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KR930002370A - 스피카마이신 유도체 및 그의 용도 - Google Patents

스피카마이신 유도체 및 그의 용도 Download PDF

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KR930002370A
KR930002370A KR1019920012373A KR920012373A KR930002370A KR 930002370 A KR930002370 A KR 930002370A KR 1019920012373 A KR1019920012373 A KR 1019920012373A KR 920012373 A KR920012373 A KR 920012373A KR 930002370 A KR930002370 A KR 930002370A
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spicaminyl
purine
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노보루 오다께
히로유키 카와이
토미코 카와사키
아쯔오 오다가와
마사루 카미쇼하라
테루유키 사카이
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마나베 케이사쿠
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    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
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    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
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    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
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Abstract

내용 없음.

Description

스피카마이신 유도체 및 그의 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (16)

  1. 하기 일반식(I)로 표시되는 스피카마이신 유도체 및 그의 염.
    식중에서 R은 아래의 i)내지 X i)로 정의되는 치환기의 어떤 것을 나타내는 것이며, R1및 R2는 서로 다른 것으로서 각각 H 또는 OH를 나타낸다. i)탄소수 9 내지 15개의 직쇄 또는 분지쇄인 알킬기, 또는 탄소수 10 내지 17개의 직쇄인 알케닐기(단, R1이 H이고 R2가 OH이어서 탄소수 11배의 직쇄 알킬기인 경우와 R1이 OH이고, R2가 H이어서 탄소수 11 내지 15개의 직쇄 또는 분지쇄인 알킬기 및 올레오일기인 경우는 제외한다. ii)탄소수 10 내지 15개의 직쇄인 할로알킬기, iii)CH3(CH2)nCH(OH)-, 또는 CH3(CH2)n-1CH(OH)-CH2-(여기서, n=9∼13의 정수). iv)아지드기 또는 시아노기를 갖는 탄소수 10 내지 15개의 알킬기 v)페녹시기 또는 할로겐이 치환된 페녹시기를 갖는 탄소수 10 내지 13개의 직쇄인 알킬기.
    (여기서, X는 O 또는 S를 나타낸다).
  2. 제1항에 있어서, R1이 이고, R2가 OH인 스피카마이신 유도체 또는 그의 염.
  3. 제1항에 있어서, R1이 이고, R2가 H인 스피카마이신 또는 그의 유도체.
  4. 제2항에 있어서, R이 탄소수 10 내지 17개의 직쇄 알케닐기인 스피카마이신 유도체 또는 그의 염.
  5. 제3항에 있어서, R이 탄소수 10 내지 17개의 직쇄 알케닐기인 스피카마이신 또는 그의 염.
  6. 제2항에 있어서, R이 탄소수 11 내지 13개의 직쇄 알카디에닐기인 스피카마이신 유도체 또는 그의 염.
  7. 제3항에 있어서, R이 탄소수 11 내지 13개의 직쇄 알카디에닐기인 스피카마이신 유도체 또는 그의 염.
  8. 제2항에 있어서, 하기 화합물 또는 그의 염으로 되는 군중에서 선택되는 스피카마이신 또는 그의 염.
    6-[4′-N-(N′-트리데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-테트라데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-10-메틸운데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-11-메틸도데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-12-메틸트리데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-11-도데세노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-12-트리데세노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-시스-9-테트라데세노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-시스-9-헥사데세노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스-2-도데세노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스-2-데트라세노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스-2-헥사데세노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스, 트란스-2,4-도데카디에닐글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스, 트란스-2,4-트리데카디에닐글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스, 트란스-2,4-데트라데카디에닐글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-11-브로모운데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-12-브로모도데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-13-브로모트리데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-14-브로모테라데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-12-클로로도데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-13-클로로트리데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-14-클로로테트라데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-14-플루오로테트라데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-15-플루오로데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-16-플루오로헥사펜타노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-N-요오도운데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-2-클로로헥사데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-2-플루오로데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-2-플루오로헥사데타노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-2,2-디플루오로테트라데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-2-히드록시헥사데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-(S)-2-히드록시헥사데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-(R)-3-히드록시테트라데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-(S)-3-히드록시헥시데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-3-히드록시헥사데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-16-디아노헥사데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-11-페녹시운데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-12-페녹시도데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-(R)-2-아세톡히헥사데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-3-아세톡시헥사카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-12-부탄술포닐옥시도데카노일글리실)-스피카미닐-아미노]푸린, 6-{4′-N-[N-11-(2′-티에닐)-10-운데시노일글리실-스피카미닐-아미노}푸린, 6-{4′-N-(N-11-(3′-티에닐)-10-운데시노일글리실]-스피카미닐-아미노}푸린, 6-{4′-N-(N-11-(3′-퓨릴)-10-운데시노일글리실)-스피카미닐-아미노}푸린,
  9. 제8항에 있어서, 하기 화합물 또는 그의 염으로 되는 군 중에서 선택되는 스피카마이신 유도체 또는 그의 염. 6-[4′-N-(N′-트리데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-11-메틸도데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-시스-9-테트라데세노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스, 트란스-2,4-도데카디에닐글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스, 트란스-2,4-트리데카디에닐글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스, 트란스-2,4-데트라데카디에닐글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-12-브로모테카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-13-브로모도데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-14-브로모도데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-13-클로로트리데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-14-클로로트리데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-14-플루오로테트라데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-15-플루오로펜타데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-2,2-디플루오로테트라데카노일글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-(S)-2-히드록시헥사데카노일글리실)-스피카미닐-아미노]푸린, 6-{4′-N-(N-11-(3′-티에닐)-10-운데시노일글리실)-스피카미닐-아미노}푸린, 6-{4′-N-(N-11-(3′-티에닐)-10-운데시노일글리실)-스피카미닐-아미노}-푸린, 6-{4′-N-[N′-11-(3′-티에닐)-10-운데시노일글리실]-스피카미닐-아미노}-푸린, 6-{4′-N-[N-11-(3′-푸릴)-10-운데시노일글리실]-스피카미닐-아미노}푸린,
  10. 제9항에 있어서, 하기 화합물 또는 그의 염으로 되는 군 중에서 선택되는 스피카마이신 유도체 또는 그의 염. 6-[4′-N-(N′-트란스, 트란스-2,4-도데카디에닐글리실)-스피카미닐-아미노]푸린, 6-[4′-N-(N′-트란스, 트란스-2,4-테트라데카디에닐글리실)-스피카미닐-아미노]푸린,
  11. 제10항에 있어서, 하기 화합물 또는 그의 염으로 되는 군 중에서 선택되는 스피카마이신 유도체 또는 그의 염. 6-[4′-N-(N′-트란스, 트란스-2,4-테트라데카디에닐글리실)-스피카미닐-아미노]푸린,
  12. 제3항에 있어서, 하기 화합물 또는 그의 염으로 되는 군 중에서 선택되는 스피카마이신 유도체 또는 그의 염. 6-[4′-N-(N′-트란스, 트란스-2,4-테트라데카디에닐글리실)-스피카미닐-아미노]푸린,
  13. 제1항에 기재된 화합물의 적어도 하나의 화합물의 유효성분으로 함유하는 항종양체.
  14. 제1항항에 기재된 화합물의 적어도 하나의 화합물의 유효량 및 담체 또는 희석제를 함유하는 항종양제.
  15. 제1항에 기재된 화합물의 적어도 하나의 화합물의 유효량을 종양억제를 필요로 하는 환자에 투여하는 것을 특징으로 하는 종양억제 방법.
  16. 제1항에 기재된 화합물의 항종양제로서의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920012373A 1991-07-12 1992-07-11 스피카 마이신 유도체 및 그의 용도 KR100253050B1 (ko)

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JP19890391 1991-07-12
JP91-198903 1991-07-12
JP91-326845 1991-11-15
JP32684591 1991-11-15
JP4110665A JP2783722B2 (ja) 1991-07-12 1992-04-03 スピカマイシン誘導体およびそれを含む抗腫瘍剤
JP92-110665 1992-04-03

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ES2281591T3 (es) * 1999-01-22 2007-10-01 Kirin Beer Kabushiki Kaisha Derivados de n-((quinolinil)oxil)-fenil)-urea y de n-((quinazolinil)oxil)-fenil)-urea con actividad antitumoral.
DE60144383D1 (de) * 2000-09-20 2011-05-19 Gen Hospital Corp Methoden zur verminderung oder verhinderung von schmerzen mit spicamycin-derivaten
US20060074014A1 (en) * 2002-11-18 2006-04-06 Vicuron Pharmaceuticals Inc. Dalbavancin compositions for treatment of bacterial infections
MXPA05005338A (es) * 2002-11-18 2005-12-14 Vicuron Pharm Inc Metodos para administrar dalbavancin para el tratamiento de infecciones bacterianas.
EP2295400A3 (en) * 2003-09-11 2012-10-24 Invista Technologies S.à.r.l. Process of hydrocyanation of unsaturated carboxylic acid derivatives
JP4608651B2 (ja) * 2004-06-24 2011-01-12 財団法人ヒューマンサイエンス振興財団 抗ガン作用を有する化合物、その製造方法及び抗ガン剤
US8119829B2 (en) * 2004-09-08 2012-02-21 Invista North America S.A.R.L. Process of hydrocyanation of unsaturated carboxylic acid derivatives
WO2010042212A2 (en) 2008-10-10 2010-04-15 Dara Biosciences, Inc. Methods for treating or preventing pain using spicamycin derivatives
EP2597082A1 (de) 2011-11-24 2013-05-29 Symrise AG Verbindungen zur Maskierung eines unangenehmen Geschmacks
CN104822369A (zh) * 2012-08-09 2015-08-05 达拉生物科学公司 包含穗霉素衍生物的组合物及其使用方法
WO2015061481A1 (en) 2013-10-23 2015-04-30 Dara Biosciences, Inc. Methods of treating liquid tumors using compositions comprising spicamycin derivatives
CN110386874B (zh) * 2018-04-16 2022-10-04 湖北金鹤化工有限公司 一种12-酮基硬脂酸酯及其制备方法

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HUT61773A (en) 1993-03-01
FI105815B (fi) 2000-10-13
NO922674D0 (no) 1992-07-08
JPH05186494A (ja) 1993-07-27
NO178500B (no) 1996-01-02
JP2783722B2 (ja) 1998-08-06
AU1960092A (en) 1993-01-14
NO922674L (no) 1993-01-13
SG52704A1 (en) 1998-09-28
CA2073567A1 (en) 1993-01-13
DE69222992T2 (de) 1998-03-05
EP0525479B1 (en) 1997-11-05
ES2111019T3 (es) 1998-03-01
HU9202285D0 (en) 1992-10-28
FI923170A (fi) 1993-01-13
DE69222992D1 (de) 1997-12-11
US5461036A (en) 1995-10-24
AU657551B2 (en) 1995-03-16
HK1001729A1 (en) 1998-07-03
EP0525479A1 (en) 1993-02-03
CA2073567C (en) 1998-05-05
NO178500C (no) 1996-04-10
DK0525479T3 (da) 1998-04-20
GR3025293T3 (en) 1998-02-27
FI923170A0 (fi) 1992-07-09

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