AR024472A1 - INHIBITORS OF THE INTEGRIN ALFAV BETA6. - Google Patents

INHIBITORS OF THE INTEGRIN ALFAV BETA6.

Info

Publication number
AR024472A1
AR024472A1 ARP000103177A ARP000103177A AR024472A1 AR 024472 A1 AR024472 A1 AR 024472A1 AR P000103177 A ARP000103177 A AR P000103177A AR P000103177 A ARP000103177 A AR P000103177A AR 024472 A1 AR024472 A1 AR 024472A1
Authority
AR
Argentina
Prior art keywords
ala
asp
arg
phe
gly
Prior art date
Application number
ARP000103177A
Other languages
Spanish (es)
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 AR024472A1 publication Critical patent/AR024472A1/en

Links

Classifications

    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Péptidos de la formula 1, que son biologicamente activos como ligandos de la integrina alfav beta6 Ac-Arg-X1-Asp-X2-X3-X4-X5-X6-NH2 (1) donde Ac significaacetilo, X1 significa Ser, Gly, Thr, Asp, Arg, Val, Tyr, His o Ala, X2 significa Leu, Ile, Nle,Val o Phe, X3 significa Asp, Glu, Lys, Phe, Aib, Nal, Gly, Ala,Bgl o Phg, X4 significa Gly, Ala, Ser, beta-Ala o omega-Abu, X5 significa Leu, Ile, Nle, Val o Phe, X6 significa Arg, Har, Lys, Orn, Phe, Ala, Tyr, Gly, Ser oAsp donde los aminoácidosmen cionados también pueden ser derivatizados los radicales de los aminoácidos están unidos entre sí en forma de péptido por medio delos grupos alfa-amino y alfa-carboxi, están incluidos tanto las formas D como las L de los radicales aminoácidoopticamen te activos, así como sus sales, ydonde queda excluido Ac-Arg-Thr-Asp-Leu-Asp-Ser-Leu-Arg-NH2. Los péptidos de acuerdo con la invencion se pueden aplicar como inhibidores efectivos del receptoralfav beta6 y, por lo tanto, se pueden emplearpara el tra tamiento de diversas enfermedades y estados patologicos.Peptides of formula 1, which are biologically active as ligands of the alpha6 integrin beta6 Ac-Arg-X1-Asp-X2-X3-X4-X5-X6-NH2 (1) where Ac means acetyl, X1 means Ser, Gly, Thr , Asp, Arg, Val, Tyr, His or Ala, X2 means Leu, Ile, Nle, Val or Phe, X3 means Asp, Glu, Lys, Phe, Aib, Nal, Gly, Ala, Bgl or Phg, X4 means Gly , Ala, Ser, beta-Ala or omega-Abu, X5 means Leu, Ile, Nle, Val or Phe, X6 means Arg, Har, Lys, Orn, Phe, Ala, Tyr, Gly, Ser oAsp where amino acids are also linked The amino acid radicals can be derivatized together in the form of a peptide by means of the alpha-amino and alpha-carboxy groups, both D and L forms of the optically active amino acid radicals, as well as their salts, are included, and where Ac-Arg-Thr-Asp-Leu-Asp-Ser-Leu-Arg-NH2 is excluded. The peptides according to the invention can be applied as effective inhibitors of the beta6 receptor and, therefore, can be used for the treatment of various diseases and pathological conditions.

ARP000103177A 1999-06-26 2000-06-23 INHIBITORS OF THE INTEGRIN ALFAV BETA6. AR024472A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19929410A DE19929410A1 (en) 1999-06-26 1999-06-26 New octapepide compounds as alpha v beta 6 integrin inhibitors useful for treating and diagnosing heart disease, tumors, osteoporosis, fibrosis, inflammation, infection and psoriasis

Publications (1)

Publication Number Publication Date
AR024472A1 true AR024472A1 (en) 2002-10-02

Family

ID=7912712

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000103177A AR024472A1 (en) 1999-06-26 2000-06-23 INHIBITORS OF THE INTEGRIN ALFAV BETA6.

Country Status (17)

Country Link
EP (1) EP1189930A1 (en)
JP (1) JP2003503422A (en)
KR (1) KR20020015704A (en)
CN (1) CN1358195A (en)
AR (1) AR024472A1 (en)
AU (1) AU771099B2 (en)
BR (1) BR0011954A (en)
CA (1) CA2377224A1 (en)
CZ (1) CZ20014484A3 (en)
DE (1) DE19929410A1 (en)
HU (1) HUP0201729A3 (en)
MX (1) MXPA01013247A (en)
NO (1) NO20016341L (en)
PL (1) PL352374A1 (en)
SK (1) SK18722001A3 (en)
WO (1) WO2001000660A1 (en)
ZA (1) ZA200200673B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6972296B2 (en) 1999-05-07 2005-12-06 Encysive Pharmaceuticals Inc. Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
JP2007523835A (en) 2003-02-06 2007-08-23 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフトング Peptidesulfonamide
GB0520068D0 (en) * 2005-10-03 2005-11-09 Cancer Res Technology av peptide ligand
ES2746925T3 (en) 2006-08-03 2020-03-09 Medimmune Ltd Antibodies Directed Towards alfaVbeta6 and Use of Them
ES2906109T3 (en) 2016-11-01 2022-04-13 Arrowhead Pharmaceuticals Inc Alpha-v beta-6 integrin ligands and uses thereof
EP3703700A4 (en) 2017-11-01 2021-08-04 Arrowhead Pharmaceuticals, Inc. Integrin ligands and uses thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2103139A1 (en) * 1991-05-14 1992-11-15 George A. Heavner Peptide inhibitors of inflammation
ATE511850T1 (en) * 1997-08-08 2011-06-15 Univ California TREATMENT OF BLADDER FIBROSIS WITH ANTIBODIES TO ALPHA-V BETA-6 INTEGRIN
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
NO20016341D0 (en) 2001-12-21
PL352374A1 (en) 2003-08-25
BR0011954A (en) 2002-05-07
EP1189930A1 (en) 2002-03-27
CN1358195A (en) 2002-07-10
CA2377224A1 (en) 2001-01-04
MXPA01013247A (en) 2002-07-02
CZ20014484A3 (en) 2002-04-17
KR20020015704A (en) 2002-02-28
SK18722001A3 (en) 2002-05-09
AU6263000A (en) 2001-01-31
DE19929410A1 (en) 2000-12-28
HUP0201729A2 (en) 2002-08-28
HUP0201729A3 (en) 2005-01-28
AU771099B2 (en) 2004-03-11
WO2001000660A1 (en) 2001-01-04
NO20016341L (en) 2002-02-25
ZA200200673B (en) 2003-04-24
JP2003503422A (en) 2003-01-28

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