54788-17-9Relevant articles and documents
NOVEL FXR (NR1H4 ) BINDING AND ACTIVITY MODULATING COMPOUNDS
-
, (2011/04/13)
The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
CYCLOHEXYLPYRAZOLE-LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
-
Page/Page column 27, (2009/05/29)
The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compound
PHARMACEUTICAL COMPOSITION COMPRISING A PYRAZOLE-O-GLUCOSIDE DERIVATIVE
-
Page/Page column 51, (2008/12/07)
The invention relates toa pharmaceutical composition comprising a pyrazole-O-glucoside derivative selected from the group of compounds (1) to (29) according to claim 1 in combination with at least one second therapeutic agent which is suitable in the trea
1-SUBSTITUTED-3- BETA-D-GLUCOPYRANOSYLATED NITROGENOUS HETERO- CYCLIC COMPOUNDS AND MEDICINES CONTAINING THE SAME
-
Page/Page column 23, (2008/06/13)
A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(β-D
METHODS FOR PREVENTING AND TREATING METABOLIC DISORDERS AND NEW PYRAZOLE-O-GLYCOSIDE DERIVATIVES
-
Page/Page column 37, (2010/11/25)
The invention relates to methods for preventing or treating metabolic disorders, for improving glycemic control, for preventing progression from impaired glucose tolerance, insulin resistance and/or from metabolic syndrome to type 2 diabetes mellitus, for
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. structure-activity relationships for chromophore modification and phenyl ring substitution
Palmer, Brian D.,Thompson, Andrew M.,Booth, R. John,Dobrusin, Ellen M.,Kraker, Alan J.,Lee, Ho H.,Lunney, Elizabeth A.,Mitchell, Lorna H.,Ortwine, Daniel F.,Smaill, Jeff B.,Swan, Leesa M.,Denny, William A.
, p. 4896 - 4911 (2007/10/03)
High-throughput screening has identified a novel class of inhibitors of the checkpoint kinase Wee1, which have potential for use in cancer chemotherapy. These inhibitors are based on a 4-phenylpyrrolo[3,4-c]-carbazole-1,3(2H,6H)- dione template and have been shown by X-ray crystallography to bind at the ATP site of the enzyme. An extensive study of the effects of substitution around this template has been carried out, which has identified substituents which lead to improvements in potency and selectivity for Wee1. While retention of the maleimide ring and pendant 4-phenyl group is necessary for potency, replacement of the carbazole nitrogen by oxygen is well tolerated and results in improved Wee1 selectivity against the related checkpoint kinase Chk1. Wee1 potency and selectivity are also enhanced by the incorporation of lipophilic functionality at the 2′-position of the 4-phenyl ring, and Wee1 selectivity against Chk1 is favored by C3-C5 alkyl substitution of the carbazole nitrogen. These studies provide a basis for the design of active analogues of the pyrrolocarbazole lead with improved physical properties.
THIENOPYRIDINE-PHENYLACET AMIDES AND THEIR DERIVATIVES USEFUL AS NEW ANTI-ANGIOGENIC AGENTS
-
Page/Page column 68, (2010/02/11)
The invention relates to compounds represented by Formula (I):, and to prodrugs thereof, pharmaceutically salts or solvates of said compounds or said prodrugs, wherein each of X1-X5 and R1-R5 are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).
1-H-3-aryl-pyrrolidine-2, 4-dione derivatives as pest-control agents
-
, (2008/06/13)
The present invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) in which A, B, G, X, Y and Z have the meanings given in the description, to processes for their preparation, and to intermediates therefor. The compounds
Synthesis and microbiological activities of some monohalogenated analogs of tyrosine
McCord,Smith,Winters,Grimes,Hulme,Robinson,Gage,Davis
, p. 26 - 29 (2007/10/06)
2 Chlorotyrosine and 2 bromotyrosine, as well as the previously reported 2 fluorotyrosine, were synthesized by hydrolysis of the condensation products from the appropriate benzyl bromide and ethyl acetamidomalonate and were compared with the corresponding