Additional Hetero Ring Which Is Unsaturated Patents (Class 544/310)
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Patent number: 11820755Abstract: A compound represented by formula (A) has excellent control efficacy against plant diseases.Type: GrantFiled: July 4, 2019Date of Patent: November 21, 2023Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Tatsuya Toriumi
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Patent number: 11104676Abstract: Provided herein are compounds of the Formula I: and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein R1, R2, R9, X1 and G are as defined herein, which are inhibitors of one or more TAM kinases and/or c-Met kinase, and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor and/or a c-Met kinase inhibitor.Type: GrantFiled: August 29, 2019Date of Patent: August 31, 2021Assignee: Array BioPharma Inc.Inventors: Ronald Jay Hinklin, Shelley Allen, Patrick Barbour, Adam Cook, Joshua Dahlke, John Gaudino, Ellen Laird, Oren T. McNulty, Qian Zhao
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Patent number: 10308660Abstract: The present invention relates to compounds of formula I: in which X1, X2, X3, Y1, Y2, Y3, R1, R2, R3a, R4a, R4b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.Type: GrantFiled: June 15, 2016Date of Patent: June 4, 2019Assignee: Novartis AGInventors: Zhuoliang Chen, Jorge Garcia Fortanet, Matthew J. LaMarche, Martin Sendzik, Victoriano Tamez, Jr., Bing Yu
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Patent number: 10202364Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of one or both of ERK1 and ERK2.Type: GrantFiled: June 14, 2018Date of Patent: February 12, 2019Assignee: CELGENE CAR LLCInventors: Antonio Christian Ferretti, Lianfeng Huang, Ying Li, John Traverse, Jean Xu, Kelvin Hin-Yeong Yong, Daozhong Zou
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Patent number: 10093655Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.Type: GrantFiled: October 10, 2017Date of Patent: October 9, 2018Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
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Patent number: 10017496Abstract: The present invention provides compounds of Formula I or pharmaceutically acceptable salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, methods of treatment and uses thereof.Type: GrantFiled: July 13, 2017Date of Patent: July 10, 2018Assignee: IGNYTA, INC.Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
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Patent number: 10005760Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of one or both of ERK1 and ERK2.Type: GrantFiled: August 12, 2015Date of Patent: June 26, 2018Assignee: Celgene CAR LLCInventors: Antonio Christian Ferretti, Lianfeng Huang, Ying Li, John Traverse, Jean Xu, Kelvin Hin-Yeong Yong, Daozhong Zou
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Patent number: 9822097Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.Type: GrantFiled: November 11, 2016Date of Patent: November 21, 2017Assignee: PFIZER INC.Inventors: Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
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Patent number: 9527831Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.Type: GrantFiled: June 23, 2014Date of Patent: December 27, 2016Assignee: PFIZER INC.Inventors: Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
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Patent number: 9522902Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.Type: GrantFiled: April 8, 2015Date of Patent: December 20, 2016Assignee: Ignyta, Inc.Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
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Patent number: 9249171Abstract: A process for making the compound of Formula I utilizes the starting compound, together with sulfilimine and sulfoxide process steps later on.Type: GrantFiled: May 22, 2013Date of Patent: February 2, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Adrian Ortiz, Tamas Benkovics, Zhongping Shi, Prashant P. Deshpande, Zhiwei Guo, David R. Kronenthal, Chris Sfouggatakis
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Patent number: 9187492Abstract: A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof: wherein R1 is an aliphatic, alicyclic, or aromatic acyloxy group, or a group of the formula —O—CH(R7)—R8 where R7 is a lower alkoxy group and R8 is an aryl group, and R2 is carboxyl, a lower alkoxycarbonyl group, or an arylmethylcarbamoyl group, or a —CH2-acyloxy group and R3 is an aliphatic, alicyclic or aromatic acyloxy group, provided that at least one of R4 and R3 is a group other than acetoxy, or R2 and R3 taken together form a group of the formula —O—CH(R5)—O— where R5 is an aryl group.Type: GrantFiled: March 25, 2011Date of Patent: November 17, 2015Assignee: School Juridical Person Kitasato InstituteInventors: Hiroshi Tomoda, Tohru Nagamitsu, Daisuke Matsuda, Taichi Ohshiro, Masaki Ohtawa, Satoshi Omura
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Patent number: 9139561Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.Type: GrantFiled: March 4, 2015Date of Patent: September 22, 2015Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
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Patent number: 9120778Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.Type: GrantFiled: April 8, 2015Date of Patent: September 1, 2015Assignee: Ignyta, Inc.Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
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Patent number: 9107923Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.Type: GrantFiled: March 4, 2015Date of Patent: August 18, 2015Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
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Publication number: 20150148340Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.Type: ApplicationFiled: May 3, 2013Publication date: May 28, 2015Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer, Kirsten Börngen
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Patent number: 9040516Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.Type: GrantFiled: July 31, 2012Date of Patent: May 26, 2015Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
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Patent number: 9034850Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.Type: GrantFiled: November 19, 2010Date of Patent: May 19, 2015Assignee: SK Chemicals Co., Ltd.Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
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Patent number: 9029538Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.Type: GrantFiled: May 13, 2014Date of Patent: May 12, 2015Assignee: Ignyta, Inc.Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
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Publication number: 20150119390Abstract: The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.Type: ApplicationFiled: April 24, 2013Publication date: April 30, 2015Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
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Publication number: 20150111891Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.Type: ApplicationFiled: January 3, 2013Publication date: April 23, 2015Applicant: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
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Publication number: 20150111892Abstract: The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.Type: ApplicationFiled: May 27, 2013Publication date: April 23, 2015Inventors: Daniele Piomelli, Natalia Realini, Marco Mor, Chiara Pagliuca, Daniela Pizzirani, Rita Scarpelli, Tiziano Bandiera
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Publication number: 20150105351Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.Type: ApplicationFiled: October 8, 2014Publication date: April 16, 2015Inventors: William L. Jorgensen, Karen S. Anderson
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Patent number: 8993779Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is 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, such as schizophrenia.Type: GrantFiled: August 5, 2011Date of Patent: March 31, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
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Publication number: 20150065532Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
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Publication number: 20150065505Abstract: 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: March 29, 2013Publication date: March 5, 2015Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
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Publication number: 20150056164Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: April 24, 2014Publication date: February 26, 2015Applicant: AbbVie Inc.Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
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Publication number: 20150051395Abstract: Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent ?4 integrin-inhibitory action.Type: ApplicationFiled: April 24, 2013Publication date: February 19, 2015Applicant: AJINOMOTO CO., LTD.Inventors: Hirokazu Ueno, Takashi Yamamoto, Ryuta Takashita, Ryohei Yokoyama, Toshihiko Sugiura, Shunsuke Kageyama, Ayatoshi Ando, Hiroyuki Eda, Agung Eviryanti, Tomoko Miyazawa, Aya Kirihara, Itsuya Tanabe, Tarou Nakamura, Misato Noguchi, Manami Shuto, Masayuki Sugiki, Mizuki Dohi
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Publication number: 20150045378Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.Type: ApplicationFiled: February 12, 2013Publication date: February 12, 2015Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
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Publication number: 20150038446Abstract: The present disclosure relates to compositions and methods for treating retinal damage and/or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and/or a nucleoside or nucleotide reverse transcriptase inhibitor.Type: ApplicationFiled: August 1, 2014Publication date: February 5, 2015Inventors: Jayakrishna Ambati, Benjamin Fowler
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Publication number: 20150031715Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.Type: ApplicationFiled: January 24, 2013Publication date: January 29, 2015Inventors: Robert Alan Goodnow, JR., Matthew Michael Hamilton, Achyutharao Sidduri
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Publication number: 20150018363Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.Type: ApplicationFiled: January 11, 2013Publication date: January 15, 2015Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Tsuyoshi Maekawa, Keiko Kakegawa, Tsuneo Yasuma, Asato Kina, Jumpei Aida, Uttam Khamrai, Mrinalkanti Kundu
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Patent number: 8933075Abstract: Novel 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives that are effective for use in treating viral infections are described. Also described are pharmaceutical compositions comprising the 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives and methods for using the compounds or compositions.Type: GrantFiled: June 17, 2011Date of Patent: January 13, 2015Assignees: FUZIANS BIOMEDICALS, Inc., The UAB Research FoundationInventors: Guoxin Wang, Ming Luo, Zhen Yang
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Publication number: 20150005313Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.Type: ApplicationFiled: June 23, 2014Publication date: January 1, 2015Inventors: MICHAEL AARON BRODNEY, JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, MICHAEL ERIC GREEN, JACLYN LOUISE HENDERSON, CHEWAH LEE, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, LEI ZHANG
