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1. 发明申请

WO2013022279A2 N1-CYCLIC AMINE-N5-SUBSTITUTED BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译： N1-环状胺-N5-取代的双胍衍生物，其制备方法和包含该化合物的药物组合物
公开(公告)号：WO2013022279A2
公开(公告)日：2013-02-14
申请号：PCT/KR2012006327
申请日：2012-08-08
申请人： HANALL BIOPHARMA CO LTD , KIM SUNG WUK , MIN CHANG HEE , PARK SE HWAN , KIM DUCK , LEE JI SUN , KIM YONG EUN , OH JU HOON
发明人： KIM SUNG WUK , MIN CHANG HEE , PARK SE HWAN , KIM DUCK , LEE JI SUN , KIM YONG EUN , OH JU HOON
IPC分类号： C07C279/26 , A61K31/155 , A61P35/00 , C07C277/02
CPC分类号： C07D295/215 , C07D205/04 , C07D213/40 , C07D307/52 , C07D333/20
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：提供了式1的N1-环胺-N5-取代的双胍衍生物或其药学上可接受的盐，其制备方法以及包含该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效果，并且即使以小剂量给药也具有与能量代谢的控制相关的活化AMPK的活化作用，因此具有抑制癌转移和癌复发的抗癌活性与传统药物相比。此外，双胍衍生物在通过AMPK活化降低血糖和脂质浓度方面非常有效，因此它们可以有效地用于治疗糖尿病，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。

2. 发明申请

WO2013022278A2 N1-CYCLIC AMINE-N5-SUBSTITUTED PHENYL BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译： N1循环胺-N5取代苯基双胍衍生物，其制备方法和包含其的药物组合物
公开(公告)号：WO2013022278A2
公开(公告)日：2013-02-14
申请号：PCT/KR2012/006326
申请日：2012-08-08
申请人： HANALL BIOPHARMA CO., LTD. , KIM, Sung Wuk , MIN, Chang Hee , PARK, Se Hwan , KIM, Duck , LEE, Ji Sun , KIM, Yong Eun , OH, Ju Hoon
发明人： KIM, Sung Wuk , MIN, Chang Hee , PARK, Se Hwan , KIM, Duck , LEE, Ji Sun , KIM, Yong Eun , OH, Ju Hoon
IPC分类号： C07C279/26 , C07C277/02 , A61K31/155 , A61P35/00
CPC分类号： C07D211/14 , C07D205/04 , C07D207/04 , C07D207/06 , C07D211/06 , C07D223/04 , C07D257/04 , C07D295/14 , C07D295/215
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，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。

3. 发明申请

WO2013019058A2 PHARMACEUTICAL COMPOSITION FOR INHIBITING CANCER RECURRENCE OR METASTASIS 审中-公开
标题翻译：用于抑制癌症复发或METASTASIS的药物组合物
公开(公告)号：WO2013019058A2
公开(公告)日：2013-02-07
申请号：PCT/KR2012006096
申请日：2012-07-31
申请人： HANALL BIOPHARMA CO LTD , KIM SUNG-WUK , MIN CHANG-HEE , KOO JA-SEONG , SUN SANG-OUK , KIM YONG-EUN
发明人： KIM SUNG-WUK , MIN CHANG-HEE , KOO JA-SEONG , SUN SANG-OUK , KIM YONG-EUN
IPC分类号： A61K31/70 , A61K31/7004 , A61P35/00
CPC分类号： A61K45/06 , A61K9/2054 , A61K31/155 , A61K31/4015 , A61K31/7004 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition for inhibiting cancer recurrence or metastasis and a method for inhibiting cancer recurrence or metastasis using the same. The present invention identified the activity of 2-deoxy-D-glucose (2-DG, below) for the inhibition of mammosphere formation and EMT, indicating its inhibitory effect against proliferation of cancer stem cell and cancer metastasis, which has not been known hitherto. The present invention also identified that the combined use of a biguanide based antidiabetic agent or its pharmaceutically acceptable salt and 2-DG can inhibit cancer metastasis and steeply decrease cancer recurrence in comparison to the single use of said active ingredients, resulting in a superior effect in the inhibition of cancer metastasis and recurrence when the same dosage is applied. Therefore, the pharmaceutical composition of the present invention can be used to show substantially more excellent effect with less amount of each active ingredient, reducing the side effects due to the use of excess drug and due to their pharmacological action, and providing more efficacious treatment. Moreover, when it is used along with an anticancer agent to which resistance is shown, it is expected that more synergistic effect can be exhibited. Therefore, the pharmaceutical composition and method for inhibiting cancer recurrence or metastasis according to the present invention can be used very advantageously for the treatment and prevention of metastasis or recurrence of various cancer diseases.
摘要翻译：本发明涉及抑制癌症复发或转移的药物组合物，以及使用该组合物抑制癌症复发或转移的方法。本发明鉴定了2-脱氧-D-葡萄糖（2-DG，以下）用于抑制乳腺球形成和EMT的活性，表明其对癌干细胞增殖的抑制作用和癌转移，迄今尚未知晓。本发明还指出，与单次使用所述活性成分相比，基于双胍类抗糖尿病药或其药学上可接受的盐和2-DG的组合使用可以抑制癌症转移并急剧降低癌症复发，导致在当施用相同的剂量时，抑制癌症转移和复发。因此，本发明的药物组合物可以用较少量的各种活性成分显示出更优异的效果，减少由于使用过量药物引起的副作用，并由于其药理作用，并提供更有效的治疗。此外，当与其所示的抗癌剂一起使用时，预期可以表现出更多的协同效应。因此，根据本发明的用于抑制癌症复发或转移的药物组合物和方法可以非常有利地用于治疗和预防各种癌症疾病的转移或复发。

