Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/221)
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Publication number: 20140128378Abstract: The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus.Type: ApplicationFiled: January 14, 2014Publication date: May 8, 2014Applicant: UCB Pharma GmbHInventor: Thomas STÖHR
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Publication number: 20140128379Abstract: The present invention provides pharmaceutical compositions for intranasal delivery of a benzodiazepine. The composition may contain a therapeutically effective amount of a benzodiazepine or a pharmaceutically acceptable salt thereof, and a permeation enhancer. The permeation enhancer may be propylene glycol or a Hsieh permeation enhancer. The present compositions have excellent bioavailability. After administration of the present compositions, therapeutically effective plasma levels of the benzodiazepine may be achieved rapidly. The present pharmaceutical composition may be used to treat a patient suffering from anxiety, epilepsy, insomnia, agitation, seizures, muscular disorders, alcohol dependence, and drug withdrawal.Type: ApplicationFiled: March 29, 2012Publication date: May 8, 2014Applicant: CPEX Pharmaceuticals, Inc.Inventors: Nils Bergenhem, Carl Reppucci, Zhengmao Li
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Publication number: 20140128381Abstract: The present invention generally relates to intranasal pharmaceutical compositions comprising a benzodiazepine and methods of use thereof that can provide a therapeutic effect without a decrease in blood pressure and/or pulse after administration of the pharmaceutical composition.Type: ApplicationFiled: January 14, 2014Publication date: May 8, 2014Inventors: Gary Bream, Moise A. Khayrallah, Myoung-Ki Baek, Jae-Hoon Jo, Hye-Jin Chang
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Publication number: 20140128377Abstract: The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus.Type: ApplicationFiled: January 14, 2014Publication date: May 8, 2014Applicant: UCB Pharma GmbHInventor: Thomas STÖHR
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Publication number: 20140128380Abstract: The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: Mimetica Pty LtdInventors: Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
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Patent number: 8716492Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: December 15, 2011Date of Patent: May 6, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
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Patent number: 8716279Abstract: The present invention includes benzodiazepine compositions formulated for intranasal administration, comprising a binary solvent system comprising a first solvent in which the benzodiazepine is soluble, the first solvent capable of penetrating nasal mucosal tissue, and a second solvent in which the benzodiazepine in less soluble. The compositions of the present invention may be used to treat a variety of disorders including, but not limited to, panic attacks, muscle spasms, anxiety, and seizures. In one aspect, the present invention relates to a fast-acting, clonazepam composition for transnasal administration that can be used for the treatment of seizure clusters.Type: GrantFiled: August 27, 2007Date of Patent: May 6, 2014Assignee: Jazz Pharmaceuticals, Inc.Inventors: Gene Jamieson, Michael Des Jardin, Clark Allphin, Sigridur Olafsdottir
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Publication number: 20140120185Abstract: The present invention provides a medicament having a wider treatment spectrum, causing a fewer side effects and superior in tolerability and safety, as compared to known typical antipsychotic agents and atypical antipsychotic agents. The present invention related to a medicament containing (I) a compound which is 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, and (II) at least one drug selected from the group consisting of a mood stabilizer, a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a serotonin and norepinephrine reuptake inhibitor, a noradrenergic and specific serotonergic antidepressant, an antianxiety drug, a tricyclic antidepressant, a tetracyclic antidepressant, an antipsychotic drug and an anti-ADHD drug, in combination.Type: ApplicationFiled: April 4, 2012Publication date: May 1, 2014Inventors: Tsuyoshi Hirose, Kenji Maeda, Tetsuro Kikuchi, Masafumi Toda
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Publication number: 20140107106Abstract: In part, the present invention is directed to antibacterial compounds.Type: ApplicationFiled: April 25, 2013Publication date: April 17, 2014Applicant: Affinium Pharmaceuticals, Inc.Inventor: Affinium Pharmaceuticals, Inc.
