Hetero Ring Is Seven-membered Consisting Of Two Nitrogens And Five Carbon Atoms Patents (Class 514/218)
  • Patent number: 11926619
    Abstract: The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.
    Type: Grant
    Filed: April 8, 2019
    Date of Patent: March 12, 2024
    Assignee: Eisai R & D Management Co., Ltd.
    Inventors: Gregg F. Keaney, John Wang, Baudouin Gerard, Kenzo Arai, Xiang Liu, Guo Zhu Zheng, Kazunobu Kira, Lisa A. Marcaurelle, Marta Nevalainen, Ming-Hong Hao, Morgan Welzel O'Shea, Parcharee Tivitmahaisoon, Sudeep Prajapati, Tuoping Luo, Nicholas C. Gearhart, Jason T. Lowe, Yoshihiko Kotake, Satoshi Nagao, Regina Mikie Kanada Sonobe, Masayuki Miyano, Norio Murai, Andrew Cook, Shelby Ellery, Atsushi Endo, James Palacino, Dominic Reynolds
  • Patent number: 11857551
    Abstract: Acquired hearing loss due to chemotherapy or noise exposure is a major health problem, and cisplatin chemotherapy often causes permanent hearing loss in cancer patients. However, there are no FDA-approved drugs for the treatment or prevention of cisplatin- or noise-induced hearing loss. In one aspect, use of compounds as an active agent to treat a hearing impairment and to prevent a hearing impairment, and methods of treating and/or preventing hearing impairments or disorders using the compositions are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: July 9, 2021
    Date of Patent: January 2, 2024
    Assignee: Ting Therapeutics LLC
    Inventors: Jian Zuo, Pezhman Salehi Dermanaki
  • Patent number: 11771704
    Abstract: Disclosed are methods of treating patients with AD using a rho kinase inhibitor. A preferred rho kinase inhibitor used according to the invention is fasudil, which is typically administered orally in a total daily dose of 70-140 mg. A preferred dosing regimen involves administering the daily dose in three equal portions throughout the day. Preferred methods continue for more than one month and typically at least 2 or 3 months. Some preferred methods do not treat mild cognitive impairment and patients have and MMSE score of?23 and/or a CDR-SOB score of?4.5.
    Type: Grant
    Filed: February 28, 2023
    Date of Patent: October 3, 2023
    Assignee: Woolsey Pharmaceuticals, Inc.
    Inventors: Thomas MacAllister, Sven Jacobson
  • Patent number: 11621054
    Abstract: A method is performed by a computer for a preprocessing for calculating binding free energy between a first substance and a second substance. The method includes: obtaining a binding structure of the first substance and the second substance under a condition where the second substance is constrained such that a binding state of the second substance to the first substance is maintained in a predetermined state; and then, based on the obtained binding structure, obtaining the binding structure under a condition where the second substance is not constrained.
    Type: Grant
    Filed: January 6, 2020
    Date of Patent: April 4, 2023
    Assignee: FUJITSU LIMITED
    Inventor: Yoshiaki Tanida
  • Patent number: 11548883
    Abstract: The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical composition containing the same. The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.
    Type: Grant
    Filed: May 15, 2018
    Date of Patent: January 10, 2023
    Assignee: LegoChem Biosciences, Inc.
    Inventors: Dae Yon Lee, Sang Eun Chae, Eun Mi Jung, Eun Hye Yang, Yoon Jeong Choi, Chul-Woong Chung, Ju Hyun Shin, Yun Ki Kim, Hyun Jin Kwon, Jeong Hee Ryu, Eun Hye Ban, Yong Zu Kim, Yeong Soo Oh, Jeiwook Chae
  • Patent number: 11542248
    Abstract: The present disclosure provides compositions and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compositions and methods of use are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
    Type: Grant
    Filed: June 7, 2018
    Date of Patent: January 3, 2023
    Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Liansheng Li, Tao Wu, Jun Feng, Pingda Ren, Yi Liu, Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jonathan Pollock
  • Patent number: 11464785
    Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.
