Abstract: The present invention relates to 2-amino-2-alkyl-4 heptenoic and heptynoic ac derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: The present invention contains novel compounds useful as nitric oxide synthase inhibitors.

Abstract: The present invention relates to 2-amino-2-alkyl-3 heptenoic and heptynoic ac derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors

Abstract: The present invention relates to 2-amino-2-alkyl-3 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

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 discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention contains halogenated 2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: The invention is directed to a method for preventing or treating the symptoms associated with sensitive skin by applying an effective amount of at least one nitric oxide synthase inhibitor to treat or prevent the symptoms associated with sensitive skin to an individual in need thereof.

Abstract: The present invention provides novel compounds of the formula I and II for the treatment of non-insulin dependent diabetes mellitius (NIDDM) and a new use of known compounds for this purpose.

Abstract: Compounds of the formula I wherein X, Y, Z, R1 and R2 are as defined in claim 1, and their salts and solvates, can be used as integrin inhibitors in particular for the prophylaxis and treatment of circulatory disorders, for thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, for pathological processes which are maintained or propagated by angiogenesis and in tumour therapy.

Abstract: The present invention relates to a process for producing creatine or creatine-monohydrate, comprising the step of reacting N-methylglycine, sodium N-methylglycinate and/or potassium N-methylglycinate with S-methylisothiourea and/or S-methylisothiourea sulfate in water or in a mixture of water and an alcohol solvent under the temperature from 15° C. to 140° C. and a pH of 7-13. By using the process of the present invention creatine or creatine-monohydrate with a higher purity can be produced at a much lower cost.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: Methods and compositions for inhibiting at least one isoform of nitric oxide synthase are provided. Pharmaceutical compositions include derivatives of arginine as well as dipeptides and dipeptide analogs that contain nitroarginine or another unnatural amino acid. Compositions can be used to selectively inhibit particular isoforms of nitric oxide synthase.

Abstract: The present invention provides methods and compositions for enhancing the effectiveness of oxazolidinone antibacterial agents against gram-negative organisms infection by using an arginine derivative.

Abstract: A dicreatine citrate or tricreatine citrate, comprising two and three creatine cations per citrate anion, respectively. The dicreatine citrate has a melting point of about 146° F., and the tricreatine citrate has a melting point of about 154° F.

Abstract: Creatine pyruvates are described which have the general formula (I) (creatine)x(pyruvate)y(H2O)n  (I) where x=1 to 100 y=1 to 10 and n=0 to 10 These creatine pyruvates, which are produced by way of the relatively simple reaction of creatine with pyruvic acid, can be used to enhance long-term performance and strength in the field of sport, to reduce weight and body fat in the field of health, to treat conditions of oxygen deficit (ischemia), obesity and overweight, as food supplements and radical scavenger.

Abstract: Creatine pyruvates are described which have the general formula (I)(creatine).sub.x (pyruvate).sub.y (H.sub.2 O).sub.n (I)wherex=1 to 100y=1 to 10 andn=0 to 10These creatine pyruvates, which are produced by way of the relatively simple reaction of creatine with pyruvic acid, can be used to enhance long-term performance and strength in the field of sport, to reduce weight and body fat in the field of health, to treat conditions of oxygen deficit (ischemia), obesity and overweight, as food supplements and radical scavenger.

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: A process for preparing guanidine derivatives, in particular creatine, is described and entails an O-alkylisourea salt and a primary or secondary amine being reacted in the presence of crystals of a guanidine derivative.

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Abstract: Selective and irreversible inhibitors of neuronal isoform of nitric oxide synthase catalyzed production of nitric oxide are L-ornithine or L-lysine derivatives having the formula ##STR1## wherein Q is H or (CH.sub.2).sub.r CH.sub.3 where r ranges from 0 to 15, x is 1 or 2, R" is CH.sub.2 or C(H) (CH.sub.2).sub.y CH.sub.3 where y ranges from 0 to 5, R' is CH.sub.2 or C(H) (CH.sub.2).sub.z CH.sub.3 where z ranges from 0 to 5, R is H or (CH.sub.2).sub.s CH.sub.3 where s ranges from 0 to 5, with none or only one of R, R' and R" providing an alkyl substituent on ornithine or lysine moiety, R.sup.III is OH or is an alkoxy group of 1 to 6 carbon atoms or is an amino acid or peptide attached in amide linkage through its free .alpha.-amino group, and R.sup.IV is --H or an acyl group of 1 to 6 carbon atoms or is an amino acid or peptide attached in amide linkage through its free .alpha.-carboxylate group, and mixtures thereof with corresponding D-isomers. A preferred compound is N.sup.

