3308-98-3Relevant academic research and scientific papers
Oxacycle synthesis via intramolecular reaction of carbanions and peroxides
Willand-Charnley, Rachel,Puffer, Benjamin W.,Dussault, Patrick H.
supporting information, p. 5821 - 5823 (2014/05/20)
The intramolecular reaction of dialkyl peroxides with carbanions, generated via chemoselective metal-heteroatom exchange or deprotonation, provides a new approach to cyclic ethers. Applied in tandem with C-C bond formation, the strategy enables a one-step annelation to form oxaospirocycles.
BETA-CARBOLINES AS INHIBITORS OF HASPIN AND DYRK KINASES
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Page/Page column 28-29, (2011/11/06)
The present disclosure is directed to compounds of Formula ( I ) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and
6-N-Linked Heterocycle-Substituted 2,3,4,5-Tetrahydro-1H-Benzo[d]Azepines as 5-Ht2c Receptor Agonists
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Page/Page column 22-23, (2008/12/08)
The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: Formula (I) where: R6 is selected from the group consisting of (a, b, c, d, e) and other substituents are as defined in the specification.
Polymethylene derivatives of nucleic bases with ω-functional groups: V. Pyrimidine- and purine-containing γ-butyrophenones
Kritzyn,Komissarov
, p. 549 - 555 (2007/10/03)
New polymethylene derivatives of nucleic bases containing a keto function in the ω-position were synthesized by alkylation of nucleic bases with 2-(3-chloropropyl)-2-phenyl-1,3-dioxolane and the subsequent deblocking of the keto group; their physicochemical properties were studied.
Synthesis of 1-aryl-4-azolylbutanones
Karachev,Popkov
, p. 987 - 993 (2007/10/03)
A convenient method was developed for the synthesis of substituted 4-azolyl-1-arylbutanones from the available γ-chlorobutyrophenones by successive stages of transformation into ketals, alkylation of sodium imidazolate or 1,2,4-triazolate by the ketals in
Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28
Hulshof, Janneke W.,Casarosa, Paola,Menge, Wiro M. P. B.,Kuusisto, Leena M. S.,Van Der Goot, Henk,Smit, Martine J.,De Esch, Iwan J. P.,Leurs, Rob
, p. 6461 - 6471 (2007/10/03)
US28 is a human cytomegalovirus (HCMV) encoded G-protein-coupled receptor that signals in a constitutively active manner. Recently, we identified 1 {5-(4-(4-chlorophenyl)-4-hydroxy-piperidin-1-yl)-2,2-diphenylpentanenitrile} as the first reported nonpeptidergic inverse agonist for a viral-encoded chemokine receptor. Interestingly, this compound is able to partially inhibit the viral entry of HIV-1. In this study we describe the synthesis of 1 and several of its analogues and unique structure-activity relationships for this first class of small-molecule ligands for the chemokine receptor US28. Moreover, the compounds have been pharmacologically characterized as inverse agonists on US28. By modification of lead structure 1, it is shown that a 4-phenylpiperidine moiety is essential for affinity and activity. Other structural features of 1 are shown to be of less importance. These compounds define the first SAR of ligands on a viral GPCR (US28) and may therefore serve as important tools to investigate the significance of US28-mediated constitutive activity during viral infection.
NPY antagonists: spiroisoquinolinone derivatives
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Page column 10, (2008/06/13)
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of spiroisoquinolinone derivatives of Formula I. As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
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.
Stereocontrol between remote atom centers in acyclic substrates. Anti addition of hydride to 1,5-, 1,6-, and 1,7-hydroxy ketones
Zhang, Han-Cheng,Harris, Bruce D.,Costanzo, Michael J.,Lawson, Edward C.,Maryanoff, Cynthia A.,Maryanoff, Bruce E.
, p. 7964 - 7981 (2007/10/03)
For conformationally unconstrained, acyclic organic compounds, the control of stereogenic centers at remote positions of a chain, that is, at a distance of four or more atom centers, remains a challenging problem in asymmetric synthesis. We report on our
Synthesis and Antiarrhythmic Activity of cis-2,6-Dimethyl-α,α-diaryl-1-piperidinebutanols
Hoefle, M. L.,Blouin, L. T.,Fleming, R. W.,Hastings, S.,Hinkley, J. M.,et al.
, p. 12 - 19 (2007/10/02)
A series of α,α-diaryl-1-piperidinebutanols was evaluated for antiarrhythmic activity in the coronary ligated dog model.Structure-activity relationship studies indicated that the 2,6-dimethylpiperidine group yielded compounds with the best antiarrhythmic