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Publication number: 20140378492Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: September 10, 2014Publication date: December 25, 2014Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
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Publication number: 20140378464Abstract: Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease.Type: ApplicationFiled: June 19, 2014Publication date: December 25, 2014Inventors: Johan Oslob, Robert Anderson, Danielle Aubele, Marc Evanchik, Jonathan Charles Fox, Brian Kane, Puping Lu, Robert McDowell, Hector Rodriguez, Yonghong Song, Arvinder Sran
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Publication number: 20140371230Abstract: 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: June 25, 2014Publication date: December 18, 2014Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Patent number: 8901143Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.Type: GrantFiled: November 8, 2012Date of Patent: December 2, 2014Assignee: Hutchison MediPharma Enterprises LimitedInventors: Wei-Guo Su, Hong Jia, Weihan Zhang, Yumin Cui, Xiaoqiang Yan, Yongxin Ren, Jifeng Duan, Yang Sai
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Publication number: 20140350026Abstract: The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R? and R? are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.Type: ApplicationFiled: November 9, 2012Publication date: November 27, 2014Inventors: Xianjin Luo, Weidong Ye
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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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Patent number: 8895573Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.Type: GrantFiled: February 13, 2013Date of Patent: November 25, 2014Assignee: Janssen Pharmaceutica, NVInventors: Steven J Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A Miskowski, Scott L. Dax, Henry J Breslin, Bart L. De Corte, Wei He
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Patent number: 8895471Abstract: The invention relates to 3-(benzylsulfinyl)-5,5-dimethyl-4,5-dihydroisoxazole derivatives and 5,5-dimethyl-3-[(1H-pyrazol-4-ylmethyl)sulfinyl]-4,5-dihydroisoxazole derivatives of the formula (I) and their salts processes for their preparation and their use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants.Type: GrantFiled: March 15, 2013Date of Patent: November 25, 2014Assignee: Bayer Cropscience AGInventors: Hansjoerg Dietrich, Arianna Martelletti, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht
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Publication number: 20140343056Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: September 12, 2012Publication date: November 20, 2014Applicant: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Dominic Suarez, Xinrong Tian, Sharad Kumar Verma
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Publication number: 20140343084Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: July 10, 2014Publication date: November 20, 2014Inventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
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Patent number: 8889701Abstract: The instant invention relates to a novel compound representing a substituted phosphoramidic acid—a (2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 1 or a (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 2, or a pharmaceutically acceptable salt, a hydrate, a crystalline form or a stereoisomer thereof, as defined in the specification. The novel compound is used for a pharmaceutical composition with at least one pharmaceutically acceptable excipient as well as with an inosine 5 monophosphate dehydrogenase inhibitor, HCV protease NS3 inhibitor, HCV protease NS3/4A inhibitor, and RNA polymerase NS5A inhibitor. The novel compound is useful as a viral polymerase HCV NS5B inhibitor and can be used for treating a disease caused by hepatitis C virus (HCV).Type: GrantFiled: October 11, 2013Date of Patent: November 18, 2014Inventors: Alexandre Vasilievich Ivachtchenko, Andrey Alexandrovich Ivashchenko, Oleg Dmitrievich Mitkin
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Publication number: 20140336195Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: May 21, 2012Publication date: November 13, 2014Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
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Publication number: 20140329799Abstract: This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.Type: ApplicationFiled: October 26, 2012Publication date: November 6, 2014Inventors: W. Michael Seganish, Stephanie Nicole Brumfield, Jongwon Lim, Julius J. Matasi, William T. Mcelroy, Deen B. Tulshian, Brian J. Lavey, Michael D. Altman, Criag R. Gibeau, John William Lampe, Joey Methot, Liang Zhu
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Patent number: 8871775Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.Type: GrantFiled: December 2, 2011Date of Patent: October 28, 2014Assignee: Glaxo Group LimitedInventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
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Publication number: 20140303162Abstract: 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: ApplicationFiled: April 1, 2014Publication date: October 9, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto KITADE, Shuichi Ohkubo, Chihoko Yoshimura, Satoshi Yamashita, Hiromi Oshiumi, Takao Uno, Yuichi Kawai
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Publication number: 20140296232Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:Type: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Applicants: Massachusetts General Hospital, The Broad Institute, Inc.Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu