C07C65/105

THERAPY

The invention addresses radioresistance in cancer treatment involving radiotherapy and, in particular, limitations associated with the use of the drug sulfasalazine. Specifically, it provides a series of compounds for use as radiosensitizers in the treatment of cancers such as glioblastomas which are lethal and inherently resistant to radiotherapy. In one embodiment, the invention provides compounds of general formula (I), their stereoisomers and pharmaceutically acceptable salts for use as radiosensitizers in the treatment of cancer:

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wherein ring A is selected from optionally substituted phenyl, biphenyl and fluorenyl; each X is independently selected from: —C.sub.1-6 alkyl (preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), —O—C.sub.1-6 alkyl (preferably —O—C.sub.1-3 alkyl, e.g. —OCH.sub.3), —S—C.sub.1-6 alkyl (preferably —S—C.sub.1-3 alkyl, e.g. —SCH.sub.3), —OH, —SH, —CO.sub.2R.sup.1 (where R.sup.1 is H or C.sub.1-6 alkyl, preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), —SO.sub.2—C.sub.1-6 alkyl (preferably —SO.sub.2—C.sub.1-3 alkyl, e.g. —SO.sub.2—CH.sub.3), —SO.sub.2—NR.sup.2R.sup.3 (where R.sup.2 is H and R.sup.3 is optionally substituted phenyl), —NR.sup.4R.sup.5 (wherein R.sup.4 and R.sup.5 are independently selected from H, C.sub.1-6 alkyl (preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), and —CO—C.sub.1-6 alkyl (preferably —CO—C.sub.1-3 alkyl, e.g. —CO—CH.sub.3), halogen (e.g. F, Cl or Br), and optionally substituted tetrazolyl; n is an integer from 0 to 5, preferably 0 to 2, e.g. 1 or 2; and custom-character denotes an E or Z double bond.

Method for preparing 4,4′-dihydroxy-[1,1′-biphenyl-3,3′-dicarboxylic acid]

The present invention relates to a method for preparing 4,4′-dihydroxy-[1,1′-biphenyl-3,3′-dicarboxylic acid], the method comprising a step for preparing a compound represented by chemical formula 1 by reacting a compound represented by chemical formula 2 with a base according to reaction formula 1. [reaction formula 1] [chemical formula 1] [chemical formula 2] According to the present invention, because use of additional carbon dioxide is unnecessary during the reaction, internal pressure is lowered during same, the reaction can be carried out at a lower temperature, the yield from the synthesis is notably improved as hardening of the resulting substance is absent, and H.sub.4dobpdc can be synthesized in large amounts as an additional process for obtaining pure ligands is unnecessary.

Method for preparing 4,4′-dihydroxy-[1,1′-biphenyl-3,3′-dicarboxylic acid]

The present invention relates to a method for preparing 4,4′-dihydroxy-[1,1′-biphenyl-3,3′-dicarboxylic acid], the method comprising a step for preparing a compound represented by chemical formula 1 by reacting a compound represented by chemical formula 2 with a base according to reaction formula 1. [reaction formula 1] [chemical formula 1] [chemical formula 2] According to the present invention, because use of additional carbon dioxide is unnecessary during the reaction, internal pressure is lowered during same, the reaction can be carried out at a lower temperature, the yield from the synthesis is notably improved as hardening of the resulting substance is absent, and H.sub.4dobpdc can be synthesized in large amounts as an additional process for obtaining pure ligands is unnecessary.

Method for preparing 4,4′-dihydroxy-[1,1′-biphenyl-3,3′-dicarboxylic acid]

The present invention relates to a method for preparing 4,4′-dihydroxy-[1,1′-biphenyl-3,3′-dicarboxylic acid], the method comprising a step for preparing a compound represented by chemical formula 1 by reacting a compound represented by chemical formula 2 with a base according to reaction formula 1. [reaction formula 1] [chemical formula 1] [chemical formula 2] According to the present invention, because use of additional carbon dioxide is unnecessary during the reaction, internal pressure is lowered during same, the reaction can be carried out at a lower temperature, the yield from the synthesis is notably improved as hardening of the resulting substance is absent, and H.sub.4dobpdc can be synthesized in large amounts as an additional process for obtaining pure ligands is unnecessary.

Carboxylated polyphenol derivatives and their cosmetic use
11253455 · 2022-02-22 · ·

A subject matter of the present invention is the cosmetic use of at least one compound of formula (I): in which: (II) denotes a divalent radical chosen from a carbon-carbon single bond *—CH.sub.2—CH.sub.2—* or double bond *—CH═CH—*, of Z or E configuration or their mixtures, b=0 or 1, c=0 or 1, d=0, 1 or 2, and R and R′ independently denote a hydrogen atom, a linear C.sub.1-C.sub.6 alkyl radical or a branched C.sub.3-C.sub.6 alkyl radical, to treat and/or prevent signs of aging and/or of photoaging of keratinous substances, preferably of the skin, and/or to depigment, lighten and/or whiten keratinous substances, preferably the skin. The present invention also relates to novel compounds and to a corresponding cosmetic method. ##STR00001##

Carboxylated polyphenol derivatives and their cosmetic use
11253455 · 2022-02-22 · ·

A subject matter of the present invention is the cosmetic use of at least one compound of formula (I): in which: (II) denotes a divalent radical chosen from a carbon-carbon single bond *—CH.sub.2—CH.sub.2—* or double bond *—CH═CH—*, of Z or E configuration or their mixtures, b=0 or 1, c=0 or 1, d=0, 1 or 2, and R and R′ independently denote a hydrogen atom, a linear C.sub.1-C.sub.6 alkyl radical or a branched C.sub.3-C.sub.6 alkyl radical, to treat and/or prevent signs of aging and/or of photoaging of keratinous substances, preferably of the skin, and/or to depigment, lighten and/or whiten keratinous substances, preferably the skin. The present invention also relates to novel compounds and to a corresponding cosmetic method. ##STR00001##

SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX

Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.

SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX

Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.

Metal organic frameworks (MOFs) and methods of synthesizing and using the same

A new metal organic framework (MOF) series and method of synthesizing the same are disclosed which includes an organic linking ligand having the formula: ##STR00001##
and a metal ion bonded to the organic linking ligand.

PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES FOR THE SYNTHESIS OF ELTROMBOPAG OR SALT THEREOF

Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of Eltrombopag, passing through/using intermediate 5′-Chloro-2′-hydroxy[1,1′-biphenyl]-3-carboxylic acid alkaline metal salt of formula: wherein A is an alkaline metal.

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