DE68928662D1 - Peptidase-Hemmer - Google Patents

Peptidase-Hemmer

Info

Publication number
DE68928662D1
DE68928662D1 DE68928662T DE68928662T DE68928662D1 DE 68928662 D1 DE68928662 D1 DE 68928662D1 DE 68928662 T DE68928662 T DE 68928662T DE 68928662 T DE68928662 T DE 68928662T DE 68928662 D1 DE68928662 D1 DE 68928662D1
Authority
DE
Germany
Prior art keywords
alpha
amino acid
group
peptidase
alkyl
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.)
Expired - Fee Related
Application number
DE68928662T
Other languages
English (en)
Other versions
DE68928662T2 (de
Inventor
Philippe Bey
Michael Angelastro
Shujaath Mehdi
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
Application granted granted Critical
Publication of DE68928662D1 publication Critical patent/DE68928662D1/de
Publication of DE68928662T2 publication Critical patent/DE68928662T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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
    • 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
DE68928662T 1988-10-07 1989-10-06 Peptidase-Hemmer Expired - Fee Related DE68928662T2 (de)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
DE68928662D1 true DE68928662D1 (de) 1998-06-10
DE68928662T2 DE68928662T2 (de) 1998-11-26

Family

ID=22965502

Family Applications (2)

Application Number Title Priority Date Filing Date
DE68928662T Expired - Fee Related DE68928662T2 (de) 1988-10-07 1989-10-06 Peptidase-Hemmer
DE68928042T Expired - Fee Related DE68928042T2 (de) 1988-10-07 1989-10-06 Verwendung von Peptidase-Hemmer zur Herstellung von Medikamenten für die Behandlung von Schlaganfällen

Family Applications After (1)

Application Number Title Priority Date Filing Date
DE68928042T Expired - Fee Related DE68928042T2 (de) 1988-10-07 1989-10-06 Verwendung von Peptidase-Hemmer zur Herstellung von Medikamenten für die Behandlung von Schlaganfällen

Country Status (18)

Country Link
EP (2) EP0364344B1 (de)
JP (2) JP3203579B2 (de)
KR (2) KR900006363A (de)
CN (2) CN1041950A (de)
AT (2) ATE153029T1 (de)
AU (1) AU617875B2 (de)
CA (2) CA2000342C (de)
DE (2) DE68928662T2 (de)
DK (2) DK494689A (de)
ES (2) ES2103709T3 (de)
FI (2) FI894748A (de)
GR (1) GR3024158T3 (de)
HU (2) HU895246D0 (de)
IL (2) IL91895A0 (de)
NO (2) NO894014L (de)
NZ (2) NZ230893A (de)
PT (2) PT91927B (de)
ZA (2) ZA897515B (de)

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 (de) * 1989-04-15 1998-09-23 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Threo (2R, 3S)-3-amino-2-hydroxypentansäure und threo (2R,3S)-3-(p-methoxy-benzyloxycarbonyl/FMOC) amino-2-hydroxy-pentansäure
EP0518955A4 (en) * 1990-03-05 1993-09-22 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
EP0587799B1 (de) * 1991-05-23 1999-07-07 Merrell Pharmaceuticals Inc. Hemmstoffe für kathepsin-g und elastase zur verhütung von bindegewebsabbau
CA2071621C (en) * 1991-06-19 1996-08-06 Ahihiko Hosoda Aldehyde derivatives
US5650508A (en) * 1991-12-27 1997-07-22 Georgia Tech Research Corporation Peptide ketoamides
US6235929B1 (en) 1991-12-27 2001-05-22 Georgia Tech Research Corporation Tripeptide α-ketoamides
US5514694A (en) * 1992-09-21 1996-05-07 Georgia Tech Research Corp Peptidyl ketoamides
EP0610744B1 (de) * 1993-02-09 1998-11-04 Bayer Corporation Sulfonamidaminomethylenderivate als Immunsuppressiva
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
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
US5541290A (en) * 1993-06-24 1996-07-30 Harbeson; Scott L. Optically pure calpain inhibitor compounds
EP0639585A1 (de) * 1993-08-20 1995-02-22 Banyu Pharmaceutical Co., Ltd. Elastase Hemmer
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
US5804560A (en) * 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US6017887A (en) * 1995-01-06 2000-01-25 Sibia Neurosciences, Inc. Peptide, peptide analog and amino acid analog protease inhibitors
US5691368A (en) * 1995-01-11 1997-11-25 Hoechst Marion Roussel, Inc. Substituted oxazolidine calpain and/or cathepsin B inhibitors
CN1142778C (zh) * 1995-01-18 2004-03-24 奥尔顿有限公司 噻唑鎓化合物用于预防和逆转高级糖基化终产物形成的用途
US5656261A (en) 1995-01-18 1997-08-12 The Picower Institute For Medical Research Preventing and reversing advanced glycosylation endproducts
FI119756B (fi) 1995-01-18 2009-03-13 Alteon Inc Tiatsoliumyhdisteiden käyttö pitkälle edenneen glykosylaation lopputuotteiden muodostumisen estossa ja suunnan muutoksessa
DE19504225A1 (de) 1995-02-09 1996-08-14 Hoechst Ag Verfahren zur Herstellung von O-Acyloxycarbonsäureaniliden
NZ302649A (en) * 1995-02-17 2000-01-28 Basf Ag Dipeptide amidine derivatives, preparation and pharmaceutical compositions thereof
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
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
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
EP0858262B1 (de) * 1995-10-24 2002-12-04 Merck & Co., Inc. Thrombininhibitoren
ES2293651T3 (es) * 1995-11-28 2008-03-16 Cephalon, Inc. Inhibidores de cisteina y serina proteasas derivados de aminoacidos d.
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
WO1998009949A1 (fr) * 1996-09-06 1998-03-12 Nippon Kayaku Kabushiki Kaisha Nouveaux derives d'acetamide et inhibiteurs de protease
JP4080541B2 (ja) * 1996-10-18 2008-04-23 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子
SI0932617T1 (en) * 1996-10-18 2002-06-30 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
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
TWI222441B (en) 1997-11-26 2004-10-21 Dimensional Pharm 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)
US6011047A (en) * 1997-11-26 2000-01-04 Corvas International Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
EP1051431A1 (de) 1998-01-26 2000-11-15 Basf Aktiengesellschaft Thrombininhibitoren
EP1052994A2 (de) 1998-02-02 2000-11-22 Trustees Of Tufts College Verwendung von dipetidylpeptidasehemmer zur regulierung des glukosemetabolismus
ATE461210T1 (de) 1998-06-11 2010-04-15 Ortho Mcneil Pharm Inc Pyrazine protease inhibitore
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
EP1150996B1 (de) 1999-01-13 2007-11-21 AstraZeneca AB Neue amidinbenzylamin-derivate und ihre verwendung als thrombin-inhibitoren
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
AU5046600A (en) 1999-05-27 2000-12-18 3-Dimensional Pharmaceuticals, Inc. Oxazaheterocycles as protease inhibitors
WO2001004117A1 (en) 1999-07-09 2001-01-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl protease inhibitors and diagnostic imaging agents
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
EP1254898A4 (de) * 2000-01-26 2003-03-12 Ono Pharmaceutical Co Benzokondensierte heterocyclische derivate sowie diese als wirkstoffe enthaltende medikamente
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
CA2415932A1 (en) 2000-07-17 2002-01-24 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
CZ2003195A3 (cs) * 2000-07-21 2003-04-16 Schering Corporation Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostředek
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
CA2417914A1 (en) 2000-08-04 2002-02-14 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
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
US7144899B2 (en) 2001-02-09 2006-12-05 Merck & Co., Inc. Thrombin inhibitors
US6610701B2 (en) 2001-02-09 2003-08-26 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
EP2769715A3 (de) 2001-11-26 2014-09-17 Trustees Of Tufts College Verfahren zur Behandlung von Autoimmunkrankheiten und damit zusammenhängende Reagenzien
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
WO2004043374A2 (en) 2002-11-06 2004-05-27 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
TW201127828A (en) 2003-09-05 2011-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
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
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
CN109600995A (zh) * 2017-08-02 2019-04-09 广岛金属与机械株式会社 分散机与浆料中颗粒的分散方法以及乳液制造方法
AU2019239953A1 (en) 2018-03-20 2020-10-15 Abraxis Bioscience, Llc Methods of treating central nervous system disorders via administration of nanoparticles of an mtor inhibitor and an albumin

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4920118A (de) * 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 (de) * 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
EP0124317B1 (de) * 1983-04-27 1990-04-11 Ici Americas 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
CA1341029C (en) * 1985-02-04 2000-06-20 Michael Kolb 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

Also Published As

Publication number Publication date
DE68928042T2 (de) 1997-08-28
CA2000342A1 (en) 1990-04-07
FI894747A0 (fi) 1989-10-06
NO894014L (no) 1990-04-09
JP3203579B2 (ja) 2001-08-27
EP0364344A3 (de) 1991-09-11
ZA897514B (en) 1990-06-27
PT91927B (pt) 1995-07-03
DE68928042D1 (de) 1997-06-19
AU4249189A (en) 1990-06-28
FI894748A (fi) 1990-04-08
EP0363284B1 (de) 1997-05-14
DK494689A (da) 1990-04-08
NO894013D0 (no) 1989-10-06
DK494789A (da) 1990-04-08
AU4262589A (en) 1990-04-12
DE68928662T2 (de) 1998-11-26
EP0364344A2 (de) 1990-04-18
IL91895A0 (en) 1990-06-10
FI894748A0 (fi) 1989-10-06
EP0363284A2 (de) 1990-04-11
DK494789D0 (da) 1989-10-06
NZ230916A (en) 1992-02-25
NO894013L (no) 1990-04-09
AU626918B2 (en) 1992-08-13
FI894747A (fi) 1990-04-08
CA2000340A1 (en) 1990-04-07
CN1041951A (zh) 1990-05-09
GR3024158T3 (en) 1997-10-31
ES2118710T3 (es) 1998-10-01
HU895246D0 (en) 1990-01-28
DK494689D0 (da) 1989-10-06
JPH02134398A (ja) 1990-05-23
KR900006362A (ko) 1990-05-08
ZA897515B (en) 1990-06-27
ATE165835T1 (de) 1998-05-15
CA2000342C (en) 2000-10-03
HU895247D0 (de) 1990-01-28
PT91927A (pt) 1990-04-30
NO894014D0 (no) 1989-10-06
NZ230893A (en) 1992-01-29
ATE153029T1 (de) 1997-05-15
CN1041950A (zh) 1990-05-09
JPH02256654A (ja) 1990-10-17
ES2103709T3 (es) 1997-10-01
HUT54105A (en) 1991-01-28
PT91926B (pt) 1995-07-03
PT91926A (pt) 1990-04-30
IL91896A0 (en) 1990-06-10
EP0364344B1 (de) 1998-05-06
EP0363284A3 (de) 1992-07-01
KR900006363A (ko) 1990-05-08
AU617875B2 (en) 1991-12-05

Similar Documents

Publication Publication Date Title
ATE165835T1 (de) Peptidase-hemmer
EP0393457B1 (de) Protease-Hemmer
DE69315079D1 (de) Beta-aminoalkyl und beta-n-peptidylaminoalkylborsäure
CO4950618A1 (es) Inhibidores de proteasas
GR3030311T3 (en) Peptide derivatives of the boronic acid having protease inhibiting activity, process for their production and pharmaceutical compositions comprising them.
DE69630160D1 (de) Selektive Thrombin-Hemmer
NO921852L (no) N-substituerte azaheterosykliske karboksylsyrer og en farmasoeytisk sammensetning
MY155273A (en) Selective thrombin inhibitors

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee