BG62004B1 - Рисперидонпамоат, състави, които го съдържат, и методи заполучаване на съставите и съединението - Google Patents

Рисперидонпамоат, състави, които го съдържат, и методи заполучаване на съставите и съединението Download PDF

Info

Publication number: BG62004B1
Authority: BG; Bulgaria
Prior art keywords: compound; risperidone; compositions; preparation; composition according
Prior art date: 1993-04-28

Application number

BG100094A

Other languages

Bulgarian (bg)

English (en)

Other versions

BG100094A (bg

Inventor

Jean L. Mesens

Jozef Peeters

Original Assignee

Janssen Pharmaceutica Nv

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1993-04-28

Filing date

1995-10-25

Publication date

1998-12-30

1995-10-25 Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv

1996-05-31 Publication of BG100094A publication Critical patent/BG100094A/bg

1998-12-30 Publication of BG62004B1 publication Critical patent/BG62004B1/bg

Links

RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 title claims abstract description 29
229960001534 risperidone Drugs 0.000 title claims abstract description 29
150000001875 compounds Chemical class 0.000 title claims abstract description 28
239000000203 mixture Substances 0.000 title claims abstract description 19
238000000034 method Methods 0.000 title claims abstract description 11
238000002360 preparation method Methods 0.000 title claims abstract description 5
WLJNZVDCPSBLRP-UHFFFAOYSA-N pamoic acid Chemical compound C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1 WLJNZVDCPSBLRP-UHFFFAOYSA-N 0.000 claims abstract description 8
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims abstract description 3
150000003839 salts Chemical class 0.000 claims description 10
-1 benzyl alcohol, sorbitan ester Chemical class 0.000 claims description 7
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
239000007900 aqueous suspension Substances 0.000 claims description 4
239000003814 drug Substances 0.000 claims description 4
239000003937 drug carrier Substances 0.000 claims description 4
239000001913 cellulose Substances 0.000 claims description 2
229920002678 cellulose Polymers 0.000 claims description 2
239000012442 inert solvent Substances 0.000 claims description 2
239000004480 active ingredient Substances 0.000 claims 1
230000008878 coupling Effects 0.000 claims 1
238000010168 coupling process Methods 0.000 claims 1
238000005859 coupling reaction Methods 0.000 claims 1
WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 9
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 9
230000000694 effects Effects 0.000 description 7
ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 6
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
241000282472 Canis lupus familiaris Species 0.000 description 5
229920001213 Polysorbate 20 Polymers 0.000 description 5
239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 5
235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 5
206010047700 Vomiting Diseases 0.000 description 4
VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 description 4
229960004046 apomorphine Drugs 0.000 description 4
VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 4
239000012458 free base Substances 0.000 description 4
239000003921 oil Substances 0.000 description 4
235000019198 oils Nutrition 0.000 description 4
230000036470 plasma concentration Effects 0.000 description 4
229940068977 polysorbate 20 Drugs 0.000 description 4
239000008159 sesame oil Substances 0.000 description 4
235000011803 sesame oil Nutrition 0.000 description 4
239000002904 solvent Substances 0.000 description 4
230000008673 vomiting Effects 0.000 description 4
241001465754 Metazoa Species 0.000 description 3
229920003171 Poly (ethylene oxide) Polymers 0.000 description 3
239000000164 antipsychotic agent Substances 0.000 description 3
239000003420 antiserotonin agent Substances 0.000 description 3
235000019445 benzyl alcohol Nutrition 0.000 description 3
229960004217 benzyl alcohol Drugs 0.000 description 3
238000009472 formulation Methods 0.000 description 3
238000007918 intramuscular administration Methods 0.000 description 3
230000003389 potentiating effect Effects 0.000 description 3
239000008213 purified water Substances 0.000 description 3
201000000980 schizophrenia Diseases 0.000 description 3
208000024891 symptom Diseases 0.000 description 3
CFKMVGJGLGKFKI-UHFFFAOYSA-N 4-chloro-m-cresol Chemical compound CC1=CC(O)=CC=C1Cl CFKMVGJGLGKFKI-UHFFFAOYSA-N 0.000 description 2
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 2
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 2
239000002253 acid Substances 0.000 description 2
239000013543 active substance Substances 0.000 description 2
230000003474 anti-emetic effect Effects 0.000 description 2
229940082988 antihypertensives serotonin antagonists Drugs 0.000 description 2
239000002585 base Substances 0.000 description 2
WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
230000037396 body weight Effects 0.000 description 2
239000001768 carboxy methyl cellulose Substances 0.000 description 2
239000004359 castor oil Substances 0.000 description 2
235000019438 castor oil Nutrition 0.000 description 2
210000003169 central nervous system Anatomy 0.000 description 2
239000003795 chemical substances by application Substances 0.000 description 2
229960003638 dopamine Drugs 0.000 description 2
239000003210 dopamine receptor blocking agent Substances 0.000 description 2
239000003136 dopamine receptor stimulating agent Substances 0.000 description 2
150000002170 ethers Chemical class 0.000 description 2
ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 2
238000009115 maintenance therapy Methods 0.000 description 2
239000002858 neurotransmitter agent Substances 0.000 description 2
239000008194 pharmaceutical composition Substances 0.000 description 2
235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
229920001451 polypropylene glycol Polymers 0.000 description 2
229920000053 polysorbate 80 Polymers 0.000 description 2
208000020016 psychiatric disease Diseases 0.000 description 2
235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 2
229920001027 sodium carboxymethylcellulose Polymers 0.000 description 2
238000007920 subcutaneous administration Methods 0.000 description 2
239000000725 suspension Substances 0.000 description 2
JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 1
LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
WJFKNYWRSNBZNX-UHFFFAOYSA-N 10H-phenothiazine Chemical compound C1=CC=C2NC3=CC=CC=C3SC2=C1 WJFKNYWRSNBZNX-UHFFFAOYSA-N 0.000 description 1
ZXVONLUNISGICL-UHFFFAOYSA-N 4,6-dinitro-o-cresol Chemical group CC1=CC([N+]([O-])=O)=CC([N+]([O-])=O)=C1O ZXVONLUNISGICL-UHFFFAOYSA-N 0.000 description 1
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
206010002942 Apathy Diseases 0.000 description 1
235000017060 Arachis glabrata Nutrition 0.000 description 1
244000105624 Arachis hypogaea Species 0.000 description 1
235000010777 Arachis hypogaea Nutrition 0.000 description 1
235000018262 Arachis monticola Nutrition 0.000 description 1
239000005711 Benzoic acid Substances 0.000 description 1
239000004255 Butylated hydroxyanisole Substances 0.000 description 1
239000004322 Butylated hydroxytoluene Substances 0.000 description 1
NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 1
229920001661 Chitosan Polymers 0.000 description 1
VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
244000124209 Crocus sativus Species 0.000 description 1
235000015655 Crocus sativus Nutrition 0.000 description 1
FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
206010011968 Decreased immune responsiveness Diseases 0.000 description 1
206010012374 Depressed mood Diseases 0.000 description 1
229920002307 Dextran Polymers 0.000 description 1
102000015554 Dopamine receptor Human genes 0.000 description 1
108050004812 Dopamine receptor Proteins 0.000 description 1
LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
239000001856 Ethyl cellulose Substances 0.000 description 1
ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
108010010803 Gelatin Proteins 0.000 description 1
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
208000004547 Hallucinations Diseases 0.000 description 1
206010022998 Irritability Diseases 0.000 description 1
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
229930195725 Mannitol Natural products 0.000 description 1
241000283973 Oryctolagus cuniculus Species 0.000 description 1
208000028017 Psychotic disease Diseases 0.000 description 1
241000207961 Sesamum Species 0.000 description 1
235000003434 Sesamum indicum Nutrition 0.000 description 1
KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
240000008042 Zea mays Species 0.000 description 1
235000016383 Zea mays subsp huehuetenangensis Nutrition 0.000 description 1
235000002017 Zea mays subsp mays Nutrition 0.000 description 1
BKPRVQDIOGQWTG-ICOOEGOYSA-N [(1s,2r)-2-phenylcyclopropyl]azanium;[(1r,2s)-2-phenylcyclopropyl]azanium;sulfate Chemical compound [O-]S([O-])(=O)=O.[NH3+][C@H]1C[C@@H]1C1=CC=CC=C1.[NH3+][C@@H]1C[C@H]1C1=CC=CC=C1 BKPRVQDIOGQWTG-ICOOEGOYSA-N 0.000 description 1
238000013019 agitation Methods 0.000 description 1
235000010443 alginic acid Nutrition 0.000 description 1
229920000615 alginic acid Polymers 0.000 description 1
239000005557 antagonist Substances 0.000 description 1
230000000259 anti-tumor effect Effects 0.000 description 1
239000002111 antiemetic agent Substances 0.000 description 1
235000010233 benzoic acid Nutrition 0.000 description 1
229960004365 benzoic acid Drugs 0.000 description 1
WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
235000019282 butylated hydroxyanisole Nutrition 0.000 description 1
CZBZUDVBLSSABA-UHFFFAOYSA-N butylated hydroxyanisole Chemical compound COC1=CC=C(O)C(C(C)(C)C)=C1.COC1=CC=C(O)C=C1C(C)(C)C CZBZUDVBLSSABA-UHFFFAOYSA-N 0.000 description 1
229940043253 butylated hydroxyanisole Drugs 0.000 description 1
235000010354 butylated hydroxytoluene Nutrition 0.000 description 1
229940095259 butylated hydroxytoluene Drugs 0.000 description 1
208000015114 central nervous system disease Diseases 0.000 description 1
238000006243 chemical reaction Methods 0.000 description 1
