Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
  • Patent number: 10703741
    Abstract: The present invention provides compounds of formula I useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
    Type: Grant
    Filed: July 27, 2017
    Date of Patent: July 7, 2020
    Assignee: Padlock Therapeutics, Inc.
    Inventors: Edward Jean Beaumont, Rajesh Devraj, Philip Stephen Kerry, Gnanasambandam Kumaravel, Pui Leng Loke, Mirco Meniconi, Jordan John Palfrey, Carl North, Cristina Lecci, Heather Tye
  • Patent number: 10696671
    Abstract: The present disclosure relates to novel imidazo[1,2-a]pyridine derivatives, and more particularly to imidazo[1,2-a]pyridine derivatives of Formula 1 wherein Y1, Y2 and Y3 are each independently H, halogen, a C1-C6 straight chain alkyl unsubstituted or substituted with R1, or hydroxy; R1 is hydroxy; Y4 is H, C1-C6 straight chain alkyl, or C1-C6 alkoxy; and X is H or halogen, and having an excellent activity of inhibiting gastric acid secretion, methods for preparing the same, and the use thereof. The imidazo[1,2-a]pyridine derivatives according to the present disclosure have gastric acid secretion inhibitory activity, and thus may be effectively used for the prevention or treatment of gastrointestinal inflammatory diseases or gastric acid-related diseases.
    Type: Grant
    Filed: July 4, 2017
    Date of Patent: June 30, 2020
    Assignee: Jeil Pharmaceutical Co., Ltd.
    Inventors: Jeongmin Kim, Hyunho Lee, Kwangwoo Chun, Chun-Ho Park, Eunsung Jang, Yoonsun Park, Joseph Kim
  • Patent number: 10669238
    Abstract: The present invention provides an inhibitor of Bruton's tyrosine kinase, which is a compound of formula (I), or its pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug. The present invention also provides a pharmaceutical composition comprising the compound. The present invention also provides a method for inhibiting the activity of tyrosine kinase activity or for treating a disease, disorder, or condition, which would benefit from the inhibition of Bruton's tyrosine kinase(s), by using the Bruton's tyrosine kinase inhibitor, as well application of the Bruton's tyrosine kinase inhibitor for the same.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: June 2, 2020
    Assignee: HEFEI INSTITUTES OF PHYSICAL SCIENCE, CHINESE ACADEMY OF SCIENCES
    Inventors: Jing Liu, Qingsong Liu, Qianmao Liang, Yongfei Chen, Cheng Chen, Aoli Wang, Hong Wu, Kailin Yu, Wei Wang, Chen Hu, Wenchao Wang, Shuang Qi, Beilei Wang, Li Wang
  • Patent number: 10646478
    Abstract: Embodiments of the present invention are directed to methods for treatment of melanoma using an inhibitor of dihydroorotate dehydrogenase (DHODH) and to combination therapies that involve administering to a subject an inhibitor of oncogenic BRAF (e.g. BRAF(V600E)), as well as an inhibitor of dihydroorotate dehydrogenase (DHODH). Assays for identifying compounds useful for the treatment of melanoma are also provided. The methods comprise screening for compounds or agents that inhibit neural crest progenitor formation in a zebra fish model of melanoma.
    Type: Grant
    Filed: July 6, 2018
    Date of Patent: May 12, 2020
    Assignees: CHILDREN'S MEDICAL CENTER CORPORATION, DANA-FARBER CANCER INSTITUTE
    Inventors: Leonard Zon, Richard M. White
  • Patent number: 10633379
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R6, X1, and X2 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula (I).
    Type: Grant
    Filed: April 14, 2017
    Date of Patent: April 28, 2020
    Assignee: AbbVie Inc.
    Inventors: Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George Sheppard, Le Wang
  • Patent number: 10611762
    Abstract: The present disclosure relates to solid forms of N-{[2?-(2,6-difluoro-3,5-dimethoxyphenyl)-3?-oxo-2?,3?-dihydro-1?H-spiro[cyclopropane-1,4?-[2,7]naphthyridin]-6?-yl]methyl}acrylamide, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: April 7, 2020
    Assignee: Incyte Corporation
    Inventors: Zhongjiang Jia, Qun Li
  • Patent number: 10577366
    Abstract: Forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the forms of Compound I.
    Type: Grant
    Filed: March 19, 2018
    Date of Patent: March 3, 2020
    Assignee: Plexxikon Inc.
    Inventors: Jack Lin, Marika Nespi, Jason Walters
  • Patent number: 10570133
    Abstract: A compound of Formula III as the raw material is hydrolyzed in an alkaline condition, then acidized to prepare a compound of Formula IV, and the resulting compound of formula IV and a solid phosgene or diphosgene are concurrently subjected to the urea cyclization and the chloroformylation reaction in the presence of an organic base and a catalyst to obtain a compound of formula V, and then the compound of formula V is amidated to obtain the final product (II). In the present invention, a “one-pot” method is adopted for urea cyclization, chloroformylation, and amidation reaction, and the intermediate products do not need post-treatments such as separation and purification.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: February 25, 2020
    Assignee: XINFA PHARMACEUTICAL CO., LTD
    Inventors: Yuxin Qi, Xinfa Li, Baolin Wang, Xin Xu, Yinlong Zhao, Yuqi Teng
  • Patent number: 10555944
    Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
    Type: Grant
    Filed: October 29, 2018
    Date of Patent: February 11, 2020
    Assignee: Eli Lilly and Company
    Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
  • Patent number: 10544161
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Grant
    Filed: January 16, 2019
    Date of Patent: January 28, 2020
    Assignee: INTERMUNE, INC.
    Inventors: Johnnie Y. Ramphal, Brad Owen Buckman, Kumaraswamy Emayan, John Beamond Nicholas, Scott D. Seiwert
  • Patent number: 10538486
    Abstract: The present invention relates to a hydroxamic acid-based contrast agent containing an isotope of fluorine, which comprises a compound having a structure of Formula (III): wherein R1 represents radioactive fluorine-18 (18F) or isotope fluorine-19 (19F), and R2 represents hydroxyamine —(NH)OH. The hydroxamic acid-based contrast agent containing an isotope of fluorine provided in the present invention has the capability of selectively inhibiting histone deacetylase (HDAC) subtypes 8/6/3, and specifically targets to the focus of spinocerebellar ataxia with over-activation of HDAC. By labeling with the radioisotope fluorine-18, a positron emission tomography (PET) image is obtained with the hydroxamic acid-based contrast agent containing radioisotope fluorine-18, whereby spinocerebellar ataxia is effectively detected.
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: January 21, 2020
    Assignee: INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN. R.O.C
    Inventors: Mei-Hui Wang, Chia-Yu Hu, Mao-Chi Weng, Jyun-Hong Chen, Chun-Hung Yang, Hung-Man Yu
  • Patent number: 10532981
    Abstract: The compounds are crystalline modifications of methyl (3Z)-3-{[4-{methyl[(4-methylpiperazin-1-yl)acetyl]amino}phenyl)amino](phenyl)methylidene}-2-oxo-2,3-dihydro-1H-indole-6-carboxylate salts of Formula I, wherein H—X represents at least one acid component, processes for the preparation thereof, and pharmaceutical compositions.
    Type: Grant
    Filed: February 20, 2017
    Date of Patent: January 14, 2020
    Assignee: Zentiva k.s.
    Inventors: Eszter Tieger, Marcela Tkadlecova, Ondrej Dammer, Tomas Gurgut
  • Patent number: 10526347
    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: October 16, 2018
    Date of Patent: January 7, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10512645
    Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: December 24, 2019
    Assignee: Hutchinson Medipharma Limited
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
  • Patent number: 10513517
    Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected from a hydrogen atom, a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, R1 does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.
    Type: Grant
    Filed: October 19, 2018
    Date of Patent: December 24, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Niall Andrew Anderson, Ian Baxter Campbell, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, Simon John Fawcett MacDonald, John Martin Pritchard, Panayiotis Alexandrou Procopiou
  • Patent number: 10494368
    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: October 9, 2018
    Date of Patent: December 3, 2019
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Andrew Edmunds, Michel Muehlebach, Roger Graham Hall, Jerome Yves Cassayre
  • Patent number: 10487080
    Abstract: The invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the description and claims, or pharmaceutically acceptable salts thereof, having ?v?6 integrin antagonist activity. The invention also relates to pharmaceutical compositions including a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and to the use of a compound of Formula (I), or a pharmaceutically acceptable salt thereof in therapy, including in the treatment of a disease or condition for which an ?v?6 integrin antagonist is indicated, in particular the treatment of idiopathic pulmonary fibrosis.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: November 26, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Niall Andrew Anderson, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, John Martin Pritchard, Panayiotis Alexandrou Procopiou, Steven Leslie Sollis
  • Patent number: 10457678
    Abstract: The present invention relates to new N1- and N7-substituted sibiriline derivatives of the following general formula (I): (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as drug, in particular for use as inhibitor of cellular necroptosis. The present invention also relates to a pharmaceutical composition comprising such a compound and processes to prepare such a compound. The present invention also encompasses the use of a compound of the general formula (I) for organs preservation.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: October 29, 2019
    Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Centre National de la Recherche Scientifique (CNRS), Sorbonne Universite, Universite Claude Bernard Lyon 1
    Inventors: Marie-Thérèse Dimanche-Boitrel, Stéphane Bach, Claire Delehouze, Peter Goekjian, Arnaud Comte
  • Patent number: 10450301
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: October 22, 2019
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Brett Granger, Guoqiang Wang, Ruichao Shen, Jing He, Yong He, Xuechao Xing, Jun Ma, Jiang Long, Bin Wang, Yat Sun Or
  • Patent number: 10435404
    Abstract: Provided are compositions comprising Compound I having the following structure: or a pharmaceutically acceptable salt thereof, and a solubilizing agent; methods of making the same; and methods of using the same.
    Type: Grant
    Filed: July 24, 2018
    Date of Patent: October 8, 2019
    Assignees: Plexxikon Inc., Daiichi Sankyo Company, Limited
    Inventors: Prabha N. Ibrahim, Hamid Rezaei, Gary Conard Visor, Tomoari Kamo, Hiroshi Yamakose
  • Patent number: 10428068
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: October 1, 2019
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Patent number: 10407422
    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: September 10, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joanne M. Smallheer, Scott A. Shaw, Oz Scott Halpern, Carol Hui Hu, Ellen K. Kick
  • Patent number: 10399976
    Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
    Type: Grant
    Filed: July 2, 2018
    Date of Patent: September 3, 2019
    Assignee: Vitae Pharmaceuticals, LLC
    Inventors: David A. Claremon, Lawrence Wayne Dillard, Chengguo Dong, Yi Fan, Lanqi Jia, Zhijie Liu, Stephen D. Lotesta, Andrew Marcus, Suresh B. Singh, Colin M. Tice, Jing Yuan, Wei Zhao, Yajun Zheng, Linghang Zhuang
  • Patent number: 10370374
    Abstract: Provided herein are heterocyclic compounds of Formula (I), pharmaceutical compositions containing such a compound and their therapeutic uses, methods for their preparation, intermediate compounds, pharmaceutical compositions containing such a compound, and their therapeutic uses.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: August 6, 2019
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Jiazhong Zhang, Songyuan Shi, Ben Powell, Yan Ma
  • Patent number: 10364232
    Abstract: The present invention relates to the following compounds wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: July 30, 2019
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jérõme Émile Georges Guillemont, Magali Madeleine Simone Motte, Pierre Jean-Marie Bernard Rabiosson, Abdellah Tahri
  • Patent number: 10358445
    Abstract: The present invention relates to respiratory formulations comprising a compound of formula (I): and use of said compounds and compositions in treatment, for example in the treatment of an inflammatory disease or a respiratory disorder, in particular an inflammatory mediated and/or virally mediated respiratory disorder such as asthma and COPD or the treatment or prevention of viral infection, for example infection by influenza virus, rhinovirus or RSV. The invention also extends to certain novel compounds of formula (I).
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: July 23, 2019
    Assignee: RESPIVERT, LTD.
    Inventors: Peter John Murray, Stuart Thomas Onions, Jonathan Gareth Williams, Kevin Joly
  • Patent number: 10342788
    Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: July 9, 2019
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Patent number: 10344031
    Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: August 13, 2018
    Date of Patent: July 9, 2019
    Assignee: Dr. Reddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
  • Patent number: 10329280
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Grant
    Filed: July 23, 2018
    Date of Patent: June 25, 2019
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim
  • Patent number: 10322116
    Abstract: A pharmaceutical compositions comprising: (a) a carbapenem antibacterial agent selected from imipenem, meropenem, ertapenem, doripenem or a pharmaceutically acceptable derivative thereof, and (b) a compound of Formula (I), or a stereoisomer or a pharmaceutical acceptable derivative thereof, are disclosed.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: June 18, 2019
    Assignee: WOCKHARDT LIMITED
    Inventors: Mahesh Vithalbhai Patel, Sachin Bhagwat, Jaykumar Satwaji Satav, Hemant Narendra Khande, Prashant Ratnakar Joshi, Snehal Rameshwar Palwe
  • Patent number: 10316022
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Grant
    Filed: July 23, 2018
    Date of Patent: June 11, 2019
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim
  • Patent number: 10316038
    Abstract: Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I): wherein R1, R2, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.
    Type: Grant
    Filed: January 25, 2018
    Date of Patent: June 11, 2019
    Assignee: ACLARIS THERAPEUTICS, INC.
    Inventors: Eric Jon Jacobsen, James Robert Blinn, John Robert Springer, Susan Landis Hockerman, David Randolph Anderson
  • Patent number: 10301261
    Abstract: Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: May 28, 2019
    Assignee: Vitae Pharmaceuticals, LLC
    Inventors: David A. Claremon, Lawrence Wayne Dillard, Yi Fan, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Linghang Zhuang
  • Patent number: 10301280
    Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: May 28, 2019
    Assignee: Plexxikon Inc.
    Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
  • Patent number: 10280163
    Abstract: Disclosed herein are 5 or 8-substituted imidazo[1,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[1,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo[1,5-a]pyridines that can be useful for inhibiting indoleamine 2,3-dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: May 7, 2019
    Assignee: BEIGENE, LTD.
    Inventors: Hexiang Wang, Guoliang Zhang, Yunhang Guo, Bo Ren, Zhiwei Wang, Changyou Zhou
  • Patent number: 10239873
    Abstract: Provided are 7-azaindole or 4,7-diazaindole derivatives as an IKK? (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor. The 7-azaindole or 4,7-diazaindole derivative effectively inhibits IKK? and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: March 26, 2019
    Assignee: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Kwang-Seop Song, Hee Jeong Seo, Sang-ho Ma, Eun-Jung Park, Younggyu Kong, So Ok Park, Kisoo Park, Ickhwan Son, Min Ju Kim, Man-Young Cha, Mi-Soon Kim, Sang Mi Kang, Dong Hyuk Jang, Jangwon Hong
  • Patent number: 10233195
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: March 19, 2019
    Assignee: INTERMUNE, INC.
    Inventors: Johnnie Y. Ramphal, Brad Owen Buckman, Kumaraswamy Emayan, John Beamond Nicholas, Scott D. Seiwert
  • Patent number: 10226453
    Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-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: 10227346
    Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: March 12, 2019
    Assignee: Pfizer Inc.
    Inventors: Mark Edward Schnute, Andrew Christopher Flick, Peter Jones, Neelu Kaila, Scot Richard Mente, John David Trzupek, Michael L. Vazquez, Goran Mattias Wennerstal, Li Xing, Edouard Zamaratski, Liying Zhang, Rayomand Jal Unwalla
  • Patent number: 10206917
    Abstract: An aqueous drug that contains the compound represented by formula (1) or a salt thereof and in which the precipitation and the chemical dissolution of the compound of formula (1) or of a salt thereof is inhibited. An aqueous drug containing: the compound represented by formula (1) or a salt thereof; and a magnesium compound. The aqueous drug has a pH of 5.8-6.9. The concentration of the compound represented by formula (1) is 3 mg/mL or more.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: February 19, 2019
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Takahiro Goto, Hitoshi Kozuka, Mizuho Shibata, Wataru Minagawa, Norihiro Kanayama, Chifuyu Toriumi
  • Patent number: 10202380
    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: June 27, 2016
    Date of Patent: February 12, 2019
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Andrew Edmunds, Michel Muehlebach
  • Patent number: 10195184
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.
    Type: Grant
    Filed: March 19, 2017
    Date of Patent: February 5, 2019
    Assignee: ANGION BIOMEDICA CORP.
    Inventors: Bijoy Panicker, Rama K. Mishra, Dong Sung Lim, Lambertus J. W. M. Oehlen, Dawoon Jung
  • Patent number: 10172851
    Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: January 8, 2019
    Assignee: Array BioPharma Inc.
    Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
  • Patent number: 10172845
    Abstract: Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: January 8, 2019
    Assignee: Array BioPharma Inc.
    Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, James Collier, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Ginelle A. Ramann, Tony P. Tang, Li Ren, Shane M. Walls
  • Patent number: 10154970
    Abstract: The present invention provides methods for modulating the immune response of a subject to a therapeutic agent, the method comprising administering an effective amount of a triphenylethylene (TRIP) compound with an effective amount of the therapeutic agent. In particular embodiments, the TRIP compound enhances the immune response of the subject to the therapeutic agent. In some embodiments, the TRIP compound is administered in different dosing schedules to provide a biphasic immunomodulation effect.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: December 18, 2018
    Assignee: The Regents of the University of California
    Inventor: Michael W. DeGregorio
  • Patent number: 10154993
    Abstract: [Problem] To provide a novel pharmaceutical composition which can suppress delayed, release of the compound represented in general formula (1) or a salt thereof. [Solution] This solid pharmaceutical composition contains the compound represented in general formula (1), or a salt thereof, and a salting-out agent.
    Type: Grant
    Filed: October 23, 2015
    Date of Patent: December 18, 2018
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Uchida, Masataka Hanada, Yoshikazu Miyazaki
  • Patent number: 10144733
    Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, R1 does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.
    Type: Grant
    Filed: September 22, 2015
    Date of Patent: December 4, 2018
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Niall Andrew Anderson, Ian Baxter Campbell, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, Simon John Fawcett MacDonald, John Martin Pritchard, Panayiotis Alexandrou Procopiou
  • Patent number: 10138249
    Abstract: The present invention is directed to [1,2,4]triazolo[4,3-a]pyridine and [1,2,4]triazolo[4,3-a]pyrazine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: August 7, 2017
    Date of Patent: November 27, 2018
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
  • Patent number: 10137124
    Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: November 27, 2018
    Assignee: Array BioPharma Inc.
    Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
  • Patent number: RE47785
    Abstract: Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided. In these crystals, decomposition due to influences of light is suppressed as compared to that in crystals of the compound (1) in free, and their storage stability is high. These crystals have higher solubility in water than the crystals of the compound (1) in free.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: December 31, 2019
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Ichiro Araya, Akinori Goto, Wataru Minagawa, Keiko Funada, Muneki Nagao