Merck Sharp + Dohme Corp.

Merck Canada Inc.

Merck Sharp & Dohme LLC

Thomas J Greshock

Scott D Kuduk

John A McCauley

James J Mulhearn

Ronald K Chang

Vanessa L Rada

John M Sanders

Ian M Bell

Peter D Williams

Deping Wang

Douglas C Beshore

Philippe G Nantermet

Oscar Miguel Moradei

Anthony J Roecker

Christopher James Bungard

Brendan M Crowley

David Jonathan Bennett

Christian Beaulieu

Ting Zhang

Vouy Linh Truong

Carmela Molinaro

Sheldon N Crane

Satyanarayana Tummanapalli

Michael W Miller

Xing Dai

Mark E Layton

Liangqin Guo

Hong Liu

Duane E DeMong

Ronald M Kim

Andrew John Harvey

Walter Won

Rajan Anand

Brian T Campbell

William D Shipe

Deodial Guy Guiadeen

Kenneth J Leavitt

Gang Zhou

Christina Ng DiMarco

Daniel Mckay

Andrew William Stamford

Harold G Selnick

Jack D Scott

Li Ni Zhang

Jianmin Fu

Michael J Kelly, Iii

Jing Li

Abbas M Walji

Kallol Basu

Christina Di Marco

Keith P Moore

Yaode Wang

Tianying Jian

Heather E Stevenson

Eric Hostetler

Linda M Suen

Jonathan T Kern

Idriss Bennacef

Katharine M Holloway

Christian Nadeau

Deodial G Guiadeen

Bernard R Neustadt

Ravi P Nargund

Mark E Fraley

Mark T Bilodeau

Craig A Stump

Christopher S Burgey

Harry R Chobanian

Richard Berger

Marc Poirier

Junying Zheng

M Katharine Holloway

Joseph Leslie Duffy

Hemaka Anthony Rajapakse

Joel M Harris

John E Stelmach

Catherine M Wiscount

Joseph E Pero

Belinda C Huff

Boyoung Kim

Jesse J Manikowski

Wei Li

Kelly-Ann S Schlegel

Karine M Villeneuve

James I Fells

Jonathan Kern

Stephanie Lessard

Kun Yang

Daniel Simard

Kristen G Jones

Duane Demong

Vijayasaradhi Sivalenka

Daniel McKay

Li Hao

Kate Holloway

Sanjay Kumar Singh

Sivalenka Vijayasaradhi

Joseph L Duffy

Abbas W Walji

Helen Juteau

The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I). 

Spiropiperidine allosteric modulators of nicotinic acetylcholine receptors

The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases. 

3-aryl- heteroaryl substituted 5-trifluoromethyl oxadiazoles as histonedeacetylase 6 (HDAC6) inhibitors

The present disclosure relates to compounds of formula (I) that are useful as modulators of &#x3b1;7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation. 

Substituted 6-membered aryl or heteroaryl allosteric modulators of nicotinic acetylcholine receptors

Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and Rto Rare defined herein, which compounds have properties for blocking Na1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same. 

Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels

Substituted bicyclic heteroaryl allosteric modulators of nicotinic acetylcholine receptors

Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Na1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same. 

Disclosed are compounds of Formula A-1, or a salt thereof: Formula A-1, where J, K, Q and R1 are as defined herein, which compounds have properties for inhibiting sodium ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-1 or their salts, and methods of treating pain (e.g. chronic pain), or cough or itch disorders using the same. 

N1-phenylpropane-1,2-diamine compounds with selective activity in voltage-gated sodium channels

Disclosed are compounds of Formula A, or a salt thereof: wherein R, R, and E are defined herein, which compounds have properties for inhibiting Na1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.

Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels

The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.

Pyrrolo[2,3-C]pyridines as imaging agents for neurofibrilary tangles

The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z, Z, V, V, V, R, R, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. 

HIV protease inhibitors

The present disclosure relates to compounds of formula I that are useful as modulators of &#x3b1;7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation 

Allosteric modulators of nicotinic acetylcholine receptors

The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

The present invention is directed to substituted indazole compounds 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. 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.

Compounds inhibiting leucine-rich repeat kinase enzyme activity

The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. 

Pyrrolo[2,3-C]pyridines as imaging agents for neurofibrillary

The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

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Collegeville, PA, United States of America

Thomas J Greshock