Additional Hetero Ring Which Is Unsaturated Patents (Class 544/333)
  • Patent number: 12139473
    Abstract: Activators of Kv3.1 and/or Kv3.2 channels which are therapeutically useful in the treatment of cognitive dysfunction and the negative symptoms which are associated with central nervous system disorders such as schizophrenia, Alzheimer's disease, Tourette's syndrome, autism, dementia, epilepsy and other disorders where gamma oscillations are dysfunctional are provided. The activators include substituted N-heteroaryl compounds.
    Type: Grant
    Filed: October 30, 2019
    Date of Patent: November 12, 2024
    Assignee: Bionomics Limited
    Inventors: Hamish Toop, Dharam Paul, Rajinder Singh, Erin Smith, Patrick Bazzini, Jean-Marie Contreras, Christophe Morice, Laurent Schaeffer, Celine Michaut-Simon, Florence Chery, Fabrice Garrido
  • Patent number: 12077523
    Abstract: The present disclosure relates to novel N-(isopropyl-triazolyl)pyridinyl)-heteroaryl-carboxamide derivatives or pharmaceutically acceptable salts thereof; a preparation method thereof; and use for preventing or treating an ASK-1 mediated disease comprising the same as an active ingredient.
    Type: Grant
    Filed: October 10, 2019
    Date of Patent: September 3, 2024
    Assignee: HK INNO.N CORPORATION
    Inventors: Dongkyu Kim, Seungin Kim, Jaeho Yoo, Seunghee Ji, Joo-hwan Kim, Joonseok Byun, Jinwoo Jung, Soo-jin Kim, Yeji Byeon, Jiwon Choi
  • Patent number: 12071425
    Abstract: Described herein are phenoxy-pyridyl-pyrimidine compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I structure or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Grant
    Filed: September 12, 2019
    Date of Patent: August 27, 2024
    Assignee: Genentech, Inc.
    Inventors: Marie-Gabrielle Braun, Cuong Q. Ly, Georgette Castanedo, Paul Gibbons, Wendy Lee, Joachim Rudolph, Nicole Alice Blaquiere, Jacob Bradley Schwarz, Ramsay Beveridge, Jean-Philippe Leclerc, Alexandre Lemire, Leo Fu
  • Patent number: 11992469
    Abstract: Provided herein are methods of treating a nerve injury in a subject in need thereof and methods of treating an injured neuron using diaryl hydrazones.
    Type: Grant
    Filed: September 21, 2021
    Date of Patent: May 28, 2024
    Assignee: City University of Hong Kong
    Inventors: Chi Him Eddie Ma, Ngan Pan Bennett Au
  • Patent number: 11991924
    Abstract: The present invention describes carbazole, dibenzofuran, dibenzothiophene and fluorene derivatives which are substituted by electron-deficient heteroaryl groups, in particular for use as triplet matrix materials in organic electroluminescent devices. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising these compounds.
    Type: Grant
    Filed: November 25, 2022
    Date of Patent: May 21, 2024
    Assignee: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Anja Jatsch, Thomas Eberle, Tobias Grossmann, Jonas Valentin Kroeber, Lars Dobelmann-Mara
  • Patent number: 11939318
    Abstract: The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH), interstitial lung disease (ILD), or chronic kidney disease (CKD).
    Type: Grant
    Filed: December 6, 2022
    Date of Patent: March 26, 2024
    Assignee: Gilead Sciences, Inc.
    Inventors: Brian P. Bestvater, Joshua A. Kaplan, Barton W. Phillips, Kin S. Yang, Anna Zagorska
  • Patent number: 11884649
    Abstract: Disclosed herein, inter alia, are compounds for inhibiting IRE1? and uses thereof.
    Type: Grant
    Filed: November 12, 2021
    Date of Patent: January 30, 2024
    Assignees: The Regents of the University of California, University of Washington
    Inventors: Feroz R. Papa, Bradley J. Backes, Dustin J. Maly
  • Patent number: 11800798
    Abstract: A charge transporting material which allows for a low driving voltage and is superior in luminous efficiency and durability is provided. The charge transporting material comprising a compound represented by any one of the general formula (1-1) to (1-3) wherein R111 to R114, R121 to R125 and R131 to R135, L111 to L113, and L121 to L123 are as defined in the specification.
    Type: Grant
    Filed: April 26, 2021
    Date of Patent: October 24, 2023
    Assignee: UDC IRELAND LIMITED
    Inventor: Kousuke Watanabe
  • Patent number: 11765972
    Abstract: A compound represented by the following formula (1), wherein X1 is O or S, and two or more of Y1, Y2 and Y3 are N, provided that the case where one or both of —Ar1-Ar2 and —Ar3-Ar4 is a p-terphenyl-3-yl group is excluded.
    Type: Grant
    Filed: February 20, 2019
    Date of Patent: September 19, 2023
    Assignee: IDEMITSU KOSAN CO., LTD.
    Inventors: Yoshinao Shirasaki, Tetsuya Masuda, Takushi Shiomi, Masatoshi Saito, Kei Yoshida, Masato Nakamura
  • Patent number: 11691965
    Abstract: Disclosed is a method for preparing a pyrrolidinyl urea derivative, which acts as a TrkA inhibitor, and further disclosed are an intermediate compound of a compound of formula (I) and a preparation method therefor.
    Type: Grant
    Filed: January 8, 2021
    Date of Patent: July 4, 2023
    Assignee: ZHANGZHOU PIEN TZE HUANG PHARMACEUTICAL CO., LTD.
    Inventors: Jinming Huang, Juan Yu, Jinxiang Zeng, Limei Yang, Tingting Yin, Yang Zhang, Wentao Wu, Zhixiang Li, Jian Qin
  • Patent number: 11673893
    Abstract: The disclosure is directed to, in part, to CDK inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.
    Type: Grant
    Filed: September 11, 2020
    Date of Patent: June 13, 2023
    Assignee: Prelude Therapeutics Incorporated
    Inventors: Liang Lu, Rupa Shetty, Andrew Paul Combs, Chaofeng Dai, Raul Andrew Leal, Klare Lazor Bersch
  • Patent number: 11530205
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as products containing such compounds, and methods of their use and synthesis. Such compounds have the structure of Formula (I) below: (I) or pharmaceutically acceptable salts thereof, wherein A, J, W1, Y, Z, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: April 26, 2018
    Date of Patent: December 20, 2022
    Assignee: Receptos LLC
    Inventors: Junko Tamiya, Philip Turnbull, Brahmachary Enugurthi, Liming Huang, Adam R. Yeager, Thomas Fowler, Greg P. Iacobini, Matthew Richard Crittall
  • Patent number: 11450814
    Abstract: The present disclosure relates to an organic electroluminescent compound represented by formula 1 and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present disclosure, an organic electroluminescent device having improved driving voltage, luminous efficiency, and/or lifespan characteristics can be provided.
    Type: Grant
    Filed: September 20, 2018
    Date of Patent: September 20, 2022
    Inventor: Jin-Ri Hong
  • Patent number: 11440908
    Abstract: The present disclosure relates to a dasatinib co-crystal form comprising dasatinib and a second compound, also referred to as a co-crystal former, wherein the second compound is selected from butyl paraben, propyl paraben and ethyl vanillin. The present disclosure is also related to an ethyl formate solvate form of dasatinib. The present disclosure is also related to processes for the preparation of the dasatinib co-crystal and solvate forms of dasatinib. Further, the present disclosure also relates to pharmaceutical compositions comprising the dasatinib co-crystal and solvate forms of dasatinib and methods for treating disease using the dasatinib co-crystal and solvate forms of dasatinib.
    Type: Grant
    Filed: October 22, 2020
    Date of Patent: September 13, 2022
    Assignee: Johnson Matthey Public Limited Company
    Inventor: Padmini Kavuru
  • Patent number: 11306078
    Abstract: The present invention relates to piperidine derivatives of formula (I) wherein Ar1, Ar2, RAr1, R1, R2, and R3 are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
    Type: Grant
    Filed: July 14, 2020
    Date of Patent: April 19, 2022
    Assignee: IDORSIA PHARMACEUTICALS LTD.
    Inventors: Hamed Aissaoui, Philippe Guerry, Francois Lehembre, Julien Pothier, Laetitia Pouzol, Sylvia Richard-Bildstein, Shuguang Yuan
  • Patent number: 10959432
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides and especially as fungicides.
    Type: Grant
    Filed: May 8, 2020
    Date of Patent: March 30, 2021
    Assignee: Syngenta Participations AG
    Inventors: Farhan Bou Hamdan, Daniel Stierli, Stephane André Marie Jeanmart, Christopher Richard Ayles Godfrey, Thomas James Hoffman, Renaud Beaudegnies, Martin Pouliot
  • Patent number: 10912775
    Abstract: Disclosed are a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: February 9, 2021
    Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Songliang Wu, Zhi Luo, Yuan Chen, Yuhe Wang, Dakun Qin, Xiaolin Li, Zheng Wang, Weidong Li, Haiying He
  • Patent number: 10898486
    Abstract: Disclosed is a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: January 26, 2021
    Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Songliang Wu, Zhi Luo, Yuan Chen, Yuhe Wang, Dakun Qin, Xiaolin Li, Zheng Wang, Weidong Li, Haiying He
  • Patent number: 10874674
    Abstract: Disclosed is a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: December 29, 2020
    Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Songliang Wu, Zhi Luo, Yuan Chen, Yuhe Wang, Dakun Qin, Xiaolin Li, Zheng Wang, Weidong Li, Haiying He
  • Patent number: 10765750
    Abstract: The purpose of the present invention is to provide a pharmaceutical composition that comprises a specific compound and exhibits a superior preservation efficacy, the specific compound being stable within the pharmaceutical composition, and to provide methods for improving the stability of the specific compound within the pharmaceutical composition and the preservation efficacy of the pharmaceutical composition. The pharmaceutical composition according to the present invention comprises isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, and further comprises edetic acid or a salt thereof.
    Type: Grant
    Filed: October 21, 2019
    Date of Patent: September 8, 2020
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventor: Yoko Endo
  • Patent number: 10687533
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides and especially as fungicides.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: June 23, 2020
    Assignee: Syngenta Participations AG
    Inventors: Farhan Bou Hamdan, Daniel Stierli, Stephane André Marie Jeanmart, Christopher Richard Ayles Godfrey, Thomas James Hoffman, Renaud Beaudegnies, Martin Pouliot
  • Patent number: 10633368
    Abstract: Provided is a synthesis method for a voriconazole intermediate condensate as shown in formula II or an acid addition salt thereof. As shown in reaction formula 1, the product is prepared via compounds III and IV. The synthesis method adjusts the feeding means, and the reaction conditions are mild and controllable, thereby reducing the production of impurity A, avoiding the use of highly toxic metal lead, and eliminating the risk of highly toxic metal remaining in a drug. The product has a higher purity and significant industrial application value.
    Type: Grant
    Filed: January 16, 2017
    Date of Patent: April 28, 2020
    Assignee: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
    Inventors: Hu Huang, Wenfeng Huang, Guoliang Tu, Jiegen Liu, Zhongming Xu, Qianghui Wu, Zhaoyang Meng, Yuling Fang
  • Patent number: 10485872
    Abstract: The purpose of the present invention is to provide a pharmaceutical composition that comprises a specific compound and exhibits a superior preservation efficacy, the specific compound being stable within the pharmaceutical composition, and to provide methods for improving the stability of the specific compound within the pharmaceutical composition and the preservation efficacy of the pharmaceutical composition. The pharmaceutical composition according to the present invention comprises isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, and further comprises edetic acid or a salt thereof.
    Type: Grant
    Filed: October 29, 2018
    Date of Patent: November 26, 2019
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventor: Yoko Endo
  • Patent number: 10221162
    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 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: July 12, 2018
    Date of Patent: March 5, 2019
    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, Julie Anne Heath, Daniel B. Horne, Jonathan Houze, Matthew R. Kaller, Aarif Yusuf Khakoo, David John Kopecky, Su-Jen Lai, Zhihua Ma, Lawrence R. McGee, Julio C. Medina, Jeffrey T. Mihalic, Nobuko Nishimura, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Kevin Yang, Wen-Chen Yeh, Mikkel V. Debenedetto, Robert P. Farrell, Simon J. Hedley, Ted C. Judd, Frank Kayser
  • Patent number: 10155741
    Abstract: The present invention relates to compounds of formula I wherein R1? is methyl; R1 is methyl, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1? and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, cyclopropylmethyl, or hydroxmethyl; R3 is Cl, F, CF3, methyl, methoxy, or cyclopropyl; R4 is hydrogen, methyl, F or Cl; X is N or CH; Y is N or CH; with the proviso that X and Y are not simultaneously CH; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.
