Nitrogen Bonded Directly To Ring Carbon Of The 1,3-diazine Ring Of The Quinazoline Ring System Patents (Class 514/266.4)
  • Patent number: 11524009
    Abstract: The present disclosure provides pharmaceutical combinations comprising at least one spliceosome modulator and at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors. Also provided are methods of treating cancer comprising administering a therapeutically effective amount of at least one spliceosome modulator and a therapeutically effective amount of at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: December 13, 2022
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Daniel Aird, Laura Corson, Ping Zhu, Markus Warmuth, Silvia Buonamici, Peter Gerard Smith, Peter Fekkes
  • Patent number: 11510912
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.
    Type: Grant
    Filed: April 14, 2020
    Date of Patent: November 29, 2022
    Assignee: Novartis AG
    Inventors: Ha-Soon Choi, James Paul Lajiness, Srinivasa Reddy Natala, Bao Nguyen, Hank Michael James Petrassi, Zhicheng Wang
  • Patent number: 11446273
    Abstract: Described is a combination of a prophylactic or therapeutic agent for glaucoma or ocular hypertension, which is useful as a prophylactic or therapeutic agent for glaucoma or ocular hypertension. By combining sepetaprost and a Rho-associated coiled-coil containing protein kinase inhibitor(s), an intraocular pressure lowering action is enhanced as compared with the case where each drug is used alone. As the form of administration, they may be administered concomitantly or may be administered as a combination drug.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: September 20, 2022
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Yasuko Yamamoto, Takazumi Taniguchi
  • Patent number: 11225464
    Abstract: The disclosures herein provide compounds of formula I, formula II, formula III, formula IV, formula V and formula VI or its pharmaceutical acceptable salts, as well as polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of gastrointestinal polyps or its associated complications.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: January 18, 2022
    Assignee: Cellix Bio Private Limited
    Inventor: Mahesh Kandula
  • Patent number: 10953016
    Abstract: The present invention provides a formulation containing the compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or their crystals, with a light-stabilizing substance and a polymer, particularly with one or more of titanium oxide and talc used as the light-stabilizing substance, and hypromellose used as the polymer, which hardly increase the amount of the related substances, and the formulation is hardly colored under light irradiation.
    Type: Grant
    Filed: January 29, 2018
    Date of Patent: March 23, 2021
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Reiji Yokoyama, Satoshi Sakuma, Shohei Aikawa, Hironori Tanaka
  • Patent number: 10947201
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: February 16, 2016
    Date of Patent: March 16, 2021
    Assignee: NEUPHARMA, INC.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Patent number: 10829479
    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: March 5, 2019
    Date of Patent: November 10, 2020
    Assignee: AstraZeneca AB
    Inventors: Jason Kettle, Stuart Pearson, Martin Packer, James Smith, Tudor Grecu
  • Patent number: 10766961
    Abstract: The invention provides for a human antibody that binds to human vascular endothelial growth factor receptor 2, preferably ramucirumab, for the treatment of hepatocellular carcinoma (HCC) in patients having levels of alpha-fetoprotein (AFP) of 1.5×ULN (Upper Limit of Normal) or greater, and as a predictive method for the treatment of HCC in patients having AFP levels of 1.5×ULN or greater.
    Type: Grant
    Filed: August 11, 2015
    Date of Patent: September 8, 2020
    Assignee: ImClone LLC
    Inventors: Paolo B. Abada, Shao-Chun Chang, Yanzhi Hsu, Ling Yang
  • Patent number: 10703746
    Abstract: Compounds of Formula I and Formula II and the pharmaceutically acceptable salts thereof are disclosed The variables A, B, Y, Z, X1, X2, R1-4 and R13-18 are disclosed herein. The compounds are useful for treating cancer disorders, especially those involving mutant IDH1 enzymes. Pharmaceutical compositions containing compounds of Formula I or Formula II and methods of treatment comprising administering compounds of Formula I and Formula II are also disclosed.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: July 7, 2020
    Assignees: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
    Inventors: Matthew Brian Boxer, Jason Matthew Rohde, Rajan Pragani, Li Liu, Mindy Irene Emily Davis, Kyle Ryan Brimacombe, Min Shen, Anton Simeonov, Surendra Karavadhi, Daniel Jason Urban, Ajit Jadhav, Xiaodong Wang, Andrew Louis McIver
  • Patent number: 10689372
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: November 6, 2018
    Date of Patent: June 23, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Patent number: 10556884
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: September 21, 2016
    Date of Patent: February 11, 2020
    Assignee: Syngenta Participations AG
    Inventors: Andrew Edmunds, Pierre Joseph Marcel Jung, Michel Muehlebach, André Jeanguenat, Daniel Emery, Roger Graham Hall, Vikas Sikervar, Jagadish Pabba
  • Patent number: 10548898
    Abstract: Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.
    Type: Grant
    Filed: January 4, 2019
    Date of Patent: February 4, 2020
    Assignees: Gilead Sciences Inc., Institute of Organic Chemistry and Biochemistry of the AS CR, V.V.I.
    Inventors: Ondrej Baszczynski, Milan Dejmek, Yunfeng Eric Hu, Petr Jansa, Eric Lansdon, Richard L. Mackman, Petr Simon
  • Patent number: 10322126
    Abstract: Disclosed are compositions including a solid dispersion comprising a dispersion polymer, a basic low-water solubility active, and an anionic counterion, as well as methods of making and using the compositions.
    Type: Grant
    Filed: August 21, 2017
    Date of Patent: June 18, 2019
    Assignee: Bend Research, Inc.
    Inventors: Warren K. Miller, Michael M. Morgen
  • Patent number: 9957237
    Abstract: Provided is a composition of N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(ethoxy)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide p-toluene sulfonate 1.5 hydrate ?-polymorph. The ?-polymorph has a stable form, a defined melting point, a good chemical stability, and a good endurance to high temperature and light irradiation, and is suitable for pharmaceutical use.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: May 1, 2018
    Assignee: SHENZHEN NEPTUNUS PHARMACEUTICAL RESEARCH INSTITUTE CO., LTD.
    Inventors: Tian Tang, Feng Jin, Yanqing Wang, Jing Wu, Xiarou Liu, Jing'an Yang, Hanlin Feng, Lin Yu
  • Patent number: 9840494
    Abstract: Disclosed are N-[4-(3-chloro-4-fluorophenylamino)-7-(2-methoxyethoxy) quinazolin-6-yl]-2 -[1-(2-methoxyethyl)piperidin-4-ylidene]acetamide and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: December 12, 2017
    Assignee: Tianjin Hemay Oncology Pharmaceutical Co., Ltd.
    Inventors: Hesheng Zhang, Guanghuai Zeng, Yingwei Chen
  • Patent number: 9750741
    Abstract: Methods of selecting a chemotherapy regimen for treatment of cancer in a patient are disclosed. A patient genetic sample from a bilary cancer such as cholangiocarcinoma is analyzed for a mutation in ERRFI1 and a chemotherapeutic agent is selected as a result of the analysis. If a mutation in ERRFI1 is present, treatment with an inhibitor of Epidermal Growth Factor Receptor (EGFR) is shown to have inhibitory effects on tumor growth. In this manner, the chemotherapy regimen is targeted to a given mutation in a patient's cancer.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: September 5, 2017
    Assignees: The Translational Genomics Research Institute, MAYO Foundation for Medical Education and Research
    Inventors: Mitesh Jivraj Borad, David Craig, John Carpten
  • Patent number: 9717792
    Abstract: Combination therapy for cancer makes use of HSP27 inhibitors and EGFR tyrosine kinase inhibitors or etiolates.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: August 1, 2017
    Assignee: The University of British Columbia
    Inventors: Martin E. Gleave, Amina Zoubeidi, Masafumi Kumano
  • Patent number: 9394261
    Abstract: A series of mono- and di-substituted quinazoline and pyrimidine derivatives based on the skeleton of erlotinib (an EGFR inhibitor) were synthesized and their bioactivities against hepatocellular carcinoma and human lung adenocarcinoma were evaluated.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: July 19, 2016
    Assignees: NATIONAL YANG-MING UNIVERSITY, NATIONAL TAIWAN UNIVERSITY
    Inventors: Chung-Wai Shiau, Kuen-Feng Chen
  • Patent number: 9388160
    Abstract: The present invention is directed to novel quinazolines, their derivatives, pharmaceutically acceptable salts, solvates, prodrug, stereoisomer, tautomer, metabolite and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: July 12, 2016
    Assignee: Teligene Ltd
    Inventor: Dawei Zhang
  • Patent number: 9359349
    Abstract: The present invention provides compounds of Formula I that modulate PI3 kinase activity and methods of treatment of diseases and conditions associated with PI3 kinase activity.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: June 7, 2016
    Assignee: INTELLIKINE LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson
  • Patent number: 9187462
    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: Grant
    Filed: August 3, 2012
    Date of Patent: November 17, 2015
    Assignees: Array BioPharma Inc., Genentech, 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 Schwarz, Christopher S. Siedem, Eli M. Wallace
  • Patent number: 9150549
    Abstract: The invention provides A combination of, a) a compound of Formula (I) or a pharmaceutically acceptable salt thereof; and b) erlotinib or a pharmaceutically acceptable salt thereof for the prophylactic or therapeutic treatment of a hyperproliferative disorder, such as cancer.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: October 6, 2015
    Assignee: Genentech, Inc.
    Inventors: Michelle Nannini, Deepak Sampath
  • Patent number: 9073985
    Abstract: Methods and products for treating proliferative diseases, and wounds, using as a pharmacon an autophagy inhibitor, a glycolytic inhibitor, and/or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherapeutic agents. In some embodiments, the invention combines a 4-aminoquinoline, exemplified by chloroquine, with a glycolytic inhibitor, exemplified by 2-deoxy-D-glucose and anti-VEGF antibodies. The systems and methods of the invention may be used to treat drug-resistant or multi-drug resistant cancers.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: July 7, 2015
    Assignee: The Regents of the University of Colorado, a body corporate
    Inventors: Martha Karen Newell, Susannah K. Rogers
  • Patent number: 9067897
    Abstract: 2,4-Diaminoquinazolines of formulae I-IV and VI are useful for treating spinal muscular atrophy (SMA).
    Type: Grant
    Filed: January 20, 2011
    Date of Patent: June 30, 2015
    Assignee: Families of Spinal Muscular Atrophy
    Inventors: Jasbir Singh, Mark E. Gurney
  • 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
  • Publication number: 20150133476
    Abstract: The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof.
    Type: Application
    Filed: November 18, 2014
    Publication date: May 14, 2015
    Inventors: Jianhui Guo, Yong Jiang
  • 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
  • Patent number: 9023354
    Abstract: Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: May 5, 2015
    Inventor: Joseph P. Errico
  • 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
  • Publication number: 20150111847
    Abstract: The present invention relates to processes for the preparation of 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: Application
    Filed: January 6, 2015
    Publication date: April 23, 2015
    Applicant: GENERICS [UK] LIMITED
    Inventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
  • Publication number: 20150112116
    Abstract: Provided herein are methods comprising providing a tyrosine derivative and a solid particulate material (and, optionally, melanin) and applying force to said tyrosine derivative and said solid particulate material for a time and under conditions effective to impregnate at least one of said tyrosine derivative and said solid particulate material with the other of said tyrosine derivative and said solid particulate material. The invention also provides compositions comprising at least one of a tyrosine derivative impregnated with a solid particulate material and a solid particulate material impregnated with a tyrosine derivative.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 23, 2015
    Inventor: STEVEN HOFFMAN
  • Publication number: 20150111907
    Abstract: The invention relates to methods of predicting the clinical outcome of brain cancer patients based on the LOH levels of the PTEN gene and on the expression levels or the polysomy/amplification levels of EGFR gene in a sample from said patients.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Michael J. DONOVAN, Anna Colomer Valero, Nadina Erill Sagales, Isidre Ferrer Abinzanda, Susana Boluda Casas
  • Publication number: 20150105412
    Abstract: Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 16, 2015
    Inventor: Joseph P. Errico
  • 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: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Publication number: 20150086543
    Abstract: The present invention provides methods of predicting response to a cancer therapy based on the methylation status of the ERBB2 gene. One aspect of the invention provides a method of predicting response to an EGFR inhibitor therapy based on the methylation status of the ERBB2 gene.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 26, 2015
    Applicant: GENENTECH, INC.
    Inventors: Thomas E. Januario, David Shames
  • Publication number: 20150079028
    Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
    Type: Application
    Filed: August 5, 2013
    Publication date: March 19, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD
    Inventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo
  • 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: 20150079079
    Abstract: The present invention provides compositions and methods of use in the treatment/prevention of chlamydial infection and/or diseases and disorders associated with chlamydial infection in a subject.
    Type: Application
    Filed: September 11, 2014
    Publication date: March 19, 2015
    Inventors: Allen W. Tsang, Cristina M. Furdui
  • Patent number: 8980321
    Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.
    Type: Grant
    Filed: July 14, 2014
    Date of Patent: March 17, 2015
    Assignee: Bend Research, Inc.
    Inventors: William J. Curatolo, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Douglas A. Lorenz
  • Publication number: 20150071919
    Abstract: The present application relates to compositions and methods for treating a proliferative disorder by administering to a subject a pharmaceutical composition of a dual kinase inhibitor. Catecholic butanes cane serve as dual kinase inhibitors for purposes of methods described herein. Patients to be treated include those that have been treated with Tarceva or other therapeutic compounds and relapsed or are resistant to treatment. The compounds described herein may exhibit a synergistic effect when administered with another agent.
