38150-01-5Relevant academic research and scientific papers
HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS
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Paragraph 0856, (2018/06/12)
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
TRIAZOLE PHENYL COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR
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Paragraph 0276, (2018/06/06)
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I), (II) where the definitions of the variables are provided herein.
TRIAZOLE PYRIDYL COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR
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Paragraph 0249, (2018/06/06)
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the structures where the definitions of the variables are provided herein.
HETEROCYCLIC TRIAZOLE COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR
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Paragraph 1004; 1005, (2017/12/01)
Compounds of Formula I and Formula II, pharmaceutically acceptable salts thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
Combination of cyclohexane and piperazine based κ-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines
Bourgeois, Christian,Werfel, Elena,Schepmann, Dirk,Wuensch, Bernhard
, p. 3316 - 3324 (2014/06/23)
Desymmetrization of the pseudochiral (2r)-configured cyclohexane-1,2,3- triamines 8 with dimethyl oxalate led to racemic aminoquinoxaline-2,3-diones 9. Selective introduction of the κ pharmacophoric structural elements pyrrolidine and 3,4-dichlorophenylacetamide with a two-carbon distance afforded conformationally restricted κ agonists 13-15 based on the quinoxaline ring system. In competitive radioligand receptor binding studies the benzylamine 13b, the secondary amine 14b, and the carbamate 15 displayed high κ receptor affinity. The Ki value of the lead compound derived methoxycarbonyl derivative 15 is 9.7 nM. However, the κ affinity of 15 is exceeded by 13b and 14b with a basic functional group instead of the methoxycarbonyl group in 1-position of the quinoxaline system. The chlorine atoms of the dichlorophenylacetyl residue are essential, since the corresponding phenylacetyl analogs show considerably reduced κ affinity. The potent κ ligands 13b, 14b and 15 are selective over the related μ- and δ-opioid receptors, σ1, σ2 and NMDA receptors. In the [35S]GTPγS-binding assay 13b behaved as partial agonist with lower activity than U-69,593.
PERHYDROQUINOXALINE DERIVATIVES USEFUL AS ANALGESICS
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Page/Page column 24; 53, (2014/12/12)
The present invention relates to perhydroquinoxaline compounds according to the general formula (1), their use as a medicament, in particular as analgesic, antipruritic and antiinflammatory agents, and their preparation.
PERHYDROQUINOXALINE DERIVATIVES
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Page/Page column 11, (2010/12/29)
The present invention relates to perhydroquinoxaline derivatives, processes for their preparation, their use for the preparation of a medicament and medicaments containing perhydroquinoxaline derivatives.
Enantioselective Saponification of Diacetates of 2-Nitro-1,3-propanediols by Pig-Liver Esterase and Preparation of Enantiomerically Pure Derivatives of 2-Nitro-allylic Alcohols (Chiral Multiple-Coupling Reagents)
Eberle, Martin,Egli, Martin,Seebach, Dieter
, p. 1 - 23 (2007/10/02)
The reproducible enantioselective saponification of open-chain and cyclic diacetates of meso-2-nitro-1,3-propanediols (see 4b-13b) with pig-liver esterase (PLE) gives monoacetates (see 4c-13c) of >95percent enantiomeric excess.The Re enantiotopic acetate group appears to be saponified preferentially, as proved by the X-ray crystal structure analysis of three camphanoates 4d, 6d, and 7d.Elimination of H2O or AcOH from the hydroxy acetates thus available gives derivatives of nitro-allylic alcohols (see 20-24, 27, and 29) which are subjected to diastereoselective Michael additions or SN2' substitutions.
Studies on Synthesis and Anticancer Activity of Selected N-(2-Fluoroethyl)-N-nitrosoureas
Johnston, Thomas P.,Kussner, Conrad L.,Carter, Ronald L.,Frye, Jerry L.,Lomax, Nancita R.,et al.
, p. 1422 - 1426 (2007/10/02)
An activated carbamate, 2-nitrophenyl (2-fluoroethyl)nitrosocarbamate (3), was used to advantage in the synthesis of the water-soluble (2-fluoroethyl)nitrosoureas 6a-d from 2-aminoethanol, (1α,2β,3α)-2-amino-1,3-cyclohexanediol, cis-2-hydroxycyclohexanol, and 2-amino-2-deoxy-D-glucose.In a variation of this method, 2,4,5-trichlorophenyl (2-fluoroethyl)carbamate (4) was used to prepare the urea from which the essentially water-insoluble N'-(2,6-dioxo-3-piperidinyl)-N-(2-fluoroethyl)-N-nitrosourea (6e) was derived.The anticancer activity of these nitrosoureas was determined against the murine tumors B16 melanoma and Lewis lung carcinoma and found to be significant and comparable to their chloroethyl counterparts.On the basis of results from both systems, the dihydroxycyclohexyl derivative 6b may be the most effective.
