145414-31-9Relevant articles and documents
SUBSTITUTED PHENYLPROPENYL PYRIDINE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL APPLICATIONS
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Paragraph 0436; 0438, (2021/12/29)
Disclosed are a substituted phenylpropenylpyridine derivative, a preparation method therefor and the use thereof as a PD-1/PD-L1 inhibitor. In particular, disclosed are a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method therefor and the use thereof. The definition of each group in the formula is detailed in the description and claims.
TRANSITION METAL COMPLEXES FOR ENANTIOSELECTIVE CATALYSIS OF CARBON-CARBON, CARBON-HETEROATOM, AND CARBON-HYDROGEN BOND FORMING REACTIONS
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Paragraph 00134; 00135, (2014/02/16)
In some embodiments, the present disclosure pertains to a compound, comprising a transition metal complex having the formula Φ-[Μ (x,y)-L1 (w,v)-L2 (t,u)-L3]p+An-mZ-p_m. In an embodiment of the present disclosure Φ may be A. In another embodiment Φ may be Δ. In some embodiments of the present disclosure, M is a transition metal. In a related embodiment, p is an integer corresponding to the oxidation state of M. In some embodiments of the present disclosure, each of x, y, w, v, t, and u independently comprise R. In other embodiments, each of x, y, w, v, t, and u independently comprise S. In an embodiment of the present disclosure, each of L1, L2, and L3 independently is a ligand comprising a substituted diamine. In some embodiments, An" comprises a lipophilic anion, where m is from 1 to 3, and where Z- comprises an optional second anion.
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1′-ligands to enhance backbone-binding interactions with protease: Synthesis, biological evaluation, and protein-ligand X-ray studies
Ghosh, Arun K.,Leshchenko-Yashchuk, Sofiya,Anderson, David D.,Baldridge, Abigail,Noetzel, Marcus,Miller, Heather B.,Tie, Yunfeng,Wang, Yuan-Fang,Koh, Yasuhiro,Weber, Irene T.,Mitsuya, Hiroaki
experimental part, p. 3902 - 3914 (2010/01/06)
Structure-based design, synthesis, and biological evaluation of a series of novel HIV-1 protease inhibitors are described. In an effort to enhance interactions with protease backbone atoms, we have incorporated stereochemically defined methyl-2-pyrrolidinone and methyl oxazolidinone as the P1′-ligands. These ligands are designed to interact with Gly-27′ carbonyl and Arg-8 side chain in the S1′-subsite of the HIV protease. We have investigated the potential of these ligands in combination with our previously developed bis-tetrahydrofuran (bis-THF) and cyclopentanyltetrahydrofuran (Cp-THF) as the P2-ligands. Inhibitor 19b with a (R)-aminomethyl-2-pyrrolidinone and a Cp-THF was shown to be the most potent compound. This inhibitor maintained near full potency against multi-PI-resistant clinical HIV-1 variants. A high resolution protein-ligand X-ray crystal structure of 19b-bound HIV-1 protease revealed that the P1′-pyrrolidinone heterocycle and the P2-Cp-ligand are involved in several critical interactions with the backbone atoms in the S1′ and S2 subsites of HIV-1 protease.
