1,3-diazines (e.g., Pyrimidines, Etc.) Patents (Class 514/256)
  • Patent number: 11053221
    Abstract: Compounds having activity as chemotherapeutic agents are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1a, R1b, R1c, R1d, L, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods for treating cancer (e.g., hematological cancers) are also provided.
    Type: Grant
    Filed: October 25, 2019
    Date of Patent: July 6, 2021
    Assignee: ARRIEN PHARMACEUTICALS LLC
    Inventor: Hariprasad Vankayalapati
  • Patent number: 11053235
    Abstract: The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
    Type: Grant
    Filed: August 9, 2019
    Date of Patent: July 6, 2021
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: Gang Deng, Yimin Jiang, Qian Liu, Chao Liang, Zhao-Kui Wan, Wing Shun Cheung, Zhanling Cheng, Yanping Xu
  • Patent number: 11046680
    Abstract: Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: June 29, 2021
    Assignee: AMGEN INC.
    Inventors: Ning Chen, Xiaoqi Chen, Yinhong Chen, Alan C. Cheng, Richard V. Connors, Jeffrey Deignan, Paul John Dransfield, Xiaohui Du, Zice Fu, James S. Harvey, Julie Anne Heath, Lars V. Heumann, Daniel B. Horne, Jonathan Houze, Matthew R. Kaller, Frank Kayser, Aarif Yusuf Khakoo, David J. Kopecky, Su-Jen Lai, Zhihua Ma, Julio C. Medina, Jeffrey T. Mihalic, Nobuko Nishimura, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Malgorzata Wanska, Kevin Yang, Wen-Chen Yeh
  • Patent number: 11034678
    Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Grant
    Filed: February 18, 2020
    Date of Patent: June 15, 2021
    Assignee: Pfizer Inc.
    Inventors: Markus Boehm, Shawn Cabral, Matthew S. Dowling, Kentaro Futatsugi, Kim Huard, Esther Cheng Yin Lee, Allyn T. Londregan, Jana Polivkova, David A. Price, Qifang Li
  • Patent number: 11008339
    Abstract: Disclosed are substituted pyrazole compounds containing pyrimidinyl as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a good spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, rice blast, cucumber anthracnosis and the like. The compounds of present invention also show good insecticidal activity.
    Type: Grant
    Filed: May 17, 2016
    Date of Patent: May 18, 2021
    Assignee: Shenyang Sinochem Agrochemicals R&D Co., Ltd.
    Inventors: Changling Liu, Aiying Guan, Junfeng Wang, Xufeng Sun, Zhinian Li, Jinbo Zhang, Lanfeng Ban, Sen Ma, Jie Lan, Xiaoli Xia, Jinlong Yang
  • Patent number: 10968172
    Abstract: The application relates to phenyl- or naphthylsulfonamide derivatives of the structural formula (I). The compounds are described as inhibitors of USP30 (ubiquitin specific peptidase 30) useful for the treatment of conditions involving mitochondrial defects including neurodegenerative diseases such as Alzheimer's and Parkinson's or a neoplastic disease such as leukemia.
    Type: Grant
    Filed: May 14, 2018
    Date of Patent: April 6, 2021
    Assignee: Mitobridge, Inc.
    Inventors: Arthur Kluge, Bharat Lagu, Pranab Maiti, Sunil Kumar Panigrahi
  • Patent number: 10954221
    Abstract: The present disclosure provides compounds of Formula (I) and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease.
    Type: Grant
    Filed: June 16, 2020
    Date of Patent: March 23, 2021
    Assignee: QILU REGOR THERAPEUTICS INC.
    Inventors: Wenge Zhong, Wei Guo
  • Patent number: 10946019
    Abstract: The invention provides a series of substituted aryl pyrimidine compounds and the use of these compounds as therapeutics to treat or prevent neurodegenerative disorders, including Parkinson's disease. Compounds of the invention are also able to treat the symptoms of such diseases and therefore represent a new treatment modality for ameliorating chronic and acute conditions. The compounds of the invention are capable of selectively potentiating the activity of the Nurr1:RXR? heterodimer, and are able to treat diseases or conditions associated with aberrant Nurr1:RXR? function. The invention further provides methods for treating neurodegenerative disorders by administration of Nurr1:RXR? activating agents.
    Type: Grant
    Filed: October 20, 2016
    Date of Patent: March 16, 2021
    Inventor: Demetrios K. Vassilatis
  • Patent number: 10940144
    Abstract: The present invention aims to find a novel pharmaceutical use of omidenepag, esters thereof, or salts thereof. The present inventors have made intensive studies to find a novel pharmaceutical use of omidenepag, an ester thereof, or a salt thereof, and have found as a result that omidenepag, an ester thereof, or a salt thereof significantly dilates retinal blood vessels, and significantly increases blood flow. Therefore, omidenepag, an ester thereof, or a salt thereof is expected to protect retinal nerve cells and be useful for prevention and/or treatment of ophthalmic diseases involving retinal nerve cell disorder.
    Type: Grant
    Filed: September 27, 2018
    Date of Patent: March 9, 2021
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Takazumi Taniguchi, Takahiro Akaishi, Hitoshi Nakazawa
  • Patent number: 10933064
    Abstract: This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: March 2, 2021
    Assignees: Novartis AG, Palobiofarma S.L.
    Inventors: Kai Cui, Julio Cesar Castro-Palomino Laria, Weiyong Kong
  • Patent number: 10934284
    Abstract: Amine compounds having activity against inflammation, fungi, unicellular parasitic microorganisms, and cancer are described. The compounds contain a monocyclic, bicyclic, or tricyclic aromatic ring having one, two, or three ring nitrogen atoms.
    Type: Grant
    Filed: February 26, 2019
    Date of Patent: March 2, 2021
    Assignee: Wellstat Therapeutics Corporation
    Inventors: David M. Simpson, Dennis Bryan Zerby, Ming Lu, Reid W. Von Borstel, Rui Li, Julian Reading, Stephen Wolpe
  • Patent number: 10927136
    Abstract: The present patent application discloses the compounds according to Formula (I) shown below, or pharmaceutically acceptable salts thereof wherein JB, n, R1, R2, R3, R4, R5, m and X as defined herein.
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: February 23, 2021
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: James Edward Sheppeck, Paul Allan Renhowe, Ara Mermerian, Timothy Claude Barden, Glen Robert Rennie, Rajesh R. Iyengar, Takashi Nakai
  • Patent number: 10912763
    Abstract: A pharmaceutical dosage form for administration twice daily, once daily or less frequently, which contains 6?-fluoro-(N-methyl- or N,N-dimethyl)-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine or a physiologically acceptable salt thereof.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: February 9, 2021
    Assignee: Grünenthal GmbH
    Inventors: Nadja Gruening, Marc Schiller, Ashish Hemani, Chris Kirby, Ingo Friedrich, John Bothmer, Andreas Scholz
  • Patent number: 10912774
    Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.
    Type: Grant
    Filed: December 17, 2019
    Date of Patent: February 9, 2021
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Dominic Reynolds, Ming-Hong Hao, John Wang, Sudeep Prajapati, Takashi Satoh, Anand Selvaraj
  • Patent number: 10874673
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: December 29, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Patent number: 10800775
    Abstract: The present invention relates to new pyrrolopyridine compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK1 and JAK3 kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: October 13, 2020
    Assignee: ACLARIS THERAPEUTICS, INC.
    Inventors: David Randolph Anderson, Susan Landis Hockerman, James Robert Blinn, Eric Jon Jacobsen
  • Patent number: 10787430
    Abstract: Described herein are compounds, including pharmaceutically acceptable salts thereof, methods of making such compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat, prevent or diagnose blood-based diseases, disorders or conditions.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: September 29, 2020
    Assignee: FRONTHERA U.S. PHARMACEUTICALS LLC
    Inventors: Bohan Jin, Qing Dong, Gene Hung
  • Patent number: 10780091
    Abstract: The present invention relates to a maleate salt of a compound represented by formula I, a method for preparing the salt, a pharmaceutical composition containing the salt, and the use of the salt. The present invention also relates to crystalline forms C, D and E of the maleate salt of the compound represented by formula I, methods for preparing the crystalline forms, crystalline compositions and pharmaceutical compositions containing the crystalline forms, and uses thereof.
    Type: Grant
    Filed: February 4, 2017
    Date of Patent: September 22, 2020
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Zhaozhong Ding, Fei Sun, Yinghu Hu, Yilong Zhou, Zheng Wang, Ling Yang
  • Patent number: 10774070
    Abstract: Described herein are compounds, such as compounds of Formula (I) and pharmaceutically acceptable salts thereof, that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions, e.g.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: September 15, 2020
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Natasja Brooijmans, Lucian V. DiPietro, Paul E. Fleming, Joseph L. Kim, Steven Mark Wenglowsky, Yulian Zhang
  • Patent number: 10759782
    Abstract: Disclosed are an EGFR inhibitor free base or acid salt polycrystalline form, a preparation method therefor, and an application thereof. The present invention specifically relates to an N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide free base or acid salt polycrystalline form, a preparation method therefor, and an application of the polycrystalline form in preparing a drug for treating an EGFR mutant activity-mediated disease. The present invention is used for inhibiting the activity of an L858R EGFR mutant, a T790M EGFR mutant and an exon 19 deletion activating mutant etc., may be widely applied in preventing and treating cancer, especially non-small cell lung cancer and other related diseases, and is expected to develop into a new generation of EGFR inhibitors.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: September 1, 2020
    Assignees: Jiangsu Hansoh Pharmaceutical Group Co., Ltd., Shanhgai Hansoh Biomecial Co., Ltd.
