1-Piperidinophthalazines as cardiac stimulants
First Claim
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1. A method of treating congestive heart failure in a human subject having such condition which comprises parenterally administering to said human subject a congestive heart failure treating amount of a compound selected from the group consisting of:
- ##STR21## and a pharmaceutically acceptable acid addition salt thereof, wherein Y is selected from the group consisting of --CH2 COR1 wherein R1 is alkyl having from one to four carbon atoms or alkoxy having from one to four carbon atoms;
--N(R2)COR3 wherein R2 is hydrogen or alkyl having from one to four carbon atoms, and R3 is alkyl having from one to four carbon atoms, alkoxy having from one to four carbon atoms, phenyl or benzyloxy;
--N(R2)SO2 R4 wherein R2 is hydrogen or alkyl having from one to four carbon atoms and R4 is alkyl having from one to four carbon atoms, phenyl, pyridyl, benzyl or dialkoxyphenyl wherein said alkoxy has from one to four carbon atoms;
--N(R2)--CONR5 R6 wherein R2 is hydrogen or alkyl having from one to four carbon atoms, R5 is alkyl having from one to four carbon atoms, benzyl or pyridyl and R6 is hydrogen or alkyl having from one to four carbon atoms;
--O--CONHR.sub. 7 wherein R7 is alkyl having from one to four carbon atoms, phenyl, benzyl or pyridyl;
hydroxy;
alkanoyloxy having from one to four carbon atoms;
alkoxy having from one to four carbon atoms;
substituted alkyl wherein said alkyl has from one to five carbon atoms and said substituent is hydroxy, alkoxy having from one to four carbon atoms or --CONR2 R6 wherein R2 and R6 are each hydrogen or alkyl having from one to four carbon atoms; and
substituted alkoxy wherein said alkoxy has from two to four carbon atoms and said substituent is hydroxy or alkoxy having from one to four carbon atoms, with the proviso that other than the alpha-carbon atoms is substituted.
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Abstract
A series of 1-piperidinophthalazine derivatives as phosphodiesterase inhibitors and cardiac stimulants.
20 Citations
20 Claims
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1. A method of treating congestive heart failure in a human subject having such condition which comprises parenterally administering to said human subject a congestive heart failure treating amount of a compound selected from the group consisting of:
- ##STR21## and a pharmaceutically acceptable acid addition salt thereof, wherein Y is selected from the group consisting of --CH2 COR1 wherein R1 is alkyl having from one to four carbon atoms or alkoxy having from one to four carbon atoms;
--N(R2)COR3 wherein R2 is hydrogen or alkyl having from one to four carbon atoms, and R3 is alkyl having from one to four carbon atoms, alkoxy having from one to four carbon atoms, phenyl or benzyloxy;
--N(R2)SO2 R4 wherein R2 is hydrogen or alkyl having from one to four carbon atoms and R4 is alkyl having from one to four carbon atoms, phenyl, pyridyl, benzyl or dialkoxyphenyl wherein said alkoxy has from one to four carbon atoms;
--N(R2)--CONR5 R6 wherein R2 is hydrogen or alkyl having from one to four carbon atoms, R5 is alkyl having from one to four carbon atoms, benzyl or pyridyl and R6 is hydrogen or alkyl having from one to four carbon atoms;
--O--CONHR.sub. 7 wherein R7 is alkyl having from one to four carbon atoms, phenyl, benzyl or pyridyl;
hydroxy;
alkanoyloxy having from one to four carbon atoms;
alkoxy having from one to four carbon atoms;
substituted alkyl wherein said alkyl has from one to five carbon atoms and said substituent is hydroxy, alkoxy having from one to four carbon atoms or --CONR2 R6 wherein R2 and R6 are each hydrogen or alkyl having from one to four carbon atoms; and
substituted alkoxy wherein said alkoxy has from two to four carbon atoms and said substituent is hydroxy or alkoxy having from one to four carbon atoms, with the proviso that other than the alpha-carbon atoms is substituted. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
- ##STR21## and a pharmaceutically acceptable acid addition salt thereof, wherein Y is selected from the group consisting of --CH2 COR1 wherein R1 is alkyl having from one to four carbon atoms or alkoxy having from one to four carbon atoms;
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Current AssigneePfizer Inc.
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Original AssigneePfizer Inc.
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InventorsDanilewicz, John C., Campbell, Simon F., Ham, Allan L., Evans, Anthony G.
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Primary Examiner(s)Fagelson, Anna P.
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Application NumberUS06/103,342Time in Patent Office642 DaysField of Search424/250US Class Current514/248CPC Class CodesA61P 9/02 Non-specific cardiovascular...A61P 9/04 Inotropic agents, i.e. stim...A61P 9/06 AntiarrhythmicsA61P 9/08 Vasodilators for multiple i...A61P 9/10 for treating ischaemic or a...C07D 401/04 directly linked by a ring-m...
