公开(公告)号：US06939892B2

公开(公告)日：2005-09-06

申请号：US10258435

申请日：2001-04-26

申请人： Tomio Takeuchi ,  Yusuke Wataya ,  Munekazu Iinuma ,  Hye-Sook Kim ,  Hiroomi Watabe ,  Hiroshi Naganawa ,  Yoshikazu Takahashi

发明人： Tomio Takeuchi ,  Yusuke Wataya ,  Munekazu Iinuma ,  Hye-Sook Kim ,  Hiroomi Watabe ,  Hiroshi Naganawa ,  Yoshikazu Takahashi

IPC分类号： A61K31/351 ,  A61P33/06 ,  C07D407/14 ,  A61K31/35 ,  A61K31/365

CPC分类号： C07D407/14 ,  A61K31/351 ,  Y02A50/411

摘要： An antibiotic SF2487 substance having the formula (I) or a salt thereof possesses an antimalarial activity against the proliferation of malarial parasites and is therefore useful as an antimalarial drug.

摘要翻译： 具有式（I）的抗生素SF2487物质或其盐具有抗疟疾寄生虫增殖的抗疟活性，因此可用作抗疟药。

公开(公告)号：US5215981A

公开(公告)日：1993-06-01

申请号：US720758

申请日：1991-07-01

申请人： Tomio Takeuchi ,  Yoshikazu Takahashi ,  Masa Hamada ,  Hiroshi Naganawa ,  Kiyoshi Sato

发明人： Tomio Takeuchi ,  Yoshikazu Takahashi ,  Masa Hamada ,  Hiroshi Naganawa ,  Kiyoshi Sato

IPC分类号： C07D493/10 ,  C12P17/18

CPC分类号： C07D493/10 ,  C12P17/181

摘要： In this invention, a new microbial strain which is a strain of Actinomycetes and belongs to the genus Actinomadura, namely Actinomadura sp. MI215-NF3 strain is cultured, and MI215-NF3 substance, a novel antibiotic classifiable as a polyether antibiotic, is recovered from the resultant culture. MI215-NF3 substance and its salts obtained according to this invention are useful for therapeutic treatment of chicken coccidiosis and also have useful antibacterial activities against certain species of bacteria.

公开(公告)号：US06214340B1

公开(公告)日：2001-04-10

申请号：US09554362

申请日：2000-05-12

申请人： Tomio Takeuchi ,  Masa Hamada ,  Yasuhiko Muraoka ,  Tetsuo Akiyama ,  Masatoshi Abe ,  Hiroshi Naganawa ,  Yoshikazu Takahashi

发明人： Tomio Takeuchi ,  Masa Hamada ,  Yasuhiko Muraoka ,  Tetsuo Akiyama ,  Masatoshi Abe ,  Hiroshi Naganawa ,  Yoshikazu Takahashi

IPC分类号： C12N120

CPC分类号： C12N9/99 ,  A61K38/00 ,  C07K14/36 ,  C12P1/06 ,  C12R1/465

摘要： 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.

摘要翻译： 本发明提供具有强二肽基肽酶IV抑制活性的生理活性物质。 通过培养属于链霉菌属的微生物并且具有生产生理活性物质硫酸钙的能力，在培养物中产生和积累该物质，并从培养物中收获生物活性物质硫酸钙得到。

公开(公告)号：US4565861A

公开(公告)日：1986-01-21

申请号：US567792

申请日：1984-01-03

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Takeshi Uchida ,  Masaya Imoto

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Takeshi Uchida ,  Masaya Imoto

IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P31/04 ,  A61P35/00 ,  C07H15/252 ,  C12P19/56 ,  C12R1/465 ,  C07H15/24

CPC分类号： C07H15/252 ,  C12P19/56 ,  C12R1/465

摘要： An anthracycline, serirubicin, of the formula: ##STR1## wherein R represents the substituent: ##STR2## is produced by a process which comprises cultivating a strain of Streptomyces in a suitable culture medium under aerobic conditions, said strain having the ability to produce the anthracycline compound, serirubicin, and then recovering the anthracycline compound, serirubicin, from the cultured medium. This serirubicin, or an acid addition salt of the serirubicin, can be contained as the active ingredient in anti-tumor agents and in pharmaceutical compositions for treatment of infections induced by gram-positive microorganisms, whereby good results are attainable.

摘要翻译： 蒽环霉素，维拉霉素，其结构式如下：其中R表示取代基：IMAMA是通过包括在需氧条件下在合适的培养基中培养链霉菌属菌株的方法产生的，所述菌株具有产生 蒽环霉素化合物，苏维菌素，然后从培养基中回收蒽环霉素化合物，丝衣霉素。 作为抗肿瘤剂和用于治疗由革兰氏阳性微生物诱导的感染的药物组合物，可以含有这种苏维菌素或者苏维菌素的酸加成盐作为活性成分，从而获得了良好的效果。

公开(公告)号：US4416899A

公开(公告)日：1983-11-22

申请号：US297458

申请日：1981-08-28

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Hiroshi Naganawa ,  Hironobu Iinuma ,  Setsuko Kunimoto

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Hiroshi Naganawa ,  Hironobu Iinuma ,  Setsuko Kunimoto

IPC分类号： C12P13/04 ,  A61K31/15 ,  A61K31/155 ,  A61K31/16 ,  A61P35/00 ,  C07C67/00 ,  C07C239/00 ,  C07C279/14 ,  C12P13/02 ,  C12R1/07 ,  C12P21/00

CPC分类号： C12R1/07 ,  C07C279/14 ,  C12P13/02 ,  Y10S435/832

摘要： A new antibiotic BMG162-aF2 having the formula ##STR1## can be obtained by cultivating a BMG162-aF2-producing strain belonging to the genus Bacillus in a culture medium to produce and accumulate the said BMG162-aF2 and then recovering it from the culture medium. The antibiotic BMG162-aF2 thus obtained or a pharmaceutically acceptable salt thereof can be used for the treatment of a transplanted tumor in warmblooded animals.

摘要翻译： 通过在培养基中培养属于芽孢杆菌属的BMG162-aF2生产菌株以产生并积累所述BMG162-aF2，然后从培养基中回收，可获得具有式的新型抗生素BMG162-aF2 。 由此获得的抗生素BMG162-aF2或其药学上可接受的盐可用于治疗温血动物中的移植肿瘤。

公开(公告)号：US4360664A

公开(公告)日：1982-11-23

申请号：US253489

申请日：1981-04-13

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Hiroshi Naganawa ,  Kuniaki Tatsuta

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Hiroshi Naganawa ,  Kuniaki Tatsuta

IPC分类号： C07H15/252 ,  C07H15/24

CPC分类号： C07H15/252

摘要： A new and improved process for the preparation of C-4' etherified anthracycline glycoside derivatives is provided. The new process involves fewer steps than the prior art process and gives the antibiotic end-products in higher yield.

摘要翻译： 提供了一种新的改进的C-4醚化蒽环苷衍生物的制备方法。 新方法涉及比现有技术方法更少的步骤，并以更高的产率给予抗生素最终产品。

公开(公告)号：US4198480A

公开(公告)日：1980-04-15

申请号：US886987

申请日：1978-03-15

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Masaaki Ishizuka ,  Hiroshi Naganawa ,  Toshikazu Oki ,  Taiji Inui

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Masaaki Ishizuka ,  Hiroshi Naganawa ,  Toshikazu Oki ,  Taiji Inui

IPC分类号： C12P1/06 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61K31/7048 ,  A61P31/04 ,  A61P35/00 ,  C07H15/252 ,  C12P19/56 ,  C12R1/465

CPC分类号： C12R1/465 ,  C07H15/252 ,  C12P19/56 ,  Y10S435/886

摘要： A novel anthracycline antibiotic complex designated herein as baumycin complex is produced by fermentation of a baumycin-producing strain of Streptomyces, e.g. Streptomyces coeruleorubidus ME 130-A4 (FERM-P3540, ATCC 31276). The complex and four bioactive components thereof designated baumycin A.sub.1, A.sub.2, B.sub.1 and B.sub.2 are useful as antibacterial and antitumor agents.

摘要翻译： 本文称为鲍曼霉素复合物的新型蒽环类抗生素复合物是通过发酵生产巴霉素的链霉菌菌株，例如， Streptomyces coeruleorubidus ME 130-A4（FERM-P3540，ATCC 31276）。 其中称为baumycin A1，A2，B1和B2的复合物和四种生物活性成分可用作抗细菌剂和抗肿瘤剂。

公开(公告)号：US4144329A

公开(公告)日：1979-03-13

申请号：US780730

申请日：1977-03-24

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Hiroshi Naganawa ,  Masaaki, all of Ishizuka ,  Norio Shibamoto ,  Toshikazu Oki ,  Taiji Inui

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Hiroshi Naganawa ,  Masaaki, all of Ishizuka ,  Norio Shibamoto ,  Toshikazu Oki ,  Taiji Inui

IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P31/04 ,  A61P35/00 ,  C07H15/252 ,  C12P19/56 ,  A61K31/71 ,  C07H17/08

CPC分类号： C12R1/465 ,  C07H15/252 ,  C12P19/56 ,  C12R1/48 ,  Y10S435/886 ,  Y10S435/888

摘要： New antitumor agents designated MA 144-M.sub.1 and MA 144-M.sub.2, which are anthracycline glycosides and inhibit the growth of gram-positive bacteria, e.g. Staphyococcus aureaus, Bacillus subtilis and Sarcina lutea, and inhibit the growth of animal tumors such as leukemia L 1210, P 388 and sarcoma 180 are produced by fermentation of MA 144-producing strains of streptomyces and by the chemical or enzymatic conversion of aclacinomycin A or cinerubin A.

摘要翻译： 称为MA 144-M1和MA 144-M2的新型抗肿瘤剂，其为蒽环类苷并抑制革兰氏阳性细菌的生长，例如， 葡萄球菌属，枯草芽孢杆菌和黄褐斑，并抑制动物肿瘤如白血病L 1210，P 388和肉瘤180的生长是通过发酵生产链霉菌MA 144的菌株和通过化学或酶促转化阿拉霉素A或 赛琳布A.

公开(公告)号：US5096924A

公开(公告)日：1992-03-17

申请号：US531109

申请日：1990-05-31

申请人： Masaaki Ishizuka ,  Hiroyuki Kumagai ,  Tsutomu Sawa ,  Hiroshi Naganawa ,  Hironobu Iinuma ,  Kunio Isshiki ,  Masa Hamada ,  Kenji Maeda ,  Tomio Takeuchi

发明人： Masaaki Ishizuka ,  Hiroyuki Kumagai ,  Tsutomu Sawa ,  Hiroshi Naganawa ,  Hironobu Iinuma ,  Kunio Isshiki ,  Masa Hamada ,  Kenji Maeda ,  Tomio Takeuchi

IPC分类号： A61K31/35 ,  A61K31/352 ,  A61P35/00 ,  C07D311/76 ,  C12N1/20 ,  C12P17/06 ,  C12R1/625

CPC分类号： C12P17/06 ,  C07D311/76

摘要： As a new antibiotic is provided a compound, now nominated as MI43-37F11 substance, which has formula ##STR1## This MI43-37F11 substance has an antitumor activity, an activity to enhance the production of interleukin-1 in vivo in a mammalian, and an activity to activate a macrophage in vivo in a mammalian. MI43-37F11 substance may be produced by cultivation of Streptoverticillium eurocidicum MI43-37F11 strain identified as FERM BP-2783.

公开(公告)号：US4918172A

公开(公告)日：1990-04-17

申请号：US252636

申请日：1988-10-03

申请人： Akihiro Yoshimoto ,  Osamu Jodo ,  Yoshio Watanabe ,  Rokuro Okamoto ,  Tomoyuki Ishikura ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Tomio Takeuchi

发明人： Akihiro Yoshimoto ,  Osamu Jodo ,  Yoshio Watanabe ,  Rokuro Okamoto ,  Tomoyuki Ishikura ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Tomio Takeuchi

IPC分类号： C07H15/252

CPC分类号： C07H15/252

摘要： Disclosed are anthracycline antibiotics of a formula (I): ##STR1## in which R.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is 1-hydroxyethyl group, R.sup.4 is hydrogen atom and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1, R.sup.2 and R.sup.4 are hydroxyl groups, R.sup.3 is ethyl group and X represents daunosamine-rhodenose, daunosamine-deoxyfucose, rhodosamine-rhodenose, N-monomethyldaunosamine-rhodenose or N-monomethyldaunosamine-deoxyfucose; orR.sup.1 is methoxy group, R.sup.2 is hydroxyl group, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.4 are hydroxy groups, R.sup.2 is hydrogen atom, R.sup.3 is ethyl group and X represents daunosamine-deoxyfucose, as well as pharmaceutically acceptable acid addition salts thereof. The antibiotics (I) have a carcinostatic activity and are useful as a carcinostatic for murine leukemia L1210 cells in culture.