Abstract: The present invention pertains to compounds of the formula (1) which are, inter alia, antiproliferative agents, anticancer agents, antimycobacterial agents, antituberculosis agents, and/or thioredoxin/thioredoxin reductase inhibitor: wherein: Q is ?O or ?N—S(?O)2—RQ;RQ is —II or optionally substituted C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; Ar is optionally substituted C5-20aryl; RO is an oxy substituent; the bond marked ? is a single bond or a double bond; the bond marked ? is a single bond or a double bond; R3 and R5 are each independently ring substituents; R2 and R6 are each independently ring substituents; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for example, in the treatment of proliferative conditions, (e.g., cancer), mycobacterial infections (e.g.

Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1, R2, R3, R4, R5, and R6 are as defined in the specification, or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof.

Abstract: A novel process for producing an optically active (E)-7-[2-cyclopropyl-4-(4-fluorophenyl quinolin-3-yl]-5-hydroxy-3-oxohept-6-enoic acid ester of formula (III) which is important as an intermediate for synthesizing medicines, comprises reacting 1,3-bis(trimethylsilyloxy)-1-alkoxybuta-1,3-diene of formula (I) with (E)-3-[2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl]-prop-2-en-1-al of formula (II) in the presence of an optically active binaphthol-titanium complex obtained from 1,1?-bi-2-naphthol with titanium tetraisopropoxide, a metal salt and an amine, and then subjecting the reaction product to desilylation

Abstract: This invention comprises the novel compounds of formula (I) wherein r, s, t, Y1—Y2, R1, R2, R3, R4, R5 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.

Abstract: Cyclohexenonequinolinoyl derivatives of the formula I where: R1 is hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxyiminomethyl, alkoxy, haloalkoxy, alkylthio, C1–C6-haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, unsubstituted or substituted amino sulfonyl, unsubstituted or substituted sulfonyl amino, unsubstituted or substituted phenoxy, unsubstituted or substituted heterocyclyloxy, unsubstituted or substituted phenylthio or unsubstituted or substituted heterocyclylthio; R2, R3 are hydrogen, alkyl, haloalkyl or halogen; R4 is substituted (3-oxo-1-cyclohexen-2-yl)carbonyl or substituted (1,3-dioxo-2-cyclohexyl)methylidene; and their agriculturally useful salts; processes for preparing the cyclohexenonequinolinoyl derivatives; compositions comprising them, and the use of these derivatives or compositions comprising them for controlling undesirable plants are described.

Abstract: A process for the production of compounds Ar—R1 by means of a cross-coupling reaction of an organometallic reagent R1-M with an aromatic or heteroaromatic substrate Ar—X catalyzed by one or several iron salts or iron complexes as catalysts or pre-catalysts, present homogeneously or heterogeneously in the reaction mixture. This new invention exhibits substantial advantages over established cross coupling methodology using palladium- or nickel complexes as the catalysts. Most notable aspects are the fact that (i) expensive and/or toxic nobel metal catalysts are replaced by cheap, stable, commercially available and toxicologically benign iron salts or iron complexes as the catalysts or pre-catalysts, (ii) commercially attractive aryl chlorides as well as various aryl sulfonates can be used as starting materials, (iii) the reaction can be performed under “ligand-free” conditons, and (iv) the reaction times are usually very short.

Abstract: Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an ethylenic or acetylenic unit to an azabicyclic moiety.

Abstract: A process for preparing substituted cyclopentadiene compounds and cyclopentadiene compounds which can be prepared thereby are described.

Abstract: There are provided novel compounds which have both antibacterial and antiparasitic properties, thereby reducing the need for using several compounds in combined antibacterial and antiparasitic treatment of livestock. The present novel compounds are especially well suited for treatment of coccidiosis, and they are represented by general formula (I) wherein R1-R6, X and A are as defined in the specification.

Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.

Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.

Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.

Abstract: Urea-containing, substituted 4-phenyl-[1,3]-dioxanes, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, obesity or a sleep/wake disorder mediated by orexin-2 are described.

Abstract: The objective of this invention is to provide a process for producing an optically active isomer of ethyl 7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxy-6-heptenoate by optically resolving an optical isomer mixture of the compound at a high productivity. The process is characterized by employing a filler comprising a carrier and a specific amount of cellulose tris (4-chlorophenyl carbamate) supported the carrier and carrying out chromatographic separation under the condition that the capacity factors have specific values.

Abstract: 8-arylquinolines of formula (I) wherein the aryl group at the 8-position contains a meta two atom bridge to an optionally substituted phenyl or pyridyl group, are PDE4 inhibitors useful to treat asthma, chronic bronchitis, chronic obstructive pulmonary disease, arthritis, respiratory distress syndrome, allergic rhinitis, neurogenic inflammation, pain, rheumatoid arthritis, and other diseases. R1-R7 and Ar are as in claim 1.

Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6?CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.

Abstract: This invention relates to compounds of the formula wherein A, B, D, E, K, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.

Abstract: A process is provided for preparing chiral diol sulfones of the structure where R3 is preferably where R4a is preferably aryl such as phenyl, and R1a is preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors.

Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, Y, and n are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Abstract: The present invention provides a production method of quinoline derivative (V) wherein each symbol is as defined in the Specification, which includes reacting quinolinecarbaldehyde (I) with any of the compounds (II) to (IV) in the presence of a base, followed by hydrolysis.

Abstract: Quinophthalone derivatives have the general formula I where R1, R2, R3 and R5 are independently hydrogen, halogen or C1-C4-alkyl; R4 is —SO3H, —SO3+N+R6R7R8R9, —SO2NR6R7, —CH2NR6R7, —CH2R10, —COOH, —COO?N+R6R7R8R9, —COOR11, —COR11, —NO2 or C1-C4-alkyl; R6, R7, R8 and R9 are independently hydrogen; C1-C22-alkyl or C2-C22-alkenyl whose carbon chains may be interrupted by one or more moieties selected from the group consisting of —O—, —S—, —NR12—, —CO— and —SO2— and/or which may each be mono- or polysubstituted by hydroxyl, halogen, aryl, C1-C4-alkoxy and/or acetyl; C3-C8-cycloalkyl whose carbon skeleton may be interrupted by one or more moieties selected from the group consisting of —O—, —S—, —NR12— and —CO— and/or which may be mono- or polysubstituted by hydroxyl, halogen, aryl, C1-C4-alkoxy and/or acetyl; dehydroabietyl or aryl; R6 and R7 or R6, R7 and R8 are together a 5- to 7-membered cyclic radical which includes the nitrogen atom and may include further heteroatoms; R10 is R11 is alkyl R6; R12 is

Abstract: The present invention relates to compounds of formulas 1 and 2 wherein R1, R2, R4, R5, R6, R7, R8, R10 and Z are as defined herein. The present invention also relates to pharmaceutical compositions containing the above compounds and to methods of treating hyperproliferative disorders, such as cancer, in a mammal by administering the above compounds.

Abstract: 2-Cyclopropyl-4-(4?-fluorophenyl)quinoline-3-carboxyaldehyde useful as a material for pharmaceutical products, can be obtained by reacting 3-cyclopropyl-3-oxopropanenitrile with 2-amino-4?-fluorobenzophenone to obtain 2-cyclopropyl-4-(4?-fluorophenyl)quinoline-3-carbonitrile, and reducing it.

Abstract: A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.

Abstract: A substituted 8-aryl quinoline and its benzenesulfonic acid salt is synthesized.

Abstract: Disclosed herein are bridged perinones/quinophthalones of the general formula (I) or tautomeric forms thereof where X1, X2, Ar1 Ar2 and B are as described herein and are particularly characterized in that the bridging B is a radical of the formula —T1—W—T2—, where T1 and T2 are independently O or S and W is alkylene, especially C1-C6-alkylene, C6-C10-arylene, especially phenylene or cycloalkylene, which are each optionally substituted or is the radical of the formula (a) where the phenyl rings are optionally substituted and A is a radical of the formula O, S, SO, SO2 or CO, optionally substituted alkylene, or optionally substituted cycloalkylene, said alkylene or cycloalkylene being attached to the adjacent phenyl rings itself or else via its substitutents, or W is a radical of the formulae where s and t are independently from 1 to 6, the ends of the radical B each being attached to an aromatic carbon atom of the two radicals Ar1

Abstract: There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1 is hydrogen etc., B is bond, or B—N—R1 forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and &agr;1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for &agr;1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which &agr;1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by &agr;1B adrenoceptor.

Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3 quinolyl]prop-2-enal is prepared in a high yield by reducing 3-[2-cyclo-propyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile with Raney nickel either in the presence of formic acid and 0.25 to 1 part by volume of water per part by volume of formic acid or in the presence of both an amine salt of formic acid and an organic acid.

Abstract: Quinophthalone derivatives have the general formula I 1

Abstract: Compounds of general formula (I) in which: A represents a hydrogen atom, a hydroxyl, a C1-3 alkoxy group, a hydroxy(C1-6 alkyl) group, a (C1-3 alkoxy)(C1-3 alkyl) group, a thiol, (C1-6 alkyl)sulfanyl or a halogen; B and D represent, independently of one another, a hydrogen atom, a C1-6 alkyl group, a fluoro(C1-6 alkyl) group or a perfluoro(C1-2 alkyl) group or B and D together from an oxo; R1 represents a phenyl, a naphthyl or a heteroaryl comprising 4 or 5 carbon atoms; R2 and R3 represent, independently of one another, a hydrogen atom, a halogen or a C1-6 alkyl group, R4 represents a hydrogen atom, a hydroxyl or a halogen, and R5 and R6 represent, independently of one another, a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a C3-6 cycloalkenyl group, a fluoro(C1-6 alkyl) group or a perfluoro(C1-2 alkyl) group or R5 and R6 together form a C2-6 alkylene chain or a C3-6 alkenylene chain, to give, with the nitrogen to which they are attached, a heteroc

Abstract: Hydrazones and hydrazone analogs are provided which are useful as upregulators of LDL receptors and can be used in the treatment of hypercholesterolemia and related disorders and conditions.

Abstract: The invention relates to compounds of the formula: and to pharmaceutically acceptable salts and solvates thereof wherein Y, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings defined in the specification. The invention also relates to pharmaceutical compositions comprising said compounds and to the use of said compounds for inhibiting abnormal cell growth in mammals. The compounds of the above formula have activity as farnesyl protein transferase inhibitors.

Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.

Abstract: The tetrahydroquinolines can be prepared by condensing appropriately substituted tetrahydroquinoline aldehydes with suitable substances and subsequently varying the substituents present by customary methods. The tetrahydroquinolines are suitable as active compounds in medicaments, in particular in medicaments. for the treatment of arteriosclerosis and dyslipidaemias.

Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile is prepared by reacting 2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-carbaldehyde with acetonitrile in the presence of a base and then adding a dehydrating to the reaction mixture to conduct dehydration. Under ordinary conditions, novel 3-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3-hydroxypropionitrile is formed as an intermediate in the above reaction. Incidentally, when the above reaction is conducted in an organic solvent, 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-prop-2-enenitrile is directly formed.

Abstract: CRF antagonists of Formulas I-V, wherein the B group in the Formulas contains an oxime The variables in the Formulas have the meanings described herein.

Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di

Abstract: Electrochemical oxidation of organic disulfides is conducted in an electrolytic solution containing an arene (e.g., anthracene, acenaphthylene, phenanthrene), and depending on the arene used and/or the product desired, an organic base (e.g., pyridine) to effect the synthesis of organothiated products in good yields.

Abstract: Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

Abstract: Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

Abstract: Quinoline compound, zinc halogenide complex and zinc complex suited for use in an electro-luminescence (EL) element, a fluorescent material and an ultraviolet absorption material, and a preparation process for these compounds are described. These compounds and a tautomer of the same has a strong luminescent intensity and is used for an EL material, the compound of zinc halogenide complex and zinc complex and a tautomer of the same has absorption at a wave length of 400 nm or less and is used for an ultraviolet absorption material, and further the quinoline compound and a tautomer has a strong luminescent intensity and is used for a fluorescent material. The zinc halogenide complex and zinc complex can be prepared by related preparation processes directly from a quinoline derivative and a phthalimide derivative, or by way of the quinoline compound which is obtained from these derivatives.

Abstract: The quenching compounds of the invention are nitrogen-substituted xanthenes that are substituted by one or more aromatic or heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable fluorescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications.

Abstract: The use of derivatives of quinoline- or quinoxaline-5,8-diones or -diols in cosmetics, especially for the dyeing of keratinous matter and, in particular, the hair. It also relates to novel compounds of this class. The invention is also directed to dyeing compositions comprising the said compounds and to the method of dyeing keratinous fibers.

Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di

Abstract: The present invention relates to novel 4-substituted quinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: wherein R1, R2, R3, R4, R5, R6, R7, R9, and Y, have the meanings provided.

Abstract: Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.

Abstract: The synthesis of asymmetric tetrasubstituted cyclooctatetraenes (“COTs”) and the use of said compounds in organic light emitting diodes is reported, wherein said COTs represent a class of wide gap electron transporters that are readily deposited in vacuum.

Abstract: This invention provides a series of substituted propanamines useful as tachykinin receptor antagonists. This invention also provides methods employing these substituted propanamines as well as pharmaceutical formulations comprising these compounds.