75017-17-3Relevant academic research and scientific papers
PYRAZINE GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Paragraph 0468-0469, (2016/02/03)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and R2 are defined herein.
TRIAZOLE AGONISTS OF THE APJ RECEPTOR
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Paragraph 01411, (2016/12/07)
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 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.
PYRAZOLE AMIDE DERIVATIVE
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Page/Page column 101, (2015/09/28)
The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.
Acceleration of the 4-exo radical cyclization to a synthetically useful rate. Cyclization of the 2,2-dimethyl-5-cyano-4-pentenyl radical
Park,Varick,Newcomb
, p. 2975 - 2978 (2007/10/02)
The title radical, formed in the reaction of the corresponding bromide with Bu3SnH, cyclizes in a 4-exo fashion to give the (3,3-dimethylcyclobutyl)cyanomethyl radical. At 50°C, the rate constant for cyclization is 1.9 x 104s-1.
gem-Dimethyl Effect in a Grignard Reagent Cyclization-Cleavage Rearrengament
Hill, Alexander E.,Link, Daniel C.,Donndelinger Peter
, p. 1177 - 1182 (2007/10/02)
(2,2-Dimethyl-4-penten-1-yl)magnesium bromide (1) is in equilibrium with its cyclic isomer, magnesium bromide (2).The equilibrium constant for this cyclization has a value of 2E-3.The gem-dimethyl substitution leads to an increase of a factor of about 22 in the equilibrium constant and also retards the rate of cleavage of 2.The sources of the gem-dimethyl effect in this system are discussed.
The Kinetics and Mechanism of Ring Opening of Radicals containing the Cyclobutylcarbinyl System
Beckwith, Athelstan L. J.,Moad, Graeme
, p. 1083 - 1092 (2007/10/02)
The kinetic parameters of β-fission of radicals containing the cyclobutylcarbinyl system have been determined by analysis of the mixtures obtained when suitable chloro-compounds are treated with tributylstannane.Under these conditions ring opening is irreversible and in the rigid bicyclic system (4) is under stereoelectronic control.For ring opening of cyclobutylcarbinyl radical (8) kf = 4.3 x 103 s-1 at 60 deg C, and the best values of the activation parameters appear to be ΔH(excit.) = 12.2 kcal mol-1 and ΔS(excit.) = -7.4 cal mol-1 K-1.Monocyclic systems undergo preferential fission of the more substituted βγ-bond.Methyl substituents at the α-, β-, or δ-positions have little effect but γ-substitution strongly enhances the rate of ring opening.The transition state is reactant-like and has a similar disposition of centres to that (1) for homolytic addition.
