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Oxyindole derivatives with motilin receptor agonist activity

机译:具有胃动素受体激动剂活性的羟吲哚衍生物

摘要

A compound of the following formula (I): ** Formula ** wherein R1 is independently selected from the group consisting of hydrogen, C1-C4 alkyl, and C3-C7 cycloalkyl; R2 is independently selected from the group consisting of C1-C4 alkyl and C3-C7 cycloalkyl; or, alternatively, R1 and R2, together with the atoms to which they are attached, form a 3- to 6-membered ring that can contain oxygen; R3 and R4 are independently hydrogen or C1-C4 alkyl; R5 is hydrogen or C1-C4 alkyl; R6 and R7 are independently selected from hydrogen, C1-C4 alkyl, and C1-C4 alkoxy, C1-C4 alkyl; or, alternatively, R6 and R7 together with the nitrogen atom to which they are attached form a 4- to 6-membered ring that can contain nitrogen or oxygen, wherein the 4- to 6-membered ring is optionally substituted with 1 to 4 substituents independently selected from the group consisting of C 1 -C 4 -alkyl, amino, C 1 -C 4 -alkylamino and di (C 1 -C 4 -alkyl) amino; ** Formula ** A is where p, q and r are independently 0 , 1 or 2; R8 and R9 are independently hydrogen or C1-C6 alkyl; said alkyl is optionally substituted with hydroxy, C1-C4-alkyl, amino, C1-C4-alkylamino and di (C1-C4-alkyl) amino; or R8 and R9 can be linked together to form a ring of C3-C7 members; or R8 and R9 can independently bind one or both of the R8 and R9 groups to form alkylene bridges between the terminal nitrogen and the alkyl portion of the R8 or R9 groups, wherein the bridge contains 1 to 5 atoms carbon; said bridge is optionally substituted with from 1 to 4 of C1-C4 alkyl; W is N-R10, said R10 is hydrogen or C1-C4 alkyl; X is C0-C4 alkylene or C0-C4-alkylene-C0-C4 alkylene, where K is -O-; said alkylene is optionally substituted with C1-C4 alkyl; Y is hydrogen or a 5-10 membered ring; said ring is optionally substituted with hydroxy, halogen, C1-C4 haloalkyl, C1-C4 alkyl or C1-C4 alkoxy; when X is C0, Y is not hydrogen; Z is halogen or C1-C4 alkyl; m is 0, 1, 2, 3 or 4; n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.
机译:下式(I)的化合物:**式**其中R 1独立地选自氢,C 1 -C 4烷基和C 3 -C 7环烷基; R2独立地选自C1-C4烷基和C3-C7环烷基;或者,R 1和R 2与它们所连接的原子一起形成可以含有氧的3至6元环。 R3和R4独立地是氢或C1-C4烷基; R5是氢或C1-C4烷基; R6和R7独立地选自氢,C1-C4烷基和C1-C4烷氧基,C1-C4烷基;或者,R 6和R 7与它们所连接的氮原子一起形成可以含有氮或氧的4至6元环,其中4至6元环任选被1至4个取代基取代独立地选自C 1 -C 4烷基,氨基,C 1 -C 4烷基氨基和二(C 1 -C 4烷基)氨基的组; **式** A是p,q和r独立为0,1或2的地方; R8和R9独立地是氢或C1-C6烷基;所述烷基任选地被羟基,C 1 -C 4烷基,氨基,C 1 -C 4烷基氨基和二(C 1 -C 4烷基)氨基取代; R8和R9可以连接在一起形成一个C3-C7成员的环。或R 8和R 9可以独立地结合一个或两个R 8和R 9基团以在末端氮和R 8或R 9基团的烷基部分之间形成亚烷基桥,其中该桥包含1-5个碳原子;所述桥任选地被1-4个C1-C4烷基取代; W为N-R10,所述R10为氢或C1-C4烷基; X为C 0 -C 4亚烷基或C 0 -C 4亚烷基-C 0 -C 4亚烷基,其中K为-O-;所述亚烷基任选地被C 1 -C 4烷基取代; Y是氢或5-10元环;所述环任选地被羟基,卤素,C 1 -C 4卤代烷基,C 1 -C 4烷基或C 1 -C 4烷氧基取代;当X为CO时,Y不是氢; Z为卤素或C1-C4烷基; m为0、1、2、3或4; n为0、1或2;或其药学上可接受的盐。

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