158985-25-2Relevant articles and documents
Affinity-Based Selectivity Profiling of an In-Class Selective Competitive Inhibitor of Acyl Protein Thioesterase 2
Won, Sang Joon,Eschweiler, Joseph D.,Majmudar, Jaimeen D.,Chong, Fei San,Hwang, Sin Ye,Ruotolo, Brandon T.,Martin, Brent R.
, p. 215 - 220 (2017)
Activity-based protein profiling (ABPP) has revolutionized the discovery and optimization of active-site ligands across distinct enzyme families, providing a robust platform for in-class selectivity profiling. Nonetheless, this approach is less straightfo
TRUNCATED ITRACONAZOLE ANALOGUES AND METHODS OF USE THEREOF
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Paragraph 0147, (2021/02/19)
Disclosed herein are analogues of itraconazole that are potent hedgehog signaling pathway inhibitors. The compounds are expected to be useful in the treatment of cell proliferation disorders such as cancer, particularly cancers that are dependent upon the hedgehog signaling pathway such as basal cell carcinoma and medulloblastoma.
ADENOSINE A2A RECEPTOR ANTAGONISTS AND USES THEREOF
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Paragraph 00372, (2021/02/12)
Disclosed herein are compounds, compositions, and methods for modulating the A2A2A adenosine receptor with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders that are mediated by the A
ADENOSINE RECEPTOR BINDING COMPOUNDS
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Paragraph 00333, (2020/02/06)
The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
Truncated Itraconazole Analogues Exhibiting Potent Anti-Hedgehog Activity and Improved Drug-like Properties
Wen, Jiachen,Chennamadhavuni, Divya,Morel, Shana R.,Hadden, M. Kyle
, p. 1290 - 1295 (2019/09/30)
We conducted a structure-activity relationship study to explore simplified analogues of the itraconazole (ITZ) scaffold for their ability to inhibit the hedgehog (Hh) signaling pathway. These analogues were based on exploring the effects of chemical modifications to the linker and triazolone/side chain region of ITZ. Analogue 11 was identified as the most potent compound in our first generation, with an IC50 value of 81 nM in a murine Hh-dependent basal cell carcinoma. Metabolic identification studies led us to identify truncated piperazine (26) as the major metabolite in human liver microsomes (HLMs) and an improved Hh pathway inhibitor (IC50 = 22 nM). This work verifies that continued truncation of the ITZ scaffold is a practical method to maintain potent anti-Hh activity while also reducing the molecular weight for the ITZ scaffold and achieving improved pharmacokinetic properties.
Potent human glutaminyl cyclase inhibitors as potential anti-Alzheimer's agents: Structure-activity relationship study of Arg-mimetic region
Ngo, Van T.H.,Hoang, Van-Hai,Tran, Phuong-Thao,Ann, Jihyae,Cui, Minghua,Park, Gyungseo,Choi, Sun,Lee, Jiyoun,Kim, Hee,Ha, Hee-Jin,Choi, Kwanghyun,Kim, Young-Ho,Lee, Jeewoo
supporting information, p. 1035 - 1049 (2018/02/12)
Pyroglutamate-modified amyloid β peptides (pGlu-Aβ) are highly neurotoxic and promote the formation of amyloid plaques. The pGlu-Aβ peptides are generated by glutaminyl cyclase (QC), and recent clinical studies indicate that QC represents an alternative t
N/O-LINKED DEGRONS AND DEGRONIMERS FOR PROTEIN DEGRADATION
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Page/Page column 310; 311, (2019/01/10)
This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.
ANTIMYCOTIC TRIAZOLE COMPOUND
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Page/Page column 3; 12, (2017/07/08)
The invention relates to Compound (I), which is 4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)-N-(4-fluorophenyl)benzamide, or a pharmaceutically acceptable salt thereof, usefu
A process for the preparation of intermediates [...] and the intermediate
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Paragraph 0054; 0055; 0056, (2016/11/02)
The invention discloses a preparation method of a vilazodone intermediate and an intermediate. The preparation method of the vilazodone intermediate (5-piperazinylbenzofuran-2-formylimine salts) comprises a step of soaking a compound represented by the formula 7 in a water solution of an inorganic strong acid to carry out hydrolysis deprotection salt-forming reactions, which are represented in the description; wherein the X represents an inorganic strong acid, and the inorganic strong acid can be hydrochloric acid, sulfuric acid, or hydrobromic acid. The invention also discloses a preparation method of a compound represented by the formula 7 and a compound represented by the formula 6. The provided preparation method has the advantages of high yield, easy purification, high purity, and low cost, and is suitable for industrial massive production.
Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents
Yempalla, Kushalava Reddy,Munagala, Gurunadham,Singh, Samsher,Kour, Gurleen,Sharma, Shweta,Chib, Reena,Kumar, Sunil,Wazir, Priya,Singh,Raina, Sushil,Bharate, Sonali S,Khan, Inshad Ali,Vishwakarma, Ram A.,Singh, Parvinder Pal
supporting information, p. 1059 - 1064 (2015/10/20)
Novel polar functionalities containing 6-nitro-2,3-dihydroimidazooxazole (NHIO) analogues were synthesized to produce a compound with enhanced solubility. Polar functionalities including sulfonyl, uridyl, and thiouridyl-bearing NHIO analogues were synthes