    Type: Grant
    Filed: November 14, 2018
    Date of Patent: October 11, 2022
    Assignee: OMEROS CORPORATION
    Inventors: Gregory A. Demopulos, George A. Gaitanaris, Roberto Ciccocioppo
  • Patent number: 11401266
    Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
    Type: Grant
    Filed: July 16, 2015
    Date of Patent: August 2, 2022
    Assignee: Merck Sharp & Dohme (UK) Ltd.
    Inventors: Carl A. Baxter, Faye Sheen
  • Patent number: 11401258
    Abstract: The Invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof: wherein W1, W2, W3, J1, J2, A, R1, R2, R3, R4, R5, a, and b are defined as set forth in the specification. The Invention also provides uses of the compounds of any one of Formulae (I)-(VIII) and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof. Compounds of the Invention are useful for treating a disorder responsive to blockade of one or more sodium channels. In certain embodiments, Compounds of the Invention are useful for treating pain.
    Type: Grant
    Filed: August 6, 2020
    Date of Patent: August 2, 2022
    Assignee: Purdue Pharma L.P.
    Inventors: Laykea Tafesse, Jae Hyun Park
  • Patent number: 11339151
    Abstract: The present invention relates to a compound represented by formula (1): the compound having antagonist activity against serotonin 5-HT2A receptors and serotonin 5-HT7 receptors; or a pharmaceutically acceptable salt of the compound. (In the formula, Z is a nitrogen atom and the like; Y is carbonyl and the like; m and n are 1 and the like; R1a through R1d, R2a through R2d, and R4a through R4d are a hydrogen atom and the like; R3 is alkyl and the like; and Q is a specific bicyclic group.
    Type: Grant
    Filed: November 17, 2021
    Date of Patent: May 24, 2022
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Yuki Fujii, Masayuki Sakuma, Yoshinori Aihara, Jeremy Besnard, Andrew Simon Bell
  • Patent number: 11311541
    Abstract: The invention relates to treatment of graft versus host disease (GVHD) using compounds that inhibit ROCK2. In preferred aspects, the present invention provides methods for the treatment of GVHD, including chronic GVHD (cGVHD) using compounds having the formulae 1-XXV, as set forth herein.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: April 26, 2022
    Assignees: KADMON CORPORATION, LLC, REGENTS OF THE UNIVERSITY OF MINNESOTA
    Inventors: Alexandra Zanin-Zhorov, Bruce Robert Blazar, Ryan Flynn
  • Patent number: 11291668
    Abstract: The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.
    Type: Grant
    Filed: March 25, 2020
    Date of Patent: April 5, 2022
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Frank Himmelsbach, Michael Mark
  • Patent number: 11091460
    Abstract: Provided are a Syk inhibitor and a use method therefor, and in particular, disclosed are quinolinone represented by formula (I) or quinazoline derivatives or pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition, and uses in preparing a medicament for treatment of Syk receptor related diseases.
    Type: Grant
    Filed: June 14, 2018
    Date of Patent: August 17, 2021
    Assignee: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    Inventors: Shilan Liu, Guibai Liang, Hongjian Wang, Ming Zhang, Shuhui Chen
  • Patent number: 11078182
    Abstract: The present invention encompasses compounds of the formula I which are suitable for the treatment of diseases related to Vanin, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.
    Type: Grant
    Filed: December 2, 2019
    Date of Patent: August 3, 2021
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Thomas Fleck, Cedrickx Godbout, Hannes Fiepko Koolman
  • Patent number: 11046731
    Abstract: The present disclosure relates to compounds useful in the treatment, imaging, and/or diagnosis of Epstein-Barr virus (EBV)-positive cells, such as cancer.
    Type: Grant
    Filed: January 17, 2019
    Date of Patent: June 29, 2021
    Assignee: Hong Kong Baptist University
    Inventors: Ka Leung Wong, Nai Ki Mak, Lijun Jiang
  • Patent number: 10993948
    Abstract: Provided are novel compounds which are capable of inhibiting an activity of RNA polymerase I, and uses thereof in treating diseases or disorders modulated by RNA polymerase I, preferably autoimmune diseases such as multiple sclerosis and proliferative diseases.
