The Other Cyclo In The Bicyclo Ring System Is A Pyrrole Ring (including Hydrogenated) (e.g., Pyrrolo[3,2-d]pyrimidine, Etc.) Patents (Class 514/265.1)
  • Patent number: 11078207
    Abstract: Provided are a novel pyrimidine compound that inhibits HER2 activity and exhibits brain penetration properties, or a salt thereof, and a pharmaceutical composition comprising the same. A compound represented by the following formula (I), or a salt thereof: wherein R1 represents a C1-C4 alkyl group optionally having a C1-C4 alkoxy group as a substituent, or a C3-C4 cycloalkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group optionally having 1 to 5 C1-C4 alkoxy groups or fluorine atoms each as a substituent(s), or a C1-C6 alkoxy group; R3 represents a hydrogen atom, or a C1-C4 alkyl group optionally having 1 to 5 fluorine atoms as a substituent(s); R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 represents a phenyl group optionally having 1 to 3 substituents selected from fluorine atoms and chlorine atoms.
    Type: Grant
    Filed: October 8, 2020
    Date of Patent: August 3, 2021
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masayuki Nakamura, Takahiro Asai, Satoru Iguchi, Kei Oguchi
  • Patent number: 11026945
    Abstract: Disclosed herein are methods of preventing and/or treating lung injury and/or lung inflammation in a subject comprising administering to the subject a therapeutically effective dose of a PERK pathway inhibitor. Pharmaceutical compositions for the prevention and/or treatment of lung injury and/or lung inflammation comprising PERK pathway inhibitors are also provided. Also disclosed are uses of a PERK inhibitor in the manufacture of a medicament for the prevention and/or treatment of a lung injury and/or inflammation.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: June 8, 2021
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Susan S. Margulies, Tamas Dolinay
  • Patent number: 11007197
    Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
    Type: Grant
    Filed: September 30, 2019
    Date of Patent: May 18, 2021
    Assignee: ACEA THERAPEUTICS, INC.
    Inventors: Xiao Xu, Xiaobo Wang, Long Mao, Li Zhao, Biao Xi
  • Patent number: 11000525
    Abstract: There are disclosed certain 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one compounds of formula (I), and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions.
    Type: Grant
    Filed: June 15, 2018
    Date of Patent: May 11, 2021
    Assignee: ASTRAZENECA AB
    Inventors: Tord Bertil Inghardt, Petra Johannesson, Ulrik Jurva, Erik Michaelsson, Eva-Lotte Lindstedt-Alstermark, Nicholas Tomkinson, Jeffrey Paul Stonehouse, Li-Ming Gan
  • Patent number: 10988479
    Abstract: An advantageous isolated morphic form of trilaciclib which is 2?-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7?,8?-dihydro-6?H-spiro[cyclohexane-1,9?-pyrazino[1?,2?:1,5]pyrrolo[2,3-d]pyrimidin]-6?-one, for example in the form of a di-hydrochloride salt or a dihydrochloride, dihydrate.
    Type: Grant
    Filed: November 13, 2020
    Date of Patent: April 27, 2021
    Assignee: G1 Therapeutics, Inc.
    Inventors: Stephen Schneider, Alexander Smith, Hannah S. White, Jay Copeland Strum, Jaroslaw Mazurek
  • Patent number: 10973913
    Abstract: The present invention provides methods for treating pruritus in a subject in need thereof comprising administering a therapeutically effective amount of a JAK inhibitor. Also provided are methods of intranasal administration of JAK inhibitors for use in treating pruritus.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: April 13, 2021
    Assignee: Washington University
    Inventor: Brian Kim
  • Patent number: 10947245
    Abstract: The present invention relates to crystalline form A of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)-benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), a method for preparing the crystalline form A, and the use thereof.
    Type: Grant
    Filed: September 25, 2019
    Date of Patent: March 16, 2021
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Zhaozhong Ding, Fei Sun, Yinghu Hu, Yilong Zhou, Zheng Wang, Rui Zhao, Ling Yang
  • Patent number: 10933066
    Abstract: Disclosed are 9-deazaaadenine derivatives of the general formula (I) and pharmaceutically acceptable salts thereof, wherein A is OH or NH2, and B is H or NH2. Methods for treating and/or suppressing a Zika virus infection with the compounds disclosed are also provided. Pharmaceutical compositions comprising the disclosed compounds are also provided. Such pharmaceutical compositions may optionally contain one or more additional active agents.
    Type: Grant
    Filed: November 22, 2019
    Date of Patent: March 2, 2021
    Assignee: Biocryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pravin L. Kotian, Shanta Bantia
  • Patent number: 10927120
    Abstract: Compounds of Formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: May 13, 2020
    Date of Patent: February 23, 2021
    Assignee: GI Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay Copeland Strum
  • Patent number: 10927118
    Abstract: A class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
    Type: Grant
    Filed: March 1, 2018
    Date of Patent: February 23, 2021
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Changhua Tang, Qingyun Ren, Junjun Yin, Kai Yi, Yibo Lei, Yejun Wang, Yingjun Zhang
  • Patent number: 10918641
    Abstract: This invention relates generally to the use of 5?-methylthioadenosine phosphorylase (MTAP) inhibitors for the treatment of lung diseases associated with inflammation, such as cystic fibrosis (CF) and chronic obstructive pulmonary disease (COPD). Small molecule inhibitors of MTAP can sustain accumulation of endogenous MTA to therapeutically beneficial levels resulting in decreased inflammation in CF and COPD.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: February 16, 2021
    Assignees: The University of North Carolina at Chapel Hill, Albert Einstein College of Medicine, Inc., Victoria Link Limited
    Inventors: Charles R. Esther, Jr., Michael R. Knowles, Wanda Kay O'Neal, Deepika Polineni, Steven Isaacman, Andrew B. Mahon
  • Patent number: 10869867
    Abstract: The present invention relates to an intravenous infusion dosage form of pemetrexed or its pharmaceutically acceptable salt, having long term stability.
    Type: Grant
    Filed: February 12, 2016
    Date of Patent: December 22, 2020
    Assignee: SUN PHARMACEUTICAL INDUSTRIES LTD.
    Inventors: Samarth Kumar, Prashant Kane, Subhas Balaram Bhowmick, Kirti Ganorkar, Nisarg Bipinchandra Mistry, Ramaji Karshanbhai Varu
  • Patent number: 10869870
    Abstract: This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.
    Type: Grant
    Filed: August 14, 2020
    Date of Patent: December 22, 2020
    Assignee: Incyte Corporation
    Inventors: Bhavnish Parikh, Bhavesh Shah, Krishnaswamy Yeleswaram
  • Patent number: 10851100
    Abstract: Disclosed are an intermediate of a pyrrolo six-membered heteroaromatic ring derivative as a JAK inhibitor and a preparation method therefor, and a method for preparing a pyrrolo six-membered heteroaromatic ring derivative using the intermediate. The method improves the reaction yield, is simple and easy to operate and control, and is conducive to expanded industrial production.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: December 1, 2020
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Bing Liu, Lin Bian, Xiaohui Gao
  • Patent number: 10849883
    Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: December 1, 2020
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, Weihe Zhang, Lakshminarayana Vogeti, Minwan Wu, Venkat R. Chintareddy, Krishnan Raman
  • Patent number: 10851116
    Abstract: The present invention relates to a compound according to formula I wherein R1 is alkyl; n is 1 or 2; R2 is selected from the group consisting of hydrogen, cyano, —SO2Ra, —SO2NRbRc, —C(O)Rb, phenyl and 5- and 6-membered heteroaryl or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to pharmaceutical compositions comprising said compounds, and to methods of treating proliferative or inflammatory skin disorders with said compounds.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: December 1, 2020
    Assignee: LEO Pharma A/S
    Inventors: Daniel Rodriguez Greve, Tue Heesgaard Jepsen, Mogens Larsen, Andreas Ritzen
  • Patent number: 10807971
    Abstract: The present invention provides compounds which are of the formula (I) and (II) wherein X is selected from the group consisting of (III) and (IV); R is selected from the group consisting of (V) and (VI); Q is selected from the group consisting of (VII) and (VIII); and (IX) R2 is selected from the group consisting of (X) and (XI); or a pharmaceutically acceptable salt thereof, methods for treating obesity, type II diabetes, and compositions.
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: October 20, 2020
    Assignee: Eli Lilly and Company
    Inventors: Koc Kan Ho, Weiguo Quan, Jingye Zhou
  • Patent number: 10799504
    Abstract: The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: October 13, 2020
    Assignee: ACEA THERAPEUTICS, INC.
    Inventors: Xiao Xu, Xiaobo Wang, Long Mao, Li Zhao, Biao Xi
  • Patent number: 10793573
    Abstract: A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided: Formula I, wherein, R is one selected from the group consisting of H and CH3; n is an integer ranging from 1 to 4; X is one selected from the group consisting of —CH2—, O, S, —NH—, —NHCHO—, —NHCOCH3—, and —NHCOCF3—; and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2?-fluoro-1,4-phenyl, and (c) 2,5-thienyl. Methods of treating a patient having cancer, targeting mitochondrial metabolism, and targeting SHMT2 and MTHFD2 using the compounds of this invention are disclosed.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: October 6, 2020
    Assignees: Duquesne University of The Holy Spirit, Wayne State University
    Inventors: Aleem Gangjee, Larry H. Matherly
  • Patent number: 10793567
    Abstract: Provided are compounds of the formula and pharmaceutically acceptable salts and composition thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g. HDAC2).
    Type: Grant
    Filed: January 11, 2018
    Date of Patent: October 6, 2020
    Assignee: Rodin Therapeutics, Inc.
    Inventors: Nathan Oliver Fuller, John A. Lowe, III
  • Patent number: 10792285
    Abstract: The present invention relates to a pharmaceutical composition with enhanced stability, containing pemetrexed or a salt thereof, and a preparation method therefor. The present invention provides an injection preparation in liquid form containing pemetrexed, capable of ensuring sufficient stability during circulation and storage by selection of an optimum material and setting of an optimum concentration range in order to secure the stability of pemetrexed. The present invention can provide a pemetrexed preparation which is readily commercially prepared, can prevent microbial contamination occurring during lyophilization or reconstitution, and has enhanced convenience of administration and stability.
    Type: Grant
    Filed: December 13, 2016
    Date of Patent: October 6, 2020
    Assignee: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Min Jae Joo, Hye Jin Seo, Shin Jung Park
  • Patent number: 10786505
    Abstract: Disclosed are methods for the treatment of various solid tumors in patients in need of such treatment. The methods comprise administering to such a patient an NEDD8-activating enzyme (NAE) inhibitor such as ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]-pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) or a pharmaceutically acceptable salt in combination with one or more chemotherapeutic agents. Also disclosed are medicaments for use in the treatment of various solid tumors.
    Type: Grant
    Filed: May 15, 2018
    Date of Patent: September 29, 2020
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Allison Berger, Eric S. Lightcap
  • Patent number: 10758540
    Abstract: Provided herein are methods of treating focal segmental glomerulosclerosis, said methods include administering to a subject in need thereof a therapeutically effective amount of a CCR2 antagonist. In some embodiments, the CCR2 antagonist is used in monotherapy. In some embodiments, the CCR2 antagonist is used in combination therapy. In some embodiments, the additional therapeutic agent is a RAAS blocker and/or an endothelin receptor inhibitor. The CCR2 antagonist may have the structure of formula (I).
    Type: Grant
    Filed: October 10, 2018
    Date of Patent: September 1, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Zhenhua Miao, Thomas J. Schall, Rajinder Singh
  • Patent number: 10725042
    Abstract: A method of determining the susceptibility of a cancer in a subject to treatment with an antimetabolite includes obtaining a sample of cancer cells from the subject, measuring the level of UDG expression in the cancer cells, and comparing the measured levels of UDG expression in the cancer cells to a control level.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: July 28, 2020
    Assignee: CASE WESTERN RESERVE UNIVERSITY
    Inventor: Stanton Gerson
  • Patent number: 10676473
    Abstract: Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: June 9, 2020
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Rongliang Chen, Tomonori Ichibakase, Chunrong Ma, Christopher F. Matthews, Hajime Motoyoshi, Colin O'Bryan, Kentaro Yaji, Naoki Yoshikawa
  • Patent number: 10676475
    Abstract: Provided herein are compounds useful for improving mRNA splicing in a cell. Exemplary compounds provided herein are useful for improving mRNA splicing in genes comprising at least one exon ending in the nucleotide sequence CAA. Methods for preparing the compounds and methods of treating diseases of the central nervous system are also provided.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: June 9, 2020
    Assignees: The General Hospital Corporation, The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Susan A. Slaugenhaupt, Graham Johnson, William D. Paquette, Wei Zhang, Juan Marugan
  • Patent number: 10669276
    Abstract: The present invention relates to compounds of formula I, wherein R1 is phenyl, lower alkyl, C3-6-cycloalkyl, —CH2—C3-6-cycloalkyl, or bridged C3-5-cycloalkyl, optionally substituted by one, two or three substituents, selected from halogen, lower alkyl or lower alkyl substituted by halogen; R2 is hydrogen, halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R3 is a five membered heteroaryl group, selected from wherein R6 is hydrogen or lower alkyl; R7 is halogen or lower alkyl; R8 is hydrogen or lower alkyl; R9 is hydrogen or lower alkyl; R4 is lower alkyl or lower alkyl substituted by hydroxy; R5/R5? is independently from each other hydrogen or lower alkyl; -( )n- is —CH2— or —CH2CH2— for n being 1 or 2; X is CH or N; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: June 2, 2020
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Sandra Steiner, Michael Reutlinger
  • Patent number: 10660895
    Abstract: Provided herein are methods for treating, delaying progression of, or reducing the severity of amyotrophic lateral sclerosis (ALS) in a subject through administration of therapeutically effective amounts of agents (e.g., JAK kinase inhibitors (e.g., tofacitinib)) capable of interfering with central nervous system related natural killer cell (NK) levels and function.
    Type: Grant
    Filed: August 13, 2019
    Date of Patent: May 26, 2020
    Assignee: The Regents of the University of Michigan
    Inventors: Eva L. Feldman, Ben Murdock, Stephen Goutman, Stacey Jacoby
  • Patent number: 10646490
    Abstract: The present invention provides for the design and synthesis of halogenated thieno- and pyrrolopyrimidine compounds and prodrugs thereof that exhibit cancer proliferation inhibitory activity and the use thereof for cancer treatment.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: May 12, 2020
    Assignee: UNIVERSITY OF MARYLAND, BALTIMORE COUNTY
    Inventor: Katherine L. Radtke
  • Patent number: 10633348
    Abstract: The present invention provides compounds of any one of Formulae (A), (I-11), (II), and (V) (e.g., compounds of Formula (A-1)-(A-18)), and methods for treating Waldenström's macroglobulinemia (WM) and other B cell neoplams in a subject using the compounds. The methods comprise administering to a subject in need thereof an effective amount of the compounds. Also provided are methods to treat B cell neoplasms using the compounds in combination with inhibitors of Bruton's tyrosine kinase (BTK), interleukin-1 receptor-associated kinase 1 (IRAK1), interleukin-1 receptor-associated kinase 4 (IRAK4), bone marrow on X chromosome kinase (BMX), phosphoinositide 3-kinase (PI3K), transforming growth factor b-activated kinase-1 (TAK1), and/or a Src family kinase.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: April 28, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Steven P. Treon, Sara Jean Buhrlage, Nathanael S. Gray, Li Tan, Guang Yang
  • Patent number: 10617692
    Abstract: A pyrrolopyrimidine comprising a cyclopentyi substituent. The present invention specifically relates to a compound represented by formula. A and a stereoisomer and pharmaceutically acceptable salt thereof. The invention further relates to a method for manufacturing the pyrrolopyrimidine comprising the cyclopentyl substituent represented by formula A, a pharmaceutical composition, and an application of the compound in treating a disease induced by Janus kinase.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: April 14, 2020
    Assignees: CENTAURUS BIOPHARMA CO., CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD.
    Inventors: Li Zhu, Yangjian Liu, Chuanyu Zhang, He Wang, Hong Luo, Yinghui Sun, Yongxin Han
  • Patent number: 10611772
    Abstract: The present invention provides a novel crystalline form of Ribociclib succinate, Ribociclib succinate Form APO-I, including Ribociclib succinate, benzyl alcohol and water, compositions thereof, processes for the preparation thereof, and the use of this crystalline form in the treatment of conditions associated with increased CDK4/6 kinase activity, and in particular, cancers, including certain forms of breast cancer.
    Type: Grant
    Filed: June 27, 2019
    Date of Patent: April 7, 2020
    Assignee: Apotex Inc.
    Inventors: Fabio E. S. Souza, Bahareh Khalili
  • Patent number: 10583131
    Abstract: The present disclosure describes methods of treating pancreatic cancer and limiting over-expression of oncogenes, activating tumor suppressor genes or regulating signaling proteins in patients comprising administering compounds and pharmaceutical combinations as described herein.
    Type: Grant
    Filed: July 31, 2019
    Date of Patent: March 10, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Petrus Bekker, Shichang Miao, Israel Charo, Tom Schall
  • Patent number: 10561659
    Abstract: Disclosed is a method of treating in a subject hair loss disorders that are beneficially treated by administering a JAK1 and/or JAK2 inhibitor. The method comprises administering to the subject an amount in the range of about 4 mg to about 50 mg of Compound (I), or a pharmaceutically acceptable salt thereof. This invention also provides compositions comprising Compound (I) and the use of such compositions in the described methods.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: February 18, 2020
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Amanda T. Wagner, James V. Cassella, Philip B. Graham, Virginia Braman, Vinita Uttamsingh, Jana Von Hehn, Colleen E. Hamilton
  • Patent number: 10561660
    Abstract: The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: February 18, 2020
    Inventors: Simona Bindi, Davide Carenzi, Ilaria Motto, Maurizio Pulici
  • Patent number: 10555949
    Abstract: The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.
    Type: Grant
    Filed: April 17, 2018
    Date of Patent: February 11, 2020
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Zhaozhong Ding, Hao Wu, Fei Sun, Lifang Wu, Ling Yang
  • Patent number: 10533011
    Abstract: Provided are methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: January 14, 2020
    Assignee: ACEA THERAPEUTICS, INC.
    Inventors: Long Mao, Jia Liu, Yile Chen, Yuning Hua, Kongen Dai, Yimei Bao, Bojie Weng, Xiaopeng Mo, Jian Wu, Xiao Xu, Wanhong Xu, Xiaobo Wang
  • Patent number: 10512649
    Abstract: Disclosed are 9-deazaaadenine derivatives of the general formula (I) and pharmaceutically acceptable salts thereof, wherein A is OH or NH2, and B is H or NH2. Methods for treating, preventing and/or suppressing a Zika virus infection with the compounds disclosed are also provided. Pharmaceutical compositions comprising the disclosed compounds are also provided. Such pharmaceutical compositions may optionally contain one or more additional active agents.
    Type: Grant
    Filed: March 6, 2017
    Date of Patent: December 24, 2019
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pravin L. Kotian, Shanta Bantia
  • Patent number: 10493073
    Abstract: The present invention relates to pyrimidine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: December 3, 2019
    Assignee: Merck Patent GmbH
    Inventors: Hui Qiu, Richard D. Caldwell, Lesley Liu-Bujalski
  • Patent number: 10494374
    Abstract: The present invention relates to methods of using compounds of Formula I, wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.
    Type: Grant
    Filed: April 5, 2019
    Date of Patent: December 3, 2019
    Assignee: CYSTIC FIBROSIS FOUNDATION
    Inventors: Joseph Walter Strohbach, David Christopher Limburg, John Paul Mathias, Atli Thorarensen, Rajiah Aldrin Denny, Christoph Wolfgang Zapf, Daniel Elbaum, Lori Krim Gavrin, Ivan Viktorovich Efremov
  • Patent number: 10463667
    Abstract: The present invention provides active metabolites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
    Type: Grant
    Filed: April 25, 2017
    Date of Patent: November 5, 2019
    Assignees: INCYTE INCORPORATION, INCYTE HOLDINGS CORPORATION
    Inventors: James D. Rodgers, Argyrios G. Arvanitis, Jack Guoen Shi, Stacey Shepard
  • Patent number: 10457640
    Abstract: Provided herein are synthetic methods for the preparation of EZH2 inhibitors.
    Type: Grant
    Filed: October 18, 2017
    Date of Patent: October 29, 2019
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Rishi G. Vaswani, Michael Charles Hewitt
  • Patent number: 10449196
    Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: October 22, 2019
    Assignee: ACEA Therapeutics, Inc.
    Inventors: Xiao Xu, Xiaobo Wang, Long Mao, Li Zhao, Biao Xi
  • Patent number: 10442811
    Abstract: The present invention relates to crystalline form A of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)-benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), a method for preparing the crystalline form A, and the use thereof.
    Type: Grant
    Filed: February 4, 2017
    Date of Patent: October 15, 2019
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Zhaozhong Ding, Fei Sun, Yinghu Hu, Yilong Zhou, Zheng Wang, Rui Zhao, Ling Yang
  • Patent number: 10407430
    Abstract: Provided are Janus kinase 1 selective inhibitors of Formula 1 or Formula 2: wherein R1, R2, and X are as described herein. Pharmaceutical uses thereof, for example, for the treatment of a disease associated with a Janus kinase, are also provided.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: September 10, 2019
    Assignees: YANG JI CHEMICAL CO., LTD., HAN WHA PHARMA CO., LTD.
    Inventors: Chieyeon Chough, Sunmin Lee, Misuk Joung, Hyun Uk Jeong, Hong-sik Moon
  • Patent number: 10398685
    Abstract: The present disclosure describes methods of treating pancreatic cancer and limiting over-expression of oncogenes, activating tumor suppressor genes or regulating signaling proteins in patients comprising administering compounds and pharmaceutical combinations as described herein.
    Type: Grant
    Filed: February 4, 2019
    Date of Patent: September 3, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Petrus Bekker, Shichang Miao, Israel Charo, Tom Schall
  • Patent number: 10385056
    Abstract: The invention relates to a 4-substituted pyrrolo[2,3-d]pyrimidine compound and the use thereof in preparing medications for treating JAK-targeted diseases such as rheumatoid, immune system diseases, and tumor. The 4-substituted pyrrolo[2,3-d]pyrimidine compound of the invention is as shown in chemical formula I. The activity experimental results of the invention show that the new compound has obvious effect and activity in inhibition of Janus kinases, JAK-STAT, cell proliferation of human lymphocytoma, and rheumatoid arthritis.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: August 20, 2019
    Assignee: JIANGSU CAREFREE PHARMACEUTICAL CO., LTD
    Inventors: Yinlin Qin, Mei Su, Shousheng Yan, Xianzhi Wu, Tao Chen, Jianhua Jiang
  • Patent number: 10385064
    Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
    Type: Grant
    Filed: July 25, 2017
    Date of Patent: August 20, 2019
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10377773
    Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, X1, X2, X3, n, and m are described herein.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: August 13, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell
  • Patent number: 10336763
    Abstract: The present invention relates to crystal forms B, C and D of Ribociclib succinate salt and derivatives thereof, and their preparation method and composition. The crystal forms B, C and D of Ribociclib succinate salts are obtained by adding 7-cyclopentyl-N,N-dimethyl-2-(5-(piperain-1-yl)pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide solution into succinic acid solution for reaction, stirring the solution under high temperature, filtering the solution after cooling off.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: July 2, 2019
    Assignee: CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO. LTD.
    Inventors: Satyanarayana Kamani, Tzu-Chiang Lu, Hsin-Yun Chang, Chin-Cheng Mai