The present invention relates to compounds of general formula I,
wherein the groups (Het)Ar and R
1
are defined as in claim
1
, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
Hydrogen-free reductive amination using iron pentacarbonyl as a reducing agent
作者:Oleg I. Afanasyev、Dmitry L. Usanov、Denis Chusov
DOI:10.1039/c7ob02795h
日期:——
We developed solvent-free reductiveaminationwithout an externalhydrogensource using iron pentacarbonyl as a reducing agent. Neither a catalyst nor any other additives were employed. Various types of substrates are suitable for the reaction, including those with low reactivity, e.g. benzophenone. Among others, the protocol tolerates bromo-, cyano-, benzyloxy-, pyrimidyl and styryl moieties.
[EN] 2, 3, 6-TRISUBSTITUTED-4-PYRIMIDONE DERIVATIVES<br/>[FR] DERIVES DE 2,3,6-TRISUBSTITUE 4-PYRIMIDONE
申请人:MITSUBISHI PHARMA CORP
公开号:WO2004085408A1
公开(公告)日:2004-10-07
A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each Y independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.
Alkylation of cyclic amines with alcohols catalyzed by Ru(II) complexes bearing N -Heterocyclic carbenes
作者:Öznur Doğan Ulu、Nevin Gürbüz、İsmail Özdemir
DOI:10.1016/j.tet.2017.09.027
日期:2018.2
includes the synthesis of 2-(1,3-dioxane-2-yl)ethyl substituted benzimidazole substituted N-heterocyclic carbenes precursors and their ruthenium complexes. Synthesized compounds were characterized by elemental analysis and NMR spectroscopy. All complexes have been tested in the alkylation of pyrrolidine and morpholine with alcohols, showing an excellent activity in this reaction.
[EN] INDOLE DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS DE D'INDOLE ET LEURS UTILISATIONS
申请人:NOVARTIS AG
公开号:WO2019021059A1
公开(公告)日:2019-01-31
The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non- therapeutic purposes.