Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/221)
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Publication number: 20140296220Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein B, R1, R2, R4, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: June 18, 2014Publication date: October 2, 2014Inventors: Gui-Dong Zhu, Jane Gong, Andrew S. Judd, Virajkumar B. Ghandi, Alexander R. Shoemaker, Thomas D. Penning, Michael R. Michaelides, Chunqiu Lai, Keith W. Woods
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Patent number: 8846662Abstract: The invention relates to a pharmaceutical composition characterized in that it comprises a benzodiazapine and/or benzodiazapine derivative, and a non-ionic solubilizer, and induces in said combination an analogous effect to an opiate, described as a Straub phenomenon.Type: GrantFiled: January 15, 2009Date of Patent: September 30, 2014Assignee: Dr. Franz Koehler Chemie GmbHInventor: Rainer Hoernecke
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Patent number: 8846660Abstract: A compound having a 7-membered nitrogen-containing ring skeleton represented by the formula (I), which is useful for the prevention or treatment of diseases, in which chymase is involved and a pharmaceutical containing the same for the prevention or treatment of a disease, in which chymase is involved.Type: GrantFiled: December 24, 2010Date of Patent: September 30, 2014Assignee: Daiichi Sankyo Company, Ltd.Inventors: Tsuyoshi Muto, Taisaku Tanaka, Junko Futamura, Seiichi Imajo, Hajime Sugawara
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Patent number: 8846664Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: November 12, 2009Date of Patent: September 30, 2014Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Wei-Sheng Huang, R. Mathew Thomas
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Patent number: 8846665Abstract: The present invention relates to a compound of formula 1 and addition salts thereof, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as neuro-muscular blocker or skeletal muscle relaxant; wherein each symbol is as defined in the Specification.Type: GrantFiled: April 11, 2012Date of Patent: September 30, 2014Assignee: King Saud UniversityInventors: Adel S. El-Azab, Hussein I. El-Subbagh, Khalid A. Al-Rashood, Kamal E. H. El-Taher, Mohamed A. Al-Omar, Ghada S. Hassan, Fatmah A. Al-Omary, Alaa A. -M. Abdelaziz, Mohamed M. Hefnawy
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Publication number: 20140288059Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.Type: ApplicationFiled: April 25, 2014Publication date: September 25, 2014Applicant: THE PENN STATE RESEARCH FOUNDATIONInventors: Gong Chen, Yanming Wang, Pingxin Li, Jing Hu, Shu Wang, Yuji Wang
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Patent number: 8841289Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by nicotinic acetylcholine receptors, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: October 11, 2010Date of Patent: September 23, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Paul David Ratcliffe, Thomas Russell Clarkson, Fiona Jeremiah, John Kinnard Ferguson MacLean
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Publication number: 20140275019Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHDInventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
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Publication number: 20140275009Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: September 18, 2014Inventors: Guy Brenchley, Jean-Damien Charrier, Chris Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Publication number: 20140256709Abstract: The present invention is directed to CNS pharmaceutical compositions and methods of use. The pharmaceutical compositions comprise a CNS active agent and preferably at least two vagal neuromodulators, one of which is a mechanoreceptor stimulator. The vagal neuromodulators are preferably in an amount sufficient to reduce a somnolence side-effect of the CNS active agent without changing its therapeutic efficacy/activity. The invention further encompasses a method of reducing CNS active agent side-effects. The method typically comprises oral administration of at least one CNS active agent to a patient at the conventionally accepted dose; and administration of at least two vagal neuromodulators to the patient so that at least one neuromodulator is administered or released from dosage form after the CNS active agent is administered and/or released.Type: ApplicationFiled: May 19, 2014Publication date: September 11, 2014Applicant: TARGIA PHARMACEUTICALSInventor: Sabina Glozman
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Publication number: 20140255344Abstract: The present invention discloses compounds of Formulae I and II, wherein the variables in Formulae I and II are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formulae I and II in the treatment of HCV infection.Type: ApplicationFiled: October 8, 2012Publication date: September 11, 2014Applicant: Hiffmann-La Roche Inc.Inventors: John A. Brinkmann, Hongju Li, Ramakanth Sarabu, Sung-Sau So
