N1-CYCLIC AMINE-N5-SUBSTITUTED PHENYL BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

Title:

N1-CYCLIC AMINE-N5-SUBSTITUTED PHENYL BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

Document Type and Number:

WIPO Patent Application WO/2013/022278

Kind Code:

A3

Abstract:

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.

Inventors:

KIM SUNG WUK (KR)
MIN CHANG HEE (KR)
PARK SE HWAN (KR)
KIM DUCK (KR)
LEE JI SUN (KR)
KIM YONG EUN (KR)
OH JU HOON (KR)

Application Number:

PCT/KR2012/006326

Publication Date:

April 25, 2013

Filing Date:

August 08, 2012

Export Citation:

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Assignee:

HANALL BIOPHARMA CO LTD (KR)
KIM SUNG WUK (KR)
MIN CHANG HEE (KR)
PARK SE HWAN (KR)
KIM DUCK (KR)
LEE JI SUN (KR)
KIM YONG EUN (KR)
OH JU HOON (KR)

International Classes:

C07C279/26; A61K31/155; A61P35/00; C07C277/02

Domestic Patent References:

WO2009113092A2

2009-09-17

Foreign References:

US3960949A	1976-06-01
KR20030029050A	2003-04-11

Other References:

MAHVASH ZAKIKHANI ET AL.: "Metformin Is an AMP Kinase-Dependent Growth Inhib itor for Breast Cancer Cells", CANCER RES., vol. 66, no. 21, 2006, pages 10269 - 10273, XP002497600

Attorney, Agent or Firm:

DANA PATENT LAW FIRM (BYC Bldg. 648-1, Yeoksam-dong, Gangnamgu, Seoul 135-080, KR)

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