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51. 发明授权

US4080455A 5-Fluoropyrimidin-4-one compositions 失效
标题翻译： 5-氟嘧啶-4-酮组合物
公开(公告)号：US4080455A
公开(公告)日：1978-03-21
申请号：US701216
申请日：1976-06-30
申请人： Mitugi Yasumoto , Junichi Yamashita , Ichiro Yamawaki , Norio Unemi , Kenji Kitazato , Sadao Hashimoto , Setsuro Fujii
发明人： Mitugi Yasumoto , Junichi Yamashita , Ichiro Yamawaki , Norio Unemi , Kenji Kitazato , Sadao Hashimoto , Setsuro Fujii
IPC分类号： C07D239/52 , A61K31/505
CPC分类号： C07D239/52
摘要： A 5-fluoropyrimidin-4-one derivative represented by the formula ##STR1## wherein R is straight-chain or branched-chain alkyl having 4 to 18 carbon atoms, straight-chain or branched-chain alkenyl having 2 to 18 carbon atoms, alkylene oxido having 3 to 10 carbon atoms, aryl or aralkyl;Processes for preparing the derivative;An anti-tumor composition containing the derivative as an effective component and an excipient.
摘要翻译：其中R为具有4至18个碳原子的直链或支链烷基，具有2至18个碳原子的直链或支链烯基，亚烷基具有3至10个碳原子的氧化物，芳基或芳烷基; 制备衍生物的方法; 包含衍生物作为有效成分和特殊物质的抗肿瘤组合物。

52. 发明授权

US4983609A 5-fluorouracil derivatives 失效
标题翻译： 5-氟尿嘧啶衍生物
公开(公告)号：US4983609A
公开(公告)日：1991-01-08
申请号：US219521
申请日：1988-07-15
申请人： Setsuro Fujii
发明人： Setsuro Fujii
IPC分类号： A61K31/505 , C07D213/69 , C07D213/80 , C07D213/85 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07F7/18 , C07H19/06 , C07D239/10
CPC分类号： C07D213/69 , A61K31/505 , C07D213/80 , C07D213/85 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07F7/1856 , C07H19/06
摘要： An anticancer compound is disclosed which is represented by the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is a phenyl-lower alkyl optionally having a substituent, phenyl-lower alkenyl or naphthyl-lower alkyl, the other of R.sup.1 and R.sup.2 is hydrogen or acyl, and R.sup.3 is hydrogen, acyl or tetrahydrofuranyl, or represented by the formula ##STR2## wherein R.sup.x is an optionally substituted pyridyl, Y is arylene and .alpha. is a known 5-fluorouracil derivative residue which can be converted to 5-fluorouracil in vivo and which is linked to the carbonyl by an ester or amide linkage.

53. 发明授权

US4898859A 2-Oxa-isocephem compounds and compositions containing same 失效
标题翻译： 2-氧杂 - 异头孢烯化合物和含有它们的组合物
公开(公告)号：US4898859A
公开(公告)日：1990-02-06
申请号：US165942
申请日：1988-03-09
申请人： Setsuro Fujii , Hiroshi Ishikawa , Koichi Yasumura , Koichiro Jitsukawa , Sachio Toyama , Hidetsugu Tsubouchi , Kimio Sudo , Kouichi Tsuji
发明人： Setsuro Fujii , Hiroshi Ishikawa , Koichi Yasumura , Koichiro Jitsukawa , Sachio Toyama , Hidetsugu Tsubouchi , Kimio Sudo , Kouichi Tsuji
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： A 2-oxa-isocephem compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined, pharmaceutically acceptable salts thereof, composition containing the same and processes for preparing the same are disclosed. The compound is useful as an antimicrobial agent.