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Publication number: 20140249140Abstract: The present invention includes compositions that are useful in treating, ameliorating, or preventing nerve agent poisoning. The present invention also includes methods of preventing, treating or ameliorating nerve agent poisoning in a subject in need thereof, the method comprising administering to the subject an effective amount of a composition of the invention. The present invention also includes methods of preventing, treating or ameliorating a seizure induced by a disease or disorder in a subject in need thereof, the method comprising administering to the subject an effective amount of a composition of the invention. The present invention also comprises a kit comprising compositions of the invention.Type: ApplicationFiled: March 14, 2013Publication date: September 4, 2014Applicant: The Regents of the University of CaliforniaInventor: The Regents of the University of California
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Publication number: 20140249141Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including inflammatory diseases and diseases associated with dysfunction of the central nervous system (CNS).Type: ApplicationFiled: August 20, 2012Publication date: September 4, 2014Applicant: Targacept, Inc.Inventors: Anatoly Mazurov, Lan Miao, Todd Showalter
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Patent number: 8822454Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.Type: GrantFiled: December 9, 2013Date of Patent: September 2, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim
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Patent number: 8822453Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.Type: GrantFiled: August 20, 2010Date of Patent: September 2, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Takashi Oshiyama, Tsuyoshi Nagase, Masataka Ueda, Kuninori Tai
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Publication number: 20140242063Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.Type: ApplicationFiled: October 10, 2013Publication date: August 28, 2014Applicant: VALEANT LABORATORIES INTERNATIONAL BERMUDAInventors: Andrew John DUFFIELD, Graham JACKSON, Steven E. FRISBEE
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Publication number: 20140238412Abstract: The present invention relates to methods for treating obstructive sleep apnea (OSA), alleviating a negative OSA symptom, reducing snoring, or improving quality of life in a subject, comprising administering to the subject an effective amount of a pharmaceutical composition comprising pyridostigmine before sleep. Also provided are related medicaments as well as methods for preparing the medicaments.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Pfantastic Medical Research Institute, LLCInventor: Jian-Qiang FAN
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Patent number: 8815845Abstract: The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity.Type: GrantFiled: November 3, 2010Date of Patent: August 26, 2014Assignee: The Regents of the University of MichiganInventor: Gary D. Glick
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Publication number: 20140234443Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: March 10, 2014Publication date: August 21, 2014Applicant: Albany Molecular Research, Inc.Inventors: Peter R. GUZZO, David D. MANNING, William EARLEY
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Publication number: 20140235622Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: January 28, 2014Publication date: August 21, 2014Applicant: Arena Pharmaceuticals, Inc.Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
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Patent number: 8809323Abstract: Benzodiazepine compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of structures: wherein R1, R2, R3 and R4 are as defined. The invention also includes enantiomers, pharmaceutically acceptable salts, prodrugs or derivatives of the benzodiazepine compounds. Any one or more of these benzodiazepine compounds can be used to treat a variety of dysregulatory disorders related to cellular death. Such disorders include autoimmune disorders, inflammatory conditions, hyperproliferative conditions, viral infections, and atherosclerosis. In addition, the above compounds can be used to prepare medicaments to treat the above-described dysregulatory disorders. The benzodiazepines can also be used in drugs screening assays and other diagnostic methods.Type: GrantFiled: May 17, 2013Date of Patent: August 19, 2014Assignee: The Regents of the University of MichiganInventors: Gary D. Glick, Anthony W. Opipari, Jr.
