At Least Four Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/117)
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Patent number: 11177442Abstract: A thermally activated delayed fluorescent material includes a structural formula (I) as follows: and D1 and D2 are different electron donors. In addition, an organic light emitting diode display device includes an anode, a cathode, and an organic functional layer disposed between the anode and the cathode. The organic functional layer includes a thermally activated delayed fluorescent material, and the thermally activated delayed fluorescent material includes a structural formula (I).Type: GrantFiled: May 15, 2019Date of Patent: November 16, 2021Assignee: WUHAN CHINA STAR OPTOELECTRONICS SEMICONDUCTOR DISPLAY TECHNOLOGY CO., LTD.Inventors: Jiajia Luo, Qu Zhang
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Patent number: 10947231Abstract: Provided herein are improved processes for the synthesis of substituted tetrahydro beta-carboline derivatives. In particular, provided herein are improved processes useful for the preparation of (S)-4-chlorophenyl 6-chloro-1-(4-methoxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate.Type: GrantFiled: September 24, 2019Date of Patent: March 16, 2021Assignee: PTC Therapeutics, Inc.Inventors: Peter Seongwoo Hwang, Young-Choon Moon, Arasu Tamil, Hongyan Qi, Neil Almstead
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Patent number: 10590129Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: GrantFiled: August 22, 2018Date of Patent: March 17, 2020Assignees: RHIZEN PHARMACEUTICALS SA, INCOZEN THERAPEUTICS PVT. LTD.Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
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Patent number: 10087182Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: GrantFiled: March 9, 2017Date of Patent: October 2, 2018Assignees: INCOZEN THERAPEUTICS PVT. LTD., RHIZEN PHARMACEUTICALS SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
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Patent number: 9815831Abstract: The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.Type: GrantFiled: February 27, 2013Date of Patent: November 14, 2017Assignee: RHIZEN PHARMACEUTICALS SAInventors: Swaroop K. V. S. Vakkalanka, Dhanapalan Nagarathnam, Srikant Viswanadha, Meyyappan Muthuppalaniappan, Govindarajulu Babu, Prashant K. Bhavar
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Patent number: 9040555Abstract: 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 abnormal or excessive fibrosis.Type: GrantFiled: January 26, 2013Date of Patent: May 26, 2015Assignee: Angion Biomedica Corp.Inventors: Bijoy Panicker, Rama K. Mishra, Dong Sung Lim, Lambertus J. W. M. Oehlen, Dawoon Jung
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Publication number: 20150133449Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: November 6, 2014Publication date: May 14, 2015Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
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Publication number: 20150133658Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: August 15, 2014Publication date: May 14, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
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Publication number: 20150080377Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, aType: ApplicationFiled: August 31, 2013Publication date: March 19, 2015Inventor: Daljit Singh Dhanoa
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Publication number: 20150057309Abstract: The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.Type: ApplicationFiled: February 27, 2013Publication date: February 26, 2015Inventors: Swaroop K. V. S. Vakkalanka, Dhanapalan Nagarathnam, Srikant Viswanadha, Meyyappan Muthuppalaniappan, Govindarajulu Babu, Prashant K. Bhavar
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Patent number: 8952034Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: July 26, 2010Date of Patent: February 10, 2015Assignee: Gilead Sciences, Inc.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Publication number: 20150025094Abstract: The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halType: ApplicationFiled: August 1, 2012Publication date: January 22, 2015Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan UniversityInventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
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Publication number: 20150018337Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 29, 2014Publication date: January 15, 2015Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Patent number: 8933094Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.Type: GrantFiled: October 16, 2013Date of Patent: January 13, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 8927720Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: January 6, 2015Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 8921319Abstract: The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.Type: GrantFiled: July 5, 2011Date of Patent: December 30, 2014Assignee: The Medicines Company (Leipzig) GmbHInventors: Torsten Steinmetzer, Sebastian Martin Saupe
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Patent number: 8912331Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: GrantFiled: May 10, 2013Date of Patent: December 16, 2014Assignees: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V. S. Vakkalanka
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Publication number: 20140364603Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
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Publication number: 20140349990Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 20, 2014Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
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Publication number: 20140315928Abstract: The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: ApplicationFiled: April 15, 2014Publication date: October 23, 2014Applicant: Pfizer Inc.Inventors: Etzer Darout, Robert Dullea, Julie Jia Li Hawkins, Allyn T. Londregan, Paula M. Loria, Bruce Maguire, Kim F. McClure, Donna N. Petersen, David W. Piotrowski
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Publication number: 20140309424Abstract: The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O—([18F]Fluoromethyl)tyrosines.Type: ApplicationFiled: June 29, 2012Publication date: October 16, 2014Applicant: PIRAMAL IMAGING SAInventors: Thomas Brumby, Keith Graham, Martin Kruger
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Publication number: 20140303158Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: May 9, 2014Publication date: October 9, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Patent number: 8846913Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3—R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: April 24, 2013Date of Patent: September 30, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
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Publication number: 20140275015Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Christa C. Chrovian, Heather R. Coate, Meri De Angelis, Curt A. Dvorak, Christine F. Gelin, Michael A. Letavic, Brad M. Savall, Akinola Soyode-Johnson, Brice M. Stenne, Devin M. Swanson
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Patent number: 8822689Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.Type: GrantFiled: September 19, 2012Date of Patent: September 2, 2014Assignees: Merial Limited, Aventis AgricultureInventors: Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Robert Toms Jacobs
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Patent number: 8779142Abstract: It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.Type: GrantFiled: July 9, 2010Date of Patent: July 15, 2014Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Makoto Kitade, Shuichi Ohkubo, Chihoko Yoshimura, Satoshi Yamashita, Hiromi Oshiumi, Takao Uno, Yuichi Kawai
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Patent number: 8754103Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: July 26, 2010Date of Patent: June 17, 2014Assignee: Gilead Sciences, Inc.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Patent number: 8754082Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: GrantFiled: May 9, 2013Date of Patent: June 17, 2014Assignee: Siga Technologies, Inc.Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
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Patent number: 8741919Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: April 29, 2010Date of Patent: June 3, 2014Assignee: Medivation Technologies, Inc.Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Publication number: 20140128426Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: ApplicationFiled: May 9, 2013Publication date: May 8, 2014Applicant: Siga Technologies Inc.Inventor: Siga Technologies Inc.
