JP2003524393A5 - - Google Patents
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- JP2003524393A5 JP2003524393A5 JP2000598533A JP2000598533A JP2003524393A5 JP 2003524393 A5 JP2003524393 A5 JP 2003524393A5 JP 2000598533 A JP2000598533 A JP 2000598533A JP 2000598533 A JP2000598533 A JP 2000598533A JP 2003524393 A5 JP2003524393 A5 JP 2003524393A5
- Authority
- JP
- Japan
- Prior art keywords
- secretase
- compound
- fragment
- seq
- protein
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 description 36
- 150000001875 compounds Chemical class 0.000 description 35
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 description 34
- 238000000034 method Methods 0.000 description 20
- 239000012634 fragment Substances 0.000 description 18
- 210000004027 cell Anatomy 0.000 description 10
- 230000000694 effects Effects 0.000 description 10
- 238000004519 manufacturing process Methods 0.000 description 7
- 102000039446 nucleic acids Human genes 0.000 description 7
- 108020004707 nucleic acids Proteins 0.000 description 7
- 150000007523 nucleic acids Chemical class 0.000 description 7
- 108090000623 proteins and genes Proteins 0.000 description 7
- 102000004169 proteins and genes Human genes 0.000 description 7
- 239000002439 beta secretase inhibitor Substances 0.000 description 6
- 238000012216 screening Methods 0.000 description 6
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 description 5
- 239000003112 inhibitor Substances 0.000 description 5
- 108090000765 processed proteins & peptides Proteins 0.000 description 5
- 208000024827 Alzheimer disease Diseases 0.000 description 4
- 150000001413 amino acids Chemical class 0.000 description 4
- 230000006933 amyloid-beta aggregation Effects 0.000 description 4
- 239000000758 substrate Substances 0.000 description 4
- 125000003275 alpha amino acid group Chemical group 0.000 description 3
- 229920001184 polypeptide Polymers 0.000 description 3
- 102000004196 processed proteins & peptides Human genes 0.000 description 3
- 230000001105 regulatory effect Effects 0.000 description 3
- 229940126585 therapeutic drug Drugs 0.000 description 3
- IMROMDMJAWUWLK-UHFFFAOYSA-N Ethenol Chemical group OC=C IMROMDMJAWUWLK-UHFFFAOYSA-N 0.000 description 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 2
- 206010002022 amyloidosis Diseases 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 230000014509 gene expression Effects 0.000 description 2
- 239000011159 matrix material Substances 0.000 description 2
- 230000002018 overexpression Effects 0.000 description 2
- 238000006467 substitution reaction Methods 0.000 description 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 description 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 210000004899 c-terminal region Anatomy 0.000 description 1
- 230000003930 cognitive ability Effects 0.000 description 1
- 230000003931 cognitive performance Effects 0.000 description 1
- 238000012258 culturing Methods 0.000 description 1
- 238000012217 deletion Methods 0.000 description 1
- 230000037430 deletion Effects 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 239000013604 expression vector Substances 0.000 description 1
- 239000001963 growth medium Substances 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 238000011813 knockout mouse model Methods 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11957199P | 1999-02-10 | 1999-02-10 | |
| US60/119,571 | 1999-02-10 | ||
| US13917299P | 1999-06-15 | 1999-06-15 | |
| US60/139,172 | 1999-06-15 | ||
| PCT/US2000/003819 WO2000047618A2 (en) | 1999-02-10 | 2000-02-10 | HUMAN β-SECRETASE ENZYME, INHIBITORS AND THEIR COMPOSITIONS AND USES |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003524393A JP2003524393A (ja) | 2003-08-19 |
| JP2003524393A5 true JP2003524393A5 (https=) | 2007-03-29 |
| JP4653318B2 JP4653318B2 (ja) | 2011-03-16 |
Family
ID=26817477
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000598533A Expired - Fee Related JP4653318B2 (ja) | 1999-02-10 | 2000-02-10 | βセクレターゼ酵素組成物および方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US6627739B1 (https=) |
| EP (1) | EP1165609A2 (https=) |
| JP (1) | JP4653318B2 (https=) |
| CN (1) | CN1390232A (https=) |
| AU (1) | AU4000900A (https=) |
| CA (1) | CA2359785A1 (https=) |
| GB (1) | GB2364059B (https=) |
| HK (2) | HK1044545A1 (https=) |
| NZ (1) | NZ534876A (https=) |
| WO (1) | WO2000047618A2 (https=) |
Families Citing this family (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9701684D0 (en) | 1997-01-28 | 1997-03-19 | Smithkline Beecham Plc | Novel compounds |
| US6699671B1 (en) | 1998-09-24 | 2004-03-02 | Pharmacia & Upjohn Company | Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
| EP1939297A1 (en) * | 1998-09-24 | 2008-07-02 | Pharmacia & Upjohn Company LLC | Alzheimer's disease secretase |
| PL205294B1 (pl) | 1998-09-24 | 2010-03-31 | Upjohn Co | Izolowany lub oczyszczony polipeptyd, oczyszczony lub izolowany polinukleotyd, wektor, wektor ekspresyjny, komórka gospodarza, sposób wytwarzania polipeptydu, sposoby identyfikowania czynnika obniżającego, modulującego lub hamującego aktywność, zastosowanie takiego czynnika, izolowany kwas nukleinowy, obejmujący go wektor i ich zastosowanie, sposoby zmniejszania komórkowego wytwarzania beta amyloidu i zastosowanie antysensownego reagenta |
| US20040234976A1 (en) * | 1998-09-24 | 2004-11-25 | Gurney Mark E. | Alzheimer's disease secretase, app substrates therefor, and uses therefor |
| US6844148B1 (en) | 1998-09-24 | 2005-01-18 | Pharmacia & Upjohn Company | Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
| US7115410B1 (en) | 1999-02-10 | 2006-10-03 | Elan Pharmaceuticals, Inc. | β-secretase enzyme compositions and methods |
| US7456007B1 (en) | 1998-12-31 | 2008-11-25 | Elan Pharmaceuticals, Inc. | β-secretase enzyme compositions and methods |
| GB2364059B (en) | 1999-02-10 | 2004-01-14 | Elan Pharm Inc | Beta-Secretase enzyme compositions and methods |
| WO2000058479A1 (en) * | 1999-03-26 | 2000-10-05 | Amgen Inc. | Beta secretase genes and polypeptides |
| US7087399B1 (en) * | 1999-05-13 | 2006-08-08 | Scios, Inc. | β-secretase and modulation of β-secretase activity |
| US7169759B1 (en) * | 1999-06-15 | 2007-01-30 | Elan Pharmaceuticals, Inc. | Tetrapeptide inhibitors of β-secretase |
| CA2374610A1 (en) * | 1999-06-28 | 2001-01-04 | Jordan J. N. Tang | Catalytically active recombinant memapsin and methods of use thereof |
| EP1496124A1 (en) * | 1999-06-28 | 2005-01-12 | Oklahoma Medical Research Foundation | Catalytically active recombinant memapsin and methods of use thereof |
