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KR930017881A - 술폰아미드 엔도텔린 길항제 - Google Patents

술폰아미드 엔도텔린 길항제 Download PDF

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KR930017881A
KR930017881A KR1019930002492A KR930002492A KR930017881A KR 930017881 A KR930017881 A KR 930017881A KR 1019930002492 A KR1019930002492 A KR 1019930002492A KR 930002492 A KR930002492 A KR 930002492A KR 930017881 A KR930017881 A KR 930017881A
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디. 스테인 필립
티. 헌트 존
무루게산 나테산
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니콜라스 피. 말라테스티닉
이이.아르.스퀴브 앤드 산즈, 인크.
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Abstract

본 발명은 엔도텔린을 억제하는 하기 일반식의 화합물에 관한 것이다.
상기 식에서, X및 Y중의 하나는 N이고, 다른 하나는 O이고, R은 나프틸 또는 R1,R2및 R3으로 치환된 나프틸이고, R1,R2및 R3은 각각 독립적으로 수소, Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬, 할로, 히드록실, 시아노, 니트로, -C(O)H,-C(O)R6,CO2H,-CO2R6,-SH,-S(O)nR6,-S(O)m-OH,-S(O)m-OR6,-O-S(O)m-R6,-O-S(O)mOH,-O-S-(O)-m-OR6,-Z4-NR7R8,또는 -Z4-N(R11)-Z5-NR9R10이고, R4및 R5는 각각 독립적으로 수소, Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬, 할로, 히드록실, 시아노, 니트로, -C(O)H,-C(O)R6,CO2H,-CO2R6,-SH,-S(O)nR6,-S(O)m-OH,-S(O)m-OR6,-O-S(O)m-R6,-O-S(O)mOH,-O-S-(O)-m-OR6,-Z4-NR7R8,또는 -Z4-N(R11)-Z5-NR9R10이거나, 또는 R4및R5는 함께 그들이 결합된 탄소 원자와 함께 4내지 8원 포화, 불포화, 또는 방향족 고리를 완성하고, Z1,Z2및 Z3으로 치환될 수 있는, 알킬렌 또는 알케닐렌이고, 여기에서, R6,R7,R8,R9,R10,R11,Z6,Z7,Z9, m및 n은 상기 정의한 바와 같다.

Description

술폰아미드 엔도텔린 길항제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (20)

  1. 하기 일반식의 화합물 또는 제약상 허용되는 그의 염.
    상기 식에서, X및 Y중의 하나는 N이고, 다른 하나는 O이고, R은 나프틸 또는 R1,R2및 R3으로 치환된 나프틸이고, R1,R2및 R3은 각각 독립적으로, (a)수소, (b)Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬, (c)할로, (d)히드록실, (e)시아노, (f)니트로, (g)-C(O)H또는-C(O)R6, (h)CO2H,-CO2R|6,(i)-SH,-S(O)n-R6,-S(O)m-OH,-S(O)m-R6,-O-S(O)m-R|6,-S(O)mOH또는-S-(O)m-OR6,-Z4-NR7R|8,또는 (k)-Z4-N(R11)-Z5-NR9R10이고, R4및 R5는 각각 독립적으로 (a)수소, (b)Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬, (c)할로, (d)히드록실, (e)시아노, (f)니트로, (g)-C(O)H 또는-C(O)R6,(h)CO2H또는-CO2R6,(i)-SH,-S(O)|n-R6,-S(O)m-OH,-S(O)m-OR6,-O-S(O)m-R6,-O-S(O)mOH 또는-S(O)|m-OR6,(j)-Z4-NR7R8또는 (k)-Z4-N(R11)-Z5-NR9R10이거나, 또는 (1)R4및R5는 함께 그들이 결합된 탄소 원자와 함께 4내지 8원 포화, 불포화, 또는 방향족 고리를 완성하는 Z1,Z2및 Z3으로 치환될 수 있는 알킬렌 또는 알케닐렌이고, R6은Z1,Z2및Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴, 또는 아랄킬이고, R7은, (a)수소, (b)Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬, (c)시아노, (d)히드록실, (e)-C(O)H 또는-C(O)R6,(f)CO2H또는-CO2R6,또는(g)-SH,-S(O)nR6,-S(O)m-OH,-S(O)m-OR6,-O-S(O)m-R6,-O-S(O)mOH 또는-0-S(O)m-OR6이고,(단,Z4가 -S(0)m-인 경우는 제외함),R8은, (a)수소, (b)-C(O)H 또는C(O)R6(단, Z4가 -C(O)-이고, R7이 -C(O)H, -C(O)R6,-CO|2H 또는 -CO2R6인 경우는 제외함),또는 (c) Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬이거나, 또는 R7및R8은 함께 그들이 결합된 질소 원자와 함께 3내지 8원 포화, 불포화 또는 방향족 고리를 완성하는 Z1,Z2및 Z3으로 치환될 수 있는 알킬렌 또는 알케닐렌이고, R9는, (a)수소, (b)히드록실, (c)-C(O)H 또는-C(O)R6,(d)-CO2H또는-CO2R6,(e)-SH,-S(O)n-R6,-S(O)m-OH,-S(O)m-OR|6,-O-S(O)m-R6,-O-S(O)mOH 또는-S(O)m-OR6,
    또는 (f) Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬이고,R10은, (a)수소,(b)-C(O)H 또는 -C(O)R6(단, Z5가 -C(O)-이고, R9가-C(O)H,-C(O)R|6,-CO2H 또는 CO2R6인 경우는 제외함),또는 (c)Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬이고,R11은, (a)수소,(b)히드록실, -CO2R6또는 CO|2H(단, R9및R10중의 하나가 히드록실, CO2R6또는CO2H인 경우는 제외함),(c) -C(O)H 또는-C(O)R6,또는 (d) Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 알콕시, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬이거나, R9,R10및 R11중의 임의의 2개는 함께 그들이 결합된 원자들과 함께 3내지 8원 포화, 불포화 또는 방향족 고리를 완성하는, Z1,Z2및 Z3으로 치환될 수 있는 알킬렌 또는 알케닐렌이고, Z1,Z2및 Z3은 각각 독립적으로, (a)수소,(b)할로, (c)히드록시, (d)알콕시, (e)-SH, -S(O)nZ6,-S(O)m-OH,-S(O)m-OZ6,-O-S(O)|m-Z6,-O-S(O)mOH또는-S(O)m-OZ6,(f)옥소,(g)니트로,(h)시아노,(i)-C(O)H 또는 -C(O)Z6,(j)-CO|2H또는CO2Z6, 또는(k)-NZ7Z8,-C(O)NZ7Z8또는-S(O)nZ7Z|8이고, Z4및Z5는 각각 독립적으로, (a)단일결합, (b)-S(O)n-,(c)-C(O)-,(d)-C(S)또는(e)Z1,Z2및 Z3으로 치환될 수 있는, 알킬, 알케닐, 알키닐, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬이고,Z6,Z7및 Z8은 각각 독립적으로 수소,알킬, 알케닐, 알키닐, 시클로알킬, 시클로알킬알킬, 시클로알케닐, 시클로알케닐알킬, 아릴 또는 아랄킬이거나, 또는 Z7및 Z8은 함께 그들이 결합된 질소 원자와 함께 3내지 8원 포호, 불포화 도는 방향족 고리를 완성하는 알킬렌 또는 알케닐이고, m은 1또는 2이고,n은 0,1또는 2이다.
  2. 제1항에 있어서, R1,R2및 R3중의 하나가 -NR7R8인 화합물,
  3. 제2항에 있어서, R7및 R8이 각각 독립적으로 수소, 알킬, 또는 C(O)알킬인 화합물.
  4. 제1항에 있어서, R이이고, 여기에서, 1또는 2위치에는 술폰아미드가 결합되고, 5또는 6위치에는 R1,R2및 R3중의 하나가 결합된 화합물.
  5. 제4항에 있어서, R1,R2및 R3중의 하나가 -NR6R8인 화합물.
  6. 제5항에 있어서, R7및 R8이 각각 독립적으로 수소,알킬 또는 C(O)알킬인 화합물.
  7. 제6항에 있어서, R7및 R8이 각각 독립적으로 수소, 메틸, 메틸에틸 또는 아세틸인 화합물.
  8. 제1항에 있어서, 하기 식을 갖는 화합물.
  9. 제8항에 있어서, R7및 R8이 각각 독립적으로 수소,알킬 또는 C(O)알킬인 화합물.
  10. 제9항에 있어서, R7및 R8이 각각 독립적으로 수소, 메틸, 메틸에틸 또는 아세틸인 화합물.
  11. 제1항에 있어서, R4및 R5가 알킬인 화합물.
  12. 제4항에 있어서, R4및 R5가 알킬인 화합물.
  13. 제1항에 있어서, R4및 R5가 메틸인 화합물.
  14. 제4항에 있어서, R4및 R5가 메틸인 화합물.
  15. 제1항에 있어서, 5-(디메틸아미노)-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,N-[5-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-1-나프탈레닐]아세트아미드, 5-아미노-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,N-[6-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-1-나프탈레닐]아세트아미드,5-아미노-N-(3,4-디메틸-5-이속사졸릴)-2-나프탈렌술폰아미드,N-[4-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-1-나프탈레닐]아세트아미드,N-[6-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-2-나프탈레닐]아세트아미드,6-아미노-N-(3,4-디메틸-5-이속사졸릴)-2-나프탈렌술폰아미드,4-아미노-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,5-디메틸아미노-N-(4,5-디메틸-3-이속사졸릴)-1-나프탈렌술폰아미드,N-[5-[[(4,5-디메틸-3-이속사졸릴)아미노]술포닐]-1-나프탈레닐]아세트아미드,N-[5-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-2-나프탈레닐]아세트아미드,N-[8-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-2-나프탈레닐]아세트아미드,N-[7-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-2-나프탈레닐]아세트아미드,N-[7-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-1-나프탈레닐]아세트아미드,N-(3,4-디메틸-5-이속사졸릴)-5-메톡시-1-나프탈렌술폰아미드,N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,5-[(1-메틸에틸)아미노]-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,N-[5-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-1-나프탈레닐]-2-메틸프로판아미드,5-클로로-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,N-(3,4-디메틸-5-이속사졸릴)-5-[(페닐메틸)아미노]-1-나프탈렌술폰아미드,N-(3,4-디메틸-5-이속사졸릴)-5-히드록시-1-나프탈렌술폰아미드,7-(디메틸아미노)-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,N-(3,4-디메틸-5-이속사졸릴)-5-[메틸(1-메틸에틸)-아미노]-1-나프탈렌술폰아미드,2-[[5-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-1-나프탈레닐]아미노]프로판산, 에틸 에스테르, N-(3,4-디메틸-5-이속사졸릴-5-(2-옥소-1-피롤리디닐)-1-나프탈렌술폰아미드,N-(3,4-디메틸-5-이속사졸릴)-5-(2-옥소-1-피페리디닐)-1-나프탈렌술폰아미드,N-(3,4-디메틸-5-이속사졸릴)-5-[[(페닐아미노)-티옥소메틸]아미노]-1-나프탈렌술폰아미드,N-(3,4-디메틸-5-이속사졸릴)-5-(1-피롤리디닐)-1-나프탈렌술폰아미드,5-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-1-나프탈렌카르복실산,5-[[[5-(디메틸아미노)-1-나프탈레닐]술포닐]아미노]-3-메틸-4-이속사졸카르복실산,에틸 에스테르,5-[[(3,4-디메틸-5-이속사졸릴)아미노]술포닐]-1-나프탈렌카르복실산,메틸 에스테르,5-(디메틸아미노)-N-(3-메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,5-[(디메틸아미노)메틸]-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,트리플루오로아세테이트(1:1)염,N-(3,4-디메틸-5-이속사졸릴)-5-(1-히드록시-1-메틸에틸)-1-나프탈렌술폰아미드,N-(3,4-디메틸-5-이속사졸릴)-5-(1-메틸에테닐)-1-나프탈렌술폰아미드, N-(3,4,-디메틸-5-이속사졸릴-5-(1-피페리디닐)-1-나프탈렌술폰아미드.트리플루오로아세테이트(2;1) 염, N-(3,4-디메틸-5-이속사졸릴)-5-(메틸아미노)-1-나프탈렌술폰아디므, N-(3,4-디메틸-5-이속사졸릴)-5-(에틸아미노)-1-나프탈렌술폰아미드, N-(3-메틸-4-페닐메틸-5-이속사졸릴)-5-[디메틸아미노]-1-나프탈렌술폰아미드, N-(3-메틸-4-페닐-5-이속사졸릴)-5-(디메틸아미노)-1-나프탈렌술폰아미드,N-(3-에틸-4-메틸-5-이속사졸릴)-5-(디메틸아미노)-1나프탈렌술폰아미드,5-(디부틸아미노)-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,일나트륨염, 4-[1-[[(3,4-디메틸-5-이속사졸릴]아미노]술포닐]나프탈렌-5-일]아미노]부탄산, 6-아미노-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,7-아미노-N-(3,4-디메틸-5-이속사졸릴)-2-나프탈렌술폰아미드,8-아미노-N-(3,4-디메틸-5-이속사졸릴)-2-나프탈렌술폰아미드,7-아미노-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,7-(디메틸아미노)-N-(3,4-디메틸-5-이속사졸릴)-2-나프탈렌술폰아미드,8-(디메틸아미노-N-(3,4-디메틸-5-이속사졸릴)-2-나프탈렌술폰아미드,6-(디메틸아미노)-N-(3,4-디메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,5-(디메틸아미노)-N-(3-메틸-4-니트로-5-이속사졸릴)-1-나프탈렌술폰아미드,5-(디메틸아미노)-N-(4,5,6,7-테트라히드로-2,1-벤즈이속사졸릴-3-일)-1-나프탈렌술폰아미드,5-(디메틸아미노)-N-(4-에틸-3-메틸-5-이속사졸릴)-1-나프탈렌술폰아미드,및 5-(디메틸아니노)-N-(4-메틸-5-이속사졸릴)-1-나프탈렌술폰아미드로 이루어진 군 중에서 선택된 화합물.
  16. 유효량의 제1항에 따른 화합물을 투여하는 것으로 이루어진 포유류에 있어서 엔도텔린 관련 질환을 치료하는 방법.
  17. 유효량의 제1항에 따른 화합물을 투여하는 것으로 이루어진 고혈압을 치료하는 방법.
  18. 유효량의 제1항에 따른 화합물을 투여하는 것으로 이루어진 신장, 시구체 또는 사구체 간질 세포 관련 질환을 치료하는 방법.
  19. 유효량의 제1항에 따른 화합물을 투여하는 것으로 이루어진 내독소혈병을 치료하는 방법.
  20. 유효량의 제1항에 따른 화합물을 투여하는 것으로 이루어진 빈혈을 치료하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930002492A 1992-02-24 1993-02-23 술폰아미드 엔도텔린 길항제 Expired - Fee Related KR100257134B1 (ko)

