首页> 外国专利> ACILO AND SULFONYL DERIVATIVES OF 2- (TRANS-1,4-DIAMINOCICLOHEXIL) -PURINS 6,9-DISUSTITUTED AND ITS USE AS ANTIPROLIFERATIVE AGENTS.

ACILO AND SULFONYL DERIVATIVES OF 2- (TRANS-1,4-DIAMINOCICLOHEXIL) -PURINS 6,9-DISUSTITUTED AND ITS USE AS ANTIPROLIFERATIVE AGENTS.

机译:2-(反式-1,4-二氨基环己基)-嘌呤6,9的苯磺酸和磺酰基衍生物是不连续的,并且可以用作抗增殖剂。

摘要

A compound according to formula (I) ** see formula ** in which Z is selected from the group consisting of -S (O) 2- and -C (O) -, when Z is -S (O) 2- , R a is selected from the group consisting of -R1 and -N (R1) (R3), or when Z is -C (O) -, R a is selected from the group consisting of -R1, -OR1, -N (R1) (R3) and -SR1, where R1 is selected from the group consisting of -C1-C11 alkyl, where each carbon can be optionally substituted with one, two or three substituents X, -C3-C10 cycloalkyl, where each carbon it may be optionally substituted with one or two substituents X, - (CH 2) nQ p (CH 2) nW, where each carbon of - (CH 2) n- may be optionally substituted with one or two substituents X, Q is O, S, or NR3, n is independently an integer from 0-6, p is independently an integer 0 or 1, W is independently selected from the group consisting of hydrogen, C 3 -C 10 cycloalkyl, - (C3-C10 cycloalkyl ) -aromatic, and one of the following aromatic rings or heteroarom Attics: ** see formula ** where B is -O-, -S-, -NR6-, where each carbon of the aromatic or heteroaromatic ring can be independently substituted by a nitrogen atom, and each carbon of the aromatic ring can be independently substituted with an X substituent; and - (CH2) nCHW2, where each substituent X is independently selected from the group consisting of hydrogen, halogen, methylenedioxy, C 1 -C 8 alkyl, C 3-C 10 cycloalkyl, substituted or unsubstituted phenyl, -C 1-C alkoxy 8, -SR3, -OH, = O, -CY 3, -OCY 3, -CO 2R3, -CN, -CO-NR4R5, -NO 2, -COR3, -NR4R5, -NH-C (O) -R3 , -NH-C (O) - (C 1 -C 6 alkyl) -aromatic, and -NH-C (O) - (C1-C6 alkyl) -heteroaromatic; where each Y is independently selected from the group consisting of hydrogen and halogen; where each R3 is independently selected from the group consisting of hydrogen, and C1-C8 alkyl, where C1-C8 alkyl can be linear or branched, saturated or unsaturated; where each R4 and R5 is independently selected from the group consisting of hydrogen, and C1-C6 alkyl, where C1-C6 alkyl can be linear or branched, saturated or unsaturated, where each C1-C6 alkyl carbon is optionally substituted. with a substituent X, or where R4 and R5 taken together with the nitrogen to which they are attached, form a heterocyclic ring of three to seven atoms including the nitrogen atom; where -NR6- is selected from the group consisting of an unsubstituted N, an N substituted with -hydrogen, - (C1-C6 alkyl), -C3-C10 cycloalkyl, -S (O) 2- (C1-C6 alkyl), -S (O) 2- (C3-C10 cycloalkyl), -C (O) R3, -C (O) - (C0-C6 alkyl) aromatic, and -S (O) 2- (C0-C6 alkyl) - aromatic, where each carbon of the aromatic ring may be optionally substituted with an X substituent; and where the phenyl is substituted with one to five substituents independently selected from the group consisting of hydrogen, halogen, methylenedioxy, -C1-C8 alkyl, -C3-C10 cycloalkyl, -C1-C8 alkoxy, -OH, -CY3, -OCY3 , -CO2R3, -CN, -NO2, -COR3, -NR4R5, -SR3, -CO-NR4R5, and -NH-C (O) -R3; and R2 is selected from the group consisting of cyclopentyl, cyclopentenyl, and isopropyl; or one of its pharmaceutically acceptable salts, optical isomers, solvates or hydrates.
机译:根据式(I)**的化合物,参见式**,其中Z选自-S(O)2-和-C(O)-,其中Z为-S(O)2-, R a选自-R1和-N(R1)(R3),或者当Z为-C(O)-时,R a选自-R1,-OR1和-N( R1)(R3)和-SR1,其中R1选自-C1-C11烷基,其中每个碳原子可任选被一个,两个或三个取代基X,-C3-C10环烷基取代,其中每个碳原子可以任选地被一个或两个取代基X,-(CH 2)nQ p(CH 2)nW取代,其中-(CH 2)n-的每个碳可以任选地被一个或两个取代基X,Q为O, S,或NR 3,n独立地是0-6的整数,p独立地是0或1的整数,W独立地选自氢,C 3 -C 10环烷基,-(C 3 -C 10环烷基)-芳香族化合物,以及以下芳香族环或杂芳香族阁楼之一:**请参见公式** e B为-O-,-S-,-NR6-,其中芳族或杂芳族环的每个碳原子可独立地被氮原子取代,且芳族环的每个碳原子可独立地被X取代基取代; -(CH 2)n CHW 2,其中每个取代基X独立地选自氢,卤素,亚甲二氧基,C 1 -C 8烷基,C 3 -C 10环烷基,取代或未取代的苯基,-C 1 -C烷氧基8,-SR3,-OH,= O,-CY 3,-OCY 3,-CO 2R3,-CN,-CO-NR4R5,-NO 2,-COR3,-NR4R5,-NH-C(O)-R3 ,-NH-C(O)-(C 1 -C 6烷基)-芳族和-NH-C(O)-(C1-C6烷基)-杂芳族其中每个Y独立地选自氢和卤素;其中每个R 3独立地选自氢和C 1 -C 8烷基,其中C 1 -C 8烷基可以是直链或支链的,饱和或不饱和的;其中每个R 4和R 5独立地选自氢和C 1 -C 6烷基,其中C 1 -C 6烷基可以是直链或支链,饱和或不饱和的,其中每个C 1 -C 6烷基碳是任选取代的。带有取代基X,或其中R 4和R 5与它们所连接的氮一起形成一个包括氮原子的三至七个原子的杂环;其中-NR 6-选自未取代的N,被-氢取代的N,-(C 1 -C 6烷基),-C 3 -C 10环烷基,-S(O)2-(C 1 -C 6烷基), -S(O)2-(C3-C10环烷基),-C(O)R3,-C(O)-(C0-C6烷基)芳香族和-S(O)2-(C0-C6烷基)-芳族的,其中芳族环的每个碳可以任选地被X取代基取代;并且其中苯基被1-5个独立地选自氢,卤素,亚甲二氧基,-C1-C8烷基,-C3-C10环烷基,-C1-C8烷氧基,-OH,-CY3,-OCY3的取代基取代,-CO 2 R 3,-CN,-NO 2,-COR 3,-NR 4 R 5,-SR 3,-CO-NR 4 R 5和-NH-C(O)-R 3; R2选自环戊基,环戊烯基和异丙基;或其药学上可接受的盐,旋光异构体,溶剂化物或水合物之一。

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