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Benzodiazepine derivatives as CCK2 / gastrin receptor antagonists
专利权人:
Trio Medicines Limited
发明人:
BOYCE, Malcolm James,THOMSEN, Liv,GILBERT, Donald Alan,WOOD, David
申请号:
ES15749865
公开号:
ES2768752T3
申请日:
2015.08.07
申请国别(地区):
ES
年份:
2020
代理人:
摘要:
A pharmaceutical composition comprising a compound of formula (A) ** Formula ** or a pharmaceutically acceptable salt thereof, wherein, R1 and R2 are each, independently, H or C1-3 aliphatic, halo or C1- haloaliphatic 3, or wherein R1 and R2 together with the intermediate carbon atom to which they are attached form a C3-6 carbocyclic structural unit; L is a bond or C1-3 alkylene; R3 is -OR6 or -SR6; W and X are independently hydrogen, halo, C1-8 alkyl or C1-8 alkoxy; and R4 and R5 are both, independently, a monocyclic aryl or heteroaryl, optionally substituted with one or more substituents independently selected from halo, hydroxy, amino, nitro, carboxyl, carboxamido, cyano, -SO3H, and optionally substituted C1-8 alkyl, alkoxy C1-8, C1-8 alkylamino or di (C1-8 alkyl) amino; and R6 is hydrogen or alkyl (preferably methyl); or the H of R3 (-OH or -SH) is replaced by a -C (O) R moiety, wherein R is an optionally substituted aliphatic, heteroaliphatic, aromatic or heteroaromatic moiety; or the H of -OH or -SH of R3 is replaced by -P (O) (OH) 2, -P (O) (O (C1-6) alkyl) 2, an alkylcarbonyloxyalkyl, N- (C1-6) alkoxycarbonylaminomethyl, succinoyl, or an α-aminoalkylcarbonyl; and optionally one or more pharmaceutically acceptable excipients; where aliphatic refers to a substituted or unsubstituted straight chain, branched or cyclic hydrocarbon, which is fully saturated or contains one or more units of unsaturation, but is not aromatic, where aliphatic groups include alkyl groups substituted or unsubstituted linear, branched or cyclic alkenyl, alkynyl, and hybrids thereof, such as (cycloalkyl) alkyl, (cycloalkenyl) alkyl or (cycloalkyl) alkenyl; "Heteroaliphatic" refers to an aliphatic group in which one or more carbon atoms are replaced by a nitrogen (N), oxygen (O), or sulfur (S) atom; aromatic refers to a C6-14 aromatic hydrocarbon, comprising one to three rings, each of which is optionally substituted, and in which two adjacent substituents on an aryl ring can be taken to
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