RU2000105271A - CRYSTALLINE DERIVATIVE OF DIBENZOTIAZEPINE AND ITS USE AS AN AGENT FOR ANTI-PSYCHOSIS - Google Patents
CRYSTALLINE DERIVATIVE OF DIBENZOTIAZEPINE AND ITS USE AS AN AGENT FOR ANTI-PSYCHOSISInfo
- Publication number
- RU2000105271A RU2000105271A RU2000105271/04A RU2000105271A RU2000105271A RU 2000105271 A RU2000105271 A RU 2000105271A RU 2000105271/04 A RU2000105271/04 A RU 2000105271/04A RU 2000105271 A RU2000105271 A RU 2000105271A RU 2000105271 A RU2000105271 A RU 2000105271A
- Authority
- RU
- Russia
- Prior art keywords
- ethyl
- thiazepine
- dibenzo
- hydroxyethoxy
- piperazinyl
- Prior art date
Links
- URKOMYMAXPYINW-UHFFFAOYSA-N Quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 claims 18
- 239000003849 aromatic solvent Substances 0.000 claims 14
- BZLVMXJERCGZMT-UHFFFAOYSA-N MeOtBu Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 238000002425 crystallisation Methods 0.000 claims 5
- 230000005712 crystallization Effects 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000011780 sodium chloride Substances 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N acetic acid ethyl ester Chemical group CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- 239000008346 aqueous phase Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N (E)-but-2-enedioate;hydron Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 2
- 150000001450 anions Chemical class 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000012071 phase Substances 0.000 claims 2
- QPPOMEOQNLTFRU-UHFFFAOYSA-N 1,4-Thiazepine Chemical compound S1C=CC=NC=C1 QPPOMEOQNLTFRU-UHFFFAOYSA-N 0.000 claims 1
- VRHJBWUIWQOFLF-WLHGVMLRSA-N 2-[2-(4-benzo[b][1,4]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol;(E)-but-2-enedioic acid Chemical compound OC(=O)\C=C\C(O)=O.C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 VRHJBWUIWQOFLF-WLHGVMLRSA-N 0.000 claims 1
- BOCDFJFSOVIHBY-UHFFFAOYSA-N 2-[2-(4-benzo[b][1,4]benzothiazepin-7-ylpiperazin-1-yl)ethoxy]ethanol Chemical compound C1CN(CCOCCO)CCN1C1=CC=CC2=C1C=NC1=CC=CC=C1S2 BOCDFJFSOVIHBY-UHFFFAOYSA-N 0.000 claims 1
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 claims 1
- 206010061920 Psychotic disease Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 239000001530 fumaric acid Substances 0.000 claims 1
- FGKJLKRYENPLQH-UHFFFAOYSA-M isocaproate Chemical compound CC(C)CCC([O-])=O FGKJLKRYENPLQH-UHFFFAOYSA-M 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 239000012074 organic phase Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 238000000746 purification Methods 0.000 claims 1
- 238000000926 separation method Methods 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- YXFVVABEGXRONW-UHFFFAOYSA-N toluene Substances CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
Claims (22)
и после этого, если требуется фармацевтически приемлемая соль, проведения реакции 11-(4-[2-(2-гидpoкcиэтoкcи)этил] -1-пиперазинил)-дибензо[b, f] [1,4] тиазепина с кислотой, которая предоставляет фармацевтически приемлемый анион.4. A method for producing crystalline 11- (4- [2- (2-hydroxyethoxy) ethyl] -1-piperazinyl) dibenzo [b, f] [1,4] thiazepine or a pharmaceutically acceptable salt thereof, which comprises the steps of 11- crystallization (4- [2- (2-hydroxyethoxy) ethyl] -1-piperazinyl) dibenzo [b, f] [1,4] thiazepine from a non-aromatic solvent;
and then, if a pharmaceutically acceptable salt is required, a reaction of 11- (4- [2- (2-hydroxyethoxy) ethyl] -1-piperazinyl) dibenzo [b, f] [1,4] thiazepine with an acid that provides a pharmaceutically acceptable anion.
а) добавления воды и кислоты к раствору 11-(4-[2-(2-гидроксиэтокси)этил] -1-пиперазинил)-дибензо[b, f] [1,4] тиазепина в ароматическом растворителе;
b) разделения водной и органической фаз;
с) добавления к водной фазе неароматического растворителя и основания;
d) разделения водной фазы и фазы неароматического растворителя;
e) высушивания фазы неароматического растворителя;
f) кристаллизации 11-(4-[2-(2-гидроксиэтокси)этил] -1-пиперазинил)дибензо[b, f] [1,4] тиазепина из неароматического растворителя; и после этого, если требуется фармацевтически приемлемая соль, проведения реакции 11-(4-[2-(2-гидроксиэтокси)этил] -пиперазинил)-дибензо[b, f] [1,4] тиазепина с кислотой, которая предоставляет фармацевтически приемлемый анион.17. A method of obtaining crystalline 11- (4- [2- (2-hydroxyethoxy) ethyl] -1-piperazinyl) dibenzo [b, f] [1,4] thiazepine or its pharmaceutically acceptable salt from a solution of 11- (4- [2- (2-hydroxyethoxy) ethyl] -1-piperazinyl) dibenzo [b, f] - [1,4] thiazepine in an aromatic solvent, the method comprising the steps of:
a) adding water and acid to a solution of 11- (4- [2- (2-hydroxyethoxy) ethyl] -1-piperazinyl) dibenzo [b, f] [1,4] thiazepine in an aromatic solvent;
b) separation of the aqueous and organic phases;
c) adding to the aqueous phase a non-aromatic solvent and base;
d) separating the aqueous phase and the non-aromatic solvent phase;
e) drying the non-aromatic solvent phase;
f) crystallization of 11- (4- [2- (2-hydroxyethoxy) ethyl] -1-piperazinyl) dibenzo [b, f] [1,4] thiazepine from a non-aromatic solvent; and then, if a pharmaceutically acceptable salt is required, reacting 11- (4- [2- (2-hydroxyethoxy) ethyl] piperazinyl) dibenzo [b, f] [1,4] thiazepine with an acid that provides a pharmaceutically acceptable anion.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9716161.6 | 1997-08-01 | ||
GBGB9716161.6A GB9716161D0 (en) | 1997-08-01 | 1997-08-01 | Process |
Publications (2)
Publication Number | Publication Date |
---|---|
RU2000105271A true RU2000105271A (en) | 2002-03-20 |
RU2224754C2 RU2224754C2 (en) | 2004-02-27 |
Family
ID=10816746
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2000105271/04A RU2224754C2 (en) | 1997-08-01 | 1998-07-28 | Crystalline derivative of dibenzothiazepine, method for preparing and pharmaceutical composition based on thereof |
Country Status (32)
Country | Link |
---|---|
US (2) | US6372734B1 (en) |
EP (2) | EP1000043B1 (en) |
JP (2) | JP2001512109A (en) |
KR (1) | KR20010022241A (en) |
CN (1) | CN1125058C (en) |
AT (2) | ATE444959T1 (en) |
AU (1) | AU739255B2 (en) |
BG (1) | BG64796B1 (en) |
BR (1) | BR9811061A (en) |
CA (1) | CA2295792C (en) |
CY (2) | CY2200162T2 (en) |
CZ (1) | CZ299225B6 (en) |
DE (4) | DE05011169T1 (en) |
EE (1) | EE04550B1 (en) |
ES (2) | ES2296568T3 (en) |
GB (2) | GB9716161D0 (en) |
HK (2) | HK1029992A1 (en) |
HU (1) | HU228620B1 (en) |
ID (1) | ID24219A (en) |
IL (1) | IL133618A (en) |
MY (1) | MY120999A (en) |
NO (1) | NO20000484L (en) |
NZ (1) | NZ501914A (en) |
PL (1) | PL338384A1 (en) |
PT (2) | PT1000043E (en) |
RU (1) | RU2224754C2 (en) |
SI (2) | SI1589008T1 (en) |
SK (1) | SK287145B6 (en) |
TR (1) | TR200000848T2 (en) |
TW (1) | TW533207B (en) |
WO (1) | WO1999006381A1 (en) |
ZA (1) | ZA986904B (en) |
Families Citing this family (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2003080065A1 (en) * | 2002-03-20 | 2003-10-02 | Teva Pharmaceutical Industries Ltd. | Crystalline forms of quetiapine hemifumarate |
CA2516646A1 (en) | 2003-02-22 | 2004-09-10 | Teva Pharmaceutical Industries Ltd. | Synthesis of quetiapine and pharmaceutically acceptable salts thereof |
