KR970010752A - 치환아미딘유도체 또는 그 약학적으로 허용되는 염 및 그것을 함유하는 혈소판 응집저해제 - Google Patents

치환아미딘유도체 또는 그 약학적으로 허용되는 염 및 그것을 함유하는 혈소판 응집저해제 Download PDF

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KR970010752A
KR970010752A KR1019960037444A KR19960037444A KR970010752A KR 970010752 A KR970010752 A KR 970010752A KR 1019960037444 A KR1019960037444 A KR 1019960037444A KR 19960037444 A KR19960037444 A KR 19960037444A KR 970010752 A KR970010752 A KR 970010752A
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pharmaceutically acceptable
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히로유키 야미시타
쿠니오 오쿠무라
토시유키 시마자키
아키히토 카네마쯔
요지 아오키
유키 나카지마
코오헤이 야자와
켄지 키바야시
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사토 아키오
미쯔이도오아쯔가가꾸 가부시기가이샤
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    • C07C257/20—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having nitrogen atoms of amidino groups acylated
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    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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Abstract

본 발명은 강력한 혈소판응집저해작용을 가지고, 경구투여에서의 유효성에 뛰어난 신규의 화합물을 제공하는 것을 목적으로 한 것이며, 상기 신규의 화합물이 하기 일반식(1)로 표시되는 치환아미딘유도체 또는 그염 및 이 화합물을 함유하는 혈소판저해제인 것을 특징으로 한 것이다.
상기 일반식(1)로 표시되는 화합물은, 피브리노겐길항작용에 기초한 뛰어난 혈소판응집저해작용을 가지고, 특히 경구투여에서의 유효성에 뛰어나고, 혈전증, 경피경관관동맥형성시술후 또는 경피경관관동맥재개통시술후의 재협착 또는 재폐쇄의 예방 또는 치료에 유효하다.

Description

치환아미딘유도체 또는 그 약학적으로 허용되는 염 및 그것을 함유하는 혈소판응집저해제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 일반식(1)
    [식 중, A는 -CON(R1)- 또는 -N(R1)CO-(R1은 수소원자 또는 탄소수 1~4의 알킬기를 표시함)을, D2, D3은 탄소원자를 표시하고, A는 D2또는 D3에 결합해 있다. B는 -CH2- 또는 -O-를 표시하고, X는 -CH- 또는 -N-을 표시함. 단, B가 -O-일 때, X는 -N-이 아니다. Z는 수소원자 또는 치환되어 있어도 되는 알킬기를 표시함. R2, R3, R4는, 수소원자, 탄소수 1~4의 알킬기, 프로파르길기, R5O(CO)- 또는 -CH2)m-Het(R5는 탄소수 1~4의 알킬기 또는 20메톡시에틸기, m은 1 또는 2를, Het는 피리딜기, 푸릴기 또는 티에닐기를 표시함)을, 또는 R2와 R3이 결합하고, 메틸렌 사슬의 임의의 위치가 탄소수 1~4의 알킬기 또는 탄소수 1~4의 알콕시기로 치환되어도 되는 -(CH2)n-W-(CH2)p-(n 및 p는 2 또는 3을, W는 결합, 또는 -CH2-, -O-, -N(R6)- 또는 -S(O)q-를, R6은 탄소수 1~4의 알킬기, 페닐기 또는 피리딜기를, q는 0, 1 또는 2를 표시함)을 표시함, 단 R2, R3, R4중 적어도 1개는, 수소원자, 탄소수 1~4의 알킬기, R5O(CO)-이외의 기로부터 선택된다]로 표시되는 것을 특징으로 하는 치환아미딘유도체 또는 그 약학적으로 허용되는 염.
  2. 제1항에 있어서, A가 D2에 결합해 있는 것을 특징으로 하는 치환아미드유도체 또는 그 약학적으로 허용되는 염.
  3. 제1항 또는 제2항에 있어서, R2와 R3이 결합해서 -(CH2)n-W-(CH2)p-이며, W가 결합, -CH2- , -O-, -S- 또는 -N(R6)인 것을 특징으로 하는 치환아미딘유도체 또는 그 약학적으로 허용되는 염.
  4. 제1항~제3항의 어느 한 항에 있어서, A가 NHCO- 또는 -CONH-인 것을 특징으로 하는 치환아미딘유도체 또는 그 약학적으로 허용되는 염.
  5. 제1항~제4항의 어느 한 항에 있어서, X가 CH-인 것을 특징으로 하는 치환아미딘유도체 또는 그 약학적으로 허용되는 염.
  6. 제1항~제5항의 어느 한 항에 있어서, B가 -CH2-인 것을 특징으로 하는 치환아미딘유도체 또는 그 약학적으로 허용되는 염.
  7. 제1항~제5항의 어느 한 항에 있어서, B가 O인 것을 특징으로 하는 치환아미딘유도체 또는 그 약학적으로 허용되는 염.
  8. 제1항~제4항의 어느 한 항에 있어서, X가 -N-인 것을 특징으로 하는 치환아미딘유도체 또는 그 약학적으로 허용되는 염.
  9. 제1항~제8항의 어느 한 항에 기재된 화합물 또는 그 약학적으로 허용되는 염을 유효성분으로서 함유하는 것을 특징으로 하는 혈소판응집저해제.
  10. 제1항~제8항의 어느 한 항에 기재된 화합물 또는 그 약학적으로 허용되는 염의 유효량을 투여하는 것으로 이루어진 것을 특징으로 하는 혈전증을 예방 또는 치료하는 방법.
  11. 제1항~제8항의 어느 한 항에 기재된 화합물 또는 그 약학적으로 허용되는 염의 유효량을 투여하는 것으로 이루어진 것을 특징으로 하는 경피경관관동맥형성시술후 또는 경피경관관동맥재개통시술후의 재협착을 예방 또는 치료하는 방법.
  12. 제1항~제8항의 어느 한 항에 기재된 화합물 또는 그 약학적으로 허용되는 염의 유효량을 투여하는 것으로 이루어진 것을 특징으로 하는 경피경관관동맥형성시술후 또는 경피경관관동맥재개통시술후의 재폐쇄를 예방 또는 치료하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960037444A 1995-08-31 1996-08-31 치환아미딘유도체 또는 그 약학적으로 허용되는 염 및 그것을 함유하는 혈소판 응집저해제 KR100225698B1 (ko)

