02-10-2014 дата публикации
Номер: US20140296241A1
Принадлежит:
The disclosure provides pharmaceutical preparations containing (2R,6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. (2R,6R)-hydroxynorketamine The disclosure also provides novel ketamine metabolite prodrugs. The disclosure provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain disorder (CRPS) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment. 57-. (canceled)11. A compound or salt of claim 9 , wherein{'sub': '1', 'Ris hydrogen or hydroxyl;'}{'sub': '3', 'Ris hydrogen or methyl;'}{'sub': 4', '5', '1', '2', '1', '2, 'Rand Rare each 0 to 2 substituents independently chosen from halogen, hydroxyl, amino, C-Calkyl, and C-Calkyl; and'}{'sub': '6', 'Ris hydrogen or methyl.'}12. A compound or salt of claim 11 , wherein{'sub': 2', '2', '2', '2', '2', '6', '6', '2', '1', '6', '2', '4', '0', '2', '3', '7', '0', '4', '0', '2', '0', '2', '2', '1', '4', '1', '4', '1', '6', '1', '4', '1', '2', '1', '2, 'Ris -ABwhere Ais a bond, —(C═O)O—, —S(O)—, —(S═O)NR—, or —(C═O)NR—, Bis C-Calkyl, C-Calkanoyl, (phenyl)C-Calkyl, (C-Ccycloalkyl)C-Calkyl, (heterocycloalkyl)C-Calkyl, (5- or 6-membered heteroaryl)C-Calkyl, or an amino acid covalently bound to Aby its C-terminus, each of which is substituted with from 0 to 4 substituents independently chosen from halogen, hydroxyl, amino, cyano, C-Calkyl, C-Calkoxy, C-Calkylester, mono- and di-(C-Calkyl)amino, C-Chaloalkyl, and C-Chaloalkoxy.'}1314-. (canceled)15. A compound or salt of claim 11 , where{'sub': 2', '2', '2', '6', '0', '2', '3', '7', '0', '4', '1', '4', '1', '4', '1', '4, 'Ais a bond or —(C═O)O— and Bis C-Calkyl, (phenyl)C-Calkyl, or (C-Calkyl)C-Calkyl, each of which is substituted with from 0 to 4 substituents independently chosen from halogen, hydroxyl, amino, cyano, C-Calkyl, C-Calkoxy, and mono- ...
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