Abstract: The invention relates to stabilized amido acid compositions. More particularly, the invention relates to compositions of amido acids, such as 6-nonanoylamidohexanoic acid, stabilized with antioxidants. The stabilized amido acid compositions are useful in the manufacture of bleach activators such as sodium nonanamidohexanoyloxybenzenesulfonate. Bleach activators made from the stabilized amido acids of the invention are capable of possessing improved coloration.

Abstract: Compounds of the formula I; useful for the treatment of pain wherein A, Z, B, R1, X and D are as defined in the specification, methods of making such compounds, methods of using such compounds and pharmaceutical compositions containing such compounds.

Abstract: Cleavable compositions and methods of use especially in MALDI MS analysis of hydrophobic proteins.

Abstract: The present invention provides non-hygroscopic, crystalline salts of levodopa ethyl ester (LDEE), wherein the salt is the octanoate salt, the myristate salt, the succinate salt, the succinate dihydrate salt, the fumarate salt or the fumarate dihydrate salt of levodopa ethyl ester. The subject invention also encompasses compositions comprising a levodopa ethyl ester salt and a carrier and processes for making these compositions. In addition, the subject invention concerns pharmaceutical compositions comprising a levodopa ethyl ester salt and a pharmaceutically acceptable carrier, as well as processes for making these pharmaceutical compositions.

Abstract: 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde may be produced from 3-(3-methyl-4-hydroxyphenyl)-3-methylbutyric acid by converting the carboxyl group into a formyl group. N-[N-[3-(3-methyl-4-hydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which is useful as a sweetener having a high potency of sweetness, can be easily and efficiently prepared on an industrial production from such an aldehyde derivative, via a reductive alkylation reaction with aspartame. Therefore, 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde is extremely excellent as an intermediate for the production of N-[N-[3-(3-methyl-4-hydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester.

Abstract: A substituted aminomethyl-phenyl-cyclohexane derivative of formula I or Ia, and their a diastereomer, enantiomer, or of a salt formed with a physiologically tolerated acid. Also disclosed are method for preparing the substituted aminomethyl-phenyl-cyclohexane derivative, pharmaceutical compositions comprising the same and method of using the same for treating pain, urinary incontinence, itching, diarrhea, inflammatory and allergic reactions, depression, drug or alcohol abuse, gastritis, cardiovascular diseases, respiratory tract diseases, coughing, mental illnesses and epilepsy.

Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: The present invention relates to a class of carbocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.

Abstract: Novel amidinophenol derivatives of formula (IB) and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of leukotine B4 and inhibitors of phospholipase A2 and/or trypsin; methods for preventing or treating diseases induced by phospholipase A2 and/or trypsin comprising administering to a patient a compound of formula (IB); and methods for treating diseases induced by leukotine B4 comprising administering to a patient a compound of formula (IB) or a known amidinophenol derivative of formula (IA)

Abstract: The present invention provides novel phenoxyacetic acid derivatives represented by the general formula: wherein R1 represents a hydroxy group, a lower alkoxy group, an aralkoxy group, an amino group, or a mono or di(lower alkyl)amino group; one of R2 and R3 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, while the other is a hydrogen atom; R4 represents a halogen atom, a lower alkyl group, a halo(lower alkyl) group, a hydroxy group, a lower alkoxy group, an aralkoxy group, a cyano group, a nitro group, an amino group, a mono or di(lower alkyl)amino group, a carbamoyl group, a mono or di(lower alkyl)carbamoyl group or a group represented by the general formula: —NHCOR5 (wherein R5 represents a hydrogen atom or a lower alkyl group); the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration, and pharmaceutically acceptable salts thereof, which have excellen

Abstract: A method is provided for processing a solution having optical isomers to obtain a (2R,3S) target isomer: 1

Abstract: N,N diacyl O-substituted imide bleach activators and compositions employing them are provided. The activators have the general formula: wherein X is selected from O, NR16 and S; e is 0 or 1; f is 0 or 1; R16 is selected from H and C1-C4 linear or branched, saturated or unsaturated alkyl groups; and R1 is preferably phenyl or C7-C13 linear or branched chain, saturated or unsaturated alkyl; R2 is preferably C1-C10 branched or unbranched, saturated or unsaturated alkyl and R3 is preferably C1-C12 linear or branched chain, saturated or unsaturated alkyl. Bleach additive and bleaching compositions including the bleach activators and methods of cleaning fabrics are also provided.

Abstract: Novel alkylenediaminediacetic acid or alkylenediaminetriacetic derivatives of formula (I): or an organic or inorganic salt thereof, their process of preparation, and their use in cosmetic and pharmaceutical compositions, such as for protecting the body against oxidative stress are discussed.

Abstract: Albuterol formulations packaged in an oxygen-permeable plastic container have a long shelf life at room temperature. The formulations consist essentially of albuterol or a pharmaceutically acceptable salt thereof, sodium chloride, and water, have a pH of about 4, and contain less than 0.08% by weight of albuterol aldehyde and less than 1 ppm dissolved oxygen.

Abstract: The invention provides a resin-immobilized imine represented by the following formula: P—Q—N—═CH—R   I [in the formula, P represents the principal chain of a resin polymer; Q represents a substituted or unsubstituted hydrocarbon side chain or a substituted or unsubstituted hydrocarbon side chain with a heteroatom interposed therein; R represents a substituted or unsubstituted hydrocarbon group or heterocyclic group] and a resin-immobilized &bgr;-aminocarbonyl compound of the following formula: which can be released as &bgr;-aminocarbonyl compound from the solid phase; and the invention also provide a resin-immobilized amine of the following formula: —P—Q1—O—Q2—NH2   III [Q1 and Q2 independently represent a hydrocarbon chain such as arylene, alkylenearylene or arylenealkylene], which is essential for solid state synthesis; and the invention has enabled the solid state synthesis of &bgr;-am

Abstract: Embodiments include reagents to modify a bioactive species for incorporating a bifunctional boronic compound complexing moiety for subsequent conjugation to a different or same bioactive species having pendant phenylboronic acid moieties of General Formula I, wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the putative bifunctional boronic compound complexing reagent with a bioactive species, wherein group R2 is selected from one of H and OH moieties, and wherein group R3 is selected from one of an alkyl and a methylene bearing an electronegative substituent. Group Z is a spacer selected from (CH2)n and CH2O(CH2CH2O)n2, wherein n is an integer of from 1 to 5, and wherein n2 is an integer of from 1 to 4. Group Z2 and Z3 is a spacer and need not be the same.

Abstract: The present invention comprises small molecular weight, non-peptidic inhibitors of formulae I-VII of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).

Abstract: 3-amino-3-arylpropan-1-ol compounds of formula I: R1 and R2 independently denoting C1-6 alkyl, or together denoting a (CH2)2-6 ring optionally substituted by phenyl, R3 denoting C3-6 alkyl, C3-6 cycloalkyl, aryl optionally containing heteroatoms and optionally substituted by R6 to R8, or a substituted C1-3 alkylphenyl of formula XII:  R4 and R5 independently denoting C1-6 alkyl, C3-6 cycloalkyl, phenyl, benzyl, or phenethyl, or together forming a (CH2)3-6 or CH2CH2OCH2CH2 ring, R6 to R8 independently denoting H, F, Cl, Br, CHF2, CF3, OH, OCF3, OR14, NR15R16, SR14, phenyl, SO2CH3, SO2CF3, C1-6 alkyl, CN, COOR14, or CONR15R16, or together forming a OCH2O, OCH2CH2O, CH═CHO, CH═C(CH3)O or (CH2)4 ring, R14 denoting C1-6 alkyl, phenyl, benzyl, or phenethyl, R15 and R16 independently denoting H, C1-6 alkyl, phenyl, benzyl or phenethyl, and A denoting optionally substituted aryl optionally containing heteroatoms, or a diastereomer or enantiomer or pharmaceutica

Abstract: The invention relates to novel azines, to a process for their preparation and to their use as fungicides.

