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: The present invention provides a method for preventing or treating a human immunodeficiency virus (HIV) infection, including a new or an asymptomatic infection as well as AIDS, comprising administering to a mammal in need thereof a HIV infection preventing or treating effective amount of a &ggr;-L-glutamnyl-L-cysteine ester compound of formula (I): wherein R is a straight chain, branched or cyclic hydrocarbon group having 1-10 carbon atoms, or a straight chain or branched hydrocarbon group having 1-5 carbon atoms substituted with an aromatic group; or the oxidized dimer obtained by dehydrogenation between two &ggr;-L-glutamyl-L-cysteine esters having formula (I).

Abstract: The present invention discloses the use, in the manufacture of a preventive and therapeutic drug of a brain disease, of a compound represented by formula (1): CH2═CH—CH2—S(O)n—R  (1) [wherein R represents a hydrogen atom, an alkyl group, an alkenyl group, a substituted alkyl group, a substituted alkenyl group, an alkylthio group, an alkenylthio group, a phenyl group, a substituted phenyl group, a heterocyclic group, or a group derived from an amino acid or an oligopeptide by deletion of one hydrogen atom, and which group may have a protective group; and n is 0, 1, or 2], a glycoside thereof, or a salt of the compound or the glycoside. The drug of the present invention for ameliorating brain diseases, inhibiting reduction of brain neurons and promoting branching of neurites, is useful for the prevention and treatment of brain diseases such as dementia in association with degeneration and sloughing of brain neurons.

Abstract: A process for the preparation of S-alkylcysteines of formula ##STR1## wherein R is a lower or branched C.sub.1 -C.sub.4 alkyl group; by S-alkylation of cysteines with dialkylcarbonates.

Abstract: It is described a process for preparing (R)-2-bromo-3-phenyl-propionic acid starting from (D)-phenyl-alanine, sodium nitrite and concentrated hydrobromic acid in a mixture of an aqueous solvent and a solvent selected from the group consisting of halogenated hydrocarbons and aromatic hydrocarbons.

Abstract: Disclosed is a method for purifying homocystine comprising treating crude homocystine with a base, a method for purifying homocystine comprising recovering homocystine by neutralizing an alkaline aqueous solution of crude homocystine with an acid, and a homocystine powder containing 1,000 ppm or less of a polysulfide.

Abstract: New hydrated salts of N,N'-diacetylcystine are described, as well as processes for the preparation thereof.

Abstract: A compound of the formulaC.sup.0 BwhereinC.sup.0 stands for ##STR1## A representing O or 2H, and R.sub.0 representing SH, NH.sub.2, or C.sub.x H.sub.y --SO.sub.2 --NH--, wherein C.sub.x H.sub.y is a straight chain saturated or unsaturated hydrocarbon, with x being between 1 and 20 and y between 3 and 41, inclusive; andB stands for --NHR, where R is an aryl group.The compounds are useful for inhibiting p21ras farnesyltransferase.

Abstract: This invention relates to a method comprising reacting an amino acid derivative of the following general formula (I); ##STR1## (wherein R.sup.1 represents an amino-protective group; R.sup.0 represents hydrogen or, taken together with R.sup.1, represents an amino-protecting group; R.sup.2 represents a carboxy-protecting group; X represents a leaving group) with a thiol compound of the following general formula (II) :R.sup.3 SH (II)(wherein R.sup.3 represents an alkyl group of 1 to 7 carbon atoms, an aryl group of 6 to 10 carbon atoms, or an aralkyl group of 7 to 10 carbon atoms) to give a cysteine derivative of the following general formula (III): ##STR2## (wherein R.sup.0, R.sup.1, R.sup.2, and R.sup.3 are as defined above), wherein the reaction is conducted in the presence of a base and water in an organic reaction solvent.

Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. 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. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.

Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.

Abstract: Disclosed are novel compounds which are used as linkers to bind peptides to solid support. The novel compounds can be used for the purification of synthesized peptides and are represented by the following structural formula:X--NH--(CH.sub.2).sub.n --SO.sub.2 --CH.sub.2 --CH.sub.2 --O--CO--Y;n is an integer from 1-4; X is a thiol functionalized with a protecting group that is cleavable under acidic conditions; and Y is a leaving group.

Abstract: Compounds which inhibit prenyl transferases, particularly farnysyltransferase and geranylgeranyl transferase I, processes for preparing the compounds, pharmaceutical compositions containing the compounds, and methods of use.

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: Novel farnesyl transferase inhibitors of general formula (I) ##STR1## preparation thereof and pharmaceutical compositions containing same. In general formula (I), R.sub.1 is Y--S--A.sub.1 -- (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl or alkoxycarbonyl radical, or a radical R.sub.4 --S--, where R.sub.4 is a C.sub.1-6 alkyl radical optionally substituted by a phenyl radical, or a radical of general formula (II), ##STR2## wherein A.sub.1, X.sub.1, Y.sub.1, R'.sub.2, R'.sub.2, X.sub.2, Y.sub.2, R.sub.3, R'.sub.3 and R are as defined below, and A.sub.1 is a C.sub.1-4 alkylene radical optionally .alpha.-substituted in the >C(X.sub.1) (Y.sub.1) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical); X.sub.1 and Y.sub.1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, a >C.dbd.O grouping; R.sub.2 is a straight or branched C.sub.1-4 alkyl radical optionally substituted by a cyclohexyl radical; R'.sub.

Abstract: Peptidomimetics of the formula C.beta.X where C is cysteine, X is any naturally occuring amino acid, and .beta. is a hydrophobic spacer, most notably 2-phenyl-4-aminobenzoic acid. These compounds are effective inhibitors of p2lras farnesyltrasferase, block Ras-dependent oncogenic signalling and inhibit human tumor growth in vivo in animal models. Pro-drugs made by functionalizing terminal amino and carboxylic acid groups of peptides and peptidomimetics are also disclosed. Such functionalized derivatives demonstrate increased cell uptake. Other structural modifications are also disclosed.

Abstract: The invention concerns pharmaceutical preparations for stimulation of the immune system which comprise a cystine derivative as active ingredient.

Abstract: An improved method for isolating and purifying a glutathione derivative is disclosed. More particularly, the invention provides a method for isolating and purifying S-(1, 2-dicarboxyethyl)glutathione or its pharmacologically acceptable salt from a reaction mixture available upon reacting glutathione or its salt with either fumaric acid or its salt or maleic acid or its salt, which comprises a first step of converting the S-(1, 2-dicarboxyethyl)glutathione or salt thereof in the reaction mixture to the corresponding copper salt, dissolving the copper salt in an aqueous solution of acetic acid, formic acid or propionic acid, and removing the contaminant glutathione, oxidized glutathione and fumaric acid copper salts with the aid of activated carbon and a second step of dissolving or suspending the isolated S-(1,2-dicarboxyethyl)glutathione copper salt in water and blowing hydrogen sulfide gas through the resulting aqueous solution or suspension to remove copper.

Abstract: A compound of the formulaC.sup.1 Rwhere C.sup.1 is 3-mercapto-2-amino-propylamino and R is an aryl group. The compounds are useful for inhibiting p21ras farnesyltransferase.

Abstract: N-Acyl-S-(2-hydroxyalkyl)cysteines, their preparation and their use as intermediates for the preparation of synthetic immunoadjuvants and synthetic vaccines.Compounds of the formula I ##STR1## in which the substances X, Y, R, R.sup.1 and R.sup.2 have the meanings mentioned, are suitable for the preparation of lipopeptides and lipoamino acids.

Abstract: New crystalline organic salts of N,N'-diacetyl cystine with immunomodulating effect, processes for their preparation, pharmaceutical compositions containing them and methods of their pharmacological use.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: A process of treatment against seborrhea and/or for the cicatrization of wounds and/or for stimulation of skin cell growth involving a topical application and/or an oral administration of any composition that contains zinc cysteate, wherein zinc cysteate is based on the following formula--O--SO.sub.2 --CH.sub.2 --CH(NH.sub.2)--CO--O--ZN--and wherein the zinc cysteate is in an anhydrous or a hydrated form. Zinc cysteate is dehydrated and based on the formulaC.sub.3 H.sub.5 O.sub.5 NSZSa, 2H.sub.2 O.

Abstract: New crystalline organic salts of N,N'-diacetyl cystine with immunomodulating effect, processes for their preparation, pharmaceutical compositions containing them and methods of their pharmacological use.

Abstract: A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid, lichen planus, and canker sores, is disclosed wherein the host is treated with an effective amount of N-acetyl ysteine or a derivative thereof, or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable diluent or carrier for systemic or topical delivery.

