Eli Lilly and Company

Bristol-Myers Squibb Compnay

Merck + Co., Inc.

Owen Brendan Wallace

Yanping Xu

Tao Wang

Nancy June Snyder

Nicholas A Meanwell

Zhongxing Zhang

Thomas Edward Mabry

Leonard Larry Winneroski, Jr

Ronald Jay Hinklin

Renhua Li

Thomas Daniel Aicher

John A Bender

Jeremy Schulenburg York

Kap-Sun Yeung

John F Kadow

Milind Deshpande

Jeffrey A Dodge

Mark Joseph Chicarelli

Timothy Alan Shepherd

John Gordon Allen

Jefferson Ray McCowan

Haiquan Fang

Zhaogen Chen

Benito Munoz

Zhiwei Yin

Qiufen May Xue

Prasad V Chaturvedula

Michael Frederick Parker

Bradley C Pearce

Zhong Yang

Peter Biagio Anzeveno

David W Smith

Carl P Bergstrom

Gregory Alan Stephenson

Alexei Pavlovych Krasutsky

Ashraf Saeed

Hongqi Tian

Robert Dean Dally

Scott Alan Frank

Marvin M Hansen

Daniel J Keavy

Julie Kay Bush

Charles P Sloan

Gary A Hite

James Lee Toth

Pin-Fang Lin

Scott Alan Jones

George Sal Lewis

Zhilei Qiu

Wade S Blair

Conrad Wilson Hummel

Rebecca Lynn Rezac Guenther

Kumar Srinivasan

Wai Yu Lau

Henry Hui Wang

Timothy P Spicer

Hui Wang

Kin Chlu Fong

Marvin Martin Hansen

Larry Leonard Winneroski

Geroge Sal Lewis

Kin Chiu Fong

Leonard Larry Junior Winneroski

Gary Alan Hite

Junior Leonard Larry Winneroski

Rebecca Lynn Guenther

Jeffrey Alan Dodge

The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause. 

Selective estrogen receptor modulators for the treatment of vasomotor symptoms

The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-HSD type 1 activity. 

Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention discloses novel compounds of Formula I: (I) possessing 11&#x3b2;-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11&#x3b2;-HSD type 1 activity. 

The present invention discloses novel compounds of Formula I: possessing 11 &#x3b2;-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 &#x3b2;-HSD type 1 activity. 

Biphenyl amide lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention discloses novel compounds of Formula I: having 11&#x3b2;-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11&#x3b2;-HSD type 1 activity. 

Cyclohexyl substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11 Beta-HSD type 1 activity. X-17377

The present invention discloses novel compounds of Formula (I): having 11&#x3b2;-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I), as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11&#x3b2;-HSD type 1 activity. 

Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention discloses novel compounds of Formula (I): having 11&#x3b2;-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11&#x3b2;-HSD type 1 activity. 

The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ris (II), or (III) Gis methylene or ethylene; L is a divalent linking group selected from &#x2014;(C-C) alkylene-, &#x2014;S&#x2014;, &#x2014;CH(OH)&#x2014;, or &#x2014;O&#x2014;; A is methylene, &#x2014;S&#x2014;, &#x2014;O&#x2014;, or &#x2014;NH&#x2014;; and the other substituents are as defined in the claims. 

Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention discloses novel compounds of Formula I: having 11&#x3b2;-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11&#x3b2;-HSD type 1 activity.

Piperidinyl substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention discloses novel compounds of Formula I: (I) having 11&#x3b2;-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11&#x3b2;-HSD type 1 activity. 

Cyclohexylimidiazole lactam derivatives as inhibitors of 11-&#x3b2;-hydroxysteroid dehydrogenase 1

Substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia. 

The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata. 

Selective estrogen receptor modulators containing a phenylsulfonyl group

The present invention provides a compound of the formula (I) wherein Ris &#x2014;H, &#x2014;OH, &#x2014;O(C-Calkyl), &#x2014;OCOCH, &#x2014;OCO(C-Calkyl), or &#x2014;OSO(C-Calkyl); R, Rand Rare each independently &#x2014;H, &#x2014;OH, &#x2014;O(C-Calkyl), &#x2014;OCOCH, &#x2014;OCO(C-Calkyl), &#x2014;OSO(C-Calkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is &#x2014;S&#x2014; or &#x2014;HC&#x2550;CH&#x2014;; G is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, SO, or &#x2014;N(R)&#x2014;, wherein Ris &#x2014;H or C-Calkyl; and Y is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;NH&#x2014;, &#x2014;NMe-, or &#x2014;CH&#x2014;, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation, and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

Dihydro-dibenzo[B,E]oxepine based selective estrogen receptor modulators, compositions and methods

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Zionsville, IN, United States of America

Owen Brendan Wallace