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公开(公告)号:US5547978A
公开(公告)日:1996-08-20
申请号:US346240
申请日:1994-11-23
申请人: Burton G. Christensen , Takashi Egawa , Yasuyuki Ichimaru , Shokichi Ohuchi , Tsuneo Okonogi , Arthur A. Patchett , Seiji Shibahara , Seiji Tsutsumni
发明人: Burton G. Christensen , Takashi Egawa , Yasuyuki Ichimaru , Shokichi Ohuchi , Tsuneo Okonogi , Arthur A. Patchett , Seiji Shibahara , Seiji Tsutsumni
IPC分类号: A61K31/40 , A61K31/401 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/505 , A61P25/00 , A61P25/28 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04 , C07D207/06 , C07D209/08 , C07D277/06
CPC分类号: C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: The invention relates to derivatives of pyrrolidin-2-ylcarbonylheterocyclic compound of the general formula ##STR1## in which R.sup.1 represents C.sub.1-6 alkyl, C.sub.1-20 cycloalkyl, aryl or heteroaryl,R.sup.2 represents a heterocyclic compound selected from the group consisting of 2-thiazole, 2-oxazole, 2-imidazole, 2-pyrrole, 2-thiophene, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 2-indole, 2-thiazolo[5,4-b]pyridine, 2-oxazolo[4,5-b]pyridine, 2-imidazo[4,5-b]pyridine, 5-thiazole, 2-thiazoline, 2-pyridine, 3-pyridine, 5-pyrimidine, 2-pyrazine, 2-triazole or 2-pyrazole wherein the heterocyclic compound may be unsubstituted or substituted independently with R.sup.4 or R.sup.5 wherein R.sup.4 and R.sup.5 are H, C.sub.1-5 alkyl, aryl or R.sup.4 and R.sup.5 may be ortho substituents on the heterocyclic compounds and connected to form an aryl or heteroaryl ring,A represents a cyclic amino acid, X is oxygen atom, thiomethlene or methylene residue, m is an integer from 1 to 5, to a process for the preparation thereof, to composition containing them, and to the use thereof.
摘要翻译: 本发明涉及通式“IMAGE”的吡咯烷-2-基羰基杂环化合物的衍生物,其中R 1表示C 1-6烷基,C 1-20的环烷基,芳基或杂芳基,R 2表示选自下列的杂环化合物:2- 噻唑,2-恶唑,2-咪唑,2-吡咯,2-噻吩,2-苯并噻唑,2-苯并恶唑,2-苯并咪唑,2-吲哚,2-噻唑并[5,4-b]吡啶,2-恶唑并[ 4,5-b]吡啶,2-咪唑并[4,5-b]吡啶,5-噻唑,2-噻唑啉,2-吡啶,3-吡啶,5-嘧啶,2-吡嗪,2-三唑或2- 吡唑,其中杂环化合物可以是未取代的或独立地被R4或R5取代,其中R4和R5是H,C1-5烷基,芳基或R4和R5可以是杂环化合物上的邻位取代基并且连接形成芳基或杂芳基环, A表示环状氨基酸,X为氧原子,巯基或亚甲基残基,m为1〜5的整数,其制备方法为组合物cont 指导他们,以及使用它们。