Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
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Patent number: 12122773Abstract: Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.Type: GrantFiled: May 31, 2023Date of Patent: October 22, 2024Assignee: Theravance Biopharma R&D IP, LLCInventor: Gene Timothy Fass
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Patent number: 12110290Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.Type: GrantFiled: July 6, 2023Date of Patent: October 8, 2024Assignee: Bristol-Myers Squibb CompanyInventors: Guanglin Luo, Jie Chen, Carolyn Diane Dzierba, David B. Frennesson, Junqing Guo, Amy C. Hart, Xirui Hu, Michael E. Mertzman, Matthew Reiser Patton, Jianliang Shi, Steven H. Spergel, Brian Lee Venables, Yong-Jin Wu, Zili Xiao, Michael G. Yang
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Patent number: 12103925Abstract: The present application provides a crystalline form of tolebrutinib, an amorphous form, and a method of preparation thereof and a use thereof, and the crystalline form of tolebrutinib provided in the present application has at least one of the following advantages: good stability, low moisture attraction, uniform particle size distribution, solubility meeting the requirements for medicinal use, stable storage, avoiding phase transformation of the drug in the process of development and in storage, and a reliable method for the preparation thereof, which has a great development value. The amorphous form of tolebrutinib provided in this application, while possessing better solubility than that of tolebrutinib in the crystalline state, still possesses good stability of placement and acceptable hygroscopicity, and has high medicinal value.Type: GrantFiled: September 27, 2023Date of Patent: October 1, 2024Assignee: HANGZHOU SOLIPHARMA CO., LTD.Inventors: Xiaohong Sheng, Xiaoxia Sheng, Yu Dai
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Patent number: 12024522Abstract: The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3K?), as well as a salt form and intermediates related thereto.Type: GrantFiled: July 1, 2021Date of Patent: July 2, 2024Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Lei Qiao, Lingkai Weng, Chongsheng Eric Shi, David Meloni, Qiyan Lin, Michael Xia, Vaqar Sharief, William Frietze, Zhongjiang Jia, Yongchun Pan, Pingli Liu, Tai-Yuen Yue, Jiacheng Zhou, Jianji Wang
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Patent number: 12018016Abstract: Compounds of formula (A) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:Type: GrantFiled: August 17, 2022Date of Patent: June 25, 2024Assignee: AMGEN INC.Inventors: Penglie Zhang, Daniel R. Marshall, Howard S. Roth, Aubrie Harland, Ju Yang, Christopher W. Lange, Rebecca M. Lui, Antoni Krasinski
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Patent number: 12012401Abstract: Provided herein is a synthetic process for preparing a compound of Formula (1). The disclosure also provides useful intermediates and salts, amorphous and polymorph forms of the compound of Formula (1). These compounds are useful for various disease including cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, and osteoarthritis as well as Wnt-related diseases.Type: GrantFiled: March 18, 2021Date of Patent: June 18, 2024Assignee: BioSplice Therapeutics, Inc.Inventor: Sunil Kumar KC
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Patent number: 11976064Abstract: The present invention relates to imidazo-pyridinyl compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject.Type: GrantFiled: May 6, 2022Date of Patent: May 7, 2024Assignee: Pfizer Inc.Inventors: Omar Ahmad, Andrew Fensome, Erik Alphie LaChapelle, Ethan Lawrence Fisher, Rayomand J. Unwalla, Jun Xiao, Lei Zhang
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Patent number: 11969412Abstract: The invention provides a p38 MAPK inhibitor of Formula I, or a pharmaceutically acceptable salt or solvate thereof: for use in the treatment or prevention of hypercytokinemia in a human patient; wherein R is C1-3alkyl, optionally substituted by one or more halo, NR1R2 or hydroxy, and R1and R2 are independently H, halo or C1-3alkyl, optionally substituted by one or more F. Also provided are compositions for use in the treatment or prevention of hypercytokinemia comprising the p38 MAPK inhibitor of Formula I; and methods for treating or preventing hypercytokinemia in a human patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a p38 MAPK inhibitor of Formula I. The invention also provides a p38 MAPK inhibitor and an antimicrobial agent, such as an antiviral agent, for use in the treatment or prevention of hypercytokinemia.Type: GrantFiled: September 23, 2022Date of Patent: April 30, 2024Assignee: Poolbeg Pharma (UK) LimitedInventors: Adrian Huw Davies, Pui-Man Choy, Vinay Saunders, Basma Bahsoun, Surender Vashist, Neil Edward Torbett, Paul Andrew Whittaker
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Patent number: 11926626Abstract: This disclosure relates to GLP-1 agonists of Formula (I), including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.Type: GrantFiled: September 21, 2022Date of Patent: March 12, 2024Assignee: Gasherbrum Bio, Inc.Inventors: Qinghua Meng, Weiqiang Xing, Haizhen Zhang, Xichen Lin, Hui Lei, Andrew Jennings
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Patent number: 11925624Abstract: The present disclosure relates to methods of administering Compound I for treating fibrotic disorders, inflammatory disorders or autoimmune disorders.Type: GrantFiled: November 17, 2021Date of Patent: March 12, 2024Assignee: GENENTECH, INC.Inventors: Lin Pan, Dorothy Sze-Wing Cheung, Jeffrey Mark Harris, Indiana Strombom
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Patent number: 11925631Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.Type: GrantFiled: May 27, 2021Date of Patent: March 12, 2024Assignee: Gilead Sciences, Inc.Inventors: Gayatri Balan, Mark J. Bartlett, Jayaraman Chandrasekhar, Julian A. Codelli, John H. Conway, Jennifer L. Cosman, Rao V. Kalla, Musong Kim, Seung H. Lee, Jennifer R. Lo, Jennifer A. Loyer-Drew, Scott A. Mitchell, Thao D. Perry, Gary B. Phillips, Patrick J. Salvo, Joshua J. Van Veldhuizen, Suet C. Yeung, Jeff Zablocki
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Patent number: 11866422Abstract: This invention is directed to novel carbocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention.Type: GrantFiled: July 14, 2021Date of Patent: January 9, 2024Assignee: Orion Ophthalmology LLCInventors: Robert Gomez, Jinyue Ding, Renata Marcella Oballa, David Andrew Powell
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Patent number: 11851429Abstract: This disclosure is directed, at least in part, to AMPK activators useful for the treatment of conditions or disorders associated with AMPK. In some embodiments, the condition or disorder is associated with the gut-brain axis. In some embodiments, condition or disorder is associated with systemic infection and inflammation from having a leaky gut barrier. In some embodiments, the AMPK activators are gut-restricted compounds. In some embodiments, the AMPK activators are agonists or partial agonists.Type: GrantFiled: January 26, 2022Date of Patent: December 26, 2023Assignee: KALLYOPE, INC.Inventors: Iyassu Sebhat, Shuwen He, Ann Weber, Nancy Thornberry, Lisa Krug, Paul Richards, Brett Lauring
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Patent number: 11833138Abstract: Certain embodiments of the present disclosure provide liquid pharmaceutical formulations, suitable for oral administration, that contain glycerol and an amount of apixaban in the solution phase of the formulations of from 0.5 mg/ml to 6 mg/ml.Type: GrantFiled: January 30, 2023Date of Patent: December 5, 2023Assignee: TaP Pharmaceuticals AGInventors: Nilesh Parikh, William Hite
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Patent number: 11767322Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.Type: GrantFiled: October 18, 2021Date of Patent: September 26, 2023Assignee: Bristol-Myers Squibb CompanyInventors: Guanglin Luo, Jie Chen, Carolyn Diane Dzierba, David B. Frennesson, Junqing Guo, Amy C. Hart, Xirui Hu, Michael C. Mertzman, Matthew Reiser Patton, Jianliang Shi, Steven H. Spergel, Brian Lee Venables, Yong-Jin Wu, Zili Xiao, Michael G. Yang
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Patent number: 11739090Abstract: Disclosed are a class of BTK kinase inhibitor compounds with a high activity and a high selectivity and the use thereof in the preparation of a drug for treating BTK target-related diseases. Specifically, disclosed are a compound shown as formula (I), and an isomer and a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 25, 2020Date of Patent: August 29, 2023Assignee: JUMBO DRUG BANK CO., LTD.Inventors: Chunli Shen, XiaWei Wei, Chengde Wu, Guoping Hu, Ning Jiang, Wei Zheng, Jian Li, Shuhui Chen
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Patent number: 11702415Abstract: Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.Type: GrantFiled: March 1, 2021Date of Patent: July 18, 2023Assignee: Theravance Biopharma R&D IP, LLCInventor: Gene Timothy Fass
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Patent number: 11647748Abstract: The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.Type: GrantFiled: July 1, 2020Date of Patent: May 16, 2023Assignee: MIGAL—GALILEE RESEARCH INSTITUTE LTD.Inventors: Itai Bloch, Elad Cohen, Rachel Amir, Maayan Gal
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Patent number: 11607405Abstract: The invention provides methods for treating triple negative breast cancer (TNBC), by co-administration of a BET bromodomain inhibitor selected from 1-benzyl-6-(3,5-dimethylisoxazol-4-yl)-N-methyl-1H-imidazo[4,5-b]pyridin-2-amine (Compound I), 1-benzyl-6-(3,5-dimethylisoxazol-4-yl)-1H-imidazo[4,5-b]pyridin-2-amine, and pharmaceutically acceptable salts/co-crystals thereof, and a second therapeutic agent to a subject in need thereof. The second therapeutic agent can be a PARP inhibitor, such as, e.g., talazoparib, olaparib or veliparib.Type: GrantFiled: September 13, 2019Date of Patent: March 21, 2023Assignee: Zenith Epigenetics Ltd.Inventors: Eric Campeau, Laura Tsujikawa, Sanjay Lakhotia
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Patent number: 11590112Abstract: The invention provides a p38 MAPK inhibitor of Formula I, or a pharmaceutically acceptable salt or solvate thereof: Formula I for use in the treatment or prevention of hypercytokinemia in a human patient; wherein R is C1-3alkyl, optionally substituted by one or more halo, NR1R2 or hydroxy, and R1 and R2 are independently H, halo or C1-3alkyl, optionally substituted by one or more F. Also provided are compositions for use in the treatment or prevention of hypercytokinemia comprising the p38 MAPK inhibitor of Formula I; and methods for treating or preventing hypercytokinemia in a human patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a p38 MAPK inhibitor of Formula I. The invention also provides a p38 MAPK inhibitor and an antimicrobial agent, such as an antiviral agent, for use in the treatment or prevention of hypercytokinemia.Type: GrantFiled: December 20, 2018Date of Patent: February 28, 2023Assignee: Orph Pharma IP Company LimitedInventors: Adrian Huw Davies, Pui-Man Choy, Vinay Saunders, Basma Bahsoun, Surender Vashist, Neil Edward Torbett, Paul Andrew Whittaker
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Patent number: 11560378Abstract: 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: GrantFiled: December 1, 2020Date of Patent: January 24, 2023Assignee: BioSplice Therapeutics, Inc.Inventors: John Hood, David Mark Wallace, Sunil Kumar KC, Yusuf Yazici, Christopher Swearingen, Luis A Dellamary
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Patent number: 11491140Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (1) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.Type: GrantFiled: July 30, 2020Date of Patent: November 8, 2022Assignee: H. Lundbeck A/SInventors: Jan Kehler, Karsten Juhl, Mauro Marigo, Paulo Jorge Vieira Vital, Mikkel Jessing, Morten Langgård, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson
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Patent number: 11427569Abstract: Described are benzoimidazole indolyl methane compounds, pharmaceutical compositions containing them, and use of the compounds to inhibit PCSK9-mediated ailments.Type: GrantFiled: February 13, 2020Date of Patent: August 30, 2022Assignee: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Weiping Tang, Gabrielle N. Winston-McPherson, Haibo Xie, Alan D. Attie, Mark Patrick Keller, Ka Yang
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Patent number: 11427581Abstract: Disclosed in the present application are a class of compounds as JAK inhibitors and use thereof in the preparation of medicaments for treating JAK and TYK2 related diseases. Specifically, a compound represented by formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof is disclosed.Type: GrantFiled: January 31, 2019Date of Patent: August 30, 2022Assignee: ZHUHAI UNITED LABORATORIES CO., LTD.Inventors: Weiwei Mao, Hao Wu, Xuejian Zheng, Guoping Hu, Changqing Wei, Jian Li, Shuhui Chen
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Patent number: 11414433Abstract: 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: GrantFiled: December 29, 2020Date of Patent: August 16, 2022Assignee: Incyte CorporationInventors: Liangxing Wu, Kaijiong Xiao, Wenqing Yao
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Patent number: 11407767Abstract: This invention related to compounds that are inhibitors of the CDK12 kinase. The compounds are useful in the treatment of disorders mediated by the CDK12 kinase including myotonic dystrophy type 1 (DM1) and other disorders caused by the generation of RNA repeat expansion transcripts. In particular, the invention relates to compounds of the formula (I), or a pharmaceutically acceptable salts or N-oxides thereof, wherein R1a, R2, R3, R4a, R4b and R4c are as defined herein.Type: GrantFiled: September 21, 2018Date of Patent: August 9, 2022Inventors: David Brook, Chris Hayes, Nicholas Bennett, Matthew Palframan, Sue Cramp, Richard Bull, Michael Bodnarchuk
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Patent number: 11401256Abstract: The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.Type: GrantFiled: March 4, 2020Date of Patent: August 2, 2022Assignee: C4 Therapeutics, Inc.Inventors: Roger Norcross, Adrian Britschgi, Fabian Dey, Annick Goergler, Eric Andre Kusznir, Moreno Attilio Wichert
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Patent number: 11377443Abstract: A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.Type: GrantFiled: May 14, 2020Date of Patent: July 5, 2022Assignee: CELLCENTRIC LIMITEDInventors: Neil Anthony Pegg, Stuart Thomas Onions, David Michel Adrien Taddei, Jonathan Shannon, Silvia Paoletta, Richard James Brown, Don Smyth, Gareth Harbottle
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Patent number: 11325907Abstract: Disclosed are a crystal form of 1H-imidazo[4,5-b]pyridine-2(3H)-one compound and a preparation process therefor, and use of the crystal form in the manufacture of a medicament for treating a disease associated with PDE4 receptor.Type: GrantFiled: January 29, 2019Date of Patent: May 10, 2022Assignee: Medshine Discovery Inc.Inventors: Maoyi Lei, Yu Xu, Yunfu Luo
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Patent number: 11312713Abstract: The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.Type: GrantFiled: March 6, 2018Date of Patent: April 26, 2022Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Thomas Allen Chappie, Jinshan Michael Chen, Jotham Wadsworth Coe, Karen Jean Coffman, Paul Galatsis, Michelle Renee Garnsey, Christopher John Helal, Jaclyn Louise Henderson, Bethany Lyn Kormos, Ravi G. Kurumbail, Luis Angel Martinez-Alsina, Martin Youngjin Pettersson, Matthew Richard Reese, Colin Richard Rose, Antonia Friederike Stepan, Patrick Robert Verhoest, Travis T. Wager, Joseph Scott Warmus, Yuan Zhang
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Patent number: 11274123Abstract: The present invention relates to compounds of formula (I), compositions, methods and uses involving the said formula (I) that inhibit CD47 signaling pathway. The present invention also relates to methods of making such compounds and their uses for the treatment of diseases or disorders mediated by CD47.Type: GrantFiled: January 11, 2019Date of Patent: March 15, 2022Assignee: AURIGENE DISCOVERY TECHNOLOGIES LIMITEDInventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli, Chennakrishnareddy Gundala
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Patent number: 11274100Abstract: The present invention provides a compound having excellent histone acetyl transferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.Type: GrantFiled: June 21, 2018Date of Patent: March 15, 2022Assignee: Daiichi Sankyo Company, LimitedInventors: Hiroyuki Naito, Yoshiko Kagoshima, Hideaki Funami, Akifumi Nakamura, Masayoshi Asano, Makoto Haruta, Takashi Suzuki, Jun Watanabe, Ryutaro Kanada, Saito Higuchi, Kentaro Ito, Akiko Egami, Katsuhiro Kobayashi
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Patent number: 11236087Abstract: The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.Type: GrantFiled: November 2, 2018Date of Patent: February 1, 2022Assignee: AiCuris GmbH & Co. KGInventors: Alastair Donald, Andreas Urban, Susanne Bonsmann, Anita Wegert, Jasper Springer
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Patent number: 11203591Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.Type: GrantFiled: October 30, 2019Date of Patent: December 21, 2021Assignee: Gilead Sciences, Inc.Inventors: Gayatri Balan, Mark J. Bartlett, Jayaraman Chandrasekhar, Julian A. Codelli, John H. Conway, Jennifer L. Cosman, Rao V. Kalla, Zachary A. Kasun, Musong Kim, Seung H. Lee, Jennifer R. Lo, Jennifer A. Loyer-Drew, Scott A. Mitchell, Thao D. Perry, Gary B. Phillips, Patrick J. Salvo, Sundaramoorthi Swaminathan, Joshua J. Van Veldhuizen, Suet C. Yeung, Jeff Zablocki
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Patent number: 11179376Abstract: The present invention provides salts of pyrazolo[1,5-?]pyridine derivative and use thereof. The invention also relates to a pharmaceutically acceptable composition comprising such salts and a method of using the salts and the pharmaceutically acceptable composition to prevent or treat a proliferative disorder or pulmonary fibrosis in a patient.Type: GrantFiled: December 15, 2018Date of Patent: November 23, 2021Assignee: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Ning Xi, Mingming Sun
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Patent number: 11130759Abstract: Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA): that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.Type: GrantFiled: February 12, 2021Date of Patent: September 28, 2021Assignee: IDEAYA BIOSCIENCE, INC.Inventors: Muzaffar Alam, Leah Cleary, Melissa Fleury, Zhonghua Pei, Richard Steel, James Sutton, John E. Knox, Zachary E. R. Newby
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Patent number: 11083724Abstract: 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: GrantFiled: May 27, 2020Date of Patent: August 10, 2021Assignee: Biohaven Pharmaceutical Ireland DACInventors: Vladimir Coric, Robert Croop
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Patent number: 10973834Abstract: 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: GrantFiled: April 16, 2019Date of Patent: April 13, 2021Assignees: Arrys Therapeutics, Inc., AskAt Inc.Inventors: Mark Manfredi, Jeffrey Ecsedy, Atsushi Nagahisa, Yukinori Take, Takako Okumura
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Patent number: 10968215Abstract: 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: GrantFiled: September 6, 2017Date of Patent: April 6, 2021Assignees: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Xuxing Chen, Meiyu Geng, Lei Jiang, Yi Chen, Jianhua Cao, Qingyun Jiang, Qianqian Shen, Jian Ding, Yucai Yao, Zhao Zhao, Yuanfang Xiong
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Patent number: 10961217Abstract: 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: GrantFiled: August 25, 2017Date of Patent: March 30, 2021Assignee: Toray Industries, Inc.Inventors: Hirozumi Takahashi, Yoko Baba, Yasuhiro Morita, Katsuhiko Iseki, Naoki Izumimoto
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Patent number: 10947228Abstract: 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: GrantFiled: July 22, 2019Date of Patent: March 16, 2021Assignee: Samumed, LLCInventors: John Hood, David Mark Wallace, Sunil Kumar KC
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Patent number: 10946071Abstract: 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: GrantFiled: October 8, 2019Date of Patent: March 16, 2021Assignee: MediciNova, Inc.Inventor: Kazuko Matsuda
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Patent number: 10947235Abstract: 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: GrantFiled: February 27, 2020Date of Patent: March 16, 2021Assignee: AskAt Inc.Inventors: Yukinori Take, Shinichi Koizumi, Takako Okumura, Kazuhiko Nonomura
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Patent number: 10913746Abstract: 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: GrantFiled: July 24, 2019Date of Patent: February 9, 2021Assignee: The Trustees of Columbia University in the City of New YorkInventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Rando Allikmets, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
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Patent number: 10889583Abstract: 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: GrantFiled: September 28, 2017Date of Patent: January 12, 2021Assignee: Syngenta Participations AGInventors: Pierre Joseph Marcel Jung, Vikas Sikervar, Indira Sen, Girish Rawal, Michel Muehlebach, Andrew Edmunds, Sebastian Rendler, Daniel Emery
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Patent number: 10882859Abstract: 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: GrantFiled: December 11, 2019Date of Patent: January 5, 2021Assignee: TOPIVERT PHARMA LIMITEDInventor: Matthew Colin Thor Fyfe
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Patent number: 10882860Abstract: 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: GrantFiled: December 11, 2019Date of Patent: January 5, 2021Assignee: Samumed, LLCInventors: John Hood, David Mark Wallace, Sunil Kumar KC, Yusuf Yazici, Christopher Swearingen, Luis A Dellamary
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Patent number: 10875854Abstract: 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: GrantFiled: December 18, 2018Date of Patent: December 29, 2020Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Rosa Maria Rodriguez Sarmiento
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Patent number: 10870651Abstract: 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: GrantFiled: December 23, 2015Date of Patent: December 22, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Yanke Liang, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Patent number: 10836727Abstract: 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: GrantFiled: September 15, 2017Date of Patent: November 17, 2020Assignee: Indena S.P.A.Inventors: Nicola Sardone, Stefano Luca Giaffreda, Andrea Gambini, Alex Petrolati, Pietro Allegrini, Enrico Modena