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1. 发明授权

US5034517A Process for producing 2,6-dideoxy-2-fluoro-L-talopyranose 失效
标题翻译：制备2,6-二脱氧-2-氟-L-吡喃葡萄糖的方法
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。

2. 发明授权

US4914192A Mycaminosyl tylonolide derivatives 失效
公开(公告)号：US4914192A
公开(公告)日：1990-04-03
申请号：US244500
申请日：1988-09-14
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 denoted hydroxyl group, a lower alkanoyloxy group, benzyloxy 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.

3. 发明授权

US5101022A Mycaminosyl tylonolide derivatives 失效
标题翻译： MYCAMINOSYL TYLONOLIDE DERIVATIVES
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.

4. 发明授权

US4945081A Mycaminosyl tylonolide derivatives 失效
标题翻译：碳霉糖太乐内酯衍生物
公开(公告)号：US4945081A
公开(公告)日：1990-07-31
申请号：US232904
申请日：1988-08-16
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, benzyloxy 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.

5. 发明授权

US4794173A Mycaminosyl tylonolide derivatives 失效
标题翻译：碳霉糖太乐内酯衍生物
公开(公告)号：US4794173A
公开(公告)日：1988-12-27
申请号：US861537
申请日：1986-05-09
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 mat 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 ), and salts thereof.
摘要翻译：由以下通式表示的碳霉糖基太乐内酯衍生物（其中R 1表示羟基，低级烷酰氧基，苯甲酰氧基，叠氮基或任选被低级烷基或低级烷酰基取代的氨基）对于氢原子或羟基; R 3表示氢原子或甲酰基;并且表示双键或由...表示的基团）及其盐。

6. 发明授权

US4576931A 23-C-Substituted mycaminosyl tylonolide, pharmaceutical compositions and method of use 失效
标题翻译： 23-C-取代的碳霉糖太乐内酯，药物组合物和使用方法
公开(公告)号：US4576931A
公开(公告)日：1986-03-18
申请号：US719286
申请日：1985-04-03
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： C07H17/08 , A61K31/78
CPC分类号： C07H17/08
摘要： Novel 23-C-substituted mycaminosyl tylonolide of the general formula (I) ##STR1## wherein R.sup.1 represents a lower alkyl group, an aryl group, a lower alkenyl group or a lower alkynyl group, R.sup.2 represents a hydrogen atom or a hydroxyl group.These compounds have excellent antibacterial activities.
摘要翻译：通式（I）的新型23-C取代的碳霉糖基太乐内酯其中R 1表示低级烷基，芳基，低级烯基或低级炔基，R 2表示氢原子或羟基。这些化合物具有优良的抗菌活性。

