Abstract: Novel compounds of the general formula (I), wherein Ar, R1, R2, X1, X2, Y1, Y, and Z are as defined in the specification, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.

Abstract: The invention relates to compounds of formula (I) as well as the salts and stereoisomers thereof wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, pharmaceutical compositions containing them, and methods for using them for treatment of cardiovascular disorders are also disclosed and claimed.

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention may include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention may include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.

Abstract: The present invention relates to the compounds of the general formula (I) and their salts and stereoisomers for the production of medicaments for the treatment of cardiovascular disorders.

Abstract: This invention relates to compounds of formula: wherein A is an unsaturated alkylene moiety; B the residue of a polyol wherein one hydroxyl moiety is esterified with one carboxyl moiety of the phthalic acid moiety; D is the residue of a polyol wherein one hydroxyl moiety is esterified with another carboxyl moiety of the phthalic acid moiety, and another hydroxyl moiety is esterified with one carboxyl moiety of the unsaturated alkylene moiety; E is the residue of polyol wherein one hydroxyl moiety is esterified with another carboxyl moiety of the unsaturated alkylene moiety; and M is a cation. The compounds can be used alone, or polymerized, or polymerized and combined with other polymers, to form effective stain and soil repellent compositions.

Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.

Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.

Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.

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: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention may include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.

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: A compound comprised of a hydrophilic polymer covalently yet reversibly linked to a amine-containing ligand through a dithiobenzyl linkage is described.

Abstract: A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d=0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; Z or Y is —SR3 and the other Z or Y is halogen or —R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R4 and R5, which may be the same or different, are: A—X, wherein A=—CH═CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(═O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; or a 5- or 6-membered het

Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

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: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, X1, R1, R2, Ra and Rb are as defined in the specification.

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: A process for producing optically active cysteine derivatives with high optical purity and good quality which is economically advantageous and is high in productivity even on a commercial scale is provided.

Abstract: The invention provides N-phenyltetrahydrophthalamic acid derivatives represented by the general formula [I], methods of producing the same, herbicides containing the same as the effective components, imidoylchloride derivatives as the intermediate products and methods of producing the same, wherein X and Y each individually represent hydrogen atoms or halogen atoms, R1 represents a lower alkoxycarbonylalkylthio group, R2 represents a lower alkyl group, a halogenated lower alkyl group or a substituted or unsubstituted phenyl group, and R3 represents a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, or a lower alkoxyalkoxy group. The herbicides of the present invention, which are very useful, can be widely applied to upland, paddy field, orchard, turf, forest, non-crop land, etc., and are not harmful to crops.

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: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.

Abstract: Pharmaceutical composition containing aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (1) and the salts thereof as active ingredient (wherein R1 is H, alkyl; R2 is COOR7, CONHOR8; E is —CONR9—, —NR9CO—, —OCO—,—COO—, —CH2—O—, —(CH2)2—, vinylene, ethynylene; J is bond, alkylene; A is H, alkyl, Ar, alkyl-OH ; R3, R4 is H, alkyl, COOR19, hydroxy, —NR20R21, Ar1 etc.); R5, R6 is H, methyl) and the novel aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (I).

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 has its objects to provide a method for reducing &agr;-aminoketone derivatives under mild conditions with high stereoselectivity.

Abstract: The present invention provides a method for preparing S-aryl cysteine. Specifically, the present invention provides enantioselective method for preparing S-aryl cysteine starting from cystine, cysteine or serine amino acid. The methods of the present invention provides S-aryl cysteine in enantiomeric excess of greater than about 96%.

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: A process for preparing a 2R-hydroxy-3-[(2-amino-phenylthio)]-3-[(p-alkoxyaryl)] propanoic acid alkyl ester of formula (V) wherein R is an alkyl, or benzoyl residue, R1 is hydrogen, an alkyl, alkoxy, aryloxy, phenyl, naphthyl, or hydroxy residue, and R2 and R3 are independently of each other hydrogen, and alkyl, alkoxy, alkylamino, alkylthio, aryl, or halogen residue, which comprises refluxing 2-aminothiophenol, or 2-aminothionaphthol with a compound of Formula (IV) that is 5S-(p-alkoxyphenyl)-4R-carboalkoxy-1,3,2-dioxathiolane-2-oxide when X is S, or the corresponding cyclic carbonate, in the presence of an organic solvent and an inert atmosphere, and recovering the resultant compound of Formula (V).

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract: A process for producing an aryl carbamate of a high purity at a high yield by reacting a diaryl carbonate with an amine compound having one or more hydrogen atoms bonded to the N position in the presence of carboxylic acid(s) of the following general formulae (I): R.sup.1 --COOH and/or (II): R.sup.2 --COOH (wherein R.sup.1 represents an alkyl or cycloalkyl group having an .alpha.-positioned carbon atom bonded to only one hydrogen atom, an alkyl group having an .alpha.-positioned carbon atom bonded to no hydrogen atom, or an aryl or heterocyclic group, and R.sup.2 represents an alkyl group having an .alpha.-positioned carbon atom bonded to two or more hydrogen atoms).

Abstract: The present invention relates to a new method for making compounds of formula ##STR1## and intermediates for making compounds of formual II. The compounds of this invention are useful intermediates for the manufacture of pharmacologically active compounds suitable for the treatment of viral infections, particularly, those caused by HIV and other retroviruses.

Abstract: A process which allows the re-use of compounds of formula ##STR1## in diltiazem synthesis through a process of conversion to a mixture of enantiomers III-(2R,3R) and III-(2S,3S) is described.

Abstract: A method for the inhibition of the binding of .alpha..sub.4 .beta..sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which .alpha..sub.4 .beta..sub.1 is involved.

Abstract: A method for producing an amide derivative of the formula [XV] ##STR1## wherein each symbol is as defined in the specification, and an enantiomer thereof, a novel intermediate useful for producing said compound and a production method thereof.The production method of the present invention is extremely easy and simple as compared to the conventional methods, and enables effective production of compound [XV] at high yields, which includes compound [XVI] having an HIV protease inhibitory action. In addition, the novel intermediates of the present invention are extremely useful as intermediates for producing not only the aforementioned compound [XVI] but also compounds useful as X-ray contrast media.

Abstract: Substituted cinnamic oxime derivatives I and cinnamic hydroxamide derivatives II ##STR1## (R.sup.1= halogen, NO.sub.2, CN, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3= H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, hydroxy-C.sub.1 -C.sub.6 -alkyl;R.sup.4= H, halogen, CN, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl orR.sup.3 +R.sup.4 =chemical bond;Y=--O--, --S--, --O--CO--, --O--SO.sub.2 -- or chemical bond;Y'=--O-- or --S--;R.sup.5= unsubst. or subst. C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl; C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, unsubst. or subst. phenyl or phenyl-C.sub.1 -C.sub.6 -alkyl, or, if Y is --O--, --S-- or a chemical bond, is (C.sub.1 -C.sub.6 -alkyl)carbonyl or (C.sub.1 -C.sub.6 -alkoxy)carbonyl; or, if Y is a chemical bond, is hydrogen or halogen;R.sup.5 '=R.sup.5, H or (C.sub.1 -C.sub.6 -haloalkyl)carbonyl;R.sup.6= H, C.sub.1 -C.

Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.

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: Process for the synthesis of .alpha.-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II).

Abstract: Naphthalene derivatives represented by formula ?I!: ##STR1## (wherein A is a hydrogen atom, a hydroxy group, a C.sub.7 -C.sub.11 aralkyloxy group, or an alkoxy group composed of an oxy group and a C.sub.1 -C.sub.12 aliphatic or alicyclic, saturated or unsaturated hydrocarbon group where the allyl may be substituted with a C.sub.6 -C.sub.10 allyloxy group; Q represents O, S, CH.sub.2, O--CH.sub.2, S--CH.sub.2, CO, or CHOR.sup.1 ; L represents CO, CR.sup.2 R.sup.3 CO, CH.sub.2 CH.sub.2 CO, or CH.dbd.CHCO; D represents a hydrogen atom, NO.sub.2, NH.sub.2, CO.sub.2 R.sup.4, or a group having the following formula ?II!: ##STR2## (wherein G represents. a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.6, CN, or a tetrazol-5-yl group); E represents a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.5, CN, or a tetrazol-5-yl group; M represents a hydrogen atom, a C.sub.1 -C.sub.4 lower alkyl group, a nitro group, or a halogen atom; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.

Abstract: The present invention provides a process to prepare a pyridine-2,3-dicarboxylate derivative via the reaction of a dailkyl alkoxy(or alkylthio)oxalacetate with an appropriately substituted acrolein compound in the presence of an ammonia source and a solvent.The present invention also provides useful intermediate compounds of formula IV.

Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.

Abstract: The present invention provides:a process for producing an alkali metal salt of an arylmercaptan compound, represented by general formula (3): ##STR1## which process comprises reacting a disulfide compound represented by general formula: ##STR2## with a hydroxide of an alkali metal M.sup.1 in the presence of a sulfur compound represented by general formula (2):H.sub.(2-i) S(M.sup.1).sub.i (2)a process for producing an alkoxycarbonylalkylthioaryl compound represented by general formula (5): ##STR3## which process comprises reacting the above-mentioned alkalimetal salt of an arylmercaptan compound with a halogenofattyacid ester compound represented by general formula (4):X.sup.1 R.sup.2 COOR.sup.3 (4)at pH 7-10; and a process for producing the above-mentioned alkoxycarbonylalkylthioaryl compound, which process comprises reacting the above-mentioned disulfide compound with the above-mentioned hydroxide of an alkali metal M.sup.

Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.

Abstract: Inhibitors for matrix metalloproteases, pharmaueutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each Tis a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 reresents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.

Abstract: The invention encompasses novel compounds of Formula Iuseful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceuticalcompositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I.

Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.

Abstract: The invention provides N-phenyltetrahydrophthalamic acid derivatives represented by the general formula ?I!, methods of producing the same, herbicides containing the same as the effective components, imidoylchloride derivatives as the intermediate products and methods of producing the same, ##STR1## wherein X and Y each individually represent hydrogen atoms or halogen atoms, R.sup.1 represents a lower alkoxycarbonylalkylthio group, R.sup.2 represents a lower alkyl group, a halogenated lower alkyl group or a substituted or unsubstituted phenyl group, and R.sup.3 represents a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, or a lower alkoxyalkoxy group. The herbicides of the present invention, which are very useful, can be widely applied to upland, paddy field, orchard, turf, forest, non-crop land, etc., and are not harmful to crops.

Abstract: A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented radially to the axis of the nucleus. Each of these ligands includes a two complexing atoms each complexed to one of the metal atoms. At least one of the bridging ligands includes a chiral center which is bonded to one of the complexing atoms. Preferably, all four of the bridging ligands include a chiral center bonded to one of the complexing atoms. The catalyst of the invention has been found to be useful in catalyzing carbenoid transformation reactions such as cyclopropanation.