C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/078 (2006.01) A61K 38/05 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2054097
ABSTRACT OF THE DISCLOSURE A 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 suitable substituent excepting 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; R7 is hydrogen or suitable substituent; A is an amino acid residue excepting D-Trp, which may have suitable substituent(s); and Y is bond, lower alkylene or lower alkenylene, and a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical activities such as tachykinin antagonism, especially substance P antagonism, neurokinin A antagonism, neurokinin B antagonism, and the like. The compounds are useful for treating or preventing tachykinin mediated diseases, fox example respiratory diseases such as asthma, bronchitis, rhinites, 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 rhumatoid arthritis, osteoarthritis, and the like; pain or aches such as migraine, headache, toothache, cancerous pain, back pain, etc. The process of producing these compounds, pharmaceutical compositions containing them and their uses in treating the above diseases are also disclosed.
Hagiwara Daijiro
Matsuo Masaaki
Miyake Hiroshi
Fujisawa Pharmaceutical Co. Ltd.
Swabey Ogilvy Renault
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