Class / Patent application number | Description | Number of patent applications / Date published |
514254090 | Indole ring system (including hydrogenated) attached directly or indirectly to the piperazine ring by nonionic bonding | 70 |
20080280923 | 1-Benzylindole-2-Carboxamide Derivatives - The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particularly for the treatment of obesity or nicotine dependence. | 11-13-2008 |
20080318973 | Urotensin II receptor antagonists - This invention is directed to a compound of Formula (I): | 12-25-2008 |
20090018141 | KINASE INHIBITORS, COMPOSITIONS THEREOF, AND METHODS OF USE THEREWITH - Provided herein are Compounds having the following structure: | 01-15-2009 |
20090023749 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL)BUTYL-4-(2- -CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 01-22-2009 |
20090042906 | METHODS FOR TREATING CANCERS ASSOCIATED WITH CONSTITUTIVE EGFR SIGNALING - Aspects of the invention relate to methods and compositions for treating cancers associated with constitutive EGFR signaling. Methods include inhibiting one or more components of the c-Met and/or Axl signaling pathways. Aspects of the invention also relate to methods for determining whether a subject is a candidate for treatment with an inhibitor of a c-Met and/or Axl signaling component. | 02-12-2009 |
20090048267 | MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES - The present invention relates to the use of indolinones of general formula | 02-19-2009 |
20090054459 | Substituted indoles - Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R | 02-26-2009 |
20090076029 | Compounds and Methods for Treating Obesity - Methods for selection of compounds for treatment of obesity, compounds selected by the disclosed methods, and methods of treatment of obesity, wherein a selective melanocortin-4 receptor compound is identified, which compound is further characterized in that it attenuates the binding of both an agonist, including alpha-melanocyte stimulating hormone, and an inverse agonist, including agouti-related protein, to a melanocortin receptor, including melanocortin-4 receptor. | 03-19-2009 |
20090105274 | Indolecarboxylic Acid Derivative Having PGD2 Receptor Antagonistic Activity - The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. | 04-23-2009 |
20090118301 | Compositions and Methods for Treating Cancer - The invention provides compounds useful for treating or effecting prophylaxis of cancers, particularly cervical cancer. | 05-07-2009 |
20090221605 | SUBSTITUTED PYRROLE-2, 5-DIONES AS PROTEIN KINASE C INHIBITORS - A compound of formula I | 09-03-2009 |
20090221606 | CRYSTALLINE (3-CYANO-1H-INDOL-7-YL)-[4-(4-FLUOROPHENETHYL) PIPERAZIN-1-YLIMETHANONE PHOSPHATE - The present invention relates to novel crystalline forms of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone phosphate and to pharmaceutical compositions containing said forms. | 09-03-2009 |
20090247547 | HYDROXAMATE-BASED INHIBITORS OF DEACETYLASES B - The present teachings relate to compounds of Formula I: | 10-01-2009 |
20090264443 | TREATMENT OF ORGANOPHOSPHATE EXPOSURE WITH TETRAHYDROINDOLONE ARYLPIPERAZINE COMPOUNDS - A method of treating exposure to organophosphate agents through the use of compounds comprising tetrahydroindolone and arylpiperazine moieties. | 10-22-2009 |
20090318471 | New Salts and Crystalline Salt Forms of an Indolinone Derivative - The present invention relates to new salts and crystalline salt forms of an indolinone derivative which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament. | 12-24-2009 |
20100016332 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL) BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)-piperazine, crystaline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 01-21-2010 |
20100056544 | Salts with CRTH2 Antagonist Activity - The potassium, sodium, ammonium, lysine, diethylamine, tromethamine (TRIS), piperazine, ethylenediamine and ethanolamine salt of a compound of general formula (I): wherein R | 03-04-2010 |
20100063062 | NOVEL USE OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYL-BENZOFURAN-5-YL)-PIPERAZINE AND ITS PHYSIOLOGICALLY ACCEPTABLE SALTS - 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof is used for the manufacture of a medicament for the treatment of sub-type anxiety disorders chosen from the sub-types panic disorder with or without agoraphobia, agoraphobia. obsessive-compulsive spectrum disorders, social phobia, posttraumatic stress disorder, acute stress indication or generalized-anxiety disorder, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, anorexia and fibromyalgia. A preferred salt is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride. | 03-11-2010 |
20100087446 | 2-SUBSTITUTED INDOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - 2-Substituted indole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 04-08-2010 |
20100267742 | COMBINATION TARGETED THERAPY FOR LUNG CANCER - A combination of compounds is described that target protein kinases and is more effective than the individual compounds against cancer where EGFR is upregulated and c-met is activated, for example, epithelial cell tumors, and particularly, non small cell lung carcinomas (NSCLC). | 10-21-2010 |
20100286167 | DIHYDROXYPHENYL ISOINDOLYLMETHANONES - This invention provides methods for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I): | 11-11-2010 |
20100305141 | TETRAHYDROINDOLONE DERIVATIVES FOR TREATMENT OF NEUROLOGICAL CONDITIONS - Compositions comprising tetrahydroindolone derivatives in which the tetrahydroindolone moiety is covalently linked to a substituted arylpiperazine moiety and methods for treating neurological and psychiatric conditions using such compositions are disclosed. | 12-02-2010 |
20100331344 | Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 12-30-2010 |
20110039863 | COMBINATIONS FOR THE TREATMENT OF DISEASES INVOLVING CELL PROLIFERATION, MIGRATION OR APOPTOSIS OF MYELOMA CELLS, OR ANGIOGENESIS - The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations. | 02-17-2011 |
20110136826 | COMBINATIONS FOR THE TREATMENT OF DISEASES INVOLVING CELL PROLIFERATION, MIGRATION OR APOPTOSIS OF MYELOMA CELLS, OR ANGIOGENESIS - The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations. | 06-09-2011 |
20110178099 | Pharmaceutical combination - The present invention relates to a pharmaceutical combination which may be useful for the treatment of diseases which involve cell proliferation, which involve migration or apoptosis of myeloma cells, which involve angiogenesis or which involve fibrosis. The invention also relates to a method for the treatment of said diseases, comprising simultaneous, separate or sequential administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations. | 07-21-2011 |
20110183994 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL) BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline Modifications of the hydrochloride of 1-[4-(5-cyanoin-dol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoin-dol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2 -carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 07-28-2011 |
20110190317 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL) BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 08-04-2011 |
20110190318 | Pharmaceutical dosage form for immediate release of an indolinone derivative - The present invention relates to a pharmaceutical dosage form delivering an immediate release profile containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate. | 08-04-2011 |
20110195976 | COMPOUNDS DERIVED FROM 2-(3-METHYLENEDIOXY)-BENZOYL INDOL - The present invention describes a series of derivatives of 2-(3-methylenedioxy)-benzoyl indol, their mixtures, their pharmaceutically acceptable salts, their enantiomers, pharmaceutical compositions comprising them, processes for preparing them, use in the prophylactic and/or curative treatment of sexual dysfunction. More specifically, the invention describes derivatives (R)-3-((2-(benzo[d][1,3]dioxol-5-carbonyl)-1H-indol-3-yl)methyl)-1-methylpiperazine-2,5-dione, and S)-3-((2-(benzo[d][1,3]dioxol-5-carbonyl)-1H-indol-3-yl)methyl)-1-methylpiperazine-2,5-dione. | 08-11-2011 |
20110294824 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL)BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 12-01-2011 |
20110294825 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL)BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 12-01-2011 |
20110301177 | Capsule pharmaceutical dosage form comprising a suspension formulation of an indolinone derivative - The present invention relates to a suspension formulation containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate, to a capsule pharmaceutical dosage form containing said suspension formulation, to a process for preparing said suspension formulation, to a process for preparing said capsule comprising said suspension formulation and to the packaging material for the finished capsule. | 12-08-2011 |
20110312971 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL) BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 12-22-2011 |
20110312972 | SUBSTITUTED 3-BENZOFURANYL-INDOL-2-ONE-3-ACETAMIDIDOPIPERAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - The invention relates to disubstituted 3-benzofuranyl-indol-2-one-3-acetamidopiperazine derivatives of the general formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are such as defined in claim | 12-22-2011 |
20120040996 | 3-BENZOFURANYL-INDOL-2-ONE DERIVATIVES SUBSTITUTED AT THE 3 POSITION, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - The invention relates to 3-benzofuranyl-indol-2-one derivatives substituted at the 3 position and of the formula (I) where R1, R2, R3, R4, R5 and n are such as defined in claim | 02-16-2012 |
20120077825 | NOVEL USE OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYL-BENZOFURAN-5-YL)-PIPERAZINE AND ITS PHYSIOLOGICALLY ACCEPTABLE SALTS - 1-[4-(5-cyanoindo1-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof is used for the manufacture of a medicament for the treatment of sub-type anxiety disorders chosen from the sub-types panic disorder with or without agoraphobia, agoraphobia. obsessive-compulsive spectrum disorders, social phobia, posttraumatic stress disorder, acute stress indication or generalized-anxiety disorder, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, anorexia and fibromyalgia. A preferred salt is 1-[4-(5-cyanoindo1-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride. | 03-29-2012 |
20120108607 | OPTICALLY ACTIVE 3-[(PHENYLPIPERAZIN-1-YL)ALKYL]-3- ALKYL-OXINDOLE DERIVATIVES HAVING CNS ACTIVITY - The present invention relates to the enantiomers of 5,7-dichloro-3-{4-[4-(4-chlorophenyl)-piperazin-1-yl]butyl}-3-ethyl-1,3-dihydro-2H-indol-2-one of the Formula (II) pharmaceutically acceptable salts thereof, process for the preparation thereof, medicinal products containing said enantiomers and the use thereof and their pharmaceutically acceptable salts in the treatment of the disorders of the central nervous system. | 05-03-2012 |
20120136004 | NEW COMBINATION THERAPY IN TREATMENT OF CANCER AND FIBROTIC DISEASES - The invention relates to new methods for the treatment of oncological and fibrotic diseases comprising the combined administration of a receptor tyrosine kinase inhibitor in conjunction with a thrombin inhibitor. | 05-31-2012 |
20120142703 | NEW COMBINATION THERAPY IN TREATMENT OF ONCOLOGICAL AND FIBROTIC DISEASES - The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of an inhibitor of vascular endothelial growth factor receptors (VEGFRs) in conjunction with a thrombin inhibitor. | 06-07-2012 |
20120157472 | METHOD FOR TREATING COLORECTAL CANCER - The present invention relates to a method of treating patients suffering from colorectal cancer characterized by coadministration of BIBF 1120 and BIBW 2992, wherein in said method BIBF 1120 is administered according to a continuous daily regimen and BIBW 2992 is administered according to a weekly alternating on-off regimen, pharmaceutical compositions and kits suitable for this method as well as their preparation. | 06-21-2012 |
20130012522 | NEW DERIVATIVES OF PROPARGYLAMINE HAVING NEUROPROTECTIVE CAPACITY FOR THE TREATMENT OF ALZHEIMER'S AND PARKINSON'S DISEASES - The present invention relates to a compound of formula (I) wherein: R | 01-10-2013 |
20130102615 | THIOAMIDE, AMIDOXIME AND AMIDRAZONE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - A compound of Formula I, including pharmaceutically acceptable salts thereof: | 04-25-2013 |
20130102616 | POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 04-25-2013 |
20130203773 | Pharmaceutical dosage form for immediate release of an indolinone derivative - The present invention relates to a pharmaceutical dosage form delivering an immediate release profile containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate. | 08-08-2013 |
20130210834 | INDIRUBIN DERIVATIVES AND USES THEREOF IN TREATING CHRONIC MYELOGENOUS LEUKEMIA - Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). One aspect of the invention relates to a method of treating CML using at least one indirubin derivative compound or a pharmaceutical composition thereof. Indirubin derivatives (IRDs) potently inhibited Signal Transducer and Activator of Transcription 5 (Stat5) protein in CML cells. Compound IRD 810 inhibits Bcr-Abl/Stat5 or Src/Stat5 signaling in human KCL-22 CML and imatinib-resistant human KCL-22 CML cells expressing the T315I mutant Bcr-Abl. Previous studies indicate that SFKs cooperate with Bcr-Abl to activate downstream Stat5 signaling. Activation of Stat5 was strongly blocked by IRD 810 in CML cells. IRDs disclosed herein have been identified as potent inhibitors of Bcr-Abl/Stat5 or SFK/Stat5 signaling pathway. IRDs disclosed herein are new therapeutics for wild type or T315I mutant Bcr-Abl-positive CML patients, and may also treat other solid tumors, including prostate cancer and lymphoma. | 08-15-2013 |
20130237549 | Pharmaceutical combination - The present invention relates to a pharmaceutical combination which may be useful for the treatment of diseases which involve cell proliferation, which involve migration or apoptosis of myeloma cells, which involve angiogenesis or which involve fibrosis. The invention also relates to a method for the treatment of said diseases, comprising simultaneous, separate or sequential administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations. | 09-12-2013 |
20130324554 | AMORPHOUS FORM OF VILAZODONE HYDROCHLORIDE SUBSTANTIALLY FREE OF CRYSTALLINE FORMS - Disclosed herein is a stable amorphous form of vilazodone hydrochloride substantially free of crystalline forms, a process for the preparation, pharmaceutical compositions, and methods of treating thereof. Disclosed also herein are stable amorphous co-precipitates of vilazodone hydrochloride and a pharmaceutically acceptable excipient, methods for the preparation, pharmaceutical compositions, and method of treating thereof. | 12-05-2013 |
20140024658 | POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 01-23-2014 |
20140057925 | AMORPHOUS FORM OF VILAZODONE HYDROCHLORIDE AND PROCESS FOR ITS PREPARATION - The present invention relates to an amorphous form of vilazodone hydrochloride and process for the preparation of amorphous form of vilazodone hydrochloride. The invention also relates to pharmaceutical compositions that include a therapeutically effective amount of the amorphous form of vilazodone hydrochloride and use of said compositions for the treatment of major depressive disorder (MDD). | 02-27-2014 |
20140066456 | COMBINATION THERAPY IN TREATMENT OF CANCER AND FIBROTIC DISEASES - The invention relates to new methods for the treatment of oncological and fibrotic diseases comprising the combined administration of a receptor tyrosine kinase inhibitor in conjunction with a thrombin inhibitor. | 03-06-2014 |
20140128408 | HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME - Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed. | 05-08-2014 |
20140128409 | MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES - The present invention relates to the use of indolinones of general formula | 05-08-2014 |
20140163040 | Pharmaceutical dosage form for immediate release of an indolinone derivative - The present invention relates to a pharmaceutical dosage form delivering an immediate release profile containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate. | 06-12-2014 |
20140179713 | POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3-YL) BUTYL] PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE AND PROCESS FOR PREPARING THEREOF - The present invention provides a solid state Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide. The present invention also provides a process for preparing Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide comprising the steps of i) reacting solid state form of 5-(1-piperazinyl)benzofuran-2-carboxamide or its salts with 3-(4-chlorobutyl)-1H-indole-5-carbonitrile an organic solvent in presence of a base to obtain crude vilazodone free base; ii) purifying the crude vilazodone free base of step (i) in an organic solvent; iii) treating the purified vilazodone free base of step (ii) with an organic solvent to obtain solid state form-Z of vilazodone. The present invention further provides a pharmaceutical composition comprising a therapeutically effective amount of an amorphous form of vilazodone hydrochloride and use of solid state Form-Z of vilazodone for the treatment of major depressive disorders. | 06-26-2014 |
20140187563 | COMBINATION THERAPY IN TREATMENT OF ONCOLOGICAL AND FIBROTIC DISEASES - The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of an inhibitor of vascular endothelial growth factor receptors (VEGFRs) in conjunction with a thrombin inhibitor. | 07-03-2014 |
20140194442 | ANTICANCER THERAPY - The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein. | 07-10-2014 |
20140200226 | ANTI-MALARIAL COMPOUNDS FROM MARINE NATURAL PRODUCTS - Novel compositions and methods for the treatment and prevention of malaria are disclosed herein. | 07-17-2014 |
20140275115 | POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 09-18-2014 |
20140303185 | NOVEL POLYMORPHS OF VILAZODONE HYDROCHLORIDE - The present invention relates to novel crystalline polymorphic forms of Vilazodone hydrochloride of formula (I). This present invention further provides the process for the preparation of novel polymorphic forms of Vilazodone hydrochloride. | 10-09-2014 |
20140323498 | SOLID STATE FORMS OF VILAZODONE AND VILAZODONE HYDROCHLORIDE - The present invention provides solid state forms of Vilazodone and Vilazodone hydrochloride, processes for preparing these solid state forms, and pharmaceutical compositions comprising one or more of these solid state forms | 10-30-2014 |
20140378472 | AMORPHOUS VILAZODONE HYDROCHLORIDE, A PROCESS FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to amorphous vilazodone hydrochloride, its process of preparation and pharmaceutical composition thereof. | 12-25-2014 |
20150018370 | Process for the preparation of form III of Vilazodone hydrochloride - The invention relates to a new solvate, Vilazodone hydrochloride monoethanol monohydrate solvate, and to a process for the preparation of polymorphic form III of Vilazodone hydrochloride via the Vilazodone hydrochloride monoethanol monohydrate solvate. | 01-15-2015 |
20150080411 | POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 03-19-2015 |
20150126525 | CRYSTALLINE FORMS OF VILAZODONE HYDROCHLORIDE AND VILAZODONE FREE BASE - Provided are crystalline and amorphous vilazodone hydrochloride. Further provided are amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carries. Also provided is a process for the preparation of form I of vilazodone free base. | 05-07-2015 |
20150126526 | CO-CRYSTAL OF AN ANTIDEPRESSANT COMPOUND - Co-crystal of a serotonin reuptake inhibitor, in stable form. | 05-07-2015 |
20160068517 | 5-BROMO-INDIRUBINS - Disclosed herein inter alia are compositions and methods for treating cancer using 5-Br-indirubin derivatives. | 03-10-2016 |
20160143906 | EFFICACIOUS TREATMENT OF NSCLC AND PREDICTIVE CLINICAL MARKER OF THE RESPONSIVENESS OF A TUMOUR TO A TREATMENT - The present invention relates to a beneficial treatment of tumours in patients suffering from NSCLC, and to a clinical marker useful as predictive variable of the responsiveness of tumours in patients suffering from NSCLC. The present invention further relates to a method for selecting patients likely to respond to a given therapy, wherein said method optionally comprises the use of a specific clinical marker. The present invention further relates to a method for delaying disease progression and/or prolonging patient survival of NSCLC patients, wherein said method comprises the use of a specific clinical marker. | 05-26-2016 |
20160250218 | PHARMACEUTICAL COMBINATION | 09-01-2016 |
20170233374 | T-TYPE CALCIUM CHANNEL MODULATOR AND USES THEREOF | 08-17-2017 |