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TW363051B (en) * 1995-08-31 1999-07-01 Mitsui Toatsu Chemicals Substituted amidine derivatives and platelet aggregation inhibitor containing the same
US6828275B2 (en) 1998-06-23 2004-12-07 Bayer Aktiengesellschaft Synergistic insecticide mixtures
EP0892044B1 (en) * 1997-07-18 2004-12-29 Mitsui Chemicals, Inc. Esterase and its use for the production of optically active chroman compounds
TR200101744T2 (tr) 1998-12-14 2001-12-21 F. Hoffmann-La Roche Ag Fenilglisin türevleri.
CA2353151A1 (en) 1998-12-16 2000-06-22 Boehringer Ingelheim Pharma Kg Substituted aryl and heteroaryl derivatives, the preparation thereof and their use as medicaments
BR0012683A (pt) 1999-07-21 2002-04-16 American Home Prod Antagonistas bicìclicos seletivos para a integrina alfavbeta3
EP2670722B1 (en) 2011-01-31 2016-10-12 Council of Scientific & Industrial Research Chiral 1-(4-methylphenylmethyl)-5-oxo-{n-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion

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JPH08511538A (ja) * 1993-06-09 1996-12-03 スミスクライン・ビーチャム・コーポレイション 二環式フィブリノゲン拮抗物質
US5731324A (en) * 1993-07-22 1998-03-24 Eli Lilly And Company Glycoprotein IIb/IIIa antagonists
IL110172A (en) * 1993-07-22 2001-10-31 Lilly Co Eli Bicycle compounds and pharmaceuticals containing them
US5629321A (en) * 1994-10-27 1997-05-13 Mitsui Toatsu Chemicals, Inc. Bicyclic compound and platelet aggregation inhibitor containing the same
TW363051B (en) * 1995-08-31 1999-07-01 Mitsui Toatsu Chemicals Substituted amidine derivatives and platelet aggregation inhibitor containing the same

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KR100225698B1 (ko) 1999-10-15
ATE194829T1 (de) 2000-08-15
EP0760364A2 (en) 1997-03-05
NO963469L (no) 1997-03-03
NO305654B1 (no) 1999-07-05
US5719145A (en) 1998-02-17
AU686515B2 (en) 1998-02-05
NO963469D0 (no) 1996-08-21
DE69609382D1 (de) 2000-08-24
EP0760364A3 (en) 1998-07-29
DE69609382T2 (de) 2001-03-08
AU6217296A (en) 1997-05-08
CN1062266C (zh) 2001-02-21
EP0760364B1 (en) 2000-07-19
DK0760364T3 (da) 2000-10-09
CN1154962A (zh) 1997-07-23
TW363051B (en) 1999-07-01
ES2149411T3 (es) 2000-11-01

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