Abstract: Described herein is a method for preparing an amino salt compound, the method including: i) providing a carbonyl compound; ii) reacting the carbonyl compound provided according to (i) in the presence of a transaminase with ii-a) at least one primary amine; and ii-b) at least one carboxylic acid; thereby obtaining a mixture including an at least partially crystallized amino salt compound including a cation and a carboxylate anion based on the at least one carboxylic acid added according to (ii-b). Also described herein is an amino salt compound obtained or obtainable by the method and to the amino salt compound, and a composition including a) an amine of general formula (IIa); and b) at least one carboxylic acid of general formula (III).

Abstract: The present invention relates to novel soluble liquid (SL) formulations comprising A) quinclorac ammonium salts of formula I wherein R1, R2, R3 and R4 are independently hydrogen or optionally substituted alkyl, and B) a solvents of formula IIa wherein R5 is alkyl; A is alkylene or oxyalkylene; and m is 0, 1, 2 or 3; and/or a solvent of formula IIb HO—B—OH??(IIb) wherein B is a straight-chain or branched alkylene or alkyleneoxyalkylene or alkyleneoxyalkyleneoxyalkylene.

Abstract: The invention provides an oral pharmaceutical composition, optionally in dose unit form, comprising a lipophilic drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, wherein said drug substance contains a functional electrostatic group having a pKa value of from 2 to 10, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic.

Abstract: The present invention relates to an acrylate-based compound that includes an organic acid having two or more acrylate groups and one or more phenolic acid structures in one molecule, and a photosensitive composition including the same. It is possible to shorten a developing time in a photolithography process without damaging photosensitivity by using the photosensitive composition according to the present invention.

Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.

Abstract: The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: The present invention relates to compounds of formula (I) for stabilizing the tetrameric form of transthyretin, compounds for use in the treatment or prevention of amyloidosis, and agents and medicaments comprising such compounds. wherein X, Y, R1, R2, R3, R4, m, n, p, q, and the linker are as defined herein.

Abstract: A compound shown by the following formula (1) can be used as a material for a radiation-sensitive composition capable of forming a resist film which effectively responds to electron beams or the like, exhibits low roughness, and can form a high precision minute pattern in a stable manner.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy. Carboxylic acid-containing compounds having a terminal cyclic moiety, a carboxylic acid group, and a C3-12 hydrocarbon chain optionally containing at least one double bond, at least one triple bond, or at least one double bond and one triple bond linking the cyclic moiety and the carboxylic acid group are inhibitors of histone deacetylase.

Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Abstract: The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.

Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.

Abstract: The invention relates to pharmaceutical compositions of alkylammonium salts of 2-aryipropionic acids, including ketoprofen, ibuprofen, naproxen and tiaprofenic acid. The compositions are suitable for parenteral administration arid, due to buffering at pH 8 to 9, cause less pain upon injection than previously known composition.

Abstract: Compounds of formula (I): with a variety of therapeutic uses, more particularly novel prodrugs that are particularly useful for delivering a parent compound for selective estrogen receptor modulation.

Abstract: This invention relates to processes for preparing asymmetrical biphenyl tetracarboxylic acids and the corresponding asymmetrical dianhydrides, namely 2,3,3?,4?-biphenyl dianhydride (a-BPDA), 2,3,3?,4?-benzophenone dianhydride (a-BTDA) and 3,4?-methylenediphthalic anhydride (-MDPA). By cross-coupling reactions of reactive metal substituted o-xylenes or by cross-coupling o-xylene derivatives in the presence of catalysts, this invention specifically produces asymmetrical biphenyl intermediates that are subsequently oxidized or hydrolyzed and oxidized to provide asymmetric biphenyl tetracarboxylic acids in comparatively high yields. These asymmetrical biphenyl tetracarboxylic acids are subsequently converted to the corresponding asymmetrical dianhydrides without contamination by symmetrical biphenyl dianhydrides.

