Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,4-benzoxazines, Etc.) Patents (Class 514/230.5)
  • Patent number: 11028075
    Abstract: The invention provides benzene sulfonamides and pharmaceutically acceptable salt thereof that are useful as sodium channel blockers for the treatment of, for example, pain.
    Type: Grant
    Filed: February 22, 2019
    Date of Patent: June 8, 2021
    Assignee: Genentech, Inc.
    Inventors: Daniel Sutherlin, Steven McKerrall, Kwong Wah Lai, Zhiguo Liu, Wenfeng Liu, Ramsay Beveridge, Jean-Philippe Leclerc, Alexandre Lemire, Liang Zhao, Claudio Sturino
  • Patent number: 11028101
    Abstract: A compound of formula Ia, Ib, Ic or Id: wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(?O)NH2, and —CH2OH; R4b is either H or Me; R5 is either H or Me; m is 1 or 2; q is 0 or 1; R11a, R11b, R11c and R11d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH—C1-4 alkyl and cyano; R12a and R12b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R12c and R12d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R12e is H or Me; R13a and R13b are independently selected from H and Me; R14 is either H or Me; R16a
    Type: Grant
    Filed: November 18, 2019
    Date of Patent: June 8, 2021
    Assignee: CTXT PTY LTD
    Inventor: Paul Anthony Stupple
  • Patent number: 11007193
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: June 19, 2019
    Date of Patent: May 18, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 10968219
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ay-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: April 6, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guohua Zhao, Pratik Devasthale, Xiang-Yang Ye, Kumaravel Selvakumar, Suresh Dhanusu, Palanikumar Balasubramanian, Leatte R. Guernon, Rita Civiello, Xiaojun Han, Michael Frederick Parker, Swanee E. Jacutin-Porte
  • Patent number: 10927116
    Abstract: The present invention relates to a process for synthesizing a compound of formula (I), R1 is phenyl, which is unsubstituted or substituted with one, two or three substituents independently selected from halogen and C1-6alkyl; R2 is C1-6alkyl; R3 is —CxH2x—; x is 1, 2, 3, 4, 5, 6 or 7; or pharmaceutically acceptable salt or diastereomer thereof, which is useful for prophylaxis and treatment of a viral disease in a patient relating to hepatitis B infection or a disease caused by hepatitis B infection.
    Type: Grant
    Filed: August 20, 2018
    Date of Patent: February 23, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Junli Chen
  • Patent number: 10888561
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Grant
    Filed: April 8, 2019
    Date of Patent: January 12, 2021
    Assignee: Heptares Therapeutics Limited
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Patent number: 10827755
    Abstract: Substituted imidazole and substituted pyrazole compounds and compositions derived therefrom can be useful in controlling insect pests. Suitable imidazole compounds can be analogues of 2,4,5-triphenyl-1H-imidazole, wherein the C-2 phenyl group bears at least one substitution, the C-4 and C-5 phenyl groups are optionally substituted, and N-1 is unsubstituted. Suitable pyrazole compounds can bear a 1,3,4-substitution pattern, with an optionally substituted aryl or optionally substituted alkyl group being present at N-1, an optionally substituted aryl or optionally substituted heteroaryl group being present at C-3, and a secondary amide group being present at C-4. These compounds and compositions derived therefrom can be administered to a plant, seed, soil or insect to control a variety of insect pests.
    Type: Grant
    Filed: November 9, 2016
    Date of Patent: November 10, 2020
    Assignee: Monsanto Technology LLC
    Inventors: Michael J. Crawford, Matthew Dimmic, Rae Lawrence, Christina Marie Taylor
  • Patent number: 10828301
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: May 3, 2019
    Date of Patent: November 10, 2020
    Assignee: Rigel Pharmceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 10792261
    Abstract: Compositions for reducing the frequency of urination and methods of manufacturing the compositions are disclosed. The compositions comprises a first component having an immediate-release subcomponent and an extended-release subcomponent, wherein the first component is formulated to release the subcomponents immediately after administration; and a second component comprising an immediate-release subcomponent and an extended-release subcomponent, wherein the second component is formulated for a delayed-release of the subcomponents.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: October 6, 2020
    Assignee: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: David A. Dill
  • Patent number: 10774091
    Abstract: The present invention generally relates to novel pharmaceutical formulations containing 2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide, methods of preparation thereof and their use in medical therapy.
    Type: Grant
    Filed: March 13, 2019
    Date of Patent: September 15, 2020
    Assignee: KaNDy Therapeutics Limited
    Inventors: Mike Trower, Monica Lazaro, Derek Bush, David Elder, Mary Kerr
  • Patent number: 10745414
    Abstract: The invention is relevant to chemistry of organic compounds, pharmacology and medicine, and is related to prevention and treatment of musculoskeletal diseases in human and animals associated with the disorder of bone and/or cartilage metabolism, particularly with such musculoskeletal diseases as osteoporosis, osteoarthritis and osteochondrosis, using a new salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazine-2-yl)amino)-2H-pyrido[3,2-b][1,4]oxazine-3(4H)-one. A salt of this compound with 4-methylbenzenesulfonic acid including its hydrates, solvates and polymorphic modifications of the salt, hydrates and solvates is featured with acceptable pharmacokinetic parameters and increased efficiency in the inhibition of Src-family kinases and Syk kinase, as well as other therapeutically significant kinases. This invention also covers pharmaceutical compositions containing therapeutically effective amount of the salt according to the invention.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: August 18, 2020
    Assignee: LIMITED “MOLECULAR TECHNOLOGIES”
    Inventors: Vladimir Evgenievich Nebolsin, Fedor Nikolaevich Novikov, Germes Grigorievich Chilov, Oleg Valentinovich Stroganov, Viktor Sergeevich Stroilov, Ilya Yurievich Titov
  • Patent number: 10730877
    Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: November 26, 2019
    Date of Patent: August 4, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Trevor C. Sherwood, Brian K. Whiteley, John L. Gilmore, Sreekantha Ratna Kumar, Laxman Pasunoori, Pitani Veera Venkata Srinivas, Srinivasan Kunchithapatham Duraisamy, Subramanya Hegde, Rushith Kumar Anumula
  • Patent number: 10689373
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein L, X, Ra, Rb, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: June 1, 2018
    Date of Patent: June 23, 2020
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Charlotte Fieldhouse, Angela Glen, Stephanie Maine, Tatsuhiko Fujimoto, John Stephen Robinson
  • Patent number: 10669283
    Abstract: A compound represented by the general formula (1) below or a pharmacologically acceptable salt thereof: [In the formula (1), R1 and R2 may be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a carboxy group, a cyano group, an optionally substituted C1-6 alkyl group et al.; R3 represents a hydrogen atom; R4 represents an optionally substituted 4- to 10-membered monocyclic heterocyclic group containing 1 to 4 heteroatoms selected from an oxygen atom, a nitrogen atom, and a sulfur atom; X represents a group represented by the following formula: —CH2—, —CH2—CH2—, —CH2—CH2—CH2—, or —CH2—O—CH2—; and Z represents a hydrogen atom or a hydroxyl group].
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: June 2, 2020
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Keiji Tamura, Takeru Yamakawa, Satoshi Isshiki, Yoshinari Wakiyama, Shohei Ouchi, Takashi Matsuhira, Natsuki Ishida, Yuji Tabata
  • Patent number: 10653626
    Abstract: This document discloses a powder formulation of lamotrigine for oral administration. Also disclosed is a suspension of lamotrigine and a method of treating diseases.
    Type: Grant
    Filed: October 26, 2018
    Date of Patent: May 19, 2020
    Assignee: Shanghai Aucta Pharmaceuticals Co., Ltd.
