Abstract: The invention relates to 1,7-diarylpentamethine and 1,9-diarylheptamethine salts, in partricular heptacarbon or nonacarbon carboxonium salts, and streptocyanines.

Abstract: Processes for preparing &agr;-substituted benzylnitroguanidines include the steps of providing a reaction mixture comprising water, alcohol, an S-alkyl nitroisothiourea, and an &agr;-substituted benzylamine; heating the reaction mixture; steam distilling the alcohol from the reaction mixture; and isolating an &agr;-substituted benzylnitroguanidine from the remaining water layer.

Abstract: The present invention provides a method and reagent composition for attachment of target molecules onto the surface of a substrate, such as microwell plates, tubes, beads, microscope slides, silicon wafers or membranes. In one embodiment, the method and composition are used to immobilize nucleic acid probes onto plastic materials such as microwell plates, e.g., for use in hybridization assays. In a preferred embodiment, the method and composition are adapted for use with substantially flat surfaces, such as those provided by microscope slides and other plastic, silicon hydride, or organosilane-pretreated glass or silicone slide support surfaces. The reagent composition can then be used to attach a target molecule such as a biomolecule (e.g., a nucleic acid) which in turn can be used for specific binding reactions (e.g., to hybridize a nucleic acid to its complementary strand).

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) is

Abstract: A process for the separation and recycling of catalyst components from a chemical reaction mixture is disclosed. The process entails at least one extraction step.

Abstract: A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitrites or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.

Abstract: A process for the removal and recovery of quaternary salt (A) and base (D) from a reaction mixture is disclosed. The reaction mixture resulting from oxidative direct carbonylation contains in addition to (A) and (D), at least one hydroxyaromatic compound (B) and at least one reaction product (C) and optionally a solvent, and the process entails a) adding acid to the reaction mixture to cause conversion of (D) into a hydroxyaromatic compound (B2) b) separating the reaction mixture into b1.) that contains (C) and optionally (B) and/or (B2) and b2.) that contains (A) and optionally (B) and/or (B2), and c) reacting b1.) with a base (E) to re-form (D).

Abstract: The preparation of quaternary salt phenolate solutions is disclosed. The preparation entails mixing an aqueous hydroxide-containing solution with an organic phase that contains phenol and quaternary salt, distilling off the water and precipitating and filtering off the resulting salt.

Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts for the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.

Abstract: The present invention provides for a coupling system (white filler/diene elastomer) for a rubber composition based on diene elastomer reinforced with a white filler, formed by the association of a polysulphurized alkoxysilane, a zinc dithiophosphate and a guanidine derivative. The invention also provides a rubber composition usable for the manufacture of tires, comprising, as base constituents, one or more diene elastomer(s), a reinforcing white filler, a polysulphurized alkoxysilane coupling agent with which are associated a zinc dithiophosphate and a guanidine derivative. Also provided is a process for preparing such a rubber composition, and a tire or semi-finished product, in particular a tread for a tire, comprising a rubber composition according to the invention.

Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: Methods of preparing NHE-1 disclosed. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.

Abstract: Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.

Abstract: The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetranikylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.

Abstract: A process for purifying creatine is described in which the creatine to be purified in the form free of water of crystallization is introduced into a saturated aqueous solution of creatine monohydrate, in which the creatine free of water of crystallization is dissolved with hydration, crystals of creatine monohydrate precipitate from the aqueous solution and these are separated off from the aqueous solution.

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: Bromide source such as alkali metal bromide, alkaline earth metal bromide, or onium bromide, present as part of a catalyst mixture in an organic oxidative carbonylation mixture further comprising diaryl carbonate and a hydroxyaromatic compound, is often at least partially converted to organic bromide such as bromophenols. The bromide source can be recycled after reaction through treatment with an aqueous acidic bromide solution such as hydrogen bromide, preferably after removal of a major proportion of hydroxyaromatic compound such as phenol.

Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: A process for the preparation of compounds of formula is described, wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl or a radical —CH2B; A is an unsubstituted or mono- to penta-substituted, aromatic or non-aromatic, monocyclic to bicyclic heterocyclic radical; and B is phenyl, 3-pyridyl or thiazolyl, which are optionally substituted by one to rhee substituents; by means of the hydrolysis of a compound of formula wherein R1, R2 and A have the same significances as given for formula (I), and R3 signifies unsubstituted or substituted C1-C10-alkyl, C3-C6-cycloalkyl, phenyl or benzyl; whereby the reaction is carried out at a pH value of between 7 and 14, as well as starting materials for carrying out the process. The compounds of formula (I) are suitable as intermediates in the preparation of pesticidal compositions.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts for the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.

Abstract: The present invention relates to compounds, compositions, and methods which are useful for the prevention and treatment of adverse health, skin, hair, and oral conditions. The compounds, compositions, and methods are also widely applicable for use in health, skin, hair, oral, beauty, and personal care applications. In particular, the present invention relates to compounds having the structure: and the tautomers, acceptable salts, and biohydrolyzable amides, esters, and imides thereof, wherein A, Q, n, P, L1, L2, L3, L4, Z, X, B1, and B2 are defined herein.

