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1. WO2020023438 - PROCESS FOR THE PREPARATION OF BROMODOMAIN INHIBITOR

Publication Number WO/2020/023438
Publication Date 30.01.2020
International Application No. PCT/US2019/042914
International Filing Date 23.07.2019
IPC
C07D 217/24 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
217Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
22with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
24Oxygen atoms
CPC
C07D 217/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
217Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
22with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
24Oxygen atoms
Applicants
  • CELGENE QUANTICEL RESEARCH, INC. [US]/[US]
Inventors
  • TRAVERSE, John Fitzgerald
  • YONG, Kelvin Hin-Yeong
  • FERRETTI, Antonio Christian
  • ALITE, Hekla
  • MOSELEY, Jonathan
  • RUDA, Antonio Maria
  • PRIMER, David
  • PHILP, Steven
Agents
  • SIMKIN, Michele
  • AGARWAL, Pavan K.
  • BECK, George
  • BERKOWITZ, Benjamin
  • BRINCKERHOFF, Courtenay C.
  • KAMINSKI, Michael D.
  • LAW, Glenn
  • MAEBIUS, Stephen
  • QUILLIN, George E.
  • RAWLINS, Andrew E.
  • SCHORR, Kristel
Priority Data
62/702,08523.07.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF BROMODOMAIN INHIBITOR
(FR) MÉTHODE DE PRÉPARATION D'UN INHIBITEUR DE BROMODOMAINE
Abstract
(EN)
The present invention provides processes of synthesis and purification of a bromodomain inhibitor, Compound 1, which compound includes crystalline forms, amorphous forms, solvates, and hydrates thereof. Embodiments of the disclosure relate to chemical synthesis routes of Compound 1 that provide a scalable method that results in highly pure final product. A further embodiment relates to methods to isolate the most stable polymorph of Compound 1 by crystallization from formic acid and water.
(FR)
La présente invention concerne des méthodes de synthèse et de purification d'un inhibiteur de bromodomaine, le composé 1, ce composé comprenant des formes cristallines, des formes amorphes, des solvates et des hydrates de celles-ci. Des modes de réalisation de l'invention concernent des voies de synthèse chimique du composé 1 qui fournissent une méthode évolutive permettabt d'obtenir un produit final très pur. Un autre mode de réalisation concerne des méthodes pour isoler le polymorphe le plus stable du composé 1 par cristallisation à partir d'acide formique et d'eau.
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