CA2374346C - Inhibitors of memapsin 2 and use thereof - Google Patents
Inhibitors of memapsin 2 and use thereof Download PDFInfo
- Publication number
- CA2374346C CA2374346C CA2374346A CA2374346A CA2374346C CA 2374346 C CA2374346 C CA 2374346C CA 2374346 A CA2374346 A CA 2374346A CA 2374346 A CA2374346 A CA 2374346A CA 2374346 C CA2374346 C CA 2374346C
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- Prior art keywords
- memapsin
- inhibitor
- leu
- ala
- pro
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- 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
- C07K1/113—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
- 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
- C07K5/06—Dipeptides
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- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
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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
- C07K5/06008—Dipeptides with the first amino acid being neutral
- 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
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- 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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- 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
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
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- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- 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
- 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
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- 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
- C12N9/6478—Aspartic endopeptidases (3.4.23)
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
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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
-
- 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
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A90/00—Technologies having an indirect contribution to adaptation to climate change
- 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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- Proteomics, Peptides & Aminoacids (AREA)
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- Biophysics (AREA)
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- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- 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 |
|---|---|---|---|
| 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 (2)
| Publication Number | Publication Date |
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| CA2374346A1 CA2374346A1 (en) | 2001-01-04 |
| CA2374346C true CA2374346C (en) | 2010-06-22 |
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| CA2374346A Expired - Fee Related CA2374346C (en) | 1999-06-28 | 2000-06-27 | Inhibitors of memapsin 2 and use thereof |
| CA002374610A Abandoned CA2374610A1 (en) | 1999-06-28 | 2000-06-27 | Catalytically active recombinant memapsin and methods of use thereof |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002374610A Abandoned CA2374610A1 (en) | 1999-06-28 | 2000-06-27 | Catalytically active recombinant memapsin and methods of use thereof |
Country Status (9)
| Country | Link |
|---|---|
| US (7) | US6545127B1 (enExample) |
| EP (2) | EP1196609A2 (enExample) |
| JP (2) | JP5138851B2 (enExample) |
| CN (1) | CN1379819A (enExample) |
| AT (1) | ATE482233T1 (enExample) |
| AU (2) | AU5771500A (enExample) |
| CA (2) | CA2374346C (enExample) |
| DE (1) | DE60045005D1 (enExample) |
| WO (2) | WO2001000665A2 (enExample) |
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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 |
| US6699671B1 (en) * | 1998-09-24 | 2004-03-02 | Pharmacia & Upjohn Company | Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
| CN1198936C (zh) | 1998-09-24 | 2005-04-27 | 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 |
| 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 |
| 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 |
| AU779875B2 (en) * | 2000-01-24 | 2005-02-17 | Merck Sharp & Dohme Limited | Gamma-secretase inhibitors |
| DK1255769T3 (da) | 2000-01-25 | 2007-09-03 | Oklahoma Med Res Found | Universel procedure til genfoldning af rekombinante proteiner |
| JP2003528071A (ja) | 2000-03-23 | 2003-09-24 | エラン ファーマスーティカルズ インコーポレイテッド | アルツハイマー病治療用組成物および方法 |
| ATE302751T1 (de) | 2000-06-30 | 2005-09-15 | Elan Pharm Inc | Verbindungen zur behandlung der alzheimerischen krankheit |
| 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 |
| US6846813B2 (en) | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
| EP1666452A2 (en) | 2000-06-30 | 2006-06-07 | Elan Pharmaceuticals, Inc. | Compounds to treat Alzheimer's disease |
