99329-68-7Relevant academic research and scientific papers
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists
Conway, Richard J.,Valant, Celine,Christopoulos, Arthur,Robertson, Alan D.,Capuano, Ben,Crosby, Ian T.
supporting information; experimental part, p. 2560 - 2564 (2012/05/05)
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.
Diastereoselective One-Pot Synthesis of 7- and 8-Substituted 5-Phenylmorphans
Lim, Hwan Jung,Deschamps, Jeffrey R.,Jacobson, Arthur E.,Rice, Kenner C.
supporting information; experimental part, p. 5322 - 5325 (2011/12/01)
Novel 7- and 8-alkyl and aryl substituted 5-phenylmorphans were synthesized from substituted allyl halides and N-benzyl-4-aryl-1,2,3,6-tetrahydropyridine by a highly efficient and diastereoselective reaction series, "one-pot" alkylation and ene-imine cycl
Biaryl piperidines as potent and selective delta opioid receptor ligands
Liras, Spiros,McHardy, Stanton F.,Allen, Martin P.,Segelstein, Barb E.,Heck, Steven D.,Bryce, Dianne K.,Schmidt, Anne W.,Vanase-Frawley, Michelle,Callegari, Ernesto,McLean, Stafford
scheme or table, p. 503 - 507 (2010/04/05)
The design and synthesis of novel opiates are reported. Based on the message-address principle a novel class of 4,4- and 3,3-biaryl piperidines was designed and synthesized. Biological evaluation confirmed that these compounds exhibit high affinity and se
Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a -agonist δ-antagonist and δ-inverse agonists
Cheng, Kejun,Kim, In Jong,Lee, Mei-Jing,Adah, Steven A.,Raymond, Tyler J.,Bilsky, Edward J.,Aceto, Mario D.,May, Everette L.,Harris, Louis S.,Coop, Andrew,Dersch, Christina M.,Rothman, Richard B.,Jacobson, Arthur E.,Rice, Kenner C.
, p. 1177 - 1190 (2008/02/04)
Enantiomeric N-phenethyl-m-hydroxyphenylmorphans with various substituents in the ortho, meta or para positions of the aromatic ring in the phenethylamine side-chain (chloro, hydroxy, methoxy, nitro, methyl), as well as a pyridylethyl and a indolylethyl m
Modulators of dopamine neurotransmission
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Page/Page column 13, (2008/06/13)
A 3-substituted 4-(phenyl-N-alkyl)-piperazine compound of the following formula: wherein R1 is selected from the group consisting of OSO2CF3, OSO2CH3, SO2R3, COCF3, CO
Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
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Page/Page column 14, (2008/06/13)
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.
4,4-Biarylpiperidine derivatives
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, (2008/06/13)
The present invention relates to compounds of the formula I, 1wherein Z1, Z2, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such
NOVEL OPIATE COMPOUNDS, METHODS OF MAKING AND METHODS OF USE
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, (2008/06/13)
The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
Piperidine derivatives having renin inhibiting activity
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, (2008/06/13)
Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.
