Bristol-myers Squibb Compnay

Vion Pharmaceuticals, Inc.

Other

Yale University

Florida State University Research Foundation, Inc.

Shu-Hui Chen

Vittorio Farina

Michael A Poss

Jianmei Wei

David J Kucera

Jerome L Moniot

Ivan D Trifunovich

John K Thottahil

Xiuyan Li

John F Kadow

Dolatrai M Vyas

Terrence W Doyle

Joydeep Kant

Gregory P Roth

Jun Li

Robert A Holton

David R Langley

Mark D Wittman

Alan C Sartorelli

Krishnamurthy Shyam

Philip G Penketh

Chuan-Sheng Niu

ChuanSheng Niu

Methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Compounds prepared by the methods of the present invention are also disclosed.

Method for the preparation of novel sidechain-bearing taxanes and intermediates thereof

Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.

Methods for the preparation of novel sidechain-bearing taxanes and

The present invention relates to a compound of the formula wherein R.sup.1 and R.sup.2 are selected from lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms; R.sup.3 is a substituted or unsubstituted lower alkyl group having 1-6 carbons; and R.sup.4 is selected from substituted or unsubstituted lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms. The present invention also relates to a pharmaceutical composition comprising the above compound, as well as a method of treating tumor cells with the compound.

N,n-bis(sulfonyl)hydrazines useful as antineoplastic agents

The present invention relates to methods for substantially enhancing the stereoselective synthesis of .beta.-anomeric nucleoside analogs. In methods according to the present invention, the introduction of a phenylseleno group onto a blocked lactone sugar precursor may be selected so that the desirable phenylseleno substituent is introduced on the side of the blocked lactone away from the blocking group. This stereospecific introduction of the phenylseleno group in sugar precursor allows the synthesis of nucleoside analogs and in particular, 2',3',-dideoxy- and 2',3'-dideoxy-2',3'-didehydronucleoside analogs in very high yield. In certain preferred embodiments, the preferred phenylseleno blocked lactone is obtained in an amount representing approximately 90% or more of the total amount of the stereoisomers obtained. In even more preferred embodiments, the amount of the preferred stereoisomer is at least 95%, even more preferably at least about 97% of the total amount of phenylseleno blocked lactone produced.

Processes for high-yield diastereoselective synthesis of

Methods for the preparation of novel sidechain-bearing taxanes

The present invention relates to improved, efficient chemical syntheses of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP).

Process for the synthesis of ribonucleotide reductase inhibitors 3-AP

The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.

C4 methoxy ether derivatives of paclitaxel

Phosphorus bearing taxanes intermediates

The present invention relates to novel prodrug forms of ribonucleoside diphosphate reductase inhibitors 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) which have increased water solubility, bioavailablity and resistance to in vivo acetylation of their amino functions. Novel compounds according to the present invention relate to those of the formula: ##STR1## where R.sup.4 is H or CH.sub.3 and

Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP

The present invention provides paclitaxel derivatives of formula I ##STR1## and pharmaceutical compositions.

6,7-modified paclitaxels

3'-aminocarbonyloxy paclitaxels

##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R;

Deoxy taxols

The present invention provides paclitaxel derivatives of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.Z is RO-- or R;

The present invention relates to 10-desacetoxytaxol and derivatives thereof, which are useful as antitumor agents. These compounds have the formula ##STR1## wherein R.sub.2 is hydrogen, hydroxy or a protected hydroxy group; R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, a protected hydroxy group, methyl, --SH, --NH.sub.2, or --NR.sub.8 R.sub.9 ; R.sub.5 is R.sub.10, or --OR.sub.10 ; R.sub.6 and R.sub.7 are independently hydrogen, alkyl, or aryl; R.sub.8 and R.sub.9 are independently hydrogen, alkyl, alkenyl, alkynyl, or aryl; and R.sub.10 is alkoxy, alkyl, alkenyl, alkynl, or aryl.

10-desacetoxytaxol derivatives

This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R;

Growing community of inventors

Hamden, CT, United States of America

Shu-Hui Chen