IL112134A - Substituted morpholine derivatives their preparation and pharmaceutical compositions containing them - Google Patents

Substituted morpholine derivatives their preparation and pharmaceutical compositions containing them

Info

Publication number: IL112134A
Authority: IL; Israel
Prior art keywords: hydrogen; 4alkyl; substituted; halogen; optionally substituted
Prior art date: 1993-12-29

Application number

IL11213494A

Other languages

English (en)

Other versions

IL112134A0 (en

Original Assignee

Merck Sharp & Dohme

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.)

1993-12-29

Filing date

1994-12-23

Publication date

1999-12-22

1993-12-29 Priority claimed from GB9326480A external-priority patent/GB9326480D0/en

1994-04-12 Priority claimed from GB9407189A external-priority patent/GB9407189D0/en

1994-04-22 Priority claimed from GB9408065A external-priority patent/GB9408065D0/en

1994-08-15 Priority claimed from GB9416428A external-priority patent/GB9416428D0/en

1994-12-23 Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme

1995-03-15 Publication of IL112134A0 publication Critical patent/IL112134A0/xx

1999-12-22 Publication of IL112134A publication Critical patent/IL112134A/xx

Links

150000002780 morpholines Chemical class 0.000 title 1
239000008194 pharmaceutical composition Substances 0.000 title 1
229910052739 hydrogen Inorganic materials 0.000 abstract 5
239000001257 hydrogen Substances 0.000 abstract 5
125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
229910052736 halogen Inorganic materials 0.000 abstract 3
150000002367 halogens Chemical class 0.000 abstract 3
150000002431 hydrogen Chemical class 0.000 abstract 3
125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
150000001875 compounds Chemical class 0.000 abstract 2
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
206010061218 Inflammation Diseases 0.000 abstract 1
208000019695 Migraine disease Diseases 0.000 abstract 1
JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
208000002193 Pain Diseases 0.000 abstract 1
206010047700 Vomiting Diseases 0.000 abstract 1
125000004103 aminoalkyl group Chemical group 0.000 abstract 1
125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
230000004054 inflammatory process Effects 0.000 abstract 1
206010027599 migraine Diseases 0.000 abstract 1
125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
229940002612 prodrug Drugs 0.000 abstract 1
239000000651 prodrug Substances 0.000 abstract 1
150000003839 salts Chemical class 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory 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
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
- 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
- A61P25/06—Antimigraine agents
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/6533—Six-membered rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Medicinal Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmacology & Pharmacy (AREA)
General Chemical & Material Sciences (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Engineering & Computer Science (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Molecular Biology (AREA)
Biochemistry (AREA)
Pain & Pain Management (AREA)
Hospice & Palliative Care (AREA)
Otolaryngology (AREA)
Psychiatry (AREA)
Immunology (AREA)
Rheumatology (AREA)
Pulmonology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Plural Heterocyclic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

IL11213494A 1993-12-29 1994-12-23 Substituted morpholine derivatives their preparation and pharmaceutical compositions containing them IL112134A (en)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date	Title
GB9326480A GB9326480D0 (en)	1993-12-29	1993-12-29	Therapeutic agents
GB9407189A GB9407189D0 (en)	1994-04-12	1994-04-12	Therapeutic agents
GB9408065A GB9408065D0 (en)	1994-04-22	1994-04-22	Therapeutic agents
GB9416428A GB9416428D0 (en)	1994-08-15	1994-08-15	Therapeutic agents

Publications (2)

Publication Number	Publication Date
IL112134A0 IL112134A0 (en)	1995-03-15
IL112134A true IL112134A (en)	1999-12-22

Family

ID=27451102

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL11213494A IL112134A (en)	1993-12-29	1994-12-23	Substituted morpholine derivatives their preparation and pharmaceutical compositions containing them

Country Status (24)

Country	Link
US (1)	US5612337A (de)
EP (3)	EP1462450B1 (de)
JP (2)	JP3071467B2 (de)
KR (1)	KR100286412B1 (de)
CN (1)	CN1067683C (de)
AT (3)	ATE364606T1 (de)
BG (1)	BG62616B1 (de)
BR (1)	BR9408442A (de)
CA (1)	CA2178219C (de)
CZ (1)	CZ288176B6 (de)
DE (3)	DE69428913T2 (de)
DK (1)	DK0737192T3 (de)
ES (1)	ES2164758T3 (de)
HU (1)	HU221139B1 (de)
IL (1)	IL112134A (de)
LV (1)	LV11687B (de)
NO (1)	NO307090B1 (de)
NZ (1)	NZ277839A (de)
PL (1)	PL181214B1 (de)
RU (1)	RU2131426C1 (de)
SG (1)	SG52217A1 (de)
SK (1)	SK283070B6 (de)
TW (1)	TW449588B (de)
WO (1)	WO1995018124A1 (de)

Families Citing this family (133)

* Cited by examiner, † Cited by third party
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GB9417956D0 (en) *	1994-09-02	1994-10-26	Merck Sharp & Dohme	Therapeutic agents
GB9426104D0 (en) *	1994-12-23	1995-02-22	Merck Sharp & Dohme	Use of surfactants and emulsions
GB9505491D0 (en) *	1995-03-18	1995-05-03	Merck Sharp & Dohme	Therapeutic agents
GB9513972D0 (en) *	1995-07-08	1995-09-06	Merck Sharp & Dohme	Pharmaceutical compositions
GB9523244D0 (en) *	1995-11-14	1996-01-17	Merck Sharp & Dohme	Therapeutic agents
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ATE265209T1 (de) *	1996-07-17	2004-05-15	Merck & Co Inc	Änderung des zirkadischen rhythmus mit nicht- peptidischen neurokinin-1 rezeptor antagonisten
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DE69732492T2 (de) *	1996-12-02	2006-03-30	Merck Sharp & Dohme Ltd., Hoddesdon	Verwendung von nk-1 rezeptorantagonisten zur behandlung von schweren depressionen, die von angstzuständen begleitet werden
US6114315A (en) *	1996-12-02	2000-09-05	Merck Sharp & Dohme Ltd.	Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety
US6100256A (en) *	1996-12-02	2000-08-08	Merck Sharp & Dohme Ltd.	Use of NK-1 receptors antagonists for treating schizophrenic disorders
CA2273810A1 (en) *	1996-12-02	1998-06-11	Merck Sharp & Dohme Limited	Use of nk-1 receptor antagonists for treating major depressive disorders
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JP2001504848A (ja) *	1996-12-02	2001-04-10	メルクシヤープエンドドームリミテツド	重症不安障害の治療のためのｎｋ−１受容体拮抗薬の使用
CA2273853A1 (en) *	1996-12-02	1998-06-11	Merck Sharp & Dohme Limited	Use of nk-1 receptor antagonists for treating cognitive disorders
JP2001504851A (ja) *	1996-12-02	2001-04-10	メルクシヤープエンドドームリミテツド	性的機能不全の治療のためのｎｋ−１受容体拮抗薬の使用
EP0942735A1 (de) *	1996-12-02	1999-09-22	MERCK SHARP & DOHME LTD.	Die verwendung von nk-1 rezeptor antagonisten für die behandlung von schizophrenischen störungen
AU734872B2 (en) *	1996-12-02	2001-06-21	Merck Sharp & Dohme Limited	Use of NK-1 receptor antagonists for treating movement disorders
EP0942730A1 (de) *	1996-12-02	1999-09-22	MERCK SHARP & DOHME LTD.	Die verwendung von nk-1 rezeptor antagonisten für die behandlung von bipolaren störungen
GB9700555D0 (en) *	1997-01-13	1997-03-05	Merck Sharp & Dohme	Therapeutic agents
