The present invention relates to a process for the preparation of high pure Eribulin and Eribulin Mesylate. The present invention involves preparation of high pure Eribulin and its mesylate salt involving chiral acid addition salts of Eribulin.

The present invention relates to a process for the preparation of high pure Eribulin and Eribulin Mesylate. The present invention involves preparation of high pure Eribulin and its mesylate salt involving chiral acid addition salts of Eribulin.

The present invention relates to novel compounds, compositions containing same and methods for inhibiting STAT3 and/or STAT5 activity or for the treatment of a cell proliferative disorder such as a cancer using a compound of formula I

##STR00001##

or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein R and R.sub.1, different, are selected from the group consisting of

##STR00002## wherein when one of R and R.sub.1 is a —H, the other of R and R.sub.1 is a cyclopentyl moiety, R.sub.2 is a benzyl substituted with 1-5 halogens, preferably —Cl or —F, and R.sub.3 is selected from the group consisting of —H or —OH.

The present invention relates to novel compounds, compositions containing same and methods for inhibiting STAT3 and/or STAT5 activity or for the treatment of a cell proliferative disorder such as a cancer using a compound of formula I

##STR00001##

or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein R and R.sub.1, different, are selected from the group consisting of

##STR00002## wherein when one of R and R.sub.1 is a —H, the other of R and R.sub.1 is a cyclopentyl moiety, R.sub.2 is a benzyl substituted with 1-5 halogens, preferably —Cl or —F, and R.sub.3 is selected from the group consisting of —H or —OH.

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

In one aspect, the present disclosure provides methods of preparing a secondary amine. In some embodiments, the secondary amine comprises two different groups or two identifical groups. Also provided herein are compositions for use in the preparation of the secondary amine.

In one aspect, the present disclosure provides methods of preparing a secondary amine. In some embodiments, the secondary amine comprises two different groups or two identifical groups. Also provided herein are compositions for use in the preparation of the secondary amine.

Compounds of Formula (Ia)

##STR00001##

wherein R is a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl, a C.sub.1-C.sub.6 substituted or unsubstituted alkyl or —NR′R′,
Q is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2 (CH2)p
Y is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2 (CH2)p
Z is H or C.sub.1-C.sub.4 alkyl,
R′ is H, C(O), S(O).sub.2, C(O).sub.2, a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl or a C.sub.1-C.sub.6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C.sub.6-C.sub.12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

Compounds of Formula (Ia)

##STR00001##

wherein R is a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl, a C.sub.1-C.sub.6 substituted or unsubstituted alkyl or —NR′R′,
Q is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2 (CH2)p
Y is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2 (CH2)p
Z is H or C.sub.1-C.sub.4 alkyl,
R′ is H, C(O), S(O).sub.2, C(O).sub.2, a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl or a C.sub.1-C.sub.6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C.sub.6-C.sub.12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.