Additional Hetero Ring Which Is Unsaturated Patents (Class 544/310)
  • Patent number: 10308660
    Abstract: 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: Grant
    Filed: June 15, 2016
    Date of Patent: June 4, 2019
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Jorge Garcia Fortanet, Matthew J. LaMarche, Martin Sendzik, Victoriano Tamez, Jr., Bing Yu
  • Patent number: 10202364
    Abstract: 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: Grant
    Filed: June 14, 2018
    Date of Patent: February 12, 2019
    Assignee: CELGENE CAR LLC
    Inventors: Antonio Christian Ferretti, Lianfeng Huang, Ying Li, John Traverse, Jean Xu, Kelvin Hin-Yeong Yong, Daozhong Zou
  • Patent number: 10093655
    Abstract: 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: Grant
    Filed: October 10, 2017
    Date of Patent: October 9, 2018
    Assignee: 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
  • Patent number: 10017496
    Abstract: 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: Grant
    Filed: July 13, 2017
    Date of Patent: July 10, 2018
    Assignee: IGNYTA, INC.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Patent number: 10005760
    Abstract: 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: Grant
    Filed: August 12, 2015
    Date of Patent: June 26, 2018
    Assignee: Celgene CAR LLC
    Inventors: Antonio Christian Ferretti, Lianfeng Huang, Ying Li, John Traverse, Jean Xu, Kelvin Hin-Yeong Yong, Daozhong Zou
  • Patent number: 9822097
    Abstract: 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: Grant
    Filed: November 11, 2016
    Date of Patent: November 21, 2017
    Assignee: 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
  • Patent number: 9527831
    Abstract: 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: Grant
    Filed: June 23, 2014
    Date of Patent: December 27, 2016
    Assignee: 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
  • Patent number: 9522902
    Abstract: 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: Grant
    Filed: April 8, 2015
    Date of Patent: December 20, 2016
    Assignee: Ignyta, Inc.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Patent number: 9249171
    Abstract: A process for making the compound of Formula I utilizes the starting compound, together with sulfilimine and sulfoxide process steps later on.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: February 2, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Adrian Ortiz, Tamas Benkovics, Zhongping Shi, Prashant P. Deshpande, Zhiwei Guo, David R. Kronenthal, Chris Sfouggatakis
  • Patent number: 9187492
    Abstract: 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: Grant
    Filed: March 25, 2011
    Date of Patent: November 17, 2015
    Assignee: School Juridical Person Kitasato Institute
    Inventors: Hiroshi Tomoda, Tohru Nagamitsu, Daisuke Matsuda, Taichi Ohshiro, Masaki Ohtawa, Satoshi Omura
  • Patent number: 9139561
    Abstract: 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: Grant
    Filed: March 4, 2015
    Date of Patent: September 22, 2015
    Assignee: 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
  • Patent number: 9120778
    Abstract: 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: Grant
    Filed: April 8, 2015
    Date of Patent: September 1, 2015
    Assignee: Ignyta, Inc.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Patent number: 9107923
    Abstract: 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: Grant
    Filed: March 4, 2015
    Date of Patent: August 18, 2015
    Assignee: 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
  • Publication number: 20150148340
    Abstract: 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: Application
    Filed: May 3, 2013
    Publication date: May 28, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer, Kirsten Börngen
  • Patent number: 9040516
    Abstract: 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: Grant
    Filed: July 31, 2012
    Date of Patent: May 26, 2015
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: 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
  • Patent number: 9029538
    Abstract: 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: Grant
    Filed: May 13, 2014
    Date of Patent: May 12, 2015
    Assignee: Ignyta, Inc.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Publication number: 20150119390
    Abstract: 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: Application
    Filed: April 24, 2013
    Publication date: April 30, 2015
    Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
  • Publication number: 20150111892
    Abstract: 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: Application
    Filed: May 27, 2013
    Publication date: April 23, 2015
    Inventors: Daniele Piomelli, Natalia Realini, Marco Mor, Chiara Pagliuca, Daniela Pizzirani, Rita Scarpelli, Tiziano Bandiera
  • Publication number: 20150111891
    Abstract: 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: Application
    Filed: January 3, 2013
    Publication date: April 23, 2015
    Applicant: 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
  • Publication number: 20150105351
    Abstract: 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: Application
    Filed: October 8, 2014
    Publication date: April 16, 2015
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Patent number: 8993779
    Abstract: 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: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: 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
  • Publication number: 20150065505
    Abstract: 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: Application
    Filed: March 29, 2013
    Publication date: March 5, 2015
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
  • Publication number: 20150065532
    Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
  • Publication number: 20150056164
    Abstract: 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: Application
    Filed: April 24, 2014
    Publication date: February 26, 2015
    Applicant: 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
  • Publication number: 20150051395
    Abstract: 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: Application