JP2001524960A (ja) *	1997-04-24	2001-12-04	メルクシヤープエンドドームリミテツド	摂食障害を治療するためのｎｋ−１受容体拮抗薬の使用
GB9716457D0 (en) *	1997-08-04	1997-10-08	Merck Sharp & Dohme	Therapeutic agents
CA2298779A1 (en) *	1997-08-04	1999-02-18	Merck Sharp & Dohme Limited	Use of nk-1 receptor antagonists for treating aggressive behaviour disorders
AU738047B2 (en) *	1997-08-04	2001-09-06	Merck Sharp & Dohme Limited	Use of NK-1 receptor antagonists for treating mania
GB9716463D0 (en) *	1997-08-04	1997-10-08	Merck Sharp & Dohme	Therapeutic agents
US6156749A (en) *	1997-12-01	2000-12-05	Merck Sharp & Dohme Limited	Use of NK-1 receptor antagonists for treating movement disorders
US6087348A (en) *	1997-12-01	2000-07-11	Merck Sharp & Dohme Ltd.	Use of NK-1 receptor antagonists for treating stress disorders
US5972938A (en) *	1997-12-01	1999-10-26	Merck & Co., Inc.	Method for treating or preventing psychoimmunological disorders
US6271230B1 (en)	1997-12-01	2001-08-07	Merck Sharp & Dohme Limited	Use of NK-1 receptor antagonists for treating cognitive disorders
GB9810092D0 (en) *	1998-05-11	1998-07-08	Merck Sharp & Dohme	Therapeutic agents
GB9812662D0 (en) *	1998-06-11	1998-08-12	Merck Sharp & Dohme	Therapeutic use
WO1999064006A1 (en) *	1998-06-11	1999-12-16	Merck Sharp & Dohme Limited	Use of a nk-1 receptor antagonist for treating psychiatric disorders
GB9812664D0 (en) *	1998-06-11	1998-08-12	Merck Sharp & Dohme	Therapeutic use
GB9812617D0 (en) *	1998-06-11	1998-08-12	Merck Sharp & Dohme	Therapeutic use
JP2002517448A (ja) *	1998-06-11	2002-06-18	メルクシャープエンドドームリミテッド	精神障害の治療用ｎｋ−１受容体アンタゴニストの使用
GB9813025D0 (en)	1998-06-16	1998-08-12	Merck Sharp & Dohme	Chemical synthesis
GB9816897D0 (en) *	1998-08-04	1998-09-30	Merck Sharp & Dohme	Therapeutic use
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1994
- 1994-12-23 IL IL11213494A patent/IL112134A/xx not_active IP Right Cessation
- 1994-12-23 NZ NZ277839A patent/NZ277839A/en unknown
- 1994-12-23 SK SK839-96A patent/SK283070B6/sk unknown
- 1994-12-23 AT AT04076888T patent/ATE364606T1/de not_active IP Right Cessation
- 1994-12-23 ES ES95904621T patent/ES2164758T3/es not_active Expired - Lifetime
- 1994-12-23 DE DE69428913T patent/DE69428913T2/de not_active Expired - Fee Related
- 1994-12-23 RU RU96116158/04A patent/RU2131426C1/ru not_active IP Right Cessation
- 1994-12-23 BR BR9408442A patent/BR9408442A/pt not_active Application Discontinuation
- 1994-12-23 DE DE69434991T patent/DE69434991T2/de not_active Expired - Fee Related
- 1994-12-23 AT AT95904621T patent/ATE207917T1/de not_active IP Right Cessation
- 1994-12-23 DK DK95904621T patent/DK0737192T3/da active
- 1994-12-23 US US08/663,201 patent/US5612337A/en not_active Expired - Fee Related
- 1994-12-23 EP EP04076888A patent/EP1462450B1/de not_active Expired - Lifetime
- 1994-12-23 WO PCT/GB1994/002819 patent/WO1995018124A1/en not_active Ceased
- 1994-12-23 PL PL94315182A patent/PL181214B1/pl not_active IP Right Cessation
- 1994-12-23 KR KR1019960703426A patent/KR100286412B1/ko not_active Expired - Fee Related
- 1994-12-23 AT AT01200308T patent/ATE278687T1/de not_active IP Right Cessation
- 1994-12-23 JP JP7517856A patent/JP3071467B2/ja not_active Expired - Lifetime
- 1994-12-23 CN CN94194722A patent/CN1067683C/zh not_active Expired - Fee Related
- 1994-12-23 CA CA002178219A patent/CA2178219C/en not_active Expired - Fee Related
- 1994-12-23 DE DE69434063T patent/DE69434063D1/de not_active Expired - Lifetime
- 1994-12-23 EP EP95904621A patent/EP0737192B1/de not_active Expired - Lifetime
- 1994-12-23 HU HU9601801A patent/HU221139B1/hu not_active IP Right Cessation
- 1994-12-23 SG SG1996000578A patent/SG52217A1/en unknown
- 1994-12-23 EP EP01200308A patent/EP1099702B1/de not_active Expired - Lifetime
- 1994-12-23 CZ CZ19961898A patent/CZ288176B6/cs not_active IP Right Cessation
1995
- 1995-03-20 TW TW084102683A patent/TW449588B/zh active
1996
- 1996-06-06 BG BG100644A patent/BG62616B1/bg unknown
- 1996-06-19 LV LVP-96-197A patent/LV11687B/lv unknown
- 1996-06-28 NO NO962749A patent/NO307090B1/no unknown
2000
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Publication number	Publication date
EP1099702A1 (de)	2001-05-16
NO307090B1 (no)	2000-02-07
DE69434063D1 (de)	2004-11-11
KR100286412B1 (ko)	2001-04-16
BR9408442A (pt)	1997-08-05
BG100644A (bg)	1997-03-31
EP1462450A1 (de)	2004-09-29
ATE207917T1 (de)	2001-11-15
TW449588B (en)	2001-08-11
NZ277839A (en)	1998-01-26
JPH09507484A (ja)	1997-07-29
AU1322395A (en)	1995-07-17
CA2178219C (en)	2005-03-22
LV11687A (lv)	1997-02-20
CN1139927A (zh)	1997-01-08
EP0737192A1 (de)	1996-10-16
JP2000219629A (ja)	2000-08-08
CZ288176B6 (en)	2001-05-16
HU9601801D0 (en)	1996-09-30
SK283070B6 (sk)	2003-02-04
PL315182A1 (en)	1996-10-14
US5612337A (en)	1997-03-18
CZ189896A3 (en)	1996-12-11
DE69428913D1 (de)	2001-12-06
LV11687B (en)	1997-10-20
NO962749L (no)	1996-08-28
IL112134A0 (en)	1995-03-15
DE69434991D1 (de)	2007-07-26
HU221139B1 (en)	2002-08-28
WO1995018124A1 (en)	1995-07-06
DK0737192T3 (da)	2001-11-26
EP1099702B1 (de)	2004-10-06
NO962749D0 (no)	1996-06-28
EP1462450B1 (de)	2007-06-13
DE69434991T2 (de)	2008-03-06
AU685209B2 (en)	1998-01-15
CN1067683C (zh)	2001-06-27
JP3071467B2 (ja)	2000-07-31
ES2164758T3 (es)	2002-03-01
PL181214B1 (pl)	2001-06-29
CA2178219A1 (en)	1995-07-06
EP0737192B1 (de)	2001-10-31
HUT75872A (en)	1997-05-28
RU2131426C1 (ru)	1999-06-10
SG52217A1 (en)	1998-09-28
SK83996A3 (en)	1996-11-06
DE69428913T2 (de)	2002-05-29
ATE278687T1 (de)	2004-10-15
BG62616B1 (bg)	2000-03-31
ATE364606T1 (de)	2007-07-15

Legal Events

Date	Code	Title
2000-06-01	FF	Patent granted
2000-08-31	KB	Patent renewed
2001-06-14	KB	Patent renewed
2005-09-25	MM9K	Patent not in force due to non-payment of renewal fees

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