Patents Assigned to Zaidan Hojin
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Patent number: 6514946Abstract: 20,23-disubstituted mycaminosyltylonolide derivatives and use of the same in the field of the prophylaxis and treatment of pasteurellosis are disclosed. The di-substituents are peperidino optionally substituted with one or two methyl groups. The derivatives have selective antibacterial activity against Pasteurella.Type: GrantFiled: August 29, 2000Date of Patent: February 4, 2003Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Toshiaki Miyake, Tomohisa Takita, Masa Hamada, Tomio Takeuchi, Sumio Umezawa
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Patent number: 6426420Abstract: Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by a formula: (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by a formula: (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a —OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.Type: GrantFiled: July 5, 2000Date of Patent: July 30, 2002Assignees: Mercian Corporation, Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Toshio Tsuchida, Hazuki Nagai, Takashi Nakashima, Masashi Yoshida, Kaname Konuki, Asako Kuroda, Kunio Isshiki, Tomio Takeuchi
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Physiologically active polyoxypeptin and deoxypolyoxypeptin and anticancer drugs containing the same
Patent number: 6245734Abstract: As novel substances having an activity of inducing an apoptosis even on the apoptosis-resistant cancer cells, there are obtained polyoxypeptin and deoxypolyoxypeptin represented by the following general formula (I) wherein R denotes a hydroxyl group for polyoxypeptin, or R denotes a hydrogen atom for deoxypolyoxypeptin, by cultivation of Streptomyces sp. MK498-98F14 strain. Polyoxypeptin and deoxypolyoxypeptin are physiologically active substances which have an activity of inducing apoptosis on a human pancreatic adenocarcinoma cell, AsPC-1 cell.Type: GrantFiled: December 13, 1999Date of Patent: June 12, 2001Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Kazuo Umezawa, Shinichi Kondo, Yoko Ikeda, Hiroshi Naganawa, Masa Hamada -
Patent number: 6245810Abstract: A novel amino acid derivative represented by the general formula (I) shown below or a salt thereof have now been provided by chemical synthesis, and it has been found that these new compounds stimulate proliferation and physiological activities of the T cells of mammals, have an immunomodulating activity and also have an antitumor activity or a carcinostatic activity. It has also been found that these new compounds have an effect of stimulating the proliferation of hematopoietic stem cells. wherein y is 0 or 1; R1 represents an unsubstituted C1-C8 alkyl group or others; R2 represents a hydrogen atom, a C1-C5 alkyl group or others; R3 represents a hydrogen atom, a C1-C8 alkyl group or others; R4 represents a hydrogen atom, a C1-C3 alkyl group or others; R5 represents a group —OR42, a group or others.Type: GrantFiled: June 30, 1998Date of Patent: June 12, 2001Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Masaaki Ishizuka, Masaji Kawazu, Toshiaki Katsumi, Yoshihide Fuse, Kenji Maeda, Tomio Takeuchi
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Patent number: 6214340Abstract: This invention provides a physiologically active substance having a strong dipeptidyl peptidase IV inhibitory activity. The physiologically active substance sulphostin is obtained by culturing a microorganism belonging to the genus Streptomyces and having an ability to produce the physiologically active substance sulphostin, producing and accumulating this substance in the cultures, and harvesting it from the cultures.Type: GrantFiled: May 12, 2000Date of Patent: April 10, 2001Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Masa Hamada, Yasuhiko Muraoka, Tetsuo Akiyama, Masatoshi Abe, Hiroshi Naganawa, Yoshikazu Takahashi
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Patent number: 6184365Abstract: 7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-&agr;-L-talopyranosyl)-daunomycinone or -adriamycinone is now synthesized as a novel daunomycinone or adriamycinone derivative having the general formula wherein R is a hydrogen atom or hydroxyl group. These novel compounds according to this invention exhibit excellent antitumor activities and have a high solubility in water, and hence they are useful as an antitumor agent.Type: GrantFiled: December 16, 1997Date of Patent: February 6, 2001Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Sumio Umezawa, Tsutomu Tsuchiya, Yasushi Takagi
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Patent number: 6160017Abstract: The invention relates to an agent for preventing and treating ulcerous colitis and/or Crohn's disease, comprising conagenin or a pharmaceutically acceptable salt thereof as an active ingredient. According to the present invention, there is provided an agent for preventing and treating ulcerous colitis and/or Crohn's disease, which has high therapeutic effect and safety.Type: GrantFiled: February 14, 2000Date of Patent: December 12, 2000Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Taiho Pharmaceutical Co., Ltd.Inventors: Masaaki Ishizuka, Kenji Maeda, Tomio Takeuchi, Tadayoshi Shiraishi, Masakazu Fukushima
