Eastman-kodak Company

Genencor International, Inc.

Sterling Winthrop Inc.

Lipitek International, Inc.

Sterling Drug Inc.

Cancer Therapy and Research Center

Other

Sanofi

Lipitek, Inc.

Alexander L Weis

Carl R Illig

Frederick H Hausheer

Charles T Goodhue

Kirupathevy Pulenthiran

Fred T Oakes

Paul F Cavanaugh, Jr

Patricia S Moskwa

William N Washburn

Barbara Boland Lussier

Lee H Latimer

Shih-Fong Chen

Daniel L Dexter

Mallaiah Mittakanti

Prasad V Chaturvedula

Ashis Kumar Saha

Daniel J Delecki

Jan M Woynarowski

Annette M Gero

Peech S Reddy

Kirupathevy Shanmuganathan

Tamas Bakos

Peech S Reedy

The invention relates to novel nucleosides and nucleoside dimers containing an L-sugar in at least one of the nucleosides, and their pharmaceutical compositions.

Nucleoside analogs and uses in treating Plasmodium falciparum infection

The invention relates to pharmaceutical compositions of nucleoside dimers containing an L-sugar in at least one of the nucleosides.

Nucleoside analogs and uses in treating disease

The invention relates to nucleoside dimers containing an L-sugar in at least one of the nucleosides and their pharmaceutical compositions.

L-Nucleoside Dimer Compounds and therapeutic uses

Nucleoside analogs and uses against parasitic infection

This invention relates to .alpha. and .beta.-L-pyranosyl nucleosides of Formula (I), wherein the nucleoside substitution on the pyranosyl carbohydrate molecule comprises a substituted or unsubstituted purine (adenine or guanine) or pyrimidine (cytosine, uracil, thymine and hypoxanthine) base. Also provided are methods to make the .alpha. and .beta.-L-pyranosyl nucleosides and methods of using such to treat cancer in a mammal.

L-pyranosyl nucleosides

The present invention relates to compounds, compositions and methods for inhibiting gene expression. The compounds of this invention comprise 1) oligonucleoside sequences of from about 6 to about 200 bases having a three atom internucleoside linkage or 2) oligonucleotide sequences of from about 9 to about 200 bases having a diol at either or both termini.

Oligonucleotide analogues containing phosphate diester linkage

This invention relates to .alpha. and .beta.-L-erythrosyl nucleosides of the formula (I), wherein the nucleoside substitution on the erythrosyl carbohydrate molecule comprises a substituted or unsubstituted purine (adenine or guanine) or pyrimidine (cytosine, uracil, thymine and hypoxanthine) base. Also provided are methods to make the .alpha. and .beta.-L-erythrosyl nucleosides and methods of using such to treat cancer in a mammal.

L-erythrosyl nucleosides

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 in vitro and in vivo tumor models, in particular, against melanoma.

Unsymmetrically linked bisnaphthalimides as antitumor agents

Compounds, compositions and methods for inhibiting gene expression are disclosed. The compounds comprise oligonucleotide sequences of from about 9 to about 200 bases having a diol at either or both termini. Preferred diols are polyalkyleneglycols, preferably polyethyleneglycols. Pharmaceutical compositions comprising the compounds and a physiologically acceptable carrier and methods of inhibiting gene expression in mammals comprising administering such compounds are also provided. Methods for inhibiting nuclease cleavage of compounds are also provided.

Nuclease resistant compounds

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 in vitro and in vivo tumor models, in particular, against melanoma. Also provided a 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.

Diamine platinum naphthalimide complexes as antitumor agents

This invention relates to .alpha. and .beta. L-ribofuranosyl nucleosides, processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat various diseases in mammals.

L-ribofuranosyl nucleosides

A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;

3,4-disubstituted anilines-immunomodulating agents

Certain 3,4-disubstituted anilines and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;

Exonuclease resistant terminally substituted oligonucleotides

A method of linking nucleosides with a siloxane bridge comprising reacting a 3'-silylated-5'-protected nucleoside with an unprotected nucleoside is disclosed. The silylated and unprotected nucleosides may be either monomeric nucleosides or the terminal nucleosides of an oligonucleotide or oligonucleotide analog. A method of synthesizing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed. The method of synthesis comprises silylating a 5'-protected nucleoside with a bifunctional silylating reagent to form a 3'-silylated nucleoside, reacting the silylated nucleoside with an unprotected nucleoside in the presence of a base catalyst and repeating these steps to form an oligonucleotide analog. A modified solid phase synthesis method for preparing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed.

Growing community of inventors

San Antonio, TX, United States of America

Alexander L Weis