首页> 外国专利> 12,13- (pyranosyl) -indolo (2,3-a) pyrrolo (3,4-c) carbazole and 12,13- (pyranosyl) -furo (3,4-c) indolo (2,3-a ) carbazole derivatives, their process of preparation and pharmaceutical compositions containing them

12,13- (pyranosyl) -indolo (2,3-a) pyrrolo (3,4-c) carbazole and 12,13- (pyranosyl) -furo (3,4-c) indolo (2,3-a ) carbazole derivatives, their process of preparation and pharmaceutical compositions containing them

机译:12,13-(吡喃基)-吲哚(2,3-a)吡咯(3,4-c)咔唑和12,13-(吡喃基)-呋喃(3,4-c)吲哚(2,3-a)咔唑衍生物,其制备方法和含有它们的药物组合物

摘要

A composition comprises 12,13-(Pyranosyl)-indolo(2,3-a)pyrrolo(3,4-c)carbazole and 12,13-(pyranosyl)-furo(3,4-c)indolo(2,3-a)carbazole derivatives (I), or their isomers, salts with acids or bases, are new A composition comprises 12,13-(Pyranosyl)-indolo(2,3-a)pyrrolo(3,4-c)carbazole and 12,13-(pyranosyl)-furo(3,4-c)indolo(2,3-a)carbazole derivatives of formula (I), or their isomers, salts with acids or bases, are new R1, R2 = U-V; U = 1-6C alkylene, optionally substituted by one or more halo or OH, and which may be unsaturated; V = H, halo, CN, NO2, N3, 1-6C alkyl, aryl, arylalkyl, OH, 1-6C alkoxy, aryloxy, aryl alkoxy, formyl, carboxy, aminocarbonyl, NRaRb, -CO-T1, -CO-NRa-T1, -NRa-CO-T1, -O-CO-T1, -CO-O-T1, -O-T2-NRaRb, -OT2-ORa, -O-T2-COORa, -NRa-T2-NRaRb, -NRa-T2-ORa, -NRa-T2-CO2Raor S(O)n-Ra; Ra, Rb = H, 1-6C alkyl, aryl, or arylalkyl, or both together with the N atom form a 5-7 membered heterocycle which may contain a second heteroatom (O or N) and may be substituted by alkyl, alkoxy, OH, amino, 1-6C alkylamino, or 1-6C dialkylamino; T1 = 1-6C alkyl, aryl, 1-6C arylalkyl, 1-6C alkylene, optionally substituted by -ORa, -NRaRb, -COORa, -CO-Ra, or -CO-NRaRb; T2 = 1-6C alkylene; n = 0 - 2; G = O or NR3; R3 = H, 1-6C alkyl, aryl, arylalkyl, cycloalkyl, cycloalkyl alkyl, -ORa, -NRaRb, -OT2-NRaRb, -NRa-T2-NRaRb, 1-6C hydroxylamino, dihydroxylamino, -CO-Ra, -NH-CO-Ra, 1-6C alkylene, optionally substituted by one or more of halogen, CN, NO2, -ORa, -NRaRb, -COORa, -CORa, hydroxylamino, dihydroxylamino, or -CO-NHRa; X = H, OH, 1-6C alkoxy, SH, or 1-6C alkylthio; Y = H, or X and Y together with the C atom form carbonyl; X1 = H, OH, 1-6C alkoxy, SH, or 1-6C alkylthio; Y1 = H or X1 and Y1 together with the C atom form carbonyl; R4, R5 = H, halogen, OH, alkoxy, aryloxy, aryl alkoxy, alkyl, arylalkyl, aryl, amino (optionally substituted by one or two alkyl, alkyl, aryl and arylalkyl groups), azido, -N=NRa, or -O-CO-Rc; Rc = 1-6C alkyl (optionally substituted by one or more halogen, OH, amino, alkylamino and dialkylamino groups), aryl, aralkyl, cycloalkyl or heterocycloalkyl; R6 = -U1-R4; U1 = a bond or methylene; or R4, R5, and R6 taken in pairs together with the C atoms may = 3-6 membered ring containing 1 or 2 O atoms, except for the following specific compounds: 1,11-dichloro-12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5,7-dio ne; 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5,7-dione; 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5-one; and 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-5,6,12,13-tetrahydro(7H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-7-one.
机译:组合物包含12,13-(吡喃糖基)-吲哚(2,3-a)吡咯并(3,4-c)咔唑和12,13-(吡喃糖基)-呋喃(3,4-c)吲哚(2,3 -a)咔唑衍生物(I)或其异构体,与酸或碱的盐。新的组合物包含12,13-(吡喃糖基)-吲哚(2,3-a)吡咯并(3,4-c)咔唑和式(I)的12,13-(吡喃基)-呋喃(3,4-c)吲哚(2,3-a)咔唑衍生物或其异构体,与酸或碱的盐是新的R 1,R 2 = UV; U = 1-6C亚烷基,任选地被一个或多个卤素或OH取代,并且可以是不饱和的; V = H,卤素,CN,NO2,N3、1-6C烷基,芳基,芳基烷基,OH,1-6C烷氧基,芳氧基,芳基烷氧基,甲酰基,羧基,氨基羰基,NRaRb,-CO-T1,-CO-NRa -T1,-NRa-CO-T1,-O-CO-T1,-CO-O-T1,-O-T2-NRaRb,-OT2-ORa,-O-T2-COORa,-NRa-T2-NRaRb, -NRa-T2-ORa,-NRa-T2-CO2Raor S(O)n-Ra; Ra,Rb = H,1-6C烷基,芳基或芳基烷基,或两者均与N原子一起形成5-7元杂环,该杂环可包含第二个杂原子(O或N),并可被烷基,烷氧基取代, OH,氨基,1-6C烷基氨基或1-6C二烷基氨基; T1 = 1-6C烷基,芳基,1-6C芳基烷基,1-6C亚烷基,任选地被-ORa,-NRaRb,-COORa,-CO-Ra或-CO-NRaRb取代; T 2 = 1-6C亚烷基; n = 0-2; G = O或NR3; R3 = H,1-6C烷基,芳基,芳基烷基,环烷基,环烷基烷基,-ORa,-NRaRb,-OT2-NRaRb,-NRa-T2-NRaRb,1-6C羟基氨基,二羟基氨基,-CO-Ra,-NH -CO-Ra,1-6C亚烷基,其任选地被卤素,CN,NO 2,-ORa,-NRaRb,-COORa,-CORa,羟基氨基,二羟基氨基或-CO-NHRa中的一个或多个取代; X = H,OH,1-6C烷氧基,SH或1-6C烷硫基; Y = H,或X和Y与C原子一起形成羰基; X1 = H,OH,1-6C烷氧基,SH或1-6C烷硫基; Y 1 = H或X 1和Y 1与C原子一起形成羰基; R 4,R 5 = H,卤素,OH,烷氧基,芳氧基,芳基烷氧基,烷基,芳基烷基,芳基,氨基(任选地被一个或两个烷基,烷基,芳基和芳基烷基取代),叠氮基,-N = NR a或- O-CO-Rc; Rc = 1-6C烷基(任选地被一个或多个卤素,OH,氨基,烷基氨基和二烷基氨基取代),芳基,芳烷基,环烷基或杂环烷基; R6 = -U1-R4; U1 =键或亚甲基;或者R4,R5和R6与C原子成对出现,可能= 3-6元环,含有1或2个O原子,但以下特定化合物除外:1,11-二氯-12,13-(1,2 -(4-(O-甲基-β-D-甘露吡喃糖基))-6,7,12,13-四氢(5H)吲哚并(2,3-a)吡咯并(3,4-c)咔唑-5,7 -二烯; 12,13-(1,2-(4-(O-甲基-β-D-甘露吡喃糖基))-6,7,12,13-四氢(5H)吲哚(2,3-a)吡咯(3,4-c)咔唑-5,7-二酮; 12,13-(1,2-(4-(O-甲基-β-D-甘露吡喃糖基))-6,7,12,13-四氢( 5H)吲哚并(2,3-a)吡咯并(3,4-c)咔唑-5-酮;和12,13-(1,2-(4-(O-甲基-β-D-甘露吡喃糖基))- 5,6,12,13-四氢(7H)吲哚(2,3-a)吡咯并(3,4-c)咔唑-7-一。

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