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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters 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
    • C07C271/22Esters 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (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)
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
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US5874424A (en) * 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US6008217A (en) * 1995-12-20 1999-12-28 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US6204261B1 (en) * 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
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
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
ATE171171T1 (de) * 1992-12-25 1998-10-15 Mitsubishi Chem Corp 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
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
ES2114654T3 (es) * 1993-06-08 1998-06-01 Vertex Pharma Piridazinas como inhibidores de la enzima de conversion de la interleuquina-1beta.
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
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
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
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
WO1998001133A1 (en) * 1996-07-08 1998-01-15 Yamanouchi Pharmaceutical Co., Ltd. Bone resorption inhibitors
JP2000517319A (ja) * 1996-08-28 2000-12-26 スミスクライン・ビーチャム・コーポレイション システインプロテアーゼのインヒビター
US5942601A (en) * 1997-11-21 1999-08-24 The Reagents Of The University Of California Peptide synthesis with sulfonyl protecting groups
WO1999046248A1 (en) 1998-03-09 1999-09-16 Vertex Pharmaceuticals Incorporated 1,2-diazepane derivatives as interleukin-1beta converting enzyme inhibitors
CA2324226C (en) 1998-03-19 2012-06-05 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
US6458760B1 (en) * 1998-11-12 2002-10-01 Henry Ford Health System 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
JP2004523506A (ja) 2000-12-22 2004-08-05 アクシス・ファーマシューティカルズ・インコーポレイテッド カテプシン阻害剤としての新規な化合物と組成物
RS19504A (sr) 2001-09-14 2007-02-05 Aventis Pharmaceuticals Inc., Nova jedinjenja i kompozicije kao inhibitori katepsina
HUP0401906A3 (en) 2001-11-14 2008-07-28 Aventis Pharma Inc Novel cathepsin s inhibitors, process for their preparation and pharmaceutical compositions containing them
US7410956B2 (en) * 2002-02-11 2008-08-12 Vertex Pharmaceuticals Incorporated Caspase inhibitor prodrugs
AU2005249503B2 (en) * 2003-11-10 2011-08-25 Vertex Pharmaceuticals Incorporated ICE inhibitors for the treatment of autoinflammatory diseases
MX2007001337A (es) * 2004-08-02 2008-03-13 Genmedica Therapeutics Sl Compuestos para inhibir amina-oxidasas que contienen cobre y usos de los mismos.
JP6490660B2 (ja) * 2013-03-15 2019-03-27 ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー 活性に基づくプローブの化合物、組成物、および使用方法
ES2819218T3 (es) 2014-10-06 2021-04-15 Cortexyme Inc Inhibidores de lisina gingipaína
WO2017083433A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
KR102780603B1 (ko) 2016-09-16 2025-03-12 라이트하우스 파마슈티컬스, 인코포레이티드 리신 진지파인의 케톤 억제제
CA3033092C (en) 2016-12-23 2023-12-19 The Board Of Trustees Of The Leland Stanford Junior University Activity-based probe compounds, compositions, and methods of use
KR102669535B1 (ko) 2017-03-30 2024-05-24 더 보드 어브 트러스티스 어브 더 리랜드 스탠포드 주니어 유니버시티 생체 내 이미징을 위한 프로테아제 활성화 조영제
US11708348B2 (en) 2021-06-11 2023-07-25 The Scripps Research Institute Protease inhibitors for treatment of coronavirus infections

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
ZA86746B (en) * 1985-02-04 1986-09-24 Merrell Dow Pharma Novel 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
JPS63253061A (ja) 1988-10-20
IE62863B1 (en) 1995-03-08
AU602547B2 (en) 1990-10-18
DK674387D0 (da) 1987-12-21
IE873467L (en) 1988-06-22
ES2061480T3 (es) 1994-12-16
CA1329862C (en) 1994-05-24
ZA879577B (en) 1989-08-30
EP0272671A2 (en) 1988-06-29
DE3789371D1 (de) 1994-04-21
EP0272671B1 (en) 1994-03-16
DE3789371T2 (de) 1994-09-08
US5055451A (en) 1991-10-08
EP0272671A3 (en) 1990-06-13
NZ223002A (en) 1991-05-28
AU8287187A (en) 1988-07-21

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