IP Library Granted Patent US 7,262,189
Granted Patent B2
US 7,262,189 · App. 10/499,164 · Granted Aug 28, 2007

Benzothiazine and benzothiadiazine derivatives, method for preparing same and pharmaceutical compositions containing same

Assignee: Les Laboratoires Server
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Quick Facts
Patent No.
US 7,262,189
App. No.
10/499,164
Granted
Aug 28, 2007
Kind
B2
Abstract

Compounds of formula (I): wherein: R 1 represents aryl or heteroaryl, R 2 represents hydrogen, halogen or hydroxy, X represents oxygen or sulphur, Y represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents CR 4 R 5 or NR 4 , R 3 represents hydrogen, alkyl or cycloalkyl, R 4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR 3 —, forms the ring wherein m represents 1, 2 or 3, R 5 represents hydrogen or halogen, their isomers and also their addition salts Medicaments.

Claims (17)

1. A compound selected from those of formula (I):

wherein:

R 1 represents aryl or heteroaryl,

R 2 represents hydrogen, halogen or hydroxy,

X represents oxygen or sulphur,

Y represents oxygen, sulphur or NR wherein R represents hydrogen or linear or branched (C 1 -C 6 )alkyl,

A represents NR 4 , and R 3 and R 4 , together with the nitrogen and carbon atoms to which they are attached form a ring

wherein m represents 1, 2 or 3,

its isomers and addition salts thereof with a pharmaceutically acceptable acid or base,

it being understood that:

“aryl” may be an aromatic monocyclic group, or a bicyclic group in which at least one of the rings is aromatic, each of those groups being optionally substituted by one or more identical or different halogen, linear or branched (C 1 -C 6 )alkyl, linear or branched (C 1 -C 6 )alkoxy, linear or branched (C 1 -C 6 )perhaloalkyl, linear or branched (C 1 -C 6 )-perhaloalkoxy, hydroxy, cyano, nitro, amino (optionally substituted by one or more linear or branched (C 1 -C 6 )alkyl), aminosulphonyl (optionally substituted by one or more linear or branched (C 1 -C 6 )alkyl), (C 1 -C 6 )alkylsulphonylamino, or phenyl (optionally substituted by one or more identical or different halogen, liner or branched (C 1 -C 6 )alkyl, linear or branched (C 1 -C 6 )perhaloalkyl, hydroxy or linear or branched (C 1 -C 6 )alkoxy),

“heteroaryl” may be an aromatic monocyclic group, or bicyclic group in which at least one of the rings is aromatic, containing one, two or three identical or different hetero atoms selected from nitrogen, oxygen and sulphur, each of those groups being optionally substituted by one or more identical or different halogen, linear or branched (C 1 -C 6 )alkyl, linear or branched (C 1 -C 6 )alkoxy, linear or branched (C 1 -C 6 )perhaloallcyl, linear or branched (C 1 -C 6 )perhaloalkoxy, hydroxy, cyano, nitro, amino (optionally substituted by one or more linear or branched (C 1 -C 6 )alkyl), aminosulphonyl (optionally substituted by one or more linear or branched (C 1 -C 6 )alkyl), or (C 1 -C 6 )-alkylsulphonylamino.

2. A compound of claim 1 wherein R 1 represents aryl.

3. A compound of claim 1 wherein R 2 represents hydrogen.

4. A compound of claim 1 wherein m represents the number 1.

5. A pharmaceutical composition comprising as active principle an effective amount of a compound of claim 1 , together with one or more pharmaceutically acceptable excipients or vehicles.

6. A method for treating a living animal body, including a human, afflicted with a condition selected from anxiety and depression, comprising the step of administering to the living animal body, including a human, an amount of a compound of claim 1 which is effective for alleviation of the condition.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2004
From: CORDI, ALEX; DESOS, PATRICE; LESTAGE, PIERRE
To: LES LABORATOIRES SERVIER
Reel/Frame 016080/0645 →
Priority Claims (1)
FR 01/16620 · Dec 21, 2001 · national
Continuity (1)
Related Publication 20050065146A1 · Mar 24, 2005