Abstract: Guanidinium phosphanes of Formula I wherein the substituents are defined as in the specification which are useful catalyst ligands for the carbon-carbon linkage reactions of the hect reaction.

Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

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

Abstract: Substituted guanidine derivatives of the formula I ##STR1## are prepared by reacting calcium cyanamide with a primary or secondary amino carboxylic acid or a primary or secondary amino sulfonic acid or their derivatives of the formula II ##STR2## where the substituents R.sup.1 and R.sup.2 have the meanings explained in the description.

Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.

Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.

Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.

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

Abstract: The present invention provides a process for making 2-amino-2-imidazoline, guanidine, and 2-amino-3,4,5,6-tetrahydroyrimidine derivatives by preparing the corresponding activated 2-thio-subsituted-2-derivative in a two-step, one-pot procedure and by further reacting yields this isolated derivative with the appropriate amine or its salts in the presence of a proton source. The present process allows for the preparation of 2-amino-2-imidazolines, quanidines, and 2-amino-3,4,5,6-tetrahydropyrimidines under reaction conditions that eliminate the need for lengthy, costly, or multiple low yielding steps, and highly toxic reactants. This process allows for improved yields and product purity and provides additional synthetic flexibility.

Abstract: The present invention relates to compounds, compositions, and methods which are useful for the prevention and treatment of adverse health, skin, hair, and oral conditions. The compounds, compositions, and methods are also widely applicable for use in health, skin, hair, oral, beauty, and personal care applications.In particular, the present invention relates to compounds having the structure: ##STR1## and the tautomers, acceptable salts, and biohydrolyzable amides, esters, and imides thereof, wherein A, Q, n, P, L.sub.1, L.sub.2, L.sub.3, L.sub.4, Z, X, B.sub.1, and B.sub.2 are defined herein.

Abstract: There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are effective inhibitors of the cellular sodium proton antiporter (Na.sup.+ /H.sup.+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases which can be attributed to increased Na.sup.+ /H.sup.+ exchange.

Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R.sup.5 wherein R.sup.5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and where X is N, R.sup.1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above acyl guanidines.

Abstract: There are described benzoylguanidines of the formula I ##STR1## having the definitions of R(1) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II ##STR2## with guanidine. They are outstanding agents for the treatment of disorders of the cardiovascular system.

Abstract: New seco-D steroid derivatives, processes for their preparation and pharmaceutical compositions are provided, which are active on the cardiovascular system.

Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts and the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.

Abstract: Disclosed are 4-(2'-trifluoromethylethyl)benzoylguanidine and 3-methylsulfonyl-4-(2'-trifluoromethylethyl)benzoylguanidine. Also disclosed are pharmaceutical compositions and the use of the compounds in the treatment of disorders induced by ischemia.

Abstract: A process for preparing clavulanic acid and other clavam derivatives using an enzyme system from Streptomyces, particularly S. Clavuligerus.

Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and mixtures thereof. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.

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: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

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: Ultracapacitors including at least one cell with two solid, non-porous current collectors, two porous electrodes, preferably of carbon, and a porous separator between the electrodes, employ as electrolytes materials comprising at least one hexasubstituted guanidinium salt. Such salts may be employed in solution in a stable organic liquid such as propylene carbonate, or neat in liquid form. They may be prepared by first preparing a hexasubstituted guanidinium halide and then performing an anion exchange reaction, either with a salt which forms an insoluble halide such as a silver salt or by a liquid--liquid extraction method.

Abstract: 1,5-Disubstituted 5a-methylperhydroinden-3a-ol derivatives of formula (I): ##STR1## where eitherthe symbol - - - - represents a single bond,the group A is in cis configuration with respect to the 3a-hydroxy, 7a-methyl and 1-L groups, andA is (CH.dbd.CH).sub.m (CH.sub.2).sub.n OR, (CH.dbd.CH).sub.m (CH.sub.2).sub.n NR.sup.1 R.sup.2, (CH.dbd.CH).sub.m (CH.sub.2).sub.p B, OH, O(CH.sub.2).sub.q OR, O(CH.sub.2).sub.q NR.sup.1 R.sup.2 or O(CH.sub.2).sub.r B;q is an integer from 2 to 5;r is an integer from 1 to 2;orthe symbol - - - - represents a double bond,A is oxygen, CH(CH.dbd.CH).sub.s (CH.sub.2).sub.n OR,CH(CH.dbd.CH).sub.s (CH.sub.2).sub.n NR.sup.1 R.sup.2 orCH(CH.dbd.CH).sub.s (CH.sub.2).sub.p B; andL is ?CH.dbd.C(R.sup.3)!.sub.s CH.dbd.NR.sup.4 or ?CH.dbd.C(R.sup.3)!.sub.s CH.sub.2 NHR.sup.4, in the E configuration, are useful for treating cardiovascular disorders such as heart failure and hypertension.