Derivatives of oxazaphosphorines and therapeutic uses thereof

Patent metadata

Field	Value
Publication number	US-10098901-B2
Application number	US-201515310455-A
Country	US
Kind code	B2
Filing date	May 13, 2015
Priority date	May 14, 2014
Publication date	Oct 16, 2018
Grant date	Oct 16, 2018

Abstract

The present invention relates to novel derivatives of oxazaphosphorines, pharmaceutical compositions and therapeutic uses thereof, in particular for treating or preventing cancer.

First claim

The invention claimed is:

1. A compound of formula (I):

wherein:
A is selected from the group consisting of:
O, S, —O—(C═S)—S—, —ONH—, —ONR′—, —NR′O—, —NHO—,
Y 1 —(CH 2 ) n —Y 2 , where n is an integer from 1 to 8, and
Y 1 —(CH 2 —CH 2 —O) a —CH 2 —CH 2 —Y 2 where a is an integer from 1 to 5,
wherein Y 1 and Y 2 are independently selected from —O—, —NH—, —S—, —OC(O)—, —C(O)NH—, —NHC(O)—, —O—C(S)—S—, S—C(S)—O—NR′—, —ONH—, —NHO—, —ONR′—, —NR′O—, —OC(O)—O—, NR′C(S)S—, —SC(S)NR′—, —NR′C(O)—, —C(O)NR′— and —C(O)O—, and R′ is a C 1 -C 6 alkyl,
and wherein —R 1 , R 2 and R 3 are independently selected from the group consisting of —H, —CH(CH 3 )—CH 2 —X and —(CH 2 ) 2 —X, X being a halogen atom,
or a pharmaceutically acceptable salt or solvate thereof.

2. A compound selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

3. A pharmaceutical composition comprising a compound as an active ingredient and a pharmaceutically acceptable excipient, wherein the compound is:

Assignees

• Roussy Inst Gustave

Inventors

• Paci Angelo
• Martens Thierry
• Rivard Michael
• Desmaele Didier
• Skarbek Charles
• Couvreur Patrick

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61K47/54

  the modifying agent being an organic compound · CPC title

• A61K31/664 Primary

  Amides of phosphorus acids · CPC title

• A61K31/185

  Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids (hydroxamic acids A61K31/16; peroxy acids A61K31/327) · CPC title

• C07F9/65846

  the phosphorus atom being part of a six-membered ring which may be condensed with another ring system · CPC title