KR970032857A - Pharmaceutical composition - Google Patents

Pharmaceutical composition Download PDF

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Publication number
KR970032857A
KR970032857A KR1019950066607A KR19950066607A KR970032857A KR 970032857 A KR970032857 A KR 970032857A KR 1019950066607 A KR1019950066607 A KR 1019950066607A KR 19950066607 A KR19950066607 A KR 19950066607A KR 970032857 A KR970032857 A KR 970032857A
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South Korea
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group
substituted
hydrogen atom
alkyl
alkyl group
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KR1019950066607A
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Korean (ko)
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김현석
표성수
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김준웅
주식회사 선경인더스트리
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Publication of KR970032857A publication Critical patent/KR970032857A/en

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Abstract

본 발명은 약제조성물에 관한 것으로서 더욱 상세하게는 혈소판 활성화인자(Platelet Activating Factor:PAF)수용체 길항제로서 효과를 나타내는 징코라이드 유도체와 5-리포옥시게나제 저해제로서의 활성을 가지는 티아졸리딘 유도체를 동시에 함유하여 두 화합물간의 상승적 작용에 의해 생체내 혈소판 활성화인자와 류코트리엔의 생성을 효과적으로 억제하여 이러한 물질에 의해 발생하는 염증질환이나 알레르기질환의 예방과 치료에 유용한 신규 약제조성물에 관한 것이다.The present invention relates to a pharmaceutical composition, and more particularly, to simultaneously contain a zincolide derivative having an effect as a platelet activating factor (PAF) receptor antagonist and a thiazolidine derivative having activity as a 5-lipooxygenase inhibitor. The present invention relates to a novel pharmaceutical composition useful for the prevention and treatment of inflammatory or allergic diseases caused by such substances by effectively inhibiting the production of platelet activators and leukotrienes in vivo by synergistic action between two compounds.

Description

약제 조성물Pharmaceutical composition

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

Claims (2)

