1, 5-DIPHENYL-3-BENZYLAMINO-1, 5-DIHYDROPYRROLIDIN-2-ONE AS CB1 RECEPTOR MODULATORS
申请人:Coffey David Scott
公开号:US20090275618A1
公开(公告)日:2009-11-05
Compounds and pharmaceutical compositions of Formula (I) by blockade of the CB
1
receptors via an inverse agonism mechanism which are useful for reducing body weight in mammals, cognitive impairment associated with schizophrenia, mitigating treatment emergent weight gain observed during treatment with antipsychotics and have increased bioavailability.
1, 5-diphenyl-3-benzylamino-1, 5-dihydropyrrolidin-2-one as CB1 receptor modulators
申请人:Eli Lilly and Company
公开号:US08168659B2
公开(公告)日:2012-05-01
Compounds and pharmaceutical compositions comprising compounds of the Formula
as CB1 receptor inverse agonists useful for reducing body weight in mammals, treating cognitive impairment associated with schizophrenia, and mitigating treatment emergent weight gain observed during treatment with antipsychotics.
The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as raPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
The present application provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R4 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient.