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2. 发明授权

US06211360B1 Ibogamine congeners 有权
标题翻译： Ibogamine同系物
公开(公告)号：US06211360B1
公开(公告)日：2001-04-03
申请号：US09011809
申请日：1998-08-31
申请人： Stanley D. Glick , Martin E. Kuehne
发明人： Stanley D. Glick , Martin E. Kuehne
IPC分类号： C07D48718
CPC分类号： C07D487/22 , A61K31/55
摘要： The present invention is directed to compounds having formula (1), wherein n is from 0 to 8; R1 is CH2OH, CH(OH)R5, CH2OR5, CO2R5, C(O)NH2, C(I)NHR5, C(O)NR5R6, C(O)NHNH2, C(O)NHNHR5, C(O)NHNR5R6, C(O)NR5NH2, C(O)NR5NHR6, C(O)NR5NR6R7, C(O)NHNH(C(O)R5), C(O)NHNR5(C(O)R6) C(O)NR5NH(C(O)R6), C(O)NR5NR6(C(O)R7), CN, or C(O)R5; R2 is H, unsubstituted or substituted alkyl, YH, YR8, YC(O)R8, C(O)YR8, C(O)NH2, C(O)NHR8, C(O)NR8R9, NH2, NHR8, NR8R9, NHC(O)R8, or NR8C(O)R9; R3 and R4 are the same or different and are selected from the group consisting of H, halogens, unsubstituted or substituted alkyl, OH, OR10, NH2, NHR10, NR10R11, NHC(O)R10, or NR10C(O)R11; R5, R6, R7, R8, R9, R10, and R11 are the same or different and are selected from the group consisting of unsubstituted alkyl and substituted alkyl and substituted alkyl; R12 is selected from the group consisting of J, unsubstituted alkyl, and substituted alkyl; and Y is O or S; provided that when n is O, R2 is selected from the group consisting of H, substituted alkyl, and unsubstituted alkyl; and pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of subjects addicted to opiates and stimulants and have reduced side effects relative to other ibogamine congeners.
摘要翻译：本发明涉及具有式（1）的化合物，其中n为0至8; R 1是CH 2 OH，CH（OH）R 5，CH 2 OR 5，CO 2 R 5，C（O）NH 2，C（I）NHR 5，C（O）NR 5 R 6，C（O）NHNH 2，C（O）NHNHR 5，C（O）NHNR 5 R 6， C（O）NR 5 NH 2，C（O）NR 5 NR 6，C（O）NR 5 NR 6 R 7，C（O）NHNH（C（O）R 5），C（O）NHNR 5（C（O）（O）R 6），C（O）NR 5 NR 6（C（O）R 7），CN或C（O） R2是H，未取代或取代的烷基，YH，YR8，YC（O）R8，C（O）YR8，C（O）NH2，C（O）NHR8，C（O）NR8R9，NH2，NHR8，NR8R9，NHC （O）R 8或NR 8 C（O）R 9; R 3和R 4相同或不同，并且选自H，卤素，未取代或取代的烷基，OH，OR 10，NH 2，NHR 10，NR 10 R 11，NHC（O）R 10或NR 10 C（O）R 11; R5，R6，R7，R8，R9，R10和R11相同或不同，选自未取代的烷基和取代的烷基和取代的烷基; R 12选自J，未取代的烷基和取代的烷基; Y为O或S; 条件是当n是O时，R 2选自H，取代的烷基和未被取代的烷基; 和药学上可接受的盐

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