The Additional Polycyclo Ring System Is A Bicyclo Ring System Having Nitrogen As The Only Ring Hetero Atom [e.g., 5-(indolyl-3-methylene)- Hydantoin, Etc.] Patents (Class 548/312.1)
  • Patent number: 11717273
    Abstract: A kit for testing for a virus and interacting with a sensor are disclosed. For example, the kit can include a first container having a first media for conditioning, catalyst formation and rinsing of the sensor. The first media can comprise V mL of 1 M KOH. The kit can have a second container with a second media for negative control (baseline solution) for the sensor. The second media can comprise W ML of 0.01 M KOH. The kit can further include a third container having a third media for sample testing with the sensor. The third media can comprise X mL of 0.01 M KOH. The third container can receive Y mL of saliva to complete a Z mL total volume in the third container prior to sample testing. In some versions, a ratio V: W: X: Y: Z=1.0: 1.0: 0.9: 0.1: 1.0 can be used.
    Type: Grant
    Filed: May 3, 2022
    Date of Patent: August 8, 2023
    Assignee: Texas Tech University System
    Inventor: Gerardine G. Botte
  • Patent number: 11453681
    Abstract: The present disclosure relates generally to certain ene-oxindole compounds, pharmaceutical compositions comprising thereof. Also disclosed are methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.
    Type: Grant
    Filed: May 21, 2020
    Date of Patent: September 27, 2022
    Assignee: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Jayaraman Chandrasekhar, Julian A. Codelli, John H. Conway, Kristyna M. Elbel, Rao V. Kalla, Samuel E. Metobo, Scott A. Mitchell, Thao D. Perry, Scott P. Simonovich, Christopher A. Ziebenhaus
  • Patent number: 10604508
    Abstract: The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: March 31, 2020
    Assignee: CrystalGenomics, Inc.
    Inventors: Yong Rae Hong, Jeong Eun Na, Im Sook Min, Hyun Ju Cha, Sool Ki Kwon, Seonggu Ro, Joong Myung Cho
  • Patent number: 9758508
    Abstract: The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
    Type: Grant
    Filed: December 26, 2013
    Date of Patent: September 12, 2017
    Assignee: CrystalGenomics, Inc.
    Inventors: Yong Rae Hong, Jeong Eun Na, Im Sook Min, Hyun Ju Cha, Sool Ki Kwon, Seonggu Ro, Joong Myung Cho
  • Patent number: 9701671
    Abstract: Provided is an organic compound represented by general formula (1) or (2): where in general formulae (1) and (2), X1 and X2 are each independently selected from a substituted or unsubstituted alkyl group and a substituted or unsubstituted aralkyl group, and R11 to R20 represent a hydrogen atom or a substituent. A1?and A2?each independently represent a monovalent anion.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: July 11, 2017
    Assignee: Canon Kabushiki Kaisha
    Inventors: Satoshi Igawa, Kenji Yamada
  • Patent number: 9365512
    Abstract: The present invention relates to isoindoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such isoindoline derivatives, and the use of such isoindoline derivatives for therapeutic purposes.
    Type: Grant
    Filed: February 11, 2013
    Date of Patent: June 14, 2016
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Wilhelm Amberg, Udo Lange, Michael Ochse, Frauke Pohlki, Charles W. Hutchins, Irini Zanze, Hongyu H. Zhao, Huan-Qiu Li, Ying X. Wang
  • Publication number: 20150133422
    Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 14, 2015
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
  • Patent number: 9029408
    Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 12, 2015
    Assignees: GTx, Inc., University of Tennessee Research Foundation
    Inventors: Duane D. Miller, Wei Li, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn
  • Patent number: 9018394
    Abstract: The invention is a method for efficiently producing an aromatic compound by an intramolecular cyclization reaction, the aromatic compound having a ring structure that includes a nitrogen atom or oxygen atom. An aromatic compound composed of tert-butyl-2-(3-oxo-3-phenylpropyl)phenyl carbamate or another aniline derivative or the like, or an aromatic compound composed of 3-(1-hydroxynaphthalene-2-yl)propionic acid or another naphthol derivative or the like is made to react in a system to which an oxidizing agent and a quaternary ammonium salt represented by general formula (1) are fed. In the formula, X is an iodine atom; and R1, R2, R3 and R4 are each independently a C1-30 hydrocarbon group in which some hydrogen atoms are optionally substituted with halogen atoms, or R1 and R2 may be combine to form a divalent organic group bonded to a nitrogen atom, and R3 and R4 may combine to form a divalent organic group bonded to a nitrogen atom.
    Type: Grant
    Filed: February 2, 2012
    Date of Patent: April 28, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Uyanik Muhammet
  • Patent number: 9006455
    Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
    Type: Grant
    Filed: August 1, 2013
    Date of Patent: April 14, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shawn K. Pack, Kenneth J. Natalie, Jr., Makonen Belema
  • Patent number: 8987305
    Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: March 24, 2015
    Assignee: Aptose Biosciences Inc.
    Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
  • Publication number: 20150057282
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Applicant: SAREUM LIMITED
    Inventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
  • Patent number: 8937303
    Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers of organic compound arranged between the pair of electrodes, wherein the organic compound layer, or one or more of the organic compound layers, comprises a compound represented by a substituted imidazole. The substituents on the imidazole ring may be selected from a range of suitable substituents, including: substituted or unsubstituted aryl groups, substituted or unsubstituted heterocyclic groups, substituted or unsubstituted alkyl groups or cyano groups. In various aspects of the invention, at least one of the substituent groups may be a substituted or unsubstituted imidazole or thiophene group.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: January 20, 2015
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: James Matthew MacDonald, Kazunori Ueno, Karl Peter Weber, Tadahiko Hirai, Juo-Hao Li
  • Patent number: 8912199
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: December 16, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Publication number: 20140364429
    Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 11, 2014
    Applicant: AB PHARMA LTD.
    Inventor: Zheng-Yun James ZHAN
  • Patent number: 8889726
    Abstract: Disclosed are compounds of Formula I, Formula II, and Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: November 18, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Subramanian Baskaran, Richard Martin Grimes, Wieslaw Mieczyslaw Kazmierski, Martin Robert Leivers
  • Publication number: 20140309259
    Abstract: The invention provides novel, water-soluble 2-aminoimidazoline derivatives having general Formula (I) as well as some precursors of Formula (I), which are very potent inducers of G2/M cell cycle arrest. In treated tumor cells, compounds of Formula (I) give gene expression profile distinct from known antimitotic agents. The invention also provides methods for preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 16, 2014
    Inventors: Stanislaw Wieslaw Pikul, Wieslaw Marek Cholody
  • Publication number: 20140309240
    Abstract: The invention provides novel, water-soluble 2-aminoimidazoline derivatives having general Formula (I) as well as some precursors of Formula (I), which are very potent inducers of G2/M cell cycle arrest. In treated tumor cells, compounds of Formula (I) give gene expression profile distinct from known antimitotic agents. The invention also provides methods for preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.
    Type: Application
    Filed: April 9, 2014
    Publication date: October 16, 2014
    Inventors: Stanislaw Wieslaw Pikul, Wieslaw Marek Cholody
  • Patent number: 8859529
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Patent number: 8846023
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: September 30, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
  • Patent number: 8846741
    Abstract: The present invention relates to N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives of the formula (I), (II), (III) or (IV) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such N-substituted amino-benzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives, and the use of such N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives for therapeutic purposes. The N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: September 30, 2014
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki, Ernesto Santandrea, Charles Hutchins
  • Publication number: 20140288084
    Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor 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: Application
    Filed: October 28, 2012
    Publication date: September 25, 2014
    Applicant: VANDERBILT UNIVERSITY
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
  • Publication number: 20140275074
    Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 24, 2012
    Publication date: September 18, 2014
    Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
  • Patent number: 8822513
    Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
    Type: Grant
    Filed: August 24, 2011
    Date of Patent: September 2, 2014
    Assignees: GTX, Inc., University of Tennessee Research Foundation
    Inventors: Yan Lu, Chien-Ming Li, Zhao Wang, Jianjun Chen, Wei Li, James T. Dalton, Duane D. Miller, Charles Duke, Sunjoo Ahn
  • Patent number: 8822444
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: September 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
  • Publication number: 20140221421
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
  • Patent number: 8796466
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: August 5, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Piyasena Hewawasam, John F. Kadow, Omar D. Lopez, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Lawrence B. Snyder, Denis R. St. Laurent, Gan Wang, Ningning Xu, Makonen Belema
  • Publication number: 20140213623
    Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.
    Type: Application
    Filed: October 9, 2013
    Publication date: July 31, 2014
    Applicants: GTx, Inc., University of Tennessee Research Foundation
    Inventors: Duane D. Miller, Li Wei, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn
  • Publication number: 20140205537
    Abstract: Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.
    Type: Application
    Filed: June 22, 2012
    Publication date: July 24, 2014
    Applicant: ZENOBIA THERAPEUTICS, INC.
    Inventors: Pierre-Yves Bounaud, Vicki Nienaber, Ruo W. Steensma, John A. Lowe, III
  • Patent number: 8785489
    Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
  • Publication number: 20140200226
    Abstract: Novel compositions and methods for the treatment and prevention of malaria are disclosed herein.
    Type: Application
    Filed: December 12, 2013
    Publication date: July 17, 2014
    Applicants: Florida Atlantic University, University of Central Florida Research Foundation, Inc.
    Inventors: Debopam Chakrabarti, Amy Wright
  • Patent number: 8765757
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: November 13, 2008
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Publication number: 20140171476
    Abstract: Disclosed are compounds of Formula I, Formula II, and Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.
