63001-30-9Relevant articles and documents
METHODS OF MANUFACTURING A BIFUNCTIONAL COMPOUND, ULTRAPURE FORMS OF THE BIFUNCTIONAL COMPOUND, AND DOSAGE FORMS COMPRISING THE SAME
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, (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
Piperazine derivatives and their use as therapeutic agents
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Paragraph 0124, (2016/03/19)
Compounds for treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the compounds are of formula (I): where x y, W, V, R 2 , R 3 , R 4 , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , R 8a , R 9 and R 9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.