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Patent number: 8809352Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 8, 2010Date of Patent: August 19, 2014Assignee: Novartis AGInventors: Karen Miller-Moslin, Bakary-Barry Toure, Michael Scott Visser, Naeem Yusuff
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Publication number: 20140227173Abstract: Provided are methods for treating cancer in a patient, comprising administering to a patient in need thereof a therapeutically effective regimen, the regimen comprising administering a gamma-secretase inhibitor, wherein the regimen results in a reduction in the cancer cell population in the patient. In some embodiments of the methods, the therapeutically effective regimen stabilizes, reduces or eliminates the cancer stem cell population. Also provided are compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, and X are as herein described.Type: ApplicationFiled: February 6, 2014Publication date: August 14, 2014Applicant: The Johns Hopkins UniversityInventors: Charles Eberhart, Xing Fan, Anirban Maitra
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Publication number: 20140221357Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 25, 2012Publication date: August 7, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Patent number: 8791104Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.Type: GrantFiled: May 17, 2013Date of Patent: July 29, 2014Assignee: The Regents of the University of MichiganInventor: Gary D. Glick
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Publication number: 20140206618Abstract: The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.Type: ApplicationFiled: August 16, 2012Publication date: July 24, 2014Inventors: Alexander Pasternak, Timothy Blizzard, Harry Chobanian, Reynalda de Jesus, Fa-Xiang Ding, Shuzhi Dong, Candido Gude, Dooseop Kim, Haifeng Tang, Shawn Walsh, Barbara Pio, Jinlong Jiang
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Patent number: 8785431Abstract: The present invention relates to diester prodrugs of cilazaprilate which undergo enzymatic cleavage to release the active metabolite cilazaprilate that is used for the treatment of hypertension and congestive heart failure. Furthermore the diester prodrugs of cilazaprilate possess all the properties necessary to be topically administered, preferably via transdermal therapeutic systems.Type: GrantFiled: June 20, 2012Date of Patent: July 22, 2014Assignee: Hexal AGInventors: Günther Bernhardt, Miriam Ertel, Armin Buschauer, Jörg Nink
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Publication number: 20140193347Abstract: The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.Type: ApplicationFiled: September 4, 2013Publication date: July 10, 2014Applicant: CAMURUS ABInventors: Krister THURESSON, Fredrik TIBERG, Markus JOHANSSON, Ian HARWIGSSON, Fredrik JOABSSON, Markus JOHNSSON
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Publication number: 20140186279Abstract: The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.Type: ApplicationFiled: December 23, 2013Publication date: July 3, 2014Applicant: CAMURUS ABInventors: Fredrik JOABSSON, Margareta LINDEN, Krister THURESSON, Fredrik TIBERG
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Patent number: 8759340Abstract: The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.Type: GrantFiled: June 5, 2013Date of Patent: June 24, 2014Assignee: The Regents of the University of MichiganInventor: Gary D. Glick
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Patent number: 8759402Abstract: Methods of treating or inhibiting ischemia and reperfusion injury are provided.Type: GrantFiled: November 4, 2009Date of Patent: June 24, 2014Assignee: Radical TherapeutixInventors: Roberta Gottlieb, Paul Wentworth, Eric F. Johnson, Mark J Yeager, David Granville
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Publication number: 20140170220Abstract: Multimodal particulate formulations of medicaments and methods for their use, e.g. by nasal or pulmonary administration for the treatment of various medical conditions, are provided.Type: ApplicationFiled: September 9, 2013Publication date: June 19, 2014Applicant: Hale Biopharma Ventures, LLCInventors: Steve Cartt, David Medeiros
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Publication number: 20140171423Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: December 10, 2013Publication date: June 19, 2014Applicant: ABBVIE INC.Inventors: Pramila A. Bhatia, John T. Randolph, Michael R. Schrimpf, Quinwei I. Zhang
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Publication number: 20140163000Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: June 12, 2014Inventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Patent number: 8748419Abstract: Provided are methods of treating obesity and effecting desired weight loss or preventing undesired weight gain by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The preferential muscarinic acetylcholine receptor M1 antagonist, optionally can be administered with an anti-obesity agent, for example, an anorexiant. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.Type: GrantFiled: June 14, 2007Date of Patent: June 10, 2014Assignee: Theracos, Inc.Inventors: Brian Seed, Jordan Mechanic
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Publication number: 20140155389Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.Type: ApplicationFiled: January 20, 2012Publication date: June 5, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
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Publication number: 20140155381Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.Type: ApplicationFiled: July 27, 2012Publication date: June 5, 2014Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
