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US4181728A Expired / Lapsed US ⏱️ 0.0 years remaining

Spiro-polycyclicimidazolidinedione derivatives

Assignee: Pfizer Inc
•
Filing: 1978-11-16
•
Granted: 1980-01-01
•
Expires: 1998-11-16
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Abstract

Abstract Novel spiro-polycyclicimidazolidinedione derivatives useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. The derivatives include 2',3'-dihydro-spiro[imidazolidine-4,4'-[4'H]-naphtho[1,2-b]pyran]-2,5- dione, 2',3'-dihydro-spiro-[imidazolidine-4, 4'-[4'H]-naphtho[1,2-b]thiopyran]-2,5-dione, 1',2',3',4'-tetrahydro-spiro[imidazolidine-4,1'-benz[a]anthracene]2,5- dione, 2',3'-dihydro-spiro[imidazolidine-4,1'phenalene]-2,5-dione, 1',2',3',4'-tetrahydro-spiro[imidazolidine-4,1'-phenanthrene]-2,5-dione, the 2,1 isomers of the 2',3'-dihydro-4'H-pyran and 2',3'-dihydro-4'H-thiopyran derivatives, the 2',3'-dihydro-4'H-anthracenopyran and 2',3'-dihydro-4'H-anthracenothiopyran derivatives, the spiro-4,4' isomer of the tetrahydrophenanthrene derivative, the [b] isomer of the benzanthracene derivative and the mono or disubstituted 2',3'-dihydro-4'H-naphthopyran, 2',3'-dihydro-4'H-naphthothiopyran and tetrahydrophenanthrene derivatives.

Inventors

  • 👤 Reinhard Sarges
  • 👤 John L. Belletire

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 10:05
CPC Classifications
C; C07; C07D; C07D235/00; C07D235/02; A; A61; A61P; A61P13/00; A61P13/02; A61P15/00; A61P25/00; A61P25/24; A61P25/26; A61P27/00; A61P27/02; A61P27/12; A61P3/00; A61P3/08; C07D491/00; C07D491/02; C07D491/10; C07D495/00; C07D495/02; C07D495/10

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 67 words
A spiro-polycyclicimidazolidinedione derivative of the formula ##STR11## or its pharmaceutically acceptable metallic salt, wherein: A is naphth-α,β-o of the formula ##STR12## anthracen-α,β-o of the formula ##STR13## or substituted naphth-α,β-o having 1 or 2 identical substituents selected from methyl, chloro or bromo; and Y is CH 2 , S, SO, SO 2 or O; or A and Y taken together are a naphth-α,θ-o ring of the formula ##STR14##
Claim 2
Dependent Claim 67 words
A spiro-polycyclicimidazolidinedione derivative of the formula ##STR11## or its pharmaceutically acceptable metallic salt, wherein: A is naphth-α,β-o of the formula ##STR12## anthracen-α,β-o of the formula ##STR13## or substituted naphth-α,β-o having 1 or 2 identical substituents selected from methyl, chloro or bromo; and Y is CH 2 , S, SO, SO 2 or O; or A and Y taken together are a naphth-α,θ-o ring of the formula ##STR14##
Claim 3
Dependent Claim 19 words
A spiro-polycyclicimidazolidinedione derivative of claim 1 wherein A is naphth-α,β-o and Y is CH 2 , S or O.
Claim 4
Dependent Claim 23 words
The spiro-polycyclicimidazolidinedione derivative of claim 1 wherein A is naphth-α,β-O, Y is S and S joins the naphth-α,β-o ring at the β position.
Claim 5
Dependent Claim 22 words
The spiro-polycyclicimidazolidinedione derivative of claim 1 wherein A is naphth-α,β-o, Y is S and S joins the naphth-α,β-o at the α position.
Claim 6
Dependent Claim 23 words
The spiro-polycyclicimidazolidinedione derivative of claim 1 wherein A is naphth-α,β-o, Y is O and O joins the naphth-α,β-o ring at the α position.
Claim 7
Dependent Claim 23 words
The spiro-polycyclicimidazolidinedione derivative of claim 1 wherein A is ε-methoxynaphth-α,62 -o, Y is O and O joins the ε-methoxynaphth-α,β-o at the α position.
Claim 8
Dependent Claim 22 words
The spiro-polycyclicimidazolidinedione derivative of claim 1 wherein A is δ-chloronaphth-α,β-o, Y is O and O joins the δ-chloronaphth-α,β-o at the α position.
Claim 9
Dependent Claim 24 words
The spiro-polycyclicimidazolidinedione derivative of claim 1 wherein A is naphth-α,β-o, Y is CH 2 and CH 2 joins the naphth-α,β-o at the α position.
Claim 10
Dependent Claim 14 words
The spiro-polycyclicimidazolidinedione derivative of claim 1 wherein A and Y taken together are naphth-α,θ-o.
Claim 11
Dependent Claim 42 words
A pharmaceutical formulation of a spiro-polycyclicimidazolidinedione derivative of claim 1, which comprises: a combination of a pharmaceutically-acceptable carrier material and the derivative in an amount effective to inhibit harmful, in vivo enzymatic reduction of aldoses or to prevent or alleviate diabetes-associated complications.
Claim 12
Dependent Claim 38 words
A method of treating a diabetic host to inhibit harmful, in vivo enzymatic reduction of aldoses or to prevent or alleviate diabetes-associated complications, which comprises: administering to the host an effective amount of a derivative of claim 1.

References Cited (Backward Citations)

US2683718A Cited
DE1032257B Cited
GB796069A Cited
GB818724A Cited
US3532744A Cited
US3821383A Cited
US4117230A Cited
US4130714A Cited
US4127665A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1982-12-31 1983-07-02 1984-01-01 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1986-12-31 1987-07-02 1988-01-01 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1990-12-31 1991-07-02 1992-01-01 $7700.00 Window Closed / Lapsed

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