Additional Nitrogen Containing Unsaturated Hetero Ring (e.g., Thiazole, Etc.) Patents (Class 544/284)
  • Patent number: 10640470
    Abstract: Disclosed are crystal forms K, E, F and G of the dimaleate of the compound as shown in formula I, and preparation methods and uses thereof. The crystal forms K, E, F and G have superior storage stability and solubility, so that they are more suitable for being used as the drug substance for drug product preparations.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: May 5, 2020
    Assignee: HANGZHOU HUADONG MEDICINE GROUP BIOPHARMACEUTICAL CO. LTD.
    Inventors: Yubin Lv, Jianming Yin, Xuehui Huang, Bangliang Li
  • Patent number: 10556906
    Abstract: [Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.
    Type: Grant
    Filed: June 5, 2019
    Date of Patent: February 11, 2020
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Kazuyuki Kuramoto, Michinori Akaiwa, Tomoaki Abe, Takanobu Araki, Susumu Yamaki, Shigeki Kunikawa, Tomoyoshi Imaizumi, Takahiro Nigawara, Keisuke Arakawa, Itsuro Shimada, Masashi Shimazaki, Yoshiki Satake, Kazushi Watanabe, Takanori Koike
  • Patent number: 10273227
    Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their preparation; pharmaceutical compositions containing them and their use in treating KIT mediated diseases.
    Type: Grant
    Filed: April 26, 2018
    Date of Patent: April 30, 2019
    Assignee: AstraZeneca AB
    Inventors: Jason Kettle, Stuart Pearson, Martin Packer, James Smith
  • Patent number: 10221194
    Abstract: The invention relates to compounds of Formula 11, and to pharmaceutically acceptable acid addition salts thereof, wherein R1—R3, R6, and X have any of the values defined in the specification. The compounds are suitable as synthetic intermediates for preparing imaging tools.
    Type: Grant
    Filed: May 26, 2017
    Date of Patent: March 5, 2019
    Assignee: Array BioPharma Inc.
    Inventors: Eli Wallace, Joseph Lyssikatos, George Topalov, Alexandre Buckmelter, Qian Zhao
  • Patent number: 10065931
    Abstract: Disclosed are crystal forms K, E, F and G of the dimaleate of the compound as shown in formula I, and preparation methods and uses thereof. The crystal forms K, E, F and G have superior storage stability and solubility, so that they are more suitable for being used as the drug substance for drug product preparations.
    Type: Grant
    Filed: May 3, 2016
    Date of Patent: September 4, 2018
    Assignee: HANGZHOU HUADONG MEDICINE GROUP BIOPHARMACEUTICAL CO. LTD.
    Inventors: Yubin Lv, Jianming Yin, Xuehui Huang, Bangliang Li
  • Patent number: 9997723
    Abstract: The present invention relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. By using the organic electroluminescent compound according to the present invention, it is possible to produce an organic electroluminescent device having low driving voltage, excellent current and power efficiencies, and noticeably improved driving lifespan.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: June 12, 2018
    Assignee: Rohm and Haas Electronic Materials Korea Ltd
    Inventors: Hee-Ryong Kang, Hyun-Ju Kang, Jin-Ri Hong, Doo-Hyeon Moon, Young-Mook Lim, Bitnari Kim, Nam-Kyun Kim, Mi-Ja Lee
  • Patent number: 9862703
    Abstract: Heterocyclic compounds of Formula (I) shown herein. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer, inflammatory disease, and autoimmune disease with the heterocyclic compounds.
    Type: Grant
    Filed: September 21, 2015
    Date of Patent: January 9, 2018
    Assignee: National Health Research Institutes
    Inventors: Kak-Shan Shia, Jiing-Jyh Jan, Lun Kelvin Tsou, Chiung-Tong Chen, Yu-Sheng Chao
  • Patent number: 9833453
    Abstract: Described herein are compounds of Formula (I)-(III), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating and/or preventing diseases are also provided.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: December 5, 2017
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, Ben C. Askew, Jinsoo Kim
  • Patent number: 9822110
    Abstract: Provided is a sulfonamide derivative represented by the following general formula (1) and having an ?4 integrin inhibitory effect with high selectivity with a low effect on ?4?1 and a high effect on ?4?7, or a pharmaceutically acceptable salt thereof (in the general formula (1), A, B, D, E, R41, and a to h are as described in the description).
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: November 21, 2017
    Assignee: EA Pharma Co., Ltd.
