Patents Examined by Patricia L. Morris
  • Antifungal compounds and processes for making
    Patent number: 10676459
    Abstract: The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.
    Type: Grant
    Filed: August 20, 2019
    Date of Patent: June 9, 2020
    Assignee: MYCOVIA PHARMACEUTICALS, INC.
    Inventors: William J. Hoekstra, David Dale Wirth, Tracy Ehiwe, Thierry Bonnaud
  • Pyridyl benzothiophenes as kinase inhibitors
    Patent number: 10669265
    Abstract: This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: June 2, 2020
    Assignee: ALLERGAN, INC.
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang
  • Crystal form of orexin receptor antagonist compound, and preparation method and application thereof
    Patent number: 10668066
    Abstract: Disclosed are a preparation method of an orexin receptor antagonist compound 5-3, Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of the preparing the orexin receptor antagonist compound 5-3 and its crystalline forms, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: June 2, 2020
    Assignees: Shanghai Haiyan Pharmaceutical Technology Co., Ltd., Yangtze River Pharmaceutical Group Co., Ltd.
    Inventors: Songliang Wu, Zhi Luo, Yuan Chen, Yuhe Wang, Dakun Qin, Xiaolin Li, Zheng Wang, Weidong Li, Haiying He
  • Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
    Patent number: 10662170
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R5, R6, W, and A are defined herein.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: May 26, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Hui Huang, Gee-Hong Kuo, Mark R. Player, Shyh-Ming Yang, Yue-Mei Zhang
  • Heterocyclic compound
    Patent number: 10662157
    Abstract: A compound of formula (I), or an N-oxide thereof is provided. In the compound of formula (I), Het1 represents Het1-1, Het1-2, Het1-3, Het1-4, Het1-5, Het1-6, Het1-7, Het1-8, or Het1-9, and the remaining variable groups are as defined in the specification. The compound of formula (I), or N-oxide thereof has a superior effect in controlling arthropod pests.
    Type: Grant
    Filed: March 27, 2017
    Date of Patent: May 26, 2020
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Kohei Orimoto, Takamasa Tanabe, Yoshihiko Nokura, Yuji Nakajima
  • 3-(benzoimidazol-2-YL)-indazole inhibitors of the Wnt signaling pathway and therapeutic uses thereof
    Patent number: 10654832
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: May 19, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, John Hood
  • Histone demethylase inhibitors
    Patent number: 10654830
    Abstract: The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: May 19, 2020
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Tetrahydroisoquinoline derived PRMT5-inhibitors
    Patent number: 10647708
    Abstract: A compound of formula (I) wherein: R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: May 12, 2020
    Assignee: CTXT PTY. LTD
    Inventors: Richard Charles Foitzik, Michelle Ang Camerino, Scott Raymond Walker, H. Rachel Lagiakos
  • Immunomodulator compounds
    Patent number: 10639284
    Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n 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: June 26, 2017
    Date of Patent: May 5, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Christopher Lange, Viengkham Malathong, Darren J. McMurtrie, Sreenivas Punna, Rajinder Singh, Ju Yang, Penglie Zhang
  • Process for preparing N-(5-(3-(7-(3-fluorophenyl)-3H-imidazo[4,5-C]pyridin-2-yl)-1H-indazol-5-yl)pyridin-3-yl)-3-methylbutanamide
    Patent number: 10633380
    Abstract: Provided herein is a synthetic process for preparing a compound of Formula (1). The disclosure also provides useful intermediates and salts, amorphous and polymorph forms of the compound of Formula (1). These compounds are useful for various disease including cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, and osteoarthritis as well as Wnt-related diseases.
    Type: Grant
    Filed: August 28, 2018
    Date of Patent: April 28, 2020
    Assignee: Samumed, LLC
    Inventor: Sunil Kumar KC
  • Pyridyl benzothiophenes as kinase inhibitors
    Patent number: 10633373
    Abstract: This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: April 28, 2020
    Assignee: Allergan, Inc.
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang
  • Synthesis of indazoles
    Patent number: 10633365
    Abstract: The present invention relates to a novel method of preparing a 2-substituted indazole of formula (I) to novel intermediate compounds, and to the use of intermediate compounds for the preparation of said 2-substituted indazole.
    Type: Grant
    Filed: April 25, 2017
    Date of Patent: April 28, 2020
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Tobias Thaler, Johannes Platzek, Nicolas Guimond
  • Solid forms of 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide, and their pharmaceutical compositions and uses
    Patent number: 10626101
    Abstract: Solid forms comprising 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.
    Type: Grant
    Filed: December 11, 2018
    Date of Patent: April 21, 2020
    Assignee: Celgene Corporation
    Inventors: Ying Li, Hon-Wah Man
  • Production method of thiazole derivative
    Patent number: 10618894
    Abstract: Provided is a production method of a thiazole derivative represented by the formula (I), which has an adenosine A2A receptor antagonistic action and is useful as a therapeutic agent for, for example, Parkinson's disease, sleep disorder, analgesic resistance to opioid, migraine, movement disorder, depression, anxiety disorder and the like. Also provided is a production method of a compound represented by the formula (C), which contains (i) a step of reacting a compound represented by the formula (A) and a compound represented by the formula (B), and the like: (wherein R1 represents furyl, R4, R5 and R6 are the same or different and each represents lower alkyl or aryl, R2 represents pyridyl or tetrahydropyranyl, and X1 represents halogen).
    Type: Grant
    Filed: January 14, 2019
    Date of Patent: April 14, 2020
    Assignee: KYOWA KIRIN CO., LTD.
    Inventors: Takamasa Sugita, Arata Yanagisawa, Iwao Chujo, Masashi Taga, Akihiro Mimura, Atsushi Tada, Masashi Aoki
  • Triazoles as Kv3 inhibitors
    Patent number: 10611735
    Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.
    Type: Grant
    Filed: November 6, 2018
    Date of Patent: April 7, 2020
    Assignee: Autifony Therapeutics Limited
    Inventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
  • Crystalline forms of PLX3397 hydrochloride, processes for preparation and use thereof
    Patent number: 10604521
    Abstract: The present disclosure relates to novel crystalline forms of PLX3397 hydrochloride and processes for preparation thereof. The crystalline forms of PLX3397 hydrochloride provided by the present disclosure have higher solubility, larger particle size which is favorable for separation in the subsequent production process, and good stability, especially mechanical stability. These novel crystalline forms of PLX3397 hydrochloride provide a better choice for PLX3397 drug products and are of great value for drug development.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: March 31, 2020
    Assignee: Crystal Pharmaceuticals (Suzhou) Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Po Zou, Xiaoyu Zhang
  • Galunisertib crystalline form, preparation method thereof and use thereof
    Patent number: 10604528
    Abstract: The present disclosure relates to a novel crystalline form of Galunisertib, processes for preparation and use thereof. The present disclosure also relates to a pharmaceutical composition comprises the novel crystalline form of Galunisertib and use of the novel crystalline form of Galunisertib and pharmaceutical composition for preparing drugs treating disease. The crystalline form of the present disclosure has good stability, solubility and hygroscopicity, which has significant value for future drug optimization and development.
    Type: Grant
    Filed: July 21, 2017
    Date of Patent: March 31, 2020
    Assignee: Crystal Pharmaceutical (Suzhou) Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Yuhao Chen, Hui Gao, Fei Lu, Xiaoyu Zhang
  • Processes for preparing ASK1 inhibitors
    Patent number: 10604490
    Abstract: The present disclosure provides processes for the preparation of a compound of formula: which exhibits apoptosis signal-regulating kinase (“ASK1”) inhibitory activity and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis. The disclosure also provides compounds that are synthetic intermediates.
    Type: Grant
    Filed: August 17, 2017
    Date of Patent: March 31, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Brandon Heath Brown, Troy Evan Reynolds
  • Solid forms of 3-(6-(1-(2,2-difluorobenzo[D][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
    Patent number: 10597384
    Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methypyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: March 24, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
  • Halogen-substituted heterocyclic compound
    Patent number: 10597375
    Abstract: A novel ?-halogen-substituted thiophene compound or a pharmacologically acceptable salt thereof, which has a potent LPA receptor-antagonist activity and is useful as a medicament is provided. A compound represented by the general formula (I) wherein A represents, a phenyl ring, a thiophene ring, or an isothiazole ring; R1 is the same or different, and represents a halogen atom, or a C1-C3 alkyl group; R2 represents a hydrogen atom, or a C1-C6 alkyl group; p represents an integer of 0 to 5; V represents CR3 wherein R3 represents a hydrogen atom, an amino group, a nitro group, or a C1-C3 alkoxy group, or V represents a nitrogen atom; and X represents a halogen atom, or a salt thereof.
    Type: Grant
    Filed: May 8, 2018
    Date of Patent: March 24, 2020
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Noriaki Iwase, Hiroshi Nishida, Makoto Okudo, Masaaki Ito, Shigeyuki Kono, Masaaki Matoyama, Shigeru Ushiyama, Eiji Okanari, Hirofumi Matsunaga, Kenji Nishikawa, Tomio Kimura