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1. WO2011001052 - NOVEL CONJUGATES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF

Publication Number WO/2011/001052
Publication Date 06.01.2011
International Application No. PCT/FR2010/050986
International Filing Date 20.05.2010
IPC
C07D 273/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
273Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/-C07D271/183
08having two nitrogen atoms and more than one oxygen atom
A61K 31/395 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/395
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/496
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 245/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
245Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
04condensed with carbocyclic rings or ring systems
06condensed with one six-membered ring
C07D 273/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
273Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
08having two nitrogen atoms and more than one oxygen atom
Applicants
  • SANOFI [FR]/[FR] (AllExceptUS)
  • BOUCHARD, Hervé [FR]/[FR] (UsOnly)
  • BRUN, Marie-Priscille [FR]/[FR] (UsOnly)
  • COMMERÇON, Alain [FR]/[FR] (UsOnly)
  • ZHANG, Jidong [FR]/[FR] (UsOnly)
Inventors
  • BOUCHARD, Hervé
  • BRUN, Marie-Priscille
  • COMMERÇON, Alain
  • ZHANG, Jidong
Agents
  • SENNINGER, Thierry
Priority Data
090317029.06.2009FR
090565125.11.2009FR
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) NOVEL CONJUGATES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
(FR) NOUVEAUX CONJUGUES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
Abstract
(EN)
The invention relates to a targeting agent, to which at least one cryptophycin is attached, of the formula (I), where: R1 is a halogen atom and R2 is an OH group, an acyl group derived from an amino acid AA or a (C1-C4)alkanoyloxy group; or else R1 and R2 together form an epoxy unit; AA denotes a natural or artificial amino acid; R3 is a (C1-C6)alkyl group; R4 and R5 are both H or together form a CH=CH double bond between C13 and C14; R6 and R7 are, independently from one another, H or a (C1-C6)alkyl group; R8 and R9 are, independently from one another, H or a (C1-C6)alkyl group; R10 is at least one substituent of the phenyl core selected from among: H, an OH group, (C1-C4)alkoxy, a halogen atom or a NH2, NH(C1-C6)alkyl, or N(C1-C6)alkyl group; R11 is at least one substituent of the phenyl core selected from among H or a (C1- C4)alkyl group; the targeting agent and the cryptophycin derivative being covalently bonded, the bond being located at the ortho (o), meta (m), or para (p) position of the phenyl core containing the CR1 unit.
(FR)
L'invention est relative à un agent de ciblage auquel est attaché au moins un dérivé de cryptophycine de formule (I) : dans laquelle : R1 représente un atome d'halogène et R2 représente un groupe -OH, un groupe acyle dérivé d'un acide aminé AA ou un groupe (C1-C4)alcanoyloxy; ou bien R1 et R2 forment ensemble un motif époxyde; AA désigne un acide aminé naturel ou non-naturel; R3 représente un groupe (C1-C6)alkyle; R4 et R5 représentent tous deux H ou forment ensemble une double liaison CH=CH entre C13 et C14; R6 et R7 représentent indépendamment l'un de l'autre H ou un groupe (C1-C6)Jalkyle; R8 et R9 représentent indépendamment l'un de l'autre H ou un groupe (C1-C6)alkyle; R10 représente au moins un substituant du noyau phényle choisi parmi : H, un groupe OH, (C1-C4)alcoxy, un atome d'halogène ou bien un groupe -NH2, -NH(C1-C6)alkyle ou -N(C1- C6)alkyle2; R11 représente au moins un substituant du noyau phényle choisi parmi H ou un groupe (C1- C4)alkyle; l'agent de ciblage et le dérivé de cryptophycine étant attachés de façon covalente, l'attachement se situant en position ortho (o), meta (m) ou para (p) du noyau phényle porteur du motif CR1.
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