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TRIPHENYLPHOSPHONIUM BIGUANIDE ANALOGUES, THEIR METHOD OF PREPARATION AND USE AS DRUGS
专利权人:
KKCG SE
发明人:
NEUZIL, Jiri,WERNER, Lukas,STURSA, Jan
申请号:
CZCZ2015/050016
公开号:
WO2016/155679A1
申请日:
2015.12.23
申请国别(地区):
WO
年份:
2016
代理人:
摘要:
The present invention provides triphenylphosphonium biguanide analogs of general formula (I), whereas the general formula (I) includes resonance structures and pharmaceutically acceptable salts, protonated form as well as free base, (Formula (I)) where each one of R1, R2, R3, R4, R5, R6, R7 is independently selected from the group comprising H C1-C6 alkyl C6-C10 aryl (C1-C6)alkyl(C6-C10)aryl -C(=O)-R -C(=O)OR -C(=O)NRR" -C(=S)R -C(=S)NRR wherein R and R" are independently selected from the group comprising H, C1-C6 alkoxy, C1-C6 alkyl, C6-C10aryl, (Cl-C6)alkyl(C6-C10)aryl whereas C1-C6 alkoxy, C1-C6 alkyl, C6-C10 aryl, (C1-C6)alkyl(C6-C10)aryl can be unsubstituted or substituted by one or more substituents selected independently from the group comprising C1-C4 alkyl, N(H or C1-C4 alkyl)2, wherein alkyls are the same or different, phenyl, benzyl, OH, SH, F, CI, Br, I, C1-C4alkoxy, C1-C4 acyloxy, C1-C4 mercapto and substituent of general formula (II) (Formula (I)) wherein Z is as defined in the claims, whereas at least one of R1, R2, R3, R4, R5, R6, R7 is the substituent of general formula (II), X- is a pharmaceutically acceptable anion, preferably an anion of inorganic or organic acid, Y- is a pharmaceutically acceptable anion, preferably an anion of inorganic or organic acid. The invention further provides a method of preparation of these derivatives. These new compounds are suitable in particular for the treatment of diabetes mellitus type 2 and/or pancreatic carcinoma.La présente invention concerne des analogues de biguanide de triphénylphosphonium de formule générale (I), la formule générale (I) comprenant des structures de résonance et des sels pharmaceutiquement acceptables, sous forme protonée en tant que base libre, (formule (I)) où chacun de R1, R2, R3, R4, R5, R6, R7 est indépendamment choisi dans le groupe comprenant H alkyle en C1-C6 aryle en C6-C10, (alkyle en C1-C6) (aryle en C6-C10) -C (= O)-R -C (= O) OR -C (= O) NRR " , -C (= S) R -C (=S) NRR
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