Patents by Inventor Jun Niijima

Jun Niijima 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).

  • Patent number: 8530654
    Abstract: Crystals, amorphous substances, salts, and hydrates of a salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid having PDE4 inhibitory action are provided. These compounds are useful for treating allergic diseases such as atopic dermatitis.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: September 10, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Eiichi Yamamoto, Osamu Asano, Jun Niijima, Kazumasa Nara
  • Patent number: 8492543
    Abstract: [4-(3-aminophenyl)-6,7-dimethoxyquinazolin-2-yl]methylamine with a favorable yield and high purity can be produced by subjecting a compound represented by the following formula (I) to a step of reacting with methylamine and a step of deprotection if desired: wherein L represents a protective group of amino.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: July 23, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Jun Niijima
  • Patent number: 8410277
    Abstract: It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): the method including reacting a compound represented by the following formula (III): and a compound represented by the following formula (II): in a solvent and in the presence of a palladium catalyst and a base, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group that may be protected with a protective group, etc.; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.
    Type: Grant
    Filed: December 25, 2008
    Date of Patent: April 2, 2013
    Assignee: Eisai R&D Managment Co., Ltd.
    Inventors: Jun Niijima, Kazuhiro Yoshizawa, Yuki Kosaka, Shinya Abe
  • Patent number: 8058444
    Abstract: There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as process for producing the same.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: November 15, 2011
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Jun Niijima, Kazutaka Nakamoto, Masayuki Matsukura, Keigo Tanaka, Eiichi Yamamoto, Takuma Minamisono
  • Publication number: 20110263845
    Abstract: It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): the method including reacting a compound represented by the following formula (III): and a compound represented by the following formula (II): in a solvent and in the presence of a palladium catalyst and a base, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group that may be protected with a protective group, etc.; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.
    Type: Application
    Filed: December 25, 2008
    Publication date: October 27, 2011
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Jun Niijima, Kazuhiro Yoshizawa, Yuki Kosaka, Shinya Abe
  • Publication number: 20110152521
    Abstract: [4-(3-aminophenyl)-6,7-dimethoxyquinazolin-2-yl]methylamine with a favorable yield and high purity can be produced by subjecting a compound represented by the following formula (I) to a step of reacting with methylamine and a step of deprotection if desired: wherein L represents a protective group of amino.
    Type: Application
    Filed: August 15, 2008
    Publication date: June 23, 2011
    Applicant: Eisai R&D Management Co., Ltd.
    Inventor: Jun Niijima
  • 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
  • Patent number: 7803949
    Abstract: An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: September 28, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Manabu Sasho, Keizo Sato, Jun Niijima, Mamoru Miyazawa, Shigeto Negi, Atsushi Kamada
  • 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: 20090192316
    Abstract: An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.
    Type: Application
    Filed: December 20, 2006
    Publication date: July 30, 2009
    Inventors: Manabu Sasho, Keizo Sato, Jun Niijima, Mamoru Miyazawa, Shigeto Negi, Atsushi Kamada
  • 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: 20090062539
    Abstract: Crystals, amorphous substances, salts, and hydrates of salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid have PDE4 inhibitory action and are useful for treating allergic diseases such as atopic dermatitis.
    Type: Application
    Filed: February 15, 2008
    Publication date: March 5, 2009
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Eiichi YAMAMOTO, Osamu Asano, Jun Niijima, Kazumasa Nara, Kazuki Miyazaki
  • 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: 20080275244
    Abstract: There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as process for producing the same.
    Type: Application
    Filed: April 25, 2008
    Publication date: November 6, 2008
    Inventors: Jun Niijima, Kazutaka Nakamoto, Masayuki Matsukura, Keigo Tanaka, Eiichi Yamamoto, Takuma Minamisono
  • 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
  • Publication number: 20080227815
    Abstract: A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)-ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13C solid NMR spectrum.
    Type: Application
    Filed: May 11, 2006
    Publication date: September 18, 2008
    Inventors: Takahisa Sakaguchi, Yuichi Suzuki, Koichi Ito, Jun Niijima, Mamoru Miyazawa, Toshikazu Shimizu, Masaharu Gotoda, Naoko Suzuki, Takashi Hasebe