C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 413/12 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 215/26 (2006.01) C07D 237/28 (2006.01) C07D 239/74 (2006.01) C07D 241/42 (2006.01) C07D 253/08 (2006.01) C07D 253/10 (2006.01) C07D 257/12 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07F 7/18 (2006.01) C07K 5/062 (2006.01)
Patent
CA 2122236
Compounds of the formula: (See formula I) wherein X1 is N or C-R6, X2 is N or C-R7, X3 is N or C-R8, R1 is hydrogen or halogen, R2 is halogen, R3 is hydrogen, nitro, amino optionally having suitable substituent(s) or a heterocyclic group optionally having suitable substituent(s), R4 and R5 are each hydrogen or halogen, R6 and R8 are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy, R7 is hydrogen or lower alkyl, A is lower alkylene, and Q is O or N-R9, in which R9 is hydrogen or acyl, provided that R3 is not hydrogen when X1 is C-R6, in which R6 is hydrogen, and pharmaceutically acceptable salts thereof. These compounds are active as, bradykinin antagonists. Processes for preparation therein, pharmaceutical compositions containing same and methods of using them in the prevention and/or the treatment bradykinin and its analogs mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like in humans or animals are also disclosed.
Abe Yoshito
Inoue Takayuki
Kayakiri Hiroshi
Oku Teruo
Satoh Shigeki
Astellas Pharma Inc.
Fujisawa Pharmaceutical Co. Ltd.
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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