54. 发明授权

US4886877A Novel 2'-deoxy-5-substituted uridine derivatives, processes for preparing the same and antitumor agent containing the same 失效
标题翻译：新的2'-脱氧-5-取代的尿苷衍生物，其制备方法和含有它们的抗肿瘤剂
公开(公告)号：US4886877A
公开(公告)日：1989-12-12
申请号：US163237
申请日：1988-02-26
申请人： Setsuro Fujii , Jun-ichi Yamashita , Hiroshi Matsumoto , Setsuo Takeda , Tadafumi Terada , Mitsugi Yasumoto , Norio Unemi
发明人： Setsuro Fujii , Jun-ichi Yamashita , Hiroshi Matsumoto , Setsuo Takeda , Tadafumi Terada , Mitsugi Yasumoto , Norio Unemi
IPC分类号： C07D405/04 , C07H19/06
CPC分类号： C07H19/06
摘要： Novel 2'-deoxy-5-substituted uridine derivative represented by the general formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a benzoyl group or a tetrahydrofuranyl group; R.sub.2 is a fluorine atom or a trifluoromethyl group; and any one of R.sub.3 and R.sub.4 is a hydrogen atom and the other one is an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, a benzyl group having as the substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a nitro group, or an alkyl group having 1 to 3 carbon atoms having one or two phenyl groups as the substituents.The novel 2'-deoxy-5-substituteduridine derivative possesses excellent antitumor activity with less toxicity, thus it is useful as antitumor agent.
摘要翻译：由通式表示的新型2'-脱氧-5-取代的尿苷衍生物，其中R1是氢原子，苯甲酰基或四氢呋喃基; R2是氟原子或三氟甲基; R 3和R 4中的任一个为氢原子，另一个为碳原子数1〜10的烷基，碳原子数为2〜6的烯基，作为取代基的苄基，选自卤原子，碳原子数为1〜4的烷基，碳原子数为1〜4的烷氧基，硝基，碳原子数为1〜3的烷基，具有一个或两个苯基作为取代基。新型2'-脱氧-5-取代尿苷衍生物具有优异的抗肿瘤活性，毒性低，因此可用作抗肿瘤剂。

55. 发明授权

US4831026A 2-oxa-isocephem compounds, compositions containing same and processes of using 失效
标题翻译： 2-氧杂 - 异头孢烯化合物，含有它们的组合物和使用方法
公开(公告)号：US4831026A
公开(公告)日：1989-05-16
申请号：US23602
申请日：1987-03-09
申请人： Setsuro Fujii , Hiroshi Ishikawa , Koichi Yasumura , Koichiro Jitsukawa , Sachio Toyama , Hidetsugu Tsubouchi , Kimio Sudo , Kouichi Tsuji
发明人： Setsuro Fujii , Hiroshi Ishikawa , Koichi Yasumura , Koichiro Jitsukawa , Sachio Toyama , Hidetsugu Tsubouchi , Kimio Sudo , Kouichi Tsuji
IPC分类号： C07D505/00 , A61K31/535 , A61P31/04 , C07D498/04 , C07D507/04 , C07D507/06 , C07D507/08
CPC分类号： C07D498/04
摘要： A 2-oxa-isocephem compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined, pharmaceutically acceptable salts thereof, esters of the carboxy group in the 4-position thereof and quaternary ammonium salts thereof, composition containing the same and processes for preparing the same are disclosed. The compound is useful as an antimicrobial compound.
摘要翻译：式（1）的2-氧杂 - 异头孢烯化合物：其中R1，R2和R3如上定义，其药学上可接受的盐，其4-位的羧基酯和季铵盐公开了含有该组合物的组合物及其制备方法。该化合物可用作抗微生物化合物。

