IP Library Granted Patent US 7,256,191
Granted Patent B2
US 7,256,191 · App. 10/931,586 · Granted Aug 14, 2007

Materials and methods for the treatment of depression

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Quick Facts
Patent No.
US 7,256,191
App. No.
10/931,586
Granted
Aug 14, 2007
Kind
B2
Abstract

The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Claims (19)

1. A method for treating a disease state which can be improved by a serotonin reuptake inhibitor wherein said method comprises administering, to an individual in need of such treatment, a compound, or salt thereof, wherein said compound has the following structure

and wherein

R 1 and R 2 are independently H or C 1-10 alkyl; or

R 1 and R 2 are methylene groups that together form part of a cyclic structure;

R 3 is a linear or branched alkyl or heteroalkyl group having 1 to 12 carbon atoms; or

R 3 is heterocycloalkyl, benzyl, aryl, or heteroaryl optionally substituted with one or more halogen atoms C 1-4 alkyl, C 1-4 alkoxy, hydroxy, cyano, amino, alkylamino, dialkylamino, trifluoromethyl,—

COOH, or —COOC 1-4 alkyl;

X is fluoro, chloro, iodo, trifluoromethyl, methoxy, cyano, nitro, amino, mono- or di-substituted amino, carboxamide, carboxylic acid, carboxylic ester, sulfonic acid, methyl sulfonate, or sulfonamide;

n is from 0 to 12, and

Z=

2. A pharmaceutical composition comprising a compound, or a salt thereof, wherein said compound has the following structure:

where R 1 and R 2 are independently H or C 1-10 alkyl or R 1 and R 2 are methylene groups that together form part of a cyclic structure; R 3 is a linear or branched alkyl or heteroalkyl group having 1 to 12 carbon atoms, or R 3 is heterocycloalkyl, benzyl, aryl, or heteroaryl optionally substituted with one or more halogen atoms, C 1-4 alkyl, C 1-4 alkoxy, hydroxy, cyano, amino, alkylamino, dialkylamino, trifluoromethyl, —COOH, or —COOC 1-4 alkyl; X is fluoro, chloro, iodo, trifluoromethyl, methoxy, cyano, nitro, amino, mono- or di-substituted amino, carboxamide, carboxylic acid, carboxylic ester, sulfonic acid, methyl sulfonate, or sulfonamide; n is from 0 to 12, and

Z is selected from the group consisting of:

3. A compound, or salt thereof, wherein said compound has the following structure:

where: R 1 and R 2 are independently H or C 1-10 alkyl or R 1 and R 2 are methylene groups that together form part of a cyclic structure; R 3 is a linear or branched alkyl or heteroalkyl group having 1 to 12 carbon atoms, or R 3 is heterocycloalkyl, benzyl, aryl, or heteroaryl optionally substituted with one or more halogen atoms, C 1-4 alkyl, C 1-4 alkoxy, hydroxy, cyano, amino, alkylamino, dialkylamino, trifluoromethyl, —COOH, or —COOC 1-4 alkyl; X is fluoro, chloro, iodo, trifluoromethyl, methoxy, cyano, nitro, amino, mono- or di-substituted amino, carboxamide, carboxylic acid, carboxylic ester, sulfonic acid, methyl sulfonate, or sulfonamide; n is from 0 to 12, Z=—CH 2 —CH 2 —N(R 6 R 7 ) where R 6 and R 7 are independently H or lower alkyl, or R 6 and R 7 are methylene groups that together with the nitrogen form a cyclic structure; or Z=

where m=1 or 2 and R 8 is H or lower alkyl.

4. The compound, according to claim 3 , wherein Z is selected from the group consisting of:

5. The compound, according to claim 3 , wherein X is CF 3 .

6. The compound, according to claim 3 , wherein n is from 0 to 4.

Assignments (3)
SECURITY AGREEMENT Recorded Oct 18, 2010
From: ARYX THERAPEUTICS, INC.
To: AYER CAPITAL PARTNERS MASTER FUND, L.P.; MPM BIOVENTURES III, L.P.; MPM BIOVENTURES III-QP, L.P.; MPM BIOVENTURES III GMBH & CO. BETEILIGUNGS KG; MPM BIOVENTURES III PARALLEL FUND, L.P.; AYER CAPITAL PARTNERS KESTREL FUND, L.P.; MPM ASSET MANAGEMENT INVESTORS 2002 BVIII LLC
Reel/Frame 025150/0379 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 29, 2007
From: ARYX THERAPEUTICS
To: ARYX THERAPEUTICS, INC.
Reel/Frame 020024/0545 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 16, 2004
From: DRUZGALA, PASCAL
To: ARYX THERAPEUTICS
Reel/Frame 015381/0966 →