EA199800404A1 - Производные 1-(1,2-дизамещенный пиперидинил)-4-замещенного пиперазина - Google Patents
Производные 1-(1,2-дизамещенный пиперидинил)-4-замещенного пиперазинаInfo
- Publication number
- EA199800404A1 EA199800404A1 EA199800404A EA199800404A EA199800404A1 EA 199800404 A1 EA199800404 A1 EA 199800404A1 EA 199800404 A EA199800404 A EA 199800404A EA 199800404 A EA199800404 A EA 199800404A EA 199800404 A1 EA199800404 A1 EA 199800404A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- het
- 6alkyl
- formula
- substituted
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
-
- 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
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Настоящее изобретение относится к соединениям формулы (I)их N-оксидным формам, фармацевтически приемлемым аддитивным солям и стереоизомерным формам, где n равно 0, 1 или 2; m равно 1 или 2, при условии, что если m равно 2, то n равно 1; p равно 1 или 2; =Q представляет =O или =NR; X представляет ковалентную связь или двухвалентный радикал формулы -O-, -S-, -NR-; Rпредставляет Ar, ArCалкил или ди(Ar)Cалкил, где каждая Cалкильная группа необязательно замещена гидрокси, Cалкилокси, оксо или кетализированным оксозаместителем, Rпредставляет Ar, ArCалкил, Hetили HetCалкил; Rпредставляет водород или Cалкил; L представляет водород; Ar; Cалкил; Cалкил, замещенный 1 или 2 заместителями, выбранными из гидрокси, Cалкилокси, Ar, ArCалкилокси и Het; Cалкенил; ArCалкенил; ди(Ar)Cалкенил или радикал формулы (а-1), (а-2), (а-3), (а-4) или (а-5); каждый из Ar, Arи Arпредставляет фенил или замещенный фенил; каждый из Hetи Hetпредставляет моноциклический или бициклический гетероцикл; в качестве антагонистов вещества P; их получению, композициям, содержащим их, и их использованию в качестве лекарственного средства.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP95202929 | 1995-10-30 | ||
EP96937248A EP0862566B1 (en) | 1995-10-30 | 1996-10-25 | 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives |
PCT/EP1996/004660 WO1997016440A1 (en) | 1995-10-30 | 1996-10-25 | 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
EA199800404A1 true EA199800404A1 (ru) | 1998-10-29 |
EA000909B1 EA000909B1 (ru) | 2000-06-26 |
Family
ID=8220780
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA199800404A EA000909B1 (ru) | 1995-10-30 | 1996-10-25 | Производные 1-(1,2-дизамещенный пиперидинил)-4-замещенного пиперазина |
Country Status (31)
Country | Link |
---|---|
US (3) | US6197772B1 (ru) |
EP (1) | EP0862566B1 (ru) |
JP (1) | JP3073238B2 (ru) |
KR (1) | KR100407067B1 (ru) |
CN (2) | CN1117744C (ru) |
AR (1) | AR004698A1 (ru) |
AT (1) | ATE188691T1 (ru) |
AU (1) | AU704155B2 (ru) |
BR (1) | BR9611184B8 (ru) |
CA (1) | CA2234096C (ru) |
CY (1) | CY2177B1 (ru) |
CZ (1) | CZ291794B6 (ru) |
DE (1) | DE69606196T2 (ru) |
DK (1) | DK0862566T3 (ru) |
EA (1) | EA000909B1 (ru) |
ES (1) | ES2143238T3 (ru) |
GR (1) | GR3033154T3 (ru) |
HR (1) | HRP960507B1 (ru) |
HU (1) | HU227341B1 (ru) |
IL (1) | IL123962A (ru) |
MX (1) | MX9803407A (ru) |
MY (1) | MY116575A (ru) |
NO (1) | NO310232B1 (ru) |
NZ (1) | NZ321575A (ru) |
PL (1) | PL185029B1 (ru) |
PT (1) | PT862566E (ru) |
SI (1) | SI0862566T1 (ru) |
TR (1) | TR199800756T2 (ru) |
TW (1) | TW460473B (ru) |
WO (1) | WO1997016440A1 (ru) |
ZA (1) | ZA969090B (ru) |
Families Citing this family (48)
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NZ321575A (en) * | 1995-10-30 | 1999-05-28 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives |
TW382017B (en) | 1995-12-27 | 2000-02-11 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivatives |
TW429256B (en) * | 1995-12-27 | 2001-04-11 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4-(benzimidazolyl- and imidazopyridinyl)-piperidine derivatives |
TW531537B (en) | 1995-12-27 | 2003-05-11 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4-substituted piperidine derivatives |
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US6391865B1 (en) | 1999-05-04 | 2002-05-21 | Schering Corporation | Piperazine derivatives useful as CCR5 antagonists |
US6689765B2 (en) | 1999-05-04 | 2004-02-10 | Schering Corporation | Piperazine derivatives useful as CCR5 antagonists |
USRE39921E1 (en) | 1999-10-07 | 2007-11-13 | Smithkline Beecham Corporation | Chemical compounds |
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GB0025354D0 (en) | 2000-10-17 | 2000-11-29 | Glaxo Group Ltd | Chemical compounds |
PL364560A1 (en) | 2001-03-29 | 2004-12-13 | Schering Corporation | Ccr5 antagonists useful for treating aids |
GB0108594D0 (en) * | 2001-04-05 | 2001-05-23 | Glaxo Group Ltd | Chemical compounds |
GB0203022D0 (en) | 2002-02-08 | 2002-03-27 | Glaxo Group Ltd | Chemical compounds |
JP2005522436A (ja) * | 2002-02-08 | 2005-07-28 | グラクソ グループ リミテッド | ピペリジルカルボキシアミド誘導体またはそのタキキニン介在疾患の治療における使用 |
GB0203020D0 (en) * | 2002-02-08 | 2002-03-27 | Glaxo Group Ltd | Chemical compounds |
ES2326800T3 (es) | 2002-06-24 | 2009-10-20 | Janssen Pharmaceutica Nv | Proceso para la produccion de n-(2,6-dimetil-fenil)-2-piperazin-1-il-acetamida. |
MY141736A (en) * | 2002-10-08 | 2010-06-15 | Elanco Animal Health Ireland | Substituted 1,4-di-piperidin-4-yi-piperazine derivatives and their use as neurokinin antagonists |
WO2004056772A1 (en) * | 2002-12-23 | 2004-07-08 | Janssen Pharmaceutica N.V. | Substituted 1,4-di-piperidin-4-yl-piperazine derivatives and their use as tachykinin antagonists |
CA2501539A1 (en) * | 2002-10-17 | 2004-04-29 | Amgen Inc. | Benzimidazole derivatives and their use as vanilloid receptor ligands |
US7514424B2 (en) | 2002-12-23 | 2009-04-07 | Janssen Pharmaceutica N.V. | Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists |
WO2004056800A1 (en) | 2002-12-23 | 2004-07-08 | Janssen Pharmaceutica N.V. | Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists |
JO2485B1 (en) * | 2002-12-23 | 2009-01-20 | شركة جانسين فارماسوتيكا ان. في | 1-Piperidine-3-Yl-4-Piperidine-4-Yl-Piperazine derivatives substituted and used as quinine antagonists |
JO2696B1 (en) | 2002-12-23 | 2013-03-03 | شركة جانسين فارماسوتيكا ان. في | Derivatives of 1-piperdine-4-yl-4-biprolidine-3-yl-piperazine substituted and used as quinine antagonists |
ES2307025T3 (es) * | 2003-06-10 | 2008-11-16 | Janssen Pharmaceutica Nv | Combinacion de opioides y un derivado de la piperazina para el tratamiento del dolor. |
WO2004110415A2 (en) * | 2003-06-10 | 2004-12-23 | Janssen Pharmaceutica N.V. | Substituted 1, 4-di-piperidin-4-yl-piperazine derivative combined with an opioid analgesic and their use for the treatment of pain and side-effects associated with opioid-based treatments |
UY28538A1 (es) * | 2003-09-26 | 2005-04-29 | Vertex Pharma | Derivados de fenil-piperazina como moduladores de receptores muscarínicos |
JO2527B1 (en) * | 2004-04-06 | 2010-03-17 | شركة جانسين فارماسوتيكا ان. في | Derivatives of second-aza-Spiro- (5,5) -andecan and their use as antihistamines |
JO2676B1 (en) * | 2004-04-06 | 2012-06-17 | جانسين فارماسوتيكا ان. في | Derivatives of second-aza-spiro- (5,4) -dikan and their use as antihistamines |
JO2525B1 (en) * | 2004-04-08 | 2010-03-17 | شركة جانسين فارماسوتيكا ان. في | Derived 4-alkyl-and-4-canoelperidine derivatives and their use as anti-neroquin |
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ATE478075T1 (de) | 2005-03-08 | 2010-09-15 | Janssen Pharmaceutica Nv | Diazaspiro-ä4,4ü-nonanderivate als neurokinin- (nk1)-antagonisten |
CN101190330A (zh) | 2006-11-30 | 2008-06-04 | 深圳市鼎兴生物医药技术开发有限公司 | 胆碱酯酶在拮抗速激肽药物中的应用 |
EA200970706A1 (ru) | 2007-01-24 | 2010-02-26 | Глэксо Груп Лимитед | Новые фармацевтические композиции |
WO2010081851A1 (en) | 2009-01-14 | 2010-07-22 | Genoscience Pharma | Piperidin-4-ylpiperazine compounds for the treatment of hcv infection |
CN101913076B (zh) * | 2010-06-23 | 2012-09-05 | 中国科学院自动化研究所 | 基于工业机器人的活塞、活塞销和连杆装配方法及装置 |
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US9980973B2 (en) | 2012-10-19 | 2018-05-29 | Astex Therapeutics Limited | Bicyclic heterocycle compounds and their uses in therapy |
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SI3083616T1 (sl) | 2013-12-20 | 2021-12-31 | Astex Therapeutics Limited | Biciklične heterociklične spojine in njihova uporaba pri zdravljenju |
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NZ321575A (en) * | 1995-10-30 | 1999-05-28 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives |
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1994
- 1994-02-24 NZ NZ321575A patent/NZ321575A/xx not_active IP Right Cessation
-
1996
- 1996-10-24 TW TW085113017A patent/TW460473B/zh not_active IP Right Cessation
- 1996-10-25 KR KR10-1998-0702659A patent/KR100407067B1/ko not_active IP Right Cessation
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- 1996-10-25 DK DK96937248T patent/DK0862566T3/da active
- 1996-10-25 ES ES96937248T patent/ES2143238T3/es not_active Expired - Lifetime
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- 1996-10-25 HU HU9802985A patent/HU227341B1/hu unknown
- 1996-10-25 AT AT96937248T patent/ATE188691T1/de active
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- 1996-10-25 AU AU74932/96A patent/AU704155B2/en not_active Expired
- 1996-10-25 CN CNB021574278A patent/CN100415716C/zh not_active Expired - Lifetime
- 1996-10-25 PT PT96937248T patent/PT862566E/pt unknown
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- 1996-10-28 AR ARP960104941A patent/AR004698A1/es active IP Right Grant
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1998
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- 1998-04-03 NO NO19981534A patent/NO310232B1/no not_active IP Right Cessation
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2000
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2001
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