G.d. Searle & Company

D. G. Searle & Co.

Robert J Chorvat

Bipinchandra N Desai

Raphael Pappo

Kerry W Fowler

Kurt J Rorig

Kathleen A Prodan

Suzanne E Radak

Gilbert W Adelstein

Kathleen T McLaughlin

George R Lenz

James P Snyder

John A Schulz

Suzanne Evans Radak

Compositions of matter are disclosed of compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein X represents a halo, lower alkyl, hydrogen, trifluoromethyl, phenyl, or lower alkoxy substituent; Y represents --CN, --CONH.sub.2, --CON(R.sub.1).sub.2 or --CO.sub.2 R.sub.1 where R.sub.1 is a lower alkyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; R.sub.2 represents lower alkyl; R.sub.3 represents lower alkyl or acetyl, aroyl, phenacetyl or trifluoroacetyl; A, B, and D are carbonyl or methylene such that when one of A, B, or D is carbonyl, the others are methylene and R.sub.3 is lower alkyl, whereas when R.sub.3 is acetyl, aroyl, phenacetyl or trifluoroacetyl, A, B, and D are methylene. These compounds have utility as antiarrhythmic agents.

Monobasic disobutamide derivatives

This invention relates to a process for preparing useful antiarrhythmic 1,3-diazabicyclo[4.4.0]dec-2-en-4-ones from 1-acyl-.alpha.-[2-[bis(1-methylethyl)amino]ethyl]-.alpha.-phenyl-2-piperid ineacetamides. This invention also relates to the 1-acyl-.alpha.-[2-[bis(1-methylethyl)amino]ethyl]-.alpha.-phenyl-2-piperid ineacetamides employed in this process.

Process for antiarrhythmic 1,3-diazabicyclo[4.4.0]dec-2-en-4-ones

The invention relates to compounds of the formula: ##STR1## which are useful cardiovascular agents.

Phenylpiperazine phosphonates

This invention relates to octahydropyrido[1,2-c]pyrimidinones and hexahydropyrido[1,2-c]pyrimidinediones that are useful as inhibitors of cardiac arrhythmias and are therefore useful in the treatment of irregular heartbeat.

Octahydropyrido[1,2-c]pyrimidinones and

Compositions of matter are disclosed of compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein X represents a halo, lower alkyl, hydrogen, trifluoromethyl, phenyl, or lower alkoxy substituent; Y represents --CN, --CONH.sub.2, --CON(R.sub.1).sub.2 or --CO.sub.2 R.sub.1 where R.sub.1 is a lower alkyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; R.sub.2 represents lower alkyl; R.sub.3 represents lower alkyl or acetyl, aroyl, phenacetyl or trifluoracetyl; A, B, and D are carbonyl or methylene such that when one of A, B, or D is carbonyl, the others are methylene and R.sub.3 is lower alkyl, whereas when R.sub.3 is acetyl, aroyl, phenacetyl or trifluoroacetyl, A, B, and D are methylene. These compounds have utility as antiarrhythmic agents.

This invention relates to hexahydroindolizinones, which are useful as inhibitors of cardiac arrhythmias and of platelet aggregation and are therefore useful in the treatment of irregular heartbeat and in the prevention of thrombus formation.

Hexahydroindolizinones useful for treating cardiac arrhythmia,

This invention relates to 5-(substituted phenyl)-5-[(substituted amino)alkyl]-1,3-diazabicyclo[4.4.0]decan-4-ones and 5-(substituted phenyl)-5-[(substituted amino)-alkyl]-1,3-diazabicyclo[4.4.0]dec-2-en-4-ones that are useful as antiarrhythmic agents.

Substituted 5-phenyl-5-(aminoalkyl)-1,3-diazabicyclo[4.4.0]decan-4-ones

This invention encompasses compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein n is 2 or 3 and R.sub.1 and R.sub.2 are n-propyl, isopropyl, or R.sub.1 and R.sub.2 together with N form a 2,6-dimethyl-1-piperidinyl group. The compounds of this invention are useful as antiarrhythmic agents.

2,5-Pyrrolidinedione derivatives useful as antiarrhythmic agents

The present invention relates to a class of novel annulated 4H-1,4-benzothiazine derivatives. The invention further relates to pharmaceutical compositions containing such annulated benzothiazine derivatives and to the use of such compounds and compositions as anorectic agents. In particular, certain of the novel annulated 4H-1,4-benzothiazine derivatives are effective anorectic agents when administered orally.

Benzothiazine derivatives

4H-1,4 benzothiazine derivatives having anorectic activity and their preparation including intermediate compounds are disclosed.

4H-1,4-Benzothiazine derivatives and intermediates thereto

4H-1,4-Benzothiazine derivatives

25-Substituted-5.alpha.-cholestane-3.beta.,22S-diols and esters thereof of Formula I which inhibit the activity of 3-hydroxy-3-methyl-glutaryl coenzyme A reductase and inhibit the formation of serum cholesterol are disclosed.

25-Substituted-5.alpha.-cholestane-3.beta.,22S-diol

24-Cyclopropylcholene-3.beta., 22-diols and esters thereof which control serum cholesterol levels and their preparation are disclosed.

24-Cyclopropylcholene-3.beta., 22-diols and esters thereof

25-Alkylcholest-5-ene-3.beta.,22-diols and esters thereof adapted to inhibit the activity of 3-hydroxy-3-methylglutaryl coenzyme A reductase are disclosed.

25-Alkylcholest-5-ene-3 .beta.,22-diols and esters thereof

25-Halocholest-5-ene-3.beta.,22-diols and esters thereof which inhibit the activity of 3-hydroxy-3-methylglutaryl coenzyme A reductase and inhibit the formation of serum cholesterol and their preparation from 3.alpha.,5-cyclo-6.beta.-methoxy-23,24-dinor-5.alpha.-cholan-20-al are disclosed.

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Arlington Heights, IL, United States of America

Robert J Chorvat