WO1995034538A3 - Purification of serine proteases and synthetic inhibitors thereof - Google Patents
Purification of serine proteases and synthetic inhibitors thereof Download PDFInfo
- Publication number
- WO1995034538A3 WO1995034538A3 PCT/EP1995/002255 EP9502255W WO9534538A3 WO 1995034538 A3 WO1995034538 A3 WO 1995034538A3 EP 9502255 W EP9502255 W EP 9502255W WO 9534538 A3 WO9534538 A3 WO 9534538A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- serine proteases
- purification
- synthetic inhibitors
- xaa
- new compounds
- Prior art date
Links
- 108010022999 Serine Proteases Proteins 0.000 title abstract 2
- 102000012479 Serine Proteases Human genes 0.000 title abstract 2
- 238000000746 purification Methods 0.000 title 1
- 239000012622 synthetic inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 101000684208 Homo sapiens Prolyl endopeptidase FAP Proteins 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
-
- 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
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Abstract
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP95923301A EP0764151A2 (en) | 1994-06-10 | 1995-06-09 | Purification of serine protease and synthetic inhibitors thereof |
US08/750,484 US6090786A (en) | 1994-06-10 | 1995-06-09 | Serine proteases, their activity and their synthetic inhibitors |
AU27908/95A AU2790895A (en) | 1994-06-10 | 1995-06-09 | Purification of serine protease and synthetic inhibitors thereof |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP94201668 | 1994-06-10 | ||
EP94201668.4 | 1994-06-10 | ||
EP94203707.8 | 1994-12-20 | ||
EP94203707 | 1994-12-20 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO1995034538A2 WO1995034538A2 (en) | 1995-12-21 |
WO1995034538A3 true WO1995034538A3 (en) | 1996-02-15 |
Family
ID=26136329
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/EP1995/002255 WO1995034538A2 (en) | 1994-06-10 | 1995-06-09 | Purification of serine proteases and synthetic inhibitors thereof |
Country Status (4)
Country | Link |
---|---|
US (1) | US6090786A (en) |
EP (1) | EP0764151A2 (en) |
AU (1) | AU2790895A (en) |
WO (1) | WO1995034538A2 (en) |
Families Citing this family (81)
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US6825169B1 (en) | 1991-10-22 | 2004-11-30 | Trustees Of Tufts College | Inhibitors of dipeptidyl-aminopeptidase type IV |
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US20020006899A1 (en) * | 1998-10-06 | 2002-01-17 | Pospisilik Andrew J. | Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals |
US5965532A (en) * | 1996-06-28 | 1999-10-12 | Trustees Of Tufts College | Multivalent compounds for crosslinking receptors and uses thereof |
US6011155A (en) * | 1996-11-07 | 2000-01-04 | Novartis Ag | N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
US6040145A (en) | 1997-05-07 | 2000-03-21 | Tufts University | Potentiation of the immune response |
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EP1062222A1 (en) * | 1998-03-09 | 2000-12-27 | Fondatech Benelux N.V. | Serine peptidase modulators |
EP1075266A1 (en) | 1998-05-04 | 2001-02-14 | Point Therapeutics, Inc. | Hematopoietic stimulation |
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DE19826972A1 (en) * | 1998-06-18 | 1999-12-23 | Univ Magdeburg Tech | Inhibiting keratinocyte activation and proliferation, for treatment of dermatological disorders such as psoriasis or actinic precancerous states |
DE19828113A1 (en) * | 1998-06-24 | 2000-01-05 | Probiodrug Ges Fuer Arzneim | Prodrugs of Dipeptidyl Peptidase IV Inhibitors |
US6979697B1 (en) | 1998-08-21 | 2005-12-27 | Point Therapeutics, Inc. | Regulation of substrate activity |
US20030176357A1 (en) * | 1998-10-06 | 2003-09-18 | Pospisilik Andrew J. | Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels |
CO5150173A1 (en) * | 1998-12-10 | 2002-04-29 | Novartis Ag | COMPOUNDS N- (REPLACED GLYCLE) -2-DIPEPTIDYL-IV PEPTIDASE INHIBITING CYANOPIRROLIDINS (DPP-IV) WHICH ARE EFFECTIVE IN THE TREATMENT OF CONDITIONS MEDIATED BY DPP-IV INHIBITION |
AU3511500A (en) | 1999-03-05 | 2000-09-21 | Trustees Of University Technology Corporation, The | Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions |
AU3731400A (en) | 1999-03-05 | 2000-09-21 | Trustees Of University Technology Corporation, The | Methods and compositions useful in inhibiting apoptosis |
US6849605B1 (en) | 1999-03-05 | 2005-02-01 | The Trustees Of University Technology Corporation | Inhibitors of serine protease activity, methods and compositions for treatment of viral infections |
US6890904B1 (en) * | 1999-05-25 | 2005-05-10 | Point Therapeutics, Inc. | Anti-tumor agents |
US6110949A (en) * | 1999-06-24 | 2000-08-29 | Novartis Ag | N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
US6172081B1 (en) | 1999-06-24 | 2001-01-09 | Novartis Ag | Tetrahydroisoquinoline 3-carboxamide derivatives |
US6617340B1 (en) | 1999-07-29 | 2003-09-09 | Novartis Ag | N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
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US6569684B2 (en) | 2000-01-06 | 2003-05-27 | University Of Central Florida | Method of identifying and treating invasive carcinomas |
US6277877B1 (en) | 2000-08-15 | 2001-08-21 | Pfizer, Inc. | Substituted n-(indole-2-carbonyl)glycinamides and derivates as glycogen phosphorylase inhibitors |
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US7524635B2 (en) * | 2003-04-17 | 2009-04-28 | Biosite Incorporated | Methods and compositions for measuring natriuretic peptides and uses thereof |
US20040176914A1 (en) * | 2001-04-13 | 2004-09-09 | Biosite Incorporated | Methods and compositions for measuring biologically active natriuretic peptides and for improving their therapeutic potential |
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US20060134774A1 (en) * | 2002-11-22 | 2006-06-22 | Marligen Biosciences, Inc. | Detection of protease enzymes |
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US20040229848A1 (en) * | 2003-05-05 | 2004-11-18 | Hans-Ulrich Demuth | Glutaminyl based DP IV-inhibitors |
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WO2004104216A2 (en) * | 2003-05-21 | 2004-12-02 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase iv (dpp4) |
DE10330842A1 (en) * | 2003-07-08 | 2005-02-10 | Institut für Medizintechnologie Magdeburg GmbH, IMTM | Use of the inhibitors of enzymes with activities of aminopeptidase N and / or dipeptidyl peptidase IV and pharmaceutical preparations thereof for the therapy and prevention of dermatological diseases with hyperproliferation and altered differentiation states of fibroblasts |
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US7169926B1 (en) | 2003-08-13 | 2007-01-30 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
CN1867560A (en) | 2003-08-13 | 2006-11-22 | 武田药品工株式会社 | 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors |
US7678909B1 (en) | 2003-08-13 | 2010-03-16 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
ES2622522T3 (en) | 2003-08-26 | 2017-07-06 | The Regents Of The University Of Colorado, A Body Corporate | Inhibitors of serine protease activity and its use in methods and compositions for the treatment of bacterial infections |
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US9115082B2 (en) | 2012-01-18 | 2015-08-25 | Catherine Yang | Dipeptidyl-peptidase-IV inhibitors for treatment of type 2 diabetes complex with hypertension |
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Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0356462A (en) * | 1989-07-24 | 1991-03-12 | Kissei Pharmaceut Co Ltd | Pyroglutamic acid derivative |
WO1993008259A2 (en) * | 1991-10-22 | 1993-04-29 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type iv |
WO1994029336A1 (en) * | 1993-06-03 | 1994-12-22 | Astra Aktiebolag | New peptide derivatives |
WO1995003278A1 (en) * | 1993-07-26 | 1995-02-02 | Zaidan Hojin Biseibutsu Kagaku Kenkyukai | Pyrrolidine derivative or pharmaceutically acceptable salt thereof |
WO1995015309A1 (en) * | 1993-12-03 | 1995-06-08 | Ferring B.V. | Dp-iv-serine protease inhibitors |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5686419A (en) * | 1994-01-21 | 1997-11-11 | Georgia Tech Research Corp. | Basic α-aminoalkylphosphonate derivatives |
US5543396A (en) * | 1994-04-28 | 1996-08-06 | Georgia Tech Research Corp. | Proline phosphonate derivatives |
US5681821A (en) * | 1994-10-18 | 1997-10-28 | Georgia Tech Research Corp. | Fluorescent 1-peptidylaminoalkanephosphonate derivatives |
-
1995
- 1995-06-09 EP EP95923301A patent/EP0764151A2/en not_active Withdrawn
- 1995-06-09 US US08/750,484 patent/US6090786A/en not_active Expired - Fee Related
- 1995-06-09 WO PCT/EP1995/002255 patent/WO1995034538A2/en not_active Application Discontinuation
- 1995-06-09 AU AU27908/95A patent/AU2790895A/en not_active Abandoned
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0356462A (en) * | 1989-07-24 | 1991-03-12 | Kissei Pharmaceut Co Ltd | Pyroglutamic acid derivative |
WO1993008259A2 (en) * | 1991-10-22 | 1993-04-29 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type iv |
WO1994029336A1 (en) * | 1993-06-03 | 1994-12-22 | Astra Aktiebolag | New peptide derivatives |
WO1995003278A1 (en) * | 1993-07-26 | 1995-02-02 | Zaidan Hojin Biseibutsu Kagaku Kenkyukai | Pyrrolidine derivative or pharmaceutically acceptable salt thereof |
WO1995015309A1 (en) * | 1993-12-03 | 1995-06-08 | Ferring B.V. | Dp-iv-serine protease inhibitors |
Non-Patent Citations (1)
Title |
---|
PATENT ABSTRACTS OF JAPAN vol. 15, no. 202 (C - 0834) 23 May 1991 (1991-05-23) * |
Also Published As
Publication number | Publication date |
---|---|
US6090786A (en) | 2000-07-18 |
EP0764151A2 (en) | 1997-03-26 |
AU2790895A (en) | 1996-01-05 |
WO1995034538A2 (en) | 1995-12-21 |
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