BENZIMIDAZOLE AND IMADAZOPYRIDINE CARBOXIMIDAMIDE COMPOUNDS
申请人:Gilead Sciences, Inc.
公开号:US20160333009A1
公开(公告)日:2016-11-17
The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDOL) inhibitors of Formula I:
or pharmaceutically acceptable salts thereof, in which X, L, n, m, R
1
, R
2a
, R
2b
, R
n
, R
m
, and R
t
are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.
本公开提供了式I的吲哌酮2,3-二氧化酶1(IDOL)抑制剂:
或其药学上可接受的盐,其中X、L、n、m、R
1
、R
2a
、R
2b
、R
n
、R
m
和R
t
如本文所定义,以及包括式I化合物的药物组合物,或其药学上可接受的盐,并使用这些方法来治疗由IDO1介导的疾病。
[EN] SOLVENTS<br/>[FR] SOLVANTS
申请人:BIONIQS LTD
公开号:WO2009034329A1
公开(公告)日:2009-03-19
There is described the use of a protic ionic liquid comprising a trialkylammonium salt as a solvent.
A procedure for the synthesis of tertiary amines via reductiveamination of aldehydes with molecular hydrogen as a reducing agent using homogeneous rhodium catalysis is presented. Using an amine to aldehyde ratio of 4/1 enabled the synthesis of tertiary amines from nine different aldehydes and nine different secondary amines with selectivities up to 99% and turnover frequencies (TOF) up to 7200 h−1
提出了一种使用均相铑催化通过分子氢作为还原剂对醛类进行还原胺化反应合成叔胺的方法。使用胺/醛比率为4/1时,可以由9种不同的醛和9种不同的仲胺合成叔胺,其选择性高达99%,周转频率(TOF)高达7200 h -1... 反应显示出对醇和酯功能的高耐受性,从而允许形成多功能分子。另外,仲胺也可以通过该合成来制备。对于所有化合物,活性都是通过吸收氢气来确定的。为了增加该过程的可持续性和效率,已经成功地制定了剂量策略。使用确定的反应指标,可以化学计量使用醛和胺,而不会显着降低选择性。
[EN] QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS<br/>[FR] DÉRIVÉS DE QUINOLONE UTILISÉS EN TANT QU'INHIBITEURS DU RÉCEPTEUR DU FACTEUR DE CROISSANCE DES FIBROBLASTES
申请人:PRINCIPIA BIOPHARMA INC
公开号:WO2016191172A1
公开(公告)日:2016-12-01
Compounds of formula (I) that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
The invention relates to compounds of formula (I):
wherein R
1
, R
2
, R
3
, R
4
, R
5
, and R
6
as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).