Additional Hetero Ring Attached Directly Or Indirectly To The 1,4-diazine Ring By Nonionic Bonding Patents (Class 514/255.05)
  • Patent number: 10351540
    Abstract: Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.
    Type: Grant
    Filed: January 17, 2018
    Date of Patent: July 16, 2019
    Assignee: SABILA BIOSCIENCES LLC
    Inventor: Tarek Suhayl Mansour
  • Patent number: 10308645
    Abstract: The present invention is directed to piperidine oxadiazole and thiadiazole orexin compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: September 27, 2015
    Date of Patent: June 4, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel Liverton, Scott D. Kuduk, Yunfu Luo, Na Meng, Tingting Yu
  • Patent number: 10272030
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: April 30, 2019
    Assignee: Cytokinetics, Inc.
    Inventors: Zhe Yang, Alex R. Muci, Jeffrey Warrington, Gustave Bergnes, Bradley P. Morgan, Chihyuan Chuang, Antonio Romero, Scott Collibee, Xiangping Qian, Pu-Ping Lu
  • Patent number: 10239857
    Abstract: Provided herein are processes for the preparation of 2-thiophenecarbonyl chloride, which is useful, for example, in the preparation of 3,5-disubstituted-1,2,4-oxadiazoles, such as tioxazafen (3-phenyl-5-(2-thienyl)-1,2,4-oxadiazole).
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: March 26, 2019
    Assignee: Monsanto Technology LLC
    Inventors: Daniel P. Walker, William H. Miller
  • Patent number: 10208064
    Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: July 9, 2015
    Date of Patent: February 19, 2019
    Inventors: Alexander Pasternak, Ian Davies, Fa-Xiang Ding, Jinlong Jiang, Shuzhi Dong, Xin Gu, Takao Suzuki, Joseph P. Vacca, Zhifa Pu, Shouning Xu
  • Patent number: 10201584
    Abstract: This disclosure is directed to pharmaceutical compositions that comprise two or more therapeutic agents that, inter alia, are useful for inhibiting hepatitis C virus (HCV) and methods for inhibiting HCV by co-administering two or more anti-HCV therapeutic agents.
    Type: Grant
    Filed: April 8, 2014
    Date of Patent: February 12, 2019
    Assignee: ABBVIE INC.
    Inventors: Christine A. Collins, Daniel E. Cohen, Gennadiy Koev, Preethi Krishnan, Tami J. Pilot-Matias
  • Patent number: 10179125
    Abstract: The disclosure relates to substituted pyridines, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: January 15, 2019
    Assignee: Zenith Epigenetics Ltd.
    Inventors: May Xiaowu Jiang, Bruce Francis Molino, Shuang Liu, Ruifang Wang, Bryan Cordell Duffy, John Frederick Quinn, Gregory Steven Wagner
  • Patent number: 10150765
    Abstract: 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: Grant
    Filed: September 7, 2016
    Date of Patent: December 11, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: 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
  • Patent number: 10138222
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1—, R2—, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: November 27, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jianwen Cui, Donghong Amy Gao, Pingrong Liu, Bryan Patrick McKibben, Craig Andrew Miller, Hossein Razavi, Elizabeth Spencer, Sabine Ruppel, Anil K. Padyana
  • Patent number: 10137125
    Abstract: Benzenesulfonamide derivatives of quinoxaline that are kinase inhibitors, pharmaceutical compositions and methods of using these derivatives, e.g., for treatment of cancer are described.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: November 27, 2018
    Assignee: NEUPHARMA, INC.
    Inventors: Yong-Liang Zhu, Xiangping Qian
  • Patent number: 10138241
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: November 27, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pingrong Liu, Craig Andrew Miller, Maolin Yu, Zhonghua Zhang, Sabine Ruppel, Anil K. Padyana
  • Patent number: 10100035
    Abstract: The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them.
    Type: Grant
    Filed: September 20, 2017
    Date of Patent: October 16, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Diego Broggini, Matteo Conza, Oliver Flögel, Stefan Horns, Susanne Lochner, Guangrong Tang, Zhaobin Wang, Lucie Lovelle
  • Patent number: 10058540
    Abstract: The present invention is directed to compounds of Formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of A? deposits is beneficial such as Alzheimer's disease.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: August 28, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Karsten Juhl, Lena Tagmose, Mauro Marigo
  • Patent number: 10053451
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: August 21, 2018
    Assignee: Genentech, Inc.
