497159-95-2Relevant academic research and scientific papers
Synthesis and evaluation of cyclopentane-based muraymycin analogs targeting MraY
Kwak, Seung-Hwa,Lim, Won Young,Hao, Aili,Mashalidis, Ellene H.,Kwon, Do-Yeon,Jeong, Pyeonghwa,Kim, Mi Jung,Lee, Seok-Yong,Hong, Jiyong
, (2021/02/21)
Antibiotic resistance is one of the most challenging global health issues and presents an urgent need for the development of new antibiotics. In this regard, phospho-MurNAc-pentapeptide translocase (MraY), an essential enzyme in the early stages of peptid
INHIBITORS OF INTEGRATED STRESS RESPONSE PATHWAY
-
Paragraph 0503; 0506, (2020/09/09)
The present disclosure relates generally to therapeutic agents that may be useful as inhibitors of Integrated Stress Response (ISR) pathway.
PYRAZOLYL COMPOUNDS AND METHODS OF USE THEREOF
-
, (2020/05/14)
Compounds having activity as chemotherapeutic agents are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1a, R1b, R1c, R1d, L, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods for treating cancer (e.g., hematological cancers) are also provided.
IRAK DEGRADERS AND USES THEREOF
-
, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
Indoleamine 2, 3-dioxygenase inhibitor and use thereof
-
Paragraph 0164; 0166; 0170, (2018/03/25)
The invention belongs to the technical field of medical technology and relates to a compound shown in the formula I and its pharmaceutically acceptable salt, isomer and prodrug. In the formula, R1, R2, R3, X, m, n and a ring A are defined in the specifica
MACROCYCLIC INHIBITORS OF MYELOPEROXIDASE
-
, (2018/02/03)
The present invention provides compounds of Formula (I): wherein the substituents are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, and may be useful for for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
1,5-NAPHTHYRIDINE DERIVATIVE OR SALT THEREOF
-
Paragraph 0746-0747, (2014/05/20)
A 1,5-naphthyridine derivative represented by Formula [1] (in which R1, R2, R3, R4 and R5 represent a hydrogen atom, -L-Z (in which Z represents a non-aromatic heterocyclic group or the like; and L re
MACROCYCLIC UREA DERIVATIVES AS INHIBITORS OF TAFIA, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
-
Page/Page column 24, (2015/01/09)
The present invention relates to macrocydic urea derivatives of the formula I (I) in which R1, R2, R3, V and Y are as defined below. The compounds of the formula I are inhibitors of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor). The invention further relates to the process for the preparation of the compounds of formula I and to the use thereof as medicaments.
PYRROLOPYRAZINE KINASE INHIBITORS
-
Page/Page column 159, (2013/03/28)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
SUBSTITUTED BI-HETEROARYL COMPOUNDS AS CDK9 1NHIBITORS AND THEIR USES
-
, (2012/08/08)
The present invention provides a compound of formula (II) where R1 is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tan-tomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancersand other conditions described herein
