Chalcogen Bonded Directly To Carbon Of The Hetero Ring Of The Quinoline Ring System Patents (Class 514/253.07)
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Patent number: 8653069Abstract: The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.Type: GrantFiled: July 28, 2008Date of Patent: February 18, 2014Assignee: Jiangsu Hengyi Pharmaceutical Co., Ltd.Inventors: Jianqi Li, Shaoping Peng, Wangping Cai, Kai Gao
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Publication number: 20140044786Abstract: An orally deliverable pharmaceutical composition provides controlled release of aripiprazole. The composition includes a therapeutically effective amount of aripiprazole and at least one pharmaceutically acceptable excipient. The compositions of the invention may exhibit one or more of the release profiles defined in the specification.Type: ApplicationFiled: October 14, 2013Publication date: February 13, 2014Applicant: ZYSIS LIMITEDInventors: Ian WILDING, Russell PENDLETON
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Patent number: 8642600Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: GrantFiled: July 19, 2011Date of Patent: February 4, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Publication number: 20140031363Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3-R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.Type: ApplicationFiled: April 15, 2013Publication date: January 30, 2014Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Scott Myers, Yesim Altas Tahirovic
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Publication number: 20140024638Abstract: The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions, and methods for treating schizophrenia.Type: ApplicationFiled: January 17, 2012Publication date: January 23, 2014Applicant: TARGACEPT, INC.Inventors: Merouane Bencherif, Geoffrey C. Dunbar, David A. Hosford, Gregory J. Gatto, Terry Hauser, Kristen G. Jordan, Anthony Carl Segreti
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Publication number: 20140018349Abstract: This invention provides an oral dosage regimen for the treatment of depression, a pharmaceutically acceptable medication dispensing package containing multiple dosage units of medicaments comprising an oral dosage regimen of D-cycloserine for the treatment of depression, a pharmaceutical composition comprising D-cycloserine formulated for oral administration providing a dosage of 1000 mg/day alone or in combination with antidepressant agents and uses thereof.Type: ApplicationFiled: January 30, 2012Publication date: January 16, 2014Inventors: Uriel Heresco-Levy, Daniel Javitt
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Publication number: 20140018365Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 26, 2011Publication date: January 16, 2014Applicants: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCCHAFTEN E.V., LEAD DISCOVERY CENTER GMBHInventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
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Publication number: 20140018369Abstract: A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.Type: ApplicationFiled: September 19, 2013Publication date: January 16, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Janusz KOSTANSKI, Takakuni MATSUDA, Manoj NERURKAR, Vijay H. NARINGREKAR
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Patent number: 8623874Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: GrantFiled: August 29, 2008Date of Patent: January 7, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Patent number: 8618109Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: November 28, 2012Date of Patent: December 31, 2013Assignee: Otsuka Parmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Hideaki Kuroda, Haruka Takahashi, Satoshi Shimizu, Tatsuyoshi Tanaka
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Publication number: 20130345234Abstract: The present invention describes methods for diagnosing, treating and determining the prognosis of breast cancer HR+ patient, the methods including detecting the amplification of one or more biomarkers comprising a FGFR ligand such as FGF3, FGF4, FGF19, and/or a FGFR, such as for example FGFR1 in a subject; determining an FGFR1 inhibitor for treating the subject based on the amplification of the one or more biomarkers in the subject; administering to the subject in need thereof the FGFR1 inhibitor and using the one or more biomarkers to indicate prognosis of the subject treated with the FGFR1 inhibitor.Type: ApplicationFiled: March 15, 2012Publication date: December 26, 2013Inventors: Humphrey Athelstan Roy Gardner, Michael Shi, Alejandro Yovine
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Publication number: 20130344146Abstract: The invention encompasses dry compression pharmaceutical compositions of aripiprazole, methods of making tablets from the compositions, and tablets of the dry compression pharmaceutical composition.Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Julia HRAKOVSKY, Ruth TENENGAUZER
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Patent number: 8614216Abstract: The present invention relates to non-hydrate crystalline forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts, solid pharmaceutical formulations containing the same and methods of use. The present invention also relates to crystalline hydrates of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-l-yl)-lH-benzimidazol-2-yl]-lH-quinolin-2-one lactic acid salts, pharmaceutical formulations containing the same and methods of use related thereto. The present invention further relates to crystalline solvates of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-l-yl)-lH-benzimidazol-2-yl]-lH-quinolin-2-one lactic acid salts.Type: GrantFiled: April 27, 2012Date of Patent: December 24, 2013Assignee: Novartis AGInventors: Augustus O Okhamafe, Joyce Chou, Rampurna Gullapalli, Eric Harwood, David Ryckman, Shuguang Zhu, Xiao Shang
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Pharmaceutically Acceptable Salts of Quinolinone Compounds Having Improved Pharmaceutical Properties
Publication number: 20130338171Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined hereinType: ApplicationFiled: August 1, 2013Publication date: December 19, 2013Applicant: Novartis AGInventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus Okhamafe, Marc S. Tesconi -
Patent number: 8604041Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: GrantFiled: August 2, 2011Date of Patent: December 10, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Patent number: 8604040Abstract: Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y1, Y2, Y3, L1, L2, RG, and R1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: GrantFiled: May 26, 2011Date of Patent: December 10, 2013Assignee: Bayer CropScience AGInventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Nicola Rahn, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
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Patent number: 8598178Abstract: A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.Type: GrantFiled: October 31, 2007Date of Patent: December 3, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Janusz W. Kostanski, Takakuni Matsuda, Manoj Nerurkar, Vijay H. Naringrekar
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Patent number: 8592427Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.Type: GrantFiled: June 24, 2011Date of Patent: November 26, 2013Assignee: Alkermes Pharma Ireland LimitedInventors: Laura Cook Blumberg, Julius F. Remenar, Örn Almarsson, Tarek A. Zeidan
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Publication number: 20130302384Abstract: The present invention provides a medical device containing a cake composition comprising aripiprazole as an active ingredient and capable of suppressing agglomeration of aripiprazole in a suspension obtained by resuspending a freeze-dried substance; and a cake composition comprising aripiprazole as an active ingredient. The present invention relates to a medical device containing, in a storage container whose inner wall is treated with silicone, a freeze-dried cake composition comprising separately prepared aripiprazole as an active ingredient, wherein there is a space between the inner wall and the cake composition; and a cake composition comprising aripiprazole as an active ingredient and having a strength of 5 to 100 N.Type: ApplicationFiled: January 17, 2012Publication date: November 14, 2013Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Shogo Hiraoka, Kiyoshi Taniguchi
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Patent number: 8580796Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.Type: GrantFiled: January 13, 2012Date of Patent: November 12, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
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Publication number: 20130296336Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: SHAUN JORDAN, TETSURO KIKUCHI, KATSURA TOTTORI, TSUYOSHI HIROSE, YASAFUMI UWAHODO
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Publication number: 20130296337Abstract: There is provided granules for the production of flash-melt pharmaceutical oral dosage forms. In addition to one or more medicaments, the granules are composed of an excipient combination consisting of a superdisintegrant, a dispersing agent, a distributing agent, and a binder and may also include other conventional ingredients such as sweetening and flavoring agents. The subject granules are advantageous in that they are stable and can be prepared without the aid of solvents and without the need for special environments or handling. Dosage forms, especially tablets, prepared therefrom on conventional equipment disintegrate in the mouth in under about twenty five seconds.Type: ApplicationFiled: July 10, 2013Publication date: November 7, 2013Inventors: Sanjeev H. Kothari, Divyakant S. Desai
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Patent number: 8575172Abstract: An orally deliverable pharmaceutical composition provides controlled release of aripiprazole. The composition includes a therapeutically effective amount of aripiprazole and at least one pharmaceutically acceptable excipient. The compositions of the invention may exhibit one or more of the release profiles defined in the specification.Type: GrantFiled: September 26, 2007Date of Patent: November 5, 2013Assignee: Zysis LimitedInventors: Ian Wilding, Russell Pendleton
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Publication number: 20130281436Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.Type: ApplicationFiled: June 24, 2013Publication date: October 24, 2013Inventors: Morten JORGENSEN, Peter Hongaard ANDERSEN, Klaus Gjervig JENSEN, Mette Graulund HVENEGAARD, Lassina BADOLO, Mikkel Fog JACOBSEN
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Patent number: 8563556Abstract: Crystalline forms or polymorphs of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one lactic acid salts, as well as to methods of making the same, pharmaceutical compositions comprising the same and methods of treatment using the same.Type: GrantFiled: March 18, 2009Date of Patent: October 22, 2013Assignee: Novartis AGInventors: Danielle Giron, Walter Hammerschmidt, Philippe Piechon, Johanne Polasek, Andreas Schreiner, Frank Stowasser
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Publication number: 20130267504Abstract: The present invention relates to a pharmaceutical composition comprising glycerol esters of a fatty acid, wherein the compositions are useful for the delivery of anti-psychotic drugs.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. PERRY, Magali B. HICKEY, Julius F. REMENAR, Jennifer VANDIVER
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Publication number: 20130267503Abstract: The present invention relates to an injectable, pharmaceutical composition comprising a C1-6 alkyl ester of a C10-20 fatty acid. In an embodiment, the fatty acid is ethyl oleate, isopropyl oleate, ethyl myristate, or isopropyl myristate. These compositions are useful for the delivery of anti-psychotic drugs.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. PERRY, Magali B. HICKEY, Julius F. REMENAR, Jennifer VANDIVER
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Publication number: 20130267536Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.Type: ApplicationFiled: December 13, 2011Publication date: October 10, 2013Applicant: ALLA CHEM, LLCInventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Publication number: 20130267505Abstract: The present invention relates to a pharmaceutical composition comprising benzyl alcohol and polyoxyethylene derivatives of sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. PERRY, Magali B. HICKEY, Julius F. REMENAR, Jennifer VANDIVER
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Publication number: 20130251702Abstract: Methods for screening compounds for treating sepsis are disclosed. The present methods and compositions are targeting NOD2 mediated signaling pathway and the agents identified by the present methods are qualified as drug candidates for clinical development. Further Methods and composition for treating sepsis are disclosed.Type: ApplicationFiled: March 21, 2013Publication date: September 26, 2013Applicant: SNU R&DB FOUNDATIONInventors: Doo Hyun CHUNG, Sae Jin OH, Ji Hyung KIM
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Patent number: 8541573Abstract: Substituted sulfonamide compounds corresponding to the formula I processes for the preparation thereof, pharmaceutical compositions containing these compounds and the use of substituted sulfonamide compounds for the preparation of pharmaceutical compositions for treating pain and other conditions at least partly mediated via the bradykinin 1 receptor.Type: GrantFiled: March 4, 2009Date of Patent: September 24, 2013Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Ruth Jostock, Klaus Schiene, Jean De Vry, Tieno Germann, Sabine Hees, Stefan Schunk, Melanie Reich
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Publication number: 20130245037Abstract: The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided.Type: ApplicationFiled: May 17, 2013Publication date: September 19, 2013Applicant: FibroGen, Inc.Inventors: Volkmar Guenzler-Pukall, Thomas B. Neff, Qingjian Wang, Michael P. Arend, Lee A. Flippin, Alex Melekhov
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Publication number: 20130245004Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.Type: ApplicationFiled: May 9, 2013Publication date: September 19, 2013Applicant: Synchroneuron Inc.Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong
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Publication number: 20130237528Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.Type: ApplicationFiled: April 25, 2013Publication date: September 12, 2013Applicant: Janssen Pharmaceutica, NVInventors: Dominique Jean-Pierre Mabire, Jerome Emile Georges Guillemont, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20130237546Abstract: The present invention provides a method for determining a response of a mammalian subject having melanoma tumor cells to treatment with a melanoma inhibitory agent. In one aspect, the method comprises (a) determining a first concentration of melanoma inhibitory activity protein (MIA) in a first biological sample taken from the mammalian subject before treatment with the melanoma inhibitory agent; (b) determining a second concentration of MIA in a second biological sample from the mammalian subject taken after treatment with the melanoma, inhibitory agent; and (c) comparing the first and second concentrations of MIA, wherein a decrease in the second concentration of MIA measured in the second biological sample as compared to the first concentration of MIA measured in the first biological sample indicates a positive response to the treatment with the melanoma inhibitory agent.Type: ApplicationFiled: October 4, 2012Publication date: September 12, 2013Applicant: Novartis AGInventors: Nguyen Tan, Eleni Venetsanakos, Michel Faure, Carla Heise
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Publication number: 20130236573Abstract: The present invention is directed to methods for the treatment of treatment-refractory depression or treatment-resistant depression comprising administering to a patient in need thereof, a therapeutically effective amount of esketamine as mono-therapy or as combination therapy with at least on antidepressant.Type: ApplicationFiled: March 12, 2013Publication date: September 12, 2013Inventors: Jaskaran Singh, Ivo Caers
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Patent number: 8518421Abstract: There is provided granules for the production of flash-melt pharmaceutical oral dosage forms. In addition to one or more medicaments, the granules are composed of an excipient combination consisting of a superdisintegrant, a dispersing agent, a distributing agent, and a binder and may also include other conventional ingredients such as sweetening and flavoring agents. The subject granules are advantageous in that they are stable and can be prepared without the aid of solvents and without the need for special environments or handling. Dosage forms, especially tablets, prepared therefrom on conventional equipment disintegrate in the mouth in under about twenty five seconds.Type: GrantFiled: May 16, 2011Date of Patent: August 27, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Sanjeev H. Kothari, Divyakant S. Desai
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Publication number: 20130217678Abstract: The present invention provides a pharmaceutical agent that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the pharmaceutical agent of the invention comprising as an active ingredient a quinolone compound represented by Formula (1): or a salt thereof, wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydroxy or the like.Type: ApplicationFiled: March 28, 2013Publication date: August 22, 2013Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventor: OTSUKA PHARMACEUTICAL CO., LTD.
