首页> 外国专利> Cyclohexylpyrazol-lactam derivatives as 11-beta-hydroxysteroid dehydrogenase 1 inhibitors

Cyclohexylpyrazol-lactam derivatives as 11-beta-hydroxysteroid dehydrogenase 1 inhibitors

机译:环己基吡唑-内酰胺衍生物作为11-β-羟基类固醇脱氢酶1抑制剂

摘要

A compound structurally represented by the formula: ** Formula ** in which: R1 is -H, 5-halogen, -O-CH3 (optionally substituted with one to three halogens) or -CH3 (optionally substituted with one to three halogens ); R2 is -H, -halogen, -O-CH3 (optionally substituted with one to three halogens) or -CH3 (optionally substituted with one to three halogens); R3 is -H or -halogen; R4 is -OH, -halogen, -cyano, -alkyl (C1-C4) (optionally substituted with one to three halogens), -alkoxy (C1-C6) (optionally substituted with one to three halogens), -SCF3, -C (O) O-C1-C4 alkyl, -O-CH2-C (O) NH2, -cycloalkyl (C3-C8), -O-phenyl-C (O) O-alkyl (C1-C4), - CH2-phenyl, -NHSO2-alkyl (C1-C4), -NHSO2-phenyl (R21) (R21), -alkyl (C1-C4) -C (O) N (R10) (R11), -C (O) N (R10) (R11), ** Formula ** in which the dashed line represents the point of attachment to the R4 position of formula I; in which m is 1, 2 or 3; where n is 0, 1 or 2; and in which when n is 0, then "(CH2) n" is a link; R5 is -H, -halogen, -OH, -CN, -C1-C4 alkyl (optionally substituted with 1 to 3 halogens), -C (O) OH, -C (O) O-C1-C4 alkyl ), -C (O) -C1-C4 alkyl, 5-O-C1-C4 alkyl (optionally substituted with 1 to 3 halogens), -SO2-C1-C4 alkyl, -N (R8) (R8), -phenyl (R21) (R21), -C (O) -NH-cycloalkyl (C3-C6), ** Formula ** in which the dashed line represents the point of attachment to the position indicated by R5 ; in which m is 1, 2 or 3; in which n is 0, 1 or 2, and in which when n is 0, then "(CH2) n" is a link; R6 is -H, -halogen, -CN or-(C1-C4) alkyl (optionally substituted with 1 to 3 halogens), -O-(C1-C4) alkyl (optionally substituted with 1 to 3 halogens) or ** Formula ** R7 is -H, -halogen or-(C1-C4) alkyl (optionally substituted with 1 to 3 halogens); R8 is, independently at each occurrence, -H, -C1-C6 alkyl (optionally substituted with 1 to 3 halogens), -C (O) -C1-C6 alkyl (optionally substituted with 1 to 3 halogens ), -C (O) -C3-C8-cycloalkyl, - S (O2) -C3-C8 -cycloalkyl or -S (O2) -C1-C3-alkyl (optionally substituted with 1 to 3 halogens); R9 is -H or -halogen; R10 and R11 are each, independently, -H or -C1-C4 alkyl, or R10 and R11 taken together with the nitrogen to which they are attached form piperidinyl, piperazinyl or pyrrolidinyl; R20 is, independently at each occurrence, -H or -C1-C3 alkyl (optionally substituted with 1 to 3 halogens); R21 is, independently at each occurrence, -H, -halogen or-(C1-C3) alkyl (optionally substituted with 1 to 3 halogens); R22 is, independently at each occurrence, -H or -C1-C6 alkyl (optionally substituted with 1 to 3 halogens); and R23 is, independently at each occurrence, -H, -C1-C4 alkyl or -C (O) O-C1-C4 alkyl; or a pharmaceutically acceptable salt thereof.
机译:结构上由以下通式表示的化合物:** **其中:R1为-H,5-卤素,-O-CH3(可选被一至三个卤素取代)或-CH3(可选被一至三个卤素) ; R 2为-H,-卤素,-O-CH 3(任选地被1-3个卤素取代)或-CH 3(任选地被1-3个卤素取代); R3是-H或-卤素; R 4为-OH,-卤素,-氰基,-烷基(C 1 -C 4)(任选地被1-3个卤素取代),-烷氧基(C 1 -C 6)(任选地被1-3个卤素取代),-SCF 3,-C (O)O-C1-C4烷基,-O-CH2-C(O)NH2,-环烷基(C3-C8),-O-苯基-C(O)O-烷基(C1-C4),-CH2-苯基,-NHSO2-烷基(C1-C4),-NHSO2-苯基(R21)(R21),-烷基(C1-C4)-C(O)N(R10)(R11),-C(O)N( R10)(R11),**式**,其中虚线表示与式I的R4位置的连接点;其中m为1、2或3;其中n为0、1或2;其中,当n为0时,则“(CH2)n”为链接; R5为-H,-卤素,-OH,-CN,-C1-C4烷基(任选地被1-3个卤素取代),-C(O)OH,-C(O)O-C1-C4烷基),- C(O)-C1-C4烷基,5-O-C1-C4烷基(可选被1-3个卤素取代),-SO2-C1-C4烷基,-N(R8)(R8),-苯基(R21) (R21),-C(O)-NH-环烷基(C3-C6),**式**,其中虚线表示与R5指示的位置的连接点;其中m为1、2或3;其中n为0、1或2,并且当n为0时,则“(CH2)n”为链接; R6为-H,-卤素,-CN或-(C1-C4)烷基(可选被1-3个卤素取代),-O-(C1-C4)烷基(可选被1-3个卤素取代)或** ** R7是-H,-卤素或-(C1-C4)烷基(任选被1-3个卤素取代); R 8在每次出现时独立地是-H,-C 1 -C 6烷基(任选地被1-3个卤素取代),-C(O)-C 1 -C 6烷基(任选地被1-3个卤素取代),-C(O )-C 3 -C 8-环烷基,-S(O 2)-C 3 -C 8环烷基或-S(O 2)-C 1 -C 3烷基(任选地被1-3个卤素取代); R9是-H或-卤素; R 10和R 11各自独立地是-H或-C 1 -C 4烷基,或R 10和R 11与它们所连接的氮一起形成哌啶基,哌嗪基或吡咯烷基。 R 20在每次出现时独立地为-H或-C 1 -C 3烷基(任选地被1-3个卤素取代); R21在每次出现时独立地为-H,-卤素或-(C1-C3)烷基(任选地被1-3个卤素取代); R22在每次出现时独立地是-H或-C1-C6烷基(任选地被1-3个卤素取代); R 23分别独立地为-H,-C 1 -C 4烷基或-C(O)O-C 1 -C 4烷基。或其药学上可接受的盐。

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