专利号:WO-2023226658-A1 优先权日:2022-05-25 标题:Nitrogen-containing five-membered heterocyclic derivatives as checkpoint kinase 1 inhibitor and uses thereof 发明人:LIU HANLAN; MA JINGJING; HUANG YUNG-JEN; CAI ZHANG; WANG XIAOHUI; YAN ZHIYU; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; RUAN JUXIN 权利人:SPEROGENIX THERAPEUTICS LTD 摘要:The present disclosure relates generally to nitrogen-containing five-membered heterocyclic derivatives usefulness in treatment of conditions associated with Checkpoint kinase (CHK), particularly more specifically CHK-1 enzymes. Methods of use, compositions, and method of synthesis are also disclosed.
专利号:US-12428395-B2 优先权日:2019-08-01 标题 :Heterocyclic compounds as kinase inhibitor and uses thereof 发明人:PENDHARKAR DHANANJAY; RAMACHANDRAN SREEKANTH A; JADHAVAR PRADEEP S; PANPATIL DAYANAND; SAEED UZMA; KUMAR VIVEK; BIST DIPSHE 权利人:SPEROGENIX THERAPEUTICS LTD 摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed.
专利号:WO-2022162606-A1 优先权日:2021-01-30 标 题:Heterocyclic compounds as kinase inhibitor and uses thereof 发明人:YAN ZHIYU; WANG XIAOHUI; LIU HANLAN; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; PENDHARKAR DHANANJAY; JADHAVAR PRADEEP S; SAEED UZMA; KUMAR VIVEK 权利人:SPEROGENIX THERAPEUTICS LTD; INTEGRAL BIOSCIENCES PRIVATE LTD 摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (J), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes such as cancer, idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed. Formula (J)
1: Zhang J, Xiang F, Hu Y, Wang J, Wang T, Zhang Z, Zhang Q, Rong C. CHK1 inhibition by prexasertib sensitizes cisplatin-resistant malignant tumor cells via checkpoint abrogation and STAT1-driven PD-L1 upregulation. Int Immunopharmacol. 2026 Feb 15;171:116126. doi: 10.1016/j.intimp.2025.116126. Epub 2025 Dec 31. 44(5):115605. doi: 10.1016/j.celrep.2025.115605. Epub 2025 Apr 17. 150:114278. doi: 10.1016/j.intimp.2025.114278. Epub 2025 Feb 14. 13(21):1752. doi: 10.3390/cells13211752. 5: Giudice E, Huang TT, Nair JR, Zurcher G, McCoy A, Nousome D, Radke MR, Swisher EM, Lipkowitz S, Ibanez K, Donohue D, Malys T, Lee MJ, Redd B, Levy E, Rastogi S, Sato N, Trepel JB, Lee JM. The CHK1 inhibitor prexasertib in BRCA wild-type platinum-resistant recurrent high-grade serous ovarian carcinoma: a phase 2 trial. Nat Commun. 2024 Mar 30;15(1):2805. doi: 10.1038/s41467-024-47215-6.
合成参考文献
参考文献:10.1007/s10565-020-09552-2 摘要:Xia X. Drug efficacy and toxicity prediction: an innovative application of transcriptomic data. Cell Biology and Toxicology. 2020 Aug 11;36(6):591–602. doi: 10.1007/s10565-020-09552-2.