Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.

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 having Formulas 5 and 6 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive compounds and intermediates.

Abstract: Compounds containing unsaturated aliphatic moieties which are linked to each other by a tertiary oxycarbonyl containing acyclic moiety are basis for compositions which are cured to polymer networks which are thermally decomposable to provide residue which can be dissolved to allow repair of inoperative assemblies by replacement of inoperative components or recovery or recycling of operative elements which are affixed in assemblies by the cured compositions.

Abstract: A process for hydrogenating benzenepolycarboxylic acids or a derivatives thereof by bringing one or more benzenepolycarboxylic acids or derivatives thereof into contact with a hydrogen-containing gas is carried out in the presence of a catalyst containing macropores. The catalyst contains, as an active metal, at least one metal of transition group VIII of the Periodic Table alone or together with at least one metal of transition group I or VII of the Periodic Table. Except that hydrogenation of dimethyl terephthalate using a catalyst containing ruthenium as active metal, either alone or together with at least one metal of transition group I, VII or VIII of the Periodic Table, applied to a support having a mean pore diameter of at least 50 nm and a BET surface are of at most 30 m2/g, where the active metal is present in an amount of from 0.01 to 30% by weight, based on the total weight of the catalyst, and the ratio of the surface areas of the active metal and the catalyst support is less than 0.

Abstract: Lipase-catalyzed transesterification reactions yield novel ferulyl-substituted or coumaryl-substituted acylglycerols with properties suitable for use as sunscreen agents having broad spectrum UV protection. These agents have the advantage of being synthesized from natural materials, while providing a value-added use for vegetable oils. They are readily incorporated into standard sunscreen formulations.

Abstract: Benzenoid HETE derivatives and methods of their use for treating dry eye are disclosed.

Abstract: The present invention relates to novel retinoid antagonists of the formula I wherein the dotted bond can be either hydrogenated or form a double bond; and, when the dotted bond forms a double bond, R1 is lower alkyl and R2 is hydrogen; and, when the dotted bond is hydrogenated, R1 and R2 taken together are methylene to form a cis-substituted cyclopropyl ring; R3 is hydroxy or lower alkoxy; R4 is alkyl or alkoxy; and R5 and R6 are, independently, a C4-12 alkyl or a 5-12 cycloalkyl substituent containing from 1-3 rings which are either unsubstituted or substituted with from 1-3 lower alkyl groups, with the carbon atom of R5 and R6 being linked to the remainder of the molecule to form a quaternary carbon atom pharmaceutically acceptable salts of carbocylic acids of the formula I; as well as method for the treatment of osteoporosis and preneoplastic and neoplastic diseases, and a method for reducing or abolishing adverse events in subjects receiving retinoid agonist treatment by administering a

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

Abstract: A novel carnosic acid derivative for promoting the synthesis of nerve growth factor (NGF), a composition comprising the carnosic acid derivative as an effective ingredient, as well as, a method of promoting the synthesis of NGF comprising administering an effective amount of the carnosic acid derivative as an effective ingredient to a subject requiring such promotion. The carnosic acid derivative, composition and method according to the present invention can safely and efficiently promote the production of NGF in the living body, without being accompanied by a side effect such as a loss of a quantitative balance of hormones in the living body.

Abstract: The invention relates to aryl vinyl ether compounds of formula (I): 1

Abstract: A process has been provided to produce semi synthetic statins, as for instance simvastatin with a high yield, for another statin, preferably a naturally occurring statin, as for instance lovastatin. Also a number of novel intermediate compounds, prepared during said process, has been provided.

Abstract: Dendrimers were directly and covalently attached to solid supports via siloxy bonds. After complexation with transition metals, the dendrimers were used as catalysts. The supported dendrimers were stable and easily separated from the reaction mixture.

Abstract: (4-oxy-3-(aryl)phenyl)pyridine compounds, in free or acid addition salt form, are useful as pharmaceuticals for treatment and prophylaxis of inflammation, particularly inflammatory or obstructive diseases of the airways, e.g. for asthma therapy. Preferred compounds are novel biphenyl pyridines, biphenyl benzamides and biphenyl phenylcarboxy compounds. The compounds are selective inhibitors of PDE 4 isoenzyme activity and also act to down regulate or inhibit TNF-&agr; release.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Novel pyrimidin-4-one derivatives of formula [1] are provided, which are useful as active ingredients of herbicides, wherein R1 is hydrogen or alkyl; R2 is alkyl optionally substituted with halogen; R3 is alkyl optionally substituted with halogen, alkenyl, or alkynyl; and Q is substituted phenyl. Also provided are intermediates for their production and processes for producing these intermediates.

