Three Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 544/95)
  • Patent number: 11958864
    Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: February 14, 2022
    Date of Patent: April 16, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Timothy John Hartingh, John A. McCauley, Tao Yu, Yonglian Zhang
  • Patent number: 11202780
    Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-(2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
    Type: Grant
    Filed: January 10, 2020
    Date of Patent: December 21, 2021
    Assignee: Gilead Sciences, Inc.
    Inventors: Ernest A. Carra, Irene Chen, Katie Ann Keaton, Scott E. Lazerwith, Vahid Zia
  • Patent number: 10457690
    Abstract: The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: October 29, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jingjun Yin, Tetsuji Itoh, Jianguo Yin, Bangping Xiang, Kevin R. Campos, Alexei Kalinin, Zhuqing Liu, Melodie Deniz Christensen, Kevin M. Belyk, Richard J. Varsolona, Andrew Brunskill
  • Patent number: 10385067
    Abstract: The present invention relates to sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I, pharmaceutical formulations, and uses thereof for treating or prophylactically preventing an HIV infection.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: August 20, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Ernest A. Carra, Irene Chen, Vahid Zia
  • Patent number: 10323044
    Abstract: An object of the present invention is to provide a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having excellent stability and favorable characteristics in terms of its production and formulation into drugs. The present invention provides a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having characteristic peaks of diffraction angle (2?±0.1°) at 7.7°, 9.5°, 10.3°, 12.3°, 14.5°, 15.6°, 16.3°, 17.8°, 18.3°, 19.3°, 20.9°, 22.8°, 24.2°, 25.7°, 26.8°, 27.7°, 29.0° and 30.1° in a powder X-ray diffraction spectrum.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: June 18, 2019
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Masaya Hashimoto
  • Patent number: 10301321
    Abstract: The present invention relates to a novel process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof using novel intermediates.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: May 28, 2019
    Assignee: LAURUS LABS LIMITED
    Inventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Lakshmi Narasimha Dammalapati, Mani Bushan Kotala, Ravindra Aduri
  • Patent number: 10202404
    Abstract: The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: February 12, 2019
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Tomokazu Yoshinaga, Kouhei Nodu
  • Patent number: 10098886
    Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
    Type: Grant
    Filed: May 5, 2017
    Date of Patent: October 16, 2018
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Ernest A. Carra, Irene Chen, Katie Ann Keaton, Scott E. Lazerwith, Vahid Zia
  • Patent number: 10087193
    Abstract: The present disclosure relates to novel crystalline dolutegravir sodium Form-M2, Form-M3, Form-M4 and process for the preparation thereof.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: October 2, 2018
    Assignee: Mylan Laboratories Limited
    Inventors: Ramakoteswara Rao Jetti, Satish Beeravelly, Madhu Murthy Nadella, Haribabu Nandipati
  • Patent number: 10011613
    Abstract: The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Grant
    Filed: August 21, 2015
    Date of Patent: July 3, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Tomokazu Yoshinaga, Kouhei Nodu
  • Patent number: 9994588
    Abstract: An object of the present invention is to provide a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having excellent stability and favorable characteristics in terms of its production and formulation into drugs. The present invention provides a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having characteristic peaks of diffraction angle (2?±0.1°) at 7.7°, 9.5°, 10.3°, 12.3°, 14.5°, 15.6°, 16.3°, 17.8°, 18.3°, 19.3°, 20.9°, 22.8°, 24.2°, 25.7°, 26.8°, 27.7°, 29.0° and 30.1° in a powder X-ray diffraction spectrum.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: June 12, 2018
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Masaya Hashimoto
  • Patent number: 9938296
    Abstract: The present invention relates to the preparation of carbamoylpyridone derivatives such as the compound of formula (VIIIa):
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: April 10, 2018
    Assignee: VIIV Healthcare Company
    Inventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
  • Patent number: 9856271
    Abstract: The present invention relates to a novel process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof using novel intermediates.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: January 2, 2018
    Assignee: LAURUS LABS LIMITED
    Inventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Lakshmi Narasimha Dammalapati, Mani Bushan Kotala, Ravindra Aduri
  • Patent number: 9708342
    Abstract: The present invention relates to sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl) carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3] oxazepin-8-olate Form I and the therapeutic uses thereof.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: July 18, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Ernest A. Carra, Irene Chen, Vahid Zia
  • Patent number: 9682084
    Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: June 20, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Ernest A. Carra, Irene Chen, Katie Ann Keaton, Scott E. Lazerwith, Vahid Zia
  • Patent number: 9242986
    Abstract: A synthesis approach providing an early ring attachment via a bromination to compound 1-1 yielding compound II-II, whereby a final product such as AA can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
    Type: Grant
    Filed: May 8, 2014
    Date of Patent: January 26, 2016
    Assignees: SHIONOGI & CO., LTD., ViiV Healthcare Company
    Inventors: Takashi Kawasuji, Daiki Nagamatsu
  • Patent number: 9206197
    Abstract: An amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.
    Type: Grant
    Filed: September 2, 2012
    Date of Patent: December 8, 2015
    Assignee: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Patent number: 9200009
    Abstract: The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: December 1, 2015
    Assignee: SHIONOGI & CO., LTD.
    Inventor: Toshiyuki Akiyama
  • Patent number: 9120817
    Abstract: The present invention relates to processes for the preparation of (4R,12aS)-7-methoxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid by contacting a pyridinone carboxylic acid aldehyde with (3R)-3-amino-1-butanol.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: September 1, 2015
    Assignee: VIIV HEALTHCARE COMPANY
    Inventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
  • Publication number: 20150141415
    Abstract: The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 21, 2015
    Inventors: Omonike Arike Olaleye, Sarah Finney John, Adaugo Chimzurum Isichei, Jun O Liu, Rosa Maldonado, Janice Endsley
  • Publication number: 20150105551
    Abstract: The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Rok GRAHEK, Darko KOCJAN, Andrej BASTARDA, Andrej KOCIJAN, Matjaz KRACUN
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20150057444
    Abstract: The present invention relates to the preparation of carbamoylpyridone derivatives and intermediates.
    Type: Application
    Filed: October 14, 2014
    Publication date: February 26, 2015
    Inventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
  • Publication number: 20150038702
    Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) wherein R1d, R2d, and R4d are as defined herein.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Yukihito SUMINO, Moriyasu MASUI, Diasuke YAMADA, Fumiya IKARASHI, Kazuya OKAMOTO
  • Publication number: 20150031876
    Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
    Type: Application
    Filed: September 5, 2014
    Publication date: January 29, 2015
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
  • Publication number: 20150025067
    Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.
    Type: Application
    Filed: February 13, 2013
    Publication date: January 22, 2015
    Applicant: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventors: Yi Zheng, Prakash Jagtap, Emily E. Bosco, Jaroslaw Meller, Marie-Dominique Filippi
  • Publication number: 20150018298
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: July 11, 2014
    Publication date: January 15, 2015
    Inventors: Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
  • Publication number: 20140350004
    Abstract: The present invention provides an amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.
    Type: Application
    Filed: September 2, 2012
    Publication date: November 27, 2014
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Publication number: 20140329808
    Abstract: Compositions of matter including (R)-2,5,6,8-tetramethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine and (R)-2,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine are disclosed herein. Further disclosed are methods of preparation of such compounds and the use of such compounds as anticancer agents.
    Type: Application
    Filed: July 21, 2014
    Publication date: November 6, 2014
    Inventors: Khalid A. El Sayed, Paul W. Sylvester, Fathy A. Behery
  • Publication number: 20140256937
    Abstract: The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 11, 2014
    Applicant: SHIONOGI & CO., LTD.
    Inventor: Toshiyuki Akiyama
  • Publication number: 20140243521
    Abstract: A synthesis approach providing an early ring attachment via a bromination to compound 1-1 yielding compound II-I1, whereby a final product such as AA can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicants: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Hiroshi YOSHIDA, Yoshiyuki TAODA, Brian Alvin JOHNS, Takashi KAWASUJI, Daiki NAGAMATSU
  • Patent number: 8816071
    Abstract: Compositions of matter including (R)-2,5,6,8-tetramethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine and (R)-2,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine are disclosed herein. Further disclosed are methods of preparation of such compounds and the use of such compounds as anticancer agents.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: August 26, 2014
    Assignee: First Tech International Limited
    Inventors: Khalid A. El Sayed, Paul W. Sylvester, Fathy A. Behery
  • Publication number: 20140221356
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Haolun JIN, Scott E. LAZERWITH, Teresa Alejandra TREJO MARTIN, Elizabeth M. BACON, Jeromy J. COTTELL, Zhenhong R. CAI, Hyung-Jung PYUN, Philip Anthony MORGANELLI, Mingzhe JI, James G. TAYLOR, Xiaowu CHEN, Michael R. MISH, Manoj C. DESAI
  • Publication number: 20140221355
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, Z2, or Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Scott E. LAZERWITH, Haolun JIN, Hyung-Jung Pyun
  • Publication number: 20140213571
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 20, 2012
    Publication date: July 31, 2014
    Inventors: Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
  • Publication number: 20140213553
    Abstract: This invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor.
    Type: Application
    Filed: May 3, 2012
    Publication date: July 31, 2014
    Applicant: CONCERT PHARMACEUTICALS INC.
    Inventor: Adam Morgan
  • Publication number: 20140200344
    Abstract: Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a L2a, L3a and na are as defined in the description.
    Type: Application
    Filed: August 10, 2012
    Publication date: July 17, 2014
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
  • Publication number: 20140200209
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.
    Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
  • Patent number: 8754214
    Abstract: A synthesis approach providing an early ring attachment via a bromination to compound I-I yielding compound II-II: whereby a final product such as AA: can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: June 17, 2014
    Assignees: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Hiroshi Yoshida, Yoshiyuki Taoda, Brian Alvin Johns, Takashi Kawasuji, Daiki Nagamatsu
  • Publication number: 20140023665
    Abstract: The invention relates to novel maytansinoid compounds having sulfoxide linkers and more specifically to novel maytansinoid compounds of structural formula (I) and (II). The invention also provides conjugates of the maytansinoid compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
    Type: Application
    Filed: March 20, 2012
    Publication date: January 23, 2014
    Applicant: IMMUNOGEN, INC.
    Inventor: Nathan Fishkin
  • Publication number: 20140011995
    Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R4d is a lower alkyl optionally substituted with substituent E, or the like; and R6d is a lower alkyl group optionally substituted with substituent group E, or the like].
    Type: Application
    Filed: August 4, 2011
    Publication date: January 9, 2014
    Inventors: Yukihito Sumino, Moriyasu Masui, Diasuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
  • Patent number: 8624023
    Abstract: A synthesis approach providing an early ring attachment via a bromination to compound I-I yielding compound II-II: whereby a final product such as AA: can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: January 7, 2014
    Assignees: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Hiroshi Yoshida, Yoshiyuki Taoda, Brian Johns, Takashi Kawasuji, Daiki Nagamatsu
  • Publication number: 20140005185
    Abstract: The present invention provides an imidazooxazine compound represented by Formula (I) or a salt thereof, wherein A, B, C, and D are as defined in the specification.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 2, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masayuki Nakamura, Kenji Niiyama, Kaori Kamijo, Mitsuru Ohkubo, Toshiyasu Shimomura
  • Publication number: 20130338134
    Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
    Type: Application
    Filed: June 12, 2013
    Publication date: December 19, 2013
    Inventors: Liangxing Wu, Colin Zhang, Chunhong He, Yaping Sun, Liang Lu, Ding-Quan Qian, Meizhong Xu, Jincong Zhuo, Wenqing Yao
  • Patent number: 8569295
    Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: October 29, 2013
    Assignee: Merck Patent GmbH
    Inventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
  • Patent number: 8557982
    Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: October 15, 2013
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
  • Publication number: 20130225549
    Abstract: The present invention relates to dihydropteridinones, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 29, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventor: Boehringer Ingelheim International GmbH
  • Publication number: 20130172551
    Abstract: The present invention relates to the preparation of carbamoylpyridone derivatives and intermediates.
    Type: Application
    Filed: March 22, 2011
    Publication date: July 4, 2013
    Inventors: Steven N. Goodman, Huan Wang, Douglas Matthew Mans
  • Publication number: 20130165435
    Abstract: Compositions of matter including (R)-2,5,6,8-tetramethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine and (R)-2,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine are disclosed herein. Further disclosed are methods of preparation of such compounds and the use of such compounds as anticancer agents.
    Type: Application
    Filed: November 30, 2012
    Publication date: June 27, 2013
    Inventors: Khalid A. El Sayed, Paul W. Sylvester, Fathy A. Behery
  • Publication number: 20130096109
    Abstract: An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Application
    Filed: April 11, 2011
    Publication date: April 18, 2013
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Kazunari Hattori, Kenji Tomita