Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/321)
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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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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: 20140079685Abstract: A method and composition for treating serotonin receptor-mediated conditions.Type: ApplicationFiled: November 25, 2013Publication date: March 20, 2014Applicant: Vanda Pharmaceuticals Inc.Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt Wolfgang
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Publication number: 20140080825Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 21, 2013Publication date: March 20, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20140080826Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: September 25, 2013Publication date: March 20, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: SARA SABINA HADIDA RUAH, Peter Diederik Jan Grootenhuis, Frederick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason Mc Cartney, Mehdi Numa, Xiaoqing Yang
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Patent number: 8673939Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: March 1, 2013Date of Patent: March 18, 2014Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Publication number: 20140073622Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.Type: ApplicationFiled: September 13, 2013Publication date: March 13, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
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Publication number: 20140073669Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: November 18, 2013Publication date: March 13, 2014Inventors: Alexander L. RUCHELMAN, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
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Publication number: 20140073595Abstract: The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.Type: ApplicationFiled: October 11, 2013Publication date: March 13, 2014Applicant: Council Of Scientific and Industrial ResearchInventors: Surrinder KOUL, Jawahir Lal KOUL, Subhash Chandra TANEJA, Pankaj GUPTA, Inshad Ali KHAN, Zahid Mehmood MIRZA, Ashwani KUMAR, Rakesh Kamal JOHRI, Monika PANDITA, Anita KHOSA, Ashok Kumar TIKOO, Subhash Chander Sharma, Vijeshwar VERMA, Ghulam Nabi QAZI
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Publication number: 20140066412Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: November 6, 2013Publication date: March 6, 2014Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
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Publication number: 20140066479Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.Type: ApplicationFiled: November 11, 2013Publication date: March 6, 2014Applicant: Janssen Pharmaceutica NVInventors: Zhihua Sui, Xuqing Zhang, Xiaojie Li
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Publication number: 20140057906Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: October 21, 2013Publication date: February 27, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Peter D.J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Publication number: 20140051702Abstract: The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient.Type: ApplicationFiled: August 15, 2013Publication date: February 20, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Sandeep Gupta, Tony Priestley, Nicholas James Laping
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Publication number: 20140051726Abstract: This invention relates to Compound A or a pharmaceutically acceptable salt thereof with 5-HT4 agonistic activities, which is useful in the treatment of gastrointestinal diseases. This invention also relates to a pharmaceutical composition for the treatment of gastrointestinal diseases which comprises a therapeutically effective amount of Compound A or a pharmaceutically acceptable salt thereof. Further this invention relates to a method for the treatment of gastrointestinal diseases in an animal subject including a mammalian subject, which comprises administering to the animal subject including a mammalian subject Compound A or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 23, 2012Publication date: February 20, 2014Applicant: Raqualia Pharma Inc.Inventor: Nobuyuki Takahashi
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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: 20140045813Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
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Publication number: 20140045811Abstract: 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 18, 2013Publication date: February 13, 2014Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
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Publication number: 20140044810Abstract: Use of amide compounds represented by formula (I), for preventing or reducing settlement and/or fouling of marine fouling organisms on a surface of a submerged object is provided, wherein “-A-” has a formula -(CnH2(n?m))- which is either unsubstituted or substituted by one or more C1 to C4 alkyls, and wherein the formula -(CnH2(n?m))- represents a divalent alkyl, or a divalent alkenyl having one or more double bonds, n is 1 to 15, m is 0 to 4, and 2(n?m)=2, and R is selected from piperidinyl, pyrrolidinyl, isobutylamino, piperazinyl or morpholinyl. Amide compounds of formula (I), a category of antifouling compounds, can be either isolated from natural resources or synthesized, which are nontoxic and environmental-friendly.Type: ApplicationFiled: April 17, 2012Publication date: February 13, 2014Applicants: YUNNAN UNIVERSITY OF NATIONALITIES, THE HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Peiyuan Qian, Xiangzhong Huang, Ying Xu, Yu Zhang, Yue Him Wong, Yan Yin, Zhuang Han
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Publication number: 20140045829Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: October 8, 2013Publication date: February 13, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: MARK E. LAYTON, Michael J. Kelly
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Publication number: 20140045893Abstract: The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms.Type: ApplicationFiled: October 23, 2013Publication date: February 13, 2014Applicant: Vanda Pharmaceuticals, Inc.Inventors: Curt Wolfgang, Mihael Polymeropoulos
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Patent number: 8648095Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: June 5, 2012Date of Patent: February 11, 2014Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 8648071Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.Type: GrantFiled: June 26, 2009Date of Patent: February 11, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Joseph Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
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Publication number: 20140039008Abstract: The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms.Type: ApplicationFiled: October 2, 2013Publication date: February 6, 2014Applicant: VANDA PHARMACEUTICALS, INC.Inventors: Curt Wolfgang, Mihael Polymeropoulos, Christian Lavedan, Simona Volpi
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Publication number: 20140024656Abstract: The present invention belongs to the medicinal chemistry field, and specifically discloses a [1,3,4]oxadiazole derivative with the structure of general formula (I) and pharmaceutically acceptable salt thereof. The compound can be used to prepare a medicine for preventing or treating a disease of the central nervous system.Type: ApplicationFiled: April 1, 2012Publication date: January 23, 2014Applicant: HUAZHONG UNIVERSITY OF SCIENCE & TECHNOLOGY NHWA PHARMA CORPORATIONInventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Bifeng Liu, Xiaojun Feng, Song Zhao, Shicheng Liu, Minquan Yu, Yu Lan, Yinli Qiu
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Publication number: 20140018390Abstract: The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents.Type: ApplicationFiled: May 24, 2013Publication date: January 16, 2014Applicant: CONCERT PHARMACEUTICALS, INC.Inventor: Roger D. Tung
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Publication number: 20140018342Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.Type: ApplicationFiled: April 4, 2012Publication date: January 16, 2014Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
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Publication number: 20140011815Abstract: The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity relative to its predecessor. The present invention further provides a continuous fluorogenic assay for measuring the anti-HIV protease activity of protease inhibitor. The present invention also provides a method of administering a therapeutic compound that reduces the chances of the emergence of drug resistance in therapy.Type: ApplicationFiled: July 2, 2013Publication date: January 9, 2014Inventors: John W. Erickson, Sergei V. Gulnik, Hiroaki Mitsuya, Arun E. Ghosh
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Publication number: 20140010883Abstract: The present invention provides a controlled release pharmaceutical composition comprising selective serotonin reuptake inhibitor and a process for preparation thereof. The controlled release pharmaceutical composition comprises: a deposit-core comprising a selective serotonin reuptake inhibitor, one or more controlled release agent(s) and one or more pharmaceutically acceptable excipient(s), a support-platform applied to the deposit-core, a controlled release coating and, an immediate release coating comprising a selective serotonin reuptake inhibitor and one or more pharmaceutically acceptable excipient(s).Type: ApplicationFiled: March 16, 2012Publication date: January 9, 2014Applicant: LUPIN LIMITEDInventors: Harshal Jahagirdar, Ganesh Katkar, Satish Kumar Dalal, Shirishkumar Kulkarni
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Publication number: 20140011796Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
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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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Publication number: 20140005191Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: November 9, 2011Publication date: January 2, 2014Applicants: Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.Inventors: Craig A. Coburn, Kun Liu, Ernest J. McEacher, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou
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Patent number: 8618135Abstract: The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.Type: GrantFiled: March 11, 2011Date of Patent: December 31, 2013Assignee: The Trustees of the University of PennsylvaniaInventor: Daniel J. Rader
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Patent number: 8618134Abstract: A method and composition for treating serotonin receptor-mediated conditions.Type: GrantFiled: December 13, 2008Date of Patent: December 31, 2013Assignee: Vanda Pharmaceuticals Inc.Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt Wolfgang
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Publication number: 20130345223Abstract: The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of tubercle bacillus, and thus are useful in the treatment of tuberculosis infection and associated conditions. The present invention is further directed to in vitro- and in vzivo-based methods of inhibiting Lpd and/or PDH activity. In certain embodiments, these methods are useful in inhibiting Lpd and/or PDH activity key to a pathogen's survival.Type: ApplicationFiled: June 28, 2011Publication date: December 26, 2013Applicant: Academia SinicaInventors: Chi-Huey Wong, Ying-Ta Wu
