KR950000145A - 혈당저하제 - Google Patents

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KR950000145A
KR950000145A KR1019940014148A KR19940014148A KR950000145A KR 950000145 A KR950000145 A KR 950000145A KR 1019940014148 A KR1019940014148 A KR 1019940014148A KR 19940014148 A KR19940014148 A KR 19940014148A KR 950000145 A KR950000145 A KR 950000145A
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hydrogen
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조셉 쿨리넌 조지
티.옌 테렌스
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피터 지.스트링거
일라이 릴리 앤드 캄파니
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Abstract

본 발명은 항에스트로겐 화합물 및 그의 약학적으로 허용가능한 염 및 용매화물을 투여하므로써 포유동물의 과혈당중을 치료하는 방법을 제공한다.

Description

혈당저하제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 혈당 농도를 감소시키는데 사용하기 위한, 1) 트리아릴에틸렌; 2) 2,3-디아릴-2H-1-벤조피란; 3) 1-아미노알킬-2-페닐인돌; 4) 2-페닐-3-아로일벤조티오펜; 5) 1-치환된-2-아릴디하이드로나프탈렌; 및 6) 벤조푸란 및 그의 약학적으로 허용가능한 염 및 용매화물로부터 선택된 항에스트로겐 화합물.
  2. 제1항에 있어서, 상기 항에스트로겐이 하기 일반식(Ⅰ),(Ⅱ) 또는 (Ⅲ)을 갖는 트리아릴에틸렌 및 그의 약학적으로 허용가능한 염 및 용매화물인 화합물:
    상기식에서, R은 일반식 -OCnH2nA (여기서, n은 2,3 또는 4이고 A는 알킬기가 1 내지 4개의 탄소원자를 포함하는 디알킬아미노 기이거나 또는 N-피페리디닐, N-피롤리디닐, N-헥사메틸렌이미노 및 N-모르폴리닐 그룹으로부터 선택되는 사이클릭 구조이다)의 염기성 에테르기이고; R1은 각각 독립적으로 수소, 하이드록시, 할로겐 또는 메톡시이고; X는 할로겐이고; R2및 R3는 독립적으로 수소 및 메틸로부터 선택되고; R4는 이소프로필, 이소프로펜-2-일, 또는 모노 또는 디하이드록시 이소프로필이고; R5는 하이드록시 또는 포스페이트(-OPO3H2)이다.
  3. 제1항에 있어서, 상기 항에스트로겐이 2,3-디아릴-2H-1-벤조피란 및 그의 약학적으로 허용가능한 염 및 용매화물인 화합물.
  4. 제3항에 있어서, 상기 2,3-디아릴-2H-1-벤조피란이 하기의 일반식(Ⅳ)을 갖는 화합물 및 그의 약학적으로 허용가능한 염 및 용매화합물인 화합물;
    상기식에서 R6및 R7은 동일하거나 또는 서로 다르며, 수소, 하이드록시, C1-C17알콕시 또는 C2-C18알콕시카보닐이고; R8은이다.
  5. 제1항에 있어서, 상기 항에스트로겐이 하기 일반식(Ⅴ)을 갖는 1-아미노알킬-2-페닐인돌 및 그의 약학적으로 허용가능한 염 및 용매화물인 화합물:
    상기식에서, R9는 수소 또는 메틸이고; R10및 R11은 메톡시 또는 하이드록시이고; m은 4 내지 8이고; Y는 NR12R13(여기서, R12및 R13은 독립적으로 수소, 메틸 및 에틸중에서 선택되거나 또는 R12및 R13중의 하나가 수소이고 다른 하나는 벤질이거나, 또는 이들이 결합된 질소원자와 함께 피롤리디닐, 피페리디닐 또는 모르폴리닐 기를 형성한다)이다.
  6. 제1항에 있어서, 상기 항에스트로겐이 하기 일반식(Ⅵ)을 갖는 2-페닐-3-아로일벤즈[b]티오펜 및 그의 약학적으로 허용가능한 염 및 용매화물인 화합물;
    상기식에서, R16는 수소, 하이드록시, R1-C5알콕시, C1-C7알카노일옥시, C3-C7사이클로알카노일옥시, (C1-C7알콕시)-C1-C7알카노일옥시, 치환되거나 또는 비치환된 아로일옥시, 또는 치환되거나 또는 비치환된 아릴옥시카보닐옥시이고; R17은 수소, 하이드록시, C1-C5알콕시, 이다만토일옥시, 클로로, 브로모, C1-C7알카노일옥시, C3-C7사이클로알카노일옥시, (C1-C8알콕시)-C1-C7알카노일옥시, 치환되거나 또는 비치환된 아로일옥시, 또는 치환되거나 또는 비치환된 아릴옥시카보닐옥시이고; R18은 -O-CH2-CH2-X'-NR19R20(여기서, X'는 결합 또는 -CH2-이고, R19및 R20은 독립적으로 C1-C4알킬이거나 또는 이들이 결합된 질소원자와 함께 피롤리디닐, 피페리디닐, 헥사메틸렌이미닐 또는 모르폴리닐 고리를 형성한다)이다.
  7. 제6항에 있어서, 상기 2-페닐-3-아로일벤조[b]티오펜이 [6-하이드록시-2-(4-하이드록시페닐)벤조[b]티엔-3-일][4-[2-(1-피페리디닐)-에톡시]페닐]메타논 및 그의 약학적으로 허용가능한 염 및 용매화물인 화합물.
  8. 제6항에 있어서, 상기 2-페닐-3-아로일벤조[b]티오펜이 [6-하이드록시-2-(4-하이드록시페닐)벤조[b]티엔-3-일][4-[2-(1-피롤리디닐)에톡시]페닐]메타논 및 그의 약학적으로 허용가능한 염 및 용매화물인 화합물.
  9. 제1항에 있어서, 상기 항에스트로겐이 하기 일반식(Ⅶ) 또는 (Ⅷ)을 갖는 1-치환된-2-아릴-디하이드로나프탈렌 및 그의 약학적으로 허용가능한 염 및 용매화물인 화합물:
    상기식에서, Z는 -CH2-CH2- 또는 -CH=CH-이고; R16은 수소, 하이드록시 또는 C1-C3알콕시이고; R17은 수소, 하이드록시, C1-C5알콕시, C1-C5아릴옥시, C1-C5알콕시카보닐옥시, 벤질옥시, 아다만토일옥시, 클로로 또는 브로모이고; R18은 C1-C5알콕시 또는 -O-CH2-CH2-NR19R20(여기서, R19및 R20의 독립적으로 C1-C4알킬이거나 또는 이들이 결합된 질소원자와 함께 피롤리디닐, 피페리디닐, 헥사메틸렌이미노 또는 모르폴리닐 고리를 형성한다)이나, 단, R17이 수소이며, R16은 수소, 하이드록시 또는 C1-C5알콕시이고 R16및 R17중의 적어도 하나는 수소가 아니고; R19및 R20은 C1-C8알킬 또는 이들이 결합된 질소원자와 함게 피롤리디닐, 2-메틸피롤리디닐, 2,2-디메틸피롤리디닐, 피페라지닐, 4-메틸피페라지닐, 2,4-디메틸피페라지닐, 모르폴리닐, 피페리디닐, 2-메틸피페리디닐, 3-메틸피페리디닐, 헥사메틸렌이미닐, 호모피페라지닐 및 호모모르폴리닐로부터 선택된 5 내지 7원의 포화된 헤테로 사이클릭 라디칼을 형성하고; q는 2 내지 6이고; p는 1 내지 4이고; R21은 C1-C8알콕시이다.
  10. 제1항에 있어서, 상기 항에스트로겐이 하기 일반식(Ⅸ)의 2-치환된-3-아릴-벤조푸란 및 그의 약학적으로 허용 가능한 염 및 용매화물인 화합물 :
    상기식에서, X2는 할로이고; Y2는 결합 또는 -CH2-이고; R22는 수소 또는 메틸이고; R23은 -NR19R20(여기서, R19및 R20은 독립적으로 C1-C4알킬이거나 또는 이들이 결합된 질소원자와 함께 피롤리디닐, 피페리디닐, 헥사메틸렌이미닐 또는 모르폴리닐 고리를 형성한다)이다.
  11. 인간의 혈당 농도를 감소시키는데 사용하기위한, 제1항 내지 제10항중 어느 한 항에서 정의된 항에스트로겐 화합물을 포함하는 약학 제형.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940014148A 1993-06-24 1994-06-22 혈당저하제 KR100325034B1 (ko)

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IL110052A0 (en) 1994-10-07
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AU669627B2 (en) 1996-06-13
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PH30490A (en) 1997-05-28
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US5567713A (en) 1996-10-22
CN1100933A (zh) 1995-04-05
RU94022479A (ru) 1997-03-20
DE69405491D1 (de) 1997-10-16
EP0635264A3 (en) 1995-04-12
ES2105525T3 (es) 1997-10-16
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JP2886453B2 (ja) 1999-04-26
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TW275584B (ko) 1996-05-11
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ATE157869T1 (de) 1997-09-15
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DE69405491T2 (de) 1998-02-19

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