Santhosh Francis Neelamkavil
Schering-Plough
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Publication
Featured researches published by Santhosh Francis Neelamkavil.
ACS Medicinal Chemistry Letters | 2016
Santhosh Francis Neelamkavil; Sony Agrawal; Thomas Bara; Chad E. 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; Hubert Josien; Stacia Kargman; Karen Marcantonio; Shouwu Miao; Randy R. Miller; Andrew Nolting; Patrick A. Pinto; Murali Rajagopalan
We have been focused on identifying a structurally different next generation inhibitor to MK-5172 (our Ns3/4a protease inhibitor currently under regulatory review), which would achieve superior pangenotypic activity with acceptable safety and pharmacokinetic profile. These efforts have led to the discovery of a novel class of HCV NS3/4a protease inhibitors containing a unique spirocyclic-proline structural motif. The design strategy involved a molecular-modeling based approach, and the optimization efforts on the series to obtain pan-genotypic coverage with good exposures on oral dosing. One of the key elements in this effort was the spirocyclization of the P2 quinoline group, which rigidified and constrained the binding conformation to provide a novel core. A second focus of the team was also to improve the activity against genotype 3a and the key mutant variants of genotype 1b. 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.
Bioorganic & Medicinal Chemistry Letters | 2009
Santhosh Francis Neelamkavil; Craig D. Boyle; Samuel Chackalamannil; William J. Greenlee; Lili Zhang; Giuseppe Terracina
Discovery of a series of azepine sulfonamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) is described. SAR studies at the 4-position of the azepane ring have resulted in the discovery of a very potent compound 30 which has an 11beta-HSD1 IC(50) of 3.0nM.
Archive | 2009
Santhosh Francis Neelamkavil; Craig D. Boyle; Joel M. Harris; Andrew Stamford; Jinsong Hao; Bernardt R. Neustadt; Samuel Chackalamannil; Yan Xia; William J. Greenlee
Archive | 2010
Santhosh Francis Neelamkavil; Bernard R. Neustadt; Andrew Stamford; Yan Xia; Joel M. Harris; Craig D. Boyle; Samuel Chackalamannil; Dipshikha Biswas; Hong Liu; Jinsong Hao; Claire M. Lankin; Unmesh G. Shah
Archive | 2010
Santhosh Francis Neelamkavil; Dipshikha Biswas; Samuel Chackalamannil; Bernard R. Neustadt; Andrew Stamford; Hong Liu
Archive | 2008
Santhosh Francis Neelamkavil; Craig D. Boyle; Samuel Chackalamannil
ACS Medicinal Chemistry Letters | 2016
Francisco Velazquez; Mariappan V. Chelliah; Martin C. Clasby; Zhuyan Guo; John A. Howe; Randy R. Miller; Santhosh Francis Neelamkavil; Unmesh G. Shah; Aileen Soriano; Yan Xia; Srikanth Venkatraman; Samuel Chackalamannil; Ian W. Davies
Archive | 2010
Santhosh Francis Neelamkavil; Andrew Stamford; Samuel Chackalamannil; William J. Greenlee
Archive | 2013
Jared N. Cumming; Jack D. Scott; Andrew Stamford; Ulrich Iserloh; Santhosh Francis Neelamkavil; Pengcheng Patrick Shao; Jonathan E. Wilson
Archive | 2013
Yan Xia; シア ヤン; Craig D. Boyle; ディー. ボイル クレイグ; William J. Greenlee; ジェイ. グリーンリー ウィリアム; Samuel Chackalamannil; チャッカラマニル サミュエル; Charles Lee Jayne; リー ジェイン チャールズ; Andrew Stamford; ダブリュー. スタンフォード アンドリュー; Xing Dai; シン ダイ; Joel M. Harris; エム. ハリス ジョエル; Bernard R. Neustadt; アール. ニュースタット ベルナルド; Santhosh Francis Neelamkavil; フランシス ニーラムカビル サンソーシュ; Unmesh G. Shah; ジー. シャー ウンメシュ; Claire M. Lankin; エム. ランキン クレアー; Hong Liu; ホン リュー