Novel Compounds with Aryl Linkers as Glucagon Receptor Agonists for Treating Type 2 Diabetes Mellitus and Obesity [0.03%]
新型联芳链GLP-1受体激动剂及其在治疗二型糖尿病和肥胖症中的应用
Ram W Sabnis
Ram W Sabnis
Provided herein are novel compounds with aryl linkers as glucagon receptor agonists, pharmaceutical compositions, use of such compounds in treating type 2 diabetes mellitus and obesity, and processes for preparing such compounds. ...
The Great Potential of the Cluster of Differentiation 38 (CD38) Inhibitors in the Treatment of Cancer and Age-Related Metabolic dysfunction [0.03%]
分化抗原簇38（CD38）抑制剂在癌症和与年龄相关的代谢功能障碍治疗中的巨大潜力
Ahmed F Abdel-Magid
Ahmed F Abdel-Magid
The invention in this patent application relates to heterobicyclic amide derivatives represented herein generally by formula 1. These compounds are inhibitors of CD38 and may be useful in the treatment of cancer and other diseases. ...
Discovery of CTX-439: A Potent and Selective CDK12 Inhibitor as a Prospective Anti-Cancer Drug [0.03%]
CTX-439的发现：一种有潜力和高度选择性的CDK12抑制剂及前景广阔的抗肿瘤药物
Kenichiro Shimokawa,Koji Ono,Moriteru Asano et al.
Kenichiro Shimokawa et al.
Cyclin-dependent kinase 12 (CDK12) is a transcription-associated kinase critical in regulating transcription, mRNA splicing, translation, cell cycle progression, and DNA damage repair (DDR) pathways. CDK12 is a notable therapeutic target in...
Paul K Spearing,Vaishali Satpute Janke,Ian M Romaine et al.
Paul K Spearing et al.
Potentiators of the Kv3.1 voltage-gated potassium channel may have utility as therapies for certain CNS disorders. A SAR survey around a previously reported Kv3.1 activator scaffold led to the identification of compounds with superior poten...
Identification of Clofibric Acid as a Synoviolin (SYVN1) Ligand for Proteolysis-Targeting Chimera (PROTAC) Development [0.03%]
一种SYVN1配体氯贝酸的鉴定及其在靶向蛋白降解剂中的应用研究
Julia Warren,Anandarao Munakala,Keith D Zientek et al.
Julia Warren et al.
Targeted protein degradation (TPD) via proteolysis-targeting chimeras (PROTACs) is a powerful therapeutic strategy, yet only a small fraction of the >600 human E3 ligases have been harnessed. To expand this repertoire, we developed clickabl...
Probe and Assay Dependent Pharmacology of Dantrolene Analogues at the GPR35 [0.03%]
丹曲林类似物在GPR35上的药物动力学及其检测方法依赖性
Yaopeng Zhao,Jingmin Cui,Hui Wen et al.
Yaopeng Zhao et al.
The G-protein-coupled receptor 35 (GPR35) plays a key role in various physiological and pathological processes and has emerged as a potential therapeutic target for the treatment of pain, inflammation, and metabolic diseases. Herein, we rep...
Novel Compounds as Plasma Kallikrein Inhibitors for Treating Hereditary Angioedema, Diabetic Macular Edema, and Diabetic Retinopathy [0.03%]
用于治疗遗传性血管水肿、糖尿病黄斑水肿和糖尿病视网膜病的新型血浆激肽释放酶抑制剂化合物
Ram W Sabnis
Ram W Sabnis
Provided herein are novel compounds as plasma kallikrein inhibitors, pharmaceutical compositions, use of such compounds in treating hereditary angioedema, diabetic macular edema, and diabetic retinopathy, and processes for preparing such co...
Novel Compounds as SARS-CoV‑2 Main Protease Inhibitors for Treating Viral Infections, in particular, Coronavirus Infections [0.03%]
作为冠状病毒感染治疗的新化合物SARS-CoV-主蛋白酶抑制剂的开发研究
Ram W Sabnis
Ram W Sabnis
Provided herein are novel compounds as main protease inhibitors, pharmaceutical compositions, use of such compounds in treating viral infections, in particular, coronavirus infections, and processes for preparing such compounds. ...
Design and Optimization of Benzoic Acid Inhibitors Targeting the EBNA1 DNA-Binding Interface [0.03%]
靶向EBNA1-DNA结合界面的水杨酸抑制剂的设计与优化
Garry R Smith,Mark E McDonnell,Yan Zhang et al.
Garry R Smith et al.
Epstein-Barr nuclear antigen 1 (EBNA1) is an essential viral DNA-binding protein required for maintenance of Epstein-Barr virus (EBV) episomes and is expressed in all EBV-associated malignancies, making it an attractive therapeutic target. ...
Jian Rong,Steven H Liang
Jian Rong
This patent discloses carboxamides as novel somatostatin receptor 4 (SSTR4) agonists, and they are potential treatments for SSTR4-related diseases. It provides details on the synthesis of carboxamides, pharmaceutical compositions, and the u...