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EP0127412A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Imidazolidinedione derivatives

Assignee: Pfizer Inc
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Filing: 1984-05-21
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Granted: —
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Expires: 2004-05-21
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Abstract

Abstract A series of novel spiro-oxindole imidazolidinedione derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as aldose reductose inhibitors for the control of certain chronic diabetic complications. Preferred compounds include 6'-amino-spiro- [imidazolidine-4,3'-indoline] -2,2', 5-trione, 5'-chloro -7'-amino-spiro [imidazolidine-4,3'-indofine) -2,2', 5-trione, 1'- (3-pyridylmethyl) -5'-fluoro-spiro [imidazolidine-4,3'-indoline) -2,2',5-trione, 1'- (3-pyridylmethyl) -5',7'-dichloro-spiro- [imidazolidine-4,3'( indoline] -2,2',5-trione and spiro- [imidazolidine-4,3'- (6- azaindoline)1 -2,2',5-trione. Methods for preparing these compounds from known starting materials are provided.

Inventors

  • 👤 Alan Jeffrey Hutchison

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-03 00:47
CPC Classifications
C; C07; C07D; C07D403/00; C07D403/02; C07D487/00; C07D487/02; C07D487/10; A; A61; A61P; A61P25/00; A61P25/02; A61P27/00; A61P27/02; A61P3/00; A61P3/08

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 445 words
An analogy process for preparing s p iro-hydantoin derivatives of the formulae: and the pharmaceutically acceptable salts thereof, wherein X and Y are each hydrogen, fluorine, chlorine, bromine, nitro or amino; Z is hydrogen or amino, with the proviso that Z is always other than amino when at least one of X and Y is other than hydrogen; R is a member selected from the group consisting of hydrogen, aryl and aralkyl having up to three carbon atoms in the alkyl moiety wherein each of said aryl moieties is chosen from the group consisting of pyridyl and ring-subsituted pyridyl, with each ring substituent being chosen from the group consisting of fluorine, chlorine, bromine and alkyl having from one to four carbon atoms, with the proviso that said R is always other than hydrogen when each of X, Y and Z is other than amino; =A- B = D - of formula II represents = N - CH =CH-, = CH - CH =N- or =CH-N=CH-; R' is a member selected from the group consisting of hydrogen, alkyl having from one to four carbon atoms, aryl and aralkyl having up to three carbon atoms in the alkyl moiety wherein each of said aryl moieties is chosen from the group consisting of pyridyl, thienyl, phenyl and mono and di-substituted phenyl, with each ring substituent being chosen from the group consisting of fluorine, chlorine, bromine, alkyl and alkoxy each having up to four carbon atoms and trifluoromethyl; and R" is hydrogen, hydroxy, fluorine, chlorine, alkyl or alkoxy each having up to four carbon atoms or trifluoromethyl, characterized by: (a) condensing an appropriately substituted carbonyl ring compound of the respectively formulae: wherein X,Y,Z,R,R' and R" are each as previously defined with an alkali metal cyanide and ammonium carbonate to form the corresponding s p iro-oxindole imidazolidinedione final product of formula I or II; (b) or when X and Y are each hydrogen and Z is amino in formula I, alkylating sodio-ethyl hydantoin-5-carboxylate with 2,4-dinitrobenzene, followed by reductive cyclization; (c) or, when R' is hydrogen in formula II, alkylating sodio-ethyl hydantoin-5-carboxylate with an appropriate halonitro-disubstituted pyridine, followed by reductive cyclization; (d) or, when X is halogen as previously defined, Y is amino and Z is hydrogen in formula I, halogenating the compound wherein X, Y and Z are each hydrogen to form the corresponding 5'-halo derivative wherein X is halogen, followed by nitration at the 7'-position and subsequent reduction; and thereafter, if required, converting a compound of formula II wherein R' is hydrogen to a corresponding compound where R' is other than hydrogen; and, if desired, converting a compound of formula I or II to a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 445 words
An analogy process for preparing s p iro-hydantoin derivatives of the formulae: and the pharmaceutically acceptable salts thereof, wherein X and Y are each hydrogen, fluorine, chlorine, bromine, nitro or amino; Z is hydrogen or amino, with the proviso that Z is always other than amino when at least one of X and Y is other than hydrogen; R is a member selected from the group consisting of hydrogen, aryl and aralkyl having up to three carbon atoms in the alkyl moiety wherein each of said aryl moieties is chosen from the group consisting of pyridyl and ring-subsituted pyridyl, with each ring substituent being chosen from the group consisting of fluorine, chlorine, bromine and alkyl having from one to four carbon atoms, with the proviso that said R is always other than hydrogen when each of X, Y and Z is other than amino; =A- B = D - of formula II represents = N - CH =CH-, = CH - CH =N- or =CH-N=CH-; R' is a member selected from the group consisting of hydrogen, alkyl having from one to four carbon atoms, aryl and aralkyl having up to three carbon atoms in the alkyl moiety wherein each of said aryl moieties is chosen from the group consisting of pyridyl, thienyl, phenyl and mono and di-substituted phenyl, with each ring substituent being chosen from the group consisting of fluorine, chlorine, bromine, alkyl and alkoxy each having up to four carbon atoms and trifluoromethyl; and R" is hydrogen, hydroxy, fluorine, chlorine, alkyl or alkoxy each having up to four carbon atoms or trifluoromethyl, characterized by: (a) condensing an appropriately substituted carbonyl ring compound of the respectively formulae: wherein X,Y,Z,R,R' and R" are each as previously defined with an alkali metal cyanide and ammonium carbonate to form the corresponding s p iro-oxindole imidazolidinedione final product of formula I or II; (b) or when X and Y are each hydrogen and Z is amino in formula I, alkylating sodio-ethyl hydantoin-5-carboxylate with 2,4-dinitrobenzene, followed by reductive cyclization; (c) or, when R' is hydrogen in formula II, alkylating sodio-ethyl hydantoin-5-carboxylate with an appropriate halonitro-disubstituted pyridine, followed by reductive cyclization; (d) or, when X is halogen as previously defined, Y is amino and Z is hydrogen in formula I, halogenating the compound wherein X, Y and Z are each hydrogen to form the corresponding 5'-halo derivative wherein X is halogen, followed by nitration at the 7'-position and subsequent reduction; and thereafter, if required, converting a compound of formula II wherein R' is hydrogen to a corresponding compound where R' is other than hydrogen; and, if desired, converting a compound of formula I or II to a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 38 words
A process as claimed in part (a) of claim 1, characterized by the fact that at least a slight molar excess of the alkali metal cyanide reagent is employed with respect to the carbonyl ring compound starting material.
Claim 4
Dependent Claim 41 words
A process as claimed in part of (a) of claim 1, characterized by the fact that said reaction is conducted in a reaction-inert polar organic solvent at a temperature that is in the range of from about 50°C. to about 150°C.
Claim 5
Dependent Claim 19 words
A process as claimed in claim 3, characterized by the fact that said solvent is a water-miscible lower alkanol.
Claim 6
Dependent Claim 17 words
The process as claimed in part (a) of claim 1 wherein the spiro-hydantoin derivative prepared is l'-(3-pyridylmethyl)-5'-fluoro-spiro-[imidazolidine-4,3'-indoline]-2,2',5-trione.
Claim 7
Dependent Claim 17 words
The process as claimed in part (a) of claim 1 wherein the spiro-hydantoin derivative prepared is 1'-(3-pyridylmethyl)-5',7'-dichloro-spiro-[imidazolidine-4,3'-indoline]-2,2',5-trione.
Claim 8
Dependent Claim 48 words
A process as claimed in part (b) or (c) of claim 1, characterized by the fact that the reductive cyclization step is carried out with iron powder in the presence of an acid at a temperature that is in the range of from about 20°C. to about 100°C.
Claim 9
Dependent Claim 18 words
The process as claimed in part (c) of claim 1 wherein the spiro-hydantoin derivative prepared is spiro-[imidazolidine-4,3'-(6-azaindoline)]-2,2',5- trione.
Claim 10
Dependent Claim 31 words
A process as claimed in part (d) of claim 1, characterized by the fact that the reduction step is carried out by catalytic hydrogenation with a platinum, palladium or nickel catalyst.
Claim 11
Dependent Claim 17 words
The process as claimed in part (d) of claim 1 wherein the spiro-hydantoin derivative prepared is 5'-chloro-7'-amino-spiro-[imidazolidine-4,3'-indoline]-2,2',5-trione.

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