WO2004078735A1 (en) * | 2003-03-03 | 2004-09-16 | Hetero Drugs Limited | Novel polymorphs of quetiapine fumarate |
US7053115B2 (en) | 2003-04-07 | 2006-05-30 | Hetero Drugs Limited | Crystalline form of dorzolamide hydrochloride |
ES2223294B2 (en) | 2003-08-08 | 2005-10-01 | Vita Cientifica, S.L. | PREPARATION PROCEDURE FOR A PHARMACEUTICALLY ACTIVE COMPOUND. |
US20060081361A1 (en) * | 2004-09-13 | 2006-04-20 | Gabbey Lawrence W | Oil cooler with integral filter |
WO2006035293A1 (en) * | 2004-09-27 | 2006-04-06 | Ranbaxy Laboratories Limited | Polymorphic forms of quetiapine hemifumarate |
GB0425729D0 (en) * | 2004-11-23 | 2004-12-22 | Pliva Res & Dev Ltd | Heterocyclic compounds |
WO2006056772A2 (en) * | 2004-11-23 | 2006-06-01 | Pliva Hrvatska D.O.O. | Salts of quetiapine |
ES2234447B1 (en) * | 2005-03-07 | 2006-03-01 | Union Quimico-Farmaceutica S.A. | PROCEDURE FOR OBTAINING A DERIVATIVE OF 11- (4-SUBSTITUTED-1-PIPERAZINIL) DIBENZO (B, F) (1,4) THIAZEPINE. |
EP1869007A1 (en) * | 2005-04-14 | 2007-12-26 | Teva Pharmaceutical Industries Ltd | Process for preparing quetiapine fumarate |
US20070072840A1 (en) * | 2005-05-30 | 2007-03-29 | Pandya Bhargav | Polymorphic forms of quetiapine |
US8044038B2 (en) * | 2005-09-30 | 2011-10-25 | Fermion Oy | Crystallization process of quetiapine hemifumarate |
WO2007048870A1 (en) * | 2005-10-28 | 2007-05-03 | Fermion Oy | Quetiapine hemifumarate purification by crystallization |
EP1951258A4 (en) * | 2005-11-18 | 2013-01-02 | Astrazeneca Ab | Liquid formulations |
US20100022510A1 (en) * | 2005-11-18 | 2010-01-28 | Astrazeneca Ab | Crystalline Forms |
US8389510B2 (en) * | 2005-11-18 | 2013-03-05 | Astrazeneca Ab | Crystalline forms |
JP2009516705A (en) * | 2005-11-18 | 2009-04-23 | アストラゼネカ・アクチエボラーグ | Salt form |
JP2009516707A (en) * | 2005-11-18 | 2009-04-23 | アストラゼネカ・アクチエボラーグ | Solid preparation |
CZ300451B6 (en) * | 2006-07-03 | 2009-05-20 | Farmak, A. S. | Process for preparing salts of 2-[2-(4-dibenzo[b,f][1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol (quetiapine) and purification process of such salts |
WO2008066620A2 (en) * | 2006-10-20 | 2008-06-05 | Concert Pharmaceuticals Inc. | Dibenzothiazepine derivatives |
EP1958617B1 (en) | 2007-02-14 | 2010-09-08 | Laboratorios Lesvi, S.L. | Pharmaceutical compositions containing quetiapine fumarate |
JP2009529062A (en) * | 2007-03-29 | 2009-08-13 | テバ ファーマシューティカル インダストリーズ リミティド | An improved method for preparing quetiapine fumarate |
WO2009004480A2 (en) * | 2007-05-07 | 2009-01-08 | Actavis Group Ptc Ehf | Quetiapine salts and their polymorphs |
US20090082334A1 (en) * | 2007-09-25 | 2009-03-26 | Protia, Llc | Deuterium-enriched quetiapine |
AU2008333226B2 (en) * | 2007-12-05 | 2013-02-07 | Janssen Pharmaceutica Nv | Dibenzoazepine and dibenzooxazepine TRPA1 agonists |
PT2262486E (en) | 2008-08-01 | 2013-03-27 | Tovarna Zdravil D D Novo Mesto Krka | Quetiapine composition |
WO2010033270A1 (en) * | 2008-09-17 | 2010-03-25 | Auspex Pharmaceuticals, Inc. | Dibenzothiazepine modulators of dopamine, alpha adrenergic, and serotonin receptors |
WO2010100623A1 (en) | 2009-03-04 | 2010-09-10 | Ranbaxy Laboratories Limited | Process for the preparation of quetiapine fumarate |
EP3216877B1 (en) | 2011-08-12 | 2020-10-21 | QIAGEN GmbH | Method for isolating nucleic acids |
Family Cites Families (3)
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BE787249A (en) | 1971-08-05 | 1973-02-05 | Squibb & Sons Inc | AMINO DERIVATIVES OF PYRAZOLOPYRIDINE CARBOXYLIC ACIDS, THEIR ESTERS AND THE SALTS OF SUCH COMPOUNDS, AS WELL AS THEIR PREPARATION PROCESSES |