    Type: Grant
    Filed: June 4, 2018
    Date of Patent: May 4, 2021
    Assignee: Tel HaShomer Medical Research Infrastructure and Services Ltd.
    Inventors: Anat Achiron, Roi Mashiach, Michael Gurevich
  • Patent number: 10980861
    Abstract: The present invention relates to the use of liver-selective glucokinase activators and a GLP1 analog in restoring insulin sensitivity and treating type II diabetes, including reducing body weight in subjects undergoing type II diabetes treatment.
    Type: Grant
    Filed: January 16, 2020
    Date of Patent: April 20, 2021
    Assignee: vTv Therapeutics LLC
    Inventors: Maria Carmen Valcarce Lopez, Tung Fong
  • Patent number: 10968238
    Abstract: Methods of producing a compound represented by formula (I) or a pharmacologically acceptable salt thereof include: wherein L1 is an optionally substituted C1-6 alkylene group or the like, L2 is a single bond or the like, L3 is a single bond or the like, R1, R2, and R3 are each independently an optionally substituted C1-4 alkyl group or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: April 6, 2021
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Noriaki Iwase, Shigeyuki Kono, Masayuki Tanaka, Masaaki Matoyama, Satoshi Umezaki, Yusuke Shiraishi, Masahiro Kojima, Hayato Nishiyama
  • Patent number: 10947504
    Abstract: The present invention provides a highly functional platelet production promoting agent which comprises one or a plurality of aryl hydrocarbon receptor (AhR) antagonists and one or a plurality of Rho-associated coiled-coil forming kinase (ROCK) inhibitors.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: March 16, 2021
    Assignees: Kyoto University, Megakaryon Corporation
    Inventors: Koji Eto, Sou Nakamura, Yukitaka Ito, Tomohiro Shigemori, Takeaki Dohda
  • Patent number: 10882841
    Abstract: Compounds and compositions are provided as inhibitors of the Wnt/?-catenin pathway for the treatment of diseases that implicate the same.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: January 5, 2021
    Assignee: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Fengtian Xue, Yan Shu
  • Patent number: 10856564
    Abstract: The present invention relates to a novel emulsion structured in an isometric crystalline network of cellulose derivatives where the emulsion comprises Omega-3 fatty acids homogeneously distributed in the same. The emulsion of the invention has been designed to have greater stability, bioavailability and gastro-resistance and may be used in special medical foods, nutritional supplements, sports nutrition, enteral nutrition or child nutrition, amongst others.
    Type: Grant
    Filed: October 3, 2016
    Date of Patent: December 8, 2020
    Assignee: Solutex NA, LCC
    Inventors: Fernando Moreno Egea, Antonio Martínez Férez
  • Patent number: 10815219
    Abstract: Novel 2,4-diaminoquinazoline derivatives are disclosed. The compounds can be used in treating diseases and conditions which are associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic ?-cell dysfunction and death, for example in the treatment of diabetes.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: October 27, 2020
    Assignee: The Board of Regents of the University of Oklahoma
    Inventors: Weidong Wang, Jae Wook Lee
  • Patent number: 10787433
    Abstract: Pyradizine derivatives that activity the excitatory amino acid transporter 2 (EAAT2) of the formula: and methods of use thereof for treating or preventing diseases, disorders, and conditions with glutamate toxicity.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: September 29, 2020
    Assignees: THE BRIGHAM AND WOMEN'S HOSPITAL, INC., OHIO STATE UNIVERSITY
    Inventors: Kevin Hodgetts, Chien-Liang Glenn Lin
  • Patent number: 10745377
    Abstract: The present invention relates to piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: August 18, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Milana M. Maletic, Yunfu Luo, Zhiqi Qi, Tingting Yu, Richard Soll
  • Patent number: 10738026
    Abstract: The Invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof: wherein W1, W2, W3, J1, J2, A, R1, R2, R3, R4, R5, a, and b are defined as set forth in the specification. The Invention also provides uses of the compounds of any one of Formulae (I)-(VIII) and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof. Compounds of the Invention are useful for treating a disorder responsive to blockade of one or more sodium channels. In certain embodiments, Compounds of the Invention are useful for treating pain.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: August 11, 2020
    Assignee: Purdue Pharma L.P.
    Inventors: Laykea Tafesse, Jae Hyun Park
  • Patent number: 10723715
    Abstract: Compounds and compositions are provided as inhibitors of the Wnt/?-catenin pathway for the treatment of diseases that implicate the same.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: July 28, 2020
    Assignee: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Fengtian Xue, Yan Shu
  • Patent number: 10683281
    Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: August 8, 2019
    Date of Patent: June 16, 2020
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Scott W. Bagley, John M. Curto, David James Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Yajing Lian, Chris Limberakis, Allyn T. Londregan, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
  • Patent number: 10676468
    Abstract: Disclosed are novel N-(3-heteroarylaryl)-4-arylarylcarboxamides and analogs thereof, represented by the Formula I: wherein C cyclic group, D1-D4, Q1, Q2, R5 are defined herein. Compounds having Formula (I) are hedgehog pathway inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of hedgehog activity, such as cancer.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: June 9, 2020
    Assignee: Impact Therapeutics, Inc.
    Inventors: Suixiong Cai, Ye Edward Tian, Sishun Kang, Zheng Meng, Chengyun Gu, Feng Yin, Shengzhi Chen, Yang Zhang, Xiuyan Zhang, Hongqiang Fei, Dongmei Wang
  • Patent number: 10676465
    Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: August 8, 2019
    Date of Patent: June 9, 2020
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Scott W. Bagley, John M. Curto, David James Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Yajing Lian, Chris Limberakis, Allyn T. Londregan, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
  • Patent number: 10654849
    Abstract: Compounds of formula (I): wherein R1, R2, J, K, L, n and W are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring pro-apoptotic and/or anti-proliferative agents.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: May 19, 2020
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: András Kotschy, Csaba Wéber, Attila Vasas, Balázs Molnár, árpád Kiss, Alba Macias, James Brooke Murray, Elodie Lewkowicz, Olivier Geneste, Mäia Chanrion, Didier Demarles, Lisa Ivanschitz
  • Patent number: 10654869
    Abstract: The present invention provides compounds as bacterial topoisomerase inhibitors with antibacterial activity. The present invention also provides pharmaceutical compositions comprising at least one of the compounds and methods of using the compounds and pharmaceutical compositions as antibacterial agents for treating infectious diseases.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: May 19, 2020
    Assignees: THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES, UNIVERSITY OF HAWAII
    Inventors: Yuk-Ching Tse-Dinh, Dianqing Sun
  • Patent number: 10632125
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: April 28, 2020
    Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNING
    Inventors: Martin Scobie, Olov Wallner, Tobias Koolmeister, Karl Sven Axel Vallin, Carl Martin Henriksson, Evert Homan, Thomas Helleday, Sylvain Jacques, Roland Julius Yu Fiskesund
  • Patent number: 10632103
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Grant
    Filed: January 26, 2018
    Date of Patent: April 28, 2020
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Patent number: 10603354
    Abstract: This invention concerns compositions and methods of treating or diagnosing inflammatory disorders and other disorders, as well as compositions and methods of treating HIV.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: March 31, 2020
    Assignees: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, ACTINOBAC BIOMED, INC.
    Inventors: Scott C. Kachlany, Benjamin A. Belinka, Jr.
