Nose drop containing condensed pyridazine

A - Human Necessities – 61 – K

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Details

A61K 31/5025 (2006.01) A61K 9/00 (2006.01) A61K 9/08 (2006.01) A61P 11/02 (2006.01) A61P 37/08 (2006.01) A61P 43/00 (2006.01) C07D 487/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2390919

Nasal drops containing compounds of general formula (I), salts of the same, or prodrugs thereof and exhibiting excellent preventive and therapeutic effects against allergic rhinitis and so on: wherein Ar1 and Ar2 are each an aromatic group, or Ar1 and Ar2 together with the carbon atom adjacent thereto may form a fused-ring group; B is a nitrogenous heterocycle; X and Y are each a free valency, O, S(O)p (wherein p is 0 to 2), NR4 (wherein R4 is H or the like), or a divalent straight-chain lower hydrocarbon group which may be interrupted by 1 to 3 heteroatoms; A is N or CR7 (wherein R7 is H or the like); R1, R2 and R3 are each H or the like; and R8 is H or the like, with the proviso that B is not a heterocycle of formula:(II)(wherein n is 0 to 1).

L'invention concerne des gouttes nasales contenant les composés représentés par la formule générale (I), les sels ou les promédicaments desdits composés, qui présentent d'excellents effets préventifs et thérapeutiques contre la rhinite spasmodique, etc. Dans la formule (I), Ar?1¿ et Ar?2¿ représentent chacun un groupe aromatique, ou Ar?1¿ et Ar?2¿ forment, avec l'atome de carbone adjacent, un groupe à cycle condensé; B désigne un hétérocycle azoté; X et Y représentent chacun une valence libre, O, S(O)¿p? (p étant compris entre 0 et 2), NR?4¿ (où R?4¿ désigne H ou analogue), ou un groupe hydrocarbure inférieur divalent à chaîne droite pouvant être entrecoupé par 1-3 hétéroatomes; A représente N ou CR?7¿ (R?7¿ désignant H ou analogue); R?1¿, R?2¿ et R?3¿ désignent chacun H ou analogue; et R?8¿ représente H ou analogue, à condition que B ne soit pas un hétérocycle représenté par la formule (II) (où n est compris entre 0 et 1).

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