[go: up one dir, main page]

ES553505A0 - Un procedimiento para la preparacion de derivados de cetona electrofilicos activados de sustratos de peptidasa, utiles en la inhibicion de enzimas proteasas - Google Patents

Un procedimiento para la preparacion de derivados de cetona electrofilicos activados de sustratos de peptidasa, utiles en la inhibicion de enzimas proteasas

Info

Publication number
ES553505A0
ES553505A0 ES553505A ES553505A ES553505A0 ES 553505 A0 ES553505 A0 ES 553505A0 ES 553505 A ES553505 A ES 553505A ES 553505 A ES553505 A ES 553505A ES 553505 A0 ES553505 A0 ES 553505A0
Authority
ES
Spain
Prior art keywords
inhibition
procedure
useful
preparation
protease enzymes
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.)
Granted
Application number
ES553505A
Other languages
English (en)
Other versions
ES8800051A1 (es
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.)
Aventis Pharmaceuticals Inc
Original Assignee
Merrell Dow Pharmaceuticals 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 Merrell Dow Pharmaceuticals Inc filed Critical Merrell Dow Pharmaceuticals Inc
Publication of ES8800051A1 publication Critical patent/ES8800051A1/es
Publication of ES553505A0 publication Critical patent/ES553505A0/es
Expired 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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0227—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the (partial) peptide sequence -Phe-His-NH-(X)2-C(=0)-, e.g. Renin-inhibitors with n = 2 - 6; for n > 6 see C07K5/06 - C07K5/10
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or 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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • 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
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • 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
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C07K5/0823—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp 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
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides 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
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
    • 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)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
ES553505A 1985-02-04 1986-03-26 Un procedimiento para la preparacion de derivados de cetona electrofilicos activados de sustratos de peptidasa, utiles en la inhibicion de enzimas proteasas Expired ES8800051A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US69798785A 1985-02-04 1985-02-04

Publications (2)

Publication Number Publication Date
ES8800051A1 ES8800051A1 (es) 1987-10-16
ES553505A0 true ES553505A0 (es) 1987-10-16

Family

ID=24803437

Family Applications (3)

Application Number Title Priority Date Filing Date
ES551597A Expired ES8800720A1 (es) 1985-02-04 1986-02-03 Un procedimiento para la preparacion de derivados carbonilicos de peptidasas electrofilicamente activadas.
ES553505A Expired ES8800051A1 (es) 1985-02-04 1986-03-26 Un procedimiento para la preparacion de derivados de cetona electrofilicos activados de sustratos de peptidasa, utiles en la inhibicion de enzimas proteasas
ES553504A Expired ES8800050A1 (es) 1985-02-04 1986-03-26 Un procedimiento para la preparacion de derivados de cetona electrofilicos activados de sustratos de peptidasa, utiles en la inhibicion de enzimas proteasas

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES551597A Expired ES8800720A1 (es) 1985-02-04 1986-02-03 Un procedimiento para la preparacion de derivados carbonilicos de peptidasas electrofilicamente activadas.

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES553504A Expired ES8800050A1 (es) 1985-02-04 1986-03-26 Un procedimiento para la preparacion de derivados de cetona electrofilicos activados de sustratos de peptidasa, utiles en la inhibicion de enzimas proteasas

Country Status (20)

Country Link
EP (1) EP0195212B1 (es)
JP (1) JP2529825B2 (es)
KR (1) KR900008004B1 (es)
CN (1) CN86101268A (es)
AR (1) AR246975A1 (es)
AT (1) ATE97652T1 (es)
AU (1) AU600226B2 (es)
CA (1) CA1341029C (es)
DE (1) DE3689314T2 (es)
DK (1) DK51586A (es)
ES (3) ES8800720A1 (es)
FI (1) FI94254C (es)
GR (1) GR860321B (es)
HU (1) HU207102B (es)
IE (1) IE60582B1 (es)
IL (1) IL77748A (es)
NO (1) NO169543C (es)
NZ (1) NZ215024A (es)
PT (1) PT81965B (es)
ZA (1) ZA86746B (es)