    Inventors: Zhongke Chen, Fuping Liu, Lei Liu, Rudi Bao
  • Patent number: 10752596
    Abstract: The invention provides a compound having a GLUT9 inhibitory activity. The compound is of Formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 3, 2018
    Date of Patent: August 25, 2020
    Assignee: JAPAN TOBACCO INC.
    Inventors: Hironobu Nagamori, Tatsuya Nishimaru, Masaki Takagi, Ikuo Mitani, Yuichi Nakagawa
  • Patent number: 10744138
    Abstract: A hair growth formulation includes minoxidil and foeniculum vulgare, atriplex nummularia extract, or a combination of foeniculum vulgare and atriplex nummularia extract. A method for increasing hair growth includes applying a hair growth formulation to a subject.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: August 18, 2020
    Assignee: GARUHDA LLC
    Inventor: David Ben Kunin
  • Patent number: 10736896
    Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: May 16, 2018
    Date of Patent: August 11, 2020
    Assignee: ADVERIO PHARMA GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
  • Patent number: 10716788
    Abstract: The present invention provides methods of treating MS using pyrimidine and pyridine compounds which are inhibitors of Bruton's tyrosine kinase (BTK).
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: July 21, 2020
    Assignee: Merck Patent GmbH
    Inventor: Tammy Dellovade
  • Patent number: 10709707
    Abstract: Described herein are methods and pharmaceutical formulations for treating ocular conditions.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: July 14, 2020
    Assignee: Oyster Point Pharma, Inc.
    Inventors: Douglas Michael Ackermann, James Loudin, Kenneth J. Mandell
  • Patent number: 10702524
    Abstract: The present invention falls within the field of medical technology, and in particular relates to the use of a compound as shown in formula (I). In particular, the present invention relates to the use of the compound as shown in formula (I) in the preparation of a pharmaceutical composition for preventing and/or treating a nerve injury, or relieving a nerve injury-associated symptom, and further relates to the use thereof in the preparation of a healthcare product for protecting an injured nerve and/or improving motor function. After a nerve injury has occurred, the compound can reduce the production of pro-inflammatory cytokine, decrease the level of apoptosis, promote the survival of neuron, inhibit the formation of glial scar, and has a significant effect in promoting the recovery of motor function.
    Type: Grant
    Filed: October 10, 2017
    Date of Patent: July 7, 2020
    Inventors: Shiqing Feng, Xue Yao
  • Patent number: 10702525
    Abstract: The pyrimidine derivatives as anti-diabetic agents are chloropyrimidinyl derivatives having the general formula of compound 81, wherein R1 is —N(CH3)CH2CH2OH (compound 81c) or —N(H)CH2CH2OH (compound 81f) or the general formula of compound 82, wherein R2 is —N(CH3)CH2CH2OH (compound 82c) or —N(CH2CH2)2O (compound 82d), as follows: The derivatives may be used for treating diabetes in humans or animals and have demonstrated efficacy, specifically in treating type 2 diabetes. Two methods of synthesizing the pyrimidine derivatives are described herein. The method using microwaves (Method B) is a green method that can provide high yields in a short time and with high purity. The compounds act as GLP-1 receptor agonists and are more potent than conventional drugs. As such, the compounds may be used in lower doses, and, hence, have fewer side effects.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: July 7, 2020
    Assignee: United Arab Emirates University
    Inventors: Abdu Adem, Shaikha S. Al Neyadi, Ibrahim M. Abdu, Alaa A. Salem, Naheed Amir
  • Patent number: 10702589
    Abstract: The present disclosure provides the use of Akr1b8, an agonist of Akr1b8, Akr1B10, or an agonist of Akr1B10 in methods and compositions for the treatment of neurological disorders and stress-induced conditions. Methods of increasing the levels of 5Thr3a on neuronal cells is also provided by contacting the neuronal cells with Akr1b8, an agonist of Akr1b8, Akr1B10, or an agonist of Akr1B10.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: July 7, 2020
    Assignee: ANN AND ROBERT H. LURIE CHILDREN'S HOSPITAL OF CHICAGO
    Inventor: Jhumku D. Kohtz
  • Patent number: 10696666
    Abstract: A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.
    Type: Grant
    Filed: October 18, 2017
    Date of Patent: June 30, 2020
    Assignee: CELLCENTRIC LIMITED
    Inventors: Neil Anthony Pegg, Stuart Thomas Onions, David Michel Adrien Taddei, Jonathan Shannon, Silvia Paoletta, Richard James Brown, Don Smyth, Gareth Harbottle
  • Patent number: 10662188
    Abstract: This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: May 26, 2020
    Assignee: ADVERIO PHARMA GmbH
    Inventors: Birgit Keil, Franz-Josef Mais, Winfried Joentgen, Alfons Grunenberg
  • Patent number: 10654861
    Abstract: A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: May 19, 2020
    Assignee: UCB Biopharma SRL
    Inventors: Michael Louis Robert Deligny, Jag Paul Heer, Jean Keyaerts, Luce Elsa Lepissier, Martin Alexander Lowe
  • Patent number: 10646429
    Abstract: The present disclosure relates to methods of retarding hair loss or facilitating hair growth and/or regrowth. More specifically, the present disclosure relates to methods of using the disclosed compositions to increase the rate of terminal hair growth and/or regrowth in a mammal.
    Type: Grant
    Filed: July 31, 2018
    Date of Patent: May 12, 2020
    Assignee: Johnson & Johnson Consumer Inc.
    Inventors: Longsheng Hu, Virginia Streusand Goldman, Josephine A. Minerva, Susan Wendling
  • Patent number: 10633356
    Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: February 19, 2019
    Date of Patent: April 28, 2020
    Assignee: ADVERIO PHARMA GMBH
    Inventors: Peter Fey, Alfons Grunenberg, Donald Bierer
  • Patent number: 10610518
    Abstract: Described herein are methods and compositions for the treatment of ocular conditions and for the improvement of vision parameters using pharmaceutically acceptable ophthalmic pilocarpine formulations. A nonlimiting example of an ocular condition that may be treated with the methods and compositions disclosed herein is presbyopia.
    Type: Grant
    Filed: April 24, 2019
    Date of Patent: April 7, 2020
    Assignee: ALLERGAN, INC.
    Inventors: Michael R. Robinson, Mohammed Dibas, Jaya Giyanani, Anuradha Gore, Sungwook Lee, Haixia Liu, Aileen Morgan, Jihao Zhou
  • Patent number: 10603294
    Abstract: The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.
    Type: Grant
    Filed: January 15, 2019
    Date of Patent: March 31, 2020
    Assignee: Innovation Pharmaceuticals Inc.
    Inventors: Richard W. Scott, Bozena Korczak
  • Patent number: 10603313
    Abstract: Disclosed herein are compounds, of the class of amine-bearing heterocycles, which act as positive allosteric modulators and silent allosteric modulators of the mu opioid receptor. These compounds are useful for the treatment of pain, drug addiction, and other CNS derived maladies that are controlled directly or indirectly by activation of the mu opioid receptor. Methods for making and using the allosteric modulators disclosed herein are also provided.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: March 31, 2020
    Assignee: CHIROMICS, LLC
    Inventors: Joel Francis Austin, Michael David VanHeyst, James S. Harvey, Elizabeth Gerig Rowley, Christophe Lamarque-Lacoste
  • Patent number: 10568885
    Abstract: The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, pharmaceutical compositions containing the same, processes for preparing the same, and methods of medical treatment using the same.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: February 25, 2020
    Assignee: Centrexion Therapeutics Corporation
    Inventors: Markus Ostermeier, Ulrike Werthmann
  • Patent number: 10556897
    Abstract: The present invention is directed to novel protein kinase inhibitors comprising the chemical compound N-(2-chloro-6-methylphenyl)-2-[[2-methyl-6-(3-hydroxypyrrolidin-1-yl)pyrimidin-4-yl]amino]thiazole-5-carboxamide, its pharmaceutically acceptable salts, enantiomers, and enantiomeric mixtures, and methods of use to treat protein kinase-mediated diseases or conditions.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: February 11, 2020
    Assignee: Princeton Drug Discovery, Inc
    Inventor: Kan He
  • Patent number: 10556890
    Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: February 11, 2020
    Assignees: Sunovion Pharmaceuticals Inc., PGI DRUG DISCOVERY LLC
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Patent number: 10543215
    Abstract: Disclosed herein are combination therapies for the treatment of heart failure using a cardiac myosin activator, such as omecamtiv mecarbil, and a sinus node If current inhibitor, such as ivabradine. Also disclosed herein are compositions comprising a cardiac myosin activator and a sinus node If current inhibitor.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: January 28, 2020
    Assignee: AMGEN INC.
    Inventors: Robert Andrew Donald Scott, Scott Wasserman
  • Patent number: 10538527
    Abstract: The present invention provides a compound of Formula II, and salts thereof, and a pharmaceutical composition comprising a compound of Formula II: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, and wherein R3 is hydrogen, an alkyl group having from one to ten carbon atoms, or a halogen. Preferably the compound of Formula II includes wherein R3 is a halogen, and most preferably wherein the halogen is chlorine. Methods of treating a patient with cancer with these compounds are also provided.
    Type: Grant
    Filed: February 4, 2019
    Date of Patent: January 21, 2020
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10537571
    Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: January 21, 2020
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Dominic Reynolds, Ming-Hong Hao, John Wang, Sudeep Prajapati, Takashi Satoh, Anand Selvaraj
  • Patent number: 10517873
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide.
    Type: Grant
    Filed: February 4, 2019
    Date of Patent: December 31, 2019
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Marie Georges Beauchamps, Antonio Christian Ferretti, Robert Hilgraf, Mohit Atul Kothare, Hon-Wah Man, Mark A. Nagy, Kelvin Hin-Yeong Yong, Nanfei Zou
  • Patent number: 10508105
    Abstract: Indazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease states associated with glutamate dysfunction.
    Type: Grant
    Filed: August 16, 2018
    Date of Patent: December 17, 2019
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Andrew S. Felts, Colleen M. Niswender, Rory A. Capstick, Paul K. Spearing, Sean R. Bollinger
  • Patent number: 10508104
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: December 17, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: George O. Tora, Heather Finlay, Wen Jiang, Wei Meng, Xiaojun Zhang
  • Patent number: 10494346
    Abstract: The present invention relates to a novel pyrimidine-4-carboxylic acid derivative having an anticancer activity, and the compound thereof is useful as a drug for treating and preventing tumor diseases, wherein the compound is represented by the Formula 1: or a pharmaceutically acceptable salt thereof, wherein: Q is a C6-C15 aryl group; or a C4-C13 heteroaryl group, wherein the heteroaryl contains 1, 2 or 3 heteroatoms substituted with 1-3 heteroatom(s) selected from the group consisting of nitrogen, oxygen or sulfur; R is a halogen; a C1-C10 haloalkyl substituted with 1-13 halogen atom(s); a C1-C10 alkoxy; a 5- or 6-membered heterocycloalkyl or (CH2)r-R1 wherein the heterocycloalkyl contains 1-2 heteroatom(s) selected from the group consisting of nitrogen and oxygen; R1 is a hydrogen; a C1-C10 alkoxy; amino; mono(C1-C10 alkyl)amino; di(C1-C10 alkyl)amino; or —NHC(O)-phenyl; n is 1, 2, 3, 4, 5, or 6; and r is 0, 1, 2, 3, 4, 5, or 6; and m is 0, 1, 2 or 3.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: December 3, 2019
    Assignees: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY, INDUSTRY-UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY
    Inventors: Tae Bo Sim, Woo Young Hur, Ho Jong Yoon, Chi Man Song, In Jae Shun, Byeong Yun Lim, Han Na Cho, Seung Hye Choi, Gu Kong, Jeong Yeon Lee
  • Patent number: 10485801
    Abstract: The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: November 26, 2019
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Gerard M. P. Giblin, David T. MacPherson, David R. Witty, Steven J. Stanway
  • Patent number: 10464906
    Abstract: This disclosure provides solid forms of 2-((2-chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide, and methods of manufacturing and using these forms.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: November 5, 2019
    Assignee: ACETYLON PHARMACEUTICALS, INC.
    Inventors: John H. van Duzer, Farzaneh Seyedi, Gui Liu
  • Patent number: 10457667
    Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from or the oxygen atom may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen or oxetanyl; R2 is hydrogen, lower alkyl lower alkoxy, halogen or cycloalkyl; --- the dotted line is nothing or may be —CH2—; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: October 29, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Patent number: RE48057
    Abstract: A pesticidal composition comprises a compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R4, R5, R6, R7, Z, Q, and Y are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests, or to an area to control pests.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: June 23, 2020
    Assignee: DOW AGROSCIENCES LLC
    Inventors: Noormohamed M. Niyaz, Ann M. Buysse, David A. Demeter, Negar Garizi, Ricky Hunter, Daniel Knueppel, Paul R. LePlae, Christian T. Lowe, Akshay Patny, Tony K. Trullinger, Martin J. Walsh, Yu Zhang