KR950701321A - 신규의 치환된 3급 아미노 화합물의 또는 이의 염(Novel substituted tertiary amino compound or salt thereof) - Google Patents

신규의 치환된 3급 아미노 화합물의 또는 이의 염(Novel substituted tertiary amino compound or salt thereof)

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KR950701321A
KR950701321A KR1019940703846A KR19940703846A KR950701321A KR 950701321 A KR950701321 A KR 950701321A KR 1019940703846 A KR1019940703846 A KR 1019940703846A KR 19940703846 A KR19940703846 A KR 19940703846A KR 950701321 A KR950701321 A KR 950701321A
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미노루 오카다
도루 요덴
에이지 가와미나미
요시아키 시마다
마사후미 구도
야스오 이소무라
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오노다 마사요시
야마노우치세이야쿠 가부시키가이샤
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Abstract

본 발명은 일반식(Ⅰ)의 치환된 3급 아미노 화합물 또는 약제학적으로 허용되는 이의 염에 관한 것이다. 이 화합물의 아로마타제 억제 활성을 가지며, 유방암, 유선증, 자궁내막증, 전립선 비대 등의 예방제 및/또는 치료제로서 유용하다.

Description

신규의 치환된 3급 아미노 화합물 또는 이의 염(Novel substituted tertiary amino compound or salt thereof)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 일반식(Ⅰ)의 치환된 3급 아미노 화합물 또는 약제학적으로 허용되는 이의 염.
    상기식에서, A는 단일 결합, 저급 알킬렌 그룹 또는 일반식의 그룹(여기서, n은 1 내지 6의 정수이고, X는 산소원자, 황원자 또는 CH2의 그룹이다)이고, 환 B는 피리미딘 환, 피리다진 환 또는 트리아진 환이고, 환 D 및 E는 동일하거나 상이할 수 있으며, 각각 치환되거나 치환되지 않은 아릴 그룹, 질소 원자, 산소 원자 및 황 원자 중에서 선택된 헤테로 원자 1 내지 3개를 함유하는 치환되거나 치환되지 않은 5- 또는 6-원 헤테로사이클릭 그룹, 또는 벤진 환과 축합된 헤테로사이클릭 그룹으로 이루어지는 치환되거나 치환되지 않은 비사이클릭 축합 헤테로사이클릭 그룹이며, 단, 환 D 및 E는 둘다 벤젠 환이며, 이들중 하나는 치환기를 갖는다.
  2. 제1항에 있어서, 환 D 및 E가 동일하거나 상이할 수 있으며, 각각 벤젠 환, 나프탈렌 환, 안트라센 환, 페난트렌 환, 푸란 환, 티오펜 환, 티아졸 환, 티아디아졸 환, 옥사졸 환, 이미다졸 환, 트리아졸 환, 피롤 환, 피리딘 환, 피리미딘 환, 피라진 환, 벤조티아졸 환, 벤즈옥사졸 환, 퀴놀린 환, 이소퀴놀린 환, 벤조트리아졸 환 또는 벤조푸라잔 환인 화합물 또는 약제학적으로 허용되는 이의 염.
  3. 제2항에 있어서, 환 D 및 E가 동일하거나 상이할 수 있으며, 각각 벤젠 환, 피리딘 환, 티아졸 환 또는 푸라진 환인 화합물 또는 약제학적으로 허용되는 이의 염.
  4. 제2항에 있어서, 환 D 또는 환 E상의 치환기 하나 이상이, 동일하거나 상이하며, 할로겐 원자, 시아노 그룹, 시아노-저급 알킬 그룹, 니트로 그룹, 트리플루오로메틸 그룹, 하이드록실 그룹, 아미노 그룹, 모노- 또는 디-저급 알킬아미노 그룹, 저급 알킬 그룹, 저급 알콕시 그룹, 카복실 그룹, 저급 알콕시카보닐 그룹, 저급 알카노일 그룹, 저급 알카노일옥시 그룹, 저급 알카노일아미노 그룹, 아로일 그룹, 아로일옥시 그룹, 카바모일 그룹, 또는 모노- 또는 디-저급 알킬설파모일 그룹인 화합물 또는 약제학적으로 허용되는 이의 염.
  5. 제4항에 있어서, 환 D 또는 환 E상의 치환기 하나 이상이 동일하거나 상이하며, 할로겐 원자, 시아노 그룹, 시아노-저급 알킬 그룹, 니트로 그룹, 트리플루오로메틸 그룹, 하이드록실 그룹, 아미노 그룹, 저급 알킬 그룹, 저급 알킬설포닐 그룹, 저급 알콕시 그룹, 카복실 그룹, 저급 알콕시카보닐 그룹, 저급 알카노일 그룹 또는 저급 알카노일아미노 그룹인 화합물 또는 약제학적으로 허용되는 이의 염.
  6. 제4항에 있어서, 환 D 또는 환 E상의 치환기 하나 이상이 동일하거나 상이하며, 할로겐 원자, 시아노 그룹 또는 니트로 그룹인 화합물 또는 약제학적으로 허용되는 이의 염.
  7. 제5항에 있어서, A가 저급 알킬렌 그룹인 화합물 또는 약제학적으로 허용되는 이의 염.
  8. 제5항에 있어서, 환 B가 피리미딘 환인 화합물 또는 약제학적으로 허용되는 이의 염.
  9. 제1항에 있어서, A가 저급 알킬렌 그룹이고, 환 B가 피리미딘 환이며, 환 D 및 E가, 동일하거나 상이하며, 각각 벤젠 환, 피리딘 환, 티아졸 환 또는 푸라잔 환이고, 환 D 또는 환 E 상의 치환기가, 동일하거나 상이하며, 각각 할로겐 원자, 시아노 그룹 또는 니트로 그룹인 화합물 또는 약제학적으로 허용되는 이의 염.
  10. 제9항에 있어서, 환 D 및 환 E가 각각 벤젠 환이고, 환 D 또는 환 E 상의 치환기가 각각 할로겐 원자, 시아노 그룹 또는 니트로 그룹인 화합물 또는 약제학적으로 허용되는 이의 염.
  11. 5-[N-(4-시아노페닐)-N-(3, 5-디플루오로벤질)아미노] 피리미딘 또는 약제학적으로 허용되는 이의 염.
  12. 제1항 내지 제11항 중의 어느 한 항에 기술된 화합물 또는 이들의 염 및 약제학적으로 허용되는 담체를 포함하는 약제학적 조성물.
  13. 제1항 내지 제11항 중의 어느 한 항에 기술된 화합물 또는 이의 염을 활성 성분으로서 포함하는 아로마타제 억제제.
  14. 제1항 내지 제11항 중의 어느 한 항에 기술된 화합물 또는 이의 염을 활성 성분으로서 포함하는 유방암, 유선증, 자궁내막증 또는 전립선 비대 치료제.
  15. 제1항 내지 제11항 중의 어느 한 항에 기술된 화합물 또는 이의 염을 활성 성분으로서 포함하는 유방암 또는 자궁내막증 치료제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940703846A 1992-04-28 1993-04-27 신규의 치환된 3급 아미노 화합물 또는 이의 염 KR0163624B1 (ko)

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Application Number Priority Date Filing Date Title
JP13776292 1992-04-28
JP92-137762 1992-04-28
JPWP92-137762GH 1992-04-28
JPWP92-234298GH 1992-08-10
JP92-234298 1992-08-10
JP23429892 1992-08-10
PCT/JP1993/000548 WO1993022290A1 (en) 1992-04-28 1993-04-27 Novel substituted tertiary amino compound or salt thereof

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KR950701321A true KR950701321A (ko) 1995-03-23
KR0163624B1 KR0163624B1 (ko) 1998-12-01

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US (1) US5538976A (ko)
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AT (1) ATE178056T1 (ko)
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WO1999057131A1 (en) * 1998-05-06 1999-11-11 Duke University Method of treating bladder and lower urinary tract syndromes
MXPA02010564A (es) * 2000-04-28 2003-03-10 Hoffmann La Roche Heteroarilos y p-(sulfonil)-arilos.
GB0120147D0 (en) * 2001-08-17 2001-10-10 Metris Therapeutics Ltd Treatment method
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EP0640595B1 (en) 1999-03-24
WO1993022290A1 (en) 1993-11-11
CN1079962A (zh) 1993-12-29
DE69324141T2 (de) 1999-08-26
AU4023093A (en) 1993-11-29
US5538976A (en) 1996-07-23
GR3030472T3 (en) 1999-10-29
TW345577B (en) 1998-11-21
DE69324141D1 (de) 1999-04-29
JP2682741B2 (ja) 1997-11-26
CA2118138A1 (en) 1993-10-29
DK0640595T3 (da) 1999-10-11
KR0163624B1 (ko) 1998-12-01
ATE178056T1 (de) 1999-04-15
EP0640595A1 (en) 1995-03-01
EP0640595A4 (en) 1995-04-12
ES2130258T3 (es) 1999-07-01
CN1039228C (zh) 1998-07-22

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