Patents by Inventor Kozo Akasaka

Kozo Akasaka 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: 20100093842
    Abstract: The present invention provides compounds having formula I: and pharmaceutically acceptable derivatives thereof, wherein R1-R10, q, t, X0, X1, A, B, D, E, G, J, K, L, M and Z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders associated with cellular hyperproliferation.
    Type: Application
    Filed: August 26, 2009
    Publication date: April 15, 2010
    Inventors: Brian M. Gallagher, JR., Charles Johannes, Xiang-Yi Li, Marc Pesant, Hongjuan Zhao, Kozo Akasaka, Francis G. Fang
  • Publication number: 20090291998
    Abstract: The present invention provides compounds having formula (1): wherein R1-R6, A, J, D, A, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.
    Type: Application
    Filed: March 3, 2009
    Publication date: November 26, 2009
    Inventors: Sergei Agoulnik, Kozo Akasaka, Francis Fang, Jean-Christophe Harmange, Lynn Hawkins, Yimin Jiang, Charles Johannes, Xiang-Yi Li, Pamela McGuinness, Erin A. Murphy, Shawn Schiller, Mary Vermeulen, Jiayi Wu
  • Patent number: 7524883
    Abstract: The present invention provides compounds having formula (1): wherein R1-R6, A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.
    Type: Grant
    Filed: January 8, 2003
    Date of Patent: April 28, 2009
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Sergei Agoulnik, Kozo Akasaka, Frank Fang, Jean-Christophe Harmange, Lynn Hawkins, Yimin Jiang, Charles Johannes, Xiang-Yi Li, Pamela McGuiness, Erin A. Murphy, Shawn Schiller, Mary Vermeulen, Jiayi Wu
  • Publication number: 20070287745
    Abstract: The present invention provides compounds having formula I: and pharmaceutically acceptable derivatives thereof, wherein R1-R10, q, t, X0, X1, A, B, D, E, G, J, K, L, M and Z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders associated with cellular hyperproliferation.
    Type: Application
    Filed: September 22, 2004
    Publication date: December 13, 2007
    Inventors: Brian Gallagher Jr, Charles Johannes, Xiang-Yi Li, Marc Pesant, Hongjuan Zhao, Kozo Akasaka, Francis Fang
  • Publication number: 20050101781
    Abstract: The present invention provides compounds haviang formula (1): wherein R1-R6, A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.
    Type: Application
    Filed: January 8, 2003
    Publication date: May 12, 2005
    Inventors: Sergei Agoulnik, Kozo Akasaka, Francis Fang, Jean-Christophe Harmange, Lynn Hawkins, Yimin Jiang, Charles Johannes, Xiang-Yi Li, Pamela McGuinness, Erin Murphy, Shawn Schiller, Mary Vermeulen, Jiayi Wu
  • Patent number: 6281214
    Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R1, R2, R3, R4, and R5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: August 28, 2001
    Assignee: Eisai Co., Ltd
    Inventors: Kozo Akasaka, Masahiro Yonaga, Akiharu Kajiwara, Kunizo Higurashi, Kohshi Ueno, Satoshi Nagato, Makoto Komatsu, Noritaka Kitazawa, Masataka Ueno, Yoshiharu Yamanishi, Yoshimasa Machida, Yuki Komatsu, Naoyuki Shimomura, Norio Minami, Toshikazu Shimizu, Atsushi Nagaoka
  • Patent number: 5849912
    Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.
    Type: Grant
    Filed: May 12, 1997
    Date of Patent: December 15, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Kozo Akasaka, Masahiro Yonaga, Akiharu Kajiwara, Kunizo Higurashi, Kohshi Ueno, Satoshi Nagato, Makoto Komatsu, Noritaka Kitazawa, Masataka Ueno, Yoshiharu Yamanishi, Yoshimasa Machida, Yuki Komatsu, Naoyuki Shimomura, Norio Minami, Toshikazu Shimizu, Atsushi Nagaoka
  • Patent number: 5668136
    Abstract: A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.
    Type: Grant
    Filed: September 11, 1991
    Date of Patent: September 16, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Teiji Kimura, Nobuhisa Watanabe, Yasutaka Takase, Kenji Hayashi, Makoto Matsui, Hironori Ikuta, Youji Yamagishi, Kozo Akasaka, Hiroshi Tanaka, Issei Ohtsuka, Takao Saeki, Motoji Kogushi, Tohru Fujimori, Isao Saito
  • Patent number: 5475014
    Abstract: An oxazolidone derivative represented by formula (I) which has a monoamine oxidase inhibition effect: ##STR1## {wherein A and B each represents a nitrogen atom, a sulfur atom or an oxygen atom, with the proviso than at least one of A and B must be a nitrogen atom,R.sup.1 represents a group of the formula: ##STR2## (in which n and m each represents 0 or an integer of 1 to 4, and R.sup.3 and R.sup.4 each represents a hydrogen atom, a hydroxyl group, a lower alkyl group, etc. ), a group represented by the formula: ##STR3## (in which p and q each represents 0 or an integer of 1 to 4 and X represents an oxygen atom, sulfur atom, etc.) and a group represented by the formula: ##STR4## R.sup.2 represents a hydrogen atom or a lower alkyl group}.
    Type: Grant
    Filed: March 8, 1994
    Date of Patent: December 12, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Kozo Akasaka, Akiharu Kajiwara, Satoshi Nagato, Youichi Iimura, Ichirou Yoshida, Atsushi Sasaki, Masanori Mizuno, Atsuhiko Kubota, Takaki Kagaya, Mariko Komatsu
  • Patent number: 5206403
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime either derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COR6, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: April 27, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 5182301
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.
    Type: Grant
    Filed: February 21, 1991
    Date of Patent: January 26, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 5103010
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: April 7, 1992
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 5064848
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.
    Type: Grant
    Filed: May 4, 1990
    Date of Patent: November 12, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 5034418
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--N4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: July 23, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 4978767
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: December 18, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 4954523
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower aralalkyl, --CH2--NHSO3--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: September 4, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 4929623
    Abstract: A benzothiazol compound having the formula is disclosed and is effective to inhibit the production of leukotriene. It is useful against allergy, asthma, affections of the skin, allergic rhinitis and affection of a cardiovascular system. ##STR1## in which R20 is ester or amide and --NR5R6 is amino in variety.
    Type: Grant
    Filed: June 16, 1988
    Date of Patent: May 29, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Shinya Abe, Mitsuaki Miyamoto, Masayuki Tanaka, Kozo Akasaka, Kenji Hayashi, Tetsuya Kawahara, Satoshi Katayama, Yoshinori Sakuma, Takeshi Suzuki, Isao Yamatsu
  • Patent number: 4886834
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(C.dbd.
    Type: Grant
    Filed: March 11, 1987
    Date of Patent: December 12, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 4833160
    Abstract: 3-(3,5-di-tert-butyl-4-hydroxy-benzylidene)-2-pyrrolidone and N-substituted derivatives thereof are described. The substituent includes alkyl, alkoxy, alkynyl phenyl-alkylene, hydroxy-alkylene and amino-alkylene. They are effective as an anti-inflammatory, analgesic and antithermic agent, and they have a low toxicity.
    Type: Grant
    Filed: April 23, 1986
    Date of Patent: May 23, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Hironori Ikuta, Youji Yamagishi, Kozo Akasaka, Isao Yamatsu, Seiichi Kobayashi, Hiroshi Shirota, Kouichi Katayama
  • Patent number: 4433159
    Abstract: Optically active alpha-tocopherol is synthesized by a multi-step process using phytol as a starting material. The process does not require an optical resolution step.
    Type: Grant
    Filed: February 18, 1982
    Date of Patent: February 21, 1984
    Assignee: Eisai Co., Ltd.
    Inventors: Kimio Hamamura, Kozo Akasaka, Youji Yamagishi