15570-42-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of HDAC degraders with CRBN E3 ligase ligands
Li, Jia,Lu, Wei,Lu, Yingxin,Shao, Yingying,Su, Mingbo,Sun, Danwen,Xiao, Donghuai,Zhou, Yubo,Zhu, Shulei
, (2021/12/02)
Histone deacetylases (HDACs) play important roles in cell growth, cell differentiation, cell apoptosis, and many other cellular processes. The inhibition of different classes of HDACs has been shown to be closely related to the therapy of cancers and other diseases. In this study, a series of novel CRBN-recruiting HDAC PROTACs were designed and synthesized by linking hydroxamic acid and benzamide with lenalidomide, pomalidomide, and CC-220 through linkers of different lengths and types. One of these PROTACs, denoted 21a, with a new benzyl alcohol linker, exhibited comparably excellent HDAC inhibition activity on different HDAC classes, acceptable degradative activity, and even better in vitro anti-proliferative activities on the MM.1S cell line compared with SAHA. Moreover, we report for the first time the benzyl alcohol linker, which could also offer the potential to be used to develop more types of potent PROTACs for targeting more proteins of interest (POI).
HDAC DEGRADER
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Page/Page column 37-38; 46, (2021/07/31)
The disclosure provides compounds of formula (I). The compounds may be used to degrade the Histone Deacetylase (HDAC) family of enzymes, particularly HDAC1, 2 and 3 that exist in corepressor complexes. Accordingly, the compounds may
DEGRADABLE HYALURONIC ACID HYDROGELS
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Page/Page column 271-272, (2020/05/13)
The present invention relates to conjugates comprising crosslinked hyaluronic acid to which a plurality of drug moieties are covalently and reversibly conjugated, wherein the hyaluronic acid exhibits a certain degree of modification and comprises degradable crosslinked moieties. It also relates to their use as medicaments and their use in the diagnosis, prevention and treatment of diseases.
GLUCOSAMINE DERIVATIVES AND PHARMACEUTICAL USES THEREOF
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Paragraph 0206, (2019/07/03)
There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a mammal of joint and bone disorders such as arthritis and osteoporosis.
HYDROGEL CROSS-LINKED HYALURONIC ACID PRODRUG COMPOSITIONS AND METHODS
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Paragraph 510; 511, (2018/10/19)
The present invention relates to hydrogel prodrug compositions comprising cross-linked hyaluronic acid (HA), or a derivative or a salt thereof, wherein the cross-linker system comprises a biodegradable spacer, wherein the cross-linked HA comprises a conjugated drug-linker, and wherein the linker is capable of releasing the drug under physiological conditions. The present invention further relates to methods for preparing the hydrogel prodrug compositions. The present invention further relates to methods for treating an ocular condition using the hydrogel compositions.
PREVENTION AND TREATMENT OF OCULAR CONDITIONS
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Paragraph 0907-0908, (2017/08/01)
The present invention relates to pharmaceutical compositions comprising hydrogel-linked prodrug for use in the treatment, prevention and/or diagnosis a condition of the eye and ophthalmic devices comprising said pharmaceutical compositions.
VEGF NEUTRALIZING PRODRUGS FOR THE TREATMENT OF OCULAR CONDITIONS
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Page/Page column 114; 115, (2014/05/07)
The present invention relates to a pharmaceutical composition comprising one or more pharmaceutically acceptable excipient(s) and a VEGF neutralizing prodrug, which comprises a VEGF neutralizing biologically active moiety, for use in a method for the treatment of one or more ocular conditions.
Esterification of dicarboxylic acids with benzyl alcohol under the action of the microwave radiation
Aver'yanov,Batrakova,Samuilov,Spiridonova,Kochnev,Galibeev,Gnezdilov
experimental part, p. 1920 - 1923 (2009/02/08)
Reaction of dicarboxylic acid with benzyl alcohol under the microwave irradiation proceeds faster as compared to the thermal conditions. The main reaction products are alkyl dicarboxylates, and the monoester and dibenzyl ether are formed as the side products. A proposal about the nature of the nonthermal effect in the reactions stimulated by the microwave irradiation is considered.
SELECTIVE MONOETHERIFICATION AND MONOESTERIFICATION OF DIOLS AND DIACIDS UNDER PHASE-TRANSFER CONDITIONS
Zerda, Jaime de la,Barak, Gabriela,Sasson, Yoel
, p. 1533 - 1536 (2007/10/02)
Research on the selectivity of etherification reactions of diols and esterification reactions of diacids by alkyl halides under phase-transfer catalysis has shown that under such conditions, selectivity of monoetherification increases in the order prim sec tert diols, though overall yield of monoether decreases from sec to tert diols.Monoesterification of diacids was accomplished with a high degree of selectivity.Optimal extraction of diols and diacids was found to correspond in general to chain lengths of around 5 carbons.This could mean that the complex formed between the catalyst and the anion to react is stabilized for certain carbon lengths by inner solvation in virtue of its spatial conformation.
