LOW-DOSED ORAL DOSAGE FORMS FOR TREATMENT OF DISEASES
    1.
    发明申请
    LOW-DOSED ORAL DOSAGE FORMS FOR TREATMENT OF DISEASES 审中-公开
    低剂量口服剂型用于治疗疾病

    公开(公告)号:WO2018011015A1

    公开(公告)日:2018-01-18

    申请号:PCT/EP2017/066618

    申请日:2017-07-04

    CPC分类号: A61K31/58 A61P17/06

    摘要: The present invention relates to a low-dosed oral dosage form for treatment and/or prophylaxis of diseases, especially of endometriosis, polycystic ovary syndrome and/or atopic dermatitis. More particularly, the present invention concerns oral dosage forms comprising up to 120 mg N- {[17-(5- Fluoropyridin-3-yl)estra-l,3,5(10),16-tetraen-3-yl]carbonyl} -N-methyl-P-alanine per day.

    摘要翻译: 本发明涉及用于治疗和/或预防疾病,尤其是子宫内膜异位,多囊卵巢综合征和/或特应性皮炎的低剂量口服剂型。 更特别地,本发明涉及口服剂型,其包含至多120mg的N - {[17-(5-氟吡啶-3-基)雌-1,3,5(10),16-四烯-3-基]羰基 } -N-甲基-β-丙氨酸/天。

    COMPOUNDS FOR THE TREATMENT OF HORMONE-DEPENDENT DISEASES
    2.
    发明申请
    COMPOUNDS FOR THE TREATMENT OF HORMONE-DEPENDENT DISEASES 审中-公开
    用于治疗依赖于HOMMONE的疾病的化合物

    公开(公告)号:WO2015024111A1

    公开(公告)日:2015-02-26

    申请号:PCT/CA2014050728

    申请日:2014-08-01

    申请人: UNIV LAVAL

    摘要: Provided are compounds of general formula A and A', wherein X1 and X2 are each C, CH or N; R3 and R4 are each H, optionally substituted C1-C30 saturated or unsaturated chemical group, or together form an optionally substituted C5-C8 cycle; Z1; Z2 and Z3 are each N or CH; V is C=0, C=S or CH2; n is from 1 to 12; W1 and W2 are each H, CH2, O or S; and R1 and R2 are each H, Cr1C6 alkyl, C1C6 aryl, C1C12 alkylaryl, optionally substituted phenyl, C1C6 alkoxy, C1C6 thioalkoxy, F, CI, Br or I. These compounds inhibit steroid sulfatase (STS), act as selective estrogen receptor modulators (SERMs), increase alkaline phosphatase (ALP) activity, and are useful in the treatment of medical conditions involving hormones such as breast cancer, prostate cancer, endometriosis, osteoporosis, benign prostatic hyperplasia and endometrial cancer.

    摘要翻译: 提供通式A和A'的化合物,其中X 1和X 2各自为C,CH或N; R 3和R 4各自为H,任选取代的C 1 -C 30饱和或不饱和化学基团,或一起形成任选取代的C 5 -C 8周期; Z1; Z2和Z3各自为N或CH; V为C = O,C = S或CH 2; n为1〜12; W1和W2分别为H,CH2,O或S; 并且R 1和R 2各自为H,C 1 -C 6烷基,C 1 -C 6芳基,C 1 -C 12烷基芳基,任选取代的苯基,C 1 -C 6烷氧基,C 1 -C 6硫代烷氧基,F,Cl,Br或I.这些化合物抑制类固醇硫酸酯酶(STS),作为选择性雌激素受体调节剂 (SERMs),增加碱性磷酸酶(ALP)活性,并且可用于治疗涉及激素如乳腺癌,前列腺癌,子宫内膜异位,骨质疏松症,良性前列腺增生和子宫内膜癌的医学病症。

    THERAPEUTICALLY ACTIVE 17-NITROGEN SUBSTITUTED ESTRATRIENTHIAZOLE DERIVATIVES AS INHIBITORS OF 17.BETA.-HYDROXYSTEROID DEHYDROGENASE
    3.
    发明申请
    THERAPEUTICALLY ACTIVE 17-NITROGEN SUBSTITUTED ESTRATRIENTHIAZOLE DERIVATIVES AS INHIBITORS OF 17.BETA.-HYDROXYSTEROID DEHYDROGENASE 审中-公开
    作为17.BETA.-羟基脱氢酶脱氢酶的抑制剂的治疗性活性的17-硝基取代的咪唑并噻吩衍生物

    公开(公告)号:WO2014207310A1

    公开(公告)日:2014-12-31

    申请号:PCT/FI2014/050518

    申请日:2014-06-25

    摘要: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2to R7are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD and in treatment or prevention of steroid hormone de- pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17β-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the afore- mentioned compounds or pharmaceutically acceptable salts thereof.

    摘要翻译: 本发明涉及式(I)化合物及其药学上可接受的盐,其中R 2至R 7如权利要求中所定义。 本发明进一步涉及它们作为17β-抑制剂-HSD的抑制剂的用途,以及用于治疗或预防类固醇激素依赖性疾病或病症,例如类固醇激素依赖性疾病或需要抑制17β-HSD1酶和/或 需要降低内源性雌二醇浓度。 本发明还涉及上述化合物的制备和药物组合物,其包含一种或多种上述化合物或其药学上可接受的盐作为活性成分。

    PROGESTERONE-RECEPTOR ANTAGONIST FOR USE IN BRCA ALONE OR AS COMBINATION WITH ANTIESTROGEN
    10.
    发明申请
    PROGESTERONE-RECEPTOR ANTAGONIST FOR USE IN BRCA ALONE OR AS COMBINATION WITH ANTIESTROGEN 审中-公开
    用于BRCA的PROGESTERONE-RECEPTOR ANTAGONIST或与ANENSTROGEN组合使用

    公开(公告)号:WO2008128791A2

    公开(公告)日:2008-10-30

    申请号:PCT/EP2008003333

    申请日:2008-04-21

    摘要: The present invention relates to the single use of the progesterone-receptor antagonist 11ß-(-4-acetylpheny)-17 ß-hydroxy-17a-(1,1,2,2,2-pentafluoroethyl)- estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, as well as to a combination comprising the progesterone- receptor antagonist 11 ß-(4-acetylphenyl)-17ß-hydroxy-17a-(1,1,2,2,2- pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one pure antiestrogen, for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, ovarian cancer endometrial cancer, gastric cancer, colorectal cancer.endometriosis, myeloma, myoma and meningioma. The present invention also relates to a combination of the progesterone-receptor antagonist 11 ß-(4-acetylphenyl)-17ß-hydroxy-17a-(1,1,2,2,2-pentafluoroethyl)-estra-4,9- dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one EGF or EGFR targeting drug, for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, ovarian cancer endometrial cancer, gastric cancer, colorectal cancer, endometriosis, myeloma, myoma and meningioma.

    摘要翻译: 本发明涉及孕酮 - 受体拮抗剂11β-( - 4-乙酰基苯基)-17β-羟基-17a-(1,1,2,2,2-五氟乙基) - 雌甾-4,9- 二烯-3-酮或其药学上可接受的衍生物或类似物,用于预防和治疗BRCA1或BRCA2介导的乳腺癌,以及包含孕酮受体拮抗剂11β-(4-乙酰基苯基)-17β (1,1,2,2,2-五氟乙基) - 雌-4,9-二烯-3-酮或其药学上可接受的衍生物或类似物以及至少一种纯抗雌激素用于预防 和BRCA1或BRCA2介导的乳腺癌,卵巢癌子宫内膜癌,胃癌,结肠直肠癌,子宫内膜异位症,骨髓瘤,肌瘤和脑膜瘤的治疗。 本发明还涉及孕酮受体拮抗剂11β-(4-乙酰基苯基)-17β-羟基-17a-(1,1,2,2,2-五氟乙基) - 雌-4,9-二烯 -3-或其药学上可接受的衍生物或类似物,以及至少一种EGF或EGFR靶向药物,用于预防和治疗BRCA1或BRCA2介导的乳腺癌,卵巢癌子宫内膜癌,胃癌,结肠直肠癌, 子宫内膜异位症,骨髓瘤,肌瘤和脑膜瘤。