179605-63-1Relevant articles and documents
Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists
Moir, Elizabeth M.,Yoshiizumi, Kazuya,Cairns, Jim,Cowley, Phillip,Ferguson, Morag,Jeremiah, Fiona,Kiyoi, Takao,Morphy, Richard,Tierney, Jason,Wishart, Grant,York, Mark,Baker, James,Cottney, Jean E.,Houghton, Andrea K.,McPhail, Petula,Osprey, Andrew,Walker, Glenn,Adam, Julia M.
scheme or table, p. 7327 - 7330 (2011/01/12)
Bicyclic piperazine derivatives were synthesized as conformationally constrained analogs of N-alkyl piperazines and were found to be potent CB1 receptor agonists. The CB1 receptor agonist activity was dependent upon the absolute configuration of the chiral center of the bicyclic ring system. Although the conformational constraint did not protect the compounds from metabolism by N-dealkylation, several bicyclic analogs were found to be more potent than the unconstrained lead compound. Compound 8b demonstrated potent antinociceptive activity in vivo.
TRICYCLIC 1-[(3-INDOL-3-YL)CARBONYL] PIPERAZINE DERIVATIVES AS CANNABINOID CB1 RECEPTOR AGONISTS
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Page 14-15, (2010/02/12)
The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH2, O or S; R represents 1-3 substituents independently selected from H, (C1-4)alkyl, (C1-4)alky
Asymmetric synthesis of octahydro-2H-pyrido[1,2-a]-pyrazines
Froelich, Olivier,Cossart, Fran?oise,Bonin, Martine,Quirion, Jean-Charles,Husson, Henri-Philippe
, p. 2065 - 2072 (2007/10/03)
A series of optically pure octahydro-2H-pyrido[1,2-a]pyrazines has been prepared from (-)-2-cyano-6-phenyloxazolopiperidine (4). 2H-Pyrido[1,2- a]pyrazin-3-(4H)-one (7) and octahydro-2H-pyrido[1,2-a]pyrazine (14) were obtained from diamino alcohol (5) by
BICYCLIC NONANE AND DECANE COMPOUNDS HAVING DOPAMINE RECEPTOR AFFINITY
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, (2008/06/13)
Described herein are D4 receptor-selective compounds of the general formula: STR1 wherein: A and B are independently selected, substituted or unsubstituted, unsaturated 5-or 6-membered, homo-or heterocyclic rings;X 1 is selected from O, S, SO, SO 2, CH. sub.2, C=O, CH--OH, CH--N(C 1-4 alkyl) 2, C= CHCl, and C=CHCN;X 2---is selected from N= , CH. sub.2--, CH= and C(O)--;n is 1 or 2; R 1 is selected from H and the α-carbon side chain of an amino acid;R 2 and R 3 are selected independently from H, OH,--NH 2,--C(O)NH 2 =O, =S,halo, cyano, C 1-9 alkyl, C 1-9 alkoxy, C 1-4 alkylS--, C 1-4 alkylSO--, C 1-4 alkylSO 2--, phenoxy, benzyloxy and piperonyloxy; andH* is in either the R-or the S-configuration,and acid addition salts, solvates and hydrates thereof.Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.