发明名称 6-cyclylmethyl-and 6-alkylmethyl-substituted pyrazolepyrimidines
摘要 The invention relates to 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines, process for their preparation, and their use for producing medicaments for improving learning and/or memory. The 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines are of the formula (I):; with the variables as defined in the claims.
申请公布号 US8822479(B2) 申请公布日期 2014.09.02
申请号 US201012950386 申请日期 2010.11.19
申请人 Boehringer Ingelheim International GmbH 发明人 Hendrix Martin;Bärfacker Lars;Erb Christina;Hafner Frank-Thorsten;Heckroth Heike;Karthaus Dagmar;Tersteegen Adrian;van der Staay Franz-Josef;van Kampen Marja
分类号 A61K31/519;A61P25/28;A61P25/18;C07D487/04 主分类号 A61K31/519
代理机构 代理人 Morris Michael P.;Lazer Edward S.
主权项 1. A method for the treatment of an impairment of learning and/or memory in a human or animal which comprises administering to the human or animal an amount effective for such treatment of a compound of the formula (I): in which R1 is C1-C8-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C3-C8-cycloalkyl, where C1- C8-alkyl is optionally substituted by oxo, and where C1-C8-alkyl, C2-C6-alkenyl, C2-C6-alkynyl and C3-C8-cycloalkyl are optionally substituted by up to 3 radicals independently of one another selected from the group of C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, cyano, amino, nitro, hydroxy, C1-C6-alkylamino, halogen, trifluoromethyl, trifluoromethoxy,C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylamino-carbonyl, C1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylamino-carbonyl, heteroarylcarbonylamino, C1-C6-alkylsulphonylamino, C1-C6-alkylsulphonyl,C1-C6-alkylthio,whereC1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylamino, C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl, C1-C6-alkoxy-carbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl, heteroarylcarbonylamino, C1-C6-alkylsulphonylamino, C1-C6-alkyl-sulphony and C1-C6-alkylthio are optionally substituted by one to three radicals independently of one another selected from the group of hydroxy, cyano, halogen, trifluoromethyl, trifluoromethoxy, hydroxy-carbonyl and a group of the formula —NR3R4,whereR3 and R4 are independently of one another hydrogen or C1-C6-alkyl,orR3 and R4 together with the nitrogen atom to which they are bonded are 5- to 8-membered heterocyclyl, R2 is phenyl or heteroaryl, where phenyl is substituted by 1 to 3 radicals and heteroaryl is optionally substituted by 1 to 3 radicals in each case independently of one another selected from the group of C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, trifluoromethoxy, amino, nitro, hydroxy, C1-C6-alkylamino, halogen, C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl, C1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl, heteroarylcarbonylamino, C1-C6-alkylsulphonyl amino, C1-C6-alkylsulphonyl and C1-C6-alkylthio, where C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylamino, C6-C10-arylcarbonyl-amino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl, C 1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl, heteroarylcarbonylamino, C1-C6-alkylsulphonylamino, C1-C6-alkylsulphonyl and C1-C6-alkylthio are optionally substituted by one to three radicals independently of one another selected from the group of hydroxy, cyano, halogen, trifluoromethyl, trifluoromethoxy, hydroxycarbonyl and a group of the formula —NR3R4, whereR3 and R4 have the meanings indicated above, or a salt, solvate or solvate of a salt thereof.
地址 Ingelheim am Rhein DE