Barrett Stephen Douglas,Ciske Fred Lawrence,Colombo Joseph Michael,Endres Gregory William,Germain Bradlee David,Kornilov Andriy,Kramer James Bernard,Uzieblo Adam,Owen Thomas Allen,O’malley James Paul
申请号:
NZ70417113
公开号:
NZ704171A
申请日:
2013.07.19
申请国别(地区):
NZ
年份:
2017
代理人:
摘要:
Abstract Disclosed is a pharmaceutical composition comprising 7-((R)-3,3-difluoro-5-((3S,4S,E)-3-hydroxy-4-methylnon-1-en-6-yn-1-yl)-2-oxopyrrolidin-1-yl)heptanoic acid, a calcium phosphate cement, and a demineralized bone matrix. Also disclosed is a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of formula (Ia), wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification. Further disclosed is the use of a compound of formula (Ia), or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for treating osteoporosis, bone fracture, or bone loss, or increasing bone density. Examples of compounds within the scope of formula (Ia) include 7-((R)-3,3-difluoro-5-((3S,4S,E)-3-hydroxy-4-methylnon-1-en-6-yn-1-yl)-2-oxopyrrolidin-1-yl)heptanoic acid, 7-((R)-3,3-difluoro-5-((3S,4S,E)-3-hydroxy-4-methyl-7-phenylhept-1-en-1-yl)-2-oxopyrrolidin-1-yl)heptanoic acid, 7-((R)-3,3-difluoro-5-((S,E)-3-hydroxyoct-1-en-1-yl)-2-oxopyrrolidin-1-yl)heptanoic acid, 5-(3-((R)-3,3-difluoro-5-((3S,4S,E)-3-hydroxy-4-methylnon-1-en-6-yn-1-yl)-2-oxopyrrolidin-1-yl)propyl)thiophene-2-carboxylic acid, 5-(3-((R)-3,3-difluoro-5-((3S,4S,E)-3-hydroxy-4-methyl-7-phenylhept-1-en-1-yl)-2-oxopyrrolidin-1-yl)propyl)thiophene-2-carboxylic acid, 5-(3-((R)-3,3-difluoro-5-((S,E)-3-hydroxyoct-1-en-1-yl)-2-oxopyrrolidin-1-yl)propyl)thiophene-2-carboxylic acid, 7-((R)-3,3-difluoro-5-((3S,4S,E)-3-hydroxy-4-methyl-8-phenyloct-1-en-1-yl)-2-oxopyrrolidin-1-yl)heptanoic acid, 5-(3-((R)-3,3-difluoro-5-((3S,4S,E)-3-hydroxy-4-methyl-8-phenyloct-1-en-1-yl)-2-oxopyrrolidin-1-yl)propyl)thiophene-2-carboxylic acid, and pharmaceutically acceptable salts thereof.