Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
  • Patent number: 11083724
    Abstract: Disclosed are methods of treating CGRP related disorders, e.g., migraine, by administering to a patient in need thereof rimegepant or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising rimegepant and kits including the pharmaceutical compositions and instructions are also disclosed.
    Type: Grant
    Filed: May 27, 2020
    Date of Patent: August 10, 2021
    Assignee: Biohaven Pharmaceutical Ireland DAC
    Inventors: Vladimir Coric, Robert Croop
  • Patent number: 10973834
    Abstract: The present invention provides use of an agent that inhibits EP4 activity and an immuno-oncology agent, or a composition thereof, for treatment of a cancer.
    Type: Grant
    Filed: April 16, 2019
    Date of Patent: April 13, 2021
    Assignees: Arrys Therapeutics, Inc., AskAt Inc.
    Inventors: Mark Manfredi, Jeffrey Ecsedy, Atsushi Nagahisa, Yukinori Take, Takako Okumura
  • Patent number: 10968215
    Abstract: The present invention provides a pyrido five-element aromatic ring compound, and a preparation method therefor and a use thereof. The compound provided in the present invention has an inhibitory effect on wild-type and/or mutant EZH2, and is well positioned to become a novel anti-tumor drug or a drug for the treatment of autoimmune diseases.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: April 6, 2021
    Assignees: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Xuxing Chen, Meiyu Geng, Lei Jiang, Yi Chen, Jianhua Cao, Qingyun Jiang, Qianqian Shen, Jian Ding, Yucai Yao, Zhao Zhao, Yuanfang Xiong
  • Patent number: 10961217
    Abstract: Crystals of a compound that exhibits an analgesic action against neuropathic pain and/or fibromyalgia syndrome are useful as pharmaceuticals. The crystals may be of (S)-1-(4-(dimethylamino)piperidin-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: March 30, 2021
    Assignee: Toray Industries, Inc.
    Inventors: Hirozumi Takahashi, Yoko Baba, Yasuhiro Morita, Katsuhiko Iseki, Naoki Izumimoto
  • Patent number: 10947235
    Abstract: This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
    Type: Grant
    Filed: February 27, 2020
    Date of Patent: March 16, 2021
    Assignee: AskAt Inc.
    Inventors: Yukinori Take, Shinichi Koizumi, Takako Okumura, Kazuhiko Nonomura
  • Patent number: 10946071
    Abstract: This disclosure is directed to methods of alleviating the negative effects of, treating, or slowing the progression of progressive multiple sclerosis in human patients using ibudilast and interferon-beta.
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: March 16, 2021
    Assignee: MediciNova, Inc.
    Inventor: Kazuko Matsuda
  • Patent number: 10947228
    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: July 22, 2019
    Date of Patent: March 16, 2021
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 10913746
    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: July 24, 2019
    Date of Patent: February 9, 2021
    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: 10889583
    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: September 28, 2017
    Date of Patent: January 12, 2021
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Vikas Sikervar, Indira Sen, Girish Rawal, Michel Muehlebach, Andrew Edmunds, Sebastian Rendler, Daniel Emery
  • Patent number: 10882859
    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: December 11, 2019
    Date of Patent: January 5, 2021
    Assignee: TOPIVERT PHARMA LIMITED
    Inventor: Matthew Colin Thor Fyfe
  • Patent number: 10882860
    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: December 11, 2019
    Date of Patent: January 5, 2021
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC, Yusuf Yazici, Christopher Swearingen, Luis A Dellamary
  • Patent number: 10875854
    Abstract: The present invention relates to compounds of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R2 is lower alkyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkyl substituted by hydroxy; Y is R4 is lower alkoxy, lower alkoxy substituted by halogen or CN; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers 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: December 18, 2018
    Date of Patent: December 29, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Rosa Maria Rodriguez Sarmiento
  • Patent number: 10870651
    Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: December 22, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Yanke Liang, Tinghu Zhang, Nicholas Paul Kwiatkowski
  • Patent number: 10836727
    Abstract: The present invention provides novel crystalline forms of 4-[3-Chloro-4-(N?-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, as well as methods for their preparation.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: November 17, 2020
    Assignee: Indena S.P.A.
    Inventors: Nicola Sardone, Stefano Luca Giaffreda, Andrea Gambini, Alex Petrolati, Pietro Allegrini, Enrico Modena
  • Patent number: 10806718
    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: October 31, 2019
    Date of Patent: October 20, 2020
    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: 10772332
    Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, A1, A2, X and n have the definitions given above, to the use thereof as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for preparation thereof.
    Type: Grant
    Filed: February 5, 2018
    Date of Patent: September 15, 2020
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Marc Mosrin, Ruediger Fischer, Dominik Hager, Laura Hoffmeister, Kerstin Ilg, Nina Kausch-Busies, David Wilcke, Matthieu Willot, Sascha Eilmus, Ulrich Goergens, Andreas Turberg
  • Patent number: 10759807
    Abstract: The present disclosure provides, inter alia, Compounds of Formula (I) or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: September 1, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Christopher W. Lange, Rebecca M. Lui, Viengkham Malathong, Venkat Reddy Mali, Sreenivas Punna, Rajinder Singh, Yibin Zeng, Penglie Zhang
  • Patent number: 10759799
    Abstract: Indazole macrocycle compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole macrocycle 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: June 13, 2019
    Date of Patent: September 1, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar K C, Gopi Kumar Mittapalli, Chandramouli Chiruta, Brian Joseph Hofilena
  • Patent number: 10738044
    Abstract: {4-[3-(Dimethylamino)propoxy]phenyl}methyl (4S)-4-(propan-2-yl)-3H,4H,5H,6H,7H-imidazo[4,5-c]pyridine-5-carboxylate, and pharmaceutically or veterinarily acceptable salts thereof.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: August 11, 2020
    Assignee: PROXIMAGEN, LLC
    Inventor: Lee Patient
  • 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: 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: 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: 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: 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: 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: 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