Families Citing this family (107)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62501147A (ja) * 1984-12-14 1987-05-07 オーストラリアン　コマーシャル　リサーチ　アンド　ディベロップメント　リミティド ヒト白血球エラスタ−ゼのアミノ酸阻害剤及びペプチド阻害剤
US5194588A (en) * 1985-01-22 1993-03-16 Ici Americas Inc. Aminoalcohol intermediates for peptide derivatives
GB8600263D0 (en) * 1985-01-22 1986-02-12 Ici America Inc Peptide derivatives
US5055450A (en) * 1985-01-22 1991-10-08 Ici Americas Inc. Peptide derivatives
US5496927A (en) * 1985-02-04 1996-03-05 Merrell Pharmaceuticals Inc. Peptidase inhibitors
GB8613704D0 (en) * 1986-06-05 1986-07-09 Ici America Inc Difluoro keto compounds
GB8619182D0 (en) * 1986-08-06 1986-09-17 Sandoz Ltd Peptides & derivatives
US5055451A (en) * 1986-12-22 1991-10-08 Syntex Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
US5158936A (en) * 1986-12-22 1992-10-27 Syntex (U.S.A.) Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
NZ223148A (en) * 1987-01-16 1989-10-27 Merrell Dow Pharma Peptide derivatives having peptidase inhibition activity
EP0276101A3 (en) * 1987-01-19 1989-11-23 Ici Americas Inc. Substituted peptide derivatives
US4820691A (en) * 1987-06-24 1989-04-11 E. R. Squibb & Sons, Inc. Amino acid 1,2-diketo derivatives as renin inhibitors
US5217958A (en) * 1988-03-03 1993-06-08 E. R. Squibb & Sons, Inc. 1,2-hydroxy phosphonates and derivatives thereof
US4981843A (en) * 1988-04-07 1991-01-01 E. R. Squibb & Sons, Inc. N-heterocyclic alcohol derivatives
US5151513A (en) * 1988-04-29 1992-09-29 E. R. Squibb & Sons, Inc. N-heterocyclic alcohol derivatives
EP0353732A3 (de) * 1988-08-05 1991-11-06 Ciba-Geigy Ag Neue Fluorolefine, Verfahren zu deren Herstellung und deren Verwendung
US5736520A (en) * 1988-10-07 1998-04-07 Merrell Pharmaceuticals Inc. Peptidase inhibitors
ZA897514B (en) * 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
EP0371179A1 (en) * 1988-10-28 1990-06-06 Merrell Dow Pharmaceuticals Inc. Novel analogs of peptidase substrates
EP0369391A3 (en) * 1988-11-15 1991-09-25 Boehringer Ingelheim Pharmaceuticals Inc. N-substituted amides
NZ235155A (en) * 1989-09-11 1993-04-28 Merrell Dow Pharma Peptidase substrates in which the carboxy terminal group has been replaced by a tricarbonyl radical
CA2018801C (en) * 1990-06-12 2000-08-22 Pierre Louis Beaulieu Antiherpes peptide derivatives having a 1,4-dioxo c n-terminus
JPH06504547A (ja) * 1990-12-28 1994-05-26 ジョージア・テック・リサーチ・コーポレーション ペプチドケトアミド、ケト酸およびケトエステル
EP1325931B1 (en) * 1991-03-01 2009-05-13 Dyax Corporation Inhibitors of human neutrophil elastase
US5391705A (en) * 1991-03-15 1995-02-21 Merrell Dow Pharmaceuticals Inc. Polyfluorinated tripeptide thrombin inhibitors
WO1992020357A1 (en) * 1991-05-23 1992-11-26 Merrell Dow Pharmaceuticals Inc. Inhibitors of cathepsin g and elastase for preventing connective tissue degradation
AU2882792A (en) * 1991-10-23 1993-05-21 Procter & Gamble Company, The Tripeptide derivative anti-inflammatory agents
US6235929B1 (en) 1991-12-27 2001-05-22 Georgia Tech Research Corporation Tripeptide α-ketoamides
US5610297A (en) * 1991-12-27 1997-03-11 Georgia Tech Research Corp. Peptides ketoamides
US5486529A (en) * 1992-04-16 1996-01-23 Zeneca Limited Certain pyridyl ketones for treating diseases involving leukocyte elastase
