1,3-diazines (e.g., Pyrimidines, Etc.) Patents (Class 514/256)
  • Patent number: 10716788
    Abstract: The present invention provides methods of treating MS using pyrimidine and pyridine compounds which are inhibitors of Bruton's tyrosine kinase (BTK).
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: July 21, 2020
    Assignee: Merck Patent GmbH
    Inventor: Tammy Dellovade
  • Patent number: 10709707
    Abstract: Described herein are methods and pharmaceutical formulations for treating ocular conditions.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: July 14, 2020
    Assignee: Oyster Point Pharma, Inc.
    Inventors: Douglas Michael Ackermann, James Loudin, Kenneth J. Mandell
  • Patent number: 10702589
    Abstract: The present disclosure provides the use of Akr1b8, an agonist of Akr1b8, Akr1B10, or an agonist of Akr1B10 in methods and compositions for the treatment of neurological disorders and stress-induced conditions. Methods of increasing the levels of 5Thr3a on neuronal cells is also provided by contacting the neuronal cells with Akr1b8, an agonist of Akr1b8, Akr1B10, or an agonist of Akr1B10.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: July 7, 2020
    Assignee: ANN AND ROBERT H. LURIE CHILDREN'S HOSPITAL OF CHICAGO
    Inventor: Jhumku D. Kohtz
  • Patent number: 10702525
    Abstract: The pyrimidine derivatives as anti-diabetic agents are chloropyrimidinyl derivatives having the general formula of compound 81, wherein R1 is —N(CH3)CH2CH2OH (compound 81c) or —N(H)CH2CH2OH (compound 81f) or the general formula of compound 82, wherein R2 is —N(CH3)CH2CH2OH (compound 82c) or —N(CH2CH2)2O (compound 82d), as follows: The derivatives may be used for treating diabetes in humans or animals and have demonstrated efficacy, specifically in treating type 2 diabetes. Two methods of synthesizing the pyrimidine derivatives are described herein. The method using microwaves (Method B) is a green method that can provide high yields in a short time and with high purity. The compounds act as GLP-1 receptor agonists and are more potent than conventional drugs. As such, the compounds may be used in lower doses, and, hence, have fewer side effects.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: July 7, 2020
    Assignee: United Arab Emirates University
    Inventors: Abdu Adem, Shaikha S. Al Neyadi, Ibrahim M. Abdu, Alaa A. Salem, Naheed Amir
  • Patent number: 10702524
    Abstract: The present invention falls within the field of medical technology, and in particular relates to the use of a compound as shown in formula (I). In particular, the present invention relates to the use of the compound as shown in formula (I) in the preparation of a pharmaceutical composition for preventing and/or treating a nerve injury, or relieving a nerve injury-associated symptom, and further relates to the use thereof in the preparation of a healthcare product for protecting an injured nerve and/or improving motor function. After a nerve injury has occurred, the compound can reduce the production of pro-inflammatory cytokine, decrease the level of apoptosis, promote the survival of neuron, inhibit the formation of glial scar, and has a significant effect in promoting the recovery of motor function.
    Type: Grant
    Filed: October 10, 2017
    Date of Patent: July 7, 2020
    Inventors: Shiqing Feng, Xue Yao
  • Patent number: 10696666
    Abstract: A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.
    Type: Grant
    Filed: October 18, 2017
    Date of Patent: June 30, 2020
    Assignee: CELLCENTRIC LIMITED
    Inventors: Neil Anthony Pegg, Stuart Thomas Onions, David Michel Adrien Taddei, Jonathan Shannon, Silvia Paoletta, Richard James Brown, Don Smyth, Gareth Harbottle
  • Patent number: 10662188
    Abstract: This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: May 26, 2020
    Assignee: ADVERIO PHARMA GmbH
    Inventors: Birgit Keil, Franz-Josef Mais, Winfried Joentgen, Alfons Grunenberg
  • Patent number: 10654861
    Abstract: A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: May 19, 2020
    Assignee: UCB Biopharma SRL
    Inventors: Michael Louis Robert Deligny, Jag Paul Heer, Jean Keyaerts, Luce Elsa Lepissier, Martin Alexander Lowe
  • Patent number: 10646429
    Abstract: The present disclosure relates to methods of retarding hair loss or facilitating hair growth and/or regrowth. More specifically, the present disclosure relates to methods of using the disclosed compositions to increase the rate of terminal hair growth and/or regrowth in a mammal.
