Additional Six-membered Hetero Ring Consisting Of Five Ring Carbons And One Ring Nitrogen Attached Directly Or Indirectly To The 1,3-diazine By Nonionic Bonding Patents (Class 514/252.18)
  • Patent number: 11103481
    Abstract: The present invention relates to treatment of cancer, in particular to methods of sensitising cancer cells to an anti-cancer therapy by administering an effective amount of a modulator of Volume Regulated Anion Channels, i.e. a VRAC modulator.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: August 31, 2021
    Assignee: Scandion Oncology A/S
    Inventors: Nils Aage Brünner, Palle Christophersen, Jan Stenvang, Jens Lichtenberg, Annemette Thougaard
  • Patent number: 11091508
    Abstract: Provided are a fosaprepitant phosphate intermediate (IV) preparation method, a fosaprepitant phosphate intermediate (IV-A) and a method of (AA) for preparing fosaprepitant dimeglumine by using the intermediate (IV-A). IV: R1 and R2 are independently selected from C1-C7 alkyl groups or benzyl groups; IV-A: R1 and R2 are independently selected from C1-C7 alkyl groups, and R1 and R2 are not both benzyl groups.
    Type: Grant
    Filed: May 9, 2017
    Date of Patent: August 17, 2021
    Assignees: SHANGHAI AOBO PHARMTECH, INC., LTD., ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
    Inventors: Jicheng Zhang, Zeng Li, Luning Huang, Qian Chen, Anping Tao, Hong Gu
  • Patent number: 10912820
    Abstract: A method for selecting an immunomodulatory kit, selected for an individual patient, for use in the treatment of patients suffering from myeloid leukemias. Different kits are available for selection and ex vivo testing which are composed of substances that have different immunomodulatory effects on leukemia cells. Each kit particularly contains GM-CSF and one (or two) more substances, selected from PICIBANIL, PGE1, PGE2, CALCIMYCIN and TNF?, as well as pharmaceutically acceptable adjuvants. The clinical aim is to modify, once the individually selected immunomodulatory kits were administered, blast cells in the body of the patient such that they turn into a “vaccine” which is able to activate the immunoreactive cells (of the patient or of the stem cell donor) in the body against blast cells.
    Type: Grant
    Filed: April 18, 2018
    Date of Patent: February 9, 2021
    Assignee: Modiblast Pharma GmbH
    Inventor: Helga Schmetzer
  • Patent number: 10906896
    Abstract: The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.
    Type: Grant
    Filed: June 26, 2019
    Date of Patent: February 2, 2021
    Assignee: Inhibikase Therapeutics, Inc.
    Inventors: Milton H. Werner, Terence A. Kelly
  • Patent number: 10829488
    Abstract: The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X1, X2, X3 R1a, R1b E, and = are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition such as cancer.
    Type: Grant
    Filed: August 4, 2017
    Date of Patent: November 10, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Jianyong Chen
  • Patent number: 10774146
    Abstract: Provided herein are methods and uses involving antibodies that specifically bind to a KIT receptor tyrosine kinase for managing, treating, or preventing an eosinophil or mast cell related disorder and/or one or more symptoms thereof, for example a mast cell related disorder of the nervous system, e.g., central nervous system, for example neuromyelitis optica (NMO), neuromyelitis optica spectrum disorder (NMOSD), multiple sclerosis (MS), and neurofibromatosis (NF).
    Type: Grant
    Filed: February 7, 2019
    Date of Patent: September 15, 2020
    Assignee: Celldex Therapeutics, Inc.
    Inventors: Theresa Marie LaVallee, Gerald McMahon
  • Patent number: 10350211
    Abstract: The present disclosure is generally directed to bumped kinase inhibitor (BKI) compositions and methods for treating cancer.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: July 16, 2019
    Assignee: UNIVERSITY OF WASHINGTON
    Inventors: Wesley C. Van Voorhis, Erkang Fan, Dustin James Maly, Kayode K. Ojo, Stephen R. Plymate, Rama Subba Rao Vidadala
  • Patent number: 10239943
    Abstract: Provided herein are methods and uses involving antibodies that specifically bind to a KIT receptor tyrosine kinase for managing, treating, or preventing an eosinophil or mast cell related disorder and/or one or more symptoms thereof, for example a mast cell related disorder of the nervous system, e.g., central nervous system, for example neuromyelitis optica (NMO), neuromyelitis optica spectrum disorder (NMOSD), multiple sclerosis (MS), and neurofibromatosis (NF).
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: March 26, 2019
    Assignee: Celldex Therapeutics, Inc.
    Inventors: Theresa Marie LaVallee, Gerald McMahon
  • Patent number: 10092569
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: October 9, 2018
    Assignee: PRINCIPIA BIOPHARMA INC.
    Inventors: Mohammad Reza Masjedizadeh, Steven Gourlay
  • Patent number: 10076520
    Abstract: The present invention provides methods for reducing apoptosis of non-cancerous cells during a cancer treatment and beneficial effects associated with reducing such apoptosis. In particular, methods of the invention comprise administering a tyrosine kinase inhibitor to a cancer patient who is undergoing cancer treatment in order to reduce apoptosis of non-cancerous cells.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: September 18, 2018
    Assignee: The Regents of the University of Colorado, a body corporate
    Inventors: Mary E. Reyland, Sten Wie, James DeGregori
  • Patent number: 10030012
    Abstract: The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: July 24, 2018
    Assignee: Heptares Therapeutics Limited
    Inventors: David Livermore, Kathryn White, Miles Congreve, Giles Brown, Michael O'Brien
  • Patent number: 9890167
    Abstract: The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R4 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: February 13, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Taishan Hu, Xingchun Han, Buyu Kou, Hong Shen, Shixiang Yan, Zhisen Zhang
  • Patent number: 9877934
    Abstract: A pharmaceutically acceptable composition and method for leukemia therapy in a patient in need of such therapy. The composition contains, as the only active agents, the combination of (a) an inhibitor of c-Fos, (b) an inhibitor of Dusp-1, and (c) an inhibitor of BCR-ABL tyrosine kinase. The composition is administered to the patient in a dosing regimen for a period sufficient to provide therapy for leukemia.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: January 30, 2018
    Assignee: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventors: Mohammad Azam, Meenu Kesarwani
  • Patent number: 9868739
    Abstract: This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salt(s) thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
    Type: Grant
    Filed: October 20, 2015
    Date of Patent: January 16, 2018
    Assignee: Novartis AG
    Inventors: John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
  • Patent number: 9796701
    Abstract: The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: October 24, 2017
    Assignee: XUANZHU PHARMA CO., LTD.
    Inventors: Frank Wu, Bo Chen
  • Patent number: 9750700
    Abstract: The invention relates to an oral pharmaceutical composition comprising, greater than 80% of Imatinib, by weight based on the total weight of the composition and the process for preparation thereof.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: September 5, 2017
    Assignee: Natco Pharma Limited
    Inventors: Kali Satya Bhujanga Rao Adibhatla, Venkaiah Chowdary Nannapaneni
  • Patent number: 9623015
    Abstract: Provided are methods for eliminating hematologic cancer stem cells in vivo, and thus preventing cancer relapse. The methods comprise a Signal Transducer and Activator of Transcription 5 (STAT5) antagonist (e.g., a PPAR? agonist) after the patient has had ana initial course of treatment with an anti-cancer agent (e.g., a TKI), to eliminate residual cancer stem cells which cause relapse.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: April 18, 2017
    Assignee: Commissariat à L'Energie Atomique et aux Energies Alternatives (CEA)
    Inventors: Stéphane Prost, Marek Kirszenbaum, Mikael Le Dantec, Philippe Rousselot, Philippe Leboulch
  • Patent number: 9533980
    Abstract: The present invention features a method for determining the prognosis for survival of a cancer patient. Methods for measuring the level of NOL3 expression in a cancer cell-containing sample from a patient, and comparing the level of NOL3 expression in the sample to a reference level of NOL3 expression are also included. A higher level of NOL3 relative to the reference level correlates with decreased survival of the patient, and an equivalent or lower level of NOL3 relative to the reference level correlates with increased survival of the patient.
    Type: Grant
    Filed: August 20, 2014
    Date of Patent: January 3, 2017
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Andrew Kung, David Ziegler
  • Patent number: 9364477
    Abstract: The invention provides the identification of the presence of mutant ROS protein in human cancer. In some embodiments, the mutant ROS are FIG-ROS fusion proteins comprising part of the FIG protein fused to the kinase domain of the ROS kinase. In some embodiments, the mutant ROS is the overexpression of wild-type ROS in cancerous tissues (or tissues suspected of being cancerous) where, in normal tissue of that same tissue type, ROS is not expressed or is expressed at lower levels. The mutant ROS proteins of the invention are anticipated to drive the proliferation and survival of a subgroup of human cancers, particularly in cancers of the liver (including bile duct), pancreas, kidney, and testes. The invention therefore provides, in part, isolated polynucleotides and vectors encoding the disclosed mutant ROS polypeptides (e.g., a FIG-ROS(S) fusion polypeptide), probes for detecting it, isolated mutant polypeptides, recombinant polypeptides, and reagents for detecting the fusion and truncated polypeptides.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: June 14, 2016
    Assignee: Cell Signaling Technology, Inc.
    Inventors: Ting-Lei Gu, Meghan Ann Tucker, Herbert Haack, Katherine Eleanor Crosby, Victoria McGuinness Rimkunas
  • Patent number: 9359401
    Abstract: The present invention relates to a peptide analog or a pharmaceutically acceptable salt thereof with excellent moisturizing effect, and use thereof for moisturization. More specifically, the present invention relates to a novel peptide analog or a pharmaceutically acceptable salt thereof, a method for preparation thereof, a moisturizing cosmetic composition comprising the same as an active ingredient, and a pharmaceutical composition for prevention and treatment of xeroderma.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: June 7, 2016
    Assignee: INCOSPHARM CORPORATION
    Inventors: Kee-Don Park, Chae-Jin Lim, Seok-Jeong Yoon, Seon-Deok Kwon
  • Patent number: 9345704
    Abstract: Germline mutations in the NF1 tumor suppressor gene cause Von Recklinghausen's neurofibromatosis type 1 (NF1), a common genetic disorder of the nervous system characterized by plexiform neurofibroma development. Using adoptive transfer of hematopoietic cells, we establish that NF1 heterozygosity of bone marrow derived cells in the tumor microenvironment is sufficient to allow neurofibroma progression in the context of Schwann cell nullizygosity. Further, genetic or pharmacologic attenuation of the c-kit signaling pathway in hematopoietic cells greatly diminishes neurofibroma initiation and progression. These studies identify haploinsufficient hematopoietic cells and the c-kit receptor as therapeutic targets for preventing plexiform neurofibromas and implicate mast cells as critical mediators of tumor initiation.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: May 24, 2016
    Assignee: Indiana University Research and Technology Corporation
    Inventors: D. Wade Clapp, David Ingram, Feng-Chun Yang
  • Patent number: 9266895
    Abstract: The present disclosure provides compounds of Formula (IA) and or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: February 23, 2016
    Assignee: Principia Biopharma Inc.
    Inventors: Tim Owens, Erik Verner
  • Patent number: 9174982
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: November 3, 2015
    Assignees: ABBVIE INC., GENENTECH, INC., THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert A. Mantei, Todd M. Hansen
  • Patent number: 9119769
    Abstract: The present invention provides gas-induced method for phase-transforming organic solids, such as pharmaceutical crystals. The inventive method subjects the polymorphs of pharmaceutical agents to various pressures of gases (such as CO2, N2O, and CH4) to induce phase transform with ease.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: September 1, 2015
    Assignee: The Curators of the University of Missouri
    Inventors: Jerry Lee Atwood, Jian Tian, Scott John Dagarno
  • Patent number: 9119862
    Abstract: Compositions, kits and methods for treating leukemia in a subject (e.g., human) include a first anti-cancer drug consisting of: ?12-prostaglandin J3 or a derivative thereof, or a prostaglandin D receptor (DP) agonist. The compositions may further include a second anti-cancer drug. ?12-prostaglandin J3 is a stable metabolite of omega-3 fatty acid, eicosapentaenoic acid (EPA), and was discovered to have anti-leukemic properties. ?12-prostaglandin J3 was shown to be highly effective in eradicating the leukemia stem cells (LSC) in two murine models of leukemia, thus increasing the survival of the mice. DP agonists were shown to induce apoptosis of human primary Acute Myelogenous Leukemia cells and may be used in compositions, kits and methods for treating leukemia in a subject. The compositions, kits and methods may be particularly useful for treating human subjects who are resistant to one or more anti-cancer drugs.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: September 1, 2015
    Assignee: The Penn State Research Foundation
    Inventors: Kumble Sandeep Prabhu, Robert Frank Paulson, Shailaja Hegde, Naveen Kaushal, Ujjawal Hitendra Gandhi
  • Patent number: 9095622
    Abstract: The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, non-peptidic oligomer.
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: August 4, 2015
    Assignee: NEKTAR THERAPEUTICS
    Inventors: Jennifer Riggs-Sauthier, Wen Zhang
  • Patent number: 9062023
    Abstract: The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (Q) or (I), which penetrate the blood-brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system.
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: June 23, 2015
    Assignee: Intra-Cellular Therapies, Inc.
    Inventor: Peng Li
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Patent number: 9040538
    Abstract: The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: May 26, 2015
    Assignee: Universite Laval
    Inventors: Giorgio Attardo, Sasmita Tripathy, Martin Gagnon
  • Publication number: 20150141427
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150141403
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: December 1, 2014
    Publication date: May 21, 2015
    Inventors: Jose Maria CID-NUNEZ, Daniel OEHLRICH, Andres Avelino TRABANCO-SUAREZ, Gary John TRESADERN, Juan Antonio VEGA RAMIRO, Gregor James MACDONALD
  • Patent number: 9034875
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: May 19, 2015
    Assignee: ABBVIE INC.
    Inventors: George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Andrew J. Souers, Zhi-Fu Tao, Gary T. Wang, Le Wang, Robert Mantei, Todd M. Hansen
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Publication number: 20150133462
    Abstract: In one aspect, the invention relates to compositions comprising BCR-ABL tyrosine kinase inhibitors and artemisinin analogues, derivatives thereof, or related compounds, which are useful as in treating Philadelphia chromosome positive leukemias; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with BCR-ABL 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: Application
    Filed: May 23, 2013
    Publication date: May 14, 2015
    Inventors: Harpreet Singh, Richard T. Williams, Kiplin R. Guy
  • Publication number: 20150133458
    Abstract: Disclosed are compositions and methods useful for oral delivery of targeted therapies for pulmonary diseases, fibrotic disorders and cancer. The compositions and methods are based on peptide sequences that selectively bind to and home to diseased tissue and enable targeted therapies to affect a beneficial therapeutic result. The disclosed targeting is useful for oral delivery of therapeutic and detectable agents to diseased tissue in an animal.
    Type: Application
    Filed: March 11, 2013
    Publication date: May 14, 2015
    Inventor: David M. Mann
  • Publication number: 20150133463
    Abstract: Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (1R,2S,5R)-(?)-menthol.
    Type: Application
    Filed: June 13, 2013
    Publication date: May 14, 2015
    Applicant: BASF SE
    Inventors: Tiziana Chiodo, Andreas Hafner, Tobias Hintermann, Beate Salvador, Martin Szelagiewicz, Fritz Blatter, Bernd Siebenhaar, Marcus Vossen
  • Publication number: 20150125534
    Abstract: The present invention relates to the pharmaceutical formulations comprising imatinib in solid dosage form reconstituted with a diluent just before use; preparation processes and use thereof.
    Type: Application
    Filed: November 30, 2011
    Publication date: May 7, 2015
    Applicant: Imuneks Farma Ilac Sanayi Ve Ticaret A.S.
    Inventor: Mehmet Nevzat Pisak
  • Publication number: 20150126484
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: May 7, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth Celeste Deselm, Yufang Xiao, Hui Qiu, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Publication number: 20150126520
    Abstract: Novel solid forms of imatinib mesilate comprising as active ingredient 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]-benzamide methanesulfonic acid salt and as co-crystal former benzoic acid, fumaric acid or succinic acid are described. The said multi-component crystalline forms possess improved physical and biological properties with respect to the crystalline forms of the active pharmaceutical ingredient previously known.
    Type: Application
    Filed: June 18, 2013
    Publication date: May 7, 2015
    Applicant: BASF SE
    Inventors: Tiziana Chiodo, Rolf Hellmann, Marcus Vossen, Beate Salvador, Andreas Hafner, Tobias Hintermann
  • Publication number: 20150126500
    Abstract: Provided are piperazinyl pyrimidine derivatives of formula I having CCR4 antagonism, and the preparation method, pharmaceutical composition and use thereof in the preparation of a medicament. The medicament is useful for the treatment and prevention of CCR4-related diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 7, 2015
    Inventors: Song Li, Ying Wang, Junhai Xiao, Dalong Ma, Hongwei Gong, Hui Qi, Lili Wang, Xiaomei Ling, Zhibing Zheng, Yang Zhang, Wu Zhong, Meina Li, Yunde Xie, Enquan Xu, Xingzhou Li, Jing Ma, Guoming Zhao, Xinbo Zhou, Xiaokui Wang, Hongying Liu
  • Publication number: 20150119403
    Abstract: The invention provides the identification of the presence of mutant ROS protein in human cancer. In some embodiments, the mutant ROS are FIG-ROS fusion proteins comprising part of the FIG protein fused to the kinase domain of the ROS kinase. In some embodiments, the mutant ROS is the overexpression of wild-type ROS in cancerous tissues (or tissues suspected of being cancerous) where, in normal tissue of that same tissue type, ROS is not expressed or is expressed at lower levels. The mutant ROS proteins of the invention are anticipated to drive the proliferation and survival of a subgroup of human cancers, particularly in cancers of the liver (including bile duct), pancreas, kidney, and testes. The invention therefore provides, in part, isolated polynucleotides and vectors encoding the disclosed mutant ROS polypeptides (e.g., a FIG-ROS(S) fusion polypeptide), probes for detecting it, isolated mutant polypeptides, recombinant polypeptides, and reagents for detecting the fusion and truncated polypeptides.
    Type: Application
    Filed: September 11, 2014
    Publication date: April 30, 2015
    Applicant: CELL SIGNALING TECHNOLOGY, INC.
    Inventors: Ting-Lei Gu, Meghan Ann Tucker, Herbert Haack, Katherine Eleanor Crosby, Victoria McGuinness Rimkunas
  • Patent number: 9018205
    Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: April 28, 2015
    Assignee: The Scripps Research Institute
    Inventors: Theodore Mark Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael Darin Cameron, Derek R. Duckett
  • Publication number: 20150110871
    Abstract: The present invention relates to a gastric retentive tablet composition comprising: (1) coated particles essentially consisting of a drug and an amino methacrylate copolymer, (2) a methacrylic acid copolymer and (3) an excipient, wherein items 1, 2, and 3 are blended together, and then compressed into a gastric retentive tablet. Thus, the coated particles (item 1), a methacrylic acid copolymer and the excipient are evenly distributed in the tablet. The excipient is selected from a group consisting of a retarding agent, a binder, a filler, a chelating agent, a diluent, a disintegrant, a lubricant, a colorant, a solubilizing agent, or a mixture thereof. The coated particles (item 1) do not contain methacrylic acid polymer.
    Type: Application
    Filed: January 3, 2015
    Publication date: April 23, 2015
    Inventor: David Wong
  • Publication number: 20150111871
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 23, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Publication number: 20150111891
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: April 23, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
  • Publication number: 20150110735
    Abstract: A centrifugal mixing device can include a shaft assembly that is operably coupled to a motor such that the motor rotates the shaft assembly about a first axis. The devices can further include a turret that is rotatably coupled to the shaft assembly such that the turret rotates about the first axis relative to the shaft assembly. The turret can include a first support, a first canister rotatably coupled to the first support such that the first canister rotates about a second axis, and a second canister rotatably coupled to the first support such that the second canister rotates about a third axis. The turret is configured to rotate about the first axis in a first rotational direction and each of the first and second canisters is configured to rotate about the second and third axes, respectively, in a second rotational direction that is opposite the first rotational direction.
    Type: Application
    Filed: October 22, 2013
    Publication date: April 23, 2015
    Inventor: Steven Hoffman
  • 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
  • Patent number: 9012455
    Abstract: Chronic myelogenous leukemia (CML), and in particular imatinib resistant CML is treated using compositions and methods in which a Rad51-inhibitor and a kinase inhibitor are administered. Most preferably, the Rad51 inhibitor comprises an indolyl isoquinoline structure and the kinase inhibitor is a BCR-ABL inhibitor.
    Type: Grant
    Filed: April 10, 2007
    Date of Patent: April 21, 2015
    Assignee: The Regents of the University of California
    Inventors: Wen-Hwa Lee, Phang-Lang Chen, Longen Zhou, Jiewen Zhu
  • Publication number: 20150105400
    Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Haruto NAKAGAWA, Naoko ANDO
  • Patent number: 9006232
    Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: April 14, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo