244022-63-7Relevant articles and documents
Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine
Nichols, Paula L.,Brand, Jonathan,Briggs, Michael,D'Angeli, Mathilde,Farge, Jennifer,Garland, Stephen L.,Goldsmith, Paul,Hutchings, Rio,Kilford, Ian,Li, Ho Y.,MacPherson, David,Nimmo, Fiona,Sanderson, Francis Dominic,Sehmi, Sanjeet,Shuker, Nicola,Skidmore, John,Stott, Michael,Sweeting, Jennifer,Tajuddin, Hasmi,Takle, Andrew K.,Trani, Giancarlo,Wall, Ian D.,Ward, Robert,Wilson, David M.,Witty, David
scheme or table, p. 1368 - 1372 (2010/07/02)
A pharmacophore model was built, based on known CGRP receptor antagonists, and this was used to aid the identification of novel leads. Analogues were designed, modelled and synthesised which incorporated alternative 'LHS' fragments linked via either an amide or urea to a privileged 'RHS' fragment commonly found in CGRP receptor antagonists. As a result a novel series of oxadiazole CGRP receptor antagonists has been identified and the subsequent optimisation to enhance both potency and bioavailability is presented.
3- (1,2,4-TRIAZOL-3YLALKYL) AZABRICLO (3.1.0) HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS
-
Page/Page column 62-63, (2008/06/13)
The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: wherein " G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; " p is an integer ranging from 0 to 5; " R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5, or corresponds to a group R5; " each R2 is independently hydrogen, fluorine or C1-4alkyl; " n is 2, 3, 4, or 5; " R3 is C1-4alkyl; " R4 is hydrogen, or a C1-4alkyl group, a benzyl group, a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5;or R4 is a -SR6 group; " R5 is selected from a group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; " R6 is C1-4alkyl or -CH2C3-4cycloalkyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1. processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
Triazole derivatives
-
, (2011/03/17)
The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.