EP0724446A4 - Electrophilic peptide analogs as inhibitors of trypsin-like enzymes - Google Patents
Electrophilic peptide analogs as inhibitors of trypsin-like enzymesInfo
- 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- Withdrawn
Links
- 102000004190 Enzymes Human genes 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- 230000001810 trypsinlike Effects 0.000 title 1
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)
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)
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 |
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 |
US5705487A (en) * | 1994-03-04 | 1998-01-06 | 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. |
US5710130A (en) * | 1995-02-27 | 1998-01-20 | Eli Lilly And Company | Antithrombotic agents |
US5914319A (en) * | 1995-02-27 | 1999-06-22 | Eli Lilly And Company | Antithrombotic agents |
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 |
US6022861A (en) * | 1995-06-07 | 2000-02-08 | Cor Therapeutics, Inc. | Ketoheterocyclic 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 |
CA2285446A1 (en) * | 1997-03-13 | 1998-09-17 | Smithkline Beecham P.L.C. | 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 |
AU6371900A (en) * | 1999-07-26 | 2001-02-13 | Du Pont Pharmaceuticals Company | Lactam inhibitors of hepatitis c virus ns3 protease |
US20050288253A1 (en) | 2002-09-09 | 2005-12-29 | Trigen Limited | Boronic acid salts |
ES2264515T3 (en) * | 2002-09-09 | 2007-01-01 | Trigen Limited | BORONIC ACID SALTS USED IN PARENTERAL FORMULATIONS FOR THE SELECTIVE INHIBITION OF THE THROMBIN. |
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 |
ES2575131T3 (en) * | 2007-12-03 | 2016-06-24 | Obe Therapy Biotechnology | Enteropeptidase boropeptide inhibitors and their uses in treatments 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 |
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 |
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 |
NZ600786A (en) | 2009-12-22 | 2013-12-20 | Cephalon Inc | Proteasome inhibitors and processes for their preparation, purification and use |
US8809012B2 (en) | 2010-08-23 | 2014-08-19 | Postach Academy-Industry Foundation | Labeling agent and methods for simultaneous sequencing and quantification of multiple peptides and proteins using the same |
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 |
BR112014015363A2 (en) * | 2011-12-22 | 2017-06-13 | Ares Trading Sa | alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
MY186911A (en) | 2014-10-01 | 2021-08-26 | Merck Patent Gmbh | Boronic acid derivatives |
US10253049B2 (en) * | 2014-10-01 | 2019-04-09 | Merck Patent Gmbh | Boronic acid derivatives |
JP6835711B2 (en) * | 2014-10-01 | 2021-02-24 | 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 derivative |
BR112017006368A2 (en) | 2014-10-01 | 2017-12-19 | Merck Patent Gmbh | boronic acid derivatives |
WO2017222914A1 (en) | 2016-06-21 | 2017-12-28 | Inception 4, Inc. | Carbocyclic prolinamide derivatives |
HUE064412T2 (en) | 2016-06-21 | 2024-03-28 | Orion Ophthalmology LLC | Heterocyclic prolinamide derivatives |
ES2874638T3 (en) | 2017-01-18 | 2021-11-05 | Principia Biopharma Inc | Immunoproteosomal inhibitors |
JP7333321B2 (en) * | 2017-11-16 | 2023-08-24 | プリンシピア バイオファーマ インコーポレイテッド | immunoproteasome inhibitor |
EA202090900A1 (en) | 2017-11-16 | 2020-10-02 | Принсипиа Биофарма Инк. | IMMUNOPROTEASOM INHIBITORS |
Citations (6)
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)
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 |
-
1994
- 1994-10-05 IL IL11117594A patent/IL111175A0/en unknown
- 1994-10-06 CA CA002174314A patent/CA2174314C/en not_active Expired - Fee Related
- 1994-10-06 WO PCT/US1994/011280 patent/WO1995009634A1/en not_active Application Discontinuation
- 1994-10-06 AU AU79664/94A patent/AU7966494A/en not_active Abandoned
- 1994-10-06 EP EP94930595A patent/EP0724446A4/en not_active Withdrawn
Patent Citations (6)
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)
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 |
---|---|
AU7966494A (en) | 1995-05-01 |
CA2174314C (en) | 2000-04-11 |
IL111175A0 (en) | 1994-12-29 |
WO1995009634A1 (en) | 1995-04-13 |
EP0724446A1 (en) | 1996-08-07 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
17P | Request for examination filed |
Effective date: 19960328 |
|
AK | Designated contracting states |
Kind code of ref document: A1 Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE |
|
A4 | Supplementary search report drawn up and despatched |
Effective date: 19971121 |
|
AK | Designated contracting states |
Kind code of ref document: A4 Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE |
|
RHK1 | Main classification (correction) |
Ipc: C07K 5/06 |
|
RAP1 | Party data changed (applicant data changed or rights of an application transferred) |
Owner name: DUPONT PHARMACEUTICALS COMPANY |
|
RAP3 | Party data changed (applicant data changed or rights of an application transferred) |
Owner name: DUPONT PHARMACEUTICALS COMPANY |
|
17Q | First examination report despatched |
Effective date: 19991116 |
|
GRAG | Despatch of communication of intention to grant |
Free format text: ORIGINAL CODE: EPIDOS AGRA |
|
GRAG | Despatch of communication of intention to grant |
Free format text: ORIGINAL CODE: EPIDOS AGRA |
|
GRAH | Despatch of communication of intention to grant a patent |
Free format text: ORIGINAL CODE: EPIDOS IGRA |
|
STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN |
|
18D | Application deemed to be withdrawn |
Effective date: 20010710 |