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    Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such
    6.
    发明授权
    Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such 有权
    咪唑烷衍生物，其用途，其制备方法和包含其的组合物

    公开(公告)号：US08168667B2

    公开(公告)日：2012-05-01

    申请号：US12751158

    申请日：2010-03-31

    申请人： Francois Nique ,  Catherine Jagerschmidt ,  Philippe Clement-Lacroix

    发明人： Francois Nique ,  Catherine Jagerschmidt ,  Philippe Clement-Lacroix

    IPC分类号： A61K31/4166 ,  C07D233/02

    CPC分类号： C07D233/78 ,  A61K31/4166 ,  C07D233/86 ,  C07D235/02 ,  C07D309/10 ,  C07D409/06

    摘要： Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.

    摘要翻译： 式（I）化合物：其中X为O或S，R1为酰基，醛，环烷基，任选取代的烷基，烯基或炔基，R2为H，烷基，羟基烷基，卤代烷基，烯基或炔基; 取代的烷基; 烷基羰基; R3和R4是H，卤素，烷基，烯基，炔基，烷氧基，烷硫基，羟基烷基，卤代烷基，卤代烯基或卤代炔基; 或R 3和R 4形成任选的芳族或杂环的任选取代的环，R 5是H，卤素，三氟甲基，-CN或-NO 2; 不是所有的R 3，R 4和R 5是H，R 6和R 9是H，卤素，OH; 烷基，羟基烷基，烷氧基，硫代烷基，卤代烷基，烯基或炔基; R7和R8是H，卤素，OH，SH; 任选被OH和/或卤素取代的烷氧基或烷硫基; R7和R8之一不是H或卤素; 或者R 7和R 8中的一个是药学上可接受的酯或硫代酯基团，或者R 6是C 1-3烷基，或者与R 1或R 2一起代表C1-3亚烷基或亚烯基连接基团，任选地被甲基，三氟甲基，OH ，或卤素及其药学上可接受的盐和酯可用作选择性雄激素调节剂。

    IMIDAZOLIDINE DERIVATIVES, USES THEREFOR, PREPARATION THEREOF AND COMPOSITIONS COMPRISING SUCH
    7.
    发明申请
    IMIDAZOLIDINE DERIVATIVES, USES THEREFOR, PREPARATION THEREOF AND COMPOSITIONS COMPRISING SUCH 有权
    咪唑啉衍生物，其用途及其制备方法和包含此类化合物的组合物

    公开(公告)号：US20100210699A1

    公开(公告)日：2010-08-19

    申请号：US12751158

    申请日：2010-03-31

    申请人： Francois NIQUE ,  Catherine Jagerschmidt ,  Philippe Clement-Lacroix

    发明人： Francois NIQUE ,  Catherine Jagerschmidt ,  Philippe Clement-Lacroix

    IPC分类号： A61K31/4166 ,  C07D233/78 ,  C07D233/86 ,  C07D409/06 ,  C07D235/02 ,  A61P19/10 ,  A61P15/00 ,  A61P35/00

    CPC分类号： C07D233/78 ,  A61K31/4166 ,  C07D233/86 ,  C07D235/02 ,  C07D309/10 ,  C07D409/06

    摘要： Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.

    摘要翻译： 式（I）化合物：其中X为O或S，R1为酰基，醛，环烷基，任选取代的烷基，烯基或炔基，R2为H，烷基，羟基烷基，卤代烷基，烯基或炔基; 取代的烷基; 烷基羰基; R3和R4是H，卤素，烷基，烯基，炔基，烷氧基，烷硫基，羟基烷基，卤代烷基，卤代烯基或卤代炔基; 或R 3和R 4形成任选的芳族或杂环的任选取代的环，R 5是H，卤素，三氟甲基，-CN或-NO 2; 不是所有的R 3，R 4和R 5是H，R 6和R 9是H，卤素，OH; 烷基，羟基烷基，烷氧基，硫代烷基，卤代烷基，烯基或炔基; R7和R8是H，卤素，OH，SH; 任选被OH和/或卤素取代的烷氧基或烷硫基; R7和R8之一不是H或卤素; 或者R 7和R 8中的一个是药学上可接受的酯或硫代酯基团，或者R 6是C 1-3烷基，或者与R 1或R 2一起代表C1-3亚烷基或亚烯基连接基团，任选地被甲基，三氟甲基，OH ，或卤素及其药学上可接受的盐和酯可用作选择性雄激素调节剂。