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1.发明公开Novel oxetanocin derivatives and their salts as well as use thereof 失效Oxetanocinderivate，ihre Salze und ihre Verwendung。
公开(公告)号：EP0416605A1
公开(公告)日：1991-03-13
申请号：EP90117162.9
申请日：1990-09-06
发明人： Kurabayashi, Katsuhiko , Seki, Junichi , Machida, Haruo , Yoshikawa, Hiroshi , Hoshino, Hiroo , Saito, Seiichi , Kitagawa, Masayuki
IPC分类号： C07H19/02 , A61K31/70 , C07H19/052
CPC分类号： C07H19/02
摘要： Oxetanocin derivatives represented by formula:
wherein X represents H or
or a pharmacologically acceptable salt thereof exhibit an anti-viral activity. Anti-viral compositions comprising the oxetanocin derivatives or their pharmacologically acceptable salts as the effective ingredient are also provided.摘要翻译： 由式：其中X代表H或
或其药理学上可接受的盐代表的氧新霉素衍生物显示抗病毒活性。 还提供了包含氧杂环丁烯衍生物或其药理学上可接受的盐作为有效成分的抗病毒组合物。 -
公开(公告)号：EP0393611A2
公开(公告)日：1990-10-24
申请号：EP90107311.4
申请日：1990-04-18
发明人： Saito, Seiichi , Hasegawa, Shigeru , Kitagawa, Masayuki , Shimada, Nobuyoshi , Yamashita, Noriyuki
CPC分类号： C07H19/02
摘要： The present invention provides a novel process for producing oxetanocin G by hydrolysis of alkoxylated 2-amino-oxetanocin A thereby to convert C-NH 2 at the 6-position thereof into C=O.
Oxetanocin G is expectedly useful as an antiviral agent.摘要翻译： 本发明提供了通过烷氧基化2-氨基 - 氧杂环丁烷A的水解制备氧杂环丁烷G的新方法，从而将其6位上的C-NH 2转化为@ C = O。 氧新霉素G有望用作抗病毒剂。
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3.发明公开Novel antibiotics NK374186A, NK374186B, NK374186B3 and NK374186C3, process for producing the same, and use of the same 失效抗生素NK374186A，NK374186B，NK374186B3和NK374186C3，其制备方法及其用途。
公开(公告)号：EP0525361A1
公开(公告)日：1993-02-03
申请号：EP92110170.5
申请日：1992-06-16
发明人： Morino, Tomio , Nishimoto, Masakazu , Nishide, Mit uyuki , Masuda, Akira , Yamada, Masatoshi , Kawano, Eiji , Nishikiori, Takaaki , Saito, Seiichi
摘要： Novel antibiotics NK374186A, NK374186B, NK374186B3 and NK374186C3 having antibacterial, antineoplastic, immunomodulation, and liver regeneration promoting activities are provided.
NK374186A, NK374186B, NK374186B3 and NK374186C3 are obtained by culturing NK374186 strain (FERM P-12285) (FERM-BP 3870) belonging to the genus Penicillium. NK374186A is a compound represented by a rational formula of C 34 H 61 N 12 S 9 and having a molecular weight of M+ 735 (FD-MS m/z); NK374186B is a compound represented by a rational formula of C 34 H 61 N 3 O 9 and having a molecular weight of M + 655 (FD-MS m/z); NK374186B3 is a compound represented by a rational formula of C 34 H 61 N 3 O 9 and having a molecular weight of M + 655 (FD-MS m/z); and NK374186C3 is a compound represented by a rational formula of C 32 H 59 N 3 O 7 and having a molecular weight of M+ 597 (FD-MS m/z).摘要翻译： 提供了新的抗生素NK374186A NK374186B NK374186B3和NK374186C3具有抗菌，抗肿瘤，免疫调节，以及肝脏的再生促销廷活动。 NK374186A NK374186B NK374186B3和NK374186C3通过培养属于青霉属菌株NK374186（FERM P-12285）（FERM BP-3870）中获得。 NK374186A是通过C34H61N3O12S9的合理配方和具有M + 735（FD-MS M / Z）的分子量表示的化合物; NK374186B是通过C34H61N3O9的合理配方和具有M + 655（FD-MS M / Z）的分子量表示的化合物; NK374186B3是通过C34H61N3O9的合理配方和具有M + 655（FD-MS M / Z）的分子量表示的化合物; 和NK374186C3是具有M + 597（FD-MS M / Z）的分子量通过C32H59N3O7的理性式表示的化合物和。
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公开(公告)号：EP0492430A1
公开(公告)日：1992-07-01
申请号：EP91121765.1
申请日：1991-12-19
摘要： The present invention relates to an oxetanocin derivative having an imidazole base group which is represented by the following general formula (A):
wherein R₁ represents a carbamoyl group or a cyano group;
R₂ represents an amino group, an acetylene group or a halogen atom; and
P represents a hydrogen atom or a protective group.
