SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS
申请人:Dahmann Georg
公开号:US20130023502A1
公开(公告)日:2013-01-24
The invention relates to new substituted pyridinyl-pyrimidines of formula
1
wherein
ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O,
wherein R
1
, R
2
, R
4
, R
3
, R
5
and R
6
are defined as in claim
1
and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
PROCESS FOR PREPARING A PROPIOLIC ACID OR A DERIVATIVE THEREOF
申请人:Goossen Lukas J
公开号:US20140012000A1
公开(公告)日:2014-01-09
The invention relates to a process for preparing a propiolic acid or a derivative thereof by reacting a terminal alkyne with carbon dioxide, which comprises performing the reaction in the presence of a base and a copper complex, especially a copper (I) complex having at least one ligand, at least one of the ligands of the copper complex being selected from monodentate ligands which have an aminic or iminic nitrogen atom capable of coordination with copper, and polydentate ligands having at least two atoms or atom groups which are capable of simultaneous coordination with copper and are selected from nitrogen, oxygen, sulfur, phosphorus and carbene carbon.
Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
申请人:Cytovia, Inc.
公开号:US20030069239A1
公开(公告)日:2003-04-10
The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I:
1
wherein A, Ar
1
, Ar
2
, R
1
and R
3
are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Series of 2-phenyl-4-methylthiazole analogues are disclosed as potential therapeutic agents for the treatment of bacterial infections, especially methicillin-resistant
Straphylococcus aureus
(MRSA) related infections. A method for the treatment of MRSA-related infections is also claimed.
Palladium(0)-Catalyzed, Copper(I)-Mediated Coupling of Cyclic Thioamides with Alkenylboronic Acids, Organostannanes, and Siloxanes
作者:Nuzhat Arshad、Jamshed Hashim、C. Oliver Kappe
DOI:10.1021/jo900848s
日期:2009.7.17
The Pd-catalyzed cross-coupling of cyclic thioamides and thioureas with alkenylboronic acids, vinyl- and (het)arylstannanes, and arylsiloxanes in the presence of stoichiometric amounts of a Cu(I) cofactor is described. The desulfitative C−C cross-coupling protocol of the Liebeskind−Srogl type is performed under neutral conditions and can be applied to a range of heterocyclic structures with embedded