Solid salts of benzazepine compounds and pharmaceutical...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C540S523000

Reexamination Certificate

active

06998398

ABSTRACT:
Pharmaceutically acceptable metal salts of compounds of formula (I):in whichR1is selected from the group consisting of (C1–C6)alkoxy(C1–C6)alkyl which may be substituted with (C1–C6)alkoxy, phenyl-(C1–C6)-alkyl and/or phenyloxy-(C1–C6)-alkyl group in which any phenyl group may be substituted with (C1–C6)alkyl, (C1–C6)alkoxy or halogen, and naphtyl-(C1–C6)-alkyl;R2and R3are each independently hydrogen or halogen;R4is a biolabile ester forming group;and in which the salt is selected from the lithium salt and salts of bivalent metal ions such as magnesium, calcium and zinc. Also described are a method for the preparation of the above salts; pharmaceutical compositions comprising the above salts; methods of using the above salts to treat heart disorders or hypertension, to improve gastrointestinal blood flow, or to treat or inhibit cardiac damage induced by adriamycin and comparable anti-cancer drugs; and crystalline S-α-methylbenzylamine salts of the compounds of formula (I) that are useful as intermediates in production of the above salts.

REFERENCES:
patent: 5783573 (1998-07-01), Rozsa et al.
patent: 0733642 (1996-09-01), None
patent: 0830863 (1998-03-01), None
patent: WO 00/48601 (2000-08-01), None
patent: WO 01/03699 (2001-01-01), None
Zeev B. Alfassi, et al., “Solventing out of Electrolytes form their Aqueous Solution”, AIChE Journal, Sep. 1984, pp. 874-876, vol. 30, No. 5.
Jerzy Mydlarz, et al., “Solubility and Density Isotherms for Potassium Sulfate-Water-2-Propanol”, J. Chem. Eng. Data, 1989, pp. 124-126, 34, American Chemical Society.
J. W. Mullin, et al., “Potassium Sulphate Precipitation from Aqueous Solution by Salting-out with Acetone”, Chem. Eng. Process., 1989, pp .93-99, 26, Elsevier Sequoia, The Netherlands.

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