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Claims for Patent: 7,943,621

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Claims for Patent: 7,943,621

Title:Salts of piperazine compounds as D.sub.3/D.sub.2 antagonists
Abstract: The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylca- rbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them.
Inventor(s): Czibula; Laszlo (Budapest, HU), Sebok; Ferenc (Mezokovacshaza, HU), Greiner; Istvan (Budapest, HU), Domany; Gyorgy (Obanya, HU), Csongor; Eva Againe (Budapest, HU)
Assignee: Richter Gedeon Nyrt. (Budapest, HU)
Application Number:12/118,437
Patent Claims: 1. Trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethy- lcarbamoyl-cyclohexylamine monohydrochloride, and hydrates and solvates thereof.

2. Crystalline trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine hydrochloride having a powder X-ray diffraction pattern that comprises peaks at about 6.6, about 7.3, about 13.2, about 21.1, and about 22.4, each about .+-.0.2 degrees 2.theta..

3. The crystalline form of claim 2, wherein the powder X-ray diffraction pattern further comprises peaks at about 14.2, about 14.6, about 16.9, about 24.8, about 26.5 and about 26.6.degree., each about .+-.0.2 degrees 2.theta..

4. The crystalline form of claim 2, having an infrared spectrum comprising characteristic peaks at about 3321, about 2914, about 1652, about 1526, about 956, and about 784 cm.sup.-1, each about .+-.4 cm.sup.-1.

5. The crystalline form of claim 4, wherein the infrared spectrum further comprises characteristic peaks at about 2931, about 2466, and about 715 cm.sup.-1, each about .+-.4 cm.sup.-1.

6. The crystalline form of claim 2, having a Raman spectrum comprising characteristic peaks at about 2969, about 2933, about 2850, about 1578, about 1052, and about 475 cm.sup.-1, each about .+-.4 cm.sup.-1.

7. The crystalline form of claim 6, wherein the Raman spectrum further comprises characteristic peaks at about 3070, about 2986, about 2914, about 2864, and about 1458 cm.sup.-1, each about .+-.4 cm.sup.-1.

8. Trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethy- lcarbamoyl-cyclohexylamine dihydrochloride, and hydrates and solvates thereof.

9. Trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethy- lcarbamoyl-cyclohexylamine monohydrobromide, and hydrates and solvates thereof.

10. Trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimeth- ylcarbamoyl-cyclohexylamine maleate, and hydrates and solvates thereof.

11. Trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimeth- ylcarbamoyl-cyclohexylamine methanesulphonate, and hydrates and solvates thereof.

12. A process for preparing a compound chosen from monohydrochloride, dihydrochloride, monohydrobromide, maleate, and methanesulphonate salts, hydrates, and solvates of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine, comprising (i) adding trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine to a solvent or mixture of solvents, (ii) adding hydrochloric acid, or a salt thereof prepared from a base which is weaker base than the trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine, or a solution thereof, to the mixture formed in step(i), and (iii) optionally isolating the compound.

13. A process for preparing trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine dihydrochloride, and hydrates and solvates thereof, comprising (i) adding trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine to a solvent or mixture of solvents, (ii) adding hydrochloric acid, or a salt thereof prepared from a base which is weaker base than the trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine, or a solution thereof, to the mixture formed in step (i), and (iii) optionally isolating the compound.

14. A process for preparing Trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethyl carbamoyl-cyclohexylamine monohydrobromide, and hydrates and solvates thereof, comprising (i) adding trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine to a solvent or mixture of solvents, (ii) adding hydrobromic acid, or a salt thereof prepared from a base which is weaker base than the trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine, or a solution thereof, to the mixture formed in step(i), and (iii) optionally isolating the compound.

15. A process for preparing trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine maleate, and hydrates and solvates thereof, comprising (i) adding trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine to a solvent or mixture of solvents, (ii) adding maleic acid, or a salt thereof prepared from a base which is weaker base than the trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimeth- ylcarbamoyl-cyclohexylamine, or a solution thereof, to the mixture formed in step (i), and (iii) optionally isolating the compound.

16. A process for preparing trans 4-{2-[4(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl- -cyclohexylamine methanesulphonate, and hydrates and solvates thereof, comprising (i) adding trans 4-{2-[4-(2,3dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl- -cyclohexylamine to a solvent or mixture of solvents, (ii) adding methanesulfonic acid, or a salt thereof prepared from a base which is weaker base than the trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine, or a solution thereof, to the mixture formed in step (i), and (iii) optionally isolating the compound.

17. A pharmaceutical composition comprising a compound chosen from monohydrochloride, dihydrochloride, monohydrobromide, maleate, and methanesulphonate salts, hydrates, and solvates of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoy- l-cyclohexylamine and a pharmaceutically acceptable carrier.
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