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: 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: 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: 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: 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: 10336750
    Abstract: The present disclosure provides compositions and methods for treating ocular disorders in mammals especially in and not limited to humans and mice. The present disclosure further provides methods of treating cancer and appetite suppression using the compositions which are novel small molecule inhibitors of CaMKK2. In addition, these derived compositions can regulate non-ocular disorders, such as cancer and appetite suppression by modulating and inhibiting CaMKK2 and the regulation of the macrophage mediated diseases.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: July 2, 2019
    Assignee: Duke University
    Inventors: Scott W. Cousins, David M. Gooden, Priyatham S. Mettu
  • 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
  • Patent number: 10301315
    Abstract: The present invention relates to 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: November 17, 2017
    Date of Patent: May 28, 2019
    Assignee: CYSTIC FIBROSIS FOUNDATION THERAPEUTICS, INC.
    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: 10251888
    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: June 13, 2017
    Date of Patent: April 9, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Petrus Bekker, Shichang Miao, Israel Charo, Tom Schall
  • Patent number: 10196390
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: March 13, 2017
    Date of Patent: February 5, 2019
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren
  • Patent number: 10189849
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: January 29, 2019
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Patent number: 10189850
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: January 29, 2019
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Patent number: 10189851
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: January 29, 2019
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Patent number: 10174056
    Abstract: A compound having the structure of below Formula(I), or pharmaceutically acceptable salts thereof, are useful as Janus kinase inhibitors, wherein R1 and L1 are as herein described.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: January 8, 2019
    Assignee: WUXI FORTUNE PHARMACEUTICAL CO., LTD
    Inventors: Hao Wu, Weiwei Mao, Yiqiang Huang, Lili Fan, Shuhui Chen
  • Patent number: 10150770
    Abstract: A crystal form I of a Janus Kinase (JAK) inhibitor (3aR,5s,6aS)—N-(3-methoxyl-1,2,4-thiadiazole-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate of formula (I) is provided. Also provided is a method of preparing the crystal form I of the JAK inhibitor of formula (I). The preparation method includes crystallizing any crystal form or amorphous compound solid of formula (I) in a single organic solvent to obtain the form I crystal. The crystal form I has excellent crystal stability and chemical stability. Additionally, the crystal solvent used to produce the crystal form I has low toxicity and a relatively low content of residual solvent, making the compound better suited for clinical treatment.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: December 11, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Piaoyang Sun, Guaili Wu, Xiaohui Gao, Yongjiang Chen, Lingjia Shen
  • Patent number: 10118928
    Abstract: Methods of treating infections due to Helicobacter pylori (H. pylori), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering inhibitors of H.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: November 6, 2018
    Assignees: Albert Einstein College of Medicine, Inc., Victoria Link Limited
    Inventors: Vern L. Schramm, Keith Clinch, Shivali Ashwin Gulab
  • Patent number: 10072012
    Abstract: The present invention provides process for preparing crystalline Pemetrexed dipotassium (I) Form-SP9 characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2?° peaks selected from the XRPD peak set of 5.0, 12.5, 17.2, 20.8, 22.4, 25.7, 26.9 and 27.9±0.2 2?°. The invention also provides process for preparing its pharmaceutical composition thereof, which may be useful for anti-cancer treatment.
    Type: Grant
    Filed: November 11, 2014
    Date of Patent: September 11, 2018
    Assignee: Shilpa Mecicare Limited
    Inventors: Bhagat Raj Pipal, Venkata Reddy Gayam, Akshay Kant Chaturvedi
  • Patent number: 10023577
    Abstract: A crystal form of JAK kinase inhibitor bisulfate and a preparation method thereof are provided. In particular, a type II crystal of (3aR,5s,6aS)—N-(3-methoxyl-1,2,4-thiadiazole-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate and a preparation method thereof are described. The preparation method includes steps of crystallizing any solid crystal form or amorphous compound of formula (I) in a single organic solvent or a mixed organic solvent to obtain a type II crystal form of the compound of formula (I). The type II crystal form of the compound of formula (I) obtained by the described methods has good crystal stability and chemical stability. In addition, the solvent used for crystallization has low toxicity and residue, which is better suited for use in clinical treatment.
    Type: Grant
    Filed: October 9, 2015
    Date of Patent: July 17, 2018
    Assignee: JIANGSU HENGRUI CO., LTD.
    Inventors: Piaoyang Sun, Guaili Wu, Quanliang Zhang, Yongjiang Chen, Lingjia Shen
  • Patent number: 10016430
    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: March 9, 2017
    Date of Patent: July 10, 2018
    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: 9975907
    Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: May 22, 2018
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Yun-Long Li, Brian W. Metcalf, Andrew P. Combs
  • Patent number: 9968608
    Abstract: A pharmaceutical composition of Pemetrexed represented by formula (I), which is a liquid ready to use solution formulation or a lyophilized pharmaceutical composition for parenteral administration comprising a pharmaceutically acceptable organic amine, an inert gas and optionally containing at least one or more pharmaceutically acceptable excipients. Also provided are processes for preparation of the ready to use solution formulation or lyophilized pharmaceutical composition of the present invention.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: May 15, 2018
    Assignee: Fresenius Kabi Oncology Limited
    Inventors: Dhiraj Khattar, Rajesh Khanna, Mukti Yadav, Krishanu Burman
  • Patent number: 9962388
    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: August 14, 2015
    Date of Patent: May 8, 2018
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Zhaozhong Ding, Hao Wu, Fei Sun, Lifang Wu, Ling Yang
  • Patent number: 9957276
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: November 10, 2016
    Date of Patent: May 1, 2018
    Assignee: GI Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Patent number: 9937183
    Abstract: Methods and compounds for treating, preventing, reducing the risk of and/or delaying the onset of a microbial infection in a subject are disclosed herein, wherein the microbial infection is caused by one or more microorganisms (e.g., one or more bacteria) which can be used as a biological weapon, such as Bacillus anthracis, Franciscella tularensis, Yersinia pestis, Burkholderia mallei, and Burkholderia pseudomallei. Also disclosed are pharmaceutical compositions or kits for treating, preventing, reducing the risk of and/or delaying the onset of a microbial infection.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: April 10, 2018
    Assignee: Melinta Therapeutics, Inc.
    Inventors: Zoltan F. Kanyo, Ashoke Bhattacharjee
  • Patent number: 9879005
    Abstract: The present disclosure provides compositions and methods for treating ocular disorders in mammals especially in and not limited to humans and mice. The present disclosure further provides methods of treating cancer and appetite suppression using the compositions which are novel small molecule inhibitors of CaMKK2. In addition, these derived compositions can regulate non-ocular disorders, such as cancer and appetite suppression by modulating and inhibiting CaMKK2 and the regulation of the macrophage mediated diseases.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: January 30, 2018
    Assignee: Duke University
    Inventors: Scott W. Cousins, David M. Gooden, Priyatham S. Mettu
  • Patent number: 9867826
    Abstract: The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: January 16, 2018
    Assignee: Merck Patent GmbH
    Inventors: Ruoxi Lan, Xiaoling Chen, Yufang Xiao, Bayard R. Huck, Andreas Goutopoulos
  • Patent number: 9855246
    Abstract: The present invention relates to stable, preservative- and antioxidant-free liquid formulations of phenylephrine and ketorolac for injection.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: January 2, 2018
    Assignee: Omeros Corporation
    Inventors: Gregory A. Demopulos, Hui-rong Shen, Clark E. Tedford
  • Patent number: 9856261
    Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: January 2, 2018
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 9833448
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman