HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES
申请人:Bunnage Mark Edward
公开号:US20130196952A1
公开(公告)日:2013-08-01
The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
Alkoxy-substituted 2-aminopyridines as ALK inhibitors
申请人:Bunnage Mark Edward
公开号:US08916593B2
公开(公告)日:2014-12-23
The invention relates to compounds of Formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
Synthesis and Catalytic Applications of an Extended Range of Tethered Ruthenium(II)/η<sup>6</sup>-Arene/Diamine Complexes
作者:Roy Hodgkinson、Václav Jurčík、Antonio Zanotti-Gerosa、Hans Günter Nedden、Andrew Blackaby、Guy J. Clarkson、Martin Wills
DOI:10.1021/om500788t
日期:2014.10.13
A series of novel enantiopure Ru(II) complexes containing a chiral diamine and eta(6)-arene connected by a tethering group have been prepared and were evaluated in the asymmetric reductions of a range of ketones. Changes to the level of steric hindrance and the addition of an electron withdrawing functionality on the sulfonyl group have a significant effect on the reactivity and enantioselectivity of the catalysts.
Synthesis of Aryl Ethers via a Sulfonyl Transfer Reaction
作者:Neal W. Sach、Daniel T. Richter、Stephan Cripps、Michelle Tran-Dubé、Huichun Zhu、Buwen Huang、Jean Cui、Scott C. Sutton
DOI:10.1021/ol301615z
日期:2012.8.3
A general synthesis of aryl ethers from primary and secondary alcohols and aryl mesylates is presented. The reaction proceeds via a sulfonyl-transfer mechanism. In this paper, we compare the sulfonyl transfer reaction to Mitsunobu ether formation. The reaction can be employed in a multistep synthesis where the aryl mesylate is used as a phenol protecting group and then as an activating group for ether formation. This protecting/activating group strategy is demonstrated using raloxifene as the target.