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161. 发明授权

US4612372A Tylosin derivatives 失效
标题翻译：泰乐菌素衍生物
公开(公告)号：US4612372A
公开(公告)日：1986-09-16
申请号：US754568
申请日：1985-07-12
申请人： Takeo Yoshioka , Miharu Maeda , Rokuro Okamoto , Yasutaka Shimauchi , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
发明人： Takeo Yoshioka , Miharu Maeda , Rokuro Okamoto , Yasutaka Shimauchi , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Novel tylosin derivatives are represented by formula: ##STR1## wherein R represents a hydrogen atom, an acetyl group or a propionyl group; X represents a group --CO-- or --SO.sub.2 --; Y represents a fluorine atom, an acetyl group, a methanesulfonyl group, a methylthio group, a benzoyl group or a methoxy group bound to the benzyl group at the 2-position or 4-position; and Z represents a hydrogen atom or a D-mycinose residue: ##STR2## The tylosin derivatives which are antibiotics of macrolide type provide improved antibacterial activity and improved ability of absorption and excretion in vivo.
摘要翻译：新型泰乐菌素衍生物由下式表示：其中R代表氢原子，乙酰基或丙酰基; X表示-CO-或-SO 2 - 基团; Y表示在2位或4位与苄基结合的氟原子，乙酰基，甲磺酰基，甲硫基，苯甲酰基或甲氧基; Z代表氢原子或D-霉菌素残留物：作为大环内酯类抗生素的泰乐菌素衍生物提供了改善的抗菌活性和提高体内吸收和排泄的能力。

162. 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。

163. 发明授权

US4565861A Serirubicum 失效
标题翻译：丝。属
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。

164. 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。

165. 发明授权

US4525465A Water-insoluble biospecific absorbent containing argininal derivative 失效
标题翻译：含有精氨酸衍生物的水不溶性生物特异性吸收剂
公开(公告)号：US4525465A
公开(公告)日：1985-06-25
申请号：US540125
申请日：1983-10-07
申请人： Tetsuya Someno , Kazuo Kato , Tetsushi Saino , Shinichi Ishii , Tomio Takeuchi , Hamao Umezawa
发明人： Tetsuya Someno , Kazuo Kato , Tetsushi Saino , Shinichi Ishii , Tomio Takeuchi , Hamao Umezawa
IPC分类号： B01J20/32 , C12N9/50 , C12N9/72 , B01J20/26 , A61K37/54 , C07C103/52
CPC分类号： C12N9/6462 , B01J20/24 , B01J20/261 , B01J20/286 , B01J20/3092 , B01J20/321 , B01J20/3212 , B01J20/3217 , B01J20/3219 , B01J20/3251 , B01J20/3253 , B01J20/3255 , C12N9/50 , C12Y304/21073 , B01J2220/54 , B01J2220/58
摘要： A biospecific adsorbent comprising pyroglutamyl-lysyl-leucyl-argininal combined with a water-insoluble support is provided. This biospecific adsorbent is useful as an adsorbent for use in affinity chromatography and can be utilized for the purification of proteases such as urokinase.
摘要翻译：提供了包含焦谷氨酰赖氨酰 - 亮氨酰 - 精氨酸与水不溶性载体组合的生物特异性吸附剂。该生物特异性吸附剂可用作用于亲和层析的吸附剂，并可用于纯化蛋白酶如尿激酶。

166. 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。

167. 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。

168. 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。

169. 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。

170. 发明授权

US4472304A (Amido)N-substituted bleomycins, salts thereof and process for preparation thereof 失效
标题翻译：（酰氨基）N-取代的白霉素，其盐及其制备方法
公开(公告)号：US4472304A
公开(公告)日：1984-09-18
申请号：US451437
申请日：1982-12-20
申请人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
发明人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
IPC分类号： C07H15/26 , A61K31/70 , A61K31/7028 , A61P35/00 , C07H17/00 , C07K9/00 , C07C103/52
CPC分类号： C07K9/003 , Y10S930/19
摘要： A promising carcinostatic (amido)N-substituted bleomycin represented by the following formula, or a salt thereof and a process for the preparation thereof: ##STR1## wherein BM represents a moiety of bleomycin skeleton; X represents an alkyl of 1 to 18 carbon atoms, an aminoalkyl of 1 to 12 carbon atoms, a lower alkyl having a halogen, phenyl indolyl, 5- or 6-membered heterocyclic group, or (lower)alkylamino (the alkyl group may have a substituent group) as a substituent, naphthyl, thiazolyl, or N-phenyl(lower)alkylpiperazinyl; and R represents a terminal amino residue of the bleomycin.
摘要翻译：由下式表示的有希望的制癌（酰氨基）N-取代的博来霉素或其盐及其制备方法：其中BM表示博来霉素骨架的部分; X表示1〜18个碳原子的烷基，1〜12个碳原子的氨基烷基，具有卤素的低级烷基，苯基吲哚基，5元或6元杂环基或（低级）烷基氨基（该烷基可以具有取代基），萘基，噻唑基或N-苯基（低级）烷基哌嗪基; R代表博来霉素的末端氨基残基。

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