  • Patent number: 10570137
    Abstract: The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein R1 is C1-C3alkyl optionally substituted with F, C3-C6cycloalkyl, C1-C3alkoxy; X represents a bond or C1-C3alkylene optionally substituted with OH, ONO, ONO2; R2 is H, OH, ONO, ONO2, C(O)OH, C(O)OC1-C3alkyl, CHO, CN, C1-C3alkoxy, OC(O)H, OC(O)—C1-C3alkyl, C(O)N(R6)OR7, OC1-C3alkylene-C(O)OH, OC1-C3alkylene-C(O)OC1-C3alkyl, OC1-C3alkylene-C(O)N(R6)OR7, S(O0-2)C1-C3alkyl, CR8?N—OR9, CR8?N—NR10R11, CR8?NR12 or CR8?N—ONO2; R3 is C1-C6alkyl optionally substituted with F, OH, ONO, ONO2, C1-C3alkoxy, C3-C6cycloalkyl; C3-C6cycloalkyl, C2-C6alkenyl, C2-C6alkynyl; R4 is C1-C6alkyl optionally substituted with C3-C6cycloalkyl, C1-C6alkoxy, F, ONO, ONO2; C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl; R5 is H, SO2NR13R14, NHSO2NR13R14; R6 is H or C1-C3alkyl; R7 is H, C1-C3alkyl, C1-C3alkoxy, C1-C3alkyl substituted with phenyl, benzyl or a heterocyclic ring, wherein said phenyl, benzyl or
    Type: Grant
    Filed: November 15, 2016
    Date of Patent: February 25, 2020
    Assignee: TOPADUR PHARMA AG
    Inventors: Reto Naef, Hermann Tenor
  • Patent number: 10548899
    Abstract: The present invention provides a compound which has a cholinergic muscarinic M1 receptor positive allosteric modulator activity and may be useful as a medicament such as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, Lewy body dementia and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. In the formula (I), each symbol is as described in the attached specification.
    Type: Grant
    Filed: October 19, 2016
    Date of Patent: February 4, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Sugimoto, Shinkichi Suzuki, Hiroki Sakamoto, Masami Yamada, Minoru Nakamura, Makoto Kamata, Kenichiro Shimokawa, Masaki Ogino, Eiji Kimura, Masataka Murakami, Takuto Kojima, Jinichi Yonemori
  • Patent number: 10478430
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase and combination therapies thereof. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: November 19, 2019
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Robert Pollard, Philip Michael Reaper, Mohammed Asmal
  • Patent number: 10449192
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Grant
    Filed: February 26, 2018
    Date of Patent: October 22, 2019
    Assignee: KUDO PHARMACEUTICALS LIMITED
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • Patent number: 10426783
    Abstract: Disclosed herein is a prophylactic or therapeutic agent for ocular fundus disease, especially diabetic retinopathy or age-related macular degeneration. The prophylactic or therapeutic agent for ocular fundus disease comprising: (S)-(?)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, a salt thereof, or a solvate thereof, as an active ingredient.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: October 1, 2019
    Assignees: KYUSHU UNIVERSITY, NAT'L UNIVERSITY CORPORATION, KOWA COMPANY, LTD.
    Inventors: Tatsuro Ishibashi, Shintaro Nakao, Ryoichi Arita, Ken Mizuno, Akifumi Tsuchiura
  • Patent number: 10407376
    Abstract: The present invention is directed to a method for preparing a final phenolic product from biomass comprising the steps of providing a furanic compound obtainable from biomass; reacting the furanic compound with a dienophile to obtain a phenolic compound; reacting the phenolic compound further to obtain the final phenolic product.
