KR860004046A - 헤테로폴리사이클릭 화합물의 제법 및 그 약학제제 - Google Patents

헤테로폴리사이클릭 화합물의 제법 및 그 약학제제 Download PDF

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KR860004046A
KR860004046A KR1019850008500A KR850008500A KR860004046A KR 860004046 A KR860004046 A KR 860004046A KR 1019850008500 A KR1019850008500 A KR 1019850008500A KR 850008500 A KR850008500 A KR 850008500A KR 860004046 A KR860004046 A KR 860004046A
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methyl
propanediol
amino
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rings
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KR920001777B1 (en
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윌토 베어 케니스
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미첼. 피토 잭슨
더웰컴 파운데이숀 리미티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/91—Dibenzofurans; Hydrogenated dibenzofurans
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D219/00—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems
    • C07D219/02—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems with only hydrogen, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/92—Naphthofurans; Hydrogenated naphthofurans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/74—Naphthothiophenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/76—Dibenzothiophenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings

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  • Organic Chemistry (AREA)
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  • Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Steroid Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

내용 없음

Description

헤테로폴리사이클릭 화합물의 제법 및 그 약학제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (19)

  1. R―CH=N=R1화합물 또는 그것의 적합하게 보호된 유도체를 환원시켜서 적절한 경우에는 탈보호시키고 그 수신기가 임의적으로 보호되었다가 적합한 경우에는 탈보호되는 R.CO.NHR1화합물을 환원시키며 RCH2L 화합물을 NH2R1화합물과 반응시키는 것을 특징으로 하는 하기 일반식(Ⅰ)화합물 또는 총29이하의 탄소를 포함하는 그것의 모노메틸 또는 모노메틸에테르의 제조방법.
  2. RCH2R1(Ⅰ)
  3. (이때 R은 3,4 또는 5환을 가지는 융합체 환시스템이며, 4n+1 탄소수로 n은 존재하는 환의수이며, n이 3 또는 4일때 세개이상의 환이 방향족이며 n이 5일때 4개 이상의 환이 방향족이며, 하나이상의 방향족환이 헤테로원자를 함유한다; 이 헤테로원자는 하나 또는 두개 치환분에 의해 임의로 치환될 수 잇다. 이 치환분들은 함께 4개이하의 탄소를 포함하며 동일하거나 또는 상이하며 할로겐; 시아노; C1-4알킬 또는 C1-4알콕시(각각 수산 또는 C1-2알콕시 임의치환됨); 할로겐 치환된 C1-2알킬 또는 C1-2알콕시; S(O)nR기, 이때 n은 정수 0,1 또는 2이며, R2는 수산 또는 C1-2알콕시로 임의 치환된 C1-2알킬로부터 선택되며; 또는 Ar이 5이하의 탄소를 함유하는 NR3R4기로 임의치환하는데, 이때 R3와 R4는동일하거나 상이하며 각각 C1-3알킬기 또는 NR3R4는 하나 또는 두개의 부가적인 헤테로원자를 임의로 함유하는 5각 또는 6각의 헤테로사이클릭환을 형성한다; R1은 8개이하의 탄소수를 포함하며 하기식으로 나타낼 수 있다.
  5. 이 때 m은 0 또는 1; R5와 R6는 동일하거나 상이하며 각각 수산기로 임의 치환된 C1-5알킬; R7과 R8은 동일하거나, 상이하며 각각 수소 또는 C1-3알킬; ―C―C는 5각 또는 6각의 포화카르보사이클릭환; R9는 수소, 메틸 또는 하이드록시메틸; R10,R11과 R12는 동일하거나 상이하며 각각 수소 또는 메틸이며; R13은 수소, 메틸, 하이드록시 또는 하이드록시메틸이며; R이 세개의 6각 카르보사이클릭환과 헤테로원자가 존재하는 하나의 5각환을 가지는 15 내지 17환 원자를 포함하는 테트라사이클릭한 시스템은 아니다).
  6. 제1항에 있어서, 하나 또는 두개의 방향족환만이 헤테로원자를 포함하는 일반식(Ⅰ) 화합물의 제조방법.
  7. 제1항 또는 2항에 있어서, 그 헤테로원자가 질소, 인, 산소, 황 또는 셀레늄인 일반식(Ⅰ) 화합물의 제조방법.
  8. 제3항에 있어서, 그 헤테로원자가 산소, 질소 또는 황인 일반식(Ⅰ) 화합물의 제조방법.
  9. 제1항에 있어서, 하기식 화합물의 제조방법.
  11. (Z=황, 산소, NMe 또는 NEt)
  12. 제1항에 있어서, 하기식 화합물의 제조방법.
  14. (Z=황, 산소, NMe 또는 NEt)
  15. 제1항에 있어서, 2―〔(9―아크리디닐메틸)아미노〕―2―메틸―1,3―프로판디올, 2―〔(1―디벤조티오페닐메틸)아미노〕―2―메틸―1,3―프로판디올, 2―〔(2―디벤조티오페닐메틸)아미노〕―2―메틸―1,3―프로판디올, 2―〔(4―디벤조티오페닐메틸)아미노〕―2―메틸―1,3―프로판디올, 2―〔(1―디벤조푸라닐메틸)아미노〕―2―메틸―1,3―프로판디올, 2―〔(2―디벤조푸라닐메틸)아미노〕―2―메틸―1, 3―프로판디올, 2-(냐프토[2,3-b]-티오펜-4-일메틸]아미노]-2-메틸-1,3-프로판디올, 2―메틸―2―〔(나프토2,1―b〕티오펜―5―일메틸)아미노〕―1,3―프로판디올, 2―메틸―2―〔(나프토〔2,1―b〕티오펜―2―일메틸)〕―1,3―아미노프로판디올, 2―메틸―2―〔(나프토〔2,1―b〕티오펜―2―일메틸)-1,3-프로판디올,2―메틸―2-[(나프트[2,1-b]-티오펜-5-일메틸)아미노]-1,3-프로판디올, 2―메틸―2―〔(나프토〔1,2―b〕푸란―2―일메틸)아미노〕1,3―프로판디올, 2―메틸―2―〔(나프토〔2,1―b〕푸란―2―일메틸)아미노〕―1,3―프로판디올, 2-아세나프토[1,2-b]퀴놀린-10-일메틸)아미노]-2메틸-1,3-프로판디올, 2―〔(아세나프토〔1,2―b〕티오펜―8―일메틸)아미노〕―2―메틸―1,3―프로판디올, 2―〔(아세나프토〔1,2―c〕티오펜―7―일메틸)아미노〕―2―메틸―1,3―프로판디올 또는 그것의 모노에틸에테르, 에스테르와 산부가염의 제조방법.
  16. 하기일반식(Ⅰ)화합물 또는 그것의 모노메틸 또는 모노에틸 에테르 또는 에스테르 또는 약학적 허용염을 그것의 약학적 허용담체와 함께 함유하는 약학체제.
  17. RCH2R1(Ⅰ)
  18. (R과 R1은 제1항의 정의와 같다.)
  19. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR8508500A 1984-11-15 1985-11-14 Process for preparing hetero-polycyclic compound KR920001777B1 (en)

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GB84-28930 1984-11-15
GB848428930A GB8428930D0 (en) 1984-11-15 1984-11-15 Polycyclic biocidal compounds

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KR860004046A true KR860004046A (ko) 1986-06-16
KR920001777B1 KR920001777B1 (en) 1992-03-02

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AT (1) ATE85333T1 (ko)
DE (1) DE3587066T2 (ko)
DK (1) DK526785A (ko)
ES (3) ES8801202A1 (ko)
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US6174913B1 (en) * 1998-06-05 2001-01-16 The University Of North Carolina At Chapel Hill Naphtho- and dihydrobenzo-thiophene derivatives as cytotoxic antitumor agents
US9312501B2 (en) 2012-09-28 2016-04-12 Polyera Corporation Semiconducting compounds and optoelectronic devices incorporating same

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* Cited by examiner, † Cited by third party
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US4022805A (en) * 1974-03-07 1977-05-10 Hoffmann-La Roche Inc. 8-Halo-dibenzofuran-3-acetic acids and certain esters thereof
JPS5283455A (en) * 1976-01-01 1977-07-12 Hoffmann La Roche Benzofuran derivatives
CH628045A5 (en) * 1976-03-24 1982-02-15 Hoffmann La Roche Process for the preparation of dibenzothiophene derivatives
US4219657A (en) * 1977-12-19 1980-08-26 Hoffmann-La Roche Inc. Dibenzothiophenes
GB8313571D0 (en) * 1983-05-17 1983-06-22 Wellcome Found Chemical compounds

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KR920001777B1 (en) 1992-03-02
ATE85333T1 (de) 1993-02-15
ES8801630A1 (es) 1988-02-16
ES557177A0 (es) 1988-03-16
DE3587066D1 (de) 1993-03-18
HUT40094A (en) 1986-11-28
EP0183439A2 (en) 1986-06-04
ES8801202A1 (es) 1987-12-16
JPH0745475B2 (ja) 1995-05-17
GR852762B (ko) 1986-03-13
EP0183439A3 (en) 1988-08-10
DK526785D0 (da) 1985-11-14
ES557176A0 (es) 1988-02-16
DK526785A (da) 1986-05-16
DE3587066T2 (de) 1993-08-12
ES8802024A1 (es) 1988-03-16
GB8428930D0 (en) 1984-12-27
HU199818B (en) 1990-03-28
JPS61122274A (ja) 1986-06-10
ES548868A0 (es) 1987-12-16
EP0183439B1 (en) 1993-02-03

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