    Inventors: Enxian Lu, Shoufeng Li
  • Patent number: 10610521
    Abstract: The present invention relates to the use of one or more biomarkers to evaluate the likelihood that a rapamycin analog would produce an anti-cancer effect in a subject. It is based, at least in part, on the results of experiments employing an integrated next-generation sequencing approach to interrogate spatially separated tumor specimens from the same individuals to decipher intra-tumor and intertumor heterogeneity and determine the oncogenomic basis of exceptional therapeutic benefit to rapalogs in kidney cancer patients. These experiments implicated loss of function mutations in TSC1 and/or TSC2 and/or gain-of-function of mTOR in therapeutic responsiveness to rapamycin analogs.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: April 7, 2020
    Assignee: MEMORIAL SLOAN KETTERING CANCER CENTER
    Inventors: James J. Hsieh, Michael Berger, Robert Motzer, Martin H. Voss, A Ari Hakimi, Can Pham, Emily Cheng, Angela Rose Brannon, Jianing Xu
  • Patent number: 10604517
    Abstract: The present invention relates to compounds of formula hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S-lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or two neighboring carbon atoms may form on phenyl an additional ring containing —O—CH2—O—; n is 1 to 5; R2 is hydrogen or lower alkyl substituted by halogen; R3 is hydrogen or lower alkyl substituted by halogen; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers or optical isomers or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: March 31, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karlheinz Baumann, Guido Galley, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Rosa Maria Rodriguez Sarmiento, Björn Bartels, Hasane Ratni
  • Patent number: 10596173
    Abstract: The present invention is directed to compositions and methods for treating hepatitis B virus infection. In particular, the present invention is directed to a combination therapy comprising administration of an HBV capsid assembly inhibitor and an interferon for use in the treatment of hepatitis B virus infections.
    Type: Grant
    Filed: May 3, 2018
    Date of Patent: March 24, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lu Gao, Isabel Najera, Hong Shen, Fang Shen, Liping Shi, Steffen Wildum, Guang Yang
  • Patent number: 10577381
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: March 3, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • Patent number: 10457676
    Abstract: The present disclosure relates generally to derivatives of capsazepine and methods of use thereof In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. In some aspects of the present disclosure, the disclosure provides capsazepine derivatives which may be useful in the treatment of cancer. Such cancers that the compounds may be used to treating include but are not limited to breast, cervical, oral, head, neck, or prostate cancer. In some aspects, the compounds may be useful in treating a tumor by direct injection of the compound into the tumor, particularly an oral tumor. In other aspects, the compounds are administered systemically. The compounds of the present disclosure may also be used to treat the pain associated with a tumor for which it is being administered.
    Type: Grant
    Filed: August 25, 2015
    Date of Patent: October 29, 2019
    Assignee: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Cara B. Gonzales, Stanton McHardy
  • Patent number: 10441590
    Abstract: The present invention provides a method of using arylpiperazine derivatives for treating pulmonary hypertension. The method comprises a step of administering to a patient in need thereof an effective amount of a compound of Formula 1, which is an arylpiperazine derivative.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: October 15, 2019
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Marc Cantillon, Ellen M. Wallis, Seema Rani Bhat
  • Patent number: 10442798
    Abstract: The invention provides tetrahydroquinoline sulfonamide compounds, tetrahydronaphthalene sulfonyl compounds, and related compounds, pharmaceutical compositions, methods of promoting RORy activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds.
    Type: Grant
    Filed: February 7, 2018
    Date of Patent: October 15, 2019
    Assignee: Lycera Corporation
    Inventors: Thomas D. Aicher, Clarke B. Taylor, Chad A. VanHuis
  • Patent number: 10407443
    Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: July 23, 2018
    Date of Patent: September 10, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Todd Macklin, Maria Hopkins, Shota Kikuchi
  • Patent number: 10358453
    Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
    Type: Grant
    Filed: February 24, 2016
    Date of Patent: July 23, 2019
    Assignee: Alios BioPharma, Inc.
    Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Karin Ann Stein
  • Patent number: 10336721
    Abstract: The present disclosure describes biaryl triazole compounds, as well as their compositions and methods of use. The compounds inhibit the activity of macrophage migration inhibitory factor and are useful for the treatment of diseases, e.g., inflammatory diseases and cancer.
