583830-08-4Relevant academic research and scientific papers
Discovery of two clinical histamine H3 receptor antagonists: Trans - N -ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl] cyclobutanecarboxamide (PF-03654746) and trans -3-fluoro-3-[3-fluoro-4- (pyrrolidin-1-ylmethyl)phenyl]- N -(2-methy
Wager, Travis T.,Pettersen, Betty A.,Schmidt, Anne W.,Spracklin, Douglas K.,Mente, Scot,Butler, Todd W.,Howard, Harry,Lettiere, Daniel J.,Rubitski, David M.,Wong, Diane F.,Nedza, Frank M.,Nelson, Frederick R.,Rollema, Hans,Raggon, Jeffrey W.,Aubrecht, Jiri,Freeman, Jody K.,Marcek, John M.,Cianfrogna, Julie,Cook, Karen W.,James, Larry C.,Chatman, Linda A.,Iredale, Philip A.,Banker, Michael J.,Homiski, Michael L.,Munzner, Jennifer B.,Chandrasekaran, Rama Y.
experimental part, p. 7602 - 7620 (2012/01/05)
The discovery of two histamine H3 antagonist clinical candidates is disclosed. The pathway to identification of the two clinical candidates, 6 (PF-03654746) and 7 (PF-03654764) required five hypothesis driven design cycles. The key to success i
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: A novel potent antibacterial analog derived from hygromycin A
Le, Phuong T.,Brickner, Steven J.,Wade, Sarah K.,Brighty, Katherine,Monahan, Rhonda,Stone, Gregory G.,Girard, Dennis,Finegan, Steve,Duignan, Joan,Schafer, John,Maloney, Meghan,Zaniewski, Richard P.,Connolly, Ann G.,Liras, Jennifer,Bordner, Jon,Samardjiev, Ivan
scheme or table, p. 276 - 279 (2011/02/27)
SAR studies and optimization of various modified Hygromycin A fluoroalkyl ethers, which led to the discovery of the highly potent 4′-(2-cyclopropyl- 2-fluoroethyl ether) antibacterial CE-156811 (1) derived from truncation of the ribose ring and difluorination of the phenyl found in Hygromycin A, are discussed.
Histamine-3 receptor modulators
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Page/Page column 18, (2010/02/13)
This invention is directed to a compound of the formula I as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by modulating histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above.
