KR930005978A - 1,4-dihydropyridine compound that antagonizes - Google Patents

1,4-dihydropyridine compound that antagonizes Download PDF

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Publication number
KR930005978A
KR930005978A KR1019920016053A KR920016053A KR930005978A KR 930005978 A KR930005978 A KR 930005978A KR 1019920016053 A KR1019920016053 A KR 1019920016053A KR 920016053 A KR920016053 A KR 920016053A KR 930005978 A KR930005978 A KR 930005978A
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South Korea
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formula
compound
general formula
alkyl
dihydropyridine
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KR1019920016053A
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Korean (ko)
Inventor
순께르 까를로스
파우 데 까사-하우나 미겔
싼토스 루이스
오르떼가 삘라르
프리에고 하이메
Original Assignee
미겔 앙헬 마르띠네스 호르까노
알떼르, 에세. 아.
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Priority claimed from EP91500103A external-priority patent/EP0531598A1/en
Application filed by 미겔 앙헬 마르띠네스 호르까노, 알떼르, 에세. 아. filed Critical 미겔 앙헬 마르띠네스 호르까노
Publication of KR930005978A publication Critical patent/KR930005978A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 directly attached to ring carbon atoms
    • C07D211/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PAF-아세테르의 길항작용을 하는 1,4-디하이드로피리딘은 일반식(Ⅰ)에서 R은 탄소수 1 내지 2인 포화알킬사슬이며, R´는 탄소수 1 내지 16인 선상, 분지상 또는 환상의 포화 또는 불포화사슬이며, 산소원자로 차단될 수 있으며, 또한 2-(N-모르폴린)에틸기를 대표할수 있다.1,4-dihydropyridine, which antagonizes PAF-aceter, is in the general formula (I) R is a saturated alkyl chain having 1 to 2 carbon atoms, and R 'is linear, branched or cyclic. It may be saturated or unsaturated, may be blocked with an oxygen atom, and may also represent a 2- (N-morpholine) ethyl group.

n은 2 또는 3의 정수이고, X는 산소, 유황 또는 SO2이고, Ar은 X=S 및 n=2일 때 페닐기를 제외한 방향족고리를 대표한다.n is an integer of 2 or 3, X is oxygen, sulfur or SO 2 , and Ar represents an aromatic ring excluding phenyl groups when X = S and n = 2.

화합물(Ⅰ)은 (a)(Ⅱ), (Ⅲ) 및 (Ⅳ)의 반응에 의해 제조되거나, (b)(Ⅴ)(Ⅵ) 및 (Ⅶ)의 반응에 의해 제조되거나, (c)(Ⅶ) 및 (Ⅵ)의 반응으로 제조될수 있다.Compound (I) is prepared by the reaction of (a) (II), (III) and (IV), (b) by the reaction of (V) (VI) and (iii), or (c) ( It can be prepared by the reaction of (iii) and (VI).

이들 일반식은 상기한 바와같이 다른 라디칼을 보유한다.These formulas bear other radicals as described above.

PAF-아세테르가 관여하는 병적상태 및 장애, 예를들어 염증의 과정, 건선, 사구체신염, 이식편거부, 급성 및 만성기관지염, 기관지천식, 쇼크의 상태 및 알레르기의 치료를 위하여 일반식(Ⅰ)의 화합물들이 사용된다.Pathology and disorders involving PAF-aceters, such as the process of inflammation, psoriasis, glomerulonephritis, graft rejection, acute and chronic bronchitis, bronchial asthma, shock conditions and allergies of general formula (I) Compounds are used.

또한 면역결핍증후군 및 방어기능이 감소된 상태와 같이 세포의 면역성을 자국할 필요가 있는 병적상태 및 장애의 치료를 위하여 사용된다.It is also used for the treatment of pathological conditions and disorders that require the immunity of cells, such as immunodeficiency syndrome and a reduced protective function.

Description

길항작용을 하는 1,4-디하이드로피리딘계화합물1,4-dihydropyridine compound that antagonizes

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

Claims (8)

일반식(Ⅰ)에서 PAF-아세테르의 길항작용을 하는 것을 특징으로 하는 4-알킬-1,4-디하이드로피리딘.4-Alkyl-1,4-dihydropyridine characterized by antagonizing PAF-aceter in general formula (I). 상기식에서 R은 메틸 또는 에틸기 등의 탄소수 1 내지 2인 포화알킬사슬이며, R´은 메틸, 에틸, 이소프로릴, 3차부틸, n-헥실, 알릴, 1-운데케닐 및 신나밀등의 탄소수 1 내지 16의 선상, 분지상 또는 환상의 포화 또는 불포황알킬사슬이며, 2-메톡시알킬 또는 테트라하이드로푸르푸릴 등의 산소원자에 의해 차단될수 있고 또한 2-(N-모르폴린)에틸기를 대표할 수 있다. n은 2 및 3의 정수이다. X는 산소원(O), 유황(S) 또는 SO2로 정의된다. Ar은 X=S 및 n=2가 아닌 페닐등의 방향족환을 대표한다. 또한 4-니트로페닐, 4-아세틸-아미노페닐, 4-클로로메틸,3,4 디클로로페닐, 4-메틸페닐, 4-메톡시페닐, 3-디메틸-아미노페놀, 4-비페닐, 4-페복시페닐, 4-벤질페닐, 4-벤질옥시페닐등의 치환페닐기를 대표한다. 또한 1-나프틸 및 2-나프틸기를 대표한다.In the above formula, R is a saturated alkyl chain having 1 to 2 carbon atoms such as methyl or ethyl group, and R 'is carbon number such as methyl, ethyl, isoproyl, tertiary butyl, n-hexyl, allyl, 1-undekenyl and cinnamil. Linear, branched or cyclic saturated or unsaturated sulfur alkyl chains of 1 to 16, which may be interrupted by oxygen atoms such as 2-methoxyalkyl or tetrahydrofurfuryl, and represent 2- (N-morpholine) ethyl groups can do. n is an integer of 2 and 3. X is defined as oxygen source (O), sulfur (S) or SO 2 . Ar represents an aromatic ring such as phenyl which is not X = S and n = 2. Also 4-nitrophenyl, 4-acetyl-aminophenyl, 4-chloromethyl, 3,4 dichlorophenyl, 4-methylphenyl, 4-methoxyphenyl, 3-dimethyl-aminophenol, 4-biphenyl, 4-pepoxy Substituted phenyl groups, such as phenyl, 4-benzylphenyl and 4-benzyloxyphenyl, are represented. Also representative of 1-naphthyl and 2-naphthyl groups. a) R´가 상기한 바와 같이 정의된 일반식(Ⅱ)의 화합물은a) a compound of formula (II) wherein R 'is defined as above n, X 및 Ar이 상기한 바와 같이 정의된 일반식(Ⅲ)의 화합물과n, X and Ar are compounds of the general formula (III) R이 상기한 바와같이 정의된 일반식(Ⅳ)의 알데히드와 반응하여 일반식(Ⅰ)의 화합물을 제조하거나,R is reacted with an aldehyde of general formula (IV) as defined above to produce a compound of general formula (I), or b) R´가 상기한 바와같이 정의된 일반식(Ⅴ)의 화합물은b) the compound of formula (V) wherein R 'is defined as n, X 및 Ar이 상기한 바와같이 정의된 일반식(Ⅳ)의 화합물과n, X and Ar are compounds of formula (IV) as defined above R은 상기한 바와같이 정의된 일반식(Ⅳ)의 알데히드와 반응하여 일반식(Ⅰ)의 화합물을 제조하거나, c) R 및 R´가 상기와 같이 정의된 일반식(Ⅶ)의 화합물은R is reacted with an aldehyde of formula (IV) as defined above to produce a compound of formula (I), or c) a compound of formula (VII) wherein R and R 'are defined as n, X 및 Ar이 상기와 같이 정의된 일반식(Ⅳ)의 화합물과 반응하여 일반식(Ⅰ)의 화합물을 제조하는 것을 특징으로 하는 (Ⅰ)의 4-알킬-1,4-디하이드로피리딘의 제조방법.4-alkyl-1,4-dihydropyridine of (I), wherein n, X and Ar are reacted with a compound of formula (IV) as defined above to produce a compound of formula (I) Manufacturing method. 일반식(Ⅰ)의 4-알킬-1,4-디하이드로피리딘이 PAF-아세테르 길항제로서 사용되는 용도.4-alkyl-1,4-dihydropyridine of formula (I) is used as PAF-aceter antagonist. 일반식(Ⅰ)의 화합물이 PAF-아세트르가 관여하는 병적상태 및 장애의 치료에 사용되는 용도.Use of the compound of formula (I) for the treatment of pathological conditions and disorders involving PAF-acetre. 제4항에 있어서, 일반식(Ⅰ)의 화합물이 염증의 과정, 건선, 사구체신염, 이식편거부, 만성 및 급성기관염, 기관지천식, 쇼크상태 및 알레르기의 치료에 사용되는 용도.Use according to claim 4, wherein the compound of formula (I) is used for the treatment of inflammation, psoriasis, glomerulonephritis, graft rejection, chronic and acute bronchitis, bronchial asthma, shock conditions and allergies. 일반식(Ⅰ)의 4-알킬-1,4-디하이드로피리딘이 세포면역의 촉진을 요하는 병적상태 및 장애의 치료에 사용되는 용도.4-alkyl-1,4-dihydropyridine of formula (I) is used for the treatment of pathological conditions and disorders requiring the promotion of cellular immunity. 제6항에 있어서, 일반식(Ⅰ)의 화합물이 면역결핍증후군 및 방어기능이 감소된 상태의 치료에 사용되는 용도.Use according to claim 6, wherein the compound of general formula (I) is used for the treatment of immunodeficiency syndrome and a condition with reduced protective function. 제3항, 4항, 5항, 6항 및 7항에 있어서, 수용성(受容性)약용 부형제와 함께 일반식(Ⅰ)의 화합물들을 함유하는 약제로서의 용도.Use according to claim 3, 4, 5, 6 and 7 as a medicament containing the compound of general formula (I) together with a water-soluble pharmaceutical excipient. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019920016053A 1991-09-09 1992-09-03 1,4-dihydropyridine compound that antagonizes KR930005978A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP91500103.6 1991-09-09
EP91500103A EP0531598A1 (en) 1988-01-21 1991-09-09 1,4-Dihydropyridines with paf-antagonistic activity

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KR930005978A true KR930005978A (en) 1993-04-20

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