US5441960A (en) * 1992-04-16 1995-08-15 Zeneca Limited 1-pyrimidinylacetamide human leukocyte elastate inhibitors
JP2602181B2 (ja) * 1992-07-31 1997-04-23 ファイザー・インク． 消炎薬としてのペプチジル４−アミノ−２，２−ジフルオロ−３−オクソ−１，６−ヘキサン二酸誘導体
US5514694A (en) * 1992-09-21 1996-05-07 Georgia Tech Research Corp Peptidyl ketoamides
US5371072A (en) * 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
IL108031A0 (en) * 1992-12-22 1994-04-12 Procter & Gamble Difluoro pentapeptide derivatives and pharmaceutical compositions containing them
US5563127A (en) * 1993-03-24 1996-10-08 The Dupont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
US5780631A (en) * 1993-06-03 1998-07-14 Astra Aktiebolag Starting materials in the synthesis of thrombin and kininogenase inhibitors
US5541290A (en) * 1993-06-24 1996-07-30 Harbeson; Scott L. Optically pure calpain inhibitor compounds
NZ274074A (en) * 1993-10-01 1997-11-24 Merrell Pharma Inc Various dipeptide derivatives having a reduced carboxy group, the aldehyde being optionally substituted; pharmaceutical compositions
US5977074A (en) * 1993-10-01 1999-11-02 Merrell Pharmaceuticals, Inc. Inhibitors of β-amyloid protein production
US6060462A (en) * 1993-10-20 2000-05-09 Dupont Pharmaceuticals Company Electrophilic peptide analogs as inhibitors of trypsin-like enzymes
ES2179093T3 (es) * 1993-12-02 2003-01-16 Merrell Pharma Inc Inhibidores de la prolilendopeptidasa.
EP0763055B1 (en) * 1994-06-02 1999-11-03 Merrell Pharmaceuticals Inc. Perfluoroalkyl ketone inhibitors of elastase and processes for making the same
PT762887E (pt) * 1994-06-02 2002-01-30 Merrell Pharma Inc Derivados do enol acetilado como pro-farmacos de inibidores de elastase
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
US5510369A (en) * 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
SE9404196D0 (sv) * 1994-12-02 1994-12-02 Astra Ab New antithrombotic formulation
GB9502152D0 (en) * 1995-02-03 1995-03-29 Zeneca Ltd Proline derivatives
KR100388185B1 (ko) * 1995-02-17 2003-11-28 애보트 게엠베하 운트 콤파니 카게 트롬빈 억제제로서의 신규 디펩티드 아미딘
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
US6069130A (en) 1995-06-07 2000-05-30 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
US6022861A (en) * 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6211154B1 (en) 1995-06-07 2001-04-03 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
SA96170106A (ar) 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
US6069232A (en) * 1995-10-02 2000-05-30 Hoechst Marion Roussel, Inc. Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors
GB9524267D0 (en) * 1995-11-28 1996-01-31 Isis Innovation Enzyme inhibitor and method
US6172044B1 (en) 1995-12-01 2001-01-09 Aventis Pharmaceuticals Inc. Acylated enol derivative of α-ketoesters and α-ketoamides
TWI238827B (en) 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
US5739354A (en) * 1996-03-26 1998-04-14 Hoechst Marion Roussel, Inc. Process for the preparation of N-methyl-D-phenylalanyl-N- 1- 3- (aminoiminomethyl)amino!propyl!-3,3-difluoro-2-oxohexyl!-L-prolinamide
US6245743B1 (en) 1996-06-05 2001-06-12 Cor Therapeutics, Inc. Inhibitors of factor Xa
