137730-67-7Relevant articles and documents
Serine derivatives and their use as therapeutic agents
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, (2008/06/13)
The present invention relates to compounds of formula (I): STR1 wherein m is zero, 1 or 2; and n is zero or 1, with the proviso that the sum total of m+n is 1 or 2; R1 represents phenyl; naphthyl; benzhydryl; or benzyl, where the naphthyl group or any phenyl moiety may be substituted; R2 represents hydrogen; phenyl; heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; naphthyl; benzhydryl; or benzyl; wherein each heteroaryl, the naphthyl group and any phenyl moiety may be substituted; R3 and R4 each independently represents hydrogen or C1-6 alkyl or R3 and R4 together are linked so as to form a C1-3 alkylene chain; Q represents CR5 R6 or NR5 ; X and Y each independently represents hydrogen, or together form a group =O; and Z represents a bond, O, S, SO, SO2, NRc or --(CRc Rd)--, where Rc and Rd each independently represent hydrogen or C1-6 alkyl; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
Piperidinylcamphorsulfonyl oxytocin antagonists
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, (2008/06/13)
Spirocyclic compounds of the formula: are oxytocin and vasopressin antagonists useful in the treatment of pre-term labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery, timing of parturition, uterine hyperactivity, endometriosis, hypertension, congestive heart failure, hyponatremia and cognitive disorders.
Orally Active, Nonpeptide Oxytocin Antagonists
Evans, Ben E.,Leighton, James L.,Rittle, Kenneth E.,Gilbert, Kevin F.,Lundell, George F.,et al.
, p. 3919 - 3927 (2007/10/02)
The first nonpeptide antagonists of the neurohypophyseal hormone, oxytocin (OT) are described.Derivatives of the spiroindenepiperidine ring system, these compounds include L-366,509, an orally bioavailable OT antagonist with good in vivo duration.The potential use of these agents for treatment of preterm labor and their significance as new nonpeptide ligands for peptide receptors are discussed.