610801-83-7Relevant academic research and scientific papers
SOLID STATE FORMS OF (2E)-N-HYDROXY-3-[3-(PHENYLSULFAMOYL)PHENYL]PROP-2-ENAMIDE AND PROCESS FOR PREPARATION THEREOF
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Page/Page column 15, (2018/03/06)
The Present invention relates to solid state forms of (2E)-N-hydroxy-3-[3-(N-phenyl sulfamoyl)phenyl]prop-2-enamide represented by the following structural formula-1 and process for the preparation thereof.
TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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Paragraph 0626, (2013/05/08)
The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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Page/Page column 239, (2011/11/01)
The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
Simple and efficient synthesis of belinostat
Yang, Lei,Xue, Xiaowen,Zhang, Yihua
experimental part, p. 2520 - 2524 (2010/09/14)
A novel synthesis of belinostat (1) starting from 3-nitrobenzaldehyde has been developed. The key step in this sequence involves the conversion of (2E)-3-(3-aminophenyl)acrylic acid methyl ester to (2E)-3-(3- chlorosulfonylphenyl)acrylic acid methyl ester via diazotization and sulfonylation. Taylor & Francis Group, LLC.
CDK INHIBITORS CONTAINING A ZINC BINDING MOIETY
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, (2009/04/25)
The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.
Novel sulfonamide derivatives as inhibitors of histone deacetylase
Finn, Paul W.,Bandara, Morwena,Butcher, Chris,Finn, Angela,Hollinshead, Ruth,Khan, Nagma,Law, Norman,Murthy, Sreenivasa,Romero, Rosario,Watkins, Clare,Andrianov, Victor,Bokaldere, Rasma M.,Dikovska, Klara,Gailite, Vija,Loza, Einars,Piskunova, Irina,Starchenkov, Igor,Vorona, Maxim,Kalvinsh, Ivars
, p. 1630 - 1657 (2007/10/03)
Inhibition of the enzyme histone deacetylase (HDAC) is emerging as a novel approach to the treatment of cancer. A series of novel sulfonamide derivatives were synthesized and evaluated for their ability to inhibit human HDAC. Compounds were identified which are potent enzyme inhibitors, with IC 50 values in the low nanomolar range against enzyme obtained from HeLa cell extracts, and with antiproliferative effects in cell culture. Extensive characterization of the structure - activity relationships of this series identified key requirements for activity. These include the direction of the sulfonamide bond and substitution patterns on the central phenyl ring. The alkyl spacer between the aromatic head group and the sulfonamide functionality also influenced the HDAC inhibitory activity. One of these compounds, m11.1, also designated PXD101, has entered clinical trials for solid tumors and haematological malignancies.
Carbamic acid compounds comprising a sulfonamide linkage as hdac inhibitors
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, (2008/06/13)
This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S (═O)2NR1— and —NR1S(═O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(═O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
