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Derivative-compound-conjugates and pharmaceutical compositions comprising same |
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Method of use of bicycloheptane substituted prostaglandin analogs as cardiovascular agents
| Details |
Inventors: Sprague, Peter W.; Loots, Melanie J.; Haslanger, Martin F.;
Assignee: E. R. Squibb & Sons, Inc. (Princeton, NJ)
Primary Examiner:
Assistant Examiner:
Attorney, Agent or Firm:
Bicycloheptane substituted prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease. |
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DETAILED DESCRIPTION What is claimed is: 1. A method of inhibiting arachidonic acid-induced platelet aggregation and bronchoconstriction, which comprises administering to the circulatory system of a mammalian host an effective amount of a compound having the structural formula ##STR13## and including all stereoisomers thereof; wherein A is --CH. sub. 2 --CH. sub. 2 or --CH. dbd. CH--; m is 0 to 5; B is --CH. dbd. CH-- or (CH. sub. 2). sub. 2 ; R is H, lower alkyl, alkali metal or tris(hydroxymethyl)aminomethane; and R. sup. 1 is aralkyl, cycloalkyl or cycloalkylalkyl or a pharmaceutically acceptable salt thereof. 2. The method as defined in claim 1 wherein said compound is administered in an amount within the range of from about 1 to about 100 mg/kg. 3. The method as defined in claim 1 where in said compound A is CH. dbd. CH. 4. The method as defined in claim 1 where in said compound B is CH. dbd. CH. 5. The method as defined in claim 1 where in said compound B is --CH. sub. 2 CH. sub. 2 --. 6. The method as defined in claim 1 where in said compound R. sup. 1 cycloalkyl. 7. The method as defined in claim 1 where in said compound R. sup. 1 is aralkyl. 8. The method as defined in claim 1 wherein said compound has the name [1. alpha. ,2. beta. (Z),3. beta. (1E,4S),4. alpha. ]-7-[3-(3-hydroxy-4-phenyl-1-p entenyl)bicyclo[2. 2. 1]hept-2-yl]-5-heptenoic acid or the methyl or ethyl ester thereof, including all stereoisomers thereof. 9. The method as defined in claim 1 wherein said compound has the name [1. alpha. ,2. beta. (Z),3. beta. (1E),4. alpha. ]-7-[3-(3-cyclohexyl-3-hydroxy-1- propenyl)bicyclo[2. 2. 1]hept-2-yl]-5-heptenoic acid including all stereoisomers thereof. 10. A method of inhibiting bronchoconstriction associated with asthma, which comprises administering to a mammalian host an effective amount of a compound having the structural formula ##STR14## and including all stereoisomers thereof; wherein A is --CH. sub. 2 --CH. sub. 2 or --CH. dbd. CH--; m is 0 to 5; B is --CH. dbd. CH-- or (CH. sub. 2). sub. 2 ; R is H, lower alkyl, alkali metal or tris(hydroxymethyl)aminomethane; and R
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