1,3-diazines (e.g., Pyrimidines, Etc.) Patents (Class 514/256)
  • 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: 10092526
    Abstract: A method for treating a respiratory injury or disease comprising: administering to a patient in need of treatment a pharmaceutical composition comprising a compound of general Formula I: or salt, ester, solvate, hydrate, or prodrug thereof; wherein: x is an integer from 1 to 10; A and B are each, independently, C3-7cycloalkyl, C3-7cycloalkyl-C1-6alkyl, C3-7heterocycloalkyl, C3-7heterocycloalkyl-C1-6alkyl, C6-10aryl, C6-10aryl-C1-6alkyl, C3-9heteroaryl, or C3-9heteroaryl-C1-6alkyl; and n and p are each, independently, integers from 1 to 10; and a pharmaceutically acceptable carrier, excipient, or diluent.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: October 9, 2018
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Beibei Chen, Rama Mallampalli
  • Patent number: 10071992
    Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: September 11, 2018
    Assignee: Pfizer Inc.
    Inventors: Markus Boehm, Shawn Cabral, Matthew S. Dowling, Kentaro Futatsugi, Kim Huard, Esther Cheng Yin Lee, Allyn T. Londregan, Jana Polivkova, David A. Price, Qifang Li
  • Patent number: 10005757
    Abstract: Provided are revaprazan hydrochloride polymorphs and a preparation method thereof. The method comprises a step of dissolving revaprazan hydrochloride in ethanol or aqueous solutions of ethanol having different proportions to perform recrystallization.
    Type: Grant
    Filed: November 12, 2015
    Date of Patent: June 26, 2018
    Assignee: Jiangsu Tasly Diyi Pharmaceutical Co., Ltd.
    Inventors: Wenzheng Liu, Guocheng Wang, Qingwei Hou, Hongguang Meng
  • Patent number: 9987262
    Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
    Type: Grant
    Filed: May 30, 2017
    Date of Patent: June 5, 2018
    Assignee: Akebia Therapeutics, Inc.
    Inventors: James Densmore Copp, Ann W. Newman, Anne Luong
  • Patent number: 9987277
    Abstract: The present invention relates to the use of carboxamide 4-[(4-pyridyl)amino]-pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections.
    Type: Grant
    Filed: October 4, 2007
    Date of Patent: June 5, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Pierre Jean-Marie Bernard Raboisson, Oliver Lenz, Tse-I Lin, Kenneth Simmen
  • Patent number: 9981918
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Grant
    Filed: August 28, 2012
    Date of Patent: May 29, 2018
    Assignee: CHDI Foundation, Inc.
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, Peter Johnson, Ignacio Muñoz-Sanjuán, Stephen Martin Courtney, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena
  • Patent number: 9975876
    Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: May 22, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 9963451
    Abstract: Provided is a pest control agent containing a fused ring pyrimidine compound represented by the following formula (I) or a salt thereof as an effective component. In formula (I), A represents a nitrogen atom or C—R4, B represents a nitrogen atom or C—R5, D represents a nitrogen atom or C—R6, X represents an oxygen atom, N—R7 or the like, each of R1, R2, R4 and R6 independently represents a hydrogen atom or the like, each of R3a and R3b independently represents a hydrogen atom or the like, R5 represents an alkylthio group or the like, R7 represents an alkoxy group or the like, and Ht represents a pyridyl group that may be substituted, or the like.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: May 8, 2018
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Takahiko Ochi, Takeo Wakita, Toshiyuki Kono, Kazuki Kitajima, Shinichi Banba, Ayumi Kawase, Atsuko Kawahara, Kazuyuki Sato
  • Patent number: 9957278
    Abstract: Compounds of formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: May 1, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Kyle J. Eastman, Zhongxing Zhang, Kyle E. Parcella, John F. Kadow
  • Patent number: 9956158
    Abstract: Technologies are described for a formulation and production of a formulation. The methods may comprise depositing a non-steroidal anti-inflammatory drug (NSAID) compound, a calcium channel blocker, an immunosuppressive component, an anti-hypertensive, a hormone, a steroid, and an enzyme inhibitor into a chamber. The methods may comprise milling and mixing the NSAID compound, the calcium channel blocker, the immunosuppressive component, the anti-hypertensive, the hormone, the steroid, and the enzyme inhibitor into a powder. The methods may comprise adding a solvent with the powder. The methods may comprise mixing the solvent with the powder to form the formulation.
