5324-80-1Relevant articles and documents
Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain
Biswas, Kaustav,Aya, Toshihiro,Qian, Wenyuan,Peterkin, Tanya A.N.,Chen, Jian Jeffrey,Human, Jason,Hungate, Randall W.,Kumar, Gondi,Arik, Leyla,Lester-Zeiner, Dianna,Biddlecome, Gloria,Manning, Barton H.,Sun, Hong,Dong, Hong,Huang, Ming,Loeloff, Richard,Johnson, Eileen J.,Askew, Benny C.
scheme or table, p. 4764 - 4769 (2009/05/11)
We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modifications of the aryl moiety led to compound 26, both of which were efficacious in rabbit biochemical challenge and pain models.
Heterocyclic amines
-
, (2008/06/13)
Heterocyclic amines of the formula wherein Ar is a bicyclic or tricyclic aromatic group which is unsubstituted or which bears one or more substituents selected from halo, nitro and cyano groups and alkyl and alkoxy groups each of up to 4 carbon atoms; wherein X is a direct link or is --O--, --S--, --SO-- or --SO2 -- or has the formula --C(R3)=CH-- wherein R3 is hydrogen or alkyl of up to 4 carbon atoms; wherein A is straight or branched alkylene or alkenylene of 3 to 8 carbon atoms which may be interrupted by --O--, --S-- or --NH--; and wherein NR1 R2 is a cyclic amino group; or a pharmaceutically acceptable acid addition salt thereof, are of value for therapeutic use, particularly in the treatment of myocardial ischaemia and hypertension and in the treatment of fungal infections.