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    • 6. 发明申请
    • AZETIDIN COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR
    • 适用于治疗响应调节SEROTONIN 5-HT6受体的疾病的AZETIDIN化合物
    • WO2008116833A1
    • 2008-10-02
    • PCT/EP2008/053389
    • 2008-03-20
    • ABBOTT GMBH & CO. KGSCHULTZ, ThomasBRAJE, WilfriedTURNER, Sean ColmHAUPT, AndreasLANGE, UdoDRESCHER, KarlaWICKE, KarstenUNGER, LilianeMEZLER, MarioMAYRER, Matthias
    • SCHULTZ, ThomasBRAJE, WilfriedTURNER, Sean ColmHAUPT, AndreasLANGE, UdoDRESCHER, KarlaWICKE, KarstenUNGER, LilianeMEZLER, MarioMAYRER, Matthias
    • C07D403/04C07D471/04A61K31/404A61P25/28
    • C07D471/04C07D403/04
    • The present invention relates to compounds of formula (I) wherein A is C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -haloalkenyl, C 3 -C 6 -cycloalkyl, aryl-C 1 -C 4 -alkyl, aryl-C 2 -C 4 -alkenyl, aryl or hetaryl; --- is a single or double bond; X 1 and X 2 are N, CR x1 , NR x2 or CR x3 R x4 ; R x1 , R x3 and R x4 are H, halogen, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 1 -C 6 -alkylcarbonyl, etc. or two geminal radicals R x3 and R x4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro- annulated ring; R x2 is hydrogen, C 1 -C 6 -alkyl, C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -haloalkyl, etc.; or two vicinal radicals R x1 , R x2 , R x3 or R x4 together with X 1 and X 2 form a five- or six- membered carbocyclic or heterocyclic fused ring; Y 1 , Y 2 and Y 3 are N or CR y ; R y is H, halogen, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -haloalkyl, etc.; wherein a maximum of 3 of the radicals X 1 , X 2 , Y 1 , Y 2 and Y 3 are selected from NR x1 and N; R 1 is hydrogen, C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 1 -C 6 -haloalkyl, etc.; R 2 is C 1 -C 4 -alkyl or C 1 -C 4 -haloalkyl; n is 0, 1 or 2; physiologically tolerated acid addition salts and the N-oxides thereof, pharmaceutical composition comprising them, a method for treating medical disorders selected from diseases of the central nervous system, addiction diseases or obesity, said method comprising administering an effective amount of such compounds to a subject in need and the use of such a compound for preparing a pharmaceutical compositions.
    • 本发明涉及式(I)的化合物,其中A是C 1 -C 6 - 烷基,C 1 -C 3 - 6个 - 卤代烷基,C 1 -C 6 - 羟基烷基,C 2 -C 6 - 烯基,C 2 -C 6 - 卤代烯基,C 3 -C 6 - 环烷基,芳基-C 芳基-C 2 -C 4 - 亚烷基,芳基或杂芳基; C 1 -C 4烷基,C 1 -C 4烷基, ---是单键或双键; X 1和X 2是N,CR 1,X 2,X 2或CR 3 x 3 > - [R X4 ; R 1,X 3和R 4是H,卤素,CN,NO 2,C 1, C 1 -C 6 - 烷基,C 1 -C 6 - 烷氧基,C 1 -C 6 - 烷基,C 1 -C 6 - C 6 - 烷基羰基等,或两个偕根基R 3和R 4以及它们所结合的碳原子一起形成 羰基或3-至6-元碳环或杂环螺环环; R 2是氢,C 1 -C 6 - 烷基,C 1 -C 6 - C 1 -C 6烷基羰基,C 1 -C 6 - 卤代烷基等; 或两个邻位基团X 1,X 2,R x 3或R x 4,以及X 1 <和< 2>和< 2>形成五元或六元碳环或杂环稠环; Y 1,Y 2和Y 3是N或CR y; R 1是H,卤素,CN,NO 2,C 1 -C 6 - 烷基,C 1 -C 6烷基, C 1 -C 6 - 烷氧基,C 1 -C 6 - 烷基羰基,C 1〜 -C 6 -C 6 - 卤代烷基等; 其中基团X 1,X 2,Y 1,Y 2和Y 2中的最多3个, SUP> 3 选自NRIX和N; R 1是氢,C 1 -C 6 - 烷基,C 1 -C 6 - 烷基,C 1 -C 6 - 羟基烷基,C 1 -C 6 - 卤代烷基等; R 2是C 1 -C 4 - 烷基或C 1 -C 4 - / - > - 卤代烷基; n为0,1或2; 生理耐受的酸加成盐及其N-氧化物,包含它们的药物组合物,治疗选自中枢神经系统疾病,成瘾疾病或肥胖症的医学病症的方法,所述方法包括向受试者施用有效量的这些化合物 并且使用这种化合物来制备药物组合物。