JP2003503072A5 - - Google Patents
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- Publication number
- JP2003503072A5 JP2003503072A5 JP2001507069A JP2001507069A JP2003503072A5 JP 2003503072 A5 JP2003503072 A5 JP 2003503072A5 JP 2001507069 A JP2001507069 A JP 2001507069A JP 2001507069 A JP2001507069 A JP 2001507069A JP 2003503072 A5 JP2003503072 A5 JP 2003503072A5
- Authority
- JP
- Japan
- Prior art keywords
- memapsin
- protein
- seq
- composition
- amino acid
- 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
- 101710150192 Beta-secretase 1 Proteins 0.000 description 30
- 102100021257 Beta-secretase 1 Human genes 0.000 description 30
- 239000000203 mixture Substances 0.000 description 13
- 125000000539 amino acid group Chemical group 0.000 description 7
- 239000000758 substrate Substances 0.000 description 7
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 5
- 239000004202 carbamide Substances 0.000 description 5
- 210000004899 c-terminal region Anatomy 0.000 description 4
- 239000003112 inhibitor Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 239000012062 aqueous buffer Substances 0.000 description 3
- 239000013598 vector Substances 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 102000057297 Pepsin A Human genes 0.000 description 2
- 108090000284 Pepsin A Proteins 0.000 description 2
- 230000001580 bacterial effect Effects 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 238000010586 diagram Methods 0.000 description 2
- 238000010790 dilution Methods 0.000 description 2
- 239000012895 dilution Substances 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 239000013604 expression vector Substances 0.000 description 2
- 230000037431 insertion Effects 0.000 description 2
- 238000003780 insertion Methods 0.000 description 2
- 229940111202 pepsin Drugs 0.000 description 2
- 108090000765 processed proteins & peptides Proteins 0.000 description 2
- 230000007704 transition Effects 0.000 description 2
- 241000588724 Escherichia coli Species 0.000 description 1
- IMROMDMJAWUWLK-UHFFFAOYSA-N Ethenol Chemical group OC=C IMROMDMJAWUWLK-UHFFFAOYSA-N 0.000 description 1
- 108010024636 Glutathione Proteins 0.000 description 1
- 108010053070 Glutathione Disulfide Proteins 0.000 description 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 102000007056 Recombinant Fusion Proteins Human genes 0.000 description 1
- 108010008281 Recombinant Fusion Proteins Proteins 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- 239000003638 chemical reducing agent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000003776 cleavage reaction Methods 0.000 description 1
- 239000002299 complementary DNA Substances 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 description 1
- YPZRWBKMTBYPTK-BJDJZHNGSA-N glutathione disulfide Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@H](C(=O)NCC(O)=O)CSSC[C@@H](C(=O)NCC(O)=O)NC(=O)CC[C@H](N)C(O)=O YPZRWBKMTBYPTK-BJDJZHNGSA-N 0.000 description 1
- 102000044297 human BACE1 Human genes 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 229920001184 polypeptide Polymers 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14136399P | 1999-06-28 | 1999-06-28 | |
| US60/141,363 | 1999-06-28 | ||
| US16806099P | 1999-11-30 | 1999-11-30 | |
| US60/168,060 | 1999-11-30 | ||
| US17783600P | 2000-01-25 | 2000-01-25 | |
| US60/177,836 | 2000-01-25 | ||
| US17836800P | 2000-01-27 | 2000-01-27 | |
| US60/178,368 | 2000-01-27 | ||
| US21029200P | 2000-06-08 | 2000-06-08 | |
| US60/210,292 | 2000-06-08 | ||
| PCT/US2000/017661 WO2001000663A2 (en) | 1999-06-28 | 2000-06-27 | Catalytically active recombinant memapsin and methods of use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003503072A JP2003503072A (ja) | 2003-01-28 |
| JP2003503072A5 true JP2003503072A5 (https=) | 2007-09-13 |
| JP5138851B2 JP5138851B2 (ja) | 2013-02-06 |
Family
ID=27538142
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001507071A Expired - Fee Related JP4484410B2 (ja) | 1999-06-28 | 2000-06-27 | メマプシン２のインヒビターおよびその使用 |