Abstract: Compounds of formula I wherein at least one R1 is H and the remainder are CH2CO2K; R2 is and L is H are described. The compounds are useful as pharmaceutical compositions in the treatment of AIDS.

Abstract: The instant invention is a route to stereospecific 3-substituted 5-membered ring isomers of Formula (A). The final products are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), inflammation especially arthritis, sleep disorders, premenstrual syndrome, and hot flashes. The invention provides novel routes to synthesize steroselectively analogs of gabapentin (Neurontin®) of Formulas (I), (II), (III) and (IV) wherein R is C1-C10 alkyl or C3-C10 cycloalkyl and pharmaceutically acceptable salts thereof.

Abstract: A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I): wherein R1 represents a dicarba-closo-dodecaboran-yl which may be substituted with a lower alkyl group, a lower alkenyl group, carboxyl group or the like; R2 represents carboxyl group, a lower alkoxycarbonyl group, or hydroxyl group; and X represents a single bond or a linking group such as —CO—Y1— wherein Y1 represents oxygen or —N(R3)— wherein R3 represents hydrogen or a lower alkyl.

Abstract: The present invention provides a process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1). The present invention more particularly relates to a process using cyclohexylphenyl ketone for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1).

Abstract: A method for treating symptoms, diseases and conditions in extra-reproductive tract tissues that are responsive to treatment with estrogen, using triarylethanes of formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; wherein R3 is an anionic substituent; m is an integer from 1 to 4; and n is an integer from 0 to 4; and wherein R2 is either H or —OH. Each of R1 and R2 can be either meta or para to its respective phenyl ethyl linkage. Compounds having the formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; R3 is an anionic substituent; m is 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; R2 is H or —OH; and wherein each of R1 and R2 is independently meta or para to its respective phenyl ethyl linkage are also provided, with the proviso that R2 is not para —OH when m is 1 and R3 is —COOH.

Abstract: This invention relates to compounds of the formula: wherein R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; or stereoisomers thereof.

Abstract: The present invention relates to the preparation of nitrobenzoic acids by oxidizing particular nitrotoluenes, nitrobenzyl alcohols, esters and/or ethers in the presence of nitric acid at elevated temperature and elevated pressure. It has been found that the particular nitrotoluenes, nitrobenzyl alcohols, esters and/or ethers may be oxidized particularly reliably and in high yields using nitric acid to the benzoic acid derivatives when they are metered into the nitric acid.

Abstract: Bis(Fluorophenyl)alkylamides have been chemically synthesized which possess beneficial pharmacological properties (e.g., anticonvulsant activity) useful for the treatment of neurological diseases or disorders, such as, for example, epilepsy, convulsions, and seizure disorders. The preferred compounds of the invention also cause little sedation and have high therapeutic and protective indices in animal models of epilepsy. These compounds further possess long pharmacologic half-lives, which, in practical clinical therapeutic application, should translate into once-a-day dosing, of great benefit to patients suffering from these diseases and/or disorders. These compounds may also be of further clinical utility in the treatment of other diseases and disorders of the central and peripheral nervous systems, or diseases or disorders affected by them, including, but not limited to, spasticity, skeletal muscle spasms and pain, restless leg syndrome, anxiety and stress, and bipolar disorder.

Abstract: The compounds of the invention are compounds represented by the following general formula (1): 1

Abstract: Novel molecular compounds containing carboxylic acid derivatives represented by general formula (I) or (II) as the constituent compound and exhibiting excellent performances in various technical fields including selective separation of useful substances, chemical stabilization, nonvolatilization, prolongation of release and powderization, wherein X is (CH2)n or p-phenylene; n is 0, 1, 2 or 3; R1 to R8 and R13 to R20 are each hydrogen, C1-C6 alkyl, C2-C4 alkenyl, phenyl optionally substituted with C1-C6 alkyl, halogeno or C1-C6 alkoxy; and R9 to R12 and R21 to R24 are each hydrogen, C1-C6 alkyl, C2-C4 alkenyl, C11-C12 aralkyl or an alkali metal.

Abstract: The present invention describes novel halogenated triphenylethylene derivatives, or pharmaceutically acceptable prodrug or salt forms thereof, as selective estrogen receptor modulators for the treatment of and/or prevention of breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as methods for making the compounds and pharmaceutical compositions of this invention.

Abstract: This invention pertains to novel salt forms of trophenylethylene compound, such as 3-[4(1,2-diphenyl-but-1-enyl)-phenyl]-acrylic acid, as selective estrogen receptor modulators. This invention also provides methods for the treatment and/or prevention of breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.

Abstract: A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.

Abstract: The present invention describes novel halogenated triphenylethylene derivatives, or pharmaceutically acceptable prodrug or salt forms thereof, as selective estrogen receptor modulators for the treatment of and/or prevention of breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as methods for making the compounds and pharmaceutical compositions of this invention.

Abstract: This invention pertains to novel salt forms of trophenylethylene compound, such as 3-[4(1,2-diphenyl-but-1-enyl)-phenyl]-acrylic acid, as selective estrogen receptor modulators. This invention also provides methods for the treatment and/or prevention of breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.

Abstract: A method for treating symptoms, diseases and conditions in extra-reproductive tract tissues that are responsive to treatment with estrogen, using triarylethanes of formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; wherein R3 is an anionic substituent; m is an integer from 1 to 4; and n is an integer from 0 to 4; and wherein R2 is either H or —OH. Each of R1 and R2 can be either meta or para to its respective phenyl ethyl linkage. Compounds having the formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; R3 is an anionic substituent; m is 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; R2 is H or —OH; and wherein each of R1 and R2 is independently meta or para to its respective phenyl ethyl linkage are also provided, with the proviso that R2 is not para —OH when m is 1 and R3 is —COOH.

Abstract: The present invention is a method of preparing a 3-aryl-1-indanamine represented by structural formula I: and physiologically acceptable salts thereof. In structure I, phenyl ring A can be unsubstituted or substituted with 1-4 substitutents. R1 is an aromatic group which can be substituted or unsubstituted. R2 and R3 are each, independently, hydrogen, an aliphantic group, a substituted aliphatic group, an aromatic group, a substituted aromatic group, an aralkyl group, or a substituted aralkyl group. Alternatively, R2 and R3, taken together with the nitrogen substitutent on the indan ring, form a non-aromatic ring system having 1-2 heteroatoms.

Abstract: The invention concerns aromatic tetralcyclic compounds of the retinoid type of general formula (I). The invention also concerns the method for preparing them and the pharmaceutical compositions containing at least one of said compounds.

Abstract: Compounds of the formula where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.

Abstract: Novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.

Abstract: A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.

Abstract: The present invention relates to a TEMPO-catalyzed oxidation of primary alcohols, RCH.sub.2 OH to corresponding carboxylic acids, RCOOH in the presence of catalytic in the presence of catalytic amount of NaClO and stoichiometric amount of NaClO.sub.2 as an oxidant.

Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

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 the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.

Abstract: Described herein are non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.

Abstract: Prescribed herein are novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.

Abstract: A process for the carbonylation of allylic alcohols such as nerolidol, farnesol, or their monocyclic analogues with carbon monoxide at a pressure of at least 30 bar in the presence of a polar solvent and a palladium halide catalyst, optionally an alkali metal halide salt, and optionally an alcoholic solvent. The carbonylated product may then be reduced to the corresponding alcohol, which is cyclized in the presence of Lewis or Bronsted acids to afford an ambergris fragrance compound.

