KR930004274A - 히단토인 유도체 - Google Patents

히단토인 유도체 Download PDF

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KR930004274A
KR930004274A KR1019920014163A KR920014163A KR930004274A KR 930004274 A KR930004274 A KR 930004274A KR 1019920014163 A KR1019920014163 A KR 1019920014163A KR 920014163 A KR920014163 A KR 920014163A KR 930004274 A KR930004274 A KR 930004274A
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aryl
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radical
alkyl
hydrogen
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쾨니히 볼프강
촐러 게르하르트
유스트 멜리타
야블론카 베른트
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한스-게오르그 우르바흐, 한스 오이흐너
카젤라 아크티엔게젤샤프트
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
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Abstract

내용 없음.

Description

히단토인 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 일반식(Ⅰ)의 화합물 및 이의 생리학적으로 허용되는 염.
    상기식에서, Y는 -(CH2)m; -CO- 또는이고, 여기서, m은 1내지 4이며, R1은 -(CH2)n-NH-X, -CH2-C6H4-NH-X, -CH2-C6H4-C(=NH)-NH2, -CH2-C6H4-CH2-NH-X 또는 -C6H4NH-X이거나,는 또한이고, 여기서 n은 3내지 5이며, X1은 -CH2NHX, -NHX 또는 -C(=NH)-NH2이고, X는 수소 또는 C1-C6-알킬, 또는 일반식(Ⅱ) R1=NH-C=N-R″)여기서, R′ 및 R″는 서로 독립적으로 수소 또는 C1-C6-알킬이다)의 라디칼이고, R2는 수소 또는알킬이며, R3는 수소 또는 페닐라디칼이고, R4는 수소, COOR5, CO-N(CH3)-R5또는 CO-NH-R5이며, 여기서, R5는 수소, NHCO-NH2또는 C1-C18알킬이며, R5는 하이드록실, 카복실, 카복스아미도, 아미노, 머캅토, C1-C18-알콕시, C1-C18-알콕시카보닐, C6-C14-아릴-C1-C3알콕시카보닐, C3-C8-사이클로 알킬, 할로겐, 니트로, 트리플루오로메틸 및 라디칼 R6을 포함하는 일련의 동일하거나 상이한 라디칼에 의해 임의로 일- 또는 다치환되며. R6은 C6-C14-아릴, C6-C14-아릴-C1-C8-알킬, 또는 모노- 또는 비사이클릭 5- 내지 12-원헤테로사이클릭 환(여기서, 이것은 방향족이고, 부분적으로 수소화되거나 완전하게 수소화될 수 있고 헤테로원자로서 1개, 2개 또는 3개의 동일하거나 상이한 질소, 산호 황원자를 함유할수 있다)이고, 상기 아릴 및 헤테로사이클릭 라디칼은 서로 독립적으로 C1-C18-알킬, C1-C18-알콕시, 할로겐, 니트로 및 트리플루오로메틸을 포함하는 일련의 동일하거나 상이한 라디칼에 외해 임의로 일- 또는 다치환될 수 있거나, R6은 라디칼 R7이고, R7은 -NR8R9, -OR8, -SR8또는 아미노산 측쇄, 또는 천연적 또는 비천연적 아미노산 라디칼, 이미노산 라디칼 또는 임의로 N-C1-C8-알킬화되거나 C6-C14-아릴-C1-C8-알킬화된 아자아미노산 라디칼 또는 디펩타이드 라디칼(여기서, 펩타이드 결합은 Nh-CH2로 환원될 수 있다) 및 이의 에스테르 및 아미드이고 유리 작용성그룹은 수소 토는 하이드록시-메틸에 의해 임의로 치환될 수 있거나. 펩타이드 화학에서 통상적인 보호 그룹에 의해 보호되거나, 라디칼-COR7′(여기서, R7′는 R7에 대해 정의된 바와같다)이며, R8은 수소, 임의로 아미노-치환된 C1-C14-아릴 C1-C8-알킬, C6-C18-알킬카보닐, C1-C18-알콕시카보닐, C6-C14-아릴카보닐, C6-C12-아릴-C1-C8-알킬카보닐, C6-C18-아릴-C1-C18-알콕시카보닐, 또는 천연적 또는 비천연적 아미노산 라디칼, 아미노산 라디칼 또는 임의로 N-C1-C8-알킬화되거나 C6-C14-아릴-C1-C8-알킬화된 아자아미노산 라디칼 또는 디펩타이드 라디칼(여기서, 펩타이드 결합은 NH-CH2아릴 또는 C6-C12-아릴-C1-C8-알킬이고, 단)R1이 -(CH2)3-4-NH-X(여기서, X는 C1-C6-알킬 또는 일반식(Ⅱ)의 라디칼이다)이며, R2및 R3가 수소이고, R4가 -CO-NH-R5이며, Y가 -CH2-CO인 일반식(Ⅰ)의 화합물은 제외된다.
  2. 제1항에 있어서, R1이 -CH2-C6H4-C(NH)-NH2또는 -CH2-C6H4-CH2-NH2이고, R2가 H 또는 CH3이며, Y가 -C2,-CO-이고, R4가 -CO-NH-R5(여기서, NH-R5는 α-아미노산 라디칼, 바람직하게는 발린 토는 페닐글리신 라디칼이다)인 일반식(Ⅰ)의 화합물.
  3. 일반식(Ⅱa), (Ⅲb) 또는 (Ⅲc)의 화합물과 일반식(Ⅳ)의 화합물을 단편 축합시킴으로써 제1항 또는 제2항에 따른 일반식(Ⅰ)의 화합물을 제조하는 방법.
    상기식에서 R1, R2, R3, R4, X1및 m은 제1항 또는 제2항에서 정의한 바와 같다.
  4. 제1항 또는 제2항에 있어서, 약물로서 사용하기 위한 화합물.
  5. 혈소판 응집을 억제하기 위한 제1항 또는 제2항에 따른 일반식(Ⅰ)의 화합물의 용도.
  6. 뼈 표면에 파골 세포의 결합을 억제하기 위한 제1항 또는 제2항에 따른 일반식(Ⅰ)의 화합물의 용도.
  7. 제1항 또는 제2항에 따른 일반식(Ⅰ)의 화합물 또는 이의 생리학적으로 허용되는 염, 및 적합한 부형제를 포함하는 약제학적 제형.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920014163A 1991-08-08 1992-08-07 히단토인유도체, 이의 제조방법 및 이를 포함하는 약제학적 조성물 KR100242621B1 (ko)

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DE4126277A DE4126277A1 (de) 1991-08-08 1991-08-08 Hydantoinderivate
DEP4126277.8 1991-08-08

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KR930004274A true KR930004274A (ko) 1993-03-22
KR100242621B1 KR100242621B1 (ko) 2000-03-02

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US (1) US5389614A (ko)
EP (1) EP0530505B1 (ko)
JP (1) JP3293885B2 (ko)
KR (1) KR100242621B1 (ko)
AT (1) ATE128985T1 (ko)
CA (1) CA2075590C (ko)
CZ (1) CZ289929B6 (ko)
DE (2) DE4126277A1 (ko)
DK (1) DK0530505T3 (ko)
ES (1) ES2081000T3 (ko)
GR (1) GR3018557T3 (ko)
HU (1) HU218922B (ko)
IL (1) IL102759A (ko)
SK (1) SK245992A3 (ko)
TW (1) TW204345B (ko)
ZA (1) ZA925934B (ko)

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DE4427979A1 (de) * 1993-11-15 1996-02-15 Cassella Ag Substituierte 5-Ring-Heterocyclen, ihre Herstellung und ihre Verwendung
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EP0796855B1 (de) 1996-03-20 2002-02-06 Hoechst Aktiengesellschaft Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten
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DE19647380A1 (de) * 1996-11-15 1998-05-20 Hoechst Ag 5-Ring-Heterocyclen als Inhibitoren der Leukozytenadhäsion und VLA-4-Antagonisten
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HU9202583D0 (en) 1992-10-28
EP0530505B1 (de) 1995-10-11
HU218922B (hu) 2000-12-28
JPH05213895A (ja) 1993-08-24
JP3293885B2 (ja) 2002-06-17
CA2075590A1 (en) 1993-02-09
DE59203976D1 (de) 1995-11-16
DK0530505T3 (da) 1996-02-12
AU2089292A (en) 1993-03-11
TW204345B (ko) 1993-04-21
AU651716B2 (en) 1994-07-28
US5389614A (en) 1995-02-14
CZ245992A3 (en) 1993-12-15
ATE128985T1 (de) 1995-10-15
ZA925934B (en) 1993-04-28
IL102759A0 (en) 1993-01-31
EP0530505A3 (en) 1993-12-29
GR3018557T3 (en) 1996-03-31
SK245992A3 (en) 2000-09-12
CA2075590C (en) 2003-01-07
EP0530505A2 (de) 1993-03-10
DE4126277A1 (de) 1993-02-11
CZ289929B6 (cs) 2002-04-17
KR100242621B1 (ko) 2000-03-02
HUT61779A (en) 1993-03-01
ES2081000T3 (es) 1996-02-16
IL102759A (en) 1997-06-10

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