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Patent Searching and Data


Title:
CYCLIC HEXAPEPTIDE OXYTOCIN ANTAGONIST
Document Type and Number:
Japanese Patent JPH05112600
Kind Code:
A
Abstract:

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.


Inventors:
MAAKU JII BOTSUKU
ROJIYAA DEE TSUNGU
ROJIYAA EMU FUREIDEINGAA
DANIERU EFU BUEBAA
PEETAA DEE UIRIAMUSU
Application Number:
JP21676991A
Publication Date:
May 07, 1993
Filing Date:
February 27, 1991
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
C07D487/14; C07D487/22; C07D513/14; C07K7/06; C07K7/16; C07K7/64; (IPC1-7): C07D487/14; C07D487/22; C07D513/14; C07K7/06; C07K7/64; C07K99/00
Attorney, Agent or Firm:
Masao Okabe (6 others)