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Patent number: 8691838Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds of Formula I, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: May 22, 2009Date of Patent: April 8, 2014Assignee: Amgen Inc.Inventors: Brian K. Albrecht, Steven Bellon, Christiane M. Bode, Alessandro Boezio, Deborah Choquette, Jean-Christophe Harmange
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Publication number: 20140080862Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.Type: ApplicationFiled: September 19, 2012Publication date: March 20, 2014Applicants: AVENTIS AGRICULTURE, MERIAL LIMITEDInventors: Mark David Soll, Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Douglas Edward Wilkinson, Robert Toms Jacobs
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Patent number: 8653260Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: June 20, 2012Date of Patent: February 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
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Publication number: 20140011997Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: THERAVANCE, INC.Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
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Publication number: 20130324531Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2 and R3 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: ApplicationFiled: May 29, 2013Publication date: December 5, 2013Applicant: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, George Kenneth Ehrlich, Jin-Jun Liu, Hanspeter Michel, Binh Thanh Vu, Chunlin Zhao
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Publication number: 20130261116Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: May 10, 2013Publication date: October 3, 2013Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
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Publication number: 20130245260Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: April 24, 2013Publication date: September 19, 2013Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
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Patent number: 8501795Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: December 15, 2010Date of Patent: August 6, 2013Assignee: H. Lundbeck A/SInventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
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Patent number: 8481739Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: GrantFiled: May 16, 2011Date of Patent: July 9, 2013Assignees: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V. S. Vakkalanka
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Patent number: 8461177Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: GrantFiled: August 26, 2008Date of Patent: June 11, 2013Assignee: Siga Technologies, Inc.Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
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Patent number: 8461176Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives substantially enriched in an enantiomer of formula (I): and compounds of formula (IH) wherein R3, R4, R5, R6, R7, R13a, R13b, R14a, R14b, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.Type: GrantFiled: November 13, 2009Date of Patent: June 11, 2013Assignee: Merial LimitedInventors: Mark David Soll, Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Douglas Edward Wilkinson, Robert Toms Jacobs, Brent Christopher Beck
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Publication number: 20130144541Abstract: Novel cross-linking compounds that can be used in mass spectrometry, tandem mass spectrometry, and multi-stage tandem mass spectrometry to facilitate structural analysis of proteins and protein complexes are provided and have the formula: where X is an N-hydroxy-succinimidyl or similar heterocyclic group. Also provided is a method of mapping protein-protein interactions of protein complexes using various mass spectrometry techniques.Type: ApplicationFiled: May 14, 2012Publication date: June 6, 2013Inventors: Scott Rychnovsky, Lan Huang
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Publication number: 20130065883Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3, and/or Flt3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: February 18, 2011Publication date: March 14, 2013Applicant: Centro Nacional de Investigaceiones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Julen Oyarzabal Santamarina, Carl-Gustaf Pierre Saluste, Carmen Blanco Aparicio, Rosa Maria Alvarez Escobar, Virginia Rivero Buceta
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Patent number: 8372860Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.Type: GrantFiled: March 2, 2010Date of Patent: February 12, 2013Assignee: PTC Therapeutics, Inc.Inventors: Young-Choon Moon, Liangxian Cao, Nadarajan Tamilarasu, Hongyan Qi, Soongyu Choi, William Joseph Lennox, Donald Thomas Corson, Seongwoo Hwang, Thomas Davis
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Patent number: 8334291Abstract: The present application relates to novel aliphatically substituted pyrazolopyridines, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: December 8, 2009Date of Patent: December 18, 2012Assignee: Bayer Intellectual Property GmbHInventors: Hartmut Schirok, Nils Griebenow, Chantal Fürstner, Joachim Mittendorf, Johannes-Peter Stasch, Frank Wunder, Stefan Heitmeier
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Publication number: 20120283239Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: ApplicationFiled: January 13, 2011Publication date: November 8, 2012Applicant: MSD OSS B.V.Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
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Publication number: 20120264739Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.Type: ApplicationFiled: December 30, 2010Publication date: October 18, 2012Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
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Publication number: 20120245138Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: May 2, 2012Publication date: September 27, 2012Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20120213807Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: February 16, 2012Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
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Publication number: 20120213806Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: February 16, 2012Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes