Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

Abstract: A production method of an optically active ?-amino acid represented by the formula (I) wherein each symbol is as defined in the specification, which includes reacting a compound represented by the formula (II) with a lithium amide represented by the formula (III) in the presence of a compound represented by the formula (IV).

Abstract: The present invention includes benzophenone compounds (I) which are useful in the treatment of HIV infections.

Abstract: The present invention provides the S enantiomer of a compound of formula (I); wherein R1 represents 2,4-difluorophenyl or cyclohexyl as well as pharmaceutically acceptable salts, solvates, crystalline forms and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Abstract: In one aspect, the invention provides a process for the preparation of a compound of Formula I wherein G is alkyl or aryl, by employing a novel halo-substituted active methylene compound of Formula III wherein X is halogen, and process of preparation thereof.

Abstract: The present invention relates to a novel retinoid derivative compound represented by the formula I: wherein X, R1, R2 and R3 are as defined herein or pharmaceutically acceptalbe salts thereof. Also, the present invention relates to processes for producing the compound of the formula I and to an anti-cancer composition comprising the compound of the formula I. The compound of the formula I according to the present invention exerts high anti-cancer effects while not causing undesirable side effects.

Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5?, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.

Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and cancer.

Abstract: The invention relates to anthranilic acid amide derivatives of formula (I), wherein Ar is represented by the subformula (Ia), wherein Ra represents H or lower alkyl, and R1 represents H or perfluoro lower alkyl, R2 represents H, halogen, C2–C7alkyl, C2–C7alkenyl or lower aklynyl; or Ar is represented by the subformula (Ib) and R1 represents perfluoro lower alkyl, and R2 represents bromo, iodo, C2–C7alkyl, C2–C7alkenyl or lower alkynyl, or R1 represents H, and R2 represents fluoro, bromo, iodo, ethyl, C5–C7alkyl, C2–C7alkenyl or lower alkynyl; to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age-related macular degeneration; to a method for the treatment of

Abstract: The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): in which Ar, X, Z, Y and K are each as defined in the description, to a plurality of processes for their preparation and to their use as herbicides and pesticides.

Abstract: An efficient, simple, high yielding, eco-friendly process for the manufacture of tosylates quaternary ammonium salts of cinnamidoalkylamines and/or benzamidoalkylamines (Formula I) has been described. These compounds are substantive UV-absorbers. They are useful in making fabric care products and personal care products. The scope of this methodology has been demonstrated by converting water soluble organic sunscreen quaternary halides to their corresponding tosylates of Formula VI.

Abstract: A process for preparing a compound of formula (II) wherein R1 denotes bromine, wherein, a compound of formula (IV) is reacted with elemental bromine in a diluent.

Abstract: Compounds of Formula I: wherein R, R1 and R2 are each independently hydrogen or linear or branched C1 to C10 alkyl, or linear or branched C1 to C10 alkoxy; R3 is selected from the group consisting of COCH3, CO2R7, CONH2, CON(R8)2, CN, COX(CH2)n-N—(R4)(R5)(R6), and the quaternized salt form of the formula COX(CH2)n-N—(R4)(R5)(R6)+Y?; X is O or NH; n is an integer of 1 to 5; Y is an anion; R4, R5 and R6 are independently linear or branched C1 to C30 alkyl; and R7 and R8 are independently hydrogen or linear or branched C1-C30 alkyl. Sunscreen formulations containing compounds of Formula I, and methods for protecting hair, skin and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.

Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.

Abstract: Described are compounds of Formula I and Formula II and their pharmaceutically acceptable salts. The compounds of Formulas I and II are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.

Abstract: The present invention provides transition-metal-catalyst-based methods for the arylation and vinylation of activated methyl, methylene, and methine carbons with aryl halides, vinyl halides, and the like. The methods of the invention provide several improvements over existing methods, including the ability to synthesize efficiently and under mild conditions ?-aryl and ?-vinyl products from a wide range of starting materials, including ketones, esters, hydrazones, and imines. Furthermore, the methods of the invention may be used in an asymmetric sense, i.e. to produce enantiomerically-enriched chiral ?-aryl and ?-vinyl products.

Abstract: Compounds having Formula I or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting angiogenesis in a mammal.

Abstract: The present application relates to a plurality of novel processes for preparing 2-(2-hydroxyphenyl)-2-(alkoxyimino)-N-methylacetamide derivatives, to novel intermediates for their preparation, and to processes for preparing these intermediates.

Abstract: Colchicine derivatives represented by the formula (I) 1

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: The present invention relates to fluorinated benzaldehydes, to a process for preparing them and also to the use of the fluorinated benzaldehydes for preparing active ingredients, especially in medicaments and agrochemicals.

Abstract: This invention relates to novel compounds of the following formula and a process for the preparation thereof. wherein X is Cl, Br or I.

Abstract: Carboxylic acid amides of general formula 1

Abstract: An anilide is reacted with an acylating agent by using as a catalyst a tri (perfluoroalkane sulfonate) compound of any of the elements belonging to groups 3 to 5 and groups 13 to 15 in periods 4 to 6 of the periodic table, thereby bonding an acyl group to the benzene ring. Thus, ketoaniline derivatives, which are useful as physiologically active compounds or intermediates in synthesizing the same, are synthesized in high reaction yield by catalytic acylation.

Abstract: An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.

Abstract: A method for prevention or treating myocarditis, dilated cardiomyopathy and heart failure comprising administering to a patient in need of such treatment a NF-&kgr;B inhibitor in a therapeutically effective amount, wherein said NF-&kgr;B inhibitor is a benzoquinone derivative represented by the following formula (I): wherein R1, R2 and R3 are each independently a hydrogen atom, an alkyl group having 1 to 5 carbons or an alkoxy group having 1 to 5 carbons; R4 is a hydrogen atom, a hydroxymethyl group, an alkyl group, or a carboxyl group which is optionally esterified or amidated; Z is and n is an integer from 0 to 6, or its hydroquinone form, or a pharmaceutically acceptable salt thereof, is provided.

Abstract: The present invention provides processes for preparing 2-(2-hydroxyphenyl)-2-(alkoxyimino)-N-methylacetamides, to intermediates for this preparation, and to processes for preparing those intermediates.

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 present invention relates to a process for preparing a &agr;-hydroxyamide or &agr;-ketoamide, said process comprising the steps of: a) reacting a resin which comprises a polymer-supported isocyanide with an aldehyde in the presence of a catalyst, to form a resin-bound &agr;-hydroxyamide; b) optionally reacting said resin-bound &agr;-hydroxyamide with a reagent which is capable of oxidizing said resin-bound &agr;-hydroxyamide to a resin-bound &agr;-ketoamide; and c) reacting said resin-bound &agr;-hydroxyamide or resin-bound &agr;-ketoamide with a reagent which cleaves the nitrogen-resin bond to form a &agr;-hydroxyamide &agr;-ketoamide.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio 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, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Abstract: The invention relates to methods of synthesizing libraries of diverse and complex highly substituted 2,4-dioxopiperidine compounds of the general formula: wherein R1, R2 and R3 are as herein described, novel intermediates useful for synthesizing such 2,4-dioxopiperidine compounds and methods for identifying and isolating the compounds.

Abstract: The invention relates to a process for preparing a compound of formula (I) wherein a compound of formula (II), wherein R1 denotes chlorine, bromine, iodine, —O—COCH3, tosylate or mesylate, is reacted with a compound of formula (III),  optionally in a suitable diluent and/or in the presence of a suitable added reagent or catalyst, the reaction being carried out in a temperature range from 20 to 80° C.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

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. A substrate of solid phase synthesis of the formula III is also disclosed.

Abstract: The invention relates to a process for preparing a compound of formula (I) 1

Abstract: The present invention discloses the identification of the inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

Abstract: Substantive UV absorbing organic-soluble quaternary salts of cinnamidoalkylamine are described. Hair, skin and fabric care compositions containing the compounds of formula I. wherein R1 is a substituent, selected from H, halo, —OH, —NH2, —NO2, —OCH3, —N(CH3)2, alkyl groups containing from 1 to 6 carbon atoms, alkoxy groups containing from 1 to 6 carbon atoms, alkylamino or N,N-dialkylamino groups containing from 1 to 6 carbon atoms; R2 is selected from hydrogen, alkyl group containing from 1 to 12 carbon atoms; R3 and R4 are independently selected from benzyl, alkyl group containing from 1 to 12 carbon atoms; n is an integer from 1 to 6; R5 is selected from an alkyl group containing from 8 to 22 carbon atoms; alkenyl groups containing from 8 to 22 carbon atoms; R7 is selected from bromo, chloro, nitro, methyl and ethyl groups.

Abstract: This invention relates to molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors of the release of tumor necrosis factor. The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases.

Abstract: Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-&kgr;B with little side effects.

Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: 1

Abstract: Method for the prevention or treatment of pruritus with anti-pruritic compounds is provided. The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure: wherein R1, R2, R3, R4; and X, X4, X5, X7, X9; Y, Z and n are as described in the specification.

Abstract: The invention concerns anti-tumor agents of formula (I), wherein each of R1, R2 and R3 has the meanings defined in the specification including hydrogen, (1-4C)alkyl, (3-4C)alkynyl and (1-4C)alkoxyl; each of R4 and R5 is (1-4C) alkyl; each of R6 and R7 is hydrogen or (1-4C)alkyl; X is N-(1-4C)alkylimino, N-(3-4C)alkenylimino, or (3-4C)alkynylimino; m is 1 or 2 and each R8 is as defined in the specification; each Y′ and Y2 is halogen, (1-4C)alkanesulphonyloxy, benzensulphonyloxy or phenyl-(1-4C)alkanesulfonyloxy; or a pharmaceutical acceptable salt thereof; provided that at least one of R1, R2 and R3 is other than hydrogen; a process for their preparation, pharmaceutical composition containing them and their use for producing an anti-proliferative effect in a warm-blooded animal.

Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.

Abstract: The present invention relates to the field of organic synthesis and more specifically to a process for the preparation of Michael-adducts, as defined below, by reacting a &bgr;,&bgr;- or a &agr;,&bgr;-disubstituted, or a &agr;,&bgr;,&bgr;-trisubstituted, &agr;,&bgr;-unsaturated ketone (I) with a &bgr;-ketoester or a &bgr;-diketone (II) in presence of a suitable catalyst of formula M(X)n, according to scheme 1: 1

Abstract: A process for the preparation of primary aromatic carboxamides by the carbonylation of an aromatic compound, which contains at least one leaving group, with carbon monoxide, in the presence of a homogeneous or heterogeneous Pd catalyst and at least stoichiometric amounts of an amidation agent at elevated temperatures, which is characterized in that a primary carboxamide or a primary urethane is used as the amidation agent, and the reaction is carried out in the presence of an acylation catalyst.

Abstract: The present invention discloses novel naphthylsalicylanilides of the general formula wherein W is a substituted or unsubstituted naphthyl ring. The substitution on W includes replacing one or more —H with —OH, alkyl, O-alkyl, branched alkyl, or cycloalkyl, containing 1-6 carbon atoms or combinations thereof. Y is a substituted or unsubstituted phenyl ring or substituted or unsubstituted naphthyl ring. The substitution for Y includes replacement of one or more —H atoms with CN, CF3, NO2, methoxy, benzoyl, phenoxy, phenoxymethyl or combinations thereof. These compounds are useful as antibacterial against gram negative and gram positive bacteria and as antiinflammatory agents.

Abstract: The present invention discloses novel naphthylsalicylanilides of the general formula 1

Abstract: The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3—N—R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells.