KR101110458B1 - 유사분열 진행을 억제하기 위한 화합물 - Google Patents
유사분열 진행을 억제하기 위한 화합물 Download PDFInfo
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- 0 COc(cccc1F)c1C(c1c-2ccc(Cl)c1)=NCc1c-2nc(Nc2ccc(C(O)=O)c(O*)c2)nc1 Chemical compound COc(cccc1F)c1C(c1c-2ccc(Cl)c1)=NCc1c-2nc(Nc2ccc(C(O)=O)c(O*)c2)nc1 0.000 description 5
- DJYNPVHWFKXVCH-UHFFFAOYSA-N CC(c1ccc(C(O)=O)c(OC)c1)c1nc(-c(ccc(-c2c(C)cc[o]2)c2)c2C(c(c(OC)ccc2)c2F)=CC2)c2cn1 Chemical compound CC(c1ccc(C(O)=O)c(OC)c1)c1nc(-c(ccc(-c2c(C)cc[o]2)c2)c2C(c(c(OC)ccc2)c2F)=CC2)c2cn1 DJYNPVHWFKXVCH-UHFFFAOYSA-N 0.000 description 1
- NRJOLMQQQLDIPP-UHFFFAOYSA-N COc(cccc1F)c1C(c1c-2ccc(C#C)c1)=NCc1c-2nc(Nc2ccc(C(O)=O)c(OC)c2)nc1 Chemical compound COc(cccc1F)c1C(c1c-2ccc(C#C)c1)=NCc1c-2nc(Nc2ccc(C(O)=O)c(OC)c2)nc1 NRJOLMQQQLDIPP-UHFFFAOYSA-N 0.000 description 1
- BTMPSJZQWXFMIF-UHFFFAOYSA-N Cc1c[s]cc1-c(cc1)cc(C(c(c(F)ccc2)c2OC)=NC2)c1-c1c2cnc(Nc2ccc(C(O)=O)c(OC)c2)n1 Chemical compound Cc1c[s]cc1-c(cc1)cc(C(c(c(F)ccc2)c2OC)=NC2)c1-c1c2cnc(Nc2ccc(C(O)=O)c(OC)c2)n1 BTMPSJZQWXFMIF-UHFFFAOYSA-N 0.000 description 1
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A—HUMAN NECESSITIES
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Abstract
Description
화합물 명칭 | |
1 | 4-{[9-클로로-7-(2-플루오로-6-메톡시페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
2 | 4-{[9-에티닐-7-(2-플루오로-6-메톡시페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
3 | 4-({9-클로로-7-[2-플루오로-6-(트리플루오로메톡시)페닐]-5H-피리미도[5,4-d][2]벤즈아제핀-2-일}아미노)-2-메톡시벤조산 |
4 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-(1-메틸-1H-피롤-2-일)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
5 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-(4-메틸-3-티에닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
6 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-(3-메틸-2-푸릴)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
7 | 4-({9-에티닐-7-[2-플루오로-6-(2,2,2-트리플루오로에톡시)페닐]-5H-피리미도[5,4-d][2]벤즈아제핀-2-일}아미노)-2-메톡시벤조산 |
8 | 4-{[9-클로로-7-(2,6-디플루오로페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
9 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-(2-메틸페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
10 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-프롭-1-인-1-일-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
11 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-비닐-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
12 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-(2-플루오로페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
13 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-(3-메톡시프롭-1-인-1-일)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
14 | 4-({7-(2-플루오로-6-메톡시페닐)-9-[(1E)-프롭-1-엔-1-일]-5H-피리미도[5,4-d][2]벤즈아제핀-2-일}아미노)-2-메톡시벤조산 |
15 | 4-({9-클로로-7-[2-플루오로-6-(2,2,2-트리플루오로에톡시)페닐]-5H-피리미도[5,4-d][2]벤즈아제핀-2-일}아미노)-2-메톡시벤조산 |
16 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-(2-푸릴)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
17 | 4-{[9-클로로-7-(2-플루오로-6-히드록시페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
18 | 4-{[7-(2-플루오로-6-메톡시페닐)-9-페닐-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산 |
화합물 | 구조식 |
pT288
IC 50 (μM) |
BrdU
HCT116 LD 50 (μM) |
BrdU
SW480 LD 50 (μM) |
1
|
0.005 | 0.03 | 0.41 | |
i
|
0.18 | 0.707 | 6.502 | |
ii
|
0.15 | 0.758 | 7.579 | |
iii
|
0.018 | 0.13 | 0.94 |
Claims (15)
- 하기 화학식 (I)의 화합물 또는 이의 약제학적으로 허용되는 염:상기 식에서,Ra는 C1-3 지방족, C1-3 플루오로지방족, -R1, -T-R1, -R2 및 -T-R2로 구성된 군으로부터 선택되고;T는 플루오로로 치환되거나 치환되지 않은 C1-3 알킬렌 사슬이고;R1은 아릴, 헤테로아릴 또는 헤테로시클릴 기이고;R2는 할로, -C≡C-R3, -CH=CH-R3, -N(R4)2 및 -OR5로 구성된 군으로부터 선택되고;R3는 수소이거나, 지방족, 아릴, 헤테로아릴 또는 헤테로시클릴 기이고;각각의 R4는 독립적으로 수소이거나, 지방족, 아릴, 헤테로아릴 또는 헤테로시클릴 기이거나; 동일한 질소 원자상의 2개의 R4는 상기 질소 원자와 함께 5원 또는 6원 헤테로아릴을 형성하거나 상기 질소 원자에 더하여 N, O, 및 S로부터 선택된 0 내지 2개의 고리 헤테로원자를 지닌 4원 내지 8원 헤테로시클릴 고리를 형성하고;R5는 수소이거나, 지방족, 아릴, 헤테로아릴 또는 헤테로시클릴 기이고;Rb는 플루오로, 클로로, -CH3, -CF3, -OH, -OCH3, -OCF3, -OCH2CH3 및 -OCH2CF3로 구성된 군으로부터 선택되고;상기 아릴 또는 헤테로아릴 기는 치환되지 않거나, -할로, -NO2, -CN, -R*, -C(R*)=C(R*)2, -C≡C-R*, -OR*, -SR, -S(O)R, -SO2R, -SO3R, -SO2N(R+)2, -N(R+)2, -NR+C(O)R*, -NR+C(O)N(R+)2, -NR+CO2R, -O-CO2R*, -OC(O)N(R+)2, -O-C(O)R*, -CO2R*, -C(O)-C(O)R*, -C(O)R*, -C(O)N(R+)2, -C(O)N(R+)C(=NR+)-N(R+)2, -N(R+)C(=NR+)-N(R+)-C(O)R*, -C(=NR+)-N(R+)2, -C(=NR+)-OR*, -N(R+)-N(R+)2, -N(R+)C(=NR+)-N(R+)2, -NR+SO2R, -NR+SO2N(R+)2, -P(O)(R*)2, -P(O)(OR*)2, -O-P(O)-OR* 및 -P(O)(NR+)-N(R+)2로 구성된 군으로부터 선택되는 1개 이상의 치환기로 치환되거나, 이들 치환기 중 2개의 인접 치환기는 이들의 개재 원자들과 함께 취해져 N, O 및 S로 구성된 군으로부터 선택된 0개 내지 3개의 고리 원자를 지닌 5원 내지 6원의 불포화 또는 부분 불포화 고리를 형성하고;상기 지방족 또는 헤테로시클릴 기는 치환되지 않거나, -할로, -NO2, -CN, -R*, -C(R*)=C(R*)2, -C≡C-R*, -OR*, -SR, -S(O)R, -SO2R, -SO3R, -SO2N(R+)2, -N(R+)2, -NR+C(O)R*, -NR+C(O)N(R+)2, -NR+CO2R, -O-CO2R*, -OC(O)N(R+)2, -O-C(O)R*, -CO2R*, -C(O)-C(O)R*, -C(O)R*, -C(O)N(R+)2, -C(O)N(R+)C(=NR+)-N(R+)2, -N(R+)C(=NR+)-N(R+)-C(O)R*, -C(=NR+)-N(R+)2, -C(=NR+)-OR*, -N(R+)-N(R+)2, -N(R+)C(=NR+)-N(R+)2, -NR+SO2R, -NR+SO2N(R+)2, -P(O)(R*)2, -P(O)(OR*)2, -O-P(O)-OR* 및 -P(O)(NR+)-N(R+)2로 구성된 군으로부터 선택되는 1개 이상의 치환기로 치환되거나, 이들 치환기 중 2개의 인접 치환기는 이들의 개재 원자들과 함께 취해져 N, O 및 S로 구성된 군으로부터 선택된 0개 내지 3개의 고리 원자를 지닌 5원 내지 6원의 불포화 또는 부분 불포화 고리를 형성하거나, 상기 지방족 또는 헤테로시클릴 기는 =O, =S, =C(R*)2, =N-N(R*)2, =N-OR*, =N-NHC(O)R*, =N-NHCO2R, =N-NHSO2R 또는 =N-R*로 구성된 군으로부터 선택되는 1개 이상의 치환기로 치환되고;상기 헤테로시클릴 기의 질소 원자는 치환되지 않거나, -R*, -N(R*)2, C(O)R*, -CO2R*, -C(O)-C(O)R*, -C(O)CH2C(O)R*, -SO2R*, -SO2N(R*)2, -C(=S)N(R*)2, -C(=NH)-N(R*)2 및 -NR*SO2R*로 구성된 군으로부터 선택되는 1개 이상의 치환기로 치환되고;각각의 R+는 독립적으로 수소이거나, 지방족, 아릴, 헤테로아릴 또는 헤테로시클릴 기이거나, 동일한 질소 원자상의 2개의 R+는 질소 원자와 함께 취해져 상기 질소 원자에 더하여 N, O 및 S로부터 선택된 0개 내 2개의 헤테로원자를 지닌 5원 내지 8원의 방향족 또는 비방향족 고리를 형성하고;각각의 R*는 독립적으로 수소이거나, 지방족, 할로지방족, 아릴, 헤테로아릴 또는 헤테로시클릴 기이고;각각의 R은 지방족 또는 아릴 기이다.
- 제 1항에 있어서, R1이 할로, C1-3 지방족 및 C1-3 플루오로지방족으로 구성된 군으로부터 독립적으로 선택된 1개 또는 2개의 치환기로 치환되거나 치환되지 않은, 5원 또는 6원 아릴, 헤테로아릴 또는 헤테로시클릴 고리인 화합물.
- 제 1항에 있어서, Ra가 할로, C1-3 지방족 및 C1-3 플루오로지방족으로 구성된 군으로부터 독립적으로 선택된 1개 또는 2개의 치환기로 치환되거나 치환되지 않은, 페닐, 푸릴, 피롤리디닐 또는 티에닐 고리이거나; Ra가 할로, C1-3 지방족, C1-3 플루오로지방족, -OH, -O(C1-3 지방족), -O(C1-3 플루오로지방족), 또는 -C≡C-R3, -CH=CH-R3이며, 여기서 R3는 수소, C1-3 지방족, C1-3 플루오로지방족 또는 -CH2-OCH3인 화합물.
- 제 3항에 있어서, Ra가 클로로, 플루오로, C1-3 지방족, C1-3 플루오로지방족, -OCH3, -OCF3, -C≡C-H, -C≡C-CH3, -C≡C-CH2OCH3, -CH=CH2, -CH=CHCH3, N-메틸피롤리디닐, 티에닐, 메틸티에닐, 푸릴, 메틸푸릴, 페닐, 플루오로페닐 및 톨릴로 구성된 군으로부터 선택되는 화합물.
- 4-{[9-에티닐-7-(2-플루오로-6-메톡시페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산인 화합물 또는 이의 약제학적으로 허용되는 염.
- 4-{[7-(2-플루오로-6-메톡시페닐)-9-(1-메틸-1H-피롤-2-일)-5H-피리미도[5,4 -d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산인 화합물 또는 이의 약제학적으로 허용되는 염.
- 4-{[9-클로로-7-(2-플루오로-6-메톡시페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조산인 화합물 또는 이의 약제학적으로 허용되는 염.
- 소듐 4-{[9-클로로-7-(2-플루오로-6-메톡시페닐)-5H-피리미도[5,4-d][2]벤즈아제핀-2-일]아미노}-2-메톡시벤조에이트인 화합물.
- 제 1항 내지 제 8항 중 어느 한 항에 따른 화합물과 약제학적으로 허용되는 담체를 포함하는, 암 치료용 약제 조성물.
- 오로라(Aurora) 키나아제의 억제가 요망되는 세포를 제 1항 내지 제 8항 중 어느 한 항에 따른 화합물과 시험관내에서 접촉시키는 것을 포함하여, 시험관내에서 세포의 오로라 키나아제 활성을 억제하는 방법.
- 제 10항에 있어서, 상기 오로라 키나아제가 오로라 A 키나아제인 방법.
- 삭제
- 삭제
- 제 9항에 있어서, 상기 암이 결장직장암, 난소암, 유방암, 위암, 전립선암 및 췌장암으로 구성된 군으로부터 선택되는 약제 조성물.
- 제 14항에 있어서, 암이 유방암, 결장직장암 및 췌장암으로 구성된 군으로부터 선택되는 약제 조성물.
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