13295-53-9Relevant academic research and scientific papers
NON-FUSED TRICYCLIC COMPOUNDS
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Paragraph 00561, (2018/11/26)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Piperazine derivatives and their use as therapeutic agents
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Paragraph 0120, (2016/03/19)
Compounds for treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the compounds are of formula (I): where x y, W, V, R 2 , R 3 , R 4 , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , R 8a , R 9 and R 9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
THIAZOLES AS MODULATORS OF RORyt
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Page/Page column 58, (2016/05/19)
The present invention comprises compounds of Formula I. Formula I wherein: R1, R2, R3, R4, R5, R7, R8, and (A) are defined in the specification. The invention also comprises a co
Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists
Liu, Yang,Zhang, Qing,Chen, Lin-Hai,Yang, Hui,Lu, Wei,Xie, Xin,Nan, Fa-Jun
supporting information, p. 579 - 583 (2016/07/06)
A series of alkylpyrimidine-4,6-diol derivatives were designed and synthesized as novel GRP84 agonists based on a high-throughput screening (HTS) hit 1. 6-Nonylpyridine-2,4-diol was identified as the most potent agonist of GPR84 reported so far, with an EC50 of 0.189 nM. These novel GPR84 agonists will provide valuable tools for the study of the physiological functions of GPR84.
MUSCARINIC AGONISTS
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Paragraph 0195, (2014/10/04)
Compounds of formula (I) and methods are provided for the treatment of disease or conditions in which modification of cholinergic, especially muscarinic receptor activity, has a beneficial effect.
DNA-dependent protein kinase (DNA-PK) inhibitors: Structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain
Clapham, Kate M.,Bardos, Julia,Finlay, M. Raymond V.,Golding, Bernard T.,Griffen, Edward J.,Griffin, Roger J.,Hardcastle, Ian R.,Menear, Keith A.,Ting, Attilla,Turner, Paul,Young, Gail L.,Cano, Céline
body text, p. 966 - 970 (2011/03/20)
Introduction of an O-alkoxyphenyl substituent at the 8-position of the 2-morpholino-4H-chromen-4-one pharmacophore enabled regions of the ATP-binding site of DNA-dependent protein kinase (DNA-PK) to be probed further. Structure-activity relationships have been elucidated for inhibition of DNA-PK and PI3K (p110α), with N-(2-(cyclopropylmethoxy)-4-(2-morpholino-4-oxo-4H- chromen-8-yl)phenyl)-2-morpholinoacetamide 11a being identified as a potent and selective DNA-PK inhibitor (IC50 = 8 nM).
COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 25, (2010/10/19)
Disclosed herein are cannabinoid receptor ligands of formula (1) wherein Ring A and R1 are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also described
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 52, (2010/04/23)
Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Peptide deformylase inhibitors with retro-amide scaffold: Synthesis and structure-activity relationships
Lee, Seung Kyu,Choi, Kwang Hyun,Lee, Sang Jae,Suh, Se Won,Kim, B. Moon,Lee, Bong Jin
body text, p. 4317 - 4319 (2010/10/03)
Peptide deformylase (PDF) is a metalloprotease catalyzing the removal of a formyl group from newly synthesized proteins. Thus inhibition of PDF activity is considered to be one of the most effective antibiotic strategies. Reported herein are the synthesis
PYRIDAZINONE GLUCOKINASE ACTIVATORS
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Page/Page column 45-46, (2009/10/30)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
