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.
GRISEOFULVIN COMPOUND AND PHARMACEUTICAL USE THEREOF
申请人:Daiichi Sankyo Company, Limited
公开号:US20200216433A1
公开(公告)日:2020-07-09
The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem. [R
1
: a C1-C6 alkyl group or the like, R
2
: a C1-C6 alkyl group or the like, A: a 5-membered aromatic hetero-ring or the like, R
3
, R
3′
: a C1-C6 alkyl group or the like]
Enantioselective Intermolecular [2+2] Photocycloaddition Reaction of Cyclic Enones and Its Application in a Synthesis of (−)-Grandisol
作者:Saner Poplata、Thorsten Bach
DOI:10.1021/jacs.8b01011
日期:2018.3.7
The intermolecular [2+2] photocycloaddition of typical cyclic α,β-unsaturated enones, such as 2-cyclohexenone, with olefins was performed in moderate to good yields (42–82%) and with high enantioselectivity (82%–96% ee). An unusual substitution pattern at the chiral oxazaborolidine-AlBr3 Lewisacid complex that promotes the reaction was found to be crucial for the success of the reaction. The method
典型的环状 α,β-不饱和烯酮(如 2-环己烯酮)与烯烃的分子间 [2+2] 光环加成以中等至良好的产率(42-82%)和高对映选择性(82%-96% ee )。发现促进反应的手性恶唑硼烷-AlBr3 路易斯酸络合物的不寻常取代模式对反应的成功至关重要。该方法用于对映选择性合成单萜(-)-格兰地醇,以3-甲基-2-环己烯酮为原料,可分六步完成,总产率为13%。
[EN] NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS<br/>[FR] NOUVEAUX ACIDES INDANYLOXYDIHYDROBENZOFURANYLACÉTIQUES
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2014086712A1
公开(公告)日:2014-06-12
The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R1 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.
[EN] TRICYCLIC COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS<br/>[FR] COMPOSÉS TRICYCLIQUES ET COMPOSITIONS UTILISÉS COMME INHIBITEURS DE KINASES
申请人:NOVARTIS AG
公开号:WO2017103824A1
公开(公告)日:2017-06-22
The present invention provides compounds of Formula (A): (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent, and methods of using the compositions and combinations to treat conditions including cancers.