KR940000433A - 신규 피라졸 유도체, 그의 제조방법 및 그를 함유하는 제약학적 조성물 - Google Patents

신규 피라졸 유도체, 그의 제조방법 및 그를 함유하는 제약학적 조성물 Download PDF

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KR940000433A
KR940000433A KR1019930011510A KR930011510A KR940000433A KR 940000433 A KR940000433 A KR 940000433A KR 1019930011510 A KR1019930011510 A KR 1019930011510A KR 930011510 A KR930011510 A KR 930011510A KR 940000433 A KR940000433 A KR 940000433A
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바르뜨 프랑시스
까젤라 비에르
꽁쥐 크리스띠앙
마르띠네 세르쥐
리날디 무리에르
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Abstract

본 발명은 하기 구조식 (Ⅰ)의 신규 피라졸 유도체, 그의 제조방법 및 그를 함유하는 제약학적 조성물에 관한 것이다.
〔상기식에서, -g2,g3,g4,g5및 g6과 w2, w3,w4,w5및 w6은 동일하거나 상이하며 독립적으로 수소, 염소 또는 브롬원자, (C1∼C3)-알킬, (C1∼C3)-알콕시, 트리플루오르메틸 또는 니트로기이고, g4는 페닐기일 수 있고, -R4는 수소 또는 (C1∼C3)-알킬이고, -X는 직접 결합 또는 기-(CH2)XN(R3)-이고, 여기에서 R3는 수소 또는 (C1∼C3)-알킬이고 x는 0 또는 1이고, -R은 -기-NR1R2(여기에서 R1및 R2는 독립적으로 (C1∼C3)-알킬, 치환될 수 있는 비 -방향족 (C3∼C15) 카르보시클릭 라디칼; 아미노가 (C1∼C3)-알킬에 의해 이 치환될 수 있는 아미노 (C1∼C4)-알킬기, 시클로알킬이 C3∼C12인 시클로알킬 -(C1∼C3)-알킬에 의해 이 치환될 수 있는 아미노 (C1∼C4)-알킬기, 시클로알킬이 C3∼C12인 시클로알킬 -(C1∼C3)-알킬, 비치환되거나 할로겐, (C1∼C3)-알킬 또는 (C1∼C5)-알콕시에 의해 일치환 또는 다치환된 페닐, 페닐 (C1∼C3)-알킬, 디페닐-(C1∼C3)-알킬, 나프틸, 안트라세닐, 비치환되거나 (C1∼C3)-알킬, 히드록실 또는 벤질기에 의해 치환된 포화 5- 내지 8- 원 복소환 라디칼, 1-아다만틸메틸, 비치환되거나 할로겐, (C1∼C5) 알킬, (C1∼C5)-알콕시에 의해 일- 또는 다치환된 방향족 복소환, 비치환되거나, 할로겐, (C1∼C5) 알킬, (C1∼C5)-알콕시에 의해 일- 또는 다치환된 방향족 복소환에 의해 치환된 (C1∼C3)-알킬이거나, R1은 수소이고, R2는 상기한 바와 같거나, R1및 R2는 그들이 결합되는 질소원자와 함께 포화 5-내지 8-원 복소환 라디칼을 형성하고, 이 복소환 라디칼은, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6이 모두 수소일때 모르폴린 이외의 것이다), -X가 (CH2)XN(R3)-일때 상기한 바와 같은 R2, 또는 -X가 직접 결합일 때 기 R5(여기에서 R5는 (C1∼C3)-알킬, 비치환되거나 (C1∼C5)-알킬에 의해 치환된 (C3∼C12)-시클로알킬, 비치환되거나 할로겐 또는 (C1∼C3)-알킬에 의해 치환된 페닐 -(C1∼C3)-알킬, 시클로알킬이 C3∼C12이고 비치환되거나 (C1∼C5)-알킬에 의해 치환된 시클로알킬 -(C1∼C5)-알킬 또는 2-노르보르닐메틸이다).이다〕

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신규 피라졸 유도체, 그의 제조방법 및 그를 함유하는 제약학적 조성물
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Claims (18)

  1. 하기 구조식(Ⅰ)의 화합물 또는 적절하다면 그의 염,
    〔상기식에서, -g2,g3,g4,g5및 g6과 w2, w3,w4,w5및 w6은 동일하거나 상이하며 독립적으로 수소, 염소 또는 브롬원자, (C1∼C3)-알킬, (C1∼C3)-알콕시, 트리플루오르메틸 또는 니트로기이고, g4는 페닐기일 수 있고, -R4는 수소 또는 (C1∼C3)-알킬이고, -X는 직접 결합 또는 기-(CH2)XN(R3)-이고, 여기에서 R3는 수소 또는 (C1∼C3)-알킬이고 x는 0 또는 1이고, -R은 -기-NR1R2(여기에서 R1및 R2는 독립적으로 (C1∼C3)-알킬, 치환될 수 있는 비 -방향족 (C3∼C15) 카르보시클릭 라디칼; 아미노가 (C1∼C3)-알킬에 의해 이 치환될 수 있는 아미노 (C1∼C4)-알킬기, 시클로알킬이 C3∼C12인 시클로알킬 -(C1∼C3)-알킬, 비치환되거나 할로겐, (C1∼C3)-알킬 또는 (C1∼C5)-알콕시에 의해 일치환 또는 다치환된 페닐, 페닐 (C1∼C3)-알킬, 디페닐-(C1∼C3)-알킬, 나프틸, 안트라세닐, 비환되거나 (C1∼C3)-알킬, 히드록실 또는 벤질기에 의해 치환된 포화 5- 내지 8- 원 복소환 라디칼, 1-아다만틸메틸, 비치환되거나 할로겐, (C1∼C5) 알킬, (C1∼C5)-알콕시에 의해 일- 또는 다치환된 방향족 복소환, 비치환되거나, 할로겐, (C1∼C5) 알킬, (C1∼C5)-알콕시에 의해 일- 또는 다치환된 방향족 복소환에 의해 치환된 (C1∼C3) 알킬이거나, R1은 수소이고, R2는 상기한 바와 같거나, R1및 R2는 그들이 결합되는 질소원자와 함께 포화 5-내지 8-원 복소환 라디칼을 형성하고, 이 복소환 라디칼은, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6이 모두 수소일때 모르폴린 이외의 것이다), -X가 (CH2)XN(R3)-일때 상기한 바와 같은 R2, 또는 -X가 직접 결할일 때 기 R5(여기에서 R5는 (C1∼C3)-알킬, 비치환되거나 (C1∼C5)-알킬에 의해 치환된 (C3∼C12)-시클로알킬, 비치환되거나 할로겐 또는 (C1∼C3)-알킬에 의해 치환된 페닐 -(C1∼C3)-알킬, 시클로알킬이 C3∼C12이고 비치환되거나 (C1∼C5)-알킬에 의해 치환된 시클로알킬 -(C1∼C5)-알킬 또는 2-노르보르닐메틸이다).이다〕
  2. 제1항에 있어서, 하기 구조식(Ia′)인 화합물 또는 그의 염.
    〔상기식에서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R4는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같고, R1은 수소 또는 (C1∼C8)-알킬이고, R2는 비방향족 (C3∼C15)카르보시클릭 라디칼 또는 1-피롤리디닐, 1-피페리디닐, 1-헥사히드로아제피닐, 4-모르폴리닐 및 4-티오모르폴리닐로 부터 선택된 포화 5- 내지 8-원 복소환 라디칼이다.〕
  3. 제1항에 있어서, 하기 구조식 (i)인 화합물 또는 그의 염,
    〔상기 식에서, R4및 X 및 R은 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다.〕
  4. 제3항에 있어서, R4가 수소 또는 메틸기인 구조식 (i)인 화합물 또는 그의 염.
  5. 제3항에 있어서, R4는 수소 또는 메틸이고, X는 직접 결합인 구조식(i)인 화합물 또는 그의 염.
  6. 제3항에 있어서, R4는 수소 또는 메틸이고, X는 직접 결합이고 R은 Rl이 수소 또는 메틸기이고 R2는 비-방향족 (C3∼C15)카르보시클릭 라디칼 또는 1-피롤리디닐, 1-피페리디닐, 1-헥사히드로아제피닐, 4-모르폴리닐 및 4-티오모르폴리닐로 부터 선택된 포화 5- 내지 8-원 복소환 라디칼인 기 NR1R2인 구조식(i)인 화합물 또는 그의 염.
