Pfizer Corporation

Daniel Paul Uccello

Matthew Frank Brown

Adam Matthew Gilbert

Ye Che

Michael Aaron Brodney

Mark Edward Flanagan

Lei Zhang

Christopher Ryan Butler

Russell Dushin

Richard Andrew Ewin

Erik Alphie LaChapelle

Christopher John O'Donnell

Timothy Allan Johnson

Elizabeth Mary Beck

Justin Ian Montgomery

Tamim F Braish

Lawrence Nathan Tumey

Laura Ann McAllister

Usa Reilly

Michael Joseph Melnick

Jeffrey Michael Casavant

Lee Richard Roberts

Mark Stephen Plummer

Loren Michael Price

Jeremy Tyson Starr

Joseph Alan Abramite

Ludivine Moine

Gary Frederick Filzen

Jennifer Young

The present invention is directed to a new fluoro-pyridinone hydroxamic acid phosphates and boronates of Formulae I, II and III wherein Q is selected from the group consisting of —P(O)(OH), —P(O)(OH)(OM), —P(O)(OM)and —P(O)(O)M; Mat each occurrence is a pharmaceutically acceptable monovalent cation; and Mis a pharmaceutically acceptable divalent cation and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

Fluoro-pyridinone phosphates and boronates useful as antibacterial agents

The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula: (wherein R, R, Het, D, E, X, Y, Z, m, n, p, q, r, s and t are as defined herein), methods for their preparation, their use in synthesizing antibody drug conjugates, and the resulting antibody drug conjugates made with components having heteroaryl sulfone-based conjugation handles.

Heteroaryl sulfone-based conjugation handles, methods for their preparation, and their use in synthesizing antibody drug conjugates

The present invention provides, in part, compounds of Formula I, or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: (R)a, (R)b, (R)c, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder. 

Dihydro-pyrrolo-pyridine derivatives

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Colchester, CT, United States of America

Daniel Paul Uccello