4. 发明申请

WO2011159100A3 ANTI-CANCER PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：抗癌药物组合物
公开(公告)号：WO2011159100A3
公开(公告)日：2012-05-03
申请号：PCT/KR2011004382
申请日：2011-06-15
申请人： HANALL BIOPHARMA CO LTD , KIM SUNG-WUK , JUN SUNG-SOO , MIN CHANG-HEE , KOO JA-SEONG , KIM JIN-WOOK , KIM YONG-EUN , SUN SANG-OUK
发明人： KIM SUNG-WUK , JUN SUNG-SOO , MIN CHANG-HEE , KOO JA-SEONG , KIM JIN-WOOK , KIM YONG-EUN , SUN SANG-OUK
IPC分类号： A61K31/155 , A61K31/70 , A61P35/00
CPC分类号： A61K31/155 , A61K31/7004 , A61K2300/00
摘要： The present invention relates to an anti-cancer pharmaceutical composition comprising phenformin or a pharmaceutically acceptable salt thereof and 2-deoxy-D-glucose as active ingredients, having anticancer activity. The pharmaceutical composition shows far superior anticancer effects through the synergistic action between each active ingredient over the case using a single active ingredient, and can reduce the side effects caused by drugs due to the decrease of dose. In addition, the present invention can remarkably reduce side effects such as lactic acidosis caused by phenformin through delayed release or delayed administration of active ingredients. Particularly, the pharmaceutical composition according to the present invention also has increased compliance of a patient, and thus can be very useful for treating various types of cancers.
摘要翻译：本发明涉及具有抗癌活性的包含苯乙双胍或其药学上可接受的盐和作为活性成分的2-脱氧-D-葡萄糖的抗癌药物组合物。通过使用单一活性成分的情况下的各活性成分之间的协同作用，药物组合物显示出优异的抗癌作用，并且可以减少由于剂量降低而引起的药物副作用。此外，本发明可以通过延迟释放或延迟施用活性成分显着降低由苯乙双胍引起的乳酸性酸中毒的副作用。特别地，根据本发明的药物组合物也具有增加患者的依从性，因此可以非常适用于治疗各种类型的癌症。

5. 发明申请

WO2011083999A2 BIGUANIDE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ACTIVE INGREDIENT 审中-公开
标题翻译： BIGUANIDE衍生物，其制备方法和含有作为活性成分的药物组合物
公开(公告)号：WO2011083999A2
公开(公告)日：2011-07-14
申请号：PCT/KR2011000098
申请日：2011-01-06
申请人： HANALL BIOPHARMA CO LTD , KIM SUNG WUK , JUN SUNG SOO , MIN CHANG HEE , PARK SE HWAN , KIM YONG EUN , KIM DUCK , LEE JI SUN , OH JU HOON
发明人： KIM SUNG WUK , JUN SUNG SOO , MIN CHANG HEE , PARK SE HWAN , KIM YONG EUN , KIM DUCK , LEE JI SUN , OH JU HOON
IPC分类号： C07C279/26 , A61K31/155 , A61P3/10 , A61P35/00 , C07C277/00
CPC分类号： A61K31/155 , A61K31/341 , A61K31/4406 , A61K31/472 , C07C277/04 , C07C279/04 , C07C279/06 , C07C279/08 , C07C279/16 , C07C279/18 , C07C279/26 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D213/38 , C07D307/52 , C07D317/58 , C07D333/20
摘要： The present invention provides a biguanide derivative or pharmaceutically acceptable salt thereof represented by Formula 1 with N4-N5-substitutions, a preparation method thereof and a pharmaceutical composition containing the biguanide derivative as an active ingredient. Compared with conventional drugs, even a small amount of the biguanide derivative of the present invention exhibits excellent effects of AMPKa activation and inhibition of cancer cell proliferation, which makes it useful for the treatment of diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer and the like.
摘要翻译：本发明提供由式1表示的具有N4-N5取代基的双胍衍生物或其药学上可接受的盐，其制备方法和含有双胍衍生物作为活性成分的药物组合物。与常规药物相比，即使少量本发明的双胍衍生物也表现出AMPKa活化和癌细胞增殖抑制作用的优异性，因此可用于治疗糖尿病，肥胖症，高脂血症，高胆固醇血症，脂肪肝，冠心病动脉疾病，骨质疏松症，多囊卵巢综合征，代谢综合征，癌症等。

