[EN] SUBSTITUTED 1,5-NAPHTHYRIDINES OR QUINOLINES AS ALK5 INHIBITORS<br/>[FR] 1,5-NAPHTYRIDINES OU QUINOLÉINES SUBSTITUÉES EN TANT QU'INHIBITEURS D'ALK5
申请人:THERAVANCE BIOPHARMA R&D IP LLC
公开号:WO2021102468A1
公开(公告)日:2021-05-27
The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
[EN] COMPOSITIONS AND METHODS FOR MODULATING THE WNT SIGNALING PATHWAY<br/>[FR] COMPOSITIONS ET PROCÉDÉS POUR MODULER LA VOIE DE SIGNALISATION WNT
申请人:IRM LLC
公开号:WO2012003189A1
公开(公告)日:2012-01-05
The present invention relates to compositions and methods for modulating the Wnt signaling pathway, using compounds having Formula (1) and (3): wherein A, B, Y and Z all represent rings, and R1, R2, R3 are as defined herein.
STRAIGHTFORWARD ENTRY TO 7-AZABICYCLO[2.2.1]HEPTANE-1-CARBONITRILES AND SUBSEQUENT SYNTHESIS OF EPIBATIDINE ANALOGUES
申请人:STEVENS Christian
公开号:US20090275616A1
公开(公告)日:2009-11-05
The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
A compound represented by the general formula:
or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C
6-14
aryl group or the like, L is —NR
e
CO— or the like (wherein R
e
is a hydrogen atom or the like), Ring B is a C
6-14
aryl group or the like, X is a C
1-3
alkylene group or the like, Y is a single bond or the like, Z is a C
1-3
alkylene group or the like, R
1
and R
2
are each independently a hydrogen atom or the like, and R
3
, R
4
, R
5
and R
6
are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
[EN] DIHYDROCYCLOPENTA-ISOQUINOLINE-SULFONAMIDE DERIVATIVES COMPOUNDS<br/>[FR] COMPOSÉS DÉRIVÉS DE DIHYDROCYCLOPENTA-ISOQUINOLINE-SULFONAMIDE
申请人:UCB BIOPHARMA SRL
公开号:WO2021130259A1
公开(公告)日:2021-07-01
The present invention relates to dihydrocyclopenta-isoquinoline-sulfonamide derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular disorders caused by the interaction of IgE with the FcεRI receptor.