178372-32-2Relevant academic research and scientific papers
SUBSTITUTED 4-(1H-BENZIMIDAZOL-2-YL)[1,4]DIAZEPANES USEFUL FOR THE TREATMENT ALLERGIC DISEASES
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, (2008/06/13)
The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4] diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases
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, (2008/06/13)
The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease
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, (2008/06/13)
The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
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.
Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists
Burkholder, Timothy P.,Kudlacz, Elizabeth M.,Maynard, George D.,Liu, Xiao-Gao,Le, Tieu-Binh,Webster, Mark E.,Horgan, Stephen W.,Wenstrup, David L.,Freund, David W.,Boyer, Fred,Bratton, Larry,Gross, Raymond S.,Knippenberg, Robert W.,Logan, Deborah E.,Jones, Bryan K.,Chen, Teng-Man,Geary, Julie L.,Correll, Melinda A.,Poole, J. Chuck,Mandagere, Arun K.,Thompson, Thomas N.,Hwang, Kin-Kai
, p. 2531 - 2536 (2007/10/03)
We recently described the synthesis and characterization of MDL 105,212, a non peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors. Here we report the synthesis and structure-activity relationships for a series of analogs of MDL 105,212 with regards to: NK1 and NK2 receptor binding affinity, physical-chemical characterization; in vitro absorption potential; in vitro metabolic stability; and efficacy in a capsaicin-challenge conscious guinea pig model after oral administration.