7. 发明授权

US4477443A Tylosin derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译：泰乐菌素衍生物，它们的制剂和含有它们的药物组合物
公开(公告)号：US4477443A
公开(公告)日：1984-10-16
申请号：US395463
申请日：1982-07-06
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Tomio Takeuchi , Akihiro Tanaka , Hidenori Iwamoto , Shuichi Sakamoto
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Tomio Takeuchi , Akihiro Tanaka , Hidenori Iwamoto , Shuichi Sakamoto
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： Tylosin compounds of the formula ##STR1## wherein R.sub.1 represents a hydroxyl group; a halogen atom; ##STR2## group (wherein R.sub.5 is a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group and R.sub.6 is a hydrogen atom, a lower alkyl group which may be substituted by a hydroxyl group, an aryl group, an aralkyl group, a cycloalkyl group having 3-10 carbon atoms, --CO(O).sub.m --R.sub.7 group (wherein m is 0 or 1 and R.sub.7 is a lower alkyl group, an aryl group, an aralkyl group, a furanyl group, or a pyridyl group), or --CH.sub.2 --R.sub.13 group (wherein R.sub.13 is a mono-, di-, or trifluoromethyl group)); --N(CH.sub.2).sub.n group (wherein n is an integer of 2-15) which may be substituted by an oxo group, a hydroxyl group, a lower alkyl group, or a hydroxy lower alkyl group; an imidazolyl group, a morpholino group, or a piperazino group each may be substituted by a lower alkyl group; or --OOCCH.sub.2 --R.sub.8 group (wherein R.sub.8 is ##STR3## group (wherein R.sub.9 and R.sub.10, which may be the same or different, each is a hydrogen atom or a lower alkyl group; said R.sub.9 and R.sub.10 may be combined with each other to form an alkylene group having 3-7 carbon atoms) or --S--R.sub.11 group (wherein R.sub.11 is a furanyl group or a pyridyl group)); R.sub.2 represents a hydrogen atom or a lower alkanoyl group; R.sub.3 represents a methyl group or --CH.sub.2 CHO group; R.sub.4 represents a hydrogen atom or a hydroxyl group; A represents 0.dbd., ##STR4## line represents a single bond or a double bond; and line ---- represents a single bond, a double bond, or ; however, when said R.sub.1 is a hydroxyl group, said R.sub.3 is a methyl group and R.sub.4 is a hydrogen atom, or said line ---- is ; or when said R.sub.1 is a halogen atom, said R.sub.3 is a methyl group of said line ---- is .The foregoing compounds of this invention are useful as antibiotics.
摘要翻译：式“IMAGE”的泰乐菌素化合物，其中R 1表示羟基; 卤素原子; 基（其中R5是氢原子或可被羟基取代的低级烷基，R6是氢原子，可被羟基取代的低级烷基，芳基，芳烷基基团，具有3-10个碳原子的环烷基，-CO（O）m-R7基团（其中m为0或1，R7为低级烷基，芳基，芳烷基，呋喃基或吡啶基）或-CH 2 -R 13基（其中R 13是单 - ，二 - 或三氟甲基））; -N（CH 2）n基（其中n为2-15的整数），其可被氧代基，羟基，低级烷基或羟基低级烷基取代; 咪唑基，吗啉代基或哌嗪子基各自可以被低级烷基取代; 或-OOCCH 2 -R 8基团（其中R 8为<基团）（其中R 9和R 10可以相同或不同，各自为氢原子或低级烷基;所述R 9和R 10可彼此组合形成具有3-7个碳原子的亚烷基）或-S-R11基（其中R11是呋喃基或吡啶基））; R2表示氢原子或低级烷酰基; R3表示甲基或-CH2CHO基; R4表示氢原子或羟基; A代表0 =，线代表单键或双键; 线----代表单键，双键，或; 然而，当所述R 1为羟基时，所述R 3为甲基，R 4为氢原子，或者当所述R 1为卤素原子时，所述R 3为所述线----甲基。本发明的前述化合物可用作抗生素。

8. 发明授权

US4297485A Production of a selectively protected N-acylated derivative of an aminoglycosidic antibiotic 失效
标题翻译：制备氨基糖苷类抗生素的选择性保护的N-酰化衍生物
公开(公告)号：US4297485A
公开(公告)日：1981-10-27
申请号：US90591
申请日：1979-11-02
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi , Tomo Jikihara
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi , Tomo Jikihara
IPC分类号： C07H15/234 , C07H23/00 , C07H15/22
CPC分类号： C07H23/00 , C07H15/234
摘要： Aminoglycosidic antibiotic comprising a 6-0-(3"-aminoglycosyl)-2-deoxystreptamine optionally having a 4-0-(aminogycosyl) group, such as kanamycins, gentamicins, sisomicin, forms reversible complex with zinc cations by association of the zinc cations with some pairs of aminohydroxyl groups in the aminoglycoside, and the zinc-complexed amino groups are blocked from acylation. Reaction of this zinc complex with an acylation reagent having an amino-blocking acyl group brings about acylation of the non-complexed amino groups to give an N-acylated zinc complex, namely a complex of zinc cation with an N-acylated aminoglycosidic antibiotic derivative. Removal of zinc cations from N-acylated zinc complex yields a partially N-acylated aminoglycosidic antibiotic where 1- and 3"-amino groups are unprotected but all other amino groups protected with acyl group. Further reaction of this partially N-acylated product with a certain alkanoic acid or N-formyl-imidazole results in preferential acylation of 3"-amino group without 1-amino group being acylated, affording a 1-N-unprotected and other N-fully-protected derivative of the aminoglycosidic antibiotic which is valuable to be 1-N-acylated with .alpha.-hydroxy-.omega.-aminoalkanoic acid for high-yield production of known semi-synthetic 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-aminoglycosidic antibiotic.
摘要翻译：包含任选具有4-0-（氨基糖基）基团的6-0-（3“ - 氨基糖基）-2-脱氧神经胺的氨基糖苷类抗生素，如卡那霉素，庆大霉素，西索米星，与锌阳离子形成与锌阳离子的可逆复合物，在氨基糖苷中具有一对氨基羟基的阳离子和锌络合的氨基被封闭以进行酰化。该锌络合物与具有氨基封闭酰基的酰化试剂的反应导致非络合氨基的酰化，得到N-酰化锌络合物，即锌阳离子与N-酰化氨基糖苷类抗生素衍生物的络合物。从N-酰化锌络合物中除去锌阳离子产生部分N-酰化的氨基糖苷类抗生素，其中1-和3“ - 氨基未被保护，但是用酰基保护的所有其它氨基。该部分N-酰化产物与某种链烷酸或N-甲酰基 - 咪唑的进一步反应导致3'-氨基的优先酰化而没有1-氨基被酰化，得到1-N-未保护的和其它N- 氨基糖苷类抗生素的完全保护的衍生物，其有价值的是用α-羟基-ω-氨基链烷酸1-N-酰化，用于高产量生产已知的半合成的1-N-（α-羟基 - ω-氨基烷酰基）氨基糖苷类抗生素。

9. 发明授权

US5719130A Anthracycline derivative having a trifluoromethylated sugar 失效
标题翻译：具有三氟甲基化糖的蒽环类衍生物
公开(公告)号：US5719130A
公开(公告)日：1998-02-17
申请号：US714050
申请日：1996-09-09
申请人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi
发明人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi
IPC分类号： C07C31/42 , C07C43/178 , C07H13/04 , C07H15/18 , C07H15/252 , A61K31/70
CPC分类号： C07H13/04 , C07C31/42 , C07C43/1786 , C07H15/18 , C07H15/252
摘要： 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.
摘要翻译： PCT No.PCT / JP95 / 00407 Sec。 371日期1996年9月9日 102（e）1996年9月9日PCT 1995年3月10日PCT PCT。公开号WO95 / 24412 PCT 日期1995年9月14日现在已经生产出新的蒽环类衍生物，其具有比已被临床用作抗癌剂的道诺霉素，阿霉素等更高的抗肿瘤活性和较低的毒性。也就是说，通式（I）表示的道诺霉素酮或阿霉素酮衍生物：其中R是氢原子或羟基。

10. 发明授权

US5958889A Anthracycline derivatives having 4-amino-2,4,6-trideoxy-2-fluoro-mannopyranosyl group 失效
标题翻译：具有4-氨基-2,4,6-三脱氧-2-氟 - 甘露吡喃糖基的蒽环类衍生物
公开(公告)号：US5958889A
公开(公告)日：1999-09-28
申请号：US981255
申请日：1997-12-22
申请人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi
发明人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/244 , C07H15/252 , C07H1/00 , C07H15/24
CPC分类号： C07H15/252 , C07H15/244 , Y02P20/55
摘要： 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.
摘要翻译： PCT No.PCT / JP96 / 01697 Sec。 371 1997年12月22日第 102（e）1997年12月22日PCT PCT 1996年6月19日PCT公布。出版物WO97 / 00880 日期1月9日，19977-O-（4-氨基-2,4,6-三脱氧-2-氟-α-L-吡喃甘露糖基）道诺霉素酮或阿德米霉素现在合成为具有通式的道诺霉素酮或阿霉素酮衍生物，其中 R是氢原子或羟基。根据本发明的这些新化合物表现出优异的抗肿瘤活性，并且在水中的溶解度高，因此它们可用作抗肿瘤剂。

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