Arena Pharmaceuticals, Inc.

Janssen Pharmaceutica Nv

H. Lundbeck A/s

Abide Therapeutics, Inc.

Lundbeck La Jolla Research Center, Inc.

Vidya Therapeutics, Inc.

Daniel J Buzard

Cheryl A Grice

Michael B Shaghafi

James Patrick Edwards

Jennifer Diane Venable

David E Kindrachuk

Olivia Delene Weber

Robert M Jones

Tawfik Gharbaoui

Michael J Martinelli

Sun Hee Kim

Antonio Garrido Montalban

John A DeMattei

Justin S Cisar

Xiuwen Zhu

Ashwin M Krishnan

Juerg Lehmann

Dipanjan Sengupta

You-An Ma

Suzanne Michiko Sato

Jeanne V Moody

Stephen R Johannsen

John J M Wiener

Young Mi Kuhlman

Todd Kevin Jones

Sangdon Han

Brett Ullman

Scott Stirn

Amy Allan

Andrew Mamoru Kawasaki

Michael D Hack

Lars Thoresen

Thomas Vetter

Heidi Lopez De Diego

Martin Juhl

James Breitenbucher

Nicholas Brian Raffaele

Nidhi Arora

Katharine K Duncan

Alice Lee-Dutra

Thomas O Schrader

Nicole Suzanne White

Abu J M Sadeque

Kristen L Arienti

Michelle Kasem

Benjamin R Johnson

Dange Vijay Kumar

Donald L Hertzog

Luis A Lopez

Scott Stim

Young Mi Khulman

Nicholas Raffaele

Antonio Cincotti

Susana Del Rio Gancedo

Adam Ross Patterson

Richard James Edwards

Samuel George Andrew

Craig Alan Coburn

Stephen Robert Johannsen

John Aldo Demattei

Michael John Martinelli

Disclosed herein are 1H-indole-7-carboxamide derivatives as protein kinase inhibitors, in particular Bruton's tyrosine kinase (BTK) inhibitors, pharmaceutical compositions comprising them, processes for preparing them and uses of such protein kinase inhibitors to treat or prevent diseases, disorders and conditions associated with kinase function. In particular, the present invention relates to selective BTK inhibitors.

Kinase inhibitors

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 spirocyclic and fused bicyclic carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

MAGL inhibitors

The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis). 

Processes for the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof

The present invention relates to certain compounds of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor: Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, an inflammatory skin disease or disorder, cancer, psoriasis, atopic dermatitis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, and acne, microbial infections or diseases and viral infections or diseases. 

Compounds useful in the treatment of autoimmune and inflammatory disorders

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.

Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Provided herein are compounds of the formula: and compositions comprising the same, which are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Spirocycle compounds and methods of making and using same

Processes for the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[B]indol-3-yl)acetic acid and salts thereof

Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Pyrazole MAGL inhibitors

Provided herein are compounds and compositions useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Piperazine carbamates and methods of making and using same

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San Diego, CA, United States of America

Daniel J Buzard