Monsanto Company

Solutia Incorporated

The Nutrasweet Company

Mallinckrodt, Inc.

Kereos, Inc.

Pfizer Corporation

Pharmacia Corporation

William D McGhee

Dennis Patrick Riley

Jerry R Ebner

Mark D Paster

John Jeffrey Talley

Indra Prakash

Arnold Hershman

Zhi Guo

Loraine M Klein

Thomas E Waldman

Barry L Parnas

Leo J Letendre

A John Solodar

George H Klemm

Henry T Gaud

Cynthia Snoddy

Kenneth W Ruettimann

Michael K Stern

Anthony K Uriarte

Erik D Sall

Michael J Gross

Christopher R Buechler

Jayne E Morris

Patrick P Notte

Arnold Herschman

Lorraine M Klein

The present invention provides a composition for the treatment of cancer including zwitterionic liposomes consisting essentially of: 50-65 mol % of a phosphatidylcholine lipid, 30-45 mol % of cholesterol, and 2-8 mol % of a PEG-lipid; and cisplatin. Cisplatin is encapsulated in the liposomes in an amount such that the ratio of the total lipid weight to the cisplatin weight is from about 65:1 to about 95:1. Methods for the preparation of liposomal cisplatin and the treatment of cancer are also disclosed.

Liposomal cisplatin compositions for cancer therapy

An improved linker which lacks chiral centers between a hydrophobic anchor for coupling to lipid-based particles and a targeting agent has suitable hydrophobic/hydrophilic properties for use in vivo.

Linkers for anchoring targeting ligands

A process for the qualitative preparation of 3-haloalkyl-1H-pyrazoles suitable for efficient, high payload commercial application.

Synthesis of diaryl pyrazoles

Compounds useful for associating with nanoparticle or microparticle emulsions to obtain magnetic resonance images permit control of the relaxivity of the signal and readily associate with the particulate components. The compounds are conveniently prepared from achiral derivatives of chelating moieties.

Lipophilic derivatives of chelate monoamides

3,3-Dimethylbutanal is prepared from 3,3-dimethybutanol. Intermediate 3,3-dimethylbutanol is obtained by reacting ethylene, isopropylene and a mineral acid to produce a 3,3-dimethylbutyl ester which is hydrolyzed to the alcohol. The hydrolysis step is effectively carried out by reactive distillation. Alternatively, 3,3-dimethylbutanal is prepared from 3,3-dimethylbutanol obtained by reduction of the corresponding carboxylic acid or 1,2-epoxy-3,3-dimethylbutane, or by hydrolysis of 1-halo-3,3-dimethylbutane. Fixed bed gas phase and stirred tank liquid phase processes are provided for converted 3,3-dimethylbutanol to 3,3-dimethylbutanal by catalytic dehydrogenation.

Process for the preparation of 3,3-dimethylbutanal

3,3-Dimethylbutanal is prepared from 3,3-dimethylbutanol. Intermediate 3,3-dimethylbutanol is obtained by reacting ethylene, isopropylene and a mineral acid to produce a 3,3-dimethylbutyl ester which is hydrolyzed to the alcohol. The hydrolysis step is effectively carried out by reactive distillation. Alternatively, 3,3-dimethylbutanal is prepared from 3,3-dimethylbutanol obtained by reduction of the corresponding carboxylic acid or 1,2-epoxy-3,3-dimethylbutane, or by hydrolysis of 1-halo-3,3-dimethylbutane. Fixed bed gas phase and stirred tank liquid phase processes are provided for converting 3,3-dimethylbutanol to 3,3-dimethylbutanal by catalytic dehydrogenation.

3,3-Dimethylbutanal is prepared from 3,3-dimethylbutanol. Intermediate 3,3-dimethylbutanol is obtained by reacting ethylene, isopropylene and sulfuric acid to produce a 3,3-dimethylbutyl ester which is hydrolyzed to the alcohol. The hvdrolysis step is effectively carried out by reactive distillation. Alternatively, 3,3-dimethylbutanal is prepared from 3,3-dimethylbutanol obtained by reduction of the corresponding carboxylic acid or 1,2-epoxy-3,3-dimethylbutane, or by hydrolysis of 1-halo-3,3-dimethylbutane. Fixed bed gas phase and stirred tank liquid phase processes are provided for converting 3,3-dimethylbutanol to 3,3-dimethylbutanal by catalytic dehydrogenation.

Inert gas additive is utilized in the catalytic oxidation of benzene with nitrous oxide to produce phenol in order to prevent excessive exothermic temperature increases and to render gaseous mixtures throughout the process non-flammable.

Chemical composition and process

A zeolite catalyst, which can be used in a process for hydroxylating benzene to phenol, is treated with an aqueous solution containing ferric or ferrous ions, and is treated with an aqueous solution containing dithionate ions. The treated catalyst exhibits improved selectivity and stability in the benzene hydroxylation process.

Selective introduction of active sites for hydroxylation of benzene

A zeolite catalyst for hydroxylating benzene to phenol is treated hydrothermally with a gas comprising approximately 1-100 mole percent water at a temperature between approximately 350.degree.-950.degree. C., and subsequently is treated with an acid. This treatment selectively removes aluminum species from the zeolite catalyst in a manner that increases catalyst stability in phenol production without reducing the activity of the catalyst.

Benzene hydroxylation catalyst stability by acid treatment

The present invention is the novel synthesis of sterically hindered penta-substituted guanidines by a process in which (1a) an isocyanate is reacted first with a di-substituted amine or (1b) a urea is reacted with two moles of a mono-substituted amine to form a tri-substituted urea followed by (2) treatment of the tri-substituted urea with an activating agent before reacting with a second di-substituted amine in the presence of a base.

Growing community of inventors

St. Louis, MO, United States of America

William D McGhee