Abstract: Peptidomimetics of the formula C-AMBA-X where C is cysteine, X is, for example, methionine or phenylalanine and AMBA is a hydrophobic spacer, notably 3-aminomethylbenzoic acid. These compounds are effective inhibitors of p21 ras farnesyltransferase. Other modifications including alternative spacers for AMBA, and replacement of the A.sub.1 A.sub.2 X component of known CA.sub.1 A.sub.2 X tetrapeptides by a non-peptide aryl or heterocyclic component are also disclosed as are various phosphonylated and arylated derivatives of peptides and peptidomimetics. Pro-drugs made by functionalizing terminal amino and carboxylic acid groups of peptides and peptidomimetics are also disclosed. Such functionalized derivatives demonstrate increased cell uptake. Other structural modifications are also referred to.

Abstract: A method of treating viral infection comprises the step of administering to a patient harboring a disease-inducing virus other than HIV-1, the virus being one for which an intracellular thiol deficit causes or exacerbates expression of viral genetic information by transcription, translation or viral replication, such as human rhinovirus, an amount effective to inhibit transcriptional or translational expression of genetic information or replication of the virus, of an N-(C.sub.1-4)-acylcysteine, such as N-acetyl cysteine, or a pharmaceutically acceptable salt thereof. Prevention of disease symptoms and reduction of their severity results from the foregoing treatment. Combination of N-(C.sub.1-4)-acylcysteine or its salt with another antiviral drug or drug for alleviating symptoms of viral infection provides additional therapeutic benefits.

Abstract: The present invention is directed to the use of a cyclopropylmethyl derivative as a protecting group for compounds containing an amino group, carboxy group, amido group, mercapto group or hydroxy group and to the compounds formed having the cyclopropylmethyl moiety as the protecting group.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: Inhibitors of nitric oxide formation from arginine useful for treating hypotension, inflammation, stroke and to restore vascular contractile sensitivity to the effects of .alpha..sub.1 adrenergic agonists are physiologically active compounds including N.sup..delta. -substituted ornithine or N.sup..epsilon. -substituted lysine moieties or monoalkyl carbon-substituted N.sup..delta. -substituted ornithine or N.sup..epsilon. -substituted lysine moieties, having the formula ##STR1## wherein R is (CH.sub.2).sub.y CH.sub.3 or H, R' is CH.sub.2 or C(H) (CH.sub.2).sub.y CH.sub.3, and R" is CH.sub.2 or C(H) (CH.sub.2).sub.y CH.sub.3, with y ranging from 0 to 5, and x is 0 or 1 and wherein none or only one of R, R' and R" provides an alkyl substituent on ornithine or lysine moiety, and wherein Q is a heme binding moiety and/or a sulfur-containing binding moiety and Q' is --NH.sub.2 when there is a double bond between the omega carbon and Q and Q' is .dbd.

Abstract: New crystalline organic salts of N,N'-diacetyl cystine with immunomodulating effect, processes for their preparation, pharmaceutical compositions containing them and methods of their pharmacological use.

Abstract: The invention comprises compositions and methods for the treatment of psoriasis.

Abstract: A compound of the formula ##STR1## wherein R is --CH(CH.sub.3).sub.2 or --C(CH.sub.3).sub.3 or a physiologically acceptable salt or optical isomer thereof useful for the treatment of particularly different lung diseases.

Abstract: A method of preparing a high specificity .sup.35 S-sulfide comprises preparing a reducing mixture comprising hydrochloric acid, hydriodic acid and hypophosphorus acid, substantially removing any sulfate present in the mixture, admixing the reducing mixture with a composition comprising an .sup.35 S-sulfate corresponding to a desired .sup.35 S-sulfide to obtain the .sup.35 S-sulfide, and recovering the .sup.35 S-sulfide from the admixture. The thus prepared .sup.35 S-sulfides are applicable to the synthesis of high specificity .sup.35 S amino acids and derivatives thereof by sulfhydrylation, e.g., in the presence of an enzyme and a .sup.35 S-sulfide or sulfhydric acid and the O-acetylated amino acid. The labeled amino acid may be separated from the reaction mixture by reverse phase chromatography.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: This invention relates to cysteine derivatives of the formula[I] and salts thereof. ##STR1## The compounds of this invention are useful for immunomodulator and treatment of liver disorder.

