亲核芳族氟化 (S N Ar) 是形成 C(sp 2 )-F 键的最常用方法之一。尽管最近取得了许多进展,但这些转化的长期限制是需要严格干燥的非质子条件来保持氟化物的亲核性并抑制副产物的产生。本报告通过利用四甲基氟化铵醇加合物 (Me 4 NF·ROH) 作为 S N Ar 氟化的氟化物来源解决了这一挑战。通过系统调整醇取代基 (R),四甲基氟化铵叔戊醇 (Me 4 NF· t-AmylOH) 被确定为在温和方便的条件下(DMSO 中 80°C,无需干燥试剂或溶剂)下用于 S N Ar 氟化的廉价、实用且台式稳定的试剂。展示了超过 50 种(杂)芳基卤化物和硝基芳烃亲电子试剂的底物范围。
[EN] THIOPHENE DERIVATIVES FOR THE TREATMENT OF DISORDERS CAUSED BY IGE<br/>[FR] DÉRIVÉS DE THIOPHÈNE POUR LE TRAITEMENT DE TROUBLES PROVOQUÉS PAR IGE
申请人:UCB BIOPHARMA SRL
公开号:WO2019243550A1
公开(公告)日:2019-12-26
Thiophene derivatives of formula (I) and a pharmaceutically acceptable salt thereof are provided. These compounds have utility for the treatment or prevention of disorders caused by IgE, such as allergy, type 1 hypersensitivity or familiar sinus inflammation.
The present invention relates to compounds of Formula (I),
or a form thereof, wherein ring A, R
1
, L and R
2
are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
[EN] PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS<br/>[FR] COMPOSES DE PYRAZINE COMME INHIBITEURS DE PHOSPHODIESTERASE 10
申请人:AMGEN INC
公开号:WO2010057121A1
公开(公告)日:2010-05-20
Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
[EN] SUBSTITUTED SULFONAMIDE COMPOUNDS<br/>[FR] COMPOSÉS DE SULFONAMIDE SUBSTITUÉS
申请人:HOFFMANN LA ROCHE
公开号:WO2014049047A1
公开(公告)日:2014-04-03
The invention is concerned with the compounds of formula (I), and salts thereof, wherein X, Y, Z, R1, R2, R3, R3, R4, R5 and R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of Formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
The present invention provides a novel bridged artificial nucleic acid and an oligomer containing the same as a monomer. The present invention provides specifically a compound represented by general formula (I) (wherein each symbol is the same as defined in the specification) or salts thereof; as well as an oligonucleotide compound represented by general formula (I′) (wherein each symbol is the same as defined in the specification) or salts thereof.