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31. 发明授权

US4008218A 1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin and the production thereof 失效
标题翻译： 1-N - （（S） - {60-取代的 - {107-氨基酰基） - 纳米颗粒或 - 瑞波霉素及其制备
公开(公告)号：US4008218A
公开(公告)日：1977-02-15
申请号：US559771
申请日：1975-03-19
申请人： Eiichi Akita , Tsutomu Tsuchiya , Shinichi Kondo , Shuntaro Yasuda , Sumio Umezawa , Hamao Umezawa
发明人： Eiichi Akita , Tsutomu Tsuchiya , Shinichi Kondo , Shuntaro Yasuda , Sumio Umezawa , Hamao Umezawa
IPC分类号： C07H15/224 , C07H15/23 , C07G11/00
CPC分类号： C07H15/224 , C07H15/23
摘要： An 1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin of the formula: ##STR1## wherein R is a hydrogen atom or .beta.-D-ribofuranosyl group of the formula ##STR2## and R.sub.3 is hydroxyl, amino-NH.sub.2 or acylamino group --NHR.sub.4 in which R.sub.4 is an acyl group, and n is a whole number of 1 to 4, may be produced by subjecting the corresponding O-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin of the formula ##STR3## or its hydroxyl-masked and amino-masked form, to the action of a basic medium to produce an acyl-migration product of the formula: ##STR4## and, optionally converting the amino-masking groups into hydrogen atoms and also the hydroxyl-masking group into hydrogen atom in a known manner if said amino-masking groups and said hydroxyl-masking groups are present in the acyl-migration product. The 1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin produced is characterized by its useful activity inhibitory to the growth of bacteria resistant to the parent substance neamine or ribostamycin.
摘要翻译：具有下式的1-N - （（S）-α-取代的ω-氨基酰基） - 微量胺或 - 瑞波霉素：其中R是式“IMAGE”的氢原子或β-D-呋喃核糖基， R 3是羟基，氨基-NH 2或酰基氨基-NHR 4，其中R 4是酰基，n是整数1至4，可以通过使相应的O - （（S）-α-取代的-ω- - 氨基酰基） - 或者其羟基掩蔽和氨基掩蔽形式的微生物胺或β-内啡霉素或碱性培养基，以产生下式的酰基迁移产物：如果所述氨基掩蔽基团和所述羟基掩蔽基团存在于酰基迁移产物中，则以已知的方式将氨基掩蔽基团转化成氢原子，并将羟基掩蔽基团转变为氢原子。产生的1-N - （（S）-α-取代的ω-氨基酰基） - 单胺或 - 生物霉素的特征在于其对母体neamine或核糖霉素具有抗性的细菌的生长有抑制作用。

32. 发明授权

US3959257A Production of coformycin and intermediates therefor 失效
标题翻译：共生霉素及其中间体
公开(公告)号：US3959257A
公开(公告)日：1976-05-25
申请号：US518030
申请日：1974-10-24
申请人： Hamao Umezawa , Kenji Maeda , Shinichi Kondo
发明人： Hamao Umezawa , Kenji Maeda , Shinichi Kondo
IPC分类号： C07H19/23 , C07H19/052 , C07H19/16 , C07H19/18
CPC分类号： C07H19/16 , C07H19/052
摘要： This invention relates to a process for the preparation of coformycin, 3-(.beta.-D-ribofuranosyl)-6,7,8-trihydroimidazo[4,5-d][1,3]diazepin-8(R)-ol, through a synthetic route from a new derivative of 9-.beta.-D-ribofuranosyl-purine and other synthetic intermediates involved in the process and their preparation.
摘要翻译：本发明涉及一种制备共转霉素3-（β-D-呋喃核糖基）-6,7,8-三氢咪唑并[4,5-d] [1,3]二氮杂-8（R） - 醇的方法，通过合成路线从9β-D-呋喃核糖基嘌呤和其他合成中间体的新衍生物参与该方法及其制备。

33. 发明授权

US4983328A N-(4-(3-aminopropyl)aminobutyl)-2-(.omega.-gua nidino-fatty-acid-amido(-2-substituted-ethanamide, salt thereof, and process for preparation thereof 失效
标题翻译： N-（4-（3-氨基丙基）氨基丁基）-2-（ω-胍基 - 脂肪酸 - 酰胺基（-2-取代的乙酰胺，其盐，及其制备方法
公开(公告)号：US4983328A
公开(公告)日：1991-01-08
申请号：US170611
申请日：1988-03-15
申请人： Hamao Umezawa , Tomio Takeuchi , Shinichi Kondo , Hironobu Iinuma , Daishiro Ikeda , Teruya Nakamura , Akio Fujii
发明人： Hamao Umezawa , Tomio Takeuchi , Shinichi Kondo , Hironobu Iinuma , Daishiro Ikeda , Teruya Nakamura , Akio Fujii
IPC分类号： A61K31/16 , A61P35/00 , C07C67/00 , C07C239/00 , C07C279/14 , C07D209/48 , C12P13/02
CPC分类号： C07D209/48 , C07C279/14 , C12P13/02 , Y10S514/908
摘要： N-[4-(3-Aminopropyl)aminobutyl]-2-(.omega.-guanidino-fatty acid-amido)-2-substituted-ethanamides represented by the general formula ##STR1## wherein Y represents --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH or ##STR2## R represents a hydrogen atom, an alkyl group of 1 to 4 carbon atoms which may have a hydroxyl group as substituent, or a benzyl group, and n is an integer of from 1 to 8, provided that when Y is ##STR3## and n is 4, R represents the groups other than the hydrogen atom; salt thereof having antitumor activity in experimental animal tumors and a process for the preparation thereof is provided.

34. 发明授权

US4547567A Derivatives of 4'-demethyl-4-epipodophyllotoxin 失效
标题翻译： 4'-去甲基-4-表鬼臼毒素的衍生物
公开(公告)号：US4547567A
公开(公告)日：1985-10-15
申请号：US631999
申请日：1984-07-18
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 , C07H15/26 , C07H17/04 , C07H15/24
CPC分类号： C07H17/04 , Y02P20/55
摘要： This invention relates to novel 4'-demethyl-4-epipodophyllotoxin derivatives represented by the general formula (I), and salts thereof: ##STR1## wherein R is a lower alkyl group, and X.sub.1 and X.sub.2 are independently a hydroxyl group or an amino group, the one being an amino group and the other being a hydroxyl group. These novel derivatives have a high carcinostatic activity and a relatively high water solubility and hence are expected to be useful as carcinostatics.
摘要翻译：本发明涉及由通式（I）表示的新型4'-去甲基-4-表鬼臼毒素衍生物及其盐：其中R为低级烷基，且X 1和X 2独立地为羟基或氨基，一个是氨基，另一个是羟基。这些新型衍生物具有高的制癌活性和较高的水溶性，因此预期可用作制癌剂。

35. 发明授权

US4518532A N-[4-(3-aminopropyl)-aminobutyl]-2-(.omega.-gua nidino-fatty-acid-amido)-2-substituted-ethanamide and salt thereof 失效
标题翻译： N- [4-（3-氨基丙基） - 氨基丁基] -2-（ω-胍基 - 脂肪酸 - 酰氨基）-2-取代的乙酰胺及其盐
公开(公告)号：US4518532A
公开(公告)日：1985-05-21
申请号：US426372
申请日：1982-09-29
申请人： Hamao Umezawa , Tomio Takeuchi , Shinichi Kondo , Hironobu Iinuma , Daishiro Ikeda , Teruya Nakamura , Akio Fujii
发明人： Hamao Umezawa , Tomio Takeuchi , Shinichi Kondo , Hironobu Iinuma , Daishiro Ikeda , Teruya Nakamura , Akio Fujii
IPC分类号： A61K31/16 , A61P35/00 , C07C67/00 , C07C239/00 , C07C279/14 , C07D209/48 , C12P13/02 , C07C129/12 , A61K31/155
CPC分类号： C07D209/48 , C07C279/14 , C12P13/02 , Y10S514/908
摘要： N-[4-(3-Aminopropyl)aminobutyl]-2-(.omega.-guanidino-fatty acid-amido)-2-substituted-ethanamides represented by the general formula ##STR1## wherein Y represents --(CH.sub.2 --CH.sub.2 --, --CH.dbd.CH or ##STR2## R represents a hydrogen atom, an alkyl group of 1 to 4 carbon atoms which may have a hydroxyl group as substituent, or a benzyl group, and n is an integer of from 1 to 8, provided that when Y is ##STR3## and n is 4, R represents the groups other than the hydrogen atom; a salt thereof having antitumor activity in experimental animal tumors and a process for the preparation thereof is provided.
摘要翻译：由通式“IMAGE”I表示的N- [4-（3-氨基丙基）氨基丁基] -2-（ω-胍基 - 脂肪酸 - 酰胺基）-2-取代的乙酰胺，其中Y表示 - （CH 2 -CH 2 - ， - -CH = CH或R 1表示氢原子，可以具有羟基作为取代基的碳原子数1〜4的烷基或苄基，n表示1〜8的整数，条件是当Y为且n为4时，R表示氢原子以外的基团，其在实验动物肿瘤中具有抗肿瘤活性的盐及其制备方法。

36. 发明授权

US4486419A 5,2',3',4',4",6"-Hexadeoxykanamycin and its 1-N-acylated derivative 失效
标题翻译： 5,2'，3'，4'，4“，6” - 六脱氧卡那霉素及其1-N-酰化衍生物
公开(公告)号：US4486419A
公开(公告)日：1984-12-04
申请号：US532058
申请日：1983-09-14
申请人： Hamao Umezawa , Shinichi Kondo
发明人： Hamao Umezawa , Shinichi Kondo
IPC分类号： C07H15/234 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： 5,2',3',4',4",6"-Hexadeoxykanamycin and 1-N-[(S)-4-amino-2-hydroxybutyryl]-5,2',3',4',4",6"-hexadeoxykanamycin are now provided, which are each a new compound useful as antibacterial agent. The hexadeoxykanamycin is semi-synthetically produced from 3',4'-dideoxykanamycin through consecutive steps which are ingeniously combined with each other to remove the 5-, 2'-, 4"- and 6"-hydroxyl groups. The 1-N-acylated hexadeoxykanamycin is produced by acylating the 1-amino group of hexadeoxykanamycin with (S)-4-amino-2-hydroxybutyric acid.
摘要翻译： 5,2'，3'，4'，4“，6” - 六氧基卡那霉素和1 -N - [（S）-4-氨基-2-羟基丁酰基] -5,2'，3'，4' 现在提供4“，6” - 六脱氧卡那霉素，它们各自是可用作抗菌剂的新化合物。通过连续步骤，将3'，4'-二脱氧卡那霉素半合成生成六脱氧卡那霉素，彼此巧妙地组合以除去5-，2'-，4“和6” - 羟基。通过用（S）-4-氨基-2-羟基丁酸将6-脱氧卡那霉素的1-氨基酰化来制备1-N-酰化的六脱氧卡那霉素。

37. 发明授权

US4479943A 3-Demethoxyistamycin B, the 2"-N-formimidoyl derivative thereof and pharmaceutical composition containing same 失效
标题翻译： 3-去甲氧草霉素B，其2'-N-亚氨基衍生物和含有它们的药物组合物
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。

38. 发明授权

US4474946A Di-N.sup.6', O.sup.3 -Demethylistamycin A preparation 失效
标题翻译： Di-N6'，O3-Demethylistamycin A制剂
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。

39. 发明授权

US4406891A N-Methanesulfonic acid derivatives of istamycin A or B and production thereof 失效
标题翻译：伊曲霉素A或B的N-甲磺酸衍生物及其制备
公开(公告)号：US4406891A
公开(公告)日：1983-09-27
申请号：US289963
申请日：1981-08-04
申请人： Hamao Umezawa , Shinichi Kondo
发明人： Hamao Umezawa , Shinichi Kondo
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
摘要： As new semi-synthetic antibiotic derivative are provided N-methanesulfonic acid derivatives of istamycin A or B which are lower toxic than the parent antibiotic and retain usefully high antibacterial activity. They are produced by N-sulfomethylation in such way that istamycin A or B is reacted with an aldehyde such as paraformaldehyde and sulfurous acid or sulfite reagent.
摘要翻译：作为新的半合成抗生素衍生物，提供比母体抗生素低毒的伊曲霉素A或B的N-甲磺酸衍生物，并保持有效的高抗菌活性。它们通过N-磺甲基化产生，使得伊曲霉素A或B与醛如多聚甲醛和亚硫酸或亚硫酸盐试剂反应。

40. 发明授权

US4268664A Process for the preparation of 1-N-isoseryl- or 1-N-(L-4-amino-2-hydroxybutyryl)-3',4'-dideoxykanamycin B and intermediates thereof 失效
标题翻译： 1-N-异丝氨酰基或1-N-（L-4-氨基-2-羟基丁酰基）-3'，4'-二脱氧卡那霉素B及其中间体的制备方法
公开(公告)号：US4268664A
公开(公告)日：1981-05-19
申请号：US97896
申请日：1979-11-26
申请人： Hamao Umezawa , Shinichi Kondo
发明人： Hamao Umezawa , Shinichi Kondo
IPC分类号： C07H15/234 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/236 , C07H15/22 , A61K31/71
CPC分类号： C07H15/234 , Y02P20/55
摘要： 1-N-Isoseryl- or 1-N-(L-4-amino-2-hydroxybutyryl)-3',4'-dideoxykanamycin B is prepared through a new route starting from 3',4'-dideoxy-3',4'-didehydrokanamycin B, which comprises the steps of protecting all or some of the four amino groups other than the 1-amino group of the starting material with an amino-protecting group, reacting the partially amino-protected derivative or derivatives thus formed with isoserine or L-4-amino-2-hydroxybutyric acid or a reactive derivative thereof having the amino group unprotected or protected whereby to acylate the 1-amino group of the former, eliminating the amino-protecting group or groups from the acylated product and reducing the 3',4'-olefinic double bond of the product by catalytic hydrogenation, the last two steps being effected in order or simultaneously or in the reverse order. Also provided are new, useful intermediate compounds during the process.
摘要翻译：通过从3'，4'-二脱氧-3'，4'-二脱氧-3'，4'-二脱氧-3'，4'-二脱氧-3'，4'-二脱氧-3 4'-脱氢卡那霉素B，其包括用氨基保护基保护除原料的1-氨基以外的四个氨基的全部或部分的步骤，使由此形成的部分氨基保护的衍生物或衍生物与异丝氨酸或L-4-氨基-2-羟基丁酸或其具有未被保护或被保护的氨基的反应性衍生物，从而酰化前者的1-氨基，从酰化产物中除去氨基保护基或还原通过催化氢化产物的3'，4'-烯烃双键，最后两个步骤按顺序或同时或以相反的顺序进行。还提供了在该过程中新的有用的中间体化合物。

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