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KR900003175A - 벤조피라놀 유도체 - Google Patents

벤조피라놀 유도체 Download PDF

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KR900003175A
KR900003175A KR1019890011280A KR890011280A KR900003175A KR 900003175 A KR900003175 A KR 900003175A KR 1019890011280 A KR1019890011280 A KR 1019890011280A KR 890011280 A KR890011280 A KR 890011280A KR 900003175 A KR900003175 A KR 900003175A
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lower alkyl
compound
amino
benzopyran
tetramethyl
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왈저 아르민
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쟝-쟈크 오게이, 롤란드 보터
에프. 호프만-라 롯슈 아크티엔게젤샤프트
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Publication of KR900003175A publication Critical patent/KR900003175A/ko
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/70—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with two hydrocarbon radicals attached in position 2 and elements other than carbon and hydrogen in position 6
    • C07D311/72—3,4-Dihydro derivatives having in position 2 at least one methyl radical and in position 6 one oxygen atom, e.g. tocopherols
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

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Abstract

내용 없음

Description

벤조피라놀 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (13)

  1. 일반식(Ⅰ)의 벤조피라놀 유도체 또는 그의 염:
    상기식에서, A는 -C C-R6, -CH2CH2-R7또는 일반식
    A1이고, R1은 H 또는 저급 알카노일이고, R2,R3및 R4는 H 또는 저급알킬이고, R5는 저급 알킬이고, R6및 R7은 헤테르방향족 라디칼, 또는 페닐, 나프틸 또는 펜안트릴로 부터 선택된 방향족 라디칼이며, 이 방향족 라디칼 R6또는 R7은 비치환되거나 또는 각각 하나이상의 치환기 Z6또는 Z7로 치환되고, Z6은 페닐-저급 알콕시, 하이드록시아미노-저급 알킬 또는 Z기이고, Z7은 페닐-C2-7-알콕시 또는 Z기이고, Z는 Cl, F, 저급 알킬, 저급 알콕시, 저급 알카노일, 저급 알카노일옥시, 하이드록시-저급 알킬, COOH, 저급 알콕시카보닐, NH2, 아미노-저급 알킬, 모노-또는 디-저급 알킬-아미노, 모노- 또는 디-저급 알킬-아미노-저급 알킬, 저급 알카노일 아미노, CONH2, 모노- 또는 디-저급 알킬-카바모일, 트리플루오로아세틸아미노, CF3, OH 또는 피리딜이거나 또는 2개의 인접 탄소원자 상의 Z는 -OCH2CH2N(R 체″)- 또는 -OCH2CON(R′″)-이고, R″는 H, 저급 알카노일 또는 트리플루오로아세틸이고, R′″은 H 또는 저급 알킬이고, R8, R9및 R10은 H, OH, 저급알킬, 저급 알콕시, 하이드록시-저급 알킬, F, Cl 또는 저급 알카노일이며, 단 이때 R8, R9또는 R10중 단지 하나만이 OH, 저급 알콕시, 하이드록시-저급 알킬, F, Cl 또는 저급 알카노일어야 하고, Y는 CH 또는 N이다.
  2. 제1항에 있어서, 상기 R6및 R7이 저급 알카노일옥시로 치환되지 않고, 상기 R7이 아미노-저급알킬, 모노- 또는 디-저급 알킬-아미노 또는 모노- 또는 디-저급 알킬-아미노-저급 알킬로 치환되지 않음을 제외하고는, 상기 A가 제1항에서 정의한 바와같은 화합물.
  3. 제1항 또는 제2항에 있어서, 상기 R1이 H이고, 상기 R2내지 R6가 메틸이고, 상기 A가 -C C-R6인 화합물.
  4. 제1항, 제2항 또는 제3항에 있어서, 상기 R6이 치환되거나 또는 비치환된 페닐이거나 티에닐, 피리딜 또는 벤조티에닐인 화합물.
  5. 제1항 또는 제2항에 있어서, 상기 R1이 H이고, 상기 R2내지 R5가 메틸이고, 상기 A가 A′(여기에서, Y는 N이고, R8내지 R10은 H 또는 저급 알킬이다)인 화합물.
  6. S(+), RS 또는, 특히 R(-) 형태의 [2-(벤조[b]티엔-3-일)에티닐]-3,4-디하이드로-2,5,7,8-테트라메틸-2H-1-벤조피란-6-올.
  7. 제1항 또는 제2항에 있어서, 하기 그룹의 화합물:R, S, 또는 RS형태의 3,4-디하이드로-2,5,7,8-테트라메틸-2-[(2-티에닐)에티닐]-2H-1-벤조피란-6-올, 3,4-디하이드로-2-(푸로[3,2-b]피리딘-2-일)-2,5,7,8-테트라메틸-2H-1-벤조피란-6-올, 2-(2-벤조푸라닐)-3,4-디하이드로-2,5,7,8-테트라메틸-2H-1-벤조피란-6-올; 및 2-(3,4-디하이드로-6-하이드록시-2,5,7,8-테트라메틸-2H-1-벤조피란-2-일)-7-메톡시벤조푸란-5-메탄올.
  8. 약제로 사용하기 위한 제1항 내지 제7항중 어느 한 항의 화합물.
  9. a) 하기 일반식(Ⅱ) 화합물과 일반식 R6X 화합물(여기에서, X는 Br, I 또는 트리플루오로메틸설포닐옥시이고 R6은 제1항에서 정의한 바와 같다)을 반응시키거나, 또는 b) A가 -C C-R6인 일반식(Ⅰ) 화합물을 수소화시키고, c) 반응 (a)에서 수득한, A가 -C C-R61(여기에서, R61은이고, R6내지 R10은 제1항에서 정의한 바와같다)인 일반식(Ⅰ) 화합물을 그 형태로 또는 A가 A′인 일반식(Ⅰ)의 상응 화합물형으로 단리하고, d) 원한다면, (a)(b) 또는 (c)에서 수득한 화합물을 염으로 전환시킴을 포함하는 제1항에 따른 화합물의 제조방법.
    (상기식에서, R1내지 R5는 제1항에서 정의한 바와 같다)
  10. 제1항 내지 제7항중 어느 한 항의 화합물 유효량과 불활성 담체를 포함하는 약학조성물.
  11. 5-리폭시게나제 및 지질 과산화 억제용 약학제제의 제조에 있어서 제1항 내지 제7항중 어느 한 항의 화합물의 용도.
  12. 제9항의 방법 또는 그와 동등한 화학적 방법에 의해 각각 제조된 제1항의 화합물.
  13. 본 명세서에 기재된 바와 실질적으로 같은 신규한 화합물, 제제, 공정 및 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890011280A 1988-08-09 1989-08-08 벤조피라놀 유도체 Withdrawn KR900003175A (ko)

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US23009488A 1988-08-09 1988-08-09
US230,094 1988-08-09
US367,082 1989-06-16
US07/367,082 US5015661A (en) 1988-08-09 1989-06-16 Chromanes and their pharmaceutical compositions and methods

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US (1) US5015661A (ko)
EP (1) EP0354508A3 (ko)
JP (1) JPH0283379A (ko)
KR (1) KR900003175A (ko)
AU (1) AU616039B2 (ko)
DK (1) DK389089A (ko)
HU (1) HU206204B (ko)
IL (1) IL91245A0 (ko)
MC (1) MC2050A1 (ko)
NO (1) NO172643C (ko)
NZ (1) NZ230233A (ko)
PH (1) PH27235A (ko)
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US5015661A (en) 1991-05-14
HU206204B (en) 1992-09-28
MC2050A1 (fr) 1990-07-17
DK389089D0 (da) 1989-08-08
NO893198L (no) 1990-02-12
NO893198D0 (no) 1989-08-08
JPH0283379A (ja) 1990-03-23
DK389089A (da) 1990-02-10
AU616039B2 (en) 1991-10-17
AU3941889A (en) 1990-02-15
JPH0579072B2 (ko) 1993-11-01
NO172643B (no) 1993-05-10
PT91400A (pt) 1990-03-08
EP0354508A2 (de) 1990-02-14
EP0354508A3 (de) 1991-03-27
HUT52493A (en) 1990-07-28
PH27235A (en) 1993-05-04
NO172643C (no) 1993-08-18
IL91245A0 (en) 1990-03-19
NZ230233A (en) 1992-03-26

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