Merck Sharp + Dohme Corp.

Mochida Pharmaceutical Co., Ltd.

Merck + Co., Inc.

Mochida Paraceuticals Co., Ltd.

Mochida Pharmacuetical Co., Ltd.

Msd R&d Co., Ltd.

Yi-Heng Chen

Cameron James Smith

Peter J Sinclair

Zhijian Lu

Hong Li

Amjad Ali

Liangqin Guo

Christopher Francis Thompson

William J Greenlee

Samuel Chackalamannil

James M Balkovec

Harold B Wood

Subharekha Raghavan

Shouwu Miao

John E Stelmach

Ting Zhang

Alan Whitehead

Joie Garfunkle

Yili Chen

Tomokazu Hirabayashi

John Qiang Tan

Mark E Fraley

Craig A Stump

Casey Cameron McComas

Ping Liu

Yong Zhang

Chun Sing Li

Guoqing Li

Derun Li

Helen J Mitchell

Jianmin Fu

Dongfang Meng

Andrew John Cooke

Qinghua Mao

Edward C Sherer

Julianne A Hunt

Melody McWherter

Swati P Mercer

Gayle E Taylor

Rui Zhang

Xu-Fang Zhang

Kathy Schirripa

Raphaelle Berger

Gang Ji

Falong Jiang

Mika Sekioka

Adrian A Dowst

Hong-Dong Li

Hua Zhou

Barbara A Pio

Emma R Parmee

Jianming Bao

Sherman Tim Waddell

Douglas C Beshore

Solomon D Kattar

Gregori J Morriello

Tin-Yau Chan

Alan W Hruza

Jing Su

Santhosh Francis Neelamkavil

Bing Li

Nunzio Sciammetta

XiaoXia Qian

Wanying Sun

Qiaolin Deng

Peter H Fuller

Linda Brockunier

Ramzi Farah Sweis

Xibin Liao

Kerim Babaoglu

Petr Vachal

John J Acton, Iii

Jiang Chang

Jiayi Xu

Guizhen Dong

Min Lu

Vladimir Simov

Keith P Moore

Debra L Ondeyka

Jian Guo

Kake Zhao

Tianying Jian

Hiroshi Nagasue

Nazia Quraishi

Zhiqi Qi

Keith Rosauer

Jonathan A Groeper

Olga Ornoski

Jane Yang Wu

Louis-Charles Campeau

Kouki Ogawa

Florida Kallashi

Xiaoqing Han

Xin Yan

Isao Sakurada

Anmol Gulati

Joann M Napolitano

Kaitlyn Marie Logan

Luis Torres

William P Kaplan

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 invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R, R, R, R, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate ('cGMP'), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.

Soluble guanylate cyclase stimulators

The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors. 

Factor IXa inhibitors

The present invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula I, and methods for using compounds of Formula I for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes.

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 six membered 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 provides a compound of Formula (I) wherein

The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate ('cGMP') and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof. 

Soluble guanylate cyclase activators

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, Ais a substituted phenyl group or indanyl group. Formula (I). 

Cyclic amine substituted oxazolidinone CETP inhibitor

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B. 

1,3-oxazolidin -2-one derivatives useful as CETP inhibitors

Compounds having a biphenyl group substituted with a phenyl or heteroaromatic group, as shown in Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: 

CETP inhibitors

1,3-oxazolidin-2-one derivatives useful as CETP inhibitors

Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B. 

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Whippany, NJ, United States of America

Yi-Heng Chen