公开(公告)号：US4728729A

公开(公告)日：1988-03-01

申请号：US709647

申请日：1985-03-08

申请人： Yuzo Tarumi ,  Toshio Atsumi ,  Masaru Fukui

发明人： Yuzo Tarumi ,  Toshio Atsumi ,  Masaru Fukui

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7056 ,  A61P35/00 ,  C07H19/052 ,  C07H19/067

CPC分类号： C07H19/052 ,  Y02P20/55

摘要： A novel cyanoimidazole nucleoside and derivative thereof, particularly 4-cyanoimidazolium-5-olate nucleoside and acyl derivatives thereof, and pharmaceutically acceptable salts thereof which are useful as antitumor agents and immunosuppressants, are prepared by dehydrating carboxamide derivatives of the formula: ##STR1## wherein R is an acyl group, and then, if desired, deacylating.

摘要翻译： 通过将下式的羧酰胺衍生物脱水制备，其可用作抗肿瘤剂和免疫抑制剂的新型氰基咪唑核苷及其衍生物，特别是4-氰基咪唑鎓-5-醇酸核苷及其酰基衍生物及其药学上可接受的盐，其中： R是酰基，然后，如果需要，进行脱酰基。

公开(公告)号：US4464531A

公开(公告)日：1984-08-07

申请号：US366423

申请日：1982-04-07

申请人： Toshio Atsumi ,  Yuzo Tarumi ,  Tetsutaro Sanjiki ,  Yoshiaki Takebayashi ,  Noboru Yoshida

发明人： Toshio Atsumi ,  Yuzo Tarumi ,  Tetsutaro Sanjiki ,  Yoshiaki Takebayashi ,  Noboru Yoshida

IPC分类号： C07H17/02 ,  A61K31/70

CPC分类号： C07H17/02

摘要： There are provided compounds of the formula: ##STR1## wherein either R.sub.1 or R.sub.2 is a hydrogen atom, a hydroxy group, an acyloxy group, a phthalimido group or an acetamido group and the other is a hydrogen atom; either R.sub.3 or R.sub.4 is a hydroxy group or an acyloxy group and the other is a hydrogen atom; either R.sub.5 or R.sub.6 is a hydroxy group or an acyloxy group and the other is a hydrogen atom; either R.sub.7 or R.sub.8 is a hydrogen atom, a methyl group, a hydroxymethyl group, an acyloxymethyl group, an alkoxycarbonyl group, a group of the formula: ##STR2## (wherein X.sub.1 and X.sub.2 are a hydrogen atom or a lower alkyl group), or a carboxyl group and the other is a hydrogen atom; either R.sub.11 or R.sub.12 is a hydrogen atom, a hydroxy group or an acyloxy group and the other is a hydrogen atom; either R.sub.13 or R.sub.14 is a hydroxy group or an acyloxy group and the other is a hydrogen atom; either R.sub.15 or R.sub.16 is a methyl group, a hydroxymethyl group or an acyloxymethyl group and the other is a hydrogen atom; and a process for producing them. These compounds are useful as antitumor agents.

摘要翻译： 提供下式的化合物：其中R 1或R 2为氢原子，羟基，酰氧基，苯二甲酰亚氨基或乙酰氨基，其中R 1或R 2为氢原子， 另一个是氢原子; R3或R4是羟基或酰氧基，另一个是氢原子; R5或R6是羟基或酰氧基，另一个是氢原子; R7或R8是氢原子，甲基，羟甲基，酰氧基甲基，烷氧基羰基，下式的基团：其中X1和X2是氢原子或低级烷基， 或羧基，另一个是氢原子; R 11或R 12是氢原子，羟基或酰氧基，另一个是氢原子; R13或R14是羟基或酰氧基，另一个是氢原子; R 15或R 16是甲基，羟甲基或酰氧基甲基，另一个是氢原子; 以及生产它们的过程。 这些化合物可用作抗肿瘤剂。

公开(公告)号：US4260774A

公开(公告)日：1981-04-07

申请号：US51741

申请日：1979-06-25

申请人： Toshio Atsumi ,  Yoshiaki Takebayashi ,  Yuzo Tarumi ,  Hisao Yamamoto

发明人： Toshio Atsumi ,  Yoshiaki Takebayashi ,  Yuzo Tarumi ,  Hisao Yamamoto

IPC分类号： C07D233/90

CPC分类号： C07D233/90

摘要： There are provided compounds of the formula: ##STR1## wherein R is an adamantyl group, or a phenyl group unsubstituted or substituted with a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halogen atom, a nitro group, a cyano group, a methylenedioxy group or an acetamido group, useful as anti-transplanted-tumor agents and immunosuppressants.

摘要翻译： 提供下式的化合物：其中R是金刚烷基，或未取代或被低级烷基，低级烷氧基，低级烷硫基，卤原子，硝基， 氰基，亚甲二氧基或乙酰氨基，可用作抗移植肿瘤剂和免疫抑制剂。

公开(公告)号：US4218457A

公开(公告)日：1980-08-19

申请号：US940131

申请日：1978-09-06

申请人： Toshio Atsumi ,  Yuzo Tarumi ,  Noboru Yoshida

发明人： Toshio Atsumi ,  Yuzo Tarumi ,  Noboru Yoshida

IPC分类号： C07D233/90 ,  A61K31/415 ,  A61K31/44 ,  C07D233/32 ,  C07D403/04

CPC分类号： C07D233/90

摘要： Compounds of the formula, ##STR1## wherein R is C.sub.2 -C.sub.17 alkyl group, C.sub.3 -C.sub.7 cycloalkyl group, 1-adamantyl group, pyridyl group, pyridine N-oxide, diphenylmethyl group, benzyl group which may or may not be substituted with nitro group, halogen atom, C.sub.1 -C.sub.3 alkyl group or C.sub.1 -C.sub.3 alkoxy group, or phenyl group which may or may not be substituted with nitro group, halogen atom, hydroxy group, C.sub.1 -C.sub.3 alkyl group, C.sub.1 -C.sub.3 alkoxy group, carboxy group, C.sub.2 -C.sub.4 alkoxycarbonyl group, phenoxycarbonyl group, carbamoyl group, N-phenylcarbamoyl group, N-adamantylcarbamoyl group, benzoylamino group, trifluoromethyl group, C.sub.2 -C.sub.4 alkanoyloxy group, 1-adamantoyloxy group or benzoyloxy group and salts thereof have an anticancer activity and an immunostimulating activity.

摘要翻译： 下式的化合物，其中R是C 2 -C 17烷基，C 3 -C 7环烷基，1-金刚烷基，吡啶基，吡啶N-氧化物，二苯基甲基，可以是也可以不是 被硝基，卤原子，C1-C3烷基或C1-C3烷氧基取代的苯基，或可以被硝基，卤素原子，羟基，C1-C3烷基，C1-C3烷氧基取代的苯基 基团，羧基，C 2 -C 4烷氧基羰基，苯氧基羰基，氨基甲酰基，N-苯基氨基甲酰基，N-金刚烷基氨基甲酰基，苯甲酰氨基，三氟甲基，C 2 -C 4烷酰氧基，1-酰胺基氧基或苯甲酰氧基及其盐 抗癌活性和免疫刺激活性。

公开(公告)号：US4140788A

公开(公告)日：1979-02-20

申请号：US849515

申请日：1977-11-07

申请人： Toshio Atsumi ,  Yuzo Tarumi ,  Norboru Yoshida

发明人： Toshio Atsumi ,  Yuzo Tarumi ,  Norboru Yoshida

IPC分类号： C07C271/22 ,  C07D233/90 ,  A61K31/415 ,  C07D233/64

CPC分类号： C07C271/22 ,  C07D233/90

摘要： N-Substituted imidazolecarboxamide compounds represented by the formula; ##STR1## wherein R.sub.1 is hydrogen atom, lower alkyl, lower alkenyl, aralkyl, R.sub.2 is hydrogen atom, lower alkyl, lower alkenyl, aralkyl, 1-adamantyl, R.sub.3 is hydrogen atom, lower alkyl, aralkyl; with the proviso that one of R.sub.1, R.sub.2 or R.sub.3 is not hydrogen when the other two are hydrogen, are produced by reacting aminomalonamide derivative with orthoformate derivative in high yields. The compounds (I) exhibit anti-tumor activity against experimental tumors such as Sarcoma 180 in mice.

摘要翻译： 由式表示的N-取代的咪唑酰甲酰胺化合物; （I）其中R 1是氢原子，低级烷基，低级烯基，芳烷基，R 2是氢原子，低级烷基，低级烯基，芳烷基，1-金刚烷基，R 3是氢原子，低级烷基，芳烷基。 条件是当另外两个是氢时，R 1，R 2或R 3中的一个不是氢，是通过氨基马来酰亚胺衍生物与原甲酸酯衍生物以高收率反应制备的。 化合物（I）对小鼠的实验性肿瘤如肉瘤180具有抗肿瘤活性。

公开(公告)号：US4209525A

公开(公告)日：1980-06-24

申请号：US971826

申请日：1978-12-19

申请人： Toshio Atsumi ,  Yuzo Tarumi ,  Takao Kiyohara

发明人： Toshio Atsumi ,  Yuzo Tarumi ,  Takao Kiyohara

IPC分类号： A61K31/415 ,  A61P37/04 ,  C07D233/90

CPC分类号： C07D233/90 ,  Y10S514/885

摘要： Imidazole derivatives represented by the formula: ##STR1## wherein Y is a hydroxy group, a lower alkoxy group or an amino group, and their non-toxic, pharmaceutically acceptable salts, which have a potent immunostimulating activity and are useful for the immunostimulatory therapy of various diseases, and their preparation and use.

摘要翻译： 由下式表示的咪唑衍生物：其中Y是羟基，低级烷氧基或氨基，及其无毒的药学上可接受的盐，它们具有有效的免疫刺激活性，可用于免疫刺激性治疗 各种疾病及其准备和使用。