- Identification of 2-substituted pyrrolo[1,2-b]pyridazine derivatives as new PARP-1 inhibitors
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A library of new 2-substituted pyrrolo[1,2-b]pyridazine derivatives were rapidly assembled and identified as PARP inhibitors. Structure-activity relationship for this class of inhibitor resulted in the discovery of most potent compounds 15a and 15b that e
- Xiang, Hao-Yue,Chen, Jian-Yang,Huan, Xia-Juan,Chen, Yi,Gao, Zhao-bing,Ding, Jian,Miao, Ze-Hong,Yang, Chun-Hao
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supporting information
(2020/12/02)
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- Significant Discovery of Tetrahydrothieno[3,2-c]pyridine-2-carboxamide Analogs as Potent P2Y12 Receptor Antagonists
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A series of analogs containing tetrahydrothieno[3,2-c]pyridine-2-carboxamide as a building block with numerous alicyclic and aromatic amines were synthesized. All analogs were characterized by spectral analysis and evaluated for their in vitro antiplatelet activity. 4-Fluorophenyl amide derivatives (compounds 8–11) have been found to be most active in the series with respect to prasugrel and aspirin, a third generation antiplatelet agents (P2Y12 receptor antagonists). Docking study also manifested the admirable binding mode of in vitro active compounds 10 and 11 with the target protein. The results may provide a new perception for future pharmacophore with simple design strategy and avoid tedious synthesis of clopidogrel and prasugrel.
- Bhalekar, Sujit B.,Shelke, Sharad N.
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- Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors
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The nuclear protein poly(ADP-ribose) polymerases-1/2 (PARP-1/2) are involved in DNA repair damaged by endogenous or exogenous process. And PARP-1/2 inhibitors have been proved to be clinically efficacious for DNA repair deficient tumors in the past decade
- Chen, Xuxing,Huan, Xiajuan,Liu, Qiufeng,Wang, Yuqin,He, Qian,Tan, Cun,Chen, Yi,Ding, Jian,Xu, Yechun,Miao, Zehong,Yang, Chunhao
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supporting information
p. 389 - 403
(2018/01/17)
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- Substituted oxazolidinone compounds and method and use thereof
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The invention provides a substituted oxazolidinone compound represented by a formula (I) shown in specifications, or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof. The compound i
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Paragraph 0190; 0195; 0196
(2017/02/02)
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- A PROCESS FOR MAKING PRASUGREL
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The present invention relates to A compound of general Formula (A), and/or acid addition salts thereof, wherein R is a hydrogen atom or a nitrogen-protecting group or an alpha- cyclopropylcarbonyl-2-fluorobenzyl group and R1,R2 is independently a C1-C10 alkyl group, optionally having one or more carbons substituted by a hydroxy group, or R1,R2 together with the bridging nitrogen may form a ring comprising from 3 to 10 carbon atoms, optionally also comprising another nitrogen, oxygen or sulfur atom in the ring and/or a nitrogen-, oxygen-, or sulfur-comprising substituent on the ring, to a process of making and use in making prasugrel.
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Page/Page column 15; 1
(2011/10/05)
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- Inhibitors of farnesyl-protein transferase
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The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent
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