Indole Ring System (including Hydrogenated) Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/254.09)
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Publication number: 20110294824Abstract: 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.Type: ApplicationFiled: May 4, 2011Publication date: December 1, 2011Applicant: Merck PatentgesellschaftInventors: Andreas BATHE, Bernd HELFERT, Steffen NEUENFELD, Heike KNIEL, Matthias BARTELS, Susanne RUDOLPH, Henning BÖTTCHER
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Publication number: 20110294825Abstract: 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.Type: ApplicationFiled: May 4, 2011Publication date: December 1, 2011Applicant: Merck PatentgesellschaftInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Publication number: 20110281849Abstract: The present invention relates to novel aryl indolyl sulfonamide compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them.Type: ApplicationFiled: March 3, 2009Publication date: November 17, 2011Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Rama Sastri Kambhampati, Anil Karbhari Shinde, Ishtiyaque Ahmad, Nagaraj Vishwottam Kandikere, Venkateswarlu Jasti
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Patent number: 8058269Abstract: There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.Type: GrantFiled: September 17, 2007Date of Patent: November 15, 2011Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Song Yang, Jing Zhang, Zhuming Zhang
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Patent number: 8058277Abstract: Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R1, D, E, R12, p, X1, E, G, X2 and Z are as defined in Claim 1, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolyties and/or antihypertonics. They can furthermore be employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, cerebral ischaemia, infarction or psychoses.Type: GrantFiled: October 3, 2008Date of Patent: November 15, 2011Assignee: Merck Patent GmbHInventors: Oliver Schadt, Henning Böttcher, Joachim Leibrock, Kai Schiemann, Timo Heinrich, Günter Hölzemann, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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Publication number: 20110269768Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Publication number: 20110269737Abstract: The present invention provides compounds according to general formula (I) which are proposed for the treatment of respiratory complaints, particularly asthma and COPD.Type: ApplicationFiled: August 26, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Birgit Jung, Frank Himmelsbach, Rolf Goeggel, Georg Dahmann
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Publication number: 20110263599Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.Type: ApplicationFiled: April 15, 2011Publication date: October 27, 2011Inventors: Xiaohong Song, Hong Ding, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Cheol-Min Park, Zhi-Fu Tao, Xilu Wang, Aaron R. Kunzer
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Publication number: 20110250135Abstract: The invention relates to compounds of formula I, their synthesis and their use, in particular for detecting amyloid deposits in a patient.Type: ApplicationFiled: September 4, 2009Publication date: October 13, 2011Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Heribert Schmitt-Willich, Ulrike Röhn, Matthias Friebe, Lutz Lehmann, Ansgar Fitzner, Sabine Krause, Damian Brockschnieder, Thomas Dyrks, Andrea Thiele, Ulf Bömer, Ursula Mönning, Tobias Heinrich
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Publication number: 20110251212Abstract: A compound which specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist is provided. It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein R1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is —N(R4)—C(?O)—C(?O)—, —N(R4)—(CR5R6)p—C(?O)—, —N(R4)—C(?O)—(CR7R8)q— or —C(?O)—N(R4)—(CR7R8)q—, p and q are each independently an integer of 1 to 3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or lower alkyl, A1 is benzoxazolinone or the like, and A2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 19, 2008Publication date: October 13, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Minoru Tomida, Naotake Kobayashi, Kousuke Anan, Aya Tazawa, Kayoko Hata
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Publication number: 20110212078Abstract: This invention relates to compounds of the following Formula (I); or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.Type: ApplicationFiled: June 24, 2009Publication date: September 1, 2011Inventors: Panduranga Adulla P. Reddy, Umar Faruk Mansoor, M. Arshad Siddiqui
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Patent number: 7998963Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.Type: GrantFiled: February 12, 2009Date of Patent: August 16, 2011Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20110195976Abstract: 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.Type: ApplicationFiled: September 30, 2009Publication date: August 11, 2011Applicant: Biolab Sanus Farmaceutica Ltda.Inventors: Sérgio Luiz Sacurai, Carlos Eduardo Da Costa Touzarim, Marcio Henrique Zaim
