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    • 4. 发明授权
    • 1-hydroxy-2-pyridones, a process for their preparation, and medicaments
which contain them, and intermediates formed in the preparation of the
1-hydroxy-2-pyridones
    • 1-羟基-2-吡啶酮,其制备方法和含有它们的药物,以及在制备1-羟基-2-吡啶酮时形成的中间体
    • US4797409A
    • 1989-01-10
    • US038903
    • 1987-04-16
    • Gerhard LohausWalter DittmarHeinz HanelWolfgang RaetherDieter ReuschlingBengt-Thomas Grobel
    • Gerhard LohausWalter DittmarHeinz HanelWolfgang RaetherDieter ReuschlingBengt-Thomas Grobel
    • A61K31/44C07D213/89C07D309/38
    • C07D213/89C07D309/38
    • New 1-hydroxy-2-pyridones of the general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3, which are identical or different, denote hydrogen or lower alkyl having 1-4 carbon atoms, R.sup.1 and R.sup.3 preferably being hydrogen, and R.sup.2 preferably being methyl,X denotes S or, preferably, O,Y denotes hydrogen or up to 2 halogen atoms, namely chlorine and/or bromine,Z denotes a single bond or the bivalent radicals O, S, --CR.sub.2 -- (R=H or C.sub.1 -C.sub.4 -alkyl) or other 2-valent radicals with 2-10 carbon and, optionally, oxygen and/or sulfur atoms linked to form a chain, it being obligatory when the radicals contain 2 or more oxygen and/or sulfur atoms for the latter to be separated by at least 2 carbon atoms, and it being possible for 2 adjacent carbon atoms also to be linked together by a double bond, and the free valencies of the carbon atoms being saturated by H and/or C.sub.1 -C.sub.4 -alkyl groups,Ar denotes an aromatic ring system which has up to two rings and can be substituted by up to three radicals from the group comprising fluorine, chlorine, bromine, methoxy, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl and trifluoromethoxy, are prepared by a variety of process variants. The compounds and their physiologically tolerated salts with inorganic or organic bases mainly have antimycotic, anti-bacterial and antiviral activity. The compounds of the formula V ##STR2## in which R.sup.1, R.sup.2, R.sup.3, X, Y, Z and Ar have the same meaning as in formula I, which occur in the preparation of the compounds of the formula I, are also new.
    • 通式I的新的1-羟基-2-吡啶酮其中R1,R2和R3相同或不同,表示氢或具有1-4个碳原子的低级烷基,R1和R3优选为氢, 并且R2优选为甲基,X表示S或优选O,Y表示氢或最多2个卤素原子,即氯和/或溴,Z表示单键或二价基团O,S,-CR 2 - (R = H或C 1 -C 4 - 烷基)或其它具有2-10个碳的任选的2-价基团和任选的连接形成链的氧和/或硫原子,当基团含有2个或更多个氧和/或 后者的硫原子被至少2个碳原子分开,并且可以通过双键将两个相邻的碳原子连接在一起,并且碳原子的自由价被H和/或C1饱和 -C4-烷基,Ar表示芳族环系,其具有多达两个环,并且可以被至少三个基团取代。 通过各种工艺变体制备氟,氯,溴,甲氧基,C 1 -C 4 - 烷基,三氟甲基和三氟甲氧基。 化合物及其与无机或有机碱的生理耐受盐主要具有抗真菌,抗细菌和抗病毒活性。 其中R 1,R 2,R 3,X,Y,Z和Ar具有与式I化合物相同的含义的式Ⅴ的化合物也是新的 。
    • 9. 发明授权
    • Cosmetic compositions
    • 化妆品组合物
    • US4711775A
    • 1987-12-08
    • US677891
    • 1984-12-04
    • Walter DittmarEberhard FuttererGerhard Lohaus
    • Walter DittmarEberhard FuttererGerhard Lohaus
    • A61K8/00A61K20060101A61K8/33A61K8/37A61K8/49A61K8/92A61K31/12A61K31/44A61P17/08A61Q5/00A61Q5/02A61Q5/12A61Q7/00C07D20060101C07D207/26C07D213/89C11D3/28C11D3/48A61K7/06
    • A61Q5/006A61K8/4926Y10S424/01Y10S424/02Y10S424/04
    • A cosmetic composition comprising a content of an 1-hydroxy-2-pyridone of the general formula ##STR1## in which R.sub.1 stands for hydrogen, alkyl of 1 to 17 carbon atoms, alkenyl of 2 to 17 carbon atoms, cycloalkyl of 5 to 8 carbon atoms, bicycloalkyl of 7 to 9 carbon atoms, cycloalkyl-alkyl of 1 to 4 alkyl carbon atoms, the cycloalkyl groups being optionally substituted by alkyl groups of 1 to 4 carbon atoms, aryl, aralkyl of 1 to 4 alkyl carbon atoms, aryl-alkenyl of 2 to 4 alkenyl carbon atoms, aryloxy-alkyl or arylthio-alkyl of 1 to 4 alkyl carbon atoms, benzhydryl, phenylsulfonyl-alkyl of 1 to 4 alkyl carbon atoms, furyl or furyl-alkenyl of 2 to 4 alkenyl carbon atoms, the aryl groups being optionally substituted by alkyl of 1 to 4 carbon atoms, by alkoxy of 1 to 4 carbon atoms, by nitro, cyano or halogen atoms,R.sub.2 stands for hydrogen, alkyl of 1 to 4 carbon atoms, alkenyl or alkinyl of 2 to 4 carbon atoms, halogen atoms or benzyl,R.sub.3 stands for hydrogen, alkyl of 1 to 4 carbon atoms or phenyl, andR.sub.4 stands for hydrogen, alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 4 carbon atoms, methoxy-methyl, halogen or benzyl, and/or salt thereof, which may be used as an anti-dandruff agent.
    • 一种化妆品组合物,其包含通式“IMAGE”的1-羟基-2-吡啶酮的含量,其中R1代表氢,1至17个碳原子的烷基,2至17个碳原子的链烯基,5至8个的环烷基 碳原子数为7〜9的双环烷基,1〜4个碳原子的环烷基 - 烷基,环烷基任选被1〜4个碳原子的烷基取代,芳基,1〜4个碳原子的芳烷基,芳基 2至4个烯基碳原子的烯基,1至4个烷基碳原子的芳氧基 - 烷基或芳硫基 - 烷基,2至4个烷基碳原子的二苯甲基,苯基磺酰基 - 烷基,2至4个烯基碳原子的呋喃基或呋喃基 - 烯基 ,芳基任选被1至4个碳原子的烷基,1至4个碳原子的烷氧基,硝基,氰基或卤素原子取代,R2代表氢,1至4个碳原子的烷基,烯基或炔基 2至4个碳原子,卤素原子或苄基,R3代表氢,1至4个碳原子的烷基 R苯基,R4代表氢,1至4个碳原子的烷基,2至4个碳原子的链烯基,甲氧基 - 甲基,卤素或苄基,和/或其盐,可用作抗头皮屑剂。
    • 10. 发明授权
    • Pyridones as antidandruff agents
    • 吡啶酮作为去头皮屑剂
    • US4185106A
    • 1980-01-22
    • US605210
    • 1975-08-15
    • Walter DittmarEberhard FuttererGerhard Lohaus
    • Walter DittmarEberhard FuttererGerhard Lohaus
    • A61K8/49A61K31/44A61Q5/00
    • A61Q5/006A61K8/4926Y10S424/04
    • A cosmetic composition comprising a content of an 1-hydroxy-2-pyridone of the general formula ##STR1## in which R.sub.1 stands for hydrogen, alkyl of 1 to 17 carbon atoms, alkenyl of 2 to 17 carbon atoms, cycloalkyl of 5 to 8 carbon atoms, bicycloalkyl of 7 to 9 carbon atoms, cycloalkyl-alkyl of 1 to 4 alkyl carbon atoms, the cycloalkyl groups being optionally substituted by alkyl groups of 1 to 4 carbon atoms, aryl, aralkyl of 1 to 4 alkyl carbon atoms, aryl-alkenyl of 2 to 4 alkenyl carbon atoms, aryloxy-alkyl or arylthio-alkyl of 1 to 4 alkyl carbon atoms, benzhydryl, phenylsulfonyl-alkyl of 1 to 4 alkyl carbon atoms, furyl or furyl-alkenyl of 2 to 4 alkenyl carbon atoms, the aryl groups being optionally substituted by alkyl of 1 to 4 carbon atoms, by alkoxy of 1 to 4 carbon atoms, by nitro, cyano or halogen atoms, R.sub.2 stands for hydrogen, alkyl of 1 to 4 carbon atoms, alkenyl or alkinyl of 2 to 4 carbon atoms, halogen atoms or benzyl, R.sub.3 stands for hydrogen, alkyl of 1 to 4 carbon atoms or phenyl, and R.sub.4 stands for hydrogen, alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 4 carbon atoms, methoxy-methyl, halogen or benzyl, and/or salt thereof, which may be used as an anti-dandruff agent.
    • 一种化妆品组合物,其包含通式“IMAGE”的1-羟基-2-吡啶酮的含量,其中R1代表氢,1至17个碳原子的烷基,2至17个碳原子的链烯基,5至8个的环烷基 碳原子数为7〜9的双环烷基,1〜4个碳原子的环烷基 - 烷基,环烷基任选被1〜4个碳原子的烷基取代,芳基,1〜4个碳原子的芳烷基,芳基 2至4个烯基碳原子的烯基,1至4个烷基碳原子的芳氧基 - 烷基或芳硫基 - 烷基,2至4个烷基碳原子的二苯甲基,苯基磺酰基 - 烷基,2至4个烯基碳原子的呋喃基或呋喃基 - 烯基 ,芳基任选被1至4个碳原子的烷基,1至4个碳原子的烷氧基,硝基,氰基或卤素原子取代,R2代表氢,1至4个碳原子的烷基,烯基或炔基 2至4个碳原子,卤素原子或苄基,R3代表氢,1至4个碳原子的烷基 R苯基,R4代表氢,1至4个碳原子的烷基,2至4个碳原子的链烯基,甲氧基 - 甲基,卤素或苄基,和/或其盐,可用作抗头皮屑剂。