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1. WO2014123364 - N1-CYCLIC AMINE-N5-SUBSTITUTED BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

Publication Number WO/2014/123364
Publication Date 14.08.2014
International Application No. PCT/KR2014/001006
International Filing Date 06.02.2014
IPC
C07C 279/26 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
279Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
20containing any of the groups X being a hetero atom, Y being any atom, e.g. acylguanidines
24Y being a hetero atom
26X and Y being nitrogen atoms, i.e. biguanides
C07C 277/02 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
277Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
02of guanidine from cyanamide, calcium cyanamide or dicyandiamides
A61K 31/155 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines, e.g. amantadine
155Amidines , e.g. guanidine , isourea , isothiourea
CPC
C07D 207/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18having one double bond between ring members or between a ring member and a non-ring member
20with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 211/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
10with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
14with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 211/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
10with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
16with acylated ring nitrogen atom
C07D 211/70
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
68having one double bond between ring members or between a ring member and a non-ring member
70with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Applicants
  • HANALL BIOPHARMA CO., LTD. [KR]/[KR]
Inventors
  • MIN, Chang Hee
  • KIM, Yong Eun
  • OH, Byung Kyu
  • LEE, Ji Sun
  • HEO, Hye Jin
  • OH, Ju Hoon
  • CHO, Woong
Agents
  • DANA PATENT LAW FIRM
Priority Data
10-2013-001417507.02.2013KR
10-2013-001417607.02.2013KR
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) N1-CYCLIC AMINE-N5-SUBSTITUTED BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
(FR) DÉRIVÉS DE BIGUANIDE À SUBSTITUTION N1-AMINE CYCLIQUE-N5, LEURS PROCÉDÉS DE PRÉPARATION ET COMPOSITION PHARMACEUTIQUE LES COMPRENANT
Abstract
(EN) The present invention provides an N1-cyclic amine-N5-substituted biguanide derivative compound represented by Formula 1, a method of preparing the same and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an actice ingredient. The biguanide derivatives have an effect of inhibiting cancer cell proliferation, cancer metastasis and cancer recurrence by activation of AMPK, even when administered in a small dose compared with conventional drugs.
(FR) La présente invention concerne un dérivé de biguanide à substitution N1-amine cyclique-N5 représenté par la formule 1, son procédé de préparation et une composition pharmaceutique comprenant le dérivé de biguanide ou le sel pharmaceutiquement acceptable de celui-ci comme principe actif. Les dérivés de biguanide ont un effet d'inhibition de la prolifération de cellule cancéreuse, de métastase cancéreuse et de rechute du cancer par activation d'AMPK, même lorsqu'il est administré dans une petite dose par comparaison avec des médicaments classiques.
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