| US20090162883A1 (en) * | 1999-09-23 | 2009-06-25 | Pharmacia & Upjohn Company | Alzheimer's Disease Secretase, APP Substrates Thereof, and Uses Thereof |
| US7514408B1 (en) | 1999-12-02 | 2009-04-07 | Elan Pharmaceuticals, Inc. | β-secretase enzyme compositions and methods |
| DE60124080T2 (de) | 2000-03-23 | 2007-03-01 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen und verfahren zur behandlung der alzheimerschen krankheit |
| US6878363B2 (en) * | 2000-05-17 | 2005-04-12 | Bristol-Myers Squibb Pharma Company | Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging |
| KR100436924B1 (ko) * | 2000-06-28 | 2004-06-23 | (주) 디지탈바이오텍 | 베타 시크리테아제의 제조 방법 |
| PE20020276A1 (es) | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
| EP1666452A2 (en) | 2000-06-30 | 2006-06-07 | Elan Pharmaceuticals, Inc. | Compounds to treat Alzheimer's disease |
| US6846813B2 (en) | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
| JP2004502664A (ja) | 2000-06-30 | 2004-01-29 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病処置用化合物 |
| CA2410898A1 (en) | 2000-07-19 | 2002-01-24 | Pharmacia & Upjohn Company | Substrates and assays for .beta.-secretase activity |
| US7806980B2 (en) * | 2000-12-23 | 2010-10-05 | Elan Pharmaceuticals, Inc. | Method for crystallizing human beta secretase in complex with an inhibitor |
| WO2002053594A2 (en) * | 2000-12-28 | 2002-07-11 | Oklahoma Medical Research Foundation | Inhibitors of memapsin 2 and use thereof |
| JP2004524843A (ja) | 2001-02-23 | 2004-08-19 | イーラン ファーマスーティカルズ、インコーポレイテッド | Ｂａｃｅ−１のトランスジェニックノックアウト |
| US7384773B1 (en) * | 2001-05-10 | 2008-06-10 | Pfizer Inc | Crystal of HIV protease-cleaved human beta secretase and method for crystallization thereof |
| US7524668B1 (en) * | 2001-05-10 | 2009-04-28 | Elan Pharmaceuticals, Inc. | Crystal of human beta secretase having monoclinic space group symmetry C2 and methods for crystallization thereof |
| EP1390497A2 (en) | 2001-05-25 | 2004-02-25 | Genset | Human cdnas and proteins and uses thereof |
| MXPA03011046A (es) | 2001-06-01 | 2004-06-25 | Elan Pharm Inc | Hidroxialquilaminas. |
| US6906104B2 (en) | 2001-06-13 | 2005-06-14 | Pharmacia & Upjohn Company | Aminediols for the treatment of Alzheimer's disease |
| BR0210721A (pt) | 2001-06-27 | 2004-07-20 | Elan Pharm Inc | Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição |
| BR0211121A (pt) | 2001-07-10 | 2004-10-26 | Elan Pharm Inc | Composto, métodos para o tratamento ou prevenção de doenças e para fabricar um composto, intermediário, e, uso de um composto ou sal |
| MXPA04000338A (es) | 2001-07-10 | 2004-07-23 | Upjohn Co | Diamindioles para tratamiento de enfermedad de alzheimer. |
| EP1285578B1 (en) * | 2001-08-21 | 2007-10-31 | Smithkline Beecham Plc | Transgenic animal model of Alzheimer's disease |
| US7186539B1 (en) | 2001-08-31 | 2007-03-06 | Pharmacia & Upjohn Company | Method for refolding enzymes |
| EP1432674A2 (en) | 2001-10-04 | 2004-06-30 | Elan Pharmaceuticals, Inc. | Hydroxypropylamines |
| JP4547152B2 (ja) | 2001-10-23 | 2010-09-22 | オクラホマ メディカル リサーチ ファウンデーション | β−セクレターゼ阻害剤および使用方法 |
| AU2002359376B2 (en) | 2001-11-08 | 2008-01-10 | Elan Pharmaceuticals, Inc. | N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives |
| AU2002360508A1 (en) | 2001-12-06 | 2003-06-23 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamines |
| CH698246B1 (de) * | 2001-12-20 | 2009-06-30 | Hoffmann La Roche | Test zur Identifizierung von Inhibitoren von Beta-Sekretasen. |
| US7273743B2 (en) | 2002-02-21 | 2007-09-25 | Elan Pharmaceuticals, Inc. | Modified BACE |
| WO2003076455A2 (en) | 2002-03-05 | 2003-09-18 | Ramot At Tel-Aviv University Ltd. | Immunizing composition and method for inducing an immune response against the ss-secretase cleavage site of amyloid precursor protein |
| WO2004058686A1 (en) | 2002-04-30 | 2004-07-15 | Elan Pharmaceuticals, Inc. | Hydroxypropyl amides for the treatment of alzheimer’s disease |
| US7442537B1 (en) | 2002-05-10 | 2008-10-28 | Elan Pharmaceuticals, Inc. | Crystals of unliganded beta secretase and/or beta secretase-like proteins and the use thereof |
| CA2507484A1 (en) | 2002-11-27 | 2004-06-17 | Elan Pharmaceuticals, Inc. | Substituted ureas and carbamates |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| TW200512195A (en) | 2003-04-21 | 2005-04-01 | Elan Pharm Inc | Benzamide 2-hydroxy-3-diaminoalkanes |
| JP4739192B2 (ja) | 2003-05-02 | 2011-08-03 | イーラン ファーマスーティカルズ、インコーポレイテッド | Ｂａｃｅのグリコシル化変異体 |
| US20050014160A1 (en) * | 2003-07-18 | 2005-01-20 | Sriram Kumaraswamy | Assays for protease enzyme activity |
| JP2007528400A (ja) | 2004-03-09 | 2007-10-11 | エラン ファーマシューティカルズ，インコーポレイテッド | 置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬 |
| WO2006010095A2 (en) | 2004-07-09 | 2006-01-26 | Elan Pharmaceuticals Inc. | Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors |
| WO2006040153A2 (en) * | 2004-10-13 | 2006-04-20 | Ablynx N.V. | Single domain camelide anti -amyloid beta antibodies and polypeptides comprising the same for the treatment and diagnosis of degenarative neural diseases such as alzheimer's disease |
| US7906625B2 (en) | 2005-01-24 | 2011-03-15 | Amgen Inc. | Humanized anti-amyloid antibody |
| US20060223849A1 (en) * | 2005-03-14 | 2006-10-05 | Mjalli Adnan M | Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors |
| CA2618508A1 (en) * | 2005-08-10 | 2007-02-22 | Oklahoma Medical Research Foundation | Truncated memapsin 2 for use for treating alzheimer's disease |
| WO2007047305A1 (en) | 2005-10-12 | 2007-04-26 | Elan Pharmaceuticals, Inc. | Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors |
| WO2007056401A1 (en) * | 2005-11-09 | 2007-05-18 | Merck & Co., Inc. | Method for identifying modulators of osbp useful for treating alzheimer's disease |
| JP4590638B2 (ja) * | 2006-03-20 | 2010-12-01 | 国立大学法人鳥取大学 | 家族性筋萎縮性側索硬化症（ｆａｌｓ）発症するトランスジェニックマウス |
| US20070292895A1 (en) * | 2006-05-19 | 2007-12-20 | Xiao-Ping Shi | Assays and methods to detect beta-secretase and its activity in body fluids and tissue extracts |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| KR20090027877A (ko) * | 2007-09-13 | 2009-03-18 | 한국생명공학연구원 | Ｂｅｔａ－ｓｉｔｅ ＡＰＰ ｃｌｅａｖｉｎ ｇｅｎｚｙｍｅ（ＢＡＣＥ）를 발현하는 형질전환 식물체 |
| CN101270359B (zh) * | 2008-04-30 | 2012-05-23 | 江苏省原子医学研究所 | 一种重组人淀粉样蛋白Aβ42的制备方法及应用 |
| TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
| EP2281824A1 (en) | 2009-08-07 | 2011-02-09 | Noscira, S.A. | Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders |
| WO2012064836A1 (en) | 2010-11-10 | 2012-05-18 | Genentech, Inc. | Methods and compositions for neural disease immunotherapy |
| EP2643299B1 (en) | 2010-11-22 | 2016-06-22 | Noscira, S.A. | Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions |
| JP6134725B2 (ja) * | 2011-10-14 | 2017-05-24 | ジェネンテック， インコーポレイテッド | Ｂａｃｅ１のペプチド阻害剤 |
| WO2016081640A1 (en) | 2014-11-19 | 2016-05-26 | Genentech, Inc. | Anti-transferrin receptor / anti-bace1 multispecific antibodies and methods of use |
| JP6859259B2 (ja) | 2014-11-19 | 2021-04-14 | ジェネンテック， インコーポレイテッド | ＢＡＣＥｌに対する抗体及び神経疾患免疫療法のためのその使用 |
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| DE19910108C2 (de) | 1999-03-08 | 2001-02-22 | Falk Fahrenholz | Zellen, die ein Amyloidvorläuferprotein und eine alpha-Sekretase coexprimieren, ein Testverfahren zur Identifikation alpha-Sekretase-aktiver Substanzen sowie eines zur Identifikation weiterer Sekretasen, ein Testverfahren zur Bestimmung der Anfälligkeit gegenüber Morbus Alzheimer und Verwendung von Nukleinsäuren, die für eine alpha-Sekretase codieren, für die Gentherapie |
| WO2000058479A1 (en) | 1999-03-26 | 2000-10-05 | Amgen Inc. | Beta secretase genes and polypeptides |
| WO2000068266A1 (en) | 1999-05-11 | 2000-11-16 | Eli Lilly And Company | Amyloid precursor protein protease and related nucleic acid compounds |
| US7087399B1 (en) | 1999-05-13 | 2006-08-08 | Scios, Inc. | β-secretase and modulation of β-secretase activity |
| CA2374610A1 (en) | 1999-06-28 | 2001-01-04 | Jordan J. N. Tang | Catalytically active recombinant memapsin and methods of use thereof |
| WO2001023533A2 (en) | 1999-09-23 | 2001-04-05 | Pharmacia & Upjohn Company | Alzheimer's disease secretase, app substrates therefor, and uses therefor |
| GB9924957D0 (en) | 1999-10-21 | 1999-12-22 | Smithkline Beecham Plc | Novel treatment |
| GB9925136D0 (en) | 1999-10-22 | 1999-12-22 | Smithkline Beecham Plc | Novel treatment |
| US6361975B1 (en) | 1999-11-16 | 2002-03-26 | Smithkline Beecham Corporation | Mouse aspartic secretase-2(mASP-2) |
| US6291223B1 (en) | 1999-11-23 | 2001-09-18 | Smithkline Beecham Corporation | Mouse aspartic secretase-1 (mASP1) |
-
2000
- 2000-02-10 GB GB0121314A patent/GB2364059B/en not_active Expired - Fee Related
- 2000-02-10 EP EP00919298A patent/EP1165609A2/en not_active Ceased
- 2000-02-10 CA CA002359785A patent/CA2359785A1/en not_active Abandoned
- 2000-02-10 HK HK02104538.9A patent/HK1044545A1/zh unknown
- 2000-02-10 AU AU40009/00A patent/AU4000900A/en not_active Abandoned
- 2000-02-10 CN CN00806471A patent/CN1390232A/zh active Pending
- 2000-02-10 NZ NZ534876A patent/NZ534876A/en not_active IP Right Cessation
- 2000-02-10 WO PCT/US2000/003819 patent/WO2000047618A2/en not_active Ceased
- 2000-02-10 JP JP2000598533A patent/JP4653318B2/ja not_active Expired - Fee Related
- 2000-02-10 HK HK02104530.7A patent/HK1044543B/zh not_active IP Right Cessation
- 2000-11-28 US US09/724,566 patent/US6627739B1/en not_active Expired - Fee Related
- 2000-11-28 US US09/724,569 patent/US7109017B1/en not_active Expired - Fee Related
- 2000-11-28 US US09/724,571 patent/US7067271B1/en not_active Expired - Fee Related
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