ES2061480T3 - Ariloxi- y arilaciloxi-metilcetonas inhibidoras de tiol proteasas. - Google Patents

Ariloxi- y arilaciloxi-metilcetonas inhibidoras de tiol proteasas.

Info

Publication number
ES2061480T3
ES2061480T3 ES87118949T ES87118949T ES2061480T3 ES 2061480 T3 ES2061480 T3 ES 2061480T3 ES 87118949 T ES87118949 T ES 87118949T ES 87118949 T ES87118949 T ES 87118949T ES 2061480 T3 ES2061480 T3 ES 2061480T3
Authority
ES
Spain
Prior art keywords
methyl
kethones
arylaciloxi
aryloxy
thiol proteases
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.)
Expired - Lifetime
Application number
ES87118949T
Other languages
English (en)
Inventor
Alexander Krantz
Heinz W Pauls
Roger A Smith
Robin W Spencer
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.)
Sandoz AG
Original Assignee
Sandoz AG
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 Sandoz AG filed Critical Sandoz AG
Application granted granted Critical
Publication of ES2061480T3 publication Critical patent/ES2061480T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE PRESENTAN INHIBIDORES DE TIOLPROTEASA QUE TIENEN LA FORMULA (I) O UN ISOMERO OPTICO, O UNA SAL FARMACOLOGICAMENTE ACEPTABLE DE LOS MISMOS, DONDE N ES 0 O 1; M ES 0, 1 O 2, X ES H O UN GRUPO N-PROTECTOR, CADA Y ES, INDEPENDIENTEMENTE UN RESTO DE ALFA-AMINOACIDO OPCIONALMENTE PROTEGIDO, R ES UNA CADENA LATERAL DE ALFA-AMINOACIDO OPCIONALMENTE PROTEGIDO, QUE ES H O CH3, O QUE ESTA UNIDA AL ATOMO DE CARBONO ALFA CORRESPONDIENTE POR UN RADICAL METILENO, METILO O FENILO, Y R'' ES ARILO OPCIONALMENTE SUSTITUIDO.
ES87118949T 1986-12-22 1987-12-21 Ariloxi- y arilaciloxi-metilcetonas inhibidoras de tiol proteasas. Expired - Lifetime ES2061480T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US94673786A 1986-12-22 1986-12-22
US07/127,282 US5055451A (en) 1986-12-22 1987-12-07 Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors

Publications (1)

Publication Number Publication Date
ES2061480T3 true ES2061480T3 (es) 1994-12-16

Family

ID=26825501

Family Applications (1)

Application Number Title Priority Date Filing Date
ES87118949T Expired - Lifetime ES2061480T3 (es) 1986-12-22 1987-12-21 Ariloxi- y arilaciloxi-metilcetonas inhibidoras de tiol proteasas.

Country Status (11)

Country Link
US (1) US5055451A (es)
EP (1) EP0272671B1 (es)
JP (1) JPS63253061A (es)
AU (1) AU602547B2 (es)
CA (1) CA1329862C (es)
DE (1) DE3789371T2 (es)
DK (1) DK674387A (es)
ES (1) ES2061480T3 (es)
IE (1) IE62863B1 (es)
NZ (1) NZ223002A (es)
ZA (1) ZA879577B (es)

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US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
US6008217A (en) * 1995-12-20 1999-12-28 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5874424A (en) * 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US4937377A (en) * 1989-11-20 1990-06-26 Occidental Chemical Corporation Preparation of 3,4-difluorobenzoic acid by the decarboxylation of 4,5-difluorophthalic anhydride or 4,5-difluorophthalic acid
US5003103A (en) * 1989-11-20 1991-03-26 Occidental Chemical Corporation Preparation of 2-choloro-4,5-difluorobenzoic acid from 4,5-difluorophthalic anhydride of 4,5-difluorophthalic acid
US6995141B1 (en) 1990-04-04 2006-02-07 Vertex Pharmaceuticals Incorporated Interleukin 1β protease and interleukin 1β protease inhibitors
US5444042A (en) * 1990-12-28 1995-08-22 Cortex Pharmaceuticals Method of treatment of neurodegeneration with calpain inhibitors
DE69226820T2 (de) * 1991-06-21 1999-05-12 Merck & Co., Inc., Rahway, N.J. Peptidylderivate als Inhibitoren von Interleukin-1B-konvertierenden Enzymen
JP3228347B2 (ja) * 1991-06-25 2001-11-12 三菱化学株式会社 シクロプロペノン誘導体
JP3190431B2 (ja) * 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
US5217994A (en) * 1991-08-09 1993-06-08 Merck & Co., Inc. Method of inhibiting osteoclast-mediated bone resorption by administration of aminoalkyl-substituted phenyl derivatives
US5204350A (en) * 1991-08-09 1993-04-20 Merck & Co., Inc. Method of inhibiting osteoclast-mediated bone resorption by administration of n-heterocyclicalkyl-substituted phenyl derivatives
US6348570B1 (en) 1991-08-16 2002-02-19 Merck & Co., Inc. Chromophore containing compounds and their use in determining interleukin-1β convertase activity
JPH05140063A (ja) * 1991-11-19 1993-06-08 Suntory Ltd ジペプチド誘導体及びそれを有効成分とする骨疾患の予防及び治療剤
CA2129976C (en) * 1992-02-21 2002-09-17 Kevin T. Chapman Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme
US5317086A (en) * 1992-03-09 1994-05-31 The Regents Of The University Of California Cysteine proteinase inhibitors and inhibitor precursors
US5374623A (en) * 1992-08-20 1994-12-20 Prototek, Inc. Cysteine protease inhibitors effective for in vivo use
US5395958A (en) * 1992-09-30 1995-03-07 Mitsubishi Kasei Corporation Cyclopropene derivatives
US5260478A (en) * 1992-12-08 1993-11-09 Sterling Winthrop Inc. Iodinated aroyloxy carboxamides
CA2111930A1 (en) * 1992-12-25 1994-06-26 Ryoichi Ando Aminoketone derivatives
DK0603769T3 (da) * 1992-12-25 1999-06-14 Mitsubishi Chem Corp Alfa-aminoketonderivater
US5545672A (en) * 1993-02-11 1996-08-13 The University Of Texas System Treatment of insulin resistance and type 2 diabetes mellitus with a thiol protease inhibitor
US5985838A (en) 1993-04-29 1999-11-16 Vertex Pharmaceuticals, Inc. Peptide analogs as irreversible interleukin-1β protease inhibitors
CA2122227A1 (en) * 1993-04-29 1994-10-30 Roland E. Dolle Peptide analogs as irreversible interleukin-1.beta. protease inhibitors
US5462939A (en) * 1993-05-07 1995-10-31 Sterling Winthrop Inc. Peptidic ketones as interleukin-1β-converting enzyme inhibitors
JPH0789951A (ja) * 1993-06-03 1995-04-04 Sterling Winthrop Inc インターロイキン−１β転換酵素阻害剤
US5843905A (en) * 1993-06-04 1998-12-01 Vertex Pharmaceuticals, Incorporated Peptidic phosphinyloxymethyl ketones as interleukin-1β-converting enzyme inhibitors
DK0628550T3 (da) 1993-06-08 1998-09-28 Vertex Pharma Pyridazin som interleukin-1 beta-omdannede enzyminhibitorer
WO1995005192A1 (en) * 1993-08-13 1995-02-23 Merck & Co., Inc. SUBSTITUTED KETONE DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
US5714484A (en) * 1993-12-08 1998-02-03 Prototek, Inc. α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
US5486623A (en) * 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
IL112759A0 (en) * 1994-02-25 1995-05-26 Khepri Pharmaceuticals Inc Novel cysteine protease inhibitors
US5847135A (en) * 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) * 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5756466A (en) * 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5574017A (en) * 1994-07-05 1996-11-12 Gutheil; William G. Antibacterial agents
US5776718A (en) * 1995-03-24 1998-07-07 Arris Pharmaceutical Corporation Reversible protease inhibitors
US5798442A (en) * 1995-04-21 1998-08-25 Merck Frosst Canada, Inc. Peptidyl derivatives as inhibitors of pro-apoptotic cysteine proteinases
US5843904A (en) * 1995-12-20 1998-12-01 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1βconverting enzyme
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US5942601A (en) * 1997-11-21 1999-08-24 The Reagents Of The University Of California Peptide synthesis with sulfonyl protecting groups
JP4499917B2 (ja) 1998-03-09 2010-07-14 バーテックス ファーマシューティカルズ インコーポレイテッド インターロイキン−１β変換酵素のインヒビターとしての１，２−ジアゼパン誘導体
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EP4218829A3 (en) 2013-03-15 2023-08-16 The Board of Trustees of the Leland Stanford Junior University Activity-based probe compounds, compositions, and methods of use
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US4539312A (en) * 1984-07-11 1985-09-03 E. R. Squibb & Sons, Inc. Use of diamino ketones as analgesic agents
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Also Published As

Publication number Publication date
DE3789371D1 (de) 1994-04-21
NZ223002A (en) 1991-05-28
ZA879577B (en) 1989-08-30
IE873467L (en) 1988-06-22
CA1329862C (en) 1994-05-24
EP0272671A2 (en) 1988-06-29
US5055451A (en) 1991-10-08
DE3789371T2 (de) 1994-09-08
IE62863B1 (en) 1995-03-08
JPS63253061A (ja) 1988-10-20
EP0272671B1 (en) 1994-03-16
DK674387D0 (da) 1987-12-21
DK674387A (da) 1988-06-23
AU602547B2 (en) 1990-10-18
EP0272671A3 (en) 1990-06-13
AU8287187A (en) 1988-07-21

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