Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/210.21)
  • Patent number: 11524957
    Abstract: The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: December 13, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Lei Zhu, John Daniel Bailey, Landon Durak, Joshua David Waetzig, Masahiro Mizuno, Kazuhiro Maeda, Tsuneo Yasuma, Hiroshi Yamaguchi, Koichiro Fukuoka, Kazuyuki Akiyama
  • Patent number: 11512090
    Abstract: Provided herein are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
    Type: Grant
    Filed: June 10, 2019
    Date of Patent: November 29, 2022
    Assignee: Pipeline Therapeutics, Inc.
    Inventors: Yifeng Xiong, Thomas Schrader, Austin Chen, Jeffrey Roger Roppe, Jill Melissa Baccei, Yalda Bravo
  • Patent number: 11512072
    Abstract: The present disclosure provides azetidine compounds of Formula I and their pharmaceutically acceptable salts, their compositions, and methods for their use in determining azetidine compound binding to proteins. The azetidine compounds are useful as probes, for monitoring diacylglycerol kinase activity, and for identifying druggable targets.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: November 29, 2022
    Assignee: University of Virginia Patent Foundation
    Inventors: Ku-Lung Hsu, Rebecca L. McCloud
  • Patent number: 11498920
    Abstract: Novel 4-(1H-imidazol-5-yl)-1H-pyrrolo[2,3-b]pyridine compounds that are useful in the treatment of lymphomas, leukaemias, and solid tumors.
    Type: Grant
    Filed: March 26, 2019
    Date of Patent: November 15, 2022
    Assignee: MASARYKOVA UNIVERZITA
    Inventors: Vitezslav Bryja, Pavlina Janovska, Michaela Gregorova, Vaclav Nemec, Prashant Khirsariya, Kamil Paruch
  • Patent number: 11459327
    Abstract: Cycloalkyl and hetero-cycloalkyl inhibitors, preparation methods therefor, and the use thereof are described. Compounds of the present invention have a structure represented by formula (I). Further disclosed are preparation methods for said compounds, and the use of said compounds as KRASG12C inhibitors. The compounds have an excellent ability to selectively inhibit KRASG12C, improved pharmacodynamic and pharmacokinetic performance, and reduced toxic side effects.
    Type: Grant
    Filed: June 7, 2021
    Date of Patent: October 4, 2022
    Assignees: Suzhou Zelgen Biopharmaceuticals Co., Ltd., Shanghai Zelgen Pharma.Tech Co., Ltd.
    Inventors: Binhua Lv, Dawei Cui, Lianjun Liu, Tao Han, Runqing Wang, Peizhong Ni, Zelin Sheng
  • Patent number: 11459337
    Abstract: Disclosed in the present invention are an IRAK4 inhibitor, and an application thereof in preparation of a drug for treating IRAK4-related diseases. Specifically disclosed are a compound represented by formula (III) and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 25, 2019
    Date of Patent: October 4, 2022
    Assignee: Chia Tai Tianqing Pharmaceutical Group Co., Inc.
    Inventors: Yang Zhang, Jianfei Wang, Haizhong Tan, Jie Li, Jian Li, Shuhui Chen
  • Patent number: 11458123
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: October 4, 2022
    Assignee: ARVINAS OPERATIONS, INC.
    Inventors: Andrew P. Crew, Michael Berlin, Hanqing Dong, Alexey Ishchenko
  • Patent number: 11446288
    Abstract: Provided are single-dose, ready-to-use formulations and methods for preparing the formulations that include a compound of Formula (I) including pharmaceutically acceptable salts and amorphous and polymorph forms thereof.
    Type: Grant
    Filed: July 27, 2020
    Date of Patent: September 20, 2022
    Assignee: BioSplice Therapeutics, Inc.
    Inventor: Luis A. Dellamary
  • Patent number: 11390632
    Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.
    Type: Grant
    Filed: March 19, 2020
    Date of Patent: July 19, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Serena Maria Fantasia, Daniel Vincent Fishlock, Fabienne Hoffmann-Emery, Gerard Moine, Christophe Pfleger, Christian Moessner
  • Patent number: 11390617
    Abstract: Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, alone or in combination with rituximab, for treating, preventing or managing non-Hodgkin lymphoma.
    Type: Grant
    Filed: April 9, 2020
    Date of Patent: July 19, 2022
    Assignee: CELGENE CORPORATION
    Inventors: Maria Soraya Carrancio Anton, Tonia J. Buchholz, Antonia Lopez-Girona, Rama Krishna Narla, Michael Pourdehnad
  • Patent number: 11365250
    Abstract: The present disclosure generally relates to compositions and methods for cancer immunotherapy, as well as hematopoietic recovery following cancer treatment such as chemotherapy or irradiation.
