KR950000695A - 헤테로환식 고리를 함유하는 우레아 유도체 - Google Patents

헤테로환식 고리를 함유하는 우레아 유도체 Download PDF

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KR950000695A
KR950000695A KR1019940013326A KR19940013326A KR950000695A KR 950000695 A KR950000695 A KR 950000695A KR 1019940013326 A KR1019940013326 A KR 1019940013326A KR 19940013326 A KR19940013326 A KR 19940013326A KR 950000695 A KR950000695 A KR 950000695A
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phenyl
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히로무 마쯔무라
도시사다 야노
히로시 하시즈메
마사미 에이교오
고오이찌 오따니
아끼노리 아리무라
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시오노기 요시히꼬
시오노기 세이야꾸 가부시기가이샤
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Publication of KR950000695A publication Critical patent/KR950000695A/ko

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Abstract

본 발명은 하기 일반식(I)로 화합물 및 이의 약제학적으로 허용되는 염을 제공한다.
[단, 상기식에서, Z1은 C 또는 N이고 ; m1은 Z1이 N일 경우에는 0이고, Z1이 C일 경우에는 1이며 ; R3는 Z1이 C일 경우 R2와 함께 결합을 형성할 수 있고 ; A1은 O, SO2또는 CH2이며 ; n1은 A1이 O 또는 SO2일 경우에는 0 또는 1이고, A1이 CH2일 경우에는 0 내지 3의 정수이며 ; R1은 축합 방향족 고리, 치환된 축합 방향족 고리, 카르복실기, 알콕시 카르보닐기 및
로 이루어진 군에서 선택된 기이고
(단, 식중에서, R11은 H 또는 OH이거나, 또는 Z1이 C이고 n1이 0일 경우 R2와 함께 결합을 형성할 수 있고 ; R12와 R13은 각기 페닐, 치환된 페닐, 헤테로환식 고리 또는 치환된 헤테로환식 고리이거나, 또는 R12와 R13은 축합 고리를 형성할 수 있다. ; R2은 R3또는 R11과 결합을 형성하지 않을 경우에는 H이며 ; R3도 R2와 결합을 형성하지 않을 경우에는 H이고 ; K1은 2 내지 5의 정수이며 ; Y1은 O, S, SO, SO2, CH2및
로 이루어진 군에서 선택된 기이고
{단, 식중에서, Z2는 N 또는 C이고 ; m2는Z2가 N일 경우에는 0이고, Z2가 C일 경우에는 1이며 ; A2는 O, SO2또는 CH2이고 ; n2는 A2가 O 또는 SO2일 경우에는 0 또는 1이고, A2가 CH2일 경우에는 0 내지 3의 정수이며 ; R4는 알킬, 페닐, 치환된 페닐, 헤테로환식 고리, 치환된 헤테로환식 고리, -CO-R41및
로 이루어진 군에서 선택된 기이고
(여기에서, R41은 OH, 알콕시, 아미노, 아릴알킬옥시, 치환된 아미노, 아릴알켄일 및 치환된 아릴알켈일중의 어느 하나이고 ; R42는 H 또는 OH이거나, 또는 Z2가 C이고, n2가 0일 경우에는 R5와 함께 결합을 형성할 수 있으며 ; R43과 R44는 각기 페닐, 치환된 페닐, 헤테로환식 고리 또는 치환식 헤테로환식 고리이다.) ; R5는 R42와 함께 결합을 형성하지 않을 경우에는 H이다} ; Y2는 CH2또는 CO이고 ; Y3는 (CH2) 또는 페닐렌이며 ; K2는 0 또는 1이다.]

Description

헤테로환식 고리를 함유하는 우레아 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (19)

  1. 하기 일반식(I)로 표시되는 화합물 및 이의 약제학적으로 허용되는 염.
    [단, 상기식에서, Z1은 C 또는 N이고 ; m1은 Z1이 N일 경우에는 0이고, Z1이 C일 경우에는 1이며 ; R3는 Z1이 C일 경우 R2와 함께 결합을 형성할 수 있고 ; A1은 O, SO2또는 CH2이며 ; n1은 A1이 O 또는 SO2일 경우에는 0 또는 1이고, A1이 CH2일 경우에는 0 내지 3의 정수이며 ; R1은 축합 방향족 고리, 치환된 축합 방향족 고리, 카르복실기, 알콕시 카르보닐기 및
    로 이루어진 군에서 선택된 기이고
    (단, 식중에서, R11은 H 또는 OH이거나, 또는 Z1이 C이고 n1이 0일 경우 R2와 함께 결합을 형성할 수 있고 ; R12와 R13은 각기 페닐, 치환된 페닐, 헤테로환식 고리 또는 치환된 헤테로환식 고리이거나, 또는 R12와 R13은 축합 고리를 형성할 후 있다.) ; R2은 R3또는 R11과 결합을 형성하지 않을 경우에는 H이며 ; R3도 R2와 결합을 형성하지 않을 경우에는 H이고 ; K1은 2 내지 5의 정수이며 ; Y1은 O, S, SO, SO2, CH2및
    로 이루어진 군에서 선택된 기이고
    {단, 식중에서, Z2는 N 또는 C이고 ; m2는 Z2가 N일 경우에는 0이고, Z2가 C일 경우에는 1이며 ; A2는 0, SO2또는 CH2이고 ; n2는 A2가 0 또는 SO2일 경우에는 0 또는 1이고, A2가 CH2일 경우에는 0 내지 3의 정수이며 ; R4는 알킬, 페닐, 치환된 페닐, 헤테로환식 고리, 치환된 헤테로환식 고리, -CO-R45및
    로 이루어진 군에서 선택된 기이고
    (여기에서, R41은 OH, 알콕시, 아미노, 아릴알킬옥시, 치환된 아미노, 아릴알켄일 및 치환된 아릴알켄일중의 어느 하나이고 ; R42는 H 또는 OH이거나, 또는 Z2가 C이고, n2가 0일 경우에는 R5와 함께 결합을 형성할 수 있으며 ; R43과 R44는 각기 페닐, 치환된 페닐, 헤테로환식 고리 또는 치환된 헤테로환식 고리이다.) ; R5는 R42와 함께 결합을 형성하지 않을 경우에는 H이다} ; Y2는 CH2또는 CO이고 ; Y3(CH|2)2또는 페닐렌이며 ; K2는 0 또는 1이다.]
  2. 제1항에 있어서, 상기한 화합물이 하기 일반식(I-1)로 표시되는 것임을 특징으로 하는 화합물.
    (단, 상기식에서 A1, R1, Y1, Y2, Y3, K1, K2및 n1은 상기에서 정의한 바와 같다.)
  3. 제1항에 있어서, 상기 식중의 R1의 퀴놀릴 또는
    인 것을 특징으로 하는 화합물.
    (단, 식중에서 R14는 H, 페닐 또는 치환된 페닐이고 ; P1은 0 내지 4의 정수이며 ; X들은 각기 Cl, F, CH3, CN 및 CH2COOH로 이루어진 군에서 선택된 기이다.)
  4. 제1항에 있어서, 상기한 화합물이 하기 일반식(I-2)로 표시되는 것임을 특징으로 하는 화합물.
    (단, 식중에서 R12, R13, Y1, Y2, Y3, K1및 K2는 상기에서 정의한 바와 같다.)
  5. 제1항에 있어서, 상기 식중의 R1이인 것을 특징으로 하는 화합물.
    [단, 식중에서 Y4는 (CH2)K3또는 CH2-Y5{여기에서, K3는 0 내지 2의 정수이고, Y5는 O, S 또는 NR5(여기에서, R5는 H 또는 CH3이다)이다}이고 ; P1은 O 내지 4의 정수이며 ; X들은 각기 Cl, F, CH3, CN 및 CH2COOH로 이루어진 군에서 선택되는 기이다.]
  6. 제1항에 있어서, 상기 식중의 R4가 피리딜, 피리미딘일, 이미다졸일, 퀴놀릴 및
    로 이루어진 군에서 선택된 기임을 특징으로 하는 화합물.
  7. 제1항에 있어서, 상기한 화합물이 하기 일반식(I-3)으로 표시되는 것임을 특징으로 하는 화합물.
    (단, 상기식에서, A1, R1, R2, R3, R43, R42, Y2, Y3, Z1, K1, K2, m1및 n|1은 상기에서 정의한 바와 같다.)
  8. 제1항에 있어서, 상기한 화합물이 하기 일반식(I-4)로 표시되는 것임을 특징으로 하는 화합물.
    (단, 상기식에서, A1, R1, R2, R3, Y1, Y2, Z1, K1, K2, m1및 n1은 상기에서 정의한 바와 같다.)
  9. 제1항에 있어서, 상기 식중의 A1이 CH2이고, R1이 카르복실기 또는 알콕시카르보닐기인 것을 특징으로 하는 화합물.
  10. 제1항에 있어서, 상기 식중의 Z1이 N이고, n1이 0인 것을 특징으로 하는 화합물.
  11. 제1항에 있어서, 상기한 Z1이 C이고, A1이 0이며, n1이 1임을 특징으로 하는 화합물.
  12. 제1항에 있어서, 상기 식중의 R1이 하기 일반식으로 표시되는 것임을 특징으로 하는 화합물.
    (단, 상기식에서, R11, R12, R13은 제1항에서 정의한 바와 같다.)
  13. 제12항에 있어서, 상기 식중의 R12와 R13이 페닐 또는 치환된 페닐인 것을 특징으로 하는 화합물.
  14. 제12항에 있어서, 상기 식중의 R12와 R13중 적어도 하나가 피리딜인 것을 특징으로 하는 화합물.
  15. 제1항에 있어서, 상기 식중의 Y3가 (CH2)2인 것을 특징으로 하는 화합물.
  16. 제15항에 있어서, 상기 식중의 Y2가 CH2이고, K2가 1인 것을 특징으로 하는 화합물.
  17. 제15항에 있어서, 상기 식중의 Y1이 S 또는 CH2이고, Y2가 CO인 것을 특징으로 하는 화합물.
  18. 제1항에 따른 화합물 또는 이의 약제학적으로 허용되는 염을 유효한 양으로 함유하는 것을 특징으로 하는 항알레르기제제.
  19. 제1항에 따른 화합물 또는 이의 약제학적으로 허용되는 염 및 담체로 이루어지는 것을 특징으로 하는 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940013326A 1993-06-14 1994-06-14 헤테로환식 고리를 함유하는 우레아 유도체 KR950000695A (ko)

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EP2655350B1 (en) 2010-12-21 2016-03-09 Agios Pharmaceuticals, Inc. Bicyclic pkm2 activators
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
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