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    • 1. 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
    • US20100137280A1
    • 2010-06-03
    • US12532406
    • 2008-03-20
    • Thomas Schultz, SR.Wilfried BrajeSean Colm TurnerAndreas HauptUdo LangeKarla DrescherKarsten WickeLiliane UngerMario MezlerMatthias Mayrer
    • Thomas Schultz, SR.Wilfried BrajeSean Colm TurnerAndreas HauptUdo LangeKarla DrescherKarsten WickeLiliane UngerMario MezlerMatthias Mayrer
    • A61K31/404A61K31/437A61K31/4184A61K31/416C07D403/10C07D413/02C07D401/14C07D471/04C07D487/04A61K31/506A61P25/00A61P3/04A61P25/30A61P25/18
    • C07D471/04C07D403/04
    • The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl, is a single or double bond; X1 and X2 are N, CRx1, NRx2, or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 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; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; wherein a maximum of 3 of the radicals X1, X2, Y1, Y2 and Y3 are selected from NRx1 and N; R1 is hydrogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, etc.; R2 is C1-C4-alkyl or C1-C4-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)化合物,其中A为C 1 -C 6 - 烷基,C 1 -C 6 - 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 1 -C 4烷基,芳基-C 2 -C 4 - 烯基,芳基或杂芳基,是单键或双键; X1和X2是N,CRx1,NRx2或CRx3Rx4; Rx1,Rx3和Rx4是H,卤素,CN,NO2,C1-C6-烷基,C1-C6-烷氧基,C1-C6-烷基羰基等,或两个偕根基Rx3和Rx4与它们所在的碳原子一起 结合可形成羰基或3-至6-元碳环或杂环螺环状环; Rx2是氢,C1-C6-烷基,C1-C6-烷基羰基,C1-C6-卤代烷基等; 或两个连位基Rx1,Rx2,Rx3或Rx4与X1和X2一起形成五元或六元碳环或杂环稠环; Y1,Y2和Y3为N或CRy; Ry是H,卤素,CN,NO 2,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 - 卤代烷基等; 其中基团X1,X2,Y1,Y2和Y3中的最多3个选自NRx1和N; R1是氢,C1-C6-烷基,C1-C6-羟基烷基,C1-C6-卤代烷基等; R2是C1-C4-烷基或C1-C4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。
    • 2. 发明授权
    • Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
    • 适用于治疗对5-羟色胺5-HT 6受体的调节作用的疾病的氮杂环丁啶化合物
    • US08507469B2
    • 2013-08-13
    • US12532406
    • 2008-03-20
    • Thomas SchultzWilfried BrajeSean Colm TurnerAndreas HauptUdo LangeKarla DrescherKarsten WickeLiliane UngerMario MezlerMatthias Mayrer
    • Thomas SchultzWilfried BrajeSean Colm TurnerAndreas HauptUdo LangeKarla DrescherKarsten WickeLiliane UngerMario MezlerMatthias Mayrer
    • A61K31/397C07D403/04C07D471/04
    • C07D471/04C07D403/04
    • The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl; is a single or double bond; X1 and X2 are N, CRx1, NRx2 or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 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; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; wherein a maximum of 3 of the radicals X1, X2, Y1, Y2 and Y3 are selected from NRx1 and N; R1 is hydrogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, etc.; R2 is C1-C4-alkyl or C1-C4-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)化合物,其中A为C 1 -C 6 - 烷基,C 1 -C 6 - 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 - 芳基-C 1 -C 4 - 烷基,芳基-C 2 -C 4 - 烯基,芳基或杂芳基; 是单键或双键; X1和X2是N,CRx1,NRx2或CRx3Rx4; Rx1,Rx3和Rx4是H,卤素,CN,NO2,C1-C6-烷基,C1-C6-烷氧基,C1-C6-烷基羰基等,或两个偕根基Rx3和Rx4与它们所在的碳原子一起 结合可形成羰基或3-至6-元碳环或杂环螺环状环; Rx2是氢,C1-C6-烷基,C1-C6-烷基羰基,C1-C6-卤代烷基等; 或两个连位基Rx1,Rx2,Rx3或Rx4与X1和X2一起形成五元或六元碳环或杂环稠环; Y1,Y2和Y3为N或CRy; Ry是H,卤素,CN,NO 2,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 - 卤代烷基等; 其中基团X1,X2,Y1,Y2和Y3中的最多3个选自NRx1和N; R1是氢,C1-C6-烷基,C1-C6-羟基烷基,C1-C6-卤代烷基等; R2是C1-C4-烷基或C1-C4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。