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KR100257134B1 (ko) 2000-05-15
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ZA93780B (en) 1993-09-08
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CA2089184A1 (en) 1993-08-25
TW224462B (ko) 1994-06-01
JPH069585A (ja) 1994-01-18
AU3319293A (en) 1993-08-26
GR3024203T3 (en) 1997-10-31
FI930774L (fi) 1993-08-25
CY2045B1 (en) 1998-04-30
ATE152713T1 (de) 1997-05-15
IL104748A0 (en) 1993-06-10
EP0558258B1 (en) 1997-05-07
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PL172035B1 (pl) 1997-07-31
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AU651922B2 (en) 1994-08-04
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RU2116301C1 (ru) 1998-07-27
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NZ245905A (en) 1995-07-26
PH30795A (en) 1997-10-17
MY109004A (en) 1996-11-30
HU219455B (hu) 2001-04-28
FI930774A0 (fi) 1993-02-22
PL297820A1 (en) 1993-09-06
JP3273818B2 (ja) 2002-04-15
CN1079468A (zh) 1993-12-15
DE69310414D1 (de) 1997-06-12
NO930633D0 (no) 1993-02-23
NO303012B1 (no) 1998-05-18
DE69310414T2 (de) 1997-12-11
ES2103061T3 (es) 1997-08-16
HU9300491D0 (en) 1993-05-28
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HUT65762A (en) 1994-07-28

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