Eli Lilly and Company

Cynthia Darshini Jesudason

Freddie Craig Stevens

Don Richard Finley

Richard Todd Pickard

Robert Alan Gadski

Lisa Selsam Beavers

Daniel Jon Sall

Philip Arthur Hipskind

William Joseph Hornback

John Arnold Werner

Christopher J Rito

Michael Gregory Bell

Mark Alan Winter

Anthony John Shuker

Takako Takakuwa

Donald Paul Matthews

John H McDonald, Iii

Thomas Alan Crowell

David Andrew Neel

Grant Mathews Vaught

Christine Ann Droste

Jolie Anne Bastian

Theo Schotten

Vincent Patrick Rocco

Patrick Gianpietro Spinazze

Andrew Michael Ratz

Terry Patrick Finn

John Xiaoqiang He

William George Trankle

Gerd Reuhter

Rushad Eruch Karanjawala

Britta Evers

Craig William Lindsley

Leonard Larry Winneroski, Jr

Matthew Joseph Fisher

Timothy Paul Burkholder

Joseph P Burkhart

Yao-Chang Xu

Wolfgang Stenzel

Russell Dean Stucky

Yanping Xu

Karen Lynn Lobb

Qing Shi

Joshua O Odingo

Danwen Huang

Shawn Christopher Miller

Karin Briner

David Michael Remick

Miles Goodman Siegel

Serge Louis Boulet

Jeffrey Thomas Mullaney

Gerd Ruehter

Roger Ryan Rothhaar

Matthew Robert Reinhard

Michael James Genin

William Harlan Gritton

William Glen Holloway

Brian Eugene Cunningham

Gary G Deng

Mark David Rekhter

Terry Patrick Eli Lilly And Company Finn

The present invention provides a compound of Formula I: wherein X is CHCH, CHCHCH, OCH, or CHO; and R is ethyl, n-propyl, cyclopropyl, or cyclobutyl; or a pharmaceutically acceptable salt thereof; with the proviso that when X is CHCH, then R is other than cyclopropyl; for use as a human PDE inhibitor. 

[1,2,4]Triazolo derivatives as PDE1 inhibitors for the treatment of diabetes

The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder. 

Azetidinyloxyphenylpyrrolidine compounds

The present invention provides a compound of Formula I: useful for treating chronic kidney disease and diabetic kidney disease.

PDE1 inhibitor

The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine&#x2014;H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. 

Histamine H3 receptor agents, preparation and therapeutic uses

The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist 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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. (Formula I). 

The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine&#x2014;H3 receptor antagonist or inverse agonist 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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor&#x2014;related diseases 

The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. 

Pyrrolidine derivatives as histamine H3 receptor antagonists

The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor 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 them to treat obesity and other histamine H3 receptor-related diseases. 

Histamine H3 receptor antagonists, preparation and therapeutic uses

The present invention provides novel compounds with histamine-H3 receptor antagonist or inverse agonist activity. In particular, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and intermediates and methods for making these compounds. The invention provides methods of using compounds and pharmaceutical compositions to treat obesity, cognitive deficiences, narcolepsy, and other histamine H3 receptor-related diseases. 

Histamine H3 receptor inhibitors, preparation and therapeutic uses

The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist 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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. 

The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist 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 these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. 

The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently &#x2014;(C&#x2014;C) alkyl (optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence &#x2014;H, -halogen, or &#x2014;CH. 

Oxazole derivatives as histamine H3 receptor agents, preparation and therapeutic uses

The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist 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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. 

The present invention relates to a &#x3b2;adrenergic receptor agonist of formula (I), wherein R is C&#x2013;Calkyl or (C&#x2013;Ccycloalkyl)C&#x2013;Calk-di-yl: Ris H, CN, halo; C&#x2013;Calkyl, C&#x2013;Chaloalkyl, COR, CONRR, NRCOR, NRR, OR, SR, SOR, S0Ror SONRR; Ris H, halo or C&#x2013;Calkyl; Ris H or C&#x2013;Calkyl; Rand Rare independently H or C&#x2013;Calkyl Ris hydrogen, optionally substituted phenyl or optionally substituted heterocycle; X is absent or is OCHor SCH; Xis absent or C&#x2013;Calk-di-yl; and Xis absent or is O, S, NH, NHSO, SONH or CH; or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity 

[object Object]

The present invention relates to a &#x3b2;3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g., for treating Type 2 diabetes and/or obesity 

&#x3b2;3 adrenergic agonists

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Indianapolis, IN, United States of America

Cynthia Darshini Jesudason