KR880007537A - Triazine derivatives - Google Patents

Triazine derivatives Download PDF

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KR880007537A
KR880007537A KR870014144A KR870014144A KR880007537A KR 880007537 A KR880007537 A KR 880007537A KR 870014144 A KR870014144 A KR 870014144A KR 870014144 A KR870014144 A KR 870014144A KR 880007537 A KR880007537 A KR 880007537A
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triazine
isothiazolo
compound
formula
alkyl
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KR870014144A
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리차드 앨우드 마이클
헤드리 크렉켙 피터
로우톤 제프리
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진 자커스 오가이, 프리돌린 클라우스너
에프.호프만-라 로슈 앤드 캄파니 아크티엔 게젤샤프트
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

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Description

트리라진 유도체Triazine derivatives

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

Claims (28)

일반식(Ⅰ)의 트리아진 유도체 및 R1및/또는 R2가 아미노를 나타내는 일반식(Ⅰ) 화합물의 약제학적으로 허용되는 산 부가염.A pharmaceutically acceptable acid addition salt of a triazine derivative of formula (I) and a compound of formula (I) in which R 1 and / or R 2 represent amino. 상기식에서, A는 다음 일반식(a), (b) 또는 (c)의 그룹을 나타낸다.Wherein A represents a group of the following general formulas (a), (b) or (c). [여기에서, R1및 R2는 각각 수소, 할로겐, 트리플루오로메틸, 니트로, 아미노, 시아노, C1-C6-알킬, C1-C6-알콕시, C3-C6-알케닐옥시, C1-C6-알킬티오, C1-C6-알카노일-아미노, 아릴옥시, 아릴-(C1-C6-알킬), 아릴-(C1-C6-알콕시), 아릴-(C1-C6-알콕시)카보닐아미노 또는 일반식 -O-CH2-R3(여기에서, R3는 하이드록시-(C1-C4-알킬) 또는 인접한 디하이드록시-(C2-C5-알킬)을 나타낸다)의 그룹을 나티내거나, R1및 R2는 인접한 탄소원자와 함께 식 -CH=CH-CH=CH- 또는 -CH2-CH2-O의 그룹을 나타낸다].[Wherein R 1 and R 2 are each hydrogen, halogen, trifluoromethyl, nitro, amino, cyano, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 3 -C 6 -al Kenyloxy, C 1 -C 6 -alkylthio, C 1 -C 6 -alkanoyl-amino, aryloxy, aryl- (C 1 -C 6 -alkyl), aryl- (C 1 -C 6 -alkoxy), Aryl- (C 1 -C 6 -alkoxy) carbonylamino or a general formula —O—CH 2 —R 3 , wherein R 3 is hydroxy- (C 1 -C 4 -alkyl) or adjacent dihydroxy- Or (C 2 -C 5 -alkyl)) or R 1 and R 2 together with adjacent carbon atoms are a group of the formula -CH = CH-CH = CH- or -CH 2 -CH 2 -O. ]. 제1항에 있어서, A가 일반식(a), (b) 또는 (c)의 그룹에서 R1및 R2가 각각 수소, 할로겐, 트리플루오로메틸, 니트로, 아미노, 시아노, C1-C6-알킬, C1-C6-알콕시, C1-C6-알킬티오, C1-C6-알카노일 아미노, 아릴옥시, 아릴-(C1-C6-알킬) 아릴-(C1-C6-알킬)또는 아릴-C4-C6-알콕시 카보닐아미노를 나타내거나, R1및 R2가 인접한 탄소원자와 함께식 -CH=CH-CH=CH- 또는 -CH2-CH2-O-의 그룹을 나타내는 화합물.A compound according to claim 1, wherein A is R 1 and R 2 in the group of formula (a), (b) or (c) is hydrogen, halogen, trifluoromethyl, nitro, amino, cyano, C 1- C 6 -alkyl, C 1 -C 6 -alkoxy, C 1 -C 6 -alkylthio, C 1 -C 6 -alkanoyl amino, aryloxy, aryl- (C 1 -C 6 -alkyl) aryl- (C 1- C 6 -alkyl) or aryl-C 4 -C 6 -alkoxycarbonylamino, or R 1 and R 2 together with the adjacent carbon atom are represented by the formula -CH = CH-CH = CH- or -CH 2- A compound representing a group of CH 2 -O-. 제1항 또는 제2항에 있어서, A가 일반식 (a)의 그룹을 나타내는 화합물.The compound of claim 1 or 2, wherein A represents a group of general formula (a). 제3항에 있어서, R1이 수소, 할로겐, 트리플루오로메틸 또는 시아노를 나타내고, R2가 C1-C6-알콕시, 아릴-(C1-C6-알콕시) 또는 일반식 -O-CH2-R3(여기에서, R3는 인접한 디하이드록시-(C2-C5-알킬)을 나타냄)을 나타내나, 단, R1및 R2중 적어도 하나는 수소 이외의 것을 나타내는 화합물.The compound of claim 3, wherein R 1 represents hydrogen, halogen, trifluoromethyl or cyano, and R 2 represents C 1 -C 6 -alkoxy, aryl- (C 1 -C 6 -alkoxy) or general formula —O. -CH 2 -R 3 , wherein R 3 represents adjacent dihydroxy- (C 2 -C 5 -alkyl), provided that at least one of R 1 and R 2 is other than hydrogen compound. 7-(3-트리플루오로메틸-4-메톡시페닐)이소티아졸로 [4,5-d]-1,2,3-트리아진-4(3H)-온.7- (3-trifluoromethyl-4-methoxyphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one. 7-(3-클로로-4-메톡시페닐)이소티아졸[4,5-d]-1,2,3-트리아진-4(3H)-온.7- (3-chloro-4-methoxyphenyl) isothiazol [4,5-d] -1,2,3-triazine-4 (3H) -one. 7-(3-플루오로-4-메톡시페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온.7- (3-fluoro-4-methoxyphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one. 7-(3-트리플루오로메틸페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온.7- (3-trifluoromethylphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one. 7-(4-이소프로폭시페닐)이소티아졸로[4,5-d]-1,2,3--트리아진-4(3H)-온.7- (4-isopropoxyphenyl) isothiazolo [4,5-d] -1,2,3--triazine-4 (3H) -one. 7-(4-벤질옥시페닐)이소티아졸로 [4,5-d]-1,2,3-트리아진-4(3H)-온.7- (4-benzyloxyphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one. 7-(3-시아노-4-메톡시페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온.7- (3-cyano-4-methoxyphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one. 7-[3-시아노-4-(2,3-디하이드록시프로폭시)페닐]이소티아졸로 [4,5-d]-1,2,3-트리아진-4(3H) -온.7- [3-cyano-4- (2,3-dihydroxypropoxy) phenyl] isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one. 제1항 또는 제2항에 있어서, A가 일반식(c)의 그룹을 나타내는 화합물.The compound of claim 1 or 2, wherein A represents a group of formula (c). 제13항에 있어서, R1이 수소를 나타내고 R2가 C1-C6-알콕시를 나타내는 화합물.The compound of claim 13, wherein R 1 represents hydrogen and R 2 represents C 1 -C 6 -alkoxy. 7-(4-메톡시페닐)-7H-피라졸로 [3,4-d]-1,2,3-트리아진-4(3H)-온.7- (4-methoxyphenyl) -7H-pyrazolo [3,4-d] -1,2,3-triazine-4 (3H) -one. 제2항에 있어서, 7-페닐이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-에틸페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-메틸페닐)이소티아졸로 [4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-클로로페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-브로모페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-시아노페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-메톡시페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-메톡시페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-플루오로페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-아세트아미도페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-벤질옥시포름아미도페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-아미노페닐)이소티아졸로 [4,5-d]-1,2,3-트리아진 -4(3H)-온, 7-(4-니트로페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-클로로페닐)이소티아졸로 [4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-브로모페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-페녹시페닐)이소티아졸로[4, 5-d]-1, 2, 3-트리아진-4(3H)-온, 7-(2-나프틸)이소티아졸로[4,5-d]-1,2, 3-트리아진-4(3H)-온, 7-(2,3-디하이드로-5-벤조푸라닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3,5-디메틸페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-벤질페닐)이소티아졸로 [4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-이소프로필페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-[3,5-비스(트리플루오로메틸)페닐]이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(3-트리플루오로메틸-4-벤질옥시페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 8-페닐피리도-[3,4-d]-1,2,3-트리아진-4(3H)-온, 8-(3-트리플루오로메틸페닐)피리도[3,4-d]-1,2,3-트리아진-4(3H)-온, 7-페닐-7H-피라졸로[3,4-d]-1, 2, 3-트리아진-4(3H)-온, 7-(3-트리플루오로메틸페닐)-7H-피라졸로[3, 4-d]-1,2,3-트리아진-4(3H)-온, 7-(3-클로로페닐)-7H-피라졸로[3,4-d]-1,2,3-트리아진-4(3H)-온, 7-(4-에틸페닐)-7H-피라졸로[3,4-d]-1,2,3-트리아진-4(3H)-온, 7-(4-에틸페닐)-7H-피라졸로[3,4-d]-1,2,3-트리아진-4(3H)-온 및 7-(3-클로로-4-메콕시페닐)-7H-피라졸로[3,4-d]-1,2,3-트리아진-4(3H)-온으로부터 선택된 화합물.The compound according to claim 2, wherein 7-phenylisothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (3-ethylphenyl) isothiazolo [4, 5-d] -1,2,3-triazine-4 (3H) -one, 7- (3-methylphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 ( 3H) -one, 7- (3-chlorophenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (3-bromophenyl) iso Thiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (3-cyanophenyl) isothiazolo [4,5-d] -1,2, 3-triazine-4 (3H) -one, 7- (3-methoxyphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (4-methoxyphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (3-fluorophenyl) isothiazolo [4,5 -d] -1,2,3-triazine-4 (3H) -one, 7- (4-acetamidophenyl) isothiazolo [4,5-d] -1,2,3-triazine- 4 (3H) -one, 7- (4-benzyloxyformamidophenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (4 -Aminophenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (4-nitrophenyl) isothiazolo [ 4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (4-chlorophenyl) isothiazolo [4,5-d] -1,2,3-triazine -4 (3H) -one, 7- (4-bromophenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (4-phenoxy Ciphenyl) isothiazolo [4, 5-d] -1, 2, 3-triazine-4 (3H) -one, 7- (2-naphthyl) isothiazolo [4,5-d] -1 , 2,3-triazine-4 (3H) -one, 7- (2,3-dihydro-5-benzofuranyl) isothiazolo [4,5-d] -1,2,3-triazine -4 (3H) -one, 7- (3,5-dimethylphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (4- Benzylphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (3-isopropylphenyl) isothiazolo [4,5-d]- 1,2,3-triazine-4 (3H) -one, 7- [3,5-bis (trifluoromethyl) phenyl] isothiazolo [4,5-d] -1,2,3-tri Azine-4 (3H) -one, 7- (3-trifluoromethyl-4-benzyloxyphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H)- On, 8-phenylpyrido- [3,4-d] -1,2,3-triazine-4 (3H) -one, 8- (3-trifluoromethylphenyl) pyrido [3,4-d ] -1,2, 3-triazine-4 (3H) -one, 7-phenyl-7H-pyrazolo [3,4-d] -1, 2, 3-triazine-4 (3H) -one, 7- (3-tri Fluoromethylphenyl) -7H-pyrazolo [3, 4-d] -1,2,3-triazine-4 (3H) -one, 7- (3-chlorophenyl) -7H-pyrazolo [3,4 -d] -1,2,3-triazine-4 (3H) -one, 7- (4-ethylphenyl) -7H-pyrazolo [3,4-d] -1,2,3-triazine- 4 (3H) -one, 7- (4-ethylphenyl) -7H-pyrazolo [3,4-d] -1,2,3-triazine-4 (3H) -one and 7- (3-chloro 4-Mexoxyphenyl) -7H-pyrazolo [3,4-d] -1,2,3-triazine-4 (3H) -one. 제1항에 있어서, 7-(4-에틸페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-이소부틸페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-(4-알릴옥시-3-시아노페닐)이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-[3-시아노-4-(2-하이드록시에톡시)페닐]이소티아졸로[4,5-d]-1,2,3-트리아진-4(3H)-온, 7-[3-시아노-4-(3-하이드록시프로폭시)페닐]이소티아졸로 [4,5-d]-1,2,3-트리아진 -4(3H)-온, 7-[3-시아노-4-메틸티오페닐]이소티아졸로 [4,5-d]-1,2,3-트리아진-4(3H)-온, 8-(4-메톡시페닐)피리도 [3,4-d]-1,2,3-트리아진-4(3H)-온, 8-(4-벤질옥시페닐)피리도[3,4-d]-1,2,3-트리아진-4(3H)-온, 8-(3-플루오로-4-메톡시페닐)피리도[3,4-d]-1,2,3-트리아진-4(3H)-온, 8-(3-클로로-4-메톡시페닐)피리도[3,4-d]-1,2,3-트리아진-4(3H)-온, 8-(4-메톡시-3-트리플루오로메틸페닐)피리도[3,4-d]-1,2,3-트리아진-4(3H)-온 및 8-(4-벤질옥시-3-트리플루오로메틸페닐)피리도[3,4-d]-1,2,3-트리아진-4(3H)-온으로부터 선택된 화합물.The compound of claim 1, wherein 7- (4-ethylphenyl) isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (4-isobutylphenyl) Isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -one, 7- (4-allyloxy-3-cyanophenyl) isothiazolo [4,5-d ] -1,2,3-triazine-4 (3H) -one, 7- [3-cyano-4- (2-hydroxyethoxy) phenyl] isothiazolo [4,5-d] -1 , 2,3-triazine-4 (3H) -one, 7- [3-cyano-4- (3-hydroxypropoxy) phenyl] isothiazolo [4,5-d] -1,2, 3-triazine-4 (3H) -one, 7- [3-cyano-4-methylthiophenyl] isothiazolo [4,5-d] -1,2,3-triazine-4 (3H) -One, 8- (4-methoxyphenyl) pyrido [3,4-d] -1,2,3-triazine-4 (3H) -one, 8- (4-benzyloxyphenyl) pyrido [ 3,4-d] -1,2,3-triazine-4 (3H) -one, 8- (3-fluoro-4-methoxyphenyl) pyrido [3,4-d] -1,2 , 3-triazine-4 (3H) -one, 8- (3-chloro-4-methoxyphenyl) pyrido [3,4-d] -1,2,3-triazine-4 (3H)- On, 8- (4-methoxy-3-trifluoromethylphenyl) pyrido [3,4-d] -1,2,3-triazine-4 (3H) -one and 8- (4-benzyloxy 3-trifluoromethylphenyl) pyrido [3,4-d] -1,2,3-triazine-4 (3H) -one. 치료학적으로 활성인 물질로서 사용되는 제1항 내지 제17항중 어느 한항의 트리아진 유도체.The triazine derivative of any one of claims 1 to 17 used as a therapeutically active substance. 국소성 빈헐 또는 통풍(痛風)의 치료 또는 예방에 사용되는 제1항 내지 제17항중 어느 한 항의 트리아진 유도체.The triazine derivative according to any one of claims 1 to 17, which is used for the treatment or prevention of topical rash or gout. (a) R1및 R2가 각각 독립적으로 수소, 할로겐, 트리플루오로메틸, 니트로, 시아노, C1-C6-알킬, C1-C6-알콕시, C3-C6-알케닐옥시, Cl-C6-알킬티오, C1-C6-알카노일아미노, 아릴옥시, 아릴-(C1-C6-알킬), 아릴-C1-C6-알콕시아일-(C1-C6-알콕시)카보닐 아미노 또는 일반식 -O-CH2-R3(여기에서, R2는 하이드록시-(Cl-C4-알킬)을 나타냄)의 그룹을 나타내거나, R1및 R2가 인접한 탄소원자와 함께 -CH=CH-CH=CH- 또는 -CH2-CH2-O-를 나타내는 일반식(Ⅰ)의 화합물을 제조하는 경우에는, 일반식(Ⅱ)의 화합물을 아질산과 반응시키거나, (b) R1및/또는 R2가 아미노를 나타내는 일반식(Ⅰ)의 화합물을 제조하는 경우에는, R1및/또는 R2가 아릴-(C1-C6-알콕시)카보닐아미노를 나타내는 일반식(Ⅰ)의 화합물중에서 아릴-C4-C6-알콕시카보닐아미노 그룹(들)을 절단하거나, (c) R1및/또는 R2가 C1-C6-알카노일아미노를 나타내는 일반식(Ⅰ)의 화합물을 제조하는 경우에는, R1및/또는 R2가 아미노를 나타내는 일반식(Ⅰ)의 화합물을 적절하게 아실화시키거나, (d) R1및/또는 R2가 일반식 -O-CH2-R3(여기에서, R3는 하이드록시-(C1-C4-알킬)을 나타냄)의 화합물을 나타내는 일반식(Ⅰ)의 화합물을 제조하는 경우에는, R1및/또는 R2가 C3-C6-알케닐옥시를 나타내는 일반식(Ⅰ)의 화합물을 오존과 반응시키고 반응 생성물을 수소화 금속 착화합물로 환원시키거나, (e) R1및/또는 R2가 일반식 -O-CH2-R3(여기에서, R3는 인접한 디하이드록시-(C2-C5-알킬)을 나타냄)을 나타내는 일반식(Ⅰ)의 화합물을 제조하는 경우에는, R1및/또는 R2가 C3-C6-알케닐옥시를 나타내는 일반식(Ⅰ)의 화합물을 사산화오스뮴과 반응시키며, (f) 필요에 따라, R1및/또는 R2가 아미노를 나타내는 수득한 일반식(Ⅰ) 화합물을 약제학적으로 허용되는 산부가염으로 전환시킴을 포함하는, 제1항 내지 졔17항중 어느 한 항의 화합물을 제조하는 방법.(a) R 1 and R 2 are each independently hydrogen, halogen, trifluoromethyl, nitro, cyano, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 3 -C 6 -alkenyl Oxy, C 1 -C 6 -alkylthio, C 1 -C 6 -alkanoylamino, aryloxy, aryl- (C 1 -C 6 -alkyl), aryl-C 1 -C 6 -alkoxyyl- (C 1 -C 6 -alkoxy) carbonyl amino or a group of the formula -O-CH 2 -R 3 , wherein R 2 represents hydroxy- (C 1 -C 4 -alkyl), or R 1 And compounds of the general formula (II) in the case of preparing a compound of the general formula (I) in which R 2 represents -CH = CH-CH = CH- or -CH 2 -CH 2 -O- with an adjacent carbon atom. Is reacted with nitrous acid or (b) when preparing a compound of formula (I) wherein R 1 and / or R 2 represents amino, R 1 and / or R 2 is aryl- (C 1 -C 6 - an alkoxycarbonyl-amino group (s) - alkoxy) -C 4 -C 6 aryl group in the compound of general formula (ⅰ) represents the amino-carbonyl Stage or, (c) R 1 and / or R 2 is C 1 -C 6 - in the case of producing a compound represented by the general formula (Ⅰ) indicating alkanoylamino, R 1 and / or R 2 represents a general amino Suitably acylating the compound of formula (I), or (d) R 1 and / or R 2 is represented by the formula -O-CH 2 -R 3 , wherein R 3 is hydroxy- (C 1 -C When preparing a compound of the general formula (I) representing a compound of the formula 4 ), R 1 and / or R 2 represents a C 3 -C 6 -alkenyloxy compound of the general formula (I) Is reacted with ozone and the reaction product is reduced to a metal hydride complex, or (e) R 1 and / or R 2 is represented by the general formula —O—CH 2 —R 3 , wherein R 3 is adjacent dihydroxy- ( In the case of preparing a compound of formula (I), which represents C 2 -C 5 -alkyl), R 1 and / or R 2 represents C 3 -C 6 -alkenyloxy. Compound of osmium tetraoxide and half Sikimyeo, (f) if necessary, R 1 and / or R 2 is which comprises conversion of a formula (Ⅰ) compound obtained representing the amino to acid addition salts pharmaceutically acceptable, the first term to jye 17 Compounds A method of making a compound of any one of the preceding. 상기식에서, A1는 일반식(a'), (b') 또는 (C')을 나타낸다 :Wherein A 1 represents general formula (a '), (b') or (C '): [여기에서, R10및 R20은 각각 독립적으로 수소, 할로겐, 트리플루오로메틸, 니트로, 시아노, C1-C6-알킬, C1-C6-알콕시, C3-C6-알케닐옥시, C1-C6-알킬티오, C1-C6-알카노일아미노, 아릴옥시, 아릴-(C1-C6-알킬), 아릴(C1-C6-알콕시), 아릴-(C1-C6-알콕시)카보닐아미노 또는 일반식 -O-CH2-R30(여기에서, R30은 하이드록시-(C1-C4-알킬)을 나타냄)의 그룹을 나타내거나, R10및 R20은 인접한 탄소원자와 함께 식 -CH=CH-CH=CH- 또는 -CH2-CH2-O-의 그룹을 나타낸다.][Wherein, R 10 and R 20 are each independently hydrogen, halogen, trifluoromethyl, nitro, cyano, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 3 -C 6 -al Kenyloxy, C 1 -C 6 -alkylthio, C 1 -C 6 -alkanoylamino, aryloxy, aryl- (C 1 -C 6 -alkyl), aryl (C 1 -C 6 -alkoxy), aryl- Or represents a group of (C 1 -C 6 -alkoxy) carbonylamino or of the general formula —O—CH 2 —R 30 , wherein R 30 represents hydroxy- (C 1 -C 4 -alkyl) , R 10 and R 20 together with adjacent carbon atoms represent a group of the formula —CH═CH—CH═CH— or —CH 2 —CH 2 —O—. 제1항 내지 제17항중 어느 한 항의 트리아진유도체 및 치료학적으로 불활성인 부형제를 함유하는 약제.A medicament containing the triazine derivative of any one of claims 1 to 17 and a therapeutically inert excipient. 제1항 내지 제17항중 어느 한 항의 트리아진 유도체 및 치료학적으로 불활성인 부형제를 함유하는 국소성 빈혈 또는 통풍의 치료 또는 예방용 약제.18. A medicament for the treatment or prevention of ischemia or gout, comprising the triazine derivative of any one of claims 1 to 17 and a therapeutically inert excipient. 병의 치료 또는 예방을 위한 제1항 내지 제17항중 어느 한 항의 트리아진 유도체의 용도.Use of the triazine derivative of any one of claims 1 to 17 for the treatment or prevention of a disease. 국소성 빈혈 또는 통풍의 치료 또는 예방을 위한 제1항 내지 제17항중 어느 한 항의 트리아진 유도체의 용도.Use of the triazine derivative of any one of claims 1 to 17 for the treatment or prevention of ischemia or gout. 국소성 빈혈 및/또는 통풍에 대한 약제의 제조를 위한 제1항 내지 제17항중 어느 한 항의 트리아진 유도체의 용도.Use of the triazine derivative of any one of claims 1 to 17 for the manufacture of a medicament for ischemia and / or gout. 제20항에서 청구된 방법 또는 이들의 화학적 대응법에 의해 제조된 제1항 내지 제17항중 어느 한 항의 트리아진 유도체.The triazine derivative of any one of claims 1 to 17 prepared by the method as claimed in claim 20 or a chemical counterpart thereof. 상기 언급한 바와 같은 발명.Invention as mentioned above. 국소성 빈혈 및/또는 통풍의 치료를 필요로 하는 환자에게 제1항 내지 제17항 중 어느 한 항의 트리아진 유도체의 효과적인 양을 투여함을 포함하는, 국소성 빈혈 및/또는 통풍의 치료 또는 예방 방법.A method of treating or preventing ischemia and / or gout, comprising administering an effective amount of the triazine derivative of any one of claims 1 to 17 to a patient in need thereof. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR870014144A 1986-12-12 1987-12-11 Triazine derivatives KR880007537A (en)

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