Piperazine derivatives

Details Piperazine derivatives Piperazine derivatives

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 241/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/14 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 473/00 (2006.01)

Patent

CA 2136712

There are described compounds of the following general formula: Image wherein X is carbony or sulfonyl; Y is bond or lower alkylene; R1 is halogen, lower alkyl, halo(lower)alkyl, aryloxy, nitro or amino which may have 1 or 2 and same or different substituent(s) selected from lower alkyl, acyl and lower alkanesulfony; R2 is aryl or an aromatic hetero(mono- or bi-)cyclic group, and each of which may have 1, 2 or 3 suitable substituent(s); R3 is hydrogen or lower alkyl; R4 is (i) a group of the formula -SO2-R5 in which R5 is lower alkyl or aryl optionally substituted with lower alkyl or lower alkoxy, (ii) a group of the formula Image in which R6 is aryl optionally substituted with lower alkyl or lower alkoxy, or (iii) a group of the formula -A-(Z)p in which A is bond, lower alkylene, lower alkenylene or lower alkynylene Z is hydrogen, halogen, hydroxy, nitrile, amino, cyclo(lower)alkyl, aryl, arloxy, acyl, acylamino, lower alkanesulfonylamino, arysulfonylamino or an aromatic hetero(mono- or bi-)cyclic group, and each of the cyclic group may have 1, 2 or 3 suitable substituent(s), and p is 1, 2 or 3; and n is 0, 1 or 2; provided that when n or p is more than 1, these R1 and Z may be the same or different group respectively; or its pharmaceutically acceptable salt. The preparation of these compounds, pharmaceutical compositions containing them and their use as a medicament 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, bronchitis, 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 arthritis, osteoarthritis, and the like, pains or aches (e.g. migraine, headache, toothache, cancerous pain, back pain, etc.); and the like in human beings and animals.

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