65202-50-8Relevant articles and documents
-
Hill,Krause
, p. 1642 (1964)
-
METHODS OF MANUFACTURING A BIFUNCTIONAL COMPOUND, ULTRAPURE FORMS OF THE BIFUNCTIONAL COMPOUND, AND DOSAGE FORMS COMPRISING THE SAME
-
, (2021/11/20)
The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A: The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
Development of a Scalable Synthesis of the Small Molecule TGFβR1 Inhibitor BMS-986260
Vetrichelvan, Muthalagu,Rakshit, Souvik,Chandrasekaran, Sathishkumar,Chinnakalai, Karthikeyan,Darne, Chetan Padmakar,Doddalingappa, Dyamanna,Gopikumar, Indasi,Gupta, Anuradha,Gupta, Arun Kumar,Karmakar, Ananta,Lakshminarasimhan, Thirumalai,Leahy, David K.,Palani, Senthil,Radhakrishnan, Vignesh,Rampulla, Richard,Savarimuthu, Antony,Subramanian, Varadharajan,Velaparthi, Upender,Warrier, Jayakumar,Eastgate, Martin D.,Borzilleri, Robert M.,Mathur, Arvind,Vaidyanathan, Rajappa
, p. 1310 - 1320 (2020/07/24)
A scalable route to the small molecule TGFβR1 inhibitor BMS-986260 (1) was developed. This alternative approach circumvented the purification of intermediates by column chromatography and provided access to multikilogram quantities of the key intermediate