    Type: Grant
    Filed: February 12, 2016
    Date of Patent: July 2, 2019
    Assignee: Yale University
    Inventors: William L. Jorgensen, Pawel Dziedzic, Jose Cisneros
  • Patent number: 10301294
    Abstract: Disclosed are compounds that can be used for treating tuberculosis.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: May 28, 2019
    Assignees: THE BROAD INSTITUTE INC., MASSACHUSETTS GENERAL HOSPITAL, BRIGHAM AND WOMEN'S HOSPITAL
    Inventors: Timothy A. Lewis, Sivaraman Dandapani, Deborah Hung, Benito Munoz, Partha Nag, Sarah Grant, Tomohiko Kawate
  • Patent number: 10287299
    Abstract: A series of substituted 3,4-dihydro-2H-.1,4-benzoxazin-3-one derivatives, and analogs thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neuradegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: May 14, 2019
    Assignee: UCB Biopharma SPRL
    Inventors: Gareth Neil Brace, Prafulkumar Tulshibhai Chovatia, Gregory Foulkes, James Andrew Johnson, Severine Danielle Jones, Boris Kroeplien, Fabien Claude Lecomte, Pui Leng Loke, Martin Alexander Lowe, Ajay Mandal, Timothy John Norman, Christopher Francis Palmer, Yolanda Pérez-Fuertes, John Robert Porter, Donald Smyth, Giancarlo Trani, Muhammed Uddin, Zhaoning Zhu
  • Patent number: 10287300
    Abstract: The invention provides novel imidazol-piperidinyl derivatives of the formula (I) in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: May 14, 2019
    Assignee: Merck Patent GmbH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao
  • Patent number: 10273235
    Abstract: Substituted dihydroisoxazole derivatives useful as inhibitors of ?-lactamases are provided. The invention further provides medical uses of substituted dihydroisoxazole derivatives, for example, as antibacterial agents.
    Type: Grant
    Filed: March 9, 2018
    Date of Patent: April 30, 2019
    Assignee: LegoChem Biosciences, Inc.
    Inventors: Hye Kyung Chang, Sung Yoon Baek, Min Jung Kim, Kyu Man Oh, Jeung Soon Choi, Soo Bong Ha, Sung Min Kim, Chul-woong Chung, Dae Hyuck Kang, Hyun Jin Kwon, Young Lag Cho, Yong Zu Kim
  • Patent number: 10253041
    Abstract: Phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds of Formula I, formulations containing those compounds, and their use as mutant isocitrate dehydrogenase 1 enzyme inhibitors.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: April 9, 2019
    Assignee: Eli Lilly and Company
    Inventors: Renato A. Bauer, Serge Louis Boulet, Timothy Paul Burkholder, Santiago Carballares Martin, James Ronald Gillig, Raymond Gilmour, Wenceslao Lumeras, Zhipei Wu
  • Patent number: 10246417
    Abstract: This disclosure relates to picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: April 2, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: Brian A. Loy, Jared W. Rigoli, Brannon Sam, Kevin G. Meyer, Chenglin Yao
  • Patent number: 10233180
    Abstract: Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.
    Type: Grant
    Filed: March 21, 2015
    Date of Patent: March 19, 2019
    Assignees: ZHEJIANG UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Xiaowu Dong, Jia Li, Bo Yang, Yongzhou Hu, Yubo Zhou, Qinjie Weng, Wenhu Zhan, Lei Xu, Tao Liu, Qiaojun He
  • Patent number: 10227305
    Abstract: The present invention relates to a process for preparing indacaterol or salts thereof. The process comprises of forming compound of Formula 1 by reacting compound of Formula 2 and compound of Formula 3 in the presence of a solvent to Form compound of Formula 4, which on removal of the protecting groups forms compound of Formula 1.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: March 12, 2019
    Inventors: G. Pratap Reddy, Venkataiah Sunku, Sunkaraneni Suresh Babu
  • Patent number: 10221161
    Abstract: The present invention provides compounds of formula (I), compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R5, R6, R7, R12, R13, A, L, B, n, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: March 5, 2019
    Assignee: Kalvista Pharmaceuticals Limited
    Inventors: Hannah Joy Edwards, David Michael Evans, Premji Meghani, Andrew Richard Novak
  • Patent number: 10213477
    Abstract: Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: February 26, 2019
    Assignee: Aileron Therapeutics, Inc.
    Inventors: Vincent Guerlavais, Carl Elkin, Huw M. Nash, Tomi K. Sawyer, Bradford J. Graves, Eric Feyfant
  • Patent number: 10208034
    Abstract: A compound represented by general formula (I) and having a quinoline skeleton has a strong Axl inhibitory activity, and therefore the compound can be an agent for treating Axl-related diseases, for example, cancer such as acute myeloid leukemia, chronic myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases.
    Type: Grant
    Filed: December 24, 2015
    Date of Patent: February 19, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Takayuki Inukai, Jun Takeuchi, Tomoko Yasuhiro
  • Patent number: 10208061
    Abstract: The invention provides tetrahydro[1,8]naphthyridine and related compounds, pharmaceutical compositions, methods of promoting ROR activity, increasing the amount of IL-17 in a subject, and treating cancer using such tetrahydro[1,8]naphthyridine and related compounds.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: February 19, 2019
    Assignee: Lycera Corporation
    Inventors: Thomas D. Aicher, Peter L. Toogood, Xiao Hu
  • Patent number: 10195205
    Abstract: This invention relates to new use of dual NK-1/NK-3 receptor antagonists or a pharmaceutically acceptable salt thereof in the treatment of sex-hormone dependent diseases.
    Type: Grant
    Filed: May 18, 2016
    Date of Patent: February 5, 2019
    Assignee: NeRRe Therapeutics Limited
    Inventor: Mike Trower
  • Patent number: 10155731
    Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: December 18, 2018
    Assignees: MITSUBISHI TANABE PHARMA CORPORATION, SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie, Miki Hirai
  • Patent number: 10155758
    Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Grant
    Filed: September 26, 2017
    Date of Patent: December 18, 2018
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
  • Patent number: 10149841
    Abstract: A compound of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently H; R3 is selected from H, a C1-C7 straight-chain, and a branched or cyclic alkyl; and R4, R5, R6, R7, and R8 are each independently selected from C1-C7 alkyl, halo C1-C7 alkyl and the like. Also provided is a method for preparing the compound, pharmaceutical compositions including the compound or pharmaceutically acceptable salts thereof, and uses of the compound or pharmaceutically acceptable salt thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: December 11, 2018
    Assignee: SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
    Inventors: Yunlong Zhou, Suixiong Cai, Guangfeng Wang, Lingling Jiao, Ping Min, Yu Jing, Ming Guo
  • Patent number: 10124004
    Abstract: The purpose of the present invention is to provide a compound having an excellent CDK4/6 inhibiting activity. The present invention is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: November 13, 2018
    Assignee: Teijin Pharma Limited
    Inventors: Tsuyoshi Mizuno, Tomohiro Shimada, Gen Unoki, Masaru Ebisawa, Susumu Takeuchi, Kunio Minamizono, Kosuke Sasaki, Takuya Yokosaka, Junji Igarashi, Akinobu Maruyama, Hiroshi Takahashi, Kyohei Horie, Yuri Sakai
  • Patent number: 10125145
    Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: November 13, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
  • Patent number: 10077259
    Abstract: The present disclosure provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n, and dotted line have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders associated as bromodomain inhibitors. The present disclosure also provides preparation of compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent, or excipient.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: September 18, 2018
    Assignee: Orion Corporation
    Inventors: Susanta Samajdar, Chandrasekhar Abbineni, Sanjita Sasmal, Subramanya Hosahalli
  • Patent number: 10064935
    Abstract: The disclosure describes HCMV ribonucleic acid (RNA) vaccines, as well as methods of using the vaccines and compositions comprising the vaccines.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: September 4, 2018
    Assignee: ModernaTX, Inc.
    Inventors: Giuseppe Ciaramella, Shinu John, Kambiz Mousavi
  • Patent number: 10034477
    Abstract: This disclosure relates to pyrido-1,3-oxazine-2,4-diones of Formula I and their use as fungicides.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: July 31, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Brannon Sam, Kevin G. Meyer, Chenglin Yao, Brian A. Loy, Jared W. Rigoli, Nicholas R. Babij
  • Patent number: 10010530
    Abstract: The present disclosure relates to solid crystalline forms of N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (I) and the diastereomers thereof, and to methods for preparing such crystalline forms. Compound (I) and the diastereomers thereof are potent androgen receptor (AR) modulators useful as a medicament.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: July 3, 2018
    Assignee: Orlon Corporation
    Inventors: Olli Törmäkangas, Terhi Heikkinen
  • Patent number: 10000450
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: June 19, 2018
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Patent number: 10000481
    Abstract: The inventions relates to compounds of (I) and therapeutic uses thereof: (I) The terms Z, Y, and R1 are as defined in the claims.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: June 19, 2018
    Assignee: Vernalis (R&D) Limited
    Inventors: Stephen Stokes, Christopher John Graham, Stuart Christopher Ray, Emma Jayne Stefaniak
  • Patent number: RE48239
    Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: October 6, 2020
    Assignee: Genetech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young