Abstract: Novel benzoic acid derivatives have the formula: ##STR1## wherein --X-- represents C.sub.1 to C.sub.6 alkylene, C.sub.2 to C.sub.6 alkenylene or a divalent moiety having the structure --(CH.sub.2).sub.m --Z-- in which m is an integer from 0 to 3 and Z represents --O--, --S-- or --NH--;--Y-- represents a direct bond, C1 to C.sub.6 alkylene, C.sub.2 to C.sub.6 alkenylene or a divalent moiety having the structure --(CH.sub.2).sub.m --Z--(CH.sub.2).sub.n in which m and n are each, independently, an integer from 0 to 3 and --Z-- represents --O--, --S-- or --NH--;R represents a 5- or 6-membered carbocyclic or heterocyclic ring or a carbocyclic or heterocyclic fused ring system containing up to 10 members in the ring, which carbocyclic, heterocyclic or fused ring system may be saturated or unsaturated and may contain up to two substituents selected from lower alkyl, methoxy, halo and trifluoromethyl; andR.sup.1 and R.sup.

Abstract: Compounds of the formula ##STR1## in which X represents hydrogen, --NO.sub.2 or --NH.sub.2 and Y represents --CH.sub.3, --COOH, --CONH.sub.2, --NH.sub.2 or --N.dbd.N--Z, in which the group --Z is ##STR2## with the proviso that if Y represents the group --N.dbd.N--Z, X is only --NO.sub.2, and if Y represents the group --CH.sub.3, X is only hydrogen, are described. A compound of the formula ##STR3## the preparation of which in a multi-stage process, in which the compounds of the general formula (I) are also obtained, is described, is preferred.The resulting 3,4'-diamino compound is suitable for the preparation of polycondensates and shaped articles, films and fibers of high heat resistance.

Abstract: A diphenylmethane compound (III) can be produced in a good yield by allowing a phenol compound (I) to react with a stilbene compound (II) in the presence of methanesulfonic acid ##STR1##

Abstract: 2,2-Difluorocyclopropyl derivatives of the formula ##STR1## in which R represents alkyl, optionally substituted aryl or optionally substituted aralkyl andX represents hydroxymethyl, 2-hydroxyethyl, isocyanato, amino, amino hydrohalide or a radical of the formula --CO--R.sup.1, whereR.sup.1 represents hydrogen, hydroxyl, alkoxy, alkyl, halogen or amino,are intermediates for fungicides.

Abstract: Nonsteroidal estrogenic triarylethylene carboxylic acids of the formula ##STR1## wherein R is (CH.sub.2).sub.m O or (CH.sub.2).sub.n, where m is an integer from 1 to 4 and n is an integer from 0 to 4, X is hydrogen or hydroxyl, Y is methyl, ethyl, chlorine, or bromine, and wherein the RCOOH and X moieties are either meta or para to the phenyl ethylene linkage. Examples of active compounds include 4-hydroxytamoxifen acid, 3-hydroxytamoxifen acid, 4-[1-(p-hydroxyphenyl)-2-phenyl-1-butenyl]benzoic acid and 4-[1-(p-hydroxyphenyl)-2-phenyl-1-butenyl]phenylacetic acid. Compositions containing these triarylethylene carboxylic acids can be administered to patients to alleviate medical conditions associated with a deficiency of estrogen, including osteoporosis, premenstrual syndrome, vasomotor symptoms associated with menopause, atrophic vaginitis, Kraurosis vulvae, female hypogonadism, primary ovarian failure, excessive hair growth and prThe U.S.

Abstract: A process for the preparation of a polycyclic dye of the Formula (1): ##STR1## by reacting a substituted acetic acid of the Formula (2): ##STR2## with a compound of the Formula (3): ##STR3## and oxidation of the intermediate leuco compound to dehydrogenate the peripheral heterocyclic rings whereinY is an optionally substituted aromatic or heteroaromatic radical;Ring A is unsubstituted or is substituted by from one to five groups;Z is --NR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 are each independently H or are independently selected from optionally substituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl and heteroaryl; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring; orR.sup.1 and R.sup.2 each independently together with the nitrogen to which they are attached and the adjacent carbon atom of Ring B form a heterocyclic ring; andX.sup.1 and X.sup.

Abstract: The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.