Pyrazoles Patents (Class 514/406)
  • Patent number: 11325903
    Abstract: Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formulae (Ia), (Ib), (Ic), (Id) and (Ie), in which R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
    Type: Grant
    Filed: November 29, 2017
    Date of Patent: May 10, 2022
    Assignee: Bantam Pharmaceutical, LLC
    Inventors: M. Arshad Siddiqui, Stephane Ciblat, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Nicolas Bruneau-Latour, Gerald W. Shipps, Alan B. Cooper, Vibha Oza, Matthew J. Kostura, Michael Luther, Jedd Levine
  • Patent number: 11312722
    Abstract: Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related diseases.
    Type: Grant
    Filed: May 6, 2020
    Date of Patent: April 26, 2022
    Assignees: TRUSTEES OF BOSTON UNIVERSITY, The Governing Council of the University of Toronto
    Inventors: Lauren Elaine Brown, David S Huang, Leah E. Cowen, Luke Whitesell, Paul Marcyk
  • Patent number: 11304932
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor and their uses for the treatment and prophylaxis of visual hallucinations associated with Lewy Body dementia.
    Type: Grant
    Filed: November 20, 2020
    Date of Patent: April 19, 2022
    Assignee: Axovant Sciences GmbH
    Inventors: Lawrence Tim Friedhoff, Shankar Ramaswamy, Yandong Wen
  • Patent number: 11242343
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
    Type: Grant
    Filed: February 10, 2020
    Date of Patent: February 8, 2022
    Assignee: Incyte Corporation
    Inventors: Kai Liu, Jun Pan, Alexander Sokolsky, Oleg Vechorkin, Hai Fen Ye, Qinda Ye, Wenqing Yao
  • Patent number: 11229624
    Abstract: Provided are methods of regulating proliferation and/or differentiation of keratinocytes and immune cells, more specifically to methods of treating pathologies characterized by hyperproliferative keratinocytes or inflammatory skin diseases by administration of FABP4-inhibitor.
    Type: Grant
    Filed: October 25, 2017
    Date of Patent: January 25, 2022
    Assignee: TICURE LTD.
    Inventor: Tali Garin-Shkolnik
  • Patent number: 11219629
    Abstract: An anesthetic pharmaceutical composition, system and method is provided. The anesthetic pharmaceutical composition comprises an intraoperative local injection and one or more postoperative medications. The intraoperative local injection is long-acting and comprises at least one local anesthetic agent, such as ropivacaine; ketorolac; and at least one steroid, such as dexamethasone. The one or more postoperative medications comprise an atypical opioid agonist, such as tramadol; a non-steroidal anti-inflammatory drug, such as a cyclooxygenase-2 inhibitor; a gamma-aminobutyric acid analogue, such as pregabalin; and acetaminophen. The method comprises the steps of commencing a surgical procedure involving one or more incision sites; injecting an intraoperative local injection at the one or more incision sites; performing and completing the surgical procedure; and administering one or more postoperative medications.
    Type: Grant
    Filed: October 17, 2019
    Date of Patent: January 11, 2022
    Inventor: Hooman M. Melamed
  • Patent number: 11192887
    Abstract: Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formulae (Ia), (Ib), (Ic), (Id) and (Ie), in which R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
    Type: Grant
    Filed: November 29, 2017
    Date of Patent: December 7, 2021
    Assignee: Bantam Pharmaceutical, LLC
    Inventors: M. Arshad Siddiqui, Stephane Ciblat, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Nicolas Bruneau-Latour, Gerald W. Shipps, Alan B. Cooper, Vibha Oza, Matthew J. Kostura, Michael Luther, Jedd Levine
  • Patent number: 11186567
    Abstract: The invention provides compounds of the formula (I): wherein R1 and R2 are defined in the specification, to pharmaceutical compositions comprising the compounds and the compounds for use as medicaments. The compounds potentiate AMPA receptor function and are expected to be useful in the treatment of central nervous system disorders, for example in the treatment of depressive disorders, mood disorders and cognitive dysfunction associated with neuropsychiatric disorders such as schizophrenia.
    Type: Grant
    Filed: February 9, 2018
    Date of Patent: November 30, 2021
    Assignee: University College Cardiff Consultants Limited
    Inventors: Simon Ward, Paul Beswick, Lewis Pennicott, Tristan Reuillon
  • Patent number: 11173144
    Abstract: Adrenergic receptor modulating compounds and methods of using the same are provided. Also provided are methods of treating a subject for a disease or condition associated with an adrenergic receptor including administering a therapeutically effective amount of the subject compound. Aspects of the disclosure include a method of modulating an inflammatory pathway in a cell, such as the production of TNF-alpha in the cell. The method can include contacting a cell with ?1-selective adrenergic receptor modulating compound to selectively activate a cAMP pathway over a beta-arrestin pathway in the cell. Pharmaceutical compositions and kits which include the subject compounds are provided.
    Type: Grant
    Filed: May 12, 2017
    Date of Patent: November 16, 2021
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Mehrdad Shamloo, Alam Jahangir, Bitna Yi, Andrew Kelley Evans, Michael John Green
  • Patent number: 11116778
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds which are prodrugs of ALOX-15 inhibitors. Also described herein are methods for using such compounds in the treatment of disease.
    Type: Grant
    Filed: January 14, 2020
    Date of Patent: September 14, 2021
    Assignee: EMPIRICO INC.
    Inventors: Omri Gottesman, Shannon Bruse, Brian Cajes, David Lewis, David Rozema
  • Patent number: 11110184
    Abstract: This invention relates to, in part, methods and compositions that are useful for the diagnosis, treatment, or prevention of a blinding eye disease, including in the discovery of drugs that are efficacious against these diseases. Diseases include, for example, age related macular degeneration and reticular pseudodrusen disease, and the methods described herein include, for example, the method named delayed near infrared analysis (DNIRA).
    Type: Grant
    Filed: November 26, 2019
    Date of Patent: September 7, 2021
    Assignee: Translatum Medicus Inc.
    Inventor: Shelley Romayne Boyd
  • Patent number: 11096912
    Abstract: The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound valaciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of valaciclovir and celecoxib.
    Type: Grant
    Filed: September 23, 2014
    Date of Patent: August 24, 2021
    Assignee: VIRIOS THERAPEUTICS, INC.
    Inventor: William L. Pridgen
  • Patent number: 11077092
    Abstract: Use of a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor for the treatment of diabetes and related conditions is disclosed.
    Type: Grant
    Filed: April 11, 2017
    Date of Patent: August 3, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hong-Ping Guan, Jose M. Castro-Perez, Harry R. Davis, Samuel E. Engel, Douglas G. Johns, Songnian Lin, Stephen F. Previs, Thomas P. Roddy, Liangsu Wang, Sheng-Ping Wang, Yusheng Xiong
  • Patent number: 11058668
    Abstract: Described herein are methods for treating transthyretin (TTR) amyloidosis in a subject. The methods include specific dosing regimens that have great efficacy in treating the subjects and that are well tolerated in subjects.
    Type: Grant
    Filed: March 22, 2019
    Date of Patent: July 13, 2021
    Assignee: EIDOS THERAPEUTICS, INC.
    Inventors: Uma Sinha, Satish Rao
  • Patent number: 11052069
    Abstract: The invention provides novel regimens of farnesoid X receptor (FXR) agonist and methods for modulating the activity of farnesoid X receptors (FXRs) using novel regimes of specific FXR agonists, in particular for treating or preventing fibrotic or cirrhotic diseases or disorders, such as liver diseases.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: July 6, 2021
    Assignee: Novartis AG
    Inventors: Bryan Laffitte, Andreas Bauer, Michael Badman, Jin Chen, Patrick Mueller, Rachel Soon
  • Patent number: 11034649
    Abstract: Disclosed are compounds of formulae: and pharmaceutically acceptable salts thereof, wherein the variables, R1, R2, R3, R4, R5, R6, R7, R11, R12, R13, R14, R15, R16, R17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.
    Type: Grant
    Filed: April 25, 2017
    Date of Patent: June 15, 2021
    Assignees: DUKE UNIVERSITY, THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
    Inventors: Pei Zhou, Eric J. Toone, Robert A. Nicholas, Ramesh Gopalaswamy, Xiaofei Liang, Frank Navas, III
  • Patent number: 10941132
    Abstract: Provided herein are compounds of the formula I: as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.
    Type: Grant
    Filed: January 5, 2016
    Date of Patent: March 9, 2021
    Assignee: Hua Medicine (Shanghai) Ltd.
    Inventors: Li Chen, Xiaowei Jin
  • Patent number: 10882846
    Abstract: The present invention relates to nitro-vinyl-pyrazole compounds of formula (B) wherein ring A, RB2 and RB3 are as defined in claim 1, as well as the manufacture of such compounds and their subsequent use in the production of agrochemicals and/or pharmaceuticals.
    Type: Grant
    Filed: February 5, 2020
    Date of Patent: January 5, 2021
    Assignee: SYNGENTA CROP PROTECTION AG
    Inventors: James Alan Morris, Sally Elizabeth Russell, Sean Ng
  • Patent number: 10875849
    Abstract: The present disclosure provides solid forms of (E)-3-[2-(2-thienyl)vinyl]-1H-pyrazole, compositions thereof, and methods of making and using the same.
    Type: Grant
    Filed: July 29, 2020
    Date of Patent: December 29, 2020
    Assignee: ANGION BIOMEDICA CORP.
    Inventors: An-Hu Li, Satish Kumar Sakilam, Dong Sung Lim
  • Patent number: 10818851
    Abstract: Provided are a condensed cyclic compound and an organic light-emitting device including the same. The material is represented by the formula A2-(A1)n1, wherein A2 may be selected from groups represented by Formula 2, A1 may be selected from groups represented by Formulae 2-1 to 2-4, and n1 may be an integer selected from 1 to 5: Organic light-emitting devices manufactured using this material were found to have lower driving voltages, higher brightness values, higher efficiencies, and longer half-lifespans.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: October 27, 2020
    Assignee: Samsung Display Co., Ltd.
    Inventors: Junha Park, Youngkook Kim, Sungsoo Bae, Munki Sim, Eunyoung Lee, Hyoyoung Lee, Eunjae Jeong, Seokhwan Hwang
  • Patent number: 10799517
    Abstract: The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or its pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: October 13, 2020
    Assignee: DR. REDDY'S LABORATORIES LTD
    Inventors: Ankit Baheti, Bijay Kumar Padhi, Supritha Vakada, Rajeev Singh Raghuvanshi
  • Patent number: 10796975
    Abstract: Semiconductor packages with electromagnetic interference supported stacked die and a method of manufacture therefor is disclosed. The semiconductor packages may house a stack of dies in a system in a package (SiP) implementation, where one or more of the dies may be wire bonded to a semiconductor package substrate. The dies may be stacked in a partially overlapping, and staggered manner, such that portions of some dies may protrude out over an edge of a die that is below it. This dies stacking may define a cavity, and in some cases, wire bonds may be made to the protruding portions of the die. Underfill material may be provided in the cavity and cured to form an underfill support. Wire bonding of the bond pads overlying the cavity formed by the staggered stacking of the dies may be performed after the formation of the underfill support.
    Type: Grant
    Filed: April 2, 2016
    Date of Patent: October 6, 2020
    Assignee: INTEL CORPORATION
    Inventor: Guo Mao
  • Patent number: 10766865
    Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: September 8, 2020
    Assignee: SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.
    Inventors: Koc-Kan Ho, Yong Xu, Michael David Saunders, Xiaohui Liu, Scott Albert Pearce, Kevin Bret Wright, Jason Marc Foulks, Kenneth Mark Parnell, Steven Brian Kanner, David Lee Vollmer, Jihua Liu
  • Patent number: 10722517
    Abstract: In certain embodiments the present invention provides methods useful in the treatment of glioma, such as glioblastoma, such methods comprising administering to a subject in need thereof a CSF-IR inhibitor together with one or more additional active agents such as IGF-IR inhibitors, PI3K inhibitors, IL4 inhibitors, NFAT inhibitors, and/or Stat6 inhibitors. In certain embodiments the present invention provides pharmaceutical compositions comprising a CSF-IR inhibitor together with one or more of such additional active agents.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: July 28, 2020
    Inventors: Daniela Francis Quail, Johanna Alexandra Joyce, Robert Lyle Bowman
  • Patent number: 10709688
    Abstract: This invention provides a pharmaceutical composition for treating or preventing synucleinopathy comprising a compound represented by formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: July 14, 2020
    Assignees: Tohoku University, National University Corporation Okayama University
    Inventors: Kohji Fukunaga, Hiroyuki Miyachi, Hiroaki Ishida, Shintaro Ban
  • Patent number: 10682359
    Abstract: Compounds discovered through a high-throughput screen, along with methods of use of the compounds, are provided. The compounds can be used to strongly inhibit key drug targets found in protozoan parasites, e.g., the target Trypanosoma cruzi glucokinase. Compounds include derivatives of N-phenylbenzenesulfonamide, barbituric acid, (R)-3-(piperidin-2-yl)pyridine, 3-nitro-2-phenyl-2H-chromene, 6-amino-3-methyl-4-phenyl-1,4-dihydropryranole[2,3-c]pyrazole-5-carbonitrile, and gossypol (2,2?-Bis(formyl-1,6,7-trihydroxy-5-isopropyl-3-methylnaphthalene).
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: June 16, 2020
    Assignee: University of South Carolina
    Inventor: Edward L. D'Antonio
  • Patent number: 10655183
    Abstract: The present invention provides methods and kits a) for preventing and/or treating cancer (e.g., colorectal cancer, neuroblastoma) that is linked, in part, to high levels of ODC activity and increased cellular polyamine content, b) for predicting cancer patient survival, especially cancer patient's whose cancer is linked, in part, to high levels of ODC activity and increased cellular polyamine contents, and c) for selecting the corresponding treatment options for such patients based on the allelic nucleotide sequence or SNP at positions +263 and/or +316 of the ODC1 gene as well as cancer treatment methods, in each case, which include the determination of the ODC1 genotype at the +263 and/or +316 positions, as a means to guide treatment selection.
    Type: Grant
    Filed: June 18, 2014
    Date of Patent: May 19, 2020
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF UNIVERSITY OF ARIZONA
    Inventors: Eugene Gerner, Patricia Thompson, Tracy Brooks, Jenaro Garcia-Huidobro
  • Patent number: 10654810
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: May 19, 2020
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 10647710
    Abstract: Disclosed in the present invention are a new thiazole compound, particularly a compound represented by formula (I), a pharmaceutical composition thereof and applications thereof in the preparation of drugs for the treatment of diseases related to herpes simplex viruses.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: May 12, 2020
    Assignee: Medshine Discovery Inc.
    Inventors: Haiying He, Zhigan Jiang, Weihua Shi, Jianhua Xia, Jian Li, Shuhui Chen
  • Patent number: 10640454
    Abstract: A process for preparation of 4-aminoindane derivatives of a first formula, salts and enantiomers thereof comprising the steps of: a) hydrogenating a 1,2-dihydroquinoline of a second formula to give a corresponding tetrahydroquinoline of a third formula; b) acylating the tetrahydroquinoline of the third formula with a carboxylic acid derivative of a fourth formula to obtain a corresponding acyl derivative compound of a fifth formula; c) rearranging the acyl derivative compound of the fifth formula under acidic conditions so as to give an acyl indane compound of a sixth formula; and d) hydrolysing the acyl group of the acyl indane compound of the sixth formula so as to obtain the 4-aminoindane derivatives of the first formula.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: May 5, 2020
    Assignee: STICHTING I-F PRODUCT COLLABORATION
    Inventors: Paolo Bellandi, Giampaolo Zanardi, Ravindra Vitthal Datar, Chockalingam Devarajan, Swamynathan Murali, Narayana Swamy
  • Patent number: 10632104
    Abstract: Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: April 28, 2020
    Assignee: SABRE THERAPEUTICS LLC
    Inventors: Gretchen Bain, Jillian Frances Evans, John Howard Hutchinson, David Lonergan
  • Patent number: 10576088
    Abstract: It was found that finafloxacin has a high solubility in the presence of Tris. Such solubility is significantly higher than in the presence of other compounds typically used as buffers (e.g. phosphate buffer). The observed significant increase in solubility of finafloxacin in compositions comprising Tris is further advantageously accompanied by a long term stability of such solutions. Tris is therefore to be regarded as a specific tool to considerably enhance the solubility of finafloxacin in solutions. By preparing compositions comprising Tris it is possible to dissolve finafloxacin in such an amount therein that these compositions can effectively be used as parenteral compositions for the treatment of bacterial infections.
    Type: Grant
    Filed: October 9, 2015
    Date of Patent: March 3, 2020
    Assignee: MerLion Pharmaceuticals Pte. Ltd.
    Inventors: Carsten Fischer, Andreas Vente, Sven-Eric Wohlert
  • Patent number: 10570086
    Abstract: The present invention relates to a novel process for converting the unwanted S enantiomer form to its useful raceme with respect to a 4-aminoindane derivative.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: February 25, 2020
    Assignee: FMC Corporation
    Inventors: Narayana Swamy, Chokalingam Devarajan, Ravindra Vitthal Datar
  • Patent number: 10570213
    Abstract: The invention provides methods and compositions for treating cancer and for enhancing immune function in an individual having cancer. The methods comprise administering a PD-1 axis binding antagonist and a taxane.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: February 25, 2020
    Assignee: Genentech, Inc.
    Inventors: Jeong Kim, Jeanne Cheung
  • Patent number: 10562858
    Abstract: A crystal form of 2-(3,5-dimethyl-1H-pyrazol-1-yl)-5-methylphenol which is stable and has high purity for preservation, industrial manufacturing, and circulation, and process for providing the same by using a boron compound.
    Type: Grant
    Filed: August 12, 2015
    Date of Patent: February 18, 2020
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Toshiro Sasaki, Takahiro Imai, Kenichiro Mori, Makoto Ohyama, Takashi Watanabe
  • Patent number: 10543193
    Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: January 28, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventors: Marlon Carlos, Weitong Dong, Mark Macias, Suzanne Michiko Sato, Lee Alani Selvey
  • Patent number: 10525144
    Abstract: The present invention provides compounds and a method for the targeted delivery of Mitochondrial Angiotensin Receptor Blockers (MARBs) to the Mitochondrial Angiotensin System (MAS) for the treatment of diseases caused by angiotensin-related mitochondrial dysfunction. The compounds include a mitochondrial targeting signal, a residue of a drug molecule, a functional moiety, and a scaffold moiety.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: January 7, 2020
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Honggang Cui, Peter M. Abadir, Jeremy D. Walston, Andrew G. Cheetham
  • Patent number: 10519137
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: December 31, 2019
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Steven John Woodhead, Michael Reader, Laurence Anne Mevellec, Patrick René Angibaud, Eddy Jean Edgard Freyne, Timothy Pietro Suren Perera, Berthold Wroblowski, Alexandra Papanikos, Olivier Alexis Georges Querolle, Isabelle Noëlle Constance Pilatte, Pascal Ghislain André Bonnet, Werner Constant Johan Embrechts, Rhalid Akkari, Lieven Meerpoel
  • Patent number: 10513497
    Abstract: Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.
    Type: Grant
    Filed: February 16, 2018
    Date of Patent: December 24, 2019
    Assignee: EIDOS THERAPEUTICS, INC.
    Inventors: Pooran Chand, Yogesh Kumar Gupta, Rakesh Kumar Kumawat, Mamoun Alhamadsheh, Robert Zamboni
  • Patent number: 10493089
    Abstract: A solid composition comprising sofosbuvir and at least one pharmaceutically acceptable matrix compound wherein at least 99 weight-% of the sofosbuvir comprised in the composition are present in amorphous form, at least 99 weight-% of the solid composition consist of the sofosbuvir and the at least one matrix compound, and wherein the solid composition contains the sofosbuvir in an amount of at least 55 weight-% based on the combined weight of the sofosbuvir and the at least one matrix compound.
    Type: Grant
    Filed: April 2, 2015
    Date of Patent: December 3, 2019
    Assignee: Sandoz AG
    Inventor: Nolwenn Martin
  • Patent number: 10471079
    Abstract: Combinations of certain analgesics with COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and the use of such combinations in methods of treatment, in particular for the treatment of pain.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: November 12, 2019
    Assignee: GRUENENTHAL GMBH
    Inventors: Klaus Schiene, Guenter Haase, Babette-Yvonne Koegel, Elmar Friderichs, Ulrich Jahnel
  • Patent number: 10472328
    Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: November 12, 2019
    Assignee: TOLERO PHARMACEUTICALS, INC.
    Inventors: Koc-Kan Ho, Yong Xu, Michael David Saunders, Xiaohui Liu, Scott Albert Pearce, Kevin Bret Wright, Jason Marc Foulks, Kenneth Mark Parnell, Steven Brian Kanner, David Lee Vollmer, Jihua Liu
  • Patent number: 10449253
    Abstract: A method of delivering or sequestering anesthetic agents by adsorption of such agents by porous partially fluorinated compounds which display high weight adsorption capacities. Such compounds have a non-covalent organic framework with a central ring, such as hexa, tetra, tri or di substituted benzenes which may be substituted or unsubstituted with alternating electron poor and electron rich groups such as tetra-, tri-, or di-fluorobenzenes, oligocyanobenzenes, oligochlorobenzene, and benzene, pirydone, triazole, pyrazole, pyridine, and substituted benzenes so that the compound forms a porous supramolecular structure; and adsorbs the anesthetic agent within the pores of a the compound.
    Type: Grant
    Filed: October 3, 2018
    Date of Patent: October 22, 2019
    Assignee: UNIVERSITY OF HOUSTON SYSTEM
    Inventors: Ognjen Miljanic, Teng-Hao Chen, Watchareeya Kaveevivitchai
  • Patent number: 10415093
    Abstract: Methods for diagnosing or monitoring endometriosis in a mammal are provided. The methods include the steps of determining the expression levels of BDNF and its receptor, Ntrk2, in a biological sample from the mammal, and determining that the mammal has endometriosis when the BDNF and Ntrk2 expression levels in the sample are elevated.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: September 17, 2019
    Assignees: MCMASTER UNIVERSITY, THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Warren Foster, Nicholas Leyland, Jocelyne Wessels, Sanjay Agarwal
  • Patent number: 10385051
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: October 22, 2018
    Date of Patent: August 20, 2019
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 10376527
    Abstract: The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or its pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: August 13, 2019
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Ankit Baheti, Bijay Kumar Padhi, Supritha Vakada, Rajeev Singh Raghuvanshi
  • Patent number: 10314841
    Abstract: The present invention provides compounds of Formula (II) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: June 11, 2019
    Assignee: Merck Patent GmbH
    Inventors: Catherine Jorand-Lebrun, Reinaldo Jones
  • Patent number: 10294207
    Abstract: Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKK? (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKK? and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.
    Type: Grant
    Filed: March 29, 2016
    Date of Patent: May 21, 2019
    Assignee: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Kisoo Park, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, Ickhwan Son, Sang-ho Ma, Kwang-Seop Song, Min Ju Kim, So Ok Park, Man-Young Cha, Mi-Soon Kim, Sang Mi Kang, Dong Hyuk Jang, Jangwon Hong
  • Patent number: 10287298
    Abstract: The present invention concerns compounds of formula (I), enantiomers, mixture of enantiomers, diastereoisomers and mixture of diasteroisomers thereof formula (I): wherein at least one of W, X and Y is selected from the group consisting of —NR1R2; —NR3—(CH2)n—NR4R5; —O—(CH2)n—NR4R5; —NR3—(CH2)n—N?R6R7R8; and —O—(CH2)n—N?R6R7R8 and Z is a functional group capable of chelating iron salts. The present invention also concerns the compounds of formula (I) for use as a drug, in particular, in the treatment of cancer and malaria.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: May 14, 2019
    Assignees: Centre National de la Recherche Scientifique (CNRS), Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Paris Descartes
    Inventors: Maryam Mehrpour, Raphael Rodriguez, Antje Hienzsch, Mai Trang, Ahmed Hamai
  • Patent number: 10251853
    Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: April 9, 2019
    Assignee: INNOVATIVE MED CONCEPTS, LLC
    Inventor: William L. Pridgen