937400-07-2Relevant academic research and scientific papers
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes
Guo, Liangqin,Parker, Dann L.,Zang, Yi,Sweis, Ramzi F.,Liu, Weiguo,Sherer, Edward C.,Buist, Nicole,Terebetski, Jenna,Kelly, Terri,Bugianesi, Randal,Priest, Birgit T.,Dingley, Karen H.,Li, Xiaofang,Mitelman, Stan,Salituro, Gino,Trujillo, Maria E.,Pachanski, Michele,Kirkland, Melissa,Powles, Mary Ann,Eiermann, George J.,Feng, Yue,Shang, Jin,Howard, Andrew D.,Ujjainwalla, Feroze,Sinz, Christopher J.,Debenham, John S.,Edmondson, Scott D.,Nargund, Ravi P.,Hagmann, William K.,Li, Derun
, p. 1107 - 1111 (2016/12/16)
GPR142 has been identified as a potential glucose-stimulated insulin secretion (GSIS) target for the treatment of type 2 diabetes mellitus (T2DM). A class of triazole GPR142 agonists was discovered through a high throughput screen. The lead compound 4 suffered from poor metabolic stability and poor solubility. Lead optimization strategies to improve potency, efficacy, metabolic stability, and solubility are described. This optimization led to compound 20e, which showed significant reduction of glucose excursion in wild-type but not in GPR142 deficient mice in an oral glucose tolerance test (oGTT) study. These studies provide strong evidence that reduction of glucose excursion through treatment with 20e is GPR142-mediated, and GPR142 agonists could be used as a potential treatment for type 2 diabetes.
NOVEL PHENYL IMIDAZOLES AND PHENYL TRIAZOLES AS GAMMA-SECRETASE MODULATORS
-
Page/Page column 52, (2010/09/18)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed
Prodrug of cinnamide compound
-
Page/Page column 50, (2009/03/07)
The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.
TRIAZOLE DERIVATIVES FOR TREATING ALZHEIMER'S DISEASE AND RELATED CONDITIONS
-
Page/Page column 34-35, (2009/01/23)
Compounds of formula I: Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain, in particular Alzheimer's disease.
Morpholine type cinnamide compound
-
Page/Page column 67-68; 70, (2008/06/13)
The present invention relates to a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein R1, R2, R3, and R4 are the same or different and each represent a hydrogen atom or a C1-6 alkyl group; X1 represents a C1-6 alkylene group that may be substituted; Xa represents a methoxy group or a fluorine atom; Xb represents an oxygen atom or a methylene group, provided that Xb is only an oxygen atom when Xa is a methoxy group; and Ar1 represents an aryl group, pyridinyl group, aryloxy group, or pyridinyloxy group that may have a substituent such as a halogen atom; and to use of the compound or salt as a pharmaceutical agent.
