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Derivatives of piperidine NK1 Antagonists
专利权人:
OPKO HEALTH; INC.
发明人:
申请号:
ARP160100524
公开号:
AR103812A2
申请日:
2016.02.29
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
Claim 1: a compound of formula (1), or pharmaceutically acceptable Salts and / or solvates thereof,Where: r u00b9 and R u00b2 are each independently selected from the group consisting of H, alkyl, haloalquilo alkyl, substituted with one or more hydroxyl groups, alquinilo, - CN, - N ( u2082, r u2076)N - (r u2076) - S (O u2082) - N - (r u2076) alkyl, - C (o) - N - (r u2079) u2082, rent - cicloalquilen - CN, - CN, - Rent - or alkyl, - C (o) - (alkyl, - C = N - or u2075) - alkyl, - C (o) - N (r u2079) u2082, - C (o) - or - alkyl, - C (o) - Rent rent,- Rent - C (o) - or - alkyl - Rent - C (o) - N ( u2082 r u2079), or a compound of formula (2), (3), (4), (5) and (6), with the condition that at least one of r u00b9 and R u00b2 is - CN, or a compound of formula (2), (3),(4), (5) or (6); w IS = (- C = N - or r u2078); X is - C (o) - O - S (O u2082), and is selected from the group consisting ch u2082 - -, -, and - N - (r u2076) C (o) -,Under the condition that: (a) The nitrogen atom of N - (r u2076) - C (o) - is linked to X, and (b) IF r u00b9 and / or R u00b2 is a remainder formula (2) and is - or is not -, X - S (- O u2082) C; Z is - (r u2077) u2082 -, -, - N (r u2076)Or - or - r u00b3 is selected from the group consisting of H, alkyl - and ch u2082or u2075,; r u2074 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, heteroaryl, heterocicloalquilo, acyl,Aroilo, alquilsulfonilo, and arilsulfonilo; r u2075 is H or alkyl; r u2076 is selected from the group consisting of H, alkyl, cycloalkyl, aryl r u2077; each is independently H or alkyl; or each r u2077,Along with the carbon ring to which they go together, form a ring cicloalquileno; r u2078 is selected from the group consisting of H, alkyl, alkyl substituted with one or more hydroxyl groups,( u2082 r u2076) - n, N - (r u2076) - S (O u2082) - N - (alkyl, r u2076) - S (O u2082 aryl) - N (r u2076) -, - C (o) - N - (r u2076) alkyl, - C (o) - alkyl - or aryl, rent and - CN; r u2079 is selected from the grou
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