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ANTAGONISTS OF TRPV1, CONTAINING DIHYDROXY GROUP AS SUBSTITUTE, AND THEIR USE
专利权人:
PURDYU FARMA El. Pi.
发明人:
TAFESS Lejki (US),ТАФЕСС Лейки (US),ANDO Shigeru (JP),АНДО Шигеру (JP),KUROSE Norijuki (JP),КУРОСЕ Норийуки (JP),TAFESS Lejki,ТАФЕСС Лейки,ANDO Shigeru,АНДО Шигеру,KUROSE Norijuki,КУРОСЕ Норийуки
申请号:
RU2014101255
公开号:
RU0002621708C2
申请日:
2012.06.21
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, in which R1 represents -halo or -CF3; R4 represents -H or -CH3; each of R8 and R9 independently represents -H, -halo, -CH3 or -OCH3, each halo independently represents -F, -Cl, -Br or -I; and m means an integer of 0 or 1; (1) provided that if R4 represents -H, the m means 1; and (2) provided that if R4 represents -H and the carbon atom in the position a of the a-b bond is in (S)-configuration, the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group, a (S)-3-methyl group or a (R)-3-methyl group; (3) provided that if R4 represents -H, the carbon atom in position a of the a-b bond is in (S)-configuration, R8 represents -H and R9 represents -halo, then the methyl group connected to piperazinonyl ring represents a (R)-3-methyl group; (4) provided that if R4 represents -H, the carbon atom in position a of the a-b bond is in (S) configuration, R8 represents -F and R9 represents -F, then the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group or a (S)-3-methyl group; and (5) provided that if R4 represents -CH3, each of the carbon atoms in positions a and c and the a-b bond and the c-d bond is in (S) configuration,R8 represents -H, R9 represents -halo, and m means 1, the methyl group connected to piperazinonyl ring is a (S)-3-methyl group or a (R)-3-methyl group. Invention also relates to a compound of formula (II) or a pharmaceutically acceptable salt thereof, a specific compound of formula (Ia) or a pharmaceutically acceptable salt thereof and / or a co-crystal of fumaric acid. Invention also relates to specific compounds of formula (Ib) or a pharmaceutically acceptable salt thereof. The compounds as per invention are intended to inhibit the function of TRPV1 in a cell and to treat pain, pain associated with osteoarthritis, osteoarthritis, urinary incontinence (UI), ulcer, inflammatory bowel disease (
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