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公开(公告)号：EP0071483A3
公开(公告)日：1983-03-09
申请号：EP82304021
申请日：1982-07-29
IPC分类号： C07C97/18 , C07D317/28 , A61K31/135 , A61K31/335
CPC分类号： C07D317/28
摘要： Aminonaphthacene derivatives of the formula:
wherein R 1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R 2 is a hydrogen atom or a hydroxyl group, R 3 and R 4 are each a lower alkyl group or, when taken together, represent an ethylenedioxy group or an oxo group and R 6 and R 8 are each a hydrogen atom, a lower alkyl group or a group of the formula: -A-Q (in which A is an alkylene group optionally bearing at least one lower alkyl and Q is a hydrogen atom, a hydroxyl group, a lower alkoxy group or a group of the formula:
wherein R 7 and R 8 are each a hydrogen atom, a lower alkyl group, a benzyl group, a hydroxy (lower) alkyl group or an amino (lower) alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a 5 to 7-membered nitrogen-containing ring optionally having an additional nitrogen or oxygen atom in the ring and optionally bearing any substituent on the ring) or, R 5 and R 6 when taken together with the adjacent nitrogen atom to which they are attached, represent a 5 to 7-membered nitrogen-containing ring optionally having an additional nitrogen or oxygen atom in the ring and optionally bearing any substituent on the ring, and their acid addition salts, which are useful as anti-tumor agents.-
公开(公告)号：EP0071483A2
公开(公告)日：1983-02-09
申请号：EP82304021.7
申请日：1982-07-29
IPC分类号： C07C97/18 , C07D317/28
CPC分类号： C07D317/28
摘要： Aminonaphthacene derivatives of the formula:
wherein R 1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R 2 is a hydrogen atom or a hydroxyl group, R 3 and R 4 are each a lower alkyl group or, when taken together, represent an ethylenedioxy group or an oxo group and R 6 and R 8 are each a hydrogen atom, a lower alkyl group or a group of the formula: -A-Q (in which A is an alkylene group optionally bearing at least one lower alkyl and Q is a hydrogen atom, a hydroxyl group, a lower alkoxy group or a group of the formula:
wherein R 7 and R 8 are each a hydrogen atom, a lower alkyl group, a benzyl group, a hydroxy (lower) alkyl group or an amino (lower) alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a 5 to 7-membered nitrogen-containing ring optionally having an additional nitrogen or oxygen atom in the ring and optionally bearing any substituent on the ring) or, R 5 and R 6 when taken together with the adjacent nitrogen atom to which they are attached, represent a 5 to 7-membered nitrogen-containing ring optionally having an additional nitrogen or oxygen atom in the ring and optionally bearing any substituent on the ring, and their acid addition salts, which are useful as anti-tumor agents.摘要翻译： 其中R 1为氢原子，羟基或低级烷氧基，R 2为氢原子或羟基，R 3和R 4为氢， 4>各自为低级烷基，或者一起表示亚乙二氧基或氧代基，R 5和R 6各自为氢原子，低级烷基或下式基团： - AQ（其中A是任选带有至少一个低级烷基的亚烷基，Q是氢原子，羟基，低级烷氧基或下式的基团：...
其中R 7和R 8是氢原子，低级烷基，苄基，羟基（低级）烷基或氨基（低级）烷基，当与它们所连接的相邻氮原子一起代表 5至7元含氮环，任选在环中具有额外的氮原子或氧原子，并且任选在环上带有任何取代基）或R 5和R 6当 与它们所连接的相邻氮原子一起代表在环中任选具有额外的氮或氧原子且任选地在环上具有任何取代基的5至7元含氮环，及其酸加成盐， 其可用作抗肿瘤剂。 -
公开(公告)号：EP0139286A3
公开(公告)日：1985-10-30
申请号：EP84112310
申请日：1984-10-12
CPC分类号： A61K9/0024 , A61K9/2063 , A61K31/405 , A61K31/415 , A61K38/212
摘要： A sustained-release preparation in the form of a needle-like or bar-like shape, which comprises an active ingredient and a pharmaceutically acceptable biodegradable carrier (e.g. proteins, polysaccharides and synthetic high molecular compounds, preferably collagen, atelocollagen, gelatin, and a mixture thereof). The sustained-release preparation can be administered to the body or implanted into the body by injection or injection-like methods and can release the active ingredient at an effective level for a long period of time when administered.
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公开(公告)号：EP0071483B1
公开(公告)日：1985-01-02
申请号：EP82304021.7
申请日：1982-07-29
IPC分类号： C07C97/18 , C07D317/28
CPC分类号： C07D317/28
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5.发明公开Antitumor substance, composition comprising it and process for preparing said substance 失效抗肿瘤物质，该组合物含有，使该物质的方法。
公开(公告)号：EP0024206A2
公开(公告)日：1981-02-25
申请号：EP80302813.3
申请日：1980-08-14
发明人： Yoshida, Noboru , Kiyohara, Takao , Fukui, Masaru , Fukui, Akio , Ogino, Shigeo , Inaba, Makoto , Tsukagoshi, Shigeru , Sakurai, Yoshio
CPC分类号： C07K14/212 , A61K38/00
摘要： The toxicity of a known antitumor substance prepared by culturing a microorganism, Acinetobacter calcoaceticus var. microformis SC-1714 is reduced by treatment with barium hydroxide and isolating an antitumor substance having an excellent antitumor activity as well as a potent immunostimulatory activity. The novel substance is effective when administered in very small amounts without harmful effects such as toxicity.
摘要翻译： 通过培养微生物而制备的公知的抗肿瘤物质的毒性，不动杆菌变种Microformis SC-1714是通过用氢氧化并具有优异的抗肿瘤活性的抗肿瘤物质的隔离钡以及强效免疫刺激活性治疗减少。 该新物质是有效的，当在非常小的量施用无有害作用：如毒性。
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6.发明公开Antitumor substance and composition, and process for preparing said substance 失效防腐剂物质和组合物，以及制备物质的方法
公开(公告)号：EP0024206A3
公开(公告)日：1981-11-25
申请号：EP80302813
申请日：1980-08-14
发明人： Yoshida, Noboru , Kiyohara, Takao , Fukui, Masaru , Fukui, Akio , Ogino, Shigeo , Inaba, Makoto , Tsukagoshi, Shigeru , Sakurai, Yoshio
CPC分类号： C07K14/212 , A61K38/00
摘要： The toxicity of a known antitumor substance prepared by culturing a microorganism, Acinetobacter calcoaceticus var. microformis SC-1714 is reduced by treatment with barium hydroxide and isolating an antitumor substance having an excellent antitumor activity as well as a potent immunostimulatory activity. The novel substance is effective when administered in very small amounts without harmful effects such as toxicity.
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7.发明公开Novel aminonaphthacene derivatives and process for preparation thereof 失效Aminonaphthacen的衍生物及其制备方法。
公开(公告)号：EP0094059A1
公开(公告)日：1983-11-16
申请号：EP83104493.8
申请日：1983-05-06
IPC分类号： C07C97/18 , A61K31/135
CPC分类号： A61K31/135
摘要： An aminonaphthacene derivative of the formula:
wherein R 1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R 2 is a hydrogen atom or a hydroxyl group, R 3 is a hydrogen atom or a lower alkanoyl group and R 4 and R 5 are, same or different, each a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group or a group of the formula:
wherein A is an alkylene group which may have one or more lower alkyl substituent(s) and R 6 and R 7 are, same or different, each a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group or a lower aminoalkyl group, and an acid addition salt thereof, which is useful as anti-tumor agent.-
公开(公告)号：EP0094059B1
公开(公告)日：1987-08-12
申请号：EP83104493.8
申请日：1983-05-06
IPC分类号： C07C97/18 , A61K31/135
CPC分类号： A61K31/135
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公开(公告)号：EP0140255A3
公开(公告)日：1985-10-30
申请号：EP84112313
申请日：1984-10-12
CPC分类号： A61K31/415 , A61K9/10 , A61K9/1658 , A61K31/405 , A61K38/212
摘要： A sustained-release injection, which comprises a suspension of a powder comprising an active ingredient and a pharmaceutically acceptable biodegradable carrier (e.g. proteins, polysaccharides and synthetic high molecular compounds, preferably collagen, atelocollagen, gelatin, and a mixture thereof) in a viscous solvent for injection (e.g. vegetable oils, polyethylene glycol, propylene glycol, silicone oil, and medium-chain fatty acid triglycerides). The sustained-release injection can release the active ingredient at an effective level for a long period of time when injected.
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公开(公告)号：EP0138216A3
公开(公告)日：1985-10-30
申请号：EP84112312
申请日：1984-10-12
IPC分类号： A61K09/22 , A61K31/405 , A61K45/02 , A61K31/415 , A61K47/00
CPC分类号： A61K9/0024 , A61K9/10 , A61K9/1658 , A61K9/2063 , A61K31/405 , A61K31/415 , A61K38/212
摘要： A sustained-release preparation of indomethacin, interferon and 4-carbamoyl-imidazolium-5-oleate (SM-108) comprising the active ingredient in admixture with a pharmaceutically acceptable biodegradable carrier, particularly a carrier selected from collagen, atelocollagen, gelatin, and a mixture thereof. Said preparation is particularly suitable for parenteral administration and can release the active ingredient in an effective amount for a long period of time. 1
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