Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Raman Kumar Bakshi

Ravi P Nargund

Gary H Rasmusson

Zhixiong Ye

Richard L Tolman

Gool F Patel

Brenda L Palucki

Arthur A Patchett

Iyassu K Sebhat

David James Witter

Xianhai Huang

David L Sloman

Phieng Siliphaivanh

Leonardus H T Van Der Ploeg

Christopher W Boyce

Kathryn Ann Lipford

Ganesh Babu Karunakaran

Joseph A Kozlowski

Bruce E Witzel

Jongwon Lim

Kevin J Wilson

Feroze Ujjainwalla

Soumya P Sahoo

Joey Lee Methot

Liangqin Guo

Umar Faruk Mansoor

Matthew H Daniels

Wei Zhou

Min K Park

Georgianna S Harris

Salem Fevrier

Danielle Falcone

Brendan O'Boyle

Ravi Kurukulasuriya

Khaled J Barakat

Qingmei Hong

James Dellureficio

Jayanth Thiruvellore Thatai

Hua Zhou

Wei Liu

Andrew S Thompson

Neville J Anthony

Thomas F Walsh

Mark T Goulet

Kenneth Jay Barr

Donald W Graham

Ling Tong

Shuwen He

Jonathan R Young

David Joseph Guerin

Milana M Maletic

Jianmin Fu

Christopher Francis Thompson

Catherine M White

Lei Chen

Mark E Scott

Ross A Miller

Shu S Yang

Edward G Corley

Ron Ferguson

Shuyi Tang

Judson E Richard

Carolyn Michele Cammarano

Danielle F Molinari

Daniel Warner

Yingjie Lai

Angie R Angeles

Peter H Dobbelaar

Ziping Liu

Zhilong Wan

Patrick G Pollard

Subhendu Kumar Mohanty

Chandra Sekhar Korapala

Prashant R Latthe

Vyjayanthi N Kambam

Sujit Kumar Sarkar

Bidhan A Shinkre

James P Dellureficio

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. 

ERK inhibitors

The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of &#x3b2;3-adrenoceptor.

Pyrrolidine derived beta 3 adrenergic receptor agonists

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1). 

Compounds that are ERK inhibitors

Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). 

Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators

Certain novel N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated piperidine derivatives as melanocortin 4-receptor agonists

Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.

Piperazine urea derivatives as melanocortin-4 receptor agonists

Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated piperazine derivatives as melanocortin-4 receptor agonists

Compounds of structural Formula (I)and pharmacologically acceptable salts and esters thereof possess 5&#x3b1;-reductase inhibitory activity. These compounds inhibit 5&#x3b1;-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.

4-Azasteroids for treatment of hyperandrogenic conditions

Certain novel-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-receptor (MC-R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated piperidine derivatives as melanocortin-4 receptor agonists

Certain novel 4-substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Substituted piperidines as melanocortin receptor agonists

Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.

Spiropiperidine derivatives as melanocortin receptor agonists

Certain novel compounds and derivatives thereof are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Melanocortin receptor agonists

The instant invention involves a process for oxidizing compounds containing an allylic group, i.e. those containing an allylic hydrogen or allylic alcohol group, to the corresponding enones, using a ruthenium-based catalyst in the presence of a hydroperoxide. Particularly, &Dgr;-5-steroidal alkenes can be oxidized to the corresponding &Dgr;-5-7-keto alkenes.

Process for oxidation of steroidal compounds having allylic groups

Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.

Substituted piperidines as melanocortin-4 receptor agonists

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Edison, NJ, United States of America

Raman Kumar Bakshi