KR940021065A - Novel derivatives of bile acids and processes for the preparation of pharmaceutical components comprising the same - Google Patents

Novel derivatives of bile acids and processes for the preparation of pharmaceutical components comprising the same Download PDF

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Publication number
KR940021065A
KR940021065A KR1019940004161A KR19940004161A KR940021065A KR 940021065 A KR940021065 A KR 940021065A KR 1019940004161 A KR1019940004161 A KR 1019940004161A KR 19940004161 A KR19940004161 A KR 19940004161A KR 940021065 A KR940021065 A KR 940021065A
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South Korea
Prior art keywords
acid
alpha
hydroxyalkyl
amino
organic salts
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KR1019940004161A
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Korean (ko)
Inventor
파렌티 마시모
보죠 코스타 에도르도
Original Assignee
에이.브루쉐티니
프로도티 케미시 에 엘리멘타리 에스피에이
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Application filed by 에이.브루쉐티니, 프로도티 케미시 에 엘리멘타리 에스피에이 filed Critical 에이.브루쉐티니
Publication of KR940021065A publication Critical patent/KR940021065A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)

Abstract

본 발명은 하기와 같은 일반식을 가지는 담즙산의 신규한 아미드로, 치료요법적 활성을 가지는 것을 특징으로 하는 N(2-하디록시알킬)타우린 유도체.The present invention is a novel amide of bile acids having the following general formula, N (2-hadioxyalkyl) taurine derivative, characterized in that it has therapeutic activity.

이때 AI은 α-OH 또는 β-OH, A2는 H 또는 α-OH 또는 β-OH, A3는 H 또는 α-OH 또는 β-OH, R은 H, 알칼리 또는 토양-알칼리 금속 또는 유기산 또는 염기성 아미노산, 제약학적 활성염기와 유기염, 아미노산(리신 또는 아르기닌)또는 무기이온(Na, Ca 등)과 이의 유기염이고, R1 은 직쇄형 또는 분지쇄 C1-C5알킬이 되고, 이는 세포막에서 세포보호 효과를 위한 지질교환에 질환, 담즙 디스펩시아, 콜레스테롤성 담결선과 같은 병리적 상태의 유용성이 있는 화학적, 대사적 약리학적 특성을 가진다.AI is α-OH or β-OH, A2 is H or α-OH or β-OH, A3 is H or α-OH or β-OH, R is H, alkali or soil-alkali metal or organic acid or basic amino acid , Pharmaceutically active bases and organic salts, amino acids (lysine or arginine) or inorganic ions (Na, Ca, etc.) and organic salts thereof, R1 is linear or branched C1-C5 alkyl, which has a cytoprotective effect on the cell membrane It has chemical and metabolic pharmacological properties that are useful for pathological conditions such as disease, biliary dispecia, and cholesterol cholangiopancreatic for lipid exchange.

Description

담즙산의 신규한 유도체와 이를 포함하는 제약학적 성분물의 제조공정Novel derivatives of bile acids and processes for the preparation of pharmaceutical components comprising the same

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

Claims (4)

하기와 같은 일반식을 가지고 치료요법적 활성을 가지는 것을 특징으로 하는 N(2-하디록시알킬)타우린 유도체.N (2-hadioxyalkyl) taurine derivative having the following general formula and having therapeutic activity. 이때 AI은 α-OH 또는 β-OH, A2는 H 또는 α-OH 또는 β-OH, A3는 H 또는 α-OH 또는 β-OH, R은 H, 알칼리 또는 토양-알칼리 금속 또는 유기산 또는 염기성 아미노산, 제약학적 활성염기와 유기염, 아미노산(리신 또는 아르기닌)또는 무기이온(Na, Ca 등)과 이의 유기염이고, R1은 직쇄형 또는 분지쇄 C1-C5알킬.AI is α-OH or β-OH, A2 is H or α-OH or β-OH, A3 is H or α-OH or β-OH, R is H, alkali or soil-alkali metal or organic acid or basic amino acid , Pharmaceutically active bases and organic salts, amino acids (lysine or arginine) or inorganic ions (Na, Ca, etc.) and organic salts thereof, R1 is straight or branched C1-C5 alkyl. 제1항에 있어서, 하이드록시알킬타우로우루소데옥시콜린산 즉, 2{[3-알파, 7β-디하이드록시-24-옥소-5-β-콜란-24-일]아미노}하이드록시알킬 에탄 설포산인 것을 특징으로 하는 N(2-하이드록시알킬)타우린 유도체.The hydroxyalkyltauurorusodeoxycholic acid of claim 1, i.e. 2 {[3-alpha, 7β-dihydroxy-24-oxo-5-β-cholan-24-yl] amino} hydroxyalkyl N (2-hydroxyalkyl) taurine derivative, characterized in that it is ethane sulfoic acid. 제1항에 있어서, 하이드록시알킬타우로우루소데옥시콜린산 즉, 2{[3-알파, 7-알파-바이하이드록시-24-옥소-5-β-콜란-24-일]아미노}하이드록시알킬 에탄 설포산인 것을 특징으로 하는 N(2-하이드록시알킬)타우린 유도체.The method of claim 1, wherein hydroxyalkyltauurorusodeoxycholic acid, ie 2 {[3-alpha, 7-alpha-bihydroxy-24-oxo-5-β-cholan-24-yl] amino} hydroxy N (2-hydroxyalkyl) taurine derivative, characterized in that oxyalkyl ethane sulfoic acid. 제1항에 있어서, 하이드록시알킬타우로우루소데옥시콜린산 즉, 2{[3-알파, 6-알파-디하이드록시-24-옥소-5-β-콜란-24-일]아미노}하이드록시알킬 에탄 설포산인 것을 특징으로 하는 N(20-하이드록시알킬)타우린 유도체.The method of claim 1, wherein the hydroxyalkyltauurorusodeoxycholic acid, ie 2 {[3-alpha, 6-alpha-dihydroxy-24-oxo-5-β-cholan-24-yl] amino} hydroxy N (20-hydroxyalkyl) taurine derivative, characterized in that oxyalkyl ethane sulfoic acid. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019940004161A 1993-03-05 1994-03-04 Novel derivatives of bile acids and processes for the preparation of pharmaceutical components comprising the same KR940021065A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI93A000420 1993-03-05
ITMI930420A IT1271429B (en) 1993-03-05 1993-03-05 New bile acid derivatives, process for their preparation and pharmaceutical compositions containing them

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KR940021065A true KR940021065A (en) 1994-10-17

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023008891A1 (en) 2021-07-26 2023-02-02 (주)샤페론 Novel compound that inhibits tnf-a generation and inflammasome activity and preparation method therefor

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023008891A1 (en) 2021-07-26 2023-02-02 (주)샤페론 Novel compound that inhibits tnf-a generation and inflammasome activity and preparation method therefor
KR20230017149A (en) 2021-07-26 2023-02-03 (주)샤페론 Novel taurine-bile acid derivatives inhibitors for TNF-αproduction and inflammasomal activation and preparation method thereof

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Publication number Publication date
IT1271429B (en) 1997-05-28
ITMI930420A1 (en) 1994-09-05
ITMI930420A0 (en) 1993-03-05

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