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Publication number: 20140105852Abstract: A process for making cross-linked polysaccharide gels, particularly cross-linked hyaluronic acid gels, under basic conditions. The resulting gels possess improved degradation characteristics, and are useful in a variety of medical and cosmetic applications.Type: ApplicationFiled: December 26, 2013Publication date: April 17, 2014Applicant: Ultraceuticals R&D Pty. LimitedInventors: Simone Charlotte Vonwiller, Geoffrey Kenneth Heber
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Patent number: 8697673Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: March 29, 2012Date of Patent: April 15, 2014Assignee: Pfizer Inc.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
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Publication number: 20140093559Abstract: A solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.Type: ApplicationFiled: November 1, 2013Publication date: April 3, 2014Applicant: GRUNENTHAL GMBHInventors: JOHANNES BARTHOLOMAEUS, HEINRICH KUGELMANN
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Patent number: 8685962Abstract: Articles of manufacturing (such as tobacco products), methods, devices and compositions for preventing or reducing tobacco-associated damage and/or disorders associated with oxidative stress in a subject, and which utilize a TSPO receptor ligand (such as diazepam), are disclosed.Type: GrantFiled: July 2, 2008Date of Patent: April 1, 2014Assignee: Technion Research & Development Foundation LimitedInventors: Moshe Gavish, Rafael M. Nagler
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Patent number: 8685451Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.Type: GrantFiled: June 18, 2008Date of Patent: April 1, 2014Assignee: Osmotica Kereskedelmi és Szolgáltató KFTInventors: Fernando G. Toneguzzo, Glenn A. Meyer, Marcelo A. Ricci, Marcelo A. Coppari, Ana C. Pastini, Gustavo A. Fischbein
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Publication number: 20140087992Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. 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; or as prodrugs of such compounds.Type: ApplicationFiled: September 20, 2013Publication date: March 27, 2014Inventors: Ashvinikumar V. Gavai, George V. DeLucca, Daniel O'Malley, Patrice Gill, Claude A. Quesnelle, Brian E. Fink, Yufen Zhao, Francis Y. Lee
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Publication number: 20140088085Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.Type: ApplicationFiled: January 12, 2012Publication date: March 27, 2014Applicants: ARRAY BIOPHARMA, INC, VENTIRX PHARMACEUTICALS, INCInventors: Laurence E. Burgess, George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones, James Jeffry Howbert, Robert Hershberg, Joseph P. Lyssikatos, Hong Woon Yang
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Publication number: 20140088091Abstract: The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as neuromuscular blocker or skeletal muscle relaxant.Type: ApplicationFiled: April 11, 2012Publication date: March 27, 2014Applicant: 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: 20140088090Abstract: The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as hypnotic agent or anesthetic agent.Type: ApplicationFiled: April 4, 2012Publication date: March 27, 2014Applicant: 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: 20140079812Abstract: Compositions and methods for the treatment of cancer are provided.Type: ApplicationFiled: November 19, 2013Publication date: March 20, 2014Applicant: Lankenau Institute for Medical ResearchInventors: Iraimoudi S. Ayene, George C. Prendergast
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Publication number: 20140080780Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.Type: ApplicationFiled: May 21, 2012Publication date: March 20, 2014Inventor: Benjamin WOLOZIN
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Publication number: 20140079666Abstract: In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: May 5, 2012Publication date: March 20, 2014Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITALInventors: Thomas R. Webb, Vincent A. Boyd
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Patent number: 8673897Abstract: The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone compounds and pharmaceutical compositions are contemplated to be useful for treating rheumatoid arthritis, graft-versus-host disease, inflammatory bowel disease, and the like.Type: GrantFiled: September 17, 2010Date of Patent: March 18, 2014Assignee: The Regents of the University of MichiganInventors: Gary D. Glick, Alexander Ross Hurd, Chad Alan Van Huis
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Patent number: 8673898Abstract: Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.Type: GrantFiled: April 12, 2012Date of Patent: March 18, 2014Assignee: Array BioPharma Inc.Inventors: George A. Doherty, Zachary Jones
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Publication number: 20140073633Abstract: The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.Type: ApplicationFiled: November 19, 2013Publication date: March 13, 2014Applicants: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENE ALT., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIEInventors: Daniel GILLET, Julien BARBIER, Ludger JOHANNES, Bahne STECHMANN, Siau-Kun BAI
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Publication number: 20140072623Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.Type: ApplicationFiled: November 8, 2013Publication date: March 13, 2014Applicant: DEPOMED, INC.Inventors: Bret Berner, Sui Yuen Eddie Hou
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Publication number: 20140072536Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.Type: ApplicationFiled: March 15, 2013Publication date: March 13, 2014Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of NevadaInventors: Ryan Wuebbles, Dean Burkin
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Publication number: 20140073574Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: November 13, 2013Publication date: March 13, 2014Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Publication number: 20140066436Abstract: The present invention relates to a compound of formula (VII)I, or pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N—(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4? are each independently H or alkyl; or R4 and R4? together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.Type: ApplicationFiled: June 5, 2013Publication date: March 6, 2014Inventors: Jonathan James HOLLICK, Stuart Donald JONES, Claire June FLYNN, Michael George THOMAS
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Patent number: 8664217Abstract: The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; Al is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.Type: GrantFiled: August 22, 2012Date of Patent: March 4, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Kunio Oshima, Takashi Oshiyama, Shinichi Taira, Yasuhiro Menjo, Hokuto Yamabe, Shuuji Matsumura, Masataka Ueda, Yasuo Koga, Kuninori Tai, Sunao Nakayama, Toshiyuki Onogawa, Kenji Tsujimae
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Publication number: 20140057903Abstract: This invention provides methods for identifying genes associated with cognitive impairment and for identifying compounds useful in the treatment of cognitive impairment. The methods can in particular be used to identify genes associated with, and compounds useful in treating, cognitive impairment in aging.Type: ApplicationFiled: July 10, 2013Publication date: February 27, 2014Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Michela Gallagher, Rebecca Haberman
