FIELD: pharmacology.
SUBSTANCE: in formula n=1 or 2; R1 and R2, independently of each other, are hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy or halogen; R3 is hydrogen or C1-4 alkyl optionally substituted with hydroxy; R4 is hydrogen or oxo; R5 and R6, independently of one another, are hydrogen, C(=O)OR7, C(=O)NR8R9, C1-4 alkyl, wherein the said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-member heterocyclic ring with 1-4 heteroatoms selected from O and N, wherein the said 5- or 6-member heterocyclic ring is optionally substituted with C1-4 alkyl or C(=O)R7; or R5 and R6 together with the carbon atom to which they are attached form =CH2 or 5- or 6-member heterocycloalkyl with 1-4 heteroatoms selected from O and N, wherein the said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are, independently of each other, hydrogen or C1-4 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a 5- or 6-membered heterocyclic ring with 1-4 heteroatoms selected from O and N. The invention also relates to a pharmaceutical composition, a method for prevention, treatment or alleviation of the severity of conditions accompanied by skin pruritus, application of the said compounds in the manufacture of a medicament for prevention, treatment or alleviation of the said diseases, and to intermediates of general formula wherein R10 is selected from the group consisting of hydrogen and C(O)OR14; R11 is selected from the group consisting of hydrogen and oxo; R12 and R13 are independently selected from the group consisting of hydrogen, C1-C4 alkyl, allyl and C(O)O(C1-C4alkyl); R14 is selected from the group consisting of C1-C4-alkyl; n is 1 or 2.
EFFECT: possibility to use the compounds for prevention, treatment or alleviation of conditions accompanied by skin pruritus.
27 cl, 3 dwg, 1 tbl, 122 ex
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Authors
Dates
2017-09-21—Published
2013-02-20—Filed