| US7205120B2 (en) * | 2000-07-19 | 2007-04-17 | Pharmacia & Upjohn Company | Substrates and assays for β-secretase activity |
| ES2282292T3 (es) * | 2000-09-22 | 2007-10-16 | Wyeth | Estructura cristalina de bace y usos de la misma. |
| 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 |
| 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 |
| 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 |
| NZ527422A (en) * | 2001-02-23 | 2005-02-25 | Dsm Ip Assets B | Tripeptidyl aminopeptidases from Aspergillus niger |
| 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 |
| IL159015A0 (en) | 2001-05-25 | 2004-05-12 | Genset Sa | Polypeptides, their preparation and use |
| US7361688B2 (en) * | 2001-06-11 | 2008-04-22 | Elan Pharmaceuticals, Inc. | Substituted aminoalcohols useful in treatment of Alzheimer's disease |
| MXPA04000140A (es) | 2001-06-27 | 2004-06-03 | Elan Pharm Inc | Derivados de beta-hidroxiamina utiles en el tratamiento de enfermedad de alzheimer. |
| JP2005503144A (ja) * | 2001-07-26 | 2005-02-03 | アステック テクノロジー リミテッド | 新規baceタンパク質、その核酸分子、新規baceタンパク質の新規結晶構造、並びに製造及び使用方法 |
| US7186539B1 (en) | 2001-08-31 | 2007-03-06 | Pharmacia & Upjohn Company | Method for refolding enzymes |
| EP1448218A4 (en) | 2001-10-23 | 2009-01-14 | Oklahoma Med Res Found | BETA SECRETASE INHIBITORS AND METHODS OF USE |
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| 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) |
| DK1255769T3 (da) * | 2000-01-25 | 2007-09-03 | Oklahoma Med Res Found | Universel procedure til genfoldning af rekombinante proteiner |
| JP2003528071A (ja) | 2000-03-23 | 2003-09-24 | エラン ファーマスーティカルズ インコーポレイテッド | アルツハイマー病治療用組成物および方法 |
| US6713276B2 (en) * | 2000-06-28 | 2004-03-30 | Scios, Inc. | Modulation of Aβ levels by β-secretase BACE2 |
| WO2002006511A2 (en) | 2000-07-19 | 2002-01-24 | Genisphere Inc | Methods for detecting and assaying nucleic acid sequences |
| WO2002014264A2 (en) | 2000-08-11 | 2002-02-21 | The Brigham And Women's Hospital, Inc. | (hydroxyethyl)ureas as inhibitors of alzheimer's beta-amyloid production |
| ES2282292T3 (es) | 2000-09-22 | 2007-10-16 | Wyeth | Estructura cristalina de bace y usos de la misma. |
| WO2002047466A2 (en) | 2000-10-27 | 2002-06-20 | The Johns Hopkins University School Of Medicine | Beta-secretase transgenic organisms, anti-beta-secretase antibodies, and methods of use thereof |
| WO2002053594A2 (en) | 2000-12-28 | 2002-07-11 | Oklahoma Medical Research Foundation | Inhibitors of memapsin 2 and use thereof |
| US20040121947A1 (en) | 2000-12-28 | 2004-06-24 | Oklahoma Medical Research Foundation | Compounds which inhibit beta-secretase activity and methods of use thereof |
| JP2009505979A (ja) * | 2005-08-10 | 2009-02-12 | オクラホマ メディカル リサーチ ファンデーション | アルツハイマー病の治療に使用するためのトランケート型メマプシン2 |
-
2000
- 2000-06-27 EP EP00943208A patent/EP1196609A2/en not_active Withdrawn
- 2000-06-27 WO PCT/US2000/017742 patent/WO2001000665A2/en not_active Ceased
- 2000-06-27 US US09/604,608 patent/US6545127B1/en not_active Expired - Lifetime
- 2000-06-27 EP EP00943236A patent/EP1194449B1/en not_active Expired - Lifetime
- 2000-06-27 AT AT00943236T patent/ATE482233T1/de not_active IP Right Cessation
- 2000-06-27 CN CN00810930A patent/CN1379819A/zh active Pending
- 2000-06-27 DE DE60045005T patent/DE60045005D1/de 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 JP JP2001507071A patent/JP4484410B2/ja not_active Expired - Fee Related
- 2000-06-27 AU AU57715/00A patent/AU5771500A/en not_active Abandoned
- 2000-06-27 CA CA2374346A patent/CA2374346C/en not_active Expired - Fee Related
- 2000-06-27 CA CA002374610A patent/CA2374610A1/en not_active Abandoned
- 2000-06-27 AU AU57735/00A patent/AU5773500A/en not_active Abandoned
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| US20040220079A1 (en) | 2004-11-04 |
| DE60045005D1 (de) | 2010-11-04 |
| WO2001000663A3 (en) | 2001-10-04 |
| JP2003503072A (ja) | 2003-01-28 |
| CA2374610A1 (en) | 2001-01-04 |
| US20020164760A1 (en) | 2002-11-07 |
| EP1194449A2 (en) | 2002-04-10 |
| JP5138851B2 (ja) | 2013-02-06 |
| US20040167075A1 (en) | 2004-08-26 |
| CN1379819A (zh) | 2002-11-13 |
| EP1194449B1 (en) | 2010-09-22 |
| EP1196609A2 (en) | 2002-04-17 |
| WO2001000665A3 (en) | 2001-09-27 |
| US20080021196A1 (en) | 2008-01-24 |
| WO2001000665A9 (en) | 2002-07-25 |
| US7678760B2 (en) | 2010-03-16 |
| AU5773500A (en) | 2001-01-31 |
| US7829669B2 (en) | 2010-11-09 |
| US6545127B1 (en) | 2003-04-08 |
| ATE482233T1 (de) | 2010-10-15 |
| WO2001000665A2 (en) | 2001-01-04 |
| CA2374346A1 (en) | 2001-01-04 |
| US7244708B2 (en) | 2007-07-17 |
| JP2003506322A (ja) | 2003-02-18 |
| JP4484410B2 (ja) | 2010-06-16 |
| AU5771500A (en) | 2001-01-31 |
| US20080112946A1 (en) | 2008-05-15 |
| WO2001000663A2 (en) | 2001-01-04 |
| US20020115600A1 (en) | 2002-08-22 |
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