PURPOSE: To obtain a new compd. useful in the treatment of preterm labor and dysmenorrhea and for stoppage of labor preparatory to Caesarian delivery as an oxytocin antagonist.
CONSTITUTION: The new compd. is a compd. of formula I [where A is Gly, Ala, etc.; B is Pro, Ser, etc.; C is Ala, His, etc.; R1 is H, glycyl, etc.; R3-R5 are H, allyl, etc.; R6 is H, phenyl, etc.; R7 is H, hydroxyl, etc.; and (m) is 0-2] or its salt, e.g. cyclo[D-phenylalanyl-L-isoleucyl-D-pipecolyl-L-pipecolyl-D(N[α]- methyl)phenylalanyl-L-prolyl. The compd. is obtd. by successively bonding protected amino acids of formulae II-IV (where Boc is t-butyloxycarbonyl and Fmoc is fluorenylmethyloxycarbonyl) to a solid phase resin substrate, cleaving the resultant straight hexsapeptide bonded to the resin from the resin and cyclizing the resultant straight hexapepetide of formula V.
WO/2005/094878 | COMPOSITION HAVING ANTITUMOR EFFECT |
JP2021152071 | BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT |
WO/2014/014951 | 5-HT3 RECEPTOR ANTAGONISTS |
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