Merck Sharp + Dohme Corp.

Keith P Moore

Philippe G Nantermet

Harold G Selnick

Li Ni Zhang

Shaun R Stauffer

Joseph P Vacca

Yi Heng Chen

Matthew G Stanton

Hemaka Anthony Rajapakse

Shawn J Stachel

Douglas C Beshore

Thomas J Greshock

Jianmin Fu

James J Mulhearn

Jing Li

Yaode Wang

Eric Hostetler

Idriss Bennacef

Mark E Fraley

Craig Alan Coburn

Samuel L Graham

Craig A Stump

James C Barrow

Casey Cameron McComas

Ping Liu

Chun Sing Li

Harold B Wood

Helen J Mitchell

Rajan Anand

Yi-Heng Chen

M Katharine Holloway

Andrew John Cooke

William D Shipe

Abbas M Walji

Qinghua Mao

Zhiqiang Yang

Melody McWherter

Xu-Fang Zhang

Swati P Mercer

Remond Moningka

Kathy Schirripa

ZhiQiang Yang

Ivory D Hills

Constantine Kreatsoulas

Hong Zhu

Kun Yang

Evan Foster Shalen

Mattahew G Stanton

Stacey Lindsley

Abbas W Walji

Thomas Greshock

James Mulhearn

Andrew J Cooke

Melody Mcwherter

Casey C Mccomas

Hemaka A Rajapakse

The present disclosure is directed to cyclohexylglycine derivatives of Formula I and their use as HIV-infected cell kill agents which accelerate the death of HIV GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve cells.

Cyclohexylglycine derivatives as selective cytotoxic agents

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 a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA. 

TRKA kinase inhibitors, compositions and methods thereof

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 certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.

Oxazole derivatives useful as modulators of FAAH

The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease

The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Macrocyclic spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease

The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease

The present invention is directed to macrocyclic aminopyridyl compounds represented by general formula (I), which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of Alzheimer's disease

The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease

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North Wales, PA, United States of America

Keith P Moore