ATE396174T1 - Hydroxyalkylaminderivate als beta-secretase- inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheiten - Google Patents
Hydroxyalkylaminderivate als beta-secretase- inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheitenInfo
- Publication number
- ATE396174T1 ATE396174T1 AT02741841T AT02741841T ATE396174T1 AT E396174 T1 ATE396174 T1 AT E396174T1 AT 02741841 T AT02741841 T AT 02741841T AT 02741841 T AT02741841 T AT 02741841T AT E396174 T1 ATE396174 T1 AT E396174T1
- Authority
- AT
- Austria
- Prior art keywords
- disease
- alzheimer
- hydroxyalkylamine
- beta
- derivatives
- Prior art date
Links
- 208000024827 Alzheimer disease Diseases 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 239000002439 beta secretase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
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- C07C317/50—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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- C—CHEMISTRY; METALLURGY
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- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings 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
- C07D307/20—Oxygen atoms
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- C—CHEMISTRY; METALLURGY
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- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings 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
- C07D309/10—Oxygen atoms
- C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
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- C—CHEMISTRY; METALLURGY
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- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
- C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D317/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D319/04—1,3-Dioxanes; Hydrogenated 1,3-dioxanes
- C07D319/06—1,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
- C07D333/30—Hetero atoms other than halogen
- C07D333/32—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
- C07D333/30—Hetero atoms other than halogen
- C07D333/34—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/46—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom
- C07D333/48—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
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- Organic Chemistry (AREA)
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- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Pyrrole Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Furan Compounds (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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| US34377201P | 2001-12-28 | 2001-12-28 |
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| EP (1) | EP1395551B1 (de) |
| JP (1) | JP2004535421A (de) |
| AT (1) | ATE396174T1 (de) |
| AU (1) | AU2002314914A1 (de) |
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| CA (1) | CA2448834A1 (de) |
| DE (1) | DE60226729D1 (de) |
| ES (1) | ES2307764T3 (de) |
| MX (1) | MXPA03011046A (de) |
| WO (1) | WO2002098849A2 (de) |
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| CA2410972A1 (en) | 2000-06-30 | 2002-01-10 | Elan Pharmaceuticals, Inc. | Compounds to treat alzheimer's disease |
| CA2448834A1 (en) * | 2001-06-01 | 2002-12-12 | Elan Pharmaceuticals, Inc. | Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer's disease and similar diseases |
| AU2002360508A1 (en) | 2001-12-06 | 2003-06-23 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamines |
| UY27967A1 (es) * | 2002-09-10 | 2004-05-31 | Pfizer | Acetil 2-hindroxi-1,3-diaminoalcanos |
| AU2003293155A1 (en) * | 2002-11-27 | 2004-06-23 | Elan Pharmaceutical, Inc. | Substituted ureas and carbamates |
| GB0300804D0 (en) * | 2003-01-14 | 2003-02-12 | Novo Pharmaceuticals De Ltd | Compounds and their use |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| WO2005070407A1 (en) * | 2004-01-21 | 2005-08-04 | Elan Pharmaceuticals, Inc. | Methods of treatment of amyloidosis using aspartyl-protease inihibitors |
| US20050239790A1 (en) * | 2004-03-09 | 2005-10-27 | Varghese John | Substituted hydroxyethylamine aspartyl protease inhibitors |
| WO2005087751A2 (en) * | 2004-03-09 | 2005-09-22 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamine aspartyl protease inhibitors |
| CA2573138A1 (en) | 2004-07-09 | 2006-01-26 | Elan Pharmaceuticals Inc. | Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors |
| US20060128715A1 (en) * | 2004-07-09 | 2006-06-15 | Jennifer Sealy | Oxime derivative hydroxyethylamine aspartyl-protease inhibitors |
| WO2006043710A1 (ja) * | 2004-10-19 | 2006-04-27 | Reverse Proteomics Research Institute Co., Ltd. | 創薬標的タンパク質及び標的遺伝子、並びにスクリーニング方法 |
| BRPI0607019A2 (pt) | 2005-04-08 | 2009-07-28 | Univ Illinois | compostos que inibem a atividade de beta -secretase e métodos de uso dos mesmos |
| WO2007047305A1 (en) | 2005-10-12 | 2007-04-26 | Elan Pharmaceuticals, Inc. | Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors |
| JP5379692B2 (ja) | 2006-11-09 | 2013-12-25 | プロビオドルグ エージー | 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての3−ヒドロキシ−1,5−ジヒドロ−ピロール−2−オン誘導体 |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| AU2008220785B2 (en) | 2007-03-01 | 2013-02-21 | Vivoryon Therapeutics N.V. | New use of glutaminyl cyclase inhibitors |
| JP5667440B2 (ja) | 2007-04-18 | 2015-02-12 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体 |
| WO2009129532A1 (en) * | 2008-04-18 | 2009-10-22 | University Of Connecticut | Compounds for lysosomal modulation and methods of use |
| EP2291181B9 (de) | 2008-04-18 | 2013-09-11 | University College Dublin National University Of Ireland, Dublin | Captodiamine zur Behandlung von depressionartigen Symptomen |
| NZ598685A (en) | 2009-09-11 | 2013-05-31 | Probiodrug Ag | Heterocylcic derivatives as inhibitors of glutaminyl cyclase |
| JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤 |
| DK2545047T3 (da) | 2010-03-10 | 2014-07-28 | Probiodrug Ag | Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5) |
| EP2560953B1 (de) | 2010-04-21 | 2016-01-06 | Probiodrug AG | Hemmer der glutaminylzyklase |
| US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
| TW201823208A (zh) | 2016-09-07 | 2018-07-01 | 美商普萊恩醫療公司 | N-醯基胺基酸化合物及其使用方法 |
| EP3461819B1 (de) | 2017-09-29 | 2020-05-27 | Probiodrug AG | Hemmer der glutaminylcyclase |
| CN112135612B (zh) | 2018-03-07 | 2025-06-17 | 普利安特治疗公司 | 氨基酸化合物和使用方法 |
| EP3952902A4 (de) | 2019-04-08 | 2022-12-21 | Pliant Therapeutics, Inc. | Darreichungsformen und therapieschemata für aminosäureverbindungen |
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| US3587742A (en) * | 1969-09-08 | 1971-06-28 | Shell Oil Co | Consolidation of shallow formations with acid modified epoxy resinous material |
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| US5211811A (en) * | 1989-02-15 | 1993-05-18 | Union Camp Patent Holding, Inc. | Process for high consistency oxygen delignification of alkaline treated pulp followed by ozone delignification |
| ATE260974T1 (de) | 1990-06-15 | 2004-03-15 | Scios Inc | Transgenes, nicht-menschliches säugetier das die amyloidbildende pathologie der alzheimerschen krankheit zeigt |
| US5912410A (en) * | 1990-06-15 | 1999-06-15 | Scios Inc. | Transgenic non-human mice displaying the amyloid-forming pathology of alzheimer's disease |
| AU652997B2 (en) * | 1991-01-21 | 1994-09-15 | Elan Pharmaceuticals, Inc. | Test and model for alzheimer's disease |
| ES2204899T3 (es) * | 1992-01-07 | 2004-05-01 | Elan Pharmaceuticals, Inc. | Modelos de animales transgenicos para la enfermedad de alzheimer. |
| US5441870A (en) * | 1992-04-15 | 1995-08-15 | Athena Neurosciences, Inc. | Methods for monitoring cellular processing of β-amyloid precursor protein |
| US5604102A (en) * | 1992-04-15 | 1997-02-18 | Athena Neurosciences, Inc. | Methods of screening for β-amyloid peptide production inhibitors |
| US5766846A (en) * | 1992-07-10 | 1998-06-16 | Athena Neurosciences | Methods of screening for compounds which inhibit soluble β-amyloid peptide production |
| US5783701A (en) * | 1992-09-08 | 1998-07-21 | Vertex Pharmaceuticals, Incorporated | Sulfonamide inhibitors of aspartyl protease |
| DK0730643T3 (da) * | 1993-10-27 | 2001-05-14 | Elan Pharm Inc | Transgene dyr, som huser APP-allel med svensk mutation |
| US5877399A (en) * | 1994-01-27 | 1999-03-02 | Johns Hopkins University | Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease |
| JPH11507538A (ja) * | 1995-06-07 | 1999-07-06 | アテナ ニューロサイエンシズ インコーポレイティド | β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ |
| US5744346A (en) * | 1995-06-07 | 1998-04-28 | Athena Neurosciences, Inc. | β-secretase |
| PT948630E (pt) | 1996-11-20 | 2008-06-11 | Oklahoma Med Res Found | Clonagem e caracterização da napsina, uma protease aspártica |
| US6191166B1 (en) * | 1997-11-21 | 2001-02-20 | Elan Pharmaceuticals, Inc. | Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis |
| ATE287402T1 (de) * | 1997-02-04 | 2005-02-15 | Univ California | Nanomolare, non-peptidische inhibitoren von cathepsin d |
| GB9812189D0 (en) | 1998-06-05 | 1998-08-05 | Glaxo Group Ltd | Methods and compositions for increasing penetration of HIV protease inhibitors |
| AU5002399A (en) | 1998-07-17 | 2000-02-07 | National Broach And Machine Company | Full form roll finishing technique |
| DK1115874T3 (da) | 1998-09-24 | 2009-04-20 | Pharmacia & Upjohn Co Llc | Alzheimer's sygdom-sekretase |
| AU4000900A (en) | 1999-02-10 | 2000-08-29 | Elan Pharmaceuticals, Inc. | Beta-secretase enzyme compositions and methods |
| JP2002539260A (ja) * | 1999-03-24 | 2002-11-19 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | アスパルチルプロテアーゼインヒビターを使用して神経変性障害を処置する方法 |
| JP2003523944A (ja) | 1999-08-09 | 2003-08-12 | ヴァンダービルト ユニヴァースティ | P−糖タンパク質修飾物質を用いる抗ウィルス療法 |
| ATE431419T1 (de) | 1999-09-23 | 2009-05-15 | Pharmacia & Upjohn Co Llc | Alzheimer krankheit sekretase, app (amyloid vorlaüfer-protein) substrate dafür und verwendungen |
| AU779875B2 (en) | 2000-01-24 | 2005-02-17 | Merck Sharp & Dohme Limited | Gamma-secretase inhibitors |
| GB0005251D0 (en) | 2000-03-03 | 2000-04-26 | Merck Sharp & Dohme | Therapeutic compounds |
| EP1265849B1 (de) | 2000-03-23 | 2006-10-25 | Elan Pharmaceuticals, Inc. | Verbindungen und verfahren zur behandlung der alzheimerschen krankheit |
| CA2410972A1 (en) | 2000-06-30 | 2002-01-10 | Elan Pharmaceuticals, Inc. | Compounds to treat alzheimer's disease |
| CA2448834A1 (en) * | 2001-06-01 | 2002-12-12 | Elan Pharmaceuticals, Inc. | Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer's disease and similar diseases |
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2002
- 2002-05-31 CA CA002448834A patent/CA2448834A1/en not_active Abandoned
- 2002-05-31 US US10/160,777 patent/US7144897B2/en not_active Expired - Fee Related
- 2002-05-31 WO PCT/US2002/017698 patent/WO2002098849A2/en not_active Ceased
- 2002-05-31 BR BR0210122-0A patent/BR0210122A/pt not_active IP Right Cessation
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- 2002-05-31 DE DE60226729T patent/DE60226729D1/de not_active Expired - Fee Related
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- 2002-05-31 EP EP02741841A patent/EP1395551B1/de not_active Expired - Lifetime
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- 2006-12-06 US US11/567,616 patent/US20070299263A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP1395551B1 (de) | 2008-05-21 |
| WO2002098849A3 (en) | 2003-11-13 |
| JP2004535421A (ja) | 2004-11-25 |
| MXPA03011046A (es) | 2004-06-25 |
| US20030166717A1 (en) | 2003-09-04 |
| DE60226729D1 (de) | 2008-07-03 |
| US7144897B2 (en) | 2006-12-05 |
| WO2002098849A2 (en) | 2002-12-12 |
| CA2448834A1 (en) | 2002-12-12 |
| EP1395551A2 (de) | 2004-03-10 |
| ES2307764T3 (es) | 2008-12-01 |
| BR0210122A (pt) | 2004-06-15 |
| AU2002314914A1 (en) | 2002-12-16 |
| US20070299263A1 (en) | 2007-12-27 |
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