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Publication number: 20110190315Abstract: The subject invention concerns methods and compounds for inhibiting Shp2.Type: ApplicationFiled: July 21, 2009Publication date: August 4, 2011Applicant: University of South FloridaInventors: Jie Wu, Nicholas J. Lawrence, Said M. Sebti
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Publication number: 20110190317Abstract: 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.Type: ApplicationFiled: November 12, 2010Publication date: August 4, 2011Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Publication number: 20110190318Abstract: 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.Type: ApplicationFiled: June 4, 2009Publication date: August 4, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roman Messerschmid, Peter Lach, Torsten Sokoliess, Peter Stopfer, Dirk Trommeshauser
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Publication number: 20110183964Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, Y, Z, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: April 8, 2011Publication date: July 28, 2011Applicant: NOVARTIS AGInventors: Michael SHULTZ, Christine Hiu-Tung CHEN, Young Shin CHO, Lei JIANG, Jianmei FAN, Gang LIU, Dyuti MAJUMDAR, Jianke LI
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Publication number: 20110183991Abstract: The present invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, especially as agonists, identified by using a pharmacophore and a descriptor's profile filter as well as to pharmaceutical compositions comprising them. These compounds are useful in therapy in particular for the treatment and or prophylaxis of a disease in which 5-HT7 is involved, such as CNS disorders.Type: ApplicationFiled: July 31, 2009Publication date: July 28, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosalia Pascual-Ramon, Helmut H. Buschmann
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Publication number: 20110183994Abstract: 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.Type: ApplicationFiled: November 12, 2010Publication date: July 28, 2011Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Publication number: 20110178099Abstract: 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.Type: ApplicationFiled: June 4, 2009Publication date: July 21, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin Friedrich Stefanic, Frank Hilberg, Rolf Kaiser, David Shapiro
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Patent number: 7981894Abstract: 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.Type: GrantFiled: September 25, 2009Date of Patent: July 19, 2011Assignee: Merck PatentgesellschaftInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Patent number: 7981897Abstract: The present invention relates to a hitherto unknown crystal form B of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)-piperazin-1-yl]methanone, hydrochloride, to a process for the preparation thereof, and to the use thereof for the preparation of a medicament.Type: GrantFiled: September 8, 2005Date of Patent: July 19, 2011Assignee: Merck Patent GmbHInventors: Andreas Bathe, Bernd Helfert, Ralf Knierieme, Christoph Saal, Ronald Keiner
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Publication number: 20110172244Abstract: The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: February 20, 2009Publication date: July 14, 2011Applicant: IRM LLCInventors: Phillip B. Alper, Robert Epple, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
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Publication number: 20110172242Abstract: A method of treating exposure to organophosphate agents through the use of compounds comprising tetrahydroindolone and arylpiperazine moieties.Type: ApplicationFiled: October 14, 2010Publication date: July 14, 2011Inventors: David HELTON, David FICK
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Publication number: 20110172206Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: ApplicationFiled: August 8, 2009Publication date: July 14, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Donald Jeffrey Zack, Zhiyong Yang, Cynthia Berlinicke, Harry Quigley
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Publication number: 20110171289Abstract: 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.Type: ApplicationFiled: November 9, 2010Publication date: July 14, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin Friedrich STEFANIC, Frank HILBERG, Gerd MUNZERT, Flavio SOLCA, Anke BAUM, Jacobus C.A. van MEEL
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Publication number: 20110172230Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.Type: ApplicationFiled: August 22, 2007Publication date: July 14, 2011Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
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Publication number: 20110166136Abstract: Compounds of formula (1), salts and pro-drugs wherein: R1, R2, R3 and R4 are hydrogen, alkyl, hydroxyalkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, nitro, amino, monalkylamino, dialkylamino, acylamino, alkoxycarbonylamino, alkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino, aminosulphonyl or cyano, or any two of R1 to R4 that are adjacent on the ring may together represent the moiety —O—(CH2)n—O— wherein n is 1 to 3; R5 is hydrogen or alkyl; R6 is hydrogen or alkyl; and X is selected from the group consisting of: (a) groups of formula OR7 wherein R7 is hydrogen or alkyl which is optionally substituted with a substituent selected from alkylsulfonylalkyl, saturated or partially unsaturated heterocyclic, alkoxy, carboxyl, nitro, amino, monalkylamino, dialkylamino, halogen, and alkoxycarbonyl, provided that when R7 is hydrogen or ethyl, then R1, R2, R3 and R4 cannot be selected from hydrogen, halogen and alkyl; and (b) groups of formula NR8R9 wherein R8Type: ApplicationFiled: July 3, 2009Publication date: July 7, 2011Applicant: LECTUS THERAPEUTICS LIMITEDInventors: Nawaz Mohammed Khan, Svenja Burckhardt, Julie Elaine Cansfield, Ngoc-Tri Vo, Richard Edward Armer, Raymond John Boffey
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Publication number: 20110160197Abstract: The invention relates to novel substituted indoles, to the use thereof in the form of pharmacological composition substances and to use of said composition for producing medicinal preparations used for preventing and treating viral diseases, in particular caused by viruses of infectious hepatitis (HCV, HBV), human immune deficiency (HIV), atypical pneumonia (SARS) and bird flu.Type: ApplicationFiled: May 17, 2007Publication date: June 30, 2011Inventors: Andrey Alexandrovich Ivashchenko, Sergey Yevgenievich Tkachenko, Alexander Viktorovich Khvat, Oleg Dmitrievich Mitkin, Ilya Matusovich Okun, Alexandr Sergeevich Kyselvev, Volodymyr Mikhailovich Kysil, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivachtchenko
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Patent number: 7968551Abstract: Chromenoneindole derivatives of the formula (I), in which R1, R2, R3, R, A and B are as defined in Claim 1, and pharmaceutically usable prodrugs, derivatives, solvates, stereoisomers and salts thereof, exhibit particular actions on the central nervous system, in particular 5-HT reuptake-inhibiting and 5-HTx-agonistic and/or -antagonistic actions. They are distinguished by particularly high bioavailability and particularly high inhibition of 5-HT reuptake.Type: GrantFiled: March 8, 2004Date of Patent: June 28, 2011Assignee: Merck Patent GmbHInventors: Kai Schiemann, Henning Böttcher, Timo Heinrich, Günter Hölzemann, Christoph Van Amsterdam, Gerd Bartoszyk, Joachim Leibrock, Christoph Seyfried
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Publication number: 20110152172Abstract: Disclosed are methods of treating or preventing a pulmonary disease or disorder in a subject, the methods comprising administering an effective amount of an compound that inhibits Calmodulin Kinase II (CaMKII) activity, either directly or indirectly, thereby treating or preventing the pulmonary disease or disorder in the subject.Type: ApplicationFiled: June 22, 2010Publication date: June 23, 2011Applicant: UNIVERSITY OF IOWA RESEARCH FOUNDATIONInventors: Mark E. Anderson, Isabella M. Grumbach, Joel N. Kline
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Patent number: 7964601Abstract: A melanocortin receptor-specific compound of the general formula of structure I: where X, R1, R2a, R2b, R3, R4a, R4b, R5a and R5b are as defined in the specification, which compound binds with high affinity to one or more melanocortin receptors and is optionally an agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.Type: GrantFiled: June 2, 2008Date of Patent: June 21, 2011Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Ramesh Rajpurohit, Zhijun Wu, Papireddy Purma, Annette M. Shadiack, Kevin D. Burris
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Publication number: 20110144106Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1.Type: ApplicationFiled: December 3, 2010Publication date: June 16, 2011Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Hongying Yun
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Publication number: 20110144074Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: ApplicationFiled: January 24, 2011Publication date: June 16, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Publication number: 20110144090Abstract: Indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.Type: ApplicationFiled: August 10, 2010Publication date: June 16, 2011Inventors: Amy Elder, Geraldine Harriman, Silvana Leit, Jie Li, Howard Sard, Yiliang Zhang, Doug Wilson
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Patent number: 7960385Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 5, 2008Date of Patent: June 14, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110135594Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: July 14, 2009Publication date: June 9, 2011Inventors: Michael Graupe, Chandrasekar Venkataramani
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Publication number: 20110136807Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: June 29, 2007Publication date: June 9, 2011Applicant: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, JR.
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Publication number: 20110136826Abstract: 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.Type: ApplicationFiled: November 15, 2010Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HILBERG, Flavio SOLCA, Anke BAUM, Jacobus C.A. van MEEL
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Publication number: 20110136808Abstract: Indirubin derivatives of formula (I) wherein R represents -(A)n- R1 or —CO—N(R2,R3) with •A being C1-C5 alkylene group, optionally substituted by one or several A1 radical, A1 being an halogen Br, OH, OR4 or NH2, R4 being C1-C5 alkyl; —R1 being halogen, OH, N(R2, R3); R2 and R3, identical or different, being C1-C5 alkyl, optionally substituted by A1 such as above defined, or R2 and R3 are part of a cycle with 5 or 6 elements optionally comprising another heteroatom such as O or N; •n=1?5. It also relates to the biological application thereof.Type: ApplicationFiled: July 21, 2009Publication date: June 9, 2011Inventors: Laurent Meijer, Leandros Skaltsounis, Emmanuel Mikros, Prokopios Magiatis, Carl Johnson
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Publication number: 20110124657Abstract: The present invention relates to compounds having pharmacological activity towards the 5-HT7 receptor; to a method for identifying them as 5-HT7 ligands, especially as agonists, by using a pharmacophore and a descriptor's profile filter; to pharmaceutical compositions comprising them; and to their use in therapy, in particular for the treatment and or prophylaxis of a disease in which 5-HT7 is involved, such as CNS disorders.Type: ApplicationFiled: July 30, 2009Publication date: May 26, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosalia Pascual-Ramon, H. Helmut Buschmann
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Publication number: 20110124628Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: November 22, 2010Publication date: May 26, 2011Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert Mantei, Todd M. Hansen
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Publication number: 20110118280Abstract: The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: January 24, 2011Publication date: May 19, 2011Applicant: SANOFI-AVENTISInventors: Marco BARONI, Letizia PULEO
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Publication number: 20110105423Abstract: The present invention relates to compounds that modulate the replication of negative-sense, single-stranded RNA viruses, such as influenza virus, and the use of such compounds. The invention relates to methods for increasing the titer of negative-sense, single-stranded RNA viruses, such as influenza virus, in substrates for virus propagation (e.g., tissue culture). The invention also relates to the use of compounds that decrease virus replication as antiviral agents. The invention further relates to methods for identifying compounds that modulate the replication of negative-sense, single-stranded RNA viruses, in particular, influenza virus.Type: ApplicationFiled: March 6, 2009Publication date: May 5, 2011Applicant: MOUNT SINAI SCHOOL OF MEDICINE OF NEW YORK UNIVERSITYInventors: Megan L Shaw, Hans-Heinrich Hoffmann, Adolfo Garcia-Sastre, Peter Palese
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Publication number: 20110076324Abstract: The present invention includes methods for the inhibition of post-operative adhesion formation between tissue surfaces in a body cavity having been subjected to a surgical procedure, which methods involve administering a histamine H4 receptor antagonist, systemically, directly to tissue surfaces in the body cavity, or both, and to delivery vehicles and compositions suitable for use for local, non-systemic administration of a drug to the body and directly to tissue within a body cavity having been subjected to a surgical procedure.Type: ApplicationFiled: June 11, 2009Publication date: March 31, 2011Applicant: JANSSEN PHARMACEUTICA NVInventors: Robin L. Thurmond, Scott A. Wadsworth
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Patent number: 7915253Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: September 4, 2008Date of Patent: March 29, 2011Assignee: Kalypsys, IncInventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen K. Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
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Publication number: 20110071132Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.Type: ApplicationFiled: July 30, 2010Publication date: March 24, 2011Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Andrea Hager-Wernet, Wilfried Hornberger, Liliane Unger
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Patent number: 7910591Abstract: The present invention is concerned with new indol-2-one derivatives of Formula (I), which have favorable activity profile for the prophylaxis and treatment of disorders in the central nervous or in the cadiovascular system.Type: GrantFiled: May 11, 2005Date of Patent: March 22, 2011Assignee: EGIS Gyogyszergyar NYRT.Inventors: Balázs Volk, József Barkóczy, Gyula Simig, Tibor Mezei, Rita Kapillerné Dezsöfi, István Gacsályi, Katalin Pallagi, Gábor Gigler, György Lévay, Krisztina Móricz, Csilla Leveleki, Nóra Sziray, Gábor Szenasi, András Egyed, László Gábor Hársing
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Publication number: 20110065691Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.Type: ApplicationFiled: September 22, 2010Publication date: March 17, 2011Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
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Publication number: 20110065661Abstract: This application relates to methods of identifying pharmacoperone agents that can restore function to a misfolded protein, such as a misfolded protein that causes disease. Also disclosed are methods of using such pharmacoperone agents to treat a disease or disorder that results from the misfolded protein.Type: ApplicationFiled: November 24, 2010Publication date: March 17, 2011Inventor: P. MICHAEL CONN