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1. 发明授权

US5292758A Sulfonamide derivatives 失效
标题翻译：磺酰胺衍生物
公开(公告)号：US5292758A
公开(公告)日：1994-03-08
申请号：US923345
申请日：1992-07-31
申请人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
IPC分类号： C07C311/48 , A61K31/18 , A61P35/00 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/74 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D239/69 , C07D307/68 , C07D333/38 , C07F9/58 , C07H15/203 , C07H15/26 , A61K31/44
CPC分类号： C07D213/74 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D307/68 , C07D333/38 , C07F9/588 , C07H15/203 , C07H15/26
摘要： Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptance salts of them, have an excellent antitumor activity.
摘要翻译：通式（I）的磺酰胺衍生物：其中优选R 1表示低级烷氧基，R 2，R 3，R 4，R 5，R 6和R 7可以彼此相同或不同，并且各自表示氢原子，卤原子或低级烷基，A和B可以相同或不同，并且各自表示= N-或= CH-，E表示可具有1或2个氮原子的芳族6元环基并且被1〜3个可以相同或不同的取代基取代，条件是可以被保护的是氢原子，低级烷基，硝基或氨基的R 1的组合， R 2和R 3各自为氢原子，A和B各自为CH-，E为可被1至3个彼此可相同或不同的取代基G所取代的苯基，不包括或它们的药理学接受盐具有优异的抗肿瘤活性。

2. 发明授权

US5610304A Pyrimidinyl or pyridinyl sulfonamide substituted compounds 失效
标题翻译：嘧啶基或吡啶基磺酰胺取代的化合物
公开(公告)号：US5610304A
公开(公告)日：1997-03-11
申请号：US453058
申请日：1995-05-26
申请人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
IPC分类号： C07C311/48 , A61K31/18 , A61P35/00 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/74 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D239/69 , C07D307/68 , C07D333/38 , C07F9/58 , C07H15/203 , C07H15/26 , C07D239/02 , C07D213/02
CPC分类号： C07D213/74 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D307/68 , C07D333/38 , C07F9/588 , C07H15/203 , C07H15/26
摘要： Sulfonamide compounds of formula (I) or a pharmacologically acceptable salt thereof: ##STR1## exhibit excellent antitumor activity and low toxicity.
摘要翻译：式（I）的磺酰胺化合物或其药理学上可接受的盐：表现出优异的抗肿瘤活性和低毒性。

3. 发明授权

US5434172A Sulfonamide derivatives 失效
标题翻译：磺酰胺衍生物
公开(公告)号：US5434172A
公开(公告)日：1995-07-18
申请号：US231272
申请日：1994-04-22
申请人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
IPC分类号： C07C311/48 , A61K31/18 , A61P35/00 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/74 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D239/69 , C07D307/68 , C07D333/38 , C07F9/58 , C07H15/203 , C07H15/26 , A61K31/44 , C07D213/02
CPC分类号： C07D213/74 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D307/68 , C07D333/38 , C07F9/588 , C07H15/203 , C07H15/26
摘要： Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded,or pharmacologically acceptance salts of them, have an excellent antitumo-activity.
摘要翻译：通式（I）的磺酰胺衍生物：其中优选R 1表示低级烷氧基，R 2，R 3，R 4，R 5，R 6和R 7可以彼此相同或不同，并且各自表示氢原子，卤原子或低级烷基，A和B可以相同或不同，并且各自表示= N-或= CH-，E表示可具有1或2个氮原子的芳族6元环基并且被1〜3个可以相同或不同的取代基取代，条件是可以被保护的是氢原子，低级烷基，硝基或氨基的R 1的组合， R 2和R 3各自为氢原子，A和B各自为CH-，E为可被1至3个彼此可相同或不同的取代基G所取代的苯基，不包括或它们的药理学接受盐具有优异的防虫活性。

4. 发明授权

US5332751A Pyridine carboxamide compounds which have useful as pharmaceutical utility 失效
标题翻译：可用作药物效用的吡啶甲酰胺化合物
公开(公告)号：US5332751A
公开(公告)日：1994-07-26
申请号：US85962
申请日：1993-06-30
申请人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
IPC分类号： C07C311/48 , A61K31/18 , A61P35/00 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/74 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D239/69 , C07D307/68 , C07D333/38 , C07F9/58 , C07H15/203 , C07H15/26 , C07D213/02 , A61K31/44
CPC分类号： C07D213/74 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D307/68 , C07D333/38 , C07F9/588 , C07H15/203 , C07H15/26
摘要： Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded,or pharmacologically acceptable salts of them, have an excellent antitumor activity.
摘要翻译：通式（I）的磺酰胺衍生物：其中优选R 1表示低级烷氧基，R 2，R 3，R 4，R 5，R 6和R 7可以彼此相同或不同，并且各自表示氢原子，卤原子或低级烷基，A和B可以相同或不同，并且各自表示= N-或= CH-，E表示可具有1或2个氮原子的芳族6元环基并且被1〜3个可以相同或不同的取代基取代，条件是可以被保护的是氢原子，低级烷基，硝基或氨基的R 1的组合， R 2和R 3各自为氢原子，A和B各自为CH-，E为可被1至3个彼此可相同或不同的取代基G所取代的苯基，不包括或其药理学上可接受的盐具有优异的抗肿瘤活性。

5. 发明授权

US5250549A Sulfonamide derivatives 失效
标题翻译：磺酰胺衍生物
公开(公告)号：US5250549A
公开(公告)日：1993-10-05
申请号：US742618
申请日：1991-08-08
申请人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Hiroyuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
IPC分类号： C07C311/48 , A61K31/18 , A61P35/00 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/74 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D239/69 , C07D307/68 , C07D333/38 , C07F9/58 , C07H15/203 , C07H15/26 , C07D213/75 , A61K31/44
CPC分类号： C07D213/74 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D307/68 , C07D333/38 , C07F9/588 , C07H15/203 , C07H15/26
摘要： Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the specification, A and B may be the same or different from each other and each represents .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and may be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptance salts of them.

6. 发明授权

US5610320A Sulfonamide phenyl substituted compounds 失效
标题翻译：磺酰胺苯基取代的化合物
公开(公告)号：US5610320A
公开(公告)日：1997-03-11
申请号：US450138
申请日：1995-05-26
申请人： Hiroshi Yoshino , Norihiro Ueda , Hirovuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Hirovuki Sugumi , Jun Niijima , Yoshihiko Kotake , Toshimi Okada , Nozomu Koyanagi , Tatsuo Watanabe , Makoto Asada , Kentaro Yoshimatsu , Atsumi Iijima , Takeshi Nagasu , Kappei Tsukahara , Kyosuke Kitoh
IPC分类号： C07C311/48 , A61K31/18 , A61P35/00 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/74 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D239/69 , C07D307/68 , C07D333/38 , C07F9/58 , C07H15/203 , C07H15/26 , C07D307/02 , C07D333/02 , C07C311/15
CPC分类号： C07D213/74 , C07C311/21 , C07C311/29 , C07C311/44 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/42 , C07D239/48 , C07D239/50 , C07D307/68 , C07D333/38 , C07F9/588 , C07H15/203 , C07H15/26
摘要： Sulfonamide compounds of the formula or pharmacologically acceptable salts thereof: ##STR1## wherein: R.sup.1 is a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, hydroxyl group, nitro group, phenoxy group, cyano group, acetyl group, amino group or a protected amino group; R.sup.2 and R.sup.3 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group; R.sup.4 and R.sup.7 may be the same or different from each other and each is a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkoxy group, amino group or amino group substituted with a lower alkyl or a phenyl group; A is .dbd.CH--; B is .dbd.CH--; and E is selected from the group consisting of ##STR2## in which Q is an oxygen atom or a sulfur atom; and R.sup.11 is a hydrogen atom, a lower alkyl group, an amino group which may be substituted with a lower alkyl group, a lower alkoxy group, a 2-thienyl group, a 2-furyl group, phenyl group or a phenyl group having from 1 to 3 substituents, said substituents being the same or different from one another and selected from the group consisting of a halogen atom, lower alkyl group, lower alkoxy group, hydroxyl group, carboxyl group, esterified carboxyl group, amidated carboxyl group, lower alkylthio group and phenoxy group; and (b) a phenyl group or a phenyl group having from 1 to 3 substituents.
摘要翻译：下式的磺酰胺化合物或其药理学上可接受的盐：其中：R1是氢原子，卤素原子，低级烷基，低级烷氧基，羟基，硝基，苯氧基，氰基，乙酰基，氨基或被保护的氨基; R2和R3可以相同或不同，各自为氢原子，卤素原子，低级烷基或低级烷氧基; R 4和R 7可以相同或不同，各自为氢原子或低级烷基; R5和R6可以相同或不同，分别为氢原子，卤素原子，低级烷氧基，氨基或被低级烷基或苯基取代的氨基; A = CH-; B为= CH-; 并且E选自其中Q是氧原子或硫原子的组; R 11为氢原子，低级烷基，可被低级烷基，低级烷氧基，2-噻吩基，2-呋喃基，苯基或苯基取代的氨基， 1至3个取代基，所述取代基彼此相同或不同，并且选自卤素原子，低级烷基，低级烷氧基，羟基，羧基，酯化羧基，酰胺化羧基，低级烷硫基组和苯氧基; 和（b）苯基或具有1至3个取代基的苯基。

7. 发明授权

US5846969A Tricyclic heterocyclic sulfonamide and sulfonic ester derivatives 失效
标题翻译：三环杂环磺酰胺和磺酸酯衍生物
公开(公告)号：US5846969A
公开(公告)日：1998-12-08
申请号：US873033
申请日：1997-06-11
申请人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
IPC分类号： C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/04 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D498/04 , C07D513/04 , C07F7/18 , A61K31/55 , A61K31/505 , C07D487/00 , C07D471/00
CPC分类号： C07D219/04 , C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D513/04 , C07F7/1856
摘要： A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).
摘要翻译：（I）表示的磺酰胺衍生物或磺酸酯衍生物：（I）{G表示芳香族5-或6-元环; L表示O或-N（R 1） - （R 1表示氢或低级烷基）; （D）环A和B各自表示不饱和的5-或6-元环; Y表示O，S（O）n，C（R3）（R4），C（O），N（R5），CH（R6）CH（R7），C（R8）= C（R9））C（O），N = C（R 11），OCH（R 12），S（O）n CH（R 13）或N（R 14）CH（R 15）。

8. 发明授权

US5854274A Tricyclic heterocyclic sulfonamide and sulfonic ester derivatives 失效
标题翻译：三环杂环磺酰胺和磺酸酯衍生物
公开(公告)号：US5854274A
公开(公告)日：1998-12-29
申请号：US760738
申请日：1996-12-05
申请人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
IPC分类号： C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/04 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D498/04 , C07D513/04 , C07F7/18 , A61K31/44 , A61K31/40 , C07D221/06 , C07D209/82
CPC分类号： C07D219/04 , C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D513/04 , C07F7/1856
摘要： Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have excellent antitumor activity and are represented by the following general formula (I) and processes for producing the same are provided. The present sulfonamide derivatives or a sulfonic ester derivatives are represented by the following general formula (I): ##STR1## wherein G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- and --R.sup.1 represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from among the following; ##STR2## rings A and B each represent an unsaturated 5- or 5 -membered ring; X represents N(R.sup.2) wherein R.sup.2 represents hydrogen or lower alkyl, or NHCO; Y represents 0, S(O).sub.n, C(R.sup.3) (R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10) C(O), N.dbd.CR.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.16); and n represents 0, 1 or 2, R.sup.3 to R.sub.13, R.sup.15 and R.sup.16 each represent hydrogen or lower alkyl, and R.sup.14 represents hydrogen, lower alkyl or lower acyl.
摘要翻译：提供具有优异抗肿瘤活性并由以下通式（I）表示的新型三环杂环磺酰胺衍生物和磺酸酯衍生物及其制备方法。本发明的磺酰胺衍生物或磺酸酯衍生物由以下通式（I）表示：其中G表示芳族5-或6-元环; L表示0或-N（R1） - ，-R1表示氢或低级烷基; M表示选自以下的三环结构：（a）（b）（c）（d）（e）（f）环A和B各自表示不饱和5-或5- 环; X表示N（R2），其中R2表示氢或低级烷基或NHCO; Y表示0，S（O）n，C（R3）（R4），C（O），N（R5），CH（R6）CH（R7），C（R8）= C（R9））C（O），N = CR 11），OCH（R 12），S（O）n CH（R 13）或N（R 14）CH（R 15）。 Z表示氮或C（R16）; 并且n表示0,1或2，R 3至R 13，R 15和R 16各自表示氢或低级烷基，R 14表示氢，低级烷基或低级酰基。

9. 发明授权

US5834462A Tricyclic heterocyclic sulfonamide and sulfonic ester derivatives 失效
标题翻译：三环杂环磺酰胺和磺酸酯衍生物
公开(公告)号：US5834462A
公开(公告)日：1998-11-10
申请号：US397254
申请日：1995-03-23
申请人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
IPC分类号： C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/04 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D498/04 , C07D513/04 , C07F7/18 , A61K31/40 , A61K31/47
CPC分类号： C07D219/04 , C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D513/04 , C07F7/1856
摘要： Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have each an antitumor action and are represented by the following general formula (I) and processes for producing the same are provided. These compounds have each an excellent antitumor activity. A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alky); and M represents a tricyclic structure selected from among the following ones; ##STR2## �rings A and B represent each an unsaturated 5- or 6-membered ring; X represents N(R.sup.2), (wherein R.sup.2 represents hydrogen or lower alkyl), or NHCO; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.16) (n represents 0, 1 or 2, R.sup.3 to R.sup.13, R.sup.15 and R.sup.16 each represents hydrogen or lower alkyl, and R.sup.14 represents hydrogen, lower alkyl or lowver acyl.)!}
摘要翻译： PCT No.PCT / JP94 / 01231 Sec。 371日期：1995年3月23日 102（e）1995年3月23日PCT PCT 1994年7月26日PCT公布。出版物WO95 / 03279 日期1995年2月2日提供了具有各自抗肿瘤作用并由以下通式（I）表示的三环杂环磺酰胺衍生物和磺酸酯衍生物及其制备方法。这些化合物各具有优异的抗肿瘤活性。由以下通式（I）表示的磺酰胺衍生物或磺酸酯衍生物：元环; L表示0或-N（R1） - （R1表示氢或低级烷基）; M表示选自以下的三环结构：（a）（b） [环A和B各自表示不饱和的5-或6-元环; X表示N（R2），（其中R2表示氢或低级烷基）或NHCO; Y表示O，S（O）n，C（R3）（R4），C（O），N（R5），CH（R6）CH（R7），C（R8）= C（R9））C（O），N = C（R 11），OCH（R 12），S（O）n CH（R 13）或N（R 14）CH（R 15） Z表示氮或C（R16）（n表示0,1或2，R3至R13，R15和R16各自表示氢或低级烷基，R14表示氢，低级烷基或低级酰基）]}

10. 发明授权

US5688800A Condensed pyrimidine derivative 失效
标题翻译：缩合嘧啶衍生物
公开(公告)号：US5688800A
公开(公告)日：1997-11-18
申请号：US413100
申请日：1995-03-29
申请人： Hiroaki Nomura , Toru Haneda , Yoshihiko Kotake , Norihiro Ueda , Kyosuke Kitoh
发明人： Hiroaki Nomura , Toru Haneda , Yoshihiko Kotake , Norihiro Ueda , Kyosuke Kitoh
IPC分类号： C07D239/70 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04 , C07D239/70
摘要： A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a hydroxyl or amino group; R.sup.2 represents a phenylene, pyridinediyl, thiendiyl furandiyl or thlazoldiyl group --CO.sub.2 R.sup.5 and --CO.sub.2 R.sup.6 may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part ##STR2## A represents an oxygen atom, a group represented by the formula: ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different from each other and each represents a hydrogen or halogen atom or a hydrocarbon group which may be substituted, or alternatively R.sup.3 and R.sup.4 may be united to form an alkylidene group which may be substituted) or a group represented by the formula: ##STR4## (wherein R.sup.70 represents a hydrogen atom or a hydrocarbon group), and n is an integer of 1 to 3, provided that the compound in which R.sup.1 represents oxygen, and hydrogen is attached to nitrogen at 3-position is included in the above shown definition, a process for preparation the same, and an antitumor drug containing the same.
摘要翻译：一种具有优异抗肿瘤活性的新型嘧啶衍生物，其由下列通式（I）表示或其药理学上可接受的盐：其中R 1表示羟基或氨基; R2表示亚苯基，吡啶二基，噻二烷基呋喃基或噻唑烷基-CO 2 R 5和-CO 2 R 6可以彼此相同或不同，并且各自表示羧基或羧酸酯，部分 A表示氧原子，由下式表示的基团：彼此不同且各自表示氢或卤素原子或可被取代的烃基，或者R3和R4可以一起形成可被取代的亚烷基）或以下式表示的基团：其中R 70表示氢原子或烃基，n为1〜3的整数，条件是其中R1表示氧，氮与氮连接的化合物为3 位置包括在上述定义中，其制备方法和含有该定义的抗肿瘤药物。

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