Abstract: The invention concerns a compound of general formula (I), wherein: X represents an oxygen or sulphur atom; R1 represents, independently of each other when n=2 or 3, a halogen atom, a hydroxy, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, a trifluoromethyloxy or a methylenedioxy; R2 represents a C1-C6 alkyl group optionally substituted, a C3-C7 cycloalkyl, piperidinyl or phenyl group, the C3-C7 cycloalkyl, piperidinyl or phenyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-C6 alkyl group optionally substituted; R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 and R5′ represent, independently of each other, a hydrogen atom, a hydroxy, a halogen atom, a C1-C3 alkyl group, or R5 and R5′ form together an oxo group; R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, or a trifluoromethoxy; in the form of a base, addition to an acid, hydrate or solvate. The invention is applicable in therapy.

Abstract: This invention relates to a method of using novel 5-(arylsulfonyl)-,5-(arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar′, R6, m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras-oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

Abstract: There is provided compounds of formula (I), wherein X1, X2, X3, Y4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.

Abstract: The present invention relates to a fiber-dyeing agent (A) prepared by mixing two components (A1) and (A2), said agent being characterized in that component (A1) contains at least one compound of formula (I) wherein X denotes a halogen atom, a methoxy group or an ethoxy group; Y denotes an oxygen atom, a sulfur atom or a selenium atom; R1 and R2 are equal or different and independently of each other denote hydrogen, a halogen atom, a (C1-C4)-alkyl group, a halogen-substituted (C1-C4)-alkyl group, a (C1-C4)-alkoxy group, a nitro group, an acetamido group or an NRaRb group, wherein the Ra and Rb groups are equal or different and independently of each other denote hydrogen, a (C1-C4)-alkyl group, an optionally substituted aromatic carbon ring or a (C1-C4)-alkanecarbonyl group, or Ra and Rb together with the nitrogen atom form a heterocyclic (C3-C6) group, and component (A2) contains at least one compound from the group consisting of amines, aminonitrobenzenes and phenols; to a method for dyeing

Abstract: The invention provides compounds of Formula I: 1

Abstract: The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.

Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract: Novel 2-arylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders that are responsive to the opening of the KCNQ potassium channels, including pain and migraine.

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: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.

Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.

Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.

Abstract: The present invention relates to compounds of the general formula 1

Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.

Abstract: The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH═CHR2, CH═C═CHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7acycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form —CHR8—CH2—CHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl.

Abstract: This invention relates aryl substituted benzimidazoles of Formula I: 1

Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the &agr;7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Abstract: A photo-induced phase transition organic material is composed of a diheteroarylethene-based compound within which the photo-chromic reaction occurs in the crystalline state. The diheteroarylethene-based compound of the present invention reversibly changes in color with light irradiation and also changes in phase from the open-ring form in the crystalline state to the closed-ring form in the crystalline state, or from the closed-ring form in the crystalline state to the open-ring form in the crystalline state via the liquid state, and can be applicable to optical recording media, display panels, sensors, optical switch devices and the like, by taking advantages of its variations in color with light irradiation and also its changes in physical property, such as the refractive index and the permeability, with its changes in phase.

Abstract: A non-resonant two-photon absorbing material is provided, comprising a specified compound and exhibiting far stronger non-resonant two-photon absorption and two-photon emission than conventional materials.

Abstract: The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.

Abstract: Compounds of the formula I 1

Abstract: The invention relates to compounds of formula: 1

Abstract: The object of the present invention is the use of 4-nitro-2,1,3-benzoxadiazole derivatives of general formula (I) as dye in colorants for keratin fibers such as, for example, wool, silk, furs or hair and particularly human hair In formula (I) X denotes oxygen, sulfur or NRa, Ra standing for hydrogen, a (C1-C4)-alkyl group, a monohydroxy-(C1-C4)-alkyl group, a polyhydroxy-(C2-C4)-alkyl group or a mono-(C1 C4)-alkoxy-(C1-C4)-alkyl group, R1 and R2 can be equal or different and independently of each other denote hydrogen, a halogen atom, a (C1-C4)-alkyl group, a halogen-substituted (C1-C4)-alkyl group, a (C1-C4)-alkoxy group, a nitro group or an NRbRc group, the Rb and Rc groups being equal or different and independently of each other denoting hydrogen, a (C1-C4)-alkyl group, an optionally substituted aromatic carbon ring or a (C1-C4)-alkanecarbonyl group, or Rb and Rc together with the nitrogen atom forming a heterocyclic (C3-C6) group, and Q denotes hydrogen, an aliphatic group, an aromati

Abstract: The invention provides an asymmetric cyanine dye compound having the structure including substituted forms thereof, wherein, at least one of R1 and R2 is linking group, X is O, S, or Se, and n ranges from 0 to 2. The invention further provides reporter-quencher dye pairs comprising the asymmetric cyanine dyes, dye-labelled polynucleotides incorporating the asymmetric cyanine dyes, and hybridization detection methods utilizing the dye-labelled polynucleotides.

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

Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.

Abstract: The present invention provides compounds of formula I 1

Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I 1

Abstract: The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), 1

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides sulfonamides, and compositions and methods utilizing sulfonamides that are useful in the treatment of diseases by blocking potassium channels associated with the onset or recurrence of the indicated conditions. Exemplary diseases treatable with the compounds, compositions and methods of the invention include sickle cell disease and glaucoma.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I: 1

Abstract: Compounds of the formula 1

Abstract: According to one embodiment the invention concerns a process for a degradation of an epothilone C or a epothilone D, wherein an epothilone C or epothilone D is subjected to an olefin metathesis in the presence of ethylene and subsequently an optional ester hydrolysis.

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates to epothilon derivatives and to their use.

Abstract: Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.

Abstract: Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.

Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.

Abstract: Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog with a thiomethyl thiazole ring stands out as the most potent.

Abstract: Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.

Abstract: Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.

Abstract: The present invention provides glucokinase activators of formula I: 1

Abstract: Aryl-benzimidazole compounds according to the formula where Ar1, R1, R2, Y, W, and N are as defined herein, bind to DNA and have antibacterial activity.

Abstract: Disclosed is an agent for inducing receptor potential, which comprises an organic dye compound capable of inducing/evoking receptor potential in response to photostimulation in the optic nerve, wherein the organic dye compound is a polymethine organic dye compound. Also disclosed is a substituent material for the retina comprising the agent.

Abstract: The invention relates to a process for preparing hydroxyindolylglyoxylamides in high yields and particularly pure form.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: 1

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