GB8607684D0 (en) * | 1986-03-27 | 1986-04-30 | Ici America Inc | Thiazepine compounds |
GB8705574D0 (en) * | 1987-03-10 | 1987-04-15 | Ici Plc | Preparation of thiazepine compound |
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1997
- 1997-08-01 GB GBGB9716161.6A patent/GB9716161D0/en active Pending
-
1998
- 1998-07-10 GB GBGB9814882.8A patent/GB9814882D0/en active Pending
- 1998-07-28 SK SK130-2000A patent/SK287145B6/en not_active IP Right Cessation
- 1998-07-28 BR BR9811061-6A patent/BR9811061A/en not_active Application Discontinuation
- 1998-07-28 AT AT98936529T patent/ATE444959T1/en active
- 1998-07-28 EE EEP200000062A patent/EE04550B1/en not_active IP Right Cessation
- 1998-07-28 IL IL13361898A patent/IL133618A/en not_active IP Right Cessation
- 1998-07-28 EP EP98936529A patent/EP1000043B1/en not_active Expired - Lifetime
- 1998-07-28 TR TR2000/00848T patent/TR200000848T2/en unknown
- 1998-07-28 RU RU2000105271/04A patent/RU2224754C2/en not_active IP Right Cessation
- 1998-07-28 ES ES05011169T patent/ES2296568T3/en not_active Expired - Lifetime
- 1998-07-28 KR KR1020007000814A patent/KR20010022241A/en active Search and Examination
- 1998-07-28 HU HU0002663A patent/HU228620B1/en not_active IP Right Cessation
- 1998-07-28 DE DE05011169T patent/DE05011169T1/en active Pending
- 1998-07-28 PL PL98338384A patent/PL338384A1/en not_active Application Discontinuation
- 1998-07-28 CA CA002295792A patent/CA2295792C/en not_active Expired - Fee Related
- 1998-07-28 AU AU85498/98A patent/AU739255B2/en not_active Ceased
- 1998-07-28 DE DE69842104T patent/DE69842104D1/en not_active Expired - Lifetime
- 1998-07-28 TW TW087112313A patent/TW533207B/en not_active IP Right Cessation
- 1998-07-28 ES ES98936529T patent/ES2296575T3/en not_active Expired - Lifetime
- 1998-07-28 PT PT98936529T patent/PT1000043E/en unknown
- 1998-07-28 CN CN98807572A patent/CN1125058C/en not_active Expired - Fee Related
- 1998-07-28 DE DE69841216T patent/DE69841216D1/en not_active Expired - Lifetime
- 1998-07-28 NZ NZ501914A patent/NZ501914A/en not_active IP Right Cessation
- 1998-07-28 PT PT05011169T patent/PT1589008E/en unknown
- 1998-07-28 DE DE98936529T patent/DE98936529T1/en active Pending
- 1998-07-28 JP JP2000505140A patent/JP2001512109A/en active Pending
- 1998-07-28 AT AT05011169T patent/ATE496037T1/en active
- 1998-07-28 US US09/463,452 patent/US6372734B1/en not_active Expired - Lifetime
- 1998-07-28 EP EP05011169A patent/EP1589008B1/en not_active Expired - Lifetime
- 1998-07-28 WO PCT/GB1998/002260 patent/WO1999006381A1/en active IP Right Grant
- 1998-07-28 ID IDW20000029A patent/ID24219A/en unknown
- 1998-07-28 SI SI9830929T patent/SI1589008T1/en unknown
- 1998-07-28 SI SI9830923T patent/SI1000043T1/en unknown
- 1998-07-28 CZ CZ20000341A patent/CZ299225B6/en not_active IP Right Cessation
- 1998-07-29 MY MYPI98003471A patent/MY120999A/en unknown
- 1998-07-31 ZA ZA986904A patent/ZA986904B/en unknown
-
2000
- 2000-01-31 NO NO20000484A patent/NO20000484L/en unknown
- 2000-02-22 BG BG104176A patent/BG64796B1/en unknown
-
2001
- 2001-02-01 HK HK01100731A patent/HK1029992A1/en not_active IP Right Cessation
-
2002
- 2002-03-21 US US10/101,948 patent/US20020147186A1/en not_active Abandoned
-
2006
- 2006-02-21 HK HK06102272.9A patent/HK1081962A1/en not_active IP Right Cessation
-
2008
- 2008-03-04 CY CY20082200005T patent/CY2200162T2/en unknown
- 2008-03-04 CY CY20082200004T patent/CY2200161T2/en unknown
- 2008-12-09 JP JP2008313248A patent/JP2009102345A/en active Pending
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