Patents by Inventor Shiro Akinaga
Shiro Akinaga 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).
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Patent number: 6376687Abstract: Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.Type: GrantFiled: January 24, 2000Date of Patent: April 23, 2002Assignees: Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.Inventors: Pui-Kai Li, Chikara Murakata, Shiro Akinaga
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Publication number: 20020028912Abstract: The present invention relates to a chemically modified polypeptide in which at least one of hydroxyl groups in the polypeptide molecule is modified with a polyalkylene glycol derivative; a method for producing the modified polypeptide; a method of treatment using the modified polypeptide; use of the modified polypeptide; a pharmaceutical preparation comprising the modified polypeptide; and a composition for treatment comprising the modified polypeptide.Type: ApplicationFiled: February 3, 1999Publication date: March 7, 2002Inventors: MOTOO YAMASAKI, TOSHIYUKI SUZAWA, KEN KOBAYASHI, NOBORU KONISHI, SHIRO AKINAGA, KUMIKO MARUYAMA
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Patent number: 6316491Abstract: Radioicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 (wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl, and the like; R7 represents hydroxyl, substituted lower alkyl, and the like), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, and the like), and the like) and the like; X represents halogen or is combined together with R4 to represent a single bond; and R4 is combined together with X to represent a single bond, or represents hydrogen, alkanoyl, and the like.Type: GrantFiled: June 24, 1998Date of Patent: November 13, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
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Publication number: 20010027208Abstract: Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: 1Type: ApplicationFiled: February 26, 2001Publication date: October 4, 2001Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
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Patent number: 6288050Abstract: Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.Type: GrantFiled: January 25, 1999Date of Patent: September 11, 2001Assignees: Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.Inventors: Pui-Kai Li, Chikara Murakata, Shiro Akinaga
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Patent number: 6262043Abstract: Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I): (wherein R1 represents hydroxy, alkoxy, or NR2R3 (wherein R2 and R3 are the same or different, and each represents hydrogen, straight-chain lower alkyl having 1 to 3 carbon atoms, or branched-chain lower alkyl having 3 to 8 carbon atoms)), or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 13, 2000Date of Patent: July 17, 2001Assignees: Kyowa Hakko Kogyo Co., Ltd., Duquesne University of the Holy GhostInventors: Yoji Ino, Nobuyoshi Amishiro, Taisuke Nakata, Hiroyuki Ishida, Shiro Akinaga, Chikara Murakata, Pui-Kai Li
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Patent number: 6239168Abstract: Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 {wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl; R7 represents hydroxyl, substituted lower alkyl), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, X represents halogen.Type: GrantFiled: February 25, 2000Date of Patent: May 29, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
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Patent number: 5977165Abstract: The present invention relates to radicicol derivatives represented by the following formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; (1) when X represents halogen, Y represents an oxygen atom or R.sup.4 --O--N (wherein R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl); and R.sup.3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R.sup.3 are combined with each other to represent a single bond; Y represents R.sup.4B --O--N (wherein R.sup.4B has the same meaning as R.sup.4). The radicicol derivatives of the present invention demonstrate tyrosine kinase inhibition activity and pharmacological activities such as antitumor, antimicrobial or immunosuppression effects.Type: GrantFiled: October 27, 1997Date of Patent: November 2, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tsutomu Agatsuma, Yutaka Saitoh, Yoshinori Yamashita, Tamio Mizukami, Shiro Akinaga, Katsushige Gomi, Kazuhito Akasaka, Isami Takahashi
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Patent number: 5965604Abstract: The present invention relates to chrolactomycin compound represented by the following formula (I): ##STR1## or pharmaceutically acceptable salts thereof having antibacterial and antitumor activities.Type: GrantFiled: December 17, 1998Date of Patent: October 12, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoshinori Yamashita, Ryuichiro Nakai, Tamio Mizukami, Shingo Kakita, Shigeru Chiba, Shiro Akinaga
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Patent number: 5798379Abstract: UCS1025 compounds represented by the following formula (I): ##STR1## wherein R represents hydrogen or hydroxyl group, or tautomers or pharmacologically acceptable salts thereof.Type: GrantFiled: December 18, 1997Date of Patent: August 25, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tamio Mizukami, Harumi Ogawa, Ryuichiro Nakai, Akira Asai, Yoshinori Yamashita, Katsuhiko Ando, Tsutomu Agatsuma, Shiro Akinaga, Kozo Ouchi, Hideki Kawasaki
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Patent number: 5728709Abstract: Described herein is a pyrrolocarbazole derivative and a pharmaceutically acceptable salt thereof having the following formula (I): ##STR1## wherein R.sup.1 is lower alkyl or aralkyl; R.sup.2 is hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, or substituted or unsubstituted aralkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different, and are hydrogen, halogen, nitro, substituted or unsubstituted lower alkanoyl, NR.sup.9 R.sup.10, or OR.sup.11 ; R.sup.8 is hydrogen or is combined with R.sup.3 to form --CONR.sup.12 --; and when R.sup.1 is benzyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are not simultaneously hydrogen. A compound of the present invention stimulates platelet production and is useful for treatment of thrombocytopenia.Type: GrantFiled: November 8, 1996Date of Patent: March 17, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ikuina, Chikara Murakata, Yutaka Saitoh, Yukimasa Shiotsu, Takako Iida, Tatsuya Tamaoki, Kinya Yamashita, Shiro Akinaga