56. 发明授权

US4824834A Pyrazolotriazine compounds 失效
标题翻译：吡唑并三嗪化合物
公开(公告)号：US4824834A
公开(公告)日：1989-04-25
申请号：US105581
申请日：1987-10-08
申请人： Setsuro Fujii , Hiroyuki Kawamura , Hiroshi Kiyokawa , Satoshi Yamada
发明人： Setsuro Fujii , Hiroyuki Kawamura , Hiroshi Kiyokawa , Satoshi Yamada
IPC分类号： A61K31/53 , A61P19/06 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04 , Y02P20/582
摘要： Pyrazolotriazine compounds of the formula: ##STR1## wherein R.sup.1 is OH or alkanoyloxy; R.sup.2 is H, OH, or SH; R.sup.3 is (1) unsaturated N- or S-containing heterocyclic group optionally having 1-2 substituents of halogen, nitro or phenylthio, (2) naphthyl, (3) phenyl optionally having 1-3 substituents of (i) alkyl, (ii) phenyl, (iii) alkoxycarbonyl, (iv) cyano, (v) nitro, (vi) alkoxy, (vii) phenylalkoxy (viii) phenylthio-alkyl, (ix) phenoxy, (x) ##STR2## R is alkyl, halo-substituted alkyl, phenyl optionally having 1-3 substituents, or pyridyl, and l is 0, 1 or 2, (xi) halogen, (xii) phenylalkyl, (xiii) carboxy, (xiv) alkanoyl, (xv) benzoyl optionally having 1-3 substituents, (xvi) amino, (xvii) OH, (xviii) alkanoyloxy, (xix) ##STR3## or (xx) ##STR4## (A is alkylene), said compounds having a xanthine oxidase inhibitory activity and are useful for the prophylaxis and treatment of gout.
摘要翻译：下式的吡唑并三嗪化合物：其中R1是OH或烷酰氧基; R2是H，OH或SH; R3是（1）任选具有1-2个卤素取代基的不饱和N-或S-杂环基，硝基或苯硫基，（2）萘基，（3）任选具有1-3个（i）烷基取代基的苯基，（ii））苯基，（iii）烷氧基羰基，（iv）氰基，（ⅴ）硝基，（vi）烷氧基，（i）苯基烷氧基（ii）苯硫基烷基，（ix）苯氧基，（Ⅹ）取代的烷基，任选具有1-3个取代基的苯基或吡啶基，l是0,1或2，（xi）卤素，（xii）苯基烷基，（xiii）羧基，（xiv）烷酰基，（xv） 1-3取代基，（xvi）氨基，（xvii）OH，（xviii）烷酰氧基，（xix）或（xx）（A是亚烷基），所述化合物具有黄嘌呤氧化酶抑制活性，用于预防和治疗痛风。

57. 发明授权

US4788141A Automatic analyzer for guanase activity 失效
标题翻译：自动分析仪进行鸟类活动
公开(公告)号：US4788141A
公开(公告)日：1988-11-29
申请号：US078009
申请日：1987-07-24
申请人： Seiichiro Yamasaki , Setsuro Fujii , Isao Nakagawa , Nobumoto Chikazawa , Toshiharu Muraoka
发明人： Seiichiro Yamasaki , Setsuro Fujii , Isao Nakagawa , Nobumoto Chikazawa , Toshiharu Muraoka
IPC分类号： G01J5/60 , A61K35/14 , C12Q1/34 , G01N33/483 , G01N33/80 , G01N35/04
CPC分类号： C12Q1/34 , G01N2333/978
摘要： An automatic analyzer comprising a plurality of sample containers for accommodating different blood samples individually, specific sample container moving means, a plurality of reagent containers for accommodating at least a reagent for an assay of guanase activity, a specific reagent container holding means, a plurality of reaction containers, specific reaction container moving means, specific sample pouring means, specific cleaning vessels, specific stirring means, specific measuring means, specific cleaning means, a specific analog-digital converter, specific counting-calculating means, a specific display means, and specific operation control means, so that the display means produces a signal for excluding the measured blood sample corresponding to a display value when the display value is above a predetermined reference value of guanase activity.
摘要翻译：一种自动分析装置，其特征在于，包括分别容纳不同的血液样本的多个检体容器，特定的检体容器移动机构，至少容纳用于检测动物活动的试剂的多个试剂容器，特定试剂容器保持机构，反应容器，特定反应容器移动装置，特定的样品注入装置，特定的清洁容器，特定的搅拌装置，特定的测量装置，特定的清洁装置，特定的模拟数字转换器，特定的计数计算装置，特定的显示装置和特定的操作控制装置，使得当显示值高于动画活动的预定参考值时，显示装置产生用于排除与显示值相对应的测量血样的信号。

58. 发明授权

US4675428A Sulfonic acid ester derivatives useful as antilipemic agents 失效
标题翻译：可用作抗脂药的磺酸酯衍生物
公开(公告)号：US4675428A
公开(公告)日：1987-06-23
申请号：US861635
申请日：1986-05-07
申请人： Setsuro Fujii , Kazuo Ogawa , Toshihiro Hamakawa , Yoshiyuki Muranaka
发明人： Setsuro Fujii , Kazuo Ogawa , Toshihiro Hamakawa , Yoshiyuki Muranaka
IPC分类号： C07C309/73 , C07C143/68
CPC分类号： C07C309/00
摘要： A sulfonic acid ester derivative represented by the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, A is a group represented by the general formula ##STR2## (wherein R.sub.2 and R.sub.3 are each alkyl having 1 to 4 carbon atoms) or by the general formula ##STR3## (wherein R.sub.4 and R.sub.5 are each alkyl having 1 to 4 carbon atoms or, when taken together with the cabon atom to which they are attached, form cycloalkyl having 4 to 6 carbon atoms), and l is an integer of from 1 to 3, and a process for preparing the derivative.
摘要翻译： PCT No.PCT / JP83 / 00300 Sec。 1984年4月30日 102（e）日期1984年4月30日PCT提交1983年9月6日PCT公布。第WO84 / 00959号公报 1984年3月15日，由通式表示的磺酸酯衍生物，其中R1是氢原子，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基，A是由通式[IMAGE]（其中R2和R3各自为具有1至4个碳原子的烷基）或通式为其中R 4和R 5各自为具有1至4个碳原子的烷基，或者当与碳原子一起与它们相连的原子，形成具有4-6个碳原子的环烷基），和l是1至3的整数，以及制备该衍生物的方法。

59. 发明授权

US4620005A 1-isopropyl-4[(4-tetrahydro-1-naphthoyloxy phenyl)(alkylene)-carbonyl(oxymethlcarbonyl)]piperazines having chymotrypsin-inhibitory activity 失效
标题翻译：具有胰凝乳蛋白酶抑制活性的1-异丙基-4 [（4-四氢-1-萘氧基苯基）（亚烷基） - 羰基（羟甲羰基）]哌嗪
公开(公告)号：US4620005A
公开(公告)日：1986-10-28
申请号：US787714
申请日：1985-10-17
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Hisashi Kunieda , Koichiro Watanabe , Hiroshi Ishihama
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Hisashi Kunieda , Koichiro Watanabe , Hiroshi Ishihama
IPC分类号： C07D295/10 , A61K31/495 , A61P1/00 , A61P43/00 , C07D295/108 , C07D295/12 , C07D295/13 , C07D295/18 , C07D295/185 , C07D241/04
CPC分类号： C07D295/185 , C07D295/108 , C07D295/13
摘要： Phenyl tetrahydronaphthylcarboxylate of the formula: ##STR1## wherein A is a direct bond, or a lower alkylene, vinylene or imino group; B is a direct bond, a lower alkylene or --NH-lower alkylene group, or an --OCH.sub.2 CO-- residual group; and R is a lower alkyl group, with the proviso that A and B are not direct bonds simultaneously, and A, B and R are not a lower alkylene group, a direct bond and a methyl group, respectively, at the same time, are effectively useful as chymotrypsin inhibitors.
摘要翻译：下式的四氢萘基羧酸苯酯：其中A是直接键，或低级亚烷基，亚乙烯基或亚氨基; B是直接键，低级亚烷基或-NH-低级亚烷基或-OCH 2 CO-残基; 并且R是低级烷基，条件是A和B不是同时是直接键，并且A，B和R不分别是低级亚烷基，直接键和甲基，同时是有效用作糜蛋白酶抑制剂。

60. 发明授权

US4605739A Benzoyl indolecarboxylates 失效
标题翻译：苯甲酰基吲哚羧酸盐
公开(公告)号：US4605739A
公开(公告)日：1986-08-12
申请号：US608957
申请日：1984-05-10
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Hisashi Kunieda , Koichiro Watanabe , Hiroshi Ishihama
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Hisashi Kunieda , Koichiro Watanabe , Hiroshi Ishihama
IPC分类号： A61K31/495 , A61P1/00 , C07D207/12 , C07D209/42 , C07D403/12
CPC分类号： C07D209/42 , C07D207/12
摘要： Benzoyl indolecarboxylates of the formula: ##STR1## where R.sup.1 is hydrogen, halogen, lower alkyl or lower alkoxy; R.sup.2 is hydrogen, lower alkyl, acetyl or benzoyl; R.sup.3 is hydrogen or lower alkyl; and A is a direct bond, or lower alkylene or vinylene substituted at the 2-, 3- or 5-position of the indole nucleus, are effective agents as chymotrypsin inhibitors.
摘要翻译：下式的苯甲酰基吲哚羧酸盐：其中R 1是氢，卤素，低级烷基或低级烷氧基; R2是氢，低级烷基，乙酰基或苯甲酰基; R3是氢或低级烷基; 并且A是直接键合，或在吲哚核的2-，3-或5-位取代的低级亚烷基或亚乙烯基，作为糜蛋白酶抑制剂是有效的试剂。

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