KR910000167A - 약제로서 유용한 하나 이상의 아미노설포닐옥시 래디칼을 지닌 화합물 - Google Patents

약제로서 유용한 하나 이상의 아미노설포닐옥시 래디칼을 지닌 화합물 Download PDF

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KR910000167A
KR910000167A KR1019900008496A KR900008496A KR910000167A KR 910000167 A KR910000167 A KR 910000167A KR 1019900008496 A KR1019900008496 A KR 1019900008496A KR 900008496 A KR900008496 A KR 900008496A KR 910000167 A KR910000167 A KR 910000167A
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ester
compound
sulfamic acid
formula
methyl
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KR1019900008496A
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노영석
쥬니어 윌리엄 죤 웰스테드
클래렌스 놀란 조셉
앨런 월쉬 데이비드
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원본미기재
에이. 에이치. 로빈스 캄파니 인코포레이티드
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Publication of KR910000167A publication Critical patent/KR910000167A/ko

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Abstract

내용 없음

Description

약제로서 유용한 하나 이상의 아미노설포닐옥시 래디칼을 지닌 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (36)

  1. 포유동물의 만성관절염 또는 골다공증의 치료 또는 예방용 약제를 제조하기 위한 일반식(I)의 화합물, 이의 약제학적으로 허용되는 염 또는 이의 광학적 이성체의 용도.
  2. (1)
  3. 상기식에서, Z는 A상에서 치환되는 동일하거나 상이한라디칼의 수로서, 적어도 하나이상이고, P는 O를 포함하여 A상의 히도록실 그룹의 수로서, 하이드록실 그룹은 A상의 적절한 위치에 존재하며, A는 아릴, 알킬, 사이클로알킬, 아릴알킬, 할로알킬, 사이클로알킬알킬, 아릴옥시알킬, 알킬옥시알킬, 아릴(저급알킬) 아미노알킬, 아릴티오알킬, 아릴설피닐알킬, 아릴설포닐알킬, 아릴아미노카보닐알킬, 알킬아미노카보닐알킬, 아릴옥시카보닐알킬, 알킬옥시카보닐알킬, 2-피롤리디논-1-알킬, 알킬카보닐알킬, 아릴카보닐알킬, 아릴알카노산, 아릴카복시알킬, 아릴할로겐 치환된 알킬, 아릴알킬옥시알킬, 아릴(알콕시카보닐)알킬, 아릴옥시(아미노카보닐옥시) 알킬, 디(아릴옥시) 알킬, 아릴옥시(할로)알킬 및 4-(디아릴메틸)피페리딘-1-일알킬에서 선택되고, A래디칼은 존재하는 특정 아릴(또는 다른 사이클릭) 또는 알킬 그룹(들)의 적절한 탄소원자(들) 상에서 아미노설포닐옥시 래디칼(들)에 의해 치환되거나,
  6. 또는와 같이 글루코스, 프락토스 또는 슈크로스 골격을 포함한 (탄수화물골격)(-)n(여기서, (-)n은 1 내지 8의 결합이다)이고, 상기의 일반식중, 적어도 하나의 결합은 그룹에 결합되며, 경우에 따라 나머지 그룹은 하이드록실에 결합되고, 아릴 또는 A를 나타내는 아릴부위는