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Patent number: 5719179Abstract: Disclosed is Compound GEX1 of formula (I), having excellent antitumor activity: ##STR1## wherein R.sup.1 represents hydroxy or ##STR2## R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen or hydroxy; R.sup.5 represents hydroxyl or lower alkoxy; provided that when R.sup.1 is hydroxy and R.sup.5 is methoxy, then at least one of R.sup.2, R.sup.3 and R.sup.4 is the group except for hydrogen, and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 24, 1996Date of Patent: February 17, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tamio Mizukami, Yasushi Sakai, Tetsuo Yoshida, Youichi Uosaki, Keiko Ochiai, Shiro Akinaga
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Patent number: 5686606Abstract: The present invention relates to UCF116 compounds represented by the formula (I) : ##STR1## wherein an example of Q.sup.1 representation is ##STR2## and an example of Q.sup.2 representation is ##STR3## which have antibacterial and antitumor activity and are useful as antibacterial and antitumor agents.Type: GrantFiled: July 12, 1996Date of Patent: November 11, 1997Assignee: Kyowa Hakko Kogyo, Co., Ltd.Inventors: Tamio Mizukami, Mikito Itoh, Mitsunobu Hara, Hirofumi Nakano, Yumiko Aotani, Keiko Ochiai, Shiro Akinaga, Akira Mihara
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Patent number: 5674867Abstract: The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt thereof as an active ingredient, and to novel indolocarbazole derivatives.Type: GrantFiled: May 18, 1994Date of Patent: October 7, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tatsuya Tamaoki, Yukimasa Shiotsu, Chikara Murakata, Shiro Akinaga, Masami Okabe, Yutaka Saito, Junichi Watanabe, Takako Shiraki
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Patent number: 5665703Abstract: A GE3 compound of the formula (I) having antibacterial and antitumor properties: ##STR1##Type: GrantFiled: December 5, 1995Date of Patent: September 9, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tamio Mizukami, Yasushi Sakai, Tetsuo Yoshida, Tsutomu Agatsuma, Keiko Ochiai, Shiro Akinaga
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Patent number: 5663298Abstract: The present invention relates to UCK14 compounds having antitumor activity which are represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or --COOC(CH.sub.3).sub.3 ; and R.sup.2 and R.sup.3 are taken together to form --CH.sub.2 --, or each R.sup.2 and R.sup.3 independently are hydrogen,and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 15, 1996Date of Patent: September 2, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tamio Mizukami, Akira Asai, Yoshinori Yamashita, Ritsuko Katahira, Atsuhiro Hasegawa, Keiko Ochiai, Shiro Akinaga
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Patent number: 5629304Abstract: The present invention provides a method of treating thrombocytopenia, which comprises administering to a patient suffering from thrombocytopenia, an effective amount of an indolocarbazole derivative represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group or a tetrahydropyranyl group; R.sup.2A and R.sup.3A, which may be the same or different, each represent a hydrogen atom, a substituted or unsubstituted lower alkyl group, a lower alkenyl group, a substituted or unsubstituted aralkyl group or a monosaccharide residue where a hydroxyl group at the anomer position is removed; R.sup.4A and R.sup.5A, which may be the same or different, each represent a hydrogen atom, a formyl group, a hydroxyl group or a halogen atom; W.sup.A1 and W.sup.A2 represent hydrogen atoms or are combined together to form an oxygen atom; and X.sup.A1 and X.sup.Type: GrantFiled: April 25, 1996Date of Patent: May 13, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Chikara Murakata, Fumihiko Kanai, Yutaka Saitoh, Yukimasa Shiotsu, Takako Shiraki, Tatsuya Tamaoki, Shiro Akinaga, Masami Okabe
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Patent number: 5604219Abstract: Disclosed is an indolocarbazole derivative represented by the following formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## [wherein R.sup.1 represents substituted or unsubstituted lower alkyl, R.sup.2 represents hydrogen, substituted or unsubstituted lower alkyl, R.sup.3 and R.sup.4 are the same or different, and represent hydrogen, nitro, NR.sup.5 R.sup.6, OR.sup.9, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, or CH.dbd.NNR.sup.10 R.sup.11, W represents two hydrogen atoms or oxygen, and Me represents methyl, provided that when R.sup.1 is unsubstituted lower alkyl, R.sup.3 and R.sup.4 are not simultaneously hydrogen.Type: GrantFiled: March 16, 1995Date of Patent: February 18, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Chikara Murakata, Junichi Watanabe, Yutaka Saitoh, Yukimasa Shiotsu, Takako Shiraki, Fumihiko Kanai, Tatsuya Tamaoki, Shiro Akinaga, Masami Okabe
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Patent number: 5565489Abstract: The present invention relates to an epoxycyclohexenedione derivative represented by formula (I): ##STR1## wherein R is a straight-chain or branched alkanoyl group having 10 to 25 carbon atoms, a straight-chain alkenoyl group having 10 to 25 carbon atoms, or a group represented by formula (A): ##STR2## wherein n is an integer of 1 to 4; or a pharmaceutically acceptable salt thereof.The compounds exhibit antimicrobial activity and antitumor activity.Type: GrantFiled: May 18, 1995Date of Patent: October 15, 1996Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Masami Kaneko, Yutaka Saitoh, Shiro Akinaga, Masami Okabe, Kazuhito Akasaka, Hirofumi Nakano
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Patent number: 5344926Abstract: Disclosed is a process for producing a staurosporine derivative represented by Formula (I): Q is defined as in specification: ##STR1## The staurosporine derivative (I-1) possesses selective protein kinase C-inhibitory and cell growth-inhibiting activities, and platelet-increasing activity.Type: GrantFiled: June 22, 1993Date of Patent: September 6, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Chikara Murakata, Toshimitsu Takiguchi, Shigeo Katsumata, Akira Mihara, Keiichi Takahashi, Hiromitsu Saito, Shiro Akinaga, Masami Okabe, Yutaka Saito