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    • 9. 发明申请
    • PHENYLKETONE CARBOXYLATE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF OSTEOPOROSIS
    • 苯甲酮羧酸酯化合物和药物组合物,用于预防和治疗卵巢功能
    • WO2016054725A1
    • 2016-04-14
    • PCT/CA2015/000530
    • 2015-10-08
    • PROMETIC BIOSCIENCES INC.
    • GAGNON, LyneGROUIX, Brigitte
    • A61K31/20A61K31/192A61P19/10C07C59/84C07C59/86C07C59/90
    • A61K31/192A61K31/20A61P19/08A61P19/10A61K2300/00
    • The present invention concerns the use of compounds for preventing and/or treating osteoporosis, for stimulating bone formation, for stimulating the differentiation and mineralization of osteoblasts, or for inhibiting bone resorption in a subject. These novel uses have been found for compounds represented by Formula I and pharmaceutically acceptable salts thereof. wherein: R 1 and R 2 are independently equal to H, F or OH; A is (CH 2 ) m COOH, W(CH2)mCOOH, or Y-CH(COOH)-(CH2)p-CH3 when B is H; or B is (CH2)mCOOH, W(CH2)mCOOH, or Y-CH(COOH)-(CH 2 ) p -CH 3 when A is H; or A and B are covalently bonded to form a five (5), six (6), or seven (7)-membered cycloalkyl substituted with COOH; where: Y is O, S, HN or CH 2 ; W is 0, S or NH; m is 0-2; and p is 3-7; D is CO(CH 2 ) n CH 3 or CHOH(CH 2 )nCH 3 or 0(CH 2 ) n CH 3 where n is 2-6; and E is H or F.
    • 本发明涉及化合物用于预防和/或治疗骨质疏松症,刺激骨形成,刺激成骨细胞的分化和矿化或抑制受试者的骨吸收的用途。 对于由式I表示的化合物及其药学上可接受的盐,已经发现了这些新用途。 其中:R1和R2独立地等于H,F或OH; 当B是H时,A是(CH 2)m COOH,W(CH 2)m COOH或Y-CH(COOH) - (CH 2)p -CH 3; 或者当A为H时,B为(CH 2)m COOH,W(CH 2)m COOH或Y-CH(COOH) - (CH 2)p -CH 3; 或A和B共价键合以形成被COOH取代的五(5),六(6)或七(7)元环烷基; 其中:Y为O,S,HN或CH2; W为0,S或NH; m为0-2; p为3-7; D是CO(CH 2)n CH 3或CHOH(CH 2)n CH 3或O(CH 2)n CH 3,其中n是2-6; E为H或F.