  8. 중에서 선택되며, 상기 아릴 그룹중의 치환위치는 공환위치중 하나이고, X는 수소, 할로,, 니트로, , 저급 알콕시, 아미노, 메틸카보닐아미노, 저급알킬, 메틸옥시 카보닐, 1H-이미다졸-1-일, 3-티아졸릴, 1-피톨릴, 페닐, 1H-트리아졸-1-일, 저급알킬아미노, 시아노, 4-저급알킬-1H-이미다졸-1-일, 4-페닐-1H-이미다졸-1-일, -COOH 또는 -COOM(여기서, M은 약제학적으로 허용되는 금속 양이온, 아릴 그룹이 6내지 10개 탄소원자를 지닌 아릴옥시 또는 아로일이다)이며, Y는 수소, 할로, 저급알콕시 또는 저급알킬이고, W는 수소, 저급알콕시 또는 저급알킬이며, R7및 R8은 각각 저급알킬이고, m은 0내지 4이며, n은 1내지 8이고, q는 1내지 10이며, R은 H 또는 저급알킬이고, R2는 H, 저급알킬, -CO2H, COO저급알킬 또는 -CO2M(여기서, M은 상기 정의한 바와 같다)이다.
  9. 유효량의 일반식(I)화합물, 이의 약제학적으로 허용되는 염 또는 이의 광학적 이성체 및 약제학적으로 허용되는 담체를 함유함을 특징으로 하는, 포유동물의 만성관절염 또는 골다공증의 치료용 약제 조성물.
  10. (I)
  11. 상기식에서, p,z,A,R1및 R2는 제1항에서 정의한 바와 같다.
  12. 만성관절염 또는 공다공증의 치료제로서 사용하기 위한 제1항에 따른 일반식(I)의 화합물 또는 이의 약제학적으로 허용되는 염 또는 이의 광학적 이성체.
  13. [단, (i) A는가 아니고, (ii) p가 0일 때 Z가 1이고, A가 아
  14. 릴부분이 일반식아릴알킬이다].
  15. 일반식(II)의 화합물,
  16. (II)
  17. 상기식에서, A1은 하나이상의 탄소원자 상에서 아미노설포닐옥시 라디칼에 의해 치환되고 아릴옥시알킬, 알킬(여기서, 아미노설포닐옥시 라디칼중 적어도 하나는 3급 탄소원자상에 위치한다), 아릴옥시, 카보닐알킬, 알킬옥시카보닐알킬, 알킬카보닐알킬, 아릴카보닐알킬, 4-페닐-티아디아졸-3-일, 2-피콜리돈-1-알킬 및 탄수화물(여기서, 탄수화물은 자당핵, 글루코즈핵 또는 프락토즈핵이며, 아릴옥시 알킬, 아릴옥시카보닐알킬 또는 아릴카보닐알킬의 아릴잔기는 제1항에서 정의된 아릴이다)로 이루어진 그룹준에서 선택되며, W, X, Y, R1,R2, p 및 제1항에서 정의한 바와 같다.
  18. 제1항 내지 4항중 어느 한 항에 있어서, A또는 A1이 하기 일반식인 용도, 조성물 또는 화합물.
  20. 상기식에서, a는 0 또는 1이고, b는 0,1,2,3 또는 4이고, c는 0 또는 1이고, d는 0 또는 1이며, 단, c가 0일 때 d는 0이고, p는 0 또는 1이며, 단 p+d는 2가 아니고, R10및 R11은 각각, 수소, 하이드록시, 메톡시 염소, 브롬, 메틸 또는 1-이미다졸릴이며, 아미노설포닐옥시 그룹은 p또는 d가 0일 때 자유원자에 결합한다.
  21. 제1항 내지 5항중 어느 한 항에 있어서, R1및 R2가 수소, 메틸, 에틸, 이소프로필, 메톡시 카보닐, 에톡시카보닐 및 이소프로필카보닐로 이루어진 그룹중에서 선택되는 OSO2NR1R2그룹중 적어도 하나를 함유하는 화합물, 용도 또는 조성물.
  22. 제1항 내지 4항중 어느 한 항에 있어서, 일반식(I)또는 (II)의 화합물이 하기 그룹중 하나인 화합물, 용도 또는 조성물; 1-[(2-메톡시페녹시)메틸]-1, 2-에탄디올 비스 설파메이트(에스테르), 1-[(2-메톡시페녹시)메틸]-1, 3-에탄디올 비스 (메틸 설파메이트)(에스테르), 3-페녹시-1, 2-프로판디올 비스 설파메이트(에스테르), 2-페녹시-1, 3-프로판디올 디설파메이트(에스테르), 3-(4-클로로페녹시)-1, 2-프로판디올 디설파메이트 에스테르, 설팜산 페닐 에스테르, 2-(4-클로로페녹시)에탄올 설파메이트 에스테르, 메틸설팜산 페닐에스테르, 에틸 설팜산 2-[[(에틸아미노)설포닐]옥시]-3-(2-메톡시페녹시)프로필 에스테르, 에틸 설팜산2-[[(에틸아미노)설포닐]옥시]-3-페녹시프로필 에스테르, (1-메틸에틸)설팜산 2-[[[(1-메틸에틸)아미노]설포닐]옥시-3-페녹시프로필에스테르, 메틸 설팜산 3-페녹시-1, 2-프로판디일 에스테르, 설팜산2-[4-(1H-이미다졸-1-일)페녹시]에틸 에스테르 또는 이의 약제학적으로 허용되는 염, 메틸 설팜산 2-[4-(1H-이미다졸-1-일)페녹시]에틸 에스테르 또는 이의 약제학적으로 허용되는 염, (S)-(-)-설팜산2-[(아미노설포닐)옥시]-3-(2-메톡시페녹시)프로필에스테르 (S)-(+)-설팜산 2[(아미노설포닐)옥시)-3-(2-메톡시 페녹시)프로필 에스테르 또는 이의 약제학적으로 허용되는 염, 디메틸설팜산 페닐에스테르, 또는 설팜산 3-요오도페닐 에스테르.
  23. 제1항 내지 4항중 어느 한 항에 있어서, 일반식(I)또는 (II)의 화합물이 하기 그룹중 하나만 화합물, 용도 또는 조성물;2-페녹시에탄올 설파메이크(에스테르), 1,7-헵타디올 비스설파메이트(에스테르), 3-페녹시-1-프로판올 설파메이트(에스테르), 벤젠프로판올 설파메이트(에스테르), 2-(4-클로로페녹시)에탄올 설파메이트 에스테르, 3-페녹시-2-프로판올 설파메이트 에스테르, 2-페녹시프로판올 설파메이트(에스테르), 2-(3,4-디클로로페녹시)에탄올 설파메이트(에스테르), 3-페녹시-1-부탄올 설파메이트(에스테르), 3-(2-메톡시페녹시)-1, 2-프로판디올과의 디메틸 설팜산 디에스테르, 설팜산 2-(3-피리디닐옥시) 에틸 에스테르 하이드로클로라이드, 설팜산 4-(1H-이미다졸-1-일)페닐 에스테르, (1-메틸에틸)-설팜산 페닐 에스테르, 설팜산(3,4-디클로로페닐) 에스테르, 에틸 설팜산 페닐 에스테르, 설팜산 2-(4-메틸-5-티아졸릴)에틸에스테르, 메틸 설팜산 2-페녹시-1, 3-프로판디일 에스테르, 메틸 설팜산 3-(2-하이드록시페녹시)-2-[[(메틸아미노)설포닐]옥시]프로필 에스테르 또는 (S)-(-)-메틸-설팜산3-(2-메톡시페녹시)-2-[[(메틸 아미노)-설포닐]옥시]프로필 에스테르.
  24. 일반식 (X)의 반응물 몰을 약 1 내지 20%의 3급 아민 염기가 함유된 비양성자 용매중, 약 50 내지 200℃의 온도에서, 일반식(Q)의 하이드록시 치환된 화합물과 반응시켜 보호된 카복시, 보호된 아미노 및 보호된 하이드록시 치환체를 갖거나 갖지 않는 설팜산 유도체의 유리염기 형태를 생성하고, 필요한 경우, R3를 수소로 전환시키며 보호된 카복시, 보호된 아미노 또는 보호된 하이드록시 치환체가 설팜산 유도체의 A2그룹상에 존재할 때 이들을 탈보호시키고, 제1항의 일반식(I)의 염기성 또는 산성 화합물을 설팜산 유도체의 약제학적으로 허용되는 염으로 전환시킴을 특징으로 하여, 제1항의 일반식(I)의 화합물을 제조하는 방법.
  26. 상기식에서, Ar은 비간섭 라디칼을 갖는 아릴 그룹이고, R1은 H 또는 저급알킬이며, R2는 H, 저급알킬 또는 -COOR3이고, R3는 저급알킬 또는 페닐 저급알킬이며, A2는 상기 A에서 정의한 바와 같고, 단, A2가 아릴일 때, 보호된 카복시, 보호된 아미노 또는 보호된 하이드록시 그룹이 치환되며, 보호된 하이드록시는 (OH)n(여기서, n은 z+p'이고, p'는 0을 포함한 비반응 하이드록시 그룹의 수이며, z는 설파메이트 에스테르화된 하이드록시 그룹의 수이다)으로부터 제외된다.
  27. (a) 일반식(III)의 화합물을 일반식(IV)의 화합물과 반응시키고, 필요한 경우, R3를 수소로 전환시키며 모든 보호된 치환체를 탈보호시켜 제4항의 일반식(II)의 화합물을 생성하거나, (b)일반식(III)의 화합물을 클로로설포닐 이소시아네이트와 반응시키고 (i)물로 처리하며, 필요한 경우, 모든 치환체 그룹을 탈보호시켜 R1및 R2가 모두 수소인 제4항의 일반식(II)의 화합물을 생성하거나, (ii)R3OH(R3는 저급알킬 또는 페닐 저급알킬이다)의 알코올로 처리하며, 필요한 경우, 모든 보호그룹을 탈보호시키고 R3를 수소로 전환시켜 R1이 수소이고 R2가 COOH또는 -COO저급알킬인 제4항의 일반식(II)의 화합물을 생성하거나; (c)제4항의 일반식(II)의 염기성 또는 생성 화합물을 약제학적으로 허용되는 염으로 전환시킴을 특징으로 하여, 제4항에 따른 일반식(II)의 화합물을 제조하는 방법.
  29. 상기식에서, A3는 제4항에서 정의한 A1또는 치환체 그룹이 필요에 따라 보호된 잔기를 나타내며, n은 하나이상의 하이드록시 그룹을 나타내고, R1은 수소, 저급알킬 또는 COOR6(여기서, R3는 저급알킬 또는 페닐 저급알킬이다)이다.
  30. 제4항에 있어서, 1-[(2-메톡시페녹시)메틸]-1, 2-에탄디올 비스 설파메이트 에스테르인 화합물.
  31. 제4항에 있어서, 1-[(2-메톡시페녹시)메틸]-1, 2-에탄디올 비스(메틸 설파메이트) 에스테르인 화합물.
  32. 제4항에 있어서, 설팜산 2-[4-(1H-이미다졸-1-일)페녹시]에틸 에스테르 또는 이의 약제학적으로 허용되는 염인 화합물.
  33. 제4항에 있어서, 메틸 설팜산 2-[4-(1H-이미다졸-1-일)페녹시]에틸 에스테르 또는 이의 약제학적으로 허용되는 염인 화합물.
  34. 제4항에 있어서, (S)-(-)설팜산2-[(아미노설포닐)옥시]-3-(2-메톡시페녹시)프로필에스테르인 화합물.
  35. 제4항에 있어서, (S)-(+)설팜산2-[(아미노 설포닐)옥시]-3-(2-메톡시페녹시)프로필 에스테르인 화합물.
  36. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900008496A 1989-06-12 1990-06-11 약제로서 유용한 하나 이상의 아미노설포닐옥시 래디칼을 지닌 화합물 KR910000167A (ko)

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JP (1) JPH0347162A (ko)
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JP4347696B2 (ja) * 2001-12-21 2009-10-21 ステリックス リミティド アルコール及びフェノールのスルファモイル化のための産業的適用方法
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EP0403185A3 (en) 1992-12-16
JPH0347162A (ja) 1991-02-28
PT94305A (pt) 1991-02-08
AU5700090A (en) 1990-12-13
CA2018700A1 (en) 1990-12-12
AU645975B2 (en) 1994-02-03
EP0403185A2 (en) 1990-12-19
PT94305B (pt) 1997-02-28

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