发明名称 SUBSTITUTED PYRAZOLOPYRIMIDINES AND METHOD OF USE
摘要 Compounds of formula (I);;and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, L1 and G1 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
申请公布号 US2016304527(A1) 申请公布日期 2016.10.20
申请号 US201615133851 申请日期 2016.04.20
申请人 AbbVie Deutschland GmbH & Co. KG ;AbbVie Inc. 发明人 FAGHIH Ramin;MOELLER Achim;OCHSE Michael;POHLKI Frauke;SCHMIDT Martin;SCHULZ Michael;SIPPY Kevin;TURNER Sean;VAN DER KAM Elizabeth Louise
分类号 C07D487/04;C07D519/00 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of formula (I): or a pharmaceutically acceptable salt or isotopically labelled form thereof, wherein: R1 is selected from the group consisting of C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, C3-C6cycloalkylC1-C6alkyl, 4-7-membered heterocycle and 4-7-membered heterocycleC1-C6alkyl, wherein each of the 4-7-membered heterocycles in the two last mentioned radicals are saturated or have one endocyclic double bond; a) the C1-C6alkyl, the C2-C6alkenyl, the C2-C6alkynyl, the C1-C6alkyl of C3-C6cycloalkylC1-C6alkyl, and the C1-C6alkyl of 4-7-membered heterocycleC1-C6alkyl are unsubstituted or substituted with one or more substituents R1a independently selected from the group consisting of C1-C6alkoxy, C1-C6alkylcarbonylamino, C1-C6alkylsulfonylamino, amido, carboxy, cyano, halogen, hydroxy, and oxo;b) the C3-C6cycloalkyl, the C3-C6cycloalkyl of C3-C6cycloalkylC1-C6alkyl, 4-7-membered heterocycle, and the 4-7-membered heterocycle of 4-7-membered heterocycleC1-C6alkyl are unsubstituted or substituted with one or more substituents R1b independently selected from the group consisting of C1-C6alkoxy, C1-C6alkyl, amido, C1-C6alkylcarbonylamino, C1-C6alkylsulfonylamino, carboxy, cyano, halogen, haloC1-C6alkyl, hydroxy, hydroxyC1-C6alkyl, and oxo; R2 is selected from the group consisting of hydrogen, C1-C6alkyl, and haloC1-C6alkyl; or R1, R2 and the nitrogen to which they are attached form a saturated 4-7-membered N-bound heterocycle, which in addition to the nitrogen atom may have one further heteroatom selected from O, S and N as a ring member, wherein: each such 4-7-membered heterocycle is unsubstituted or substituted with one or more identical or different substituents R1c, where R1c is selected from the group consisting of C1-C6alkoxy, C1-C6alkyl, C1-C6alkylcarbonylamino, C1-C6alkylsulfonylamino, amido, carboxy, cyano, halogen, haloC1-C6alkyl, amino, hydroxy, hydroxyC1-C6alkyl, oxo, spirocyclic bound C3-C6cycloalkyl; and spirocyclic bound saturated 4-6-membered heterocycle; wherein each spirocyclic bound C3-C6cycloalkyl and spirocyclic bound 4-6-membered heterocycle is unsubstituted or substituted with one or more substituents independently selected from the group consisting of C1-C6alkyl, cyano, halogen, haloC1-C6alkyl, hydroxy, and hydroxyC1-C6alkyl; R3 is hydrogen, C1-C6alkyl, or haloC1-C6alkyl; R4 is hydrogen, C1-C6alkyl, or haloC1-C6alkyl; or R3 and R4 are joined to form a C3-C7alkylene; L1 is selected from the group consisting of —(CR5R6)m—, —(CH2)nCR5a═CR6a(CH2)p—, and wherein c) R5, R5a, R5b, R6, R6a and R6b are, at each occurrence, independently selected from the group consisting of hydrogen, C1-C6alkyl, fluorine, haloC1-C6alkyl and phenyl, wherein; phenyl is unsubstituted or substituted with one or more substituents selected from the group consisting of C1-C6alkyl, halogen, or haloC1-C6alkyl; ord) R5 or R6 is a C2-C4alkylene attached to G1;e) m is 1, 2, 3 or 4;f) n is, at each occurrence, independently 0, 1, or 2;g) p is, at each occurrence, independently 0, 1, or 2; and G1 is selected from the group consisting of C5-C10cycloalkyl, 5-6-membered heteroaryl, 5-6-membered heterocycle, which is saturated or has one endocyclic double bond, and phenyl; wherein each C5-C10cycloalkyl, 5-6-membered heteroaryl, 5-6-membered heterocycle, and phenyl is unsubstituted or substituted with one or more identical or different substituents RG, where RG is selected from the group consisting of C1-C6alkyl, cyano, haloC1-C6alkyl, halogen, C1-C6alkoxy and haloC1-C6alkoxy.
地址 Wiesbaden DE