H. Lundbeck A/s

American Life Science Pharmaceuticals, Inc.

Dart Neuroscience, LLC

Amy Allan

Cheryl A Grice

Daniel J Buzard

John J M Wiener

Justin S Cisar

Olivia Delene Weber

Michael B Shaghafi

Jeanne V Moody

Thomas Vetter

Robert J Ternansky

Heidi Lopez De Diego

Laurent Gomez

Brian Dyck

Martin Juhl

Nicholas Brian Raffaele

Michael I Weinhouse

Marco Peters

Bryan Branstetter

Tami Jo Marrone

Gregory Hook

Nicholas Raffaele

Antonio Cincotti

Susana Del Rio Gancedo

Adam Ross Patterson

Richard James Edwards

Samuel George Andrew

Tammi Jo Marrone

Greg Hook

Described herein are crystalline forms of the MAGL inhibitor 1,1,1,3,3,3-Hexafluoropropan-2-yl(S)-1-(pyridazin-3-ylcarbamoyl)-6-azaspiro[2.5]octane-6-carboxylate.

Crystalline forms of a MAGL inhibitor

Described herein are new crystalline forms of the MAGL inhibitor 1-(1-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)-1,8-diazaspiro[4.5]decane-8-carbonyl)-1H-pyrazole-3-carboxylic acid, or a pharmaceutically acceptable salt thereof.

Provided herein are substituted 1,1,1,3,3,3-hexafluoropropan-2-yl 6-azaspiro[2.5]octane-6-carboxylate compounds and pharmaceutical compositions comprising said compounds. The compounds and compositions provided herein are useful as inhibitors of MAGL. Furthermore, the compounds and compositions as provided herein are useful for the treatment of diseases and disorders benefiting from the inhibition of MAGL.

MAGL inhibitors

In alternative embodiments the invention provides compositions and methods for ameliorating diseases and conditions having a beta-amyloid component, including Alzheimer's disease (AD), Vascular Dementia (VD), dementia, pre-dementia, Cognitive Dysfunction Syndrome (CDS) and loss of cognition in humans and in non-human animal. In alternative embodiment the invention provides analogs of AB-007 and its acid form E64c (loxistatin), their preparation, and pharmaceutical compositions thereof and methods of making and using same. In alternative embodiments compositions of the invention are deuterated analogs of AB-007 (or E64d) and E64c (or loxistatin). In alternative embodiments compositions of the invention are metabolically blocked forms as compared to AB-007 and loxistatin. In alternative embodiments compositions of the invention are used to ameliorate (including treat, slow, reverse or prevent) a disease or condition which can be ameliorated by partial or complete inhibition of a cysteine protease, e.g., AD, VD, CDS. The invention also provides alternative dosage forms and formulations for AB-007 and loxistatin, and for compounds of this invention, which can be used e.g., to treat AD, VD and CDS, in humans and in non-human animals.

Compositions and methods for treating beta-amyloid related diseases

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San Diego, CA, United States of America

Amy Allan