KR960004334A - Novel acetylsalicylic acid derivatives and preparation method thereof - Google Patents

Novel acetylsalicylic acid derivatives and preparation method thereof Download PDF

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Publication number
KR960004334A
KR960004334A KR1019940017520A KR19940017520A KR960004334A KR 960004334 A KR960004334 A KR 960004334A KR 1019940017520 A KR1019940017520 A KR 1019940017520A KR 19940017520 A KR19940017520 A KR 19940017520A KR 960004334 A KR960004334 A KR 960004334A
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South Korea
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group
unsubstituted
substituted
compound
acetylsalicylic acid
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KR1019940017520A
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Korean (ko)
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정원근
문창규
천문우
유충규
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정원근
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Priority to KR1019940017520A priority Critical patent/KR960004334A/en
Publication of KR960004334A publication Critical patent/KR960004334A/en

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Abstract

본 발명은 혈소판 응집 억제효과를 갖는 하기 일반식(Ⅰ)의 신규한 아세틸사릴실산 유도체 및 그이 약제학적으로 허용되는 염에 관한 것이다.The present invention relates to novel acetylsarylsilic acid derivatives of the following general formula (I) having a platelet aggregation inhibitory effect and pharmaceutically acceptable salts thereof.

상기식에서, Q는 치환되거나 비치환된 쿠마릴 그룹, N-치환되거나 비치환된 2-퀴놀린 그룹, 치환되거나 비치환된 2-옥소-1,2H-피라닐 그룹 또는 1,2-디(부틸아미노카보닐옥시)프로필 그룹을 나타낸다.Wherein Q is a substituted or unsubstituted couaryl group, an N-substituted or unsubstituted 2-quinoline group, a substituted or unsubstituted 2-oxo-1,2H-pyranyl group or 1,2-di (butyl Aminocarbonyloxy) propyl groups.

본 발명은 또한 상기 일반식(Ⅰ)의 화합물을 제조하는 방법 및 이 화합물을 함유하는 혈전형성 예방 및 치료용 약제학적 조성물에 관한 것이다.The present invention also relates to a method for preparing the compound of formula (I) and a pharmaceutical composition for preventing and treating thrombus formation containing the compound.

Description

신규한 아세틸살리실산 유도체 및 그의 제조방법Novel acetylsalicylic acid derivatives and preparation method thereof

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

Claims (9)

하기 일반식(Ⅰ)의 신규한 아세틸살리실산 유도체 및 그이 약제학적으로 허용되는 염;Novel acetylsalicylic acid derivatives of the general formula (I) and pharmaceutically acceptable salts thereof; 상기식에서, Q는 치환되거나 비치환된 쿠마릴 그룹, N-치환되거나 비치환된 2-퀴놀린 그룹, 치환되거나 비치환된 2-옥소-1,2H-피라닐 그룹 또는 1,2-디(부틸아미노카보닐옥시)프로필 그룹을 나타낸다.Wherein Q is a substituted or unsubstituted couaryl group, an N-substituted or unsubstituted 2-quinoline group, a substituted or unsubstituted 2-oxo-1,2H-pyranyl group or 1,2-di (butyl Aminocarbonyloxy) propyl groups. 제1항에 있어서, Q가 다음 일반식(a),(b),(c) 또는 (d)의 그룹을 나타내거나, 1,2-디(부틸아미노카보닐옥시)프로필 그룹을 나타내는 화합물.The compound according to claim 1, wherein Q represents a group of the following general formulas (a), (b), (c) or (d) or represents a 1,2-di (butylaminocarbonyloxy) propyl group. 상기식에서, R은 수소 또는 알킬을 나타내며, R1,R2및 R3는 각각 독립적으로 수소,알킬 또는 알킬 또는 할로겐을 나타낸다.Wherein R represents hydrogen or alkyl, and R 1 , R 2 and R 3 each independently represent hydrogen, alkyl or alkyl or halogen. 제2항에 있어서, Q가 쿠마릴, 4-메틸쿠마릴, 3,4-디메틸쿠마릴, 3,4,8-트리메틸쿠마릴, 3-클로로-4-메틸쿠마릴, N-메틸-2-퀴놀론, 6-메틸-2-옥소-1,2H-피라닐 또는 1,2-디(부틸디메틸카보닐옥시)프로필을 나타내는 화합물.The compound of claim 2, wherein Q is coumaryl, 4-methylcoumariyl, 3,4-dimethylcoumariyl, 3,4,8-trimethylcoumariyl, 3-chloro-4-methylcoumariyl, N-methyl-2 -Quinolone, 6-methyl-2-oxo-1,2H-pyranyl or 1,2-di (butyldimethylcarbonyloxy) propyl. 하기 구조식(Ⅱ)의 아세틸살리실산 또는 그의 염을 일반식(Ⅲ)의 화합물 또는 그의 염과 반응시킴을 특징으로 하는 일반식(Ⅰ)의 아세틸살리실산 유도체 또는 그의 염을 제조하는 방법.A method for preparing an acetylsalicylic acid derivative of the general formula (I) or a salt thereof, characterized by reacting an acetylsalicylic acid of the formula (II) or a salt thereof with a compound of the general formula (III) or a salt thereof. 상기식에서, Q는 치환되거나 비치환된 쿠마릴 그룹, N-치환되거나 비치환된 2-퀴놀린 그룹, 치환되거나 비치환된 2-옥소-1,2H-피라닐 그룹 또는 1,2-디(부틸아미노카보닐옥시)프로필 그룹을 나타내며, L은 반응성 이탈 그룹을 나타낸다.Wherein Q is a substituted or unsubstituted couaryl group, an N-substituted or unsubstituted 2-quinoline group, a substituted or unsubstituted 2-oxo-1,2H-pyranyl group or 1,2-di (butyl Aminocarbonyloxy) propyl group, and L represents a reactive leaving group. 제4항에 있어서, 아세틸살리실산(Ⅱ)을 일반식(Ⅲ)의 화합물과 반응시키기 전에 활성화시키는 방법.The method of claim 4, wherein the acetylsalicylic acid (II) is activated before reacting with the compound of formula (III). 제5항에 있어서, 아세틸살리실산의 활성화 유도체가 산 할라이드, 산 에스테르, 산 아미드 또는 산 무수물의 형태임을 특징으로 하는 방법.The method of claim 5 wherein the activating derivative of acetylsalicylic acid is in the form of an acid halide, acid ester, acid amide or acid anhydride. 제4항에 있어서, 아세틸살리실산(Ⅱ)과 일반식(Ⅲ)의 화합물의 반응을 염기 및 디사이클로헥실카보디이미드의 존재하에서 수행함을 특징으로 하는 방법.5. A process according to claim 4, wherein the reaction of acetylsalicylic acid (II) with a compound of formula (III) is carried out in the presence of a base and dicyclohexylcarbodiimide. 제4항에 있어서, 반응을 무수 조건하에서 수행함을 특징으로 하는 방법.The process according to claim 4, wherein the reaction is carried out under anhydrous conditions. 제1항 내지 3항 중의 어느 하나에 따르는 일반식(Ⅰ)의 화합물 또는 그의 약제학적으로 허용되는 염을 함유함을 특징으로 하는 혈전형성 예방 및 치료제 조성물.A composition for preventing and treating thrombosis, comprising a compound of formula (I) according to any one of claims 1 to 3 or a pharmaceutically acceptable salt thereof. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019940017520A 1994-07-20 1994-07-20 Novel acetylsalicylic acid derivatives and preparation method thereof KR960004334A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100309747B1 (en) * 1999-05-29 2001-09-29 서병만 A decoration-matter insert apparatus for accessary
KR100309746B1 (en) * 1999-05-29 2001-09-29 서병만 A decoration-matter insert apparatus for accessary

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100309747B1 (en) * 1999-05-29 2001-09-29 서병만 A decoration-matter insert apparatus for accessary
KR100309746B1 (en) * 1999-05-29 2001-09-29 서병만 A decoration-matter insert apparatus for accessary

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