NO894013L - Fremgangsmaate for fremstilling av peptidase-inhibitorer. - Google Patents

Fremgangsmaate for fremstilling av peptidase-inhibitorer.

Info

Publication number
NO894013L
NO894013L NO89894013A NO894013A NO894013L NO 894013 L NO894013 L NO 894013L NO 89894013 A NO89894013 A NO 89894013A NO 894013 A NO894013 A NO 894013A NO 894013 L NO894013 L NO 894013L
Authority
NO
Norway
Prior art keywords
alpha
amino acid
group
peptidase
alkyl
Prior art date
Application number
NO89894013A
Other languages
English (en)
Norwegian (no)
Other versions
NO894013D0 (no
Inventor
Philippe Bey
Michael Angelastro
Shujaath Mehdi
Original Assignee
Merrell Dow Pharma
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 Pharma filed Critical Merrell Dow Pharma
Publication of NO894013D0 publication Critical patent/NO894013D0/no
Publication of NO894013L publication Critical patent/NO894013L/no

Links

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
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • C07K5/02—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
    • C07K5/0207—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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • 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
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • 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
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • 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
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Detergent Compositions (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
NO89894013A 1988-10-07 1989-10-06 Fremgangsmaate for fremstilling av peptidase-inhibitorer. NO894013L (no)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US25476288A 1988-10-07 1988-10-07

Publications (2)

Publication Number Publication Date
NO894013D0 NO894013D0 (no) 1989-10-06
NO894013L true NO894013L (no) 1990-04-09

Family

ID=22965502

Family Applications (2)

Application Number Title Priority Date Filing Date
NO89894013A NO894013L (no) 1988-10-07 1989-10-06 Fremgangsmaate for fremstilling av peptidase-inhibitorer.
NO89894014A NO894014L (no) 1988-10-07 1989-10-06 Fremgangsmaate for fremstilling av peptidase-inhibitorer.

Family Applications After (1)

Application Number Title Priority Date Filing Date
NO89894014A NO894014L (no) 1988-10-07 1989-10-06 Fremgangsmaate for fremstilling av peptidase-inhibitorer.

Country Status (18)

Country Link
EP (2) EP0363284B1 (da)
JP (2) JP3203579B2 (da)
KR (2) KR900006362A (da)
CN (2) CN1041950A (da)
AT (2) ATE153029T1 (da)
AU (1) AU617875B2 (da)
CA (2) CA2000340A1 (da)
DE (2) DE68928042T2 (da)
DK (2) DK494789A (da)
ES (2) ES2103709T3 (da)
FI (2) FI894748A (da)
GR (1) GR3024158T3 (da)
HU (2) HU895246D0 (da)
IL (2) IL91895A0 (da)
NO (2) NO894013L (da)
NZ (2) NZ230893A (da)
PT (2) PT91926B (da)
ZA (2) ZA897514B (da)

