343564-44-3Relevant articles and documents
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ETA antagonists
Jae,Winn,Von Geldern,Sorensen,Chiou,Nguyen,Marsh,Opgenorth
, p. 3978 - 3984 (2001)
The synthesis and structure-activity relationships (SAR) of a series of pyrrolidine-3-carboxylic acids as endothelin antagonists are described. The data shows an increase in selectivity when the methoxy of Atrasentan (ABT-627) is replaced with methyl, and the benzodioxole is replaced with dihydrobenzofuran. Adding a fluorine further increases the binding activity and provides a metabolically stable and orally bioavailable ETA-selective antagonist.
KCNQ2-5 CHANNEL ACTIVATOR
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Paragraph 0590-0592, (2017/08/26)
The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 cha
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors
Cheng, Hengmiao,Lundy DeMello, Kristin M.,Li, Jin,Sakya, Subas M.,Ando, Kazuo,Kawamura,Kato, Tomoki,Rafka, Robert J.,Jaynes, Burton H.,Ziegler, Carl B.,Stevens, Rod,Lund, Lisa A.,Mann, Donald W.,Kilroy, Carolyn,Haven, Michelle L.,Nimz, Erik L.,Dutra, Jason K.,Li, Chao,Minich, Martha L.,Kolosko, Nicole L.,Petras, Carol,Silvia, Annette M.,Seibel, Scott B.
, p. 2076 - 2080 (2007/10/03)
The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure-activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrated a ca
Sulfamoylheteroaryl pyrazole compounds as anti-inflammatory/analgesic agents
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, (2008/06/13)
This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is NH2; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
