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Title:
1 - PHENYLMORPHOLINE DERIVATIVES AS HYDROXYBUPROPION ANALOGUES FOR TREATING DRUG DEPENDENCE
Document Type and Number:
WIPO Patent Application WO/2011/146821
Kind Code:
A3
Abstract:
The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepbephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.

Inventors:
CARROLL F IVY (US)
BLOUGH BRUCE E (US)
NAVARRO HERNAN A (US)
MASCARELLA S WAYNE (US)
MURESAN ANA ZAMFIRA (US)
DAMAJ M IMAD (US)
LUKAS RONALD J (US)
Application Number:
PCT/US2011/037312
Publication Date:
January 12, 2012
Filing Date:
May 20, 2011
Export Citation:
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Assignee:
RES TRIANGLE INST (US)
CARROLL F IVY (US)
BLOUGH BRUCE E (US)
NAVARRO HERNAN A (US)
MASCARELLA S WAYNE (US)
MURESAN ANA ZAMFIRA (US)
DAMAJ M IMAD (US)
LUKAS RONALD J (US)
International Classes:
C07D265/32; A61K31/5375; A61P25/24
Domestic Patent References:
WO2001062257A22001-08-30
WO2000042030A12000-07-20
Foreign References:
US20100016312A12010-01-21
Other References:
LUKAS, RONALD J.: "Synthesis and Characterization of in Vitro and in Vivo Profiles of Hydroxybupropion Analogues: Aids to Smoking Cessation", JOURNAL OF MEDICINAL CHEMISTRY , 53(12), 4731-4748 CODEN: JMCMAR; ISSN: 0022-2623, vol. 53, no. 12, 28 May 2010 (2010-05-28), XP002647769
CARROLL, F. IVY ET AL: "Synthesis of 2-(Substituted Phenyl)-3,5,5-trimethylmorpholine Analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine", JOURNAL OF MEDICINAL CHEMISTRY , 54(5), 1441-1448 CODEN: JMCMAR; ISSN: 0022-2623, 14 February 2011 (2011-02-14), XP002647770
Attorney, Agent or Firm:
GORCZYNSKI, Jessica L. (PLLCP.O. Box 703, Atlanta Georgia, US)
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