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1. WO1998035982 - COMPOUNDS FOR USE IN ADEPT

Publication Number WO/1998/035982
Publication Date 20.08.1998
International Application No. PCT/GB1998/000413
International Filing Date 10.02.1998
Chapter 2 Demand Filed 31.07.1998
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07C 235/52 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
52having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07K 5/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 47/6899
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
6891Pre-targeting systems involving an antibody for targeting specific cells
6899Antibody-Directed Enzyme Prodrug Therapy [ADEPT]
B82Y 5/00
BPERFORMING OPERATIONS; TRANSPORTING
82NANOTECHNOLOGY
YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
5Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
C07C 235/52
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
52having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07K 5/06026
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06008with the first amino acid being neutral
06017and aliphatic
06026the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
C07K 5/06034
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06008with the first amino acid being neutral
06017and aliphatic
06034the side chain containing 2 to 4 carbon atoms
Applicants
  • ZENECA LIMITED [GB]/[GB] (AllExceptUS)
  • DAVIES, David, Huw [GB]/[GB] (UsOnly)
  • DOWELL, Robert, Ian [GB]/[GB] (UsOnly)
  • MARSHAM, Peter, Robert [GB]/[GB] (UsOnly)
  • PEASE, Janet, Elizabeth [GB]/[GB] (UsOnly)
Inventors
  • DAVIES, David, Huw
  • DOWELL, Robert, Ian
  • MARSHAM, Peter, Robert
  • PEASE, Janet, Elizabeth
Agents
  • GILES, Allen, Frank
Priority Data
9703201.515.02.1997GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPOUNDS FOR USE IN ADEPT
(FR) COMPOSES DESTINES A ETRE UTILISES DANS UNE THERAPIE PAR PROMEDICAMENT ENZYMATIQUE DIRIGE CONTRE UN ANTICORPS
Abstract
(EN)
Compounds of Formula (I) wherein A is optionally substituted phenyl or naphthyl; X is a direct bond, CH2 or oxygen; V is NH or O; r is 0-2, provided that when V is O then r is zero; Y1 and Y2 are independently selected from chloro, bromo, iodo, -O-SO2-C1-4alkyl and -O-SO2-phenyl; W is COOH or 1H-1,2,3,4-tetrazol-5-yl; R1 is hydrogen, fluoro, chloro, bromo, C1-4alkyl or C1-4alkoxy; p is 0-4 wherein values of R1 may be the same or different and when p is less than 4 remaining substituent values are hydrogen; R2 is C1-6alkyl, hydroxyC1-6alkyl, phenylC1-6alkyl, C1-4alkoxyC1-4alkyl, phenylC1-4alkoxyC1-4alkyl, C1-4alkylthioC1-4alkyl, phenylC1-4alkylthioC1-4alkyl or carbamoylC1-4alkyl; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, $i(in-vivo) hydrolysable ester or solvate thereof. These compounds are useful for cancer treatment using antibody directed enzyme prodrug therapy (ADEPT), particularly as carboxypeptidase B activatable prodrugs.
(FR)
On décrit des composés de formule (I) dans laquelle, A représente phényle ou naphtyle facultativement substitué; X représente une liaison directe, CH2 ou oxygène; V représente NH ou O; r représente un entier compris entre 0 et 2 à condition que lorsque V représente O, r représente alors zéro; Y1 et Y2 sont indépendamment sélectionnés parmi chloro, bromo, iodo, -O-SO2-C1-4alkyle et -O-SO2-phényl; W représente COOH or 1H-1,2,3,4-tétrazol-5-yle; R1 représente hydrogène, fluoro, chloro, bromo, C1-4alkyle ou C1-4alcoxy; p représente un entier compris entre 0 et 4, les valeurs de R1 pouvant être identiques ou différentes et lorsque p est inférieur à 4, les valeurs de substituant restant représentent hydrogène; R2 représente C1-6alkyle, hydroxyC1-6alkyle, phénylC1-6alkyle, C1-4alcoxyC1-4alkyle, phénylC1-4alcoxyC1-4alkyle, C1-4alkylthio1-4alkyle, phénylC1-4alkylthioC1-4alkyle ou carbamoylC1-4alkyle ou un énantiomère, un diastéréoisomère, un sel pharmaceutiquement acceptable, un ester ou un solvate de ce dernier hydrolysable $i(in vivo). Ces composés sont utiles pour le traitement du cancer à l'aide d'une thérapie par promédicament enzymatique dirigé contre un anticorps et plus particulièrement en tant que promédicaments pouvant être activés par la carboxypeptidase B.
Also published as
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