Yan Xia
Merck & Co.
16 Papers
162 Citations
Yan Xia is an academic researcher from Merck & Co.. The author has contributed to research in topics: Himbacine & Vorapaxar. The author has an hindex of 10, co-authored 16 publications.
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Papers
Discovery of MK-8831, A Novel Spiro-Proline Macrocycle as a Pan-Genotypic HCV-NS3/4a Protease Inhibitor.
Santhosh Neelamkavil,Sony Agrawal,Thomas Bara,Chad Bennett,Sathesh Bhat,Dipshikha Biswas,Linda Brockunier,Nicole Buist,Duane Burnette,Mark Cartwright,Samuel Chackalamannil,Robert Chase,Mariappan V. Chelliah,Austin Chen,Martin C. Clasby,Vincent J. Colandrea,Ian W. Davies,Keith Eagen,Zhuyan Guo,Yongxin Han,John A. Howe,Charles Lee Jayne,Josien Hubert B,Stacia Kargman,Karen Marcantonio,Shouwu Miao,Randy R. Miller,Andrew Nolting,Pinto Patrick A,Murali Rajagopalan,Rebecca T. Ruck,Shah Unmesh G,Aileen Soriano,Donald M. Sperbeck,Francisco Velazquez,Jin Wu,Yan Xia,Srikanth Venkatraman +37 more
TL;DR: The rational application of structural chemistry with molecular modeling guided the design and optimization of the structure-activity relationships have resulted in the identification of the clinical candidate MK-8831 with excellent pan-genotypic activity and safety profile.
31
Patent
Substituted bicyclic and tricyclic thrombin receptor antagonists
Mariappan V. Chelliah,Samuel Chackalamannil,Yan Xia +2 more
- 27 Jun 2007
TL;DR: Substituted bicyclic and tricyclic modified himbacine derivative of the formula (I) : or a pharmaceutically acceptable salt or solvate of said compound wherein (DU) represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, resten
25
Patent
Spirocyclic thrombin receptor antagonists
Samuel Chackalamannil,Mariappan V. Chelliah,Yan Xia +2 more
- 29 Mar 2006
TL;DR: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein An, En, Mn, Un, Gn, Jn, Kn, R9, R10, R11, R32, R33, B and Het are described and the remaining substitu
23
Patent
Bicyclic and tricyclic derivatives as thrombin receptor antagonists
Samuel Chackalamannil,Mariappan V. Chelliah,Yuguguang Wang,Yan Xia +3 more
- 02 Oct 2007
TL;DR: Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement.
22
Design and Synthesis of P2–P4 Macrocycles Containing a Unique Spirocyclic Proline: A New Class of HCV NS3/4A Inhibitors
Francisco Velazquez,Mariappan V. Chelliah,Martin C. Clasby,Zhuyan Guo,John A. Howe,Randy R. Miller,Santhosh Neelamkavil,Shah Unmesh G,Aileen Soriano,Yan Xia,Srikanth Venkatraman,Samuel Chackalamannil,Ian W. Davies +12 more
TL;DR: A new class of hepatitis C NS3/4A inhibitors was identified by introducing a novel spirocyclic proline-P2 surrogate onto the P2-P4 macrocyclic core of MK-5172 (grazoprevir), showing excellent pan-genotypic activity for most compounds.