3-deoxy-mannosamine derivatives
AssigneeFarmitalia Carlo Erba S.p.A.
InventorsNicola Mongelli, Alberto Bargiotti, Nuccia Oneto, Cristina Geroni
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Abstract
The present invention relates to 3-deoxy-derivatives of D-mannosamine of formula ##STR1## wherein R is --NH.sub.2 or a C.sub.2 -.sub.5 alkanoyl-NH-- or CF.sub.3 CONH-- group; each of R.sub.1 and R.sub.2 independently is C.sub.1 -C.sub.4 alkyl, or R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and R.sub.2 is hydrogen or both of R.sub.1 and R.sub.2 are fluorine; and wherein, when R.sub.1 is methoxy and R.sub.2 is hydrogen then R is other than --NH.sub.2, or a pharmaceutically acceptable salt thereof, which are useful as angiogenesis inhibitors, in particular as development of metastasis inhibitors.
Claims5
A compound of formula (I) ##STR15## wherein R is --NH.sub.2 or a C.sub.2 -C.sub.5 alkanoyl-NH-- or CF.sub.3 CONH-- group;
- each of R.sub.1 and R.sub.2 independently is C.sub.1 -C.sub.4 alkyl, or R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and
- R.sub.2 is hydrogen or both of R.sub.1 and R.sub.2 are fluorine;
- and wherein, when R.sub.1 is methoxy and R.sub.2 is hydrogen then R is other than --NH.sub.2, or a pharmaceutically acceptable salt thereof.
A compound selected from the group consisting of:
- 2-amino-2,3-dideoxy-D-mannopyranose;
- 2-acetamido-2,3-dideoxy-D-mannopyranose;
- 2-amino-2,3-dideoxy-3-iodo-D-mannopyranose;
- 2-acetamido-2,3-dideoxy-3-iodo-D-mannopyranose;
- 2-acetamido-2-deoxy-3-0-methyl-D-mannopyranose;
- 2-amino-2,3-dideoxy-3-fluoro-D-mannopyranose;
- 2-acetamido-2,3-dideoxy-3-fluoro-D-mannopyranose;
- 2-amino-2,3-dideoxy-3-C-methyl-D-mannopyranose;
- 2-acetamido-2,3-dideoxy-3-C-methyl-D-mannopyranose;
- 2-amino-2,3-dideoxy-3-C-ethyl-D-mannopyranose;
- 2-acetamido-2,3-dideoxy-3-C-ethyl-D-mannopyranose;
- 2-amino-2,3-dideoxy-3,3-C-dimethyl-D-mannopyranose;
- 2-acetamido-2,3-dideoxy-3,3-C-dimethyl-D-mannopyranose;
- 2-amino-2,3-dideoxy-3,3-difluoro-D-mannopyranose;
- 2-acetamido-2,3-dideoxy-3,3-difluoro-D-mannopyranose;
- or, a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising, as an active agent, a compound of formula (I) ##STR16## wherein R is --NH.sub.2 or a C.sub.2 -C.sub.5 alkanoyl-NH-- or CF.sub.3 CONH-- group;
- each of R.sub.1 and R.sub.2, independently, is C.sub.1 -C.sub.4 alkyl, or R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy and R.sub.2 is hydrogen or both of R.sub.1 and R.sub.2 are fluorine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and/or diluent.
Dependencies are inferred from the claim text.