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1. 发明授权

US4728729A Cyanoimidazole nucleoside derivatives 失效
标题翻译：氰基咪唑核苷衍生物
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。

2. 发明授权

US4410696A Antitumor and immunosuppressive 4-carbamoylimidazolium-5-olate derivatives 失效
标题翻译：抗肿瘤剂和免疫抑制剂4-氨基甲酰基咪唑鎓-5-醇酸酯衍生物
公开(公告)号：US4410696A
公开(公告)日：1983-10-18
申请号：US305347
申请日：1981-09-24
申请人： Toshio Atsumi , Tetsutaro Sanjiki , Takao Kiyohara
发明人： Toshio Atsumi , Tetsutaro Sanjiki , Takao Kiyohara
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 a mono-substituted benzoyl group wherein the substituent is a phenyl group, an alkanoyl group, a formyl group, a halogeno-alkyl group, an aralkyloxy group, a phenoxy group, an alkoxycarbonyl group, an aralkyloxycarbonyl group, an alkanoyloxy group, a benzoyl group, a carboxyl group, a hydroxy group, a group of the formula: ##STR2## (wherein X.sub.1 and X.sub.2 are a hydrogen atom or a lower alkyl group), an aralkyloxycarbonylamino group, a lower alkoxycarbonylamino group, a carboxyamino group or a carbamoyl group; a cinnamoyl group which may be substituted at the .alpha. position or the phenyl ring with an alkyl group, an alkoxy group, an aryl group, a nitro group, a methylenedioxy group, a formyl group, a halogeno-alkyl group, a halogen atom, a hydroxy group, a carboxyl group, an amino group or a cyano group; or a benzoyl group substituted with from two to five of the same or different substituents selected from the group consisting of alkyl groups, alkoxy groups, aralkyloxy groups, nitro group, halogen atoms, hydroxy group, alkanoyloxy groups, formyl group, carboxyl group, alkylthio groups, alkylsulfonyl groups, groups of the formula: ##STR3## (wherein X.sub.1 and X.sub.2 are a hydrogen atom or a lower alkyl group), sulfo group and sulfamoyl group; or its non-toxic salt, and a process for producing them. The compounds are useful as antitumor agents and immunosuppressants.
摘要翻译：提供下式的化合物：其中R是单取代的苯甲酰基，其中取代基是苯基，烷酰基，甲酰基，卤代烷基，芳烷氧基，苯氧基，烷氧基羰基，芳烷氧基羰基，烷酰氧基，苯甲酰基，羧基，羟基，下式的基团：其中X 1和X 2是氢原子或低级烷基，芳烷氧基羰基氨基，低级烷氧基羰基氨基，羧基氨基或氨基甲酰基; 可以在α位置取代的肉桂酰基或具有烷基，烷氧基，芳基，硝基，亚甲二氧基，甲酰基，卤代烷基，卤素原子，羟基，羧基，氨基或氰基; 或被两个至五个相同或不同的取代基取代的苯甲酰基，所述取代基选自烷基，烷氧基，芳烷氧基，硝基，卤素原子，羟基，烷酰氧基，甲酰基，羧基，烷硫基基团，烷基磺酰基，下式的基团：其中X 1和X 2是氢原子或低级烷基，磺基和氨磺酰基; 或其无毒盐，以及其生产方法。该化合物可用作抗肿瘤剂和免疫抑制剂。

