Discovery of 4-((2 S ,4 S )-4-Ethoxy-1-((5-methoxy-7-methyl-1 H -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.

Autor: Mainolfi N; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Ehara T; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Karki RG; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Anderson K; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Mac Sweeney A; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Liao SM; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Argikar UA; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Jendza K; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Zhang C; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Powers J; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Klosowski DW; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Crowley M; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Kawanami T; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Ding J; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., April M; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Forster C; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Serrano-Wu M; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Capparelli M; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Ramqaj R; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Solovay C; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Cumin F; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Smith TM; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Ferrara L; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Lee W; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Long D; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Prentiss M; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., De Erkenez A; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Yang L; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Liu F; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Sellner H; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Sirockin F; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Valeur E; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Erbel P; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Ostermeier D; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Ramage P; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Gerhartz B; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Schubart A; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Flohr S; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Gradoux N; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Feifel R; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Vogg B; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Wiesmann C; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Maibaum J; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Eder J; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Sedrani R; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Harrison RA; Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4056 Basel, Switzerland., Mogi M; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Jaffee BD; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States., Adams CM; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2020 Jun 11; Vol. 63 (11), pp. 5697-5722. Date of Electronic Publication: 2020 Feb 19.

Enantioselective Halolactonization Reactions using BINOL-Derived Bifunctional Catalysts: Methodology, Diversification, and Applications.

Autor: Klosowski DW; Department of Chemistry , The University of Texas at Austin , Austin , Texas 78712 , United States., Hethcox JC; Department of Chemistry , The University of Texas at Austin , Austin , Texas 78712 , United States., Paull DH; Department of Chemistry , The University of Texas at Austin , Austin , Texas 78712 , United States., Fang C; Department of Chemistry , The University of Texas at Austin , Austin , Texas 78712 , United States., Donald JR; Department of Chemistry , The University of Texas at Austin , Austin , Texas 78712 , United States., Shugrue CR; Department of Chemistry , The University of Texas at Austin , Austin , Texas 78712 , United States., Pansick AD; Department of Chemistry , The University of Texas at Austin , Austin , Texas 78712 , United States., Martin SF; Department of Chemistry , The University of Texas at Austin , Austin , Texas 78712 , United States.

Publikováno v: The Journal of organic chemistry [J Org Chem] 2018 Jun 01; Vol. 83 (11), pp. 5954-5968. Date of Electronic Publication: 2018 May 22.

Synthesis of (+)-Disparlure via Enantioselective Iodolactonization.

Autor: Klosowski DW; Department of Chemistry, The University of Texas at Austin , Austin, Texas 78712, United States., Martin SF; Department of Chemistry, The University of Texas at Austin , Austin, Texas 78712, United States.

Publikováno v: Organic letters [Org Lett] 2018 Mar 02; Vol. 20 (5), pp. 1269-1271. Date of Electronic Publication: 2018 Feb 12.