Merck Sharp + Dohme Corp.

Lycera Corporation

Merck Sharp & Dohme LLC

Vladimir Simov

Kenneth Jay Barr

Blair T Lapointe

Thomas Daniel Aicher

Nunzio Sciammetta

Catherine M White

William L Thomas

Kun Liu

Brian M Andresen

Peter H Fuller

Matthew H Daniels

Chad A VanHuis

John K MacLean

Corey E Bienstock

Yuan Liu

Neville J Anthony

Santhosh Francis Neelamkavil

Hakan Gunaydin

Peter Laurence Toogood

Joey Lee Methot

Chad A Van Huis

Hua Zhou

Barbara A Pio

Ping Liu

Solomon D Kattar

Harold B Wood

Gregori J Morriello

Derun Li

Weiguo Liu

John J Acton, Iii

Karin Ann Stein

J Michael Ellis

Anmol Gulati

David Annunziato Candito

Xin Yan

Michael J Ardolino

Kaitlyn Marie Logan

Luis Torres

William P Kaplan

John Acton

Joanna L Chen

Hongjun Zhang

Ling Tong

Thomas H Graham

Jing Su

Yi-Heng Chen

Benjamin Wesley Trotter

Min Lu

John K F Maclean

Danielle F Molinari

Mitchell H Keylor

Wesley B Trotter

Rebecca Elizabeth Johnson

Ryan Wing-Kun Chau

Mitchell Henry Keylor

Chad Van Huis

John J Iii Acton

Santhosh F Neelamkavil

Joey Methot

The present invention is directed to substituted certain 1-pyrazolyl, 5-, 6-disubstituted indazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and ring A are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.

1-pyrazolyl, 5-, 6-disubstituted indazole derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof

The present invention is directed to substituted certain N-heteroaryl indazole derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R, R, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.

N-heteroaryl indazole derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof

The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R, X, Y, Rand Rare as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved. 

Indazolyl-spiro[2.3]hexane-carbonitrile derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof

The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved. 

Indazolyl-spiro[2.2]pentane-carbonitrile derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof

The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X, X, R, R, R, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT. 

Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease

The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR&#x3b3; activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.

Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease

The present invention relates to compounds according to Formula (I-1) and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions. 

Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof

The invention provides certain bicyclic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X, X, R, R, R, R, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT. 

The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof wherein R, R, R, R, R, R, R, R, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT. 

Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease

The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, R, R, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT. 

2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease

Tetrahydronaphthyridine and related bicyclic compounds for inhibition of ROR&#x3b3; activity and the treatment of disease

The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.

Bicyclic sulfone compounds for inhibition of RORgamma activity and the treatment of disease

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Boston, MA, United States of America

Vladimir Simov