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1. 发明授权

KR100588222B1 히드록시알킬 인돌로카르바졸 유도체, 제조방법 및 이들을함유하는 약제 조성물 失效
标题翻译：新型羟基间苯二酚衍生物，制备方法和含有其的药物组合物
公开(公告)号：KR100588222B1
公开(公告)日：2006-06-12
申请号：KR1020047005995
申请日：2002-10-21
申请人： 르 라보레또레 쎄르비에르
发明人： 프르드옴므,미첼레 , 마르미논,크리스텔레 , 모레유,파스칼 , 히크만,존 , 피에르,알렝 , 피페이퍼,브루노 , 레나르드,피에르 , 비조트-에스피알드,쟝-가이
IPC分类号： C07H19/23
CPC分类号： C07H19/23
摘要： Compound of formula (I): wherein: R1 and R2 each represents a group selected from hydrogen, alkyl, arylalkyl, hydroxy, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkoxyalkyl, amino and aminoalkyl (optionally substituted), Ra and Rb each represents an alkylene chain, X1, X2 and X3 each represents a group selected from hydroxy, alkoxy, aryloxy, arylalkoxy, alkyl, amino (optionally substituted), halogen, alkylcarbonyloxy and azido, X4 represents a methylidene group or a group of formula -Rc-X1 as defined in the description, their isomers and also their addition salts with a pharmaceutically acceptable acid or base.

2. 发明公开

KR1020040054735A 히드록시알킬 인돌로카르바졸 유도체, 제조방법 및 이들을함유하는 약제 조성물 失效
标题翻译：羟烷基吲哚并咔唑衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：KR1020040054735A
公开(公告)日：2004-06-25
申请号：KR1020047005995
申请日：2002-10-21
申请人： 르 라보레또레 쎄르비에르
发明人： 프르드옴므,미첼레 , 마르미논,크리스텔레 , 모레유,파스칼 , 히크만,존 , 피에르,알렝 , 피페이퍼,브루노 , 레나르드,피에르 , 비조트-에스피알드,쟝-가이
IPC分类号： C07H19/23
CPC分类号： C07H19/23
摘要： 본 발명은 하기 화학식 (I)의 화합물, 이들의 이성질체 및 이들의 약제학적으로 허용되는 산 또는 염기 부가 염에 관한 것이다:

상기 식에서,
R
1 및 R
2 각각은 수소, 알킬, 아릴알킬, 히드록시, 히드록시알킬, 디히드록시알킬, 알콕시, 알콕시알킬, 아미노, 아미노알킬(치환되거나 치환되지 않고)을 나타내고,
Ra 및 Rb 각각은 알킬렌 사슬을 나타내고,
X
1 , X
2 및 X
3 각각은 수소, 알콕시, 아릴옥시, 아릴알콕시, 아미노(치환되거나 치환되지 않음), 할로겐, 알킬카르보닐옥시, 아지도로부터 선택된 기를 나타내고,
X
4 는 상세한 설명에서 정의된 바와 같이, 메틸리덴기 또는 화학식 -Rc-X
1 의 기를 나타낸다. 본 발명은 약제로서 사용된다.

3. 发明授权

KR100433706B1 7-옥소-2,3,7,14-테트라히드로-1Ｈ-벤조[ｂ]피라노[3,2-ｈ]아크리딘 카르복실레이트의 화합물, 이것의 제조 방법 및이를 함유하는 약제 조성물 失效
标题翻译： 7-옥소-2,3,7,14-테트라히드로중벤조[b]피라노[3,2-h]아크리딘카르실레이트의화합물，이것의제조방법및이를함유하는약제조성물
公开(公告)号：KR100433706B1
公开(公告)日：2004-05-31
申请号：KR1020000033220
申请日：2000-06-16
申请人： 르 라보레또레 쎄르비에르
发明人： 코스,미셸 , 틸레껭,프랑스와 , 미셸,실비에 , 아타시,가넴 , 피에르,알렝 , 레나르드,피에르 , 프페이페르,브루노
IPC分类号： C07D491/00
CPC分类号： C07D491/04
摘要： 7-Oxo-2,3,7,14-tetrahydro-1H-benzo(b)pyrano(3,2-h) acridine derivatives (I), their salts with acids and bases, their isomers, N-oxides, their preparation, and pharmaceutical compositions containing them. The new compounds are of formula (I) X and Y = H, halogen, OH, SH, CN, NO2, 1-6C alkyl, alkoxy, or trihaloalkyl, amino (optionally by one or two 1-6C alkyl groups which may be substituted by alkoxy groups or by a group of formula NR7R8) or together form a methylenedioxy or ethylene dioxy group, the groups X and Y being present on either of the two adjacent benzene rings; R7 and R8 = H or 1-6C alkyl, aryl, or aralkyl; R1 = H or 1-6C alkyl; R2 = H, OH, 1-6C alkyl or alkoxy (optionally substituted by NR9R10, or by a 5-7 membered saturated or unsaturated mono- or bicyclic heterocycle having one or two hetero atoms selected from O, N, and S), alkyl carbonyloxy, or amino (optionally substituted by one or two alkyl, aryl, or aralkyl groups, an alkylcarbonyl group that may be substituted by NR7R8, a group -R11-NR9R10, an alkylene group substituted by a heterocycle, or a group -R11-CO-R12; R9 and R10 = H, or 1-6C alkyl or hydroxyalkyl; R11 = 1-6C alkylene; R12 = OH or 1-6C alkoxy; R3 and R4 = H or 1-6C alkyl; one or both of R5 and R6 = a group -O-CO-U-V, and if only one has this meaning the other represents a group Z; U = 1-8C alkylene, optionally substituted by one or more groups selected from aryl, OH, or 1-6C alkoxy; V = COOH, COOR13, OH, 1-6C alkoxy, -NR7R8, -NR7-COOR13, -NR7-CO-R13, -COR13, or CONR7R8; R13 = 1-6C alkyl optionally substituted OH, aryl, or aralkyl; Z = OH, 1-6C alkoxy, alkoxycarbonyl, alkylcarbonyloxy, arylcarbonyloxy, arylalkyl carbonyloxy, or amino optionally substituted by one or two alkyl groups
摘要翻译： 7-氧代-2,3,7,14-四氢-1H-苯并（b）吡喃并（3,2-h）吖啶衍生物（I），它们与酸和碱的盐，它们的异构体，N-氧化物，它们的制备和含有它们的药物组合物。新化合物具有式（I）X和Y = H，卤素，OH，SH，CN，NO 2，1-6C烷基，烷氧基或三卤代烷基，氨基（任选地被一个或两个1-6C烷基被烷氧基取代或被式NR7R8基团取代）或一起形成亚甲基二氧基或亚乙基二氧基，基团X和Y存在于两个相邻苯环中的任一个上; R7和R8 = H或1-6C烷基，芳基或芳烷基; R1 = H或1-6C烷基; R2 = H，OH，1-6C烷基或烷氧基（任选被NR9R10取代，或被具有一个或两个选自O，N和S的杂原子的5-7元饱和或不饱和单环或双环杂环取代），烷基羰基氧基或氨基（任选被一个或两个烷基，芳基或芳烷基取代，可被NR7R8取代的烷基羰基，基团-R11-NR9R10，被杂环取代的亚烷基或基团-R11- CO-R12; R9和R10 = H或1-6C烷基或羟烷基; R11 = 1-6C亚烷基; R12 = OH或1-6C烷氧基; R3和R4 = H或1-6C烷基; R5 和R6 =基团-O-CO-UV，并且如果只有一个具有该含义，则另一个表示基团Z; U = 1-8C亚烷基，任选被一个或多个选自芳基，OH或1-6C 烷氧基; V = COOH，COOR13，OH，1-6C烷氧基，-NR7R8，-NR7-COOR13，-NR7-CO-R13，-COR13或CONR7R8; R13 = 1-6C烷基，任选取代的OH，芳基或芳烷基 ; Z = OH，1-6C烷氧基，烷氧基羰基，烷基羰基氧基，芳基羰基氧基，芳基烷基羰基氧基或任选被一个或两个烷基取代的氨基

4. 发明公开

KR1020010029811A 7-옥소-2,3,7,14-테트라히드로-1Ｈ-벤조[ｂ]피라노[3,2-ｈ]아크리딘 카르복실레이트의 화합물, 이것의 제조 방법 및이를 함유하는 약제 조성물 失效
标题翻译： 7-OXO-2,3,7,14-四氢-1H-苯并（B）吡喃（3,2-H）吡啶羧酸酯化合物，其制备方法和含有该化合物的药物组合物
公开(公告)号：KR1020010029811A
公开(公告)日：2001-04-16
申请号：KR1020000033220
申请日：2000-06-16
申请人： 르 라보레또레 쎄르비에르
发明人： 코스,미셸 , 틸레껭,프랑스와 , 미셸,실비에 , 아타시,가넴 , 피에르,알렝 , 레나르드,피에르 , 프페이페르,브루노
IPC分类号： C07D491/00
CPC分类号： C07D491/04
摘要： PURPOSE: A 7-oxo-2,3,7,14-tetrahydro- 1H-benzo(b)pyrano (3,2-h) acridine carboxylate compound, its producing method and a pharmaceutical composition containing the same are provided, which compound has improved anticancer activity. CONSTITUTION: The 7-oxo-2,3,7,14-tetrahydro- 1H-benzo(b)pyrano (3,2-h) acridine carboxylate compound represented by formula(I), its isomers, N-oxide and pharmaceutically acceptable acid or base may have improved anticancer activity, in which X and Y are hydrogen, halogen or hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, selectively substituted amino, methylene oxy or ethyleneoxy; R1 is hydrogen or alkyl; R2 is hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy or selectively substituted amino; R3 and R4 are hydrogen or alkyl; R5 and R6 are -O-CO-U-V or Z, wherein at least one of R5 and R6 are -O-CO-U-V.
摘要翻译：目的：提供7-氧代-2,3,7,14-四氢-1H-苯并（b）吡喃并（3,2-h）吖啶羧酸酯化合物及其制备方法和含有该化合物的药物组合物，该化合物具有改善的抗癌活性。构成：由式（I）表示的7-氧代-2,3,7,14-四氢-1H-苯并（b）吡喃并（3,2-h）吖啶羧酸酯化合物，其异构体，N-氧化物和药学上可接受的酸或碱可以具有改善的抗癌活性，其中X和Y是氢，卤素或羟基，巯基，氰基，硝基，烷基，烷氧基，三卤代烷基，选择性取代的氨基，亚甲氧基或亚乙氧基; R1是氢或烷基; R2是氢，羟基，烷基，烷氧基，烷基羰基氧基或选择性取代的氨基; R3和R4是氢或烷基; R5和R6是-O-CO-U-V或Z，其中R5和R6中的至少一个是-O-CO-U-V。

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