  7. 제3항에 있어서, R4는 수소 또는 메틸이고, X는 -(CH2)2-N(R3)-이고, R은 -기-NR1R2이며, 여기에서 x는 0 또는 1이고, R3은 수소이며, R3는 수소 또는 메틸기이고 R2는 하나 또는 두개의 할로겐원자, (C1∼C5)-알킬기 또는 (C1∼C5)-알콕시기에 의해 치환된 페닐기 또는 비방향족 C3∼C15카르보시클릭 라디칼 구조식(i)인 화합물 또는 그의 염.
  8. 제1항에 있어서, 하기 구조식(ⅱ)인 화합물 또는 그의 염.
    〔상기 식에서, X 및 R은 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같고 w4는 메틸 또는 메톡시기이다.〕
  9. 제8항에 있어서, w4는 메틸 또는 메톡시기이고, X는 직접 결합이고 R은 R1이 수소 또는 메틸기이고, R2는 비-방향족 C3∼C15카르보시클릭 라디칼기-NR1R2인 구조식(ⅱ)인 화합물 또는 그의 염.
  10. 제8항에 있어서, w4는 메틸 또는 메톡시기이고, X는 -(CH2)2-N(R3)-이며, 여기에서 x는 0 또는 1이고, R3는 수소 또는 메틸기이고 R은 R1이 수소이고, R2는 비치환되거나 하나 또는 두개의 할로겐원자, (C1∼C4)-알킬기 또는 (C1∼C4)-알콕시기에 의해 치환된 페닐 또는 비-방향족 C3∼C15카르보시클릭 라디칼인 -NR1R2인 구조식(ⅱ)인 화합물 또는 그의 염.
  11. 제1항에 있어서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R4및 X가 제1항에 정의한 바와 같고 R은 R1이 수소 또는 (C1∼C8)-알킬이고, R2는 2- 또는 3-인돌릴-(C1∼C3)-알킬기 또는 2- 또는 3-인돌릴기인 기 -NR1R2인 구조식(Ⅰ)인 화합물 또는 그의 염.
  12. 제1항에 있어서, 하기 구조식(ⅲ)인 화합물 또는 그의 염.
    〔상기 식에서, X가 제1항에 정의한 바와 같고, R은 R1이 수소 또는 (C1∼C6)-알킬이고, R2는 2- 또는 3-인돌릴-(C1∼C3)-알킬기 또는 2- 또는 3-인돌릴기인 기 -NR1R2이고, w2는 수소이고 w4는 메틸 또는 메톡시기이거나 w2및 w4는 염소원자이다〕
  13. 제1항에 있어서, 하기 구조식(ⅳ)인 화합물 또는 그의 염.
    〔상기 식에서, X 및 R은 제1항에 정의한 바와 같고, g4는 브롬 원자 또는 메틸 또는 트리플루오로메틸기이다.〕
  14. 하기 구조식(Ⅱa)의 피라졸-3-카르복실산 유도체 또는 그의 활성형 중 하나, 즉 그의 에스테르 또는 산 염화물 중 하나;
    〔상기 식에서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R4는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다〕를 -구조식 NHR1R2(여기에서, R1및 R2는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다)의 아민과 반응시켜 하기 구조식(Ia)의 아미드 :
    〔상기 식에서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R4는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다〕를 수득하거나, -또는 임의적으로 일차 아민 R1NH2(여기에서, R3는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다)와 반응시켜 하기 구조식(Ⅴ)의 중간체 아미드 :
    〔상기 식에서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R4및 R3는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다.〕를 수득하거나, 금속 수소화물과의 환원에 의해 하기 구조식(Ⅵ)의 중간체 아민 :
    〔상기 식에서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R4및 R3는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다〕를 수득하고, 각각 구조식 R2COCl(여기에서, R2는 상기 구조식(Ⅰ)에 정의한 바와 같다)의 산 염화물 또는 구조식 R2-N=C=O(여기에서, R2는 상기(Ⅰ)에 정의한 바와 같다)의 이소시아네이트와의 반응에 의해 하기 구조식(Ib) 또는 (Ic)의 아미드 또는 우레아 :
    〔상기 식에서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R2, R3및 R4는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다〕로 전환시키거나, -염기성 매질내에서의 디페닐포스포릴 아지도 유도체와 반응시킨 후에 알콜 매질내에서 산 처리하여, 하기 구조식(Ⅶ)의 중간체 아민 :
    〔상기 식에서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R4는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같다〕을 수득하고, 이를 산염화물 R2COCl 또는 이소시아네이트 R2-N=C=O와 반응시켜 각각 하기 구조식(Id) 및 (Ie)의 아미드 및 우레아 :
    〔상기 식들에서, w2, w3,w4,w5및 w6과 g2,g3,g4,g5및 g6과 R4는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같고 R3는 수소이다.〕를 수득하거나, R3가 수소가 아닌 구조식 (Id) 및 (Ie)의 화합물은 상기 1차 아민(Ⅶ)를 하기 구조식(Ⅶb)의 2차 아민 :
    〔상기 식에서, w2, w3,w4,w5및 w6, g2,g3,g4,g5및 g6과 R4는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같고 R'3는 (C1∼C2)-알킬이다〕으로 전환시키고, 이를 산 염화물 R2COCl 또는 이소시아네이트 R2-N=C=O와 반응시켜 R3가 수소가 아닌 상기 정의한 바와 같은 구조식 (Id) 및 (Ie)의 아미드 및 우레아를 수득하거나 : -유기 망간 시약 R5MnX1(여기에서, R5는 제1항의 상기 구조식(Ⅰ)에 정의한 바와 같고 X1은 할로겐이다)와 반응시켜서, 하기 구조식(If)의 케톤 유도체 :
    를 수득하고, 생성 화합물을 적절하다면 염으로 전환시킬 수 있는 제1항에 따른 구조식(Ⅰ)의 화합물의 제조방법.
  15. 하기 구조식(Ⅱ′a) 또는 (Ⅱ′b)의 화합물.
    〔상기 식에서, R4는 제1항에 정의한 바와 같고 Alk는 (C1∼C5)-알킬이다.〕
  16. 제1항 내지 제13항중 어느 한 항에 따른 구조식(Ⅰ)의 화합물을 활성 성분으로 함유하는 제약학적 조성물.
  17. 제16항에 있어서, 활성 성분이 1종 이상의 제약학적 부형제와 혼합된 투여단의 형태인 제약학적 조성물.
  18. 제17항에 있어서, 2.5 내지 1000㎎의 활성 성분을 함유하는 제약학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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MY113022A (en) 2001-11-30
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FI113169B (fi) 2004-03-15
AU4143893A (en) 1994-01-06
IL106099A (en) 1998-07-15
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JP3238801B2 (ja) 2001-12-17
CZ289487B6 (cs) 2002-02-13
RU2119917C1 (ru) 1998-10-10
ATE149489T1 (de) 1997-03-15
UA27728C2 (uk) 2000-10-16
AU664281B2 (en) 1995-11-09
EP0576357B1 (fr) 1997-03-05
DE69308395D1 (de) 1997-04-10
GR3023535T3 (en) 1997-08-29
JPH0673014A (ja) 1994-03-15
IL120517A0 (en) 1997-07-13
NO932296L (no) 1993-12-27
CA2098944C (en) 1999-09-07
FR2692575B1 (fr) 1995-06-30
NZ247961A (en) 1995-08-28
MX9303664A (es) 1994-01-31
IL106099A0 (en) 1993-10-20
DK0576357T3 (da) 1997-09-15
HU222577B1 (hu) 2003-08-28
HUT64526A (en) 1994-01-28
US5624941A (en) 1997-04-29
HU218797B (hu) 2000-12-28
ZA934511B (en) 1994-02-22
NO932296D0 (no) 1993-06-22
BR1100409A (pt) 1999-10-13
TW494096B (en) 2002-07-11
CA2098944A1 (en) 1993-12-24
FR2692575A1 (fr) 1993-12-24
NO302819B1 (no) 1998-04-27
DE69308395T2 (de) 1997-10-16
ES2101258T3 (es) 1997-07-01
HU9301851D0 (en) 1993-09-28
BR9302435A (pt) 1994-01-11
SK283399B6 (sk) 2003-07-01
EP0576357A1 (fr) 1993-12-29
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