KR20090087127A - 단백질 키나제 억제제로서의 화합물 및 조성물 - Google Patents
단백질 키나제 억제제로서의 화합물 및 조성물 Download PDFInfo
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- KR20090087127A KR20090087127A KR1020097014175A KR20097014175A KR20090087127A KR 20090087127 A KR20090087127 A KR 20090087127A KR 1020097014175 A KR1020097014175 A KR 1020097014175A KR 20097014175 A KR20097014175 A KR 20097014175A KR 20090087127 A KR20090087127 A KR 20090087127A
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- 0 CCNN(*)c1c(*)c(*)c(*)c(N(*)c2c(*)cccc2)n1 Chemical compound CCNN(*)c1c(*)c(*)c(*)c(N(*)c2c(*)cccc2)n1 0.000 description 4
- MHOGOHDSQCSMJH-UHFFFAOYSA-N CC(C)Oc(cc(C=O)c(C)c1)c1[N+]([O-])=O Chemical compound CC(C)Oc(cc(C=O)c(C)c1)c1[N+]([O-])=O MHOGOHDSQCSMJH-UHFFFAOYSA-N 0.000 description 1
- KDXSCKVUTIHYKF-UHFFFAOYSA-N CC(C)Oc(cc(CN(C1CCNCC1)C1=O)c1c1)c1Nc(nc1Nc2ccccc2S(C(C)C)(=O)=O)ncc1Cl Chemical compound CC(C)Oc(cc(CN(C1CCNCC1)C1=O)c1c1)c1Nc(nc1Nc2ccccc2S(C(C)C)(=O)=O)ncc1Cl KDXSCKVUTIHYKF-UHFFFAOYSA-N 0.000 description 1
- FGDOUMVPHJHSCK-UHFFFAOYSA-N CC(C)Oc(cc(c(C)c1)-c2ccncc2)c1[N+]([O-])=O Chemical compound CC(C)Oc(cc(c(C)c1)-c2ccncc2)c1[N+]([O-])=O FGDOUMVPHJHSCK-UHFFFAOYSA-N 0.000 description 1
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Abstract
Description
Claims (20)
- 하기 화학식 1을 갖는 화합물 또는 그의 제약상 허용가능한 염.<화학식 1>상기 식에서,A1 및 A4는 독립적으로 C 또는 N이며;A2 및 A3은 각각 C이거나, 또는 R6 및 R7이 고리를 형성하는 경우 A2 및 A3 중 하나는 N이고;B 및 C는 독립적으로 임의로 치환된 5 내지 7원 카르보시클릭 고리, 아릴, 또는 N, O 또는 S를 함유하는 헤테로아릴 또는 헤테로시클릭 고리이며;Z1, Z2 및 Z3은 독립적으로 NR11, C=O, CR-OR, (CR2)1-2 또는 =C-R12이고;R1 및 R2는 독립적으로 할로, OR12, NR(R12), SR12, 또는 임의로 치환된 C1-6 알 킬, C2-6 알케닐 또는 C2-6 알키닐이거나; 또는 R1 및 R2 중 하나는 H이며;R3은 (CR2)0-2SO2R12, (CR2)0-2SO2NRR12, (CR2)0-2CO1-2R12, (CR2)0-2CONRR12 또는 시아노이고;R4, R6, R7 및 R10은 독립적으로 임의로 치환된 C1-6 알킬, C2-6 알케닐 또는 C2-6 알키닐; OR12, NR(R12), 할로, 니트로, SO2R12, (CR2)pR13 또는 X이거나; 또는 R4, R7 및 R10은 독립적으로 H이며;R, R5 및 R5'는 독립적으로 H 또는 C1-6 알킬이고;R8 및 R9는 독립적으로 C1-6 알킬, C2-6 알케닐, C2-6 알키닐, 할로 또는 X이거나, 또는 R1 및 R2가 고리를 형성하는 경우 R8 및 R9 중 하나는 H이되; 단 R8 및 R9 중 하나는 X이며;다르게는, R1 및 R2, 또는 탄소 원자에 결합되는 경우 R6 및 R7, R7 및 R8, 또는 R9 및 R10은 임의로 치환된 5 내지 7원 모노시클릭 또는 접합 카르보시클릭 고리, 아릴, 또는 N, O 및/또는 S를 포함하는 헤테로아릴 또는 헤테로시클릭 고리를 형성할 수 있거나; 또는 R7, R8, R9 및 R10은 N에 결합되는 경우 부재하고;R11은 H, C1-6 알킬, C2-6 알케닐, (CR2)pCO1-2R, (CR2)pOR, (CR2)pR13, (CR2)pNRR12, (CR2)pCONRR12 또는 (CR2)pSO1-2R12이며;R12 및 R13은 독립적으로 임의로 치환된 3 내지 7원 포화 또는 부분 불포화 카르보시클릭 고리, 또는 N, O 및/또는 S를 포함하는 5 내지 7원 헤테로시클릭 고리; 아릴 또는 헤테로아릴이거나; 또는 R12는 H, C1-6 알킬이고;X는 (CR2)qY, 시아노, CO1-2R12, CONR(R12), CONR(CR2)pNR(R12), CONR(CR2)pOR12, CONR(CR2)pSR12, CONR(CR2)pS(O)1-2R12 또는 (CR2)1-6NR(CR2)pOR12이며;Y는 임의로 치환된 3 내지 12원 카르보시클릭 고리, 5 내지 12원 아릴, 또는 N, O 및/또는 S를 포함하는 5 내지 12원 헤테로아릴 또는 헤테로시클릭 고리이고, (CR2)qY에서 q가 0인 경우 상기 헤테로아릴 또는 헤테로시클릭 고리의 탄소 원자를 통해 A2 또는 A3 또는 이들 둘 다에 결합되고;n, p 및 q는 독립적으로 0 내지 4이다.
- 제1항에 있어서,R1이 할로 또는 C1-6 알킬이고;R2가 H 또는 NH2이거나; 또는R1 및 R2가 함께 임의로 치환된 5 내지 6원 아릴, 또는 1개 내지 3개의 질소 원자를 포함하는 헤테로아릴 또는 헤테로시클릭 고리를 형성하는 화합물.
- 제1항 또는 제2항에 있어서,R3이 SO2R12, SO2NH2, SO2NRR12, CO2NH2, CONRR12, CO1-2R12, 또는 시아노이고;R12가 C1-6 알킬, 임의로 치환된 C3-7 시클로알킬, C3-7 시클로알케닐, 피롤리디닐, 피페라지닐, 피페리디닐, 모르폴리닐 또는 아제티디닐인 화합물.
- 제1항 내지 제3항 중 어느 한 항에 있어서, R5, R5', R7 및 R10이 독립적으로 H이고, n이 0인 화합물.
- 제1항 내지 제3항 중 어느 한 항에 있어서, R6이 OR12이고, R12가 C1 -6 알킬인 화합물.
- 제1항 내지 제3항 중 어느 한 항에 있어서, 하기 화학식 2를 갖는 화합물.<화학식 2>상기 식에서,R1은 할로 또는 C1-6 알킬이고;R2는 H이거나; 또는R1 및 R2는 함께 1개 또는 2개의 질소 원자를 포함하는 임의로 치환된 5 내지 6원 헤테로아릴 또는 헤테로시클릭 고리를 형성하고;R6은 이소프로폭시 또는 메톡시이며;R8 및 R9 중 하나는 (CR2)qY이고, 다른 하나는 C1-6 알킬, 시아노, CO1-2R12, CONR(R12) 또는 CONR(CR2)pNR(R12)이고;Y는 임의로 치환된 C3-7 시클로알킬, C3-7 시클로알케닐, 또는 페닐이거나; 또는 Y는 피리딜, 피라졸릴, 이속사졸릴, 이미다졸릴, 티아졸릴, 벤즈이미다졸릴, 피롤리디닐, 피페라지닐, 피페리디닐, 모르폴리닐, 아제티디닐, 헵타메틸렌이민 또는 옥타메틸렌이민이며, (CR2)qY에서 q가 0인 경우 이들은 각각 탄소 원자를 통해 페닐 고리에 결합되며;n은 0 내지 1이고;q는 0 내지 4이다.
- 제6항에 있어서, R8 및 R9 중 하나가 (CR2)qY이고, 다른 하나가 C1-6 알킬이며; n 및 q가 독립적으로 0인 화합물.
- 제8항에 있어서,R11이 각각 (CR2)pCO1-2R, (CR2)pOR, (CR2)pR13, (CR2)pNRR12 또는 (CR2)pCONRR12이고;R 및 R12가 독립적으로 H 또는 C1-6 알킬이며;R13이 임의로 치환된 피페리디닐, 아제티디닐, 테트라히드로피라닐, 시클로헥실, 모르폴리닐, 피롤리디닐, 헵타메틸렌이민, 옥타메틸렌이민, 바이시클릭 아민 또는 디아민 유도체, 퀴누클리딘-3-일, 8-메틸-8-아자-바이시클로[3.2.1]옥트-6-일, 또는 9-메틸-9-아자-바이시클로[4.2.1]노난-7-일인 화합물.
- 하기 화학식 5를 갖는 화합물 또는 그의 제약상 허용가능한 염.<화학식 5>상기 식에서,A1 및 A4는 독립적으로 C 또는 N이며;A2 및 A3은 각각 C이거나, 또는 R6 및 R7이 고리를 형성하는 경우 A2 및 A3 중 하나는 N이고;B 및 C는 독립적으로 임의로 치환된 5 내지 7원 카르보시클릭 고리, 아릴, 또는 N, O 또는 S를 함유하는 헤테로아릴 또는 헤테로시클릭 고리이며;Z1, Z2 및 Z3은 독립적으로 NR11, C=O, CR-OR, (CR2)1-2 또는 =C-R12이고;R1 및 R2는 독립적으로 할로, OR12, NR(R12), SR12, 또는 임의로 치환된 C1-6 알킬, C2-6 알케닐 또는 C2-6 알키닐이거나; 또는 R1 및 R2 중 하나는 H이며;R3은 (CR2)0-2SO2R12, (CR2)0-2SO2NRR12, (CR2)0-2CO1-2R12, (CR2)0-2CONRR12 또는 시아노이고;R4, R6, 및 탄소 원자에 결합되는 경우 R7 및 R10은 독립적으로 H, 임의로 치환된 C1-6 알킬, C2-6 알케닐 또는 C2-6 알키닐; OR12, NR(R12), 할로, 니트로, SO2R12, (CR2)pR13 또는 X이되; 단 R6 및 R7은 둘 다 H는 아니며;R, R5 및 R5'는 독립적으로 H 또는 C1-6 알킬이고;R8 및 R9는 독립적으로 C1-6 알킬, C2-6 알케닐, C2-6 알키닐, 할로 또는 X이거나, 또는 R8 및 R9 중 하나는 H이되; 단 R8 및 R9 중 하나는 X이며;다르게는, R1 및 R2, 또는 탄소 원자에 결합되는 경우 R6 및 R7, R7 및 R8, 또는 R9 및 R10은 임의로 치환된 5 내지 7원 모노시클릭 또는 접합 카르보시클릭 고리, 아릴, 또는 N, O 및/또는 S를 포함하는 헤테로아릴 또는 헤테로시클릭 고리를 형성할 수 있거나; 또는 R7, R8, R9 및 R10은 N에 결합되는 경우 부재하고;R11은 H, C1-6 알킬, C2-6 알케닐, (CR2)pCO1-2R, (CR2)pOR, (CR2)pR13, (CR2)pNRR12, (CR2)pCONRR12 또는 (CR2)pSO1-2R12이며;R12 및 R13은 독립적으로 임의로 치환된 3 내지 7원 포화 또는 부분 불포화 카르보시클릭 고리, 또는 N, O 및/또는 S를 포함하는 5 내지 7원 헤테로시클릭 고리; 아릴 또는 헤테로아릴이거나; 또는 R12는 H, C1-6 알킬이고;X는 (CR2)qY, 시아노, CO1-2R12, CONR(R12), CONR(CR2)pNR(R12), CONR(CR2)pOR12, CONR(CR2)pSR12, CONR(CR2)pS(O)1-2R12 또는 (CR2)1-6NR(CR2)pOR12이며;Y는 임의로 치환된 3 내지 12원 카르보시클릭 고리, 5 내지 12원 아릴, 또는 N, O 및/또는 S를 포함하는 5 내지 12원 헤테로아릴 또는 헤테로시클릭 고리이고, (CR2)qY에서 q가 0인 경우 상기 헤테로아릴 또는 헤테로시클릭 고리의 탄소 원자를 통해 A2 또는 A3 또는 이들 둘 다에 결합되고;n, p 및 q는 독립적으로 0 내지 4이다.
- 제12항에 있어서,R1이 할로 또는 C1-6 알킬이고;R2가 H 또는 NH2이거나; 또는R1 및 R2가 함께 임의로 치환된 5 내지 6원 아릴, 또는 1개 내지 3개의 질소 원자를 포함하는 헤테로아릴 또는 헤테로시클릭 고리를 형성하는 화합물.
- 치료 유효량의 제1항 내지 제15항 중 어느 한 항의 화합물 및 제약상 허용가능한 담체를 포함하는 제약 조성물.
- 세포계 또는 조직계에 또는 포유동물 대상체에게 치료 유효량의 제1항 내지 제15항 중 어느 한 항의 화합물 또는 그의 제약상 허용가능한 염을 투여함으로써 역형성 림프종 키나제를 억제하는 것을 포함하는, 상기 키나제의 억제 방법.
- 임의로는 제2 치료제와 조합된, 제1항 내지 제15항 중 어느 한 항의 화합물 또는 그의 제약 조성물의, 자가면역 질환, 이식 질환, 감염병 또는 세포 증식성 질환인 역형성 림프종 키나제에 의해 매개되는 질환의 치료를 위한 의약 제조에서의 용도.
- 임의로는 제2 치료제와 조합된, 제1항 내지 제15항 중 어느 한 항의 화합물 또는 그의 제약 조성물의, 림프종, 골육종, 흑색종, 또는 유방, 신장, 전립선, 직장결장, 갑상선, 난소, 췌장, 신경세포, 폐, 자궁의 종양 또는 위장관 종양인 세포 증식성 질환의 치료를 위한 의약 제조에서의 용도.
- 제19항에 있어서, 상기 제2 치료제가 화학요법제인 용도.
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