a (3-12C cycloalkyl)-(1-4C alkyl) radical, or an optionally substituted phenyl or phenyl(1-4C alkyl) radical, or R.sup.1 and R.sup.2 and the nitrogen atom to which they are attached, or R.sup.3 and R.sup.4 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical each of which may bear 1-3C alkyl substituents; each of R.sup.6 and R.sup.7, which may be the same or different, is hydrogen or a 1-8C alkyl radical; and X is a substituted ethylene or ethylidene radical of the formula:--CH.

Abstract: A bis(1-substituted biguanide) derivative of the formula:R.sup.3 R.sup.4 N.C(:NR.sup.5)NH.C(NR.sup.9)NR.sup.1 --X--NR.sup.2.C(:NR.sup.9)NH.C(:NR.sup.6)--NR.sup.7 R.sup.8 Vor a tautomeric form thereof, wherein R.sup.1, R.sup.2 and R.sup.9, which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 3-16C cycloalkyl radical, a (3-12C cycloalkyl)-(1-4C alkyl) radical, an optionally substituted phenyl or naphthyl radical, an optionally substituted phenyl(1-4C)alkyl or naphthyl(1-4C)alkyl radical or an optionally substituted diphenylmethyl radical, provided that at least one of R.sup.1, R.sup.2 and R.sup.9 is other than hydrogen; R.sup.3, R.sup.4, R.sup.7 and R.sup.8, which may be the same or different are each hydrogen, or an alkyl, cycloalkyl, (cycloalkyl)alkyl, phenyl, naphthyl, phenylalkyl, naphthylalkyl, or diphenylmethyl radical as defined above, or a 2-16 alkoxyalkyl radical, or R.sup.3, R.sup.4 and the nitrogen atom to which they are attached, or R.sup.7 and R.sup.

Abstract: Polyether biguanide salts of the formula: ##STR1## wherein: y ranges from 0 to 6,z ranges from 2 to 7,A is an anion selected from the group consisting of chloride, bromide, sulfate, bisulfate, phosphate, dihydrogen phosphate and hydrogen phosphate,n is the valence of the anion, andR.sub.1 is an alkyl of 9 to 18 carbon atoms or alkylphenyl of 15 to 18 carbon atoms, are diluted in water solution. In a preferred embodiment, R.sub.1 is nonylphenyl.These salts are surface active agents used as hair conditioning agents, foam boosters, corrosion inhibitors, ore flotation agents, fabric softeners or germicides, etc.

Abstract: This invention describes novel chemical compounds which are 1-amidino-3-phenylureas. The method of preparing these compounds and their pharmaceutical uses is also disclosed.