Families Citing this family (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5510531A (en) * 1989-04-10 1996-04-23 Suntory Limited Proteinase inhibitor
EP0672648B1 (en) * 1989-04-15 1998-09-23 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Threo (2R,3S)-3-amino-2-hydroxypentanoic acid and threo (2R,3S)-3-(p-methoxy-benzyloxycarbonyl/FMOC) amino-2-hydroxy-pentanoic acid
EP0732399A3 (en) * 1990-03-05 1997-03-12 Cephalon Inc Chymotrypsin-like proteases and their inhibitors
GB9019558D0 (en) * 1990-09-07 1990-10-24 Szelke Michael Enzyme inhibitors
EP0564561A4 (en) * 1990-12-28 1994-08-10 Georgia Tech Res Inst Peptides ketoamides, ketoacids, and ketoesters
US5444042A (en) * 1990-12-28 1995-08-22 Cortex Pharmaceuticals Method of treatment of neurodegeneration with calpain inhibitors
ATE181925T1 (de) * 1991-05-23 1999-07-15 Merrell Pharma Inc Hemmstoffe für kathepsin-g und elastase zur verhütung von bindegewebsabbau
CA2071621C (en) * 1991-06-19 1996-08-06 Ahihiko Hosoda Aldehyde derivatives
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
US5514694A (en) * 1992-09-21 1996-05-07 Georgia Tech Research Corp Peptidyl ketoamides
DE69414279T2 (de) * 1993-02-09 1999-04-08 Bayer Corp., Pittsburgh, Pa. Sulfonamidaminomethylenderivate als Immunsuppressiva
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
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
EP0639585A1 (en) * 1993-08-20 1995-02-22 Banyu Pharmaceutical Co., Ltd. Elastase inhibitor
US5977074A (en) * 1993-10-01 1999-11-02 Merrell Pharmaceuticals, Inc. Inhibitors of β-amyloid protein production
IT1270882B (it) * 1993-10-05 1997-05-13 Isagro Srl Oligopeptidi ad attivita' fungicida
US6060462A (en) * 1993-10-20 2000-05-09 Dupont Pharmaceuticals Company Electrophilic peptide analogs as inhibitors of trypsin-like enzymes
US5486623A (en) 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US6660268B1 (en) 1994-03-18 2003-12-09 The President And Fellows Of Harvard College Proteasome regulation of NF-KB activity
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
DE4421884A1 (de) 1994-06-23 1996-01-04 Hoechst Ag Verfahren zur Herstellung von Hydroxycarbonsäureaniliden
US5510369A (en) * 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
DE4427837A1 (de) 1994-08-05 1996-02-08 Hoechst Ag Verfahren zur Herstellung von O-Acylglykolsäureaniliden
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
SE9404196D0 (sv) * 1994-12-02 1994-12-02 Astra Ab New antithrombotic formulation
US6017887A (en) * 1995-01-06 2000-01-25 Sibia Neurosciences, Inc. Peptide, peptide analog and amino acid analog protease inhibitors
US5804560A (en) * 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US5691368A (en) * 1995-01-11 1997-11-25 Hoechst Marion Roussel, Inc. Substituted oxazolidine calpain and/or cathepsin B inhibitors
DE69629176T2 (de) * 1995-01-18 2004-06-03 Alteon Inc. Verwendung von thiazoliumverbindungen zum verhindern und umkehren der bildung von endprodukten der fortgeschrittenen glykosylierung
US5656261A (en) 1995-01-18 1997-08-12 The Picower Institute For Medical Research Preventing and reversing advanced glycosylation endproducts
NO315930B1 (no) * 1995-01-18 2003-11-17 Picower Inst For Medical Res T Anvendelse av tiazoliumforbindelser ved fremstilling av farmasöytiske preparater, preparater som inneholder forbindelsene, samt nyetiazoliumforbindelser
DE19504225A1 (de) 1995-02-09 1996-08-14 Hoechst Ag Verfahren zur Herstellung von O-Acyloxycarbonsäureaniliden
MX9706069A (es) * 1995-02-17 1997-10-31 Basf Ag Nuevos inhibidores de la trombina.
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
US6022861A (en) * 1995-06-07 2000-02-08 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
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
US6211154B1 (en) 1995-06-07 2001-04-03 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
SA96170106A (ar) 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
US5827877A (en) 1995-09-14 1998-10-27 Cephalon, Inc. Ketomethylene group-containing cysteine and serine protease inhibitors
US5723580A (en) * 1995-09-14 1998-03-03 Cephalon, Inc. Ketomethylene group-containing aldehyde cysteine and serine protease inhibitors
US5763576A (en) * 1995-10-06 1998-06-09 Georgia Tech Research Corp. Tetrapeptide α-ketoamides
DE69625230T2 (de) * 1995-10-24 2003-09-04 Merck & Co., Inc. Thrombininhibitoren
CA2238175A1 (en) * 1995-11-28 1997-06-19 Cephalon, Inc. D-amino acid derived inhibitors of cysteine and serine proteases
TW541316B (en) 1995-12-21 2003-07-11 Astrazeneca Ab Prodrugs of thrombin inhibitors
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
TW498068B (en) * 1996-09-06 2002-08-11 Nippon Kayaku Kk Novel acetamide derivatives and protease inhibitors
SI0932617T1 (en) * 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
EP2314598A1 (en) * 1996-10-18 2011-04-27 Vertex Pharmaceuticals Incorporated Inhibitors of Hepatitis C virus NS3 serine protease
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
DE19648793A1 (de) 1996-11-26 1998-05-28 Basf Ag Neue Benzamide und deren Anwendung
AU6134498A (en) * 1997-03-07 1998-09-22 Hoechst Marion Roussel, Inc. Method of treating trauma associated with brain, spinal cord or peripheral nerveinjury using carbobenzyloxy n-protected di- and tripeptide phenylalaninals
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
US6011047A (en) * 1997-11-26 2000-01-04 Corvas International Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors
US6204384B1 (en) 1997-11-26 2001-03-20 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)
AU751412B2 (en) 1997-11-26 2002-08-15 3-Dimensional Pharmaceuticals, Inc. Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
CA2317761A1 (en) 1998-01-26 1999-07-29 Basf Aktiengesellschaft Thrombin inhibitors
EP2823812A1 (en) 1998-02-02 2015-01-14 Trustees Of Tufts College Dipeptidylpeptidase IV inhibitors for use in the treatment of Type II diabetes
DE69926884T2 (de) 1998-06-11 2006-06-14 Johnson & Johnson Pharm Res Pyrazine protease inhibitore
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
CA2355792A1 (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.
EP1189901A1 (en) 1999-05-27 2002-03-27 3-Dimensional Pharmaceuticals, Inc. Oxazaheterocycles as protease inhibitors
DE60005351D1 (de) 1999-07-09 2003-10-23 Dimensional Pharm Inc Heteroaryl protease inhibitoren und diagnostische bilderzeugungsmittel
US6630510B1 (en) * 1999-10-28 2003-10-07 Merck & Co., Inc. Substituted succinic acid metallo-β-lactamase inhibitors and their use in treating bacterial infections
US6809092B2 (en) * 2000-01-26 2004-10-26 Ono Pharmaceutical Co., Ltd. Benezene-fused heteroring derivatives and pharmaceutical agents comprising the same as active ingredient
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
AU2001265094A1 (en) 2000-06-01 2001-12-11 Merck And Co., Inc. Pyrazinone thrombin inhibitors
AU2001278927A1 (en) 2000-07-17 2002-01-30 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine pyrazinones as protease inhibitors
US7012066B2 (en) 2000-07-21 2006-03-14 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
CN1446201A (zh) * 2000-07-21 2003-10-01 先灵公司 用作丙型肝炎病毒ns3－丝氨酸蛋白酶抑制剂的新型肽
JP2004505956A (ja) 2000-08-04 2004-02-26 ３−ディメンショナル　ファーマシューティカルズ，　インコーポレイテッド 環式オキシグアニジンプロテアーゼインヒビター
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin inhibitors
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
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
WO2002050056A1 (en) 2000-12-18 2002-06-27 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
US6610701B2 (en) 2001-02-09 2003-08-26 Merck & Co., Inc. Thrombin inhibitors
US7144899B2 (en) 2001-02-09 2006-12-05 Merck & Co., Inc. Thrombin inhibitors
AR034517A1 (es) 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
US6777431B2 (en) 2001-07-13 2004-08-17 Corvas International, Inc. Non-convalent thrombin inhibitors
JP2005511636A (ja) 2001-11-26 2005-04-28 トラスティーズ オブ タフツ カレッジ 自己免疫疾患の治療方法及びそれに関する試薬
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
GB0217136D0 (en) 2002-07-24 2002-09-04 Renovo Ltd Wound healing & treatment of fibrosis
CA2504933C (en) 2002-11-06 2012-10-16 Dana-Farber Cancer Institute, Inc. Methods and compositions for treating cancer using proteasome inhibitors
US20050014747A1 (en) 2003-04-18 2005-01-20 Emily Reinhard Dihydrothiazine prodrugs of thiazolium agents
US7781424B2 (en) 2003-05-27 2010-08-24 Astrazeneca Ab Modified release pharmaceutical formulation
PE20050374A1 (es) 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
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
US20100048450A1 (en) 2005-10-07 2010-02-25 Klinken S Peter Sumoylation Control Agent and Uses Thereof
JP3975226B2 (ja) 2006-01-11 2007-09-12 生化学工業株式会社 シクロアルキルカルボニルアミノ酸誘導体及びその製造方法
JP4047365B2 (ja) 2006-01-11 2008-02-13 生化学工業株式会社 シクロアルカンカルボキサミド誘導体及びその製造方法
US8829209B2 (en) 2006-01-11 2014-09-09 Seikagaku Corporation Cycloalkylcarbonylamino acid ester derivative and process for producing the same
JP2009532038A (ja) 2006-04-07 2009-09-10 バイオファルミカ リミテッド 転写因子モジュレーター
TW200827336A (en) 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
EP2922535B1 (en) 2012-11-20 2021-11-10 Merck Sharp & Dohme Corp. Thrombin inhibitors
KR102455946B1 (ko) * 2017-08-02 2022-10-20 가부시키가이샤 히로시마 메탈 앤드 머시너리 분산기와, 슬러리 중 입자의 분산 방법 및 에멀젼 제조 방법
BR112020018910A2 (pt) 2018-03-20 2020-12-29 Abraxis Bioscience, Llc Métodos de tratamento de transtorno do sistema nervoso central através da administração de nanopartículas de um unibidor de mtor e de uma albumina

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4920118A (da) * 1972-06-23 1974-02-22
JPS594415B2 (ja) * 1974-02-18 1984-01-30 帝人株式会社 Ｄ，ｌ−２− アミノ −１− ブタノ−ルノ コウガクブンカツホウ
JPS50142505A (da) * 1974-05-08 1975-11-17
HU177098B (en) * 1979-01-04 1981-07-28 Gyogyszerkutato Intezet Process for producing new peptidyl-n-carboxy-l-arginin-a
JPS55138389A (en) * 1979-04-14 1980-10-29 Denki Kagaku Kogyo Kk Preparation of amino alcohols
FR2537131B1 (fr) * 1980-04-17 1986-05-09 Roques Bernard Nouveaux derives d'acides amines et leur application therapeutique
JPS5754157A (en) * 1980-09-19 1982-03-31 Nippon Kayaku Co Ltd L-argininal derivative and its preparation
JPS58198296A (ja) * 1982-05-12 1983-11-18 Chisso Corp ｄ−２−アミノブタノ−ルの製造法
WO1984000365A1 (en) * 1982-07-19 1984-02-02 Nat Res Dev Synthetic peptides and their preparation
DE3481913D1 (de) * 1983-04-27 1990-05-17 Ici America Inc Prolin-derivate.
GB8312339D0 (en) * 1983-05-05 1983-06-08 Austen B M Peptides
FR2546164B1 (fr) * 1983-05-16 1987-07-17 Centre Nat Rech Scient Nouveaux derives de peptides, leur preparation et leur application comme inhibiteurs de l'elastase
JPS59227851A (ja) * 1983-06-09 1984-12-21 Sankyo Co Ltd レニン阻害作用を有するペプチド類
CA1267499A (en) * 1983-07-12 1990-04-03 Cedric H. Hassall Peptide amides and aldehydes
DK34086A (da) * 1985-01-23 1986-07-24 Abbott Lab Peptidylaminodioler
AU600226B2 (en) * 1985-02-04 1990-08-09 Merrell Pharmaceuticals Inc. Novel peptidase inhibitors
EP0264106B1 (en) * 1986-10-14 1994-03-16 Banyu Pharmaceutical Co., Ltd. 5-Substituted amino-4-hydroxy-pentanoic acid derivatives and their use
MY103189A (en) * 1986-10-31 1993-05-29 Pfizer Nor-statine and nor-cyclostatine polypeptides
FI89058C (fi) * 1987-02-27 1993-08-10 Yamanouchi Pharma Co Ltd Foerfarande foer framstaellning av som remin-inhibitorer anvaenda 2-(l-alanyl-l-histidylamino)-butanol-derivat
US4820691A (en) * 1987-06-24 1989-04-11 E. R. Squibb & Sons, Inc. Amino acid 1,2-diketo derivatives as renin inhibitors
US4913296A (en) * 1988-03-30 1990-04-03 Applied Power Inc. Storing and dispensing system
DE3827415A1 (de) * 1988-08-12 1990-02-15 Behringwerke Ag Peptidderivate, verfahren zu ihrer herstellung und ihre verwendung

