203859-94-3Relevant academic research and scientific papers
AROMATIC AMINE AR AND BET TARGETING PROTEIN DEGRADATION CHIMERA COMPOUND AND USE
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, (2022/04/03)
An aromatic amine androgen receptor (AR) and BET targeting protein degradation chimera compound and its use. Specifically provided is a compound represented by formula I. Experimental results show that the compound can target and degrade both AR and BRD4, and down-regulate the expression of AR and BRD4 proteins; the compound can inhibit the proliferation of a variety of prostate cancer cells; the compound can inhibit the proliferation of a prostate cancer cell line LNCaP/AR, which overexpresses the AR, and can achieve a good inhibition effect on a prostate cancer cell line 22RV1, which is resistant to a marketed prostate cancer drug (enzalutamide); the compound also shows good metabolic stability, and has a good application prospect in the preparation of an AR and/or BET protein degradation targeting chimera, and a drug for the treatment of related diseases regulated by the AR and BET.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00962; 002898-002900, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
ALKOXYBENZO-FIVE-MEMBERED (SIX-MEMBERED) HETEROCYCLIC AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF
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Paragraph 0127-0128, (2020/12/22)
The invention relates to alkoxybenzeno five- or six-member heterocyclic amines compounds as scheme I , in which the R1, R2 and R3 are consistent with the detailed description in the patent claim. The compounds can act as selective sphingomyelin synthase 2 (SMS2) inhibitors to treat diseases caused by abnormal increasing of sphingomyelin (SM). This invention also includes compounds as scheme I , including pharmaceutically acceptable salts, pharmaceutical compositions as the active ingredients, and their application in drugs which can prevent and cure diseases caused by abnormal increasing of SM. These diseases caused by abnormal increasing of SM include atherosclerosis, type II diabetes, fatty liver, obesity, metabolic syndromes, enteritis and other inflammatory diseases.
PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
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Page/Page column 93, (2018/04/27)
Piperidine compounds of the Formular: (I) and pharmaceutically acceptable salts thereof, wherein X, Y, R 1, R 2, R 3, L, R 4, L 1, Q and R 5 are as defined herein. The compounds and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
PIPERIDINE DERIVATIVES AND COMPOSITIONS FOR THE INHIBITION OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT)
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Page/Page column 126; 127, (2013/02/27)
The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: Formula (I)
Design and synthesis of novel sulfonamide-containing bradykinin hB 2 receptor antagonists. Synthesis and structure-relationships of α,α-tetrahydropyranylglycine
Fincham, Christopher I.,Bressan, Alessandro,D'Andrea, Piero,Ettorre, Alessandro,Giuliani, Sandro,Mauro, Sandro,Meini, Stefania,Paris, Marielle,Quartara, Laura,Rossi, Cristina,Squarcia, Antonella,Valenti, Claudio,Daniela, Fattori,Maggi, Carlo Alberto
supporting information; experimental part, p. 2091 - 2100 (2012/05/05)
A series of α,α-cycloalkylglycine sulfonamide compounds of general formula 1 has previously been identified by our group as selective human B2(hB2) receptor antagonists. Here we report the in vitro and in vivo BK antagonist activity
AMINO - PYRIMIDINE COMPOUNDS AS INHIBITORS OF TBK1 AND/OR IKK EPSILON
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Page/Page column 129; 131, (2011/05/05)
The invention relates to certain aminopyrimidine compounds which inhibit TBK1 and/or IKK epsilon and which may therefore find application in treating inflammation, cancer, septic shock and/or Primary open Angle Glaucoma (POAG).
COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
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Page/Page column 43-44, (2009/10/18)
The invention provides compounds of Formula (I): pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
NEW PHENYLSULFAMOYL BENZAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS
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Page/Page column 25, (2008/12/05)
The present invention relates to new sulfonamide derivatives of formula (I), wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
NEW SULFONAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS
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Page/Page column 28, (2008/12/05)
The present invention relates to new sulfonamide derivatives of formula (I), wherein R1 -R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
