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Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).

Autor: Gonzalez-Lopez de Turiso F; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Hao X; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Shin Y; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Bui M; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Campuzano ID; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Cardozo M; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Dunn MC; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Duquette J; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Fisher B; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Foti RS; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Henne K; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., He X; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Hu YL; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Kelly RC; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Johnson MG; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Lucas BS; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., McCarter J; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., McGee LR; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Medina JC; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Metz D; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., San Miguel T; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Mohn D; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Tran T; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Vissinga C; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Wannberg S; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Whittington DA; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Whoriskey J; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Yu G; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Zalameda L; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Zhang X; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States., Cushing TD; Department of Therapeutic Discovery, §Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.; Department of Therapeutic Discovery, #Department of Inflammation Research, ⊥Drug Product Technologies, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.; Department of Therapeutic Discovery, ¶Department of Pharmacokinetics and Drug Metabolism, Amgen Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2016 Aug 11; Vol. 59 (15), pp. 7252-67. Date of Electronic Publication: 2016 Jul 25.

Synthesis and SAR study of potent and selective PI3Kδ inhibitors.

Autor: Bui M; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Hao X; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Shin Y; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Cardozo M; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., He X; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Henne K; Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Suchomel J; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., McCarter J; Department of Therapeutic Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States., McGee LR; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., San Miguel T; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States., Medina JC; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Mohn D; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States., Tran T; Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Wannberg S; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States., Wong J; Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Wong S; Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States., Zalameda L; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States., Metz D; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States., Cushing TD; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Mar 01; Vol. 25 (5), pp. 1104-9. Date of Electronic Publication: 2015 Jan 17.

Inhibiting NF-κB-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures.

Autor: Li K; Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. kli@amgen.com, McGee LR, Fisher B, Sudom A, Liu J, Rubenstein SM, Anwer MK, Cushing TD, Shin Y, Ayres M, Lee F, Eksterowicz J, Faulder P, Waszkowycz B, Plotnikova O, Farrelly E, Xiao SH, Chen G, Wang Z

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Mar 01; Vol. 23 (5), pp. 1238-44. Date of Electronic Publication: 2013 Jan 11.

PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.

Autor: Cushing TD; Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, California 94080, USA. tcushing@amgen.com, Metz DP, Whittington DA, McGee LR

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2012 Oct 25; Vol. 55 (20), pp. 8559-81. Date of Electronic Publication: 2012 Sep 13.