FIELD: organic chemistry, pharmacy. SUBSTANCE: risperidone pamoate of the formula (I) is synthesized by treatment of 3-[2-[4- -(6-fluoro-1,2-benzisoxazole-3-yl)-1-piperidinyl] ethyl]- -6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one with pamoic acid in an inert solvent. Compounds of the formula (I) provide the prolonged release from low water-soluble pamoates. These compounds are dopamine antagonists exhibiting the prolonged effect. EFFECT: improved method of synthesis, prolonged antipsychotic activity. 9 cl, 1 tbl, 2 ex
Title |
Year |
Author |
Number |
2,9-DISUBSTITUTED 4H-PYRIDO-(1,2-A)-PYRIMIDINE-4-ONES AND ANTIPSYCHOTIC COMPOSITION |
1991 |
- Ljudo Ehdmond Zhozefin Kennis[Be]
- Jan Vandenberk[Be]
- Al'Bertus Khendrikus Marija Terezija Van Khehrtum[Be]
|
RU2037495C1 |
ESTER DERIVATIVES OF 9-HYDROXY-PYRIDO[1,2-A]PYRIMIDINE-4-ONE, A METHOD OF THEIR SYNTHESIS, A COMPOSITION SHOWING ANTIPSYCHOTIC ACTIVITY AND A METHOD OF ITS PREPARING |
1994 |
- Jan Vandenberk
- Ljudo Ehdmon Zhozefin Kenni
|
RU2126406C1 |
RISPERIDONE-CONTAINING MICROCAPSULES, PHARMACEUTICAL COMPOSITION AND METHODS OF THEIR MAKING |
1994 |
- Mesens Zhan-Lui
- Riki Majkl E.
- Atkins Tomas Dzh.
|
RU2178695C2 |
METHOD FOR PREPARATION OF 3-PIPERAZINYLBENZAZOL DERIVATIVES OR THEIRS PHARMACEUTICALLY ACCEPTABLE ADDITIVE SALTS |
0 |
- Lyudo Edmond Zhozefin Kennis
- Yan Vandenbek
- Zhozefus Karolus Mertens
|
SU1687030A3 |
AQUEOUS RISPERIDONE COMPOSITIONS |
1995 |
- Mark Karel Jozef Fransua
- Villi Marija Al'Bert Karlo Dris
|
RU2161965C2 |
USE OF CYCLODEXTRIN AS MUCOADHESIVE AGENT, COMPOSITION BASED ON INTRACONAZOL AND CYCLODEXTRIN AND METHOD OF ITS PREPARING |
1995 |
- Peter Putteman
- Mark Karel Jozef Fransua
- Ehrik Karolus Leonarda Snuks
|
RU2164418C2 |
METHOD OF PRODUCING DERIVATIVES OF 1,2-BENZISOXAZOLYL-3, OR 1,2-BENZISOTHIAZOLYL-3 OR STEREOSIOMERS THEREOF OR ACID-ADDITIVE SALTS THEREOF |
0 |
- Lyudo Edmon Zhozefin Kennis
- Yan Vandenberk
|
SU1468419A3 |
SUBSTITUTED DIHYDROPYRANOPYRIDINES, METHOD OF THEIR SYNTHESIS, INTERMEDIATE COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING |
1994 |
- Gi Rozalia Ehzhen Van Lommen
- Fransisko Khav'Er Fernandes-Gadea
- Khose Ignasio Andreskhil'
- Marija Ehnkarnas'On Matesans-Ballesteros
|
RU2135501C1 |
IMIDAZOAZEPINE DERIVATIVE, PHARMACEUTICAL COMPOSITION, METHOD OF ITS PREPARING, METHOD OF SYNTHESIS OF IMIDAZOAZEPINE DERIVATIVE |
1994 |
- Frans Ehduard Zhansens
- Jozef Ehlizabet Lehnarts
|
RU2133249C1 |
SABELUZOL AQUEOUS SUSPENSION FOR ORAL USE AND METHOD OF ITS PREPARING |
1995 |
- Mark Karel Jozef Fransua
- Kristin Frida Ogjusta Agemans
|
RU2141821C1 |