An enantiomerically pure opioid diarylmethylpiperazine and...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 409/06 (2006.01) A61K 31/496 (2006.01) C07D 333/20 (2006.01)

Patent

CA 2459577

(-)3-((S)-((2S,5R)-4-Allyl-2,5-dimethyl-l-piperazinyl)(3-thienyl)methyl)phenol and pharmaceutically acceptable esters or salts thereof, in essentially enantiomerically pure form have utility as receptor-binding species, e.g., as therapeutic agents for mediating analgesia; as co-administered agents with various other bioactive compositions, including anesthetics, barbiturates, analgesics, etc., for reducing, treating, reversing or preventing drug- mediated respiratory depression that may be directly or indirectly caused by use of such various bioactive compositions; as a conjugate in agonist/antagonist pairs for verifying/assaying receptor and neurotransmitter function; and as a therapeutic agent having utility in combating drug addiction, cardiac disorders, alcohol addiction, drug overdose, cough, lung edema, diarrhea, respiratory, and gastro-intestinal disorders.

L'invention concerne (-)3-((S)-((2S,5R)-4-Allyl-2,5-dimethyl-l-piperazinyl)(3-thienyl)methyl)phenol et des esters ou des sels de ce composé pharmaceutiquement acceptables, sous forme énantiomère essentiellement pure. On utilise ce composé comme espèce de liaison de récepteur, par exemple, comme agent thérapeutique pour induire une analgésie; comme agent co-administré avec d'autres compositions bioactives variées, notamment des substances anesthésiques, des barbituriques, des analgésiques, etc., afin de réduire, de traiter, d'inverser ou de prévenir une dépression respiratoire induite par un médicament pouvant directement ou indirectement être provoquée par l'utilisation des compositions bioactives variées; comme conjugué dans des paires agonistes/antagonistes afin de contrôler/doser une fonction de récepteur et de neurotransmetteur; et comme agent thérapeutique servant à combattre l'addiction à la drogue, les troubles cardiaques, l'addiction à l'alcool, une surdose de drogue, la toux, l'oedème des poumons, la diarrhée, et les troubles respiratoires et gastro-intestinaux.

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