Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and comprising at least one therapeutic agent selected from an agent interacting with a 5-HT3 receptor and/or an agent interacting with 5-HT4 receptor, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are methods of treating a disorder of the stomach, intestine or duodenum in a human subject. The method includes administering to the subject, a pharmaceutical composition comprising a compound that increases gastrointestinal motility (e.g., by modulating myenteric nerve activity) and/or induces the secretion or production of growth hormone.

Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.

Abstract: The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.

Abstract: The present invention relates to uses of 2-(1H-indolylsulfanyl)-benzyl amine derivatives of general formula (I): in the treatment of affective disorders.

Abstract: The present invention relates to novel methods for the identification of compounds useful for the treatment of drug resistance, and to novel treatment methods using the identified compounds.

Abstract: The present invention relates to 2-(1H-indolylsulfanyl)-benzyl amine derivatives of general formula (I):

Abstract: The present invention is related to the use of a Glepp-1 inhibitor for the manufacture of a medicament for the treatment of an autoimmune and/or an inflammatory disorder.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —O—, —S—, or —S(O)—; and the other substituents are as defined in the specification; or individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to a compound represented by the formula (I), wherein all symbols are as defined in the description, a salt thereof, a solvate thereof, or a prodrug thereof, which has a leukotriene receptor antagonistic activity which is expected to be more effective than those of the leukotriene receptor antagonists currently used in clinical trials. Therefore, it is useful as an agent for the prevention and/or treatment of a leukotriene-mediated disease such as a respiratory diseases such as bronchial asthma, chronic obstructive pulmonary disease, pulmonary emphysema, chronic bronchitis, pneumonia (e.g. interstitial pneumonia etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), or the like, or as an expectorant or an antiitussive.

Abstract: The present invention relates to uses of 2-(1H-indolylsulfanyl)-benzyl amine derivatives of general formula (I): in the treatment of affective disorders.

Abstract: Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Significantly, NSC-87877 is active in cell-based assays and has no detectable off-target effects in the EGF-stimulated Erk1/2 activation pathway. Additionally, a number of analogs of NSC-117199 have been produced. These analogs exhibit enhanced protein tyrosine phosphatase inhibition and are found to be potent and/or selective inhibitors of Shp1 and/or Shp2 protein tyrosine phosphatases.

Abstract: The present invention provides new compounds of formula Ia and Ib: as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Abstract: The present invention relates to pharmaceutical compositions containing 2-oxo-1-pyrrolidine derivatives and methods for treating Parkinson's Disease in a chronic dopamine replacement therapy using L-DOPA by administering the derivatives.

Abstract: A compound including at least one type of an optionally substituted indolocarbazole moiety and at least one divalent linkage.

Abstract: The present invention relates to compounds of formula I: wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification and claims, which compounds are active on the GABAB receptor and are useful in the control or prevention of CNS illnesses, especially of illnesses and disorders comprising anxiety, depression, epilepsy, schizophrenia, and cognitive disorders.

Abstract: Biodegradable implants comprising dopamine modulating compounds are described.

Abstract: Processes are disclosed for preparing indolinone phenylaminopropanol derivatives, particularly chiral indolinone phenylaminopropanol derivatives of the general formula: The processes disclosed may be used to prepare, inter alia, 7-fluoro-1-[(1S, 2R)-1-(3-fluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one and 7-fluoro-1-[(1S, 2R)-1-(3,5-difluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one. Intermediates of the processes are also disclosed.

Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.

Abstract: The present invention discloses a novel process and novel intermediates for the Preparation of 4-[2-(di-n-propyl amino) ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole (I) and pharmaceutical composition comprising the same. Further the present invention also discloses a method of treatment for cardiovascular disorders and Parkinson's disease.

Abstract: The invention relates to the use of an inhibitor of the biosynthesis and/or function of LTB4 for the manufacture of a medicament for the treatment of B-cell chronic lymphocytic leukemia (B-CLL), B-prolymphocytic leukemia (B-PLL) or B-cell lymphoma. Preferably, the inhibitor of the biosynthesis and/or function of LTB4 is the inhibitor of 5-LO BWA4C or the inhibitor of FLAP MK-886.

Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical uses of these compounds are related to contraception, the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minication of side effects of cyclid menstrual bleeding. Additional uses of the invention include stimulation of food intake.

Abstract: A 5-fluorooxindole-3-carboxylic acid ester represented by a formula (2): wherein R1 is a group selected from the group consisting of an unsubstituted or substituted alkyl group having 1 to 10 carbon atoms, an unsubstituted or substituted cycloalkyl group having 3 to 7 carbon atoms, an aralkyl group having 7 to 10 carbon atoms or an aryl group having 6 to 14 carbon atoms.

Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.

Abstract: The present invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a derivative thereof, X is —CO2H, 1H-tetrazol-5-yl or 2H-tetrazol-5-yl and R1 and R2 are each independently selected from the group consisting of: C1-6alkyl and C3-6cycloalkyl, as well as pharmaceutical composition comprising said compounds and methods of using said compounds. The compounds of the present invention lower the level of A?42 and are therefore useful for preventing, delaying or reversing the progression of Alzheimer's Disease.

