955360-05-1Relevant articles and documents
The discovery of quinoline based single-ligand human H1and H3receptor antagonists
Procopiou, Panayiotis A.,Ancliff, Rachael A.,Gore, Paul M.,Hancock, Ashley P.,Hodgson, Simon T.,Holmes, Duncan S.,Keeling, Steven P.,Looker, Brian E.,Parr, Nigel A.,Rowedder, James E.,Slack, Robert J.
, p. 5855 - 5859 (2016/12/06)
A novel series of potent quinoline-based human H1and H3bivalent histamine receptor antagonists, suitable for intranasal administration for the potential treatment of allergic rhinitis associated nasal congestion, were identified. Com
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis
Procopiou, Panayiotis A.,Browning, Christopher,Buckley, Jennifer M.,Clark, Kenneth L.,Fechner, Lise,Gore, Paul M.,Hancock, Ashley P.,Hodgson, Simon T.,Holmes, Duncan S.,Kranz, Michael,Looker, Brian E.,Morriss, Karen M. L.,Parton, Daniel L.,Russell, Linda J.,Slack, Robert J.,Sollis, Steven L.,Vile, Sadie,Watts, Clarissa J.
supporting information; experimental part, p. 2183 - 2195 (2011/06/10)
A series of potent phthalazinone-based human H1 and H 3 bivalent histamine receptor antagonists, suitable for intranasal administration for the potential treatment of allergic rhinitis, were identified. Blockade of H3 receptors is thought to improve efficacy on nasal congestion, a symptom of allergic rhinitis that is currently not treated by current antihistamines. Two analogues (56a and 56b) had slightly lower H1 potency (pA2 9.1 and 8.9, respectively, vs 9.7 for the clinical gold-standard azelastine, and H3 potency (pK i 9.6 and 9.5, respectively, vs 6.8 for azelastine). Compound 56a had longer duration of action than azelastine, low brain penetration, and low oral bioavailability, which coupled with the predicted low clinical dose, should limit the potential of engaging CNS-related side-effects associated with H 1 or H3 antagonism.
2-SUBSTITUTED 4-BENZYLPHTHALAZINONE DERIVATIVES AS HISTAMINE H1 AND H3 ANTAGONISTS
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Page/Page column 76, (2008/06/13)
The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis.