Vasopressin-2 receptor agonists, pharmaceutical compositions thereof and methods for using the foregoing for treating diabetes insipidus, primary nocturnal enuresis, and nocturia.

Vasopressin-2 receptor agonists, pharmaceutical compositions thereof and methods for using the foregoing for treating diabetes insipidus, primary nocturnal enuresis, and nocturia.

Compound of Formula I being cyclic metabolites of oxytocin. These derivatives have enhanced selectivity for the oxytocin receptor.

Compound of Formula I being cyclic metabolites of oxytocin. These derivatives have enhanced selectivity for the oxytocin receptor.

Methods and compositions are provided for treating and preventing preterm labor using liposome encapsulated tocolytic agents, such as indomethacin. In certain aspects, targeted liposomes are provided that allow delivery of tocolytic agents directly to the uterus, such as by targeting to the oxytocin receptor.

Methods and compositions are provided for treating and preventing preterm labor using liposome encapsulated tocolytic agents, such as indomethacin. In certain aspects, targeted liposomes are provided that allow delivery of tocolytic agents directly to the uterus, such as by targeting to the oxytocin receptor.

The present invention relates to crystalline forms of carbetocin, a method of their manufacture, and pharmaceutical compositions thereof.

The present invention relates to crystalline forms of carbetocin, a method of their manufacture, and pharmaceutical compositions thereof.

The present disclosure discloses a liquid-phase synthesis method of oxytocin under mild conditions for the first time, which is characterized in that three oxytocin fragments which include Boc-Cys(Acm)-Tyr(tBu)-OH, H-Ile-Gln(Trt)-Asn(Trt)-Cys(Acm)-Pro-OMe and H-Leu-Gly-NH.sub.2 are synthesized for the first time, the fragments are assembled to synthesize an all-protected oxytocin amino acid sequence, iodine is used to remove Acm while cyclization is performed to form a disulfide bond to obtain protected cyclic oxytocin, trifluoroacetic acid is used to remove residual protecting groups to obtain crude oxytocin, ethyl acetate is used to perform recrystallization, and reversed-phase chromatography purification is performed to reach high-purity (crude product purity reaches 95%) and high biological value of oxytocin (588 IU/mg). In the present invention, a Boc-polypeptide synthesis and Fmoc-polypeptide synthesis combined method is provided, wherein, all the reactions are carried out under mild conditions without using the ammonia-sodium-method decapping reaction which is reported by literature referring to oxytocin liquid-phase synthesis domestically and abroad. Furthermore, the liquid-phase synthesis method of oxytocin is first performed without highly toxic reagents and unsafe reaction conditions, thus greatly reducing the cost of oxytocin synthesis and providing access to industrial production of oxytocin.

The present disclosure discloses a liquid-phase synthesis method of oxytocin under mild conditions for the first time, which is characterized in that three oxytocin fragments which include Boc-Cys(Acm)-Tyr(tBu)-OH, H-Ile-Gln(Trt)-Asn(Trt)-Cys(Acm)-Pro-OMe and H-Leu-Gly-NH.sub.2 are synthesized for the first time, the fragments are assembled to synthesize an all-protected oxytocin amino acid sequence, iodine is used to remove Acm while cyclization is performed to form a disulfide bond to obtain protected cyclic oxytocin, trifluoroacetic acid is used to remove residual protecting groups to obtain crude oxytocin, ethyl acetate is used to perform recrystallization, and reversed-phase chromatography purification is performed to reach high-purity (crude product purity reaches 95%) and high biological value of oxytocin (588 IU/mg). In the present invention, a Boc-polypeptide synthesis and Fmoc-polypeptide synthesis combined method is provided, wherein, all the reactions are carried out under mild conditions without using the ammonia-sodium-method decapping reaction which is reported by literature referring to oxytocin liquid-phase synthesis domestically and abroad. Furthermore, the liquid-phase synthesis method of oxytocin is first performed without highly toxic reagents and unsafe reaction conditions, thus greatly reducing the cost of oxytocin synthesis and providing access to industrial production of oxytocin.