NO930731L - kininogenase inhibitor - Google Patents

kininogenase inhibitor

Info

Publication number
NO930731L
NO930731L NO93930731A NO930731A NO930731L NO 930731 L NO930731 L NO 930731L NO 93930731 A NO93930731 A NO 93930731A NO 930731 A NO930731 A NO 930731A NO 930731 L NO930731 L NO 930731L
Authority
NO
Norway
Prior art keywords
amino acid
group
analog
amide
conformational
Prior art date
Application number
NO93930731A
Other languages
Norwegian (no)
Other versions
NO930731D0 (en
Inventor
Michael Szelke
David Michael Evans
David Michael Jones
Original Assignee
Ferring Peptide Research Partn
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 Ferring Peptide Research Partn filed Critical Ferring Peptide Research Partn
Publication of NO930731D0 publication Critical patent/NO930731D0/en
Publication of NO930731L publication Critical patent/NO930731L/en

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

Kininogenaseinhibitorer, som optimalt ikke overskrider størrelsen av et heksapeptid, represen-tert ved (II), hvor A og B = aminoacyl (omfattende aminoacylanalog) som er de samme eller forskjellige og danner en dipeptidgruppe hvor aminosyren A "har en terminalgruppe og er en hvilken som helst amino- eller iminosyrerest (men fortrinnsvis med D-konfigurasjon, og B er en lipofil aminosyrerest med D- eller L-konfigurasjon, men ikke prolin eller en prolinanalog, eller en konformasjonsanalog av nevnte dipeptidgruppe hvor peptidbindingen er erstattet med -CH-NH- ("redusert"), -CH(OH)-CH- ("hydroksy"), -CO-CH("keto"), -CHCH- ("hydrokarbon") eller en annen konformasjonsetterligning av peptidbindingen og i (III) skal sidekjeden Rvære sidekjeden i en basisk aminosyre eller aminosyreanalog (fortrinnsvis med L-konfigurasjon), og R være H eller lavere alkyl(0-0) eller C eller peptidbindingen omfattende -N(R)- er erstattet, hvilket farer til en konformasjonsetterligning som ovenfor; V = en bindingsøkende eller karbonylaktiverende gruppe, fortrinnsvis valgt fra H (når A eller B må være cykloheksylalanin, fortrinnsvis D dersom den er A eller L dersom den er B) eller alkyl (CCq) eller fluoralkyl (C-C); substituert oksymetylen; tiometylen; sulfoksymetylen; sulfonylmetylen; aminometylen; hydrazino-metylen; -CH-Het (hvor Het = en substituert eller usubstituert heterocyklus); substituert amino (men når den resulterende forbindelse er et sekundært alkylamid, må B ikke være fenylalanin); en aminosyregruppe eller dens ester eller amid; et karboksylisk sekundært amid eller primært amid, når B må være cykloheksylalanin eller adamantylalanin eller en annen svær lipofil, ikke-aromatisk aminosyre (ikke Ala Leu Ile Val Nva Met Nie Phe Tyr Trp Nal (1)); tertiært karboksamid; karboksyalkylgruppe eller dens ester eller amid eller aminoacylderivat.Quininogenase inhibitors, which optimally do not exceed the size of a hexapeptide, represented by (II), wherein A and B = aminoacyl (comprising aminoacyl analog) which are the same or different and form a dipeptide group where amino acid A "has a terminal group and is a any amino or amino acid residue (but preferably with D-configuration, and B is a lipophilic amino acid residue with D- or L-configuration, but not proline or a proline analog, or a conformational analog of said dipeptide group in which the peptide bond is replaced by -CH-NH - ("reduced"), -CH (OH) -CH- ("hydroxy"), -CO-CH ("keto"), -CHCH- ("hydrocarbon") or other conformational imitation of the peptide bond and in (III) the side chain R should be the side chain of a basic amino acid or amino acid analog (preferably with L-configuration), and R is H or lower alkyl (0-0) or C or the peptide bond comprising -N (R) - is replaced, leading to a conformational imitation which above; V = a binding search nd or carbonyl activating group, preferably selected from H (when A or B must be cyclohexylalanine, preferably D if it is A or L if it is B) or alkyl (Cqq) or fluoroalkyl (C-C); substituted oxymethylene; thiomethylene; sulfoxymethylene; sulfonylmethylene; aminomethylene; hydrazinomethylene; -CH-Het (wherein Het = a substituted or unsubstituted heterocycle); substituted amino (but when the resulting compound is a secondary alkylamide, B must not be phenylalanine); an amino acid group or its ester or amide; a carboxylic secondary amide or primary amide, when B must be cyclohexylalanine or adamantylalanine or another major lipophilic, non-aromatic amino acid (not Ala Leu Ile Val Nva Met Nie Phe Tyr Trp Nal (1)); tertiary carboxamide; carboxyalkyl group or its ester or amide or aminoacyl derivative.

NO93930731A 1990-09-07 1993-02-26 kininogenase inhibitor NO930731L (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB909019558A GB9019558D0 (en) 1990-09-07 1990-09-07 Enzyme inhibitors
PCT/GB1991/001479 WO1992004371A1 (en) 1990-09-07 1991-09-02 Kininogenase inhibitors

Publications (2)

Publication Number Publication Date
NO930731D0 NO930731D0 (en) 1993-02-26
NO930731L true NO930731L (en) 1993-05-07

Family

ID=10681831

Family Applications (1)

Application Number Title Priority Date Filing Date
NO93930731A NO930731L (en) 1990-09-07 1993-02-26 kininogenase inhibitor

Country Status (13)

Country Link
EP (1) EP0652893A1 (en)
JP (1) JPH06501461A (en)
AU (1) AU8438791A (en)
CA (1) CA2090858A1 (en)
FI (1) FI930946A (en)
GB (1) GB9019558D0 (en)
HU (1) HUT64084A (en)
IE (1) IE913120A1 (en)
MC (1) MC2313A1 (en)
NO (1) NO930731L (en)
PT (1) PT98885A (en)
WO (1) WO1992004371A1 (en)
ZA (1) ZA917096B (en)

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US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
SE9301911D0 (en) * 1993-06-03 1993-06-03 Ab Astra NEW PEPTIDE DERIVATIVES
US5780631A (en) * 1993-06-03 1998-07-14 Astra Aktiebolag Starting materials in the synthesis of thrombin and kininogenase inhibitors
GB9318637D0 (en) * 1993-09-08 1993-10-27 Ferring Res Ltd Enzyme inhibitors
US5486623A (en) 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
SE9404196D0 (en) * 1994-12-02 1994-12-02 Astra Ab New antithrombotic formulation
US6025472A (en) * 1994-12-21 2000-02-15 Corvas International, Inc. N-substituted glycine derivatives as enzyme inhibitors
US5696231A (en) * 1994-12-21 1997-12-09 Corvas International, Inc. N-substituted glycine derivatives as enzyme inhibitors
SK56798A3 (en) 1995-10-30 1998-12-02 Smithkline Beecham Corp Protease inhibitors, pharmaceutical composition containing them and their use
US6586466B2 (en) 1995-10-30 2003-07-01 Smithkline Beecham Corporation Carbohydrazide-protease inhibitors
AR005245A1 (en) 1995-12-21 1999-04-28 Astrazeneca Ab THROMBIN INHIBITOR PRODROGES, A PHARMACEUTICAL FORMULATION THAT INCLUDES THEM, THE USE OF SUCH PRODROGES FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND A PROCEDURE FOR ITS PREPARATION
JP2003529528A (en) 1998-04-24 2003-10-07 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 Amino acid amidinohydrazones, alkoxyguanidines, and aminoguanidines as protease inhibitors
YU42401A (en) 1998-12-14 2003-12-31 Ortho-Mcneil Pharmaceuticals Inc. Substituted heterociclic acyl-tripeptides useful as thrombin receptor modulators
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
KR100699404B1 (en) 1999-02-18 2007-03-23 가켄 세야쿠 가부시키가이샤 Novel Amide Derivatives as Growth Hormone Secretagogues
JP2003513972A (en) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
JP2003513924A (en) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
AU1588901A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
SK13632002A3 (en) 2000-03-21 2003-02-04 Smithkline Beecham Corporation C1-6-alkyl-4-amino-azepan-3-one compounds, process for the preparation thereof, pharmaceutical composition comprising the same and intermediates
GB0205527D0 (en) * 2002-03-08 2002-04-24 Ferring Bv Inhibitors
WO2004005318A2 (en) 2002-07-03 2004-01-15 Bio Science International, Inc. Peptides comprising aromatic d-amino acids and methods of use
FR2846969A1 (en) * 2002-11-08 2004-05-14 Salles Jean Pierre New modified active agent derivatives with improved bioavailability comprising parent drug, e.g. anticancer agent, plus fluorinated hydrocarbon chain and recognition or hydrophilizing moiety
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GB0918922D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Aminopyridine derivatives
GB2494851A (en) 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
GB201212081D0 (en) 2012-07-06 2012-08-22 Kalvista Pharmaceuticals Ltd New polymorph
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Also Published As

Publication number Publication date
FI930946A0 (en) 1993-03-03
WO1992004371A1 (en) 1992-03-19
GB9019558D0 (en) 1990-10-24
MC2313A1 (en) 1993-09-27
CA2090858A1 (en) 1992-03-08
PT98885A (en) 1992-08-31
IE913120A1 (en) 1992-03-11
EP0652893A1 (en) 1995-05-17
JPH06501461A (en) 1994-02-17
HU9300610D0 (en) 1993-05-28
HUT64084A (en) 1993-11-29
ZA917096B (en) 1992-04-29
NO930731D0 (en) 1993-02-26
FI930946A (en) 1993-04-26
AU8438791A (en) 1992-03-30

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