239000007795 chemical reaction product Substances 0.000 description 1
229960002242 chlorocresol Drugs 0.000 description 1
238000004587 chromatography analysis Methods 0.000 description 1
230000001684 chronic effect Effects 0.000 description 1
238000002425 crystallisation Methods 0.000 description 1
230000008025 crystallization Effects 0.000 description 1
229960003964 deoxycholic acid Drugs 0.000 description 1
239000008121 dextrose Substances 0.000 description 1
UGMCXQCYOVCMTB-UHFFFAOYSA-K dihydroxy(stearato)aluminium Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[Al](O)O UGMCXQCYOVCMTB-UHFFFAOYSA-K 0.000 description 1
BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
239000002552 dosage form Substances 0.000 description 1
229940079593 drug Drugs 0.000 description 1
239000003623 enhancer Substances 0.000 description 1
150000002148 esters Chemical class 0.000 description 1
235000019325 ethyl cellulose Nutrition 0.000 description 1
229920001249 ethyl cellulose Polymers 0.000 description 1
LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
229940093471 ethyl oleate Drugs 0.000 description 1
238000002474 experimental method Methods 0.000 description 1
238000000605 extraction Methods 0.000 description 1
238000001914 filtration Methods 0.000 description 1
229920000159 gelatin Polymers 0.000 description 1
239000008273 gelatin Substances 0.000 description 1
235000019322 gelatine Nutrition 0.000 description 1
235000011852 gelatine desserts Nutrition 0.000 description 1
150000002314 glycerols Chemical class 0.000 description 1
238000000227 grinding Methods 0.000 description 1
239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
239000008101 lactose Substances 0.000 description 1
239000000787 lecithin Substances 0.000 description 1
235000010445 lecithin Nutrition 0.000 description 1
229940067606 lecithin Drugs 0.000 description 1
150000004668 long chain fatty acids Chemical class 0.000 description 1
230000007774 longterm Effects 0.000 description 1
RLSSMJSEOOYNOY-UHFFFAOYSA-N m-cresol Chemical compound CC1=CC=CC(O)=C1 RLSSMJSEOOYNOY-UHFFFAOYSA-N 0.000 description 1
235000009973 maize Nutrition 0.000 description 1
239000000594 mannitol Substances 0.000 description 1
235000010355 mannitol Nutrition 0.000 description 1
150000004667 medium chain fatty acids Chemical class 0.000 description 1
239000002207 metabolite Substances 0.000 description 1
229940100630 metacresol Drugs 0.000 description 1
229920000609 methyl cellulose Polymers 0.000 description 1
239000001923 methylcellulose Substances 0.000 description 1
235000010981 methylcellulose Nutrition 0.000 description 1
239000003176 neuroleptic agent Substances 0.000 description 1
230000000701 neuroleptic effect Effects 0.000 description 1
231100000252 nontoxic Toxicity 0.000 description 1
230000003000 nontoxic effect Effects 0.000 description 1
239000000346 nonvolatile oil Substances 0.000 description 1
239000002245 particle Substances 0.000 description 1
235000020232 peanut Nutrition 0.000 description 1
230000000144 pharmacologic effect Effects 0.000 description 1
229960003742 phenol Drugs 0.000 description 1
229950000688 phenothiazine Drugs 0.000 description 1
WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
229940068968 polysorbate 80 Drugs 0.000 description 1
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
239000001267 polyvinylpyrrolidone Substances 0.000 description 1
229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
239000000843 powder Substances 0.000 description 1
239000002244 precipitate Substances 0.000 description 1
238000001556 precipitation Methods 0.000 description 1
239000012429 reaction media Substances 0.000 description 1
239000004248 saffron Substances 0.000 description 1
235000013974 saffron Nutrition 0.000 description 1
YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
238000007873 sieving Methods 0.000 description 1
239000011780 sodium chloride Substances 0.000 description 1
FHHPUSMSKHSNKW-SMOYURAASA-M sodium deoxycholate Chemical compound [Na+].C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 FHHPUSMSKHSNKW-SMOYURAASA-M 0.000 description 1
229910052938 sodium sulfate Inorganic materials 0.000 description 1
235000011152 sodium sulphate Nutrition 0.000 description 1
239000000600 sorbitol Substances 0.000 description 1
239000003549 soybean oil Substances 0.000 description 1
235000012424 soybean oil Nutrition 0.000 description 1
239000003381 stabilizer Substances 0.000 description 1
238000003756 stirring Methods 0.000 description 1
239000000375 suspending agent Substances 0.000 description 1
238000013268 sustained release Methods 0.000 description 1
239000012730 sustained-release form Substances 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
239000002562 thickening agent Substances 0.000 description 1
230000001256 tonic effect Effects 0.000 description 1
150000003626 triacylglycerols Chemical class 0.000 description 1
239000000080 wetting agent Substances 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
- C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
- C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems

Landscapes

Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Neurosurgery (AREA)
Life Sciences & Earth Sciences (AREA)
Biomedical Technology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Neurology (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Psychiatry (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Preparation Of Compounds By Using Micro-Organisms (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Saccharide Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

BG100094A 1993-04-28 1995-10-25 Рисперидонпамоат, състави, които го съдържат, и методи заполучаване на съставите и съединението BG62004B1 (bg)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
EP93201216		1993-04-28
PCT/EP1994/001296 WO1994025460A1 (en)	1993-04-28	1994-04-22	Risperidone pamoate

Publications (2)

Publication Number	Publication Date
BG100094A BG100094A (bg)	1996-05-31
BG62004B1 true BG62004B1 (bg)	1998-12-30

Family

ID=8213799

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
BG100094A BG62004B1 (bg)	1993-04-28	1995-10-25	Рисперидонпамоат, състави, които го съдържат, и методи заполучаване на съставите и съединението

Country Status (31)

Country	Link
US (2)	US5612346A (de)
EP (1)	EP0697019B1 (de)
JP (1)	JP3478397B2 (de)
KR (1)	KR100307101B1 (de)
CN (1)	CN1041727C (de)
AT (1)	ATE163418T1 (de)
AU (1)	AU675136B2 (de)
BG (1)	BG62004B1 (de)
CA (1)	CA2160366C (de)
CY (1)	CY2107B1 (de)
CZ (1)	CZ286688B6 (de)
DE (1)	DE69408666T2 (de)
DK (1)	DK0697019T3 (de)
ES (1)	ES2113652T3 (de)
FI (1)	FI109125B (de)
GR (1)	GR3026028T3 (de)
HU (1)	HU218212B (de)
IL (1)	IL109448A (de)
LV (1)	LV12315B (de)
NO (1)	NO305083B1 (de)
NZ (1)	NZ266143A (de)
PH (1)	PH30476A (de)
PL (1)	PL182466B1 (de)
RO (1)	RO115955B1 (de)
RU (1)	RU2131428C1 (de)
SG (1)	SG47046A1 (de)
SI (1)	SI9420031B (de)
SK (1)	SK280589B6 (de)
TW (1)	TW376319B (de)
WO (1)	WO1994025460A1 (de)
ZA (1)	ZA942909B (de)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
ATE288270T1 (de)	1993-11-19	2005-02-15	Janssen Pharmaceutica Nv	Mikroverkapselte 1,2-benzazole
US5453425A (en) *	1994-07-11	1995-09-26	Janssen Pharmaceutica N.V.	Risperidone oral formulation
TW487572B (en) *	1996-05-20	2002-05-21	Janssen Pharmaceutica Nv	Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters
CA2304568C (en) *	1997-09-30	2008-08-12	Eli Lilly And Company	Olanzapine pamoate formulations
US6617321B2 (en) *	1997-09-30	2003-09-09	Eli Lilly And Company	2-methyl-thieno-benzodiazepine formulation
UA72189C2 (uk) *	1997-11-17	2005-02-15	Янссен Фармацевтика Н.В.	Фармацевтична композиція, що містить водну суспензію субмікронних ефірів 9-гідроксирисперидон жирних кислот
DE69917663T2 (de) *	1998-09-30	2005-05-25	Eli Lilly And Co., Indianapolis	2-methyl-thieno-benzodiazepin-formulierung
WO2000027849A2 (en) *	1998-11-12	2000-05-18	Merck & Co., Inc.	Therapeutic polymorphs of a gaba-a alpha-5 inverse agonist and pamoate formulations of the same
FR2802101B1 (fr)	1999-12-10	2003-02-28	Aventis Pharma Sa	Association de cymemazine et d'un neuroleptique atypique
US6770478B2 (en) *	2000-02-10	2004-08-03	The Regents Of The University Of California	Erythrocytic cells and method for preserving cells
US6495164B1 (en) *	2000-05-25	2002-12-17	Alkermes Controlled Therapeutics, Inc. I	Preparation of injectable suspensions having improved injectability
WO2002043766A1 (en) *	2000-11-29	2002-06-06	Takeda Chemical Industries, Ltd.	Medicinal compositions and process for producing the same
US20050232995A1 (en)	2002-07-29	2005-10-20	Yam Nyomi V	Methods and dosage forms for controlled delivery of paliperidone and risperidone
RU2321391C2 (ru) *	2002-07-29	2008-04-10	Алза Корпорейшн	Способы и лекарственные формы для контролируемой доставки палиперидона
EP1534288A1 (de) *	2002-08-23	2005-06-01	Ranbaxy Laboratories, Ltd.	Stabilisierte wässrige risperidonhaltige lösungen und verfahren zu deren herstellung
KR20040034996A (ko) *	2002-10-18	2004-04-29	한미약품 주식회사	리스페리돈의 개선된 제조방법
EP1615924A1 (de) *	2003-04-22	2006-01-18	Synthon B.V.	Wasserlöslich salze von risperidon
RU2249456C1 (ru) *	2003-07-15	2005-04-10	Боев Игорь Викторович	Способ комбинированного купирования шизоаффективных синдромов психотического и субпсихотического уровня в условиях дневного стационара
US6987111B2 (en) *	2003-08-06	2006-01-17	Alkermes Controlled Therapeutics, Ii	Aripiprazole, olanzapine and haloperidol pamoate salts
BRPI0415531B8 (pt) *	2003-10-23	2021-05-25	Otsuka Pharma Co Ltd	formulação de aripiprazol injetável estéril de liberação controlada e método para a sua preparação
WO2005053796A1 (en) *	2003-12-02	2005-06-16	B & B Beheer Nv	Use of d4 and 5-ht2a antagonists, inverse agonists or partial agonists
US7884096B2 (en) *	2003-12-02	2011-02-08	Pharmaneuroboost N.V.	Method of treating mental disorders using of D4 and 5-HT2A antagonists, inverse agonists or partial agonists
WO2005072705A1 (en) *	2004-01-29	2005-08-11	Neuromolecular, Inc.	Combination of a nmda receptor antagonist and a mao-inhibitor or a gadpf-inhibitor for the treatment of central nervous system-related conditions
EP1838716B1 (de) *	2005-01-05	2011-06-01	Eli Lilly And Company	Olanzapinpamoat-dihydrat
EP1695973A1 (de) *	2005-02-24	2006-08-30	Neuro3D	Ocaperidonsalz und dieser enthaltende pharmazeutische Zubereitung
AR055099A1 (es) *	2005-07-28	2007-08-08	Alza Corp	Formulaciones liquidas para la administracion controlada de derivados de bencisoxazol
CA2622758A1 (en) *	2005-09-15	2007-03-29	Elan Pharma International, Limited	Nanoparticulate aripiprazole formulations
US8852638B2 (en)	2005-09-30	2014-10-07	Durect Corporation	Sustained release small molecule drug formulation
BRPI0811319A2 (pt)	2007-05-25	2015-02-10	Tolmar Therapeutics Inc	Composição fluida, método de formação de uma composição fluida, implante biodegrádavel formado in situ, método de formação de um implante biodegradável in situ, kit, implante e método de trataento
JP4879349B2 (ja) *	2007-07-31	2012-02-22	大塚製薬株式会社	アリピプラゾール懸濁液及び凍結乾燥製剤の製造方法
CN101932327A (zh) *	2007-12-19	2010-12-29	詹森药业有限公司	与长效注射用帕潘立酮酯相关的给药方案
US9034867B2 (en)	2011-03-18	2015-05-19	Alkermes Pharma Ireland Limited	Pharmaceutical compositions comprising sorbitan esters
US9040695B2 (en) *	2011-04-26	2015-05-26	Torrent Pharmaceuticals Limited	Acid addition salts of risperidone and pharmaceutical compositions thereof
JP6219918B2 (ja)	2012-03-19	2017-10-25	アルカームスファーマアイルランドリミテッド	グリセロールエステルを含む医薬組成物
WO2013142205A1 (en)	2012-03-19	2013-09-26	Alkermes Pharma Ireland Limited	Pharmaceutical compositions comprising benzyl alcohol
WO2013142198A1 (en)	2012-03-19	2013-09-26	Alkermes Pharma Ireland Limited	Pharmaaceutical compositions comprising fatty acid esters
BR112014024833B1 (pt)	2012-04-04	2022-10-04	Intervet International B.V.	Produto farmacêutico veterinário mastigável macio, processo para sua fabricação e seu uso, bem como uso de pamoato de sódio
CN102659577B (zh) *	2012-04-07	2014-07-02	安徽绩溪县徽煌化工有限公司	一种亚甲基双羟基萘酸的制备方法
EP3718536A1 (de)	2012-09-19	2020-10-07	Alkermes Pharma Ireland Limited	Pharmazeutische zusammensetzungen mit verbesserter lagerstabilität
US9375433B2 (en)	2012-09-26	2016-06-28	Tangent Reprofiling Limited	Modulators of androgen synthesis
HK1211868A1 (en) *	2012-09-26	2016-06-03	Tangent Reprofiling Limited	Modulators of androgen synthesis
EP3119399A4 (de)	2014-03-20	2017-09-27	Alkermes Pharma Ireland Limited	Aripiprazolformulierungen mit erhöhten injektionsgeschwindigkeiten
CN106831594B (zh) *	2017-01-18	2018-02-02	力赛生物医药科技（厦门）有限公司	可乐定双羟萘酸盐及其制备方法
CA3092335A1 (en)	2018-03-05	2019-09-12	Alkermes Pharma Ireland Limited	Aripiprazole dosing strategy
CN120698949A (zh) *	2022-02-22	2025-09-26	上海云晟研新生物科技有限公司	卡利拉嗪药用盐及其晶型、药物组合物、制备方法和用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4352811A (en) *	1981-11-12	1982-10-05	Hoechst-Roussel Pharmaceuticals Inc.	3-(1-Substituted-4-piperidyl)-1,2-benzisoxazoles
US4452799A (en) *	1981-12-23	1984-06-05	Mead Johnson & Company	Benzisothiazole and benzisoxazole piperazine derivatives
US4485107A (en) *	1982-11-01	1984-11-27	Janssen Pharmaceutica N.V.	[[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones
US4588722A (en) *	1984-01-09	1986-05-13	Janssen Pharmaceutica N.V.	N-(4-piperidinyl) bicyclic condensed 2-imidazolamine derivatives
US4804663A (en) *	1985-03-27	1989-02-14	Janssen Pharmaceutica N.V.	3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
GB9008850D0 (en) *	1990-04-19	1990-06-13	Janssen Pharmaceutica Nv	Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones

1994
- 1994-03-31 TW TW083102808A patent/TW376319B/zh not_active IP Right Cessation
- 1994-04-08 PH PH48074A patent/PH30476A/en unknown
- 1994-04-22 RO RO95-01879A patent/RO115955B1/ro unknown
- 1994-04-22 ES ES94915538T patent/ES2113652T3/es not_active Expired - Lifetime
- 1994-04-22 SG SG1996004131A patent/SG47046A1/en unknown
- 1994-04-22 SI SI9420031A patent/SI9420031B/sl unknown
- 1994-04-22 HU HU9501934A patent/HU218212B/hu unknown
- 1994-04-22 US US08/522,422 patent/US5612346A/en not_active Expired - Lifetime
- 1994-04-22 CA CA002160366A patent/CA2160366C/en not_active Expired - Lifetime
- 1994-04-22 DK DK94915538T patent/DK0697019T3/da active
- 1994-04-22 DE DE69408666T patent/DE69408666T2/de not_active Expired - Lifetime
- 1994-04-22 AT AT94915538T patent/ATE163418T1/de active
- 1994-04-22 EP EP94915538A patent/EP0697019B1/de not_active Expired - Lifetime
- 1994-04-22 SK SK1313-95A patent/SK280589B6/sk not_active IP Right Cessation
- 1994-04-22 RU RU95119831A patent/RU2131428C1/ru active
- 1994-04-22 WO PCT/EP1994/001296 patent/WO1994025460A1/en not_active Ceased
- 1994-04-22 NZ NZ266143A patent/NZ266143A/en not_active IP Right Cessation
- 1994-04-22 JP JP52386294A patent/JP3478397B2/ja not_active Expired - Lifetime
- 1994-04-22 PL PL94311282A patent/PL182466B1/pl unknown
- 1994-04-22 CN CN94191934A patent/CN1041727C/zh not_active Expired - Lifetime
- 1994-04-22 KR KR1019950704171A patent/KR100307101B1/ko not_active Expired - Lifetime
- 1994-04-22 AU AU67216/94A patent/AU675136B2/en not_active Expired
- 1994-04-22 CZ CZ19952706A patent/CZ286688B6/cs not_active IP Right Cessation
- 1994-04-26 ZA ZA942909A patent/ZA942909B/xx unknown
- 1994-04-27 IL IL109448A patent/IL109448A/xx not_active IP Right Cessation
1995
- 1995-10-25 BG BG100094A patent/BG62004B1/bg unknown
- 1995-10-26 NO NO954275A patent/NO305083B1/no not_active IP Right Cessation
- 1995-10-27 FI FI955166A patent/FI109125B/fi not_active IP Right Cessation
1996
- 1996-12-24 US US08/773,737 patent/US5723467A/en not_active Expired - Lifetime
1998
- 1998-02-26 GR GR980400198T patent/GR3026028T3/el unknown
- 1998-06-16 CY CY9800009A patent/CY2107B1/xx unknown
1999
- 1999-02-24 LV LVP-99-32A patent/LV12315B/en unknown

Also Published As

Publication number	Publication date
EP0697019B1 (de)	1998-02-25
NO305083B1 (no)	1999-03-29
JP3478397B2 (ja)	2003-12-15
LV12315B (en)	2000-03-20
WO1994025460A1 (en)	1994-11-10
US5612346A (en)	1997-03-18
SG47046A1 (en)	1998-03-20
TW376319B (en)	1999-12-11
IL109448A0 (en)	1994-07-31
NO954275D0 (no)	1995-10-26
JPH08509482A (ja)	1996-10-08
ATE163418T1 (de)	1998-03-15
CN1041727C (zh)	1999-01-20
PL182466B1 (pl)	2002-01-31
PL311282A1 (en)	1996-02-05
DE69408666T2 (de)	1998-06-18
PH30476A (en)	1997-05-28
NZ266143A (en)	1996-07-26
ES2113652T3 (es)	1998-05-01
HUT72970A (en)	1996-06-28
IL109448A (en)	1997-03-18
DE69408666D1 (de)	1998-04-02
CA2160366C (en)	2006-06-06
EP0697019A1 (de)	1996-02-21
BG100094A (bg)	1996-05-31
CA2160366A1 (en)	1994-11-10
SK280589B6 (sk)	2000-04-10
HU218212B (hu)	2000-06-28
KR100307101B1 (ko)	2001-11-30
US5723467A (en)	1998-03-03
LV12315A (lv)	1999-07-20
DK0697019T3 (da)	1998-09-28
GR3026028T3 (en)	1998-04-30
CZ286688B6 (en)	2000-06-14
CY2107B1 (en)	2002-04-26
ZA942909B (en)	1995-10-26
HU9501934D0 (en)	1995-09-28
HK1006059A1 (en)	1999-02-05
AU6721694A (en)	1994-11-21
SK131395A3 (en)	1996-06-05
CZ270695A3 (en)	1996-01-17
SI9420031A (en)	1996-08-31
SI9420031B (sl)	2002-08-31
RU2131428C1 (ru)	1999-06-10
NO954275L (no)	1995-10-26
FI955166A0 (fi)	1995-10-27
FI109125B (fi)	2002-05-31
RO115955B1 (ro)	2000-08-30
AU675136B2 (en)	1997-01-23
FI955166L (fi)	1995-10-27
CN1121719A (zh)	1996-05-01

Publication	Publication Date	Title
EP0697019B1 (de)	1998-02-25	Risperidon pamoate
KR0138529B1 (ko)	1998-05-15	카르보스티릴 유도체
US3676557A (en)	1972-07-11	Long-acting narcotic antagonist formulations
EP1075477B1 (de)	2003-03-12	Neue Benzonaphtyridin-N-oxide
DE69719778T2 (de)	2004-02-05	Benzonaphthyridine als bronchialtherapeutika
EP2586780A1 (de)	2013-05-01	2-aryl-imidazo-[1,2-a]-pyridin-3-acetamid-derivate,verfahren zu ihrer herstellung und ihre verwendung
JP2007502297A (ja)	2007-02-08	コリンエステラーゼ阻害剤を用いる睡眠障害の処置
US4647580A (en)	1987-03-03	Treatment of Alzheimer's disease
US4663456A (en)	1987-05-05	2-(substituted piperazinylalkyl)β-carbolines useful in treatment of psychological disorders
US3632653A (en)	1972-01-04	Ethano-anthracenes
HK1006059B (en)	1999-02-05	Risperidone pamoate
CN100457737C (zh)	2009-02-04	喹啉酰胺衍生物、其制备方法和用途
JPH0597827A (ja)	1993-04-20	新規の薬学活性成分としての２−イミノチアゾリジン−４−オン誘導体
US3432490A (en)	1969-03-11	2-(beta-hexamethylene imino ethyl) cyclohexanone - 2 - carboxylic acid benzyl ester and salts thereof
EP0407016A2 (de)	1991-01-09	Verwendung von Benzodioxinopyrrol-Derivaten zur Herstellung eines Arzneimittels zur Behandlung von Angstzuständen
EP0330468A2 (de)	1989-08-30	Verwendung von heterocyclischen Derivaten als kappa-Opiat-Rezeptoragonisten zur Behandlung der zerebralen Ischämie
JPH0368576A (ja)	1991-03-25	薬学的に活性な２―置換された３―（２―エトキシエチル）イミダゾ〔４，５―ｂ〕ピリジンおよび該化合物を含有する薬学的組成物
JPH0368575A (ja)	1991-03-25	薬理学的に活性なピペリジニルイミダゾピリジン
WO1994025030A1 (en)	1994-11-10	SUBSTITUTED DIOXOLO[4,5-g]FURO[3',4':6,7]INDOLIZINO[1,2-b]QUINOLINONES
EP0212783A2 (de)	1987-03-04	Verwendung von Imidazolinylaminoisoindolen und verwandten Verbindungen zur Behandlung von Hyperglykämie
HK1017852A1 (en)	1999-12-03	Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters
HK1017852B (en)	2002-03-08	Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters