NO20020176L - Cyclic peptide derivatives as inhibitors of intergrin <alfa> v <beta> 6 - Google Patents

Cyclic peptide derivatives as inhibitors of intergrin <alfa> v <beta> 6

Info

Publication number
NO20020176L
NO20020176L NO20020176A NO20020176A NO20020176L NO 20020176 L NO20020176 L NO 20020176L NO 20020176 A NO20020176 A NO 20020176A NO 20020176 A NO20020176 A NO 20020176A NO 20020176 L NO20020176 L NO 20020176L
Authority
NO
Norway
Prior art keywords
phe
peptide derivatives
intergrin
alfa
inhibitors
Prior art date
Application number
NO20020176A
Other languages
Norwegian (no)
Other versions
NO20020176D0 (en
Inventor
Alfred Jonczyk
Beate Diefenbach
Simon Goodman
Ulrich Groth
Gunther Zischinsky
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of NO20020176L publication Critical patent/NO20020176L/en
Publication of NO20020176D0 publication Critical patent/NO20020176D0/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Oppfinnelsen vedrører nye peptidderivater med formel (I): syklo-(Arg-X'-Asp-X2-X3-X4-X5-X6-R1); som er biologisk aktive som Ugander for integrin avp6) X1 er Ser, Gly eller Thr; X2 er Leu, Ile, Nle, Val eller Phe; X3 er Asp, Glu, Lys eller Phe; X4 er Gly, Ala eller Ser; X5 er Leu, Ile, Nle, Val eller Phe; X6 er Arg, Har eller Lys; og R1 er utelatt eller er ett eller flere co-amino- karboksylsyreradikaler, hvor o-aminokarboksyl- syreradikalet eller -radikalene er fra 500 til 2500 pm lange. Aminosyrene kan også være derivatisert og D- og L-formene av de optisk aktive aminosyreradikalene er omfattet. Oppfinnelsen vedrører også de fysiologisk egnede salter og solvater av derivatene ifølge oppfinnelsen.The invention relates to novel peptide derivatives of formula (I): cyclo- (Arg-X'-Asp-X2-X3-X4-X5-X6-R1); which are biologically active as Ugander for integrin avp6) X1 is Ser, Gly or Thr; X 2 is Leu, Ile, Nle, Val or Phe; X3 is Asp, Glu, Lys or Phe; X 4 is Gly, Ala or Ser; X5 is Leu, Ile, Nle, Val or Phe; X6 is Arg, Har or Lys; and R1 is omitted or is one or more co-amino carboxylic acid radicals, wherein the o-amino carboxylic acid radical or radicals are from 500 to 2500 µm long. The amino acids may also be derivatized and the D and L forms of the optically active amino acid radicals are included. The invention also relates to the physiologically suitable salts and solvates of the derivatives according to the invention.

NO20020176A 1999-07-15 2002-01-14 Cyclic peptide derivatives as inhibitors of intergrin <alfa> v <beta> 6 NO20020176D0 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19933173A DE19933173A1 (en) 1999-07-15 1999-07-15 Cyclic peptide derivatives as inhibitors of the integrin alpha¶v¶beta¶6¶
PCT/EP2000/006188 WO2001005810A2 (en) 1999-07-15 2000-07-03 CYCLIC PEPTIDE DERIVATIVES AS INHIBITORS OF INTEGRIN αVβ¿6?

Publications (2)

Publication Number Publication Date
NO20020176L true NO20020176L (en) 2002-01-14
NO20020176D0 NO20020176D0 (en) 2002-01-14

Family

ID=7914891

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20020176A NO20020176D0 (en) 1999-07-15 2002-01-14 Cyclic peptide derivatives as inhibitors of intergrin <alfa> v <beta> 6

Country Status (23)

Country Link
EP (2) EP1196433B1 (en)
JP (1) JP2003505395A (en)
KR (1) KR20020010928A (en)
CN (1) CN1361792A (en)
AR (1) AR024742A1 (en)
AT (1) ATE340803T1 (en)
AU (1) AU772782C (en)
BR (1) BR0012418A (en)
CA (1) CA2379022A1 (en)
CZ (1) CZ200226A3 (en)
DE (2) DE19933173A1 (en)
DK (1) DK1196433T3 (en)
ES (1) ES2273703T3 (en)
HK (1) HK1048641A1 (en)
HU (1) HUP0201925A3 (en)
MX (1) MXPA02000465A (en)
NO (1) NO20020176D0 (en)
PL (1) PL354363A1 (en)
PT (1) PT1196433E (en)
SK (1) SK262002A3 (en)
TW (1) TWI226890B (en)
WO (1) WO2001005810A2 (en)
ZA (1) ZA200201275B (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002232176B2 (en) * 2001-02-19 2006-06-15 Takara Bio Inc. Cyclic peptide
DE10118550A1 (en) * 2001-04-14 2002-10-17 Merck Patent Gmbh New 3-ethanoylamino-3-phenyl-propionic acid derivatives, are integrin agonists or antagonists useful e.g. for treating angiogenic, cardiovascular, inflammatory, osteolytic or tumor diseases or infections
US7538084B2 (en) 2003-03-17 2009-05-26 Amr Technology, Inc. Cyclosporins
ATE399542T1 (en) * 2003-10-01 2008-07-15 Merck Patent Gmbh ALFAVBETA3 AND ALFAVBETA6 INTEGRIN ANTAGONISTS AS ANTIFIBROTIC AGENTS
ES2436170T3 (en) * 2003-12-03 2013-12-27 The Scripps Research Institute Antibodies and peptides specific for integrin alfa II beta3
JP2008514701A (en) 2004-09-29 2008-05-08 エーエムアール テクノロジー インコーポレイテッド Cyclosporine alkyne analogs and their pharmaceutical use
JP2008514702A (en) 2004-09-29 2008-05-08 エーエムアール テクノロジー インコーポレイテッド Novel cyclosporine analogues and their pharmaceutical use
JP2008515886A (en) 2004-10-06 2008-05-15 エーエムアール テクノロジー インコーポレイテッド Cyclosporine alkynes and their usefulness as medical drugs
GB0520068D0 (en) 2005-10-03 2005-11-09 Cancer Res Technology av peptide ligand
US7696165B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders
US7696166B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders
EP2064244B1 (en) 2006-08-03 2019-06-05 MedImmune Limited ANTIBODIES DIRECTED TO alphaVbeta6 AND USES THEREOF
EP2784511A1 (en) 2013-03-27 2014-10-01 Universität Zürich Integrin alpha-v-beta6 for diagnosis/prognosis of colorectal carcinoma
SI3350222T1 (en) 2015-09-18 2022-01-31 Technische Universitaet Muenchen Ligands for integrin avbeta6, synthesis and uses thereof
MA52117A (en) 2017-02-28 2022-04-06 Morphic Therapeutic Inc INHIBITORS OF INTEGRIN (ALPHA-V) (BETA-6)
MX394210B (en) 2017-02-28 2025-03-04 Morphic Therapeutic Inc Inhibitors of (alpha-v)(beta-6) integrin
US11332498B2 (en) 2017-03-17 2022-05-17 Technische Universitat Munchen Ligands for integrin αVβ8, synthesis and uses thereof
GB201706472D0 (en) * 2017-04-24 2017-06-07 Cancer Res Tech Ltd Tumour-targeting peptide variants
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
WO2020047239A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. INHIBITING αV β6 INTEGRIN
SI3844162T1 (en) 2018-08-29 2025-06-30 Morphic Therapeutic, Inc. Inhibitors of alpha v beta6 integrin
WO2021180969A1 (en) * 2020-03-12 2021-09-16 Technische Universität München Cyclic peptides and their conjugates for addressing alpha-v-beta-6 integrin in vivo

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4472305A (en) 1983-05-17 1984-09-18 Sterling Drug Inc. Hexapeptide amides
DE4310643A1 (en) 1993-04-01 1994-10-06 Merck Patent Gmbh Cyclic adhesion inhibitors
DE19538741A1 (en) 1995-10-18 1997-04-24 Merck Patent Gmbh Cyclopeptide derivatives
CZ20012212A3 (en) * 1998-12-19 2001-09-12 Merck Patent Gmbh Peptidic compound, use thereof and pharmaceutical preparation in which the compound is comprised

Also Published As

Publication number Publication date
CZ200226A3 (en) 2002-04-17
JP2003505395A (en) 2003-02-12
KR20020010928A (en) 2002-02-06
MXPA02000465A (en) 2002-07-30
DK1196433T3 (en) 2007-02-12
HK1048641A1 (en) 2003-04-11
CA2379022A1 (en) 2001-01-25
PL354363A1 (en) 2004-01-12
TWI226890B (en) 2005-01-21
ES2273703T3 (en) 2007-05-16
EP1196433B1 (en) 2006-09-27
AU772782C (en) 2005-01-27
AU5823600A (en) 2001-02-05
AU772782B2 (en) 2004-05-06
PT1196433E (en) 2007-01-31
DE19933173A1 (en) 2001-01-18
NO20020176D0 (en) 2002-01-14
CN1361792A (en) 2002-07-31
ZA200201275B (en) 2003-08-22
BR0012418A (en) 2002-03-26
HUP0201925A2 (en) 2002-10-28
HUP0201925A3 (en) 2002-11-28
EP1754714A1 (en) 2007-02-21
ATE340803T1 (en) 2006-10-15
AR024742A1 (en) 2002-10-23
WO2001005810A2 (en) 2001-01-25
DE50013525D1 (en) 2006-11-09
WO2001005810A3 (en) 2001-05-17
SK262002A3 (en) 2002-07-02
EP1196433A2 (en) 2002-04-17

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