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Patent number: 6075135Abstract: 7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-.alpha.-L-mannopyranosyl)-daunomycinon e or -adriamycinone is now synthesized as a daunomycinone or adriamycinone derivative having the general formula ##STR1## wherein R is a hydrogen atom or hydroxyl group. These novel compounds according to this invention exhibit excellent antitumor activities and have a high solubility in water, and hence they are useful as an antitumor agent.Type: GrantFiled: March 31, 1999Date of Patent: June 13, 2000Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Sumio Umezawa, Tsutomu Tsuchiya, Yasushi Takagi
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Patent number: 6043217Abstract: Novel amide derivatives of amythiamicin are now provided, which are soluble in water and exhibit antibacterial activities, some of which exhibit an excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).Type: GrantFiled: August 20, 1997Date of Patent: March 28, 2000Assignee: Zaidan Hojin Biseibutsu Kagaku Kenyu KaiInventors: Yasuhiko Muraoka, Hironobu Iinuma, Tomio Takeuchi, Tsuneo Okonogi
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Patent number: 6020363Abstract: Compounds of the formula (I) ##STR1## wherein R is a hydrogen atom or a C.sub.1-6 alkyl group and n is an integer of 0 or 1, and pharmaceutical preparations thereof are provided. These pharmaceutical preparations are useful for the prevention or treatment of diseases associated with an abnormality in immunological regulatory function or vascularization.Type: GrantFiled: December 17, 1998Date of Patent: February 1, 2000Assignees: Mercian Corporation, Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Shin-ichi Hirano, Toshiyuki Mase, Naoki Agata, Hiroshi Iguchi, Naoki Matsumoto, Takeo Yoshioka, Hiroshi Tone, Hiroyuki Kumagai, Masaaki Ishizuki, Tomio Takeuchi
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Patent number: 5965556Abstract: The invention relates to novel pyrrolidine derivatives represented by formula (1): ##STR1## wherein: R1 represents (1) a lower alkyl group having 1 to 6 carbon atoms, or (2) a 3- to 15-membered mono- or fused cyclic hydrocarbon group which may contain a hetero atom on the ring, or which may be substituted with a substituent(s); each of n and m represents an integer and the sum of n and m is an integer of 0 to 2; each of X and E represents oxygen, NR' (wherein R' is hydrogen or a lower alkyl group having 1 to 6 carbon atoms), sulfur, phenylene, CH.dbd.CH or CH.sub.2 ; A represents an amino acid residue or an imino acid residue, which functional group may be optionally protected, or a glycine residue which may be substituted at the amino moiety thereof; and, Y1 represents a cycloalkyl group having 3 to 8 carbon atoms; or a salt thereof. The pyrrolidine derivatives inhibit a prolyl endopeptidase and are expected to be effective for the treatment of amnesia.Type: GrantFiled: February 5, 1998Date of Patent: October 12, 1999Assignee: Zaidan Hojin Biseibutsu Kagaku KenkyukaiInventors: Tomio Takeuchi, Takaaki Aoyagi, Yasuhiko Muraoka, Makoto Tsuda
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Patent number: 5958889Abstract: 7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-.alpha.-L-mannopyranosyl)daunomycinone or -adriamycinone is now synthesized as a daunomycinone or adriamycinone derivative having the general formula ##STR1## wherein R is a hydrogen atom or hydroxyl group. These novel compounds according to this invention exhibit excellent antitumor activities and have a high solubility in water, and hence they are useful as an antitumor agent.Type: GrantFiled: December 22, 1997Date of Patent: September 28, 1999Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Sumio Umezawa, Tsutomu Tsuchiya, Yasushi Takagi
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Patent number: 5952380Abstract: A pharmaceutical composition for treating diarrhea comprising an anti-diarrhea effective amount of conagenin or a salt thereof, and a pharmaceutically acceptable carrier. The pharmaceutical composition is particularly useful against diarrhea caused by the administration of cancer chemotherapeutic agents.Type: GrantFiled: March 27, 1997Date of Patent: September 14, 1999Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Taino Pharmaceutical Co., Ltd., Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Masaaki Ishizuka, Kenji Maeda, Tomio Takeuchi, Toshiyuki Toko, Tadayoshi Shiraishi
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Patent number: 5886167Abstract: 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.Type: GrantFiled: December 15, 1997Date of Patent: March 23, 1999Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Sumio Umezawa, Tsutomu Tsuchiya, Yoshiaki Takahashi
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Patent number: 5883406Abstract: A multiplicity of field effect type semiconductor memory elements are formed perpendicular to a surface of a semiconductor wafer. Charge carriers are transported in the semiconductor bulk perpendicular to the surface and a potential barrier is formed in the current path to accomplish storing. Since the bulk mobility of a semiconductor is far larger than the surface mobility, the transit time of the carriers is much improved. Furthermore, since each structure of the memory cells is formed perpendicular to the semiconductor surface, the surface occupation area per memory cell is reduced. Thus, a high-speed and high-density semiconductor memory device is provided.Type: GrantFiled: February 24, 1992Date of Patent: March 16, 1999Assignee: Zaidan Hojin Handotai Kenkyu ShinkokaiInventor: Jun-ichi Nishizawa
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Patent number: 5849797Abstract: Now are provided (R)-3,6-diamino-N-(.omega.-aminoalkyl)-hexanamides which are novel compounds having the general formula (I): ##STR1## wherein n stands for 2-5, and which may be for example, (R)-3,6-diamino-N-(2-aminoethyl)hexanamide (n=2) and (R)-3,6-diamino-N-(3-aminopropyl)hexanamide (n=3). Their preparation process is also provided. These novel compounds and acid addition salts thereof have activities inhibitory against Gram-positive bacteria, Gram-negative bacteria and AIDS virus, as well as tumor cells and are chemically stable.These novel compounds and their salts are useful as chemotherapeutic agents for diseases caused by these bacteria or virus and also as antitumor agent.Type: GrantFiled: February 24, 1997Date of Patent: December 15, 1998Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Shinichi Kondo, Yoko Ikeda, Tomio Takeuchi, Rie Shinei, Shuichi Gomi, Seiji Shibahara, Hiroo Hoshino
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Patent number: 5831072Abstract: An object of this invention is to provide a novel process for the synthesis of a 2'-deoxy-2'-halocoformycin having an inhibitory activity against adenosine deaminase in a practically high yield. Thus, there is provided a process comprising multi-stage reactions with using as the starting intermediate a tert-butyl 1-(3,5-di-O-acyl-2-deoxy-2-halo-.beta.-D-ribofuranosyl or arabinofuranosyl)-5-aminoimidazole-4-carboxylate of formula (II) ##STR1## whereby there are produced a 2'-deoxy-2'-halocoformycin or a 2'-deoxy-2'-epi-2'-halocoformycin of formula (I-a) ##STR2## and also a 2'-deoxy-8-epi-2'-halocoformycin or a 2'-deoxy-8,2'-diepi-2'-halocoformycin of formula (I-b) ##STR3## It is expectable that a 2'-deoxy-2'-halocoformycin and epimers thereof are useful as a drug for lymphocytic leukemias and as drugs for various diseases attributable to the actions of adenosine deaminase.Type: GrantFiled: March 4, 1997Date of Patent: November 3, 1998Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Sumio Umezawa, Tsutomu Tsuchiya, Yoshiaki Takahashi
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Patent number: 5808328Abstract: A multiplicity of field effect type semiconductor memory elements are formed perpendicular to a surface of a semiconductor wafer. Charge carriers are transported in the semiconductor bulk perpendicular to the surface and a potential barrier is formed in the current path to accomplish storing. Since the bulk mobility of a semiconductor is far larger than the surface mobility, the transit time of the carriers is much improved. Furthermore, since each structure of the memory cells is formed perpendicular to the semiconductor surface, the surface occupation area per memory cell is reduced. Thus, a high-speed and high-density semiconductor memory device is provided.Type: GrantFiled: June 5, 1995Date of Patent: September 15, 1998Assignee: Zaidan Hojin Handotai Kenkyu ShinkokaiInventor: Jun-ichi Nishizawa
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Patent number: 5801257Abstract: Novel anthracycline derivatives have now been produced, which exhibit higher antitumor activities and lower toxicities than those of daunomycin, adriamycin etc. that have been clinically used as anticancer agents. That is, a daunomycinone or adriamycinone derivative represented by the general formula (I): ##STR1## wherein R is a hydrogen atom or a hydroxyl group, and 7-O-(2,6-dideoxy-6,6,6-trifluoro-.alpha.-L-lyxo-hexopyranosyl)adriamycinon e derivative which is an adriamycinone derivative represented by formula (II): ##STR2## have now been newly synthesized. The novel anthracycline derivatives having the general formula (I) and formula (II), respectively, show excellent anticancer or antitumor activities and are of low toxicities. These novel compounds are very useful as anticancer or antitumor agents and are expected to be useful for the therapeutic treatments of a variety of cancers and tumors, similarly to daunomycin or adriamycin.Type: GrantFiled: October 20, 1997Date of Patent: September 1, 1998Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Sumio Umezawa, Tsutomu Tsuchiya, Yasushi Takagi
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Patent number: 5798387Abstract: A novel amino acid derivative represented by the general formula (I) shown below or a salt thereof have now been provided by chemical synthesis, and it has been found that these new compounds stimulate proliferation and physiological activities of the T cells of mammals, have an immunomodulating activity and also have an antitumor activity or a carcinostatic activity. It has also been found that these new compounds have an effect of stimulating the proliferation of hematopoietic stem cells. ##STR1## wherein y is 0 or 1; R.sup.1 represents an unsubstituted C.sub.1 -C.sub.8 alkyl group or others;R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or others;R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or others;R.sup.4 represents a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group or others;R.sup.5 represents a group --OR.sup.42, a group ##STR2## or others.Type: GrantFiled: November 25, 1996Date of Patent: August 25, 1998Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Masaaki Ishizuka, Masaji Kawazu, Toshiaki Katsumi, Yoshihide Fuse, Kenji Maeda, Tomio Takeuchi