JOHN AITKEN GRAHAM,ALAN JAMES BAILLIE,KEVIN RICHARD WARD,THOMAS PEACOCK
申请号：
ARP130101779
公开号：
AR092008A1
申请日:
2013.05.22
申请国别(地区):
AR
年份:
2015
代理人:
摘要：
Claim 1: A composition comprising at least one benzodiazepine comprising at least one carboxylic acid ester group or a pharmaceutically acceptable salt thereof, characterized in that the composition a) comprises at least one pharmaceutically acceptable hygroscopic excipient, and / or b) the Composition is at least partly amorphous. Claim 2: A composition according to claim 1, characterized in that benzodiazepine is a compound according to formula (1) wherein W is H, a branched or straight chain C₁₋₄ alkyl； X is CH₂,NH, or NCH₃；N is 1 or 2, O / c832222；m is 0 or 1； Z is O； p is 0 or 1； R¹ is a straight chain C₁₋₇ alkyl, a C₃₋₇ branched chain alkyl, a C₁₋₄ haloalkyl,One c8323-83318327a,1. Arilo, heteromorphic arilo, aralquilo or heteromorphic aralquilo； R 2 is phenyl, 2-Halophenyl or 2-pyridine, R3 is h, Cl, Br, F, I, cf8323 or no832222；(i) R83088eh, a c83318324o or a dialect carat, together with r83099 and r8310c, represents a single oxygen or S atom, which is connected with diazepina ring through duplex, P is zero or 1； or (II) r830808 and r83099 are added together in diazepina ring, representing nhr831183； 1. Lease of c83218331 and 83242431；Calcium hydroxide c83216c831832424；a. Independently add halogen, tar c83321i833183248pillo or tar c83321i833183248midazilo and P to zero； or (III) r83408；R83099a and r8310a form a group - cr831222 = U-V = where c831222 is hydrogen, c83218331a / c834a or c83218331a / c8332323；U is N or CR⁹ where R⁹ is H, C₁₋₄ alkyl,e. Hidroxialquilo c83216c83183223 or alcoxi c83218c833124；V is n or h, P is zero. 11. Characteristic 11: the composition in accordance with characteristic 9, which is characterized by remazolam besilato as the salt of benzodiazepine.Reivindicación 1: Una composición que comprende al menos una benzodiazepina que comprende al menos un grupo éster de ácido carboxílico o una sal farmacéuticamente aceptable de la misma, caracterizada porque la composición a) comprende al menos un excipiente higroscópico farmacéuticamente
