KR870008842A - N-[2-{[(2- 히드록시 페닐)(페닐)메틸렌]아미노}에틸]아세트아미드 유도체, 그의 제법 및 치료에의 응용 - Google Patents

N-[2-{[(2- 히드록시 페닐)(페닐)메틸렌]아미노}에틸]아세트아미드 유도체, 그의 제법 및 치료에의 응용 Download PDF

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KR870008842A
KR870008842A KR870002176A KR870002176A KR870008842A KR 870008842 A KR870008842 A KR 870008842A KR 870002176 A KR870002176 A KR 870002176A KR 870002176 A KR870002176 A KR 870002176A KR 870008842 A KR870008842 A KR 870008842A
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piperazinyl
piperidyl
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halogen atom
atom
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꼬마트몽 쟉끄
뤼르셀 토마스
자르드 리디아
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에뚜레 레메뜨르
신떼라보 소시에떼 아노님
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Publication of KR870008842A publication Critical patent/KR870008842A/ko

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/52Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
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    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/26Oxygen atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

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Abstract

내용 없음

Description

N-[2-{[(2-히드록시페닐)(페닐)메틸렌]아미노}에틸]아세트아미드 유도체, 그의 제법 및 치료에의 응용
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 일반식(Ⅰ)에 해당하는 것을 특징으로 하는 순수한 광학 이성질체 또는 공학 이성질체의 혼합물 형태의 화합물, 뿐만 아니라 약리적으로 허용되는 산과의 그의 부과염.
    상기식에서,
    A와 B는 각각 수소원자를 나타내거나 또는 다르게는 함께 탄소-질소 결합을 나타내며,
    X1은 수소 또는 할로겐원자 또는(C1-C4) 알킬기를 나타내고,
    X2는 수소 또는 할로겐원자 또는 메틸기를 나타내며,
    X3는 수소 또는 할로겐원자 또는 히드록실기를 나타내고,
    X4는 수소 또는 할로겐원자를 나타내며,
    X5는 수소 또는 할로겐원자 또는 메틸 또는(C1-C4) 알킬술포닐기, 또는 할로겐원자 또는 메톡시기로 임의적으로 파라 치환된 벤질술포닐기를 나타내고,
    R은 1-모르폴리닐, 4-히드록시-1-피페리딜, 4-아미노 카르보닐-1-피페리딜, 4-히드록시-4-페닐-1-피페리딜, 4-(1-피페리딜)-1-피페리딜, 4-(2-옥소-1-벤조이미다졸리닐)-1-피페리딜, 1-피페라지닐, 4-메틸-1-피페라지닐, 4-에톡시카르보닐-1-피페라지닐, 4-페닐-1-피페라지닐, 4-클로로페닐-1-피페라지닐, 4-메틸페닐-1-피페라지닐, 또는4-(2-피리딜)-1-피페라지닐기를 나타낸다.
  2. 제 1 항에 있어서, A와 B는 함께 탄소-질소결합을 나타내고 R은 4-히드록시 피페리딜기를 나타내는 것을 특징으로 하는 화합물.
  3. 제 1 항과 제 2 항 중 어느 하나에 있어서, X1,X4및 X5는 각각 수소원자를 나타내고, X2는 염소원자 또는 메틸기를 나타내며,
    X3는 염소원자를 나타내는 것을 특징으로 하는 화합물.
  4. 일반식(Ⅱ)
    (여기서 X1,X2,X3,X4및 X5는 제 1 항에 기재된 바와 같다)의 벤조페논을 클로로포름과 같은 용매에서 및 환류온도에서 과량의 에틸렌 디아민과 반응시킨 다음, 얻은 화합물을 실온에서 염기의 존재하에 염화 2-클로로 아세틸과 반응시키고,
    다음에, 일반식(Ⅲ)
    의 얻은 화합물을 실온에서 또는 온화하게 가열하면서 저급알코올과 같은 용매에서 및 임의적으로 염기의 존재하에 일반식 RH(여기서 R은 제 1 항에 정의한 바와 같다)의 아민과 반응시키며, 만일 일반식(Ⅰ)에서, A와 B가 각각 수소원자를 나타낸다면 얻은 화합물을 실온에서 및 저급알코올과 같은 용매에서 알칼리금속의 수소화 붕소화물에 의해 환원시키는 것을 특징으로 하는 제 1 항에 정의된 화합물의 제조방법.
  5. 제 1 항 내지 제 3 항 중 어느 하나에 따르는 화합물로 구성되는 것을 특징으로 하는 의약 조성물.
  6. 제 1 항 내지 제 3 항 중 어느 하나에 따르는 화합물을 제약부형제와 조합하여 포함하는 것을 특징으로 하는 제약 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR870002176A 1986-03-12 1987-03-11 N-[2-{[(2- 히드록시 페닐)(페닐)메틸렌]아미노}에틸]아세트아미드 유도체, 그의 제법 및 치료에의 응용 KR870008842A (ko)

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FR86.03489 1986-03-12
FR8603489A FR2595695B1 (fr) 1986-03-12 1986-03-12 Derives de n-(((hydroxy-2 phenyl) (phenyl) methylene) amino-2) ethyl) acetamide, leur preparation et leur application en therapeutique

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EP (1) EP0239461A1 (ko)
JP (1) JPS62230767A (ko)
KR (1) KR870008842A (ko)
AU (1) AU6991087A (ko)
DK (1) DK123987A (ko)
FI (1) FI871067A (ko)
FR (1) FR2595695B1 (ko)
HU (1) HUT43820A (ko)
IL (1) IL81858A0 (ko)
NO (1) NO870998L (ko)
PT (1) PT84452B (ko)
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CS103091A3 (en) * 1991-04-12 1992-10-14 Ustav Organicke Chemie A Bioch Protected substituted benzhydrylamines as shoulders for the synthesis ofpeptides on solid phase, process of their preparation and use
ES2165880T3 (es) * 1993-06-21 2002-04-01 Selectide Corp Conectores segmentables selectivamente basados en enlaces ester de acido iminodiacetico.
US6063794A (en) * 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
AU747531B2 (en) * 1997-04-14 2002-05-16 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
EP0975659A1 (en) * 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
JP2001523226A (ja) 1997-04-14 2001-11-20 シーオーアール セラピューティクス インコーポレイテッド 選択的Xa因子阻害剤
JP2002514214A (ja) 1997-04-14 2002-05-14 シーオーアール セラピューティクス インコーポレイテッド 選択的Xa因子阻害剤
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
JP2006522742A (ja) * 2003-04-08 2006-10-05 ニューロームド テクノロジーズ、インク. ピペラジンから距離をおいて配置したベンズヒドリル基から成る一群のカルシウムチャンネル阻害剤

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FR2516509B1 (fr) * 1981-11-18 1985-07-26 Synthelabo Derives benzylideniques, leur preparation et leur application en therapeutique

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HUT43820A (en) 1987-12-28
AU6991087A (en) 1987-09-17
FI871067A (fi) 1987-09-13
DK123987A (da) 1987-09-13
FR2595695B1 (fr) 1988-12-02
NO870998L (no) 1987-09-14
PT84452B (fr) 1989-03-17
JPS62230767A (ja) 1987-10-09
EP0239461A1 (fr) 1987-09-30
FI871067A0 (fi) 1987-03-11
IL81858A0 (en) 1987-10-20
FR2595695A1 (fr) 1987-09-18
DK123987D0 (da) 1987-03-11
NO870998D0 (no) 1987-03-11
PT84452A (fr) 1987-04-01
ZA871766B (en) 1987-09-01

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