    Filed: April 24, 2013
    Publication date: February 19, 2015
    Applicant: 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
  • Publication number: 20150045378
    Abstract: 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: Application
    Filed: February 12, 2013
    Publication date: February 12, 2015
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
  • Publication number: 20150038446
    Abstract: 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: Application
    Filed: August 1, 2014
    Publication date: February 5, 2015
    Inventors: Jayakrishna Ambati, Benjamin Fowler
  • Publication number: 20150031715
    Abstract: 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: Application
    Filed: January 24, 2013
    Publication date: January 29, 2015
    Inventors: Robert Alan Goodnow, JR., Matthew Michael Hamilton, Achyutharao Sidduri
  • Publication number: 20150018363
    Abstract: 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: Application
    Filed: January 11, 2013
    Publication date: January 15, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Tsuyoshi Maekawa, Keiko Kakegawa, Tsuneo Yasuma, Asato Kina, Jumpei Aida, Uttam Khamrai, Mrinalkanti Kundu
  • Patent number: 8933075
    Abstract: 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: Grant
    Filed: June 17, 2011
    Date of Patent: January 13, 2015
    Assignees: FUZIANS BIOMEDICALS, Inc., The UAB Research Foundation
    Inventors: Guoxin Wang, Ming Luo, Zhen Yang
  • Publication number: 20150005313
    Abstract: 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: Application
    Filed: June 23, 2014
    Publication date: January 1, 2015
    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
  • Publication number: 20140378464
    Abstract: 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: Application
    Filed: June 19, 2014
    Publication date: December 25, 2014
    Inventors: Johan Oslob, Robert Anderson, Danielle Aubele, Marc Evanchik, Jonathan Charles Fox, Brian Kane, Puping Lu, Robert McDowell, Hector Rodriguez, Yonghong Song, Arvinder Sran
  • Publication number: 20140378492
    Abstract: 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: Application
    Filed: September 10, 2014
    Publication date: December 25, 2014
    Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
  • Publication number: 20140371230
    Abstract: 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: Application
    Filed: June 25, 2014
    Publication date: December 18, 2014
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • Patent number: 8901143
    Abstract: 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: Grant
    Filed: November 8, 2012
    Date of Patent: December 2, 2014
    Assignee: Hutchison MediPharma Enterprises Limited
    Inventors: Wei-Guo Su, Hong Jia, Weihan Zhang, Yumin Cui, Xiaoqiang Yan, Yongxin Ren, Jifeng Duan, Yang Sai
  • Publication number: 20140350026
    Abstract: 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: Application
    Filed: November 9, 2012
    Publication date: November 27, 2014
    Inventors: Xianjin Luo, Weidong Ye
  • Publication number: 20140349990
    Abstract: 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: Application
    Filed: May 20, 2014
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
  • Patent number: 8895471
    Abstract: 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: Grant
    Filed: March 15, 2013
    Date of Patent: November 25, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Hansjoerg Dietrich, Arianna Martelletti, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht
  • Patent number: 8895573
    Abstract: 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: Grant
    Filed: February 13, 2013
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: 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
  • Publication number: 20140343056
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: November 20, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: 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
  • Publication number: 20140343084
    Abstract: 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: Application
    Filed: July 10, 2014
    Publication date: November 20, 2014
    Inventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
  • Patent number: 8889701
    Abstract: 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: Grant
    Filed: October 11, 2013
    Date of Patent: November 18, 2014
    Inventors: Alexandre Vasilievich Ivachtchenko, Andrey Alexandrovich Ivashchenko, Oleg Dmitrievich Mitkin
  • Publication number: 20140336195
    Abstract: 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: Application
    Filed: May 21, 2012
    Publication date: November 13, 2014
    Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
  • Publication number: 20140329799
    Abstract: 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: Application
    Filed: October 26, 2012
    Publication date: November 6, 2014
    Inventors: 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
  • Patent number: 8871775
    Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: October 28, 2014
    Assignee: Glaxo Group Limited
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
  • Publication number: 20140303162
    Abstract: 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: Application
    Filed: April 1, 2014
    Publication date: October 9, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Makoto KITADE, Shuichi Ohkubo, Chihoko Yoshimura, Satoshi Yamashita, Hiromi Oshiumi, Takao Uno, Yuichi Kawai
  • Publication number: 20140296232
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicants: Massachusetts General Hospital, The Broad Institute, Inc.
    Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu
  • Publication number: 20140288049
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Application
    Filed: June 9, 2014
    Publication date: September 25, 2014
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Publication number: 20140275077
    Abstract: 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: Application
    Filed: May 13, 2014
    Publication date: September 18, 2014
    Applicant: Cephalon, Inc.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy