N1-cyclic amine-N5-substituted phenyl biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same
    1.
    发明授权
    N1-cyclic amine-N5-substituted phenyl biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same 有权
    N 1 - 环胺-N 5取代的苯基双胍衍生物,其制备方法和包含其的药物组合物

    公开(公告)号:US09540325B2

    公开(公告)日:2017-01-10

    申请号:US14237514

    申请日:2012-08-08

    摘要: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.

    摘要翻译: 提供式1的N 1 - 环胺-N 5 - 取代的苯基双胍衍生物或其药学上可接受的盐,其制备方法和包含双胍衍生物或其药学上可接受的盐作为活性成分的药物组合物。 双胍衍生物具有抑制癌细胞增殖的作用,并且还表现出抗肿瘤活性,包括抑制癌症转移和癌症复发,因为即使以小剂量施用也能有效地激活与能量代谢控制有关的AMPK 与常规药物相比。 此外,双胍衍生物通过AMPK活化降低血糖和脂质浓度高度有效,因此可有效用于治疗糖尿病,肥胖症,高脂血症,高胆固醇血症,脂肪肝,冠状动脉疾病,骨质疏松症,多囊卵巢综合征和代谢 综合征

    N1-cyclic amine-N5-substituted biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same
    2.
    发明授权
    N1-cyclic amine-N5-substituted biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same 有权
    N 1 - 环胺-N 5取代双胍衍生物,其制备方法和包含其的药物组合物

    公开(公告)号:US09321742B2

    公开(公告)日:2016-04-26

    申请号:US14237546

    申请日:2012-08-08

    摘要: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.

    摘要翻译: 提供式1的N 1 - 环胺-N 5 - 取代双胍衍生物或其药学上可接受的盐,其制备方法和包含双胍衍生物或其药学上可接受的盐作为活性成分的药物组合物。 双胍衍生物具有抑制癌细胞增殖的作用,并且还表现出抗肿瘤活性,包括抑制癌症转移和癌症复发,因为即使以小剂量施用也能有效地激活与能量代谢控制有关的AMPK 与常规药物相比。 此外,双胍衍生物通过AMPK活化降低血糖和脂质浓度高度有效,因此可有效用于治疗糖尿病,肥胖症,高脂血症,高胆固醇血症,脂肪肝,冠状动脉疾病,骨质疏松症,多囊卵巢综合征和代谢 综合征

    N1-Cyclic Amine-N5-Substituted Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same
    3.
    发明申请
    N1-Cyclic Amine-N5-Substituted Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same 有权
    N1环状胺-N5取代双胍衍生物,其制备方法和药物组合物

    公开(公告)号:US20140179661A1

    公开(公告)日:2014-06-26

    申请号:US14237546

    申请日:2012-04-08

    摘要: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.

    摘要翻译: 提供式1的N 1 - 环胺-N 5 - 取代双胍衍生物或其药学上可接受的盐,其制备方法和包含双胍衍生物或其药学上可接受的盐作为活性成分的药物组合物。 双胍衍生物具有抑制癌细胞增殖的作用,并且还表现出抗肿瘤活性,包括抑制癌症转移和癌症复发,因为即使以小剂量施用也能有效地激活与能量代谢控制有关的AMPK 与常规药物相比。 此外,双胍衍生物通过AMPK活化降低血糖和脂质浓度高度有效,因此可有效用于治疗糖尿病,肥胖症,高脂血症,高胆固醇血症,脂肪肝,冠状动脉疾病,骨质疏松症,多囊卵巢综合征和代谢 综合征

    N1-Cyclic Amine-N5-Substituted Phenyl Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same
    5.
    发明申请
    N1-Cyclic Amine-N5-Substituted Phenyl Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same 有权
    N1环状胺-N5取代苯基双胍衍生物,其制备方法和药物组合物

    公开(公告)号:US20140179660A1

    公开(公告)日:2014-06-26

    申请号:US14237514

    申请日:2012-08-08

    摘要: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.

    摘要翻译: 提供式1的N 1 - 环胺-N 5 - 取代的苯基双胍衍生物或其药学上可接受的盐,其制备方法和包含双胍衍生物或其药学上可接受的盐作为活性成分的药物组合物。 双胍衍生物具有抑制癌细胞增殖的作用,并且还表现出抗肿瘤活性,包括抑制癌症转移和癌症复发,因为即使以小剂量施用也能有效地激活与能量代谢控制有关的AMPK 与常规药物相比。 此外,双胍衍生物通过AMPK活化降低血糖和脂质浓度高度有效,因此可有效用于治疗糖尿病,肥胖症,高脂血症,高胆固醇血症,脂肪肝,冠状动脉疾病,骨质疏松症,多囊卵巢综合征和代谢 综合征