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KR960701000A - 안트라닐산 유도체(anthranilic acid derivative) - Google Patents

안트라닐산 유도체(anthranilic acid derivative) Download PDF

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Publication number
KR960701000A
KR960701000A KR1019950703620A KR19950703620A KR960701000A KR 960701000 A KR960701000 A KR 960701000A KR 1019950703620 A KR1019950703620 A KR 1019950703620A KR 19950703620 A KR19950703620 A KR 19950703620A KR 960701000 A KR960701000 A KR 960701000A
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South Korea
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group
halogen
substituent
formula
substituted
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KR1019950703620A
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KR100189863B1 (ko
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후미히로 오자키
게이지 이시바시
히로노리 이쿠타
히로키 이시하라
시게루 소우다
Original Assignee
나이토 하루오
에자이 가부시키가이샤
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    • 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40Acylated substituent nitrogen atom
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07C217/56Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
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    • C07C237/44Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having carbon atoms of carboxamide groups, amino groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
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Abstract

cGMP-PDE 저해작용을 가진 안트라닐산 유도체를 제공한다.
일반식(Ⅰ)
[식중, R1, R2, R3및 R4는 동일 또는 상이한 수소원자, 할로겐원자, 수산기, 할로겐 치환되어 있어도 좋은 저급알킬기, 할로겐치환되어 있어도 좋은 저급알콕시기, 니트로기, 히드록시알킬기, 시아노기 등을 의미하며, R5, R6은 동일 또는 상이한 수소원자, 할로겐원자, 수산기, 시아노기, 할로겐치환되어 있어도 좋은 저급알킬기, 할로겐 치환되어 있어도 좋은 저급알콕시기 등을 의미한다. W는 식 -N=으로 표시되는 기 또는 식 -CH=로 표시되는 기를 의미한다. R7, R8은 동일 또는 상이한 수소원자, 할로겐치환되어 있어도 좋은 저급알킬기 등을 의미한다. A는 수소원자, 할로겐치환되어 있어도 좋은 저급알킬기 등을 의미한다. Z는 수산기, 할로겐치환되어 있어도 좋은 저급알콕시기, 시아노기, 할로겐원자 등을 의미한다. Y는 산소원자 또는 황원자를 의미한다. n은 0 또는 1~6의 정수를 의미한다.]으로 표시되는 안트라닐산 유도체 또는 그 약리학적으로 허용될수 있는 염.

Description

안트라닐산 유도체(ANTHRANILIC ACID DERIVATIVE)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 일반식(I)
    [식중, R1, R2, R3및 R4는 동일 또는 상이한 수소원자, 할로겐원자, 수산기, 할로겐 치환되어 있어도 좋은 저급알킬기, 할로겐치환되어 있어도 좋은 저급알콕시기, 니트로기, 히드록시알킬기, 시아노기, 식(식중 R9, R10은 동일 또는 상이한 수소원자, 할로겐치환되어 있어도 좋은 저급알킬기, 아릴알킬기, 헤테로아릴 일킬기, 아실기, 보호되어 있어도 좋은 카르복실기를 의미한다. 또 R9, R10은 그들이 결합하고 있는 질소원자와 함께 고리를 형성하고 있어도 좋다. 더욱, 이 고리는 치환기를 갖고 있어도 좋다. p는 0 또는 1~6의 정수를 의미한다)로 표시되는 기, 치환기를 갖고 있어도 좋은 테트라졸일기, 보호되어 있어도 좋은 카르복실기, 치환기를 갖고 있어도 좋은 카르바모일기, 치환기를 갖고 있어도 좋은 피라조일기, 치환기를 갖고 있어도 좋은 이미다졸일기, 식(식중 R13은 수소 원자 또는 할로겐치환되어 있어도 좋은 저급일킬기를 의미한다. q는 0 또는 1~2의 정수를 의미한다.)로 표시되는 기를 의미한다. 더욱, R1, R2, R3, R4로부터 선택되는 서로 이웃한 2개의 치환기는 그들이 결합하고 있는 탄소원자와 함께 고리를 형성하고 있어도 좋다. R5, R6은 동일 또는 상이한 수소원자, 할로겐원자, 수산기, 시아노기, 할로겐치환되어 있어도 좋은 저급알킬기, 할로겐치환되어 있어도 좋은 저급알콕시기를 의미한다. 더욱, R5, R6은 그들이 결합하고 있는 탄소원자와 함께 시클로알킬고리, 옥솔란고리, 1, 3-디옥솔란고리, 1, 4-디옥산고리를 형성할 수 있다. W는 식 -N=으로 표시되는 기 또는 식 -CH=로 표시되는 기를 의미한다. R7, R8은 동일 또는 상이한 수소원자, 할로겐치환되어 있어도 좋은 저급알킬기를 의미한다. 더욱, R1, R7이, 각각 결합하고 있는 탄소원자와 함께, 그외에 질소원자, 산소원자, 또는 황원자를 포함하고 있어도 좋은 고리를 형성하고 있어도 좋다. 더욱이 고리는 치환기를 갖고 있어도 좋다. A는 수소원자, 할로겐치환되어 있어도 좋은 저급알킬기, 또는 식 -X-(CH2)m-Z(식중 X는 식 -CO-로 표시되는 기, 식 -CS-로 표시되는 기, 식 -CH2-로 표시되는 기 또는 식 -S(O)2-로 표시되는 기를 의미한다. Z는 수산기, 할로겐치환되어 있어도 좋은 저급알콕시기, 시아노기, 할로겐원자, 보호되어 있어도 좋은 카르바모일기, 치환기 갖고 있어도 좋은 아릴기, 치환기를 갖고 있어도 좋은 아릴옥시기, 치환기를 갖고 있어도 좋은 헤테로아릴기, 치환기를 갖고 있어도 좋은 헤테로아릴알킬옥시기, 식-NR11R12(식중 R11, R12는 동일 또는 상이한 수소원자, 할로겐치환되어 있어도 좋은 저급알킬기, 치환기를 갖고 있어도 좋은 아릴알킬기, 치환기를 갖고 있어도 좋은 헤테로아릴알킬기, 아실기, 보호되어 있어도 좋ㅇㄴ 카르복실기, 치환기를 갖고 있어도 좋은 카르바모일기를 의미한다. 또 R11과 R12는 그들이 결합하고 있는 질소원자와 함께 고리를 형성하고 있어도 좋다. 더욱 이 고리는 치환기를 갖고 있어도 좋다.)로 표시되는 기, 치환기를 갖고 있어도 좋은 시클로알킬기를 의미한다. m은 0 또는 1~6의 정수를 의미한다.)로 표시되는 기를 의미한다. Y는 산소원자 또는 황원자를 의미한다. n은 0 또는 1~6의 정수를 의미한다.]으로 표시되는 안트라닐산 유도체 또는 그 약리학적으로 허용될 수 있는 염.
  2. 일반식(II)
    (식중, R1, R2, R3, R4는 상기의 의미를 갖는다. R14는 수소원자, 할로겐 치환되어 있어도 좋은 저급알킬기, 치환기를 갖고 있어도 좋은 아릴알킬기를 의미한다. R15는 니트로기 또는 아미노기를 의미한다.)으로 표시되는 화합물 및 약리학적으로 허용될 수 있는 염.
  3. 일반식(III)
    (식중, R1, R2, R3, R4, R8, R14및 A는 상기의 의미를 갖는다)으로 표시되는 화합물 또는 그 약리학적으로 허용될 수 있는 염.
  4. 일반식(IV)
    (식중, R1, R2, R3, R4, m 및 Z는 상기의 의미를 갖는다.X2는 식 -CH2-로 표시되는 기를 의미한다.)으로 표시되는 화합물 또는 그 약리학적으로 허용될 수 있는 염.
  5. 제1항에 있어서, Y가 산소원자인 안트라니란 유도체 또는 그 약리학적으로 허용될수 있는 염.
  6. 제1항에 기재된 안트라닐산 유도체 또는 그 약리학적으로 허용될 수 있는 염을 유효성분으로 하는 포스포디에스테라제 저해작용이 유효한 질환의 예방ㆍ치료제
  7. 제1항에 기재된 안트라닐산 유도체 또는 그 약리학적으로 허용될 수 있는 염을 유효성분으로 하는 사이클릭-GMP 또는 포스포디에스테라제 저해작용이 유효한 지로한의 예방ㆍ치료제
  8. 제7항에 있어서, 질환이 허혈성 심질환, 협심증, 고혈압증, 폐고혈압증, 심부전 또는 천식인 예방ㆍ치료제.
  9. 약리학적으로 유효한 양의 제1항에 기재된 안트라닐산 유도체 또는 그 약리학적으로 허용될 수 있는 염과 약리학적으로 허용될 수 있는 담체를 함유한는 의약 조성물.
  10. 약리학적으로 유효한 양의 재1항에 기대된 안트라닐산 유도체 또는 그 약리적으로 허용될 수 있는 염을 투여하여, 그 포스포디에스테라제 저해작용은 행함으로써 질환을 예방ㆍ치료하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950703620A 1993-12-27 1994-12-27 안트라닐산 유도체 KR100189863B1 (ko)

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CN1118595A (zh) 1996-03-13
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AU1282495A (en) 1995-07-17
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EP0686625B1 (en) 1999-05-26
WO1995018097A1 (fr) 1995-07-06
DE69418704D1 (de) 1999-07-01
ATE180468T1 (de) 1999-06-15
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