[EN] POLYSUBUNIT OPIOID PRODRUGS RESISTANT TO OVERDOSE AND ABUSE<br/>[FR] PROMÉDICAMENTS D'OPIOÏDES À SOUS-UNITÉS MULTIPLES RÉSISTANTS AUX SURDOSES ET AUX ABUS
申请人:ELYSIUM THERAPEUTICS INC
公开号:WO2018170465A1
公开(公告)日:2018-09-20
The invention provides compositions and methods for the treatment or prevention of pain. Compositions provided are resistant to overdose and abuse. Compositions provided comprise two or more different molecules, where each molecule comprises at least one GI enzyme-labile opioid agonist releasing subunit comprising an opioid agonist that is covalently linked to at least one GI enzyme inhibitor subunit.
POLYSUBUNIT OPIOID PRODRUGS RESISTANT TO OVERDOSE AND ABUSE
申请人:Elysium Therapeutics, Inc.
公开号:US20170100390A1
公开(公告)日:2017-04-13
The invention provides compositions and methods for the treatment or prevention of pain. The invention provides constructs whereby hydrolysis of the construct by a specified gastrointestinal enzyme directly, or indirectly, releases an opioid when taken orally as prescribed. The gastrointestinal enzyme mediated release of opioid from constructs of the invention is designed to be attenuated in vivo via a saturation or inhibition mechanism when overdoses are ingested. The invention further provides constructs that are highly resistant to oral overdose, chemical tampering, and abuse via non-oral routes of administration.
Quinolines and nitrogenated derivatives thereof substituted in 4-position by a piperazine-containing moiety and their use as antibacterial agents
申请人:——
公开号:US20040077656A1
公开(公告)日:2004-04-22
Piperazine derivatives, containing a quinoline analog moiety, of formula (I) and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammal, particularly in man.
Piperazine derivatives for treatment of bacterial infections
申请人:——
公开号:US20040077655A1
公开(公告)日:2004-04-22
Piperazine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
哌嗪衍生物及其药用可接受衍生物在哺乳动物,特别是人类的细菌感染治疗方法中有用。
Pyridine and pyrimidine derivatives
申请人:——
公开号:US20030216382A1
公开(公告)日:2003-11-20
The present invention provides compounds of formula (I)
1
wherein R
1
, R
2
, R
3
, R
4
and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.