    Type: Grant
    Filed: January 18, 2016
    Date of Patent: September 10, 2019
    Assignee: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO
    Inventors: Marc Crockatt, Jan Harm Urbanus, Paul Mathijs Konst, Martijn Constantijn De Koning
  • Patent number: 10369128
    Abstract: A method for treating a proliferative disease, disorder, or condition comprising administering a cis-diamine platinum(II) thione complex. A cis-diamine platinum(II) thione complex and compositions containing it.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: August 6, 2019
    Assignee: King Fahd University of Petroleum and Minerals
    Inventors: Mohammed Yagoub Jomaa, Anvarhusein A. Isab
  • Patent number: 10364234
    Abstract: Pyridinecarboxamide derivatives, preparation methods, and a pharmaceutical uses thereof are provided. In particular, pyridinecarboxamide derivatives represented by general formula (I), wherein the substituents of the formula (I) are defined in the specification are provided. Also provided are a preparation method for the pyridinecarboxamide derivatives of formula (I), a pharmaceutical composition containing the pyridinecarboxamide derivatives, and uses of the pyridinecarboxamide derivatives as therapeutic agents, especially as inhibitors of the Renal Outer Medullary Potassium channel (ROMK) and in the preparation of medicaments for treating and/or preventing hypertension and heart failure.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: July 30, 2019
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Xin Li, Qing Dong, Piaoyang Sun
  • Patent number: 10363244
    Abstract: The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator.
    Type: Grant
    Filed: August 8, 2018
    Date of Patent: July 30, 2019
    Assignee: vTv Therapeutics LLC
    Inventors: Adnan M. M. Mjalli, Maria Carmen Valcarce Lopez
  • Patent number: 10357503
    Abstract: This invention relates to a method for the prevention of cardiovascular disease, a formulation for the prevention of cardiovascular disease, the use of specified active principals for the manufacture of such a formulation for use in the method and to a method of preparing said formulation. The formulation of the present invention is a combination of active principals for use in the prevention of cardiovascular disease, notably ischaemic heart disease (including heart attacks) and stroke among the general adult population.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: July 23, 2019
    Inventors: Nicholas J Wald, Malcolm R Law
  • Patent number: 10357473
    Abstract: A method for treating a proliferative disease, disorder, or condition comprising administering a cis-diamine platinum(II) thione complex. A cis-diamine platinum(II) thione complex and compositions containing it.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: July 23, 2019
    Assignee: King Fahd University of Petroleum and Minerals
    Inventors: Mohammed Yagoub Jomaa, Anvarhusein A. Isab
  • Patent number: 10351535
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opioid receptor and more particularly to piperazine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: July 16, 2019
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Félix Cuevas-Cordobés, Carmen Almansa-Rosales, Monica Garcia Lopez
  • Patent number: 10329270
    Abstract: The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: June 25, 2019
    Assignee: Merck Patent GmbH
    Inventors: Hui Qiu, Richard D. Caldwell, Constantin Neagu, Igor Mochalkin, Lesley Liu-Bujalski, Reinaldo Jones, Devon Tate, Theresa L. Johnson, Anna Gardberg
  • Patent number: 10292968
    Abstract: The present application relates to substituted heterocycles compound of Formula I and pharmaceutical compositions thereof useful for the inhibition of BET protein function by binding to bromodomains (Formula I).
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: May 21, 2019
    Assignee: Zenith Epigenetics Ltd.
    Inventors: Samuel David Brown, Craig Alan Coburn, Olesya Kharenko
  • Patent number: 10292990
    Abstract: A nanoparticulate composition of abiraterone acetate that allows treatment at a lower dose than convention abiraterone acetate formulations is described as in a method of treating prostate cancer by administering the composition together with a glucocorticoid.
    Type: Grant
    Filed: November 7, 2016
    Date of Patent: May 21, 2019
    Assignee: SUN PHARMA GLOBAL FZE
    Inventors: Paul Nemeth, Matt Callahan, H. William Bosch, Marck Norret
  • Patent number: RE49698
    Abstract: The invention relates to substituted dihydroquinazolines and to processes for their preparation and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for use as antiviral agents, in particular against cytomegalo viruses.
    Type: Grant
    Filed: July 21, 2020
    Date of Patent: October 17, 2023
    Assignee: AIC246 AG & Co. KG
    Inventors: Tobias Wunberg, Judith Baumeister, Ulrich Betz, Mario Jeske, Thomas Lampe, Susanne Nikolic, Jurgen Reefschlager, Rudolf Schohe-Loop, Frank Sussmeier, Holger Zimmermann, Rolf Grosser, Kerstin Henninger, Guy Hewlett, Jorg Keldenich, Dieter Lang, Peter Nell