    Inventors: Sharada Labadie, Jun Liang, Daniel Fred Ortwine, Xiaojing Wang, Birong Zhang, Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Andiliy G. Lai, Johnny Y. Nagasawa, Simon Charles Goodacre, Nicholas Charles Ray
  • Patent number: 10016417
    Abstract: Extended release formulations of 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide (DPOC-4088) that provide for better control of blood plasma levels. The extended release formulations maintain substantially constant plasma levels of the active ingredient for at least about 16 hours and provide for once-daily dosing.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: July 10, 2018
    Assignee: Diakron Pharmaceuticals, Inc.
    Inventors: Sankar Ramakrishnan, Elumalal Venkatesan, Jayanthi Suryakumar, Stephane Allard
  • Patent number: 10011596
    Abstract: The present invention provides compounds of Formula I for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula I.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: July 3, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Karsten Juhl, Lena Tagmose, Mauro Marigo
  • Patent number: 10004738
    Abstract: The present invention is directed to the combined use of BACE1 inhibitor of Formula I and a compound useful in active or passive Tau immunotherapy, a compound useful in active or passive A? peptide immunotherapy, an NMDA receptor antagonists, an acetylcholine esterase inhibitor, an antiepileptic, an anti-inflammatory drug, a Tau aggregation inhibitor or an SSRI for the treatment of neurodegenerative or cognitive disorders.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: June 26, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Karsten Juhl, Mauro Marigo, Lena Tagmose, Thomas Jensen
  • Patent number: 9957254
    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: Grant
    Filed: July 2, 2015
    Date of Patent: May 1, 2018
    Assignee: Novartis AG
    Inventors: Christopher M. Adams, David B. Belanger, Doug Bevan, Philippe Bolduc, Takeru Ehara, Luciana Ferrara, Nan Ji, Mitsunori Kato, Erik Meredith, Muneto Mogi, James J. Powers, Ganesh Prasanna
  • Patent number: 9944606
    Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 17, 2018
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Robert M Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
  • Patent number: 9938276
    Abstract: The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: April 10, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Scott D. Kuduk, Nigel Liverton, Gang Zhou
  • Patent number: 9920017
    Abstract: The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests including arthropods, insects and nematodes, and to processes and intermediates for preparation of the novel compounds.
    Type: Grant
    Filed: March 4, 2015
    Date of Patent: March 20, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Eike Kevin Heilmann, Heinz-Juergen Wroblowsky, Axel Trautwein, Joerg Greul, Hardwin Dembski, Kerstin Ilg, Daniela Portz, Ulrich Goergens
  • Patent number: 9908845
    Abstract: The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: March 6, 2018
    Assignee: PELOTON THERAPEUTICS, INC.
    Inventors: Darryl David Dixon, Jonas Grina, John A. Josey, James P. Rizzi, Stephen T. Schlachter, Eli M. Wallace, Bin Wang, Paul Wehn, Rui Xu, Hanbiao Yang
  • Patent number: 9895446
    Abstract: Intralesional injections including poloxamer compounds and anticancer drugs are disclosed. The combination of the poloxamer-based composition with chemotherapeutic agents within the disclosed intralesional injections provides a synergistic effect, thereby allowing lower dosages of the active drugs and enhancing the treatment effectiveness. The disclosed poloxamer-based intralesional injections are employed for treating different types of cancer in humans and other animal species. The disclosed intralesional injections can be used as the sole therapy or in combination with one or more additional therapies, such as, chemotherapy, electrotherapy, immunotherapy and/or radiation therapy. The disclosed intralesional injections can be employed in virotherapy and gene therapy treatments. The disclosed intralesional injections are designed for immediate release or controlled release of the active drugs. The disclosed intralesional injections are employed for local or systemic administration of active drugs.
    Type: Grant
    Filed: July 14, 2016
    Date of Patent: February 20, 2018
    Assignees: Professional Compounding Centers of America, Best Pet Rx IP, Inc.
    Inventors: Chris V. Simmons, Danny Carrero
  • Patent number: 9856240
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: January 2, 2018
    Assignee: CALCIMEDICA, INC.
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
  • Patent number: 9844542
    Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: December 19, 2017
    Assignee: Vanderbilt University
    Inventors: Kyle A. Emmitte, Craig W. Lindsley, P. Jeffrey Conn, Andrew S. Felts, Alice L. Rodriguez, Katrina A. Smith, Carrie K. Jones
  • Patent number: 9802918
    Abstract: The present disclosure describes pyridineamine compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: October 31, 2017
    Assignee: Incyte Corporation
    Inventors: Oleg Vechorkin, Yun-Long Li, Jincong Zhuo
  • Patent number: 9790183
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Grant
    Filed: February 4, 2016
    Date of Patent: October 17, 2017
    Assignee: GENENTECH, INC.
