Patent IL-119243-A (IL)
Title: Phosphonocarboxylate compounds and pharmaceutical compositions containing them
IPC: C07F9/38
Filed: 1993-05-28
Abstract: A pharmaceutical composition comprising pharaceutically-acceptable carriers and a safe and effective amount of a phosphonocarboxylate, or pharmaceutically-acceptable salts thereof, of the formula wherein (A)(1) A is hydroxy; and (2) B is wherein (a) m is an integer from 0 to 10; n is an integer from 0 to 10; and m+n is an integer from 0 to 10; (b) R8 is independently selected from the group consisting of nil; -R3SR1; hydrogen; substituted or unsubstituted C1-C8 alkyl; -R3 OR4; -R3CO2R4; -R3O2CR4; -R3N(R4)2; -R3[N(R5)3]+; -R3N(R4)C(O)R4; -R3N(R4)C(S)R4; -R3N(R4)C(N)R4; -R3C(O)N(R4)2; halogen; -R3C(O)R4; nitro; hydroxy; substituted or unsubstituted saturated monocyclic or polycyclic carbocyclic rings; substituted or unsubstituted unsaturated monocyclic or polycyclic carbocyclic rings; substituted or unsubstituted saturated monocyclic or polycyclic heterocyclic rings; and substituted or unsubstituted unsaturated monocyclic or polycyclic 3127 ה' בכסלו התשס" ג - November 10, 2002 heterocyclic rings; (c) R1 is independently selected from the group consisting of hydrogen; -C(O)R7; -C(S)R7; -C(O)N(R7)2; -C(O) OR7; -C(S)N(R7)2; and -C(S)OR7; where R7 is hydrogen or substituted or unsubstituted C1-C8 alkyl; (d) R3 is selected from the group consisting of nil and substituted or unsubstituted C1-C8 alkyl; (e) R4 is independently selected from the group consisting of hydrogen; substituted or unsubstituted C1-C8 alkyl; and -R2SR1; (f) R5 is independently selected from the group consisting of substituted or unsubstituted C1-C15 alkyl; substituted or unsubstituted phenyl; benzyl; and R2-SR1; (f1) R2 is a substituted or unsubstituted C1-C8 alkylene; (g) L is selected from the group consisting of nil; -N(R8)-; [N(R5)2-]+; -S-; -O-; and -D-C(=E)-S-, where D is selected from the group consisting of covalent bond, O, or S, and E is O or S; and wherein (i) when L is -N(R8)-, or when L is [-N(R5)2-]+ and m is an integer from 1 to 10, R9 is independently selected from the group consisting of nil; hydrogen; substituted or unsubstituted C1-C35 alkyl; R2SR1; and R10; (ii) when L is [-N(R5)2-]+ and m = 0, R9 is selected from the group consisting of substituted or unsubstituted C1-C35 alkyl; R2SR1; and R10; or (iii) when L is nil, -S-, -O-, or -D-C(=E)-S, R9 is R10; (h) R10 is a saturated, unsaturated, or aromatic monocyclic or polycyclic carbocycle, or a saturated, unsaturated, or aromatic monocyclic or polycyclic heterocycle containing one or more heteroatoms; where said carbocycle or heterocycle is substituted with one or more R11 substitutents; and (i) each R11 is independently selected from the group consisting of -R3SR1; hydrogen; substituted or unsubstituted C1-C8 alkyl; -R3OR4; -R3CO2R4; -R3O2CR4; -R3N(R4)2; -R3[-N(R5)3]+; -R3N(R4)C(O)R4; -R3N(R4)C(S)R4; -R3N(R4)C(N)R4; -R3C(O)N(R4)2; halogen; -R3C(O)R4; hydroxy; substituted or unsubstituted arylalkyl; nitro; and unsubstituted or substituted aryl; or (B) A and B are covalently linked together with C* to form a monocyclic or bicyclic ring having the following structure: wherein (a) A and B are independently selected from the group consisting of nil, -O-, -S-, and -NR12; (b) Q is selected from the group consisting of nil; -NR12; and [-N(R13)2]+; (c) X and X' are independently selected from C or N; (d) R12 is independently selected from the group consisting of nil; -R3SR1; hydrogen; substituted or unsubstituted C1-C8 alkyl; -R3OR4; -R3CO2R4; -R3O2CR4; -R3N(R4)2; R3[-N(R5)3]+; 3128 ה' בכסלו התשס" ג - November 10, 2002 -R3N(R4)C(O)R4; -R3C(O)N(R4)2; halogen; -R3C(O)R4; hydroxy; substituted or unsubstituted arylalkyl; nitro; and unsubstituted or substituted aryl; (e) R13 is selected from the group consisting of nil; substituted or unsubstituted C1-C35 alkyl; substituted or unsubstituted phenyl; benzyl; and -R2 SR1; (f) when Q is other than nil, k and j and k+j are integers from 0 to 5; when Q is nil, k and j and k+j are integers from 0 to 6; a