676445-27-5Relevant academic research and scientific papers
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents
Ahmad, Saleem,Ngu, Khehyong,Miller, Keith J.,Wu, Ginger,Hung, Chen-pin,Malmstrom, Sarah,Zhang, Ge,O'Tanyi, Eva,Keim, William J.,Cullen, Mary Jane,Rohrbach, Kenneth W.,Thomas, Michael,Ung, Thao,Qu, Qinling,Gan, Jinping,Narayanan, Rangaraj,Pelleymounter, Mary Ann,Robl, Jeffrey A.
scheme or table, p. 1128 - 1133 (2010/06/15)
Agonists of the 5-HT2C receptor have been shown to suppress appetite and reduce body weight in animal models as well as in humans. However, agonism of the related 5-HT2B receptor has been associated with valvular heart disease. Synthesis and biological evaluation of a series of novel and highly selective dihydroquinazolinone-derived 5-HT2C agonists with no detectable agonism of the 5-HT2B receptor is described. Among these, compounds (+)-2a and (+)-3c were identified as potent and highly selective agonists which exhibited weight loss in a rat model upon oral dosing.
Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists
Kuduk, Scott D.,Di Marco, Christina N.,Chang, Ronald K.,Wood, Michael R.,Schirripa, Kathy M.,Kim, June J.,Wai, Jenny M. C.,DiPardo, Robert M.,Murphy, Kathy L.,Ransom, Richard W.,Harrell, C. Meacham,Reiss, Duane R.,Holahan, Marie A.,Cook, Jacquelynn,Hess, J. Fred,Sain, Nova,Urban, Mark O.,Tang, Cuyue,Prueksaritanont, Thomayant,Pettibone, Douglas J.,Bock, Mark G.
, p. 272 - 282 (2007/10/03)
A series of biphenylaminocyclopropane carboxamide based bradykinin B 1 receptor antagonists has been developed that possesses good pharmacokinetic properties and is CNS penetrant. Discovery that the replacement of the trifluoropropionamide in t
2-(biarylalkyl)amino-3-(fluoroalkanoylamino)pyridine derivatives
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Page/Page column 15, (2010/11/30)
Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
