2-substituted-1,3-propylidenediphosphonate derivatives, and...

Details 2-substituted-1,3-propylidenediphosphonate derivatives, and... 2-substituted-1,3-propylidenediphosphonate derivatives, and...

C - Chemistry, Metallurgy

07

F

260/291, 260/267

C07F 9/38 (2006.01) C07F 9/40 (2006.01) C07F 9/547 (2006.01) C07F 9/58 (2006.01) C07F 9/59 (2006.01) C07F 9/6509 (2006.01) C07F 9/653 (2006.01) C07F 9/6533 (2006.01) C07F 9/655 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 1284320

ABSTRACT OF THE DISCLOSURE: The invention relates to a novel class of compounds, 2-substituted 1,3-diphosphonate derivatives of formula (I): Image (I) where R1 and R2, identical or different, are hydrogen, sodium, potassium, magnesium, ammonium, substituted ammonium groups, alkyl groups from 1 to 8 carbon atoms, alkenyl or alkynyl groups from 2 to 8 carbon atoms, or cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexyl-methyl, phenyl, benzyl, CH2CH2OCH3, CH2CH2OCH2CH3, CH2CH2OH, CH2CH2NMe2, and A is selected from the group consisting of: CbH2b+1 , Image , Image Image , Image , Image Image , Image Image , Image Image , Image Image , Image Image , Image Image , Image Image , Image Image , Image Image , Image where b is an integer from 3 to 16, m is zero or 1, n is an integer from zero to 8, k is an integer from zero to 4, t is an integer from 1 to 4, X, Y and Z, identical or different, are an atom or a group H, F, Cl, Br, I, CF3, CHF2, NO2, CN, CH3, C2H5, CH2=CH-CH2, normal-C3H7, iso-C3H7, normal-C4H9, iso-C4H9, tertio-C4H9, OH, CH2OH, -O-CH2-O-, OCH3, OC2H5, OC3H7, OC4H9, SCH3, NH2, NMe2, NEt2, (CH2)t-NMe2, (CH2)t-NEt2 where t is described as above. This novel class of 1,3-diphosphonates of formula (I) are potent calcium entry blockers and vasoactive agents and therefore have a therapeutic potential for the treatment of various disease states such as angina pectoris, arrhythmia and hypertension.

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