Nitrogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/426)
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Patent number: 11584716Abstract: A process A for the production of compounds of formula I is provided. Process A includes Step A of reacting compounds of formula II with 2,3-dihalopropionitrile or 2-haloacrylonitrile in the presence of DIPEA. A process B for the production of compounds of formula III is also provided. Process B includes Step B of reacting compounds of formula I with Br2 in the presence of DIPEA. A process C for the production of compounds of formula IV is further provided. Process C includes Step C of reacting compounds of formula III with di(C1-C4-alkoxy)methane and either POCl3, or a mixture comprising POCl3 and DMF, in the presence of DIPEA. Additionally, the use of DIPEA as a base in the production of compounds of formula I, compounds of formula III, or compounds of formula IV is provided.Type: GrantFiled: March 5, 2018Date of Patent: February 21, 2023Assignee: BASF AGRO B.V.Inventors: David A. Cortes, Ryan Michael Phillips
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Patent number: 11186640Abstract: This invention relates to systems and methods for evaluating the differentiality of a set of discrete random variables between two or more conditions, such as a malignant condition responding to treatment regime and one that is not. It also provides for the identification and selection of drugs that act in coordinated manner to phenocopy a genetic network of a malignant condition that responds to at least an immune checkpoint blockade agent.Type: GrantFiled: July 31, 2015Date of Patent: November 30, 2021Assignee: THE UNIVERSITY OF WESTERN AUSTRALIAInventors: Willem Joost Lesterhuis, Richard Andrew Lake, Anthony Bosco
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Patent number: 10259786Abstract: Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more disorders associated with an abnormality in levels of dopamine and/or serotonin in the brain.Type: GrantFiled: November 28, 2017Date of Patent: April 16, 2019Assignee: LB PHARMACEUTICALS INC.Inventors: Andrew R. Vaino, Vincent T. Grattan, Zachary Prensky
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Patent number: 9827228Abstract: Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method for treating an opioid receptor-associated condition using a compound of Formula (I) and a pharmaceutical composition containing the same.Type: GrantFiled: July 12, 2016Date of Patent: November 28, 2017Assignees: National Health Research Institutes, Regents of the University of MinnesotaInventors: Shau-Hua Ueng, Shiu-Hwa Yeh, Horace Loh, Yu-Sheng Chao
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Patent number: 9604949Abstract: Prostaglandin conjugates and derivatives and methods for their use to treat glaucoma and/or lower intraocular pressure are disclosed. Additionally, ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma and elevated intraocular pressure are disclosed. Such compositions comprise an effective amount of prostaglandin conjugates or derivatives of the present invention.Type: GrantFiled: October 15, 2015Date of Patent: March 28, 2017Assignee: Novartis AGInventors: David Archer Ellis, Lukas Scheibler, Najam A. Sharif
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Patent number: 9550749Abstract: An object of the present invention is to provide a novel endoparasite control agent as a parasiticide, an antiprotozoal or the like. Provided is an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient.Type: GrantFiled: August 29, 2013Date of Patent: January 24, 2017Assignees: The University of Tokyo, Nihon Nohyaku Co., Ltd.Inventors: Kiyoshi Kita, Akiyuki Suwa, Masatsugu Oda, Koji Tanaka
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Patent number: 9346786Abstract: The present application relates to compounds of formula wherein R1, R2, R3, R4, and n are defined herein or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: March 13, 2013Date of Patent: May 24, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
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Patent number: 9226916Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: February 28, 2013Date of Patent: January 5, 2016Assignee: HOFFMANN-LA ROCHE INC.Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
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Patent number: 9150558Abstract: The invention relates to the design and synthesis of novel anabaseine-based compounds, which are useful in treating or preventing a wide variety of conditions, including nervous system diseases or disorders, such as, schizophrenia, Alzheimer's disease, Parkinson's disease, drug dependence, and substance addiction, and compositions, kits, and methods thereof. The invention also provides novel anabaseine-based compounds, compositions, kits, and methods thereof for treating or preventing non-nerve system diseases or disorders (such as, inflammation and cancer) in a subject identified in need thereof. Certain enantiomeric compounds of the invention exhibited enhanced selectivity toward ?7 nAChRs relative to alpha4beta2 nAChRs. Other enantiomeric compounds of the invention exhibited enhanced selectivity for alpha4beta2 nAChRs relative to ?7 nAChRs.Type: GrantFiled: December 11, 2012Date of Patent: October 6, 2015Assignee: University of Florida Research Foundation, Inc.Inventors: William R. Kem, Ferenc Soti, Hong Xing
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Publication number: 20150119396Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.Type: ApplicationFiled: October 22, 2012Publication date: April 30, 2015Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
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Patent number: 9000190Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.Type: GrantFiled: April 29, 2014Date of Patent: April 7, 2015Assignees: University of Tokyo, Otsuka Chemical Co., Ltd.Inventors: Hiroaki Suga, Jun Igarashi
