Eli Lilly and Company

Robert Alan Gadski

Lisa Selsam Beavers

Richard Todd Pickard

Cynthia Darshini Jesudason

Philip Arthur Hipskind

Takako Takakuwa

William Joseph Hornback

Don Richard Finley

Freddie Craig Stevens

Thomas F Bumol

Grant Mathews Vaught

Craig William Lindsley

Karen Lynn Lobb

Terry Patrick Finn

John M Schaus

Brian Morgan Watson

James Arthur Nixon

Serge Louis Boulet

Barbara J Weigel

Joann Strnad

J Richard Sportsiman

Amy E Hamilton

Terry Patrick Eli Lilly And Company Finn

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 present invention discloses novel chimeric monoclonal antibodies, directed against proteoglycans of human melanoma cells, having antigen-specific variable regions of defined amino acid sequences. DNA constructs for the light and heavy chain variable regions comprising the novel antibodies of the invention are provided. Eukaryotic host cells capable of expression of the chimeric antibodies and comprising the novel chimeric antibody-encoding DNA constructs are also provided.

Chimeric antibodies directed against a human glycoprotein antigen

The present invention comprises novel recombinant DNA compounds which encode the .about.40,000 dalton adenocarcinoma antigen recognized by monoclonal antibody KS 1/4. Eukaryotic and prokaryotic expression vectors have been constructed that comprise novel KSA-encoding DNA and drive expression of KSA when transformed into an appropriate host cell. The novel expression vectors can be used to produce KSA derivatives, such as non-glycosylated KSA, and to produce KSA precursors, such as nascent KSA, and to produce subfragments of KSA. The recombinant-produced KSA is useful for the diagnosis, prognosis and treatment of disease states including adenocarcinomas of the lung, prostate, breast, ovary and colon/rectum; and for the creation of novel antibodies for treatment or diagnosis of the above.

Vectors and DNAS for expression of a human adenocarcinoma antigen

The present invention comprises novel recombinant DNA compounds which encode monoclonal antibody KS1/4 and chimeric derivatives of monoclonal antibody KS1/4. Eukaryotic expression vectors have been constructed that comprise novel KS1/4-encoding DNA and drive expression of KS1/4 when transformed into an appropriate host cell. The novel expression vectors can be used to create modified and chimeric derivatives of KS1/4. The recombinant-produced KS1/4, KS1/4 derivatives and KS1/4 chimeras are useful for the diagnosis, prognosis and treatment of disease states including adenocarcinoma.

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Indianapolis, IN, United States of America

Robert Alan Gadski