Abstract: A process for producing a 2-aralkyl-3-hydroxypropionic acid (or its ester), comprising the steps of: reacting a 3-hydroxy-2-methylene-3-arylpropionic acid ester, easily obtained by the reaction of an arylaldehyde with an acrylic acid ester, with an acid anhydride to form a 2-aralkylidene-3-acyloxypropionic acid ester; subjecting the same to hydrolysis or alcoholysis; and reducing the resulting 2-aralkylidene-3-hydroxypropionic acid or its ester. The reduction step may be conducted in the presence of a base.

Abstract: The invention relates to an improved process for the preparation of a compound of formula I wherein R1 represents an optionally substituted aryl group, R2 represents an optionally substituted alkyl group, and R3 and R4 each individually represent an alkyl group; which comprises heating a mixture of a compound of formula II an alcohol, a tri-alkoxymethane, an acid and, optionally, an inert diluent.

Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Abstract: A guanidine derivative represented by formula (1), (2), (3) or its acid addition salt and a production process thereof wherein each of A and B is a C2-C8 alkylene, D is a single bond, —CO— or a C1-C6 alkylene, E is H, a lower alkyl or the like, m is 1 to 6, n is 0 to 6 and R1 is H, a lower alkyl or the like, 1 is 1 to 10 and G is H, —OH or the like and a skin cosmetic containing the same. It can exert excellent keratin layer softening effect continuously for a long period of time.

Abstract: The invention is directed to an improved process for the preparation of a compound of formula (I) wherein R is alkyl, n is 0 to 2, m is 1 to 4 and A is alkyl, interrupted or uninterrupted alkylene, alkanetriyl or pentaerythrityl, by transesterifying the corresponding lower alkyl with a higher alkanol of the formula A-(OH)m in the presence of a tin catalyst; wherein the improvement comprises reacting the tin catalyzed transesterification reaction mass with a carboxylic acid or hydrate thereof neat, in the absence of an aqueous medium, until the tin catalyst forms an insoluble derivative, and then separating the insoluble derivative from the reaction mass by filtration without the assistance of a filtration aid. The invention allows for a convenient method by which to remove the residual tin catalyst from the substituted hydroxyphenylcarboxylic acid ester compounds of formula (I).

Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.

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

Abstract: Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing ligands or receptors. Also disclosed are methods for preparing the compounds of the formula (I).

Abstract: An organic compound which is basic and soluble in an organic solvent, does not have a problem in preparation or handling and exhibits catalytic activity as a basic compound, i.e., a phosphine sulfide represented by formula (1), and a manufacturing process therefor, i.e., manufacturing a phosphine sulfide represented by formula (1), by reacting one molecule of thiophosphoryl chloride with three molecules of a phosphorane represented by formula (2). The phosphine sulfide can be used in a process for effectively manufacturing a poly(alkylene oxide) by polymerizing an alkylene oxide in the presence of the phosphine sulfide or of the phosphine sulfide and an active hydrogen compound selected from water and organic compounds having a partial structure of --OH or --NH--; and 2) a process for manufacturing a 1,2-dioxyethane derivative from an epoxy compound, i.

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

Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and particularly augmenting expression of a tumor suppressor gene and inducing tolerance to an antigen. The methods of the invention use unsaturated oxyalkylene esters.

Abstract: A 3-alkoxypropionic ester derivative, an olefin polymerization solid catalyst component using the same, an olefin polymerization catalyst using the same, and a process for the preparation of a polyolefin using the same. The 3-alkoxypropionic ester derivative is represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrocarbon group having from 1 to 10 carbon atoms; R.sup.2 represents a hydrocarbon group having from 1 to 20 carbon atoms; R.sup.3 represents a hydrocarbon group having from 1 to 20 carbon atoms; and R.sup.4 represents a branched hydrocarbon group having 3 or more carbon atoms.

Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.

Abstract: Palladium-catalyzed arylation of an olefin (e.g., ethylene) with an aromatic halide (e.g., 2-bromo-6-methoxynaphthalene, m-bromobenzophenone, or 4-isobutyl-1-bromobenzene) is conducted in specified media. After a special acid or base phase separation procedure, palladium-catalyzed carbonylation of the olefinically-substituted aromatic intermediate is conducted in specified media using CO and water or an alcohol to form arylalkylcarboxylic acid or ester or substituted arylalkylcarboxylic acid or ester (e.g., racemic 2-(6-methoxy-2-naphthyl)propionic acid, 2-(3-benzoylphenyl)propionic acid, or 2-(4-isobutylphenyl)propionic acid). Catalyst recovery procedures enabling recycle of catalyst residues and efficient recovery of amine hydrogen halide scavenger and solvent used in the arylation reaction are described, as well as novel, highly efficient methods of conducting the carbonylation reaction.

Abstract: The present application relates to a series of novel sulfonic acid metal cation salts of the formula ##STR1## which are useful intermediates to prepare antifolate 5-substituted pyrrolo[2,3-d]pyrimidines. The present invention also relates to a novel process for preparing the sulfonic acid metal cation salts and to a novel process for preparing aldehydes of the formula ##STR2## from the corresponding sulfonic acid metal cation salts.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: The invention relates to novel propynyl or dienyl biaromatic compounds which have the general formula (I) ##STR1## as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.

Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dedendent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, augmenting expression of tumor suppressor genes, inducing tolerance to antigens, or treating, preventing or ameliorating protozoan infection or inhibiting histone deacetylase in cells. The compositions of the invention are to and the methods of the invention use hydroxy and ether-containing oxyalkylene esters.

Abstract: The instant invention provides intermediates and processes for the preparation of compounds of formula IV ##STR1## wherein: n is 0, 1, or 2;R is hydrogen or C.sub.1 -C.sub.4 alkyl;X.sup.1 is hydrogen, cyano, 4-hydroxybenzoyl, 4-halobenzoyl, or 4-(C.sub.1 -C.sub.4 alkoxy)benzoyl;Y is NR.sup.4 R.sup.5, 4-hydroxyphenyl, or 4-(C.sub.1 -C.sub.4 alkoxy)phenyl;and R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.4 alkyl.

Abstract: The present invention relates to novel substituted acrylic acids, to methods for their preparation, compositions containing them, and their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention also relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings.

Abstract: Compounds of formula (I) wherein: R.sub.1 is --(CR.sub.4 R.sub.5).sub.n C(O)O(CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n C(O)NR.sub.4 (CR.sub.4 R.sub.5).sub.m R.sub.6, (CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6, or --(CR.sub.4 R.sub.5).sub.r R.sub.6 : W is alkynyl or 2 carbon atoms; R.sub.3 is H or R.sub.7 ; Z is C(O)R.sub.13, (CH.sub.2).sub.0-1 C(O)OR.sub.13, (CH.sub.2).sub.0-1 C(O)NR.sub.10 R.sub.13, (CH.sub.2).sub.0-1 C(R.sub.8 R.sub.8)OR.sub.8, --NHC(O)R.sub.7, (CH.sub.2).sub.0-1 NR.sub.10 R.sub.13, NH[C(O)C(O)OR.sub.8 ], CH.sub.2 NH[C(O)CNR.sub.10 R.sub.13 ], CH.sub.2 S(O).sub.q R.sub.7, CH[S(O).sub.q R.sub.7 ].sub.2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R.sub.7 is --(CR.sub.4 R.sub.5).sub.q R.sub.11 or C.sub.1-6 alkyl wherein the R.sub.11 or C.sub.

Abstract: The invention relates to new fluoromethoxyacrylic acid derivatives, a process for their preparation and their use as pesticides, as well as to new intermediates and a plurality of processes for their preparation.It has already been disclosed that certain fluoromethoxyacrylic acid derivatives which are similar in constitution to the compounds described below have fungicidal properties (compare, for example, WO 9517376). The fungicidal action of these compounds, however, is unsatisfactory in many cases.

Abstract: Water-borne polymeric vehicles are described where the polymeric vehicle includes the amine or ammonium salt of a phenolic ester alcohol.