3. 发明授权

US4332806A Antitumor and immunosuppresive 4-carbamoyl imidazolium-5-olate derivatives, pharmaceutical composition and production thereof 失效
标题翻译：抗肿瘤和免疫抑制性4-氨基甲酰基咪唑鎓-5-醇酸酯衍生物，药物组合物及其制备方法
公开(公告)号：US4332806A
公开(公告)日：1982-06-01
申请号：US205980
申请日：1980-11-12
申请人： Toshio Atsumi , Yoshiaki Takebayashi , Takao Kiyohara
发明人： Toshio Atsumi , Yoshiaki Takebayashi , Takao Kiyohara
IPC分类号： A61K31/415 , A61P35/00 , C07D233/90
CPC分类号： C07D233/90 , Y10S514/885
摘要： There are provided compounds of the formula: ##STR1## wherein R is an adamantoyl group substituted with a lower alkyl group, a lower alkoxy group, a hydroxy group, a lower alkanoyloxy group, an aroyloxy group, a halogen atom, an acetamido group, a nitro group, an azide group, a trifluoromethyl group or a phenyl group which may be substituted with a nitro group, a halogen atom, a lower alkyl group or a lower alkoxy group and a process producing them. These compounds are useful as antitumor agents and immunosuppressants.
摘要翻译：提供下式的化合物：其中R是被低级烷基，低级烷氧基，羟基，低级烷酰氧基，芳酰氧基，卤素原子，乙酰氨基基团取代的亚甲酰基，硝基，叠氮基，三氟甲基或可以被硝基，卤素原子，低级烷基或低级烷氧基取代的苯基，以及制备它们的方法。这些化合物可用作抗肿瘤剂和免疫抑制剂。

4. 发明授权

US4317825A Antitumor and immunosuppressive 4-carbamoyl imidazolium-5-olate derivatives 失效
标题翻译：抗肿瘤剂和免疫抑制剂4-氨基甲酰基咪唑鎓-5-醇酸酯衍生物
公开(公告)号：US4317825A
公开(公告)日：1982-03-02
申请号：US175688
申请日：1980-08-05
申请人： Toshio Atsumi , Tetsutaro Sanjiki , Takao Kiyohara
发明人： Toshio Atsumi , Tetsutaro Sanjiki , Takao Kiyohara
IPC分类号： A01N53/00 , C07D233/90 , C07F7/18 , A61K31/415 , A61K31/495 , C07D405/12 , C07D409/12
CPC分类号： A01N53/00 , C07D233/90 , C07F7/1804
摘要： There are provided compounds of the formula: ##STR1## wherein R is a heteroaroyl group containing a nitrogen, sulfur or oxygen atom which may be substituted with a lower alkyl group, an aralkyl group, an acyl group or a halogen atom; or a cycloalkanoyl group which may be substituted with a lower alkyl group, a lower alkenyl group, a halogen atom, a halogeno-lower alkenyl group, a phenyl group, a halogenophenyl group, a lower alkoxyphenyl group, a lower alkylphenyl group, a formyl group, a hydroxy group, an amino group, a carboxyl group, an aminomethyl group or an oxo group, its non toxic salt and a process for producing them. These compounds are useful as antitumor agents and immunosuppressants.
摘要翻译：提供下式的化合物：其中R是含有可被低级烷基，芳烷基，酰基或卤素原子取代的氮，硫或氧原子的杂芳酰基; 或可以被低级烷基，低级烯基，卤原子，卤代低级烯基，苯基，卤代苯基，低级烷氧基苯基，低级烷基苯基，甲酰基基团，羟基，氨基，羧基，氨基甲基或氧代基，其无毒盐及其制备方法。这些化合物可用作抗肿瘤剂和免疫抑制剂。

5. 发明授权

US4283422A 3-Amino-4-homoisotwistane derivatives 失效
标题翻译： 3-氨基-4-异亮氨酸衍生物
公开(公告)号：US4283422A
公开(公告)日：1981-08-11
申请号：US120834
申请日：1980-02-12
申请人： Toshio Atsumi , Yoshiaki Takebayashi , Hideki Okajima
发明人： Toshio Atsumi , Yoshiaki Takebayashi , Hideki Okajima
IPC分类号： A61K31/13 , A61P25/00 , A61P31/12 , C07C67/00 , C07C209/00 , C07C209/50 , C07C211/38 , C07C211/41 , C07C87/40
CPC分类号： C07C211/41 , C07C2103/70
摘要： Novel 3-amino-4-homoisotwistane derivatives of the formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.5 alkenyl group, and R.sub.2 is a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.5 alkenyl group, or non-toxic pharmaceutically acceptable salts thereof, which are very valuable as medicines for the treatment of virus-caused diseases and as antiviral agents for animals and useful for the treatment of parkinsonean disease.
摘要翻译：新颖的下式的3-氨基-4-异亮氨酸衍生物，其中R1是氢原子，C1-C4烷基或C3-C5烯基，R2是C1-C4烷基或C3- C5烯基或其无毒的药学上可接受的盐，其作为用于治疗病毒引起的疾病的药物和用作动物的抗病毒剂是非常有价值的，并且可用于治疗帕金森病。

6. 发明授权

US4260774A 5-Carbamoyl imidazoles 失效
标题翻译： 5-氨基甲酰咪唑
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。

7. 发明授权

US3962446A Analgesic compositions containing 2-cyanoalkylbenzomorphan derivatives and salts thereof 失效
标题翻译：含有2-氰基烷基苯并喃衍生物及其盐的止痛组合物
公开(公告)号：US3962446A
公开(公告)日：1976-06-08
申请号：US523412
申请日：1974-11-13
申请人： Toshio Atsumi , Kenji Kobayashi , Yoshiaki Takebayashi , Hisao Yamamoto
发明人： Toshio Atsumi , Kenji Kobayashi , Yoshiaki Takebayashi , Hisao Yamamoto
IPC分类号： A61K31/395 , A61K31/485
CPC分类号： A61K31/395
摘要： An analgesic composition comprising an analgesically effective amount of at least one 6,7-benzomorphan derivative of the formula: ##SPC1##Wherein R is a hydrogen atom, a hydroxyl group, a C.sup.1 - C.sup.3 alkoxy group or a C.sup.1 - C.sup.8 alkanoyloxy group; R.sub.1 is a hydrogen atom, a C.sup.1 - C.sup.5 alkyl group, a phenyl group, a halophenyl group, an alkylphenyl group wherein the alkyl moiety has 1 to 3 carbon atoms, an alkoxyphenyl group wherein the alkoxy moiety has 1 to 3 carbon atoms, a trifluoromethylphenyl group, an alkylthiophenyl group wherein the alkylthio moiety has 1 to 3 carbon atoms or a group of the formula (C.sub.m H.sub.2m.sub.-p.sub.+1) - (R.sub.9).sub.p wherein m is an integer of 1 - 6, p is an integer of 1 - 2 and R.sub.9 is a C.sup.1 - C.sup.3 alkoxy group; R.sub. 2 is a hydrogen atom or a C.sup.1 - C.sup.3 alkyl group; R.sub.3 is a hydrogen atom, a C.sup.1 - C.sup.3 alkyl group, a phenyl group or an alkoxyphenyl group wherein the alkoxy moiety has 1 to 3 carbon atoms; R.sub.4 is a hydrogen atom or a hydroxyl group, or R.sub.3 and R.sub.4 may form a C.sup.1 - C.sup.3 alkylidene group or a carbonyl group together with a carbon atom to which these substituents are bonded; R.sub.5 is a hydrogen atom or C.sup.1 - C.sup.3 alkyl group; R.sub.6 is a hydrogen atom or a methyl group; R.sub.7 and R.sub.8 are independently a hydrogen atom or a C.sup.1 - C.sup.2 alkyl group; and n is an integer of 0 - 2; or an acid addition salt thereof, and a pharmaceutically acceptable carrier or diluent, is disclosed.
摘要翻译：一种止痛组合物，其包含镇痛有效量的至少一种下式的6,7-苯并吗啉衍生物：WHEREIN R是氢原子，羟基，C1-C3烷氧基或C1-C8烷酰氧基; R1为氢原子，C1-C5烷基，苯基，卤代苯基，烷基部分为碳原子数1〜3的烷基苯基，烷氧基部分为碳原子数1〜3的烷氧基苯基，三氟甲基苯基，其中烷硫基部分具有1至3个碳原子的烷硫基苯基或式（CmH2m-p + 1） - （R9）p的基团，其中m是1-6的整数，p是整数1 - 2和R9是C1-C3烷氧基; R 2是氢原子或C 1 -C 3烷基; R3是氢原子，C1-C3烷基，苯基或烷氧基苯基，其中烷氧基部分具有1至3个碳原子; R4是氢原子或羟基，或者R3和R4可以与这些取代基结合的碳原子一起形成C1-C3亚烷基或羰基; R5是氢原子或C1-C3烷基; R6是氢原子或甲基; R 7和R 8独立地为氢原子或C 1 -C 2烷基; n为0-2的整数; 或其酸加成盐，以及药学上可接受的载体或稀释剂。

8. 发明授权

US3950346A Novel process for producing 2-ketoethylbenzomorphan derivatives and salts thereof 失效
标题翻译：生产2-乙基苯并吡喃衍生物的新方法及其制备方法
公开(公告)号：US3950346A
公开(公告)日：1976-04-13
申请号：US356807
申请日：1973-05-03
申请人： Toshio Atsumi , Kenji Kobayashi , Yoshiaki Takebayashi , Hisao Yamamoto
发明人： Toshio Atsumi , Kenji Kobayashi , Yoshiaki Takebayashi , Hisao Yamamoto
IPC分类号： C07D221/26
CPC分类号： C07D221/26
摘要： 2-Ketoethyl-6,7-benzomorphan derivatives of the formula: ##SPC1##And their pharmaceutically acceptable non-toxic salts, which are useful as non-addictive analgesics and pain-relieving agents and can be prepared by reacting the corresponding 6,7-benzomorphan derivative of the formula: ##SPC2##With a vinyl carbonyl compound of the formula: ##EQU1## [wherein R' is a hydrogen atom or a group of the formula: --OR" (wherein R" is a hydrogen atom, an alkanoyl group, an alkyl group, an aralkyl group, an alkoxycarbonylmethyl group or a tetrahydropyranyl group), R.sub.1 is a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, R.sub.2 is a hydrogen atom or an alkyl group and A is an alkyl group, an alkoxy group, a substituted or unsubstituted aryl group or a substituted or unsubstituted amino group].

9. 发明授权

US4464531A 4-Carbamoylimidazolium-5-olate derivatives 失效
标题翻译： 4-氨基甲酰基咪唑鎓-5-醇酸酯衍生物
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。

10. 发明授权

US5081139A N-substituted triazole derivatives and fungicidal use thereof 失效
标题翻译： N-取代三唑衍生物及其杀真菌剂
公开(公告)号：US5081139A
公开(公告)日：1992-01-14
申请号：US783185
申请日：1985-10-02
申请人： Ikutaro Saji , Yoshihiro Tanaka , Katsuaki Ichise , Tomoharu Tanio , Takao Okuda , Toshio Atsumi
发明人： Ikutaro Saji , Yoshihiro Tanaka , Katsuaki Ichise , Tomoharu Tanio , Takao Okuda , Toshio Atsumi
IPC分类号： C07D249/08 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： An N-substituted triazole compound of the formula: ##STR1## wherein Ph is a phenyl group or a phenyl group substituted with one or two halogen atoms, R.sup.1 is a C.sub.1 -C.sub.3 alkyl group, R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, R.sup.3 is a C.sub.1 -C.sub.8 alkyl group, a C.sub.4 -C.sub.8 cycloalkylalkyl group or a C.sub.3 -C.sub.6 cycloalkyl group and n is 0, 1 or 2, or an acid addition salt thereof, which is useful as an antifungal agent.
摘要翻译：下式的N-取代的三唑化合物：其中Ph是苯基或被一个或两个卤素原子取代的苯基，R 1是C 1 -C 3烷基，R 2是氢原子或 C1-C3烷基，R3是C1-C8烷基，C4-C8环烷基烷基或C3-C6环烷基，n是0,1或2，或其酸加成盐，可用作抗真菌剂代理商

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