Also Published As

Publication number Publication date
ES2103709T3 (es) 1997-10-01
FI894748A (fi) 1990-04-08
NZ230893A (en) 1992-01-29
JPH02134398A (ja) 1990-05-23
DK494789A (da) 1990-04-08
DK494789D0 (da) 1989-10-06
CN1041951A (zh) 1990-05-09
IL91896A0 (en) 1990-06-10
DE68928662D1 (de) 1998-06-10
ZA897514B (en) 1990-06-27
FI894748A0 (fi) 1989-10-06
GR3024158T3 (en) 1997-10-31
KR900006362A (ko) 1990-05-08
KR900006363A (ko) 1990-05-08
EP0364344A3 (en) 1991-09-11
EP0363284B1 (en) 1997-05-14
PT91926A (pt) 1990-04-30
NZ230916A (en) 1992-02-25
PT91927B (pt) 1995-07-03
HU895246D0 (en) 1990-01-28
CN1041950A (zh) 1990-05-09
DE68928042T2 (de) 1997-08-28
AU626918B2 (en) 1992-08-13
NO894013D0 (no) 1989-10-06
EP0364344A2 (en) 1990-04-18
NO894014L (no) 1990-04-09
DK494689A (da) 1990-04-08
EP0364344B1 (en) 1998-05-06
IL91895A0 (en) 1990-06-10
ATE153029T1 (de) 1997-05-15
DK494689D0 (da) 1989-10-06
CA2000342A1 (en) 1990-04-07
AU617875B2 (en) 1991-12-05
PT91926B (pt) 1995-07-03
HUT54105A (en) 1991-01-28
ZA897515B (en) 1990-06-27
AU4262589A (en) 1990-04-12
ES2118710T3 (es) 1998-10-01
FI894747A0 (fi) 1989-10-06
JPH02256654A (ja) 1990-10-17
AU4249189A (en) 1990-06-28
DE68928042D1 (de) 1997-06-19
FI894747A (fi) 1990-04-08
DE68928662T2 (de) 1998-11-26
ATE165835T1 (de) 1998-05-15
NO894014D0 (no) 1989-10-06
CA2000342C (en) 2000-10-03
EP0363284A3 (en) 1992-07-01
EP0363284A2 (en) 1990-04-11
PT91927A (pt) 1990-04-30
JP3203579B2 (ja) 2001-08-27
HU895247D0 (da) 1990-01-28
CA2000340A1 (en) 1990-04-07

Similar Documents

Publication Publication Date Title
NO894013D0 (no) Fremgangsmaate for fremstilling av peptidase-inhibitorer.
EP0393457B1 (en) Proteinase inhibitor
ATE159945T1 (de) Beta-aminoalkyl und beta-n- peptidylaminoalkylborsäure
GR3030311T3 (en) Peptide derivatives of the boronic acid having protease inhibiting activity, process for their production and pharmaceutical compositions comprising them.
CO4950618A1 (es) Inhibidores de proteasas
ATE251146T1 (de) Selektive thrombin-hemmer
NO921852D0 (no) N-substituerte azaheterosykliske karboksylsyrer og en farmasoeytisk sammensetning
MY155266A (en) Selective thrombin inhibitors
MY155273A (en) Selective thrombin inhibitors
MY155271A (en) Selective thrombin inhibitors