| JP2001507069A Expired - Fee Related JP5138851B2 (ja) | 1999-06-28 | 2000-06-27 | 触媒的に活性な組換えメマプシンおよびその使用方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001507071A Expired - Fee Related JP4484410B2 (ja) | 1999-06-28 | 2000-06-27 | メマプシン２のインヒビターおよびその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (7) | US6545127B1 (https=) |
| EP (2) | EP1196609A2 (https=) |
| JP (2) | JP4484410B2 (https=) |
| CN (1) | CN1379819A (https=) |
| AT (1) | ATE482233T1 (https=) |
| AU (2) | AU5773500A (https=) |
| CA (2) | CA2374346C (https=) |
| DE (1) | DE60045005D1 (https=) |
| WO (2) | WO2001000663A2 (https=) |
Families Citing this family (114)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9701684D0 (en) | 1997-01-28 | 1997-03-19 | Smithkline Beecham Plc | Novel compounds |
| US20040234976A1 (en) * | 1998-09-24 | 2004-11-25 | Gurney Mark E. | Alzheimer's disease secretase, app substrates therefor, and uses therefor |
| CN1300320C (zh) * | 1998-09-24 | 2007-02-14 | 法玛西雅厄普约翰美国公司 | 阿尔茨海默氏疾病分泌酶 |
| US6844148B1 (en) | 1998-09-24 | 2005-01-18 | Pharmacia & Upjohn Company | Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
| US6699671B1 (en) | 1998-09-24 | 2004-03-02 | Pharmacia & Upjohn Company | Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
| US7456007B1 (en) | 1998-12-31 | 2008-11-25 | Elan Pharmaceuticals, Inc. | β-secretase enzyme compositions and methods |
| US7115410B1 (en) | 1999-02-10 | 2006-10-03 | Elan Pharmaceuticals, Inc. | β-secretase enzyme compositions and methods |
| CN1390232A (zh) | 1999-02-10 | 2003-01-08 | 艾兰制药公司 | 人β分泌酶、抑制剂、其组合物和用途 |
| EP1196609A2 (en) * | 1999-06-28 | 2002-04-17 | 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 |
| 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 |
| US7514408B1 (en) | 1999-12-02 | 2009-04-07 | Elan Pharmaceuticals, Inc. | β-secretase enzyme compositions and methods |
| CA2397543A1 (en) * | 2000-01-24 | 2001-07-26 | Timothy Harrison | Gamma-secretase inhibitors |
| US6583268B2 (en) | 2000-01-25 | 2003-06-24 | Oklahoma Medical Research Foundation | Universal procedure for refolding recombinant proteins |
| DE60124080T2 (de) | 2000-03-23 | 2007-03-01 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen und verfahren zur behandlung der alzheimerschen krankheit |
| EP1666452A2 (en) | 2000-06-30 | 2006-06-07 | Elan Pharmaceuticals, Inc. | Compounds to treat Alzheimer's disease |
| 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 |
| EP1299352B1 (en) | 2000-06-30 | 2005-12-28 | 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 |
| US7205120B2 (en) * | 2000-07-19 | 2007-04-17 | Pharmacia & Upjohn Company | Substrates and assays for β-secretase activity |
| US7630838B2 (en) * | 2000-09-22 | 2009-12-08 | American Home Products Corporation | Method for identifying agents that interact with beta-site APP cleaving enzyme (BACE) |
| US7601528B1 (en) | 2000-12-23 | 2009-10-13 | Elan Pharmaceuticals, Inc. | Crystallization and structure determination of glycosylated human beta secretase, an enzyme implicated in alzheimer's disease |
| US7217556B1 (en) | 2000-12-23 | 2007-05-15 | Pfizer Inc | Crystallization and structure determination of glycosylated human beta secretase, an enzyme implicated in Alzheimer's disease |
| US7806980B2 (en) | 2000-12-23 | 2010-10-05 | Elan Pharmaceuticals, Inc. | Method for crystallizing human beta secretase in complex with an inhibitor |
| US20040121947A1 (en) * | 2000-12-28 | 2004-06-24 | Oklahoma Medical Research Foundation | Compounds which inhibit beta-secretase activity and methods of use thereof |
| EP1233021A3 (en) * | 2001-02-20 | 2002-11-20 | Pfizer Products Inc. | An inhibitor of Beta amyloid cleavage enzyme |
| WO2002068623A2 (en) * | 2001-02-23 | 2002-09-06 | Dsm Ip Assets B.V. | Genes encoding proteolytic enzymes from aspargilli |
| 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 |
| US7196163B2 (en) | 2001-05-22 | 2007-03-27 | Merk & Co., Inc. | Assays using amyloid precursor proteins with modified β-secretase cleavage sites to monitor β-secretase activity |
| EP1390497A2 (en) | 2001-05-25 | 2004-02-25 | Genset | Human cdnas and proteins and uses thereof |
| CA2450557A1 (en) * | 2001-06-11 | 2002-12-19 | Michel Maillard | Substituted aminoalcohols useful in treatment of alzheimer's disease |
| EP1401452A1 (en) | 2001-06-27 | 2004-03-31 | Elan Pharmaceuticals, Inc. | Beta-hydroxyamine derivatives useful in the treatment of alzheimer's disease |
| EP1409660A2 (en) * | 2001-07-26 | 2004-04-21 | Astex Technology Limited | Crystal structure of beta-site app cleaving enzyme (bace) and use thereof |
| US7186539B1 (en) * | 2001-08-31 | 2007-03-06 | Pharmacia & Upjohn Company | Method for refolding enzymes |
| CA2464736A1 (en) * | 2001-10-23 | 2003-05-15 | Oklahoma Medical Research Foundation | Beta-secretase inhibitors and methods of use |
| US20060234944A1 (en) * | 2001-10-23 | 2006-10-19 | Oklahoma Medical Reseach Foundation | Beta-secretase inhibitors and methods of use |
| WO2003040393A2 (en) * | 2001-11-06 | 2003-05-15 | Decode Genetics Ehf. | Nucleic acids encoding proteases |
| CH698246B1 (de) * | 2001-12-20 | 2009-06-30 | Hoffmann La Roche | Test zur Identifizierung von Inhibitoren von Beta-Sekretasen. |
| AU2003213252A1 (en) | 2002-02-21 | 2003-09-09 | Pharmacia And Upjohn Company | Modified bace |
| KR101011657B1 (ko) | 2002-03-01 | 2011-01-28 | 다케다 야쿠힌 고교 가부시키가이샤 | 항우울제 |
| 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 |
| AU2003230392A1 (en) | 2002-05-17 | 2003-12-12 | Merck And Co., Inc. | Beta-secretase inhibitors |
| US7166454B1 (en) | 2002-05-24 | 2007-01-23 | Schering Corporation | Codon-optimized β-secretase and methods of refolding and processing |
| US6746303B2 (en) | 2002-05-31 | 2004-06-08 | Mattel, Inc. | Flexible toy figure with wire armature |
| WO2004011641A2 (en) * | 2002-07-26 | 2004-02-05 | Astex Technology Limited | Crystal structure of beta-site app-cleaving enzyme (bace) mutants and uses thereof |
| US20050074456A1 (en) * | 2002-12-04 | 2005-04-07 | Marcus Ballinger | Constructs for homogenously processed preparations of beta site APP-cleaving enzyme |
| US7371853B2 (en) | 2003-01-07 | 2008-05-13 | Merck & Co., Inc. | Macrocyclic β-secretase inhibitors for the treatment of Alzheimer's disease |
| EP1473362A1 (en) | 2003-05-02 | 2004-11-03 | Elan Pharmaceuticals, Inc. | Glycosylation variants of BACE |
| CN100430377C (zh) | 2003-06-30 | 2008-11-05 | 麦克公司 | 用于治疗阿尔茨海默病的N-烷基苯基甲酰胺β分泌酶抑制剂 |
| CN1909897A (zh) | 2003-07-01 | 2007-02-07 | 默克公司 | 用于治疗阿尔茨海默病的苯基羧化物β－分泌酶抑制剂 |
| AU2004277981B2 (en) | 2003-10-03 | 2009-10-01 | Merck & Co., Inc. | Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease |
| FR2860796B1 (fr) * | 2003-10-14 | 2006-02-10 | Centre Nat Rech Scient | Procede de dissociation de la molecule d'hemoglobine extracellulaire d'arenicola marina, chaines proteiques constituant ladite molecule et sequences nucleotidiques codant pour lesdites chaines proteiques |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US20060019368A1 (en) * | 2004-07-20 | 2006-01-26 | Marcus Ballinger | Constructs for homogenously processed preparations of beta site APP-cleaving enzyme |
| US7906625B2 (en) * | 2005-01-24 | 2011-03-15 | Amgen Inc. | Humanized anti-amyloid antibody |
| ES2400287T3 (es) * | 2005-03-14 | 2013-04-08 | High Point Pharmaceuticals, Llc | Derivados de benzazol, composiciones y procedimientos de uso como inhibidores de beta-secretasa |
| CA2603404A1 (en) | 2005-03-30 | 2006-10-05 | Boehringer Ingelheim International Gmbh | Substituted 1,2-ethylendiamines, medicaments comprising said compound; their use and their method of manufacture |
| AU2006279896A1 (en) * | 2005-08-10 | 2007-02-22 | Oklahoma Medical Research Foundation | Truncated memapsin 2 for use for treating Alzheimer's disease |
| WO2007020888A1 (ja) | 2005-08-12 | 2007-02-22 | Takeda Pharmaceutical Company Limited | 脳・神経細胞保護剤および睡眠障害治療薬 |
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| WO2007081534A2 (en) * | 2005-12-22 | 2007-07-19 | Pfizer Products Inc | Method of producing catalytically active bace2 enzymes |