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Patent number: 8741889Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.Type: GrantFiled: April 19, 2012Date of Patent: June 3, 2014Assignee: Hoffmann-La Roche IncInventors: John Frederick Boylan, Leopoldo Ladores Luistro, Kathryn Elizabeth Packman
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Patent number: 8741893Abstract: The present invention relates to a compound represented by formula 1 or an addition salt thereof, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as an hypnotic agent or anesthetic agent: wherein each symbol is as defined in the Specification.Type: GrantFiled: April 4, 2012Date of Patent: June 3, 2014Assignee: King Saud UniversityInventors: Ghada S. Hassan, Hussein I. El-Subbagh, Mohamed A. Al-Omar, Kamal E. H. El-Taher, Khalid A. Al-Rashood, Abdulrahman M. Al-Obaid, Adel S. El-Azab, Alaa A.-M. Abdelaziz, Fatmah A. Al-Omary, Mohamed M. Hefnawy
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Publication number: 20140148445Abstract: In one aspect, the invention is directed to a method of identifying an individual that has amyotrophic lateral sclerosis (ALS) or is at risk of developing ALS comprising detecting one or more alterations in a profilin 1 (PFN1) sequence of an individual in need thereof compared to a wild type profilin sequence. In another aspect, the invention is directed to a method of identifying an individual that has amyotrophic lateral sclerosis (ALS) or is at risk of developing ALS comprising selectively sequencing a profilin 1 (PFN1) sequence of an individual in need thereof; and detecting one or more alterations in the PFN1 sequence of the individual. If the one or more alterations are detected then the individual has ALS.Type: ApplicationFiled: March 15, 2013Publication date: May 29, 2014Applicant: THE UNIVERSITY OF MASSACHUSETTSInventors: John E. Landers, Robert H. Brown
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Publication number: 20140147477Abstract: The present invention relates to diester prodrugs of cilazaprilate which undergo enzymatic cleavage to release the active metabolite cilazaprilate that is used for the treatment of hypertension and congestive heart failure. Furthermore the diester prodrugs of cilazaprilate possess all the properties necessary to be topically administered, preferably via transdermal therapeutic systems.Type: ApplicationFiled: June 20, 2012Publication date: May 29, 2014Applicant: HEXAL AGInventors: Günther Bernhardt, Miriam Ertel, Armin Buschauer, Jörg Nink
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Publication number: 20140148433Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: August 31, 2011Publication date: May 29, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
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Publication number: 20140140982Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.Type: ApplicationFiled: November 21, 2013Publication date: May 22, 2014Applicant: ACADIA PHARMACEUTICALS INC.Inventors: David M. Weiner, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam
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Publication number: 20140141089Abstract: The disclosure is directed to a nanoparticle comprising a porous framework core including a porous framework material and a compound, and a lipid layer disposed on the surface of the porous framework core.Type: ApplicationFiled: February 11, 2010Publication date: May 22, 2014Applicant: Colorado School of MinesInventor: Hongjun Liang
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Patent number: 8729070Abstract: The present invention is directed to CNS pharmaceutical compositions and methods of use. The pharmaceutical compositions comprise a CNS active agent and preferably at least two vagal neuromodulators, one of which is a mechanoreceptor stimulator. The vagal neuromodulators are preferably in an amount sufficient to reduce a somnolence side-effect of the CNS active agent without changing its therapeutic efficacy/activity. The invention further encompasses a method of reducing CNS active agent side-effects. The method typically comprises oral administration of at least one CNS active agent to a patient at the conventionally accepted dose; and administration of at least two vagal neuromodulators to the patient so that at least one neuromodulator is administered or released from dosage form after the CNS active agent is administered and/or released.Type: GrantFiled: August 20, 2010Date of Patent: May 20, 2014Assignee: Targia PharmaceuticalsInventor: Sabina Glozman
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Publication number: 20140135318Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: May 23, 2012Publication date: May 15, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Zhen-Wei Cai, Andrew J. Tebben, Heidi L. Perez, Liping Zhang, Gretchen M. Schroeder, Donna D. Wei
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Publication number: 20140135317Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: September 26, 2013Publication date: May 15, 2014Applicant: Gilead Sciences, Inc.Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Rubin Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20140135315Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: April 9, 2013Publication date: May 15, 2014Applicant: KuDOS Pharmaceuticals LimitedInventor: KuDOS Pharmaceuticals Limited
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Publication number: 20140134256Abstract: Provided are microparticles of active pharmaceutical ingredients, drug delivery vehicles comprising same, and methods for making them.Type: ApplicationFiled: January 16, 2014Publication date: May 15, 2014Inventors: E. Itzhak LERNER, Vered ROSENBERGER, Moshe FLASHNER-BARAK, Anna DRABKIN, Naomi MOLDAVSKI
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Patent number: 8722667Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.Type: GrantFiled: December 17, 2012Date of Patent: May 13, 2014Assignee: The Regents of the University of MichiganInventors: Gary D. Glick, Anthony W. Opipari