Analogues of buprenorphine and its use in the treatment of Pain

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专利权人:

PURDUE PHARMA L.P.

发明人:

申请号：

ARP110103431

公开号：

AR083062A1

申请日:

2011.09.20

申请国别(地区):

AR

年份:

2013

代理人:

摘要：

Similar compounds of the formula (1) of buprenorphine. The compounds are useful for treating Pain, constipation, and other conditions Modulated by the activity of Opioid Receptors and orl-1.Claim 1: a compound characterized by the formula (1) wherein R1 is selected from Hydrogen, alkyl alquenil C1 - C2 - 10, - 12, - 12 alquinil C1, C2, C3 cicloalquil alkoxy - 10, - 12, - 12 cicloalquil cicloalquenil C4, C1 - C3 - 12 alkyl - 6 - cicloalquenil C1 - C4 - 12 - 6 - alkyl -, aryl (5 to 1 2 - (aryl), member 5 to 12 members) - alkyl of C1 - 6 - - heteroaryl (5 to 12 members)Heteroaryl (5 to 12 members) - alkyl of C1 - 6 - - heterocycle (3 to 12 members), heterocycle (3 to 12 members) - C1 - 6 - alkyl, phenyl and benzyl； each of which is optionally substituted with 1, 2 or 3 substituents selected from the Group independently which consists of alkyl C1 - 6 Oh, Halo (Halo) C, - 3, - 2, - ch (Halo) CH2 (Halo) - alkyl - coor7 C1 - 6, - coor7, NH2, NH - alkyl - C1 - 6- nr9r10, - CN, - conr9r10 nr9cor10 SR11, -, -, - carboc u00edclico ring (5 to 12 members) - heterocycle (5 to 12 members), phenyl and benzyl； R2 and R8 are each independently Hydrogen, alkyl alquenil C1 - C2 - 10, - 12, alquinil alkoxy C1 C2 - 12, - 10, - (och2ch2 S - O - (alkyl) - 6 - (C1), ch2ch2o) S - (alkyl C1 - 6) NH, NH2, - (alkyl C1 - CN, - 6), conr5r6 C1 -, alkyl - 6 - CO - nr5r6, coor7,C1 - alkyl - 6 - CO or7, 6 - alkoxy - C1 - C3 - cicloalquil coor7, - 12, - 12 - cicloalquil C3 alkyl of C1 - C4 cicloalquenil - 6, - 12, - 12 - cicloalquenil C4 alkyl C1 - C6, bicicloalquil - 14 - 14 - bicicloalquil C1 - C6 alkyl 6 - 20 tricicloalquil tricicloalquil C8 C8 alkyl -, 20 - - 6 - - bicicloalquenil C1, C7 - 14, bicicloalquenil C7 - 14 - alkyl - 6 - tricicloalquenil C1, C8 - 20 - 20, tricicloalquenil C8 alkyl C1 - 6 -- aryl (5 to 12 members), aril (5 to 12 members) - alkyl of C1 - 6 - bicyclic Ring System (7 to 12 members), the bicyclic Ring System (7 to 12 members) - C1 - 6 - alkyl -, aryl bicyclic (7 to 12 members

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