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Journal: Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines. (Pubmed Central) - Oct 4, 2023 Altogether, this provides a highly modular access to four isomeric THN cores from a common set of unprotected primary amine starting materials, using the same bond disconnections. The simplifying power of the methodology is illustrated by a concise synthesis of the spirocyclic THN core of Pfizer's MC4R antagonist PF-07258669.
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Trial completion, Enrollment change: A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) - Aug 22, 2023 P1, N=40, Completed, The simplifying power of the methodology is illustrated by a concise synthesis of the spirocyclic THN core of Pfizer's MC4R antagonist PF-07258669. Recruiting --> Completed | N=150 --> 40
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Trial completion date, Trial primary completion date: A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) - Jun 7, 2023 P1, N=150, Recruiting, Recruiting --> Completed | N=150 --> 40 Trial completion date: Apr 2023 --> Aug 2023 | Trial primary completion date: Apr 2023 --> Aug 2023
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Enrollment change: A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) - Dec 1, 2022 P1, N=150, Recruiting, This synthetic route consisting of total of 25 synthetic steps (15 linear) delivered API against tight deadlines. N=70 --> 150
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Trial completion date, Trial primary completion date: A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) - Sep 29, 2022 P1, N=70, Recruiting, N=70 --> 150 Trial completion date: Jul 2022 --> May 2023 | Trial primary completion date: Jul 2022 --> May 2023
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Discovery of PF-07258669: A selective and potent small molecule melanocortin-4 receptor antagonist (W183a (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_11434; Antagonism of MC4R signaling has the potential to mitigate decreased appetite and body weight loss in the setting of anorexia or cachexia due to underlying disease. We will report on the identification of a series of orally bioavailable, small-molecule MC4R antagonists using a focused hit identification effort and the optimization of these antagonists for potency, brain penetration, and ADME attributes leading to the identification of PF-07258669 as a clinical candidate.
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Enrollment open: A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) - Jan 4, 2022 P1, N=70, Recruiting, We will report on the identification of a series of orally bioavailable, small-molecule MC4R antagonists using a focused hit identification effort and the optimization of these antagonists for potency, brain penetration, and ADME attributes leading to the identification of PF-07258669 as a clinical candidate. Not yet recruiting --> Recruiting
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