    Inventors: Janet L. Gunzner-Toste, Daniel Sutherlin, Mark S. Stanley, Liang Bao, Georgette M. Castanedo, Rebecca L. Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F. T. Koehler
  • Patent number: 9744170
    Abstract: The present disclosure relates to solid dosage forms comprising antiviral compounds and methods of using such dosage forms to treat antiviral infection.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: August 29, 2017
    Assignee: AbbVie Inc.
    Inventors: Jonathan M. Miller, John B. Morris, Nancy E. Sever, Eric A. Schmitt, Ping X. Gao, Yi Shi, Yi Gao, Bernd Liepold, Anna Moosmann, Mirko Pauli, Fatih Durak, Thomas Kessler, Peter Hoelig, Karin Rosenblatt, Drazen Kostelac, Rajeev Gokhale, Mark Costello, Carl Knable
  • Patent number: 9730886
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 12, 2015
    Date of Patent: August 15, 2017
    Assignee: Cytokinetics, Inc.
    Inventors: Zhe Yang, Alex R. Muci, Jeffrey Warrington, Gustave Bergnes, Bradley P. Morgan, Chihyuan Chuang, Antonio Romero, Scott Collibee, Xiangping Qian, Pu-Ping Lu
  • Patent number: 9701674
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. Certain compounds of this invention are of formula II, V, and/or VII: wherein the variables are as defined herein.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: July 11, 2017
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Patent number: 9688642
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and R2 are defined herein.
    Type: Grant
    Filed: July 9, 2015
    Date of Patent: June 27, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Sanath Meegalla, Hui Huang, Mark R. Player
  • Patent number: 9663513
    Abstract: The present invention is directed to pyrimidine compounds 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: Grant
    Filed: November 15, 2013
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
  • Patent number: 9650338
    Abstract: The present invention is aimed at providing an opioid antagonist compound and preparation method thereof, and its medical use. The medical use for opioid antagonists such as the compound of formula (I) (shown below) include complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, such as heroin, fentanyl, oxycodone, hydrocodone, morphine, propoxyphene, methadone and certain narcotic-antagonist analgesics, such as nalbuphine, pentazocine and butorphanol. An opioid antagonist may also be useful as an adjunctive agent to increase blood pressure in the management of septic shock. Further, opioid antagonists also have been shown to reduce the craving for alcohol.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: May 16, 2017
    Assignee: VDM Biochemicals, Inc.
    Inventor: Vardan Martirosyan
  • Patent number: 9642872
    Abstract: The invention relates to microRNA-34a and related microRNAs for use in the treatment of B-cell lymphoma. Likewise it relates to microRNA-34a for use in the preparation of a medicament for the treatment of B-cell lymphoma, and for a method of treatment of B-cell lymphoma comprising administering microRNA-34a. These claims are based on the observation that microRNA-34a shows strong anti-proliferative effects when overexpressed in diffuse large B-cell lymphoma (gDLBCL) cell lines, or when delivered intratumorally or systemically in xenograft models of DLBCL.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: May 9, 2017
    Assignee: UNIVERSITY OF ZURICH
    Inventors: Vanessa Craig, Anne Mueller
  • Patent number: 9643920
    Abstract: The present invention provides crystal forms A and B of 4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid having excellent stability and use as pharmaceutical ingredients. The present invention also provides industrially advantageous processes for producing these crystalline compounds.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: May 9, 2017
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Hiroshi Miyazaki, Takao Komasaka, Joji Tsurumoto, Takeshi Uemura, Yuuji Morita
  • Patent number: 9611214
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: June 10, 2014
    Date of Patent: April 4, 2017
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Patent number: 9604966
    Abstract: The present invention relates to the technical field of medicine and organic synthesis, particularly to a method for preparing crizotinib. The method comprises the compound of formula b and the compound of formula e undergoing Suzuki coupling reaction to produce the compound of formula a which then was subjected to deprotection to afford (±) crizotinib.
    Type: Grant
    Filed: February 13, 2014
    Date of Patent: March 28, 2017
    Assignee: Zhejiang Jiuzhou Pharmaceutical Co., Ltd
    Inventors: Yuanqiang Li, Jianqiang Qian, Daqing Che
  • Patent number: 9572808
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: February 21, 2017
    Assignee: NeuPharma, Inc.
    Inventors: Yong-Liang Zhu, Xiangping Qian
  • Patent number: 9550765
    Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: January 24, 2017
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Chu-Biao Xue, Yun-Long Li, Hao Feng, Ke Zhang, Wenqing Yao
  • Patent number: 9540347
    Abstract: The present disclosure describes pyridineamine compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: January 10, 2017
    Assignee: Incyte Corporation
    Inventors: Oleg Vechorkin, Hao Feng, Yun-Long Li, Song Mei, Anlai Wang, Wenyu Zhu, Jincong Zhuo
  • Patent number: 9533995
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I). Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: January 3, 2017
    Assignee: Sanofi
    Inventors: Zhongli Gao, Daniel Hall, David Stefany
  • Patent number: 9522886
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: December 20, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Beat Frei, Luca Gobbi, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch
  • Patent number: 9512125
    Abstract: The present invention provides anti-inflammatory compounds useful in the treatment of diseases and conditions in which inflammation is involved in disease progression or the manifestation of symptoms of the disease or condition.
    Type: Grant
    Filed: November 21, 2005
    Date of Patent: December 6, 2016
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Kevan M. Shokat, Nikolai Sepetov, Chao Zhang, Heinz W. Gschwend, Eric J. Kunkel
  • Patent number: 9505735
    Abstract: The present invention provides compounds of Formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting fungal or parasitic growth. The compounds are useful as inhibitors of glycosylphosphatidylinositol (GPI)-anchor biosynthesis, in particular, as inhibitors of fungal Gwt1 activity. The present invention further provides methods of using the compounds described herein for treating fungal or parasitic infections. The compounds can also be used as biological probes to study the effects of inhibiting Gwt1 activity.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: November 29, 2016
    Assignees: Whitehead Institute for Biomedical Research, The General Hospital Corporation
    Inventors: Catherine McLellan, Ralph Mazitschek, Luke Whitesell, Susan L. Lindquist
  • Patent number: 9493432
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, L, X, Ra, Rb, R1, R2 and R3 their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: November 15, 2016
    Assignee: Takeda Pharmaceuticals Company Limited
    Inventors: Charlotte Fieldhouse, Angela Glen, John Stephen Robinson, Tatsuhiko Fujimoto
  • Patent number: 9480744
    Abstract: Methods of inhibiting melanoma tumor growth, methods of treating melanoma and metastatic melanoma, and methods of reducing the frequency of tumor initiating cells (or cancer stem cells) in melanoma tumors are described. The methods described comprise administering a DLL4 antagonist (e.g., an antibody that specifically binds the extracellular domain of human DLL4) to a subject. Related polypeptides and polynucleotides, compositions comprising the DLL4 antagonists, and methods of making the DLL4 antagonists are also described.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: November 1, 2016
    Assignee: OncoMed Pharmaceuticals, Inc.
    Inventors: Timothy C. Hoey, Lucia Beviglia
  • Patent number: 9453038
    Abstract: Novel pyridine-2-carboxamide derivatives of formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: September 27, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Rui Zhang, Brian Campbell, Sunita V. Dewnani, Jiayi Xu, Libo Xu, Emma R. Parmee, Roman Kats-Kagan
  • Patent number: 9403808
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. In particular, the compound may be used as a preferential agonist of Cannabinoid Receptor 2.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: August 2, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Baledi Dhurwasulu, Uwe Grether, Anindya Hazra, Paul Hebeisen, Stephan Roever, Mark Rogers-Evans
  • Patent number: 9382260
    Abstract: The present invention is directed to Buprenorphine Analog compounds of Formula I, II, III, IV or V and including various stereoisomers (such as Formula IA shown below), wherein R1, R3a, R3b, R16, R15, G, Q, X, A and Z are as defined herein. Compounds of the Invention may be useful for preparing medicaments useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors. Compounds of the Invention may be useful for treating Conditions such as pain, constipation, and others modulated by activity of opioid and ORL-1 receptors.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: July 5, 2016
    Assignee: Purdue Pharma L.P.
    Inventors: R. Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Patent number: 9370504
    Abstract: Provided is a pharmaceutical composition that contains a 1,2-dithiolthionederivative, and is effective to prevent and treat a disease caused by overactivity of a liver X receptor? (LXR?) or a sterol response element binding protein (SREBP-1). Specifically, the pharmaceutical composition includes 1,2-dithiolthione derivatives such as 4-methyl-5-(2-pyrazinyl)-1,2-dithiol-3-thione, 3-methyl-1,2-dithiol-3-thione, or 5-(6-methoxypyrazinyl)-4-methyl-1,2-dithiol-3-thione. The pharmaceutical composition is effective for preventing and treating hypertension caused by renin, aldosteronism, adrenoleukodystrophy, glomerulosclerosis, proteinuria, nephropathy, liver steatosis, hypertriglyceridemia or hyperreninemia.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: June 21, 2016
    Assignee: SNU R&DB FOUNDATION
    Inventors: Sang Geon Kim, Sung Hwan Ki, Seong Hwan Hwang