专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4503045A 2'-Deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine derivatives, a process for the preparation of the derivatives and anti-tumor agents containing the derivatives 失效
标题翻译： 2'-脱氧-3'，5'-二-O-烷基羰基-5-氟尿苷衍生物，制备衍生物的方法和含有衍生物的抗肿瘤剂
公开(公告)号：US4503045A
公开(公告)日：1985-03-05
申请号：US234569
申请日：1981-02-13
申请人： Setsuro Fujii , Bompei Yasui , Tomohisa Miyamoto , Masatoshi Shiga , Kazuko Ando , Iwao Hashimoto , Masahiro Kawasaki , Yoichiro Kawai , Yuji Mino
发明人： Setsuro Fujii , Bompei Yasui , Tomohisa Miyamoto , Masatoshi Shiga , Kazuko Ando , Iwao Hashimoto , Masahiro Kawasaki , Yoichiro Kawai , Yuji Mino
IPC分类号： C07H19/073 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/00 , C07H19/06 , C07H19/08
CPC分类号： C07H19/06
摘要： 2'-Deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine derivatives possessing strong anti-tumor activity with weak toxicity and represented by the general formula: ##STR1## wherein R stands for an alkyl group, an alkoxy group or a halogen atom, m for zero or an integer of 1-3, and n for an integer of 1-14, with the proviso that when m is 2 or 3, R's may be the same or different and that when m is 2 and the adjacent two R's are alkoxy groups, the two alkyl moieties of the alkoxy groups may be combined to form together with the two adjacent oxa bridging members an alkylenedioxy group as a whole. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administration.
摘要翻译： 2'-脱氧-3'，5'-二-O-烷基羰基-5-氟尿苷衍生物具有强的抗肿瘤活性，毒性弱，由以下通式表示：其中R代表烷基，烷氧基基团或卤素原子，m为0或1-3的整数，n为1-14的整数，条件是当m为2或3时，R可以相同或不同，当m为 2并且相邻的两个R是烷氧基，烷氧基的两个烷基部分可以与两个相邻的氧杂桥连成员一起与亚烷基二氧基整体形成。这些衍生物通过用相应的苯甲酰卤酰化2'-脱氧-3'，5'-二-O-烷基羰基-5-氟尿苷来制备，并且可用作抗肿瘤剂的活性成分，特别是用于口服给药。

2. 发明授权

US4425335A Ester derivatives of alkoxybenzoyldeoxyfluorouridine 失效
标题翻译：烷氧基苯甲酰基脱氧氟尿苷的酯衍生物
公开(公告)号：US4425335A
公开(公告)日：1984-01-10
申请号：US291809
申请日：1981-08-10
申请人： Setsuro Fujii , Bompei Yasui , Mitsuo Nakamura , Mitsuru Hirohashi , Tomohisa Miyamoto , Kazuko Ando , Iwao Hashimoto , Naoki Umeda , Masahiro Kawasaki
发明人： Setsuro Fujii , Bompei Yasui , Mitsuo Nakamura , Mitsuru Hirohashi , Tomohisa Miyamoto , Kazuko Ando , Iwao Hashimoto , Naoki Umeda , Masahiro Kawasaki
IPC分类号： C07H19/073 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/06 , C07H19/08
CPC分类号： C07H19/06
摘要： New ester derivatives of alkoxybenzoyldeoxyfluorouridine of the general formula ##STR1## wherein R stands for an alkoxy group having 1 to 4 carbon atoms, m for 1 or 2, and n for 3 or 4 with the proviso that when m is 2, the adjacent two R's may be combined to form an alkylenedioxy group as a whole. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administration.
摘要翻译：通式为“IMAGE”的烷氧基苯甲酰基脱氧氟尿酸的新酯衍生物，其中R代表具有1至4个碳原子的烷氧基，m为1或2，n为3或4，条件是当m为2时， R可以组合形成亚烷基二氧基整体。这些衍生物通过用相应的苯甲酰卤酰化2'-脱氧-3'，5'-二-O-烷基羰基-5-氟尿苷来制备，并且可用作抗肿瘤剂的活性成分，特别是用于口服给药。

3. 发明授权

US4416875A Ester derivatives of deoxyfluorouridine 失效
标题翻译：脱氧氟尿苷酯衍生物
公开(公告)号：US4416875A
公开(公告)日：1983-11-22
申请号：US290420
申请日：1981-08-06
申请人： Setsuro Fujii , Bompei Yasui , Mitsuo Nakamura , Tomohisa Miyamoto , Kazuko Ando , Iwao Hashimoto , Yoneichi Sawai , Naoki Umeda , Masahiro Kawasaki
发明人： Setsuro Fujii , Bompei Yasui , Mitsuo Nakamura , Tomohisa Miyamoto , Kazuko Ando , Iwao Hashimoto , Yoneichi Sawai , Naoki Umeda , Masahiro Kawasaki
IPC分类号： C07H19/073 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/06 , C07H19/08
CPC分类号： C07H19/06
摘要： New ester derivatives of deoxyfluorouridine of the general formula: ##STR1## wherein R and R.sup.40, may be identical or different, and may be hydrogen, halogen or methyl and n is 3 or 4. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administeration.
摘要翻译：脱氧氟尿苷的新酯衍生物，其通式如下：其中R和R40可以相同或不同，并且可以是氢，卤素或甲基，n是3或4.这些衍生物是通过酰化2'-脱氧 -3'，5'-二-O-烷基羰基-5-氟尿苷与相应的苯甲酰基卤化物，并且可用作抗肿瘤剂的活性成分，特别是用于口服给药。

4. 发明授权

US5162305A Polypeptide derivatives 失效
标题翻译：多肽衍生物
公开(公告)号：US5162305A
公开(公告)日：1992-11-10
申请号：US314018
申请日：1989-02-23
申请人： Setsuro Fujii , Yoshihito Yamamoto , Fumio Shimizu , Masatoshi Inai , Mitsuru Hirohashi
发明人： Setsuro Fujii , Yoshihito Yamamoto , Fumio Shimizu , Masatoshi Inai , Mitsuru Hirohashi
IPC分类号： A61K38/23 , A61K38/00 , A61P5/12 , C07K7/06 , C07K14/575 , C07K14/585
CPC分类号： C07K14/585 , A61K38/00
摘要： Novel synthetic polypeptide derivatives, i.e., novel calcitonin derivatives, having improved basic physiological activities of the corresponding natural calcitonins, i.e., the activity for lowering the blood level of calcium, the activity as an analgesic, as well as the activity for inhibiting the secretion of the gastric juice. Thus these synthetic calcitonins are effective as agents for curing hypercalcemia, analgetic agents, anti-ulcerative agents and the like.

5. 发明授权

US5047521A 5-fluorouracil derivatives 失效
标题翻译： 5-氟尿嘧啶衍生物
公开(公告)号：US5047521A
公开(公告)日：1991-09-10
申请号：US150407
申请日：1988-02-09
申请人： Setsuro Fujii , Mitsuru Hirohashi , Yoshihito Yamamoto , Yutaka Kojima
发明人： Setsuro Fujii , Mitsuru Hirohashi , Yoshihito Yamamoto , Yutaka Kojima
IPC分类号： A61K31/505 , A61K31/70 , C07D239/54 , C07D239/553 , C07D401/12 , C07D409/06 , C07D409/14 , C07H19/06 , C07H19/073 , H01S4/00
CPC分类号： C07D239/553 , C07D401/12 , C07D409/14 , C07H19/06
摘要： This invention relates to a novel 5-fluorouracil derivative represented by the formula ##STR1## wherein R.sup.y is a hydrogen atom or a specific acyl group, Z is a phenyl-lower alkoxy-lower alkyl group, thienyl-lower alkyl group optionally substituted with halogen atom on the thienyl ring, or a group ##STR2## wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a specific acyl group, phenyl-lower alkyl group having a group R.sup.x OCO-- on the phenyl ring, or a group --(A).sub.n B, R.sup.x being a specific organic group, A being a lower alkylene group, n being 0 or 1, and B being a 5- or 6-membered unsaturated heterocyclic group having 1 to 4 hetero-atoms selected from N, O and S and optionally having a benzene ring, naphthalene ring or pyridine ring condensed therewith, with the proviso that R.sup.1 and R.sup.2 are not hydrogen atoms or specific acyl groups at the same time; to a process for preparing the same; and to an anticancer composition comprising the same as an effective ingredient.
摘要翻译： PCT No.PCT / JP87 / 00275 Sec。 371日期1988年2月9日 102（e）1988年2月9日PCT PCT公开1987年4月30日PCT公布。公开号WO87 / 06582 日本公开日：1987年11月5日。本发明涉及由式（1）表示的新型5-氟尿嘧啶衍生物，其中R y为氢原子或特定酰基，Z为苯基 - 低级烷氧基 - 低级烷基任选被噻吩基环上的卤素原子取代的噻吩基 - 低级烷基，或其中R 1和R 2各自为氢原子，特定酰基，具有基团R xOCO-的苯基 - 低级烷基基团环，或基团 - （A）nB，Rx是特定的有机基团，A是低级亚烷基，n是0或1，B是具有1〜4个杂原子的5或6元不饱和杂环基，选自N，O和S且任选具有苯环的原子，萘环或与其缩合的吡啶环，条件是R1和R2不同时为氢原子或特定酰基; 一个制备它的过程; 以及包含其作为有效成分的抗癌组合物。

6. 发明授权

US4652570A 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：US4652570A
公开(公告)日：1987-03-24
申请号：US645165
申请日：1984-08-28
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 treating cancers sensitive to 5-fluorouracil therapy in warm-blooded animals, comprising 5-fluorouracil and uracil.
摘要翻译：一种用于治疗温血动物中对5-氟尿嘧啶治疗敏感的癌症的抗癌组合物，其包含5-氟尿嘧啶和尿嘧啶。

7. 发明授权

US4570006A Amidine compound, process for producing same and anti-complement agent comprising same 失效
标题翻译：脒化合物，其制备方法和包含其的抗补体剂
公开(公告)号：US4570006A
公开(公告)日：1986-02-11
申请号：US664261
申请日：1984-10-24
申请人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Yojiro Sakurai , Shigeki Nunomura , Toshiyuki Okutome
发明人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Yojiro Sakurai , Shigeki Nunomura , Toshiyuki Okutome
IPC分类号： A61K31/155 , A61K31/215 , A61K31/24 , C07C45/54 , C07C271/06 , C07C271/22 , C07C279/18 , C07C335/22 , C07D317/68 , C07C119/00 , A61K31/22 , A61K31/235
CPC分类号： C07C255/00 , C07C271/22 , C07C279/18 , C07C335/22 , C07C45/54 , C07D317/68
摘要： Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsine, anti-plasmin, anti-kallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof. ##STR2##
摘要翻译：由式（I）表示的脒基化合物及其药学上可接受的酸加成盐是新型化合物，可用作强抗胰蛋白酶，抗纤溶酶，抗激肽释放酶和抗凝血酶剂。具有强大的抗Cl（Cl＆upbar＆r，Cl＆upbar＆s）活性和抗补体活性，它们也可用作抗补体剂。这些脒基化合物通过通式（II）R 1 -COOH（II）表示的羧酸化合物与脒基苯酚化合物（III）的酯化反应制备，如果需要，可以将其转化为其药学上可接受的酸加成盐。（三）

8. 发明授权

US4532255A Amidine compounds and anticomplement agent comprising same 失效
标题翻译：脒化合物和包含其的抗补体剂
公开(公告)号：US4532255A
公开(公告)日：1985-07-30
申请号：US572269
申请日：1984-01-20
申请人： Setsuro Fujii , Toshiyuki Okutome , Toyoo Nakayama , Takashi Yaegashi , Masateru Kurumi
发明人： Setsuro Fujii , Toshiyuki Okutome , Toyoo Nakayama , Takashi Yaegashi , Masateru Kurumi
IPC分类号： C07C249/02 , A61K31/155 , C07C257/18 , C07C279/18 , C07D317/68 , C07C101/00 , A61K31/34 , C07C101/48
CPC分类号： C07D317/68 , C07C279/18
摘要： Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.

9. 发明授权

US4514416A Amidine compound, process for producing same and anti-complement agent comprising same 失效
标题翻译：脒化合物，其制备方法和包含其的抗补体剂
公开(公告)号：US4514416A
公开(公告)日：1985-04-30
申请号：US611937
申请日：1984-05-21
申请人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Yojiro Sakurai , Shigeki Nunomura , Toshiyuki Okutome
发明人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Yojiro Sakurai , Shigeki Nunomura , Toshiyuki Okutome
IPC分类号： A61K31/155 , A61K31/215 , A61K31/24 , C07C45/54 , C07C271/06 , C07C271/22 , C07C279/18 , C07C335/22 , C07D317/68 , C07C119/00 , A61K31/22 , A61K31/235
CPC分类号： C07C255/00 , C07C271/22 , C07C279/18 , C07C335/22 , C07C45/54 , C07D317/68
摘要： Amidino compounds represented by the formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof. ##STR2##
摘要翻译：由式（I）表示的脒基化合物及其药学上可接受的酸加成盐是新的化合物，可用作强效的抗胰蛋白酶，抗血纤维蛋白酶，抗激肽释放酶和抗凝血酶剂。具有强大的抗Cl（Cl＆upbar＆r，Cl＆upbar＆s）活性和抗补体活性，它们也可用作抗补体剂。这些脒基化合物通过通式（II）R 1 -COOH（II）表示的羧酸化合物与脒基苯酚化合物（III）的酯化反应制备，如果需要，可以将其转化为其药学上可接受的酸加成盐。（三）

10. 发明授权

US4452813A Sulfonate derivatives, process for preparing same and antilipemic compositions containing the derivative 失效
标题翻译：磺酸衍生物，其制备方法和含有衍生物的抗血小板组合物
公开(公告)号：US4452813A
公开(公告)日：1984-06-05
申请号：US377074
申请日：1982-05-11
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 , C07C45/63 , C07C45/64 , C07C45/78 , C07C62/24 , C07C245/14 , C07C303/00 , C07C309/65 , C07C143/68
CPC分类号： C07C245/14 , C07C309/00 , C07C45/63 , C07C45/64 , C07C45/78 , C07C62/24
摘要： A sulfonate derivative represented by the formula ##STR1## wherein R.sub.1 is lower alkyl, lower alkoxy or halogen, l is an integer of from 0 to 3, n is 0 or 1, A is straight-chain or branched-chain alkylene having 1 to 4 carbon atoms, and R.sub.2 is hydrogen or lower alkyl but, when n is 0 or 1 and A is straight-chain alkylene with 1 to 4 carbon atoms, is not hydrogen and the method for preparing the same.
摘要翻译：式中，R 1为低级烷基，低级烷氧基或卤素，l为0〜3的整数，n为0或1的磺酸酯衍生物，A为直链或支链的亚烷基，具有1〜 4个碳原子，R2为氢或低级烷基，但当n为0或1且A为具有1至4个碳原子的直链亚烷基时，不是氢及其制备方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式