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| CA2687750C (en) | 2007-07-06 | 2016-10-18 | Boehringer Ingelheim International Gmbh | Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture |
| KR20100059919A (ko) * | 2007-09-24 | 2010-06-04 | 코멘티스, 인코포레이티드 | 치료를 위한 베타-세크레타제 억제제로서 (3-히드록시-4-아미노-부탄-2일)-3-(2-티아졸-2-일-피롤리딘-1-카르보닐) 벤즈아미드 유도체 및 관련 화합물 |
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| MX346500B (es) | 2010-11-10 | 2017-03-22 | Genentech Inc * | Metodos y composiciones para inmunoterapia para enfermedad neural. |
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| PL2763979T3 (pl) | 2011-10-07 | 2019-06-28 | Takeda Pharmaceutical Company Limited | Związki 1-arylokarbonyl-4-oksy-piperydynowe użyteczne do leczenia chorób neurodegeneracyjnych |
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| CN108588040B (zh) * | 2018-06-08 | 2021-06-15 | 中国医学科学院病原生物学研究所 | 重组MtMetRS、其晶体及它们在制备抗结核药物中的应用 |
| JP7339250B2 (ja) | 2018-06-29 | 2023-09-05 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
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| WO2020153414A1 (ja) | 2019-01-24 | 2020-07-30 | 武田薬品工業株式会社 | 複素環化合物及びその用途 |
| JP7253640B2 (ja) | 2019-01-31 | 2023-04-06 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
| KR20220062361A (ko) | 2019-09-13 | 2022-05-16 | 다케다 야쿠힌 고교 가부시키가이샤 | 과도한 졸림의 치료를 위한 오렉신 2 수용체 효능제의 용도 |
| AU2020346456A1 (en) | 2019-09-13 | 2022-04-14 | Takeda Pharmaceutical Company Limited | TAK-925 for use in treating narcolepsy |
| JP2021080177A (ja) | 2019-11-14 | 2021-05-27 | 武田薬品工業株式会社 | 複素環化合物及びその用途 |
| US12448377B2 (en) | 2019-11-27 | 2025-10-21 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| JP2021183586A (ja) | 2020-05-22 | 2021-12-02 | 武田薬品工業株式会社 | 複素環化合物 |
| JP2021183587A (ja) | 2020-05-22 | 2021-12-02 | 武田薬品工業株式会社 | 複素環化合物 |
| US20230313196A1 (en) * | 2020-07-23 | 2023-10-05 | John Mansell | Compositions and methods for treating pain and anxiety disorders |
| TW202302100A (zh) | 2021-03-12 | 2023-01-16 | 日商武田藥品工業股份有限公司 | 食慾激素２受體促效劑於治療食慾激素介導之疾病或病症之用途 |
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| TW202428580A (zh) | 2022-10-31 | 2024-07-16 | 日商武田藥品工業股份有限公司 | 雜環化合物 |
| AR131202A1 (es) | 2022-11-30 | 2025-02-26 | Takeda Pharmaceuticals Co | Compuesto heterocíclico y uso del mismo |
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-
2000
- 2000-06-27 EP EP00943208A patent/EP1196609A2/en not_active Withdrawn
- 2000-06-27 AU AU57735/00A patent/AU5773500A/en not_active Abandoned
- 2000-06-27 JP JP2001507071A patent/JP4484410B2/ja not_active Expired - Fee Related
- 2000-06-27 CA CA2374346A patent/CA2374346C/en not_active Expired - Fee Related
- 2000-06-27 AT AT00943236T patent/ATE482233T1/de not_active IP Right Cessation
- 2000-06-27 EP EP00943236A patent/EP1194449B1/en not_active Expired - Lifetime
- 2000-06-27 WO PCT/US2000/017661 patent/WO2001000663A2/en not_active Ceased
- 2000-06-27 JP JP2001507069A patent/JP5138851B2/ja not_active Expired - Fee Related
- 2000-06-27 DE DE60045005T patent/DE60045005D1/de not_active Expired - Lifetime
- 2000-06-27 AU AU57715/00A patent/AU5771500A/en not_active Abandoned
- 2000-06-27 CA CA002374610A patent/CA2374610A1/en not_active Abandoned
- 2000-06-27 WO PCT/US2000/017742 patent/WO2001000665A2/en not_active Ceased
- 2000-06-27 CN CN00810930A patent/CN1379819A/zh active Pending
- 2000-06-27 US US09/604,608 patent/US6545127B1/en not_active Expired - Lifetime
-
2001
- 2001-02-28 US US09/795,903 patent/US20020164760A1/en not_active Abandoned
- 2001-04-30 US US09/845,226 patent/US20020115600A1/en not_active Abandoned
-
2004
- 2004-02-06 US US10/773,754 patent/US20040220079A1/en not_active Abandoned
- 2004-04-08 US US10/820,953 patent/US7244708B2/en not_active Expired - Fee Related
-
2007
- 2007-06-14 US US11/763,342 patent/US7678760B2/en not_active Expired - Fee Related
- 2007-08-03 US US11/888,920 patent/US7829669B2/en not_active Expired - Fee Related
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