Bryn Mawr College

Napro Biotherapeutics, Inc.

Neuromedica, Inc.

Luitpold Pharmaceuticals, Inc.

Protarga, Inc.

Other

Phyton Holdings, LLC

Alvi, Khisal

Srinivasan, Venkatesh

Gorr, Gilbert

Alford, Jennifer

Horn, Michael

Slusar-Place, Beth

Swindell, Charles

Charles S Swindell

Victor E Shashoua

Matthews O Bradley

Nigel L Webb

Nicholas J Sisti

Nancy Krauss

Madhavi C Chander

Glenn J Fegley

Gilbert Gorr

Venkatesh Srinivasan

Khisal Alvi

Jennifer Alford

Beth Slusar-Place

Michael Horn

Glenn Fegley

The present invention relates to the production of alkaloids from Liliaceae cell culture.

Production of alkaloids by liliaceae cell culture

The invention provides conjugates of fatty amines and pharmaceutical agents useful in treating cancer, viruses, psychiatric disorders. Compositions, pharmaceutical preparations, and methods of preparations of the fatty amine-pharmaceutical agent conjugates are provided.

Fatty amine drug conjugates

The invention provides conjugates of fatty acids and pharmaceutical agents useful in treating noncentral nervous system conditions. Methods for selectively targeting pharmaceutical agents to desired tissues are provided.

Fatty acid-pharmaceutical agent conjugates

The invention provides conjugates of fatty alcohols and pharmaceutical agents useful in treating cancer, viruses, psychiatric disorders. Compositions, pharmaceutical preparations, and methods of preparation of the fatty alcohols-pharmaceutical agent conjugates are provided.

Fatty alcohol drug conjugates

The invention provides conjugates of cis-docosahexaenoic acid and pharmaceutical agents useful in treating noncentral nervous system conditions. Methods for selectively targeting pharmaceutical agents to desired tissues are provided.

DHA-pharmaceutical agent conjugates of taxanes

Dha-pharmaceutical agent conjugates to improve tissue selectivity

The invention provides conjugates of fatty acids and antiviral agents useful in treating liver disorders.

Method of treating a liver disorder with fatty acid-antiviral agent conjugates

Synthesis of taxol, taxol analogs and their intermediates with variable a-ring side chain structures and compositions thereof

The present invention concerns alkyl esters of &bgr;-amino acid derivatives which are useful in the synthesis of taxol and analogs.

Synthesis of taxol, taxol analogs and their intermediates with variable A-ring side chain structures and compositions thereof

The present invention relates to chemical compounds that are useful in the production of taxanes. The chemical compounds according to the present invention have a generalized formula:

Syntheses of taxol, taxol analogs and their intermediates with variable A-ring side chain structures and compositions thereof

The invention provides compositions that include conjugates of a fatty acid molecule, preferably cis-docosahexaenoic acid, and clozapine. The conjugates are useful in treating psychological disorders such as schizophrenia.

Clozapine compositions and uses thereof

A compound for use in the production of taxanes and intermediates therefor having the formula: ##STR1## wherein R is an alkyl group.

C-7 CBZ baccatin III and production method therefor

C7, C10 di-CBZ 10-deacetyl baccatin III of the formula: ##STR1## provides an intermediate for the production of docetaxel. A method of producing this C7, C10 di-CBZ 10-deacetyl Baccatin III is provided. Here, 10-deacetyl Baccatin III is acylated with at least 1.5 equivalents of n-butyl lithium and at least 1.5 equivalents of benzyl chloroformate in tetrahydrofuran. The 10-deacetyl Baccatin III may first be dissolved in tetrahydrofuran after which the n-butyl lithium is added followed by the addition of the benzyl chloroformate. The reaction is preferably at a reduced temperature of less than -20.degree. C. The resulting solution may be quenched with ammonium chloride and reduced to residue. The residue may then be redissolved in an organic solvent, washed, dried and recrystallized to purify the compound.

Intermediate for use in docetaxel synthesis and production method

The invention provides taxanes that are conjugates of cis-docosahexaenoic acid and taxotere. The conjugates are useful in treating cancer.

Taxanes

An efficient protocol for the synthesis of taxol, taxol analogs and their intermediates is described. The process incudes the attachment of the taxol A-ring side chain to baccatin III and for the synthesis of taxol and taxol analogs with variable A-ring side chain structures. A rapid and highly efficient esterification of O-protected isoserine and 3-phenylisoserine acids having N-benzyoloxycarbonyl groups to the C-13 hydroxyl of 7-O-protected baccatin III is followed by a deprotection-acylation sequence to make taxol, cephalomanninne and various analogs, including photoaffinity labeling candidates.

Growing community of inventors

Merion, PA, United States of America

Charles S Swindell