Publication number: 20220169609
Abstract: The present invention relates to carbazoles of general formula (I), and process for the preparation thereof: wherein ‘R1’ is H, C1-C6 alkyl, benzyl, or allyl; R2 is H, C1-C6 alkyl, cyclopropyl, phenyl, aryl, heteroaryl, or NO2; R3 is H, C1-C6 alkyl, cyclopropyl, phenyl aryl, heteroaryl, 4-methoxy phenyl, 4-ethyl phenyl, 2-methyl phenyl, or 2-Fluoro phenyl; R4 is H, benzoyl, —CO2Et, —CHO, Br, or —OMe; R5 is OH, OMOM, OMe, CN, or OTf; R6 is H, or O-alkyl; and R3-R4 is —CHNCH2CH2-. This invention also relates to the process for the preparation of carbazomycin A of Formula (1), calothrixin B of Formula (2) and staurosporinone of Formula (3) involving carbazoles of general formula (I) as an intermediate.
Type:
Application
Filed:
March 24, 2020
Publication date:
June 2, 2022
Inventors:
Srihari PABBARAJA, Goverdhan MEHTA, Ramesh SAMINENI, Shweta SINGH
Publication number: 20220169611
Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
Type:
Application
Filed:
February 15, 2022
Publication date:
June 2, 2022
Inventors:
Michael D. Bartberger, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Dequette, I, John Eksterowicz, Benjamin Fisher, Brian M. Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael W. Gribble, Darin J. Gustin, Julie A. Heath, Xin Huang, XianYun Jiao, Michael G. Johnson, Frank Kayser, David John Kopecky, SuJen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan D. Low, Brian S. Lucas, Zhihua Ma, Lawrence R. McGee, Josel McIntosh, Dustin L. McMinn, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yossup Rew, Philip M. Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
Publication number: 20220169631
Abstract: Provided herein are compounds of Formula (I?) or (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers (e.g., carcinoma); lung cancer, breast cancer, liver cancer, pancreatic cancer, gastric cancer, ovarian cancer, colon cancer, colorectal cancer)), metabolic disorders (e.g., diabetes), autoimmune diseases, and neurological diseases (e.g., Alzheimer's disease, gliosis, spinal cord injury)) in a subject, as well as for male contraception (e.g., reducing or inhibiting spermatogenesis, or reducing the rate of male fertility in a healthy fertile male subject). Provided are methods of inhibiting a CDK (e.g., CDK14, CDK15, CDK16, CDK17, CDK18) in a subject.
Type:
Application
Filed:
June 24, 2019
Publication date:
June 2, 2022
Applicant:
Dana-Farber Cancer Institute, Inc.
Inventors:
Nathanael S. Gray, Fleur M. Ferguson, Zainab M. Doctor