17429-02-6Relevant academic research and scientific papers
1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES AS BCL-2 INHIBITORS FOR THE TREATMENT OF NEOPLASTIC AND AUTOIMMUNE DISEASES
-
, (2021/07/02)
The present invention relates to lH-pyrrolo[2,3-b]pyridine derivatives and related compounds as BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 162 to 233; examples 1 to 8; table; compound examples cpd-1 to cpd-135; biological examples 1 to 4).
Application of Transaminases in a Disperse System for the Bioamination of Hydrophobic Substrates
Berglund, Per,Fiorati, Andrea,Humble, Maria S.,Tessaro, Davide
, (2020/02/04)
The challenging bioamination of hydrophobic substrates has been attained through the employment of a disperse system consisting of a combination of a low polarity solvent (e. g. isooctane or methyl-tert-butylether), a non-ionic surfactant and a minimal amount of water. In these conditions, amine transaminases (ATA) were shown to efficiently carry out the reductive amination of variously substituted cyclohexanones, providing good conversions often coupled with a superior stereoselectivity if compared with the corresponding chemical reductive amination. An array of synthetically useful 4-substituted aminocyclohexanes was consequentially synthesized through biocatalysis, analyzed and stereochemically characterized. (Figure presented.).
Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy
Riggs, Jennifer R.,Elsner, Jan,Cashion, Dan,Robinson, Dale,Tehrani, Lida,Nagy, Mark,Fultz, Kimberly E.,Krishna Narla, Rama,Peng, Xiaohui,Tran, Tam,Kulkarni, Ashutosh,Bahmanyar, Sogole,Condroski, Kevin,Pagarigan, Barbra,Fenalti, Gustavo,Lebrun, Laurie,Leftheris, Katerina,Zhu, Dan,Boylan, John F.
, p. 4401 - 4410 (2019/05/17)
Triple negative breast cancer (TNBC) is an aggressive disease with high relapse rates and few treatment options. Outlined in previous publications, we identified a series of potent, dual TTK/CLK2 inhibitors with strong efficacy in TNBC xenograft models. P
Bcl-2 INHIBITORS
-
, (2019/11/19)
Disclosed herein is a compound of Formula (I) for inhibiting Bcl-2 and treating disease associated with undesirable bcl-2 activity (Bcl-2 related diseases), a method of using the compounds disclosed herein for treating dysregulated apoptotic diseases including cancers and treating autoimmune disease, and a pharmaceutical composition comprising the same.
A vicarious, one-pot synthesis of benzo- and naphthofurans: Applications to the syntheses of stereumene B and paeoveitols
Rashid, Showkat,Bhat, Bilal A.,Mehta, Goverdhan
supporting information, p. 1122 - 1125 (2019/03/26)
An interesting albeit unexpected deviation during attempted Tanabe γ-lactone annulation on 4-hydroxycyclohexanones has led to a general, one-pot synthesis of benzofurans and naphtho[2,3–b]furans from readily assembled precursors. The utility of this adaptable methodology has been demonstrated through concise syntheses of natural products, stereumene B, paeoveitol D and (±)-paeoveitol.
PYRAZOLOPYRIMIDINE DERIVATIVES AS BTK INHIBITORS FOR THE TREATMENT OF CANCER
-
, (2017/05/02)
This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of t
COMPOUNDS USEFUL AS KINASE INHIBITORS
-
, (2017/07/14)
This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK).The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.
The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatment of Triple Negative Breast Cancer Initiated from a Phenotypic Screen
Riggs, Jennifer R.,Nagy, Mark,Elsner, Jan,Erdman, Paul,Cashion, Dan,Robinson, Dale,Harris, Roy,Huang, Dehua,Tehrani, Lida,Deyanat-Yazdi, Gordafaried,Narla, Rama Krishna,Peng, Xiaohui,Tran, Tam,Barnes, Leo,Miller, Terra,Katz, Jason,Tang, Yang,Chen, Ming,Moghaddam, Mehran F.,Bahmanyar, Sogole,Pagarigan, Barbra,Delker, Silvia,Lebrun, Laurie,Chamberlain, Philip P.,Calabrese, Andrew,Canan, Stacie S.,Leftheris, Katerina,Zhu, Dan,Boylan, John F.
, p. 8989 - 9002 (2017/11/14)
Triple negative breast cancer (TNBC) remains a serious unmet medical need with discouragingly high relapse rates. We report here the synthesis and structure-activity relationship (SAR) of a novel series of 2,4,5-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines with potent activity against TNBC tumor cell lines. These compounds were discovered from a TNBC phenotypic screen and possess a unique dual inhibition profile targeting TTK (mitotic exit) and CLK2 (mRNA splicing). Design and optimization, driven with a TNBC tumor cell assay, identified potent and selective compounds with favorable in vitro and in vivo activity profiles and good iv PK properties. This cell-based driven SAR produced compounds with strong single agent in vivo efficacy in multiple TNBC xenograft models without significant body weight loss. These data supported the nomination of CC-671 into IND-enabling studies as a single agent TNBC therapy.
Scalable, Electrochemical Oxidation of Unactivated C-H Bonds
Kawamata, Yu,Yan, Ming,Liu, Zhiqing,Bao, Deng-Hui,Chen, Jinshan,Starr, Jeremy T.,Baran, Phil S.
supporting information, p. 7448 - 7451 (2017/06/13)
A practical electrochemical oxidation of unactivated C-H bonds is presented. This reaction utilizes a simple redox mediator, quinuclidine, with inexpensive carbon and nickel electrodes to selectively functionalize "deep-seated" methylene and methine moieties. The process exhibits a broad scope and good functional group compatibility. The scalability, as illustrated by a 50 g scale oxidation of sclareolide, bodes well for immediate and widespread adoption.
Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection
-
, (2016/08/17)
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
