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41. 发明授权

US5155113A Composition for increasing the anti-cancer activity of an anti-cancer compound 失效
标题翻译：用于增加抗癌化合物的抗癌活性的组合物
公开(公告)号：US5155113A
公开(公告)日：1992-10-13
申请号：US437315
申请日：1989-11-17
申请人： Setsuro Fujii
发明人： Setsuro Fujii
IPC分类号： A61K31/505 , C07D213/69 , C07D213/80 , C07D213/85 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07F7/18 , C07H19/06
CPC分类号： C07D213/69 , A61K31/505 , C07D213/80 , C07D213/85 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07F7/1856 , C07H19/06
摘要： A composition for increasing the anti-cancer activity of an anti-cancer compound selected from among 5-fluorouracil and a compound capable of producing 5-fluorouracil in vivo, the composition comprising an effective amount of a pyridine derivative represented by the formula ##STR1## wherein R.sup.1 is hydroxy or acyloxy, R.sup.2 and R.sup.4 are each hydrogen, halogen, amino, carboxyl, carbamoyl, cyano, nitro, lower alkyl, lower alkenyl or lower alkoxycarbonyl, R.sup.3 and R.sup.5 are each hydrogen, hydroxy or acyloxy; when at least one or R.sup.1, R.sup.3 and R.sup.5 is hydroxy, the structure of 1-position on the pyridine ring can be ##STR2## due to the keto-enol tautomerism, said hydrogen attached to nitrogen being optionally substituted with a substituent selected from the group consisting of lower alkyl, tetrahydrofuranyl, tetrahydropyranyl, lower alkoxy-lower alkyl, phthalidyl, carbamoyl, lower alkoxycarbonyl-lower alkylcarbamoyl, phenyl-lower alkoxy-lower alkyl, phenylcarbamoyl which may have a substituent on the phenyl ring, lower alkylcarbamoyl, carboxy-lower alkylcarbamoyl, lower alkylthio-lower alkyl and lower alkenyl, provided that the compound having the following formula is excluded, ##STR3## wherein .alpha. is hydrogen, lower alkyl, tetrahydrofuranyl, tetrahydropyranyl, lower alkoxy-lower alkyl, lower alkylcarbamoyl, lower alkylthio-lower alkyl or lower alkenyl.
摘要翻译：一种用于增加选自5-氟尿嘧啶和能够在体内产生5-氟尿嘧啶的化合物的抗癌化合物的抗癌活性的组合物，该组合物包含有效量的由式表示的吡啶衍生物，（1）其中R1是羟基或酰氧基，R2和R4各自为氢，卤素，氨基，羧基，氨基甲酰基，氰基，硝基，低级烷基，低级烯基或低级烷氧基羰基，R3和R5分别为氢，羟基或酰氧基; 当至少一个或R 1，R 3和R 5为羟基时，由于酮 - 烯醇互变异构，吡啶环上的1-位的结构可以是“IMAGE”，所述与氮连接的氢任选被选自以下的取代基取代：低级烷基，四氢呋喃基，四氢吡喃基，低级烷氧基 - 低级烷基，邻苯二甲酰基，氨基甲酰基，低级烷氧基羰基 - 低级烷基氨基甲酰基，苯基 - 低级烷氧基 - 低级烷基，苯基上可具有取代基的苯基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基甲酰基，低级烷基或低级烯基。

42. 发明授权

US4898876A Benzoylpiperazine esters and a process for their production 失效
标题翻译：苯甲酰哌嗪酯及其制备方法
公开(公告)号：US4898876A
公开(公告)日：1990-02-06
申请号：US796525
申请日：1985-11-12
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Kazuhiro Onogi , Masahiko Nagakura
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Kazuhiro Onogi , Masahiko Nagakura
IPC分类号： C07D209/48 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D237/28 , C07D241/44 , C07D261/18 , C07D295/192 , C07D307/79 , C07D307/84 , C07D307/86 , C07D311/12 , C07D311/58 , C07D311/84 , C07D317/68 , C07D319/18 , C07D333/54 , C07D333/60
CPC分类号： C07D209/48 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D237/28 , C07D241/44 , C07D261/18 , C07D295/192 , C07D307/79 , C07D307/84 , C07D307/86 , C07D311/12 , C07D311/58 , C07D311/84 , C07D317/68 , C07D319/18 , C07D333/54 , C07D333/60
摘要： A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group, excepting the case where A is a single bond, R.sub.1 is ##STR2## and R.sub.2 is a methyl group, exhibits excellent chymotrypsin inhibitive activity.
摘要翻译：下式的苯甲酰基哌嗪酯：其中A表示单键或亚烷基，亚乙烯基，-O-亚烷基或次甲基，R 1表示可被低级烷基取代的双环碳环残基，低级烷氧基，氧代基或硝基或卤素原子，或可部分饱和; 可含有氧代基的芴残基; 亚芴基; 蒽残基; 可以被低级烷基取代的菲残基，或可以部分饱和; 可以被低级烷基或低级烷氧基取代的苯并呋喃残基或硫杂残基; 可被氧代基或苯基取代并部分饱和的苯并吡喃残基或苯并嗪残基; 邻苯二甲酰亚胺残基; 苯并二氮残基; 可以被低级烷基或苯基取代的异唑残基; 或亚烷基二氧基苯残基或呫吨残基; 除了A为单键，R 1为甲基，R 2为甲基的情况外，R 2表示烷基，环烷基，环烷基烷基或芳烷基，表现出优异的糜蛋白酶抑制活性。

43. 发明授权

US4864021A 5-fluorouracil derivatives 失效
标题翻译： 5-氟尿嘧啶衍生物
公开(公告)号：US4864021A
公开(公告)日：1989-09-05
申请号：US903824
申请日：1986-09-03
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
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.
摘要翻译：公开了由式（1a）表示的抗癌化合物，其中R1和R2之一是任选具有取代基的苯基 - 低级烷基，苯基 - 低级烯基或萘基 - 低级烷基，R1和R2中的另一个或者R 3是氢，酰基或四氢呋喃基，或由式（1b）表示，其中Rx是任选取代的吡啶基，Y是亚芳基，α是可以转化的已知的5-氟尿嘧啶衍生物残基到5-氟尿嘧啶，其通过酯或酰胺键与羰基连接。

44. 发明授权

US4755383A Pharmaceutical composition suitable for intestinal administration 失效
标题翻译：适合肠道给药的药物组合物
公开(公告)号：US4755383A
公开(公告)日：1988-07-05
申请号：US879946
申请日：1986-06-30
申请人： Setsuro Fujii , Touru Yokoyama , Kouji Ikegaya , Nobuo Yokoo , Masahiko Nagakura
发明人： Setsuro Fujii , Touru Yokoyama , Kouji Ikegaya , Nobuo Yokoo , Masahiko Nagakura
IPC分类号： A61K31/495 , A61K38/00 , A61K38/23 , A61K38/46 , A61K38/48 , A61K38/55 , A61K39/395 , A61K45/06 , A61P43/00 , A61K37/54
CPC分类号： A61K45/06 , A61K31/495 , A61K38/005 , Y10S514/808
摘要： A pharmaceutical composition is disclosed which comprises a physiologically active substance possessing peptide bonds in its structure and being inactivable by digestive enzymes, the active substances being other than insulin, and a synthetic chymotrypsin inhibitor. The composition is particularly suitable for intestinal absorption of the active substance.

45. 发明授权

US4622325A Anti-cancer composition for delivering 5-fluorouracil 失效
标题翻译：用于递送5-氟尿嘧啶的抗癌组合物
公开(公告)号：US4622325A
公开(公告)日：1986-11-11
申请号：US591459
申请日：1984-03-20
申请人： Setsuro Fujii , Norio Unemi , Setsuo Takeda
发明人： Setsuro Fujii , Norio Unemi , Setsuo Takeda
IPC分类号： A61K31/505 , C07D239/54 , C07D239/553
CPC分类号： C07D239/553 , A61K31/505 , Y10S514/922
摘要： An anti-cancer composition for delivering 5-fluorouracil to cancer tissues in a warm-blooded animal, wherein the cancer is a cancer sensitive to 5-fluorouracil, comprising 1-n-hexylcarbamoyl-5-fluorouracil and uracil (or salt there-of), wherein the composition contains less than 0.1 mole of the 5-fluorouracil per mole of the uracil.
摘要翻译：一种用于将5-氟尿嘧啶递送至温血动物的癌症组织的抗癌组合物，其中所述癌症是对5-氟尿嘧啶敏感的癌症，其包含1-正己基氨基甲酰基-5-氟尿嘧啶和尿嘧啶（或其中的盐）），其中所述组合物每摩尔尿嘧啶含有少于0.1摩尔的5-氟尿嘧啶。

46. 发明授权

US4599404A 2-deoxy-5-fluorouridine derivative and a process for producing the same and an antitumor agent comprising the same 失效
标题翻译： 2-脱氧-5-氟尿苷衍生物及其制备方法和包含其的抗肿瘤剂
公开(公告)号：US4599404A
公开(公告)日：1986-07-08
申请号：US068340
申请日：1979-08-21
申请人： Setsuro Fujii , Eiichi Sakakibara
发明人： Setsuro Fujii , Eiichi Sakakibara
IPC分类号： C07H19/073 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/06
CPC分类号： C07H19/06
摘要： A 2'-deoxy-5-fluorouridine derivative represented by the formula; ##STR1## wherein R represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, an acetyloxy group or a halogen atom, and n is an integer of 1 to 3.

47. 发明授权

US4507301A Anti-cancer composition for delivering 5-fluorouracil 失效
标题翻译：用于递送5-氟尿嘧啶的抗癌组合物
公开(公告)号：US4507301A
公开(公告)日：1985-03-26
申请号：US214022
申请日：1980-12-08
申请人： Setsuro Fujii , Norio Unemi , Setsuo Takeda
发明人： Setsuro Fujii , Norio Unemi , Setsuo Takeda
IPC分类号： A61K31/505 , C07D239/54 , C07D239/553
CPC分类号： C07D239/553 , A61K31/505 , Y10S514/922
摘要： An anti-cancer composition comprising a 5-fluorouracil (including derivatives thereof) and uracil (or salt thereof), is disclosed, wherein the composition contains less than 0.1 mole of the 5-fluorouracil per mole of the uracil.
摘要翻译：公开了包含5-氟尿嘧啶（包括其衍生物）和尿嘧啶（或其盐）的抗癌组合物，其中组合物每摩尔尿嘧啶含有少于0.1摩尔的5-氟尿嘧啶。

48. 发明授权

US4481203A Composition containing 1-(n-hexylcarbamoyl)-5-fluorouracil and uracil 失效
标题翻译：含有1-（正己基氨基甲酰基）-5-氟尿嘧啶和尿嘧啶的组合物
公开(公告)号：US4481203A
公开(公告)日：1984-11-06
申请号：US212543
申请日：1980-12-03
申请人： Setsuro Fujii , Norio Unemi , Setsuo Takeda
发明人： Setsuro Fujii , Norio Unemi , Setsuo Takeda
IPC分类号： A61K31/505 , C07D239/54 , C07D239/553
CPC分类号： C07D239/553 , A61K31/505 , Y10S514/922
摘要： A composition for delivering 5-fluorouracil to cancer tissues, of a cancer sensitive to 5-fluorouracil, in warm blooded animals, comprising effective amounts of 1-(n-hexylcarbamoyl)-5-fluorouracil and uracil in a molar ratio of 1:0.1-10, respectively.
摘要翻译：用于向温血动物中向5-氟尿嘧啶敏感的癌症组织递送5-氟尿嘧啶的组合物，其包含有效量的1-（正己基氨基甲酰基）-5-氟尿嘧啶和尿嘧啶的摩尔比为1:0.1 -10。

49. 发明授权

US4443603A Piperazine derivatives, of aromatic acids 失效
标题翻译：哌嗪衍生物，芳香酸
公开(公告)号：US4443603A
公开(公告)日：1984-04-17
申请号：US381443
申请日：1982-05-24
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Hiroshi Ishihama
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Hiroshi Ishihama
IPC分类号： C07D295/18 , A61K31/495 , A61P43/00 , C07D207/24 , C07D209/18 , C07D295/088 , C07D295/13 , C07D295/15 , C07D295/185 , C07D403/12 , C07D241/04
CPC分类号： C07D295/185 , C07D207/24 , C07D209/18 , C07D295/088 , C07D295/13 , C07D295/15
摘要： A piperazine derivartive represented by the following formula: ##STR1## wherein R.sub.1 : an indolyl group which may optionally be substituted by one or more lower alkyl and/or lower alkoxy groups, naphthyl group which may optionally be saturated partially with 2 or 4 hydrogen atoms, or phenyl or cyclohexyl group which may optionally be substituted by one or more lower alkyl groups;A: a single bond or alkylene group;P: a single bond or vinylene group;Q: an -O-alkylene group or -NH-alkylene group when P is a single bond, or a single bond when P is a vinylene group; andR.sub.2 : a lower alkyl, morpholino-lower alkyl, morpholino-carbonyl lower alkyl, piperidinocarbonyl lower alkyl, piperazinocarbonyl lower alkyl or lower alkylaminocarbonyl lower alkyl group, or an acid addition salt thereof is a proteolytic enzyme inhibitor.
摘要翻译：由下式表示的哌嗪衍生物：其中R 1：可任选被一个或多个低级烷基和/或低级烷氧基取代的吲哚基，可任选地被2或4个氢原子部分饱和的萘基，或可任意被一个或多个低级烷基取代的苯基或环己基; A：单键或亚烷基; P：单键或亚乙烯基; Q：当P为单键时为-O-亚烷基或-NH-亚烷基，或当P为亚乙烯基时为单键; R2为低级烷基，吗啉代低级烷基，吗啉代羰基低级烷基，哌啶子基羰基低级烷基，哌嗪基羰基低级烷基或低级烷基氨基羰基低级烷基，或其酸加成盐为蛋白水解酶抑制剂。

50. 发明授权

US4411911A Method of treating hyperlipidemia and inflammation with sulfonate derivatives 失效
标题翻译：用磺酸衍生物治疗高脂血症和炎症的方法
公开(公告)号：US4411911A
公开(公告)日：1983-10-25
申请号：US225979
申请日：1981-01-19
申请人： Setsuro Fujii , Toshihiro Hamakawa , Kazuo Ogawa , Yoshiyuki Muranaka , Sadao Hashimoto
发明人： Setsuro Fujii , Toshihiro Hamakawa , Kazuo Ogawa , Yoshiyuki Muranaka , Sadao Hashimoto
IPC分类号： A61K31/255 , A61K31/335 , C07C309/65 , C07C309/68 , C07C309/71 , C07C309/73 , C07C309/74 , C07C309/75 , C07C309/76 , C07C309/77 , C07D307/12 , C07D307/24 , C07D307/46 , C07D309/04 , C07D309/06 , C07D317/18 , C07D317/32 , A61K31/35 , A61K31/34
CPC分类号： C07D307/12 , A61K31/255 , C07C309/65 , C07C309/68 , C07C309/71 , C07C309/73 , C07C309/74 , C07C309/75 , C07C309/76 , C07C309/77 , C07D307/24 , C07D309/04 , C07D309/06 , C07D317/32 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要： Novel sulfonate derivatives represented by the formulaR.sub.1 SO.sub.3 CH.sub.2 CO(CH.sub.2).sub.n R.sub.2act to inhibit esterases and chymotripsin and are useful as antilipemic agents, anti-inflammatory agents, immunity controlling agents, etc.
摘要翻译：由式R 1 SO 3 CH 2 CO（CH 2）n R 2表示的新型磺酸酯衍生物用于抑制酯酶和糜蛋白酶，并且可用作抗消瘦剂，抗炎剂，免疫控制剂等。

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