Abstract: Metallated compounds can be used to extract or precipitate proteins from solution. The compounds can be polymers, such as polyalkylene glycols, which can be mono- or bimetallated or smaller bis-metal chelates, such as ethylenebis(oxyethylenenitrilo)tetraacetic acid. The monometallated polymers are preferred in the extraction process whereas the bimetallated compounds are preferred in the precipitation process. In addition, new PEG compounds which are capable of chelating a variety of metals are described. Both mono- and bi-metallated forms are set forth. The new metallated compounds are very effective in extracting or precipitating proteins from solution.

Abstract: This invention relates to a glutathione-S-lower fatty acid derivative of the formula ##STR1## [wherein R.sub.1 is a lower alkyl group which may be substituted; R.sub.2 is a hydrogen atom; R.sub.3 is a hydrogen atom or a lower alkyl group which may be substituted; R.sub.4 is a hydroxyl group, a lower alkoxy group which may be substituted; n means 1] or a salt thereof, and a method for production thereof.The glutathione-S-lower fatty acid derivative of the present invention or a salt thereof shows an excellent antihepatopathic activity and can be used with advantage as a drug for the treatment of various hepatic disorders.

Abstract: This invention relates to novel diaminoalkanoic acid derivatives that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease and disseminated intravascular coagulation, to pharmaceutical compositions including such compounds, and to their use in inhibiting thrombus formation and platelet aggregation in mammals.

Abstract: Amino acids and amino acid derivatives bearing isotopic hydrogen labels at both the .alpha.- and .beta.-positions are produced when N-substituted azomethine derivatives of carboxylic acids and carboxylic acid derivatives are hydrogenated over metal catalysts in isotopically-enriched protic solvents with molecular hydrogen.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The invention features a compound of the formulaW-Y-Q-Z or W-Y-ZwhereinW is a farnesyl group, a geranylgeranyl group, a substituted farnesyl group or a substituted geranylgeranyl group; ##STR1## wherein n=1, 2, 3, 4, 5, or 6; each of T.sub.1' . . . T.sub.n' and T.sub.1" . . . T.sub.n" is independently: Fl, Br, --NHCOCH.sub.3, --NH.sub.2, a peptide, an alkane group, an alkene group, an polyethyleneglycol group, a saturated fatty acid, an unsaturated fatty acid, a monosaccharide, or a disaccharide; andZ is --COOH or salts or esters thereof, --CONH.sub.2, --NO.sub.2, --PO.sub.3 or salts or esters thereof, --C N, or --SO.sub.3 or salts or esters thereof, provided that when W is farnesyl, Y is --S--, n=2, and either T.sub.2' or T.sub.2" is --NHCOCH.sub.3, then Z is not --COOH.The compounds of the invention are capable of interfering with enzymatic methylation of a peptide having the carboxyl-terminal motif --CAAX wherein C=cysteine, A=aliphatic amino acid, and X=any amino acid.

Abstract: A compound of the formula:AN/xSwherein A represents an amino acid, N represents an .alpha.-keto acid, S represents a lower alcohol or acetone; and x ranges from 0.1 to 3.

Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.

Abstract: This invention pertains to amino acids attached to a solid support in a racemization free manner and to a method of covalently linking amino acids to solid supports for use in solid phase peptide syntheses.

Abstract: An alkylene oxide is reacted in a loop reactor with an organic compound having a reactive hydrogen atom, a gas circulation and a liquid circulation around the reactor being provided and being coupled with one another via an ejector mixing nozzle. To ensure completeness of the reaction and suppression of the formation of by-products such as dioxane, it is essential to reduce the temperature of the entire alkylene oxide gas phase to a temperature below that of the liquid phase, and this is effected by feeding and evaporating liquid alkylene oxide and by cooling of the gas phase on the unit walls.

Abstract: Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are z-2-acylamino-3-monosubstituted propenoates.

Abstract: Peptide compounds of formula (I): ##STR1## wherein A is hydrogen or an amino-protecting group; X is a member selected from the group consisting of Gly, Glu, Tyr, Asp, Phe, Ile, Ala, Pro, Leu, Hyp, Val, His, Arg, Ser, Thr, Pyr, Trp, 5-HTP, Cys, Met, .tau.-Glu, .beta.-Asp; Y is a (CH.sub.2).sub.3-6 or (CH.sub.2).sub.3-6 having an hydroxy group; R is an hydroxy group or an oxygen atom with a carboxy-protecting group; are useful as neurotropic agents.

Abstract: The invention relates to new pure D- or L-N-hydroxy-alpha-amino acids and the derivatives thereof, including optically active N-hydroxy-phenylglycine amide, which has antibiotic and antitumor activity.