    Type: Application
    Filed: September 9, 2014
    Publication date: March 12, 2015
    Inventors: Thomas F. WHITE, Dan HOTH
  • Publication number: 20150065526
    Abstract: This disclosure relates to methods of treating cancer comprising administering an effective amount of a STAT3 inhibitor, prodrugs, or derivatives thereof, in combinations with an EGFR tyrosine kinase inhibitors, prodrugs, or derivatives thereof, to a subject in need thereof. In certain embodiments, the STAT3 inhibitor is niclosamide or salt thereof. In certain embodiments, the EGFR tyrosine kinase inhibitor is erlotinib or salt thereof.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 5, 2015
    Inventors: Xingming Deng, Rui Li, Fadio R. Khuri, Taofeek Kunle Owonikoko
  • Publication number: 20150057275
    Abstract: This invention relates generally to methods and materials for rapid detection of mutations for tumor genotyping.
    Type: Application
    Filed: September 2, 2014
    Publication date: February 26, 2015
    Inventors: Dora Dias-Santagata, Anthony John Iafrate
  • Publication number: 20150057267
    Abstract: The invention provides a method for treating viral infections and coinfections through the use of inhibitory agents that prevent a unique viral structural protein motifs from binding to host proteins from the clathrin adaptor proteins family and subsequently preventing viral replication.
    Type: Application
    Filed: December 6, 2012
    Publication date: February 26, 2015
    Applicant: The Board of Trustees of the Leland Stanford Junior university
    Inventors: Shirit Einav, Rina Barouch-Bentov, Gregory Neveu, Amotz Zivav
  • Publication number: 20150056193
    Abstract: The present disclosure provides methods of that include detecting in a biological sample from a patient having or suspected of having cancer the presence of a polypeptide having ROS1 kinase activity or a polynucleotide encoding the same and detecting in the biological sample the presence of a mutant EGFR polypeptide or a polynucleotide encoding the same. In some aspects, the disclosure provides methods of treating a patient for cancer that include determining that a biological sample from a tumor in the patient includes a polypeptide having ROS1 kinase activity or a polynucleotide encoding the same and a mutant EGFR polypeptide or a polynucleotide encoding the same and administering to the patient a therapeutically effective amount of a ROS1 inhibitor and an EGFR inhibitor, thereby treating the patient for cancer.
    Type: Application
    Filed: April 18, 2013
    Publication date: February 26, 2015
    Applicant: CELL SIGNALING TECHNOLOGY, INC.
    Inventors: Katherine Eleanor Crosby, Victoria McGuinness Rimkunas, Matthew Ren Silver, Herbert Haack
  • Publication number: 20150050239
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 19, 2015
    Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Publication number: 20150045363
    Abstract: Hedgehog pathway inhibitors, such as small molecules, are used to prevent, slow, block the formation of cartilage tumors as well as exostosis or enchondromas.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 12, 2015
    Inventors: Wentian Yang, Benjamin G. Neel
  • Publication number: 20150038520
    Abstract: The invention relates to methods for determining the clinical outcome of patients suffering lung cancer and being under treatment with an EGFR inhibitor. The methods are based on the detection of the presence of mutations in the EGFR gene conferring resistance to inhibitors of the EGFR tyrosine kinase activity, wherein the appearance of said mutations in the biofluid of the patient is indicative of a high probability that the patient suffers a relapse of the disease. The invention also provides therapeutic methods for said patients.
    Type: Application
    Filed: December 22, 2011
    Publication date: February 5, 2015
    Applicant: Pangaea Biotech S.L.
    Inventors: Miguel Tarón Roca, Rafael Rosell Costa
  • Publication number: 20150030588
    Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.
    Type: Application
    Filed: November 12, 2012
    Publication date: January 29, 2015
    Inventors: Katayoun Jessen, Xin Guo, Pingda Ren, Christian Rommel, Yi Liu
  • Publication number: 20150031695
    Abstract: Small molecule compounds for the treatment of inflammatory conditions, and pharmaceutical compositions and methods relating thereto. The compositions may be used for the treatment of conditions such as multiple sclerosis, type 2 diabetes, psoriasis, rheumatoid arthritis, Hashimoto's thyroiditis, and Crohn's disease. In some embodiments, the pharmaceutical composition and methods pertain to small molecule compounds previously known for the treatment of another condition, such as non-small-cell lung cancer (NSCLC).
    Type: Application
    Filed: May 12, 2014
    Publication date: January 29, 2015
    Inventor: Michael West Brooks