Patents by Inventor Takashi Yaegashi
Takashi Yaegashi 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: 6310210Abstract: The present invention relates to new camptothecin derivatives shown by the below formula, which are water-soluble and excellent in an anti-tumor activity, and to salts thereof. In the formula, R1 represents a hydrogen atom or an alkyl group with 1-6 carbon atoms, R2 represents identically or differently 0-4 alkyl groups with 1-6 carbon atoms, a halogen atom, an alkoxyl or hydroxyl group, R3 represents a lower alkylamino, di-lower alkylamino, arylamino, cyclicamino or lower alkoxyl group, and salts thereof.Type: GrantFiled: May 3, 2000Date of Patent: October 30, 2001Assignee: Kabushiki Kaisha Yakult HonshaInventors: Takanori Ogawa, Takashi Yaegashi, Seigo Sawada, Tomio Furuta
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Patent number: 6025385Abstract: This invention relates to a taxane derivative represented by the following formula (1): wherein at least one of X and Y represents a group --CO--A--B in which A represents a single bond, an alkylenecarbonyl group or the like and B represents a substituted or unsubstituted piperidino group or the like, the other represents a tert-butoxycarbonyl group or the like, and Z represents a hydrogen atom or a triethylenesilyl group, and also to a drug containing the same.This compound has high solubility in water and also has excellent antitumor activities.Type: GrantFiled: January 14, 1999Date of Patent: February 15, 2000Assignee: Kabushiki Kaisha Yakult HonshaInventors: Hideaki Shimizu, Atsuhiro Abe, Takashi Yaegashi, Seigo Sawada, Hiroshi Nagata
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Patent number: 5843954Abstract: New camptothecin derivatives of the general formula (1): ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.2 represents a hydrogen or a C.sub.1 -C.sub.6 alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, C.sub.2 -C.sub.6 acyloxy or methoxyethoxymethoxy group, R.sup.4 represents a hydrogen or halogen atom, and R.sup.5 represents a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 unsaturated alkyl, alkylthioalkyl, alkoxyalkyl, pyridyl or substituted phenyl group, with the proviso that all of the R.sup.2, R.sup.3 and R.sup.4 substituents should not be a hydrogen atom, and a process for preparing the new camptothecin derivatives by subjecting the camptothecin derivatives of the general formula (2): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.Type: GrantFiled: November 21, 1997Date of Patent: December 1, 1998Assignees: Kabushiki Kaisha Yakult Honsha, Daiichi Pharmaceutical Co., Ltd.Inventors: Takashi Yaegashi, Seigo Sawada, Tomio Furuta, Teruo Yokokura
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Patent number: 5061800Abstract: New campotothecin derivatives and a process for preparing same are disclosed, which are represented by the general formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R.sup.4 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R.sup.5 represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 substituents should not be a hydrogen atom and also that if any one of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is a hydroxyl or lower alkoxy group, all of the other three substituents should not be a hydrogen atom.Type: GrantFiled: January 19, 1989Date of Patent: October 29, 1991Assignee: Kabushiki Kaisha Yakult HonshaInventors: Takashi Yaegashi, Satoru Okajima, Seigo Sawada, Kenichiro Nokata, Kenichi Tezuka, Hiroshi Nagata, Teruo Yokokura, Tadashi Miyasaka, Tadashi Miyasaka
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Patent number: 4914205Abstract: New camptothecin derivatives, useful as antitumor agents or intermediates therefor, of the general formula (I) ##STR1## wherein X is a lower alkyl group, and R is a hydrogen atom or the grouping -COY where Y is a linear or branched unsubstituted C.sub.1 -C.sub.18 alkyl group; a lower alkyl group substituted by a halogen atom or a lower alkylthio, amino, acylamino, hydroxyl, lower alkoxy, aryloxy or lower alkoxycarbonyl group; a C.sub.3 -C.sub.19 alkenyl, C.sub.3 -C.sub.19 alkynyl or C.sub.3 -C.sub.8 cycloalkyl group; a C.sub.3 -C.sub.Type: GrantFiled: June 24, 1988Date of Patent: April 3, 1990Assignee: Kabushiki Kaisha Yakult HonshaInventors: Seigo Sawada, Kenichiro Nokata, Satoru Okajima, Hisako Nagai, Takashi Yaegashi, Kenichi Tezuka, Tadashi Miyasaka
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Patent number: 4598077Abstract: Amidine derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent each a hydrogen atom or a lower alkyl group, or R.sub.1 and R.sub.2 together with an intermediary carbon atom and/or hetero atom may form a ring; X represents ##STR2## (wherein R.sub.8 represents a hydrogen atom, a lower alkyl group, or --CH.sub.2 COOR.sub.9, where R.sub.9 represents a hydrogen atom or a lower alkyl group; Z represents a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, or --CH.dbd.CH--); R.sub.3 represents a hydrogen or chlorine atom, methoxy group, nitro group, or amino group; Y represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O--, or --OCH.sub.2 --; R.sub.4 represents a hydrogen atom, methoxy group, benzoyl group, nitro group, or amino group; and R.sub.5, R.sub.6 and R.sub.Type: GrantFiled: December 14, 1984Date of Patent: July 1, 1986Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Takuo Sato, Hiroyuki Kawamura, Takashi Yaegashi, Masateru Kurumi, Takuo Aoyama
