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Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.

Autor: Morriello GJ; Discovery Chemistry, Merck & Co., Inc., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA. Electronic address: greg_morriello@merck.com., Dwyer MP; Discovery Chemistry, Merck & Co., Inc., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA., Chen Y; Discovery Chemistry, Merck & Co., Inc., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA., Ginetti AT; Discovery Chemistry, Merck & Co., Inc., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA., Xu S; Discovery Chemistry, Merck & Co., Inc., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA., Lu J; Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA., Abeywickrema P; Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA., Wang D; Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA., Crespo A; Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA., Cabalu TD; Drug Metabolism, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA., Wilson JE; Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA., Stachel SJ; Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA., Paone DV; Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA., Sinz C; Discovery Chemistry, Merck & Co., Inc., 213 E. Grand Avenue, South San Fransisco, CA 94080, USA.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Jul 15; Vol. 44, pp. 128082. Date of Electronic Publication: 2021 May 13.

Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.

Autor: Bungard CJ; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Williams PD; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Schulz J; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Wiscount CM; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Holloway MK; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Loughran HM; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Manikowski JJ; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Su HP; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Bennett DJ; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Chang L; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Chu XJ; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Crespo A; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Dwyer MP; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Keertikar K; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Morriello GJ; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Stamford AW; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Waddell ST; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Zhong B; WuXi AppTec, 288 Fute Zhong Road, Shanghai 200131, China., Hu B; WuXi AppTec, 288 Fute Zhong Road, Shanghai 200131, China., Ji T; WuXi AppTec, 288 Fute Zhong Road, Shanghai 200131, China., Diamond TL; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Bahnck-Teets C; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Carroll SS; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Fay JF; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Min X; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Morris W; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States., Ballard JE; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., Miller MD; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States., McCauley JA; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2017 Nov 13; Vol. 8 (12), pp. 1292-1297. Date of Electronic Publication: 2017 Nov 13 (Print Publication: 2017).

Structure-activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors.

Autor: Tong L; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA. Electronic address: ling.tong@merck.com., Yu W; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Coburn CA; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Chen L; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Selyutin O; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Zeng Q; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Dwyer MP; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Nair AG; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Shankar BB; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Kim SH; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Yang DY; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Rosenblum SB; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Ruck RT; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Davies IW; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Hu B; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China., Zhong B; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China., Hao J; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China., Ji T; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China., Zan S; Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China., Liu R; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Agrawal S; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Carr D; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Curry S; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., McMonagle P; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Bystol K; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Lahser F; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Ingravallo P; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Chen S; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Asante-Appiah E; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA., Kozlowski JA; Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Nov 01; Vol. 26 (21), pp. 5354-5360. Date of Electronic Publication: 2016 Sep 02.