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DK674387A - Proteaseinhibitorer - Google Patents

Proteaseinhibitorer

Info

Publication number
DK674387A
DK674387A DK674387A DK674387A DK674387A DK 674387 A DK674387 A DK 674387A DK 674387 A DK674387 A DK 674387A DK 674387 A DK674387 A DK 674387A DK 674387 A DK674387 A DK 674387A
Authority
DK
Denmark
Prior art keywords
protease inhibitors
protease
inhibitors
Prior art date
Application number
DK674387A
Other languages
English (en)
Other versions
DK674387D0 (da
Inventor
Alexander Krantz
Heinz W Pauls
Roger Astbury Smith
Robin Whitney Spencer
Original Assignee
Syntex Inc
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 Syntex Inc filed Critical Syntex Inc
Publication of DK674387D0 publication Critical patent/DK674387D0/da
Publication of DK674387A publication Critical patent/DK674387A/da

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)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
DK674387A 1986-12-22 1987-12-21 Proteaseinhibitorer DK674387A (da)

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 (2)

Publication Number Publication Date
DK674387D0 DK674387D0 (da) 1987-12-21
DK674387A true DK674387A (da) 1988-06-23

Family

ID=26825501

Family Applications (1)

Application Number Title Priority Date Filing Date
DK674387A DK674387A (da) 1986-12-22 1987-12-21 Proteaseinhibitorer

Country Status (11)

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

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
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
CA2071674C (en) * 1991-06-21 2003-08-19 Kevin T. Chapman Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme
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
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
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
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
JP3386125B2 (ja) * 1992-02-21 2003-03-17 メルク エンド カンパニー インコーポレーテッド インターロイキン−１β変換酵素阻害剤としてのペプチジル誘導体
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
DE69321087T2 (de) * 1992-12-25 1999-05-20 Mitsubishi Chemical Corp., Tokio/Tokyo Alpha-aminoketon Derivate
CA2111930A1 (en) * 1992-12-25 1994-06-26 Ryoichi Ando Aminoketone derivatives
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
CA2122227A1 (en) * 1993-04-29 1994-10-30 Roland E. Dolle Peptide analogs as irreversible interleukin-1.beta. protease inhibitors
US5985838A (en) * 1993-04-29 1999-11-16 Vertex Pharmaceuticals, Inc. Peptide analogs as irreversible interleukin-1β 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
US5866545A (en) * 1993-08-13 1999-02-02 Merck & Co., Inc. Substituted ketone derivatives as inhibitors of interleukin-1β converting enzyme
US5486623A (en) * 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
US5714484A (en) * 1993-12-08 1998-02-03 Prototek, Inc. α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
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
US5756466A (en) * 1994-06-17 1998-05-26 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
US5716929A (en) * 1994-06-17 1998-02-10 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
AU3359697A (en) * 1996-07-08 1998-02-02 Yamanouchi Pharmaceutical Co., Ltd. Bone resorption inhibitors
WO1998008802A1 (en) * 1996-08-28 1998-03-05 Smithkline Beecham Corporation Inhibitors of cysteine protease
US5942601A (en) * 1997-11-21 1999-08-24 The Reagents Of The University Of California Peptide synthesis with sulfonyl protecting groups
EP1062210B1 (en) 1998-03-09 2005-06-01 Vertex Pharmaceuticals Incorporated 1,2-diazepane derivatives as interleukin-1beta converting enzyme inhibitors
EP2261232A3 (en) * 1998-03-19 2011-04-20 Vertex Pharmaceuticals Incorporated Inhibitors of caspases
JP2003524603A (ja) * 1998-10-06 2003-08-19 スミスクライン・ビーチャム・コーポレイション カスパーゼおよびアポトーシス
WO2000027418A2 (en) * 1998-11-12 2000-05-18 Research Corporation Technologies, Inc. A method for treating tissue damaged from ischemia
JP2002537293A (ja) * 1999-02-20 2002-11-05 アストラゼネカ アクチボラグ カテプシンｌおよび／またはカテプシンｓの阻害剤としてのアセタミドアセトニトリル誘導体
US6506733B1 (en) 1999-03-15 2003-01-14 Axys Pharmaceuticals, Inc. Compounds and compositions as protease inhibitors
PE20011350A1 (es) * 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
WO2002051983A2 (en) 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
KR20040044920A (ko) 2001-09-14 2004-05-31 아벤티스 파마슈티칼스 인크. 카뎁신 억제제로서 신규한 화합물 및 조성물
CA2467391A1 (en) 2001-11-14 2003-05-22 Aventis Pharmaceuticals Inc. Oligopeptides and compositions containing them as cathepsin s inhibitors
WO2003068242A1 (en) * 2002-02-11 2003-08-21 Vertex Pharmaceuticals Incorporated Phospholipids as caspase inhibitor prodrugs
JP2008500374A (ja) * 2004-05-27 2008-01-10 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 自己炎症性疾患の処置のためのｉｃｅインヒビター
CA2575928A1 (en) * 2004-08-02 2006-02-09 Genmedica Therapeutics Sl Compounds for inhibiting copper-containing amine oxidases and uses thereof
WO2014145257A2 (en) * 2013-03-15 2014-09-18 The Board Of Trustees Of The Leland Stanford Junior University Activity-based probe compounds, compositions, and methods of use
CN111349053A (zh) 2014-10-06 2020-06-30 库特克希米公司 赖氨酸牙龈卟啉菌蛋白酶的抑制剂
WO2017083433A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
CA3036862A1 (en) 2016-09-16 2018-03-22 Cortexyme, Inc. Ketone inhibitors of lysine gingipain
WO2018119476A1 (en) 2016-12-23 2018-06-28 The Board Of Trustees Of The Leland Stanford Junior University Activity-based probe compounds, compositions, and methods of use
EP3601261A4 (en) 2017-03-30 2021-07-14 The Board of Trustees of the Leland Stanford Junior University PROTEASE-ACTIVATED CONTRAST AGENTS FOR IN-VIVO IMAGING
KR20240035454A (ko) * 2021-06-11 2024-03-15 더 스크립스 리서치 인스티튜트 코로나바이러스 감염 치료용 프로테아제 억제제들

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4692552A (en) * 1983-05-09 1987-09-08 G. D. Searle & Co. Protease inhibitors
US4539312A (en) * 1984-07-11 1985-09-03 E. R. Squibb & Sons, Inc. Use of diamino ketones as analgesic agents
US4636492A (en) * 1984-08-29 1987-01-13 E. I. Du Pont De Nemours And Company Inhibition of viral protease activity by peptide halomethyl ketones
US4652552A (en) * 1984-09-10 1987-03-24 E. I. Du Pont De Nemours And Company Tetrapeptide methyl ketone inhibitors of viral proteases
CA1341029C (en) * 1985-02-04 2000-06-20 Michael Kolb Peptidase inhibitors
US4820691A (en) * 1987-06-24 1989-04-11 E. R. Squibb & Sons, Inc. Amino acid 1,2-diketo derivatives as renin inhibitors

Also Published As

Publication number Publication date
DE3789371D1 (de) 1994-04-21
EP0272671A3 (en) 1990-06-13
AU8287187A (en) 1988-07-21
AU602547B2 (en) 1990-10-18
EP0272671A2 (en) 1988-06-29
US5055451A (en) 1991-10-08
ES2061480T3 (es) 1994-12-16
JPS63253061A (ja) 1988-10-20
IE62863B1 (en) 1995-03-08
ZA879577B (en) 1989-08-30
EP0272671B1 (en) 1994-03-16
DK674387D0 (da) 1987-12-21
IE873467L (en) 1988-06-22
NZ223002A (en) 1991-05-28
DE3789371T2 (de) 1994-09-08
CA1329862C (en) 1994-05-24

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Legal Events

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AHB Application shelved due to non-payment