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Patent number: 4570006Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsine, anti-plasmin, anti-kallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: October 24, 1984Date of Patent: February 11, 1986Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Takashi Yaegashi, Toyoo Nakayama, Yojiro Sakurai, Shigeki Nunomura, Toshiyuki Okutome
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Patent number: 4532255Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: January 20, 1984Date of Patent: July 30, 1985Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Toshiyuki Okutome, Toyoo Nakayama, Takashi Yaegashi, Masateru Kurumi
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Patent number: 4514416Abstract: Amidino compounds represented by the formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: May 21, 1984Date of Patent: April 30, 1985Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Takashi Yaegashi, Toyoo Nakayama, Yojiro Sakurai, Shigeki Nunomura, Toshiyuki Okutome
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Patent number: 4496584Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsin, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-Cl activity and anti-complement activity, they are also useful as anti-complement agents. These amidino compounds are prepared by reacting carboxylic compounds represented by the formulaR.sub.1 --COOHor their reactive intermediates with amidinonaphthol represented by the formula ##STR2## and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: April 21, 1982Date of Patent: January 29, 1985Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Takashi Yaegashi, Toyoo Nakayama, Shigeki Nunomura, Yojiro Sakurai, Toshiyuki Okutome
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Patent number: 4490388Abstract: Amidino compounds represented by the formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with 4-(.beta.-amidinoethenyl)phenol represented by the formula (III) ##STR2## and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: February 22, 1982Date of Patent: December 25, 1984Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Takuo Aoyama, Yojiro Sakurai, Toyoo Nakayama, Shigeki Nunomura, Takashi Yaegashi, Toshiyuki Okutome
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Patent number: 4454338Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceuticlly acceptable acid addition salts thereof.Type: GrantFiled: September 9, 1981Date of Patent: June 12, 1984Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Toshiyuki Okutome, Toyoo Nakayama, Takashi Yaegashi, Masateru Kurumi
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Patent number: 4418012Abstract: A leucylalanyarginine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or an amino-protecting group; R.sub.2 and R.sub.3 represent hydrogen or guanidino-protecting groups; and R.sub.4 represents naphthyl. The above compound is useful as an excellent substrate for various enzymes, such as trypsin, plasmin, kallikrein, urokinase, Cl-esterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.Type: GrantFiled: September 9, 1981Date of Patent: November 29, 1983Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Mamoru Sugimoto, Takashi Yaegashi
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Patent number: 4379764Abstract: A phenylalanylarginine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or an amino-protecting group; R.sub.2 and R.sub.3 represent hydrogen or guanidino-protecting groups; R.sub.4 represents naphthyl. The above compound is useful as an excellent substrate for various enzymes, such as trypsin, plasmin, kallikrein, urokinase, Cl-esterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.Type: GrantFiled: September 9, 1981Date of Patent: April 12, 1983Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Mamoru Sugimito, Takashi Yaegashi
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Patent number: 4308201Abstract: A phenylalanylvalylarginine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or benzoyl and R.sub.2 represents naphthyl. The above compound is useful as an excellent substrate for various enzymes, such as trypsin, plasmin, kallikrein, urokinase, Cl-esterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.Type: GrantFiled: October 25, 1979Date of Patent: December 29, 1981Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Mamoru Sugimoto, Takashi Yaegashi
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Patent number: 4308202Abstract: A prolylphenylalanylarginine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or benzoyl; R.sub.2 represents naphthyl or 6-bromo-2-naphthyl. The above compound is useful as an excellent substrate for various enzymes, such as trypsin, plasmin, kallikrein, urokinase, Clesterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.Type: GrantFiled: October 25, 1979Date of Patent: December 29, 1981Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Mamoru Sugimoto, Takashi Yaegashi
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Patent number: 4257940Abstract: A valylleucyllysine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or benzoyl and R.sub.2 represented naphthyl. The above compound is useful as an excellent substrate for various anzymes, such as, trypsin, plasmin, kallikrein, urokinase, Cl-esterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.Type: GrantFiled: October 25, 1979Date of Patent: March 24, 1981Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Mamoru Sugimoto, Takashi Yaegashi