6. 发明申请

WO2013022278A3 N1-CYCLIC AMINE-N5-SUBSTITUTED PHENYL BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译： N1-环状胺-N5-取代的苯基双胍衍生物，其制备方法和包含该化合物的药物组合物
公开(公告)号：WO2013022278A3
公开(公告)日：2013-04-25
申请号：PCT/KR2012006326
申请日：2012-08-08
申请人： HANALL BIOPHARMA CO LTD , KIM SUNG WUK , MIN CHANG HEE , PARK SE HWAN , KIM DUCK , LEE JI SUN , KIM YONG EUN , OH JU HOON
发明人： KIM SUNG WUK , MIN CHANG HEE , PARK SE HWAN , KIM DUCK , LEE JI SUN , KIM YONG EUN , OH JU HOON
IPC分类号： C07C279/26 , A61K31/155 , A61P35/00 , C07C277/02
CPC分类号： C07D211/14 , C07D205/04 , C07D207/04 , C07D207/06 , C07D211/06 , C07D223/04 , C07D257/04 , C07D295/14 , C07D295/215
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：提供了式1的N1-环胺-N 5 - 取代苯基双胍衍生物或其药学上可接受的盐，其制备方法以及包含该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效果，并且即使以小剂量给药也具有与能量代谢的控制相关的活化AMPK的活化作用，因此具有抑制癌转移和癌复发的抗癌活性与传统药物相比。此外，双胍衍生物在通过AMPK活化降低血糖和脂质浓度方面非常有效，因此它们可以有效地用于治疗糖尿病，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。

7. 发明申请

WO2013022280A3 N1-CYCLIC AMINE-N2-SUBSTITUTED BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译： N1循环胺-N 2取代的双胍衍生物，其制备方法和包含其的药物组合物
公开(公告)号：WO2013022280A3
公开(公告)日：2013-04-25
申请号：PCT/KR2012006328
申请日：2012-08-08
申请人： HANALL BIOPHARMA CO LTD , KIM SUNG WUK , MIN CHANG HEE , PARK SE HWAN , KIM DUCK , LEE JI SUN , KIM YONG EUN , OH JU HOON
发明人： KIM SUNG WUK , MIN CHANG HEE , PARK SE HWAN , KIM DUCK , LEE JI SUN , KIM YONG EUN , OH JU HOON
IPC分类号： C07C279/26 , A61K31/155 , A61P35/00 , C07C277/02
CPC分类号： C07D307/52 , C07D295/215 , C07D333/20
摘要： An N1-cyclic amine-N2-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 2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，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。

8. 发明申请

WO2013022279A3 N1-CYCLIC AMINE-N5-SUBSTITUTED BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
公开(公告)号：WO2013022279A3
公开(公告)日：2013-02-14
申请号：PCT/KR2012/006327
申请日：2012-08-08
申请人： HANALL BIOPHARMA CO., LTD. , KIM, Sung Wuk , MIN, Chang Hee , PARK, Se Hwan , KIM, Duck , LEE, Ji Sun , KIM, Yong Eun , OH, Ju Hoon
发明人： KIM, Sung Wuk , MIN, Chang Hee , PARK, Se Hwan , KIM, Duck , LEE, Ji Sun , KIM, Yong Eun , OH, Ju Hoon
IPC分类号： C07C279/26 , C07C277/02 , A61K31/155 , A61P35/00
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.

9. 发明申请

WO2013019058A3 PHARMACEUTICAL COMPOSITION FOR INHIBITING CANCER RECURRENCE OR METASTASIS 审中-公开
公开(公告)号：WO2013019058A3
公开(公告)日：2013-02-07
申请号：PCT/KR2012/006096
申请日：2012-07-31
申请人： HANALL BIOPHARMA CO., LTD. , KIM, Sung-Wuk , MIN, Chang-Hee , KOO, Ja-Seong , SUN, Sang-Ouk , KIM, Yong-Eun
发明人： KIM, Sung-Wuk , MIN, Chang-Hee , KOO, Ja-Seong , SUN, Sang-Ouk , KIM, Yong-Eun
IPC分类号： A61K31/70 , A61K31/7004 , A61P35/00
摘要： The present invention relates to a pharmaceutical composition for inhibiting cancer recurrence or metastasis and a method for inhibiting cancer recurrence or metastasis using the same. The present invention identified the activity of 2-deoxy-D-glucose (2-DG, below) for the inhibition of mammosphere formation and EMT, indicating its inhibitory effect against proliferation of cancer stem cell and cancer metastasis, which has not been known hitherto. The present invention also identified that the combined use of a biguanide based antidiabetic agent or its pharmaceutically acceptable salt and 2-DG can inhibit cancer metastasis and steeply decrease cancer recurrence in comparison to the single use of said active ingredients, resulting in a superior effect in the inhibition of cancer metastasis and recurrence when the same dosage is applied. Therefore, the pharmaceutical composition of the present invention can be used to show substantially more excellent effect with less amount of each active ingredient, reducing the side effects due to the use of excess drug and due to their pharmacological action, and providing more efficacious treatment. Moreover, when it is used along with an anticancer agent to which resistance is shown, it is expected that more synergistic effect can be exhibited. Therefore, the pharmaceutical composition and method for inhibiting cancer recurrence or metastasis according to the present invention can be used very advantageously for the treatment and prevention of metastasis or recurrence of various cancer diseases.

10. 发明申请

WO2011083998A3 BIGUANIDE DERIVATIVE, A PREPARATION METHOD THEREOF AND A PHARMACEUTICAL COMPOSITION CONTAINING THE BIGUANIDE DERIVATIVE AS AN ACTIVE INGREDIENT 审中-公开
标题翻译：双胍衍生物及其制备方法和含有双胍衍生物作为活性成分的药物组合物
公开(公告)号：WO2011083998A3
公开(公告)日：2011-10-27
申请号：PCT/KR2011000097
申请日：2011-01-06
申请人： HANALL BIOPHARMA CO LTD , KIM SUNG WUK , JUN SUNG SOO , MIN CHANG HEE , KIM YOUNG WOONG , KANG MIN SEOK , OH BYUNG KYU , PARK SE HWAN , KIM YONG EUN , KIM DUCK , LEE JI SUN , OH JU HOON
发明人： KIM SUNG WUK , JUN SUNG SOO , MIN CHANG HEE , KIM YOUNG WOONG , KANG MIN SEOK , OH BYUNG KYU , PARK SE HWAN , KIM YONG EUN , KIM DUCK , LEE JI SUN , OH JU HOON
IPC分类号： C07C279/26 , A61K31/155 , A61P3/10 , A61P35/00 , C07C277/02
CPC分类号： A61K31/155 , A61K31/341 , A61K31/4406 , A61K31/472 , C07C277/04 , C07C279/04 , C07C279/06 , C07C279/08 , C07C279/16 , C07C279/18 , C07C279/26 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D213/38 , C07D307/52 , C07D317/58 , C07D333/20
摘要： The present invention provides a biguanide derivative or pharmaceutically allowable salt thereof represented by Formula 1 with N1-N5 substitution, a preparation method thereof and a pharmaceutical composition containing the biguanide derivative as an active ingredient. Compared with conventional drugs, even a small amount of the biguanide derivative of the present invention exhibits excellent effects of AMPKa activation and inhibition of cancer cell proliferation, which makes it useful for the treatment of diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer and the like.
摘要翻译：本发明提供由式1表示的双胍衍生物或其药学允许的盐以及N1-N5取代物，其制备方法和含有该双胍衍生物作为活性成分的药物组合物。与常规药物相比，即使少量本发明的双胍衍生物也表现出优异的AMPKα活化作用和抑制癌细胞增殖的作用，这使其可用于治疗糖尿病，肥胖症，高脂血症，高胆固醇血症，脂肪肝，冠状动脉动脉疾病，骨质疏松症，多囊卵巢综合征，代谢综合征，癌症等。

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