1644575-06-3Relevant academic research and scientific papers
MACROCYCLIC INHIBITORS OF PEPTIDYLARGININE DEIMINASES
-
Page/Page column 259-260, (2021/11/06)
The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.
BIFUNCTIONAL DEGRADERS OF HEMATOPOIETIC PROGENITOR KINASE AND THERAPEUTIC USES THEREOF
-
Page/Page column 71-72, (2021/11/13)
The present disclosure provides bifunctional compounds as HPK1 degraders via ubiquitin proteosome pathway, and method for treating diseases modulated by HPK1.
Preparation method of long-chain aliphatic dicarboxylic acid mono-tert-butyl ester
-
Paragraph 0030-0033, (2021/07/09)
The invention provides a method for obtaining the long-chain aliphatic dicarboxylic acid mono-tert-butyl ester through monohydrolysis of the long-chain aliphatic dicarboxylic acid di-tert-butyl ester by controlling the reaction conditions of monohydrolysis; and the raw material cost is low, the yield is high, the post-treatment method is simple, and the method is suitable for industrial production.
BIFUNCTIONAL DEGRADERS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASES AND THERAPEUTIC USE THEREOF
-
Page/Page column 110-111, (2021/08/27)
The present disclosure provides bifunctional compounds as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4.
A Bioorthogonal Click Chemistry Toolbox for Targeted Synthesis of Branched and Well-Defined Protein–Protein Conjugates
Baalmann, Mathis,Bitsch, Sebastian,Deweid, Lukas,Ilkenhans, Nadja,Kolmar, Harald,Neises, Laura,Schneider, Hendrik,Werther, Philipp,Wilhelm, Jonas,Wolfring, Martin,Wombacher, Richard,Ziegler, Michael J.
supporting information, p. 12885 - 12893 (2020/06/02)
Bioorthogonal chemistry holds great potential to generate difficult-to-access protein–protein conjugate architectures. Current applications are hampered by challenging protein expression systems, slow conjugation chemistry, use of undesirable catalysts, or often do not result in quantitative product formation. Here we present a highly efficient technology for protein functionalization with commonly used bioorthogonal motifs for Diels–Alder cycloaddition with inverse electron demand (DAinv). With the aim of precisely generating branched protein chimeras, we systematically assessed the reactivity, stability and side product formation of various bioorthogonal chemistries directly at the protein level. We demonstrate the efficiency and versatility of our conjugation platform using different functional proteins and the therapeutic antibody trastuzumab. This technology enables fast and routine access to tailored and hitherto inaccessible protein chimeras useful for a variety of scientific disciplines. We expect our work to substantially enhance antibody applications such as immunodetection and protein toxin-based targeted cancer therapies.
Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)
Hu, Jiantao,Hu, Biao,Wang, Mingliang,Xu, Fuming,Miao, Bukeyan,Yang, Chao-Yie,Wang, Mi,Liu, Zhaomin,Hayes, Daniel F.,Chinnaswamy, Krishnapriya,Delproposto, James,Stuckey, Jeanne,Wang, Shaomeng
, p. 1420 - 1442 (2019/01/30)
The estrogen receptor (ER) is a validated target for the treatment of estrogen receptor-positive (ER+) breast cancer. Here, we describe the design, synthesis, and extensive structure-activity relationship (SAR) studies of small-molecule ERα degraders base
STILBENE DERIVATIVES FOR THE TREATMENT OF CNS AND OTHER DISORDERS
-
Paragraph 00148, (2018/12/03)
The present application discloses stilbene derivative compounds and compositions, and methods for treating ocular diseases, neurological disorders and protein aggregation-related disorders in patients using the compounds and compositions as disclosed herein.
STILBENE AND FUSED STILBENE DERIVATIVES AS SOLAR CELL DYES
-
Paragraph 0078, (2018/12/02)
The present application discloses stilbene derivative compounds and phenyl- benzofuran compositions, useful in the manufacture of dye-sensitized solar cells and other similar technology.
