Patents Examined by Laura L. Stockton
  • Patent number: 10703717
    Abstract: A novel type of water-soluble isatin derivatives, and manufacturing method and application thereof. An isatin derivative comprising a phenolic hydroxy group is used as the substrates. A dimethylaminomethylene group is introduced to an ortho position of the phenolic hydroxy group to significantly improve the water solubility of a class of compounds provided by the invention. An antitumor activity study showed that the activity of the class of compounds was not reduced, and even improved. The class of compounds has great prospects for applications in developing an antitumor pharmaceutical product.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: July 7, 2020
    Assignee: Tianjin University of Science & Technology
    Inventors: Peng Yu, Dong Wang, Yuou Teng, Longfei Miao, Jing Wang, Qian Zhang, Yuan Yuan
  • Patent number: 10703727
    Abstract: The present invention relates to a method for preparing substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives of the general formula (I) in which R1 represents a hydrogen atom or R1 represents a group selected from the series of C1-C3-alkyl-, C1-C3-alkoxy-, C1-C3-haloalkyl- and C1-C3-haloalkoxy-, R2 represents a hydrogen atom or a C1-C3-alkyl group, R3 represents a hydrogen atom or a C1-C3-alkyl group, R4 represents a cyclohexyl group, which is optionally singly or multiply substituted by a C1-C3-alkyl group, and R5 represents a hydrogen atom or a C1-C6-alkyl group; and also intermediates which may be used to prepare substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives.
    Type: Grant
    Filed: July 25, 2016
    Date of Patent: July 7, 2020
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventor: Heiko Schirmer
  • Patent number: 10696639
    Abstract: The present invention is directed to compounds of Formula (I), pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: June 30, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tanweer Khan, Elizabeth Smith, Peter Williams, Catherine Wiscount, Brian McKittrick, John McCauley
  • Patent number: 10696649
    Abstract: Compounds of Formula 1 and pharmaceutically acceptable compositions thereof are useful as TLR7/8 antagonists.
    Type: Grant
    Filed: November 26, 2019
    Date of Patent: June 30, 2020
    Assignee: Merck Patent GmbH
    Inventors: Brian A. Sherer, Nadia Brugger
  • Patent number: 10696687
    Abstract: Disclosed herein is a compound of formula (I) and/or a pharmaceutically acceptable salt thereof that can serve as Erk inhibitors. They are potentially useful in the treatment of diseases treatable by inhibition of Erk, such as cancers. Also disclosed herein is a pharmaceutical composition, comprising a compound of formula I and/or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: June 30, 2020
    Assignee: Changzhou Jiekai Pharmatech Co., LTD.
    Inventors: Jintao Zhang, Wen Xu, Shanzhong Jian
  • Patent number: 10689343
    Abstract: The invention relates to a compound of Formula I: Formula I, or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of tryptophan 2,3-dioxygenase. The invention also relates to the use of the compounds of Formula (I) for the treatment or prevention of cancer and central nervous system disease or disorder, either as a single agent or in combination with other therapies.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: June 23, 2020
    Assignee: NETHERLANDS TRANSLATIONAL RESEARCH CENTER B.V.
    Inventors: Adrianus Petrus Antonius De Man, Joost Cornelis Marinus Uitdehaag, Jan Gerard Sterrenburg, Joeri Johannes Petrus De Wit, Nicole Wilhelmina Cornelia Seegers, Antonius Maria Van Doornmalen, Rogier Christian Buijsman, Guido Jenny Rudolf Zaman
  • Patent number: 10689398
    Abstract: The present invention relates to oxa-diazaspiro compounds having pharmacological activity towards the sigma (?) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: June 23, 2020
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Marina Virgili-Bernado, Carmen Almansa-Rosales, Carlos Alegret-Molina
  • Patent number: 10669266
    Abstract: Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds have the following structure: in which Z is an oxadiazole. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2/Smad3 signaling pathway.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: June 2, 2020
    Assignees: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI, UNIVERSITY OF KANSAS
    Inventors: John Cijiang He, Ruijie Liu, Bhaskar Das, Wenzhen Xiao, Zhengzhe Li, Kyung Lee
  • Patent number: 10647703
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, X, R3a, R3b, R4a, R4b, G1, G2, G3, G4, L1, L2, m1, m2, m3, m4, and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: May 12, 2020
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Pingda Ren, Yi Liu
  • Patent number: 10647727
    Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: May 12, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Lehua Chang, Ashley Forster, Richard Berger, Kausik K. Nanda, William D. Shipe
  • Patent number: 10647721
    Abstract: The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; and R1 may be different if n is 2 or 3; R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, CN, lower alkoxy or lower alkoxy substituted by halogen; X is CH or N; m is 1, 2 or 3; -( )m is —(CH2)m—; n is 1, 2 or 3; Ar is a five membered heteroaryl group, selected from formula (A), (B), (C), (D), (E) or (F), wherein R3 is hydrogen, methyl or chloro; R4 is hydrogen or methyl; R5 is F, Cl, CHF2 or CF3; or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: May 12, 2020
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Michael Reutlinger, Greta Vastakaite
  • Patent number: 10640476
    Abstract: The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.
    Type: Grant
    Filed: September 30, 2019
    Date of Patent: May 5, 2020
    Assignee: XW LABORATORIES INC.
    Inventors: Jia-Ning Xiang, Xuesong Xu, Wei Zhou
  • Patent number: 10644249
    Abstract: The present disclosure relates to compounds of Formula (I), (II), (III), (IV), or (V): as compounds capable of emitting delayed fluorescence, and uses of the compounds in organic light-emitting diodes.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: May 5, 2020
    Assignee: KYULUX, INC.
    Inventors: Yu Seok Yang, Shuo-Hsien Cheng, Yoshitake Suzuki, Hayato Kakizoe, Ayataka Endo, Jorge Aguilera-Iparraguirre, Rafael Gomez-Bombarelli, Timothy D. Hirzel
  • Patent number: 10633351
    Abstract: A halogenated compound, an axially chiral isomer thereof, and an application thereof in preparing drugs for disorders closely related to aberrant levels of uric acid.
    Type: Grant
    Filed: June 13, 2017
    Date of Patent: April 28, 2020
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Jianfei Wang, Yang Zhang, Shuhui Chen
  • Patent number: 10633354
    Abstract: Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R2 is —OH or —OP(O)(OH)2; and R1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: April 28, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: David Marcoux, Hai-Yun Xiao, T. G. Murali Dhar, Alaric J. Dyckman
  • Patent number: 10626092
    Abstract: Crystalline polymorph forms of 3-[2-butyl-1-(2-diethylamino-ethyl)-1H-benzoimidazol-5-yl]-N-hydroxy-acrylamide are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of diseases and conditions are also presented.
    Type: Grant
    Filed: May 1, 2017
    Date of Patent: April 21, 2020
    Assignee: MEI PHARMA, INC.
    Inventor: David Duncan
  • Patent number: 10618890
    Abstract: Benzimidazole sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma ROR?t are described. Pharmaceutical compositions including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: April 14, 2020
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Gilles Ouvry, Etienne Thoreau, Claire Bouix-Peter
  • Patent number: 10611737
    Abstract: The present disclosure relates to a method for preparing aryl 2-tetrazol-2-yl ketone of the following Formula 1a with improved selectivity: wherein R1 and R2 are the same as defined herein.
    Type: Grant
    Filed: October 24, 2019
    Date of Patent: April 7, 2020
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Kyuwoong Lee, Kyungmi Cha, Suyeon Yeom, Jiseon Woo
  • Patent number: 10611730
    Abstract: Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: April 7, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Suchitra Ravula, Devin M. Swanson, Bradley M. Savall
  • Patent number: 10604530
    Abstract: Crystalline solid forms of methyl {(2S)-1-[(2S,5S)-2-(9-{2-[(2S,4S)-1-{(2R)-2-[(methoxycarbonyl)amino]-2-phenylacetyl}-4-(methoxymethyl)pyrrolidin-2-yl]-1H-imidazol-5-yl}-1,11-dihydroisochromeno[4?,3?:6,7]naphtho[1,2-d]imidazol-2-yl)-5-methylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl}carbamate (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using these crystalline forms.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: March 31, 2020
    Assignee: Gilead Pharmasset LLC
    Inventors: Olga Viktorovna Lapina, Bing Shi, Fang Wang, Scott Alan Wolckenhauer