[EN] 3-SUBSTITUTED 2-AMINO-INDOLE DERIVATIVES<br/>[FR] DÉRIVÉS DE 2-AMINO-INDOLE 3-SUBSTITUÉS
申请人:TAKEDA PHARMACEUTICAL
公开号:WO2015198045A1
公开(公告)日:2015-12-30
The present invention provides compounds of formula (I) (Formula (I)) and pharmaceutically acceptable salts thereof, wherein Q, X% X4,X5 X6, X7,R1, R2, R3 and R8 are as defined in the specification, processes for the preparation of such compounds, pharmaceutical compositions containing them and the use of such compounds in therapy.
A three‐component reaction of aryldiazonium tetrafluoroborates, sodium metabisulfite, and 3‐azido‐2‐methylbut‐3‐en‐2‐ol under mild conditions is described. By using abundant and cheap sodium metabisulfite as the sulfur dioxide surrogate, this protocol features good functional group compatibility, affording 2‐arylsulfonylacetonitriles in moderate to good yields. The reaction proceeds smoothly at room
3-azido-2-methylbut-3-en-2-ol under ultraviolet irradiation at room temperature is achieved, giving rise to 2-(arylsulfonyl)acetonitriles in moderate to good yields. Alkyl iodide is also workable under these conditions. This transformation proceeds smoothly undermildconditions with a broad substrate scope. Various functional groups are compatible including amino, ester, halo, and trifluoromethyl groups. No metal catalyst
Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT
6
receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT
6
receptor such as psychosis, schizophrenia, manic depression, depression, neurological disorder, memory disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.
[EN] NOVEL COMPOUNDS FOR TREATMENT OF OBESITY<br/>[FR] NOUVEAUX COMPOSES POUR LE TRAITEMENT DE L'OBESITE
申请人:NOVO NORDISK AS
公开号:WO2004101505A1
公开(公告)日:2004-11-25
Hydroxyl styrene sulfonyl derivatives of formula (I), in which the variables are as defined in the claims, are provided which are useful in the treatment of obesity.