The compound of the present invention, which acts on an immune system, is useful as an active ingredient of an immunosuppressant. Further, useful intermediates of this compound are disclosed.摘要翻译： 本发明涉及具有由下述通式（A）表示的咪唑碱基的氧杂环丁烷（oxetanocin）衍生物：其中R 1表示氨基甲酰基或氰基; R 2代表氨基，乙炔基或卤素原子; P代表氢原子或保护基。 作用于免疫系统的本发明化合物可用作免疫抑制剂的活性成分。 此外，公开了该化合物的有用中间体。
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公开(公告)号：EP0393611A3
公开(公告)日：1991-01-23
申请号：EP90107311.4
申请日：1990-04-18
发明人： Saito, Seiichi , Hasegawa, Shigeru , Kitagawa, Masayuki , Shimada, Nobuyoshi , Yamashita, Noriyuki
CPC分类号： C07H19/02
摘要： The present invention provides a novel process for producing oxetanocin G by hydrolysis of alkoxylated 2-amino-oxetanocin A thereby to convert C-NH 2 at the 6-position thereof into C=O. Oxetanocin G is expectedly useful as an antiviral agent.
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6.发明公开Novel antibiotic NK130119, process for production of the same and application of the same 失效Antibiotikum NK130119，Verfahren zu dessen Herstellung und Verwendung。
公开(公告)号：EP0381124A2
公开(公告)日：1990-08-08
申请号：EP90101758.2
申请日：1990-01-30
发明人： Nishikiori, Takaaki , Yamazaki, Masanori , Saito, Seiichi , Shimada, Nobuyoshi , Kurokawa, Takashi , Hirose, Kiyonobu , Yamashita, Takumi , Harada, Takashi
IPC分类号： C07D498/20 , A61K31/365 , C12P17/08 , C12N1/20 , A01N43/90
CPC分类号： C07D493/20 , A01N43/90 , C12P17/181
摘要： This invention relates to an antibiotic NK130119 of the formula:
which exhibits antifungal, antitumor, vascularizations-inhibitory and insecticidal activities.摘要翻译： 本发明涉及具有抗真菌，抗肿瘤，血管形成抑制和杀虫活性的下式的抗生素NK130119：
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7.发明公开Oxetanocin-related compounds and process for producing same 失效Oxetanocinderivate和Verfahren zu ihrer Herstellung。
公开(公告)号：EP0334250A2
公开(公告)日：1989-09-27
申请号：EP89104910.8
申请日：1989-03-18
发明人： Saito, Seiichi , Hasegawa, Shigeru , Takahashi, Katsutoshi , Shimada, Nobuyoshi , Seki, Jun-ichi , Hoshino, Hiroo , Nishiyama, Yukihiro 8-25, Shiratori-2-chome , Matsubara, Kenichi , Nagahata, Takemitsu Senri Sakanoki Haitsu 208
IPC分类号： C07H19/16 , C07D473/00 , A61K31/52 , A61K31/70 , C12P19/40
CPC分类号： C07H19/02 , C07D305/06 , C07D305/08 , C07D305/10
摘要： This invention relates to oxetanocin-related compounds represented by the following formula (I):
[in formula (I), R 1 , Y and B have the following meanings:
(a) R 1 represents -CH 2 0H or -CN 2 OCO-(alkyl),
(b) Y represents
provided that R 2 is -H, -OH or -CHzOH and R 3 is -H, -OH, halogen atom, -CH 2 OH, lower alkyl group, -CH z -N 3 , -CH 2 -F, -N 3 , -COOH, -NH 2 , -CH 2 OSO 3 H or -CH 2 OCO-(lower alkyl), and
(c) B represents a residue of purine base,
(d) provided that R 1 and R 3 cannot simultaneously represente -CH 2 OH]
and their salts which have activities such as an antiviral activity and the like and are expectedly useful as a pharmaceutical and the like.摘要翻译： 本发明涉及由下式（I）表示的氧杂环丁霉素相关化合物：
[式（I）中，R 1，Y和B具有以下含义：（a）R 1表示-CH 2 OH或-CH 2 OOC- ），（b）Y表示 ，条件是R2是-H，-OH或-CH2OH，R3是-H，-OH，卤素原子，-CH2OH，低级烷基，-CH2-N3，-CH2-F ，-N3，-COOH，-NH2，-CH2OSO3H或-CH2OCO-（低级烷基），（c）B表示嘌呤碱基的残基，（d）R1和R3不能同时表示-CH2OH] 其具有抗病毒活性等活性，并且预期可用作药物等。 -
8.发明授权Novel antibiotics NK374186A, NK374186B, NK374186B3 and NK374186C3, process for producing the same, and use of the same 失效抗生素NK374186A，NK374186B，NK374186B3和NK374186C3，其制备方法及其应用
公开(公告)号：EP0525361B1
公开(公告)日：1996-10-23
申请号：EP92110170.5
申请日：1992-06-16
发明人： Morino, Tomio , Nishimoto, Masakazu , Nishide, Mit uyuki , Masuda, Akira , Yamada, Masatoshi , Kawano, Eiji , Nishikiori, Takaaki , Saito, Seiichi
摘要： Novel antibiotics NK374186A, NK374186B, NK374186B3 and NK374186C3 having antibacterial, antineoplastic, immunomodulation, and liver regeneration promoting activities are provided. NK374186A, NK374186B, NK374186B3 and NK374186C3 are obtained by culturing NK374186 strain (FERM P-12285) (FERM-BP 3870) belonging to the genus Penicillium. NK374186A is a compound represented by a rational formula of C34H61N3O12S9 and having a molecular weight of M+ 735 (FD-MS m/z); NK374186B is a compound represented by a rational formula of C34H61N3O9 and having a molecular weight of M+ 655 (FD-MS m/z); NK374186B3 is a compound represented by a rational formula of C34H61N3O9 and having a molecular weight of M+ 655 (FD-MS m/z); and NK374186C3 is a compound represented by a rational formula of C32H59N3O7 and having a molecular weight of M+ 597 (FD-MS m/z).
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9.发明授权Novel antibiotic NK130119, process for production of the same and application of the same 失效新型抗生素NK130119，其生产方法及其应用
公开(公告)号：EP0381124B1
公开(公告)日：1993-07-28
申请号：EP90101758.2
申请日：1990-01-30
发明人： Nishikiori, Takaaki , Yamazaki, Masanori , Saito, Seiichi , Shimada, Nobuyoshi , Kurokawa, Takashi , Hirose, Kiyonobu , Yamashita, Takumi , Harada, Takashi
IPC分类号： C07D498/20 , A61K31/365 , C12P17/08 , C12N1/20 , A01N43/90
CPC分类号： C07D493/20 , A01N43/90 , C12P17/181
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10.发明公开Phosphoric acid esters of oxetanocins and process for producing the same as well as use thereof 失效Phosphorsäureestervon Oxetanocinen，Verfahren zu ihrer Herstellung sowie ihre Verwendung。
公开(公告)号：EP0392403A1
公开(公告)日：1990-10-17
申请号：EP90106714.0
申请日：1990-04-07
发明人： Saito, Seiichi , Hasegawa, Shigeru , Kitagawa, Masayuki , Shimada, Nobuyoshi , Takahashi, Katsutoshi , Seki, Jun-Ichi , Hoshino, Hiroo , Nishiyama, Yukihiro , Matsubara, Kenichi , Nagahata, Takemitsu
CPC分类号： C07H19/02
摘要： The present invention relates to phosphoric acid esters of oxetanocins having an antiviral activity which are represented by general formula (I):
wherein R, represents a phosphoric acid ester residue, X represents hydrogen, hydroxy or hydroxymethyl group, and B represents a purine base residue, and pharmacologically acceptable salts thereof.摘要翻译： 本发明涉及由通式（I）表示的具有抗病毒活性的氧杂环丁啶的磷酸酯：其中R1表示磷酸酯残基，X表示氢，羟基或羟甲基，B表示嘌呤 碱残基及其药理学上可接受的盐。
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