70922-35-9Relevant academic research and scientific papers
Design and synthesis of thrombin inhibitors: Analogues of MD-805 with reduced stereogenicity and improved potency
Brundish, Derek,Bull, Alice,Donovan, Vera,Fullerton, Joseph D.,Garman, Sheila M.,Hayler, Judy F.,Janus, Diana,Kane, Peter D.,McDonnell, Mark,Smith, Garrick P.,Wakeford, Robert,Walker, Clive V.,Howarth, Graham,Hoyle, William,Allen, Mark C.,Ambler, John,Butler, Keith,Talbot, Mark D.
, p. 4584 - 4603 (2007/10/03)
Mitsubishi's MD-805, a potent and selective inhibitor of thrombin which contains four stereogenic centers, has been the starting point for an optimization program. A systematic synthetic study resulted in thrombin inhibitors achiral at P2 and P3 but with
Cardiac stimulant 1-(3- or 4-substituted piperidino)phthalazines
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, (2008/06/13)
1-(3- or 4-substituted piperidino)phthalazines of the formula wherein R is C1-6 alkyl; Y is a 3- or 4-position substituent and is -X-(CHR1)m-Z wherein R1 is hydrogen or C1-6 alkyl; m is 1 or 2; X is oxygen or a direct link provided that when m is 1, X is a direct link; and Z is -N(R2)COR3, -N(R2)COOR3, -N(R2)SO2R3, -N(R2)SO2NR4R5, -N(R2)SOR3, -N(R2)CONR4R5 or -OCONR4R5, wherein R2 and R5 are each independently hydrogen or C1-6 alkyl; R3 is C1-6 alkyl, phenethyl, benzyl, C3-7 cycloalkyl, phenyl or pyridyl; R4 is hydrogen or R3; provided that when X is a direct link, R3 or R4 is C3-7 cycloalkyl; the pharmaceutically acceptable acid addition salts thereof; processes for their preparation; and their use as cardiac stimulants and phosphodiesterase inhibitors
