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1. (WO2002050050) 2-(2-(4-((2R)-2-METHYL-3-(10H-PHENOTHIAZIN-10-YL)PROPYL)-1-PIPERAZINYL)-ETHOXY)ETHANOL, PROCEDE DE PREPARATION ASSOCIE, COMPOSITIONS PHARMACEUTIQUES CONTENANT CE COMPOSE ET UTILISATION THERAPEUTIQUE DUDIT COMPOSE
Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique
CLAIMS

1. Process for preparing 2-(2-(4-((2R)-2-methyl-3-(10H-phenothiazin-10-yl)propyl)-l- piperazinyl)ethoxy)ethanol characterized in that it comprises a reaction of 10-[(2S)- 3-chloro-2-methylpropyl]-10H-phenothiazine with 2-[2-(l-piperazinyl)ethoxy]- ethanol.

2. Pharmaceutical composition containing 2-(2-(4-((2R)-2-methyl-3-(10H- phenothiazin-10-yl)propyl)-l-piperazinyl)ethoxy)ethanol or its pharmaceutically acceptable salts free of the (S) enantiomer and further containing a suitable carrier.

3. 2-(2-(4-((2R)-2-methyl-3-(l OH-phenothiazin- 10-yl)propyl)-l - piperazinyl)ethoxy)ethanol, or its pharmaceutically acceptable salts for use as a medicament.

4. 2-(2-(4-((2R)-2-methyl-3-(10H-phenothiazin-10-yl)propyl)-l- piperazinyl)ethoxy)ethanol, or its pharmaceutically acceptable salts for use as an antiemetic agent.

5. Therapeutic use of 2-(2-(4-((2R)-2-methyl-3-(10H-phenothiazin-10-yl)propyl)-l- piperazinyl)ethoxy)ethanol, or its pharmaceutically acceptable salts.

6. Therapeutic use according to claim 5 in the treatment or prevention of emesis.

7. A method of preventing or treating, in humans or mammals, disorders or conditions associated with nausea or vomiting, such as radiation induced emesis, cancerotherapy, HIV-therapy, motion sickness, migraine, post operative nausea, Meniere's disease and related disorders, method comprising the administration of

2-(2-(4-((2R)-2-methyl-3-(10H-phenothiazin-10-yl)propyl)-l- piperazinyl)ethoxy)ethanol, or its pharmaceutically acceptable salts to said human.

8. Use of 2-(2-(4-((2R)-2-methyl-3-(10H-phenothiazin-10-yl)propyl)-l- piperazinyl)ethoxy)ethanol, or its pharmaceutically acceptable salts for the manufacture of a medicament for preventing or treating disorders or conditions associated with nausea or vomiting.

9. A process, pharmaceutical composition, use or method according to any of the preceding claims characterized in that the 2-(2-(4-((2R)-2-methyl-3-(10H- phenothiazin-10-yl)propyl)-l-piperazinyl)ethoxy)ethanol is in the form of the dihydrochloride salt.

10. A chemical compound selected from the group consisting of
- 10-[(2S)-2-methyl-3-(tetrahydro-2H-pyran-2-ylθ3Q)propyl]- 10H- phenothiazine;
10-[(2S)-3-chloro-2-methylpropyl]-10H-phenothiazine;
- 10-[(2R)-2-methyl-3-(tetrahydro-2H-pyran-2-yloxy)propyl]-10H- phenothiazine;
10-[(2R)-3-chloro-2-methylpropyl]-10H-phenothiazine; and
- 10-[(2) -2-methyl-3-(tetrahydro-2H-pyran-2-yloxy)propyl] - 10H- phenothiazine.