    Type: Application
    Filed: August 6, 2012
    Publication date: June 19, 2014
    Applicant: GlaxoSmith Kline LLC
    Inventors: Subramanian Baskaran, Richard Martin Grimes, Wieslaw Mieczyslaw Kazmierski, Martin Robert Leivers
  • Publication number: 20140165223
    Abstract: Described are methods and compositions for inhibiting the trimerization of ligands belonging to the TNF superfamily, in particular, inhibiting RANKL trimerization. Accordingly, the methods and compositions provided herein can be used to treat disorders associated with increased RANK signaling, in particular those related to bone loss. Compounds that inhibit trimerization of ligands belonging to the TNF superfamily are also described.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Applicant: B.S.R.C. "Alexander Fleming"
    Inventors: Eleni Ntouni, Georgios Kollias
  • Patent number: 8741942
    Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: June 3, 2014
    Assignees: President and Fellows of Harvard College, The Brigham and Women's Hospital, Inc.
    Inventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
  • Patent number: 8729273
    Abstract: The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: May 20, 2014
    Assignee: LG Life Sciences Ltd.
    Inventors: Jeong Uk Song, Geun Tae Kim, Sung Pil Choi, Cheol Kyu Jung, Deok Seong Park, Eun Sil Choi, Tae Hun Kim, Hyun Jung Park, Wan Su Park, Heui Sul Park, Ki Chul Koo, Vasily Artemov
  • Publication number: 20140073622
    Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 13, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Publication number: 20140017195
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: September 9, 2013
    Publication date: January 16, 2014
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavole, Omar D. Lopez, Alain Martel, Nicolas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
  • Publication number: 20140018389
    Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Application
    Filed: September 16, 2013
    Publication date: January 16, 2014
    Inventors: Rico Lavoie, John A. Bender, Jeffrey Lee Romine, Edward H. Ruediger, Carol Bachand, Omar D. Lopez, Qi Chen, Makonen Belema, John F. Kadow, Lawrence G. Hamann
  • Patent number: 8629285
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: January 14, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
  • Publication number: 20130338371
    Abstract: The invention is a method for efficiently producing an aromatic compound by an intramolecular cyclization reaction, the aromatic compound having a ring structure that includes a nitrogen atom or oxygen atom. An aromatic compound composed of tert-butyl-2-(3-oxo-3-phenylpropyl)phenyl carbamate or another aniline derivative or the like, or an aromatic compound composed of 3-(1-hydroxynaphthalene-2-yl)propionic acid or another naphthol derivative or the like is made to react in a system to which an oxidizing agent and a quaternary ammonium salt represented by general formula (1) are fed. In the formula, X is an iodine atom; and R1, R2, R3 and R4 are each independently a C1-30 hydrocarbon group in which some hydrogen atoms are optionally substituted with halogen atoms, or R1 and R2 may be combine to form a divalent organic group bonded to a nitrogen atom, and R3 and R4 may combine to form a divalent organic group bonded to a nitrogen atom.
    Type: Application
    Filed: February 2, 2012
    Publication date: December 19, 2013
    Applicant: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Uyanik Muhammet
  • Patent number: 8598217
    Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: December 3, 2013
    Assignees: Astex Therapeutics Ltd., Novartis AG
    Inventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'Reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Giraldes, Michael Joseph Luzzio, Lawrence Blas Perez
  • Patent number: 8598181
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: December 3, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Publication number: 20130317213
    Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
    Type: Application
    Filed: August 1, 2013
    Publication date: November 28, 2013
    Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
  • Publication number: 20130303538
    Abstract: The invention relates to compounds of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them.
    Type: Application
    Filed: January 20, 2012
    Publication date: November 14, 2013
    Inventors: Joachim Nozulak, Dieter Oser
  • Patent number: 8574563
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: November 5, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
  • Publication number: 20130281451
    Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.
    Type: Application
    Filed: April 3, 2013
    Publication date: October 24, 2013
    Applicant: ANNJI PHARMACEUTICAL CO., LTD.
    Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
  • Publication number: 20130274260
    Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.
    Type: Application
    Filed: December 13, 2011
    Publication date: October 17, 2013
    Inventors: Gerard Griffioen, Tom Van Dooren, Verónica Rojas De La Parra, Sara Allasia, Arnaud Marchand, Amuri Kilonda, Patrick Chaltin
  • Publication number: 20130264554
    Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers of organic compound arranged between the pair of electrodes, wherein the organic compound layer, or one or more of the organic compound layers, comprises a compound represented by a substituted imidazole. The substituents on the imidazole ring may be selected from a range of suitable substituents, including: substituted or unsubstituted aryl groups, substituted or unsubstituted heterocyclic groups, substituted or unsubstituted alkyl groups or cyano groups. In various aspects of the invention, at least one of the substituent groups may be a substituted or unsubstituted imidazole or thiophene group.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 10, 2013
    Inventors: James Matthew MacDonald, Kazunori Ueno, Karl Peter Weber, Tadahiko Hirai, Juo-Hao Li