Patent · US Expired

Spiro [imidazolidine 4,3'-indoline]2,2',5-triones, compositions and use

US4386100A · kind A · utility

5Cited by
1References
12Claims
0Family size

Assignee

Inventors

Key dates

Filing dateMay 11, 1982
Grant dateMay 31, 1983
Priority date
Expiry dateMay 11, 2002

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07F7/1804
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The invention provides novel non-toxic biodegradable derivatives of the formula: ##STR1## wherein Ra is (1-12C)alkyl, phenyl, naphthylmethyl or cinnamyl, the aromatic rings of which optionally bear one or two halogeno substituents, or Ra is benzyl optionally bearing up to 3 substituents independently selected from halogeno, trifluoromethyl, (1-4C)alkyl, (1-4C)alkoxy, nitro, cyano and hydroxy; Rb and Rc are independently selected from hydrogen and non-toxic biodegradable protecting radicals, but are not both hydrogen; and benzene ring A optionally bears one substituent selected from halogeno, (1-4C)alkyl, (1-4C)alkoxy, nitro and hydroxy, or bears two substituents independently selected from halogeno, (1-4C)alkyl and nitro; pharmaceutical compositions thereof; and processes for their manufacture. The amides of formula I in which Rb.dbd.Rc.dbd.H are potent inhibitors of the enzyme aldose reductase. The derivatives of formula I provided by the invention are of use in vivo in the treatment or prophylaxis of certain complications of diabetes or galactosemia.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.