The Additional Five-membered Hetero Ring Consists Of Three Ring Carbons, And Of Nitrogen And Chalcogen In Adjacent Ring Positions (e.g., Isoxazolyl, Isothiazolyl, Etc.) Patents (Class 514/254.04)
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Patent number: 8835653Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: August 18, 2010Date of Patent: September 16, 2014Assignee: SanofiInventors: Markus Follmann, Volkmar Wehner, Jean-Michel Altenburger, Gilbert Lassalle, Jean-Pascal Herault
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Publication number: 20140256700Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.Type: ApplicationFiled: February 26, 2014Publication date: September 11, 2014Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
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Publication number: 20140256740Abstract: 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: September 11, 2014Applicant: Tempero Pharmaceuticals, Inc.Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
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Publication number: 20140248378Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: July 5, 2012Publication date: September 4, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
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Patent number: 8822517Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.Type: GrantFiled: September 16, 2011Date of Patent: September 2, 2014Assignee: Adamed SP. Z O.O.Inventors: Marcin Kolaczkowski, Piotr Kowalski, Jolanta Jaśkowska, Monika Marcinkowska, Katarzyna Mitka, Adam Bucki, Anna Wesolowska, Maciej Pawlowski
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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: 20140235651Abstract: A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]-heptanedicarboxylmide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.Type: ApplicationFiled: February 18, 2014Publication date: August 21, 2014Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventor: Kazuyuki FUJIHARA
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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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Patent number: 8809530Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF recptor TrkA.Type: GrantFiled: April 18, 2014Date of Patent: August 19, 2014Assignee: VM Pharma LLCInventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20140228331Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.Type: ApplicationFiled: April 18, 2014Publication date: August 14, 2014Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20140228365Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: February 7, 2014Publication date: August 14, 2014Applicant: Merck Serono S.A.Inventors: Anna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
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Publication number: 20140220112Abstract: Sparingly water-soluble agents can be formulated as cyclodextrin complexes, however, these water-soluble drug-cyclodextrin complexes dissociate when the complex is administered into patients. The dilution of the complex in the patient leads to the drug being released from the complex, so the drug is not effectively targeted. In contrast, drugs encapsulated in the aqueous core of a lipid vesicles are not released when the liposome is diluted in blood. This invention describes compositions and methods whereby cyclodextrin or polyanionic beta-cyclodextrin drug-complexes are mixed with a preformed liposome containing the amine salts of an acidic compound. This results in the drug cyclodextrin complex being transferred into the liposome where it is stably retained. The liposome-encapsulated drug can then be injected into a patient.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Inventors: Francis C. SZOKA, JR., Charles O. Noble, Mark E. Hayes
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Patent number: 8796257Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: November 30, 2012Date of Patent: August 5, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 8791111Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in Claim (1), can and be employed for the treatment of tumors.Type: GrantFiled: September 19, 2008Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Publication number: 20140206667Abstract: The invention relates to methods and compositions for treating schizophrenia or bipolar disorder (in particular, mania) by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an antipsychotic or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs thereof. In some embodiments, the methods and the compositions are for treating one or more positive and/or negative symptoms, as well as cognitive impairment, associated with schizophrenia or bipolar disorder (in particular, mania).Type: ApplicationFiled: November 14, 2013Publication date: July 24, 2014Inventor: Michela Gallagher
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Patent number: 8778940Abstract: The present invention relates to compounds and methods for inducing neuronal differentiation in normal neural stem cells and brain cancer stem cells. The methods may take place in vitro, such as in isolates from the adult mammalian brain, or in vivo. Compounds and methods described herein may find use in the treatment of neurodegenerative and psychiatric diseases, the repair and regeneration of the nervous system, and in treatment of neurologic malignancy.Type: GrantFiled: June 4, 2012Date of Patent: July 15, 2014Assignee: The Board of Regents of the University of Texas SystemInventors: Jay Schneider, Jenny Hsieh, Douglas Frantz, Steven L. McKnight, Joseph M. Ready
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Publication number: 20140194409Abstract: The present invention relates to 4-((1R,3S)-6-chloro-3-phenyl-indan-1yl)-1,2,2-trimethyl-piperazine and the salts thereof with activity at dopamine D1 and D2 receptors as well as the serotonin 5HT2 receptor for the treatment of diseases in the central nervous system in a once weekly dosing regime.Type: ApplicationFiled: June 20, 2012Publication date: July 10, 2014Applicant: H. Lundbeck A/SInventors: René Holm, Lone Bruun
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Publication number: 20140171441Abstract: Pharmaceutical compositions of a low-solubility drug and lower alkanoate-, phthalate- and trimellitate esters of hydroxypropyl methyl cellulose and lower alkanoate- and succinate esters of cellulose and methyl cellulose are disclosed that provide enhanced concentrations of the drug in a use environment.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: BEND RESEARCH, INC.Inventors: Walter C. Babcock, Dwayne T. Friesen, Warren K. Miller, Daniel T. Smithey
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Publication number: 20140171442Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.Type: ApplicationFiled: July 31, 2012Publication date: June 19, 2014Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Miquan Yu, Yinli Qiu
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Patent number: 8754053Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: GrantFiled: February 17, 2011Date of Patent: June 17, 2014Assignee: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Publication number: 20140148457Abstract: Compounds of the formula I in which R, R1, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: April 12, 2012Publication date: May 29, 2014Applicant: MERCK PATENT GMBHInventors: Srinivasa R. Karra, Wolfgang Staehle, Eike Staub, Margarita Wucherer-Plietker
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Patent number: 8722683Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: GrantFiled: February 10, 2012Date of Patent: May 13, 2014Assignee: Hoffmann LA-Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8716277Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: December 10, 2012Date of Patent: May 6, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
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Publication number: 20140113911Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a benzopyrone derivative and a use thereof. The benzopyrone derivative is compound having a structure of formula (I) or a pharmaceutically acceptable salt thereof. It has been found by experiments that, this type of compounds is useful in prevention or treatment of neuropsychical diseases.Type: ApplicationFiled: April 6, 2012Publication date: April 24, 2014Applicant: NHWA PHARMA CORPORATIONInventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Bifeng Liu, Xin Liu, Song Zhao, Shicheng Liu, Minquan Yu, Heng Zhang, Xinghua Liu
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Publication number: 20140113912Abstract: The present disclosure relates to methods of treating certain CNS disorders. The present disclosure also relates to biomarkers for monitoring or predicting the efficacy of a treatment for a CNS disorder by lurasidone, or a pharmaceutically acceptable salt, solvate, clathrate or stereoisomer thereof.Type: ApplicationFiled: May 11, 2012Publication date: April 24, 2014Inventors: Antony D. Loebel, Robert M. Silva
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Publication number: 20140107129Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: December 11, 2013Publication date: April 17, 2014Applicant: Galderma Research & DevelopmentInventors: Laurence CLARY, Sandrine CHAMBON, Laurent CHANTALAT, Carine ROSIGNOLI, Olivier ROYE, Jean-Claude PASCAL, Marlene SCHUPPLI-NOLLET
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Patent number: 8691824Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: GrantFiled: August 3, 2009Date of Patent: April 8, 2014Assignee: CHDI Foundation, Inc.Inventors: John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
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Patent number: 8680090Abstract: The present invention provides compounds of Formula (I): 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: GrantFiled: July 8, 2013Date of Patent: March 25, 2014Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
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Patent number: 8664220Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: GrantFiled: September 29, 2010Date of Patent: March 4, 2014Assignee: Amira Pharmaceuticals, Inc.Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas J. Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
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Patent number: 8658642Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: March 15, 2013Date of Patent: February 25, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Jared Andrew Forrester
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Patent number: 8653127Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: January 14, 2010Date of Patent: February 18, 2014Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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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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Patent number: 8648081Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.Type: GrantFiled: May 8, 2012Date of Patent: February 11, 2014Assignee: Eli Lilly and CompanyInventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
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Publication number: 20140038979Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: October 14, 2013Publication date: February 6, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristof VAN EMELEN, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van Heusden
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Publication number: 20140031364Abstract: Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient.Type: ApplicationFiled: March 30, 2012Publication date: January 30, 2014Applicant: IL-YANG PHARM. CO., LTD.Inventors: Dong Yeon Kim, Dae Jin Cho, Gong Yeal Lee, Hong Youb Kim, Seok Hun Woo, Hae Un Lee, Sung Moo Kim, Choong Am Ahn, Seung Bin Yoon
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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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Publication number: 20140031330Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: July 11, 2013Publication date: January 30, 2014Inventors: Monique Bodil van Niel, Benjamin Fauber, Simon Gaines, Alberto Gobbi, Olivier Rene, David Vesey, Stuart Ward
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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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Patent number: 8633196Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 22, 2013Date of Patent: January 21, 2014Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlène Schuppli-Nollet
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Publication number: 20140018348Abstract: Compositions and methods tor the treatment of depression and psychoses in humans are disclosed. More particularly, the invention is directed to formulations containing antipsychotic and/or antidepressant medications and also containing an NMPAR antagonist. The present invention is also directed to methods for the treatment of humans suffering from depression and other psychoses, including, schizophrenia, by administration of the inventive compositions in antidepressant and/or antipsychotic effective amounts.Type: ApplicationFiled: July 7, 2013Publication date: January 16, 2014Inventor: Daniel C. Javitt
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Publication number: 20140011799Abstract: The present invention provides compounds of Formula (I): 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: July 8, 2013Publication date: January 9, 2014Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
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Patent number: 8623875Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.Type: GrantFiled: June 10, 2008Date of Patent: January 7, 2014Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Ty Wagerle, Ming Xu
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Patent number: 8618110Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: GrantFiled: February 9, 2010Date of Patent: December 31, 2013Assignee: VM Discovery Inc.Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20130345236Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.Type: ApplicationFiled: June 11, 2013Publication date: December 26, 2013Inventors: William J. Curatolo, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Douglas A. Lorenz
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Publication number: 20130324538Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on warm-blooded animals.Type: ApplicationFiled: February 9, 2012Publication date: December 5, 2013Inventors: Noëlle Gauvry, Steve Nanchen
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Patent number: 8598162Abstract: 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: GrantFiled: October 11, 2011Date of Patent: December 3, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Jun Matsubara, Yohji Sakurai
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Patent number: 8575161Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).Type: GrantFiled: March 30, 2009Date of Patent: November 5, 2013Assignee: Merck Patent GmbHInventors: Didier Roche, Gisèle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
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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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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: 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