NO323979B1 - Olanzapindihydrat D, farmasoytisk formulering, anvendelse av forbindelsen samt fremgangsmate for fremstilling av krystallinsk olanzapindihydrat D. - Google Patents

Olanzapindihydrat D, farmasoytisk formulering, anvendelse av forbindelsen samt fremgangsmate for fremstilling av krystallinsk olanzapindihydrat D. Download PDF

Info

Publication number: NO323979B1
Authority: NO; Norway
Prior art keywords: dihydrate; olanzapine; formulation; ray powder; approx
Prior art date: 1996-09-23

Application number

NO19991339A

Other languages

English (en)

Norwegian (no)

Other versions

NO991339L (no

NO991339D0 (no

Inventor

John R Nichols

Gregory A Stephenson

Susan M Reutzel

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

1999-03-19

Publication date

2007-07-30

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=21832112&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO323979(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1999-03-19 Application filed by Lilly Co Eli filed Critical Lilly Co Eli

1999-03-19 Publication of NO991339L publication Critical patent/NO991339L/no

1999-03-19 Publication of NO991339D0 publication Critical patent/NO991339D0/no

2007-07-30 Publication of NO323979B1 publication Critical patent/NO323979B1/no

Links

238000000034 method Methods 0.000 title claims description 22
150000001875 compounds Chemical class 0.000 title claims description 21
238000002360 preparation method Methods 0.000 title claims description 11
239000008194 pharmaceutical composition Substances 0.000 title 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 title claims description 7
230000008569 process Effects 0.000 title claims description 5
150000004683 dihydrates Chemical class 0.000 claims description 59
239000000203 mixture Substances 0.000 claims description 39
KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims description 30
229960005017 olanzapine Drugs 0.000 claims description 27
238000009472 formulation Methods 0.000 claims description 22
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OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
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239000013011 aqueous formulation Substances 0.000 description 6
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QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 3
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239000005711 Benzoic acid Substances 0.000 description 2
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
229930006000 Sucrose Natural products 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
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241000416162 Astragalus gummifer Species 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
239000004097 EU approved flavor enhancer Substances 0.000 description 1
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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
206010026749 Mania Diseases 0.000 description 1
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238000005481 NMR spectroscopy Methods 0.000 description 1
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ZVLDJSZFKQJMKD-UHFFFAOYSA-N [Li].[Si] Chemical compound [Li].[Si] ZVLDJSZFKQJMKD-UHFFFAOYSA-N 0.000 description 1
235000010489 acacia gum Nutrition 0.000 description 1
235000010443 alginic acid Nutrition 0.000 description 1
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229910021529 ammonia Inorganic materials 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
230000015572 biosynthetic process Effects 0.000 description 1
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239000002480 mineral oil Substances 0.000 description 1
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VOMXSOIBEJBQNF-UTTRGDHVSA-N novorapid Chemical compound C([C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CS)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CS)NC(=O)[C@H](CS)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(O)=O)C1=CC=C(O)C=C1.C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CS)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 VOMXSOIBEJBQNF-UTTRGDHVSA-N 0.000 description 1
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239000004033 plastic Substances 0.000 description 1
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239000003755 preservative agent Substances 0.000 description 1
238000011321 prophylaxis Methods 0.000 description 1
235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
239000012066 reaction slurry Substances 0.000 description 1
102000005962 receptors Human genes 0.000 description 1
108020003175 receptors Proteins 0.000 description 1
239000012056 semi-solid material Substances 0.000 description 1
239000011343 solid material Substances 0.000 description 1
239000000600 sorbitol Substances 0.000 description 1
235000010356 sorbitol Nutrition 0.000 description 1
238000010561 standard procedure Methods 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
239000000829 suppository Substances 0.000 description 1
230000002459 sustained effect Effects 0.000 description 1
238000013268 sustained release Methods 0.000 description 1
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239000000454 talc Substances 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
235000012222 talc Nutrition 0.000 description 1
238000010257 thawing Methods 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
235000010487 tragacanth Nutrition 0.000 description 1
239000000196 tragacanth Substances 0.000 description 1
229940116362 tragacanth Drugs 0.000 description 1
230000037317 transdermal delivery Effects 0.000 description 1
QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
238000003828 vacuum filtration Methods 0.000 description 1
239000003981 vehicle 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- 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
- 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
- A61P25/22—Anxiolytics
- 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
- A61P25/24—Antidepressants
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/38—[b, e]- or [b, f]-condensed with six-membered rings

