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1. 发明申请

WO1997003076A1 HETEROCYCLE-FUSED THIAZOLE DERIVATIVES 审中-公开
标题翻译：杂交 - 热熔化的噻唑衍生物
公开(公告)号：WO1997003076A1
公开(公告)日：1997-01-30
申请号：PCT/KR1996000082
申请日：1996-06-01
申请人： YUNGJIN PHARMACEUTICAL CO., LTD. , YOO, Han, Yong , CHUNG, Kae, Jong , CHAI, Jun, Pyo , CHANG, Man, Sik , KIM, Sung, Gyu , CHOI, Wahn, Soo , KIM, Young, Hun , CHUN, Jae, Kwang , CHUNG, Young, Kuk , KIM, Young, Heui , PAEK, Jang, Hoon , SEO, Kwi, Hyon , KANG, Dae, Pil
发明人： YUNGJIN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D513/04
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 C1-C6 lower alkyl group, a C1-C4 lower alkoxy group, phenyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, fluorine, chlorine, bromine and an amino group, a C1-C5 alkylphenyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, fluorine, chlorine, bromine and an amino group, a substituted or unsubstituted guanidino group, or an amino group having a general formula: NR3R4 in which R3 and R4, identical to or different from each other, represent independently a hydrogen atom, a C1-C6 lower alkyl group, a C3-C6 cycloalkyl group, a substituted or unsubstituted pyridyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, a halogen atom, an amino group, a cyano group and a nitro group, a piperidine group or C1-C4 alkylpiperidine group; R1 and R2, identical to or different from each other, are independently a hydrogen atom, a hydroxy group, a C1-C6 lower alkyl group, phenyl group, a phenyl group having one substituent selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, a halogen atom, a nitro and a cyano group, a C1-C5 alkylphenyl group, or a pyridine group; R5, R6, R7 and R8, identical to or different from each other, are independently a hydrogen atom, a hydroxy group, a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, phenyl group, or a phenyl group substituted with a C1-C4 alkyl group, a C1-C4 alkoxy group or a halogen atom, or a C1-C3 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.
摘要翻译：由通式（I）表示的噻唑化合物，其中R是氢原子，羟基，直链或支链C 1 -C 6低级烷基，C 1 -C 4低级烷氧基，苯基，具有1至3个选自C1-C4低级烷基，C1-C4低级烷氧基，氟，氯，溴和氨基的取代基，C1-C5烷基苯基，具有1〜3个选自由C1-C4低级烷基，C1-C4低级烷氧基，氟，氯，溴和氨基组成的基团，取代或未取代的胍基，或具有通式NR 3 R 4的氨基，其中R 3 和R 4彼此相同或不同，分别独立地表示氢原子，C1-C6低级烷基，C3-C6环烷基，取代或未取代的吡啶基，具有1〜3个选自由C1-C4低级烷基组成的组 C1-C4低级烷氧基，卤素原子，氨基，氰基和硝基，哌啶基或C1-C4烷基哌啶基; R1和R2彼此相同或不同，独立地为氢原子，羟基，C1-C6低级烷基，苯基，具有一个取代基的苯基，所述取代基选自C1-C4低级烷基，C1-C4低级烷氧基，卤素原子，硝基和氰基，C1-C5烷基苯基或吡啶基; R5，R6，R7和R8彼此相同或不同，独立地为氢原子，羟基，C1-C4低级烷基，C1-C4低级烷氧基，苯基或苯基取代 C1-C4烷基，C1-C4烷氧基或卤原子，或C1-C3烷基苯基; Het是3-，4-或5-元不饱和单环基团，或6至12元不饱和稠合环基团，所述单环和稠环基团由一个或多个选自氧，氧化氮和氧化氮的杂原子组成硫原子。这些化合物显示出优异的抗溃疡活性。

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