    Type: Grant
    Filed: July 31, 2018
    Date of Patent: May 12, 2020
    Assignee: Johnson & Johnson Consumer Inc.
    Inventors: Longsheng Hu, Virginia Streusand Goldman, Josephine A. Minerva, Susan Wendling
  • Patent number: 10633356
    Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: February 19, 2019
    Date of Patent: April 28, 2020
    Assignee: ADVERIO PHARMA GMBH
    Inventors: Peter Fey, Alfons Grunenberg, Donald Bierer
  • Patent number: 10610518
    Abstract: Described herein are methods and compositions for the treatment of ocular conditions and for the improvement of vision parameters using pharmaceutically acceptable ophthalmic pilocarpine formulations. A nonlimiting example of an ocular condition that may be treated with the methods and compositions disclosed herein is presbyopia.
    Type: Grant
    Filed: April 24, 2019
    Date of Patent: April 7, 2020
    Assignee: ALLERGAN, INC.
    Inventors: Michael R. Robinson, Mohammed Dibas, Jaya Giyanani, Anuradha Gore, Sungwook Lee, Haixia Liu, Aileen Morgan, Jihao Zhou
  • Patent number: 10603294
    Abstract: The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.
    Type: Grant
    Filed: January 15, 2019
    Date of Patent: March 31, 2020
    Assignee: Innovation Pharmaceuticals Inc.
    Inventors: Richard W. Scott, Bozena Korczak
  • Patent number: 10603313
    Abstract: Disclosed herein are compounds, of the class of amine-bearing heterocycles, which act as positive allosteric modulators and silent allosteric modulators of the mu opioid receptor. These compounds are useful for the treatment of pain, drug addiction, and other CNS derived maladies that are controlled directly or indirectly by activation of the mu opioid receptor. Methods for making and using the allosteric modulators disclosed herein are also provided.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: March 31, 2020
    Assignee: CHIROMICS, LLC
    Inventors: Joel Francis Austin, Michael David VanHeyst, James S. Harvey, Elizabeth Gerig Rowley, Christophe Lamarque-Lacoste
  • Patent number: 10568885
    Abstract: The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, pharmaceutical compositions containing the same, processes for preparing the same, and methods of medical treatment using the same.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: February 25, 2020
    Assignee: Centrexion Therapeutics Corporation
    Inventors: Markus Ostermeier, Ulrike Werthmann
  • Patent number: 10556897
    Abstract: The present invention is directed to novel protein kinase inhibitors comprising the chemical compound N-(2-chloro-6-methylphenyl)-2-[[2-methyl-6-(3-hydroxypyrrolidin-1-yl)pyrimidin-4-yl]amino]thiazole-5-carboxamide, its pharmaceutically acceptable salts, enantiomers, and enantiomeric mixtures, and methods of use to treat protein kinase-mediated diseases or conditions.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: February 11, 2020
    Assignee: Princeton Drug Discovery, Inc
    Inventor: Kan He
  • Patent number: 10556890
    Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: February 11, 2020
    Assignees: Sunovion Pharmaceuticals Inc., PGI DRUG DISCOVERY LLC
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Patent number: 10543215
    Abstract: Disclosed herein are combination therapies for the treatment of heart failure using a cardiac myosin activator, such as omecamtiv mecarbil, and a sinus node If current inhibitor, such as ivabradine. Also disclosed herein are compositions comprising a cardiac myosin activator and a sinus node If current inhibitor.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: January 28, 2020
    Assignee: AMGEN INC.
    Inventors: Robert Andrew Donald Scott, Scott Wasserman
  • Patent number: 10538527
    Abstract: The present invention provides a compound of Formula II, and salts thereof, and a pharmaceutical composition comprising a compound of Formula II: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, and wherein R3 is hydrogen, an alkyl group having from one to ten carbon atoms, or a halogen. Preferably the compound of Formula II includes wherein R3 is a halogen, and most preferably wherein the halogen is chlorine. Methods of treating a patient with cancer with these compounds are also provided.
    Type: Grant
    Filed: February 4, 2019
    Date of Patent: January 21, 2020
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10537571
    Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: January 21, 2020
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Dominic Reynolds, Ming-Hong Hao, John Wang, Sudeep Prajapati, Takashi Satoh, Anand Selvaraj
  • Patent number: 10517873
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide.
    Type: Grant
    Filed: February 4, 2019
    Date of Patent: December 31, 2019
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Marie Georges Beauchamps, Antonio Christian Ferretti, Robert Hilgraf, Mohit Atul Kothare, Hon-Wah Man, Mark A. Nagy, Kelvin Hin-Yeong Yong, Nanfei Zou
  • Patent number: 10508105
    Abstract: Indazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease states associated with glutamate dysfunction.
    Type: Grant
    Filed: August 16, 2018
    Date of Patent: December 17, 2019
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Andrew S. Felts, Colleen M. Niswender, Rory A. Capstick, Paul K. Spearing, Sean R. Bollinger
  • Patent number: 10508104
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: December 17, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: George O. Tora, Heather Finlay, Wen Jiang, Wei Meng, Xiaojun Zhang
  • Patent number: 10494346
    Abstract: The present invention relates to a novel pyrimidine-4-carboxylic acid derivative having an anticancer activity, and the compound thereof is useful as a drug for treating and preventing tumor diseases, wherein the compound is represented by the Formula 1: or a pharmaceutically acceptable salt thereof, wherein: Q is a C6-C15 aryl group; or a C4-C13 heteroaryl group, wherein the heteroaryl contains 1, 2 or 3 heteroatoms substituted with 1-3 heteroatom(s) selected from the group consisting of nitrogen, oxygen or sulfur; R is a halogen; a C1-C10 haloalkyl substituted with 1-13 halogen atom(s); a C1-C10 alkoxy; a 5- or 6-membered heterocycloalkyl or (CH2)r-R1 wherein the heterocycloalkyl contains 1-2 heteroatom(s) selected from the group consisting of nitrogen and oxygen; R1 is a hydrogen; a C1-C10 alkoxy; amino; mono(C1-C10 alkyl)amino; di(C1-C10 alkyl)amino; or —NHC(O)-phenyl; n is 1, 2, 3, 4, 5, or 6; and r is 0, 1, 2, 3, 4, 5, or 6; and m is 0, 1, 2 or 3.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: December 3, 2019
    Assignees: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY, INDUSTRY-UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY
    Inventors: Tae Bo Sim, Woo Young Hur, Ho Jong Yoon, Chi Man Song, In Jae Shun, Byeong Yun Lim, Han Na Cho, Seung Hye Choi, Gu Kong, Jeong Yeon Lee
  • Patent number: 10485801
    Abstract: The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: November 26, 2019
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Gerard M. P. Giblin, David T. MacPherson, David R. Witty, Steven J. Stanway
  • Patent number: 10464906
    Abstract: This disclosure provides solid forms of 2-((2-chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide, and methods of manufacturing and using these forms.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: November 5, 2019
    Assignee: ACETYLON PHARMACEUTICALS, INC.
    Inventors: John H. van Duzer, Farzaneh Seyedi, Gui Liu
  • Patent number: 10457667
    Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from or the oxygen atom may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen or oxetanyl; R2 is hydrogen, lower alkyl lower alkoxy, halogen or cycloalkyl; --- the dotted line is nothing or may be —CH2—; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: October 29, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Patent number: 10420757
    Abstract: The current disclosure relates to methods for treating pancreatic cancer or chronic pancreatitis in a subject comprising administering an antagonist of a dopamine receptor to the subject wherein the dopamine receptor is, in some specific cases dopamine receptor D2 (DRD2). The antagonist in some specific cases is an RNAi construct, an antibody, or a small molecule and in more specific cases pimozide or L-741,626. The disclosure also relates to diagnostic methods comprising the detection of the expression of DRD2 in pancreatic tissue and kits for doing the same.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: September 24, 2019
    Assignees: Deutsches Krebsforschungszentrum Stiftung des Öffentlichenrechts, The Royal Institution for the Advancement of Learning/McGill University
    Inventors: Pouria Jandaghi, Jörg Hoheisel, Yasser Riazalhosseini
  • Patent number: 10421756
    Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I) or any one of Compounds 100-175) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
    Type: Grant
    Filed: July 5, 2016
    Date of Patent: September 24, 2019
    Assignee: Rodin Therapeutics, Inc.
