公开(公告)号：US4267312A

公开(公告)日：1981-05-12

申请号：US75302

申请日：1979-09-12

申请人： Toshikazu Oki ,  Akihiro Yoshimoto ,  Taiji Inui ,  Tomio Takeuchi ,  Hamao Umezawa

发明人： Toshikazu Oki ,  Akihiro Yoshimoto ,  Taiji Inui ,  Tomio Takeuchi ,  Hamao Umezawa

IPC分类号： C07H15/252 ,  C12P19/56 ,  C12R1/465 ,  A61K31/71 ,  C07H15/24

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

摘要： New anthracycline derivatives, 1-hydroxy-13-dihydrodaunomycin and N-formyl-1-hydroxy-13-dihydrodaunomycin are produced by microbial transformation of .epsilon.-pyrromycinone and .epsilon.-isorhodomycinone with daunomycin-producing streptomyces and their mutants. The derivatives herein are useful as cancer chemotherapeutic agents.

摘要翻译： 新的蒽环类衍生物，1-羟基-13-二氢青霉素和N-甲酰基-1-羟基-13-二氢青霉素通过ε-吡咯酮酮和ε-异亮霉素酮与道诺霉素生产链霉菌及其突变体的微生物转化产生。 本文的衍生物可用作癌症化学治疗剂。

公开(公告)号：US4245045A

公开(公告)日：1981-01-13

申请号：US37804

申请日：1979-05-10

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Toshikazu Oki ,  Taiji Inui

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Toshikazu Oki ,  Taiji Inui

IPC分类号： C07H15/252 ,  C12P19/56

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

摘要： New anthracycline glycosides designated MA 144-G1, -G2, -L, -S1, -N1, -U1 and -Y which inhibit the growth of gram-positive bacteria and mammalian tumors are produced by fermentation of certain species of Streptomyces and by the chemical or enzymatic conversion of certain anthracycline glycosides. New microbiological and chemical processes are also provided for preparation of the anthracycline glycosides MA 144-S2 and -U2 which have been found to be identical with the previously reported anthracyclines, marcellomycin and musettamycin.

摘要翻译： 名称为MA 144-G1，-G2，-L，-S1，-N1，-U1和-Y的新型蒽环类苷，其抑制革兰氏阳性细菌和哺乳动物肿瘤的生长是通过某些种类的链霉菌的发酵和 某些蒽环类苷的化学或酶转化。 还提供了新的微生物和化学方法用于制备蒽环类甙MA 144-S2和-U 2，其已被发现与先前报道的蒽环霉素，马塞罗霉素和musettamycin相同。

公开(公告)号：US4238507A

公开(公告)日：1980-12-09

申请号：US21222

申请日：1979-03-16

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Takaaki Aoyagi ,  Masaaki Ishizuka ,  Hajime Morishima ,  Ikuo Matsumoto ,  Takuzo Yamamoto

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Takaaki Aoyagi ,  Masaaki Ishizuka ,  Hajime Morishima ,  Ikuo Matsumoto ,  Takuzo Yamamoto

IPC分类号： A61K31/195 ,  A61P37/00 ,  A61P37/04 ,  C07C51/00 ,  C07C65/01 ,  C07C67/00 ,  C07C227/00 ,  C07C227/02 ,  C07C227/18 ,  C07C227/20 ,  C07C227/26 ,  C07C229/36 ,  C07D317/46 ,  C07D319/08 ,  A01N37/12 ,  C07C101/72

CPC分类号： C07D319/08 ,  C07D317/46 ,  Y02P20/55

摘要： A new compound having the formula ##STR1## and now designated forphenicinol is produced, which exhibits an immunopotentiating activity. This new compound as well as its pharmaceutically acceptable salts and hydrates are useful for immunotherapy and treatment of immune diseases and disorders in living animals, including human beings. The new compound can be produced by hydrolysis of the corresponding aminonitrile compound of the formula ##STR2## or by reduction of forphenicine.

摘要翻译： 产生具有式“IMAGE”和现在指定为苯酚的新化合物，其具有免疫增强活性。 这种新化合物及其药学上可接受的盐和水合物可用于免疫治疗和治疗包括人在内的活的动物中的免疫疾病和病症。 新化合物可以通过水解相应的式“IMAGE”的氨基腈化合物或通过还原吩噻嗪来制备。

公开(公告)号：US4207313A

公开(公告)日：1980-06-10

申请号：US838617

申请日：1977-10-03

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Toshikazu Oki ,  Taiji Inui

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Toshikazu Oki ,  Taiji Inui

IPC分类号： C07H15/252 ,  C12P19/56 ,  A61K31/71 ,  C07H15/24

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

摘要： New anthracycline glycosides designated MA 144-G1, -G2, -L, -S1, -N1, -U1 and -Y which inhibit the growth of gram-positive bacteria and experimental animal tumors are produced by fermentation of certain species of Streptomyces and by the chemical or enzymatic conversion of certain anthracycline glycosides. New microbiological and chemical processes are also provided for preparation of the anthracycline glycosides MA 144-S2 and -U2 which have been found to be identical with the previously reported anthracyclines, marcellomycin and musettamycin.

