Patents by Inventor Yoshihiko Kotake

Yoshihiko Kotake has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20190100513
    Abstract: The present disclosure provides a novel solid state form of pladienolide pyridine compounds, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.
    Type: Application
    Filed: November 17, 2016
    Publication date: April 4, 2019
    Inventors: Gregg F. Keaney, John Wang, Baudouin Gerard, Kenzo Arai, Xiang Liu, Guo Zhu Zheng, Kazunobu Kira, Parcharee Tivitmahaisoon, Sudeep Prajapati, Nicholas C. Gearhart, Yoshihiko Kotake, Satoshi Nagao, Regina Mikie Kanada Sonobe, Masayuki Miyano, Norio Murai, Silvia Buonamici, Lihua Yu, Eunice Sun Park, Betty Chan, Peter G. Smith, Michael P. Thomas, Ermira Pazolli, Kian Huat Lim, Atsushi Endo, Arani Chanda
  • Patent number: 9481669
    Abstract: The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.
    Type: Grant
    Filed: May 13, 2015
    Date of Patent: November 1, 2016
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Gregg F. Keaney, John Wang, Baudouin Gerard, Kenzo Arai, Xiang Liu, Guo Zhu Zheng, Kazunobu Kira, Parcharee Tivitmahaisoon, Sudeep Prajapati, Nicholas C. Gearhart, Yoshihiko Kotake, Satoshi Nagao, Regina Mikie Kanada Sonobe, Masayuki Miyano, Norio Murai, Silvia Buonamici, Lihua Yu, Eunice Sun Park, Betty Chan, Peter G. Smith, Michael P. Thomas, Ermira Pazolli, Kian Huat Lim
  • Publication number: 20150329528
    Abstract: The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.
    Type: Application
    Filed: May 13, 2015
    Publication date: November 19, 2015
    Inventors: Gregg F. Keaney, John Wang, Baudouin Gerard, Kenzo Arai, Xiang Liu, Guo Zhu Zheng, Kazunobu Kira, Parcharee Tivitmahaisoon, Sudeep Prajapati, Nicholas C. Gearhart, Yoshihiko Kotake, Satoshi Nagao, Regina Mikie Kanada Sonobe, Masayuki Miyano, Norio Murai
  • Patent number: 7893068
    Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: February 22, 2011
    Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.
    Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
  • Patent number: 7884128
    Abstract: Process for producing compound of Formula: wherein P2, P3 and R2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein P3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein P2 means a protecting group for hydroxy group; and R2 means a phenyl group which may be substituted, in the presence of a base.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: February 8, 2011
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Regina Mikie Kanada, Daisuke Ito, Takashi Sakai, Naoki Asai, Yoshihiko Kotake, Jun Niijima
  • Patent number: 7816401
    Abstract: A process for producing a compound represented by Formula (11): wherein P1, P7, P8, P9 and R1 are the same as defined herein, characterized by including reacting a compound represented by Formula (12): with a compound represented by Formula (13): in the presence of a catalyst.
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: October 19, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Regina Mikie Kanada, Daisuke Ito, Takashi Sakai, Naoki Asai, Yoshihiko Kotake, Jun Niijima
  • Publication number: 20100204490
    Abstract: Process for producing compound of Formula: wherein P2, P3 and R2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein P3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein P2 means a protecting group for hydroxy group; and R2 means a phenyl group which may be substituted, in the presence of a base.
    Type: Application
    Filed: April 21, 2010
    Publication date: August 12, 2010
    Inventors: Regina Mikie KANADA, Daisuke Ito, Takashi Sakai, Naoki Asai, Yoshihiko Kotake, Jun Niijima
  • Patent number: 7667052
    Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it.
    Type: Grant
    Filed: August 30, 2005
    Date of Patent: February 23, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yoshiharu Mizui, Takashi Sakai, Satoshi Yamamoto, Keisuke Komeda, Masanori Fujita, Akifumi Okuda, Kumiko Kishi, Jun Niijima, Mitsuo Nagai, Kiyoshi Okamoto, Masao Iwata, Yoshihiko Kotake, Toshimitsu Uenaka, Naoki Asai, Motoko Matsufuji, Tomohiro Sameshima, Naoto Kawamura, Kazuyuki Dobashi, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Susumu Takeda, Tomonari Yamada, Koji Norihisa, Takao Yamori
  • Patent number: 7619100
    Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: November 17, 2009
    Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.
    Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
  • Publication number: 20090227795
    Abstract: A method of measuring the binding activity of a test compound to a splicing factor 3b (SF3b), which comprises the following steps of: (a) contacting a labeled pladienolide compound and a test compound with a cell or a cell fraction; and (b) measuring the distribution of the bound labeled compound. The method enables to screen for a novel active compound capable of acting on (binding to) a pladienolide target molecule or the like.
    Type: Application
    Filed: August 2, 2007
    Publication date: September 10, 2009
    Applicant: Eisai R & D Management Co., Ltd.
    Inventors: Yoshihiko Kotake, Koji Sagane, Takashi Owa, Yoshiharu Mizui, Hajime Shimizu, Yuko Kiyosue
  • Patent number: 7550503
    Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
    Type: Grant
    Filed: June 23, 2006
    Date of Patent: June 23, 2009
    Assignees: Eisai R& D Management Co., Ltd., Merican Corporation
    Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
  • Publication number: 20090030023
    Abstract: A compound represented by the following formula (I), a salt, or a solvate thereof: wherein, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a non-aromatic heterocyclic group, an aromatic hydrocarbon cyclic group, an aromatic heterocyclic group, an acyl group or an alkylsulfonyl group all of which may be substituted and wherein one, or both, of R1 or R2 is an aromatic, or non-aromatic, heterocyclic group which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, an aromatic heterocyclic group, a nitrogen atom, an oxygen atom or a sulfur atom all of which may be substituted if possible; and R4 is a pyridyl group which may be substituted.
    Type: Application
    Filed: March 24, 2008
    Publication date: January 29, 2009
    Inventors: Hitoshi Harada, Masato Ueda, Yoshihiko Kotake, Masahiro Yasuda, Daisuke Iida, Junichi Nagakawa, Makoto Nakagawa
  • Publication number: 20080275059
    Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
    Type: Application
    Filed: October 29, 2007
    Publication date: November 6, 2008
    Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
  • Publication number: 20080255146
    Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
    Type: Application
    Filed: October 29, 2007
    Publication date: October 16, 2008
    Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
  • Patent number: 7396836
    Abstract: A compound having excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, R1 and R2, same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an aromatic hydrocarbon cyclic group, an acyl group or an alkylsulfonyl group, which groups may be substituted (except the hydrogen atom); R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, a nitrogen atom, an oxygen atom or a sulfur atom, which groups may be substituted (except the hydrogen atom, the halogen atom and the cyano group); R4 represents an aromatic hydrocarbon cyclic group which may be substituted, and R5 represents an aromatic hydrocarbon cyclic group which may be substituted.
    Type: Grant
    Filed: October 22, 2002
    Date of Patent: July 8, 2008
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Hitoshi Harada, Masato Ueda, Yoshihiko Kotake, Masahiro Yasuda, Daisuke Iida, Junichi Nagakawa, Makoto Nakagawa
  • Publication number: 20080021226
    Abstract: [Problems to be Solved] To provide an effective process for total synthesis of pladienolide B and pladienolide D having excellent anti-tumor activity and to provide useful intermediates in the above-described process. [Measure for Solving the Problem] A process for producing a compound represented by Formula (11): wherein P1, P7, P8, P9 and R1 are the same as defined below, characterized by including reacting a compound represented by Formula (12): wherein P7 means a hydrogen atom or a protecting group for hydroxy group; R1 means a hydrogen atom or a hydroxy group, with a compound represented by Formula (13): wherein P1 means a hydrogen atom or a protecting group for hydroxy group; P8 means a hydrogen atom, an acetyl group or a protecting group for hydroxy group; P9 means a hydrogen atom or a protecting group for hydroxy group; or P8 and P9 may form together a group represented by a formula: wherein R5 means a phenyl group which may have a substituent, in the presence of a catalyst.
    Type: Application
    Filed: October 13, 2006
    Publication date: January 24, 2008
    Inventors: Regina Kanada, Daisuke Ito, Takashi Sakai, Naoki Asai, Yoshihiko Kotake, Jun Niijima
  • Patent number: 7256178
    Abstract: Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R3, R7, R16, R17, R20, R21 and R21? are the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: August 14, 2007
    Assignees: Eisai Co., Ltd., Mercian Corporation
    Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Susumu Takeda, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Tomohiro Sameshima
  • Patent number: 7189717
    Abstract: The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: March 13, 2007
    Assignee: Eisai Co., Ltd.
    Inventors: Masahiro Yasuda, Hitoshi Harada, Shuhei Miyazawa, Seiichi Kobayashi, Kokichi Harada, Takayuki Hida, Hisashi Shibata, Nobuyuki Yasuda, Osamu Asano, Yoshihiko Kotake
  • Publication number: 20070054876
    Abstract: The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.
    Type: Application
    Filed: November 8, 2006
    Publication date: March 8, 2007
    Inventors: Masahiro Yasuda, Hitoshi Harada, Shuhei Miyazawa, Seiichi Kobayashi, Kokichi Harada, Takayuki Hida, Hisashi Shibata, Nobuyuki Yasuda, Osamu Asano, Yoshihiko Kotake
  • Patent number: 7160892
    Abstract: The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of both: (1) wherein R1 and R2 are each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a C6-14 aromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, C1-6 acyl, or C1-6 alkylsulfonyl; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; R4 is a C6-14 aromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and R5 is a C6-14 aromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).
    Type: Grant
    Filed: October 22, 2002
    Date of Patent: January 9, 2007
    Assignee: Eisai Co., Ltd.
    Inventors: Hitoshi Harada, Osamu Asano, Masato Ueda, Shuhei Miyazawa, Yoshihiko Kotake, Yasuhiro Kabasawa, Masahiro Yasuda, Nobuyuki Yasuda