DE60045005D1 - Inhibitoren des memapsin 2 und ihre verwendung - Google Patents

Inhibitoren des memapsin 2 und ihre verwendung

Info

Publication number: DE60045005D1
Authority: DE; Germany
Prior art keywords: memapsin; substrate; ala; bond; leu
Prior art date: 1999-06-28
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 - Lifetime

Application number

DE60045005T

Other languages

English (en)

Inventor

Jordan J Tang

Lin Hong

Arun K Ghosh

Xinli Lin

Gerald Koelsch

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Oklahoma Medical Research Foundation

University of Illinois

Original Assignee

Oklahoma Medical Research Foundation

University of Illinois

Priority date (The priority date 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 date listed.)

1999-06-28

Filing date

2000-06-27

Publication date

2010-11-04

2000-06-27 Application filed by Oklahoma Medical Research Foundation, University of Illinois filed Critical Oklahoma Medical Research Foundation

2010-11-04 Application granted granted Critical

2010-11-04 Publication of DE60045005D1 publication Critical patent/DE60045005D1/de

2020-06-28 Anticipated expiration legal-status Critical

Status Expired - Lifetime legal-status Critical Current

Links

102100021257 Beta-secretase 1 Human genes 0.000 title abstract 9
101710150192 Beta-secretase 1 Proteins 0.000 title abstract 8
239000003112 inhibitor Substances 0.000 title abstract 4
239000000758 substrate Substances 0.000 abstract 9
NIOCOJFPGCXNKL-ZKZXETMPSA-N (4s)-4-amino-5-[[(2s)-1-[[(2s)-4-amino-1-[[(4s,5s,7r)-8-[[(2s)-1-[[(2s)-4-carboxy-1-[[(1s)-1-carboxy-2-phenylethyl]amino]-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-ox Chemical compound OC(=O)CC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)[C@@H](O)C[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 NIOCOJFPGCXNKL-ZKZXETMPSA-N 0.000 abstract 4
108010011140 OM99-2 Proteins 0.000 abstract 4
238000000034 method Methods 0.000 abstract 3
108090000765 processed proteins & peptides Proteins 0.000 abstract 2
208000024827 Alzheimer disease Diseases 0.000 abstract 1
102000004190 Enzymes Human genes 0.000 abstract 1
108090000790 Enzymes Proteins 0.000 abstract 1
IMROMDMJAWUWLK-UHFFFAOYSA-N Ethenol Chemical group OC=C IMROMDMJAWUWLK-UHFFFAOYSA-N 0.000 abstract 1
125000000539 amino acid group Chemical group 0.000 abstract 1
230000015572 biosynthetic process Effects 0.000 abstract 1
238000002050 diffraction method Methods 0.000 abstract 1
230000005764 inhibitory process Effects 0.000 abstract 1
238000004519 manufacturing process Methods 0.000 abstract 1
230000002265 prevention Effects 0.000 abstract 1
108090000623 proteins and genes Proteins 0.000 abstract 1
102000004169 proteins and genes Human genes 0.000 abstract 1
238000003786 synthesis reaction Methods 0.000 abstract 1

Classifications

- 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
- C07K5/10—Tetrapeptides
- C07K5/1021—Tetrapeptides with the first amino acid being acidic
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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
- 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
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
- 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
- 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
- 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
- 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)
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- 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

Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Genetics & Genomics (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Engineering & Computer Science (AREA)
Biochemistry (AREA)
Molecular Biology (AREA)
Bioinformatics & Cheminformatics (AREA)
Biophysics (AREA)
Biomedical Technology (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Zoology (AREA)
Wood Science & Technology (AREA)
General Engineering & Computer Science (AREA)
General Chemical & Material Sciences (AREA)
Microbiology (AREA)
Biotechnology (AREA)
Chemical Kinetics & Catalysis (AREA)
Crystallography & Structural Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Analytical Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

DE60045005T 1999-06-28 2000-06-27 Inhibitoren des memapsin 2 und ihre verwendung Expired - Lifetime DE60045005D1 (de)

Applications Claiming Priority (6)

Application Number	Priority Date	Filing Date	Title
US14136399P	1999-06-28	1999-06-28
US16806099P	1999-11-30	1999-11-30
US17783600P	2000-01-25	2000-01-25
US17836800P	2000-01-27	2000-01-27
US21029200P	2000-06-08	2000-06-08
PCT/US2000/017742 WO2001000665A2 (en)	1999-06-28	2000-06-27	Inhibitors of memapsin 2 and use thereof

Publications (1)

Publication Number	Publication Date
DE60045005D1 true DE60045005D1 (de)	2010-11-04

Family

ID=27538142

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DE60045005T Expired - Lifetime DE60045005D1 (de)	1999-06-28	2000-06-27	Inhibitoren des memapsin 2 und ihre verwendung

Country Status (9)

Country	Link
US (7)	US6545127B1 (de)
EP (2)	EP1196609A2 (de)
JP (2)	JP4484410B2 (de)
CN (1)	CN1379819A (de)
AT (1)	ATE482233T1 (de)
AU (2)	AU5773500A (de)
CA (2)	CA2374610A1 (de)
DE (1)	DE60045005D1 (de)
WO (2)	WO2001000663A2 (de)

Families Citing this family (107)

* Cited by examiner, † Cited by third party
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2000
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Publication number	Publication date
ATE482233T1 (de)	2010-10-15
US20020164760A1 (en)	2002-11-07
CA2374346C (en)	2010-06-22
US6545127B1 (en)	2003-04-08
US7678760B2 (en)	2010-03-16
JP4484410B2 (ja)	2010-06-16
AU5771500A (en)	2001-01-31
US7829669B2 (en)	2010-11-09
WO2001000663A2 (en)	2001-01-04
JP2003503072A (ja)	2003-01-28
AU5773500A (en)	2001-01-31
WO2001000665A3 (en)	2001-09-27
WO2001000665A2 (en)	2001-01-04
US20080112946A1 (en)	2008-05-15
JP5138851B2 (ja)	2013-02-06
US20020115600A1 (en)	2002-08-22
CN1379819A (zh)	2002-11-13
EP1194449A2 (de)	2002-04-10
US20040220079A1 (en)	2004-11-04
CA2374610A1 (en)	2001-01-04
WO2001000665A9 (en)	2002-07-25
JP2003506322A (ja)	2003-02-18
US7244708B2 (en)	2007-07-17
EP1194449B1 (de)	2010-09-22
EP1196609A2 (de)	2002-04-17
CA2374346A1 (en)	2001-01-04
US20080021196A1 (en)	2008-01-24
US20040167075A1 (en)	2004-08-26
WO2001000663A3 (en)	2001-10-04

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