Abstract: Processes for the preparation of pyrrolidones (7 and 8) and pyrrolidines (9 and 10) from tri-O-acetyl-D-erythro-4-pentulosonic acid esters are described. The compounds are aza sugar analogs of D-ribofuranoside and are intermediates to drugs which regulate nucleoside and nucleic acid synthesis.

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

Abstract: Phosphonamide compounds and methods of forming those compounds are provided. The inventive methods comprise forming a template opened-ring phosphonamide compound and optionally subjecting the template to a ring-closing metathesis reaction in the presence of a ring-closing catalyst (e.g., a Grubbs catalyst) to yield a heterocyclic phosphonamide. Advantageously, the template structures can be provided with a wide array of functional groups (e.g., amino acid side chains, peptides) chosen to provide particular properties to the compound.

Abstract: N-methyleneglycinates of formula (I) 1

Abstract: A process for the preparation of 1,5-dideoxy -1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.

Abstract: This invention concerns low viscosity aldimine and ketimine reactive diluents having multi-imine functionality, which are useful in automotive refinish coating compositions, including a process for making them and the coatings that contain them.

Abstract: The present invention is directed to a method for purifying pyruvic acid compounds, which method comprises reacting a pyruvic acid compound of general formula (I): wherein R1 is an optionally substituted lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl group, an aryl group, or a heterocyclic group, and R2 is a lower alkyl group, with a bisulfite of general formula (II): MHSO3  (II) wherein M is NH4 or an alkali metal, to give a bisulfite adduct of the pyruvic acid compound and then decomposing the adduct with an acid. According to the present invention, pyruvic acid compounds can be purified by simple and easy procedures without using purification techniques such as distillation or column chromatography, and the above method is advantageous as a process for the production on an industrial scale.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

Abstract: This invention provides pyridazinone derivatives encompassed by the following the formula: wherein, R1, R2, R3, R4, R5 and R7 represent a hydrogen atom and the like, and R6 represents a C1-C3 alkyl and the like. The pyridazinone derivatives have excellent herbicidal activity, therefore, they can be used as an active ingredient for herbicidal compositions and can be utilized in herbicidal method, which are also described.

Abstract: The compounds of formula I ##STR1## wherein: a) X is O, andY is OC.sub.1 -C.sub.4 alkyl; orb) X is O or S, andY is NHCH.sub.3have fungicidal properties and can be used in plant protection for controlling and preventing disease infestation.

Abstract: This invention includes an alkyl 3-oxoalkanoate, and processes for its preparation and use for the synthesis of fatty hydroxylated amino acids, fatty amino alcohols and ceramides.

Abstract: This invention provides novel cationic lipids, particularly guanidino lipids, and methods for their preparation. Also provided are polyanionic-lipid complexes comprising the lipids of the invention, their preparation and use to deliver biologically active substances, particularly nucleic acids to cells.

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 current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.

Abstract: This invention provides 1,3-oxazin-4-one derivatives represented by following general formula (I): ##STR1## in which R.sup.1 represents a phenyl group which may be substituted; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkyl group, an aralkyl group or a phenyl group which may be substituted; R.sup.4 and R.sup.5 each independently represent a lower alkyl group; and W represents an oxygen atom or a group represented by the formula --N(R.sup.6)-- in which R.sup.6 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group. There are also provided herbicidal compositions containing the derivatives and intermediates for preparing them. The compounds according to the present invention exhibit strong herbicidal activities and thus they are useful as active ingredients of agricultural chemicals.

Abstract: .alpha.-(hydroxyimino)phosphonoacetic acids (also referred to as ".alpha.,.alpha.-disubstituted trifunctional oximes" and "Troika Acids") and their derivatives, and methods to prepare them are disclosed. Also disclosed are the structures and fragmentation pathways of the .alpha.-(hydroxyimino)phosphonoacetic acids. The .alpha.-(hydroxyimino)phosphonoacetic acids and derivatives are useful as pH sensitive chelating agents, enzyme activated drugs, drug delivery agents, phosphorylating reagents and photo-activated reagents.

Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.

Abstract: The invention relates to new competitive tripeptide inhibitors of trypsin-like serine proteases, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory inhibitors for prophylaxis and treatment of related diseases.

Abstract: The present invention relates to mixtures of .alpha.-amino acids and/or derivatives thereof and cyclopentane-.beta.-amino acids and/or derivatives thereof, dipeptides of the abovementioned .alpha.-amino acids and cyclopentane-.beta.-amino acids and mixtures of the abovementioned mixtures and dipeptides which have an improved tolerability in warm-blooded animals compared with the pure cyclopentane-.beta.-amino acids.

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: 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 nitrosating C-H-acidic compounds. The process substantially avoids producing polluted wastewater.

Abstract: The present invention relates to a process for preparing compounds containing aspartate and aldimine groups corresponding to the formula ##STR1## by a) reacting 50 to 95 mole % of the primary amino groups present in a polyamine containing 2 to 6 primary amino groups with a maleic or fumaric acid ester until at least 98% of the unsaturated groups have reacted andb) subsequently reacting the remaining primary amino groups with an aldehyde.

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: 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: The present invention is directed to a new class of compound which are useful as inhibitors of the biosynthesis of nitric oxide.

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: 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: Process for preparing methyl isopropylideneaminooxyacetoxyacetate I ##STR1## by reacting in an integrated process, a) acetone with hydroxylammonium sulfate and sodium hydroxide solution to give acetone oxime, the reaction being performed in the presence of toluene and/or the acetone oxime being extracted from the reaction mixture with toluene,b) treating the toluene solution thus obtained with sodium hydroxide solution and removing water,c) exchanging toluene for a dipolar aprotic solvent by distillation,d) reacting the crystal mash thus obtained with the sodium salt of chloroacetic acid to give the sodium salt of isopropylideneaminooxyacetic acid and then treating the reaction mixture with methyl chloroacetate ande) isolating the methyl isopropylideneaminooxyacetoxyacetate formed in d).

Abstract: The present invention relates to the preparation of polymers bearing reactive functional groups. More particularly, this invention relates to the preparation of polymers containing functional acetoacetate groups and then following the polymerization reacting the acetoacetate group with a functional amine to form an enamine.Polymers of the present invention have many uses including coatings, sealants, adhesives and saturant applications, and are most useful as solutions or dispersions in water or water-cosolvent mixtures.

Abstract: This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.

Abstract: The present invention relates to an aldimine/aspartate corresponding to the formula ##STR1## wherein X represents an organic group which has a valency of n and is inert towards isocyanate groups at a temperature of 100.degree. C. or less,R.sub.1 and R.sub.2 may be the same or different and represent optionally substituted hydrocarbon radicals, or R.sub.1 and R.sub.2 together with the .beta.-carbon atom form a cycloaliphatic or heterocyclic ring andR.sub.3 and R.sub.4 may be identical or different and represent organic groups which are inert towards isocyanate groups at a temperature of 100.degree. C. or less,R.sub.5 and R.sub.6 may be identical or different and represent hydrogen or organic groups which are inert towards isocyanate groups at a temperature of 100.degree. C. or less, anda and b represent integers with a value of 1 to 5, provided that the sum of a and b is 2 to 6.

Abstract: Intermediate compounds useful for producing transfecting lipopolyamines, comprising: ##STR1## wherein m is an integer between 2 and 6 inclusive, wherein n is an integer between 2 and 5 inclusive, wherein R.sub.5 represents a hydrogen atom or a carboxyl radical but no more than one R.sub.5 represents a carboxyl, the values of m in the different fragments (CH).sub.m may be identical or different, and wherein the symbol Z R.sub.5 represent a group protecting the amine function.

Abstract: The invention relates to the field of organic chemistry and more particularly to that of therapeutic chemistry.More particularly it relates to new quaternary ammonium salts of general formula (I): ##STR1## in which Hal is a halogen atom other than fluorine R and R.sub.1, identical or different, are lower alkyl radicals, n is an integer varying from 2 to 16, Z is an alkenyl radical having up to 3 carbon atoms, a carboxyl, or the OR.sub.2 group in which R.sub.2 is a hydrogen, a lower alkyl radical, an acyl remainder, a tocol radical, a sterol radical or a carboxamide chain and A is a hydroxyl or an anion of a mineral or organic acid.The compounds according to the invention are the active ingredients of pharmaceutical compositions with an anti-tumorous and/or immuno-suppressive action.

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

Abstract: The invention relates to a process for the production of organic compounds containing aldimine or ketimine groups by the reaction of compounds containing .beta.-ketoester groups with bis-aldimines or bis-ketimines with elimination of aldehyde or ketone and to the preferred compounds obtained by this process.

Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.

Abstract: Process for preparing haloketo acid derivatives [I]: ##STR1## wherein R is H or C.sub.1-6 alkyl, and X is chlorine or bromine, which comprises reacting .beta.-oxo-acid ester [II]: ##STR2## wherein R.sup.1 is H or C.sub.1-6 alkyl, R.sup.2 is C.sub.1-5 alkyl or OR.sup.3 (R.sup.3 is C.sub.1-6 alkyl), and X is the same as above, with nitrosating agent [IV]:ONOR.sup.4 [IV]wherein R.sup.4 is H, alkyl, halogen or SO.sub.3 H to give 7-halo-2-hydroxyminoheptanoic acid ester [III]: ##STR3## wherein R.sup.1 and X are the same as above, following by reacting the product with aldehyde or ketone; and intermediates therefor, and process for preparing said intermediates. Said haloketo acid derivatives are useful as intermediate for synthesis of cilastatin, which is useful as medicament, especially as dehydropeptidase inhibitor.

Abstract: A terpene derivative represented by the general formula (I): ##STR1## wherein R.sup.1 represents a lower alkyl group; R.sup.2 represents an alkyl group, a cycloalkyl group, a cycloalkylalkyl group, an aryl group, an arylalkyl group or a heteroaryl group; n is 0 or 1 or 2; and the symbol " " represents a single or double bond with the proviso that both of the linkages adjacent to each other are not simultaneously single bonds or double bonds which are useful for the preparation of drug, food, perfume and so on, and a process for preparing thereof.

Abstract: Pesticidal substituted oxime ethers of the formula ##STR1## in which R represents in each case unsubstituted or substituted alkyl, cycloalkyl, aryl or heterocyclyl andX represents nitrogen or a CH group.

Abstract: This invention relates to the use of .alpha.- halomethyl, .alpha.-acetylenic or .alpha.-allenic derivatives of arginine and agmatine, or their dehydro analogs, in the treatment of Chagas disease and Coccidiosis.

Abstract: Emulsifier compositions capable of forming an emulsion which is stable over a wide range of temperatures and contains at least one of a N.sup..alpha. -long-chain acyl arginine higher alkyl ester of the general formula (I) or an acid-addition salt thereof: ##STR1## wherein R.sup.1 CO is a straight-chain C.sub.8-22 acyl group; and R.sup.2 is a straight-chain or branched C.sub.12-22 alkyl group, are disclosed.

Abstract: A process for preparing N-substituted amino acid esters having the formula (I): ##STR1## wherein R.sub.1 and R.sub.4, the same or different, are an alkyl, aralkyl, cycloalkyl or aryl group; and R.sub.2 and R.sub.3, the same or different,are an alkyl, aralkyl, aryl, heterocycle-alkyl, aminoalkyl or guanidylalkyl, by the reaction of .alpha.-amino acid esters with .alpha.-substituted carboxylic acid esters, under the condition of substantially free from solvent, which can afford their optical isomers in a good yield.

Abstract: Disclosed are some new aminoethylphosphinic acid derivatives useful as antibacterial agents.

Abstract: A hydroxamic acid compound represented by the general formula (I) or a salt thereof; ##STR1## wherein R.sup.1 represents a hydrogen atom, or a substituted or unsubstituted alkanoyl group, R.sup.2 represents an unsubstituted alkanoyl, substituted lower alkanoyl or substituted lower alkyl group, and m represents an integer of 3 to 7, which are useful for the prevention and/or treatment of diseases caused by lipoxygenase-mediated metablites.

Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonization of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.

Abstract: Azulenesquaric acid dyes of the formula ##STR1## where L is substituted or unsubstituted C.sub.1 -C.sub.12 -alkylene,R.sup.1 is C.sub.1 -C.sub.20 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl or substituted or unsubstituted phenyl andR.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently of the others hydrogen or substituted or unsubstituted C.sub.1 -C.sub.12 -alkyl,with the proviso that when R.sup.5 is hydrogen the positions of the substituents CH.sub.2 --L--O--CO--NHR.sup.1 and R.sup.4 on an azulene ring may also be interchanged within a ring in either or both of the azulene rings, derived from azulene intermediates that contain urethane groups, are suitable for use in an optical recording medium.

Abstract: A process is disclosed for the preparation of intermediates useful in the synthesis of aminothiazoloximino cephalosporins.

Abstract: A process for the preparation of 4-halo-3-oxo-2-alkoxyiminobutyric esters.A process for the preparation of 4-halo-3-oxo-2-alkoxyiminobutyric esters by solvent-free halogenation of the liquid substrate of a 3-oxo-2-alkoxyaiminobutyric ester with elemental halogen.

Abstract: Compounds having the formula: ##STR1## wherein R.sup.1 is --NH(C.dbd.O)OR.sup.5, --NH(C.dbd.NH)NH.sub.2 or --NH(C.dbd.N--NO.sub.2)HN.sub.2 ; R.sup.2 is hydrogen, C.sub.1-8 alkyl or C.sub.6-8 aryl; n is 2 to 6; and R.sup.5 is hydrogen,C.sub.1-8 alkyl, C.sub.6-8 aryl, or C.sub.7-8 alkaryl; are disclosed in addition to methods to employ such compounds to induce migration of endothelial cells into denuded areas of vessel lining and to treat malignant hypercalcemia.