Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Msd R&d (china) Co., Ltd.

John J Acton, Iii

Melissa S Egbertson

Jianming Bao

Ling Tong

Michael Man-Chu Lo

Harold B Wood

Robert D Mazzola, Jr

David M Tellers

Xiaolei Gao

Fengqi Zhang

Scott T Harrison

Chunsing Li

Regina M Black

Oleg B Selyutin

Michael T Rudd

Peter T Meinke

Sandra Lee Knowles

Zhaoyang Meng

William H Parsons

Kun Liu

Gregori J Morriello

Derun Li

Santhosh Francis Neelamkavil

Timothy J Henderson

Qiaolin Deng

Takao Suzuki

Peter H Fuller

Vladimir Simov

Sheryl Davis Debenham

A Brian Jones

Ronald Dale Ferguson, Ii

Xin Yan

Meng Na

Michael J Ardolino

William P Kaplan

Luis Torres

Kaitlyn Marie Logan

Robert M Burk

Tesfaye Biftu

Qun Dang

Barbara A Pio

Ashok Arasappan

Peter J Sinclair

Joey Lee Methot

Ping Liu

Iyassu Sebhat

Mitree M Ponpipom

Solomon D Kattar

Lin Chu

Nunzio Sciammetta

Jing Su

Alan D Adams

Rajan Anand

James Francis Dropinski

Robert L Bugianesi

Yi-Heng Chen

Petr Vachal

Hakan Gunaydin

James J Mulhearn

Guizhen Dong

Yuan-Ching P Chiang

Min Lu

Vincent Colandrea

Deyou Sha

Feng Ye

Debra L Ondeyka

Conrad Santini

Narindar N Girotra

Gregory D Berger

Yi Zang

Claude Dufresne

Vanessa L Rada

Alexander J Kim

Chan-Hwa Kuo

James D Bergstrom

Jeffrey Donald Hermes

Jeffrey W Schubert

Zhifa Pu

Jenny Miu-Chun Wai

Robert W Marquis, Jr

Lori L Whiting

Joanna L Chen

Anmol Gulati

Anthony Brian Jones

Sandra P Plevyak

Rebecca Elizabeth Johnson

Mitchell H Keylor

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 cinnolinyl and quinolinyl pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor

The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 

Indole derivatives useful as anti-diabetic agents

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. 

Cyclic amine substituted heterocyclic CETP inhibitors

Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

Indoles having anti-diabetic activity

A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.

Acyl sulfamides for treatment of obesity, diabetes and lipid disorders

Certain N-substituted indoles having aryloxyacetic acid, substituents are agonists or partial agonists of PPAR gamma, and are useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR mediated diseases, disorders and conditions.

N-substituted indoles useful in the treatment of diabetes

Compounds of the formula ##STR1## are inhibitors of peptide binding to major histocompatibility complex type II proteins and are useful in the treatment and prevention of autoimmune diseases including: rheumatoid arthritis, Type I diabetes, multiple sclerosis, lupus erythematosis, Graves disease and pemphigus. The present invention also provides novel compositions, methods of treatment employing the compounds of the present invention and methods of manufacture of the compounds of structural formula (I).

Pseudopeptide lactam inhibitors of peptide binding to MHC class II

Cholesterol lowering compounds

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Cranford, NJ, United States of America

John J Acton, Iii