    Type: Grant
    Filed: September 8, 2017
    Date of Patent: May 1, 2018
    Assignee: Synergistic Therapeutics, LLC
    Inventors: Anthony H. Salce, Jr., William F. Greenwood, Shivsankar Misir
  • Patent number: 9951065
    Abstract: The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: April 24, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Mark J. Bartlett, Julian Andrew Codelli, Britton Kenneth Corkey, Jennifer Leigh Cosman, Kristyna Elbel, Jennifer Alissa Loyer-Drew, David Sperandio, Joshua Van Veldhuizen, Hai Yang, Suet Chung Yeung
  • Patent number: 9931342
    Abstract: The present disclosure provides compositions and methods for the treatment of cancer, relating to the specific inhibition of Abelson (ABL) kinases.
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: April 3, 2018
    Inventor: Ann Marie Pendergast
  • Patent number: 9926280
    Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: March 27, 2018
    Assignee: Buck Institute for Research on Aging
    Inventors: Varghese John, Dale E. Bredesen
  • Patent number: 9913863
    Abstract: The present invention relates to a phenotypically distinct CD1dhighCD5+ B cell subset that regulates T cell mediated inflammatory responses through the secretion of interleukin-10 (IL-10). The invention also relates to the use of these IL-10 producing regulatory B cells in the manipulation of immune and inflammatory responses, and in the treatment of disease. Therapeutic approaches involving adoptive transfer of these regulatory B cells, or expansion of their endogenous levels for controlling autoimmune or inflammatory diseases and conditions are described. Ablation of this subset of regulatory B cells, or inhibition of their IL-10 production can be used to upregulate immunodeficient conditions, and/or to treat tumors/cancer. Diagnostic applications also are encompassed.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: March 13, 2018
    Assignee: Duke University
    Inventors: Thomas F. Tedder, Koichi Yanaba, Jean-David Bouaziz
  • Patent number: 9814714
    Abstract: The present disclosure provides methods of treating a subject suffering from or at risk of a BRAF V600 mutation or BRAF fusion mutation related disease or condition, without activating the MAPK pathway or inducing expression of MAPK pathway genes in cells harboring wild-type BRAF.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: November 14, 2017
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Chao Zhang, Wayne Spevak, Jiazhong Zhang, Guoxian Wu, Jack Lin, Hanna Cho, Marika Nespi, Songyuan Shi, Todd Ewing, Ying Zhang, Gideon Bollag
  • Patent number: 9814688
    Abstract: Topical and wash compositions comprising a polymeric biguanide or a bis(biguanide) compound, a chelating agent and a buffering agent and methods for using these compositions for the prevention or treatment of skin or ear tissue infections is provided.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: November 14, 2017
    Assignee: Dermcare-Vet Pty Ltd
    Inventor: Kenneth Vincent Mason
  • Patent number: 9808459
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: November 7, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Patent number: 9796677
    Abstract: Provided is a novel compound which has an excellent A? aggregation inhibitory effect and is useful as a pharmaceutical. An amide compound represented by the formula (1) or a salt thereof, wherein Z represents CH or N; A and B are the same or different and each represents —CH2—, —O—, —S—, or —NH—; R1 and R2 are the same or different and each represents a branched alkyl group, a branched alkenyl group, an optionally substituted aromatic hydrocarbon group, an optionally substituted aralkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aromatic heterocyclic group; and R3 represents a branched alkyl group, a branched alkenyl group, an optionally substituted cycloalkyl group, or an optionally substituted aralkyl group.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: October 24, 2017
    Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Motomu Kanai, Yohei Soma, Tadamasa Arai, Takushi Araya
  • Patent number: 9776962
    Abstract: Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity and a GLP-1 secretagogue action, is useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and affords superior efficacy.
    Type: Grant
    Filed: August 8, 2014
    Date of Patent: October 3, 2017
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Jumpei Aida, Yayoi Yoshitomi, Yuko Hitomi, Naoyoshi Noguchi, Yasuhiro Hirata, Hideki Furukawa, Akito Shibuya, Koji Watanabe, Yasufumi Miyamoto, Tomohiro Okawa, Nobuyuki Takakura, Seiji Miwatashi
  • Patent number: 9738633
    Abstract: The invention relates generally to muscarinic agonists, which are useful for stimulating muscarine receptors, and treating cognitive disorders. Included among the muscarinic agonists disclosed herein are oxadiazole derivatives, compositions, and preparations thereof. Methods of synthesizing oxadiazole compounds also are provided. This disclosure also relates in part to compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. This disclosure relates in part to methods of treating animals such as humans by administering such compositions.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: August 22, 2017
    Assignee: Neurosolis, Inc.
    Inventors: Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson, Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone
  • Patent number: 9730931
    Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: August 15, 2017
    Assignee: EISAI R&D Management Co., Ltd.
    Inventors: Dominic Reynolds, Ming-Hong Hao, John Wang, Sudeep Prajapati, Takashi Satoh, Anand Selvaraj
  • Patent number: 9730930
    Abstract: Compounds I and II, as well as prodrugs, hydrates, solvates, N-oxides, salts and pharmaceutical compositions containing them, are useful for treating vitiligo. In certain embodiments, the compounds are provided in topical compositions.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: August 15, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventor: Daniel Magilavy
  • Patent number: 9718788
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: August 1, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil
  • Patent number: 9708293
    Abstract: The present invention relates to N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: July 18, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich Lücking, Niels Böhnke, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Dirk Kosemund, Rolf Bohlmann, Ludwig Zorn
  • Patent number: 9700503
    Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include bimatoprost and minoxidil in a vehicle for topical application to the skin of a mammal, e.g. a human, whereby the combination of bimatoprost and minoxidil produces a faster onset of hair growth in humans or other mammals and wherein said composition brings about a synergistic result of faster onset of hair growth as compared to compositions comprising bimatoprost and minoxidil, alone.
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: July 11, 2017
    Assignee: ALLERGAN, INC.
    Inventors: David F. Woodward, Jenny W. Wang
  • Patent number: 9701636
    Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: July 11, 2017
    Assignee: Akebia Therapeutics, Inc.
    Inventors: James Densmore Copp, Ann W. Newman, Anne Luong
  • Patent number: 9694024
    Abstract: The present invention relates to compounds and methods for treating retroviral infections and/or Hepatitis B viral infections. Some compounds of the invention are described by Formula I: or a stereoisomer, a diastereomer, an enantiomer or racemate thereof.
    Type: Grant
    Filed: February 16, 2016
    Date of Patent: July 4, 2017
    Assignee: Chimerix, Inc.
    Inventor: Ernest Randall Lanier
  • Patent number: 9657007
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: May 23, 2017
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Liang Wang, Tingjin Wang
  • Patent number: 9643955
    Abstract: The present invention is directed to 2-pyridyloxy-3-nitrile-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-nitrile-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: May 9, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 9637458
    Abstract: The present disclosure provides substituted pyrimidine carboxamides of Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: May 2, 2017
    Inventors: Jeffrey Lockman, Chiyou Ni, Jae Hyun Park, Minnie Park, Bin Shao, Laykea Tafesse, Jiangchao Yao, Mark A. Youngman
  • Patent number: 9636296
    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: October 10, 2014
    Date of Patent: May 2, 2017
    Assignee: Johnson & Johnson Consumer Inc.
    Inventors: Longsheng Hu, Virginia Streusand Goldman, Josephine A. Minerva, Susan Wendling
  • Patent number: 9604948
    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: July 10, 2015
    Date of Patent: March 28, 2017
    Assignee: ADVERIO PHARMA GMBH
    Inventors: Peter Fey, Alfons Grunenberg, Donald Bierer
  • Patent number: 9597330
    Abstract: It is intended to provide a therapeutic agent and/or a preventive agent for a respiratory disease or a therapeutic agent and/or a preventive agent for a sodium channel associated disease.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: March 21, 2017
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Sakiko Takahashi, Yuki Domon, Yutaka Kitano, Tsuyoshi Shinozuka