Landscapes

Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Neurology (AREA)
Chemical Kinetics & Catalysis (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Psychiatry (AREA)
Pain & Pain Management (AREA)
Epidemiology (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)

NO19991339A 1996-09-23 1999-03-19 Olanzapindihydrat D, farmasoytisk formulering, anvendelse av forbindelsen samt fremgangsmate for fremstilling av krystallinsk olanzapindihydrat D. NO323979B1 (no)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US2648696P	1996-09-23	1996-09-23
PCT/US1997/016586 WO1998011893A1 (fr)	1996-09-23	1997-09-18	Dihydrate d d'olanzapine

Publications (3)

Publication Number	Publication Date
NO991339L NO991339L (no)	1999-03-19
NO991339D0 NO991339D0 (no)	1999-03-19
NO323979B1 true NO323979B1 (no)	2007-07-30

Family

ID=21832112

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NO19991339A NO323979B1 (no)	1996-09-23	1999-03-19	Olanzapindihydrat D, farmasoytisk formulering, anvendelse av forbindelsen samt fremgangsmate for fremstilling av krystallinsk olanzapindihydrat D.

Country Status (34)

Country	Link
US (1)	US6251895B1 (fr)
EP (1)	EP0831097B1 (fr)
JP (1)	JP2001500878A (fr)
KR (1)	KR100516088B1 (fr)
CN (1)	CN1146567C (fr)
AR (1)	AR009801A1 (fr)
AT (1)	ATE221074T1 (fr)
AU (1)	AU720366B2 (fr)
BR (1)	BR9711541A (fr)
CA (1)	CA2266444C (fr)
CO (1)	CO4900057A1 (fr)
CZ (1)	CZ299247B6 (fr)
DE (1)	DE69714165T2 (fr)
DK (1)	DK0831097T3 (fr)
EA (1)	EA001881B1 (fr)
EG (1)	EG23815A (fr)
ES (1)	ES2180899T3 (fr)
HU (1)	HU226167B1 (fr)
ID (1)	ID21924A (fr)
IL (1)	IL128956A0 (fr)
MY (1)	MY125467A (fr)
NO (1)	NO323979B1 (fr)
NZ (1)	NZ334346A (fr)
PE (1)	PE110298A1 (fr)
PL (1)	PL194074B1 (fr)
PT (1)	PT831097E (fr)
RS (1)	RS49597B (fr)
SI (1)	SI0831097T1 (fr)
SV (1)	SV1997000079A (fr)
TR (1)	TR199900639T2 (fr)
TW (1)	TW518335B (fr)
UA (1)	UA56184C2 (fr)
WO (1)	WO1998011893A1 (fr)
ZA (1)	ZA978512B (fr)

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- 1997-09-18 IL IL12895697A patent/IL128956A0/xx not_active IP Right Cessation
- 1997-09-18 CA CA002266444A patent/CA2266444C/fr not_active Expired - Fee Related
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- 1997-09-18 CZ CZ0098999A patent/CZ299247B6/cs not_active IP Right Cessation
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Publication number	Publication date
HU226167B1 (hu)	2008-05-28
CA2266444C (fr)	2007-01-09
CO4900057A1 (es)	2000-03-27
KR100516088B1 (ko)	2005-09-22
SI0831097T1 (en)	2003-02-28
CZ98999A3 (cs)	1999-08-11
EA199900325A1 (ru)	1999-08-26
CZ299247B6 (cs)	2008-05-28
EP0831097A3 (fr)	1998-04-29
ATE221074T1 (de)	2002-08-15
MY125467A (en)	2006-08-30
DK0831097T3 (da)	2002-09-02
SV1997000079A (es)	1999-01-13
JP2001500878A (ja)	2001-01-23
RS49597B (sr)	2007-06-04
EG23815A (en)	2007-08-19
PL194074B1 (pl)	2007-04-30
NO991339L (no)	1999-03-19
DE69714165T2 (de)	2003-01-23
DE69714165D1 (de)	2002-08-29
AU4424197A (en)	1998-04-14
NZ334346A (en)	2000-05-26
HUP0000065A3 (en)	2000-11-28
YU15499A (sh)	2000-03-21
AU720366B2 (en)	2000-06-01
ZA978512B (en)	1999-03-23
PE110298A1 (es)	1999-01-18
BR9711541A (pt)	1999-08-24
US6251895B1 (en)	2001-06-26
EP0831097A2 (fr)	1998-03-25
KR20000048519A (ko)	2000-07-25
NO991339D0 (no)	1999-03-19
AR009801A1 (es)	2000-05-03
EP0831097B1 (fr)	2002-07-24
IL128956A0 (en)	2000-02-17
CN1146567C (zh)	2004-04-21
UA56184C2 (uk)	2003-05-15
ES2180899T3 (es)	2003-02-16
CA2266444A1 (fr)	1998-03-26
WO1998011893A1 (fr)	1998-03-26
TR199900639T2 (xx)	1999-06-21
TW518335B (en)	2003-01-21
PT831097E (pt)	2002-10-31
PL332541A1 (en)	1999-09-13
EA001881B1 (ru)	2001-10-22
HK1009809A1 (en)	1999-06-11
ID21924A (id)	1999-08-12
CN1234738A (zh)	1999-11-10
HUP0000065A2 (hu)	2000-06-28

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2016-04-25	MM1K	Lapsed by not paying the annual fees

Publication	Publication Date	Title
AU720366B2 (en)	2000-06-01	Olanzapine dihydrate D
KR100399688B1 (ko)	2004-02-18	2-메틸-티에노-벤조디아제핀의결정형및그의제조방법
US5703232A (en)	1997-12-30	Process and solvate of 2-methyl-thieno-benzodiazepine
US5637584A (en)	1997-06-10	Solvate of olanzapine
EP1606231A1 (fr)	2005-12-21	Procede de preparation de clopidogrel, ses sels et compositions pharmaceutiques
US7897613B2 (en)	2011-03-01	Crystalline polymorphs of clopidogrel
IL85277A (en)	1994-02-27	Al-Mimi sodium salt, crystals of 5-chloro-3-) 2-methanol (-2-oxaindole-1 and its preparation
US5776928A (en)	1998-07-07	Method for treating dyskinesias with olanzapine
WO2011140816A1 (fr)	2011-11-17	Dérivé d'ester de thiénopyridine contenant du nitrile, procédé de préparation, utilisation et composition associés
KR101110738B1 (ko)	2012-02-17	(ｓ)-(+)-클로피도그렐 비설페이트의 상이한 형태의 제조 방법
CN108218928A (zh)	2018-06-29	葡萄糖苷的二环衍生物及其制备方法和用途
NO318553B1 (no)	2005-04-11	Anvendelse av 2-metyl-4-(4-metyl-1-piperazinyl)-10H-tieno[2,3-b][1,5]benzodiazepin for behandling av en kognitiv dysfunksjon.
JP2000506860A (ja)	2000-06-06	自閉症の処置方法
JPH08325151A (ja)	1996-12-10	食欲不振を治療する方法
CN105461569B (zh)	2017-06-06	一种枸橼酸阿尔维林新晶型及其制备方法
HK1009809B (en)	2003-05-09	Olanzapine dihydrate d
JP2000506858A (ja)	2000-06-06	過剰攻撃性の処置方法
US6506746B2 (en)	2003-01-14	Method for treating cognitive dysfunction
MXPA98001705A (en)	1998-10-23	Form of alternate glass of the tazofel
CA2219902A1 (fr)	1996-12-05	Utilisation du 2-methyl-4-(4-methyl-1-piperazinyl)-10h-thieno¬2,3b\|¬1,5\|benzodiazepine pour le traitement du dysfonctionnement cognitif
HK1009393B (en)	2003-05-16	Method for treating cognitive dysfunction