147081-29-6Relevant articles and documents
TRICYCLIC INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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Paragraph 00293; 00351, (2019/07/13)
The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
Development of an Efficient Manufacturing Process for Reversible Bruton's Tyrosine Kinase Inhibitor GDC-0853
Zhang, Haiming,Cravillion, Theresa,Lim, Ngiap-Kie,Tian, Qingping,Beaudry, Danial,Defreese, Jessica L.,Fettes, Alec,James, Philippe,Linder, David,Malhotra, Sushant,Han, Chong,Angelaud, Remy,Gosselin, Francis
, p. 978 - 990 (2018/07/15)
Efforts toward the process development of reversible Bruton's tyrosine kinase (BTK) inhibitor GDC-0853 (1) are described. A practical synthesis of GDC-0853 was accomplished via a key highly regioselective Pd-catalyzed C-N coupling of tricyclic lactam 5 with 2,4-dichloronicotinaldehyde (6) to afford the C-N coupling product 3, a Suzuki-Miyaura cross-coupling of intermediate 3 with boronic ester 4 derived from a Pd-catalyzed borylation of tetracyclic bromide 7, to generate penultimate aldehyde intermediate 2 and subsequent aldehyde reduction and recrystallization. Process development of starting materials 5, 6, and 7 is also discussed.
CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF
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Paragraph 1665; 1666, (2016/02/21)
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
