公开(公告)号：US4795743A

公开(公告)日：1989-01-03

申请号：US21781

申请日：1987-03-04

申请人： Yoshiro Okami ,  Shinichi Kondo ,  Daishiro Ikeda ,  Hamao Umezawa, deceased

发明人： Yoshiro Okami ,  Shinichi Kondo ,  Daishiro Ikeda ,  Hamao Umezawa, deceased

IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/222 ,  C07H15/224 ,  C07H15/22

CPC分类号： C07H15/224

摘要： As new 2'-deamino-2'-hydroxyistamycin B.sub.o derivatives are provided four compounds, namely 2'-deamino-2'-hydroxyistamycin B; 2'-deamino-2'-hydroxy-3-O-demethylistamycin B; 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxyistamycin B.sub.o ; and 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxy-3-O-demethylistamycin B.sub.o which all exhibit high antibacterial activity and low acute toxicity in combination. These new compounds are useful as antibacterial agent.

摘要翻译： 作为新的2'-脱氨基-2'-羟基毛霉素Bo衍生物，提供四种化合物，即2'-脱氨基-2'-羟基毛霉素B; 2'-脱氨基-2'-羟基-3-O-脱甲基霉素B; 4-N-（β-丙氨酰基）-2'-脱氨基-2'-羟基毛霉素Bo; 和4-N-（β-丙氨酰基）-2'-脱氨基-2'-羟基-3-O-脱甲基丝杆霉素B B，其组合表现出高的抗菌活性和低的急性毒性。 这些新化合物可用作抗菌剂。

公开(公告)号：US4479943A

公开(公告)日：1984-10-30

申请号：US545686

申请日：1983-10-26

申请人： Hamao Umezawa ,  Shinichi Kondo ,  Daishiro Ikeda

发明人： Hamao Umezawa ,  Shinichi Kondo ,  Daishiro Ikeda

IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/224 ,  A61K31/71 ,  C07H15/22

CPC分类号： C07H15/224 ,  Y02P20/55

摘要： As new compounds are provided 3-demethoxyistamycin B and 3-demethoxy-2"-N-formimidoylistamycin B which each is useful as antibacterial agent because of its high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria including mycobacteria. These new compounds may be produced by removal of the 3-hydroxyl group of an N,O-protected 3-O-demethylistamycin B.sub.o, followed by glycylation of the liberated 4-methylamino group and, further, if necessary, followed by formimidoylation of the 2"-amino group of an intermediate N-protected 3-demethoxyistamycin B derivative.

摘要翻译： 作为新化合物，提供3-脱甲氧基霉素B和3-脱甲氧基-2'-N-甲脒基丝霉素B，其各自可用作抗菌剂，因为其对多种革兰氏阳性和革兰氏阴性菌（包括分枝杆菌）具有高抗菌活性 。 这些新化合物可以通过除去N，O-保护的3-O-脱甲基丝马杆霉Bo的3-羟基，随后释放的4-甲基氨基糖基化，并且如果需要，然后进行甲酰化 2“ - 中间体N-保护的3-脱甲氧基霉素B衍生物的氨基。

公开(公告)号：US4474946A

公开(公告)日：1984-10-02

申请号：US530006

申请日：1983-09-07

申请人： Hamao Umezawa ,  Shinichi Kondo ,  Daishiro Ikeda

发明人： Hamao Umezawa ,  Shinichi Kondo ,  Daishiro Ikeda

IPC分类号： A61K31/35 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/224 ,  C07H15/22

CPC分类号： C07H15/224 ,  Y02P20/55

摘要： A new istamycin A derivative called di-N.sup.6', O.sup.3 -demethylistamycin A exhibits a high antibacterial activity against various bacteria, particularly Pseudomonas aeruginosa. This compound can be prepared by selective acylation of the methylamino group at the 4-position of 1,2',6'-tri-N-protected N.sup.4 -deglycyl-di-N.sup.6', O.sup.3 -demethylistamycin A with glycine or an N-protected derivative thereof, followed by N-deprotection.

摘要翻译： 称为di-N6'，O3-脱甲基霉素A的新型istamycin A衍生物对各种细菌，特别是铜绿假单胞菌表现出高抗菌活性。 该化合物可以通过在1,2'，6'-三-N-保护的N4-脱乙酰基 - 二-N6'，O-脱甲基丝霉素A的4-位选择性酰化甘氨酸或N- 保护的衍生物，然后进行N-去保护。

公开(公告)号：US5849797A

公开(公告)日：1998-12-15

申请号：US793912

申请日：1997-02-24

申请人： Shinichi Kondo ,  Yoko Ikeda ,  Tomio Takeuchi ,  Rie Shinei ,  Shuichi Gomi ,  Seiji Shibahara ,  Hiroo Hoshino

发明人： Shinichi Kondo ,  Yoko Ikeda ,  Tomio Takeuchi ,  Rie Shinei ,  Shuichi Gomi ,  Seiji Shibahara ,  Hiroo Hoshino

IPC分类号： A61K31/16 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07C231/02 ,  C07C231/12 ,  C07C237/10 ,  C07C233/05

CPC分类号： C07C237/10

摘要： 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.

摘要翻译： PCT No.PCT / JP95 / 01680 Sec。 371日期1997年2月24日 102（e）1997年2月24日PCT PCT 1995年8月24日PCT公布。 公开号WO96 / 06069 日期：1996年2月29日提供（R）-3,6-二氨基-N-（ω-氨基烷基） - 己酰胺，它们是具有通式（I）的新化合物：其中n代表2 -5，其可以是例如（R）-3,6-二氨基-N-（2-氨基乙基）己酰胺（n = 2）和（R）-3,6-二氨基-N-（3-氨基丙基 ）己酰胺（n = 3）。 还提供了他们的准备过程。 这些新化合物及其酸加成盐具有抑制革兰氏阳性菌，革兰氏阴性菌和艾滋病病毒以及肿瘤细胞的活性，并具有化学稳定性。 这些新化合物及其盐可用作由这些细菌或病毒引起的疾病的化学治疗剂，也可用作抗肿瘤剂。

公开(公告)号：US5055453A

公开(公告)日：1991-10-08

申请号：US264888

申请日：1988-10-31

申请人： Tomio Takeuchi ,  Takeshi Hara ,  Masa Hamada ,  Shinichi Kondo ,  Masaji Sezaki ,  Haruo Yamamoto ,  Shuichi Gomi

发明人： Tomio Takeuchi ,  Takeshi Hara ,  Masa Hamada ,  Shinichi Kondo ,  Masaji Sezaki ,  Haruo Yamamoto ,  Shuichi Gomi

IPC分类号： C07H15/24 ,  C12P19/56

CPC分类号： C12R1/01 ,  C07H15/24 ,  C12P19/56 ,  Y10S435/826

摘要： Two new antibiotics which are now nominated as benanomicin A and benanomicin B, respectively, are fermentatively produced by the cultivation of a new microorganism, designated as MH193-16F4 strain, of Actinomycetes. Benanomicins A and B each show antifungal activity and are useful as a therapeutic antifungal agent. A new compound, dexylosylbenanomicin B is now produced by chemical conversion of benanomicin B, and this semi-synthetic antibiotic also shows antifungal activity and is useful as a therapeutic antifungal agent.

公开(公告)号：US4929633A

公开(公告)日：1990-05-29

申请号：US203888

申请日：1988-06-08

申请人： Seiji Shibahara ,  Yukiko Takahashi ,  Yuji Matsuhashi ,  Mitsugu Hachisu ,  Shinichi Kondo ,  Tomio Takeuchi ,  Takaaki Aoyagi

发明人： Seiji Shibahara ,  Yukiko Takahashi ,  Yuji Matsuhashi ,  Mitsugu Hachisu ,  Shinichi Kondo ,  Tomio Takeuchi ,  Takaaki Aoyagi

IPC分类号： A61K31/40 ,  A61P25/28 ,  C07D207/08

CPC分类号： C07D207/08

摘要： As new compounds are provided a class of derivatives of actinonin represented by the general formula ##STR1## where R is a hydrogen or a lower alkyl group, which can exhibit the enzyme-inhibitory activities to a limited range of peptidases and show a remarkable enzyme-specificity, and which are effective to treat a cycloheximide-induced experimental amnesia in mice and are expectable to be useful to treat an amnesia in a mammalian animal, including human.

公开(公告)号：US4716221A

公开(公告)日：1987-12-29

申请号：US842286

申请日：1986-03-21

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Shinichi Kondo ,  Wataru Tanaka ,  Tomohisa Takita ,  Yoshio Nishimura ,  Hiroshi Yoshikawa

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Shinichi Kondo ,  Wataru Tanaka ,  Tomohisa Takita ,  Yoshio Nishimura ,  Hiroshi Yoshikawa

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P35/00 ,  C07H17/04 ,  C07H15/24

CPC分类号： C07H17/04

摘要： This invention relates to a novel 4'-demethyl-4-epipodophylltoxin derivative of the formula: ##STR1## (wherein R.sub.1 is a lower alkyl group; X.sub.1 and X.sub.2 are each a hydroxyl group or an amino group substituted by one or two lower alkyls, provided that either one of X.sub.1 and X.sub.2 is an amino group substituted by one or two lower alkyls and the other is a hydroxyl group) and salts thereof.

摘要翻译： 本发明涉及下式的新型4'-去甲基-4-表鬼臼毒素衍生物：其中R1是低级烷基; X1和X2分别是羟基或被一个或两个低级烷基取代的氨基 ，条件是X1和X2中的任一个是被一个或两个低级烷基取代的氨基，另一个是羟基）及其盐。

公开(公告)号：US4049497A

公开(公告)日：1977-09-20

申请号：US747470

申请日：1976-12-06

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Shinichi Kondo ,  Masaaki Ishizuka ,  Hiroshi Naganawa

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Shinichi Kondo ,  Masaaki Ishizuka ,  Hiroshi Naganawa

IPC分类号： C07G11/00

CPC分类号： A61K36/06 ,  C07G11/00 ,  Y10S435/886

摘要： There are disclosed two new antibiotics formerly denominated MC916-A and MC916-B and now called neothramycin A and neothramycin B which are potent inhibitors of the growth of leukemia cells, e.g. Leukema L-1210 cells in mice. They are produced by controlled fermentation of Streptomyces FERM-P 2452 (A.T.C.C. 31123).

摘要翻译： 已经公开了两种以前称为MC916-A和MC916-B的新抗生素，现在称为新西霉素A和新霉素B，其是白血病细胞生长的有效抑制剂，例如。 白血病L-1210细胞在小鼠中。 它们通过Frep-P 2452链霉菌（A.T.C.C. 31123）的对照发酵生产。

公开(公告)号：US4889926A

公开(公告)日：1989-12-26

申请号：US204363

申请日：1988-06-09

申请人： Tomoya Machinami ,  Takeshi Nakamura ,  Ken Nishihata ,  Shinichi Kondo ,  Tomio Takeuchi

发明人： Tomoya Machinami ,  Takeshi Nakamura ,  Ken Nishihata ,  Shinichi Kondo ,  Tomio Takeuchi

IPC分类号： C07H15/252

CPC分类号： C07H15/252

摘要： A new compound, i.e., 14-chlorodaunomycin, and its method of preparation are provided. The new compound, useful as an antitumor agent and as an intermediate in the preparation of (2"R)-4'-O-tetrahydropyranyladriamycin, is obtained by reaction of daunomycin with an alkyl ortho-formate and a brominating agent to produce a 14-bromo-13-dialkylketaldaunomycin, hydrolysis of the latter compound, then adding an excess of a solid metal/chloride to produce an acid addition salt of 14-chlorodaunomycin and concurrently salting out the latter compound from the reaction solution, followed by recovering the 14-chlorodaunomycin acid addition salt.

公开(公告)号：US4420473A

公开(公告)日：1983-12-13

申请号：US296923

申请日：1981-08-27

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Shinichi Kondo ,  Kiyoto Ishii

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Shinichi Kondo ,  Kiyoto Ishii

IPC分类号： C07H17/04 ,  A61K35/74 ,  A61P31/04 ,  A61P35/00 ,  C07G11/00 ,  C12P1/06 ,  C12P19/00 ,  C12P19/60 ,  C12R1/465 ,  A61K35/00

CPC分类号： C12R1/465 ,  C12P1/06

摘要： New antibiotic designated MF266 substance is now obtained from fermentaton of a new microorganism Streptomyces MF266-g4 (desposited under FERM-P 5401 or ATCC 31910). This new substance is useful as antibacterial agent and/or an antitumor agent for the inhibition of experimental animal tumors.

摘要翻译： 现在从新发微生物链霉菌MF266-g4的发酵得到新的指定为MF266物质的抗生素（在FERM-P 5401或ATCC 31910下进行）。 这种新物质可用作抑制实验动物肿瘤的抗菌剂和/或抗肿瘤剂。