|Abstract:||Fluorenes bearing a 9-aminoalkyl substituent are useful antiarrhythmic agents. Pharmaceutical formulations containing such compounds are provided, as well as a method of treatment.|
|Inventor(s):||Lacefield; William B. (Indianapolis, IN), Simon; Richard L. (Greenwood, IN)|
|Assignee:||Eli Lilly and Company (Indianapolis, IN)|
1. A pharmaceutical formulation useful in the treatment of cardiac arrhythmias which comprises a carrier or diluent admixed with an antiarrhythmic amount of a 9-aminoalkylfluorene
antiarrhythmic agent of the formula ##STR12## wherein: R.sup.o is hydroxy, cyano, CONR.sup.4 R.sup.5 or COOR.sup.9 in which R.sup.4 and R.sup.5 independently are hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.9 is hydrogen or C.sub.1 -C.sub.4 alkyl;
R.sup.2 and R.sup.3 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, CH.sub.2 C.sub.2 -C.sub.5 alkenyl, phenyl-C.sub.1 -C.sub.3 alkyl; or taken together with the nitrogen to which they are attached are a cyclic group of the formula ##STR13## in which R.sup.8 is hydrogen or C.sub.1 -C.sub.4 alkyl; A is CH.sub.2, O or NH; and y is zero or one; provided that R.sup.2 is hydrogen when R.sup.1 is hydroxy;
n is 3, 4 or 5;
R.sup.6 and R.sup.7 independently are hydrogen, C.sub.1 -C.sub.4 alkyl or halogen; and the pharmaceutically acceptable salts thereof.
2. The formulation of claim 1 wherein R.sup.o is hydroxy, cyano or CONR.sup.4 R.sup.5.
3. The formulation of claim 2 wherein n is 3.
4. The formulation of claim 3 wherein R.sup.2 is hydrogen.
5. The formulation of claim 4 wherein R.sup.3 is C.sub.1 -C.sub.6 alkyl.
6. The formulation of claim 5 wherein R.sup.6 and R.sup.7 both are hydrogen.
7. The formulation of claim 6 wherein R.sup.3 is C.sub.1 -C.sub.3 alkyl.
8. The formulation of claim 7 wherein R.sup.3 is isopropyl.
9. The formulation of claim 8 wherein the active ingredient is 9-(3-isopropylaminopropyl)-9-aminocarbonylfluorene.
10. The formulation of claim 6 wherein the active ingredient is a pharmaceutically acceptable salt.
11. The formulation of claim 10 wherein the active ingredient is 9-(3-isopropylaminopropyl)-9-aminocarbonylfluorene hydrochloride.
12. The formulation of claim 1 wherein R.sup.o is COOR.sup.9.
13. The formulation of claim 12 wherein R.sup.9 is C.sub.1 -C.sub.4 alkyl.
14. The formulation of claim 1 wherein n is 4.
15. The formulation of claim 1 wherein n is 5.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.