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Patent

Process for the preparation of 11-amino-3-chloro-6,11-dihydro-5,5-dioxo-6-methyl-dibenzo[c,f][1,2]-thiazepine and application to the synthesis of tianeptine

TL;DR: In this paper, the synthesis of 11-amino-3-chloro-6,11-dihydro-5,5-dioxo-six-methyl dibenzo(c,f)(1,2) was described.
Abstract: Synthesis of 11-amino-3-chloro-6,11-dihydro-5,5-dioxo-6-methyl dibenzo(c,f)(1,2)thiazepine (I) and its salts, from 3-chloro-6,11-dihydro-6-methyl-5,5,11-trioxo dibenzo(c,f)(1,2)thiazepine (III). Synthesis of 11-amino-3-chloro-6,11-dihydro-5,5-dioxo-6-methyl dibenzo(c,f)(1,2)thiazepine of formula (I) and its salts, from 3-chloro-6,11-dihydro-6-methyl-5,5,11-trioxo dibenzo(c,f)(1,2)thiazepine of formula (III): Independent claims are also included for the use of (I) to prepare tianeptine (II) and its salts.
Citations
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Patent
02 Feb 2004
TL;DR: In this paper, a formula for the treatment of irritable bowel syndrome and nonulcer dyspepsia is defined. But this formula is not suitable for the use of colorectal cancer patients.
Abstract: Compounds according to the formula as defined herein are administered for the treatment of irritable bowel syndrome and nonulcer dyspepsia.

11 citations

Patent
18 Nov 2009
TL;DR: In this paper, a novel process for the preparation of sodium 7-((3-Chloro-6-methyl-5,5-dioxo)-6,11-dihydrodibenzo(c,f)(1,2)thiazepin-11-yl)amino)heptanoate and intermediates is described.
Abstract: The present invention relates to a novel process for the preparation of sodium 7-((3-Chloro-6-methyl-5,5-dioxo-6,11-dihydrodibenzo(c,f)(1,2)thiazepin-11-yl)amino)heptanoate and intermediates. The invention also encompasses isolation of an essentially non-hygroscopic compound which is substantially pure.

8 citations

Patent
05 May 2008
TL;DR: In this paper, a method of treating corticosteroid-induced cognitive impairment comprises administering an effective amount of at least one compound of formula I, or pharmaceutically acceptable salts thereof, to a subject in need of such treatment.
Abstract: A method of treating corticosteroid-induced cognitive impairment comprises administering an effective amount of at least one compound of formula I, or pharmaceutically acceptable salts thereof, to a subject in need of such treatment. Formula I is: wherein: A is a bridge selected from the following radicals: —(CH2)m—, —CH═CH—, —(CH2)p—O—, —(CH2)p—S—, —(CH2)p—SO2—, —(CH2)p—NR1— and —SO2—NR2—, and wherein: m is an integer of from 1 to 3 inclusive; p is an integer selected from 1 and 2; R1 is selected from the group consisting of hydrogen and C1-C5 alkyl; and R2 is C1-C5 alkyl; X and Y are independently selected from the group consisting of hydrogen and halogen; R and R′ are independently selected from the group consisting of hydrogen and C1-C5 alkyl; n is an integer from 1 to 12 inclusive; and * denotes an asymmetric carbon.

7 citations

Patent
24 Mar 2017
TL;DR: In this paper, a compound having the structure: a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder was presented.
Abstract: The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.

4 citations

Patent
23 Oct 2009
TL;DR: In this article, a novel sulfate salt of tianeptine with improved properties is described, as well as its methods of making and related methods of treatment, which are described in detail.
Abstract: Disclosed herein is a novel sulfate salt of tianeptine with improved properties. Also described herein are novel pharmaceutical compositions comprising tianeptine sulfate salt, methods of making, and related methods of treatment.

4 citations

References
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Patent
23 Feb 1995
TL;DR: In this article, the use of the (+) isomer (Ia) of formula (I) or its salts in medicaments for treating memory/cognitive disorders is claimed, and the pref. isomer is of the sodium salt of tianeptine (sodium (+)7-((3-chloro-6-methyl-5,5-dioxo)-6,11-dihydrobenzo(c,f)-1,2-thiazepi n-11-yl)amino)heptanoate) described in FR
Abstract: Use of the (+) isomer (Ia) of formula (I) or its salts in medicaments for treating memory/cognitive disorders is claimed. The pref. isomer is of the sodium salt of tianeptine (sodium (+)7-((3-chloro-6-methyl-5,5-dioxo-6,11-dihydrobenzo(c,f)-1,2-thiazepi n-11-yl)amino)heptanoate) described in FR2104728 and FR2635461.

8 citations