Pfizer Corporation

Bethany Lyn Kormos

Patrick Robert Verhoest

Travis T Wager

Jaclyn Louise Henderson

Thomas Allen Chappie

Antonia Friederike Stepan

Paul Galatsis

Ravi G Kurumbail

Christopher John Helal

Matthew Richard Reese

Yuan Zhang

Jamison Bryce Tuttle

Luis Angel Martinez-Alsina

David Andrew Griffith

Lei Zhang

Matthew Merrill Hayward

Kevin James Filipski

Martin Youngjin Pettersson

Michelle Renee Garnsey

Rachel Jane Roth Flach

Leanne Marie Buzon

Samit Kumar Bhattacharya

Joseph Michael Young

Nandini Chaturbhai Patel

Simone Sciabola

Karen Jean Coffman

Russell Alan Miller

Joseph Walter Tucker

Michael Aaron Brodney

Christopher Ryan Butler

Jotham Wadsworth Coe

Joseph Scott Warmus

Brian Kenneth Raymer

Jinshan Michael Chen

Kimberly O'Keefe Cameron

Colin Richard Rose

Jamison Byrce Tuttle

Shenping Liu

Luis Angel Martinez Alsina

Kevin Francis Deboyace

Kiyoyuki Omoto

Described herein are compounds of Formula I, wherein the variables are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors and/or degraders, pharmaceutical compositions containing such compounds and their use to treat, for example, diabetes, kidney disease, NASH and heart failure.

BCKDK inhibitors and/or degraders

Described herein are compounds of Formula I, wherein R, R, and Rare defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.

BCKDK inhibitors

The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof wherein the variables R, R, R, R, R, a and A are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D3-mediated (or D3-associated) disorders including, e.g., substance addiction, substance abuse, schizophrenia (e.g., its cognitive symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD or PD), Parkinson's disease, mania, anxiety, impulse control disorders, sexual disorders and depression. 

6,7,8,9-tetrahydro-5H-pyrido[2,3-d]azepine dopamine D3 ligands

The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R, Rand Rare as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy. 

Imidazo[4,5-C]quinoline derivatives as LRRK2 inhibitors

The present invention provides novel cyclic substituted imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof; wherein R, R, R, R, R, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy. 

Cyclic substituted imidazo[4,5-c]quinoline derivatives

The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R, R, R, R, R, R, R, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives as LRRK2 inhibitors

The present invention provides novel 3,4-disubstituted-1H-pyrrolo[2,3-b]pyridine derivatives and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R, R, R, Rand X are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

3,4-disubstituted-1 H-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazines as LRRK2 inhibitors

The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R, R, R, Rand Rare as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Substituted pyrrolo[2,3-d]pyrimidines as LRRK2 inhibitors

The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R, R, R, and Rare as defined herein and to the use of the compounds as PDE10 inhibitors. 

Triazine derivatives

4-(substituted amino)-7H-pyrrolo[2,3-d] pyrimidines as LRRK2 inhibitors

Growing community of inventors

Somerville, MA, United States of America

Bethany Lyn Kormos