C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/5.06, 167/10
C07K 5/06 (2006.01) A61K 38/05 (2006.01) C07K 5/02 (2006.01) C07K 5/068 (2006.01) C07K 5/072 (2006.01) C07K 5/078 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2015359
ABSTRACT Compound of the formula: Image wherein R1 is lower alkyl, aryl, arylamino, pyridyl, pyrrolyl, pyrazolopyridyl, quinolyl, or a group of the formula : Image wherein the symbol of a line and dotted line is a single bond or a double bond, X is CH or N, and Z is O, S or NH, each of which may have suitable substituent(s); R2 is hydrogen or lower alkyl R3 is hydrogen or hydroxy; R4 is lower alkyl which may have suitable substituent(s), and R5 is ar(lower)alkyl which may have suitable substituent(s) or pyridyl(lower)alkyl, or R4 and R5 are linked together to form benzene-condensed lower alkylene; A is an amino acid residue excepting D-Trp, which may have suitable substituen-t(s); and Y is bond, lower alkylene or lower alkenylene, and pharmaceutically acceptable salts thereof. Pro- cesses for the preparation of these compounds, pharma- ceutical compositions containing them, and their uses as medicines are also disclosed These compounds are useful as tachykinin antagonist, especially substance P antagonist, neurokinin A antagonist or neurokinin B antagonist, for treating or preventing tachykinin mediated diseases, for example, respiratory diseases such as asthma, rhinitis, cough, expectoration, and the like; ophthalmic diseases such as conjunctivitis, vernal conjunctivitis, and the like; cutaneous diseases such as contact dermatitis, atopic dermatitis, urticaria, and other eczematoid dermatitis, and the like; inflammatory diseases such as rheumatoid arthri- tis, and the like; pains or aches (e.g., migraine, headache, toothache, cancerous pain, etc.); and the like in human being or animals.
Hagiwara Daijiro
Matsuo Masaaki
Miyake Hiroshi
Fujisawa Pharmaceutical Co. Ltd.
Swabey Ogilvy Renault
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