WO1996020725A3 - Peptide, peptide analog and amino acid analog protease inhibitors - Google Patents

Peptide, peptide analog and amino acid analog protease inhibitors Download PDF

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Publication number
WO1996020725A3
WO1996020725A3 PCT/US1996/000360 US9600360W WO9620725A3 WO 1996020725 A3 WO1996020725 A3 WO 1996020725A3 US 9600360 W US9600360 W US 9600360W WO 9620725 A3 WO9620725 A3 WO 9620725A3
Authority
WO
WIPO (PCT)
Prior art keywords
peptide
analog
amino acid
protease inhibitors
butyl
Prior art date
Application number
PCT/US1996/000360
Other languages
French (fr)
Other versions
WO1996020725A2 (en
Inventor
Benito Munoz
Ian Alexander Mcdonald
Elisabeth Albrecht
Original Assignee
Salk Inst Biotech Ind
Benito Munoz
Ian Alexander Mcdonald
Elisabeth Albrecht
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.)
Filing date
Publication date
Priority claimed from US08/369,422 external-priority patent/US5804560A/en
Application filed by Salk Inst Biotech Ind, Benito Munoz, Ian Alexander Mcdonald, Elisabeth Albrecht filed Critical Salk Inst Biotech Ind
Priority to AU46973/96A priority Critical patent/AU4697396A/en
Publication of WO1996020725A2 publication Critical patent/WO1996020725A2/en
Publication of WO1996020725A3 publication Critical patent/WO1996020725A3/en

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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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III), in which R1 is preferably 2-methyl propene, 2-butene, norleucine; R2, R4, and R8 are each independently methyl or ethyl; R3 is preferably iso-butyl or phenyl; R5 is preferably iso-butyl; R6 is H or methyl; R7 - (Q)n is preferably benzyloxycarbonyl or acetyl; Q is preferably -C(O)-; RB is preferably iso-butyl; RA = -(T)m-(D)m-R1, in which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C3-4 alkenyl; and X is an alcohol, particularly a secondary alcohol.
PCT/US1996/000360 1995-01-06 1996-01-05 Peptide, peptide analog and amino acid analog protease inhibitors WO1996020725A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU46973/96A AU4697396A (en) 1995-01-06 1996-01-05 Peptide, peptide analog and amino acid analog protease inibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US369,422 1995-01-06
US08/369,422 US5804560A (en) 1995-01-06 1995-01-06 Peptide and peptide analog protease inhibitors
US403,420 1995-03-13
US08/403,420 US5969100A (en) 1995-01-06 1995-03-13 Peptide, peptide analog and amino acid analog protease inhibitors

Publications (2)

Publication Number Publication Date
WO1996020725A2 WO1996020725A2 (en) 1996-07-11
WO1996020725A3 true WO1996020725A3 (en) 1996-10-17

Family

ID=27004573

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1996/000360 WO1996020725A2 (en) 1995-01-06 1996-01-05 Peptide, peptide analog and amino acid analog protease inhibitors

Country Status (3)

Country Link
US (3) US6017887A (en)
AU (1) AU4697396A (en)
WO (1) WO1996020725A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11851422B2 (en) 2021-07-09 2023-12-26 Aligos Therapeutics, Inc. Anti-viral compounds

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996039194A1 (en) * 1995-06-06 1996-12-12 Athena Neurosciences, Inc. Novel cathepsin and methods and compositions for inhibition thereof
US5849711A (en) * 1995-06-06 1998-12-15 Athena Neurosciences, Inc. Cathepsin and methods and compositions for inhibition thereof
US6207710B1 (en) 1996-11-22 2001-03-27 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6096782A (en) * 1996-11-22 2000-08-01 Athena Neurosciences, Inc. N-(aryl/heteroaryl) amino acid derivatives pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6211235B1 (en) 1996-11-22 2001-04-03 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
TR199901132T2 (en) * 1996-11-22 1999-08-23 Elan Pharmaceuticals, Inc. To inhibit the release and/or synthesis of β-amyloid peptide using N-(aryl/heteoaryl) amino acid derivatives, pharmaceutical compositions containing them, and such compounds for methods.
US6191166B1 (en) 1997-11-21 2001-02-20 Elan Pharmaceuticals, Inc. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6642261B2 (en) 1997-11-21 2003-11-04 Athena Neurosciences, Inc. N-(aryl/heteroarylacety) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
AR016751A1 (en) * 1996-11-22 2001-08-01 Athena Neurosciences Inc METHOD FOR INHIBITING THE RELEASE OF THE BETA-AMYLOID PEPTIDE IN A CELL, PHARMACEUTICAL COMPOSITION AND USEFUL COMPOUNDS IN THIS METHOD
US6683075B1 (en) 1996-12-23 2004-01-27 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use
US6635632B1 (en) 1996-12-23 2003-10-21 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US7119105B2 (en) * 1997-02-04 2006-10-10 The Regents Of The University Of California Methods for treating neurodegenerative disorders using aspartyl protease inhibitors
US6423688B1 (en) 1997-07-31 2002-07-23 Athena Neurosciences, Inc. Dipeptide and related compounds which inhibit leukocyte adhesion mediated by VLA-4
US6489300B1 (en) 1997-07-31 2002-12-03 Eugene D. Thorsett Carbamyloxy compounds which inhibit leukocyte adhesion mediated by VLA-4
US6291453B1 (en) 1997-07-31 2001-09-18 Athena Neurosciences, Inc. 4-amino-phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
US6362341B1 (en) 1997-07-31 2002-03-26 Athena Neurosciences, Inc. Benzyl compounds which inhibit leukocyte adhesion mediated by VLA-4
US7030114B1 (en) 1997-07-31 2006-04-18 Elan Pharmaceuticals, Inc. Compounds which inhibit leukocyte adhesion mediated by VLA-4
US6939855B2 (en) 1997-07-31 2005-09-06 Elan Pharmaceuticals, Inc. Anti-inflammatory compositions and method
US6559127B1 (en) 1997-07-31 2003-05-06 Athena Neurosciences, Inc. Compounds which inhibit leukocyte adhesion mediated by VLA-4
US6583139B1 (en) 1997-07-31 2003-06-24 Eugene D. Thorsett Compounds which inhibit leukocyte adhesion mediated by VLA-4
US6492421B1 (en) 1997-07-31 2002-12-10 Athena Neurosciences, Inc. Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
US6423689B1 (en) 1997-12-22 2002-07-23 Warner-Lambert Company Peptidyl calcium channel blockers
KR20010052503A (en) 1998-06-03 2001-06-25 다니엘 피. 맥컬럼 N-linked sulfonamides of n-heterocyclic carboxylic acids or carboxylic acid isosteres
US6774125B2 (en) 1998-06-22 2004-08-10 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6569851B1 (en) 1998-06-22 2003-05-27 Elan Pharmaceutials, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6509331B1 (en) 1998-06-22 2003-01-21 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6528505B1 (en) 1998-06-22 2003-03-04 Elan Pharmaceuticals, Inc. Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6958330B1 (en) 1998-06-22 2005-10-25 Elan Pharmaceuticals, Inc. Polycyclic α-amino-ε-caprolactams and related compounds
US6552013B1 (en) 1998-06-22 2003-04-22 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
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
US6407066B1 (en) 1999-01-26 2002-06-18 Elan Pharmaceuticals, Inc. Pyroglutamic acid derivatives and related compounds which inhibit leukocyte adhesion mediated by VLA-4
AU2985100A (en) 1999-02-08 2000-08-25 Checkpoint Genetics, Inc. (n)-substituted amino acids, antioxidant pharmaceutical compositions containing same and methods using same
EP1445263A1 (en) * 1999-02-10 2004-08-11 Elan Pharmaceuticals, Inc. Human beta-secretase enzyme, inhibitors and their compositions and uses
WO2000047618A2 (en) 1999-02-10 2000-08-17 Elan Pharmaceuticals, Inc. HUMAN β-SECRETASE ENZYME, INHIBITORS AND THEIR COMPOSITIONS AND USES
GB2389182B (en) * 1999-02-10 2004-02-04 Elan Pharm Inc Method of purifying b-secretase
US6395897B1 (en) 1999-03-02 2002-05-28 Boehringer Ingelheim Pharmaceuticals, Inc. Nitrile compounds useful as reversible inhibitors of #9 cathepsin 5
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US7253169B2 (en) 1999-11-12 2007-08-07 Gliamed, Inc. Aza compounds, pharmaceutical compositions and methods of use
US6417189B1 (en) 1999-11-12 2002-07-09 Gpi Nil Holdings, Inc. AZA compounds, pharmaceutical compositions and methods of use
US7514408B1 (en) 1999-12-02 2009-04-07 Elan Pharmaceuticals, Inc. β-secretase enzyme compositions and methods
US6992081B2 (en) 2000-03-23 2006-01-31 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
EP1265849B1 (en) 2000-03-23 2006-10-25 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
EP1295876A4 (en) * 2000-06-30 2005-10-19 Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them
KR20030058959A (en) * 2000-06-30 2003-07-07 엘란 파마슈티칼스, 인크. Compounds to treat alzheimer's disease
US6846813B2 (en) * 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
PE20020276A1 (en) 2000-06-30 2002-04-06 Elan Pharm Inc SUBSTITUTE AMINE COMPOUNDS AS ß-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER
US20030096864A1 (en) * 2000-06-30 2003-05-22 Fang Lawrence Y. Compounds to treat alzheimer's disease
US6696488B2 (en) 2000-08-11 2004-02-24 The Brigham And Women's Hospital, Inc. (Hydroxyethyl)ureas as inhibitors of alzheimer's β-amyloid production
BR0210721A (en) * 2001-06-27 2004-07-20 Elan Pharm Inc Pharmaceutically acceptable compound, salt or ester, method for making a compound, and method for treating a patient having, or preventing the patient from acquiring a disease or condition.
US20070213407A1 (en) * 2001-06-29 2007-09-13 Elan Pharmaceuticals And Pharmacia & Upjohn Company Llc Compounds to treat Alzheimer's disease
CH698246B1 (en) * 2001-12-20 2009-06-30 Hoffmann La Roche Test to identify inhibitors of beta secretases.
US7153822B2 (en) * 2002-01-29 2006-12-26 Wyeth Compositions and methods for modulating connexin hemichannels
AU2003256305A1 (en) * 2002-06-24 2004-01-06 Axys Pharmaceuticals, Inc. Peptidic compounds as cysteine protease inhibitors
US9119846B2 (en) 2003-04-29 2015-09-01 Neurim Pharmaceuticals (1991) Ltd. Method and composition for enhancing cognition in alzheimer's patients
IL155666A (en) * 2003-04-29 2013-12-31 Neurim Pharma 1991 Composition for treating insomnia
EP1760076A1 (en) 2005-09-02 2007-03-07 Ferring B.V. FAP Inhibitors
US8163800B2 (en) 2008-07-28 2012-04-24 Blanchette Rockefeller Neurosciences Institute PKC-activating compounds for the treatment of neurodegenerative diseases
US9290759B2 (en) * 2010-08-25 2016-03-22 The Trustees Of Columbia University In The City Of New York Optimized miRNA constructs

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0068551A1 (en) * 1981-06-25 1983-01-05 THE PROCTER & GAMBLE COMPANY Non-nutritive sweeteners
EP0266950A2 (en) * 1986-10-31 1988-05-11 Pfizer Inc. Nor-statine and nor-cyclostatine polypeptides
EP0393457A1 (en) * 1989-04-10 1990-10-24 Suntory Limited Proteinase inhibitor
WO1992014696A2 (en) * 1991-02-22 1992-09-03 The Du Pont Merck Pharmaceutical Company SUBSTITUTED α-AMINOALDEHYDES AND DERIVATIVES
EP0528629A2 (en) * 1991-08-12 1993-02-24 Bend Research, Inc. Enzymatic synthesis of renin inhibitors
EP0543310A2 (en) * 1991-11-19 1993-05-26 Suntory Limited Dipeptide derivative and prophylactic and therapeutic agent for bone diseases containing the same
EP0555537A2 (en) * 1991-12-04 1993-08-18 Banyu Pharmaceutical Co., Ltd. Endothelin antagonistic substance
EP0578978A1 (en) * 1992-06-15 1994-01-19 Suntory Limited Dipeptide derivative and prophylactic or therapeutic agent for bone diseases containing same as active ingredient
EP0615969A1 (en) * 1993-03-12 1994-09-21 Sandoz Ltd. 2,4-Diamino-3-hydroxycarboxylic acid derivatives

Family Cites Families (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1429184A (en) * 1972-04-20 1976-03-24 Allen & Hanburys Ltd Physically anti-inflammatory steroids for use in aerosols
US4044126A (en) * 1972-04-20 1977-08-23 Allen & Hanburys Limited Steroidal aerosol compositions and process for the preparation thereof
CA1161431A (en) * 1979-05-11 1984-01-31 Lars G. Svendsen Tripeptide derivatives
US4701407A (en) * 1982-11-24 1987-10-20 Baylor College Of Medicine Diagnosis of Alzheimer disease
US4472305A (en) * 1983-05-17 1984-09-18 Sterling Drug Inc. Hexapeptide amides
US4845079A (en) * 1985-01-23 1989-07-04 Luly Jay R Peptidylaminodiols
FR2585708B1 (en) * 1985-07-31 1989-07-07 Sanofi Sa RESIN AND ACID PROTEIN INHIBITOR AMINOALCOHOL DERIVATIVES, PREPARATION METHOD THEREOF AND THERAPEUTIC APPLICATION THEREOF
US4666829A (en) * 1985-05-15 1987-05-19 University Of California Polypeptide marker for Alzheimer's disease and its use for diagnosis
US4829052A (en) * 1986-06-11 1989-05-09 Monsanto Company Serine protease inhibitors
US5034376A (en) * 1986-10-31 1991-07-23 Pfizer Inc. Nor-statine and nor-cyclostatine polypeptides
AU611122B2 (en) * 1986-11-17 1991-06-06 Scios Nova Inc. Recombinant alzheimer's amyloid protein
GB2197663B (en) * 1986-11-21 1990-07-11 Manganese Bronze Ltd High density sintered ferrous alloys
DE3702789A1 (en) * 1987-01-30 1988-08-18 Bayer Ag PROCUREMENT PROTEIN OF APC POLYPEPTIDE, FOR CODING DNA AND DIAGNOSTIC USE OF DNA AND PROTEIN
JPS63245689A (en) * 1987-03-31 1988-10-12 Suntory Ltd Human amyloid-related protein monoclonal antibody
AU620327B2 (en) * 1987-04-08 1992-02-20 Salutar, Inc. Amyloidosis and alzheimer's disease diagnostic assay and reagents therefor
US5039511A (en) * 1987-04-08 1991-08-13 Salutar, Inc. Amyloidosis and alzheimer's disease diagnostic assay and reagents therefor
GB8809316D0 (en) * 1987-05-11 1988-05-25 Ici America Inc Heterocyclic ketones
CA1313828C (en) * 1987-06-25 1993-02-23 Yves Fradet Monoclonal antibodies to superficial papillary bladder tumor cells
US5231000A (en) * 1987-10-08 1993-07-27 The Mclean Hospital Antibodies to A4 amyloid peptide
US5547841A (en) * 1987-10-08 1996-08-20 The Mclean Hospital Corporation In vitro method for screening for drugs that inhibit production or degradation of human A4-amyloid
US4906465A (en) * 1987-10-19 1990-03-06 Massachusetts Institute Of Technology Antithrombogenic devices containing polysiloxanes
US5015570A (en) * 1988-05-13 1991-05-14 Molecular Therapeutics, Inc. Molecular diagnosis of Alzheimer Disease
DE3823454A1 (en) * 1988-07-11 1990-01-25 Henkel Kgaa MERCERIZING AND / OR LYING AGENT
DE3833572A1 (en) * 1988-10-03 1990-04-05 Pfersee Chem Fab STABLE, FINE-PARTIC, AQUEOUS COMPONENT SILICONE CATALYSTS, METHOD FOR THE PRODUCTION AND USE THEREOF
ZA897515B (en) * 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
WO1990005138A1 (en) * 1988-11-08 1990-05-17 The Children's Medical Center Corporation Cytotoxic amyloid precursors and screening assays using them
US5262332A (en) * 1989-04-05 1993-11-16 Brigham And Women's Hospital Diagnostic method for Alzheimer's disease: examination of non-neural tissue
WO1990012871A1 (en) * 1989-04-14 1990-11-01 Research Foundation For Mental Hygiene, Inc. Cerebrovascular amyloid protein-specific monoclonal antibody sv17-6e10
US5234814A (en) * 1989-06-01 1993-08-10 Du Pont Merck Pharmaceutical Company Diagnostic assay for alzheimer's disease
US5039842A (en) * 1989-06-07 1991-08-13 Fairchild Industries, Inc. Mold heater moisture detection and dry out apparatus
US5232928A (en) * 1989-07-25 1993-08-03 Boehringer Ingelheim Pharmaceuticals, Inc. Tetrahydroisoquinoline amides
CA2021660A1 (en) * 1989-07-26 1991-01-27 Philippe Bey Peptidase inhibitors
CA2065404C (en) * 1989-09-18 2002-12-24 Barbara Cordell Assays and reagents for amyloid deposition
US5221665A (en) * 1989-10-27 1993-06-22 Boehringer Ingelheim Pharmaceuticals, Inc. N-substituted amides
AU7121191A (en) * 1990-02-26 1991-10-10 Albert Einstein College Of Medicine Of Yeshiva University Diagnostic assay for alzheimer's disease
GB9007922D0 (en) * 1990-04-07 1990-06-06 Oxford Virology Plc A diagnostic test method
CA2079880A1 (en) * 1990-04-24 1991-10-25 William E. Van Nostrand Purification, detection and methods of use of protease nexin-2
US5213962A (en) * 1990-04-24 1993-05-25 The Regents Of The University Of California Purification, detection and methods of use of protease Nexin-2
US5430022A (en) * 1990-05-14 1995-07-04 Fujisawa Pharmaceutical Co., Ltd. Peptide compound and its preparation
US5284828A (en) * 1990-05-14 1994-02-08 Fujisawa Pharmaceutical Co. Ltd. Peptide compound and its preparation
US5242932A (en) * 1991-12-17 1993-09-07 The Rockefeller University Treatment of amyloidosis associated with alzheimer disease
US5496928A (en) * 1990-06-07 1996-03-05 Banyu Pharmaceutical Co., Ltd. Endothelin antagonistic substance
CA2043741C (en) * 1990-06-07 2003-04-01 Kiyofumi Ishikawa Endothelin antagonistic peptide derivatives
AU8215391A (en) * 1990-06-29 1992-01-23 Case Western Reserve University Diagnostic and prognostic methods based on soluble derivatives of the beta amyloid protein precursor
US5223633A (en) * 1990-06-30 1993-06-29 Bayer Aktiengesellschaft Preparation of sec. or tert. alcohols
US5200339A (en) * 1990-08-17 1993-04-06 Abraham Carmela R Proteases causing abnormal degradation of amyloid β-protein precursor
WO1992003542A1 (en) * 1990-08-17 1992-03-05 Boston University PROTEASES CAUSING ABNORMAL DEGRADATION OF AMYLOID β-PROTEIN PRECURSOR
US5292652A (en) * 1990-10-05 1994-03-08 Athena Neurosciences, Inc. Amyloidin protease and uses thereof
ATE147098T1 (en) * 1990-10-12 1997-01-15 Max Planck Gesellschaft MODIFIED RIBOZYMES
BE1003316A5 (en) * 1990-11-27 1992-02-25 Will L F & Cie Sa MONOCLONAL ANTIBODY USEFUL FOR THE DIAGNOSIS OF ALZHEIMER'S DISEASE, SECRETARY HYBRIDOMA OF SUCH A MONOCLONAL ANTIBODY AND PROCESS FOR PREPARING THE SAME.
EP0504938A3 (en) * 1991-03-22 1993-04-14 Suntory Limited Prophylactic and therapeutic agent for bone diseases comprising di- or tripeptide derivative as active ingredient
DE69229552T2 (en) * 1991-05-23 1999-12-23 Merrell Pharma Inc INHIBITORS FOR KATHEPSIN-G AND ELASTASE FOR THE PREVENTION OF TISSUE DISABLING
AU2765992A (en) * 1991-10-03 1993-05-03 Indiana University Foundation Method for screening for alzheimer's disease
WO1993010459A1 (en) * 1991-11-12 1993-05-27 The University Of Melbourne A method for assaying and treating alzheimer's disease
US5538845A (en) * 1992-02-05 1996-07-23 Athena Neurosciences, Inc. Beta-amyloid peptide production inhibitors and methods for their identification
CA2086165A1 (en) * 1992-04-09 1993-10-10 Paul P. Tamburini Diagnostic assay for alzheimer's disease based on the proteolysis of alzheimer's precursor protein
US5441870A (en) * 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
US5604102A (en) * 1992-04-15 1997-02-18 Athena Neurosciences, Inc. Methods of screening for β-amyloid peptide production inhibitors
TW327194B (en) * 1992-05-01 1998-02-21 American Cyanamid Co Novel amyloid precursor proteins and methods of using same
WO1995013084A1 (en) * 1992-05-11 1995-05-18 Miles Inc. Cathepsin d is an amyloidogenic protease in alzheimer's disease
AU679675B2 (en) * 1992-05-11 1997-07-10 Bayer Corporation Methods for detecting beta amyloid precursor protein processing enzymes
AU4544993A (en) * 1992-06-24 1994-01-24 Cortex Pharmaceuticals, Inc. Use of calpain inhibitors in the inhibition and treatment of medical conditions associated with increased calpain activity
US5766846A (en) * 1992-07-10 1998-06-16 Athena Neurosciences Methods of screening for compounds which inhibit soluble β-amyloid peptide production
WO1994001772A1 (en) * 1992-07-13 1994-01-20 The Children's Medical Center Corporation SCREEN FOR ALZHEIMER'S DISEASE THERAPEUTICS BASED ON β-AMYLOID PRODUCTION
EP0580161A1 (en) * 1992-07-22 1994-01-26 THE McLEAN HOSPITAL CORPORATION Prophylactic and therapeutic treatment of Alzheimer's disease
ATE173088T1 (en) * 1992-07-22 1998-11-15 Mclean Hospital Corp METHOD FOR DETECTING ALZHEIMER'S DISEASE
US5374623A (en) * 1992-08-20 1994-12-20 Prototek, Inc. Cysteine protease inhibitors effective for in vivo use
JP3265577B2 (en) * 1992-10-13 2002-03-11 デューク・ユニバーシティ Method for measuring type 4 isoform of apolipoprotein E
US5605811A (en) * 1992-10-26 1997-02-25 Athena Neurosciences, Inc. Methods and compositions for monitoring cellular processing of beta-amyloid precursor protein
AU5968994A (en) * 1992-12-16 1994-07-04 Johanna E. Bergmann Agents for the prevention and treatment of human alzheimer's disease
GB2290543B (en) * 1993-03-16 1996-05-22 British Biotech Pharm Hydroxamic acid derivatives as metalloproteinase inhibitors
JP3599287B2 (en) * 1993-04-28 2004-12-08 三菱化学株式会社 Sulfonamide derivative
CA2122227A1 (en) * 1993-04-29 1994-10-30 Roland E. Dolle Peptide analogs as irreversible interleukin-1.beta. protease inhibitors
JPH0789951A (en) * 1993-06-03 1995-04-04 Sterling Winthrop Inc Interleukin-1 beta transfer enzyme inhibitor
JPH06345722A (en) * 1993-06-04 1994-12-20 Mitsubishi Kasei Corp Thioacetal derivative
EP0627400A1 (en) * 1993-06-04 1994-12-07 Merrell Dow Pharmaceuticals Inc. Aromatic acetylcholinesterase inhibitors
JP2745188B2 (en) * 1993-06-21 1998-04-28 矢崎総業株式会社 Connection terminal for fuse
US5541290A (en) * 1993-06-24 1996-07-30 Harbeson; Scott L. Optically pure calpain inhibitor compounds
GB9313330D0 (en) * 1993-06-28 1993-08-11 Fujisawa Pharmaceutical Co New compound and its preparation
HUT73527A (en) * 1993-08-13 1996-08-28 Seikagaku Kogyo Co Ltd Remedy for nervous diseases
AU7714594A (en) * 1993-08-13 1995-03-14 Merck & Co., Inc. Substituted ketone derivatives as inhibitors of interleukin-1beta converting enzyme
JPH09502202A (en) * 1993-09-07 1997-03-04 ザ、プロクター、エンド、ギャンブル、カンパニー Composition containing amino acid salt of propionic acid non-steroidal anti-inflammatory drug and caffeine
DE4331134A1 (en) * 1993-09-14 1995-03-16 Bayer Ag New antiviral pseudopeptides
GB9402680D0 (en) * 1994-02-11 1994-04-06 Zeneca Ltd Pyrrolidine derivatives
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US5414945A (en) * 1994-05-10 1995-05-16 Black & Decker, Inc. Iron assembly including water cassette and base
JP3274034B2 (en) * 1994-12-26 2002-04-15 三菱電機株式会社 Semiconductor acceleration detector
GB9510162D0 (en) * 1995-05-19 1995-07-12 Bouras Elias Compositions for the treatment of skin conditions
EP0823827A3 (en) * 1996-08-09 1999-09-29 Hewlett-Packard Company Mobile communications systems and methods of operating such systems
NL1004577C2 (en) * 1996-11-20 1998-05-25 Geesink Bv Device for lifting and / or tilting containers.
EP2698610B1 (en) 2012-08-17 2015-04-29 Siemens Aktiengesellschaft Displacement sensor, in particular for use in a subsea device

