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Withdrawn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Withdrawn legal-status Critical Current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 Table
    • 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 Table
    • 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)
  • Biochemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (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 (49)

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IL109319A0 (en) * 1993-04-27 1994-07-31 Du Pont Merck Pharma Amidino and guanidino substituted boronic acid compounds
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
US5885967A (en) * 1994-03-04 1999-03-23 Eli Lilly And Company Antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
ZA951618B (en) * 1994-03-04 1996-08-27 Lilly Co Eli 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
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
US6046169A (en) * 1995-06-07 2000-04-04 Cor Therapeutics, Inc. Inhibitors of factor XA
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
US5721214A (en) * 1995-06-07 1998-02-24 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
EP0970062A2 (en) 1997-03-13 2000-01-12 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
AU6371900A (en) * 1999-07-26 2001-02-13 Du Pont Pharmaceuticals Company Lactam inhibitors of hepatitis c virus ns3 protease
US7122627B2 (en) 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
US20050288253A1 (en) 2002-09-09 2005-12-29 Trigen Limited Boronic acid salts
BR0314450A (en) * 2002-09-09 2005-07-26 Trigen Ltd Salts of boronic acid with the addition of a pharmaceutically acceptable base, pharmaceutical formulation, and use of said salts to prepare a pharmaceutical formulation.
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
HRP20160569T1 (en) * 2007-12-03 2016-07-29 Obe Therapy Biotechnology BOROPEPTIDE ENTEROPEPTIDASE INHIBITORS AND THEIR USES FOR THE TREATMENT OF OBSERVATION
US20210130285A1 (en) 2008-03-19 2021-05-06 Aurimmed Pharma, Inc. Novel compounds advantageous in the treatment of central nervous system diseases and disorders
US8228139B2 (en) * 2008-03-19 2012-07-24 Powerwave Technologies Sweden Ab Transmission line comprised of a center conductor on a printed circuit board disposed within a groove
RU2010142655A (en) * 2008-03-19 2012-04-27 Ауриммед Фарма, Инк. (Us) COMPOUND SUITABLE FOR TREATMENT OF DISEASES AND DISORDERS OF THE CENTRAL NERVOUS SYSTEM, AND METHOD FOR ITS OBTAINING
US10793515B2 (en) 2008-03-19 2020-10-06 Aurimmed Pharma, Inc. Compounds advantageous in the treatment of central nervous system diseases and disorders
AU2010341530B2 (en) 2009-12-22 2016-03-10 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
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
WO2012026743A2 (en) * 2010-08-23 2012-03-01 포항공과대학교 산학협력단 Labeling agent and amino acid sequence using same, and method for performing simultaneous quantitative analysis of multiple proteins
SG11201403254QA (en) * 2011-12-22 2014-07-30 Ares Trading Sa Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors
US10294246B2 (en) * 2014-10-01 2019-05-21 Merck Patent Gmbh Substituted boronic acids and boronate esters as immunoproteasome inhibitors
EP3201205B1 (en) * 2014-10-01 2020-05-13 Merck Patent GmbH Boronic acid derivatives
EP3201208B1 (en) * 2014-10-01 2021-03-24 Merck Patent GmbH Boronic acid derivatives
CN107001391B (en) 2014-10-01 2020-11-27 默克专利股份公司 Boronic acid derivatives
PL3472149T3 (en) 2016-06-21 2024-02-12 Orion Ophthalmology LLC Heterocyclic prolinamide derivatives
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
PT3571208T (en) 2017-01-18 2021-04-13 Principia Biopharma Inc Immunoproteasome inhibitors
EP3710458B1 (en) 2017-11-16 2026-03-25 Principia Biopharma Inc. Immunoproteasome inhibitors
ES2928787T3 (en) * 2017-11-16 2022-11-22 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
CA2174314C (en) 2000-04-11
AU7966494A (en) 1995-05-01
WO1995009634A1 (en) 1995-04-13
IL111175A0 (en) 1994-12-29
EP0724446A1 (en) 1996-08-07

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Owner name: DUPONT PHARMACEUTICALS COMPANY

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