167261-59-8Relevant articles and documents
CARBOXYSUBSTITUTED CYCLIC CARBOXAMIDE DERIVATIVES
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, (2008/06/13)
The present invention relates to novel carboxy substituted cyclic carboxamide derivatives of formula (1), STR1 and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, coughs and bronchitis.
SUBSTITUTED PYRROLIDIN-3-YL-ALKYL-PIPERIDINES
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, (2008/06/13)
The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors
Burkholder, Timothy P.,Kudlacz, Elizabeth M.,Le, Tieu-Binh,Knippenberg, Robert W.,Shatzer, Scott A.,Maynard, George D.,Webster, Mark E.,Horgan, Stephen W.
, p. 951 - 956 (2007/10/03)
We have synthesized and identified MDL 105,212, a non-peptide tachykinin receptor antagonist that has high affinity for human NK1 ((IC50 = 3.11 nM) and NK2 (IC50 = 8.40 nM) receptors. The chemical synthesis of M