Abstract: A tryptase inhibitor comprising as an active ingredient at least one member selected from among guanidinoaliphatic acid derivatives of the formula (I), guanidinobenzoic acid derivatives of the formula (II), guanidinophenol derivatives of the formula (III), amidinophenol derivatives of the formula (IV), and novel guanidinophenol derivatives of the formula (V) (in the formulae, Gu is guanidino).

Abstract: Compounds represented by general formula I or salts thereof, wherein n is an integer of 2 or 3; R represents a straight-chain or branched saturated alkyl group having 4 or 4 carbon atoms, a cyclopentyl group, a cyclohexyl group or the like, Y represents a hydroxyl or amino group, A represents a hydrogen atom, a hydroxyl, methoxy, nitro group or the like, Q represents a hydrogen atom or a hydroxyl or methoxy group. They can be formulated to give pharmaceutical compositions that are effective as prophylactic or therapeutic agents for allergic diseases associated with IgE production inhibitors or IgE antibodies.

Abstract: The invention relates to novel substituted oximes, to a process for their preparation and to their use as fungicides.

Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.

Abstract: Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halog

Abstract: Picornaviral 3C protease inhibitors of formula I, obtainable by chemical synthesis, that inhibit or block the biological activity of the picornaviral 3C protease are described. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: Compounds of the formula I and the isomers thereof, in which either a) X is an N atom and Y is OR11 or N(R12)R13, or b) X is CH and Y is OR11, and in which furthermore: R11 is C1-C4alkyl; R12 and R13, independenty, are hydrogen or C1-C4alkyl; A is an O atom or the group NR4; and wherein R1, R2 and R3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.

Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B  (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.

Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.

Abstract: Disclosed are “acid-amide” calixarenes of formula (I) wherein: L is [—CH2—] or [—O—CH2—O—] and may be the same or different between each aryl group; R5 is H, halogen, or C1-C10 aliphatic hydrocarbyl group, C6-C20 aryl group, C6-C10 hydrocarbyaryl group, any of which may optionally be substituted by one or more halo or oxo groups or interrupted by one or more oxo groups, and R5 may be the same or different on each aryl group; R1 comprises an optionally protected carboxy group; two groups out of R2, R3, and R4 are H; the one group out of R2, R3, and R4 not being H comprises an amide group. The amide group may be linked to a second calixarene to form a dimer. Also disclosed are methods of use of such calixarenes for the purposes of metal sequestration, especially of lanthanides and actinides. Also disclosed are calixarene dimer derivatives of the calixarenes of the invention. Also disclosed are processes for preparing the calixarenes and dimers.

Abstract: N,N diacyl O-substituted imide bleach activators and compositions employing them are provided. Bleach additive and bleaching compositions including the bleach activators and methods of cleaning fabrics are also provided.

Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.

Abstract: The present invention relates to new phenylamine derivatives, processes for preparing them and their use as pharmaceutical compositions.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: Novel amidinophenol derivatives of formula (IB) and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of leukotine B4 and inhibitors of phospholipase A2 and/or trypsin; methods for preventing or treating diseases induced by phospholipase A2 and/or trypsin comprising administering to a patient a compound of formula (IB); and methods for treating diseases induced by leukotine B4 comprising administering to a patient a compound of formula (IB) or a known amidinophenol derivative of formula (IA)

Abstract: A naphthol derivative represented by the general formula (I), [wherein Y and Y′ indicate —(CONH)n—X or —COR; X is a phenyl group, a naphthyl group, an anthraquinonyl group, a benzimidazolonyl group or a carbazolyl group; R is a hydroxyl group, an alkoxy group having 1 to 6 carbon atoms, a halogen atom, a benzyloxy group, a phenyloxy group or a phenacyloxy group; R2 is a hydrogen atom, an alkaline metal, an alkyl group having 1 to 6 carbon atoms, an acyl group having 1 to 6 carbon atoms or a phenylalkyl group; Z is a group selected from the group consisting of a hydrogen atom, a halogen atom, a nitro group, a nitroso group and an amino group (Z may be substituted on any ring of the naphthalene ring); and n is an integer of 1 or 2; provided that R2 and Z do not simultaneously indicate a hydrogen atom when both R simultaneously indicate a hydroxyl group], and a process for producing the same.

Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,

Abstract: A photoactive compound that is the reaction product of an alkenyl azlactone compound and a nucleophilic aromatic ketone is described. Mer units derived from this compound can be used, for example, to crosslink via a hydrogen abstracting mechanism acrylic polymers in which they are incorporated.

Abstract: This invention discloses an improved method for the [2+2+2] cyclotrimerization reaction in aqueous solutions using a water soluble transition metal catalyst.

Abstract: Novel alkylenediaminediacetic acid or alkylenediaminetriacetic derivatives of formula (I): or an organic or inorganic salt thereof, their process of preparation, and their use in cosmetic and pharmaceutical compositions, such as for protecting the body against oxidative stress are discussed.

Abstract: A process for manufacturing a highly purified, stable, non-hygroscopic, crystalline composition of L-DOPA ethyl ester. The L-DOPA ethyl ester is an active ingredient in many pharmaceutical preparations for the treatment of patients suffering from Parkinson's Disease and related indications.

Abstract: Method for the acylation of amines are disclosed in which includes reacting a first reactant containing an amine group with a second reactant containing an acyl halide group, wherein the reaction takes place in the presence of secondary carboxylic acid salt form, of formula I: R4R5CHCOOH  I wherein R4 is an alkyl group having 1 to 10 carbon atoms; and R5 is an alkyl group having 1 to 10 carbon atoms.

Abstract: Disclosed are compounds of the formula: R represents hydrogen or is a C-3 to C-6 cycloalkyl or C-4 to C-10 straight or branched carbon chain alkyl-cycloalkyl or a group —B—D, where B is C-2 to C-10 straight or branched carbon chain alkyl and D is hydroxy or alkyloxy or 2,3-dihydroxypropyl or 2,3-dialkyloxypropyl or 2,2-dialkyl-1,3-dioxolane-5-methyl, where alkyl is C-1 to C-10 straight or branched carbon chain; W represents CH(CH3)CH2—, C(CH3)2CH2—; Z represents hydrogen, —NHCOR2, —NHCONR2R3 or —NHSO2R2 or —NHSO2NR2R3 or —NHCOOR4 wherein R4 is alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, alkoxyaryl, cycloalkyl of from 3 to about 8 carbon atoms.

Abstract: The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.

Abstract: A pharmaceutical composition for treatment of Parkinson's disease comprising a compound of levodopa dissolved in a non-degradative solvent which allows transdermal administrtion of levodopa. The compound of levodopa is an alkyl-ester of levodopa and the solvent is a formulation comprising a substantially non-aqueous solvent, a transdermal enhancer and a detergent. The alkyl-ester of levodopa is preferably levodopa-ethyl-ester (LDEE).

Abstract: 14-Aza analogs of PGF.sub.2.alpha., PGD.sub.2, and PGE.sub.2 and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: Reagents suitable for the modification of a bioactive species for the purpose of incorporating a bifunctional boronic compound complexing moiety for subsequent conjugation to a different (or the same) bioactive species having pendant phenylboronic acid moieties of General Formula 1, ##STR1## wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the putative bifunctional boronic compound complexing reagent with a bioactive species, wherein group R.sub.2 is selected from one of H and OH moieties, and wherein group R.sub.3 is selected from one of an alkyl and a methylene bearing an electronegative substituent. Group Z is a spacer selected from (CH.sub.2).sub.n and CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.n.sbsb.2, wherein n is an integer of from 1 to 5, and wherein n.sub.2 is an integer of from 1 to 4. Each of group Z.sub.2 and Z.sub.3 is a spacer selected from CH.sub.2 Ar, CH.sub.2 CONHCH.sub.2 Ar, CH.sub.2 CONH(CH.sub.2).sub.n.sbsb.3 CO--NHCH.sub.2 Ar, and (CH.sub.2).sub.n.sbsb.

Abstract: The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.