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Publication number: 20140050789Abstract: Provided are compositions comprising a benzodiazepine and a neurosteroid, containing one or both of the benzodiazepine and the neurosteroid in a subtherapeutic dose, and administration of such compositions for mitigation of an epileptic seizure. Further provided are compositions comprising a benzodiazepine, a neurosteroid, and an NMDA blocker, and administration of such compositions for mitigation of an epileptic seizure.Type: ApplicationFiled: August 12, 2013Publication date: February 20, 2014Applicant: The Regents of the University of CaliforniaInventors: Michael A. ROGAWSKI, Isaac N. PESSAH, Zhengyu CAO, Pamela J. LEIN
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Publication number: 20140051681Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: ApplicationFiled: May 3, 2013Publication date: February 20, 2014Inventors: David John AUGERI, Jeffrey Thomas BAGDANOFF, Simon David Peter BAUGH, Marianne CARLSEN, Kenneth Gordon CARSON, John Anthony GILLERAN, Wei HE, Tamas ORAVECZ, Konstantin SALOJIN, Leonard SUNG
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Publication number: 20140050797Abstract: The present invention is directed to pharmaceutical compositions and dosage forms comprising TPR beads, wherein said TPR beads comprise a solid dispersion of at least one active pharmaceutical ingredient in at least one solubility-enhancing polymer, and a TPR coating comprising a water insoluble polymer and an enteric polymer, wherein the active pharmaceutical ingredient comprises a weakly basic active pharmaceutical ingredient having a solubility of not more than 100 ?g/mL at pH 6.8.Type: ApplicationFiled: June 6, 2013Publication date: February 20, 2014Inventors: Gopi VENKATESH, Luigi BOLTRI, Italo COLOMBO, Jin-Wang LAI, Flavio FABIANI, Luigi MAPELLI
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Publication number: 20140051690Abstract: There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anticonvulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant.Type: ApplicationFiled: October 23, 2013Publication date: February 20, 2014Applicant: SK Biopharmaceuticals Co., Ltd.Inventors: Myoung-Ki Baek, Jae-Hoon Jo, Hye-Jin Chang
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Publication number: 20140051679Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: October 12, 2012Publication date: February 20, 2014Applicant: UNIVERISTY HEALTH NETWORKSInventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey
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Publication number: 20140038935Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: January 21, 2013Publication date: February 6, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20140038947Abstract: 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: ApplicationFiled: May 17, 2013Publication date: February 6, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Gary D. Glick, Anthony W. Opipari, JR.
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Publication number: 20140031334Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. 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: September 20, 2013Publication date: January 30, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
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Publication number: 20140030249Abstract: 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: September 27, 2013Publication date: January 30, 2014Applicant: Valeant International BermudaInventors: Andrew John DUFFIELD, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
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Patent number: 8637502Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.Type: GrantFiled: January 12, 2012Date of Patent: January 28, 2014Assignees: Purde Pharma L.P., Shionogi & Co., Ltd.Inventors: Kevin C. Brown, R. Richard Goehring
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Publication number: 20140024641Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.Type: ApplicationFiled: January 7, 2013Publication date: January 23, 2014Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
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Publication number: 20140018352Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: April 26, 2013Publication date: January 16, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francoise Pierard, Jean-Damien Charrier
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Patent number: 8629136Abstract: 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: March 22, 2012Date of Patent: January 14, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim, Francis Y. Lee
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Patent number: 8629137Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: October 2, 2012Date of Patent: January 14, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
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Publication number: 20140011772Abstract: The present invention relates to compositions and methods for the treating and empirically investigating conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity). In particular, the present invention provides compositions and methods for using flufenamic acid in the treatment and empirical investigation of conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity).Type: ApplicationFiled: June 13, 2013Publication date: January 9, 2014Applicant: NORTHWESTERN UNIVERSITYInventors: Marco Martina, A. Vania Apkarian
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Publication number: 20140011770Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: September 10, 2013Publication date: January 9, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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Patent number: 8623857Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.Type: GrantFiled: May 24, 2011Date of Patent: January 7, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
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Publication number: 20140005135Abstract: Disclosed is a stable liquid formulation for parenteral injection comprising a biocompatible non-aqueous solvent and a small molecule drug, or a salt thereof, solubilized within the non-aqueous solvent, wherein the liquid formulation comprises less than 10% by weight residual water, and wherein the volume of the liquid formulation to be parenterally injected is from 0.1 ?l to 3 ml.Type: ApplicationFiled: March 14, 2013Publication date: January 2, 2014Applicant: XERIS PHARMACEUTICALS, INC.Inventors: Steven J. Prestrelski, Nancy Scott
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Publication number: 20140005173Abstract: Compositions and methods for treating psychotic and neurological disorders in a subject are disclosed. The compositions and methods utilize a pharmaceutical compound that reverses or negates the effects of an NMDA receptor antagonist. The compositions and methods are effective in reducing at least catatonic features in the subject.Type: ApplicationFiled: March 20, 2012Publication date: January 2, 2014Inventor: James Conour
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Publication number: 20140004082Abstract: A method for treating core binding factor (CBF) leukemia in a subject, comprising administering to a subject having CBF leukemia a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or ester thereof, that inhibits CBF? and RUNX1 binding in the subject, thereby treating the CBF leukemia.Type: ApplicationFiled: March 15, 2012Publication date: January 2, 2014Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Pu Liu, Wei Zheng, Juan Marugan, Noel T. Southall, Lea Cunningham