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    • 1. 发明授权
    • Topical application agents against mimic and age-related wrinkles
    • 针对模仿和年龄相关皱纹的局部应用剂
    • US07964630B2
    • 2011-06-21
    • US11718496
    • 2005-11-01
    • Dominic ImfeldHugo ZieglerPeter Wikstroem
    • Dominic ImfeldHugo ZieglerPeter Wikstroem
    • A61K31/40C07D207/16
    • C07K5/0821C07K5/0202C07K5/0806C07K5/0815C07K5/1008
    • The compounds of formula (I) wherein X represents a bond or NH—CH(C═O)—(CH2)3+n—NH—R5, n represents 0, 1 or 2, R1, R4 and R5—independently from each other—represent hydrogen, possibly substituted C1-C6-alkyl, amidino or tetra-C1-C6-alkylamidinium, R2 represents hydrogen or possibly substituted C1-C6-alkyl or R1 and R2 together with the residue to which they are bound represent a 5- to 7-membered, saturated ring, R3 represents C1-C12-alkoxy, C1-C12-alkylamino, possibly substituted aryl-C1-C6-alkylamino, possibly substituted heteroaryl-C1-C6-alkylamino, possibly substituted aryl-C1-C6-alkoxy or possibly substituted heteroaryl-C1-C6-alkoxy, and R6 represents hydrogen or, when n is 1, also amino or together with R1 and the residue to which R6 and R1 are bound a 5- to 7-membered, saturated ring, as well as their physiologically acceptable salts are new. They can be manufactured according to common methods and processed to topically applicable compositions that are appropriate for treating mimic and age-related wrinkles in human skin.
    • 其中X表示键或NH-CH(C = O) - (CH 2)3 + n-NH-R 5的式(I)化合物,n表示0,1或2,R 1,R 4和R 5 - 各自独立地 其它代表氢,可能被取代的C 1 -C 6 - 烷基,脒基或四-C 1 -C 6 - 烷基脒,R 2表示氢或可能被取代的C 1 -C 6 - 烷基或R 1和R 2与它们所连接的残基表示5 至7元饱和环,R 3表示C 1 -C 12 - 烷氧基,C 1 -C 12 - 烷基氨基,可能被取代的芳基-C 1 -C 6 - 烷基氨基,可能被取代的杂芳基-C 1 -C 6烷基氨基,可能被取代的芳基-C 1 -C 6 - 烷氧基或可能取代的杂芳基-C 1 -C 6 - 烷氧基,R 6表示氢,或者当n为1时也是氨基或与R 1和R 6和R 1结合的残基为5-至7-元饱和环 ,以及它们的生理学上可接受的盐是新的。 它们可以根据常规方法制造并加工成适用于治疗人类皮肤中模拟和年龄相关皱纹的局部适用组合物。
    • 2. 发明申请
    • NOVEL TOPICAL APPLICATION AGENTS AGAINST MIMIC AND AGE-RELATED WRINKLES
    • 关于MIMIC和AGE相关皱纹的新型局部应用代理
    • US20090111731A1
    • 2009-04-30
    • US11718496
    • 2005-11-01
    • Dominic ImfeldHugo ZieglerPeter Wikstroem
    • Dominic ImfeldHugo ZieglerPeter Wikstroem
    • A61K38/00C07D207/22C07D401/06C07D403/06A61Q19/00C07K5/00A61K31/40A61K31/454
    • C07K5/0821C07K5/0202C07K5/0806C07K5/0815C07K5/1008
    • The compounds of formula (I) wherein X represents a bond or NH—CH(C═O)—(CH2)3+n—NH—R5, n represents 0, 1 or 2, R1, R4 and R5—independently from each other—represent hydrogen, possibly substituted C1-C6-alkyl, amidino or tetra-C1-C6-alkylamidinium, R2 represents hydrogen or possibly substituted C1-C6-alkyl or R1 and R2 together with the residue to which they are bound represent a 5- to 7-membered, saturated ring, R3 represents C1-C12-alkoxy, C1-C12-alkylamino, possibly substituted aryl-C1-C6-alkylamino, possibly substituted heteroaryl-C1-C6-alkylamino, possibly substituted aryl-C1-C6-alkoxy or possibly substituted heteroaryl-C1-C6-alkoxy, and R6 represents hydrogen or, when n is 1, also amino or together with R1 and the residue to which R6 and R1 are bound a 5- to 7-membered, saturated ring, as well as their physiologically acceptable salts are new. They can be manufactured according to common methods and processed to topically applicable compositions that are appropriate for treating mimic and age-related wrinkles in human skin.
    • 其中X表示键或NH-CH(CO) - (CH 2)3 + n-NH-R 5的式(I)化合物,n表示0,1或2,R 1,R 4和R 5 - 代表氢,可能被取代的C 1 -C 6 - 烷基,脒基或四-C 1 -C 6 - 烷基脒,R 2表示氢或可能被取代的C 1 -C 6烷基或R 1和R 2与它们所连接的残基一起代表5- 7元饱和环,R 3表示C 1 -C 12烷氧基,C 1 -C 12烷基氨基,可能被取代的芳基-C 1 -C 6烷基氨基,可能被取代的杂芳基-C 1 -C 6 - 烷基氨基,可能被取代的芳基-C 1 -C 6 - 烷氧基 或可能被取代的杂芳基-C 1 -C 6 - 烷氧基,并且R 6表示氢,或者当n为1时也是氨基或与R 1一起并且与R 6和R 1结合的残基为5-至7-元饱和环,如 以及它们的生理上可接受的盐是新的。 它们可以根据常规方法制造并加工成适用于治疗人类皮肤中模拟和年龄相关皱纹的局部适用组合物。