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Page 1
Optimization of a Class of Dihydrobenzofurane Analogs toward Orally Efficacious YAP-TEAD Protein-Protein Interaction Inhibitors.
Sellner H, Chapeau E, Furet P, Voegtle M, Salem B, Le Douget M, Bordas V, Groell JM, Le Goff AL, Rouzet C, Wietlisbach T, Zimmermann T, McKenna J, Brocklehurst CE, Chène P, Wartmann M, Scheufler C, Kallen J, Williams G, Harlfinger S, Traebert M, Dumotier BM, Schmelzle T, Soldermann N. Sellner H, et al. Among authors: harlfinger s. ChemMedChem. 2023 Jun 1;18(11):e202300051. doi: 10.1002/cmdc.202300051. Epub 2023 Apr 13. ChemMedChem. 2023. PMID: 36988034
Structure-Based and Property-Driven Optimization of N-Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors.
Hoegenauer K, Kallen J, Jiménez-Núñez E, Strang R, Ertl P, Cooke NG, Hintermann S, Voegtle M, Betschart C, McKay DJJ, Wagner J, Ottl J, Beerli C, Billich A, Dawson J, Kaupmann K, Streiff M, Gobeau N, Harlfinger S, Stringer R, Guntermann C. Hoegenauer K, et al. Among authors: harlfinger s. J Med Chem. 2019 Dec 12;62(23):10816-10832. doi: 10.1021/acs.jmedchem.9b01291. Epub 2019 Dec 3. J Med Chem. 2019. PMID: 31729873
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Velcicky J, Wilcken R, Cotesta S, Janser P, Schlapbach A, Wagner T, Piechon P, Villard F, Bouhelal R, Piller F, Harlfinger S, Stringer R, Fehlmann D, Kaupmann K, Littlewood-Evans A, Haffke M, Gommermann N. Velcicky J, et al. Among authors: harlfinger s. J Med Chem. 2020 Sep 10;63(17):9856-9875. doi: 10.1021/acs.jmedchem.0c01020. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32856916
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Harlfinger S, Hanson L, Howard M, Howells R, Jackson A, Kemmitt P, Kingston JK, Lamont S, Lewis HJ, Li S, Liu L, Ogg D, Phillips C, Polanski R, Robb G, Robinson D, Ross S, Smith JM, Tonge M, Whiteley R, Yang J, Zhang L, Zhao X. Kettle JG, et al. Among authors: harlfinger s. J Med Chem. 2020 May 14;63(9):4468-4483. doi: 10.1021/acs.jmedchem.9b01720. Epub 2020 Feb 13. J Med Chem. 2020. PMID: 32023060
Discovery of a Novel Cabazitaxel Nanoparticle-Drug Conjugate (CRLX522) with Improved Pharmacokinetic Properties and Anticancer Effects Using a β-Cyclodextrin-PEG Copolymer Based Delivery Platform.
Metcalf CA 3rd, Svenson S, Hwang J, Tripathi S, Gangal G, Kabir S, Lazarus D, Cole R, Sweryda-Krawiec B, Shum P, Brown D, Case RI, van der Poll D, Rohde E, Harlfinger S, Teng CH, Eliasof S. Metcalf CA 3rd, et al. Among authors: harlfinger s. J Med Chem. 2019 Nov 14;62(21):9541-9559. doi: 10.1021/acs.jmedchem.9b00892. Epub 2019 Oct 24. J Med Chem. 2019. PMID: 31593466
Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists.
Schunk S, Linz K, Frormann S, Hinze C, Oberbörsch S, Sundermann B, Zemolka S, Englberger W, Germann T, Christoph T, Kögel BY, Schröder W, Harlfinger S, Saunders D, Kless A, Schick H, Sonnenschein H. Schunk S, et al. Among authors: harlfinger s. ACS Med Chem Lett. 2014 Jun 24;5(8):851-6. doi: 10.1021/ml500116x. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147602 Free PMC article.
Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.
Schunk S, Linz K, Hinze C, Frormann S, Oberbörsch S, Sundermann B, Zemolka S, Englberger W, Germann T, Christoph T, Kögel BY, Schröder W, Harlfinger S, Saunders D, Kless A, Schick H, Sonnenschein H. Schunk S, et al. Among authors: harlfinger s. ACS Med Chem Lett. 2014 Jun 24;5(8):857-62. doi: 10.1021/ml500117c. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147603 Free PMC article.
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration.
Kettle JG, Bagal SK, Barratt D, Bodnarchuk MS, Boyd S, Braybrooke E, Breed J, Cassar DJ, Cosulich S, Davies M, Davies NL, Deng C, Eatherton A, Evans L, Feron LJ, Fillery S, Gleave ES, Goldberg FW, Cortés González MA, Guerot C, Haider A, Harlfinger S, Howells R, Jackson A, Johnström P, Kemmitt PD, Koers A, Kondrashov M, Lamont GM, Lamont S, Lewis HJ, Liu L, Mylrea M, Nash S, Niedbala MJ, Peter A, Phillips C, Pike K, Raubo P, Robb GR, Ross S, Sanders MG, Schou M, Simpson I, Steward O. Kettle JG, et al. Among authors: harlfinger s. J Med Chem. 2023 Jul 13;66(13):9147-9160. doi: 10.1021/acs.jmedchem.3c00746. Epub 2023 Jul 3. J Med Chem. 2023. PMID: 37395055
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Boyd S, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Davies NL, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Hanson L, Harlfinger S, Howard M, Howells R, Jackson A, Kemmitt P, Lamont G, Lamont S, Lewis HJ, Liu L, Niedbala MJ, Phillips C, Polanski R, Raubo P, Robb G, Robinson DM, Ross S, Sanders MG, Tonge M, Whiteley R, Wilkinson S, Yang J, Zhang W. Kettle JG, et al. Among authors: harlfinger s. J Med Chem. 2022 May 12;65(9):6940-6952. doi: 10.1021/acs.jmedchem.2c00369. Epub 2022 Apr 26. J Med Chem. 2022. PMID: 35471939
33 results