发明名称 Organic compounds
摘要 The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment and/or prophylaxis of narcolepsy.
申请公布号 US9198924(B2) 申请公布日期 2015.12.01
申请号 US200712514712 申请日期 2007.11.13
申请人 INTRA-CELLULAR THERAPIES, INC. 发明人 Mates Sharon;Fienberg Allen A.
分类号 A61K31/519;A61K31/52;A61K45/06;A61K31/70;A61K31/00;A61K31/165;A61K31/19 主分类号 A61K31/519
代理机构 Hoxic & Associates LLC 代理人 Hoxic & Associates LLC
主权项 1. A method of treatment for narcolepsy comprising administering an effective amount of a PDE 1 inhibitor to a patient in need thereof wherein the PDE 1 inhibitor is a compound of the formula (I): wherein (i) R1 is H or C1-4 alkyl; (ii) R4 is H or C1-4 alkyl and R2 and R3 are, independently, H or C1-4 alkyl, aryl, heteroaryl, heteroarylalkoxy, arylalkoxy, heteroarylalkyl, or arylalkyl; or R2 is H and R3 and R4 together form a di-, tri-, or tetra-methylene bridge; (iii) R5 is a substituted heteroarylalkyl, or R5 is attached to one of the nitrogen atoms on the pyrazolo portion of Formula I and is a moiety of Formula Q wherein X, Y and Z are, independently, N or C; R8, R9, R11 and R12 are independently H or halogen; and R10 is halogen, alkyl, cycloalkyl, haloalkyl, aryl, heteroaryl, or thiadiazolyl, diazolyl, triazolyl, tetrazolyl, arylcarbonyl, alkylsulfonyl, heteroarylcarbonyl, or alkoxycarbonyl; provided that when X, Y, or Z is nitrogen, R8, R9, or R10, respectively, is not present; (iv) R6 is phenylamino or benzylamino; and (v) n=0; wherein: said aryl is optionally substituted with alkyl, halogen, haloalkyl, hydroxy, carboxy or an additional aryl or heteroaryl; andsaid heteroaryl is optionally substituted with alkyl, halogen, haloalkyl, hydroxy or carboxy, in free, pharmaceutically acceptable salt or prodrug form.
地址 New York NY US