KR970021072A - Novel Iridoid Derivatives That Inhibit Replication of Hepatitis B Virus and Methods for Preparing the Iridoid Derivatives - Google Patents

Novel Iridoid Derivatives That Inhibit Replication of Hepatitis B Virus and Methods for Preparing the Iridoid Derivatives Download PDF

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Publication number
KR970021072A
KR970021072A KR1019950038181A KR19950038181A KR970021072A KR 970021072 A KR970021072 A KR 970021072A KR 1019950038181 A KR1019950038181 A KR 1019950038181A KR 19950038181 A KR19950038181 A KR 19950038181A KR 970021072 A KR970021072 A KR 970021072A
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South Korea
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substituted
hepatitis
unsubstituted
group
iridoid derivatives
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KR1019950038181A
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Korean (ko)
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KR100450880B1 (en
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박문수
김제현
정동훈
문기호
하종열
임재욱
조인구
최건혁
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이병언
주식회사 중외제약
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 B형 간염 바이러스의 복제를 억제하는 하기 일반식(I)의 신규한 이리도이드 유도체, 그의 약제학적으로 허용되는 염 및 이성체에 관한 것이다.The present invention relates to novel iridoide derivatives of the general formula (I), pharmaceutically acceptable salts and isomers thereof which inhibit the replication of hepatitis B virus.

상기 식에서,는 이중결합 또는 단일결합을 나타내고, R1은 하이드록시 또는 저급알콕시를 나타내며, R2는 포르밀; 클로로, 아지도, 치환되거나 비치환된 아미노, 페닐티오 또는 하이드록시이미노로 구성된 그룹에서 선택된 1종에 의해 치환되거나 비치환된 C1-C5아릴; 에톡시카보닐 또는 페닐에 의해 치환되거나 비치환된 C2-C5알케닐을 나타내거나 R1및 R2는 함께또는그룹을 나타내고, 여기서, n은 0 내지 2의 정수를 나타내며, R3는 하이드록시, 아세톡시 또는 C1-C5알킬을 나타낸다.Where Represents a double bond or a single bond, R 1 represents hydroxy or lower alkoxy, R 2 is formyl; C 1 -C 5 aryl unsubstituted or substituted by one member selected from the group consisting of chloro, azido, substituted or unsubstituted amino, phenylthio or hydroxyimino; C 2 -C 5 alkenyl substituted or unsubstituted by ethoxycarbonyl or phenyl, or R 1 and R 2 together or Group, where n represents an integer from 0 to 2 and R 3 represents hydroxy, acetoxy or C 1 -C 5 alkyl.

본 발명은 또한, 상기 일반식(Ⅰ)의 화합물을 제조하는 방법 및 이 화합물을 유효성분으로 함유함으로써 B형 간염의 치료에 사용될 수 있는 약제학적 조성물에 관한 것이다.The present invention also relates to a method for preparing a compound of formula (I) and a pharmaceutical composition which can be used for the treatment of hepatitis B by containing the compound as an active ingredient.

Description

B형 간염 바이러스의 복제를 억제하는 신규한 이리도이드 유도체 및 그의 제조방법Novel Iridoid Derivatives That Inhibit Replication of Hepatitis B Virus and Methods for Preparing the Iridoid Derivatives

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (5)

하기 일반식(I)의 신규한 이리도이드 유도체, 그의 약제학적으로 허용되는 염 및 이성체.Novel iridoid derivatives of the general formula (I) below, pharmaceutically acceptable salts and isomers thereof. 상기 식에서,는 이중결합 또는 단일결합을 나타내고, R1은 하이드록시 또는 저급알콕시를 나타내며, R2는 포르밀; 클로로, 아지도, 치환되거나 비치환된 아미노, 페닐티오 또는 하이드록시이미노로 구성된 그룹에서 선택된 1종에 의해 치환되거나 비치환된 C1-C5알킬; 에톡시카보닐 또는 페닐에 의해 치환되거나 비치환된 C2-C5알케닐을 나타내거나 R1및 R2는 함께또는의 그룹을 나타내고, 여기서, n은 0 내지 2의 정수를 나타내며, R3는 하이드록시, 아세톡시 또는 C1-C5알킬을 나타낸다.Where Represents a double bond or a single bond, R 1 represents hydroxy or lower alkoxy, R 2 is formyl; C 1 -C 5 alkyl unsubstituted or substituted by one member selected from the group consisting of chloro, azido, substituted or unsubstituted amino, phenylthio or hydroxyimino; C 2 -C 5 alkenyl substituted or unsubstituted by ethoxycarbonyl or phenyl, or R 1 and R 2 together or Wherein n represents an integer of 0 to 2 and R 3 represents hydroxy, acetoxy or C 1 -C 5 alkyl. 제1항에 있어서 양쪽이 둘다 이중결합인 경우, R1은 메톡시를 나타내고, R2는 포르밀; 클로로, 아지도, 아미노, 푸르푸릴메틸아미노, 페닐티오 또는 하이드록시이미노로 구성된 그룹에서 선택된 1종에 의해 치환된 메틸; 에톡시카보닐 또는 페닐에 의해 치환된 에테닐; 또는 펜타디에닐을 나타내는 화합물.The method of claim 1, wherein both When both are double bonds, R 1 represents methoxy and R 2 is formyl; Methyl substituted by one selected from the group consisting of chloro, azido, amino, furfurylmethylamino, phenylthio or hydroxyimino; Ethenyl substituted by ethoxycarbonyl or phenyl; Or a compound representing pentadienyl. 제1항에 있어서, 6원환의이 이중결합을 나타내고 5원환의이 단일결합을 나타내는 경우, R1및 R2는 함께을 나타내고, 여기서 R3는 하이드록시 또는 아세톡시를 나타내는 화합물.According to claim 1, wherein the six-membered ring This double bond represents a five-membered ring When this single bond is represented, R 1 and R 2 together Wherein R 3 represents hydroxy or acetoxy. 제1항에 따른 일반식(I)의 화합물을 유효성분으로 함유하고, 이를 약제학적으로 허용되는 불활성 담체와 배합시킨 B형 간염 치료제 조성물.A hepatitis B therapeutic composition containing a compound of formula (I) according to claim 1 as an active ingredient and combined with a pharmaceutically acceptable inert carrier. 제4항에 있어서, 불활성 담체가 유당, 전분, 만니톨 및 면실유중에서 선택된 1종 이상인 조성물.The composition of claim 4, wherein the inert carrier is at least one selected from lactose, starch, mannitol, and cottonseed oil. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019950038181A 1995-10-30 1995-10-30 New Iridoid Derivatives to Suppress Replication of Hepatitis B Virus and Methods for Making the Same KR100450880B1 (en)

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JPS5781466A (en) * 1981-09-14 1982-05-21 Taito Kk Polymer of novel nitrogen-containing monoterpene derivative
JP2540871B2 (en) * 1987-07-20 1996-10-09 株式会社ツムラ Antihyperlipidemic agent
AU651849B2 (en) * 1990-10-09 1994-08-04 Tsumura & Co. Iridoid derivatives and their use as medicines
KR100218052B1 (en) * 1992-07-15 1999-09-01 이병언 Pharmaceutical preparation inhibiting duplication of hbv

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