EP0724446A4 - Electrophilic peptide analogs as inhibitors of trypsin-like enzymes - Google Patents

Electrophilic peptide analogs as inhibitors of trypsin-like enzymes

Info

Publication number
EP0724446A4
EP0724446A4 EP94930595A EP94930595A EP0724446A4 EP 0724446 A4 EP0724446 A4 EP 0724446A4 EP 94930595 A EP94930595 A EP 94930595A EP 94930595 A EP94930595 A EP 94930595A EP 0724446 A4 EP0724446 A4 EP 0724446A4
Authority
EP
European Patent Office
Prior art keywords
trypsin
enzymes
inhibitors
peptide analogs
electrophilic
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.)
Withdrawn
Application number
EP94930595A
Other languages
German (de)
French (fr)
Other versions
EP0724446A1 (en
Inventor
Robert Anthony Galemmo Jr
Matthew Mark Abelman
Eugene Cruz Amparo
John Matthew Fevig
Robert Madara Knabb
William Henry Miller
Gregory James Pacofsky
Patricia Carol Weber
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.)
Bristol Myers Squibb Pharma Co
Original Assignee
DuPont Merck Pharmaceutical Co
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
Application filed by DuPont Merck Pharmaceutical Co filed Critical DuPont Merck Pharmaceutical Co
Publication of EP0724446A1 publication Critical patent/EP0724446A1/en
Publication of EP0724446A4 publication Critical patent/EP0724446A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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 System
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/50—Organo-phosphines
    • C07F9/53—Organo-phosphine oxides; Organo-phosphine thioxides
    • C07F9/5325—Aromatic phosphine oxides or thioxides (P-C aromatic linkage)
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP94930595A 1993-10-07 1994-10-06 Electrophilic peptide analogs as inhibitors of trypsin-like enzymes Withdrawn EP0724446A4 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US13325193A 1993-10-07 1993-10-07
US133251 1993-10-07
US13944593A 1993-10-20 1993-10-20
US139445 1993-10-20
PCT/US1994/011280 WO1995009634A1 (en) 1993-10-07 1994-10-06 Electrophilic peptide analogs as inhibitors of trypsin-like enzymes

Publications (2)

Publication Number Publication Date
EP0724446A1 EP0724446A1 (en) 1996-08-07
EP0724446A4 true EP0724446A4 (en) 1998-01-07

Family

ID=26831202

Family Applications (1)

Application Number Title Priority Date Filing Date
EP94930595A Withdrawn EP0724446A4 (en) 1993-10-07 1994-10-06 Electrophilic peptide analogs as inhibitors of trypsin-like enzymes

Country Status (5)

Country Link
EP (1) EP0724446A4 (en)
AU (1) AU7966494A (en)
CA (1) CA2174314C (en)
IL (1) IL111175A0 (en)
WO (1) WO1995009634A1 (en)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL109319A0 (en) * 1993-04-27 1994-07-31 Du Pont Merck Pharma Amidino and guanidino substituted boronic acid compounds
ZA951618B (en) * 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5885967A (en) * 1994-03-04 1999-03-23 Eli Lilly And Company Antithrombotic agents
CA2143533A1 (en) * 1994-03-04 1995-09-05 Kenneth D. Kurz Antithrombotic agents
US5602101A (en) * 1994-03-04 1997-02-11 Eli Lilly And Company Antithrombotic agents
FR2721611B1 (en) * 1994-06-22 1996-09-27 Adir New peptide derivatives of boronic acid, their process of preparation and the pharmaceutical compositions which contain them.
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
US6022861A (en) * 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6069130A (en) * 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
US5721214A (en) * 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
US6046169A (en) * 1995-06-07 2000-04-04 Cor Therapeutics, Inc. Inhibitors of factor XA
US6211154B1 (en) 1995-06-07 2001-04-03 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5952306A (en) * 1996-01-16 1999-09-14 Merck & Co., Inc. Integrin receptor antagonists
US6245743B1 (en) 1996-06-05 2001-06-12 Cor Therapeutics, Inc. Inhibitors of factor Xa
WO1998040056A2 (en) * 1997-03-13 1998-09-17 Smithkline Beecham Plc Pyrrolidine and thiazole derivatives with metallo-beta-lactamase inhibitory properties
US6294549B1 (en) 1997-07-23 2001-09-25 Merck & Co., Inc. Method for eliciting an αvβ5 or dual αvβ3/αvβ5 antagonizing effect
US7122627B2 (en) 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
WO2001007407A1 (en) * 1999-07-26 2001-02-01 Bristol-Myers Squibb Pharma Company Lactam inhibitors of hepatitis c virus ns3 protease
JP2006509034A (en) 2002-09-09 2006-03-16 トライジェン・リミテッド Boronates useful in parenteral formulations for selective thrombin inhibition
US20050288253A1 (en) 2002-09-09 2005-12-29 Trigen Limited Boronic acid salts
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7223745B2 (en) 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7417040B2 (en) 2004-03-01 2008-08-26 Bristol-Myers Squibb Company Fused tricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7727978B2 (en) 2006-08-24 2010-06-01 Bristol-Myers Squibb Company Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
HUE028064T2 (en) * 2007-12-03 2016-11-28 Obe Therapy Biotechnology Boropeptide inhibitors of enteropeptidase and their uses in treatment of obesity, overweight and/or diseases associated with an abnormal fat metabolism
AU2009225647C1 (en) * 2008-03-19 2015-11-19 Aurimmed Pharma, Inc. Novel compounds advantageous in the treatment of central nervous system diseases and disorders
US10793515B2 (en) 2008-03-19 2020-10-06 Aurimmed Pharma, Inc. Compounds advantageous in the treatment of central nervous system diseases and disorders
SG188916A1 (en) * 2008-03-19 2013-04-30 Aurimmed Pharma Inc Novel compounds advantageous in the treatment of central nervous system diseases and disorders
CN102725300B (en) 2009-12-22 2015-03-11 赛福伦公司 Proteasome inhibitors and processes for their preparation, purification and use
EP2610243A4 (en) * 2010-08-23 2014-04-02 Postech Acad Ind Found Labeling agent and amino acid sequence using same, and method for performing simultaneous quantitative analysis of multiple proteins
KR101207742B1 (en) * 2010-10-14 2012-12-03 포항공과대학교 산학협력단 Labeling reagent and analytical methods for simultaneous peptide sequencing and multiplexed protein quantification using thereof
EP2793900B1 (en) 2011-12-22 2018-08-22 Ares Trading S.A. Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors
MX2017004043A (en) * 2014-10-01 2017-07-04 Merck Patent Gmbh Boronic acid derivatives.
AU2015327346B2 (en) * 2014-10-01 2019-12-05 Merck Patent Gmbh Boronic acid derivatives
KR102457840B1 (en) * 2014-10-01 2022-10-21 메르크 파텐트 게엠베하 Boronic acid derivatives
CA2963186A1 (en) * 2014-10-01 2016-04-07 Merck Patent Gmbh Boronic acid derivatives
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
AU2017282651B2 (en) 2016-06-21 2021-08-12 Orion Ophthalmology LLC Heterocyclic prolinamide derivatives
KR102534947B1 (en) 2017-01-18 2023-05-23 프린시피아 바이오파마, 인코퍼레이티드 immunoproteasome inhibitors
NZ764393A (en) 2017-11-16 2023-11-24 Principia Biopharma Inc Immunoproteasome inhibitors
WO2019099576A1 (en) * 2017-11-16 2019-05-23 Principia Biopharma Inc. Immunoproteasome inhibitors

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0293881A2 (en) * 1987-06-05 1988-12-07 The Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
EP0471651A2 (en) * 1990-08-13 1992-02-19 Sandoz Ltd. Peptide boronic acid derivatives having protease inhibiting activity
WO1992007869A1 (en) * 1990-11-06 1992-05-14 Thrombosis Research Institute Inhibitors and substrates of thrombin
EP0504064A1 (en) * 1991-03-15 1992-09-16 Merrell Pharmaceuticals Inc. Novel thrombin inhibitors
WO1994021650A1 (en) * 1993-03-24 1994-09-29 The Du Pont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
WO1994025049A1 (en) * 1993-04-27 1994-11-10 The Du Pont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4537773A (en) * 1983-12-05 1985-08-27 E. I. Du Pont De Nemours And Company α-Aminoboronic acid derivatives
EP0315574A3 (en) * 1987-11-05 1990-08-22 Hoechst Aktiengesellschaft Renin inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0293881A2 (en) * 1987-06-05 1988-12-07 The Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
EP0471651A2 (en) * 1990-08-13 1992-02-19 Sandoz Ltd. Peptide boronic acid derivatives having protease inhibiting activity
WO1992007869A1 (en) * 1990-11-06 1992-05-14 Thrombosis Research Institute Inhibitors and substrates of thrombin
EP0504064A1 (en) * 1991-03-15 1992-09-16 Merrell Pharmaceuticals Inc. Novel thrombin inhibitors
WO1994021650A1 (en) * 1993-03-24 1994-09-29 The Du Pont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
WO1994025049A1 (en) * 1993-04-27 1994-11-10 The Du Pont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CLAESON G ET AL: "NOVEL PEPTIDE MIMETICS AS HIGHLY EFFICIENT INHIBITORS OF THROMBIN BASED ON MODIFIED D-PHE-PRO-ARG SEQUENCES", AMERICAN PEPTIDE SYMPOSIUM, 1992, pages 824/825, XP000609384 *
ELGENDY S ET AL: "NEW PEPTIDE BORONIC ACID INHIBITORS OF THROMBIN", TETRAHEDRON LETTERS, vol. 33, no. 29, 14 July 1992 (1992-07-14), pages 4209 - 4212, XP000609104 *
MATTESON, D.S.: "(R)-1-acetamido-2-phenylethaneboronic acid", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY., vol. 103, 1981, DC US, pages 5241 - 5242, XP000609113 *
See also references of WO9509634A1 *

Also Published As

Publication number Publication date
WO1995009634A1 (en) 1995-04-13
AU7966494A (en) 1995-05-01
IL111175A0 (en) 1994-12-29
EP0724446A1 (en) 1996-08-07
CA2174314C (en) 2000-04-11

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RAP1 Party data changed (applicant data changed or rights of an application transferred)

Owner name: DUPONT PHARMACEUTICALS COMPANY

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