    Type: Grant
    Filed: April 17, 2018
    Date of Patent: December 18, 2018
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Marius Hoener, Juergen Wichmann
  • Patent number: 10149908
    Abstract: The purpose of the present invention is to provide a pharmaceutical composition that comprises a specific compound and exhibits a superior preservation efficacy, the specific compound being stable within the pharmaceutical composition, and to provide methods for improving the stability of the specific compound within the pharmaceutical composition and the preservation efficacy of the pharmaceutical composition. The pharmaceutical composition according to the present invention comprises isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, and further comprises edetic acid or a salt thereof.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: December 11, 2018
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventor: Yoko Endo
  • Patent number: 10034886
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Grant
    Filed: September 21, 2017
    Date of Patent: July 31, 2018
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs, Daniel Glynn, Mark Mills
  • Patent number: 9994567
    Abstract: Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.
    Type: Grant
    Filed: September 14, 2017
    Date of Patent: June 12, 2018
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Jack Lin, Wayne Spevak, Jiazhong Zhang
  • Patent number: 9957252
    Abstract: The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: May 1, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Michael R. Loso, Gary D. Gustafson, Asako Kubota, Maurice C. Yap, Zachary A. Buchan, Kimberly M. Steward, Michael T. Sullenberger, William J. Hoekstra, Christopher M. Yates
  • Patent number: 9937175
    Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: April 10, 2018
    Assignee: Sanofi
    Inventor: Christopher L. VanDeusen
  • Patent number: 9839664
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: December 12, 2017
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Patent number: 9795613
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: October 24, 2017
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs, Daniel Glynn, Mark Mills
  • Patent number: 9776998
    Abstract: Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: October 3, 2017
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Jack Lin, Wayne Spevak, Jiazhong Zhang
  • Patent number: 9598430
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: March 21, 2017
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Patent number: 9550737
    Abstract: A series of benzimidazole derivatives, 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: June 11, 2013
    Date of Patent: January 24, 2017
    Assignee: UCB Biopharma SPRL
    Inventors: Daniel Christopher Brookings, Mark Daniel Calmiano, Ellen Olivia Gallimore, Helen Tracey Horsley, Martin Clive Hutchings, James Andrew Johnson, Boris Kroeplien, Fabien Claude Lecomte, Martin Alexander Lowe, Timothy John Norman, John Robert Porter, Joanna Rachel Quincey, James Thomas Reuberson, Matthew Duncan Selby, Michael Alan Shaw, Zhaoning Zhu, Anne Marie Foley
  • Patent number: 9533982
    Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: March 20, 2015
    Date of Patent: January 3, 2017
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Andrew S. Felts
  • Patent number: 9505746
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: November 29, 2016
    Assignee: Genentech, Inc.
    Inventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
  • Patent number: 9499551
    Abstract: Disclosed herein are substituted pyrrolopyridine and pyrrolopyrazine compounds and compositions useful in the treatment of TAK mediated diseases, such as cancer, having the structure of Formula (I): wherein R1, R2, R3, and R4 are as defined in the detailed description. Methods of modulation of TAK activity in a human or animal subject are also provided, providing therapeutic benefit to subjects with disease conditions, especially cancer.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: November 22, 2016
    Assignee: Confluence Life Sciences, Inc.