Abstract: The present invention comprises compositions for pharmaceutical drug delivery of an indolone (e.g., ropinirole), or a pharmaceutically acceptable salt thereof. The composition may, for example, be a gel suitable for transdermal application. The compositions of the present invention typically comprise a hydroalcoholic vehicle, one or more antioxidant, and one or more buffering agent, wherein the pH of the gel is usually between about pH 7 and about pH 9. The compositions may include further components, for example, the hydroalcoholic vehicle may further comprise additional solvent(s), antioxidant(s), cosolvent(s), penetration enhancer(s), buffering agent(s), and/or gelling agent(s). The compositions may be used for the treatment of a variety of neurological disorders.

Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.

Abstract: This invention pertains to certain 4-(1-(sulfonyl)-1H-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds, and analogs thereof, including compounds of the following formula, which are, inter alia, antiproliferative agents, anticancer agents, and/or thioredoxin/thioredoxin reductase inhibitors: formula (I) wherein: Ar is a 1-(sulfonyl)-1H-indol-2-yl group; the bond marked ? is independently: (a) a single bond; or: (b) a double bond; the bond marked ? is independently: (a) a single bond; or: (b) a double bond; the group —ORO is independently: (a) —OH; (b) an ether group (e.g., —OMe); or: (c) an acyloxy (i.e., reverse ester) group (e.g.

Abstract: Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine.

Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.

Abstract: The present invention relates to cycloalkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

Abstract: The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation, particularly congestive heart failure, comprising administering to a patient in need thereof an effective amount of a compound of the formula: I or a pharmaceutically acceptable salt thereof.

Abstract: The present invention discloses novel sulfenate derivatives and their bioconjugates for phototherapy of tumors and other lesions. The sulfenates of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photofragmentation of the sulfenate moiety, with the tissue of interest.

Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, R5, R6, L1, L2, M, n, p, X, Y and Z are as described in the specification; pharmaceutical compositions thereof, methods of making said pharmaceutical compositions; and methods of use thereof.

Abstract: ACE inhibitor nitroderivatives of formula (I): A—(X1—ONO2)s ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating cardiovascular and renal diseases and inflammatory processes.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity c-kit kinase.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

Abstract: This invention relates to the use of compounds of Formula (I) as vascular damaging agents: wherein X is selected from: —O—, —S—, —S(O)—, —S(O2)—, —N(R5)—, —C(O)—, —C(O)N(R5)—, —N(R5)C(O)—, —S(O2)N(R5)—, or —N(R5)S(O2)—; R1 is independently selected from: amino, halo, hydroxy, —OPO3H2, C1-4alkyl, or C1-4alkoxy, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified; R2 is selected from: hydrogen or C1-4alkyl; R3 is selected from: hydrogen, halo, hydroxy, hydroxyC1-4alkyl, cyano, cyanoC1-4alkyl, carboxy, carboxyC1-4alkyl, C1-4alkanoyl, C1-4alkanoylC1-4alkyl, carbamoyl, carbamoylC1-4alkyl, C1-4alkoxy, C1-4alkoxycarbonyl, C1-4alkoxycarbonylC1-4alkyl, C1-4alkoxycarbonylamino, amino, N—C1-4alkylamino, NN-diC1-4alkylamino, aminoC1-4alkyl, N—C1-4alkylaminoC1-4alkyl, NN-diC1-4alkylaminoC1-4alkyl, ureido, or C1-4alkylureyleno; R4 is independently selected from: C1-4alkyl, C1-4alkoxy or halo; R5 is selected from: hydrogen or C1-4alkyl; n is 0 or 1; p is

Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical uses of these compounds are related to contraception, the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minication of side effects of cyclid menstrual bleeding. Additional uses of the invention include stimulation of food intake.

Abstract: The present invention relates to aryl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).

Abstract: The present invention provides novel N-substituted fluorooxindoles having the general Formula I wherein the wavy bond represents the racemate, the (R)-enantiomer or the (S)-enantiomer and m, n, p, q, A, B, D, Q, X, and Z are as defined below, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

Abstract: This invention is directed to indolone derivatives which are selective antagonists for the GalR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.

Abstract: The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with 5-HT6 receptors, including schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders selected from the group consisting of age-related cognitive decline, mild cognitive impairment, and dementia, comprising: administering to a patient in need thereof an effective amount of a compound of formula I.

Abstract: The present invention relates to phthalimide carboxylic acid derivatives of formula (I), methods for their preparation, pharmaceutical compositions containing them and their use in medicine, specifically in the treatment of cancer. (I), wherein X is O or S; R1 is a phthalimide carboxylic acid group of formula (II).

Abstract: The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is: and wherein R1–R5 and Q1 are defined as described herein. Specifically, methods for treating acne, hirsutism, and a composition for conditioning the skin are described.

Abstract: A method for inhibiting neoplastic cells and related conditions by exposing them to substituted indole derivatives.

Abstract: The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.