Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond Patents (Class 514/275)
  • Patent number: 11389434
    Abstract: The inventors demonstrate for the first time the activation of the Hedgehog (HH) signaling pathway in normal and abnormal human mast cells (MCs). These results prompt the inventors to explore the consequence of the inhibition of the HH pathway, especially the canonical pathway, on MC proliferation. They demonstrate that Hedgehog inhibitors inhibit proliferation and induces apoptosis of mast cells. Accordingly the present invention relates to a method of treating a mast cell disease in a patient in need there of comprising administering to the patient a therapeutically effective amount of a Hedgehog inhibitor.
    Type: Grant
    Filed: May 17, 2018
    Date of Patent: July 19, 2022
    Assignees: INSERM, FONDATION IMAGINE, UNIVERSITE PARIS DESCARTES, ASSISTANCE PUBLIQUE-HOPITAUX DE PARIS (APHP), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: Leila Maouche-Chretien, Christine Bodemer, Olivier Hermine, Laura Polivka
  • Patent number: 11351170
    Abstract: The present disclosure relates to a compound of formula (I), or a pharmaceutically acceptable salt, a solvate, a stereoisomer, or tautomer thereof, a pharmaceutical composition comprising a compound of formula (A) or formula (B), and any subgenera thereof, and use of said compounds and compositions thereof, wherein R1, R2, R3a, R3b, R5, R6, X1, X2, Y and n are described herein.
    Type: Grant
    Filed: August 15, 2018
    Date of Patent: June 7, 2022
    Assignee: Beijing Xuanyi PharmaSciences Co., Ltd.
    Inventors: Yuntao Song, Xiaoqi Chen
  • Patent number: 11318124
    Abstract: The present invention provides a medicament comprising a compound represented by general formula (1) which has Axl inhibitory activity, and an EGFR tyrosine kinase inhibitor in combination, and a method for treating cancer using this combination. The present invention provides an excellent medicament and method for treating cancer which is highly effective for inhibiting resistance to an EGFR tyrosine kinase inhibitor in cancer treatment, and causes less adverse reactions such as weight loss.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: May 3, 2022
    Assignee: Daiichi Sankyo Company, Limited
    Inventor: Takeshi Jimbo
  • Patent number: 11299477
    Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.
    Type: Grant
    Filed: February 26, 2020
    Date of Patent: April 12, 2022
    Assignee: Laurus Labs Limited
    Inventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Sunil Kumar Indukuri, Sanjay Kumar Dehury, Nagaraju Mekala, Jahangeer Baba Shaik, Durga Prasad Kuchipudi
  • Patent number: 11285151
    Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
    Type: Grant
    Filed: August 23, 2019
    Date of Patent: March 29, 2022
    Assignee: EMORY UNIVERSITY
    Inventors: Michael G. Natchus, Richard Arrendale, Dennis Liotta, Ketan Desai, Hyunsuk Shim
  • Patent number: 11285149
    Abstract: The present invention relates to a combination of a signal transducer and activator of transcription 3 (STAT3) activity inhibitor; and an immune checkpoint inhibitor for use in treating or preventing the hyperproliferative disorder in a subject. Preferably, the STA3 activity inhibitor is pyrimethamine or atovaquone, and the immune checkpoint inhibitor is an anti-PD1 antibody. Preferably, the hyperproliferative disorder is a glioma or a glioblastoma.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: March 29, 2022
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: David Frank, Darwin Ye
  • Patent number: 11279677
    Abstract: Provided herein are compounds for use as photochromic molecular switches having very long thermal isomerization half-lives and switchable fluorescence properties both in solution and the solid state.
    Type: Grant
    Filed: May 2, 2019
    Date of Patent: March 22, 2022
    Assignee: THE TRUSTEES OF DARTMOUTH COLLEGE
    Inventors: Ivan Abrahamian, Hai Qian, Susnata Pramanik, Baihao Shao, Quan Li
  • Patent number: 11266147
    Abstract: The present invention relates to heterocyclylaminophenyloxadiazole and derivatives thereof that may be used and as fungicides.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: March 8, 2022
    Assignee: BAYER AKTIENGESELLSCHAFT
    Inventors: Anne-Sophie Rebstock, Sebastien Naud, Stephane Brunet, Mathieu Gourgues, Harald Jakobi, Andreas Goertz, Emmanuelle Hilt, Sophie Ducerf
  • Patent number: 11260056
    Abstract: Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined herein.
    Type: Grant
    Filed: September 23, 2016
    Date of Patent: March 1, 2022
    Assignee: AFFERENT PHARMACEUTICALS, INC.
    Inventors: Anthony P. Ford, Kathleen Sereda Glaub, Michael M. Kitt, Steven Smith
  • Patent number: 11253516
    Abstract: The present invention relates to a N2,N4-diphenylpyrimidin-2,4-diamine derivative, a method for preparing the same, and a pharmaceutical composition for the prevention or treatment of cancer, containing the same as an active ingredient. The derivative shows a relatively weak EGFR activity inhibitory effect on wild-type EGFR, a high inhibitory ability on EGFR mutation, and a high inhibitory ability on even FLT3 and FLT3 mutation, and thus, can be effectively used for the treatment of cancer with EGFR mutation or cancer with FLT3 or a mutation thereof, and the derivative shows a synergy effect at the time of combination administration, and thus can be effectively used for the treatment of combination administration.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: February 22, 2022
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Kwangho Lee, Inji Shin, Gildon Choi, Chong Hak Chae, Hyeon Jeong Choe, Myoung Eun Jung, Byeong Uk Jeon, Byoung Chul Cho, Chae Won Park, Hwan Kim, Krishna Babu Duggirala
  • Patent number: 11242323
    Abstract: Described herein are urea compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Olig2 inhibitors may be used to treat glioblastoma.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: February 8, 2022
    Assignee: CURTANA PHARMACEUTICALS, INC.
    Inventors: Graham Beaton, Stanton F. McHardy, Ambrosio Lopez, Jr., Bismarck Campos, Hua-Yu Leo Wang
  • Patent number: 11234980
    Abstract: The present invention relates to high doses of macitentan, i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof, or of aprocitentan, for use in the treatment and/or prevention of pulmonary arterial hypertension (PAH). Moreover, the present invention relates to the use of high doses of macitentan, or of aprocitentan, for the manufacture of a medicament for the treatment and/or prevention of PAH, as well as to a method for the treatment and/or prevention of PAH comprising high doses of macitentan or of aprocitentan. Further, the present invention relates to a dosage regimen for the treatment and/or prevention of PAH as well as to a combination of macitentan, or of aprocitentan, with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators.
    Type: Grant
    Filed: March 2, 2021
    Date of Patent: February 1, 2022
    Assignee: Actelion Pharmaceuticals Ltd
    Inventors: Dénes Csonka, Wassim Fares, Hans Hoogkamer, Koen Torfs
  • Patent number: 11180480
    Abstract: A process for manufacturing 2-isobutyl-6-(3-(methylamino)azetidin-1-yl)pyrimidin-4-amine of Formula (I): including starting from 6-chloro-2-isobutylpyrimidin-4-amine and tert-butyl azetidin-3-yl(methyl)carbamate, or another N-protected N-methylazetidin-3-amine, and performing the following steps: (a) coupling reaction of both compounds in dimethylsulfoxide in presence of potassium carbonate to afford an intermediate protected compound; and (b) deprotection of the protected compound to afford 2-isobutyl-6-(3-(methylamino)azetidin-1-yl)pyrimidin-4-amine. Also, a process for manufacturing the intermediate protected compound, wherein deprotection step (b) is omitted, and the compounds obtained from the processes.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: November 23, 2021
    Assignee: SENSORION
    Inventors: Daan Copmans, Amandine Mohr, Maurice Hubert Bonten, Dawn Toronto
  • Patent number: 11166927
    Abstract: The present specification provides RXR agonist compounds, compositions comprising such RXR agonists, and methods using such compounds and compositions to treat an autoimmune disorder, inflammation associated with an autoimmune disorder and/or a transplant rejection as well as use of such RXR agonists to manufacture a medicament and use of such compounds and compositions to treat an autoimmune disorder, inflammation associated with an autoimmune disorder and/or a transplant rejection.
    Type: Grant
    Filed: December 18, 2020
    Date of Patent: November 9, 2021
    Assignee: Io Therapeutics, Inc.
    Inventors: Roshantha A. Chandraratna, Ethan Dmitrovsky, Elizabeth Nowak, Randolph Noelle
  • Patent number: 11160868
    Abstract: The present invention relates to compositions and methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells.
    Type: Grant
    Filed: January 4, 2019
    Date of Patent: November 2, 2021
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Will McLean, Megan Harrison, Michael R. Jirousek
  • Patent number: 11160273
    Abstract: An aqueous suspoemulsion (SE) comprising: a dispersed oil phase of Component (a), comprising: (i) lambda-cyhalothrin as the first active ingredient; (ii) at least one solvent having lambda-cyhalothrin dissolved therein; a continuous water phase of Component (b), comprising: (i) imidacloprid as the second active ingredient; and (ii) water having imidacloprid suspended therein; and optionally at least one additive is provided. A process for preparing an aqueous suspoemulsion comprising: Step 1: Preparing lambda-cyhalothrin EC phase by mixing the active ingredient with a suitable solvent; Step 2: Preparing a dispersion of imidacloprid in a continuous water phase by mixing the active ingredient, a dispersant and a required amount of water; and Step 3: Combining the EC phase in Step 1 with the water phase in Step 2.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: November 2, 2021
    Assignee: ROTAM AGROCHEM INTERNATIONAL COMPANY LIMITED
    Inventor: James Timothy Bristow
  • Patent number: 11136328
    Abstract: Disclosed are chemical entities of Formula (I), wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
    Type: Grant
    Filed: March 5, 2020
    Date of Patent: October 5, 2021
    Assignee: Rugen Holdings (Cayman) Limited
    Inventor: Gideon Shapiro
  • Patent number: 11116770
    Abstract: The present invention relates to a method of treating or preventing hair loss or excessive hair shedding in a subject by administering to a subject an oral dose of minoxidil. In particular, the present invention relates to a method of treating telogen effluvium in a subject by administering to a subject an oral dose of minoxidil.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: September 14, 2021
    Inventor: Rodney Sinclair
  • Patent number: 11111233
    Abstract: An amino pyrimidine compound for inhibiting protein tyrosine kinase activity, a pharmaceutical composition thereof, preparation therefor, and an application thereof. Specifically, an amino pyrimidine compound represented by formula (I), R1, R2, L, Y, R6, W, A, m, and n being defined in the specification, and a pharmaceutically acceptable salt, a stereoisomer, a solvent compound, a hydrate, a polymorphism, a prodrug, or an isotope variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases such as cell proliferative diseases, cancers, and immune diseases.
    Type: Grant
    Filed: January 24, 2019
    Date of Patent: September 7, 2021
    Assignee: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Xingye Ren, Jian Jin, Huanyin Li, Yixin Ai
  • Patent number: 11091476
    Abstract: The embodiments disclosed herein provide compounds as shown in formula I or a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer, a deuterated compound, a prodrug or a mixture thereof, or a pharmaceutically acceptable salt or solvate of the compounds as shown in formula I or a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer, a deuterated compound, a prodrug or a mixture thereof, wherein R1 to R7 are as defined in the description. This application also provides a preparation method and a medical use of the compounds. The compounds of this disclosure have an activity superior or equivalent to the candidate drug LY2835219 currently under phase III clinical trial, and some of the compounds exhibit better selectivity. Moreover, the preferred compounds exhibit good absorption and good blood-brain distribution when administered orally.
    Type: Grant
    Filed: November 28, 2016
    Date of Patent: August 17, 2021
    Assignee: Gan & Lee Pharmaceuticals
    Inventors: Lei Yin, Wenjian Liu, Heng Li, Dianxi Zhu
  • Patent number: 11083728
    Abstract: The present invention provides, in part, compositions comprising an inhibitor of cyclin-dependent kinase 7 (CDK7) and sulfobutyl ether-?-cyclodextrin. Also provided are methods of using a disclosed composition for treating proliferative diseases. The present invention also provides methods of making disclosed compositions.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: August 10, 2021
    Assignee: Syros Pharmaceuticals, Inc.
    Inventor: Neera Jain
  • Patent number: 11065230
    Abstract: The present invention relates to methods and pharmaceutical compositions for the treatment of systemic mastocytosis. The inventors showed the effect of KPT-251 treatment on SCF-dependent human Mast cell (MC) line without KIT mutation (WT ROSA) and on two factor-independent MC lines with KIT mutations : ROSA ? 417-419 insY and ROSA D816V. KPT is a Selective Inhibitor of Nuclear Export (SINE) that specifically inhibits the activity of the exportin-1 (XPO1). KPT-251 treatment induces minimal toxicity in non-cancerous hematopoietic cells both in vitro and in vivo. In particular, the present invention relates a method of treating systemic mastocytosis in patient in need thereof comprising administering to the patient a therapeutically effective amount of a XPO1 inhibitor.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: July 20, 2021
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), FONDATION IMAGINE, UNIVERSITE PARIS DESCARTES, ASSISTANCE PUBLIQUE—HOPITAUX DE PARIS (APHP), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE CAEN NORMANDIE, CENTRE HOSPITALIER REGIONAL UNIVERSITAIRE DE CAEN
    Inventors: Olivier Hermine, Flavia Guillem, Gandhi Damaj, Sophia Ladraa
  • Patent number: 11033546
    Abstract: The present invention relates to compositions and methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: June 15, 2021
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Will McLean, Megan Harrison, Michael R. Jirousek
  • Patent number: 11028080
    Abstract: The present disclosure relates generally to compounds of formula (I) or a pharmaceutically acceptable salt, prodrug, deuterated analog, tautomer, stereoisomer, or mixture of stereoisomers thereof and their use as LRRK2 inhibitors.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: June 8, 2021
    Assignee: DENALI THERAPEUTICS INC.
    Inventors: Anthony A. Estrada, Jianwen A. Feng, Joseph P. Lyssikatos, Zachary K. Sweeney, Javier de Vicente Fidalgo
  • Patent number: 10988476
    Abstract: The present invention discloses a substituted pyridine compound represented by formula I, and a pharmaceutically acceptable salt, stereoisomer and tautomer thereof. The compounds of the present invention are useful in the treatment of cancers.
    Type: Grant
    Filed: April 15, 2020
    Date of Patent: April 27, 2021
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Qian Wang, Chen Shi, Xiong Zhai, Hui Ge, Xuemei Liao, Yu Mao, Zhixiong Xiang, Yanan Han, Guoyong Huo, Yanjun Liu
  • Patent number: 10988470
    Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
    Type: Grant
    Filed: August 12, 2020
    Date of Patent: April 27, 2021
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Jennifer Kozak, Ryan Hudson, Robert Murray McKinnell, Gary E. L. Brandt
  • Patent number: 10980741
    Abstract: Compositions and methods for inducing pterygium regression from visual axis/central cornea, stabilizing pterygium, treating hyperemia and symptoms in pterygium patients, and treating pterygium recurrence following pterygiectomy are disclosed. The methods include administration of a multikinase inhibitor, an antimetabolite or a combination thereof to patients in need thereof.
    Type: Grant
    Filed: December 5, 2018
    Date of Patent: April 20, 2021
    Assignee: Cloudbreak Therapeutics, LLC
    Inventor: Jinsong Ni
  • Patent number: 10976306
    Abstract: Provided are: a protein degradation inducing tag which is a molecule that has affinity with proteases and does not inhibit degradation of a protein by proteases; a protein degradation inducing molecule that is a conjugate of at least one protein degradation inducing tag and at least one protein binding molecule that binds to a protein; and a usage of those.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: April 13, 2021
    Assignee: Tokyo University of Science Foundation
    Inventors: Etsuko Miyamoto, Masaaki Ozawa
  • Patent number: 10961240
    Abstract: Provided are compositions comprising Compound I having the following structure: or a pharmaceutically acceptable salt thereof, and a solubilizing agent; methods of making the same; and methods of using the same.
    Type: Grant
    Filed: July 12, 2019
    Date of Patent: March 30, 2021
    Assignees: Plexxikon Inc., Daiichi Sankyo Company, Limited
    Inventors: Prabha N. Ibrahim, Hamid Rezaei, Gary Conard Visor, Tomoari Kamo, Hiroshi Yamakose
  • Patent number: 10954236
    Abstract: Bicyclic dihydropyrimidine-carboxamide compounds of formula I described herein inhibit Rho Kinase and may be used for the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Type: Grant
    Filed: October 18, 2019
    Date of Patent: March 23, 2021
    Assignee: CHIESI FARMACEUTICI S.P.A.
    Inventors: Alessandro Accetta, Fabio Rancati, Anna Maria Capelli, David Edward Clark, Patrizia Tisselli, Christine Edwards, Gurdip Bhalay, Arnaud Jean Francois Auguste Cheguillaume
  • Patent number: 10946017
    Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of TBK1.
    Type: Grant
    Filed: February 25, 2019
    Date of Patent: March 16, 2021
    Assignee: ARVINAS OPERATIONS, INC.
    Inventors: Andrew P. Crew, Jing Wang, Hanqing Dong, Yimin Qian
  • Patent number: 10874671
    Abstract: Amorphous solid dispersions of nilotinib fumarate or nilotinib tartrate are provided, as well as pharmaceutical compositions thereof, wherein the compositions exhibit enhanced bioavailability in the fasted state. Preferably, the compositions may be orally administered to a patient in either the fed or fasted state, with a decrease or elimination of the food effect. Preferably, following oral administration of the pharmaceutical compositions, there is no substantial difference in the pharmacokinetic parameters (e.g., Cmax, AUC0-t and/or AUC0-infinity) of nilotinib, regardless of whether the pharmaceutical compositions are administered to a subject in the fed or fasted state.
    Type: Grant
    Filed: February 18, 2020
    Date of Patent: December 29, 2020
    Assignee: SLAYBACK PHARMA LLC
    Inventors: Paras P. Jain, Ajay Kumar Singh, Keerthi Priya, Girish Kumar Jain, Girish G. Kore, Sandeep Jain, Hanimi Reddy Bapatu
  • Patent number: 10851069
    Abstract: The present invention provides, in certain embodiments, compositions comprising a uniform population of free, single crystals of a hydrophobic compound. Methods of administering, and processes for preparing, compositions comprising a uniform population of free, single crystals of a hydrophobic compound are also provided.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: December 1, 2020
    Assignee: Massachusetts Institute of Technology
    Inventors: Shady Farah, Joshua C. Doloff, Robert S. Langer, Daniel G. Anderson
  • Patent number: 10793551
    Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I or Formula II, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X1, X2, X3, X4, X5, Y1, Y2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the specification. The inventive Formula I and Formula II compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: October 6, 2020
    Assignee: eFFECTOR Therapeutics Inc.
    Inventors: Justin T. Ernst, Siegfried H. Reich, Paul A. Sprengeler, Alan X. Xiang
  • Patent number: 10774080
    Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
    Type: Grant
    Filed: January 8, 2020
    Date of Patent: September 15, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Jennifer Kozak, Ryan Hudson
  • Patent number: 10765677
    Abstract: The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and/or an amorphous form.
    Type: Grant
    Filed: June 7, 2019
    Date of Patent: September 8, 2020
    Assignee: ForSight Vision4, Inc.
    Inventors: Judit Horvath, Irina Astafieva, Signe Erickson, Kathleen Cogan Farinas
  • Patent number: 10738035
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y—Z-L-R1??(I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: August 11, 2020
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Wei Li, Hui Cao, Meizhong Jin, Xuri Gao, Xiaowen Peng, Jorden Kass, Yat Sun Or
  • Patent number: 10730859
    Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: August 4, 2020
    Assignee: Laurus Labs Limited
    Inventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Sunil Kumar Indukuri, Sanjay Kumar Dehury, Nagaraju Mekala, Jahangeer Baba Shaik, Durga Prasad Kuchipudi
  • Patent number: 10722512
    Abstract: The invention relates to combinations comprising an HDAC inhibitor and a Her2 inhibitor for the treatment of breast cancer in a subject in need thereof. The invention also relates to combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of breast cancer in a subject in need thereof. Also provided herein are methods for treating breast cancer in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations. Further provided are methods for inhibiting migration and/or invasion of a breast cancer cell in a subject by administering to the subject a HDAC6 specific inhibitor.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: July 28, 2020
    Assignee: Acetylon Pharmaceuticals, Inc.
    Inventors: David Lee Tamang, Min Yang, Simon S. Jones
  • Patent number: 10717725
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: December 6, 2018
    Date of Patent: July 21, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Elizabeth Anne Jurica, Zhenqiu Hong
  • Patent number: 10710983
    Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 ?M to 3.7 ?M; a TAK1 IC50 of from 0.008 ?M to 132 ?M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
    Type: Grant
    Filed: June 26, 2017
    Date of Patent: July 14, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Patent number: 10709705
    Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, and R7 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to inhibition of ALK such as cancer.
    Type: Grant
    Filed: August 28, 2017
    Date of Patent: July 14, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Jianyong Chen
  • Patent number: 10710979
    Abstract: The present invention provides an EGFR kinase inhibitor and a preparation method and use thereof. Specifically, the present invention provides a compound as shown in formula (I), the definition of each group therein being as described in the description. Said compound is an efficient EGFR inhibitor.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: July 14, 2020
    Assignee: ZHEJIANG BOSSAN PHARMACEUTICAL CO. LTD.
    Inventors: Dawei Ma, Qiang Yu, Junying Yuan, Hongguang Xia, Dongpo Cai, Kailiang Wang, Chen Zhang, Shanghua Xia
  • Patent number: 10702527
    Abstract: The present disclosure provides combination therapy of a transcription inhibitor and a kinase inhibitor. The combination of the transcription inhibitor and the kinase inhibitor may be useful in treating and/or preventing in a subject a proliferative disease, such as proliferative a disease that is resistant to the transcription inhibitor alone or the kinase inhibitor alone. In certain embodiments, the proliferative disease is a cancer. The combination of the transcription inhibitor and the kinase inhibitor is expected to be synergistic.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: July 7, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Peter Hammerman, Kwok-kin Wong, Nathanael S. Gray
  • Patent number: 10682352
    Abstract: Provided in the present invention are a compound having the effects of preventing and treating diseases related to IDH mutation, and a preparation method and use thereof.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: June 16, 2020
    Assignees: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Lei Jiang, Meiyu Geng, Qiangang Zheng, Min Huang, Huixin Wan, Shuai Tang, Xianlei Fu, Xiaojing Lan, Jianhua Cao, Feifei Liu, Jian Ding
  • Patent number: 10662186
    Abstract: The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.
    Type: Grant
    Filed: December 30, 2016
    Date of Patent: May 26, 2020
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Qian Wang, Chen Shi, Xiong Zhai, Hui Ge, Xuemei Liao, Yu Mao, Zhixiong Xiang, Yanan Han, Guoyong Huo, Yanjun Liu
  • Patent number: 10647686
    Abstract: The present invention relates to compounds represented by Formula 1 or a pharmaceutically acceptable salt thereof, wherein: R1 is chloro or methyl; R2 is hydrogen or chloro; R3 is hydrogen, fluoro, chloro, bromo, methyl, ethyl, isopropyl, pentyl, hexyl, octyl, methoxy, phenoxy, (4-nitrophenyl)sulfonyl, piperidin-4-yl, or piperazin-1-yl; R4 is hydrogen, chloro, methyl or trifluoromethyl, phenoxy, (4-nitrophenyl)sulfonyl or piperidin-4-yl; or R3 and R4, together with the carbons to which they are attached, form a fused ring selected form the group consisting of: n is 1 or 2. These compounds according to the present invention remarkably inhibits activity of DRAK that inhibits signal systems of TGF-?, which is known to suppress cancer growth, and thus the novel pyrimidine compounds can be used as a pharmaceutical composition for preventing or treating cancer and can be used as a pharmaceutical composition for preventing or treating inflammatory disease.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: May 12, 2020
    Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Kwangho Lee, Gildon Choi, Na Ri Lee, Sang Jun Park, Myoung Eun Jung, Seong Jin Kim, Kyung-Min Yang, Jihee Lee
  • Patent number: 10632192
    Abstract: The present invention provides a compound of the formula (1): wherein X, R1, R2, R3, R4, R5, R6, Y1, Y2, L, and m are as defined in the description, and a pharmaceutically acceptable salt thereof, which are useful as a vaccine adjuvant.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: April 28, 2020
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Hidenori Kimura, Hitoshi Ban, Yoshiaki Isobe, Hitoshi Watanabe
  • Patent number: 10633413
    Abstract: This invention relates to methods of stimulating the activity of the human and animal enteric nervous system. The method comprises orally administering an aminosterol, such as squalamine, a naturally occurring aminosterol isolated from Squalus acanthias, or derivatives thereof, to a subject in need.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: April 28, 2020
    Assignee: ENTERIN, INC.
    Inventor: Michael Zasloff
  • Patent number: RE48547
    Abstract: There are disclosed aminopyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: May 11, 2021
    Assignee: Syntrix Biosystems Inc.
    Inventors: Dean Y. Maeda, John A. Zebala, Aaron D. Schuler