6,7-DIHYDRO-5H-PYRROLO[3,4-B]PYRIDIN-5-ONE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR
申请人:BAO JIANMING
公开号:US20170183342A1
公开(公告)日:2017-06-29
The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
The invention discloses compounds of Formula (I)
wherein R
1
, R
2
, R
2A
, R
3
, R
3A
, R
4
, R
4A
, and R
5
are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
[EN] PYRIDINE-1-OXIDE DERIVATIVES AND THEIR USE AS FACTOR XIA INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIDINE-1-OXYDE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DU FACTEUR XIA
申请人:MERCK SHARP & DOHME
公开号:WO2018039094A1
公开(公告)日:2018-03-01
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
[EN] MODULATOR OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR, PHARMACEUTICAL COMPOSITIONS, METHODS OF TREATMENT, AND PROCESS FOR MAKING THE MODULATOR<br/>[FR] MODULATEUR DE RÉGULATEUR DE CONDUCTANCE TRANSMEMBRANAIRE DE FIBROSE KYSTIQUE, COMPOSITIONS PHARMACEUTIQUES, PROCÉDÉS DE TRAITEMENT ET PROCÉDÉ DE FABRICATION DU MODULATEUR
申请人:VERTEX PHARMA
公开号:WO2018107100A1
公开(公告)日:2018-06-14
Compounds of Formula (I) pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed. Also disclosed are solid state forms of Compound 1 and salts and solvates thereof.