Three Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 544/95)
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Patent number: 11958864Abstract: 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: GrantFiled: February 14, 2022Date of Patent: April 16, 2024Assignee: Merck Sharp & Dohme LLCInventors: Timothy John Hartingh, John A. McCauley, Tao Yu, Yonglian Zhang
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Patent number: 11202780Abstract: 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: GrantFiled: January 10, 2020Date of Patent: December 21, 2021Assignee: Gilead Sciences, Inc.Inventors: Ernest A. Carra, Irene Chen, Katie Ann Keaton, Scott E. Lazerwith, Vahid Zia
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Patent number: 10457690Abstract: 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: GrantFiled: June 3, 2016Date of Patent: October 29, 2019Assignee: 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
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Patent number: 10385067Abstract: 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: GrantFiled: June 15, 2017Date of Patent: August 20, 2019Assignee: Gilead Sciences, Inc.Inventors: Ernest A. Carra, Irene Chen, Vahid Zia
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Patent number: 10323044Abstract: 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: GrantFiled: February 26, 2016Date of Patent: June 18, 2019Assignee: Taiho Pharmaceutical Co., Ltd.Inventor: Masaya Hashimoto
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Patent number: 10301321Abstract: The present invention relates to a novel process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof using novel intermediates.Type: GrantFiled: November 10, 2017Date of Patent: May 28, 2019Assignee: LAURUS LABS LIMITEDInventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Lakshmi Narasimha Dammalapati, Mani Bushan Kotala, Ravindra Aduri
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Patent number: 10202404Abstract: 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: GrantFiled: May 24, 2018Date of Patent: February 12, 2019Assignee: SHIONOGI & CO., LTD.Inventors: Tomokazu Yoshinaga, Kouhei Nodu
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Patent number: 10098886Abstract: 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: GrantFiled: May 5, 2017Date of Patent: October 16, 2018Assignee: GILEAD SCIENCES, INC.Inventors: Ernest A. Carra, Irene Chen, Katie Ann Keaton, Scott E. Lazerwith, Vahid Zia
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Patent number: 10087193Abstract: The present disclosure relates to novel crystalline dolutegravir sodium Form-M2, Form-M3, Form-M4 and process for the preparation thereof.Type: GrantFiled: February 4, 2015Date of Patent: October 2, 2018Assignee: Mylan Laboratories LimitedInventors: Ramakoteswara Rao Jetti, Satish Beeravelly, Madhu Murthy Nadella, Haribabu Nandipati
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Patent number: 10011613Abstract: 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: GrantFiled: August 21, 2015Date of Patent: July 3, 2018Assignee: SHIONOGI & CO., LTD.Inventors: Tomokazu Yoshinaga, Kouhei Nodu
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Patent number: 9994588Abstract: 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: GrantFiled: February 26, 2016Date of Patent: June 12, 2018Assignee: Taiho Pharmaceutical Co., Ltd.Inventor: Masaya Hashimoto
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Patent number: 9938296Abstract: The present invention relates to the preparation of carbamoylpyridone derivatives such as the compound of formula (VIIIa):Type: GrantFiled: March 31, 2017Date of Patent: April 10, 2018Assignee: VIIV Healthcare CompanyInventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
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Patent number: 9856271Abstract: The present invention relates to a novel process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof using novel intermediates.Type: GrantFiled: January 20, 2015Date of Patent: January 2, 2018Assignee: LAURUS LABS LIMITEDInventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Lakshmi Narasimha Dammalapati, Mani Bushan Kotala, Ravindra Aduri
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Patent number: 9708342Abstract: 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: GrantFiled: June 19, 2015Date of Patent: July 18, 2017Assignee: Gilead Sciences, Inc.Inventors: Ernest A. Carra, Irene Chen, Vahid Zia
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Patent number: 9682084Abstract: 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: GrantFiled: June 19, 2015Date of Patent: June 20, 2017Assignee: Gilead Sciences, Inc.Inventors: Ernest A. Carra, Irene Chen, Katie Ann Keaton, Scott E. Lazerwith, Vahid Zia
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Patent number: 9242986Abstract: 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: GrantFiled: May 8, 2014Date of Patent: January 26, 2016Assignees: SHIONOGI & CO., LTD., ViiV Healthcare CompanyInventors: Takashi Kawasuji, Daiki Nagamatsu
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Patent number: 9206197Abstract: An amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.Type: GrantFiled: September 2, 2012Date of Patent: December 8, 2015Assignee: MAPI PHARMA LTD.Inventors: Ehud Marom, Shai Rubnov
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Patent number: 9200009Abstract: 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: GrantFiled: October 12, 2012Date of Patent: December 1, 2015Assignee: SHIONOGI & CO., LTD.Inventor: Toshiyuki Akiyama
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Patent number: 9120817Abstract: 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: GrantFiled: October 14, 2014Date of Patent: September 1, 2015Assignee: VIIV HEALTHCARE COMPANYInventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
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Publication number: 20150141415Abstract: 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: ApplicationFiled: November 7, 2014Publication date: May 21, 2015Inventors: Omonike Arike Olaleye, Sarah Finney John, Adaugo Chimzurum Isichei, Jun O Liu, Rosa Maldonado, Janice Endsley
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Publication number: 20150105551Abstract: 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: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Rok GRAHEK, Darko KOCJAN, Andrej BASTARDA, Andrej KOCIJAN, Matjaz KRACUN
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Publication number: 20150065485Abstract: 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: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20150057444Abstract: The present invention relates to the preparation of carbamoylpyridone derivatives and intermediates.Type: ApplicationFiled: October 14, 2014Publication date: February 26, 2015Inventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
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Publication number: 20150038702Abstract: 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: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Inventors: Yukihito SUMINO, Moriyasu MASUI, Diasuke YAMADA, Fumiya IKARASHI, Kazuya OKAMOTO
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Publication number: 20150031876Abstract: 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: ApplicationFiled: September 5, 2014Publication date: January 29, 2015Applicant: Shionogi & Co., Ltd.Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
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Publication number: 20150025067Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.Type: ApplicationFiled: February 13, 2013Publication date: January 22, 2015Applicant: CHILDREN'S HOSPITAL MEDICAL CENTERInventors: Yi Zheng, Prakash Jagtap, Emily E. Bosco, Jaroslaw Meller, Marie-Dominique Filippi
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Publication number: 20150018298Abstract: 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: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
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Publication number: 20140350004Abstract: 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: ApplicationFiled: September 2, 2012Publication date: November 27, 2014Applicant: MAPI PHARMA LTD.Inventors: Ehud Marom, Shai Rubnov
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Publication number: 20140329808Abstract: 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: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Inventors: Khalid A. El Sayed, Paul W. Sylvester, Fathy A. Behery
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Publication number: 20140256937Abstract: 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: ApplicationFiled: October 12, 2012Publication date: September 11, 2014Applicant: SHIONOGI & CO., LTD.Inventor: Toshiyuki Akiyama
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Publication number: 20140243521Abstract: 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: ApplicationFiled: May 8, 2014Publication date: August 28, 2014Applicants: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Hiroshi YOSHIDA, Yoshiyuki TAODA, Brian Alvin JOHNS, Takashi KAWASUJI, Daiki NAGAMATSU
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Patent number: 8816071Abstract: 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: GrantFiled: November 30, 2012Date of Patent: August 26, 2014Assignee: First Tech International LimitedInventors: Khalid A. El Sayed, Paul W. Sylvester, Fathy A. Behery
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Publication number: 20140221356Abstract: 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: ApplicationFiled: December 19, 2013Publication date: August 7, 2014Inventors: 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
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Publication number: 20140221355Abstract: 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: ApplicationFiled: December 19, 2013Publication date: August 7, 2014Inventors: Scott E. LAZERWITH, Haolun JIN, Hyung-Jung Pyun
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Publication number: 20140213571Abstract: 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: ApplicationFiled: August 20, 2012Publication date: July 31, 2014Inventors: 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
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Publication number: 20140213553Abstract: 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: ApplicationFiled: May 3, 2012Publication date: July 31, 2014Applicant: CONCERT PHARMACEUTICALS INC.Inventor: Adam Morgan
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Publication number: 20140200209Abstract: 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: ApplicationFiled: March 14, 2014Publication date: July 17, 2014Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
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Publication number: 20140200344Abstract: 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: ApplicationFiled: August 10, 2012Publication date: July 17, 2014Applicant: Nissan Chemical Industries, Ltd.Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
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Patent number: 8754214Abstract: 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: GrantFiled: December 4, 2013Date of Patent: June 17, 2014Assignees: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Hiroshi Yoshida, Yoshiyuki Taoda, Brian Alvin Johns, Takashi Kawasuji, Daiki Nagamatsu
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Publication number: 20140023665Abstract: 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: ApplicationFiled: March 20, 2012Publication date: January 23, 2014Applicant: IMMUNOGEN, INC.Inventor: Nathan Fishkin
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Publication number: 20140011995Abstract: 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: ApplicationFiled: August 4, 2011Publication date: January 9, 2014Inventors: Yukihito Sumino, Moriyasu Masui, Diasuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
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Patent number: 8624023Abstract: 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: GrantFiled: December 8, 2009Date of Patent: January 7, 2014Assignees: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Hiroshi Yoshida, Yoshiyuki Taoda, Brian Johns, Takashi Kawasuji, Daiki Nagamatsu
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Publication number: 20140005185Abstract: 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: ApplicationFiled: April 5, 2012Publication date: January 2, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Masayuki Nakamura, Kenji Niiyama, Kaori Kamijo, Mitsuru Ohkubo, Toshiyasu Shimomura
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Publication number: 20130338134Abstract: 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: ApplicationFiled: June 12, 2013Publication date: December 19, 2013Inventors: Liangxing Wu, Colin Zhang, Chunhong He, Yaping Sun, Liang Lu, Ding-Quan Qian, Meizhong Xu, Jincong Zhuo, Wenqing Yao
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Patent number: 8569295Abstract: 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: GrantFiled: July 28, 2010Date of Patent: October 29, 2013Assignee: Merck Patent GmbHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
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Patent number: 8557982Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.Type: GrantFiled: August 13, 2012Date of Patent: October 15, 2013Assignee: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20130225549Abstract: 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: ApplicationFiled: February 14, 2013Publication date: August 29, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Boehringer Ingelheim International GmbH
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Publication number: 20130172551Abstract: The present invention relates to the preparation of carbamoylpyridone derivatives and intermediates.Type: ApplicationFiled: March 22, 2011Publication date: July 4, 2013Inventors: Steven N. Goodman, Huan Wang, Douglas Matthew Mans
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Publication number: 20130165435Abstract: 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: ApplicationFiled: November 30, 2012Publication date: June 27, 2013Inventors: Khalid A. El Sayed, Paul W. Sylvester, Fathy A. Behery
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Publication number: 20130096109Abstract: 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: ApplicationFiled: April 11, 2011Publication date: April 18, 2013Applicant: SHIONOGI & CO., LTD.Inventors: Kazunari Hattori, Kenji Tomita