- 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
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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
- 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.
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p. 7602 - 7620
(2012/01/05)
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- TOLUENE SULFONIC ACID SALT OF A THERAPEUTIC COMPOUND AND PHARMACEUTICAL COMPOSITIONS THEREOF
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The present invention is directed to the tosylate salt of trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide (1): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), 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 comprising administering a therapeutically effective amount thereof.
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Page/Page column 7-8
(2008/12/07)
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