600138 Disclosed herein is a compound of formula (I), wherein the variables are defined in the specification, and the use thereof in the treatment of psychotic disorders, intellectual impairment disorders and inflammatory diseases. Specific embodiments of a compound of formula (I) include: N-[[2-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-5-(2,6-dimethyl-4-pyridinyl)-4-thiazolyl]methyl]-cyclopropaneacetamide (Compound 1)

This invention provides a novel dicarboxylic acid salt forms of varenicline namely varenicline fumarate and methods for making same. Varenicline salts are useful for treating smoking addition. In one embodiment of the instant invention the varenicline fumarate shows an XRD pattern (2theta)) (±0.2° having characteristic peaks at 10.6 11.9 13.2 16.2 16.6 18.0 21.5 22.6 25.7 28.5 and 29.1°. In another embodiment the varenicline fumarate is prepared by (i) contacting varenicline with fumaric acid op...

Provided herein is an impurity of varenicline, methylvarenicline, 6-methyl-5,8,14-triazatetracyclo[10.3.1.02,11,04,9]hexadeca-2(11),3,5,7,9-pentaene, and a process for the preparation and isolation thereof. Provided further herein is a highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure varenicline or a pharmaceutically acceptable salt ...

Provided herein is an impurity of varenicline methylvarenicline 6-methyl-5814-triazatetracyclo[10.3.1.0211049]hexadeca-2(11)3579-pentaene and a process for the preparation and isolation thereof. Provided further herein is a highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity processes for the preparation thereof and pharmaceutical compositions comprising highly pure varenicline or a pharmaceutically acceptable salt thereof substa...

The present invention provides an improved method for preparing a compound of formula (IIIA), which is a varenicline synthesis intermediate. Furthermore, the present invention provides an improved method for preparing varenicline, or a salt or a solvate thereof. Moreover, the present invention provides a process for decolouring varenicline, or a salt or a solvate thereof. Moreover, the present invention provides a process for preparing varenicline L-tartrate, with an improved yield. Moreover, th...

Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4 ,5-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02....

Provided herein is an improved convenient commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4 5-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca-2(7)35-trien-10-yl)-222-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(45-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca...

It is disclosed a process for the preparation of a compound of formula (I) or a salt thereof, comprising: nitrating a compound of formula (II) or a salt thereof, to obtain a compound of formula (IV) or a salt thereof, reducing it, to obtain a compound of formula (V) or a salt thereof, and subsequently cyclizing it to obtain a compound of formula (I) or a salt thereof and, if desired, converting a compound of formula (I) to a salt thereof, or vice versa, characterized in that: the nitration of a ...

It is disclosed a process for the preparation of a compound of formula (I) or a salt thereof comprising: nitrating a compound of formula (II) or a salt thereof to obtain a compound of formula (IV) or a salt thereof reducing it to obtain a compound of formula (V) or a salt thereof and subsequently cyclizing it to obtain a compound of formula (I) or a salt thereof and if desired converting a compound of formula (I) to a salt thereof or vice versa characterized in that: the nitration of a compound ...

It is disclosed a process for the preparation of a compound of formula (I) or a salt thereof, comprising: nitrating a compound of formula (II) or a salt thereof, to obtain a compound of formula (IV) or a salt thereof, reducing it, to obtain a compound of formula (V) or a salt thereof, and subsequently cyclizing it to obtain a compound of formula (I) or a salt thereof and, if desired, converting a compound of formula (I) to a salt thereof, or vice versa, characterized in that: the nitration of a ...