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0068551A1 (en) * 1981-06-25 1983-01-05 THE PROCTER & GAMBLE COMPANY Non-nutritive sweeteners
EP0266950A2 (en) * 1986-10-31 1988-05-11 Pfizer Inc. Nor-statine and nor-cyclostatine polypeptides
EP0393457A1 (en) * 1989-04-10 1990-10-24 Suntory Limited Proteinase inhibitor
WO1992014696A2 (en) * 1991-02-22 1992-09-03 The Du Pont Merck Pharmaceutical Company SUBSTITUTED α-AMINOALDEHYDES AND DERIVATIVES
EP0528629A2 (en) * 1991-08-12 1993-02-24 Bend Research, Inc. Enzymatic synthesis of renin inhibitors
EP0543310A2 (en) * 1991-11-19 1993-05-26 Suntory Limited Dipeptide derivative and prophylactic and therapeutic agent for bone diseases containing the same
EP0555537A2 (en) * 1991-12-04 1993-08-18 Banyu Pharmaceutical Co., Ltd. Endothelin antagonistic substance
EP0578978A1 (en) * 1992-06-15 1994-01-19 Suntory Limited Dipeptide derivative and prophylactic or therapeutic agent for bone diseases containing same as active ingredient
EP0615969A1 (en) * 1993-03-12 1994-09-21 Sandoz Ltd. 2,4-Diamino-3-hydroxycarboxylic acid derivatives

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
D. W. PATEL ET. AL.: "Activated Ketone Inhibitors of Human Renin.", JOURNAL OF MEDICINAL CHEMISTRY, vol. 36, no. 17, 20 August 1993 (1993-08-20), WASHINGTON DC, US, pages 2432 - 47, XP002004099 *
H. L. SHAM ET. AL.: "Highly potent and specific inhibitors of human renin.", FEBS LETTERS, vol. 220, no. 2, 17 August 1987 (1987-08-17), AMSTERDAM, NL, pages 299 - 301, XP002004100 *
H. W. KLAFKI ET. AL.: "Calpain inhibitor I decreases beta-A4 secretion from human embryonal kidney cells expressing beta-amyloid precursor protein carrying the APP670/671 double mutation.", NEUROSCIENCE LETTERS, vol. 201, no. 1, January 1995 (1995-01-01), SHANNON, IE, pages 29 - 32, XP002004102 *
T. SASAKI ET. AL.: "Inhibitory effect of di- and tripeptidyl aldehydes on calpains and cathespins.", JOURNAL OF ENZYME INHIBITION, vol. 3, 1990, NEW YORK, US, pages 195 - 201, XP002004101 *
T. TSUJINAKA ET. AL.: "Synthesis of a new cell penetrating calpain inhibitor (Calpeptin).", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, vol. 153, no. 3, 30 June 1988 (1988-06-30), NEW YORK, US, pages 1201 - 8, XP002011631 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11851422B2 (en) 2021-07-09 2023-12-26 Aligos Therapeutics, Inc. Anti-viral compounds

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