Eli Lilly and Company

Richard Todd Pickard

Robert Alan Gadski

Lisa Selsam Beavers

Cynthia Darshini Jesudason

Philip Arthur Hipskind

Takako Takakuwa

William Joseph Hornback

John D Sharp

Beth Ann Strifler

Ruth M Kramer

Freddie Craig Stevens

Don Richard Finley

Grant Mathews Vaught

Xue-Chiou C Choiu

Craig William Lindsley

Karen Lynn Lobb

Terry Patrick Finn

John M Schaus

Brian Morgan Watson

James Arthur Nixon

Serge Louis Boulet

Victor H Obungu

Malgorzata Donata Gonciarz

Terry Patrick Eli Lilly And Company Finn

Compounds are provided herein for inducing weight loss and for treating diabetes, dyslipidemia, NASH and/or obesity. Also provided are pharmaceutical compositions containing such compounds and therapeutic uses of such compounds and compositions, where such compounds act as GDF15 agonists with extended time of action and other advantageous properties.

Growth differentiation factor 15 agonist compounds and methods of using the same

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 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 substituted aryl alkylamine compounds of Formula (I) or pharmaceutically acceptable salts thereof which have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases 

Non-imidazole aryl alkylamines compounds as histamine H3 receptor antagonists, preparation and therapeutic uses

The invention provides a novel phospholipase A,enzyme, polynucleotides encoding such enzyme and methods for screening unknown compounds for anti-inflammatory activity mediated by the arachidonic acid cascade.

Human phospholipase A2 and related nucleic acid compounds

The invention provides a novel phospholipase A,enzyme, polynucleotides encoding such enzyme and methods for screening unknown compounds for anti-inflammatory activity mediated by the arachidonic add cascade.

The invention provides a novel phospholipase A.sub.2 enzyme, polynucleotides encoding such enzyme and methods for screening unknown compounds for anti-inflammatory activity mediated by the arachidonic acid cascade.

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Noblesville, IN, United States of America

Richard Todd Pickard