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Modulators of 5-ht receptors and methods of use thereof

A technology of m-g1 and -NO2, applied in the modulator of 5-HT receptor and its application field, can solve the problems of limiting treatment efficacy, affecting patient cooperation, primary negative and cognitive symptom recognition, etc.

Inactive Publication Date: 2012-05-30
ABBVIE INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] A further complication of the symptoms of schizophrenia is the appearance of drug-induced so-called secondary negative symptoms and cognitive deficits, which are difficult to recognize from primary negative and cognitive symptoms [Remington G and Kapur S (2000). Atypical antipsychotics : are some more atypical than others? Psychopharmacol 148: 3 - 15]
The appearance of secondary negative symptoms not only limits the efficacy of the treatment but, together with these side effects, negatively affects patient compliance

Method used

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  • Modulators of 5-ht receptors and methods of use thereof
  • Modulators of 5-ht receptors and methods of use thereof
  • Modulators of 5-ht receptors and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 42

[0606] Example 42 significantly and dose-dependently attenuated AMP-induced hyperactivity (main effect F(3,29)=6.2, Pfigure 1 ).

[0607] Example 181 administered to animals at 1.0 and 3.0 mg / kg before AMP significantly and in a dose-dependent manner attenuated AMP-induced hyperactivity (main effect F(7,29)=11.5, P Figure 2a ). In addition, no effect of Example 181 was seen in the spontaneous activity ( Figure 2b ).

[0608] Example 169 given to animals at 10 and 30 mg / kg before AMP; significantly and in a dose-dependent manner attenuated AMP-induced hyperactivity (main effect F(7,29)=12.6, P Figure 3a ). In addition, no effect of Example 169 was seen in the spontaneous activity ( Figure 3b ).

Embodiment 2

[0609] Example 2 significantly and in a dose-dependent manner weakened PCP-induced hyperactivity (main effect F(4,26)=3.5, P Figure 4 ).

[0610] d. Methods of Using Compounds

[0611] The compound of the present invention is 5-HT 2C receptor or 5-HT 6 receptor modulator or 5-HT 2C and 5-HT 6 Modulator of both receptors. In certain embodiments of the invention, the compound of formula (I) is 5-HT 2C Agonists and partial agonists of receptors or 5-HT 6 receptor antagonists. In certain other embodiments of the invention, the compound of formula (I) is 5-HT 2C Agonists and partial agonists of receptors and 5-HT 6 receptor antagonists. Thus, such compounds are useful in the prevention or treatment of 5-HT 2C and 5-HT 6 It is of interest in disease conditions in which either or both receptors are involved. Accordingly, the present invention provides methods of preventing or treating such conditions in a subject in need thereof. A subject in need of treatment thereof ma...

Embodiment 1

[0729] 1,2,3,4,4a,5-Hexahydropyrazino[1,2-a][1,5]benzodiazepine-6(7H)-one

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Abstract

The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Description

[0001] Cross References to Related Applications [0002] This patent application claims priority from US Provisional Patent Application 61 / 171,912, filed April 23, 2009, the entire contents of which are incorporated herein by reference. technical field [0003] The present invention relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2, 3,4,4a,5,6,7-Octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6 ,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyridine Azino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4 ,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxy Azapine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4 ]diazepine derivatives, including these 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepines Heterene, 1,2,3,4,4a,5,6,7-Octahydropyrazino[1,2-a][1,5]benzodiazepine, 2 ,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a...

Claims

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Application Information

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IPC IPC(8): C07D498/04A61K31/551A61K31/553A61P25/00C07D471/04C07D471/14C07D487/04C07D491/04A61K31/4985
CPCY02E60/321C07D471/04C07D491/04C07D471/14C07D487/04C07D498/04C07D487/14A61P1/00A61P1/04A61P1/14A61P3/04A61P3/10A61P7/12A61P9/10A61P9/12A61P13/02A61P13/10A61P15/00A61P15/10A61P17/06A61P25/00A61P25/04A61P25/06A61P25/08A61P25/10A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30A61P25/34A61P25/36A61P27/02A61P27/06A61P43/00
Inventor Y.王J.T.布鲁尔I.阿克里托普罗赞泽S.W.久里克F.波尔基W.布拉耶A-L.雷洛
Owner ABBVIE INC
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