    Type: Grant
    Filed: November 29, 2018
    Date of Patent: June 21, 2022
    Assignee: The Board of Regents of The University of Texas System
    Inventors: Bruce Beutler, Evan Nair-Gill, Xue Zhong, Jinglei Zhang, Pingping Wang
  • Patent number: 11358952
    Abstract: Provided herein are 4-aminoisoindoline-1,3-dione compounds having the following structure: wherein R, Ring A, and n are as defined herein, compositions comprising an effective amount of a 4-aminoisoindoline-1,3-dione compound, and methods for treating or preventing disorders.
    Type: Grant
    Filed: April 22, 2019
    Date of Patent: June 14, 2022
    Assignee: Celgene Corporation
    Inventors: Matthew D. Alexander, Soraya Carranclo, Matthew D. Correa, Virginia Heather Sharron Grant, Joshua Hansen, Roy L. Harris, Dehua Huang, Timothy S. Kercher, Antonia Lopez-Girona, Mark A. Nagy, Veronique Plantevin-Krenitsky
  • Patent number: 11352353
    Abstract: A heterocyclic compound which is an inhibitor of FGFR4 (fibroblast growth factor receptor 4) is described. Specifically, a compound represented by the following formula (I), including an isomer (enantiomer or diastereomer) which may be present, or a pharmaceutically acceptable salt thereof, prodrugs, deuterated derivatives, hydrates, solvates, are described. The definition of each group in the formula (I) is as described in the specification. The compounds have FGFR4 inhibitory activity and can be used for the prevention or treatment of diseases associated with FGFR4 activity or expression, and can also be used in combination with other drugs for the treatment of various related diseases, as described.
    Type: Grant
    Filed: May 27, 2017
    Date of Patent: June 7, 2022
    Assignee: Hangzhou Innogate Pharma Co., Ltd.
    Inventors: Hancheng Zhang, Shifeng Liu, Xiangyang Ye
  • Patent number: 11339162
    Abstract: Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as cancer.
    Type: Grant
    Filed: December 20, 2021
    Date of Patent: May 24, 2022
    Assignee: Recurium IP Holdings, LLC
    Inventors: Guobao Zhang, Peter Qinhua Huang, Kevin Duane Bunker, Sayee Gajanan Hegde
  • Patent number: 11319295
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: May 3, 2022
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Catherine M. White, Meredeth Ann McGowan, Yongxin Han, Nunzio Sciammetta
  • Patent number: 11306069
    Abstract: Novel benzimidazole enantiomeric derivatives, their process of preparation and their therapeutical uses as dual H1 and H4 receptor ligands are disclosed.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: April 19, 2022
    Assignee: BIOPROJET
    Inventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
  • Patent number: 11306093
    Abstract: A process for preparing the compound of formula I comprising: a) coupling a compound of formula 2 wherein a leaving group O—SO2—R is selected from the triflate group, the tosylate group, the mesylate group, the besylate group, the nosylate group or the brosylate group, with a suitable boronic acid, a trifluoroborate or a boronic acid ester under argon condition and in the presence of a catalyst and a base in a suitable solvent and then isolating the product as an acid addition salt to afford the compound of formula Ia and b) converting the acid addition salt of formula Ia wherein the acid HX comprises suitable organic or inorganic acids into the compound of formula I by treatment with at least a stoichiometric equivalent of a suitable base.
    Type: Grant
    Filed: March 6, 2019
    Date of Patent: April 19, 2022
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Bjoern Bartels, Philipp Cueni, Matthias Koerner, Dieter Muri
  • Patent number: 11279702
    Abstract: 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: Grant
    Filed: October 15, 2021
    Date of Patent: March 22, 2022
    Assignee: KALLYOPE, INC.
    Inventors: Iyassu Sebhat, Shuwen He
  • Patent number: 11274107
    Abstract: Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated to modulate the NMDA receptor.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: March 15, 2022
    Assignee: Cadent Therapeutics, Inc.
    Inventors: David R. Anderson, Robert A. Volkmann, Frank Menniti, Christopher Fanger, Yuelian Xu
  • Patent number: 11267806
    Abstract: The present invention relates to an indazole compound for use in inhibiting kinase activity, and relates to a preparation and use thereof. Specifically disclosed in the present invention is an indazole compound represented by formula (I), or a crystal form, a prodrug, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a solvate or a hydrate thereof, or a pharmaceutical composition thereof. The compound of the present invention and the composition containing the compound have an excellent inhibitory effect on kinase proteins, and have better pharmacokinetic parameter characteristics, may increase the drug concentration of the compound in an animal, and improve the efficacy and safety of the drug.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: March 8, 2022
    Assignee: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Huanyin Li
  • Patent number: 11254668
    Abstract: A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein variables are defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: February 22, 2022
    Assignee: Pfizer Inc.
    Inventors: Brian Stephen Gerstenberger, Andrew Fensome, Dafydd Rhys Owen, Matthew Frank Brown, Matthew Merrill Hayward, Felix Vajdos, Li Huang Xing, Stephen Wayne Wright
  • Patent number: 11254669
    Abstract: The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 11, 2019
    Date of Patent: February 22, 2022
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Gary E. L. Brandt, Cameron Smith, Steven D. E. Sullivan, Lori Jean Van Orden
  • Patent number: 11248007
    Abstract: Provided herein are compounds that inhibit MALT1, a protein whose activity is responsible for constitutive NF-?B signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating MALT1-related diseases and disorders (e.g., cancer) with the compounds in a subject, by administering the compounds and/or compositions described herein.
    Type: Grant
    Filed: March 8, 2018
    Date of Patent: February 15, 2022
    Assignees: Cornell University, Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, David A. Scott, John Hatcher, Ari M. Melnick, Lorena Fontan Gabas
  • Patent number: 11247990
    Abstract: Provided herein are compounds of the Formula (I): and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein Ring A, X1, X2, X3, R1, R2 and R3 are as defined herein, which are inhibitors of one or more TAM kinases and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor.
    Type: Grant
    Filed: December 5, 2018
    Date of Patent: February 15, 2022
    Assignee: ARRAY BIOPHARMA INC
    Inventors: Shelley Allen, Mark Laurence Boys, Adam Cook, John Gaudino, Ronald Jay Hinklin, Ellen Laird, Oren T. McNulty, Andrew T. Metcalf, Brad Newhouse, John E. Robinson
  • Patent number: 11234976
    Abstract: Described herein are methods for using compounds that activate pyruvate kinase.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: February 1, 2022
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Samuel V. Agresta, Yue Chen, Marvin B. Cohen, Lenny Dang, Charles Kung, Elizabeth A. Merica, Bruce A. Silver, Hua Yang
  • Patent number: 11229649
    Abstract: Methods for treating or prophylaxis of a cryptosporidium infection using compositions comprising a structure disclosed herein. Also provided are pharmaceutical compositions and kits for alleviating the symptoms of, for treating, or for preventing the occurrence of cryptosporidium infection. The kits comprise one or more compounds having a structure disclosed herein, such as in an oral composition, and instructions for use, storage, and the like.
    Type: Grant
    Filed: July 29, 2019
    Date of Patent: January 25, 2022
    Assignee: University of Vermont and State Agricultural College
    Inventors: Christopher D. Huston, Kovi Bessoff, Rajiv Satish Jumani
  • Patent number: 11220496
    Abstract: Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I wherein X and Y independently are O or NR1; each R1 is independently H or C1-C6 alkyl; ring A is aryl; each R2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R3 and R4 independently are H or C1-C6 alkyl; and R5 is halo, cyano, or C1-C6 alkyl.
    Type: Grant
    Filed: August 26, 2019
    Date of Patent: January 11, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Rajinder Singh, Vanessa Taylor, Donald G. Payan
  • Patent number: 11214573
    Abstract: The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: November 13, 2019
    Date of Patent: January 4, 2022
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Wenqing Yao, David M. Burns, Jincong Zhuo
  • Patent number: 11180501
    Abstract: Disclosed in the present disclosure are a crystal form of a ?-lactamase inhibitor and a preparation method therefor, as well as an application of the crystal form in preparing a ?-lactamase inhibitor drug.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: November 23, 2021
    Assignee: QILU PHARMACEUTICAL CO., LTD.
    Inventors: Cheng Li, Zhigang Huang, Charles Z. Ding, Weidong Li
  • Patent number: 11174232
    Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.
    Type: Grant
    Filed: May 6, 2020
    Date of Patent: November 16, 2021
    Assignee: Aurigene Discovery Technologies Limited
    Inventors: Susanta Samajdar, Ramulu Poddutoori, Chetan Pandit, Subhendu Mukherjee, Rajeev Goswami
  • Patent number: 11174251
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
    Type: Grant
    Filed: October 17, 2019
    Date of Patent: November 16, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Patent number: 11161852
    Abstract: Compounds having activity as inhibitors of NEK7 are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein, A, X, Y, R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of the NLRP3 inflammasome are also provided.
    Type: Grant
    Filed: May 7, 2021
    Date of Patent: November 2, 2021
    Assignee: HALIA THERAPEUTICS, INC.
    Inventors: David James Bearss, John Sai Keong Kauwe, III, Alexis Henri Abel Mollard
  • Patent number: 11155879
    Abstract: The present invention relates to a method of predicting the likelihood that a patient will respond therapeutically to a pancreatic cancer treatment comprising the administration of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one (Compound 1) and/or tautomers thereof or a pharmaceutically acceptable salt or hydrate thereof, comprising the steps of: STEP (1): determining a KRAS gene mutation status of a sample from a patient, and STEP (2): predicting an increased likelihood that the patient will respond therapeutically to the pancreatic cancer treatment if the patient has the presence of KRAS gene mutation(s), and to methods of treating pancreatic cancer.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: October 26, 2021
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Akihiro Ohashi, Kenichi Iwai, Tadahiro Nambu, Ryo Dairiki, Yuko Ishii
  • Patent number: 11154539
    Abstract: The invention provides a compound for use in the treatment of T-Cell Acute Lymphoblastic Leukaemia (T-ALL), the compound having the formula (1): or being a pharmaceutically acceptable salt thereof; wherein: n is 0, 1 or 2; Ar1 is selected from an optionally substituted phenyl, pyridyl, thienyl and furanyl; Q1 is selected from C(?O), S(?O) and SO2; A is absent or is NR2; R1 is selected from: hydrogen; an optionally substituted C1-6 non-aromatic hydrocarbon group; and optionally substituted 3- to 7-membered non-aromatic carbocyclic and heterocyclic rings containing one or two heteroatom ring members selected from O, N and S, and bridged bicyclic heterocyclic rings of seven to nine ring members of which one or two are nitrogen atoms, the carbocyclic and heterocyclic rings and bridged bicyclic heterocyclic rings; R2 is selected from hydrogen and C1-4 alkyl; or NR1R2 forms an optionally substituted 4- to 7-membered non-aromatic nitrogen-containing heterocyclic ring optionally containing a second hete
    Type: Grant
    Filed: October 20, 2017
    Date of Patent: October 26, 2021
    Assignee: Sareum Limited
    Inventor: John Charles Reader
  • Patent number: 11149025
    Abstract: This invention provides, among other things, compounds useful for treating diseases such as cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.
    Type: Grant
    Filed: February 13, 2020
    Date of Patent: October 19, 2021
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Csaba J. Peto, David Jablons, Hassan Lemjabbar-Alaoui
  • Patent number: 11117896
    Abstract: A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
    Type: Grant
    Filed: October 22, 2019
    Date of Patent: September 14, 2021
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki, Seiichi Inamura, Akihiro Morinaka
  • Patent number: 11091489
    Abstract: Provided herein are crystalline forms of a triazolopyrimidine compound, which is useful for treating a PRC2-mediated disease or disorder.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: August 17, 2021
    Assignee: Novartis AG
    Inventors: Ying Huang, Bo Liu, Liang Mao, Long Wang, Liladhar Murlidhar Waykole, Lijun Zhang
  • Patent number: 11077128
    Abstract: Provided herein are alpha2-selective Na,K-ATPase inhibitors and prodrugs thereof, characterized by having a cyclic moiety attached to a digoxin or digitoxin derivative, as well as uses thereof in lowering intraocular pressure and in treating glaucoma and heart conditions.
    Type: Grant
    Filed: April 14, 2020
    Date of Patent: August 3, 2021
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Steven J. D. Karlish, Adriana Katz, Daniel M. Tal, Arie Marcovich
  • Patent number: 11053239
    Abstract: Bcl-2 inhibitors, pharmaceutical compositions thereof, and methods of use thereof are provided. In particular, Bcl-2 inhibitors of formula (I) are provided, wherein the variable groups are as defined in the specification. The Bcl-2 inhibitors can be used to treat cell proliferative disorders.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: July 6, 2021
    Assignee: Fochon Pharmaceuticals, Ltd.
    Inventors: Xingdong Zhao, Zuwen Zhou, Chengxi He, Zhifu Li, Yue Rong, Rui Tan, Huajie Zhang, Hongbin Liu, Weipeng Zhang, Haohan Tan, Zhifang Chen, Lihua Jiang, Yanxin Liu, Min Lin, Jing Sun, Weibo Wang
  • Patent number: 11028085
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
    Type: Grant
    Filed: September 14, 2020
    Date of Patent: June 8, 2021
    Assignee: Nimbus Saturn, Inc.
    Inventors: Neelu Kaila, Ian Linney, Stuart Ward, Grant Wishart, Ben Whittaker, Alexandre Cote, Jeremy Robert Greenwood, Abba Leffler, Steven K. Albanese, Daniel L. Severance
  • Patent number: 11028081
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Grant
    Filed: December 30, 2019
    Date of Patent: June 8, 2021
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 10988482
    Abstract: The present invention relates to a compound inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (particularly humans). The compound has a structural formula I.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: April 27, 2021
    Assignee: BEIJING HANMI PHARMACEUTICAL CO., LTD.
    Inventors: Baoyu Xue, Runa Zheng, Mi Young Cha, Maengsup Kim
  • Patent number: 10981909
    Abstract: Provided herein is a synthetic process for preparing a compound of Formula (1). The disclosure also provides useful intermediates and salts, amorphous and polymorph forms of the compound of Formula (1). These compounds are useful for various disease including cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, and osteoarthritis as well as Wnt-related diseases.
    Type: Grant
    Filed: March 9, 2020
    Date of Patent: April 20, 2021
    Assignee: Samumed, LLC
    Inventor: Sunil Kumar Kc
  • Patent number: 10966980
    Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing them, and therapeutic uses thereof.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: April 6, 2021
    Assignee: Pfizer Inc.
    Inventors: Michael L. Vazquez, Neelu Kaila, Jamison B. Tuttle, Patrick Robert Verhoest, Matthew R. Reese, Karen J. Coffman, Tarek Samad, James M. Duerr, Simone Sciabola, Mihir D. Parikh
  • Patent number: 10954253
    Abstract: The present invention provides a 1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one compound having an inhibitory effect on Wee1, and includes an application of the compound in treating various types of tumors.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: March 23, 2021
    Assignee: SHIJIAZHUANG SAGACITY NEW DRUG DEVELOPMENT CO., LTD.
    Inventors: Wenyuan Qian, Chundao Yang, Zhengwei Li, Jie Li, Jian Li, Shuhui Chen
  • Patent number: 10934295
    Abstract: The present disclosure relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, reducing the risk of, and delaying the onset of microbial infections in humans and animals. In some embodiments, the present disclosure provides a compound of Formula (I): or a tautomer thereof or a pharmaceutically acceptable salt of the compound or tautomer.
    Type: Grant
    Filed: May 5, 2017
    Date of Patent: March 2, 2021
    Assignee: BIOVERSYS AG
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Zoltan F. Kanyo, Joseph A. Ippolito
  • Patent number: 10927126
    Abstract: Disclosed herein are thieno[2,3-b:5,4-c?]dipyridin-8-amine and pyrido[4?,3?:4,5]thieno[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: February 23, 2021
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Alison R. Gregro, Kayla Temple, Paul K. Spearing, Madeline F. Long, Julie L. Engers
  • Patent number: 10894793
    Abstract: The present invention relates to bicyclic pyridine, pyrazine, and pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K? inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: January 19, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Didier Jean-Claude Berthelot, Laurence Anne Mevellec, Patrick Rene Angibaud, Sophie Coupa, Christophe Gabriel Marcel Demestre, Lieven Meerpoel, Guillaume Jean Maurice Mercey, Christophe Meyer, Elisabeth Therese Jeanne Pasquter, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Olivier Alexis Georges Querolle
  • Patent number: 10875829
    Abstract: The disclosure provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula (I): (I) or an isotope labelled analog thereof, or a pharmaceutically acceptable salt thereof, wherein: each of R1, R2, R3, R6 and R7 represents H or F, R4 represents H or CH3 R5 represents H or C1-C4alkyl, wherein at least two of R1, R2, R3, R6 and R7 represent F, together with at least one pharmaceutically acceptable carrier, excipient and/or diluent.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: December 29, 2020
    Assignee: INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB
    Inventors: Clas Sonesson, Fredrik Pettersson
  • Patent number: 10857138
    Abstract: Pharmaceutical compositions comprising aztreonam or a pharmaceutically acceptable derivative, and a compound of Formula (I) or a stereoisomer or a pharmaceutically acceptable derivative thereof are disclosed.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: December 8, 2020
    Assignee: WOCKHARDT LIMITED
    Inventors: Sachin Bhagwat, Snehal Rameshwar Palwe, Prashant Ratnakar Joshi, Hemant Narendra Khande, Kushal Umarkar, Mahesh Vithalbhai Patel