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Publication number: 20130345195Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Michael J. BURKE, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Anil Kumar PADYANA, Lana Louise SMITH KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, QIANG ZHANG, Qing ZHANG
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Patent number: 8614247Abstract: The invention relates to a method for preventing, attenuating or treating pulmonary hypertension in an individual in need thereof, comprising administering at least one 5-HTT inhibitor to said individual.Type: GrantFiled: October 11, 2005Date of Patent: December 24, 2013Assignees: Institut National de la Sante et de la Recherche Medicale, Assistance Publique-Hopitaux de ParisInventors: Serge Adnot, Saadla Eddahibi
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Patent number: 8614232Abstract: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.Type: GrantFiled: September 14, 2012Date of Patent: December 24, 2013Assignee: Novartis AGInventors: Dierk Wieckhusen, Alexandra Glausch, Markus Ahlheim
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Publication number: 20130338192Abstract: A method of treating a subject for a serotonergic neurotransmission dysregulation disorder, comprises administering the subject a serotonin enhancer (e.g., a serotonin reuptake inhibitor) in an amount effective to treat the disorder; and concurrently administering the subject 5-hydroxytryptophan in an amount effective to enhance the activity of the serotonin enhancer, (e.g., serotonin reuptake inhibitor). In preferred embodiments the disorder is depression, anxiety, or substance abuse.Type: ApplicationFiled: June 6, 2013Publication date: December 19, 2013Applicant: Duke UniversityInventors: RANGA R. KRISHNAN, MARC G. CARON, XIAODONG ZHANG, MARTIN BEAULIEU, RAUL R. GAINETDINOV, TATIANA D. SOTNIKOVA
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Patent number: 8609663Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.Type: GrantFiled: November 17, 2010Date of Patent: December 17, 2013Assignee: University of MassachusettsInventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
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Publication number: 20130331394Abstract: Methods of identifying new treatments for schizophrenia, and the use of the same.Type: ApplicationFiled: June 11, 2013Publication date: December 12, 2013Inventor: Peter Siekmeier
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Patent number: 8604021Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.Type: GrantFiled: May 10, 2011Date of Patent: December 10, 2013Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
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Publication number: 20130323203Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: August 2, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman Belmont, Philip Anthony Morganelli, William J. Watkins
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Publication number: 20130324556Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.Type: ApplicationFiled: January 27, 2012Publication date: December 5, 2013Inventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mark Mountford, Edward Daniel Savory
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Patent number: 8598181Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: July 2, 2010Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Patent number: 8598357Abstract: 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 pharmaceuticals.Type: GrantFiled: February 27, 2012Date of Patent: December 3, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8580968Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.Type: GrantFiled: March 1, 2012Date of Patent: November 12, 2013Assignee: AbbVie Inc.Inventors: Lawrence A. Black, Marlon D. Cowart, Gregory A. Gfesser, Brian D. Wakefield, Robert J. Altenbach, Huaqing Liu, Chen Zhao, Gin C. Hsieh
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Patent number: 8580752Abstract: The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.Type: GrantFiled: March 29, 2006Date of Patent: November 12, 2013Assignee: Council of Scientitic and Industrial ResearchInventors: Surrinder Koul, Jawahir Lal Koul, Subhash Chandra Taneja, Pankaj Gupta, Inshad Ali Khan, Zahid Mehmood Mirza, Ashwani Kumar, Rakesh Kamal Johri, Monika Pandita, Anita Khosa, Ashok Kumar Tikoo, Subhash Chander Sharma, Vijeshwar Verma, Ghulam Nabi Qazi
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Patent number: 8580777Abstract: The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoagulability or fibrotic changes.Type: GrantFiled: May 22, 2009Date of Patent: November 12, 2013Assignee: SanofiInventors: Christopher Kallus, Mark Broenstrup, Andreas Evers, Anja Globisch, Herman Schreuder, Michael Wagner
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Publication number: 20130296324Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.Type: ApplicationFiled: February 25, 2013Publication date: November 7, 2013Applicant: VIVUS, Inc.Inventor: Jerry M. Held
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Publication number: 20130296366Abstract: The present invention relates to novel isomers of a metabolite of Iloperidone, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.Type: ApplicationFiled: October 26, 2012Publication date: November 7, 2013Inventors: Dominique Grimler, Hans O. Kalkman, Hequn Yin