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1. 发明授权

US5223508A Pyridyl carboximidamide compounds useful in treating blood pressure 失效
标题翻译：用于治疗血压的吡啶基亚甲基酰胺化合物
公开(公告)号：US5223508A
公开(公告)日：1993-06-29
申请号：US843847
申请日：1992-02-28
申请人： Toshio Izawa , Tomoko Kashiwabara , Shohachi Nakajima , Nobuyuki Ogawa
发明人： Toshio Izawa , Tomoko Kashiwabara , Shohachi Nakajima , Nobuyuki Ogawa
IPC分类号： C07C257/18 , C07C335/32 , C07D213/78 , C07D213/81 , C07D215/54 , C07D241/24 , C07D307/68 , C07D333/38 , C07D409/12
CPC分类号： C07D213/78 , C07C257/18 , C07C335/32 , C07D213/81 , C07D215/54 , C07D241/24 , C07D307/68 , C07D333/38 , C07D409/12
摘要： Novel carboximidamide derivatives represented by the following formula (A) and acid adduct salts thereof are disclosed: ##STR1## wherein all the substituents have the same meanings as defined above. N-cyano-pyridinecarboxyimidate compounds represented by the following formula (II) which are the intermediates for preparing of N-cyano-N'-substituted-pyridinecarboximidamide derivatives wherein the substituent B in the above described formula (A) is pyridine are also disclosed: ##STR2## wherein all the substituents have the same meanings as defined above. The process for preparing the compounds, the pharmaceutical agents comprising the compound having vasodilating effect, and the therapeutic method of dosing the compound on patients for therapy are also disclosed.
摘要翻译：公开了由下式（A）表示的新型甲脒类衍生物及其酸加成盐：其中全部取代基具有与上述相同的含义。还公开了作为制备上述式（A）中的取代基B为吡啶的N-氰基-N'-取代的吡啶甲酰胺衍生物的中间体的下式（II）表示的N-氰基 - 吡啶羧酰亚胺酸酯化合物：（II）其中所有取代基具有与上述相同的含义。还公开了制备该化合物的方法，包含具有血管舒张作用的化合物的药剂，以及将该化合物给予患者治疗的治疗方法。

2. 发明授权

US5166347A Carboximidamide derivatives 失效
标题翻译：羧甲酰胺衍生物
公开(公告)号：US5166347A
公开(公告)日：1992-11-24
申请号：US455973
申请日：1989-12-22
申请人： Toshio Izawa , Tomoko Kashiwabara , Shohachi Nakajima , Nobuyuki Ogawa
发明人： Toshio Izawa , Tomoko Kashiwabara , Shohachi Nakajima , Nobuyuki Ogawa
IPC分类号： C07D213/53 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4433 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/08 , C07C257/18 , C07C335/32 , C07D213/61 , C07D213/78 , C07D213/81 , C07D215/54 , C07D241/24 , C07D307/68 , C07D333/38 , C07D409/12
CPC分类号： C07D213/78 , C07C257/18 , C07C335/32 , C07D213/81 , C07D215/54 , C07D241/24 , C07D307/68 , C07D333/38 , C07D409/12
摘要： Novel carboximidamide derivatives represented by the following formula (A) and acid adduct salts thereof are disclosed: ##STR1## wherein all the substituents have the same meanings as defined above. N-cyano-pyridinecarboximidate compounds represented by the following formula (II) which are the intermediates for preparing of N-cyano-N'-substituted-pyridinecarboximidamide derivatives wherein the substituent B in the above described formula (A) is pyridine is also disclosed: ##STR2## wherein all the substitutents have the same meanings as defined above. The process for preparing the compounds, the pharmaceutical agents comprising the compound having vasodilating effect, and the therapeutic method of dosing the compound on patients for therapy are also disclosed.
摘要翻译：公开了由下式（A）表示的新型甲脒类衍生物及其酸加成盐：其中全部取代基具有与上述相同的含义。还公开了作为上述式（A）中的取代基B为吡啶的N-氰基-N'-取代的吡啶甲酰胺衍生物的制造中间体的下述式（II）表示的N-氰基 - 吡啶甲脒化合物：（II）其中所有取代基具有与上述相同的含义。还公开了制备该化合物的方法，包含具有血管舒张作用的化合物的药剂，以及将该化合物给予患者治疗的治疗方法。

3. 发明授权

US5272164A Carboximidamide derivatives 失效
标题翻译：羧甲酰胺衍生物
公开(公告)号：US5272164A
公开(公告)日：1993-12-21
申请号：US843816
申请日：1992-02-28
申请人： Toshio Izawa , Tomoko Kashiwabara , Shohachi Nakajima , Nobuyuki Ogawa
发明人： Toshio Izawa , Tomoko Kashiwabara , Shohachi Nakajima , Nobuyuki Ogawa
IPC分类号： C07C257/18 , C07C335/32 , C07D213/78 , C07D213/81 , C07D215/54 , C07D241/24 , C07D307/68 , C07D333/38 , C07D409/12 , A01N43/40 , C07D24/00
CPC分类号： C07D213/78 , C07C257/18 , C07C335/32 , C07D213/81 , C07D215/54 , C07D241/24 , C07D307/68 , C07D333/38 , C07D409/12
摘要： Novel carboximidamide derivatives represented by the following formula (A) and acid adduct salts thereof are disclosed: ##STR1## wherein all the substituents have the same meanings as defined above. N-cyano-pyridinecarboximidate compounds represented by the following formula (II) which are the intermediates for preparing of N-cyano-N'-substituted-pyridinecarboximidamide derivatives wherein the substituent B in the above described formula (A) is pyridine are also disclosed: ##STR2## wherein all the substituents have the same meanings as defined above. The process for preparing the compounds, the pharmaceutical agents comprising the compound having vasodilating effect, and the therapeutic method of dosing the compound on patients for therapy are also disclosed.
摘要翻译：公开了由下式（A）表示的新型甲脒类衍生物及其酸加成盐：其中全部取代基具有与上述相同的含义。还公开了作为用于制备上述式（A）中的取代基B为吡啶的N-氰基-N'-取代的吡啶甲酰胺衍生物的中间体的下式（II）表示的N-氰基 - 吡啶甲脒化合物：（II）其中所有取代基具有与上述相同的含义。还公开了制备该化合物的方法，包含具有血管舒张作用的化合物的药剂，以及将该化合物给予患者治疗的治疗方法。

4. 发明授权

US4855414A Process for production of anthracycline compound R20X2 失效
标题翻译：生产蒽环类化合物R20X2的方法
公开(公告)号：US4855414A
公开(公告)日：1989-08-08
申请号：US68627
申请日：1987-06-30
申请人： Hamao Umezawa , Atsuo Odagawa , Shiro Kataoka , Shohachi Nakajima
发明人： Hamao Umezawa , Atsuo Odagawa , Shiro Kataoka , Shohachi Nakajima
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252
CPC分类号： C07H15/252
摘要： An anthracycline compound, R20X2, of the following formula (II) is produced by a process which comprises subjecting an anthracycline compound, R20X3, of the following formula (I) or a salt thereof to reaction in the co-presence of (1) acetone and/or dimethylformamide and (2) an aqueous solution containing ammonium ion and/or trialkylamine. ##STR1## The anthracycline compound, R20X2, can be produced not only by the cultivation of actinomycetes but also, in accordance with the process as shown above, by chemical conversion of the anthracycline compound, R20X3, in a high yield.
摘要翻译：通过以下方法制备下式（II）的蒽环类化合物R20X2：将下式（I）的蒽环类化合物R20X3或其盐在（1）丙酮共存下进行反应和/或二甲基甲酰胺和（2）含有铵离子和/或三烷基胺的水溶液。（II）蒽环类化合物R20X2不仅可以通过放线菌的培养产生，而且可以根据上述方法通过蒽环类化合物R20X3的化学转化产生，以高收益。

5. 发明授权

US4710564A Anthracycline compounds 失效
标题翻译：蒽环类化合物
公开(公告)号：US4710564A
公开(公告)日：1987-12-01
申请号：US818867
申请日：1986-01-14
申请人： Noboru Otake , Kuniaki Tatsuta , Shigeyuki Mizobuchi , Nobuyasu Komeshima , Shohachi Nakajima , Hiroyuki Kawai , Atsuo Odagawa
发明人： Noboru Otake , Kuniaki Tatsuta , Shigeyuki Mizobuchi , Nobuyasu Komeshima , Shohachi Nakajima , Hiroyuki Kawai , Atsuo Odagawa
IPC分类号： C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Disclosed is a novel anthracycline compound of the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are each a hydroxyl group or a hydrogen atom and satisfy the condition that, when R.sup.2 is a hydroxyl group, R.sup.1 is a hydroxyl group or a hydrogen atom, whereas, when R.sup.2 is a hydrogen atom, R.sup.1 is a hydrogen atom, or an acid addition salt thereof.These compounds can be contained as active ingredients in antitumor agents, whereby good results are attainable.
摘要翻译：公开了下式（I）的新型蒽环类化合物：其中R 1和R 2各自为羟基或氢原子，并且满足以下条件：当R 2为羟基时，R 1为羟基基团或氢原子，而当R 2为氢原子时，R 1为氢原子或其酸加成盐。这些化合物可以作为活性成分包含在抗肿瘤剂中，从而可获得良好的结果。

6. 发明授权

US4959460A 3'-deamino-3'-(2"-substituted-4"-morpholino)-anthracycline compounds 失效
标题翻译： 3'-脱氨基-3' - （2“ - 取代-4” - 吗啉代） - 蒽环类化合物
公开(公告)号：US4959460A
公开(公告)日：1990-09-25
申请号：US400470
申请日：1989-08-29
申请人： Shohachi Nakajima , Nobuyasu Komeshima
发明人： Shohachi Nakajima , Nobuyasu Komeshima
IPC分类号： C12P19/56 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61P35/02 , C07H15/252 , C07H19/02 , C12R1/03
CPC分类号： C07H15/252
摘要： Disclosed is an anthracycline compound of the formula (I): ##STR1## wherein Ra is -R.sup.1, ##STR2## or --OR.sup.3, R.sup.1 being (1) alkyl, alkenyl, alkynyl, fluoroalkyl, aryl or aralkyl, or (2) alkyl, alkenyl, alkynyl. fluoroalkyl, aryl or aralkyl having carboxyl, azido, amino, hydroxy, alkoxy or a halogen atom; R.sup.2 being R.sup.1, a hydrogen atom or hydroxy; and R.sup.3, which may be the same or different when one substituent has two R.sup.3 's, being R.sup.1 or a hydrogen atom; or the formula (II): ##STR3## wherein Rb is -R.sup.1, ##STR4## or --OR.sup.3, R.sup.1, R.sup.2 and R.sup.3 being as defined above; and R.sup.4 being the same as R.sup.3 except that methyl is not included; or an acid addition salt thereof.This compound can be contained as an active ingredient in an antitumor agent, whereby good results are attainable.
摘要翻译：公开了式（I）的蒽环类化合物：其中R a是-R 1，-OR 3，R 1是（1）烷基，烯基，炔基，氟代烷基，芳基或芳烷基或（ 2）烷基，烯基，炔基。具有羧基，叠氮基，氨基，羟基，烷氧基或卤素原子的氟代烷基，芳基或芳烷基; R2为R1，氢原子或羟基; 和R 3，当一个取代基具有两个R 3时，它们可以相同或不同，R 1或氢原子; 或式（II）：其中R b为-R 1，-IG 3或-OR 3，R 1，R 2和R 3如上所定义; 和R 4与R 3相同，不同之处在于不包括甲基; 或其酸加成盐。该化合物可以作为抗肿瘤剂中的活性成分而含有，可以得到良好的效果。

7. 发明授权

US4888418A Derivatives of 13-deoxycarminomycin 失效
标题翻译： 13-脱氧卡明霉素的衍生物
公开(公告)号：US4888418A
公开(公告)日：1989-12-19
申请号：US166707
申请日：1988-03-11
申请人： Hiroyuki Kawai , Shohachi Nakajima , Tomio Takeuchi
发明人： Hiroyuki Kawai , Shohachi Nakajima , Tomio Takeuchi
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252
CPC分类号： C07H15/252
摘要： An anthracycline compound (13-deoxycarminomycin) selected from the group consisting of anthracycline compounds represented by the following formula ##STR1## R1 is a hydroxy group, R2 represents a hydrogen atom or a hydroxyl group,R3 is a hydrogen atom,R4 represents one of the following groups (a) to (d) ##STR2## and if R2 is hydroxyl, R4 is not (d).

8. 发明授权

US4877870A Process for producing 10-hydroxyanthracyclines 失效
标题翻译：生产10-羟基蒽环的方法
公开(公告)号：US4877870A
公开(公告)日：1989-10-31
申请号：US68630
申请日：1987-06-30
申请人： Hamao Umezawa, deceased , Kuniaki Tatsuta , Hiroyuki Kawai , Shohachi Nakajima
发明人： Hamao Umezawa, deceased , Kuniaki Tatsuta , Hiroyuki Kawai , Shohachi Nakajima
IPC分类号： C07C50/36 , A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C45/00 , C07C46/00 , C07C50/38 , C07C67/00 , C07H15/252 , C12P19/56 , C12R1/03
CPC分类号： C07H15/252
摘要： Disclosed is a process for producing a 10-hydroxyanthracycline of the following formula (II) which comprises reacting a compound of the following formula (I) or an acid addition salt thereof with an N-oxide of a tertiary amine ##STR1## wherein: R.sup.1 through R.sup.6 each designate any of H, OH and OCH.sub.3 ; R.sup.7 designates any of H, OH and a sugar residue; and R.sup.8 designates any of C.sub.2 H.sub.5, COCH.sub.3, CH(OH)CH.sub.3, CH(OH)CH.sub.2 (OH) and COCH.sub.2 OH. In accordance with this process, it is possible to efficiently introduce a hydroxyl group into the 10-position of an anthracycline having no substitutent at the same position thereof.
摘要翻译：公开了一种制备下式（II）的10-羟基蒽环的方法，其包括使下式（I）的化合物或其酸加成盐与叔胺的N-氧化物反应（I）（II）其中：R 1至R 6各自表示H，OH和OCH 3中的任一个; R7表示H，OH和糖残基中的任一个; 并且R 8表示任何C 2 H 5，COCH 3，CH（OH）CH 3，CH（OH）CH 2（OH）和COCH 2 OH。根据该方法，可以在相同位置的无结构的蒽环类的10位上有效地引入羟基。

9. 发明授权

US4833241A Anthracycline compound 失效
标题翻译：蒽环类化合物
公开(公告)号：US4833241A
公开(公告)日：1989-05-23
申请号：US68629
申请日：1987-06-30
申请人： Hamao Umezawa , Hiroyuki Kawai , Shohachi Nakajima
发明人： Hamao Umezawa , Hiroyuki Kawai , Shohachi Nakajima
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P19/56
CPC分类号： C07H15/252 , C12P19/56
摘要： Disclosed is an anthracycline compound of the following formula (I) or an acid addition salt thereof: ##STR1## These compounds are useful as intermediates in the synthesis of an anthracycline compound, M-R20X or M-R20X2, which has antitumor activity.
摘要翻译：公开了下式（I）的蒽环类化合物或其酸加成盐：（I）这些化合物可用作合成具有抗肿瘤性的蒽环类化合物M-R20X或M-R20X2的中间体活动。

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