IL111175A0 - Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them - Google Patents

Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them

Info

Publication number
IL111175A0
IL111175A0 IL11117594A IL11117594A IL111175A0 IL 111175 A0 IL111175 A0 IL 111175A0 IL 11117594 A IL11117594 A IL 11117594A IL 11117594 A IL11117594 A IL 11117594A IL 111175 A0 IL111175 A0 IL 111175A0
Authority
IL
Israel
Prior art keywords
trypsin
inhibitors
pharmaceutical compositions
compositions containing
serine proteases
Prior art date
Application number
IL11117594A
Original Assignee
Du Pont Merck Pharma
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 Du Pont Merck Pharma filed Critical Du Pont Merck Pharma
Publication of IL111175A0 publication Critical patent/IL111175A0/en

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)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
IL11117594A 1993-10-07 1994-10-05 Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them IL111175A0 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13325193A 1993-10-07 1993-10-07
US13944593A 1993-10-20 1993-10-20

Publications (1)

Publication Number Publication Date
IL111175A0 true IL111175A0 (en) 1994-12-29

Family

ID=26831202

Family Applications (1)

Application Number Title Priority Date Filing Date
IL11117594A IL111175A0 (en) 1993-10-07 1994-10-05 Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them

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
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5885967A (en) * 1994-03-04 1999-03-23 Eli Lilly And Company Antithrombotic agents
ZA951618B (en) * 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5602101A (en) * 1994-03-04 1997-02-11 Eli Lilly And Company Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
CA2143533A1 (en) * 1994-03-04 1995-09-05 Kenneth D. Kurz 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
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6211154B1 (en) 1995-06-07 2001-04-03 Cor Therapeutics, Inc. Ketoheterocyclic 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
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
EP1206449A1 (en) * 1999-07-26 2002-05-22 Bristol-Myers Squibb Company Lactam inhibitors of hepatitis c virus ns3 protease
US7371729B2 (en) 2002-09-09 2008-05-13 Trigen Limited Boronic acid salts useful in parenteral formulations
PT1396270E (en) * 2002-09-09 2006-08-31 Trigen Ltd PROCESS FOR THE PREPARATION OF UTEISNCOMO INTERMEDIATE COMPOUNDS.
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 (en) * 2007-12-03 2009-06-11 Obe Therapy Biotechnology Boropeptide inhibitors of enteropeptidase and their uses in treatment of obesity, overweight and/or diseases associated with an abnormal fat metabolism
US10793515B2 (en) 2008-03-19 2020-10-06 Aurimmed Pharma, Inc. Compounds advantageous in the treatment of central nervous system diseases and disorders
MX2010010233A (en) * 2008-03-19 2011-03-15 Aurimmed Pharma Inc Star Novel compounds advantageous in the treatment of central nervous system diseases and disorders.
US9206143B2 (en) * 2008-03-19 2015-12-08 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
CN103228621B (en) * 2010-08-23 2016-06-15 浦项工科大学校产学协力团 Labelled reagent and utilize its polypeptide and the order-checking of albumen and quantivative approach
EP2793900B1 (en) * 2011-12-22 2018-08-22 Ares Trading S.A. Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors
BR112017006349A2 (en) * 2014-10-01 2017-12-12 Merck Patent Gmbh boronic acid derivatives
JP6662865B2 (en) * 2014-10-01 2020-03-11 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Boronic acid derivatives
EP3201207B1 (en) * 2014-10-01 2021-02-24 Merck Patent GmbH Boronic acid derivatives
MX2017004037A (en) 2014-10-01 2017-07-04 Merck Patent Gmbh Boronic acid derivatives.
JP7164521B2 (en) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー carbocyclic prolinamide derivatives
CN114685453A (en) 2016-06-21 2022-07-01 奥瑞恩眼科有限责任公司 Heterocyclic prolinamide derivatives
AU2018210839B2 (en) 2017-01-18 2022-01-20 Principia Biopharma Inc. Immunoproteasome inhibitors
CA3080949C (en) 2017-11-16 2024-04-16 Principia Biopharma Inc. Immunoproteasome inhibitors
HRP20221292T1 (en) * 2017-11-16 2022-12-23 Principia Biopharma Inc. Immunoproteasome inhibitors

Family Cites Families (8)

* 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
US5187157A (en) * 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
EP0315574A3 (en) * 1987-11-05 1990-08-22 Hoechst Aktiengesellschaft Renin inhibitors
GB9017694D0 (en) * 1990-08-13 1990-09-26 Sandoz Ltd Improvements in or relating to organic chemistry
GB9024129D0 (en) * 1990-11-06 1990-12-19 Thrombosis Research Trust Inhibitors and substrates of thrombin
EP0503203A1 (en) * 1991-03-15 1992-09-16 Merrell Dow 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
IL109319A0 (en) * 1993-04-27 1994-07-31 Du Pont Merck Pharma Amidino and guanidino substituted boronic acid compounds

Also Published As

Publication number Publication date
EP0724446A1 (en) 1996-08-07
CA2174314C (en) 2000-04-11
EP0724446A4 (en) 1998-01-07
AU7966494A (en) 1995-05-01
WO1995009634A1 (en) 1995-04-13

Similar Documents

Publication Publication Date Title
IL111175A0 (en) Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them
HUP9900964A3 (en) Protease inhibitors and pharmaceutical compositions containing these compounds
IL129407A0 (en) Inhibitors of serine proteases particularly hepatitis C virus NS3 protease pharmaceutical compositions containing the same and the use thereof
HUP0103806A3 (en) Serine protease inhibitor and pharmaceutical compositions containing them
IL99163A0 (en) Inhibitors for serine proteases,their preparation and pharmaceutical compositions containing them
HUP0100669A3 (en) Peptide derivatives as serine protease inhibitors, their use and pharmaceutical compositions comprising thereof
NZ243675A (en) Isosteric peptide inhibitor of thrombin and pharmaceutical compositions
IL86613A0 (en) Peptide boronic acid derivatives and compositions containing them for inhibiting trypsin-like proteases
IL109867A0 (en) alpha-heteroaryloxymethyl ketones as interleukin -1beta protease inhibitors and pharmaceutical compositions containing them
IL120311A0 (en) Serine protease inhibitors and pharmaceutical compositions containing them
IL111176A0 (en) Dipeptide boronic acid inhibitors of trypsin-like enzymes and pharmaceutical compositions containing them
HUP0200503A2 (en) N-cyanomethyl amides as protease inhibitors and pharmaceutical compositions containing them
PL314838A1 (en) Inhibitors of bp-iv-serine protease
IL109503A0 (en) Hiv protease inhibitors and pharmaceutical compositions containing them
HUP0001796A3 (en) Dipeptide benzamidine as a kininogenase inhibitor and pharmaceutical compositions containing them
HUP9702035A3 (en) Inhibitors of leukocita-adhesion- and vla-4-antagonists and pharmaceutical compositions containing them
HUP9702036A3 (en) Inhibitors of leucocita-adhesion and wla-4-antagonists and pharmaceutical compositions containing them
IL128378A0 (en) Inhibitors of cysteine protease
IL120310A0 (en) Serine protease inhibitors and pharmaceutical compositions containing them
HUP0201479A2 (en) Novel macrocyclic compounds as metalloprotease inhibitors and pharmaceutical compositions containing them
HUP0002951A3 (en) Bis-aminomethylcarbonyl compounds as protease inhibitors and pharmaceutical compositions containing them
HU9602886D0 (en) Methods of prouducing effective recombinant serine protease inhibitors and uses of these inhibitors
HUP9902256A3 (en) Amidino protease inhibitors and pharmaceutical compositions containing them
EP0923535A4 (en) Inhibitors of cysteine protease
IL92671A0 (en) Pharmaceutical compositions containing peptide isosteres as retroviral protease inhibitors