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    • 2. 发明申请
    • ACYLAMINOCYCLOALKYL COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF DOPAMINE D3 RECEPTOR
    • 适用于治疗多巴胺D3受体调节障碍的ACYLAMINOCOCLOALKYL化合物
    • WO2014140246A1
    • 2014-09-18
    • PCT/EP2014/055062
    • 2014-03-14
    • ABBVIE DEUTSCHLAND GMBH & CO. KGABBVIE INC.
    • HAUPT, AndreasDINGES, JürgenUNGER, LilianeWICKE, KarstenVAN WATERSCHOOT, RobertDRESCHER, KarlaRELO, Ana Lucia
    • C07D239/42A61K31/506A61P25/00
    • C07D295/155A61K31/496C07D239/42C07D403/04
    • The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. In formula I, the variables have the following meanings: m is 1 or 2, n is 1 or 2, A is selected from the group consisting of CH 2 , CH 2 CH 2 , CHFCH 2 and CF 2 CH 2 , R 1 is an oxygen containing cyclic radical selected such as C 3 -C 6 cycloalkyl, which carries one or two oxygen containing radicals selected from the group consisting of OH, C 1 -C 2 -alkoxy, fluorinated C 1 -C 2 -alkoxy, and a carbonyl oxygen,, R 2 is selected from the group consisting of hydrogen, OH and fluorine, R 3a is selected from the group consisting of hydrogen and methyl, R 3b is selected from the group consisting of hydrogen and methyl, R 4 is branched C 4 -C 6 alkyl or branched fluorinated C 4 -C 6 alkyl, and R 5 is inter alia C 1 -C 6 alkyl, fluorinated C 1 -C 3 alkyl, C 1 -C 2 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkoxy-C 1 -C 4 -alkyl, hydroxy-C 1 -C 4 -alkyl, fluorinated hydroxy-C 1 -C 4 -alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C 3 -C 5 cycloalkyl, fluorinated C 3 -C 5 cycloalkyl, etc.
    • 本发明涉及新的酰氨基环烷基化合物,特别是涉及本文所述的式I化合物及其盐和N-氧化物。 该化合物具有有价值的治疗性质,特别适用于治疗对多巴胺D3受体调节作出反应的疾病。 在式I中,变量具有以下含义:m为1或2,n为1或2,A选自CH 2,CH 2 CH 2,CHFCH 2和CF 2 CH 2,R 1为选自氧的环状基团,例如C 3 -C 6环烷基,其携带一个或两个选自OH,C 1 -C 2烷氧基,氟化C 1 -C 2烷氧基和羰基氧的含氧基团,R 2选自氢,OH 和氟,R3a选自氢和甲基,R3b选自氢和甲基,R4是支链C4-C6烷基或支链氟化C4-C6烷基,R5特别是C1-C6 烷基,氟化C 1 -C 3烷基,C 1 -C 2烷氧基-C 1 -C 4烷基,氟化C 1 -C 2烷氧基-C 1 -C 4 - 烷基,羟基-C 1 -C 4 - 烷基,氟化羟基-C 1 -C 4烷基, 氧杂环丁烷基,氟化氧杂环丁烷基,氧杂环戊烷基,氟代氧杂环戊烷基,C3-C5环烷基,氟化C3-C5环烷基等
    • 6. 发明公开
    • ACYLAMINOCYCLOALKYL COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF DOPAMINE D3 RECEPTOR
    • ACYLAMINOCYCLOALKYLVERBINDUNGEN FOR疾病对调制多巴胺D 3受体应答的治疗
    • EP2970146A1
    • 2016-01-20
    • EP14710261.0
    • 2014-03-14
    • AbbVie Deutschland GmbH & Co. KGAbbVie Inc.
    • HAUPT, AndreasDINGES, JürgenUNGER, LilianeWICKE, KarstenVAN WATERSCHOOT, RobertDRESCHER, KarlaRELO, Ana Lucia
    • C07D239/42A61K31/506A61P25/00
    • C07D295/155A61K31/496C07D239/42C07D403/04
    • The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. In formula I, the variables have the following meanings: m is 1 or 2, n is 1 or 2, A is selected from the group consisting of CH
      2 , CH
      2 CH
      2 , CHFCH
      2 and CF
      2 CH
      2 , R
      1 is an oxygen containing cyclic radical selected such as C
      3 -C
      6 cycloalkyl, which carries one or two oxygen containing radicals selected from the group consisting of OH, C
      1 -C
      2 -alkoxy, fluorinated C
      1 -C
      2 -alkoxy, and a carbonyl oxygen,, R
      2 is selected from the group consisting of hydrogen, OH and fluorine, R
      3a is selected from the group consisting of hydrogen and methyl, R
      3b is selected from the group consisting of hydrogen and methyl, R
      4 is branched C
      4 -C
      6 alkyl or branched fluorinated C
      4 -C
      6 alkyl, and R
      5 is inter alia C
      1 -C
      6 alkyl, fluorinated C
      1 -C
      3 alkyl, C
      1 -C
      2 -alkoxy-C
      1 -C
      4 -alkyl, fluorinated C
      1 -C
      2 -alkoxy-C
      1 -C
      4 -alkyl, hydroxy-C
      1 -C
      4 -alkyl, fluorinated hydroxy-C
      1 -C
      4 -alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C
      3 -C
      5 cycloalkyl, fluorinated C
      3 -C
      5 cycloalkyl, etc.
    • 本发明涉及新颖的化合物acylaminocycloalkyl,特别是我在和它们的盐和N-氧化物中描述的下式的化合物。 这些化合物具有有价值的治疗性质和是合适的,特别是用于治疗疾病并于多巴胺D3受体的调节有反应的。 2 1或2,m是1或,n为A的选自CH 2,CH 2 CH 2,CHFCH2和CF 2 CH 2的选择,R 1是含有氧的环状基团中选择检查作为C3:在式I中,变量具有以下含义 C6环烷基,其携带选自OH中选择的一个或两个氧含有自由基,C1-C2烷氧基,氟化的C 1 -C 2 - 烷氧基,和具有羰基氧,R 2是选自氢由......组成,OH和 氟,R 3A为选自氢和甲基中选择,R 3b中选自氢和甲基中选择,R 4是支链的C4-C6烷基或支链氟代C 4 -C 6烷基,而R5是尤其C1-C6烷基 ,C1-C3氟代烷基,C1-C2烷氧基-C 1 -C 4 - 烷基,氟化的C 1 -C 2 - 烷氧基-C 1 -C 4 - 烷基,羟基-C 1 -C 4 - 烷基,氟化的羟基-C 1 -C 4 - 烷基,氧杂环丁烷基 ,氟化氧杂环丁基,氧杂环戊基,氧杂环戊基氟化,C3-C5环烷基,氟化的C 3 -C 5环烷基,等等。