1260982-47-5Relevant academic research and scientific papers
7-HYDROXY-INDOLINYL ANTAGONISTS OF P2Y1 RECEPTOR
-
, (2014/02/16)
The present invention provides compounds of Formula (I): Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used medicaments.
Identification of 1-{2-[4-chloro-1′-(2,2-dimethylpropyl)-7-hydroxy-1, 2-dihydrospiro[indole-3,4′-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3] thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y1 antagonist as an antiplatelet agent
Jeon, Yoon T.,Yang, Wu,Qiao, Jennifer X.,Li, Ling,Ruel, Rejean,Thibeault, Carl,Hiebert, Sheldon,Wang, Tammy C.,Wang, Yufeng,Liu, Yajun,Clark, Charles G.,Wong, Henry S.,Zhu, Juliang,Wu, Dauh-Rurng,Sun, Dawn,Chen, Bang-Chi,Mathur, Arvind,Chacko, Silvi A.,Malley, Mary,Chen, Xue-Qing,Shen, Hong,Huang, Christine S.,Schumacher, William A.,Bostwick, Jeffrey S.,Stewart, Anne B.,Price, Laura A.,Hua, Ji,Li, Danshi,Levesque, Paul C.,Seiffert, Dietmar A.,Rehfuss, Robert,Wexler, Ruth R.,Lam, Patrick Y.S.
, p. 1294 - 1298 (2014/03/21)
Spiropiperidine indoline-substituted diaryl ureas had been identified as antagonists of the P2Y1 receptor. Enhancements in potency were realized through the introduction of a 7-hydroxyl substitution on the spiropiperidinylindoline chemotype. SAR studies were conducted to improve PK and potency, resulting in the identification of compound 3e, a potent, orally bioavailable P2Y1 antagonist with a suitable PK profile in preclinical species. Compound 3e demonstrated a robust antithrombotic effect in vivo and improved bleeding risk profile compared to the P2Y12 antagonist clopidogrel in rat efficacy/bleeding models.
7-HYDROXY-SPIROPIPIPERIDINE INDOLINYL ANTAGONISTS OF P2Y1 RECEPTOR
-
Paragraph 00151; 00157, (2014/02/16)
The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of Ρ2Y1 receptor and may be used as medicaments in the treatment and/or prophylaxis of thromboembolic disorders.
