515824-43-8Relevant articles and documents
INHIBITORS OF CYCLIN-DEPENDENT KINASES
-
Paragraph 00220, (2021/02/12)
Provided herein are compounds which are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
Small molecule inhibitors of leucine-rich repetitive kinase 2 and their applications
-
Paragraph 0078-0082, (2022/01/07)
The present invention provides a small molecule inhibitor of leucine-rich repetitive kinase 2 and applications thereof; compounds as small molecule inhibitors such as compounds shown in formula I of the present invention or isotopic forms thereof, stereoisomers, tautomers, pharmaceutically acceptable salts, pharmaceutically acceptable solvates, hydrates, prodrugs and polymorphs. The compound has a high LRRK2 inhibitory activity and has high application value in the preparation of drugs for the treatment of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease and other diseases.
PHARMACEUTICAL COMPOSITION COMPRISING COMPOUND CAPABLE OF PENETRATING BLOOD-BRAIN BARRIER AS EFFECTIVE INGREDIENT FOR PREVENTING OR TREATING BRAIN CANCER
-
Paragraph 0088, (2020/01/22)
Disclosed is a pharmaceutical composition for the prevention or treatment of brain cancer, containing a compound capable of penetrating the blood-brain barrier as an active ingredient, the pharmaceutical composition for the prevention or treatment of brain cancer is capable of efficiently penetrating the blood-brain barrier of the brain to thereby effectively inhibit LRRK2 protein expression, and is thus useful in the prevention or treatment of brain cancer.
Synthesis and Preliminary Evaluation of [11C]GNE-1023 as a Potent PET Probe for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2) in Parkinson's Disease
Chen, Zhen,Shao, Tuo,Gao, Wei,Fu, Hualong,Collier, Thomas Lee,Rong, Jian,Deng, Xiaoyun,Yu, Qingzhen,Zhang, Xiaofei,Davenport, April T.,Daunais, James B.,Wey, Hsiao-Ying,Shao, Yihan,Josephson, Lee,Qiu, Wen-Wei,Liang, Steven
, p. 1580 - 1585 (2019/08/30)
Leucine-rich repeat kinase 2 (LRRK2) is a large protein involved in the pathogenesis of Parkinson's disease (PD). It has been demonstrated that PD is mainly conferred by LRRK2 mutations that bring about increased kinase activity. As a consequence, selecti
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies
Liang, Xuewu,Zang, Jie,Li, Xiaoyang,Tang, Shuai,Huang, Min,Geng, Meiyu,Chou, C. James,Li, Chunpu,Cao, Yichun,Xu, Wenfang,Liu, Hong,Zhang, Yingjie
, p. 3898 - 3923 (2019/04/25)
Concurrent inhibition of Janus kinase (JAK) and histone deacetylase (HDAC) could potentially improve the efficacy of the HDAC inhibitors in the treatment of cancers and resolve the problem of HDAC inhibitor resistance in some tumors. Here, a novel series
2-polysubstituted aromatic ring-pyrimidine derivative and preparation and medical application
-
Paragraph 0159; 0371; 0372; 0373, (2017/05/20)
The invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative, an optical isomer of the derivative or a medically acceptable salt or solvate of the derivative, and application of the compound, the optical isomer of the derivative or the medically acceptable salt or solvate of the derivative in preparing antineoplastic medicine. According to the 2-polysubstituted aromatic ring-pyrimidine derivative, by adopting N-substituted pyridine-2-minopyrimidine as a lead compound obtained based on virtual screening of a structure, a series of brand new small molecule Chk1 inhibitors are designed and synthesized, and a Chk1 kinase inhibitory activity test of a molecular level is conducted on the compound. Experiments prove that the compound is a Chk1 inhibitor with a strong antitumous effect, Chk1 kinase inhibitory activity and a prospect, and new cancer treating medicine, and can be used for treating solid tumor or leukemia related with human or animal cell proliferation. The 2-polysubstituted aromatic ring-pyrimidine derivative has a structure shown in the general formula I.
Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (PET) imaging for LRRK2
-
Page/Page column 71, (2015/11/16)
A method for positron emission tomography (PET) imaging of LRRK2 in tissue of a subject, the method comprising: administering a compound of formula I, formula II or formula III, or a pharmaceutically acceptable salt thereof to the subject, wherein the com
PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
-
Page/Page column 36, (2013/11/19)
Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS FOR USE IN THE TREATMENT OF PARKINSON'S DISEASE
-
Page/Page column 43, (2013/11/19)
Compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease
AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
-
Page/Page column 40, (2013/06/27)
Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using t