Spermine derivatives as heparin antidotes
AssigneesConsejo Superior De Investigaciones Cientificas (Csic), Institut Quimic De Sarria Cets, Fundacio Privada
InventorsIgnacio ALFONSO RODRIGUEZ, Daniel CARBAJO LÓPEZ, Yolanda PÉREZ RUIZ, Jordi BUJONS VILÁS, Eva PRATS MIRAVITLLAS, Marta GUERRA REBOLLO
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Abstract
The invention relates to new spermine derivatives of Formula (I), wherein the meaning of the groups R1, R2, n and m is defined in the description, to a pharmaceutical composition thereof and to their use as heparin antidotes in the control of blood coagulation. The invention was developed based on the realization that it would be desirable to have improved heparin antidotes with good anticoagulant rates, based on simple, easy to produce synthetic small molecules.
Claims11
A compound of Formula I:
- wherein:
- n is an integer between 0 and 3;
- each m is independently an integer between 0 and 3;
- R1 is phenyl, naphthyl or fluorenyl, wherein R1 is optionally substituted by one to three groups R3;
- R2 is naphthyl or fluorenyl, wherein R2 is optionally substituted by one to three groups R3;
- each R3 is independently —OH, —OR4, halogen, —C1-4 alkyl, —CHO or —OPO(OH)2;
- and
- R4 is C1-4 alkyl,
- with the proviso that:
- if R1 is 2-methoxyphenyl, 2-hydroxyphenyl or 2-methoxy-1-naphthalen-1-yl, n=2 and m=1, then R2 is not 1-naphthyl or 2-methoxy-1-naphthalen-1-yl;
- and
- the compound of Formula I is not
- N1,N1′-(butane-1,4-diyl)bis(N3-(naphthalen-1-ylmethyl)propane-1,3-diamine, or
- N1,N1′-(butane-1,4-diyl)bis(N3-(naphthalen-2-ylmethyl)propane-1,3-diamine.
(canceled)
Dependencies are inferred from the claim text.