Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
  • Patent number: 10702506
    Abstract: Provided herein are small molecule inhibitors of pendrin. More specifically, the small molecules disclosed herein may be used to inhibit pendrin-mediated anion exchange. These small molecules may be used for treatment of diseases and disorders that are treatable by inhibiting pendrin, such as cystic fibrosis, rhinitis, chronic rhinosinusitis, exposure to an industrial toxin, certain viral infections, certain bacterial infections, and chronic obstructive pulmonary disease. The small molecules may further be used to potentiate a diuretic effect of a diuretic compound. The small molecules may additionally be used to treat hypertension or thyroid conditions.
    Type: Grant
    Filed: February 24, 2017
    Date of Patent: July 7, 2020
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Peter M. Haggie, Onur Cil
  • Patent number: 10689376
    Abstract: Substituted-3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and related compounds, which are useful as inhibitors of ENPP1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the ENPP1.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: June 23, 2020
    Assignees: Stingray Therapeutics, Inc., The University of Utah
    Inventors: Hariprasad Vankayalapati, Xiaohui Liu, Gurusankar Ramamoorthy, Sunil Sharma, Mohan Rao Kaadige, Alexis Weston, Trason Thode
  • 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
  • Patent number: 10618916
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
    Type: Grant
    Filed: May 10, 2019
    Date of Patent: April 14, 2020
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Kaijiong Xiao, Wenqing Yao
  • Patent number: 10617676
    Abstract: Substituted 1H-imidazo[4,5-b]pyridin-2(3H)-ones as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.
    Type: Grant
    Filed: October 5, 2017
    Date of Patent: April 14, 2020
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Christa C Chrovian, Michael A Letavic, Jason C Rech, Dale A Rudolph, Akinola Soyode-Johnson, Brice M Stenne, Jessica L Wall
  • 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
  • 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
  • Patent number: 10596154
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: November 9, 2017
    Date of Patent: March 24, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar Kc, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10590088
    Abstract: Disclosed are 4-(benzimidazol-2-ylamino)benzamide derivatives useful in slowing the expansion of cancer cells and methods of synthesizing derivatives of formula 5 or formula 7: wherein R and R? are defined herein.
    Type: Grant
    Filed: October 16, 2018
    Date of Patent: March 17, 2020
    Assignee: Translational Drug Development, LLC
    Inventors: Tong Wang, Stephen Gately
  • Patent number: 10590103
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate are also disclosed.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: March 17, 2020
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Patent number: 10584121
    Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: March 10, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hongjun Zhang, Kenneth Jay Barr, Blair T. Lapointe, Hakan Gunaydin, Kun Liu, B. Wesley Trotter
  • Patent number: 10577372
    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 3, 2020
    Assignee: Crystal Pharmaceutical (Suzhou) Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Yuhao Chen, Hui Gao, Fei Lu, Xiaoyu Zhang
  • Patent number: 10562855
    Abstract: The present disclosure relates to a novel crystalline form of lenvatinib mesylate and the preparation method thereof. The novel crystalline form of mesylate of the present disclosure can be used for treating invasive and differentiated thyroid cancer. The novel crystalline form of mesylate of the present disclosure has good solubility, stability, and remarkable purification effect in process. The preparation method of this novel crystalline form is simple, low cost, and has an important value for future optimization and development of the drug.
    Type: Grant
    Filed: March 25, 2019
    Date of Patent: February 18, 2020
    Assignee: CRYSTAL PHARMATECH CO., LTD.
    Inventors: Minhua Chen, Yanfeng Zhang, Xiaojuan Diao, Xiaoyu Zhang
  • Patent number: 10556901
    Abstract: There are provided compounds of formula I, wherein X, Ak, s, A, R1 and R2 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of the JAK family) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: February 11, 2020
    Assignee: Topivert Pharma Limited
    Inventor: Matthew Colin Thor Fyfe
  • Patent number: 10544139
    Abstract: Provided are compositions and methods for treating osteoarthritis including intra-articular administration of a compound of Formula (I) including amorphous and polymorph forms thereof.
    Type: Grant
    Filed: November 7, 2016
    Date of Patent: January 28, 2020
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC, Yusuf Yazici, Christopher Swearingen, Luis A Dellamary
  • Patent number: 10538506
    Abstract: The present invention relates to a crystal form of a potassium-competitive acid blocker, that is, 1-[5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrole-3-yl]-N-methyl methylamine fumaric acid salt (which is briefly referred to as a formula I) and a preparation method thereof. An X-ray powder diffraction characteristic peak thereof is shown in FIG. 1. The crystal form that is represented by formula I, provided in the present invention, is stable, reproducible, and is suitable for drug development.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: January 21, 2020
    Assignee: Jiangsu Hansoh Pharmaceutical Group Co., Ltd.
    Inventors: Hongwei Tang, Changan Sun, Ruijun Wang, Hengli Yuan
  • Patent number: 10533020
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: September 27, 2017
    Date of Patent: January 14, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar K C, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10519186
    Abstract: A hemi-sulfate salt of the structure: to treat a host infected with hepatitis C, as well as pharmaceutical compositions and dosage forms, including solid dosage forms, thereof.
    Type: Grant
    Filed: January 31, 2018
    Date of Patent: December 31, 2019
    Assignee: Atea Pharmaceuticals, Inc.
    Inventors: Adel Moussa, Jean-Pierre Sommadossi
  • Patent number: 10512632
    Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: December 24, 2019
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Karsten Juhl, Mauro Marigo, Paulo Jorge Vieira Vital, Mikkel Jessing, Morten Langgård, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson
  • Patent number: 10508111
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting IRAK family kinases, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases and/or proliferative diseases by administering the compound of the invention.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: December 17, 2019
    Assignee: GALAPAGOS NV
    Inventors: Reginald Christophe Xavier Brys, Raphaël Jean Joël Geney, Agnès Marie Joncour, Julien Georges Pierre-Olivier Doyon, Frédéric Gilbert Labéguère, Jean-Michel Lefrançois, Oscar Mammoliti, Benoît Antoine Schmitt, Steven Emiel Van Der Plas, Christel Jeanne Marie Menet
  • Patent number: 10494371
    Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: December 3, 2019
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Michael John Bennett, Juan Manuel Betancort, Amogh Boloor, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 10494361
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate are also disclosed.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: December 3, 2019
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Patent number: 10487069
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate are also disclosed.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: November 26, 2019
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Patent number: 10456382
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Grant
    Filed: December 6, 2018
    Date of Patent: October 29, 2019
    Assignees: FORMA TM, LLC, Genentech, Inc.
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
  • Patent number: 10450311
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable 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: May 21, 2018
    Date of Patent: October 22, 2019
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Andrew Edmunds, André Jeanguenat, Michel Muehlebach, André Stoller, Daniel Emery, Roger Graham Hall
  • Patent number: 10407433
    Abstract: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 8, 2018
    Date of Patent: September 10, 2019
    Assignee: The Trustees of Columbia University In The City of New York
    Inventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Rando Allikmets, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
  • Patent number: 10407425
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention 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: May 1, 2018
    Date of Patent: September 10, 2019
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 10399978
    Abstract: It relates to the imidazopyridine thioglycolic acid derivatives, the preparation, and use thereof. The invention contained imidazopyridine thioglycolic acid derivatives with the formula I or II or III. Also described here are preparation of imidazopyridine thioglycolic acid derivatives, pharmaceutical compositions comprising these compounds as therapy and prevention for gout.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: September 3, 2019
    Assignee: SHANDONG UNIVERSITY
    Inventors: Xinyong Liu, Qing Meng, Peng Zhan, Zengjun Fang, Tong Zhao, Zhuosen Sun, Xiukun Sun
  • Patent number: 10392358
    Abstract: Provided herein are methods of producing halomethylfuroic and acyloxymethylfuroic acid and ester compounds from furfural starting compounds. For example, 5-chloromethyl-2-furoic acid may be produced from 5-chloromethylfurfural, in the presence of various oxidants. Salts of the furoic acids may also be produced.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: August 27, 2019
    Assignee: Micromidas, Inc.
    Inventors: Daniel R. Henton, Makoto Nathanael Masuno, Ryan L. Smith, Alex B. Wood, Dimitri A. Hirsch-Weil, Christian T. Goralski, Robert Joseph Araiza
  • Patent number: 10369222
    Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment and prevention of stroke and the sequelae of stroke. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools to treat or prevent stroke and the long term effects of stroke in mammalian subjects.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: August 6, 2019
    Assignee: BIOSUCCESS BIOTECH CO., LTD.
    Inventors: Zheng Tao Han, Hung-Fong Chen
  • Patent number: 10316034
    Abstract: The mesylate and sulphate salts of (3S)-Tetrahydrofuran-3-yl (4S)-4-isopropyl-,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-5-carboxylate mesylate, and hydrates thereof, and their use in medicine.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: June 11, 2019
    Assignee: BENEVOLENTAI CAMBRIDGE LIMITED
    Inventors: Edward Savory, Michael Higginbottom
  • Patent number: 10301305
    Abstract: The invention relates to the compounds (I) and their acids and bases salts: wherein: Formula (I) the dotted line indicates a double bond; X is N or C—R1 and Y is N or C—R2, X and Y not being simultaneously N; A is selected from the group consisting of phenyl, naphthyl and (5-11) membered monocyclic or bicyclic unsaturated cycle or heterocycle possibly substituted as defined in the application, and A can also comprise either a further (4-7) membered heterocycle, said heterocycle being a monocycle, fused, saturated or unsaturated, the polycyclic system then comprising up to 14 members and up to 5 heteroatoms selected from N, O and S; B is selected from the group of substituents as defined in the application, or B is a 4 or (6-10) membered mono or bicyclic saturated or unsaturated heterocycle containing 1-3 heteroatoms selected from N, O and S, linked by a carbon atom, and possibly substituted as defined in the application; R1 is Hydrogen or a substituent as defined in the application; R2 is Hydrogen or Halogen;
    Type: Grant
    Filed: February 24, 2015
    Date of Patent: May 28, 2019
    Assignee: MUTABILIS
    Inventors: Dmytro Atamanyuk, Francis Chevreuil, Fabien Faivre, Nicolas Lecointe, Benoît Ledoussal, Chrystelle Oliveira, Christophe Simon, Vincent Gerusz
  • Patent number: 10287286
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, Y1, Y2, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: May 14, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Saleh Ahmed, Gregory Barker, Hannah Canning, Richard Davenport, David Harrison, Kerry Jenkins, David Livermore, Susanne Wright, Natasha Kinsella
  • Patent number: 10272035
    Abstract: A method to provide a therapeutic agent to an eye of a patient by implanting or inject a device that stably fits a particular location or position in the eye. The method thus provides agent inside the eye for a longer duration of agent release over a space-occupying area inside the eye.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: April 30, 2019
    Inventor: Gholam A. Peyman
  • Patent number: 10266522
    Abstract: The present disclosure discusses salt forms of 4-cyano-N-[2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl]-1H-imidazole-2-carboxamide.
    Type: Grant
    Filed: July 17, 2017
    Date of Patent: April 23, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nagy E. Fawzy, David Breslin
  • Patent number: 10251874
    Abstract: The present invention provides crystalline hydrates of the oxalate and succinate salts of 5-ethyl-2-fluoro-4-(3-(5-(1-methylpiperidin-4-yl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-6-yl)phenol. The invention also provides pharmaceutical compositions comprising such crystalline hydrates, methods of using such crystalline hydrates to treat respiratory and other diseases, and processes useful for preparing such crystalline oxalate and succinate hydrates.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: April 9, 2019
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Marta Dabros, Venkat R. Thalladi, Jerry Nzerem, Melanie A. Kleinschek, Glenn D. Crater
  • Patent number: 10246418
    Abstract: The present disclosure relates to a novel crystalline form of lenvatinib mesylate and the preparation method thereof. The novel crystalline form of mesylate of the present disclosure can be used for treating invasive and differentiated thyroid cancer. The novel crystalline form of mesylate of the present disclosure has good solubility, stability, and remarkable purification effect in process. The preparation method of this novel crystalline form is simple, low cost, and has an important value for future optimization and development of the drug.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: April 2, 2019
    Assignee: Crystal Pharmatech Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Xiaojuan Diao, Xiaoyu Zhang
  • Patent number: 10226448
    Abstract: 7-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 7-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: August 3, 2016
    Date of Patent: March 12, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10214527
    Abstract: The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: February 26, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Shaw, Joanne M. Smallheer
  • Patent number: 10206929
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: December 15, 2017
    Date of Patent: February 19, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar Kc, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10196436
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: February 5, 2019
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventor: Chandrasekhar V. Miduturu
  • Patent number: 10188645
    Abstract: The disclosure is directed to a method of easing a patient's symptoms related to termination of opioid pain therapy, and compositions for achieving said method. The method and compositions comprise a series of self tapering dosages of a pharmaceutical composition that is configured to alleviate or prevent symptoms of the patient's termination of opioid pain therapy. The series of self tapering dosages may be supplied in a dosage package.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: January 29, 2019
    Inventors: Ian Cain Smith, Robert W. Mooney
  • Patent number: 10189870
    Abstract: The present invention relates to a novel crystalline form of oxazolidinone antibiotics, which has advantages in the aspects of solubility, hygroscopicity, crystallinity and stability; the present invention also relates to a method for preparing the novel crystalline form, a pharmaceutical composition containing thereof and the use thereof in the preparation of drugs for treating and/or preventing diseases caused by microbial infection.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: January 29, 2019
    Assignee: HANGZHOU PUSHAI PHARMAEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Xiaoxia Sheng, Xiaohong Sheng, Tao Zhu, Qiang Jia
  • Patent number: 10189808
    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: January 6, 2017
    Date of Patent: January 29, 2019
    Assignee: Celgene Corporation
    Inventors: Paul F. Fernandez, Antonio C. Ferretti, Mohit A. Kothare, Ying Li, Hon-Wah Man, Weihong Zhang
  • Patent number: 10155751
    Abstract: The invention relates to new substituted heteroaryls of formula 1 or of formula 1? wherein A is either N or CH, wherein R2 is selected from the group consisting of —C1-3-alkyl, —C1-3-haloalkyl, F, Br, Cl, wherein Y is selected from —O— or —CH2—, and wherein R3 is defined as in claim 1, and the pharmaceutically acceptable salts thereof, and the use of these aforementioned compounds for the treatment of diseases such as asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: December 18, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Hoffmann, Georg Dahmann, Christian Gnamm, Daniel Robert Fandrick, John Scott, Clive McCarthy
  • Patent number: 10138242
    Abstract: The present invention relates to pyrazolopyridine derivatives, which are useful as medicaments, pharmaceutical compositions comprising one or more of the pyrazolopyridine derivatives, and the use of one or more of the pyrazolopyridine derivatives in methods for treating and/or preventing a disease caused or mediated by a parasite of the family Trypanosomatidae.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: November 27, 2018
    Inventors: Michael Sattler, Grzegorz Popowicz, Maciej Dawidowski, Leonidas Emmanouilidis, Ralf Erdmann, Wolfgang Schliebs, Vishal Kalel
  • Patent number: 10105370
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: October 23, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Patent number: 10100045
    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: October 23, 2017
    Date of Patent: October 16, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Brian Ngo Laforteza, Brad M. Savall, Warren Stanfield Wade, Stephen Todd Meyer, Márió Gyuris
  • Patent number: 10093649
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate are also disclosed.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: October 9, 2018
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Patent number: 10093648
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate are also disclosed.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: October 9, 2018
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood