Additional Hetero Ring Attached Directly Or Indirectly To The 1,4-diazine Ring By Nonionic Bonding Patents (Class 514/255.05)
  • Patent number: 11512097
    Abstract: The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5D”). The compounds have a general Formula I wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
    Type: Grant
    Filed: November 24, 2020
    Date of Patent: November 29, 2022
    Assignee: AMGEN INC.
    Inventors: Jennifer R. Allen, Michela Beltrani, Matthew P. Bourbeau, Teodora P. Damyanova, Iain Lingard, Ana E. Minatti, Paolo Vincetti
  • Patent number: 11498905
    Abstract: Disclosed herein are small molecule inhibitors of platelet function, and methods of using the small molecules to treat diseases, such as platelet hemostasis and thrombosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
    Type: Grant
    Filed: April 17, 2019
    Date of Patent: November 15, 2022
    Assignees: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Michael Holinstat, Reheman Adili, Andrew White, Theodore R. Holman
  • Patent number: 11479541
    Abstract: Provided is an acid addition salt of 3-(1H-indol-5-yl)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine selected from a tartrate salt, a phosphate salt, and a fumarate salt. Also provided are pharmaceutical compositions comprising an acid addition salt disclosed herein and a pharmaceutically acceptable excipient, and a method of treating a disease or disorder, such as disease or disorder associated with neuroinflammation, comprising administering to a subject in need thereof, a therapeutically effective amount of an acid addition salt disclosed herein or the pharmaceutical composition of the acid addition salt.
    Type: Grant
    Filed: January 31, 2022
    Date of Patent: October 25, 2022
    Assignee: Pioneura Corporation
    Inventors: Harris A. Gelbard, John M. McCall, Jesse Damsker, Arthur Romero
  • Patent number: 11447475
    Abstract: The present invention provides compounds of Formula (Ia) and (Ib): (Ia) or (Ib), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: September 20, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter Tai Wah Cheng, Yan Shi, Robert F. Kaltenbach, III, Ying Wang, Hao Zhang
  • Patent number: 11413284
    Abstract: The present disclosure relates to use of a protein kinase C (PKC) inhibitor in the treatment or prevention of proliferative diseases. The disclosure also relates to corresponding pharmaceutical formulations, uses, methods, combinations, and related disclosure embodiments. The disclosure further relates to use of a pharmaceutical combination comprising a PKC inhibitor and another therapeutic agent, such as an MDM2 inhibitor, in the treatment or prevention of a proliferative disease.
    Type: Grant
    Filed: September 11, 2018
    Date of Patent: August 16, 2022
    Assignee: Novartis AG
    Inventors: Vesselina Cooke, Michael Scott Visser, Andrew Wylie, Padmaja Yerramilli-Rao, Xu Zhu
  • Patent number: 11365187
    Abstract: Compounds of formula (I), as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, molluse and nematode pests.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: June 21, 2022
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Denis Gribkov, Myriem El Qacemi, André Stoller, André Jeanguenat, Aurelien Bigot
  • Patent number: 11332448
    Abstract: The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.
    Type: Grant
    Filed: September 25, 2020
    Date of Patent: May 17, 2022
    Assignee: Bayer Cropscience AG
    Inventors: Eike Kevin Heilmann, Joerg Greul, Axel Trautwein, Hans-Georg Schwarz, Isabelle Adelt, Roland Andree, Peter Luemmen, Maike Hink, Martin Adamczewski, Mark Drewes, Angela Becker, Arnd Voerste, Ulrich Goergens, Kerstin Ilg, Johannes-Rudolf Jansen, Daniela Portz
  • Patent number: 11311535
    Abstract: Compositions and methods related to the amelioration of pancreatitis through the pharmaceutical manipulation of calcium signaling are disclosed. Such compositions and methods may be used to ameliorate symptoms of acute or chronic pancreatitis or to reduce the chance or severity of pancreatitis in an individual at risk of the condition. In other embodiments, disclosed herein are compositions and methods related to the amelioration of viral diseases through the pharmaceutical manipulation of calcium signaling. In further embodiments, disclosed herein are compositions and methods related to the amelioration of Th17-induced diseases through the pharmaceutical manipulation of calcium signaling.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: April 26, 2022
    Assignee: CALCIMEDICA, INC.
    Inventors: Gonul Velicelebi, Kenneth Stauderman, Michael Dunn, Jack Roos
  • Patent number: 11214570
    Abstract: Provided is a novel pyrrolopyridine compound represented by Chemical Formula I, a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and to a method for preparing the same. A compound represented by Chemical Formula I shows high selectivity and antiviral activity against human immunodeficiency virus (HIV), with low toxicity; therefore, it is useful as a therapeutic agent for viral infection, in particular, HIV infection.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: January 4, 2022
    Assignee: ST PHARM CO., LTD.
    Inventors: Bong Jin Kim, Ill Young Lee, Jae Hak Kim, Hong Suk Shin, Jong Chan Son, Chong-Kyo Lee, Kyungjin Kim, Uk-Il Kim, Hwa Jung Nam
  • Patent number: 11198691
    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, A, B, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: February 28, 2020
    Date of Patent: December 14, 2021
    Assignee: KalVista Pharmaceuticals Limited
    Inventors: Rebecca Louise Davie, Hannah Joy Edwards, David Michael Evans, Simon Teanby Hodgson
  • Patent number: 11179367
    Abstract: A pharmaceutical composition comprising Compound I: Methods of treating cystic fibrosis comprising administering one or more of such pharmaceutical compositions to a patient.
    Type: Grant
    Filed: February 4, 2019
    Date of Patent: November 23, 2021
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Cathy Chu, Varsha Dhamankar, Eleni Dokou, Eric L. Haseltine, Samuel Moskowitz, Sarah Robertson, David Waltz, Weichao George Chen
  • Patent number: 11160799
    Abstract: An aqueous composition for intranasal administration by spray including a mixture of (a) sufentanil, a salt and/or analogs thereof and (b) ketamine, a salt and analogs thereof in solution. Also, an aqueous composition for intranasal administration by spray including (a) sufentanil, a salt and/or analogs thereof in solution and an aqueous composition for intranasal administration by spray including (b) ketamine, a salt and/or analogs thereof in solution, for use in a method for the treatment or prevention of pain in a child. The composition is useful for treating or preventing pain in a child of 17 years or younger. The composition is delivered from a nasal spray device to treat or prevent the pain such as procedural pain in a child.
    Type: Grant
    Filed: September 11, 2020
    Date of Patent: November 2, 2021
    Assignee: Cessatech A/S
    Inventors: Steen Henneberg, Bettina Nygaard Nielsen
  • Patent number: 11142516
    Abstract: Provided herein is a novel process for the preparation of an amino-pyrimidine and salts thereof. Also provided herein are novel intermediates used in this process and their preparation.
    Type: Grant
    Filed: December 26, 2018
    Date of Patent: October 12, 2021
    Assignee: Cytokinetics, Inc.
    Inventors: Matthew Peterson, Kevin Lu, Bradley Morgan, David Morgans, Tohru Fukuyama
  • Patent number: 11001578
    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, A, B, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: June 11, 2019
    Date of Patent: May 11, 2021
    Assignee: KALVISTA PHARMACEUTICALS LIMITED
    Inventors: Rebecca Louise Davie, Hannah Joy Edwards, David Michael Evans, Simon Teanby Hodgson
  • Patent number: 10968209
    Abstract: The present invention relates to a novel compound useful as a TRPV4 antagonist, specifically the compound 1-(((5S,7R)-3-(5-cyclopropylpyrazin-2-yl)-7-hydroxy-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl)methyl)-1H-benzo[d]imidazole-6-carbonitrile, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compound.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: April 6, 2021
    Inventors: Patrick Stoy, Carl A. Brooks, Guosen Ye
  • Patent number: 10961215
    Abstract: In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-? receptor (LXR?) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
    Type: Grant
    Filed: October 9, 2017
    Date of Patent: March 30, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael T. Rudd, Zhaoyang Meng, Jenny Wai, David Jonathan Bennett, Edward J. Brnardic, Nigel J. Liverton, Shawn J. Stachel, Yongxin Han, Paul Tempest, Jiuxiang Zhu, Xuewang Xu
  • Patent number: 10933068
    Abstract: Disclosed herein are methods and compositions for the treatment of facioscapulohumeral muscular dystrophy and other muscle diseases or disorders. In some cases, the methods and compositions involve the use of methyltransferase inhibitors to inhibit or repress DUX4 expression in muscle cells. Further disclosed herein are methods and cell based assays for screening compounds for the treatment of facioscapulohumeral muscular dystrophy and other muscle diseases.
    Type: Grant
    Filed: May 26, 2017
    Date of Patent: March 2, 2021
    Assignee: Sonic Master Limited
    Inventors: Amanda Rickard, Anabel De La Garza, Uli Schmidt, Alexander Kiselyov
  • Patent number: 10793580
    Abstract: The present invention relates to novel pyrazoloazepin-8-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: October 6, 2020
    Assignee: LEO Pharma A/S
    Inventors: Xifu Liang, Jens Larsen
  • Patent number: 10765672
    Abstract: The present disclosure relates to pharmaceutical formulations of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid and methods of use thereof.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: September 8, 2020
    Assignee: FibroGen, Inc.
    Inventors: David Conca, Lee Allen Flippin, Scott David Leigh, Claudia Witschi, Lee Robert Wright
  • Patent number: 10736894
    Abstract: Methods of treating developmental syndromes with a PDE10A inhibitor are provided.
    Type: Grant
    Filed: February 15, 2019
    Date of Patent: August 11, 2020
    Assignee: Ovid Therapeutics Inc.
    Inventor: Matthew During
  • Patent number: 10722505
    Abstract: The present invention relates to novel 2-primary amino-4-secondary amino-quinoline derivatives, their manufacture, pharmaceutical compositions comprising them and their use as medicaments. The active compounds of the present invention are useful for the treatment and prevention of proliferative neoplastic and non-neoplastic diseases.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: July 28, 2020
    Assignee: GENOSCIENCE PHARMA
    Inventors: Firas Bassissi, Antoine Beret, Sonia Brun, Jérôme Courcambeck, Clarisse Dubray, Gregory Nicolas, Philippe Halfon
  • Patent number: 10717736
    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 inhibitors 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 ?v-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: July 21, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guohua Zhao, James Mignone
  • Patent number: 10703749
    Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
    Type: Grant
    Filed: November 20, 2018
    Date of Patent: July 7, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Christa C. Chrovian, Heather R. Coate, Meri De angelis, Curt A. Dvorak, Christine F. Gelin, Michael A. Letavic, Brad M. Savall, Akinola Soyode-Johnson, Brice M. Stenne, Devin M. Swanson
  • Patent number: 10647661
    Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: May 12, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Nadia Ahmad, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Joanne Louise Camp, Lev Tyler Dewey Fanning, Sara Sabina Hadida Ruah, Dennis Hurley, Yvonne Schmidt, David Shaw, Urvi Patel, Stephen Andrew Thomson, Lidio Marx Carvalho Meireles
  • Patent number: 10640492
    Abstract: Provided are a new tubulin inhibitor and applications thereof, the tubulin inhibitor being a series of compounds based on substituted heterocyclic skeletons, targeting the colchicine binding sites of tubulin. The structure is: Formula (I), wherein: formula (A), n independently expresses an integer between 0 and 5, the condition being that n?5, A represents mono- or poly-substituted groups, the groups being selected from the group consisting of H, C1-C20 amide group, C1-C20 acyloxy group, C1-C20 alkanoyl group, C1-C20 alkoxycarbonyl group, C1-C20 alkoxy group, C1-C20 alkylamino group, C1-C20 alkylcarboxyamino group, aroyl group, aralkanoyl group, carboxyl group, cyano group, halogen group, hydroxyl group, nitro group and methylthienyl group.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: May 5, 2020
    Assignee: SHENZHEN NEPTUNUS PHARMACEUTICAL RESEARCH INSTITUTE CO., LTD.
    Inventors: Tian Tang, Yanqing Wang, Xiaorou Liu, Jin Wang, Ruyi Jin, Hanlin Feng
  • Patent number: 10590090
    Abstract: The present disclosure is directed to inhibitors of SHP2, such as pyrazine compounds, and their use in the treatment of disease associated with SHP2 modulation, such as Noonan Syndrome, Leopard Syndrome, juvenile myelomonocytic leukemias, neuroblastoma, melanoma, acute myeloid leukemia and cancers of the breast, lung and colon. Also disclosed are pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: March 17, 2020
    Assignee: REVOLUTION MEDICINES, INC.
    Inventors: Elena S. Koltun, Kevin Mellem, Adrian Gill, Gert Kiss, Christopher Semko, Naing Aay, Andreas Buckl, Ashutosh Jogalekar, Walter Won
  • Patent number: 10577365
    Abstract: The present invention relates to the compound of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof. The present invention is further concerned with the use of such a compound or salt, stereoisomer, tautomer or N-oxide thereof as medicament and a pharmaceutical composition comprising said compound.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: March 3, 2020
    Assignees: Felicitex Therapeutics, Inc., Selvita S.A.
    Inventors: Agnieszka Dreas, Charles-Henry Fabritius, Andrzej Dzienia, Anna Buda, Michal Galezowski, Georgiy Kachkovskyi, Urszula Kulesza, Katarzyna Kucwaj-Brysz, Agnieszka Szamborska-Gbur, Wojciech Czardybon, Maria Vilenchik, Michael Frid, Alexandra Kuznetsova
  • Patent number: 10561652
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.
    Type: Grant
    Filed: April 4, 2019
    Date of Patent: February 18, 2020
    Assignee: NEUPHARMA, INC.
    Inventors: Yong-Liang Zhu, Xiangping Qian
  • Patent number: 10550127
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: February 2, 2018
    Date of Patent: February 4, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Holger Wagner, Stefan Peters
  • Patent number: 10478435
    Abstract: Described herein are methods of treatment of stroke and traumatic brain injury comprising administration of a CRAC channel inhibitor.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: November 19, 2019
    Assignees: CALCIMEDICA, INC., THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
    Inventors: Kenneth Stauderman, Michael Dunn, Sudarshan Hebbar, Midori Yenari, Rachid Kacimi
  • Patent number: 10472347
    Abstract: Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein “R1”, “RA-1”, “R2”, “R3”, and “Het” are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: November 12, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rongze Kuang, Pauline Ting, Amjad Ali, Heping Wu, Michael Berlin, Andrew Stamford, Hongwu Wang, Gang Zhou, David Kim, Qiaolin Deng, Yeon-Hee Lim, Younong Yu
  • Patent number: 10456385
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Grant
    Filed: May 23, 2018
    Date of Patent: October 29, 2019
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Eun Jung Yi
  • Patent number: 10450297
    Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: April 5, 2018
    Date of Patent: October 22, 2019
    Assignee: Pfizer, Inc.
    Inventors: Michael J. Luzzio, Kevin D. Freeman-Cook, Samit K. Bhattacharya, Matthew M. Hayward, Catherine A. Hulford, Christopher L. Autry, Xumiao Zhao, Jun Xiao, Kendra L. Nelson
  • Patent number: 10420766
    Abstract: Described herein are methods of treatment of stroke and traumatic brain injury comprising administration of a CRAC channel inhibitor.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: September 24, 2019
    Assignees: CALCIMEDICA, INC., THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
    Inventors: Kenneth Stauderman, Michael Dunn, Sudarshan Hebbar, Midori Yenari, Rachid Kacimi
  • Patent number: 10351540
    Abstract: Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.
    Type: Grant
    Filed: January 17, 2018
    Date of Patent: July 16, 2019
    Assignee: SABILA BIOSCIENCES LLC
    Inventor: Tarek Suhayl Mansour
  • Patent number: 10308645
    Abstract: The present invention is directed to piperidine oxadiazole and thiadiazole orexin compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: September 27, 2015
    Date of Patent: June 4, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel Liverton, Scott D. Kuduk, Yunfu Luo, Na Meng, Tingting Yu
  • Patent number: 10272030
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: April 30, 2019
    Assignee: Cytokinetics, Inc.
    Inventors: Zhe Yang, Alex R. Muci, Jeffrey Warrington, Gustave Bergnes, Bradley P. Morgan, Chihyuan Chuang, Antonio Romero, Scott Collibee, Xiangping Qian, Pu-Ping Lu
  • Patent number: 10239857
    Abstract: Provided herein are processes for the preparation of 2-thiophenecarbonyl chloride, which is useful, for example, in the preparation of 3,5-disubstituted-1,2,4-oxadiazoles, such as tioxazafen (3-phenyl-5-(2-thienyl)-1,2,4-oxadiazole).
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: March 26, 2019
    Assignee: Monsanto Technology LLC
    Inventors: Daniel P. Walker, William H. Miller
  • Patent number: 10208064
    Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: July 9, 2015
    Date of Patent: February 19, 2019
    Inventors: Alexander Pasternak, Ian Davies, Fa-Xiang Ding, Jinlong Jiang, Shuzhi Dong, Xin Gu, Takao Suzuki, Joseph P. Vacca, Zhifa Pu, Shouning Xu
  • Patent number: 10201584
    Abstract: This disclosure is directed to pharmaceutical compositions that comprise two or more therapeutic agents that, inter alia, are useful for inhibiting hepatitis C virus (HCV) and methods for inhibiting HCV by co-administering two or more anti-HCV therapeutic agents.
    Type: Grant
    Filed: April 8, 2014
    Date of Patent: February 12, 2019
    Assignee: ABBVIE INC.
    Inventors: Christine A. Collins, Daniel E. Cohen, Gennadiy Koev, Preethi Krishnan, Tami J. Pilot-Matias
  • Patent number: 10179125
    Abstract: The disclosure relates to substituted pyridines, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: January 15, 2019
    Assignee: Zenith Epigenetics Ltd.
    Inventors: May Xiaowu Jiang, Bruce Francis Molino, Shuang Liu, Ruifang Wang, Bryan Cordell Duffy, John Frederick Quinn, Gregory Steven Wagner
  • Patent number: 10150765
    Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: December 11, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Christa C. Chrovian, Heather R. Coate, Meri De Angelis, Curt A. Dvorak, Christine F. Gelin, Michael A. Letavic, Brad M. Savall, Akinola Soyode-Johnson, Brice M. Stenne, Devin M. Swanson
  • Patent number: 10138241
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: November 27, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pingrong Liu, Craig Andrew Miller, Maolin Yu, Zhonghua Zhang, Sabine Ruppel, Anil K. Padyana
  • Patent number: 10137125
    Abstract: Benzenesulfonamide derivatives of quinoxaline that are kinase inhibitors, pharmaceutical compositions and methods of using these derivatives, e.g., for treatment of cancer are described.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: November 27, 2018
    Assignee: NEUPHARMA, INC.
    Inventors: Yong-Liang Zhu, Xiangping Qian
  • Patent number: 10138222
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1—, R2—, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: November 27, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jianwen Cui, Donghong Amy Gao, Pingrong Liu, Bryan Patrick McKibben, Craig Andrew Miller, Hossein Razavi, Elizabeth Spencer, Sabine Ruppel, Anil K. Padyana
  • Patent number: 10100035
    Abstract: The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them.
    Type: Grant
    Filed: September 20, 2017
    Date of Patent: October 16, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Diego Broggini, Matteo Conza, Oliver Flögel, Stefan Horns, Susanne Lochner, Guangrong Tang, Zhaobin Wang, Lucie Lovelle
  • Patent number: 10058540
    Abstract: The present invention is directed to compounds of Formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of A? deposits is beneficial such as Alzheimer's disease.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: August 28, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Karsten Juhl, Lena Tagmose, Mauro Marigo
  • Patent number: 10053451
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: August 21, 2018
    Assignee: Genentech, Inc.
    Inventors: Sharada Labadie, Jun Liang, Daniel Fred Ortwine, Xiaojing Wang, Birong Zhang, Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Andiliy G. Lai, Johnny Y. Nagasawa, Simon Charles Goodacre, Nicholas Charles Ray
  • Patent number: 10016417
    Abstract: Extended release formulations of 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide (DPOC-4088) that provide for better control of blood plasma levels. The extended release formulations maintain substantially constant plasma levels of the active ingredient for at least about 16 hours and provide for once-daily dosing.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: July 10, 2018
    Assignee: Diakron Pharmaceuticals, Inc.
    Inventors: Sankar Ramakrishnan, Elumalal Venkatesan, Jayanthi Suryakumar, Stephane Allard
  • Patent number: 10011596
    Abstract: The present invention provides compounds of Formula I for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula I.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: July 3, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Karsten Juhl, Lena Tagmose, Mauro Marigo