NO323980B1 - Krystallinsk dihydrat B eller E olanzapin, fremgangsmate for fremstilling av Form II olanzapin samt preparat - Google Patents

Krystallinsk dihydrat B eller E olanzapin, fremgangsmate for fremstilling av Form II olanzapin samt preparat Download PDF

Info

Publication number: NO323980B1
Authority: NO; Norway
Prior art keywords: dihydrate; olanzapine; preparation; ray powder; approx
Prior art date: 1996-09-23

Application number

NO19991382A

Other languages

English (en)

Norwegian (no)

Other versions

NO991382D0 (no

NO991382L (no

Inventor

John R Nichols

Gregory A Stephenson

Susan M Reutzel

Charles A Bunnell

Samuel D Larsen

Original Assignee

Lilly Co Eli

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.)

1996-09-23

Filing date

1999-03-22

Publication date

2007-07-30

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=21832120&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO323980(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1999-03-22 Application filed by Lilly Co Eli filed Critical Lilly Co Eli

1999-03-22 Publication of NO991382D0 publication Critical patent/NO991382D0/no

1999-03-22 Publication of NO991382L publication Critical patent/NO991382L/no

2007-07-30 Publication of NO323980B1 publication Critical patent/NO323980B1/no

Links

150000004683 dihydrates Chemical class 0.000 title claims description 56
KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 title claims description 35
229960005017 olanzapine Drugs 0.000 title claims description 33
238000000034 method Methods 0.000 title claims description 22
238000002360 preparation method Methods 0.000 title claims description 11
150000001875 compounds Chemical class 0.000 claims description 18
238000000634 powder X-ray diffraction Methods 0.000 claims description 12
238000004519 manufacturing process Methods 0.000 claims description 8
FUOBHGGXKJHKDF-UHFFFAOYSA-N 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine dihydrate Chemical compound O.O.C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 FUOBHGGXKJHKDF-UHFFFAOYSA-N 0.000 claims description 5
238000001035 drying Methods 0.000 claims description 3
239000013067 intermediate product Substances 0.000 claims description 2
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 14
239000000126 substance Substances 0.000 description 10
239000000843 powder Substances 0.000 description 9
239000000047 product Substances 0.000 description 9
238000006243 chemical reaction Methods 0.000 description 8
239000000543 intermediate Substances 0.000 description 8
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
238000002441 X-ray diffraction Methods 0.000 description 5
239000000203 mixture Substances 0.000 description 5
RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 4
239000003125 aqueous solvent Substances 0.000 description 4
229910052802 copper Inorganic materials 0.000 description 4
239000010949 copper Substances 0.000 description 4
238000003756 stirring Methods 0.000 description 4
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
241000124008 Mammalia Species 0.000 description 3
YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
238000004458 analytical method Methods 0.000 description 3
239000003960 organic solvent Substances 0.000 description 3
239000007787 solid Substances 0.000 description 3
239000011877 solvent mixture Substances 0.000 description 3
238000003828 vacuum filtration Methods 0.000 description 3
QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
239000012065 filter cake Substances 0.000 description 2
239000002904 solvent Substances 0.000 description 2
238000011282 treatment Methods 0.000 description 2
208000028017 Psychotic disease Diseases 0.000 description 1
241000251539 Vertebrata <Metazoa> Species 0.000 description 1
ZVLDJSZFKQJMKD-UHFFFAOYSA-N [Li].[Si] Chemical compound [Li].[Si] ZVLDJSZFKQJMKD-UHFFFAOYSA-N 0.000 description 1
229910021529 ammonia Inorganic materials 0.000 description 1
230000009286 beneficial effect Effects 0.000 description 1
210000003169 central nervous system Anatomy 0.000 description 1
239000003153 chemical reaction reagent Substances 0.000 description 1
239000013078 crystal Substances 0.000 description 1
238000000113 differential scanning calorimetry Methods 0.000 description 1
238000002050 diffraction method Methods 0.000 description 1
-1 dihydrate compound Chemical class 0.000 description 1
229940079593 drug Drugs 0.000 description 1
239000003814 drug Substances 0.000 description 1
230000008030 elimination Effects 0.000 description 1
238000003379 elimination reaction Methods 0.000 description 1
238000009472 formulation Methods 0.000 description 1
238000007429 general method Methods 0.000 description 1
238000004128 high performance liquid chromatography Methods 0.000 description 1
239000012535 impurity Substances 0.000 description 1
239000000463 material Substances 0.000 description 1
229910052757 nitrogen Inorganic materials 0.000 description 1
238000011321 prophylaxis Methods 0.000 description 1
239000011541 reaction mixture Substances 0.000 description 1
239000012066 reaction slurry Substances 0.000 description 1
239000013557 residual solvent Substances 0.000 description 1
239000002002 slurry Substances 0.000 description 1
239000012453 solvate Substances 0.000 description 1
239000007858 starting material Substances 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
- 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

NO19991382A 1996-09-23 1999-03-22 Krystallinsk dihydrat B eller E olanzapin, fremgangsmate for fremstilling av Form II olanzapin samt preparat NO323980B1 (no)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US2648796P	1996-09-23	1996-09-23
PCT/US1997/016499 WO1998012199A1 (en)	1996-09-23	1997-09-18	Intermediates and process for preparing olanzapine

Publications (3)

Publication Number	Publication Date
NO991382D0 NO991382D0 (no)	1999-03-22
NO991382L NO991382L (no)	1999-03-22
NO323980B1 true NO323980B1 (no)	2007-07-30

Family

ID=21832120

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NO19991382A NO323980B1 (no)	1996-09-23	1999-03-22	Krystallinsk dihydrat B eller E olanzapin, fremgangsmate for fremstilling av Form II olanzapin samt preparat

Country Status (36)

Country	Link
US (1)	US6020487A (id)
EP (1)	EP0831098B1 (id)
JP (2)	JP2001500877A (id)
KR (1)	KR100560015B1 (id)
CN (1)	CN1122036C (id)
AR (1)	AR013838A1 (id)
AT (1)	ATE209208T1 (id)
AU (1)	AU719441B2 (id)
BR (1)	BR9712100A (id)
CA (1)	CA2265712C (id)
CO (1)	CO4910140A1 (id)
CZ (1)	CZ299248B6 (id)
DE (1)	DE69708428T2 (id)
DK (1)	DK0831098T3 (id)
EA (1)	EA001642B1 (id)
EG (1)	EG23861A (id)
ES (1)	ES2166051T3 (id)
HK (1)	HK1009807A1 (id)
HU (1)	HU226484B1 (id)
ID (1)	ID27275A (id)
IL (1)	IL128962A (id)
IN (1)	IN187156B (id)
MY (1)	MY125565A (id)
NO (1)	NO323980B1 (id)
NZ (1)	NZ334448A (id)
PE (1)	PE110398A1 (id)
PL (3)	PL196069B1 (id)
PT (1)	PT831098E (id)
RS (1)	RS49598B (id)
SI (1)	SI0831098T1 (id)
SV (1)	SV1997000081A (id)
TR (1)	TR199900640T2 (id)
TW (1)	TW470746B (id)
UA (1)	UA59371C2 (id)
WO (1)	WO1998012199A1 (id)
ZA (1)	ZA978515B (id)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
SK2502003A3 (en) *	2000-08-31	2004-03-02	Reddys Lab Ltd Dr	Process for preparation of hydrates of olanzapine and their conversion into crystalline forms of olanzapine
US6740753B2 (en)	2001-01-04	2004-05-25	Geneva Pharmaceuticals, Inc.	Olanzapine crystal modification
WO2003037903A1 (en) *	2001-10-29	2003-05-08	Dr. Reddy's Laboratories Ltd.	Olanzapine dihydrate-ii a process for its preparation and use thereof
AU2002367119A1 (en)	2001-12-24	2003-07-15	Sun Pharmaceutical Industries Limited	Crystalline form I of 2-methyl-4-(4-methyl-1-piperazinyl) 10H thieno [2,3-b][1,5]benzodiazepine
WO2003091260A1 (en) *	2002-04-23	2003-11-06	Dr. Reddy's Laboratories Limited	Novel crystalline polymorph form-vi of olanzapine and a process for preparation thereof
WO2003101997A1 (en) *	2002-05-31	2003-12-11	Geneva Pharmaceuticals, Inc.	Process of preparation of olanzapine form i
SI21270A (sl)	2002-07-15	2004-02-29	Krka, Tovarna Zdravil, D.D., Novo Mesto	Kristalne oblike olanzapina in postopki za njihovo pripravo
AU2003300324A1 (en)	2002-12-24	2004-07-22	Teva Pharmaceutical Industries Ltd.	Novel crystal forms of olanzapine, methods for their preparation and method for the preparation of known olanzapine crystal forms
EP1684734A2 (en) *	2003-11-18	2006-08-02	3M Innovative Properties Company	Olanzapine containing transdermal drug delivery compositions
ES2308304T3 (es) *	2003-12-22	2008-12-01	Teva Pharmaceutical Industries Ltd.	Procedimientos de preparacion de la olanzapina.
ATE504588T1 (de)	2004-01-27	2011-04-15	Synthon Bv	Stabile salze von olanzapin
WO2005080401A1 (en) *	2004-02-19	2005-09-01	Neuland Laboratories Limited	Process for the preparation of olanzapine form 1 useful as antipsychotic drug
EP1781666A1 (en) *	2004-07-14	2007-05-09	Shasun Chemicals and Drugs Limited	Improved process for making form i of olanzapine.
ES2253091B1 (es)	2004-07-27	2007-02-01	Inke, S.A.	Solvato mixto de olanzapina, procedimiento para su obtencion y procedimiento de obtencion de la forma i de olanzapina a partir del mismo.
WO2006027800A1 (en) *	2004-09-06	2006-03-16	Shasun Chemicals And Drugs Limited	A novel process for preparation of a pharmaceutically pure polymorphic form 1 of olanzapine
EA200701065A1 (ru) *	2004-11-16	2007-12-28	Элан Фарма Интернэшнл Лтд.	Инъецируемые составы, содержащие нанодисперсный оланзапин
US7834176B2 (en)	2006-01-26	2010-11-16	Sandoz Ag	Polymorph E of Olanzapine and preparation of anhydrous non-solvated crystalline polymorphic Form I of 2-methyl-4(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine (Olanzapine Form I) from the polymorphic Olanzapine Form E
CA2591644A1 (en) *	2007-06-14	2008-12-14	Apotex Pharmachem Inc.	Novel processes to form-i of olanzapine
EP2486913A1 (en)	2011-02-14	2012-08-15	Labtec GmbH	Rapidly disintegrating oral film formulation for Olanzapin
JP6008734B2 (ja) *	2012-12-20	2016-10-19	株式会社トクヤマ	オランザピンｉｉ型結晶の製造方法

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5302716A (en) *	1986-01-16	1994-04-12	Schering Corporation	Fused benzazepines
CA2002596A1 (en) *	1988-11-14	1990-05-14	Thomas M. Eckrich	Hydrates of b-lactam antibiotic
GB9009229D0 (en) *	1990-04-25	1990-06-20	Lilly Industries Ltd	Pharmaceutical compounds
US5229382A (en) *	1990-04-25	1993-07-20	Lilly Industries Limited	2-methyl-thieno-benzodiazepine
AU668159B2 (en) *	1992-05-29	1996-04-26	Lilly Industries Limited	Pharmaceutical compounds
US5550231A (en) *	1993-06-15	1996-08-27	Eli Lilly And Company	Loracarbef hydrochloride C1-C3 alcohol solvates and uses thereof
US5602124A (en) *	1994-12-12	1997-02-11	Allelix Biopharmaceuticals, Inc.	5-HT2 receptor ligands
US5637584A (en) *	1995-03-24	1997-06-10	Eli Lilly And Company	Solvate of olanzapine
EG24221A (en) *	1995-03-24	2008-11-10	Lilly Co Eli	Process for preparing olanzapine
EG23659A (en) *	1995-03-24	2007-03-26	Lilly Co Eli	Process and crystal forms of methyl-thieno-benzodiazepine
US5631250A (en) *	1995-03-24	1997-05-20	Eli Lilly And Company	Process and solvate of 2-methyl-thieno-benzodiazepine
EA001881B1 (ru) *	1996-09-23	2001-10-22	Эли Лилли Энд Компани	Форма d дигидрата оланзапина

1997
- 1997-09-02 ZA ZA978515A patent/ZA978515B/xx unknown
- 1997-09-18 CN CN97198137A patent/CN1122036C/zh not_active Expired - Lifetime
- 1997-09-18 PL PL381478A patent/PL196069B1/pl unknown
- 1997-09-18 CZ CZ0099099A patent/CZ299248B6/cs not_active IP Right Cessation
- 1997-09-18 BR BR9712100-2A patent/BR9712100A/pt not_active Application Discontinuation
- 1997-09-18 NZ NZ334448A patent/NZ334448A/en not_active IP Right Cessation
- 1997-09-18 HU HU0000066A patent/HU226484B1/hu unknown
- 1997-09-18 JP JP10514842A patent/JP2001500877A/ja not_active Withdrawn
- 1997-09-18 IL IL12896297A patent/IL128962A/xx not_active IP Right Cessation
- 1997-09-18 RS YUP-155/99A patent/RS49598B/sr unknown
- 1997-09-18 EA EA199900326A patent/EA001642B1/ru not_active IP Right Cessation
- 1997-09-18 TR TR1999/00640T patent/TR199900640T2/xx unknown
- 1997-09-18 AU AU44841/97A patent/AU719441B2/en not_active Expired
- 1997-09-18 UA UA99031635A patent/UA59371C2/uk unknown
- 1997-09-18 PL PL97332482A patent/PL194565B1/pl unknown
- 1997-09-18 ID IDW990058D patent/ID27275A/id unknown
- 1997-09-18 WO PCT/US1997/016499 patent/WO1998012199A1/en not_active Application Discontinuation
- 1997-09-18 CA CA002265712A patent/CA2265712C/en not_active Expired - Lifetime
- 1997-09-18 KR KR1019997002424A patent/KR100560015B1/ko not_active IP Right Cessation
- 1997-09-18 PL PL381479A patent/PL196068B1/pl unknown
- 1997-09-19 IN IN1736CA1997 patent/IN187156B/en unknown
- 1997-09-22 PT PT97307383T patent/PT831098E/pt unknown
- 1997-09-22 ES ES97307383T patent/ES2166051T3/es not_active Expired - Lifetime
- 1997-09-22 EP EP97307383A patent/EP0831098B1/en not_active Expired - Lifetime
- 1997-09-22 SI SI9730288T patent/SI0831098T1/xx unknown
- 1997-09-22 MY MYPI97004392A patent/MY125565A/en unknown
- 1997-09-22 DK DK97307383T patent/DK0831098T3/da active
- 1997-09-22 CO CO97055061A patent/CO4910140A1/es unknown
- 1997-09-22 AT AT97307383T patent/ATE209208T1/de active
- 1997-09-22 SV SV1997000081A patent/SV1997000081A/es not_active Application Discontinuation
- 1997-09-22 DE DE69708428T patent/DE69708428T2/de not_active Expired - Lifetime
- 1997-09-23 PE PE1997000855A patent/PE110398A1/es active IP Right Grant
- 1997-09-23 AR ARP970104362A patent/AR013838A1/es not_active Application Discontinuation
- 1997-09-23 EG EG98697A patent/EG23861A/xx active
- 1997-09-23 US US08/935,884 patent/US6020487A/en not_active Expired - Lifetime
1998
- 1998-02-27 TW TW086113832A patent/TW470746B/zh not_active IP Right Cessation
- 1998-09-21 HK HK98110796A patent/HK1009807A1/xx not_active IP Right Cessation
1999
- 1999-03-22 NO NO19991382A patent/NO323980B1/no not_active IP Right Cessation
2009
- 2009-06-05 JP JP2009135901A patent/JP2009242407A/ja active Pending

Also Published As

Publication number	Publication date
HU226484B1 (en)	2009-03-02
BR9712100A (pt)	1999-08-31
PL196068B1 (pl)	2007-12-31
PL196069B1 (pl)	2007-12-31
MY125565A (en)	2006-08-30
NZ334448A (en)	2000-08-25
WO1998012199A1 (en)	1998-03-26
UA59371C2 (uk)	2003-09-15
DK0831098T3 (da)	2002-05-21
CN1234802A (zh)	1999-11-10
EA001642B1 (ru)	2001-06-25
NO991382D0 (no)	1999-03-22
DE69708428D1 (de)	2002-01-03
KR20000048520A (ko)	2000-07-25
JP2001500877A (ja)	2001-01-23
JP2009242407A (ja)	2009-10-22
KR100560015B1 (ko)	2006-03-15
EP0831098A2 (en)	1998-03-25
EA199900326A1 (ru)	1999-08-26
SI0831098T1 (en)	2002-04-30
AU4484197A (en)	1998-04-14
ID27275A (id)	2001-03-22
CA2265712C (en)	2006-10-31
HUP0000066A2 (hu)	2000-06-28
EG23861A (en)	2007-11-18
TW470746B (en)	2002-01-01
EP0831098A3 (en)	1998-04-29
CZ299248B6 (cs)	2008-05-28
CA2265712A1 (en)	1998-03-26
PL194565B1 (pl)	2007-06-29
NO991382L (no)	1999-03-22
IN187156B (id)	2002-02-16
PL332482A1 (en)	1999-09-13
SV1997000081A (es)	1999-01-14
ZA978515B (en)	1999-03-23
ES2166051T3 (es)	2002-04-01
ATE209208T1 (de)	2001-12-15
RS49598B (sr)	2007-06-04
AR013838A1 (es)	2001-01-31
PT831098E (pt)	2002-04-29
TR199900640T2 (xx)	1999-06-21
CN1122036C (zh)	2003-09-24
US6020487A (en)	2000-02-01
PE110398A1 (es)	1999-01-14
HUP0000066A3 (en)	2000-11-28
HK1009807A1 (en)	1999-06-11
IL128962A (en)	2003-01-12
YU15599A (sh)	2001-12-26
AU719441B2 (en)	2000-05-11
CO4910140A1 (es)	2000-04-24
DE69708428T2 (de)	2002-07-04
IL128962A0 (en)	2000-02-17
CZ99099A3 (cs)	1999-11-17
EP0831098B1 (en)	2001-11-21

Legal Events

Date	Code	Title	Description
2017-10-09	MK1K	Patent expired

Publication	Publication Date	Title
NO323980B1 (no)	2007-07-30	Krystallinsk dihydrat B eller E olanzapin, fremgangsmate for fremstilling av Form II olanzapin samt preparat
EP1313742A1 (en)	2003-05-28	Process for preparation of hydrates of olanzapine and their conversion into crystalline forms of olanzapine
JP6055817B2 (ja)	2016-12-27	ナフチリジンの調製方法
EP0733634B1 (en)	2000-11-22	Process for preparing a thieno(2,3-B)(1,5) benzodiazepine derivative
HRP20050039A2 (en)	2005-08-31	Crystal forms of olanzapine and processes for their preparation
CZ200641A3 (cs)	2006-05-17	Zpusob prípravy krystalického polymorfu inhibitoru srázení krevních desticek
US20040067936A1 (en)	2004-04-08	Process for preparation of hydrates of olanzapine and their conversion into crystalline forms of olanzapine
US7829700B2 (en)	2010-11-09	Process for preparation of a pharmaceutically pure polymorphic form I of Olanzapine
WO2007102167A1 (en)	2007-09-13	A process for the preparation of anhydrous polymorphic form of olanzapine
AU2003249262B2 (en)	2008-08-14	Process for the preparation of imidazo(1,2-a)pyridine-3-acetamides
EP1730153A1 (en)	2006-12-13	Isopropanol water solvate of olanzapine
ZA200301640B (en)	2004-02-03	Process for preparation of hydrates of Olanzapine and their conversion into cystalline forms of Olanzapine.
MXPA03001827A (es)	2004-11-01	Proceso para la preparacion de hidratos de olanzapina y su conversion a formas cristalinas de olanzapina.
ITMI20012597A1 (it)	2003-06-11	Sintesi dell'1-(3-trifluorometilfenil)-2-(-2-benzoilossietilammino)-propano
KR20030078086A (ko)	2003-10-04	미르타자핀 중간체의 제조방법
HU226773B1 (en)	2009-09-28	Process for the production of clopidogrel hydrogensulfate polymorph 1
SI21746A (sl)	2005-10-31	Kristalne oblike olanzapina in postopki za njihovo pripravo
MX2008014836A (es)	2008-12-01	Sales y modificaciones del cristal de las mismas.