Use of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
a technology of galr3 receptor and antagonist, which is applied in the direction of heterocyclic compound active ingredients, drug compositions, biocides, etc., can solve the problems of inflicting substantial morbidity and psychosocial impairment on its sufferers, loss of interest in life, and underdiagnosis and undertreatmen
Inactive Publication Date: 2007-03-08
KONKEL MICHAEL +2
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Problems solved by technology
Depression is the most common of mental disorders and yet is often underdiagnosed and undertreated, inflicting substantial morbidity and psychosocial impairment on its sufferers.
The key features of depressive illness are a markedly gloomy mood in which there is a loss of interest in life, and general feelings of hopelessness and worthlessness.
The “blackness” of the presentation in the depressed patient is most often accompanied by severe motor retardation with profound sleep and appetite disturbance and suicidal ideation.
Furthermore, depressive illness can also present in a highly anxious or agitated state.
However, SSRIs have largely displaced TCAs because of side effects associated with TCAs and the need to monitor EKG and plasma drug concentration.
Although the SSRIs are viewed as an improvement over other antidepressants, they are not without their clinical problems.
However, it is clear from the issues raised earlier relating to the efficacy and side-effect profile of SSRIs and for that matter the more widely prescribed benzodiazapines, there still exists a real medical need for novel approaches for the treatment of anxiety and depression.
Consequently, many past studies have only measured or scored immobility after the administration of the test agent.
Unfortunately, this method does not score any other active behaviors that may be produced by potential antidepressants.
In general, these tests lack ethological validity.
Method used
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example 91
3-[(2-METHOXYPHENYL)IMINO]-1-PHENYL-1,3-DIHYDRO-2H-INDOL-2-ONE
example 92
1-PHENYL-3-[[3-(TRIFLUOROMETHYL)PHENYL]IMINO]-1,3-DIHYDRO-2H-INDOL-2-ONE
example 93
3-[(3-METHYLPHENYL)IMINO]-1-PHENYL-1,3-DIHYDRO-2H-INDOL-2-ONE
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Abstract
This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.
Description
[0001] This application is a continuation-in-part and claims priority of U.S. Ser. No. 10 / 214,873, filed Aug. 7, 2002, which is a continuation-in-part and claims priority of U.S. Ser. No. 10 / 066,175, filed Jan. 31, 2002, which claims the benefit of U.S. Provisional Application No. 60 / 265,586, filed Jan. 31, 2001, the contents of which is incorporated by reference into the subject application.BACKGROUND OF THE INVENTION [0002] Throughout this application, various publications are referenced in parentheses by author and year. Full citations for these references may be found at the end of the specification immediately preceding the claims. The disclosures of these publications in their entireties are hereby incorporated by reference into this application to describe more fully the art to which this invention pertains. [0003] Depression is the most common of mental disorders and yet is often underdiagnosed and undertreated, inflicting substantial morbidity and psychosocial impairment on...
Claims
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IPC IPC(8): A61K31/53A61K31/52A61K31/498A61K31/497A61K31/4745A61K31/4709A61K31/405C07D403/02A61K31/404A61K31/407A61P25/00A61P25/22A61P25/24C07D209/40C07D401/06C07D401/12C07D403/12C07D405/12C07D409/04C07D409/06C07D409/12C07D409/14C07D413/06C07D417/12
CPCA61K31/404C07D417/12A61K31/407A61K31/4709A61K31/4745A61K31/497A61K31/498A61K31/52A61K31/53C07D209/40C07D401/06C07D401/12C07D403/02C07D403/12C07D405/12C07D409/04C07D409/06C07D409/12C07D409/14C07D413/06A61K31/405A61P25/00A61P25/22A61P25/24
InventorKONKEL, MICHAELWETZEL, JOHN M.TALISMAN, JAMIE
OwnerKONKEL MICHAEL