Substituted 1,5-dihydropyrrol-2-on derivatives as NMDA receptor antagonists for treatment of painThe invention relates to substituted 1,5-dihydropyrrol-2-on derivatives of general formula (I), to a method for the preparation thereof, drugs containing said compounds and to the use of said derivatives for the production of drugs.1 of the replacement of general formula i, 5-pyrrolin-2-ketone derivatives whereinx represents o, s or nr 7, r 1represent h, or 11, sr 11, cor 8, csr 8, nr 9r 10, coor 8, conr 9r 10, csnr 9r 10, cocor 8, c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, r 2, r 3identical or different, and represent h, f, cl, br, cf 3, or 11, sr 11, nr 9r 10, c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, r 4represent h, oh, or 11, sr 11, cor 8, coor 8, cocor 8, conr 9r 10, csnr 9r 10, c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, r 5, r 6identical or different, and represent h, o, oh, or 11, sr 11, cor 8, csr 8, coor 8, cocor 8, conr 9r 10, csnr 9r 10, c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, perhaps r 5and r 6represent group=o together, r 7represent h, or 11, sr 11, cor 8, coor 8, cocor 8, conr 9r 10, csnr 9r 10, c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, r 8represent h, or 11, sr 11, nr 9r 10, c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, r 9represent c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, r 10represent c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, r 11represent c 1-10-alkyl, aryl or heteroaryl, or representative is via c 1-6the aryl of-alkylidene group bonding, described compound of formula i is the form of racemic modification, enantiomorph, diastereomer or corresponding alkali or corresponding physiological acceptable salt,wherein do not comprise following racemic modification:1-methyl-3-acetylaminohydroxyphenylarsonic acid 5-oxyethyl group methylene radical tetramic acid,3-acetylaminohydroxyphenylarsonic acid 5-oxyethyl group methylene radical tetramic acid,α-acetylamino-γ-benzylthio-methylene radical tetramic acid,n-[2,5-dihydro-2-oxo--4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] ethanamide,n-[2,5-dihydro-2-oxo--1-(phenyl methyl)-4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] ethanamide,n-[2,5-dihydro-2-oxo--1-(phenyl methyl)-4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] benzamide,n-[2,5-dihydro-1-methyl-2-oxo-4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] ethanamide,n-[2,5-dihydro-1-methyl-2-oxo-4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] propionic acid amide,with following geometrical isomer:(e)-n-[2,5-dihydro-1-methyl-2-oxo-4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] ethanamide,(z)-n-[2,5-dihydro-1-methyl-2-oxo-4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] ethanamide,(e)-n-[2,5-dihydro-1-methyl-2-oxo-4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] propionic acid amide and(z)-n-[2,5-dihydro-1-methyl-2-oxo-4-[(phenyl methyl) sulfenyl]-the 5-[[(phenyl methyl) sulfenyl] methylene radical]-1h-pyrroles-3-yl] propionic acid amide.
통증 치료용 ＮＭＤＡ 수용체 길항제로서의 치환된1,5-디하이드로피롤-2-온 유도체본 발명은 화학식 I의 치환된 1,5-디하이드로피롤-2-온 유도체, 이의 제조방법, 이를 함유하는 약제 및 약제를 제조하기 위한 이의 용도에 관한 것이다. 화학식 I  화학식 I의 치환된 1,5-디하이드로피롤-2-온 유도체, 이의 라세미체, 이의 거울상이성체, 이의 부분입체이성체, 상응하는 염기 또는 상응하는 생리학적으로 허용되는 염. 화학식 I [이미지] 위의 화학식 I에서, X는 O, S 또는 NR7이고, 라디칼 R1은 H, OR11, SR11, COR8, CSR8, NR9 R10, COOR8, CONR9R10, CSNR9R10, COCOR8, C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이고, 라디칼 R2 및 R3은 동일하거나 상이하고 H, F, Cl, Br, CF3, OR11 , SR11, NR9NR10, C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이고, 라디칼 R4는 H, OH, OR11, SR11, COR8, COOR8, COCOR 8, CONR9R10, CSNR9R10, C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이고, 라디칼 R5 및 R6은 동일하거나 상이하고 H, O, OH, OR11, SR11, COR8, CSR8, COOR8, COCOR8, CONR9R10, CSNR9R10, C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이거나, 라디칼 R5와 R6은 함께 그룹 =O이고, 라디칼 R7은 H, OR11, SR11, COR8, COOR8, COCOR 8, CONR9R10, CSNR9R10, C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이고, 라디칼 R8은 H, OR11, SR11, NR9R10, C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이고, 라디칼 R9는 C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이고, 라디칼 R10은 C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이고, 라디칼 R11은 C1-10 알킬, 아릴 또는 헤테로아릴 라디칼이거나, C1-6 알킬렌 그룹을 통해서 결합된 아릴 라디칼이고, 단, 다음 화합물들은 제외된다: 1-메틸-3-아세트아미노-5-에톡시메틸렌테트람산의 라세미체, 3-아세트아미노-5-에톡시메틸렌테트람산의 라세미체, α-아세틸아미노-γ-벤질티오메틸렌테트람산의 라세미체, N-[2,5-디하이드로-2-옥소-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 아세트아미드의 라세미체, N-[2,5-디하이드로-2-옥소-1-(페닐메틸)-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 아세트아미드의 라세미체, N-[2,5-디하이드로-2-옥소-1-(페닐메틸)-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 벤즈아미드의 라세미체, N-[2,5-디하이드로-1-메틸-2-옥소-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 아세트아미드의 라세미체, N-[2,5-디하이드로-1-메틸-2-옥소-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 프로판아미드의 라세미체, N-[2,5-디하이드로-1-메틸-2-옥소-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 아세트아미드의 (E)-기하이성체, N-[2,5-디하이드로-1-메틸-2-옥소-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 아세트아미드의 (Z)-기하이성체, N-[2,5-디하이드로-1-메틸-2-옥소-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 프로판아미드의 (E)-기하이성체 및 N-[2,5-디하이드로-1-메틸-2-옥소-4-[(페닐메틸)티오]-5-[[(페닐메틸)티오]메틸렌]-1H-피롤-3-일]의 프로판아미드의 (Z)-기하이성체.