公开(公告)号：US6043373A

公开(公告)日：2000-03-28

申请号：US849739

申请日：1997-07-03

申请人： Han Yong Yoo ,  Kae Jong Chung ,  Jun Pyo Chai ,  Man Sik Chang ,  Sung Gyu Kim ,  Wahn Soo Choi ,  Young Hun Kim ,  Jae Kwang Chun ,  Young Kuk Chung ,  Young Heui Kim ,  Jang Hoon Paek ,  Kwi Hyon Seo ,  Dae Pil Kang

发明人： Han Yong Yoo ,  Kae Jong Chung ,  Jun Pyo Chai ,  Man Sik Chang ,  Sung Gyu Kim ,  Wahn Soo Choi ,  Young Hun Kim ,  Jae Kwang Chun ,  Young Kuk Chung ,  Young Heui Kim ,  Jang Hoon Paek ,  Kwi Hyon Seo ,  Dae Pil Kang

IPC分类号： A61K31/425 ,  A61K31/429 ,  A61K31/4439 ,  A61P1/04 ,  A61P43/00 ,  C07D513/04 ,  C07D513/14

CPC分类号： C07D513/04 ,  C07D513/14

摘要： A thiazole compound represented by general formula (I), wherein R is hydrogen atom, a hydroxy group, a straight or branched C.sub.1 -C.sub.6 lower alkyl group, a C.sub.1 -C.sub.4 lower alkoxy group, phenyl group, a phenyl group having one to three substituents selected from a group consisting of a C.sub.1 -C.sub.4 lower alkyl group, a C.sub.1 -C.sub.4 lower alkoxy group, fluorine, chlorine, bromine and an amino group, a C.sub.1 -C.sub.5 alkylphenyl group, a phenyl group having one to three substituents selected from a group consisting of a C.sub.1 -C.sub.4 lower alkyl group, a C.sub.1 -C.sub.4 lower alkoxy group, fluorine, chlorine, bromine and an amino group, a substituted or unsubstituted guanidino group, or an amino group having a general formula: NR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4, identical to or different from each other, represent independently a hydrogen atom, a C.sub.1 -C.sub.6 lower alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group, a substituted or unsubstituted pyridyl group, a phenyl group having one to three substituents selected from a group consisting of a C.sub.1 -C.sub.4 lower alkyl group, a C.sub.1 -C.sub.4 lower alkoxy group, a halogen atom, an amino group, a cyano group and a nitro group, a piperidine group or C.sub.1 -C.sub.4 alkylpiperidine group; R.sub.1 and R.sub.2, identical to or different from each other, are independently a hydrogen atom, a hydroxy group, a C.sub.1 -C.sub.6 lower alkyl group, phenyl group, a phenyl group having one substituent selected from a group consisting of a C.sub.1 -C.sub.4 lower alkyl group, a C.sub.1 -C.sub.4 lower alkoxy group, a halogen atom, a nitro and a cyano group, a C.sub.1 -C.sub.5 alkylphenyl group, or a pyridine group; R.sub.5, R.sub.6, R.sub.7 and R.sub.8, identical to or different from each other, are independently a hydrogen atom, a hydroxy group, a C.sub.1 -C.sub.4 lower alkyl group, a C.sub.1 -C.sub.4 lower alkoxy group, phenyl group, or a phenyl group substituted with a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group or a halogen atom, or a C.sub.1 -C.sub.3 alkylphenyl group; Het is a 3-, 4- or 5-membered unsaturated monocyclic group, or 6- to 12-membered unsaturated fused cyclic group, said monocyclic and fused cyclic group being comprised of one or more hetero atoms selected from oxygen, oxidative nitrogen and oxidative sulfur atom are disclosed. These compounds show excellent anti-ulcer activity. ##STR1##

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。