The Effect of N-Alkyl Azole Difluorination on Molecular Properties Relevant for Compound Optimization: A Comparative Study [0.03%]
N-烷基唑二氟化对化合物优化相关分子属性影响的比较研究
Ryan M Herrick,Samantha A Green,Sharyl Rich et al.
Ryan M Herrick et al.
Despite recent interest in N-trifluoromethyl azoles, N-α,α-difluoroalkyl azoles [(azole)N-CF2R] remain understudied and underutilized in medicinal chemistry. To address this deficiency, we have conducted a comparative study of medicinally...
Discovery of Potent, Selective, and Brain-Penetrant Small Molecule CD38 Inhibitors [0.03%]
高效、选择性及可通过血脑屏障的小分子CD38抑制剂的发现
Andrew J Stott,Roland W Bürli,Kevin J Doyle et al.
Andrew J Stott et al.
Cluster of differentiation 38 (CD38) is a nicotinamide adenine dinucleotide (NAD+)-consuming ectoenzyme abundantly expressed in brain regions involved in motor control and cognition. Given the central role of NAD+ in maintaining neuronal he...
Ram W Sabnis
Ram W Sabnis
Provided herein are novel compounds as MALT1 inhibitors, pharmaceutical compositions, use of such compounds in treating cancer, and processes for preparing such compounds. ...
Novel Cyclopentapyrrole Compounds as Orexin Receptor Agonists for Treating Sleep Disorders, namely, Narcolepsy and Hypersomnia [0.03%]
新型环戊并吡咯衍生物作为食欲素受体激动剂用于治疗嗜睡症和过度睡眠症等睡眠障碍疾病及其制备方法
Ram W Sabnis
Ram W Sabnis
Provided herein are novel cyclopentapyrrole compounds as orexin receptor agonists, pharmaceutical compositions, use of such compounds in treating sleep disorders, namely, narcolepsy and hypersomnia, and processes for preparing such compound...
5,5'-Methylenedisalicylic Acid Derivatives as Inhibitors of the Protein Phosphatase CppA in Chlamydia trachomatis [0.03%]
曲霉中丝裂素活化蛋白激酶基因簇的鉴定及特性分析
Krishna Pandey,Olivia Slater,Gabrielle E Jeschke et al.
Krishna Pandey et al.
A structure-based designed library of new 5,5'-methylenedisalicylic acid (MDSA) derivatives were synthesized as a functional core and explored for their antibacterial activity against Chlamydia trachomatis. Various well-established reaction...
Allosteric Induction of Estrogen Receptor Ligand Binding Domain Tetramerization by a Distinct Complete Estrogen Receptor Antagonist [0.03%]
一种全新的雌激素受体拮抗剂通过别构诱导雌激素受体配体结合域寡聚化对抗雌激素信号通路
Emma C Fink,Reena Chawla,Govinda R Hancock et al.
Emma C Fink et al.
Complete estrogen receptor antagonists (CERANs) are effective against advanced estrogen receptor-positive (ER+) breast cancers, but current chemical scaffolds limit our ability to explore the full range of ER pharmacology. We report the syn...
From Solid-State Control to Predictive Precision: Building a Deployable Ecosystem for Psychedelic Therapeutics [0.03%]
从固态控制到预测精准：构建可部署的迷幻治疗生态系统
Anna C Renner,Robert B Kargbo
Anna C Renner
Two recent patent applications illustrate how psychedelic drug development is expanding beyond molecules and experiences toward deployable therapeutic systems. One focuses on solid-state optimization of a lysergamide analogue to ensure manu...
Targeting RAD51-BRCA2 Interaction to Enhance Synthetic Lethality with Olaparib in Pancreatic Cancer: Development of a Novel Phenyl Furan-Quinoline-Carboxylic Acid Series [0.03%]
靶向RAD51-BRCA2相互作用，增强Olaparib在胰腺癌中的合成致死性：开发新型苯并菲戎-喹啉-羧酸系列化合物
Giovanni Ferrandi,Greta Bagnolini,Laura Poppi et al.
Giovanni Ferrandi et al.
Synthetic lethality has proven to be a tactical paradigm to design synergistic anticancer drug combinations. In this context, we leveraged BRCA2 and PARP as a synthetic lethal target pair to consolidate the use of small molecule inhibitors ...
Novel Compounds as Glucagon-Like Peptide‑1 Receptor Agonists for Treating Diabetes [0.03%]
一类新的化合物作为治疗糖尿病的胰高血糖素样肽-1受体激动剂
Ram W Sabnis
Ram W Sabnis
Provided herein are novel compounds as glucagon-like peptide-1 receptor agonists, pharmaceutical compositions, use of such compounds in treating diabetes, and processes for preparing such compounds. ...
Novel Substituted Pyrazolo-Pyrimidine Compounds as PIKfyve Inhibitors for Treating Neurological Diseases [0.03%]
新型取代的吡唑并嘧啶化合物作为PIKfyve抑制剂用于治疗神经性疾病
Ram W Sabnis,Anika R Sabnis
Ram W Sabnis
Provided herein are novel substituted pyrazolo-pyrimidine compounds as PIKfyve inhibitors, pharmaceutical compositions, use of such compounds in treating neurological diseases, and processes for preparing such compounds. ...