KR940018372A - 피페라진 유도체 - Google Patents

피페라진 유도체 Download PDF

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KR940018372A
KR940018372A KR1019940001512A KR19940001512A KR940018372A KR 940018372 A KR940018372 A KR 940018372A KR 1019940001512 A KR1019940001512 A KR 1019940001512A KR 19940001512 A KR19940001512 A KR 19940001512A KR 940018372 A KR940018372 A KR 940018372A
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간테 요아힘
라다쯔 페테르
유라스지크 호르스트
베르노타트-다니엘로우스키 자비네
멜쩨르 구이도
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위르겐 호이만, 라인하르트 슈틀러
메르크 파텐트 게젤샤프트 미트 베쉬랭크터 하프퉁
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Abstract

하기 일반식(Ⅰ)의 신규 피레라진 유도체는 피브리노겐 수용체에의 피브리노겐의 결합을 억제하며 혈전증, 중풍, 심근경색, 염증, 죽상동맥경화증 및 종양의 치료에 사용될 수 있다:
Y-(CmH2m-CHR1)n-CO-(NH-CHR2-CO)r-Z (Ⅰ)

Description

피페라진 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 하기 일반식(Ⅰ)의 화합물 및 그의 염:
    Y-(CmH2m-CHR1)n-CO-(NH-CHR2-CO)r-Z (Ⅰ)
    상기식에서, Y는또는이고, Z는이거나 또는 Y가인 경우,이고, R1, R2및 R3은 각각 -CtH2t-R9, 벤질, 하이드록시벤질, 이미다졸릴메틸 또는 인돌릴메틸이고, R3는 H 또는 H1N-C(=NH)-이고, R4및 R6은 각각(H,H) 또는 =0 이고, R5는 H, H2N-C(=NH)-또는 H2N-C(=NH)-NH이고, R8은 OH, OA 또는 NHOH이고, R9는 H, OH, NH2, SH, SA, COOH, CONH2또는 NH-C(=NH)-NH2이고, A는 각 경우에 탄소원자수 1 내지 4의 알킬이고, m 및 t는 각각 0, 1, 2, 3 또는 4이고, n 및 r은 각각 0 또는 1이고, p는 0, 1 또는 2이고, 피페라진 고리는 1내지 4의 그룹 A로 치환될 수 있다.
  2. 3-(3-(4-아미디노피페라진-1-일아세트아미도)벤즈아미도)프로피온산.
  3. a)일반식(Ⅰ)의 화합물을 가용매분해제 또는 가수소분해제로 처리하여 그의 작용성 유도체중의 하나로 부터 유리시키거나 또는 b)하기 일반식(Ⅱ)의 가복실산 또는 그의 반응성 유도체중의 하나를 하기 일반식(Ⅲ)이 아미노 화합물과 반응시키거나, (c)R3또는 R5가 H2N-C(=NH)-인 일반식(Ⅰ)의 화합물을 제조하기 위하여, 라디칼 R3또는 R5대신에 CN그룹을 포함함을 제외하곤 일반식(Ⅰ)을 갖는 니트릴에 암모니아를 첨가하고, 및/또는 경우에 따라, 일반식(Ⅰ)의 카복실산(R8-OH)을 대응 에스테르(I, R8=OA)로 전환시키거나 또는 대응 하이드록삼산(I, R8=NHOH)로 전환시키고/시키거나, H원자를 아미딘-형성제로 처리하여 아미디노 그룹으로 대체하거나, 또는 일반식(Ⅰ)(R8=OA)에 에스테르를 비누화하고/하거나, 일반식(Ⅰ)의 화합물을 산 또는 염기로 처리하여 그의 염중의 하나로 전환시킴을 특징으로 하는, 일반식(Ⅰ)의 화합물 및 그의 염을 제조하는 방법.
    Y-(CmH2m-CHR1)n-CO-(NH-CHR2-CO)r-Z (Ⅰ)
    Y-(CmH2m-CHR1)n-CO-G1-OH(Ⅱ)
    H-G2(Ⅲ)
    [상기식에서, G1은 1)존재하지 않거나, 2)-NH-CHR2-CO- 또는 3)이고, G2는 1)-(NH-CHR2-CO)r-Z, 2)Z 또는 3)-NH-CpH2p-CHR7-CO-R8이고, Y는또는이고, Z는이거나 또는 Y가인 경우,이고, R1, R2및 R3은 각각 -CtH2t-R9, 벤질, 하이드록시벤질, 이미다졸릴메틸 또는 인돌릴메틸이고, R3는 H 또는 H2N-C(=NH)-이고, R4및 R6은 각각(H,H) 또는 =0 이고, R5는 H, H2N-C(=NH)-또는 H2N-C(=NH)-NH이고, R8은 OH, OA 또는 NHOH이고, R9는 H, OH, NH2, SH, SA, COOH, CONH2또는 NH-C(=NH)-NH2이고, A는 각 경우에 탄소원자수 1 내지 4의 알킬이고, m 및 t는 각각 0, 1, 2, 3 또는 4이고, n 및 r은 각각 0 또는 1이고, p는 0, 1 또는 2이고, 피페라진 고리는 1내지 4의 그룹 A로 치환될 수 있다.
  4. 제 1 항에 따른 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용가능한 염을 적어도 하나의 고체, 액체 또는 반고체의 부형제 또는 보조제와 함께 적합한 투여형으로 전환시킴을 특징으로 하는 약학적 제제의 제조방법.
  5. 적어도 하나의 제 1 항에 따른 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용가능한 염을 포함함을 특징으로 하는 약학적 제제.
  6. 약제를 제조하기 위한 제 1 항에 따른 일반식(Ⅰ)의 화합물 또는 그의 생리학적으로 허용가능한 염의 용도.
  7. 혈전증, 심근경색증, 중풍, 골다공증, 죽상동맥경화증, 염증 및/또는 종양의 치료하기 위한 제 1 항에 따른 일반식(Ⅰ)의 화합물 또는 그의 생리학적으로 허용가능한 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940001512A 1993-01-29 1994-01-28 피페라진유도체 KR100312539B1 (ko)

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DE4302485A DE4302485A1 (de) 1993-01-29 1993-01-29 Piperazinderivate
DEP4302485.8 1993-01-29

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TWI820276B (zh) 2018-12-19 2023-11-01 美商西建公司 經取代之3-((3-胺基苯基)胺基)哌啶-2,6-二酮化合物、其組合物及使用彼等之治療方法

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ATE204570T1 (de) 2001-09-15
CN1056141C (zh) 2000-09-06
DE59409833D1 (de) 2001-09-27
CZ16394A3 (en) 1994-08-17
GR3036838T3 (en) 2002-01-31
PT608759E (pt) 2002-02-28
NO312550B1 (no) 2002-05-27
EP0608759B1 (de) 2001-08-22
UA34429C2 (uk) 2001-03-15
CN1099759A (zh) 1995-03-08
SK281842B6 (sk) 2001-08-06
AU670649B2 (en) 1996-07-25
SK6894A3 (en) 1994-08-10
HUT70042A (en) 1995-09-28
NO940308D0 (no) 1994-01-28
ZA94615B (en) 1994-09-13
DE4302485A1 (de) 1994-08-04
JPH06271549A (ja) 1994-09-27
US5908843A (en) 1999-06-01
NO940308L (no) 1994-08-01
KR100312539B1 (ko) 2002-02-19
DK0608759T3 (da) 2001-12-03
EP0608759A3 (de) 1994-10-05
CA2114361A1 (en) 1994-07-30
PL302069A1 (en) 1994-08-08
RU2154639C2 (ru) 2000-08-20
HU222013B1 (hu) 2003-03-28
PL172716B1 (pl) 1997-11-28
EP0608759A2 (de) 1994-08-03
ES2162825T3 (es) 2002-01-16
AU5470294A (en) 1994-08-04
HU9400249D0 (en) 1994-05-30
CZ288122B6 (cs) 2001-04-11

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