    Inventors: Martin R. Jefson, John A. Lowe, III, Fabian Dey, Andreas Bergmann, Andreas Schoop
  • Patent number: 10414766
    Abstract: The present invention relates to novel polymorph of riociguat and process for preparing the polymorph. The present invention also relates to the improved process for the preparation of riociguat.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: September 17, 2019
    Assignee: ALEMBIC PHARMACEUTICALS LIMITED
    Inventors: Mahender Rao Siripragada, Mahendar Velisoju, Tejas Shah, Chetan Patil, Kalpesh Jadav, Ashvinkumar Bhuva, Saisuryanaraya Donthukurthi
  • Patent number: 10398694
    Abstract: An oral disintegrating tablet which contains rosuvastatin or a salt thereof and is stable to light is provided. An oral disintegrating tablet stable to light, temperature and humidity can be provided by preparing a multi-layered tablet containing rosuvastatin or a pharmaceutically acceptable salt thereof as an active ingredient, a light stabilizer, and an inorganic salt or a basic oxide.
    Type: Grant
    Filed: May 3, 2017
    Date of Patent: September 3, 2019
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Kentaro Hayashi, Toshitada Toyoda, Yoshitsugu Muguruma
  • Patent number: 10370371
    Abstract: Amine substituted pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: August 6, 2019
    Assignee: PTC Therapeutics, Inc.
    Inventors: Wu Du, Ramil Baiazitov, Chang-Sun Lee, Young-Choon Moon, Steven D. Paget, Hongyu Ren, Nadiya Sydorenko, Richard Gerald Wilde
  • Patent number: 10335518
    Abstract: A method to prepare a catheter locking formulation, comprising in a first step, dissolving trimethoprim in propylene glycol at a temperature greater than room temperature, and in a final step, adding absolute ethanol at about room temperature to a solution of trimethoprim, propylene glycol, EDTA Calcium Disodium Hydrate, phosphate buffered saline, and glycerin.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: July 2, 2019
    Inventors: Krzysztof Appelt, Michael Lanzilotti
  • Patent number: 10316032
    Abstract: Solid forms of Compound I (and its S-enantiomer, Compound II), active on protein kinases, were prepared and characterized: Also provided are methods of using the solid forms.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: June 11, 2019
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Gary Conard Visor
  • Patent number: 10307423
    Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: June 4, 2019
    Assignees: University of Pittsburgh - Of the Commonwealth System of Higher Education, The United States Government as represented by the Department of Veterans Affairs
    Inventors: Beibei Chen, Rama K. Mallampalli
  • Patent number: 10292391
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: July 18, 2016
    Date of Patent: May 21, 2019
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Michel Muehlebach, Pierre Joseph Marcel Jung, Andrew Edmunds, Daniel Emery, Anke Buchholz
  • Patent number: 10246420
    Abstract: The present invention relates to novel pyrazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for controlling harmful microorganisms in crop protection and in the protection of materials. Further, the present invention also relates to certain intermediates useful for producing said novel pyrazole derivatives.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: April 2, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Joachim Telser, Peter Dahmen, Ulrike Wachendorff-Neumann, Pierre Cristau, Philippe Rinolfi
  • Patent number: 10213428
    Abstract: The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, pharmaceutical compositions containing the same, processes for preparing the same, and methods of medical treatment using the same.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: February 26, 2019
    Assignee: Centrexion Therapeutics Corporation
    Inventors: Markus Ostermeier, Ulrike Werthmann
  • Patent number: 10206894
    Abstract: The present invention provides methods for treating and/or preventing mucositis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: February 19, 2019
    Assignee: Innovation Pharmaceuticals Inc.
    Inventors: Richard W. Scott, Bozena Korczak
  • Patent number: 10206904
    Abstract: Derivatives of licofelone for the treatment of chronic inflammatory diseases and epithelial cancers associated with chronic inflammation are disclosed. The agents target mPGES-1 and 5-LOX.
    Type: Grant
    Filed: July 13, 2016
    Date of Patent: February 19, 2019
    Assignee: The Board of Regents of the University of Oklahoma
    Inventors: Chinthalapally V. Rao, Naveena B. Janakiram, Hariprasad Gali, Altaf Mohammed, Gopal Pathuri
  • Patent number: 10202365
    Abstract: Described herein are compounds, such as compounds of Formula (I) and pharmaceutically acceptable salts thereof, that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions, e.g.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: February 12, 2019
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Natasja Brooijmans, Lucian V. DiPietro, Paul E. Fleming, Joseph L. Kim, Steven Mark Wenglowsky, Yulian Zhang
  • Patent number: 10202378
    Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1-R6 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various TAF1-mediated disorders.
    Type: Grant
    Filed: July 24, 2017
    Date of Patent: February 12, 2019
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Marc Adler, Daniel J. Burdick, Terry Crawford, Martin Duplessis, Steven R. Magnuson, Christopher G. Nasveschuk, F. Anthony Romero, Yong Tang, Vickie Hsiao-Wei Tsui, Shumei Wang
  • Patent number: 10179131
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: 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: July 13, 2016
    Date of Patent: January 15, 2019
    Assignee: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Hui Cao, Wei Li, Xiaowen Peng, Meizhong Jin, Jorden Kass, Xuri Gao, Yat Sun Or
  • Patent number: 10174018
    Abstract: The present invention is directed to novel protein kinase inhibitors comprising the chemical compound N-(2-chloro-6-methylphenyl)-2-[[2-methyl-6-(3-hydroxypyrrolidin-1-yl)pyrimidin-4-yl]amino]thiazole-5-carboxamide, its pharmaceutically acceptable salts, enantiomers, and enantiomeric mixtures, and methods of use to treat protein kinase-mediated diseases or conditions.
    Type: Grant
    Filed: December 12, 2017
    Date of Patent: January 8, 2019
    Assignee: Princeton Drug Discovery Inc
    Inventor: Kan He
  • Patent number: 10130619
    Abstract: The present invention is related to amino thiazole derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: November 20, 2018
    Assignee: GENKYOTEX SUISSE SA
    Inventors: Peter Machin, Andrew Sharpe, Christopher James Lock, Mark S. Chambers, Alastair Hodges, Vivienne Allen, John M. Ellard
  • Patent number: 10125144
    Abstract: The invention provides novel inhibitors of ROCK1 and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCK1 and/or ROCK2. The present invention includes pharmaceutical compositions comprising the compounds of the invention and a pharmaceutically acceptable carrier and/or diluents. The present invention includes compositions comprising a substantially pure compound of the invention and a pharmaceutically acceptable salt, steroisomer, or hydrate thereof: and a pharmaceutically acceptable excipient and/or diluents.
    Type: Grant
    Filed: October 7, 2014
    Date of Patent: November 13, 2018
    Assignee: KADMON CORPORATION, LLC
    Inventors: Ji-in Kim, Kevin Liu, Masha Poyurovsky, Dan Lu, Zhenping Zhu
  • Patent number: 10123995
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: November 13, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric Mertz, Weiguo Liu, Scott D. Edmondson, Amjad Ali, Ying-Duo Gao, Santhosh F. Neelamkavil, Sung-Sau So, Remond Moningka, Wanying Sun, Alan Hruza, Linda L. Brockunier
  • Patent number: 10111827
    Abstract: The embodied invention generally pertains to compositions, and the methods of making and using said compositions for promoting hair growth, slowing hair loss, and for preventing or minimizing hair loss that are effective and able to treat multiple aspects of the problem in one product and additionally is comprised of natural oils and minerals which greatly reduce the toxicities and side effect issues associated with present products. The compositions or formulations of the present invention relate to a hair loss solution that solves the problems associated with the loss, and damage of hair by working from the root to the surface of the scalp and to the hair shaft by treating a plurality of the causes and/or triggers associated with hair loss, or the prevention of hair re-growth.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: October 30, 2018
    Assignee: Blooming Rose Cosmetics, Inc.
    Inventor: Ruzanna Kirakosyan
  • Patent number: 10106524
    Abstract: The present invention relates to 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase having the structure shown in Formula (I) wherein the radicals are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes or metabolic disorders.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: October 23, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Andrés Avelino Trabanco-Suárez, Óscar Delgado-González, Henricus Jacobus Maria Gijsen, Michiel Luc Maria Van Gool, Sven Franciscus Anna Van Brandt, Michel Anna Jozef De Cleyn, Santos Fustero Lardiés, Natalia Mateu Sanchís
  • Patent number: 10098949
    Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminum salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: October 16, 2018
    Assignee: GLAXOSMITHKLINE BIOLOGICALS S.A.
    Inventors: Manmohan Singh, David A. G. Skibinksi, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
  • Patent number: RE48057
    Abstract: A pesticidal composition comprises a compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R4, R5, R6, R7, Z, Q, and Y are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests, or to an area to control pests.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: June 23, 2020
    Assignee: DOW AGROSCIENCES LLC
    Inventors: Noormohamed M. Niyaz, Ann M. Buysse, David A. Demeter, Negar Garizi, Ricky Hunter, Daniel Knueppel, Paul R. LePlae, Christian T. Lowe, Akshay Patny, Tony K. Trullinger, Martin J. Walsh, Yu Zhang