Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Merck Sharpe & Dohme Corp.

Peter J Sinclair

Matthew J Wyvratt

William H Parsons

Frederick Wong

Amjad Ali

Zhijian Lu

Mark T Goulet

Christopher Francis Thompson

Cameron James Smith

Yi-Heng Chen

Ramzi Farah Sweis

Hong Li

Qiaolin Deng

Sander G Mills

Helmut H Mrozik

Dennis M Zaller

Dong-Ming Shen

Hong Shen

Kathleen M Rupprecht

Jianming Bao

Zhicai Wu

Dooseop Kim

Richard Thomas Beresis

Anthony K Ogawa

Robert J DeVita

Yuguang Wang

Ping Lan

Frank Kayser

Kun Liu

James B Doherty

Robert K Baker

XiaoXia Qian

Alan D Adams

Wanying Sun

Hyun O Ok

Timothy A Blizzard

Shouwu Miao

Petr Vachal

John J Acton, Iii

Julianne A Hunt

Joung L Goulet

Gayle E Taylor

Nazia Quraishi

Helen M Organ

Florida Kallashi

Xingfang Hong

Changhe Qi

Alejandro Crespo

John Qiang Tan

Zhongxiang Sun

Rudrajit Mal

Min Shu

Ellen K Vande Bunte

Mark A Holmes

Joann Bohn

Joann M Napolitano

Adrian A Dowst

Guizhen Dong

John E Stelmach

Meng-Hsin Chen

Andrew Kotliar

Debra L Ondeyka

A Brian Jones

Liya Chen

Rose M Cubbon

Swaminathan R Natarajan

Kake Zhao

Luping Liu

Jeffrey Donald Hermes

Richard Beresis

Helen M Armstrong

David D Wisnoski

Richard T Cummings

Jennifer Kowalchick

Samantha E Adamson

Mark G Steiner

Rowena D Ruzck

James E Thompson

Gaye Marino

Gayle E Hallett

Rogelio L Martinez

Xiaoxia Qian

Robert J Devita

Jennifer E Kowalchick

The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.

Mineralocorticoid receptor antagonists

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

Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too. 

Compounds 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), Ais a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group. 

Cholesteryl ester transfer protein inhibitors

Compounds having the structures 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 or Ris a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a &#x2014;CH&#x2014;.

CETP inhibitors

Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety.

CETP inhibitors derived from benzoxazole arylamides

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 the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety. 

Compounds 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. 

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.

Compounds 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 1, Aand A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring. 

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: 

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. 

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 or Ris a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or Ris also a cyclic group. 

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Scotch Plains, NJ, United States of America

Peter J Sinclair