FICKES, MICHAEL G.,SUN, MINGHUA,ZHAO, CHEN,SHEIKH, AHMAD Y.,HENRY, RODGER F.,BARNES, DAVID M.,GREGG, ROBERT J.,HAIGHT, ANTHONY R.,KOLACZKOWSKI, LAWRENCE,WITTENBERGER, STEVEN J.,ZHANG, GEOFF G.Z.,COWAR
申请号：
AU2007220889
公开号：
AU2007220889B2
申请日:
2007.02.16
申请国别(地区):
AU
年份:
2012
代理人:
摘要：
Octahydro-pyrrolo[3,4-b]pyrrole derivatives or a pharmaceutically acceptable salt, ester, amide, prodrug, or radiolabeled form thereof, wherein R is alkyl, C-C cycloalkyl. or (C-C cycloalkyl)methyl； R, R, R, R, R, and R each are independently hydrogen, methyl, or fluoromethyl； R, R, R, and R each are independently hydrogen, alkyl, fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile, with the proviso that when one or more of R, R, R, and R are alkyl, then at least one of R, R, R, and R is fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile； L is a bond, oxygen, sulfur, carbonyl, alkylene,. alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR, -C(=O) NR-, or -NR4C(=O)-； R is hydrogen or alkyl； Cy is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle； Z is a substituent R or a group represented by -L-Cy； R is hydrogen, acyl, acyloxy, alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxyimino, alkoxysulfonyl, alkyl, alkylcarbonyl, alkylsulfonyl, alkynyl, amido, carboxy, cyano, cycloalkyl, fiuoroalkoxy, haloalkoxy, haloalkyl, halogen, hydroxy, hydroxyalkyl, mercapto, nitro, alkylthio, amino, NHR, NRR, -N(R)C(=O)R, -C(=O)NRR, or N(R)SO(R)； L is a bond, oxygen, sulfur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR, -C(=O) NR-, or -NRC(=O)-；Cy is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle； R, R, R, R, and R at each occurrence are independently hydrogen,C alkyl, C-C cycloalkyl, or a (C-C cycloalkyl)amine； are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.