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds
US5792761A (en) * 1996-08-12 1998-08-11 Merck & Co., Inc. Thrombin inhibitors
UA79749C2 (en) 1996-10-18 2007-07-25 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
EP1136498A1 (en) * 1996-10-18 2001-09-26 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
US5854011A (en) * 1996-12-19 1998-12-29 Idexx Laboratories Incorporated Method and components for the detection of yeasts and/or molds in a sample
PL336589A1 (en) * 1997-05-02 2000-07-03 Akzo Nobel Nv Serinic protease inhibitors
AR013084A1 (es) 1997-06-19 2000-12-13 Astrazeneca Ab Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
CN1289341A (zh) 1998-01-26 2001-03-28 Basf公司 凝血酶抑制剂
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
WO2000042059A1 (en) 1999-01-13 2000-07-20 Astrazeneca Ab New amidinobenzylamine derivatives and their use as thrombin inhibitors
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
WO2001092234A1 (en) 2000-06-01 2001-12-06 Merck & Co., Inc. Pyrazinone thrombin inhibitors
CN1498224A (zh) 2000-07-21 2004-05-19 ���鹫˾ 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
WO2002008187A1 (en) 2000-07-21 2002-01-31 Schering Corporation Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin inhibitors
US6951843B2 (en) 2000-11-06 2005-10-04 Taiho Pharmaceutical Co., Ltd. Peptide derivatives and their pharmaceutically acceptable salts, thereof, processes for preparation of both and use thereof
US7129233B2 (en) 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
AR035216A1 (es) 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
JP2004516286A (ja) 2000-12-18 2004-06-03 メルク エンド カムパニー インコーポレーテッド ベンジルアミン誘導体およびそれのトロンビン阻害薬としての使用
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
US6610701B2 (en) 2001-02-09 2003-08-26 Merck & Co., Inc. Thrombin inhibitors
WO2002064559A2 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
AR034517A1 (es) 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
EP2204181A3 (en) * 2002-04-30 2010-09-22 Trustees Of Tufts College Protease inhibitors
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
US6989369B2 (en) 2003-02-07 2006-01-24 Dyax Corp. Kunitz domain peptides
US7781424B2 (en) 2003-05-27 2010-08-24 Astrazeneca Ab Modified release pharmaceutical formulation
TWI359147B (en) 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
US7795205B2 (en) 2004-04-12 2010-09-14 Canyon Pharmaceuticals, Inc. Methods for effecting regression of tumor mass and size in a metastasized pancreatic tumor
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
TW200827336A (en) 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
HUE060305T2 (hu) 2011-08-30 2023-02-28 Tufts College FAP-aktivált proteaszóma inhibitorok a szolid tumorok kezelésére
CA2963305A1 (en) * 2014-10-06 2016-04-14 Cortexyme, Inc. Inhibitors of lysine gingipain
CA3004095A1 (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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4277395A (en) 1980-06-16 1981-07-07 Richardson-Merrell Inc. Novel enzyme inhibitors
US4518528A (en) * 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
GB8600263D0 (en) * 1985-01-22 1986-02-12 Ici America Inc Peptide derivatives

Also Published As

Publication number Publication date
AU600226B2 (en) 1990-08-09
ES8800720A1 (es) 1987-11-16
AR246975A1 (es) 1994-10-31
EP0195212A2 (en) 1986-09-24
HU207102B (en) 1993-03-01
CN86101268A (zh) 1987-02-04
AU5288186A (en) 1986-08-07
DE3689314T2 (de) 1994-05-19
PT81965B (pt) 1988-01-22
JPS61183253A (ja) 1986-08-15
KR900008004B1 (ko) 1990-10-29
NO860371L (no) 1986-08-05
ES8800051A1 (es) 1987-10-16
ATE97652T1 (de) 1993-12-15
IL77748A (en) 1991-11-21
ES553504A0 (es) 1987-10-16
FI860484A0 (fi) 1986-02-03
PT81965A (en) 1986-03-01
EP0195212B1 (en) 1993-11-24
IE60582B1 (en) 1994-07-27
DK51586D0 (da) 1986-02-03
DK51586A (da) 1986-08-05
HUT40142A (en) 1986-11-28
FI860484L (fi) 1986-08-05
ES8800050A1 (es) 1987-10-16
FI94254B (fi) 1995-04-28
FI94254C (fi) 1995-08-10
DE3689314D1 (de) 1994-01-05
CA1341029C (en) 2000-06-20
GR860321B (en) 1986-06-04
EP0195212A3 (en) 1988-10-05
ZA86746B (en) 1986-09-24
NZ215024A (en) 1989-08-29
NO169543C (no) 1992-07-08
IE860303L (en) 1986-08-04
JP2529825B2 (ja) 1996-09-04
NO169543B (no) 1992-03-30
KR860006488A (ko) 1986-09-11
ES551597A0 (es) 1987-11-16

Similar Documents

Publication Publication Date Title
ES553505A0 (es) Un procedimiento para la preparacion de derivados de cetona electrofilicos activados de sustratos de peptidasa, utiles en la inhibicion de enzimas proteasas
ES553044A0 (es) Un procedimiento para la preparacion de nuevos derivados de fenoxialquilaminopirimidina.
ES552502A0 (es) Un procedimiento para la preparacion de nuevos derivados de tiazolidina.
ES541336A0 (es) Un procedimiento para la preparacion de derivados de benzotiazol y benzotiofen.
ES539852A0 (es) Un nuevo procedimiento para la preparacion de nuevos derivados. de carbazolona.
ES544644A0 (es) Un procedimiento para la preparacion de derivados de carboxamidoadenosina.
ES555834A0 (es) Un procedimiento para la preparacion de nuevas piranopiridinas.
ES551249A0 (es) Un procedimiento para la preparacion de peptidilaminodioles.
ES556738A0 (es) Un procedimiento para la preparacion de nuevos piridazinaminas.
EP0252057A3 (en) Serine protease inhibitors
ES556377A0 (es) Un metodo para la preparacion de una composicion detergente liquida.
ES556145A0 (es) Un procedimiento para la preparacion de nuevos derivados de piperazina.
ES546236A0 (es) Un procedimiento para la preparacion de derivados de bencimidasol.
ES552189A0 (es) Un procedimiento para la preparacion de derivados de piridimilmidazolidiona.
ES554983A0 (es) Un procedimiento para la preparacion de silileteres.
AU640517B2 (en) Chromogenic merocyanine enzyme substrates
ES553415A0 (es) Un procedimiento para la preparacion de derivados de ariletanolamina.
ES550504A0 (es) Un procedimiento para la preparacion de derivados de podofilotoxina.
MX18736A (es) Inhibidores retrovirales de proteasa y procedimiento para su preparacion.
ES539853A0 (es) Un procedimiento para la preparacion de nuevos derivados penem.
ES547805A0 (es) Un procedimiento para la preparacion de nuevos derivados de guanina.
ES555723A0 (es) Un procedimiento para la preparacion de tetrahidroimidazoquinazolinonas.
ES552241A0 (es) Un procedimiento para la preparacion de nuevos derivados de pirazolopiridinas.
ES549459A0 (es) Un procedimiento para la preparacion de derivados enzimaticos.
FI853369A7 (fi) Uusi -glukosidaasi-inhibiitti, menetelmäsen valmistamiseksi, sen käyttö ja farmaseuttisia valmisteita.

Legal Events

Date Code Title Description
FD1A Patent lapsed

Effective date: 20070807