PE45295A1 - PROTEASE INHIBITING PEPTIDES - Google Patents

PROTEASE INHIBITING PEPTIDES

Info

Publication number
PE45295A1
PE45295A1 PE1995260194A PE26019495A PE45295A1 PE 45295 A1 PE45295 A1 PE 45295A1 PE 1995260194 A PE1995260194 A PE 1995260194A PE 26019495 A PE26019495 A PE 26019495A PE 45295 A1 PE45295 A1 PE 45295A1
Authority
PE
Peru
Prior art keywords
alkyl
compounds
formula
aralkyl
aryl
Prior art date
Application number
PE1995260194A
Other languages
Spanish (es)
Inventor
Rainer Metternich
Anette Wienand
Carlo Tapparelli
Original Assignee
Sandoz Ag
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 Sandoz Ag filed Critical Sandoz Ag
Publication of PE45295A1 publication Critical patent/PE45295A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Physics & Mathematics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I DONDE: 1) Y1, Y2 SON OH, F, o FORMAN UNA PORCION DERIVADA DE UN COMPUESTO DIHIDROXI; 2) R1 ES -(CH2)2-X, -CH(CH3)-(CH2)2-X, -CH2-CH(CH3)-(CH2)2-X, Y OTROS, DONDE X ES NH2, -NH-C(NH)-NH2, -S-C(NH)-NH2; 3) r, o, p, q SON 0 o 1; m ES 1 o 2; 4) A, A2, A3 SON AMINOACIDOS; 5) W ES UN GRUPO QUELANTE UNIDO AL GRUPO AMINO TERMINAL, QUE PUEDE SER DE FORMULA W`-CH2-Xa-NH, SIENDO W' UN QUELANTE DERIVADO DE ACIDO o ANHIDRIDO POLIAMINO-POLIACETICO NO CICLICO o CICLICO Y Xa ES FENILENO o ALQUILENO C1-C3; 6) Z ES UN ENLACE DIRECTO O UN SEPARADOR; Y A COMPUESTOS DE FORMULA II, DONDE: 1) Y ES UNA SECUENCIA DE AMINOACIDOS; 2) Q1 Y Q2 SE SELECCIONAN DE OH, COR2, -CONR2R3, -NR2R3, -OR6; DONDE R2, R3, R6 SON ALQUILO C1-C10, ARILO C6-C10, ARALQUILO C6-C10, FENILO SUSTITUIDO o Q1 Y Q2 TOMADOS JUNTOS FORMAN UN RESIDUO DIOL; 3) R4 ES H, ALQUILO C1-C10; 4) R5 ES -Z1-X1, DONDE Z1 ES UN ALQUILO QUE PUEDE ESTAR RAMIFICADO, ARILO o ARALQUILO Y X1 ES NH2, -NH-C(NH)-NH2, -S-C-(NH)-NH2, -N3, ALCOXI Y OTROS; ESTOS COMPUESTOS PUEDEN SER UTILES COMO INHIBIDORES DE PROTEASAS DE SERINA, TAL COMO TROMBINA, O COMO AGENTES DE DIAGNOSTICO, AL PODER UNIRSE EL QUELATO A UN METAL POSIBLE DE DETECTAR, PERMITIENDO LA VISUALIZACION DE TROMBOSIT REFERS TO COMPOUNDS OF FORMULA I WHERE: 1) Y1, Y2 ARE OH, F, or FORM A PORTION DERIVED FROM A DIHYDROXY COMPOUND; 2) R1 IS - (CH2) 2-X, -CH (CH3) - (CH2) 2-X, -CH2-CH (CH3) - (CH2) 2-X, AND OTHERS, WHERE X IS NH2, -NH -C (NH) -NH2, -SC (NH) -NH2; 3) r, o, p, q ARE 0 or 1; m IS 1 or 2; 4) A, A2, A3 ARE AMINO ACIDS; 5) W IS A CHELANT GROUP JOINED TO THE TERMINAL AMINO GROUP, WHICH MAY BE OF THE FORMULA W`-CH2-Xa-NH, W IS A CHELANT DERIVED FROM A POLYAMINE-POLYACETIC ACID OR NON-CYCLICAL OR ANKYLENE AND Xa IS PHENYLENE OR ALKYLENE C1-C3; 6) Z IS A DIRECT LINK OR A SPACER; AND TO COMPOUNDS OF FORMULA II, WHERE: 1) AND IT IS A SEQUENCE OF AMINO ACIDS; 2) Q1 AND Q2 ARE SELECTED FROM OH, COR2, -CONR2R3, -NR2R3, -OR6; WHERE R2, R3, R6 ARE ALKYL C1-C10, ARYL C6-C10, ARALKYL C6-C10, SUBSTITUTED PHENYL or Q1 AND Q2 TAKEN TOGETHER FORM A DIOL WASTE; 3) R4 IS H, C1-C10 ALKYL; 4) R5 IS -Z1-X1, WHERE Z1 IS AN ALKYL THAT MAY BE BRANCHED, ARYL or ARALKYL AND X1 IS NH2, -NH-C (NH) -NH2, -SC- (NH) -NH2, -N3, ALCOXI AND OTHERS; THESE COMPOUNDS MAY BE USEFUL AS SERINE PROTEASE INHIBITORS, SUCH AS THROMBINE, OR AS DIAGNOSTIC AGENTS, BY BEING ABLE TO JOIN THE CHELATE TO A METAL POSSIBLE TO DETECT, ALLOWING THE DISPLAY OF THROMBS

PE1995260194A 1994-01-26 1995-01-24 PROTEASE INHIBITING PEPTIDES PE45295A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB9401483A GB9401483D0 (en) 1994-01-26 1994-01-26 Organic compounds

Publications (1)

Publication Number Publication Date
PE45295A1 true PE45295A1 (en) 1995-12-29

Family

ID=10749357

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1995260194A PE45295A1 (en) 1994-01-26 1995-01-24 PROTEASE INHIBITING PEPTIDES

Country Status (10)

Country Link
EP (1) EP0741747A1 (en)
JP (1) JPH09509653A (en)
AU (1) AU1576495A (en)
CA (1) CA2179889A1 (en)
GB (1) GB9401483D0 (en)
IL (1) IL112423A0 (en)
PE (1) PE45295A1 (en)
SG (1) SG47079A1 (en)
WO (1) WO1995020603A1 (en)
ZA (1) ZA95636B (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9515489D0 (en) * 1995-07-28 1995-09-27 Sandoz Ltd Organic compounds
DE10046514A1 (en) 2000-09-15 2002-04-25 Diagnostikforschung Inst Process for imaging and diagnosis of thrombi using magnetic resonance imaging using particulate contrast media
MXPA05002662A (en) 2002-09-09 2005-09-20 Trigen Ltd Multivalent metal salts of boronic acids for treating thrombosis.
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7223745B2 (en) 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
WO2011087822A1 (en) 2009-12-22 2011-07-21 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
UA124672C2 (en) 2016-06-21 2021-10-27 Оріон Офтальмолоджі Ллс Heterocyclic prolinamide derivatives
JP7164521B2 (en) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー carbocyclic prolinamide derivatives

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4668503A (en) * 1982-07-26 1987-05-26 Trustees Of University Of Massachusetts Process for labeling amines with 99m Tc
US5187157A (en) * 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
DE69023394T2 (en) * 1989-06-16 1996-07-04 Merck Frosst Canada Inc Chelate derivatives of atrial-natriurethic factor (ANF).
GB9017694D0 (en) * 1990-08-13 1990-09-26 Sandoz Ltd Improvements in or relating to organic chemistry
US5252721A (en) * 1990-09-28 1993-10-12 Neorx Corporation S3 N chelating compounds
EP0584256B1 (en) * 1991-04-22 1999-11-10 Mallinckrodt Medical, Inc. Compounds and pharmaceutical compositions for detecting and localizing tissues having neurokinine 1 receptors

Also Published As

Publication number Publication date
CA2179889A1 (en) 1995-08-03
GB9401483D0 (en) 1994-03-23
EP0741747A1 (en) 1996-11-13
JPH09509653A (en) 1997-09-30
AU1576495A (en) 1995-08-15
IL112423A0 (en) 1995-03-30
WO1995020603A1 (en) 1995-08-03
ZA95636B (en) 1996-07-26
SG47079A1 (en) 1998-03-20

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Legal Events

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FG Grant, registration
FD Application declared void or lapsed