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1. 发明授权

US5952504A 4-amino-3-acylnaphthyridine derivatives 失效
标题翻译： 4-氨基-3-酰基萘啶衍生物
公开(公告)号：US5952504A
公开(公告)日：1999-09-14
申请号：US849740
申请日：1997-07-03
申请人： Han Yong Yoo , Kae Jong Chung , Man Sik Chang , Sung Gyu Kim , Wahn Soo Choi , Dae Pil Kang , Young Hun Kim , Jang Hoon Paek , Sang Kwon Sohn , Bog Goo Kang , Young Heui Kim , Kwi Hyon Seo
发明人： Han Yong Yoo , Kae Jong Chung , Man Sik Chang , Sung Gyu Kim , Wahn Soo Choi , Dae Pil Kang , Young Hun Kim , Jang Hoon Paek , Sang Kwon Sohn , Bog Goo Kang , Young Heui Kim , Kwi Hyon Seo
IPC分类号： A61K31/435 , A61K31/4375 , A61P1/04 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Novel 4-amino-3-acylnaphthyridine derivatives represented by formula (I), wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 lower alkyl group, C.sub.1 -C.sub.6 lower alkoxy group, C.sub.1 -C.sub.6 lower alkoxyalkyl group, C.sub.3 -C.sub.6 cycloalkyl group, C.sub.3 -C.sub.6 cycloalkyl C.sub.1 -C.sub.6 alkyl group, a or phenyl group which maybe substituted with C.sub.1 -C.sub.6 alkyl group; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 lower alkyl group, C.sub.1 -C.sub.6 alkoxy group, C.sub.1 -C.sub.6 alkylthio group, or a group of the formula: NR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7, identical to or different from each other, are independently hydrogen or C.sub.1 -C.sub.6 lower alkyl group, or R.sub.6 and R.sub.7 may form together 5-membered or 6-membered cycloalkyl group; R.sub.3 is hydrogen, C.sub.1 -C.sub.6 lower alkyl group, C.sub.1 -C.sub.6 alkoxy group, C.sub.1 -C.sub.6 alkylthio group, an amino group substituted with one or two C.sub.1 -C.sub.6 alkyl groups, halogen, cyano group, C.sub.1 -C.sub.6 alkanoyl group, or trifluoromethyl group; R.sub.4 is hydrogen or a substituted or unsubstituted C.sub.1 -C.sub.6 alkyl group; R.sub.5 is hydrogen atom, C.sub.1 -C.sub.6 lower alkyl group, C.sub.1 -C.sub.6 alkoxy group, amino group substituted with one or two C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkylthio group, halogen, cyano group, hydroxycarbamoyl group, carboxy group, a C.sub.1 -C.sub.6 alkanoyl group, or trifluoromethyl group, or alkyl group which forms together with R.sub.4 a 5-membered or 6-membered cycloalkyl group; m is an integer from 0 to 4, inclusive; and n is an integer from 1 to 3 inclusive; with the proviso that all alkyl and alkoxy groups may be linear or branched, and said halogen means fluorine, chlorine or bromine atom, or a pharmaceutically acceptable salt therefore. These compounds show excellent anti-ulcer activity.
摘要翻译： PCT No.PCT / KR96 / 00080 Sec。 371日期1997年7月3日 102（e）日期1997年7月3日PCT PCT 1996年6月1日PCT公布。公开号WO97 / 03074 日期1997年1月30日由式（I）表示的新型4-氨基-3-酰基萘啶衍生物，其中R1为氢，C1-C6低级烷基，C1-C6低级烷氧基，C1-C6低级烷氧基烷基，C3-C6 环烷基，C3-C6环烷基C1-C6烷基，或可被C1-C6烷基取代的苯基; R 2是氢，C 1 -C 6低级烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基或下式的基团：NR 6 R 7其中R 6和R 7彼此相同或不同，独立地为氢或C1- C6低级烷基，或R6和R7可以一起形成5元或6元环烷基; R3是氢，C1-C6低级烷基，C1-C6烷氧基，C1-C6烷硫基，被一个或两个C1-C6烷基取代的氨基，卤素，氰基，C1-C6烷酰基或三氟甲基组; R4是氢或取代或未取代的C1-C6烷基; R5是氢原子，C1-C6低级烷基，C1-C6烷氧基，被一个或两个C1-C6烷基取代的氨基，C1-C6烷硫基，卤素，氰基，羟基氨基甲酰基，羧基，C1 -C 6烷酰基或三氟甲基，或与R 4一起形成5元或6元环烷基的烷基; m为0〜4的整数，包括0和4; n为1〜3的整数，条件是所有烷基和烷氧基可以是直链或支链的，并且所述卤素是指氟，氯或溴原子，或其药学上可接受的盐。这些化合物显示出优异的抗溃疡活性。

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