COMPOUNDS BASED ON BENZOXAZINE AND INDOLE, WITH ANTAGONISTIC EFFECT ON cysLT RECEPTOR Russian patent published in 2009 - IPC C07D265/36 C07D413/04 C07D413/10 C07D417/04 A61K31/538 A61K45/00 A61P11/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I-a), where R¹ and R², each independently, represent -COOR^A (where R^A is hydrogen or C_1-8 alkyl), -CONR^BSO₂R^C (where R^B is hydrogen or C_1-8 alkyl, R^C is C_1-8 hydrocarbon), -D-R¹ is -CO-(CH₂)₂-R¹, -CO-(CH₂)₃-R¹, -CO-(CH₂)₄-R¹ or C1-4alkylene-R¹; E is a bond or C1-4alkylene; ring formula represents a 3,4-dihydro-2H-1,4-benzoxazine or 1H-indole ring; V is , where R¹¹⁰ is hydrogen or C1-8 alkyl, and the arrow shows that it is bonded to ring A; the group with formula is a phenyl group, which can contain a group with formula , where ring 2 is a C5-10 mono- or bicyclic aromatic carbocyclic ring, which can be partially or completely saturated, spirobicyclic carbocyclic ring, or a carbocyclic ring bonded by a bridge bond; where W is -O-CH₂-, -O-(CH₂)₂, -O-(CH₂)₃, -O-(CH₂)₄, -O-(CH₂)₅, -CH₂-O, -(CH₂)₂-O-, -(CH₂)₃-O-, -(CH₂)₄-O-, -(CH₂)₅-O-, -O-(CH₂)₃-O-, -O-(CH₂)₄-O-, -O-(CH₂)₅-O-, C1-6 alkylene, its N-oxide, its salt or its solvate. The invention also relates to a pharmaceutical composition based on formula I-a compound and its use.

EFFECT: obtaining new derivatives of benzoxazine and indole, with antagonistic effect on cysLT₂ and which are useful for preventing and/or curing respiratory diseases, such as bronchial asthma, chronic obstructive lung diseases.

8 cl, 57 tbl, 261 ex