다음 구조식(Ⅰ)로 표시되는 징코라이드 유도체와 다음 구조식(Ⅱ)로 표시되는 티아졸리딘 유도체를 함유하는 약제조성물.A pharmaceutical composition containing a zinc chloride derivative represented by the following structural formula (I) and a thiazolidine derivative represented by the following structural formula (II). 상기식에서, R2는 수소원자 또는 R1을 나타내며, R1는 -A-Ar, -A-Z-Ar, -CO-Ar, SO2-Ar, -A-Het, 또는 -A-NR4R5를 나타내고, 여기서 A는 C1~C8의 알킬렌기, 또는 C1~C5의 직쇄 또는 측쇄의 알킬기로 치환된 C1~C8의 알킬렌기를 나타내고; Z는 탄소, 산소, 황 또는 질소원자를 나타내며; Ar는 페닐기, 피리딜기, 나프티리, 피리미딜기, 퀴놀릴기, 또는 관능기를 1~5개 가지는 치환된 페닐기. 피리딜기, 나프틸기, 피리미딜기 또는 퀴놀릴기를 나타내며; Het, 는 질소, 산소 또는 황원자를1개 또는 그 이상 포함하는 포화 또는 불포화 헤테로시클릭기를 나타내며; R4및 R5는 각각 서로 같거나 다른 것으로서 수소원자, 알킬기 또는 시클로알킬기를 나타낸다. 이때 Ar에 치환될 수 있는 관능기로는 수소원자, 할로겐원자, 하이드록실기, 카르복실산기, C1-C10의 알킬기, C1~C10의 알케닐기, C1~C10의 알키닐기, C1~C10의 할로알킬기, C1~C10의 알콕시기, C1~C10의 알케닐옥시기, C1~C10의 알키닐옥시기, C1~C10의 할로알콕시기, 페닐기, 페녹시기, 아랄킬기, 아랄킬옥시기, 치환된 페닐기, 치환된 페녹시기, 치환된 아랄킬기, 치환된 아랄킬옥시기, COR4, -CONR4R5, -CO2R4, -NHCOR4, -NH(OH), -N(OH)COR4, -CH2OR4, -OCH2CO2R4, -CH2SR4, -CH2NR4R5, -SR4, -OSR4, -SO2NR4R5, -NR4R5, NR4SO2R5(이때, r4및 R5는 각각 서로 같거나 다른 것으로서 수소원자, C1~C10알킬기 또는 C3~C10의 시클로알킬기.)-SCX3(X는 할로겐원자), -CN, -NO2또는 Ar에 환형으로 연결된 -Z-A-Z'-(Z는 A는 각각 상기에서 정의한 바와 같고, Z'는 탄소, 산소 황 또는 질소원자)이고, N은 0,1,2 또는 3이고, Q는 알킬기, 페닐기, 치환된 페닐기 또는 피리딜기를 나타내고, G1, G2및 G3은 각각 서로 같거나 또는 다른 것으로서 수소원자, 알킬기, 시클로알킬기, 페닐기, 치환된 페닐기를 나타내고, G4,G5, G6, G7및 G8은 각각 서로 같거나 다른 것으로서 수소원자, 하이드록실기, 할로겐원자, 알킬기, 알콕시기, 니트로기, 아미노기, 치환된 아미노기, 할로알킬기, 랄킬옥시기Wherein R 2 represents a hydrogen atom or R 1 , and R 1 represents -A-Ar, -AZ-Ar, -CO-Ar, SO 2 -Ar, -A-Het, or -A-NR 4 R 5 represents a, where a is C 1 ~ C 8 alkyl group, or C 1 ~ C 5 straight or represents alkylene of C 1 ~ C 8 alkyl group substituted with a group of the side chain; Z represents a carbon, oxygen, sulfur or nitrogen atom; Ar is a substituted phenyl group having 1 to 5 phenyl groups, pyridyl groups, naphthyri, pyrimidyl groups, quinolyl groups, or functional groups. A pyridyl group, a naphthyl group, a pyrimidyl group or a quinolyl group; Het, represents a saturated or unsaturated heterocyclic group containing one or more nitrogen, oxygen or sulfur atoms; R 4 and R 5 are the same as or different from each other, and represent a hydrogen atom, an alkyl group, or a cycloalkyl group. In this case, a functional group which may be substituted with Ar is a hydrogen atom, a halogen atom, a hydroxyl group, a carboxylic acid group, a C 1 -C 10 alkyl group, a C 1 ~ C 10 alkenyl group, C 1 ~ C 10 alkynyl group, C 1 -C 10 haloalkyl group, C 1 -C 10 alkoxy group, C 1 -C 10 alkenyloxy group, C 1 -C 10 alkynyloxy group, C 1 -C 10 haloalkoxy group, phenyl group, Phenoxy group, aralkyl group, aralkyloxy group, substituted phenyl group, substituted phenoxy group, substituted aralkyl group, substituted aralkyloxy group, COR 4 , -CONR 4 R 5 , -CO 2 R 4 , -NHCOR 4 ,- NH (OH), -N (OH) COR 4 , -CH 2 OR 4 , -OCH 2 CO 2 R 4 , -CH 2 SR 4 , -CH 2 NR 4 R 5 , -SR 4 , -OSR 4 ,- SO 2 NR 4 R 5 , -NR 4 R 5 , NR 4 SO 2 R 5 , wherein r 4 and R 5 are the same as or different from each other and are each selected from a hydrogen atom, a C 1 to C 10 alkyl group or a C 3 to C 10 A cycloalkyl group.)-SCX 3 (X is a halogen atom), -CN, -NO 2 or -ZA-Z '-(Z is A as defined above and Z' is each Carbon, oxygen sulfur or nitrogen atom), N is 0,1,2 or 3, Q represents an alkyl group, a phenyl group, a substituted phenyl group or a pyridyl group, and G 1 , G 2 and G 3 are each the same or Others represent a hydrogen atom, an alkyl group, a cycloalkyl group, a phenyl group, a substituted phenyl group, and G 4 , G 5 , G 6 , G 7 and G 8 each represent the same or different hydrogen atoms, hydroxyl groups, halogen atoms, alkyl groups. , Alkoxy group, nitro group, amino group, substituted amino group, haloalkyl group, ralkoxyoxy group 를 나타내며 (이때, G15는 알킬기를 나타냄),(Wherein G 15 represents an alkyl group), T는 수소원자, 하이드록시기, 알킬기, -(CH3)2-O-G10,T is a hydrogen atom, a hydroxyl group, an alkyl group,-(CH 3 ) 2 -OG 10 , 또는 -(CH2)3-NG13G14를 나타낸다. 이때, m은 1,2,3 또는 4이고; G9는 수소원자, 페닐기, 치환된 페닐기 또는 피리딜기이고; G10은 수소원자, 알킬기 또는 알카노일기이고; G11은 알킬기, 알콕시기 또는 치환된 아미노기이고; G12는 알킬기 또는 페닐기이고; G16은 수소원자 또는 알킬기이고; G13수소원자, 알킬기 또는 알카노일기이고; G14는 수소원자, 알킬기 또는 G13과 G14가 서로 연결된 5~7각형의 시클로아미노기, 치환된 시클로아미노기 또는 또 다른 헤테로원자를 서택적으로 포함하는 시클로아미노기를 나타낸다.Or-(CH 2 ) 3 -NG 13 G 14 . Wherein m is 1,2,3 or 4; G 9 is a hydrogen atom, a phenyl group, a substituted phenyl group or a pyridyl group; G 10 is a hydrogen atom, an alkyl group or an alkanoyl group; G 11 is an alkyl group, an alkoxy group or a substituted amino group; G 12 is an alkyl group or a phenyl group; G 16 is a hydrogen atom or an alkyl group; G 13 is a hydrogen atom, an alkyl group or an alkanoyl group; G 14 represents a hydrogen atom, an alkyl group or a cycloamino group alternatively containing a 5- to 7-membered cycloamino group, a substituted cycloamino group or another hetero atom, to which G 13 and G 14 are connected to each other. 제1항에 있어서, 상기 구조식(Ⅰ)로 표시되는 징코라이드 유도체와 상기 구조식(Ⅱ)로 표시되는 티아졸리딘 유도체가 1:3~3:1 중량비로 혼합된 것임을 특징으로 하는 약제조성물.The pharmaceutical composition according to claim 1, wherein the zincolide derivative represented by the structural formula (I) and the thiazolidine derivative represented by the structural formula (II) are mixed at a weight ratio of 1: 3 to 3: 1. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019950066607A 1995-12-29 1995-12-29 Pharmaceutical composition KR970032857A (en)

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0316723A1 (en) * 1987-11-20 1989-05-24 Hoechst-Roussel Pharmaceuticals Incorporated 3-[4(1-Substituted-4-piperazinyl)butyl]-4-thiazolidinones a process for their preparation and their use as medicaments
JPH01190679A (en) * 1988-01-22 1989-07-31 Sumitomo Pharmaceut Co Ltd Optically active novel thiazolidine-4-one derivative and acid-addition salt thereof
US4992455A (en) * 1987-05-22 1991-02-12 Sumitomo Pharmaceuticals Company, Limited Thiazolidin-4-one derivatives useful for treating diseases caused by platelet activating factor
JPH05255341A (en) * 1991-04-09 1993-10-05 Soc Conseils Rech Appl Scient Sa (Scras) Preparation of ginkgolide b from ginkgollide c
KR960022486A (en) * 1994-12-29 1996-07-18 김준웅 New Thiazolidin-4-one Derivatives
KR0136986B1 (en) * 1993-12-31 1998-04-25 김준웅 New ginkoride derivatives and a process preparing them

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4992455A (en) * 1987-05-22 1991-02-12 Sumitomo Pharmaceuticals Company, Limited Thiazolidin-4-one derivatives useful for treating diseases caused by platelet activating factor
EP0316723A1 (en) * 1987-11-20 1989-05-24 Hoechst-Roussel Pharmaceuticals Incorporated 3-[4(1-Substituted-4-piperazinyl)butyl]-4-thiazolidinones a process for their preparation and their use as medicaments
JPH01190679A (en) * 1988-01-22 1989-07-31 Sumitomo Pharmaceut Co Ltd Optically active novel thiazolidine-4-one derivative and acid-addition salt thereof
JPH05255341A (en) * 1991-04-09 1993-10-05 Soc Conseils Rech Appl Scient Sa (Scras) Preparation of ginkgolide b from ginkgollide c
KR0136986B1 (en) * 1993-12-31 1998-04-25 김준웅 New ginkoride derivatives and a process preparing them
KR960022486A (en) * 1994-12-29 1996-07-18 김준웅 New Thiazolidin-4-one Derivatives

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