Tetrahydro isoquinoline derivatives, preparation methods and...

C - Chemistry – Metallurgy – 07 – D

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C07D 217/06 (2006.01) A61K 31/472 (2006.01) A61K 31/4725 (2006.01) A61P 9/12 (2006.01) A61P 25/04 (2006.01) A61P 25/20 (2006.01) A61P 25/36 (2006.01) A61P 29/00 (2006.01) A61P 31/18 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 471/10 (2006.01)

Patent

CA 2657355

A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as k-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The subsutituents R1, R2, R3, R4 of general formula (I) are defined as the description: (see formula I) wherein R1 represents: (see formula II), (see formula III), (see formula IV), (see formula V), (see formula VI), (see formula VII), (see formula VIII), (see formula IX), (see formula X), (see formula XI), (see formula XII), (see formula XII), (see formula XIII), R2 each independently represents H, F, Cl, Br, C1-C4 alkyl, OR5, or NR6R7, or form 5,6-methylenedioxy, 6,7-methylenedioxy, or 7,8-methylenedioxy together; R3 and R4 each independently represent H, F, Cl, Br, trifluoromethyl, C1-C4 alkyl, OR5, NR8R9, or form 4,5-methylenedioxy, 5,6-methylenedioxy, or 6,7- methylenedioxy together; R5 represents H, C1-C4 alkyl, or allyl; R6 and R7 each independently represent H, and C1-C4 alkyl; R8 and R9 independently represent H, C1-C4 alkyl, and allyl.

L'invention porte sur: des dérivés de tétrahydro isoquinoline (I), leurs procédés de préparation, des médicaments les contenant, et leurs utilisations médicales, et notamment sur leurs utilisations en tant que récepteur opioïde k à action analgésique. Les groupes R1,R2,R3 et R4 de la formule générale (I) sont définis dans la description.

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