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Publication number: 20130209552Abstract: The present invention discloses compositions of liquid and gel formulation containing aripiprazole in the form of a patch for transdermal delivery.Type: ApplicationFiled: October 20, 2011Publication date: August 15, 2013Applicant: TRANSDERMAL RESEARCH PHARM LABORATORIES, LLCInventors: Fotios M. Plakogiannis, Muhammed Anwar Hossain
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APPLICATION OF 5-HT6 RECEPTOR ANTAGONISTS FOR THE ALLEVIATION OF COGNITIVE DEFICITS OF DOWN SYNDROME
Publication number: 20130210829Abstract: Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT6) receptor antagonists are provided for improving the cognition of a Down syndrome patient.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Inventor: THE UNIVERSITY OF UTAH RESEARCH FOUNDATION -
Publication number: 20130203768Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: September 28, 2011Publication date: August 8, 2013Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
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Publication number: 20130203766Abstract: The invention relates to new pharmaceutical compositions for the treatment of sexual disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment of sexual disorders and methods for the preparation thereof.Type: ApplicationFiled: October 18, 2012Publication date: August 8, 2013Applicant: SPROUT PHARMACEUTICALS, INC.Inventor: Sprout Pharmaceuticals, Inc.
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Patent number: 8501742Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: GrantFiled: August 2, 2011Date of Patent: August 6, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Patent number: 8481546Abstract: The disclosure generally relates to the compound of formula I, (R)—N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide, including pharmaceutically acceptable salts, which is a CGRP-receptor antagonist. The disclosure also relates to pharmaceutical compositions and methods for using the compound in the treatment of CGRP related disorders including migraine headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and cancer.Type: GrantFiled: March 2, 2011Date of Patent: July 9, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Gene M. Dubowchik, John E. Macor
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Publication number: 20130171237Abstract: The present invention discloses compositions of liquid and gel formulation containing aripiprazole in the form of a patch for transdermal delivery.Type: ApplicationFiled: November 5, 2012Publication date: July 4, 2013Inventors: Fotios M. Plakogiannis, Anwar Muhammed Hossain
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Publication number: 20130158044Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: November 28, 2012Publication date: June 20, 2013Applicant: Otsuka Pharmaceutical Co., Ltd.Inventor: Otsuka Pharmaceutical Co., Ltd.
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Publication number: 20130143867Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.Type: ApplicationFiled: January 18, 2013Publication date: June 6, 2013Applicant: SYCHRONEURON INC.Inventor: SYCHRONEURON INC.
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Publication number: 20130123272Abstract: The use of 4-amino-5-fluoro-3[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one or a pharmaceutically acceptable salt or a tautomer thereof, or a hydrate or a solvate for the manufacture of pharmaceutical compositions for use in the treatment of hepatocellular carcinoma or liver cancer.Type: ApplicationFiled: April 14, 2011Publication date: May 16, 2013Applicant: Novartis AGInventors: Diana Graus Porta, Herbert Schmid, Michael Shi
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Publication number: 20130123238Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.Type: ApplicationFiled: July 13, 2012Publication date: May 16, 2013Inventors: Anthony Alexander McKinney, Frank Bymaster
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Publication number: 20130123344Abstract: Disclosed are compounds and pharmaceutical compositions containing compounds that inhibit JMJD2 proteins, including those of the formula (I): wherein R1, R2, R3, R4, and R5 are as defined herein or pharmaceutically acceptable salts thereof. Also disclosed is a method of preventing or treating a viral infection of a host, comprising administering to the host an effective amount of an inhibitor of the JMJD2 family of histone demethylases, for example, a compound of the formula (I). The viral infection may be a primary infection, reactivation of a virus after latency in a host, or may be in a mammal that has undergone, is undergoing, or will undergo immunosuppressive therapy.Type: ApplicationFiled: January 22, 2013Publication date: May 16, 2013Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventor: The United States of America, as Represented by the Secretary, Department of Health and Human Services