PHOSPHITE-BORANE COMPOUNDS, AND METHOD OF MAKING AND USING THE SAME

Title:

PHOSPHITE-BORANE COMPOUNDS, AND METHOD OF MAKING AND USING THE SAME

Document Type and Number:

WIPO Patent Application WO1992020650

Kind Code:

A3

Abstract:

Phosphite-borane compounds of the formula wherein: each R1 is independently selected from: H; C1-C10 alkyl; alkylaryl; aralkyl; aryl; monovalent metal ions; nucleosides; and quaternary ammonium ions, (R4)4N+, in which the substituents R4 of the ammonium nitrogen atom are H or C1-C10 alkyl; R2 is H or C1-C10 alkyl; and R3 is CNCH2CH3+BF4-, COOH, carboxyl salts, COOR5, or CONHR5, wherein R5 is C1-C10 alkyl, alkylaryl, aralkyl, or aryl; with the proviso that if at least one of the R1 substituents is H, nucleoside, monovalent metal ion, or quaternary ammonium ion, then R3 may also be CN. The phosphorous-boron adducts of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and hypolipidemic activity. Also disclosed are various synthetic methods for making such phosphorous-boron compounds, and for formulating same in unit dosage forms as well as other pharmaceutically and pharmacologically acceptable formulations.

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Inventors:

SPIELVOGEL BERNARD F (US)
SOOP ANUP (US)
HALL IRIS H (US)

Application Number:

PCT/US1992/003833

Publication Date:

March 04, 1993

Filing Date:

May 08, 1992

Export Citation:

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Assignee:

BORON BIOLOG INC (US)

International Classes:

A61K31/69; A61K31/70; A61K31/7135; A61P3/06; A61P29/00; A61P35/00; C07F9/06; C07F9/141; C07F19/00; C07H23/00; (IPC1-7): A61K31/69; A61K31/70; C07F9/06; C07F9/142; C07H19/10; C07H19/20

Other References:

Tetrahedron, Volume 47, Issue 34, issued 19 August 1991, SOOD, A. et al., "Boron Analogs of Phosphonoacetates: Synthesis, Characterization and Antitumor Properties of Sodium diethylphosphite-carboxyborane and Related Compounds", pages 6915-6930.
See also references of EP 0583394A4

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