    Inventors: Eric Jon Jacobsen, James Robert Blinn, John Robert Springer, Susan L. Hockerman
  • Patent number: 9474755
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: October 25, 2016
    Assignee: Celgene International II SARL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Patent number: 9469627
    Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: October 18, 2016
    Assignee: Sanofi
    Inventors: Christopher L. Vandeusen, Franz J. Weiberth, Harpal S. Gill, George Lee, Andrea Hillegass
  • Patent number: 9464084
    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: May 18, 2015
    Date of Patent: October 11, 2016
    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: 9315502
    Abstract: The present invention relates to compounds of general formula wherein Ar is phenyl or pyridinyl; X1 is N or CH, X2 is N or CH, with the proviso that only one of X1 or X2 is N and the other is CH; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(O)2-lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: April 19, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
  • Patent number: 9266870
    Abstract: A heteroaromatic methyl cyclic amine derivative represented by formula (IA) or a pharmaceutically acceptable salt thereof is useful for treatment or prophylaxis of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, cephalalgia, hemicrania, pain, digestive diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases and hypertension, on the basis of an orexin (OX) receptor antagonist activity.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: February 23, 2016
    Assignee: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Aya Futamura, Yuko Araki, Masahito Abe, Hiroshi Ohta, Ryo Suzuki, Dai Nozawa
  • Patent number: 9221791
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: August 12, 2014
    Date of Patent: December 29, 2015
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
  • Patent number: 9206180
    Abstract: A quantitative model that describes the assembly of diketopyrrolopyrrole-based donors and a perylenediimide acceptor into chiral superstructures, as a result of both hydrogen bonding and ?•••? stacking. This model provides thermodynamic parameters (?H° and ?S°) for all noncovalent interactions involved in the assembly and explains the subtle supramolecular cues that convert disordered aggregates into well-defined helical assemblies.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: December 8, 2015
    Assignee: New York University
    Inventors: Adam B. Braunschweig, Stephen Rieth, Zhong Li, Charlotte E. Hinkle
  • Patent number: 9209408
    Abstract: Novel benzoxazole derivatives are provided to reduce driving voltage of light-emitting elements, and to reduce power consumption of light-emitting elements, light-emitting devices, and electronic devices. A benzoxazole derivative represented by the general formula (G1) is provided. Since the benzoxazole derivative represented by the general formula (G1) has an electron-injecting property, the benzoxazole derivative can be suitably used for light-emitting elements, light-emitting devices, and electronic devices.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: December 8, 2015
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Sachiko Kawakami, Hiroko Nomura, Takahiro Ushikubo, Satoshi Seo
  • Patent number: 9173396
    Abstract: The present application relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which also include arthropods and especially insects.
    Type: Grant
    Filed: October 17, 2011
    Date of Patent: November 3, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Thomas Bretschneider, Adeline Köhler, Joachim Kluth, Martin Füβlein, Peter Jeschke, Reiner Fischer, Friedrich August Mühlthau, Olga Malsam, Arnd Voerste, Klaus-Helmut Müller, Yoshitaka Sato
  • Patent number: 9085562
    Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: July 21, 2015
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates, Brian A. Chauder
  • Patent number: 9045466
    Abstract: An amidine compound represented by formula (I) (wherein A1 represents a nitrogen atom or a group represented by formula CR6; A2 and A3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R2 and R3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a C1-6 alkoxy group; and R4 and R5 are the same as or different from each other and independently represent a hydrogen atom, a C1-6 haloalkyl group, a C1-6 alkyl group or the like) or a salt thereof. The compound is useful as an anti-fungal agent.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: June 2, 2015
    Assignees: TAISHO PHARMACEUTICAL CO., LTD, TOYAMA CHEMICAL CO., LTD.
    Inventors: Tetsuya Tanikawa, Yasunobu Ushiki, Fumihito Ushiyama, Toru Yamaguchi, Naoya Ono, Keiko Yamamoto, Risa Tsuruta, Yasuhiro Tsutsui, Noritomo Fujino, Ayumu Mori
  • Patent number: RE48183
    Abstract: Provided is a pharmaceutical preparation for treatment or prevention of glaucoma or ocular hypertension, comprising 0.0003 to 0.01% (w/v) of isopropyl (6-{[4-(pyrazol-1-yl)benzyl] (pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino) acetate, or a salt thereof. The pharmaceutical preparation has an excellent intraocular pressure lowering effect and may be used as a therapeutic or preventive agent for glaucoma or ocular hypertension or an intraocular pressure lowering agent.
    Type: Grant
    Filed: August 28, 2018
    Date of Patent: September 1, 2020
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Naveed Shams, Henk-Andre Kroon, Hisashi Kawata, Noriko Kawabata