Imidazolidinedione analogs useful as anticoagulants and antithrombotics
AssigneeSchering Corporation
InventorsDamian Arnaiz, Yuo-Ling Chou, Brian Griedel, Raju Mohan, Kenneth Shaw
Life of this patent
Estimating the term…
Abstract
A compound is disclosed, which is useful in treating a mammal having a disease-state characterized by thrombotic activity. The compound is of the following formula: wherein A, B, R1, R2, R3 and R4 are as defined herein or an isomer or isomeric mixture thereof or a pharmaceutically acceptable salt thereof.
Claims8
A compound of the following formula, or a pharmaceutically acceptable salt thereof:
- wherein
- R1 is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, benzyl, carbocyclic, heterocyclic, heteroaryl and hydrogen;
- R2 and R3 are each selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, C-amido, carbocyclic, C-carboxy, heteroaryl, heterocyclic and hydrogen;
- or, R2 and R3 are combined to form a carbocyclic group;
- A is a branched or straight chain alkylene, a branched or straight chain alkylidene, a branched or straight chain alkylidyne, oxo, or sulfonyl;
- B is aryl or heteroaryl;
- and
- R4 is amidine, carboxyamidine, hydroxyamidine or ketoamidine,
- as a single stereoisomer, a mixture of individual stereoisomers or a racemic mixture;
- and,
- wherein the following compound is excluded:
- 7-[3-(3-aminobenzyl)-4-(4-aminophenyl)-4-methyl-2,5-dioxo-imidazolidin-1-ylmethyl]-naphthalene-2-carboxamidine.
3-8. (canceled)
A pharmaceutical composition, which composition comprises a pharmaceutically acceptable excipient and a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, wherein the compound is of the following formula:
- wherein
- R1 is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, benzyl, carbocyclic, heterocyclic, heteroaryl and hydrogen;
- R2 and R3 are each selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, C-amido, carbocyclic, C-carboxy, heteroaryl, heterocyclic and hydrogen;
- or, R2 and R3 can be combined to form a carbocyclic group;
- A is a branched or straight chain alkylene, a branched or straight chain alkylidene, a branched or straight chain alkylidyne, oxo, or sulfonyl;
- B is aryl or heteroaryl;
- and
- R4 is amidine, carboxyamidine, hydroxyamidine or ketoamidine;
- as a single stereoisomer, a mixture of individual stereoisomers or a racemic mixture;
- and,
- wherein the following compound is excluded:
- 7-[3-(3-aminobenzyl)-4-(4-aminophenyl)-4-methyl-2,5-dioxo-imidazolidin-1-ylmethyl]-naphthalene-2-carboxamidine.
A method of inhibiting blood clot formation comprising administering a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, the compound having the following formula:
- wherein
- R1 is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, benzyl, carbocyclic, heterocyclic, heteroaryl and hydrogen;
- R2 and R3 are each selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, C-amido, carbocyclic, C-carboxy, heteroaryl, heterocyclic and hydrogen;
- or, R2 and R3 can be combined to form a carbocyclic group;
- A is a branched or straight chain alkylene, a branched or straight chain alkylidene, a branched or straight chain alkylidyne, oxo, or sulfonyl;
- B is aryl or heteroaryl;
- and
- R4 is amidine, carboxyamidine, hydroxyamidine or ketoamidine;
- as a single stereoisomer, a mixture of individual stereoisomers or a racemic mixture.
Dependencies are inferred from the claim text.