101048-77-5Relevant articles and documents
A CLASS OF BIFUNCTIONAL CHIMERIC HETEROCYCLIC COMPOUNDS FOR TARGETED DEGRADATION OF ANDROGEN RECEPTORS AND USE THEREOF
-
, (2022/03/07)
The present invention relates to a class of bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and use thereof, and specifically provides a compound of formula (I), or an isotopic compound thereof, or an optical isomer thereof, or a tautomer thereof, or a pharmacologically acceptable salt thereof, or a prodrug thereof, or a solvate thereof, wherein ARB is an androgen receptor recognition/binding part, L is a link part, and U is a ubiquitin protease recognition/binding part; and the three parts are connected by means of chemical bonds. The compound can perform the targeted degradation on androgen receptors in prostate cancer cells, and suppress the proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The compound has good application prospect in the preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating the related diseases regulated by the androgen receptors.
Identification and Structure–Activity Relationship (SAR) of potent and selective oxadiazole-based agonists of sphingosine-1-phosphate receptor (S1P1)
Liu, Tianqi,Jin, Jing,Chen, Yonghui,Xi, Qiumu,Hu, Jinping,Jia, Wenqiang,Chen, Xiaoguang,Li, Yan,Wang, Xiaojian,Yin, Dali
, p. 41 - 57 (2018/10/02)
Agonism of S1P1 receptor has been proven to be responsible for peripheral blood lymphopenia and elicts the identification of various S1P1 modulators. In this paper we described a series of oxadiazole-based S1P1 direct-acting agonists disubstituted on terminal benzene ring, with high potency for S1P1 receptor and favorable selectivity against S1P3 receptor. In addition, two representative agents named 16-3b and 16-3g demonstrated impressive efficacy in lymphocyte reduction along with reduced effect on heart rate when orally administered. Furthermore, these compounds have been shown to possess desired pharmacokinetic (PK) and physicochemical profiles. The binding mode between 16-3b and the activated S1P1 model was also studied.
Carboxylic acid compound containing diphenyl oxadiazole, and preparation method and medical application of compound
-
Paragraph 0032-0038, (2019/07/16)
The invention relates to the field of medicinal chemistry, and particularly relates to a carboxylic acid compound (I) containing a diphenyl oxadiazole skeleton, a preparation method and pharmaceuticalpreparation of the compound, and a use of the compound
Sphingosine-1-phosphate receptor modulator and application thereof
-
Paragraph 0077-0079, (2018/04/21)
The invention relates to a sphingosine-1-phosphate receptor modulator compound and a preparation method and application thereof. A compound, racemate, stereisomer, tautomer, solvent compound, hydrateor pharmaceutically acceptable salts shown in a formula (I) are specifically provided. (The formula (I) is shown in the attached figure.).
THIAZOLE DERIVATIVES FOR THE TREATMENT OF ANIMAL TRYPANOSOMIASIS
-
Page/Page column 67; 72, (2016/10/04)
The present invention relates to a novel class of compounds of general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein, to their use in human and veterinary medicine, and in the treatment of animal trypanosomiasis in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
NEW IMIDAZOLYLKETONE DERIVATIVES
-
Paragraph 0032; 0333, (2014/05/20)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds.
IMIDAZOLYLKETONE DERIVATIVES ASD ALDOSTERONE SYNTHASE INHIBITORS
-
Page/Page column 50-51, (2013/08/28)
The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds as inhibitors of aldosterone synthase.
Substituted phenyl farnesyltransferase inhibitors
-
, (2012/09/25)
Compounds of formula (I) or pharmaceutically acceptable salts thereof, inhibit farnesyltransferase. Methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.