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Positive allosteric modulators of the α7 nicotinic acetylcholine receptor: SAR investigation around PNU-120596.

Autor: Acker BA; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Badescu VO; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Berkenpas MB; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Groppi VE; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Hajós M; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Higdon NR; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Hurst RS; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Jon Jacobsen E; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Margolis BJ; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., McWhorter WW; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Myers JK; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Piotrowski DW; Pfizer Worldwide Research & Development, Groton, CT 06340, USA. Electronic address: david.w.piotrowski@comcast.net., Rogers BN; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Sarapa D; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Vetman TN; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Walker DP; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Wall TM; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Wilhite DM; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Wishka DG; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Xu W; Pfizer Worldwide Research & Development, Groton, CT 06340, USA., Yates KM; Pfizer Worldwide Research & Development, Groton, CT 06340, USA.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2023 Sep 01; Vol. 93, pp. 129433. Date of Electronic Publication: 2023 Aug 07.

Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model.

Autor: Fales KR; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Njoroge FG; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Brooks HB; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Thibodeaux S; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Torrado A; Centro de Investigación Lilly , S. A., Avda. de la Industria 30, 28108 Alcobendas, Madrid, Spain., Si C; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Toth JL; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Mc Cowan JR; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Roth KD; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Thrasher KJ; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Frimpong K; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Lee MR; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Dally RD; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Shepherd TA; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Durham TB; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Margolis BJ; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Wu Z; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Wang Y; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Atwell S; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Wang J; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Hui YH; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Meier TI; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Konicek SA; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States., Geeganage S; Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 46285, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2017 Dec 14; Vol. 60 (23), pp. 9599-9616. Date of Electronic Publication: 2017 Nov 09.

Beyond PAINs: Chemotype Sensitivity of Protein Methyltransferases in Screens.

Autor: Gao C; Lilly Research Laboratories, Eli Lilly and Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States., Margolis BJ; Lilly Research Laboratories, Eli Lilly and Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States., Strelow JM; Lilly Research Laboratories, Eli Lilly and Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States., Vidler LR; Research and Development, Eli Lilly and Company Ltd. , Sunninghill Road, Windlesham, Surrey GU20 6PH, United Kingdom., Mader MM; Lilly Research Laboratories, Eli Lilly and Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2015 Nov 19; Vol. 7 (2), pp. 156-61. Date of Electronic Publication: 2015 Nov 19 (Print Publication: 2016).

Assembly of 4-aminoquinolines via palladium catalysis: a mild and convenient alternative to SNAr methodology.

Autor: Margolis BJ; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA. margolis_brandon_j@lilly.com, Long KA, Laird DL, Ruble JC, Pulley SR

Publikováno v: The Journal of organic chemistry [J Org Chem] 2007 Mar 16; Vol. 72 (6), pp. 2232-5. Date of Electronic Publication: 2007 Feb 13.