JP4484410B2 - メマプシン２のインヒビターおよびその使用 - Google Patents
メマプシン２のインヒビターおよびその使用 Download PDFInfo
- Publication number
- JP4484410B2 JP4484410B2 JP2001507071A JP2001507071A JP4484410B2 JP 4484410 B2 JP4484410 B2 JP 4484410B2 JP 2001507071 A JP2001507071 A JP 2001507071A JP 2001507071 A JP2001507071 A JP 2001507071A JP 4484410 B2 JP4484410 B2 JP 4484410B2
- Authority
- JP
- Japan
- Prior art keywords
- memapsin
- substrate
- tert
- leu
- butoxycarbonyl
- 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.)
- Expired - Fee Related
Links
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Classifications
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- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
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- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
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- C07K1/1136—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure by reversible modification of the secondary, tertiary or quarternary structure, e.g. using denaturating or stabilising agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
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- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
- C07K5/06043—Leu-amino acid
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
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- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
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- C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
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- C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
- C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes
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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
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- Y02A90/10—Information and communication technologies [ICT] supporting adaptation to climate change, e.g. for weather forecasting or climate simulation
Landscapes
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
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| 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/US2000/017742 WO2001000665A2 (en) | 1999-06-28 | 2000-06-27 | Inhibitors of memapsin 2 and use thereof |
Publications (3)
| Publication Number | Publication Date |
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| JP2003506322A JP2003506322A (ja) | 2003-02-18 |
| JP2003506322A5 JP2003506322A5 (https=) | 2007-09-13 |
| JP4484410B2 true JP4484410B2 (ja) | 2010-06-16 |
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| 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 |
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| Application Number | Title | Priority Date | Filing Date |
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| 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 |
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| 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=) |
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| 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 |
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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
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- 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
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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
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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
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2007
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Also Published As
| Publication number | Publication date |
|---|---|
| JP2003506322A (ja) | 2003-02-18 |
| US7244708B2 (en) | 2007-07-17 |
| WO2001000665A9 (en) | 2002-07-25 |
| DE60045005D1 (de) | 2010-11-04 |
| AU5771500A (en) | 2001-01-31 |
| EP1194449B1 (en) | 2010-09-22 |
| CA2374346A1 (en) | 2001-01-04 |
| WO2001000663A3 (en) | 2001-10-04 |
| JP5138851B2 (ja) | 2013-02-06 |
| US20080112946A1 (en) | 2008-05-15 |
| WO2001000663A2 (en) | 2001-01-04 |
| US20020115600A1 (en) | 2002-08-22 |
| AU5773500A (en) | 2001-01-31 |
| US20080021196A1 (en) | 2008-01-24 |
| CA2374610A1 (en) | 2001-01-04 |
| WO2001000665A2 (en) | 2001-01-04 |
| US7829669B2 (en) | 2010-11-09 |
| EP1194449A2 (en) | 2002-04-10 |
| WO2001000665A3 (en) | 2001-09-27 |
| US6545127B1 (en) | 2003-04-08 |
| CN1379819A (zh) | 2002-11-13 |
| EP1196609A2 (en) | 2002-04-17 |
| US20020164760A1 (en) | 2002-11-07 |
| JP2003503072A (ja) | 2003-01-28 |
| ATE482233T1 (de) | 2010-10-15 |
| US20040220079A1 (en) | 2004-11-04 |
| US7678760B2 (en) | 2010-03-16 |
| CA2374346C (en) | 2010-06-22 |
| US20040167075A1 (en) | 2004-08-26 |
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