Abstract: Compounds of Formula I Each R is independently linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy or one R is H and the other R is linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy; R1 is selected from the group consisting of COCH3, CO2R3, CONH2, CONH(R4)2, CN, COX(CH2)n-N—(R2)(R4)(R3), and the quaternized salt form of the formula COX(CH2)n-N—(R2)(R4)(R3)+Y−; X is O or NH; n is an integer of 1 to 5; Y is an anion; and R2, R3 and R4 are independently linear or branched C1 to C20. Hair care formulations and other compounds containing compounds of Formula I, and methods for protecting hair and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.

Abstract: The compounds of the invention which encompasses a class of compounds having the property of anti-carcinogenic activity against human myeloma r comprising 4-oxo-2-butenoic acid compounds and 3-hydrazino-2,4-dioxobutanoic acid compounds and more specifically those novel derivatives: 4-(4-Chloro-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-4-oxo-but-2-enoic acid methyl ester (OF-07); 2-{N′-[(2-Bromo-phenyl)-phenyl-methylene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-09); 2-{N′-[(4-Dimethylamino-phenyl)-phenyl-methylene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-10) and 2-{N′-[1-(4-Chloro-phenyl)-ethylidene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-20) and the use of 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (OF-06); 4-(4-Ethoxy-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester (OF-13); 4-b

Abstract: The present invention relates to an uracil compound of the formula [I]: wherein W represents oxygen, sulfur, imino or C1 to C3 alkylimino; Y represents oxygen, sulfur, imino or C1 to C3 alkylimino; R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl; R2 represents C1 to C3 alkyl; R4 represents hydrogen or methyl; R5 represents C1 to C6 alkyl, C1 to C6 haloalkyl, or the like; X1 represents halogen, cyano or nitro; X2 represents hydrogen or halogen; and each of X3 and X4 independently represents hydrogen, halogen, C1 to C6 alkyl, or the like. The present compound has an excellent herbicidal activity.

Abstract: An organic compound useful for detecting the total quantity of isocyanate in an environmental sample is provided. The compound is 9-anthrcenylmethyl-1-piperazinecarboxylate (PAC), an isocyanate derivatizing agent. A process for producing PAC and methods for detecting a particular isocyanate monomer or the total isocyanate in environmental samples using PAC & related isocyanate derivatizing agents are also provided.

Abstract: A process of reacting a nitroaniline compound of formula (2): with an acid anhydride or acid halide is carried out in the presence of an alkali metal compound or an alkaline earth metal compound to produce an acylnitroaniline derivative. The process further includes the step of reacting the resulting product with a compound of formula (5); R2—Y to produce an N-acylnitroaniline derivative of formula (1): The N-acylnitroaniline derivative of formula (1) is a useful intermediate for the production of pharmaceuticals.

Abstract: The invention features screening assays for compounds that are potentially useful for treating or preventing a proliferative disease. The assays are based on contacting a candidate compound with a cell containing a nucleic acid including a HER2 regulatory element and a reporter sequence. In addition, the invention features compounds identified by the assays of the invention. The invention further features compounds structurally related to those identified by the screening assays. Finally, the invention features methods of treating or preventing a proliferative disease using the compounds of the invention.

Abstract: This invention encompasses a method for the treatment or prevention of prostaglandin mediated diseases comprising administering to a mammalian patient a compound of formula I: in an amount that is effective to treat or prevent said prostaglandin mediated disease. Novel compounds are also disclosed.

Abstract: Disclosed are compounds of formula I wherein A, R1, R2, R3, R4 and R5 are described in the specification, pharmaceutical formulations comprising these compounds, the use of these compounds are medicaments, the use of these medicaments in the treatment of and/or prevention of diabetes, especially non-insulin dependent diabetes (NIDDM or Type 2 diabetes), as well as methods for treating diabetes comprising administration of these compounds.

Abstract: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: Wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, hydroxy, phenyl-(CH2)0-6—, phenyl-(CH2)0-6O—, C3-C6 cycloalkyl, —(CH2)—C3-C6 cycloalkyl, halogen, C1-C3 perflouroalkyl and C1-C3 perfluoroalkoxy where phenyl can be substituted with from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl or trifluoromethoxy; R1 is hydrogen, C1-C6 alkyl or phenyl-(CH2)1-6— where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R2 and R3 are H, C1-C6 alkyl, phenyl-(CH2)0-3—, halo and C1-C3 perflu

Abstract: An analgesic agent is provided which has analgesic action and anti-inflammatory action without significant side effects found in conventional analgesics.

Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.

Abstract: This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carbosyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and water.

Abstract: A method of selectively controlling undesirable vegetation in crops by using a postemergent application of an herbicidally effective amount of a metal chelate of a 2-(substituted benzoyl)-1,3-cyclohexanedione compound to the locus of such undesirable vegetation.

Abstract: The present invention relates to a process for producing a bis(4-hydroxy-3-nitrophenyl) compounds, characterized by nitrating a bis(4-hydroxyphenyl) compound wherein two phenyl groups are bonded to each other directly or through an electron-donating bridging group, sulfoxide group, sulfone group or carbonyl group in an inert solvent using nitric acid under the condition of substantially free from any other acid. According to the process, the target compounds reduced in the content of trinitrates can be produced in high yield and further recrystallizing the compound easily gives in high yield a high-purity products suitable for use as a raw material of producing a heat-resistant polymer and so on because the content of a trinitro-substitued compound in that compound is low.

Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.

Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.

Abstract: Novel naphthol derivatives, and various azo compounds and metal complexes prepared by using the derivatives are provided.

Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.

Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioarylalkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selec

Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.

Abstract: Bidentate phosphine ligands of the formula 1

Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solvent

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 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: A process for producing (2R, 3S)-3-amino-4-phenylbutane-1,2-epoxide compounds which comprises treating a (2S, 3S)-3-amino-1-halo-2-hydroxy-4-phenylbutane compound or a (2S, 3S)-3-amino-4-phenylbutane-1,2-epoxide with a carboxylic acid quaternary ammonium salt or a carboxylic acid metal salt a quaternary ammonium salt and a quaternary ammonium salt, to give a (2S, 3S)-1-acyloxy-3-amino-2-hydroxy-4-phenylbutane compound, further treating the same with a sulfonic acid halide in the presence of an organic base to give a (2S, 3S)-1-acyloxy-3-amino-2-sulfonyloxy-4-phenylbutane compound, furthermore treating said compound with an inorganic base. An intermediate for the production of an HIV protease inhibitor can be produced from L-phenylalanine.

Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Het is an optionally substituted heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12.

Abstract: The present invention relates to a class of compounds represented by Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.

Abstract: The present invention provides a simple and inexpensive method for producing &agr;-hydroxy-&bgr;-aminocarboxylic acids and their esters. An ester of an N-protected &agr;-amino acid ester is converted into a &bgr;-ketosulfoxide, which is then processed with an acid to give an &agr;-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected &agr;-acyloxy-&bgr;-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce &agr;-hydroxy-&bgr;-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.

Abstract: A new family of inadone and tetralone tubulin-binding compounds (TBs) is disclosed. Unlike classical TBs, which inhibit mitosis among affected dividing cells, the TBs of the invention possess two unique properties: (1) they induce apoptosis among stationary phase (non-dividing) malignant cells, yet do not impair the viability of normal nonproliferating cells; and, (2) they affect cells which have acquired MDR more powerfully than they affect cells without MDR. Thus, the TBs of the invention provide means to target malignant cells for chemotherapy, even after previous therapies have failed, without affecting normal cells and tissues in the host.

Abstract: Novel phenyl derivatives which are useful as endothelin receptor antagonists.

Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.

Abstract: A chemical compound having the formula: ##STR1## wherein P.sub.1 is a hydroxyl protecting group, R.sub.1 may be H or electron withdrawing group, R.sub.2 may be H or electron withdrawing group, R.sub.3 may be H or electron withdrawing group, R.sub.4 may be H or electron withdrawing group, R.sub.5 may be H or electron withdrawing group, R.sub.6 may be an alkyl group, an olefinic group, an aromatic group, Ph, PhCH.sub.2, an O-alkyl group, an O-olefinic group, an O-aromatic group, O--Ph, or O--CH.sub.2 Ph.

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: The present invention relates to dimethyl-substituted cyclohexanediene derivatives, to a process for their preparation, to their use as pharmaceuticals and to corresponding pharmaceuticals.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: A process for the preparation of a compound of general formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, any of which may optionally be substituted with one or more substituents selected from halogen and OH; or COOR.sup.4, COR.sup.6, CONR.sup.4 R.sup.5 or CONHSO.sub.2 R.sup.4 ;R.sup.4 and R.sup.5 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted with one or more halogen atoms;R.sup.6 is a halogen atom or a group R.sup.4 ;R.sup.2 is hydrogen or halo;R.sup.3 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl, any of which may optionally be substituted with one or more halogen atoms; or halo;the process comprising reacting a compound of general formula II: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.

Abstract: The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.

Abstract: This invention relates to componds of formula I ##STR1## which are useful as PDE IV inhibitors and for treating diseases related thereto.

Abstract: The invention provides compounds of formula (I) and (II) wherein X and Y are independently chlorine, bromine, iodine, a mesyl group CH.sub.3 SO.sub.3 or a tosyl group OSO.sub.2 phenyl (wherein phenyl is optionally substituted by 1, 2, 3, 4 or 5 substituents independently selected from C.sub.1-4 alkyl, halogen, cyano or nitro; R.sup.1 and R.sup.2 are independently 1 to 4 optional substituents; Z.sup.1 and Z.sup.2 are each independently --O-- or --NH--; R.sup.3 is hydrogen, t-butyl or allyl; Z.sup.3 is a hydrocarbyl group such as carboxyethyl, optionally containing heteroatoms, and physiologically acceptable derivatives thereof. The compounds can be converted in situ into nitrogen mustard agents by the actions of enzymes such as carboxypeptidase or nitroreductase and are useful for the treatment of cancer.

Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.

Abstract: A process for the nitration of an aromatic or heteroaromatic compound with a nitrating agent comprising nitric acid or a mixture of nitric and sulphuric acids, characterised in that nitration is performed in a solvent comprising at least 50% v/v of a C.sub.1 -C.sub.6 alkyl ester of a C.sub.1 -C.sub.4 carboxylic acid. The process is of particular use for the nitration of diphenyl ethers to give compounds which are useful as herbicides or as intermediates in the synthesis of herbicides.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: The present invention relates to a class of compounds represented by Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.

Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.

Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.