KR920000778A - 비스포스폰산 유도체, 그의 제조와 용도 - Google Patents

비스포스폰산 유도체, 그의 제조와 용도 Download PDF

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KR920000778A
KR920000778A KR1019910010616A KR910010616A KR920000778A KR 920000778 A KR920000778 A KR 920000778A KR 1019910010616 A KR1019910010616 A KR 1019910010616A KR 910010616 A KR910010616 A KR 910010616A KR 920000778 A KR920000778 A KR 920000778A
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다까시 소다
이와오 야마자끼
노리야끼 가와무라
시게히사 다께또미
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우메모또 요시마사
다께다야꾸힝고오교 가부시끼가이샤
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Abstract

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Description

비스포스폰산 유도체, 그의 제조와 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 하기 일반식(I)의 비스포스폰산 유도체 또는 그것의 염:
    (식중, A는 임의로 치환된 고리기이고, R1은 수소원자 또는 저급 알카노일기이며, R2, R3, R4및 R5는 같거나 다르고, 수소원자 또는 저급알킬기이며, m은 0,1 또는 2이며, n은 2-10의 정수이다.)
  2. 제1항에 있어서, 임의로 치환된 고리기의 고리기는 C6-14방향족 탄화수소기, 1-4개의 헤테로원자를 함유하는 5 또는 6원 방향족 헤테로고리기, C6-14방향족 탄화수소고리 또는 1-4개의 질소, 산소 및/또는 황원자를 함유하는 5 또는 6원 방향족 헤테로고리와 공역된 1-4개의 질소, 산소 및/또는 황원자를 함유하는 5 또는 6원 방향족 헤테로고리기, C3-7시클로알킬기, 또는 1-4개의 헤테로원자들을 함유하는 5 또는 6원 비-방향족 헤테로 고리기이며, 이들 고리기는 (1)할로겐원자, (2)니트로, (3)할로겐원자, 히드록시기 및 C1-6알콕시기로 구성되는 군에서 선택된 1-3개의 치환체로 치환될수 있는 C1-7알킬기, (4)할로겐 원자, 히드록시기 및 C1-6알콕시기로 구성되는 군에서 선택된 1-3개의 치환체로 치환될 수 있는 C3-7시클로알킬기, (5)히드록실, (6)할로겐, 히드록실 및 C1-6알콕시기로 구성되는 군에서 선택된 1-3개의 치환체로 치환될 수 있는 C1-6알콕시기, C4-6시클로알콕시기, C2-6알켄일옥시, C6-19아랄킬옥시, C2-7알카노일옥시 및 C6-14아릴옥시로 구성되는 군에서 선택된 보호된 히드록시기, (7)티올 및 (8)할로겐, 히드록시기 및 C1-6알콕시기로 구성되는 군에서 선택되는 1-3개의 치환체로 치환될 수 있는 C1-6알킬티오, C4-7시클로알킬티오, C7-19아랄킬티오 및 C2-7알카노일 티오기로 구성되는 군에서 선택되는 보호된 티올기의 군에서 선택되는 1-4개의 치환체로 임의로 치환된 것임을 특징으로 하는 화합물.
  3. 제1항에 있어서, R1으로 표시되는 저급알카노일이 C1-6알킬-카르보닐기인 화합물.
  4. 제1항에 있어서, R2, R3, R4및 R5로 표시되는 저급 알킬기가 C1-4알킬기인 화합물.
  5. 제1항에 있어서, A가 페닐기인 화합물.
  6. 제1항에 있어서, A는 피리딜기인 화합물.
  7. 제1항에 있어서, 4-(페닐티오)부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬에스테르인 화합물.
  8. 제1항에 있어서, 4-(페닐티오)부틸아미노메틸렌비스폰스폰산인 화합물.
  9. 제1항에 있어서, 4-(2-피리딜티오)부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬에스테르기인 화합물.
  10. 제1항에 있어서, 4-(2-피리딜티오)부틸아미노메틸렌비스포스폰산인 화합물.
  11. 제1항에 있어서, 4-[(4-메톡시페닐)티오)부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬 에스테르기인 화합물.
  12. 제1항에 있어서, 4-[(1-메틸-1,2,3,4-테트라졸-5-일)티오]부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬에스테르기인 화합물.
  13. 제1항에 있어서, 4-[(2-티아졸일)티오]부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬에스테르기인 화합물.
  14. 일반식(Ⅱ)의 아민유도체를 일반식(Ⅲ)의 오르토포름산 유도체 및 일반식(Ⅳ)의 포스파이트 유도체와 반응시킨 다음, 임의로 아실화, 산화 및/또는 가수분해 시키는 것을 특징으로 하는 하기 일반식(I)의 화합물의 제조방법.
    (식중, A는 임의로 치환된 고리기이고, R1은 수소원자 또는 저급 알카노일기이며, R2, R3, R4및 R5는 같거나 다르고, 수소원자 또는 저급알킬기이며, m은 0,1 또는 2이며, n은 2-10의 정수이며, R6는 저급 알킬기이고, R7, R8, R9및 R10은 같거나 다르며 저급 알킬기이다.)
  15. 하기 일반식(I)의 화합물 또는 그것의 염, 그리고 약학적 허용가능한 담체, 희석제 또는 부형제를 함유하는 골-재흡수억제 조성물.
    (식중, A는 임의로 치환된 고리기이고, R1은 수소원자 또는 저급 알카노일기이며, R2, R3, R4및 R5는 같거나 다르고, 수소원자 또는 저급알킬기이며, m은 0,1 또는 2이며, n은 2-10의 정수이다.)
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910010616A 1990-06-25 1991-06-25 비스포스폰산 유도체, 그의 제조와 용도 KR920000778A (ko)

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JP16760090 1990-06-25
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NO912462L (no) 1991-12-27
US5512552A (en) 1996-04-30
AU7928791A (en) 1992-01-02
CA2045293A1 (en) 1991-12-26
ATE127123T1 (de) 1995-09-15
FI913067A0 (fi) 1991-06-24
EP0464509A1 (en) 1992-01-08
DE69112511D1 (de) 1995-10-05
DE69112511T2 (de) 1996-02-08
US5376647A (en) 1994-12-27
EP0464509B1 (en) 1995-08-30
HUT57787A (en) 1991-12-30
NO912462D0 (no) 1991-06-24
FI913067A (fi) 1991-12-26
IE912115A1 (en) 1992-01-01
AU637508B2 (en) 1993-05-27
CN1057654A (zh) 1992-01-08
JP3072390B2 (ja) 2000-07-31
JPH05294979A (ja) 1993-11-09

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