    Inventors: Hirokazu Ueno, Takashi Yamamoto, Tomoko Miyazawa, Kenji Shinkai, Harumi Arisaka, Toshiyuki Takanohashi
  • Patent number: 9714234
    Abstract: Disclosed are compounds of Formula (I); and salts thereof, wherein: Formula (II); Q is: R1 is —C(CH3)2OH, —NHC(=0)C(CH3)3, —N(CH3)2, or —CH2Rd; R2 is CI or —CH3; R3 is H, F, or —CH3; Ra is H or —CH3; Rb is H, F, CI, or —OCH3 Rc is H or F; and Rd is —OH, —OCH3, —NHC(=0)CH3, or fORMULA (III), Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: July 25, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Soo Sung Ko, Douglas G Batt, Myra Beaudoin Bertrand, George Delucca, Charles M. Langevine, Qingjie Liu, Anurag S. Srivastava, Scott Hunter Watterson
  • Patent number: 9676791
    Abstract: This invention provides quinazoline analogs of Formula I: where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: June 13, 2017
    Assignee: Array BioPharma Inc.
    Inventors: Eli Wallace, George Topalov, Joseph Lyssikatos, Alexandre Buckmelter, Qian Zhao
  • Patent number: 9675615
    Abstract: Use of 2,3-dihydroquinazolin-4(1H)-one cyclic derivatives of formula (I) for the treatment of infection with viruses entering cells by endocytosis, especially filovirus such as Ebolavirus.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: June 13, 2017
    Assignees: Commissariat a l'Energie Atomique et aux Energies Alternatives, The Board of Regents of the University of Texas System
    Inventors: Daniel Gillet, Julien Barbier, Robert Davey, Jean-Christophe Cintrat, Romain Noel
  • Patent number: 9527865
    Abstract: This invention provides quinazoline analogs of Formula I: where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: December 27, 2016
    Assignee: Array BioPharma Inc.
    Inventors: Eli Wallace, George Topalov, Joseph Lyssikatos, Alexandre Buckmelter, Qian Zhao
  • Patent number: 9518046
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
    Type: Grant
    Filed: March 15, 2015
    Date of Patent: December 13, 2016
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Liang Wang, Zuping Wu, Xuejin Feng, Yanjun Wu
  • Patent number: 9221795
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts or isomers thereof, in which n, m, R1, R2, R4, and R3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts or isomers thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: December 29, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Jerry Evarts, Joshua Kaplan, Musong Kim, Leena Patel, Stephane Perreault, Gary Phillips, Jennifer A. Treiberg, Joshua Van Veldhuizen
  • Patent number: 9199969
    Abstract: A series of new 6-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones have been synthesized. The compounds are structurally related to adoprazine, a potential atypical antipsychotics bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling of suitably modified aryl bromides with tert-butyl piperazine-1-carboxylate afforded the advanced intermediate piperazinyl-3,4-dihydroquinazolin-2(1H)-one. The reductive amination of the latter with appropriately designed biarylaldehydes accomplished the synthesis of these compounds.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: December 1, 2015
    Assignees: King Fahd University of Petroleum and Minerals, King Abdulaziz City for Science and Technology
    Inventor: Nisar Ullah
  • Patent number: 9040548
    Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3, wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3, wherein R3 is as defined herein; 3) C2-5alkynylR3, wherein R3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: January 3, 2014
    Date of Patent: May 26, 2015
    Assignee: AstraZeneca AB
    Inventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
  • Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • Publication number: 20150141400
    Abstract: The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 21, 2015
    Inventors: Takeshi Murata, Hatsuo Kawada, Satoshi Niizuma, Sousuke Hara, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Toshiyuki Mio
  • Publication number: 20150141443
    Abstract: Provided herein is an optically active pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.
    Type: Application
    Filed: November 18, 2014
    Publication date: May 21, 2015
    Inventors: Mark W. HOLLADAY, Eduardo SETTI
  • Publication number: 20150140104
    Abstract: Described herein are polymeric nanoparticles that include a therapeutic agent which is 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide (also known as AZD1152 hqpa) or a pharmaceutically acceptable salt thereof, and methods of making and using such therapeutic nanoparticles.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 21, 2015
    Applicant: ASTRAZENECA AB
    Inventors: Marianne Bernice ASHFORD, James Martin NOLAN III, Eyoung SHIN, Young-Ho SONG, Greg TROIANO, Hong WANG
  • Publication number: 20150141442
    Abstract: Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described.
    Type: Application
    Filed: September 19, 2014
    Publication date: May 21, 2015
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson
  • Patent number: 9034886
    Abstract: The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: May 19, 2015
    Assignees: Shanghai Institute of Pharmaceutical Industry, Jiangsu Hengyi Pharmaceutical Co., Ltd.
    Inventors: Jianqi Li, Qingwei Zhang, Wangping Cai
  • Publication number: 20150133439
    Abstract: The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
    Type: Application
    Filed: July 9, 2014
    Publication date: May 14, 2015
    Inventors: Anjali Pandey, Robert M. Scarborough, Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shinichi Ide, Eiji Tsukuda, Junko Sasaki, Shoji Oda
  • Publication number: 20150133662
    Abstract: The present invention relates to novel organic electroluminescent compounds and an organic electroluminescent device comprising the same. The organic electroluminescent compounds according to the present invention have high luminescent efficiency and a long lifespan, and thus an organic electroluminescent device having a long operating lifespan can be prepared by using the organic electroluminescent compounds according to the present invention.
    Type: Application
    Filed: June 12, 2013
    Publication date: May 14, 2015
    Inventors: Hee-Choon Ahn, Young-Jun Cho, Bong-Ok Kim, Nam-Kyun Kim, Jong-Seok Ku, Hyuck-Joo Kwon, Doo-Hyeon Moon
  • Patent number: 9029384
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which n, m, R1, R2, and R3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: May 12, 2015
    Assignee: Gilead Calistoga, LLC.
    Inventors: Jerry Evarts, Leena Patel, Joshua Kaplan, Jennifer A. Treiberg, Stephane Perreault, Gary Phillips
  • Publication number: 20150126537
    Abstract: The present invention is directed to novel bicyclic compounds, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions. Novel bicyclic compounds disclosed herein include quinazolines and quinolines.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Inventor: Dawei Zhang
  • Publication number: 20150119405
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: October 23, 2014
    Publication date: April 30, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Patent number: 9018221
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: April 28, 2015
    Assignee: Gilead Calistoga, LLC
    Inventors: Jerry Evarts, Leena Patel, Jennifer A. Treiberg, Stephane Perreault, Arthur Yeung, Lafe J. Purvis, II, Musong Kim
  • Publication number: 20150110723
    Abstract: The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.
    Type: Application
    Filed: May 28, 2013
    Publication date: April 23, 2015
    Applicant: EMORY UNIVERSITY
    Inventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
  • Publication number: 20150111874
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 23, 2015
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Martin R. TREMBLAY
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor 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: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Patent number: 9006255
    Abstract: Compounds of the formula I in which R, X, L2 and A1-A6 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Patent GmbH
    Inventor: Markus Klein
  • Patent number: 9006257
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: April 14, 2015
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram Gharat, Abhisek Banerjee, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Publication number: 20150094467
    Abstract: The dihydroquinone derivatives of piperidine and piperazine are 7-piperazinyl and 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones that exhibit D2 and 5-HT1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: where X is carbon or nitrogen and R is a group selected from a through f having the formula: or a pharmaceutically acceptable salt thereof. The piperazine compounds are prepared by condensing 4-bromo-2-nitro-benzonitrile with 1-Boc-piperazine (1-tert-butoxycarbonyl-piperazine) to form an intermediate that is converted to a piperazinyl-3,4-dihydroquinazolin-2(1H)-one. Subsequent reductive amination with the biarylaldehydes a through f completes the synthesis of the 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones.
    Type: Application
    Filed: November 17, 2014
    Publication date: April 2, 2015
    Inventor: NISAR ULLAH
  • Patent number: 8993595
    Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Michel Derock, Frederic Leroy, Jean-Christophe Meillon, Thierry Convard, Dominique Surleraux
  • Publication number: 20150087664
    Abstract: Compounds having the formula (I) wherein R1, R2, R3 and Ar as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
    Type: Application
    Filed: August 3, 2012
    Publication date: March 26, 2015
    Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.
    Inventors: James F. Blake, Huifen Chen, Mark Joseph Chicarelli, Jason Demeese, Rustam Ferdinand Garrey, John Gaudino, Lewis Gazzard, Robert J. Kaus, Samuel Kintz, Peter J. Mohr, David A. Moreno, Jacob Schwartz, Christopher S. Siedem, Eli M. Wallace
  • Publication number: 20150087663
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not limited to leukemias and solid tumors, in mammals, especially humans.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 26, 2015
    Applicants: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLC
    Inventors: Ning Xi, Liang Wang, Zuping Wu, Xuejin Feng, Yanjun Wu
  • Patent number: 8987284
    Abstract: Disclosed are novel quinazoline derivatives containing phosphorus substitutions and methods for the treatment of hyperproliferative diseases (e.g. cancer) using the compounds. These compounds are type I receptor protein kinase inhibitors useful in treating disorders related to abnormal protein kinase activities such as cancer and inflammation in mammals. Also disclosed are pharmaceutical compositions containing the compounds, methods for the preparation of the compounds and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: March 24, 2015
    Assignee: Newgen Therapeutics, Inc.
    Inventors: Wang Shen, Aimin Zhang, Junfa Fan, Xiaoling Zheng
  • Patent number: 8987285
    Abstract: The present invention relates to a novel crystalline anhydrous form of [(5-chlorothiophene-2-ylsulfonylcarbamoyl)-(4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)phenyl)amide, potassium salt, and its use in the treatment or prevention of a condition or a disorder with platelet ADP receptor inhibition, in particular, P2Y12 inhibition, in animals, particularly humans. It also relates processes for making such a novel crystalline form. The present invention also relates to a solid, oral formulation of this novel crystalline form, its preparation and use thereof.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: March 24, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Ulrich Meier, Nicole Bieri, Dieter Becker, Julien Taillemite, Marie-Pierre Filliot, Tanja Meister
  • Publication number: 20150080409
    Abstract: Embodiments of the present disclosure, in one aspect, relate to a 2,4-diaminoquinazoline compound, pharmaceutical compositions including a 2,4-diaminoquinazoline compound, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
    Type: Application
    Filed: October 31, 2014
    Publication date: March 19, 2015
    Applicant: University of South Florida (A Florida Non-Profit Corporation)
    Inventors: Roman Manetsch, Lindsey Neil Shaw, Kurt Steven Van Horn, Whittney Nicole Burda
  • Publication number: 20150060833
    Abstract: The present specification provides a novel compound that is capable of largely improving an expected life span, efficiency, electrochemical stability, and thermal stability of an organic electronic device, and an organic electronic device that includes an organic material layer including the compound.
    Type: Application
    Filed: September 24, 2014
    Publication date: March 5, 2015
    Inventors: Hyok Joon KWON, Kidong KOO, Kongkyeom KIM, Minjun KIM, Seong So KIM, Hyoung Seok KIM, Hyoungcheul KIM, Sang Young JEON, Heungwoo CHOI
  • Publication number: 20150065709
    Abstract: The invention discloses a new amino-quinazoline derivative and its use in preparing drugs for preventing and/or treating malignancies. The amino-quinazoline derivative of the invention is an ideal, high effective, dual and irreversible EGFR and HER2 kinase inhibitor, and can treat or prevent various malignancy diseases, such as breast cancer, ovarian cancer, gastrointestinal cancer, oesophageal cancer, lung cancer, head and neck squamous cancer, pancreatic cancer, epidermis squamous cell cancer, prostatic cancer, neuroglioma and nasopharynx cancer.
    Type: Application
    Filed: March 13, 2013
    Publication date: March 5, 2015
    Inventors: Jianming Yin, Junhua Tao
  • Patent number: 8969325
    Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: March 3, 2015
    Assignee: AbbVie Inc.
    Inventors: Michael J. Dart, Philip R. Kym, Eric A. Voight, Anurupa Shrestha, Jerome F. Daanen, Tammie K. Jinkerson, Ryan G. Keddy, Sridhar Peddi, Arthur Gomtsyan, Michael E. Kort, Gregory A. Gfesser, Kevin R. Woller, Derek W. Nelson
  • Publication number: 20150057218
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 26, 2015
    Inventors: Min ZHONG, Leping LI
  • Patent number: 8962835
    Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 24, 2015
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • 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
  • Patent number: 8957073
    Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: February 17, 2015
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
  • Publication number: 20150045323
    Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.
    Type: Application
    Filed: September 13, 2013
    Publication date: February 12, 2015
    Inventors: Linda N. Casillas, Pamela A. Haile, Robert W. Marquis, JR., Gren Wang
  • Patent number: 8952022
    Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: February 10, 2015
    Assignee: Generics [UK] Limited
    Inventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav