Palladium(0)-Catalyzed Coupling of Organozinc Iodide Reagents with Bromopyridines: Synthesis of Selectively Protected Pyridine-Containing Azamacrocycles
摘要:
The synthesis of azamacrocycles in which the ring nitrogens are regioselectively functionalized is described. An organozinc palladium(0)-catalyzed coupling with an appropriately functionalized bromopyridine generated a key intermediate, which was transformed in two steps to a desired precursor and subjected to an intramolecular N-alkylation to effect a macrocyclization affording selectively protected azamacrocycles 1-3.
Palladium(0)-Catalyzed Coupling of Organozinc Iodide Reagents with Bromopyridines: Synthesis of Selectively Protected Pyridine-Containing Azamacrocycles
摘要:
The synthesis of azamacrocycles in which the ring nitrogens are regioselectively functionalized is described. An organozinc palladium(0)-catalyzed coupling with an appropriately functionalized bromopyridine generated a key intermediate, which was transformed in two steps to a desired precursor and subjected to an intramolecular N-alkylation to effect a macrocyclization affording selectively protected azamacrocycles 1-3.
The present invention relates to compounds of formula I:
1
in which R
1
is a linear group or a five membered heterocycle optionally fused to a phenyl ring, R
2
is a 5-membered heterocycle, R
3
is chosen from a range of substituents, m is 0-3 and n is 0 or 1; the compounds are generally inverse agonists at GABA-A receptors containing the alpha 5 subunit and so are useful in methods of enhancing cognition in subjects with diminished cognition in diseases such as Alzheimer's Disease.
NOVEL ALKYNYL DERIVATIVES AS MODULATORS OF METATROPIC GLUTAMATE RECEPTORS
申请人:Bessis Anne-Sophie
公开号:US20090124625A1
公开(公告)日:2009-05-14
The present invention relates to novel compounds of formula (I) wherein W, n, X and W′ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
Pyridine, pyrimidine and pyrazine derivatives as gpcr agonists
申请人:Bradley Stuart Edward
公开号:US20100035897A1
公开(公告)日:2010-02-11
Compounds of formula (I): R
1
-A-V—B—R
2
, wherein V is phenyl or a 6-membered heteroaryl ring containing up to three N-atoms, or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.
NOVEL ALKYNYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
申请人:Bessis Anne-Sophie
公开号:US20120277237A1
公开(公告)日:2012-11-01
The present invention relates to novel compounds of formula I wherein W, n, X and W′ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
Alkynyl derivatives as modulators of metabotropic glutamate receptors
申请人:Addex Pharma SA
公开号:EP2426115A2
公开(公告)日:2012-03-07
The present invention relates to novel compounds of formula I wherein W, n, X and W' are defined in the description; invention compounds are modulators of metabotropic glutamate receptors - subtype 5 ("mGluR5") which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
本发明涉及式 I 的新型化合物,其中 W、n、X 和 W' 在描述中定义;本发明化合物是代谢谷氨酸受体-亚型 5("mGluR5")的调节剂,可用于治疗中枢神经系统疾病以及受 mGluR5 受体调节的其他疾病。