摘要翻译： 名称为MA 144-G1，-G2，-L，-S1，-N1，-U1和-Y的新型蒽环类苷，其抑制革兰氏阳性细菌和实验动物肿瘤的生长，是通过某些种类的链霉菌的发酵和 某些蒽环类苷的化学或酶转化。 还提供了新的微生物和化学方法用于制备蒽环类甙MA 144-S2和-U 2，其已被发现与先前报道的蒽环霉素，马塞罗霉素和musettamycin相同。

公开(公告)号：US4164567A

公开(公告)日：1979-08-14

申请号：US801492

申请日：1977-05-31

申请人： Hamao Umezawa ,  Tomio Takeuchi

发明人： Hamao Umezawa ,  Tomio Takeuchi

IPC分类号： C12P1/06 ,  A61K35/00

CPC分类号： C12R1/465 ,  C12P1/06

摘要： There is provided a process for recovering macromomycin (hereinafter referred to as MCR) which comprises adding coagulants or coagulants and neutralizers to a culture filtrate saturated with ammonium sulfate and collecting the resulting precipitate containing MCR in a high yield at low centrifugal force. From the precipitate obtained, MCR powders can be prepared according to the methods described in U.S. Pat. No. 3,595,954 and others.

摘要翻译： 提供了一种用于回收大分子霉素（以下称为MCR）的方法，该方法包括将凝结剂或凝结剂和中和剂加入到用硫酸铵饱和的培养物滤液中，并以低离心力以高产率收集含有MCR的沉淀。 从得到的沉淀物中，可以根据美国专利No. 第3,595,954号等。

公开(公告)号：US4163839A

公开(公告)日：1979-08-07

申请号：US858928

申请日：1977-12-09

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Shinichi Kondo ,  Masami Shimazaki

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Shinichi Kondo ,  Masami Shimazaki

IPC分类号： C07H19/052 ,  C07H19/16 ,  C07H19/04 ,  A61K31/70

CPC分类号： C07H19/16 ,  C07H19/052

摘要： A novel, unique nucleoside, 3-.beta.-D-ribofuranosyl-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-7-ol, named isocoformycin, of the formula ##STR1## is provided by ring expansion of derivatives of 9-.beta.-D-ribofuranosyl-6-hydroxymethyl-1,6-dihydropurine. Isocoformycin markedly inhibits deaminating enzymes which inactivate formycin and adenine arabinoside (also known as ara-A and Vidarabine). Formycin and adenine arabinoside are used as antiviral and antitumor agents in mammals and birds and isocoformycin is advantageous to prolong the activity and effect of formycin and adenine arabinoside.

摘要翻译： 一种新颖独特的核苷，3β-D-呋喃核糖基-3,6,7,8-四氢咪唑并[4,5-d] [1,3]二氮杂-醇，命名为异青霉素，式为“IMAGE” 由9-β-D-呋喃核糖基-6-羟甲基-1,6-二氢嘌呤衍生物的环扩展提供。 异青霉素显着抑制脱氨酶，其使得霉菌和阿拉伯糖腺苷（也称为ara-A和阿糖腺苷）失活。 霉菌素和阿拉伯糖腺苷在哺乳动物和鸟类中用作抗病毒和抗肿瘤剂，异青霉素有利于延长霉素和阿拉伯糖腺苷的活性和作用。

公开(公告)号：US4052449A

公开(公告)日：1977-10-04

申请号：US690457

申请日：1976-05-27

申请人： Hamao Umezawa ,  Takaaki Aoyagi ,  Tomio Takeuchi ,  Masa Hamada ,  Yoshiro Okami

发明人： Hamao Umezawa ,  Takaaki Aoyagi ,  Tomio Takeuchi ,  Masa Hamada ,  Yoshiro Okami

IPC分类号： C12P13/04 ,  C12P21/02 ,  C07C101/72

CPC分类号： C12P13/04 ,  C12P21/02

摘要： This invention provides a new chemical named bestatin which inhibits aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase, enhances the antitumor effect of bleomycin, has the chemical name [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine and has the following structure: ##STR1## and also provides a process for the production thereof which comprises cultivating a strain of streptomyces which produces bestatin in a nutrient medium under aerobic conditions until substantial activity inhibitory to aminopeptidase B is imparted to said cultured medium and then recovering said bestatin from said cultured medium. A preferred strain is Streptomyces olivoreticuli FERM-P No. 2590 (A.T.C.C. 31159).

公开(公告)号：US5288898A

公开(公告)日：1994-02-22

申请号：US56619

申请日：1993-05-04

申请人： Hamao Umezawa ,  Toshiharu Nagatsu ,  Tomio Takeuchi ,  Hajime Morishima ,  Yoshio Sawasaki ,  Hiroshi Takezawa ,  Fujinori Sasaki

发明人： Hamao Umezawa ,  Toshiharu Nagatsu ,  Tomio Takeuchi ,  Hajime Morishima ,  Yoshio Sawasaki ,  Hiroshi Takezawa ,  Fujinori Sasaki

IPC分类号： A61K31/195 ,  C07C229/36 ,  A61K31/24

CPC分类号： A61K31/195

摘要： As new compounds are now provided N-methyl-3-(3,4-dihydroxyphenyl)serine alkyl esters which are effective as an .alpha.-adrenergic and .beta.-adrenergic agent to stimulate the .alpha.-adrenergic and .beta.-adrenergic functions of the central nervous system of mammalian animals and are expectable to be useful for therapeutic treatment of disorders as invoked by reduced biological activities or functions of the .alpha.- and/or .beta.-adrenergic neurons. N-methyl-L-threo-3-(3,4-dihydroxyphenyl)serine (C.sub.1 -C.sub.6) alkyl esters are preferred amongst the new compounds of this invention.

摘要翻译： 由于新化合物现在提供作为（α） - 肾上腺素能和（β） - 肾上腺素能药物有效的N-甲基-3-（3,4-二羟基苯基）丝氨酸烷基酯，以刺激（α） - 肾上腺素能和（β ） - 哺乳动物中枢神经系统的肾上腺素能功能，并且预期可用于通过减少（α） - 和/或（β） - 肾上腺素能神经元的生物活性或功能引起的病症的治疗性治疗。 N-甲基-L-苏式-3-（3,4-二羟基苯基）丝氨酸（C1-C6）烷基酯在本发明的新化合物中是优选的。

公开(公告)号：US5101022A

公开(公告)日：1992-03-31

申请号：US650060

申请日：1991-02-04

申请人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomio Takeuchi ,  Akihiro Tanaka ,  Shuichi Sakamoto

发明人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomio Takeuchi ,  Akihiro Tanaka ,  Shuichi Sakamoto

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08 ,  Y02P20/55

摘要： Mycaminosyl tylonolide derivatives represented by the following general formula ##STR1## (wherein R.sup.1 denotes hydroxyl group, a lower alkanoyloxy group, benzoyloxy group, azido group, or amino group which may optionally be substituted with a lower alkyl or a lower alkanoyl radical; R.sup.2 stands for hydrogen atom or hydroxyl group; R.sup.3 expresses hydrogen atom or formyl group; and means a double bond or a radical represented by ##STR2## and salts thereof.

公开(公告)号：US5034517A

公开(公告)日：1991-07-23

申请号：US488871

申请日：1990-03-06

申请人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomio Takeuchi ,  Yasushi Takagi

发明人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomio Takeuchi ,  Yasushi Takagi

IPC分类号： A61K31/70 ,  A61K31/7024 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P31/04 ,  C07H1/00 ,  C07H5/02 ,  C07H13/04 ,  C07H13/06 ,  C07H15/04 ,  C07H15/252

CPC分类号： C07H5/02 ,  C07H13/04 ,  C07H15/04 ,  Y02P20/55

摘要： 2,6-Dideoxy-2-fluoro-L-talopyranose and 1-substituted derivatives thereof, including methyl 2,6-dideoxy-2-fluoro-L-talopyranoside and 3,4-di-O-protected-2,6-dideoxy-2-fluoro-L-talopyranosyl halides, are now provided and these new compounds are useful as intermediates for use in the synthesis of new compounds having antitumor activity, especially 7-O-(2,6-dideoxy-2-fluoro-.alpha.-L-talopyranosyl) daunomycinone or -adriamycinone. 2,6-Dideoxy-2-fluoro-L-talopyranose shows antibacterial activity. 2,6-Dideoxy-fluoro-L-talopyranose and the 1-substituted derivatives thereof may be produced by a multi-stage process starting from L-fucose.

摘要翻译： 2,6-二脱氧-2-氟-L-吡喃葡萄糖及其1-取代衍生物，包括2,6-二脱氧-2-氟-L-吡喃葡萄糖苷和3,4-二-O-保护的2,6-二 现在提供二脱氧-2-氟-L-吡喃葡萄糖基卤化物，这些新化合物可用作合成具有抗肿瘤活性的新化合物的中间体，特别是7-O-（2,6-二脱氧-2-氟 - α-L-吡喃葡萄糖基）道诺霉素或阿霉素酮。 2,6-二脱氧-2-氟-L-吡喃葡萄糖显示出抗菌活性。 2,6-二脱氧 - 氟-L-吡喃葡萄糖及其1-取代衍生物可以通过从L-岩藻糖开始的多阶段方法制备。