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PT91927A - Processo para a preparacao de novos inibidores de peptidase - Google Patents

Processo para a preparacao de novos inibidores de peptidase

Info

Publication number
PT91927A
PT91927A PT91927A PT9192789A PT91927A PT 91927 A PT91927 A PT 91927A PT 91927 A PT91927 A PT 91927A PT 9192789 A PT9192789 A PT 9192789A PT 91927 A PT91927 A PT 91927A
Authority
PT
Portugal
Prior art keywords
alpha
amino acid
group
peptidase
alkyl
Prior art date
Application number
PT91927A
Other languages
English (en)
Other versions
PT91927B (pt
Inventor
Philippe Bey
Shujaath Mehdi
Michael Angelastro
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 PT91927A publication Critical patent/PT91927A/pt
Publication of PT91927B publication Critical patent/PT91927B/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • 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
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides 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
    • 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
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • 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
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-amino acid
    • 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
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • 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
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (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)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Saccharide Compounds (AREA)
  • Detergent Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
PT91927A 1988-10-07 1989-10-06 Processo para a preparacao de novos inibidores de peptidase PT91927B (pt)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
PT91927A true PT91927A (pt) 1990-04-30
PT91927B PT91927B (pt) 1995-07-03

Family

ID=22965502

Family Applications (2)

Application Number Title Priority Date Filing Date
PT91926A PT91926B (pt) 1988-10-07 1989-10-06 Processo para a preparacao de novos inibidores de peptidase
PT91927A PT91927B (pt) 1988-10-07 1989-10-06 Processo para a preparacao de novos inibidores de peptidase

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PT91926A PT91926B (pt) 1988-10-07 1989-10-06 Processo para a preparacao de novos inibidores de peptidase

Country Status (18)

Country Link
EP (2) EP0364344B1 (pt)
JP (2) JP3203579B2 (pt)
KR (2) KR900006363A (pt)
CN (2) CN1041951A (pt)
AT (2) ATE153029T1 (pt)
AU (1) AU617875B2 (pt)
CA (2) CA2000340A1 (pt)
DE (2) DE68928042T2 (pt)
DK (2) DK494689A (pt)
ES (2) ES2103709T3 (pt)
FI (2) FI894748A (pt)
GR (1) GR3024158T3 (pt)
HU (2) HU895246D0 (pt)
IL (2) IL91896A0 (pt)
NO (2) NO894014L (pt)
NZ (2) NZ230893A (pt)
PT (2) PT91926B (pt)
ZA (2) ZA897514B (pt)

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
WO1990012805A1 (en) * 1989-04-15 1990-11-01 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Postostatin and related compound thereof, or their salts
WO1991013904A1 (en) * 1990-03-05 1991-09-19 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
HU217612B (hu) * 1991-05-23 2000-03-28 Merrel Dow Pharmaceuticals Inc. Eljárás elasztáz és katepszin G inhibitor hatású peptidek előállítására
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
US5783563A (en) * 1993-06-03 1998-07-21 Astra Aktiebolag Method for treatment or prophylaxis of venous thrombosis
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
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
US5863902A (en) * 1995-01-06 1999-01-26 Sibia Neurosciences, Inc. Methods of treating neurodegenerative disorders using 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
FI119756B (fi) * 1995-01-18 2009-03-13 Alteon Inc Tiatsoliumyhdisteiden käyttö pitkälle edenneen glykosylaation lopputuotteiden muodostumisen estossa ja suunnan muutoksessa
US5656261A (en) 1995-01-18 1997-08-12 The Picower Institute For Medical Research Preventing and reversing advanced glycosylation endproducts
DE19504225A1 (de) 1995-02-09 1996-08-14 Hoechst Ag Verfahren zur Herstellung von O-Acyloxycarbonsäureaniliden
WO1996025426A1 (de) * 1995-02-17 1996-08-22 Basf Aktiengesellschaft Neue dipeptidische amidine als thrombin-inhibitoren
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
US6211154B1 (en) 1995-06-07 2001-04-03 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6022861A (en) * 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic 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
US5721214A (en) * 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
SA96170106A (ar) * 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
US5723580A (en) * 1995-09-14 1998-03-03 Cephalon, Inc. Ketomethylene group-containing aldehyde cysteine and serine protease inhibitors
US5827877A (en) * 1995-09-14 1998-10-27 Cephalon, Inc. Ketomethylene group-containing 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
AU714324B2 (en) * 1995-11-28 2000-01-06 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
IL128514A (en) * 1996-09-06 2003-07-06 Nippon Kayaku Kk Acetamide derivatives, pharmaceutical compositions comprising them and a process for producing such derivatives
SI0932617T1 (en) * 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
KR100509388B1 (ko) * 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 c 바이러스 ns3 프로테아제의 저해제
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
CA2311969A1 (en) 1997-11-26 1999-06-03 3-Dimensional Pharmaceuticals, Inc. Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
US6204384B1 (en) 1997-11-26 2001-03-20 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
KR100689923B1 (ko) 1998-01-26 2007-03-09 애보트 게엠베하 운트 콤파니 카게 트롬빈 억제제
AU766219B2 (en) 1998-02-02 2003-10-09 1149336 Ontario Inc. Method of regulating glucose metabolism, and reagents related thereto
NZ508669A (en) 1998-06-11 2003-06-30 Dimensional Pharm Inc Pyrazinone protease inhibitors
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
CZ20012529A3 (cs) 1999-01-13 2001-11-14 Astrazeneca Ab Nový amidinobenzylamidový derivát a jeho pouľití jako inhibitoru thrombinu
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
ATE250056T1 (de) 1999-07-09 2003-10-15 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
KR20020067937A (ko) * 2000-01-26 2002-08-24 오노 야꾸힝 고교 가부시키가이샤 벤젠 축합 헤테로환 유도체 및 그 유도체를 유효성분으로서 함유하는 약제
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
AU2001278927A1 (en) 2000-07-17 2002-01-30 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine pyrazinones as protease inhibitors
CN102372764A (zh) 2000-07-21 2012-03-14 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
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
CA2410682A1 (en) * 2000-07-21 2002-01-31 Schering Corporation Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
EP1307432A1 (en) 2000-08-04 2003-05-07 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine protease inhibitors
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin 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
US7129233B2 (en) 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
AU2002230836A1 (en) 2000-12-18 2002-07-01 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
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
CA2436176A1 (en) 2001-02-09 2002-08-22 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
WO2003045228A2 (en) 2001-11-26 2003-06-05 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
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
GB0217136D0 (en) 2002-07-24 2002-09-04 Renovo Ltd Wound healing & treatment of fibrosis
JP5354836B2 (ja) 2002-11-06 2013-11-27 デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド プロテアソームインヒビターを使用する癌を処置するための方法および組成物
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
UY28500A1 (es) 2003-09-05 2005-04-29 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
JP2009510131A (ja) 2005-10-07 2009-03-12 バイオファルミカ リミテッド Sumo化制御剤及びその用途
CA2636765C (en) 2006-01-11 2014-03-18 Seikagaku Corporation Cycloalkylcarbonylamino acid ester derivative and process for producing the same
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
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
WO2007115364A1 (en) 2006-04-07 2007-10-18 Biopharmica Limited Transcription factor modulator
TW200827336A (en) 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
WO2014081618A1 (en) 2012-11-20 2014-05-30 Merck Sharp & Dohme Corp. Thrombin inhibitors
WO2019026208A1 (ja) * 2017-08-02 2019-02-07 株式会社広島メタル&マシナリー 分散機と、スラリー中粒子の分散方法及びエマルジョン製造方法
CN112188892A (zh) 2018-03-20 2021-01-05 阿布拉科斯生物科学有限公司 通过mTOR抑制剂和白蛋白的纳米颗粒的施用治疗中枢神经系统障碍的方法

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4920118A (pt) * 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 (pt) * 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
GB2124233B (en) * 1982-07-19 1985-09-18 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
US4851387A (en) * 1986-10-14 1989-07-25 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

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FI894747A0 (fi) 1989-10-06
CN1041950A (zh) 1990-05-09
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PT91927B (pt) 1995-07-03
HU895247D0 (pt) 1990-01-28
ES2118710T3 (es) 1998-10-01
EP0364344A3 (en) 1991-09-11
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DE68928662T2 (de) 1998-11-26
GR3024158T3 (en) 1997-10-31
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IL91896A0 (en) 1990-06-10
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DK494689D0 (da) 1989-10-06
CA2000342C (en) 2000-10-03
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NO894013D0 (no) 1989-10-06
ATE153029T1 (de) 1997-05-15
JPH02134398A (ja) 1990-05-23
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DK494689A (da) 1990-04-08
ZA897515B (en) 1990-06-27
NO894014L (no) 1990-04-09
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EP0363284B1 (en) 1997-05-14
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CA2000342A1 (en) 1990-04-07
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DK494789A (da) 1990-04-08
PT91926B (pt) 1995-07-03
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