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公开(公告)号:US4508648A
公开(公告)日:1985-04-02
申请号:US422378
申请日:1982-09-24
IPC分类号: A61K31/675 , A61P31/04 , C07D477/20 , C07F9/6561 , C12P17/18 , C12R1/13 , C07D487/04 , A61K31/40
CPC分类号: C07D477/20 , C07F9/65611 , C12P17/184
摘要: Novel phosphoric ester of antibiotic OA-6129 presented by the formula ##STR1## wherein R is a hydrogen atom, hydroxyl or hydroxysulfonyloxy, and its salts and the preparation method thereof.
摘要翻译: 新型抗生素OA-6129的磷酸酯通过其中R为氢原子,羟基或羟基磺酰氧基及其盐及其制备方法由式
+ TR 呈现。 -
公开(公告)号:US4456592A
公开(公告)日:1984-06-26
申请号:US333950
申请日:1981-12-23
申请人: Yasushi Okumura , Kazuhiko Okamura , Yasuo Fugakawa , Tomoyuki Ishikura , Kageaki Kouno , Joseph Lein
发明人: Yasushi Okumura , Kazuhiko Okamura , Yasuo Fugakawa , Tomoyuki Ishikura , Kageaki Kouno , Joseph Lein
IPC分类号: A61K38/00 , C07K7/06 , A61K37/00 , C07C103/52
CPC分类号: C12R1/465 , C07K7/06 , A61K38/00 , Y10S930/19 , Y10S930/27
摘要: A group of novel depsipeptide antibiotics, neoviridogriseins I, II and III are produced by fermentation of Streptomyces sp. P8648 (FERM-P 3562; ATCC 31289). The antibiotics are highly active against Gram-positive bacteria and mycoplasmas.
摘要翻译: 一组新型depsipeptide抗生素,neoviridogriseins I,II和III通过Streptomyces sp。 P8648(FERM-P 3562; ATCC 31289)。 抗生素对革兰氏阳性菌和支原体具有高度的活性。
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公开(公告)号:US4451401A
公开(公告)日:1984-05-29
申请号:US394166
申请日:1982-07-01
申请人: Mitsuyasu Okabe , Takeo Yoshioka , Yasuo Fukagawa , Rokuro Okamoto , Kageaki Kouno , Tomoyuki Ishikura
发明人: Mitsuyasu Okabe , Takeo Yoshioka , Yasuo Fukagawa , Rokuro Okamoto , Kageaki Kouno , Tomoyuki Ishikura
IPC分类号: C07D477/20 , C12P17/18 , C07D487/04
CPC分类号: C07D477/20 , C12P17/184
摘要: A compound represented by the following formula ##STR1## wherein R represents a hydrogen atom or a methyl group,R.sup.1 represents a hydrogen atom or an ester residue, andR.sup.2 and R.sup.3 represent hydrogen atoms respectively, or taken together, a group of the formula ##STR2## in which each of R.sup.4 and R.sup.5 represents a hydrogen atom, a lower alkyl group or a phenyl group,and its salt; and a process for the production thereof.
摘要翻译: 由下式表示的化合物其中R表示氢原子或甲基,R1表示氢原子或酯残基,R2和R3分别表示氢原子,或一起形成, 其中R4和R5各自表示氢原子,低级烷基或苯基的式“IMAGE”及其盐; 及其生产方法。
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公开(公告)号:US4418192A
公开(公告)日:1983-11-29
申请号:US370212
申请日:1982-04-20
申请人: Hiroshi Tanaka , Takeo Yoshioka , Yasutaka Shimauchi , Toshikazu Oki , Tomoyuki Ishikura , Tomio Takeuchi , Hamao Umezawa
发明人: Hiroshi Tanaka , Takeo Yoshioka , Yasutaka Shimauchi , Toshikazu Oki , Tomoyuki Ishikura , Tomio Takeuchi , Hamao Umezawa
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号: C07H15/252
摘要: Disclosed are novel anthracyclinone glycosides represented by the chemical formula ##STR1## wherein R.sup.1 is hydrogen or methyl;R.sup.2 is hydrogen or hydroxyl;R.sup.3 is hydrogen or methoxycarbonyl;R.sup.4 is two hydrogen atoms or an oxygen atom;R.sup.5 is hydrogen, hydroxyl or --OCOX (wherein X is lower alkyl or aralkyl);R.sup.6 is amino, monomethylamino or dimethylamino;R.sup.7 is hydrogen or acetyl; andR.sup.8 is hydrogen or L-cinerulose A ##STR2## but, when R.sup.1 and R.sup.3 are hydrogen and methoxycarbonyl respectively, R.sup.2 is hydrogen; R.sup.4 is two hydrogen atoms; R.sup.5 is hydrogen; R.sup.6 is amino, monoethylamino or dimethylamino; R.sup.7 is acetyl; and R.sup.8 is L-cinerulose A,and their acid addition salts and a method for preparation thereof which consists of treating O-alpha-L-cinerulosyl-(1.fwdarw.4)-O-(3-O-acetyl-2-deoxy-alpha-L-fucosyl)-(1.fwdarw.4)-alpha-L-rhodosamine with corresponding aglycones.
摘要翻译: 公开了由化学式(IMAGE)(I)表示的新型蒽环酸苷,其中R1是氢或甲基; R2是氢或羟基; R3是氢或甲氧基羰基; R4是两个氢原子或氧原子; R5是氢,羟基或-OCOX(其中X是低级烷基或芳烷基); R6是氨基,单甲基氨基或二甲基氨基; R7是氢或乙酰基; 并且R 8是氢或L-果糖醛酸A,但是当R 1和R 3分别是氢和甲氧基羰基时,R 2是氢; R4是两个氢原子; R5是氢; R6是氨基,单乙基氨基或二甲基氨基; R7是乙酰基; R8为L-丝瓜糖苷A及其酸加成盐及其制备方法,其由O-α-L-脯氨酰基 - (1-> 4)-O-(3-O-乙酰基-2-脱氧 α-L-岩藻糖基) - (1→4)-alpha-L-罗丹明与相应的糖苷配基。
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公开(公告)号:US4373094A
公开(公告)日:1983-02-08
申请号:US288072
申请日:1981-07-29
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P19/56 , A61K31/71 , C07H15/24
CPC分类号: C07H15/252 , C12P19/56 , C12R1/465
摘要: New anthracycline compounds, 2-hydroxy-aclacinomycins M, N, S and T having potent antitumor activity and low toxicity, and the processes for the preparation thereof from 2-hydroxy-aclacinomycin A by reduction or acid hydrolysis are disclosed.
摘要翻译: 公开了新的蒽环类化合物,具有有效的抗肿瘤活性和低毒性的2-羟基 - 阿拉伯霉素M,N,S和T,并且通过还原或酸水解由2-羟基 - 阿拉伯霉素A制备它们的方法。
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公开(公告)号:US4897470A
公开(公告)日:1990-01-30
申请号:US34879
申请日:1987-04-06
申请人: Akihiro Yoshimoto , Osamu Jodo , Yoshio Watanabe , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa, deceased
发明人: Akihiro Yoshimoto , Osamu Jodo , Yoshio Watanabe , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa, deceased
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P29/00 , C12R1/465
CPC分类号: C07H15/252
摘要: New anthracycline antibiotics of a formula (I) are provided, which are usable as an anticancer agent ##STR1## (where R represents a hydrogen atom or a hydroxyl group). The antibiotics (I) can be produced by incubation of a dye-nonproductive or hardly dye-productive mutant strain which has an ability of converting .alpha.-citromycinone or .beta.-isorhodomycinone into the antibiotics (I), in the presence of .alpha.-citromycinone or .beta.-isorhodomycinone in a pertinent nutrient medium.
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公开(公告)号:US4853407A
公开(公告)日:1989-08-01
申请号:US197446
申请日:1988-05-20
IPC分类号: C12N9/99 , A61K31/19 , A61K31/194 , A61K31/40 , A61K31/403 , A61K31/4035 , A61P43/00 , C07C67/00 , C07C313/00 , C07C323/59 , C07D209/48
CPC分类号: C07D209/48
摘要: Compounds represented by formula ##STR1## wherein Y.sup.1 and Y.sup.2 are identical or different, and respectively denote benzoylamino groups or phthalimide groups. This compound is useful for inhibition of dipeptidase.
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公开(公告)号:US4812563A
公开(公告)日:1989-03-14
申请号:US24160
申请日:1987-03-10
IPC分类号: C07D477/00 , C07C205/42 , C07D205/085 , C07D403/04 , C07D477/24 , C07D487/04
CPC分类号: C07D403/04 , C07C205/42 , C07D205/085 , C07D477/24 , Y02P20/55
摘要: A compound represented by the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group; R.sub.2 represents a lower alkyl group, a lower haloalkyl group, an aralkyl group, or a group of the formula --COOR.sub.4 or --SO.sub.2 R.sub.5 in which R.sub.4 represents an alkyl group or a substituted or unsubstituted aralkyl group and R.sub.5 represents an alkyl group or a substituted or unsubstituted aryl group; and R.sub.3 represents a hydrogen atom or a carboxyl protecting group which can be easily split off. This compound is useful in the production of a 6-(disubstituted amino)carbapenem-series antibiotic.
摘要翻译: 由式(I)表示的化合物,其中R 1表示低级烷基或低级卤代烷基; R2表示低级烷基,低级卤代烷基,芳烷基或式-COOR4或-SO2R5的基团,其中R4表示烷基或取代或未取代的芳烷基,R5表示烷基或取代的 或未取代的芳基; 并且R 3表示氢原子或可以容易地分离的羧基保护基。 该化合物可用于生产6-(二取代氨基)碳青霉烯类抗生素。
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公开(公告)号:US4778883A
公开(公告)日:1988-10-18
申请号:US16106
申请日:1987-02-18
IPC分类号: C07D205/08 , C07B39/00 , C07D405/04 , C07F7/10
CPC分类号: C07D205/08 , Y02P20/55
摘要: An azetidinone derivative of the formula ##STR1## wherein R.sub.1 represents a formyl group, a carboxyl group, an acetyloxy group or a group of the formula ##STR2## in which R.sub.2 and R.sub.3 each represent a lower alkyl group or together represent a lower alkylene group, and Z represents a hydrogen atom or an amino-protecting group.
摘要翻译: 式(I)的氮杂环丁酮衍生物,其中R 1表示甲酰基,羧基,乙酰氧基或式“IMAGE”的基团,其中R 2和R 3各自表示低级烷基或一起表示 低级亚烷基,Z表示氢原子或氨基保护基。
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公开(公告)号:US4528397A
公开(公告)日:1985-07-09
申请号:US479982
申请日:1983-03-29
IPC分类号: C12N9/99 , A61K31/19 , A61K31/195 , A61K31/40 , A61P43/00 , C07C67/00 , C07C229/16 , C07C313/00 , C07C323/51 , C07C323/52 , C07D209/48 , C07C101/24
CPC分类号: C07D209/48 , A61K31/40 , C07C323/51
摘要: An aminocarboxylic acid derivative represented by the formula ##STR1## wherein R.sub.1 and R.sub.2, independently from each other, represent a hydrogen atom or an alkyl group which may have a substituent, and Y represents --NH-- or --S--, provided that when Y represents --NH--, at least one of R.sub.1 and R.sub.2 represents an alkyl group which may have a substituent. These compounds have excellent inhibitory activity on dipeptidase in animals, and are useful for administration in combination with carbapenem antibiotics.
摘要翻译: 由式(Ia)表示的氨基羧酸衍生物,其中R1和R2彼此独立地表示氢原子或可具有取代基的烷基,Y表示-NH-或-S-,提供 当Y表示-NH-时,R 1和R 2中的至少一个表示可以具有取代基的烷基。 这些化合物对动物中的二肽酶具有优异的抑制活性,并且可用于与碳青霉烯类抗生素组合施用。
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