6717-00-6Relevant academic research and scientific papers
Benzo aliphatic ring derivatives, and applications thereof
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Paragraph 0293; 0296-0299, (2019/03/12)
The invention discloses benzo aliphatic ring derivatives, and applications thereof. The benzo aliphatic ring derivatives are prepared through substation of benzo aliphatic ring compounds with nitrogenheterocyclic ring containing substituent groups. Most o
Drug Repurposing of Haloperidol: Discovery of New Benzocyclane Derivatives as Potent Antifungal Agents against Cryptococcosis and Candidiasis
Ji, Changjin,Liu, Na,Tu, Jie,Li, Zhuang,Han, Guiyan,Li, Jian,Sheng, Chunquan
, (2019/10/16)
Despite the high morbidity and mortality of invasive fungal infections (IFIs), effective and safe antifungal agents are rather limited. Starting from antifungal lead compound haloperidol that was identified by drug repurposing, a series of novel benzocycl
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder
Marcin, Lawrence R.,Warrier, Jayakumar,Thangathirupathy, Srinivasan,Shi, Jianliang,Karageorge, George N.,Pearce, Bradley C.,Ng, Alicia,Park, Hyunsoo,Kempson, James,Li, Jianqing,Zhang, Huiping,Mathur, Arvind,Reddy, Aliphedi B.,Nagaraju,Tonukunuru, Gopikishan,Gupta, Grandhi V. R. K. M.,Kamble, Manjunatha,Mannoori, Raju,Cheruku, Srinivas,Jogi, Srinivas,Gulia, Jyoti,Bastia, Tanmaya,Sanmathi, Charulatha,Aher, Jayant,Kallem, Rajareddy,Srikumar, Bettadapura N.,Vijaya, Kumar Kuchibhotla,Naidu, Pattipati S.,Paschapur, Mahesh,Kalidindi, Narasimharaju,Vikramadithyan, Reeba,Ramarao, Manjunath,Denton, Rex,Molski, Thaddeus,Shields, Eric,Subramanian, Murali,Zhuo, Xiaoliang,Nophsker, Michelle,Simmermacher, Jean,Sinz, Michael,Albright, Charlie,Bristow, Linda J.,Islam, Imadul,Bronson, Joanne J.,Olson, Richard E.,King, Dalton,Thompson, Lorin A.,Macor, John E.
supporting information, p. 472 - 477 (2018/05/23)
There is a significant unmet medical need for more efficacious and rapidly acting antidepressants. Toward this end, negative allosteric modulators of the N-methyl-d-aspartate receptor subtype GluN2B have demonstrated encouraging therapeutic potential. We
Selective NR2B Antagonists
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Paragraph 0441, (2015/07/15)
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the c
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.
4-ARYLMORPHOLIN-3-ONE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE THEREOF
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Page/Page column 21, (2008/06/13)
The invention relates to compounds corresponding to formula (I): in which: Ar represents a mono- or disubstituted phenyl; R1 represents an unsubstituted or substituted phenyl; R2 represents: a pyridyl; an unsubstituted or substituted phenyl; a benzyl that is unsubstituted or substituted on the phenyl; R2 may moreover represent: a heterocyclic radical; R3 represents various values. The invention also comprises methods for the compounds preparation, formulations comprising them and therapeutic applications thereof.
A critical structural determinant of opioid receptor interaction with phenolic 5-phenylmorphans.
Kim, In Jong,Dersch, Christina M,Rothman, Richard B,Jacobson, Arthur E,Rice, Kenner C
, p. 4543 - 4550 (2007/10/03)
The opioid receptor binding affinities of N-methyl- and N-phenethyl-5-phenylmorphans with a meta-hydroxy substituent [3-(2-methyl-2-azabicyclo[3.3.1]non-5-yl)-phenol (1a), and 3-(2-phenethyl-2-azabicyclo[3.3.1]non-5-yl)-phenol (1b)] were compared with the
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.
Studies on the N-dealkylated metabolite of haloperidol
Lyles-Eggleston,Margaret,McCollough,Craig,Fan,Pingchen,Ablordeppey,Mardenborough, Joy H.,Leroy,Ablordeppey,Seth,Borne
, p. 686 - 695 (2007/10/03)
The recent detection of 4-Chlorophenyl-4-piperidinol (CPPO), in rats fed haloperidol and the subsequent demonstration that CPPO produces a freezing action in frogs, has encouraged us to study the structural features that might be responsible for the freezing action. In this study, we have shown that removal of the chloro from the phenyl ring has little effect on the freezing action and the removal of the tertiary alcohol from the piperidine only decreases somewhat the effectiveness of the freezing action. In addition, since replacing the piperidine ring with tetrahydropyridine and piperazine moieties led to compounds without the freezing action, and because 4-phenylpiperidine is the common entity in all the compounds with the freezing action, it is reasonable to suggest that the 4-phenylpiperidine moiety may be responsible for the freezing action observed in CPPO.
Substituted piperidines - Highly potent renin inhibitors due to induced fit adaptation of tile active site
Vieira, Eric,Binggeli, Alfred,Breu, Volker,Bur, Daniel,Fischli, Walter,Gueller, Rolf,Hirth, Georges,Maerki, Hans Peter,Mueller, Marcel,Oefner, Christian,Scalone, Michelangelo,Stadler, Heinz,Wilhelm, Maurice,Wostl, Wolfgang
, p. 1397 - 1402 (2007/10/03)
The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified.