Abstract: A surfactant, an emusifier for emulsion polymerization, a dispersant for suspension polymerization and a modifier for modification of resin properties are disclosed, each of these agents being comprised of a novel compound having a dibasic carboxyl group. The compound is represented by Formula (1)[X--O--(R.sup.1 O).sub.m --OC--R.sup.2 --COO].sub.y M (1)where M is a hydrogen atom, a metal atom or a quaternary nitrogen-containing group, y is equal to the valence of M, R.sup.1 is at least one hydrocarbon group, R.sup.2 is a moiety of a dibasic acid or a moiety of its anhydride, m is 0 or an integer of 1 to 1,000, and X is a hydrocarbon group having at least one polymerizable double bond of carbon--ncarbon which may contain an oxygen atom and a fluorine atom.

Abstract: The present invention provides a process for the preparation of pesticidal fluoroolefin compounds having the structural formula I ##STR1## The present invention also provides intermediate compounds which are utilized in the process of this invention.

Abstract: The invention is novel analogs of 9-cis-retinoic acid which are useful for the treatment and prevention of coronary artery disease and to protect against premature atherosclerosis by increasing HDL levels. The invention includes processes for preparing the novel 9-cis-retinoic acid analogs.

Abstract: Tricyclic compounds are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.

Abstract: Compounds with fungicidal and insecticidal properties having formula ##STR1## wherein A is N or CH; V is O or NH; m and n are the integers 0 and 1, provided that m+n is 0 or 1;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, and (C.sub.1 -C.sub.4)alkoxy;R is independently selected from hydrogen, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.12)alkenyl, (C.sub.2 -C.sub.12)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, halo(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.12)alkenyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.12)alkynyl, (C.sub.1 -C.sub.12)alkyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.12)alkenyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.12)alkynyl(C.sub.3 -C.

Abstract: The present application describes m-amidino phenyl analogs of formula I: ##STR1## wherein D can be amidino and E can be phenyl, which are useful as inhibitors of factor Xa.

Abstract: We proposed a novel compound having an activity of PGI.sub.2 receptor agonist.A phenoxyacetic acid derivative of the formula ##STR1## A is --C(R.sup.1).dbd.N.about.OR.sup.2, --CH(R)NH--OR.sup.2, --COE, --SO.sub.2 E, --CH.sub.2 --NR.sup.3 --Y, --Z--NR.sup.3 --CONR.sup.4 R.sup.5, --CH.sub.2 --OR.sup.6, --CO.sub.2 R.sup.6, --CH.sub.2 --O.about.N.dbd.CR.sup.7 R.sup.8, --CH.sub.2 --O--NHCHR.sup.7 R.sup.8, substituted by imidazolyl(methyl), pyrazolylmethyl, oxazolyl(methyl), thioxazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolylmethyl;T is alkylene, alkenylene, etc.;D is --CO.sub.2 R.sup.10, --CONR.sup.11 R.sup.12 ;E is (substitution) amino, hydradino;Y is substituted (thio) carbonyl, substituted sulfonyl;Z is --CH.dbd.N--, --CH.sub.2 NR.sup.3 --;R.sup.1, R.sup.3, R.sup.10 --R.sup.13 is each H or alkyl, etc.;R.sup.2, R.sup.4 --R.sup.9 is each H, alkyl or alkyl substituted by phenyl or hetero ring ,etc. and non-toxic salts thereof, non-toxic acid addition salts thereof, possess an agonistic on PGI.sub.

Abstract: An ester compound represented by the formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represent a C.sub.1 -C.sub.6 alkyl group, or other specified groups, which may be optionally substituted with one or more halogen atoms; and R.sub.3 represents a pyrethroid acid residue (a group resulting from elimination of the carboxyl group from pyrethroid acid), and a pesticidal composition containing the ester compound as an active ingredient.

Abstract: The present invention relates to a process for the preparation of compounds of the formula (1)R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 ArCOOR (1)in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, a halogen, an alkyl or alkoxy group having 1 to 6 carbon atoms or OR, NHR, NR.sub.2, SR or COOR, in which R is an alkyl radical having 1 to 4 carbon atoms, Ar is an aryl radical having 6 to 12 carbon atoms and the radical R shown in formula (1) has the above meaning, by reacting a compound of the formula (2)R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 ArCOOH (2)in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, a halogen, an alkyl or alkoxy group having 1 to 6 carbon atoms, OH, NH.sub.2, NHR, SH or COOH and Ar has the same meaning as in formula (1), with a sulfate of the formula (RO).sub.2 SO.sub.2, in which R has the above meaning, in the presence of a water-insoluble tertiary amine and water at a temperature of 10.degree.