- PYRROLOPYRIMIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS
-
Disclosed are chemical entities of formula I: [INSERT CHEMICAL FORMULA HERE] wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula I, and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.
- -
-
Paragraph 0268
(2016/04/09)
-
- Naphthyridin derivatives
-
The present invention relates to heterocyclic derivatives of formula I wherein R1, R2 and R3 are as defined in the description and claims, which compounds are metabotropic glutamate receptor 5 antagonists.
- -
-
Page/Page column 29
(2008/06/13)
-
- Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1
-
A structurally unique and new class of opioid receptor antagonists (OpRAs) that bear no structural resemblance with morphine or endogenous opioid peptides has been discovered. A series of carboxamido-biaryl ethers were identified as potent receptor antagonists against mu, kappa and delta opioid receptors. The structure-activity relationship indicated para-substituted aryloxyaryl primary carboxamide bearing an amine tether on the distal phenyl ring was optimal for potent in vitro functional antagonism against three opioid receptor subtypes.
- Takeuchi, Kumiko,Holloway, William G.,McKinzie, Jamie H.,Suter, Todd M.,Statnick, Michael A.,Surface, Peggy L.,Emmerson, Paul J.,Thomas, Elizabeth M.,Siegel, Miles G.,Matt, James E.,Wolfe, Chad N.,Mitch, Charles H.
-
p. 5349 - 5352
(2008/02/13)
-
- IMIDAZOPYRIDINE COMPOUND
-
The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents -(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.
- -
-
Page/Page column 35
(2008/06/13)
-
- Method for preparing 2,5-dihalo- and 2,5,6-trihalopyridines
-
A method for preparing 2,5-dihalo- and 2,5,6-trihalopyridines corresponding to the formula SPC1 Wherein each X independently represents chloro, fluoro or bromo and R represents hydrogen, chloro, fluoro or bromo which comprises reacting a halohydrazinopyridine of one of the formulas SPC2 With an excess of an aqueous alkali metal hydroxide in the presence of a reaction medium from the group consisting of loweralkanols of 1 to 4 carbon atoms and loweralkylglycols of 2 to 4 carbon atoms.
- -
-
-