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1. WO1996003384 - BIS-NAPHTHALIMIDES WITH LINKERS HAVING HETEROATOMS AND USES THEREOF

Publication Number WO/1996/003384
Publication Date 08.02.1996
International Application No. PCT/US1995/009998
International Filing Date 24.07.1995
Chapter 2 Demand Filed 22.02.1996
IPC
C07D 221/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
221Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/-C07D219/187
02condensed with carbocyclic rings or ring systems
04Ortho- or peri-condensed ring systems
06Ring systems of three rings
14Aza-phenalenes, e.g. 1,8-naphthalimide
C07F 15/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
15Compounds containing elements of Groups 8, 9, 10 or 18 of the Periodic System
CPC
C07D 221/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
221Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
02condensed with carbocyclic rings or ring systems
04Ortho- or peri-condensed ring systems
06Ring systems of three rings
14Aza-phenalenes, e.g. 1,8-naphthalimide
C07F 15/0093
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
15Compounds containing elements of Groups 8, 9, 10 or 18 of the Periodic System
0006compounds of the platinum group
0086Platinum compounds
0093without a metal-carbon linkage
Applicants
  • CTRC RESEARCH FOUNDATION [US]/[US]
Inventors
  • WEIS, Alexander, L.
  • CHEN, Shih-Fong
  • REDDY, Peech, S.
  • MITTAKANTI, Mallaiah
  • DEXTER, Daniel, L.
  • WOYNAROWSKI, Jan, M.
Agents
  • KITCHELL, Barbara, S.
Priority Data
08/279,17322.07.1994US
08/380,84130.01.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BIS-NAPHTHALIMIDES WITH LINKERS HAVING HETEROATOMS AND USES THEREOF
(FR) BIS-NAPHTALIMIDES AVEC SEGMENTS DE LIAISON PRESENTANT DES HETEROATOMES ET UTILISATION DE CES DERNIERS
Abstract
(EN)
The present invention provides novel bis-naphthalimides characterized by having a linker containing a heteroatom, their preparation, pharmaceutical compositions thereof, and various methods of using the bis-naphthalimides. Particularly preferred bis-naphthalimides have a linker of about 8-16 atoms where the heteroatom is oxygen, sulfur, sulfur oxide or sulfur dioxide. The bis-naphthalimides provided herein have exceptional DNA binding properties and demonstrate cytotoxicity in both $i(in vitro) and $i(in vivo) tumor models, in particular, against melanoma. Also provided are novel mono-naphthalimides linked to a DNA alkylating agent. These agents are shown to have conformational effects on double-stranded DNA and to form covalent adducts after an extended incubation period.
(FR)
La présente invention a pour objet des nouveaux bis-naphtalimides caractérisés par un segment de liaison contenant un hétéroatome, la préparation de ces derniers, leurs compositions pharmaceutiques et divers procédés d'utilisation de ces composés. Les bis-naphtalimides préférés comportent un segment de liaison d'environ 8-16 atomes, où l'hétéroatome est de l'oxygène, du soufre, de l'oxyde de soufre ou du dioxyde de soufre. Les bis-naphtalimides prévus présentent une propriété de liaison à l'ADN exceptionnelle, et une cytotoxicité dans les modèles de tumeurs $i(in vitro) et $i(in vivo), en particulier, contre les mélanomes. L'invention se rapporte également à de nouveaux mono-naphtalimides liés à un agent alkylant d'ADN. Ces agents présentent des effets de conformation sur l'ADN à double brins et forment des adduits covalents après une période d'incubation prolongée.
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