Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

Filters

My NCBI Filters

Text availability

Article attribute

Article type

Publication date

Search Results

70 results

Filters applied: . Clear all
Results are displayed in a computed author sort order. The Results By Year timeline is not available.
Page 1
Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Mainolfi N, Ehara T, Karki RG, Anderson K, Mac Sweeney A, Liao SM, Argikar UA, Jendza K, Zhang C, Powers J, Klosowski DW, Crowley M, Kawanami T, Ding J, April M, Forster C, Serrano-Wu M, Capparelli M, Ramqaj R, Solovay C, Cumin F, Smith TM, Ferrara L, Lee W, Long D, Prentiss M, De Erkenez A, Yang L, Liu F, Sellner H, Sirockin F, Valeur E, Erbel P, Ostermeier D, Ramage P, Gerhartz B, Schubart A, Flohr S, Gradoux N, Feifel R, Vogg B, Wiesmann C, Maibaum J, Eder J, Sedrani R, Harrison RA, Mogi M, Jaffee BD, Adams CM. Mainolfi N, et al. Among authors: jaffee bd. J Med Chem. 2020 Jun 11;63(11):5697-5722. doi: 10.1021/acs.jmedchem.9b01870. Epub 2020 Feb 19. J Med Chem. 2020. PMID: 32073845
Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.
Schubart A, Anderson K, Mainolfi N, Sellner H, Ehara T, Adams CM, Mac Sweeney A, Liao SM, Crowley M, Littlewood-Evans A, Sarret S, Wieczorek G, Perrot L, Dubost V, Flandre T, Zhang Y, Smith RJH, Risitano AM, Karki RG, Zhang C, Valeur E, Sirockin F, Gerhartz B, Erbel P, Hughes N, Smith TM, Cumin F, Argikar UA, Haraldsson B, Mogi M, Sedrani R, Wiesmann C, Jaffee B, Maibaum J, Flohr S, Harrison R, Eder J. Schubart A, et al. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. doi: 10.1073/pnas.1820892116. Epub 2019 Mar 29. Proc Natl Acad Sci U S A. 2019. PMID: 30926668 Free PMC article.
Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
Karki RG, Powers J, Mainolfi N, Anderson K, Belanger DB, Liu D, Ji N, Jendza K, Gelin CF, Mac Sweeney A, Solovay C, Delgado O, Crowley M, Liao SM, Argikar UA, Flohr S, La Bonte LR, Lorthiois EL, Vulpetti A, Brown A, Long D, Prentiss M, Gradoux N, de Erkenez A, Cumin F, Adams C, Jaffee B, Mogi M. Karki RG, et al. J Med Chem. 2019 May 9;62(9):4656-4668. doi: 10.1021/acs.jmedchem.9b00271. Epub 2019 Apr 30. J Med Chem. 2019. PMID: 30995036
Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration.
Meredith EL, Mainolfi N, Poor S, Qiu Y, Miranda K, Powers J, Liu D, Ma F, Solovay C, Rao C, Johnson L, Ji N, Artman G, Hardegger L, Hanks S, Shen S, Woolfenden A, Fassbender E, Sivak JM, Zhang Y, Long D, Cepeda R, Liu F, Hosagrahara VP, Lee W, Tarsa P, Anderson K, Elliott J, Jaffee B. Meredith EL, et al. J Med Chem. 2015 Dec 10;58(23):9273-86. doi: 10.1021/acs.jmedchem.5b01227. Epub 2015 Nov 30. J Med Chem. 2015. PMID: 26568411
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J. Lorthiois E, et al. J Med Chem. 2017 Jul 13;60(13):5717-5735. doi: 10.1021/acs.jmedchem.7b00425. Epub 2017 Jun 30. J Med Chem. 2017. PMID: 28621538
The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
Adams CM, Anderson K, Artman G 3rd, Bizec JC, Cepeda R, Elliott J, Fassbender E, Ghosh M, Hanks S, Hardegger LA, Hosagrahara VP, Jaffee B, Jendza K, Ji N, Johnson L, Lee W, Liu D, Liu F, Long D, Ma F, Mainolfi N, Meredith EL, Miranda K, Peng Y, Poor S, Powers J, Qiu Y, Rao C, Shen S, Sivak JM, Solovay C, Tarsa P, Woolfenden A, Zhang C, Zhang Y. Adams CM, et al. J Med Chem. 2018 Feb 22;61(4):1622-1635. doi: 10.1021/acs.jmedchem.7b01731. Epub 2018 Feb 5. J Med Chem. 2018. PMID: 29400470
Small-molecule factor D inhibitors targeting the alternative complement pathway.
Maibaum J, Liao SM, Vulpetti A, Ostermann N, Randl S, Rüdisser S, Lorthiois E, Erbel P, Kinzel B, Kolb FA, Barbieri S, Wagner J, Durand C, Fettis K, Dussauge S, Hughes N, Delgado O, Hommel U, Gould T, Mac Sweeney A, Gerhartz B, Cumin F, Flohr S, Schubart A, Jaffee B, Harrison R, Risitano AM, Eder J, Anderson K. Maibaum J, et al. Nat Chem Biol. 2016 Dec;12(12):1105-1110. doi: 10.1038/nchembio.2208. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775713
Complement factor B is critical for sub-RPE deposit accumulation in a model of Doyne honeycomb retinal dystrophy with features of age-related macular degeneration.
Crowley MA, Garland DL, Sellner H, Banks A, Fan L, Rejtar T, Buchanan N, Delgado O, Xu YY, Jose S, Adams CM, Mogi M, Wang K, Bigelow CE, Poor S, Anderson K, Jaffee BD, Prasanna G, Grosskreutz C, Fernandez-Godino R, Pierce EA, Dryja TP, Liao SM. Crowley MA, et al. Among authors: jaffee bd. Hum Mol Genet. 2023 Jan 6;32(2):204-217. doi: 10.1093/hmg/ddac187. Hum Mol Genet. 2023. PMID: 35943778 Free PMC article.
70 results