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Publication number: 20150025042Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 16, 2013Publication date: January 22, 2015Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
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Publication number: 20150025054Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.Type: ApplicationFiled: October 22, 2012Publication date: January 22, 2015Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
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Publication number: 20140341986Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.Type: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
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Patent number: 8889736Abstract: Formulations and methods are provided for the treatment of pain, and neuropathic pain in particular. The formulations are eutectic mixtures of a capsaicinoid and a local anesthetic agent and/or an anti-pruritic agent.Type: GrantFiled: September 14, 2011Date of Patent: November 18, 2014Assignee: Acorda Therapeutics, Inc.Inventor: Manoj Maniar
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Publication number: 20140336158Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: ApplicationFiled: July 25, 2014Publication date: November 13, 2014Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
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Patent number: 8883852Abstract: Provided herein are methods, for reducing, preventing, mitigating and treating damage caused by radiation. The methods comprise delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation or to mitigate apoptosis. The compounds comprise glyburide or other sulfonylurea hypoglycemic compounds or potassium channel inhibitors.Type: GrantFiled: October 21, 2009Date of Patent: November 11, 2014Assignee: University of Pittburgh—Of the Commonwealth System of Higher EducationInventors: Michael Epperly, Joel Greenberger, Jianfei Jiang, Valerian Kagan, John Lazo, Peter McDonald
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Publication number: 20140329871Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.Type: ApplicationFiled: December 2, 2012Publication date: November 6, 2014Applicant: ANGION BIOMEDICA CORP.Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
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Publication number: 20140329833Abstract: The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.Type: ApplicationFiled: May 21, 2012Publication date: November 6, 2014Applicant: ORYZON GENOMICS, S.AInventors: Tamara Maes, Marc Martinell Pedemonte, Julio Castro-Palomino Laria
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Publication number: 20140296255Abstract: The invention relates to methods and compositions for the treatment or prevention of thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. In particular, the invention relates to an LSD inhibitor such as a 2-cyclylcyclopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event.Type: ApplicationFiled: May 21, 2012Publication date: October 2, 2014Applicant: ORYZONG GENOMICS, S.A.Inventors: Tamara Maes, Marc Martinell Pedemonte
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Patent number: 8846742Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.Type: GrantFiled: February 14, 2007Date of Patent: September 30, 2014Assignee: The Trustees of Columbia University in the City of New YorkInventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
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Publication number: 20140288065Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
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Patent number: 8835480Abstract: The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.Type: GrantFiled: April 22, 2008Date of Patent: September 16, 2014Assignee: California Institute of TechnologyInventors: Peter B. Dervan, Nicholas G. Nickols
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Publication number: 20140256729Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.Type: ApplicationFiled: October 22, 2012Publication date: September 11, 2014Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
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Patent number: 8815871Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: GrantFiled: March 11, 2013Date of Patent: August 26, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
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Patent number: 8802719Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.Type: GrantFiled: July 11, 2013Date of Patent: August 12, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Shiek Mohamed Mujeebur Rahuman, Ramar Subbiah
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Patent number: 8778628Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 17, 2013Date of Patent: July 15, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Patent number: 8759387Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: December 17, 2012Date of Patent: June 24, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20140163041Abstract: The present invention relates to methods and compositions for the treatment or prevention of diseases and disorder associated with myeloproliferative and lymphoproliferative disorders. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing diseases and disorder associated with myeloproliferative and lymphoproliferative disorders.Type: ApplicationFiled: February 8, 2012Publication date: June 12, 2014Applicant: ORYZON GENOMICS S.A.Inventors: Matthew Colin Thor Fyfe, Tamara Maes, Marc Martinell Pedemonte
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Patent number: 8710049Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: GrantFiled: July 16, 2012Date of Patent: April 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
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Patent number: 8703721Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 12, 2011Date of Patent: April 22, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20140080770Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 17, 2013Publication date: March 20, 2014Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi MIYAZAKI, Junko OKABE, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAI, Tetsuya YANAGIDA, Yutaka HISADA
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Publication number: 20140080833Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: ApplicationFiled: November 11, 2013Publication date: March 20, 2014Applicant: MannKind CorporationInventors: Gary A. Flynn, Sandra A. Lee, Mary Faris, David W. Brandt, Subrata Chakravarty
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Publication number: 20140045910Abstract: Novel amino-pyrrolinic derivatives, their pharmacologically acceptable salts and use thereof in the prevention and/or treatment of metabolic syndrome.Type: ApplicationFiled: April 17, 2012Publication date: February 13, 2014Applicant: UNIVERSITE DE STRASBOURGInventors: Pascal Bousquet, Jean Daniel Ehrhardt, Lyne Fellmann, Vincent Gasparik, Hugues Greney, Mohamed Hadjeri, Andre Mann, Nathalie Niederhoffer, Stephan Schann
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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: 20130310379Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.Type: ApplicationFiled: November 21, 2011Publication date: November 21, 2013Applicant: CONSTELLATION PHARMACEUTICALSInventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
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Publication number: 20130274267Abstract: The present invention relates to the use of potent selective LSD1 inhibitors and LSD1/MAO-B iithibitors for treating or preventing viral infections. Furthermore, the present invention relates to the new use of cyclopropylamine acetamide derivatives or cyclopropylamine derivatives, as defmed herein, for treating or preventing viral infection and treating or preventing reacti - vation of a virus after latency.Type: ApplicationFiled: February 24, 2011Publication date: October 17, 2013Inventors: Julio Cesar Castro Palomino Laria, Alberto Ortega Munoz, Nathalie Guibourt, Jonathan Alleman Baker
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Publication number: 20130231332Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.Type: ApplicationFiled: September 1, 2011Publication date: September 5, 2013Inventors: James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
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Patent number: 8497282Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.Type: GrantFiled: December 30, 2009Date of Patent: July 30, 2013Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Sheik Mohamed Mujeebur Rahuman, Ramar Subbiah
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Patent number: 8497383Abstract: Compounds of Formula (I) are disclosed; wherein XA, k, A, B, R3A, R3B, R4 and R5 are defined herein. The compounds of Formula (I) are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: May 18, 2010Date of Patent: July 30, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Craig A. Coburn, M. Katharine Holloway, Joseph P. Vacca
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Patent number: 8492111Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 7, 2010Date of Patent: July 23, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
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Publication number: 20130184262Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: ApplicationFiled: July 16, 2012Publication date: July 18, 2013Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
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Patent number: 8466182Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.Type: GrantFiled: November 2, 2011Date of Patent: June 18, 2013Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, BaltimoreInventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Publication number: 20130150374Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: December 17, 2012Publication date: June 13, 2013Applicant: Mitsubishi Tanabe Pharma CorporationInventor: Mitsubishi Tanabe Pharma Corporation
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Patent number: 8450345Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.Type: GrantFiled: February 22, 2010Date of Patent: May 28, 2013Assignees: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics CorporationInventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
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Patent number: 8410150Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 6, 2008Date of Patent: April 2, 2013Assignee: University Health NetworkInventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
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Patent number: 8404738Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.Type: GrantFiled: January 17, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
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Patent number: 8383668Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: GrantFiled: September 16, 2011Date of Patent: February 26, 2013Assignee: High Point Pharmaceuticals, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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Publication number: 20130035325Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.Type: ApplicationFiled: November 16, 2010Publication date: February 7, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
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Patent number: 8362003Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: June 16, 2011Date of Patent: January 29, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han