Abstract: The present invention relates to substituted indole oximes and methods of using them.

Abstract: The present invention provides substituted 3,3-diphenyl indole compounds, as well as analogues thereof, which are specific potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Abstract: The present invention relates to crystals of phosphorylated Aurora-A kinase fragment alone and in complex with a ligand, amino acid residues 1-43 of human TPX2. This invention also relates to methods for designing and selecting ligands, in particular allosteric inhibitors of Aurora-A, that bind to the Aurora-A kinase and their use. Further, the present invention relates to certain indene and indole derivatives. The present invention relates to crystals of phosphorylated Aurora-A kinase alone and in complex with a ligand, amino acid residues 1-43 of human TPX2. This invention also relates to methods for designing and selecting ligands that bind to the Aurora-A kinase and their use. Further, the present invention relates to certain indene and indole derivative.

Abstract: The present invention relates generally to substituted indoles such as substituted 1H-indole-2-carboxylic acid derivatives, and methods of using them.

Abstract: Indolestyryl compounds and use thereof for a high density recording media and method for fabricating the same. The indolestyryl compounds exhibit strong absorbance in the visible light region (400˜700 nm) of the spectrum, resistance to heat and light, high light sensitivity, and excellent solubility, resulting from their special chemical configuration. Furthermore, the indolestyryl compounds can be used as recording layer materials in high density recording media for matching a reading laser wavelength and enhancing the reflective index and carrier-to-noise ratio (CNR) of the high density recording media. Accordingly, the recording sensitivity and the readout characteristics of high density recording media comprising the indolestyryl compound according to the present invention can be improved.

Abstract: Anthranylic compounds having anti-CCK activity of general formula (I) in which, n is a whole number lying between 0 and 7; R1 is chosen independently from the groups (II), in which X1 is chosen independently from, S, O, NR2 and X2 is a group chosen from: H, C1-C4 alkyl, F, Cl, CF3, OCH3, OC2H5, CN; R2 is chosen from H or CH3; R3 is chosen from H, CH3, F, Cl, CF3, OCH3; R4 is chosen from the groups: H, —S—(CH2)m-R5, —SO2—(CH2)m-R5 (n different from 0), a branched alkyl group, a cyclo alkyl, a cyclo alkenyl, the group 1 or 2 adamantile, a phenyl group optionally substituted; R5 is chosen from the groups: H, linear or branched alkyl, cyclo alkyl, the group 1 or 2 adamantile, a suitably substituted phenyl group

Abstract: Compounds of formula (I) or salts or solvates thereof or physiologically functional derivatives thereof are potent binders at the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.

Abstract: The present invention relates generally to substituted indoles and methods of using them.

Abstract: The present invention relates to compounds of formula (I): wherein —X—Y—, R1 to R11 and n are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are mediated by CETP inhibitors.

Abstract: Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor (PAI-1) and as therapeutic composition for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis, coronary heart disease and pulmonary fibrosis.

Abstract: A catalytic transfer hydrogenation process is provided. The catalyst employed in the process is a metal hydrocarbyl complex which is coordinated to defined bidentate ligands substituted with at least one group selected from an optionally substituted sulphonated hydrocarbyl group, a sulphonated perhalogenated hydrocarbyl group, or an optionally substituted sulphonated heterocyclyl group. Preferred metals include rhodium, ruthenium and iridium. Preferred bidentate ligands are diamines and aminoalcohols, particularly those comprising chiral centres. The hydrogen donor is advantageously a secondary alcohol or a mixture of triethylamine and formic acid. The process can be employed to transfer hydrogenate ketones and imines, which are preferably prochiral. Catalysts for use in such a process are also provided.

Abstract: Compounds of the general formula I or IA or a salt in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours.

Abstract: The present invention synthesizes a series of novel indole analogs of 1-benzyl-3-(5?-hydroxymethyl-2?-furyl)indazole (YC-1), and their anti-platelet activity.

Abstract: The invention relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5, R6, A, m, n and p are defined as in claim 1. These compounds can be used as pharmaceutical compositions for the treatment of, for example, diabetes.

Abstract: The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lymphocytes).

Abstract: This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure: wherein: R1 is alkyl or optionally substituted cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl; R8 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; R9 is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene, 4-imidazolylmethylene, HSCH2—, CH3SCH2CH2—, H2NC(?O)CH2—, H2NC(?O)CH2CH2—, HO2CCH2—, HO2CCH2CH2—, H2NCH2CH2CH2CH2—, H2NC(?NH)NHCH2CH2CH2—, or taken together with R8 as —CH2CH2CH2—; or a pharmaceutically acceptab

Abstract: The present invention relates to a compound represented by the following formula (I): (wherein, W represents WA-A1-WB- (in which, WA is substituted or unsubstituted aryl, etc., A1 is —NR1—, single bond, —C(O)—, etc., and WB is substituted or unsubstituted arylene, etc.), R is single bond, —NH—, —OCH2—, alkenylene, etc., X is —C(O)—, —CH2—, etc., and M is, for example, the following formula: (in which, R11, R12 and R13 each independently represents hydrogen, hydroxyl, amino, halogen, etc., R14 is hydrogen or lower alkyl, Y represents —CH2—O—, etc., Z is substituted or unsubstituted arylene, etc., A2 is single bond, etc, and R10 is hydroxyl or lower alkoxy)), or salt thereof; and a medicament containing the same.

Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.

Abstract: A process is disclosed for modifying a parent ligand by attaching to the parent ligand a conjugation agent that is reactive with a moiety of a target receptor to which the parent ligand binds such that a covalent bond is formable between the conjugation agent and the receptor moiety. Also disclosed are compositions, probes and methods of detecting and/or quantifying receptors using the modified ligands of the invention.

Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.

Abstract: Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds. Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl); inhibiting Wnt signaling.

Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: The invention relates to novel ligands of the phosphanylbenzothiophenyl-dihydroisoxazoline, phosphanyl-dihydrooxazolyl-indole and phosphanyl-dihydrooxazolyl-benzofuran type, especially compounds of formula I and mixtures of such compounds, wherein X is oxygen, sulfur, selenium or NQ, wherein Q is unsubstituted or substituted aryl, or alkyl or substituted alkyl; n is 0, 1, 2, 3 or 4; A1 and A2 are each an organic radical capable of bonding to phosphorus, especially unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted cycloalkyl, or —N(D)2 wherein D2 is alkyl or substituted alkyl; or A1 and A2 together with the bonding phosphorus atom form a ring, which may be unsubstituted or substituted; Y, Y?, Y? and Y?? are each independently of the other hydrogen or alkyl, substituted alkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heterocyclyl, at least one of the radicals Y, Y?, Y? or Y?? being one of

Abstract: This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure: wherein: R1 is alkyl or optionally substituted cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl; R8 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; R9 is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene, 4-imidazolylmethylene, HSCH2—, CH3SCH2CH2—, H2NC(?O)CH2—, H2NC(?O)CH2CH2—, HO2CCH2—, HO2CCH2CH2—, H2NCH2CH2CH2CH2—, H2NC(?NH)NHCH2CH2CH2—, or taken together with R8 as —CH2CH2CH2—; or a pharmaceutically acceptab

Abstract: Compounds of the general formula (I): or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.

Abstract: The present invention provides novel synthetic intermediates for the production of indoline derivatives, which exhibit excellent ACAT inhibitory activity, and processes for the preparation thereof.

Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.

Abstract: The present invention relates to sulfonyl-containing 2,3-diarylindole, especially to new compounds of general Formula, to a preparation method for their preparation, to pharmaceutical compositions containing said compound, and to the medical use thereof in the treatment of diseases relating to the inhibition of cyclooxygenase-2 (COX-2).

Abstract: The invention concerns the use of a compound of formula (I), in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, in the treatment of a disease or condition mediated by monocyte chemoattractant protein-1 (MCP-1). Certain of the components of formula (I) are novel and are provided, together with pharmaceutical compositions thereof, as further features of the invention.

Abstract: Novel compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.

Abstract: Indole compounds of the formula: wherein L1 is CO; L2 is a bond; R1 is aryl or heteroaryl; R2 is H, aryl, heteroaryl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR?, SO2R, SO3R, SO2NRR?, SR, NRR?, NRSO2NR?R?, NRSO2R?, NRSO3R?, NRC(O)R?, NRC(O)NR?R?, NRC(O)OR?, NRC(N)NR?R?, C(O)OR, or C(O)NRR?; each of Ra, Rb, Rc, and Rd, independently, is R, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR?, SO2R, SO3R, SO2NRR?, SR, NRR?, NRSO2NR?R?, NRSO2R?, NRSO3R?, NRC(O)R?, NRC(O)NR?R?, NRC(O)OR?, NRC(N)NR?R?, C(O)R, C(O)OR, C(O)NRR?, or Rb and Rc, Ra and Rb, or Rc and Rd taken together are O(CH2)nO; and Rc is H, alkyl, alkenyl, alkynyl, cyclyl, heterocyclyl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR?, SO2R, SO3R, SO2NRR?, SR, NRR?, NRSO2NR?R?, NRSO2R?, NRSO3R?, NRC(O)R?, NRC(O)NR?R?, NRC(O)OR?, NRC(N)NR?R?, C(O)R, C(O)OR, or C(O)NRR?; in which each of R, R?, and R?, independently, is H, alkyl, alkenyl, alky

Abstract: The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.

Abstract: The invention concerns the use of indoline derivatives of formula (I): in which R1, R2, R3, R4 and R5 independently of one another represent hydrogen or C1-4 alkyl groups, or R4 and R5 together with the oxygen atoms to which they are attached represent a C1-4 alkylenedioxy group, or of salts of such indoline derivatives, as additives to hair dyeing agents of the direct dyeing or primary intermediate/secondary intermediate type, thus producing hair dyeing with excellent color fastness characteristics.

Abstract: Anionic polymerization initiators useful in the preparation of polymers having a protected amine functional group. The amine functionality includes a first protecting group, which can be aralkyl, methyl, allyl or tertiary alkyl group. The other of the amine protecting groups can be the same as the first protecting group. Alternatively, the second protecting group can be different from the first protecting group, in which case it is selected to have differential stability to agents used to remove the aralkyl, methyl, allyl or tertiary alkyl protecting group.

Abstract: Methods for making bis-heterocyclic compounds, especially bis-heterocyclic compounds having five and six-membered heterocyclic linkers are described.

Abstract: A hybrid dye is provided that is useful for coloring keratin fibers and skin. The hybrid dye has the structure X-S-Y, where X is derived from a substantive dye, Y is derived from an oxidation dye precursor or a melanin precursor, and S is a direct bond or spacer group. The present invention also provides a composition for coloring keratin fibers that contains the hybrid dye.

Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.

Abstract: This invention relates to novel substituted tryptamines and related derivatives, as well as pharmaceutical compositions formulated therefrom. These compounds, compositions and their salts can be used in the manufacture of medicaments for interacting with the melatoninergic system. These compounds and conditions can be used for treating several types of medical conditions, such as central nervous system and psychiatric disorders (sleep disorders, epilepsy and other convulsive disorders, anxiety, neurodegenerative diseases), chronobiological-based disorders (jet lag, delayed sleep syndrome, shift-work, seasonal affective disorder), neoplastic conditions, and conditions associated with senescence.

Abstract: The present invention relates to compound of formula (I) wherein R1, R2, R3, R4, R5 and n are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment of diseases which are associated with cysteine proteases such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.

Abstract: A compound of formula (1) wherein R1 is hydrogen, halo or methoxy, R2 is hydrogen, halo, methyl, ethyl or methoxy; R3 is carboxy, tetrazolyl, or —CONHSO2R4 where R4 is methyl, ethyl, phenyl, 2,5-dimethylisoxazolyl or trifluoromethyl; T is —CH2— or —SO2—; and ring A is 3-chlorophenyl, 4-chlorophenyl, 3-trifluoromethylphenyl, 3,4-dichlorophenyl, 3,4-difluorophenyl, 3-fluoro-4-chlorophenyl, 3-chloro-4-fluorophenyl or 2,3-dichloropyrid-5-yl; or a pharmaceutically acceptable salt or prodrug thereof, as well as pharmaceutical compositions containing them are described and claimed. These compounds and compositions are useful in the treatment of disease mediated by monocyte chemoattractant protein-1 or RANTES (Regulated Upon Activation, Normal T-cell Expressed and Secreted), such as inflammatory disease.

Abstract: Disclosed are multibinding compounds which are &bgr;2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: The instant invention discloses a process for the synthesis of substituted indole cell proliferation inhibitors.

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an indole compound represented by the following formula (I), its pharmacologically acceptable salt or hydrates thereof: In the formula, R1 represents hydrogen atom, a halogen atom or cyano group; R2 and R3 are the same as or different from and each represents hydrogen atom, a C1˜C4 lower alkyl group or a halogen atom; R4 represents hydrogen atom or a C1˜C4 lower alkyl group; and the ring A represents cyanophenyl group, aminosulfonylphenyl group, aminopyridyl group, aminopyrimidyl group, a halopyridyl group or cyanothiophenyl group, provided that the case where all of R1, R2 and R3 are hydrogen atoms, where both R2 and R3 are hydrogen atoms or where the ring A is aminosulfonyl group and both R1 and R2 are halogen atoms is excluded.

Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.

Abstract: Anionic polymerization initiators useful in the preparation of polymers having a protected amine functional group. The amine functionality includes a first protecting group, which can be aralkyl, methyl, allyl or tertiary alkyl group. The other of the amine protecting groups can be the same as the first protecting group. Alternatively, the second protecting group can be different from the first protecting group, in which case it is selected to have differential stability to agents used to remove the aralkyl, methyl, allyl or tertiary alkyl protecting group.

Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description

Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of &agr;,&bgr;-unsaturated aldehydes.

Abstract: A heterocyclic derivative of the formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.