Abstract: The present invention is directed to peptides of the formulas (i) Xaa-Yaa-Arg, wherein either Xaa is any amino acid residue and Yaa is Glu or Xaa is absent and Yaa is any amino acid residue with the exception of Pro; (ii) Arg-Yaa-Xaa, wherein either Xaa is any amino acid residue and Yaa is Glu or Xaa is absent and Yaa is any amino acid residue with the exception of Asn; (iii) Xaa-Arg-Yaa, wherein Xaa is any amino acid residue and Yaa is Glu; and (iv) Yaa-Arg-Xaa, wherein Xaa is any amino acid residue and Yaa is Glu, and to derivatives thereof, which exert an inhibitory effect on macrophage migration and/or macrophage phagocytic activity. In addition, the peptides and derivatives thereof exert an inhibitory effect on the ability of macrophages and T cells to adhere to extracellular matrix and/or fibronectin. The peptides and derivatives thereof exert an inhibitory effect on a humoral and/or cellular immune response.

Abstract: Compounds of this invention have the formula:X--(CH.sub.2).sub.n --C(O)NH--A--C(COOR.sup.5)R.sup.3 R.sup.4or a pharmaceutically acceptable salt thereof, e.g. ##STR1## which are useful for inhibiting fibrinogen binding to blood platelets, thereby inhibiting platelet aggregation.

Abstract: Substituted guanidine derivatives of the formula I ##STR1## are prepared by a) converting urea into an alkylated isourea of the formula II ##STR2## and b) reacting the alkylated isourea with a primary or secondary amine of the formula III ##STR3## where the substituents R.sup.1, R.sup.2 and R.sup.10 have the meanings explained in the description.

Abstract: Novel N-carboxyalkylpeptidyl compounds represented by the formula ##STR1## which are found to be useful inhibitors of matrix metalloendoproteinases which degrade major components of articular cartilage and basement membranes causing degenerative diseases such as arthritis, periodontal disease, corneal ulceration and the like, and certain cancers, are described.

Abstract: A new use of the enantiomer (R)-ketoprofen and of its salts with suitable organic and inorganic bases in the therapy of neutrophil-dependent diseases and phlogistic processes is described as well as pharmaceutical preparations containing such compounds and useful for oral, parenteral or topical administration.

Abstract: Azoamidine compounds shown by the general formula [1] ##STR1## wherein R.sup.1 and R.sup.2 are independently a lower alkyl group, R.sup.3 and R.sup.4 are independently a hydrogen atom or a lower alkyl group, and X is a divalent hydrocarbon group, or its hydrate, show high reactivity and are capable of forming an intramolecule salt with an amidino group and having high solubility into water, methanol and other solvents.

Abstract: The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases.

Abstract: Peptide-copper complexes are disclosed which stimulate the growth of hair on warm-blooded animals. In one aspect of this invention, the peptide-copper complexes are dipeptides or tripeptides chelated to copper at a molar ratio ranging from about 1:1 to 3:1, with the second position of the peptide from the amino terminus being histidine, arginine or a derivative thereof. The peptide-copper complexes may be formulated for administration by, for example, topical application or injection. Any affliction associate with hair loss, including hair loss associated with both androgenetic and secondary alopecia, may be treated with the peptide-copper complexes of this invention.

Abstract: Substituted guanidine derivatives of the formula I, ##STR1## are prepared by reacting haloformamidinium salts of the formula II, ##STR2## where Hal can be Cl, F, Br and I, with primary or secondary amines of the formula III ##STR3## where the substituents R.sup.1 and R.sup.2 have the meanings explained in the description.

Abstract: The present invention provides novel compounds of the formula I and II for the treatment of non-insulin dependent diabetes mellitius (NIDDM) and a new use of known compounds for this purpose.

Abstract: The present invention relates to the formation of a salt between carnitine and creatine which has unique and useful attributes over creatine monohydrate or carnitine base. An acid-base reaction between carnitine and creatine causes the formation of the salt composition. Further, the invention provides a salt form of carnitine which is very stable and non-hygroscopic. The carnitine creatinate product of the present invention is represented by the following: ##STR1## wherein X is an integer between about 0 and 5.

Abstract: Hydrosoluble organic salts of creatine are disclosed. The salts are useful in the dietetic and food industry.

Abstract: A stable aqueous solution of creatine acid sulfate provides a source of creatine to an animal when taken orally. The aqueous solution of creatine acid sulfate (after neutralization and buffering) has a pH of about 7.2 to about 7.8 and is stable for at least six months at room temperature. The creatine acid sulfate is produced by adding creatine monohydrate to a sulfuric acid solution in a stoichiometric amount to result in creatine acid sulfate having a pH initially of 2.0-3.0. The resulting creatine acid sulfate is diluted with water and neutralized to raise the pH and avoid the formation of creatinine. The resulting creatine acid sulfate solution preferably contains a buffering and neutralizing agent such as tribasic potassium phosphate which forms mono- and dibasic potassium phosphates by interaction with the hydrogen ions liberated from the acid sulfate.

Abstract: Substituted guanidine derivatives of the formula I, ##STR1## are prepared by a) reacting calcium cyanamide with an alcohol of the formula R.sup.10 --OH to give an isourea derivative of the formula II, ##STR2## and b) reacting the substituted isourea with a primary or secondary amine of the formula III, ##STR3## where the substituents R.sup.1 and R.sup.2 and R.sup.10 have the meanings explained in the description.

Abstract: Disclosed is an acid-funtionalized polyurethane adduct and a process for the preparation of such adduct. The adduct having a linear or preferably branched structure comprises a plurality of internal urethane linkages and one or more terminal carboxylic acid groups per molecule. Such acid-funtionalized polyurethane adducts find value in the manufacture of crosslinked aqueous rubber latexes such as might be used in paint compositions.

Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.

Abstract: Provided is a novel surfactant which is less irritating to the skin or the mucous membrane than prior art surfactants, which exhibits excellent conditioning effects and fabric softening effects, and which can be widely used in a toiletry or detergent composition. Basic amino-acid derivatives or salts thereof obtained by reacting glycidyl ethers with basic amino acids or salts thereof are incorporated into a toiletry or detergent composition or a conditioning agent.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Crystalline N.sup.G -monomethyl-L-arginine hydrochloride is disclosed. At least three distinguishable isomorphic forms are present. The solid salt can be made by dissolving N.sup.G -monomethyl-L-arginine in hydrochloric acid and crystallising out N.sup.G -monomethyl-L-arginine hydrochloride. The crystallising step requires several months at low temperature. However, the process can be facilitated by seeding with crystals of N.sup.G -monomethyl-L-arginine hydrochloride. Alternatively, crystalline N.sup.G -monomethyl-L-arginine hydrochloride can be prepared by dissolving a salt of N.sup.G -monomethyl-L-arginine other than the hydrochloride salt with hydrochloric acid and removing the original salt forming ion by crystallising out the hydrochloride salt.

Abstract: Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C.sub.1-3 alkyl groups; a group of formula --(CH.sub.2).sub.p X(CH.sub.2).sub.q -- where p is 2 or 3, q is 1 or 2 and X is S(O).sub.x where x is 0, 1 or 2, O or NR.sup.2 where R.sup.2 is H or C.sub.1-6 alkyl; or a group of formula --(CH.sub.2).sub.r A(CH.sub.2).sub.s -- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or diC.sub.

Abstract: A process for preparing crystalline N.sup.G -monomethyl-L-arginine hydrochloride is disclosed. The process comprises dissolving N.sup.G -monomethyl-L-arginine in hydrochloric acid and crystallising out N.sup.G -monomethyl-L-arginine hydrochloride. The crystallising step requires several months at low temperature. However, the process can be facilitated by seeding with crystals of N.sup.G -monomethyl-L-arginine hydrochloride. Alternatively, crystalline N.sup.G -monomethyl-L-arginine hydrochloride can be prepared by dissolving a salt of N.sup.G -monomethyl-L-arginine other than the hydrochloride salt with hydrochloric acid and removing the original salt forming ion by crystallising out the hydrochloride salt.

Abstract: A process is disclosed for the preparation of N.sup.G -monoalkyl-L-arginine and related compounds and salts thereof, for example N.sup.G -monomethyl-L-arginine by reacting N-alkylaminoiminomethane sulphonic acid of formula (II) with an amino acid of formula (III).

Abstract: The present invention relates to advaced glycosylation endproducts formed by the reaction of arginine-lysine or lysine-arginine dipeptides, optionally as part of a larger protein or amino-containing-biomolecule, with reducing sugars. These AGEs can be used in various diagnostic and therapeutic methods.

Abstract: The salts of S(+) 2-(3-benzoylphenyl)propionic acid and of R(-) 2-(3-benzoylphenyl)propionic acid with an organic base such as D-lysine, L-lysine, L-arginine, (R) 3-(4-phenylpiperazin-1-yl)propane-1,2-diol and (S) 3-(4-phenylpiperazin-1-yl)propane-1,2-diol, the process for their preparation and the corresponding pharmaceutical compositions containing said salts are described.

Abstract: The present invention is directed to the use of an inhibitor of NO activity, such as a nitric oxide scavenger or an NO synthase inhibitor, as an antitumor therapy to reduce tumor blood flow and oxygenation. The invention is also directed to administration of a nitric oxide scavenger or a nitric oxide synthase inhibitor to enhance the effectiveness of tumor therapy with hypoxic or acidic chemotherapeutic agents or hyperthermia. The invention is also directed to the administration of a nitric oxide synthase substrate to a subject previously administered a nitric oxide synthase inhibitor, in order to selectively inhibit tumor perfusion. In a specific example, administration of cell free hemoglobin, a nitric oxide scavenger, in conjunction with mitomycin C, a hypoxic cytotoxin, results in a significant delay in tumor growth of a human tumor xenograft in a mouse compared to mitomycin C alone.

Abstract: Crystalline N.sup.G -monomethyl-L-arginine hydrochloride is disclosed. At least three distinguishable isomorphic forms are present. The solid salt can be made by dissolving N.sup.G -monomethyl-L-arginine in hydrochloric acid and crystallising out N.sup.G -monomethyl-L-arginine hydrochloride. The crystallising step requires several months at low temperature. However, the process can be facilitated by seeding with crystals of N.sup.G -monomethyl-L-arginine hydrochloride. Alternatively, crystalline N.sup.G -monomethyl-L-arginine hydrochloride can be prepared by dissolving a salt of N.sup.G -monomethyl-L-arginine other than the hydrochloride salt with hydrochloric acid and removing the original salt forming ion by crystallising out the hydrochloride salt.

Abstract: The present specification discloses a ruminant feed additive composition which contains as an active ingredient a phosphoric acid-amino acid-polyvalent metal composite salt (final composite salt) which is insoluble in neutral or alkaline water and is soluble in acidic water and which can be obtained by treating a composite salt composed of a basic amino acid, magnesium and phosphoric acid with a salt of a divalent or trivalent (polyvalent) metal other than magnesium, or by treating the above-mentioned composite salt with the polyvalent metal salt and a condensed phosphoric acid component (alone) or the condensed phosphoric acid component and a phosphoric acid component (in combination), this composition taking the form of a powder or granules.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Administration of argininosuccinate synthetase activity reducing agents, e.g., argininosuccinate synthetase induction blocking agents (e.g., antibiotics that bind to DNA sequences present in the upstream regulatory region of the argininosuccinate synthetase gene, such as mithramycin) and argininosuccinate synthetase inhibitors (e.g., L-citrulline antagonists such as methyl citrulline and L-aspartate antagonists such as D-aspartate) is useful to prevent or treat sepsis or cytokine-induced systemic hypotension, is useful in the treatment of sepsis or cytokine-induced systemic hypotension to restore vascular sensitivity to the effects of .alpha..sub.1 -adrenergic agonists, and is useful to suppress an immune response, e.g., in treating inflammation. In one embodiment, certain argininosuccinate synthetase activity reducing agents are used together with arginine antagonists to treat sepsis or cytokine induced hypotension.