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EP0724446A4 - Analogues peptidiques electrophiles servant d'inhibiteurs a des enzymes apparentees a la trypsine - Google Patents

Analogues peptidiques electrophiles servant d'inhibiteurs a des enzymes apparentees a la trypsine

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Withdrawn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)
English (en)
Other versions
EP0724446A1 (fr
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/fr
Publication of EP0724446A4 publication Critical patent/EP0724446A4/fr
Withdrawn legal-status Critical Current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)
  • 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 Analogues peptidiques electrophiles servant d'inhibiteurs a des enzymes apparentees a la trypsine Withdrawn EP0724446A4 (fr)

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 (fr) 1993-10-07 1994-10-06 Analogues peptidiques electrophiles servant d'inhibiteurs a des enzymes apparentees a la trypsine

Publications (2)

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

Family

ID=26831202

Family Applications (1)

Application Number Title Priority Date Filing Date
EP94930595A Withdrawn EP0724446A4 (fr) 1993-10-07 1994-10-06 Analogues peptidiques electrophiles servant d'inhibiteurs a des enzymes apparentees a la trypsine

Country Status (5)

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

Families Citing this family (48)

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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
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
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
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5602101A (en) * 1994-03-04 1997-02-11 Eli Lilly And Company Antithrombotic agents
CA2143533A1 (fr) * 1994-03-04 1995-09-05 Kenneth D. Kurz Agents antithrombotiques
FR2721611B1 (fr) * 1994-06-22 1996-09-27 Adir Nouveaux dérivés peptidiques de l'acide boronique, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent .
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
US6211154B1 (en) 1995-06-07 2001-04-03 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6022861A (en) * 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
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
US5721214A (en) * 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
US6069130A (en) 1995-06-07 2000-05-30 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
JP2001524074A (ja) 1997-03-13 2001-11-27 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 金属−β−ラクタマーゼ阻害特性を有するピロリジンおよびチアゾール誘導体
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
CA2376961A1 (fr) * 1999-07-26 2001-02-01 Bristol-Myers Squibb Pharma Company Inhibiteurs lactame de la protease ns3 du virus de l'hepatite c
MXPA05002662A (es) * 2002-09-09 2005-09-20 Trigen Ltd Sales de metal multivalente de acidos boronicos para el tratamiento de trombosis.
US7112572B2 (en) 2002-09-09 2006-09-26 Trigen Limited Multivalent metal salts of boronic acids
US7223745B2 (en) 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7576206B2 (en) 2003-08-14 2009-08-18 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
WO2009071601A1 (fr) * 2007-12-03 2009-06-11 Obe Therapy Biotechnology Inhibiteurs boropeptidiques de l'entérokinase et leurs utilisations dans le traitement de l'obésité, de la surcharge pondérale et/ou des maladies associées avec un métabolisme anormal des lipides
RU2010142655A (ru) * 2008-03-19 2012-04-27 Ауриммед Фарма, Инк. (Us) Соединение, пригодное для лечения болезней и нарушений центральной нервной системы, и способ его получения
CN104710327B (zh) * 2008-03-19 2018-09-07 奥里梅德制药公司 有益于治疗中枢神经系统疾病和病症的化合物
US10793515B2 (en) 2008-03-19 2020-10-06 Aurimmed Pharma, Inc. Compounds advantageous in the treatment of central nervous system diseases and disorders
EP2516449A1 (fr) 2009-12-22 2012-10-31 Cephalon, Inc. Inhibiteurs du protéasome et leurs procédés de préparation, d'épuration et d'utilisation
KR101207742B1 (ko) * 2010-10-14 2012-12-03 포항공과대학교 산학협력단 라벨링제 및 이를 이용한 아미노산 서열 및 단백질 다중 정량 동시 분석방법
WO2012026743A2 (fr) * 2010-08-23 2012-03-01 포항공과대학교 산학협력단 Agent de marquage et séquence d'acides aminés l'utilisant, et procédé pour réaliser une analyse quantitative simultanée de multiples protéines
EP2793900B1 (fr) * 2011-12-22 2018-08-22 Ares Trading S.A. Dérivés d'acide boronique alpha-aminé, inhibiteurs selectives d'immunoproteasomes
BR112017006349A2 (pt) * 2014-10-01 2017-12-12 Merck Patent Gmbh derivados de ácido borônico
CA2963203A1 (fr) * 2014-10-01 2016-04-07 Merck Patent Gmbh Derives d'acide boronique
WO2016050359A1 (fr) * 2014-10-01 2016-04-07 Merck Patent Gmbh Dérivés d'acide boronique
SG11201702625PA (en) * 2014-10-01 2017-04-27 Merck Patent Gmbh Boronic acid derivatives
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
UA124672C2 (uk) 2016-06-21 2021-10-27 Оріон Офтальмолоджі Ллс Гетероциклічні похідні пролінаміду
RS61811B1 (sr) 2017-01-18 2021-06-30 Principia Biopharma Inc Inhibitori imunoproteazoma
WO2019099582A1 (fr) 2017-11-16 2019-05-23 Principia Biopharma Inc. Inhibiteurs d'immunoprotéasome
AU2018369787B2 (en) * 2017-11-16 2023-04-20 Principia Biopharma Inc. Immunoproteasome inhibitors

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0293881A2 (fr) * 1987-06-05 1988-12-07 The Du Pont Merck Pharmaceutical Company Inhibiteurs peptides de l'acide boronique de proteases de type trypsine
EP0471651A2 (fr) * 1990-08-13 1992-02-19 Sandoz Ltd. Dérivés de l'acide boronique peptidique ayant une activité inhibante de protéase
WO1992007869A1 (fr) * 1990-11-06 1992-05-14 Thrombosis Research Institute Inhibiteurs et substrats de thrombine
EP0504064A1 (fr) * 1991-03-15 1992-09-16 Merrell Pharmaceuticals Inc. Nouveaux inhibiteurs de la thrombine
WO1994021650A1 (fr) * 1993-03-24 1994-09-29 The Du Pont Merck Pharmaceutical Company Acide boronique et ester inhibiteurs de la thrombine
WO1994025049A1 (fr) * 1993-04-27 1994-11-10 The Du Pont Merck Pharmaceutical Company Acide boronique a substitution amidino et guanidino en tant qu'inhibiteur d'enzymes de type trypsine

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 (fr) * 1987-11-05 1990-08-22 Hoechst Aktiengesellschaft Inhibiteurs de la rénine

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0293881A2 (fr) * 1987-06-05 1988-12-07 The Du Pont Merck Pharmaceutical Company Inhibiteurs peptides de l'acide boronique de proteases de type trypsine
EP0471651A2 (fr) * 1990-08-13 1992-02-19 Sandoz Ltd. Dérivés de l'acide boronique peptidique ayant une activité inhibante de protéase
WO1992007869A1 (fr) * 1990-11-06 1992-05-14 Thrombosis Research Institute Inhibiteurs et substrats de thrombine
EP0504064A1 (fr) * 1991-03-15 1992-09-16 Merrell Pharmaceuticals Inc. Nouveaux inhibiteurs de la thrombine
WO1994021650A1 (fr) * 1993-03-24 1994-09-29 The Du Pont Merck Pharmaceutical Company Acide boronique et ester inhibiteurs de la thrombine
WO1994025049A1 (fr) * 1993-04-27 1994-11-10 The Du Pont Merck Pharmaceutical Company Acide boronique a substitution amidino et guanidino en tant qu'inhibiteur d'enzymes de type trypsine

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
IL111175A0 (en) 1994-12-29
EP0724446A1 (fr) 1996-08-07
AU7966494A (en) 1995-05-01
WO1995009634A1 (fr) 1995-04-13
CA2174314C (fr) 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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