RU99112517A - ANTI-THROMBOSIS ORGANIC NITRATES - Google Patents

Claims (11)

1. The compound of the general formula:
A- (X ₁ -NO ₂ ) t _o
or their salts,
where t _o is an integer equal to 1 or 2;
A = RN _o , where N _o = (COX _u ) _t - or COON ₁ , where t is an integer equal to zero or 1; u is an integer equal to 0 or 1;
X = O, NH, NR _1c , where R _1c is a straight or branched chain alkyl having from 1 to 10 carbon atoms; N ₁ is a straight or branched chain alkyl having from 1 to 10 carbon atoms or hydrogen;
R is selected from the following groups:
* Group A)
Ia)

where R _Ia and R _IIa are the same or different and are H or linear or, when possible, branched alkyl of 1-3 C atoms, preferably, R _Ia = R _IIa = H; n _Ia is an integer of 1-6, preferably 2-4;
R _Ia can be

where N ₂ has the same meaning as N _o ; moreover, at least one of the groups N _o or N ₂ has one free valency capable of binding to X ₁ (i.e., t = 1),
Ib)

R _Ia , R _IIa , n _Ia are as defined for Ia; N ₃ is H, (CH ₃ ) ₂ CH-CH-OOSCH ₂ CH ₃ , or the free valence with which X ₁ is bound (i.e., N _{3 is} absent); R _Ib selected from

N ₂ is as defined above, wherein at least one of the groups N ₃ or N ₂ has a free valency capable of binding to X ₁ (when it is N ₂ , t = 1);
Ic) where t = 1

where N _o has the meanings indicated above, where t = 1, i.e. it has a free valency capable of binding to X ₁ ;
R _Ic is selected from H, —COCH ₃ or

Id)

where N ₂ is as defined above and at least one of the groups N ₂ has a free valence (t = 1) capable of binding to X ₁ ;
when in group Ic) R _Ic is H or COCH ₃ , X cannot be -NH. * Group B
where t = 1 and u = 0
IIa)

where R _Ia , R _IIa have the meanings specified for Ia);
R _IIb is R _ia ;
R _{sa is} selected from:

Iib)

where in group B) N ₂ has the meanings indicated above, and at least one of the N ₂ groups has a free valency capable of binding to X ₁ (that is, at least one substituent N ₂ has t = 1);
X ₁ is a bivalent bridge chosen from:
-YO, where Y is C ₁ -C ₂₀ straight or optionally branched chain alkylene, preferably having 2 to 5 carbon atoms, or optionally substituted cycloalkylene, having 5 to 7 carbon atoms;
-Y ₁ selected from

where n ₃ is an integer of 0 - 3;

where nf 'is an integer of 1-6, preferably 2-4;

where R _1f = H, CH ₃ , and nf is an integer from 1 to 6, preferably from 2 to 4. 2. Compounds according to claim 1, in which R, R _I , R _Ib , R _Ic , R _BA and compounds Id) and IIb) are residues of alapecil, benazepril, captopril, caronapril, cilazapril, deprile, enalapril, enalaprilat, fosinapril, imidapril, lisinopril, quinapril, ramipril, spirapril, temocapril, tradolapryl, movtilipril, perindopril, befunolol, betaxolol, bupranolol, carteolol, levobunolol, methipranolol, timolol, oxprenolol, mepindololol, oxprenolol, mepindololol, lepunolol, mepiphenolol, timololol, oxprenolol, mepindololol, oxprenolol, mepindolol, lepunolol, mepiphenolol, timololol 3. Compounds according to claims 1 and 2, in which X ₁ selected from
-YO, where Y is a C ₁ -C ₂₀ alkylene with a straight or, where possible, branched chain, preferably having 2 to 5 carbon atoms, or an optionally substituted cycloalkylene having 5 to 7 carbon atoms;
-Y ₁ selected from

where n ₃ is an integer from 0 to 3.  4. Connection on PP. 1-3 for use as a medicine.  5. The compound according to claims 1 to 3 for obtaining a medicinal product for use as an anti-thrombotic agent.  6. The compound according to claims 1 to 3 for obtaining a medicinal product for use as an antihypertensive agent.  7. Connection on PP. 1-3 for obtaining a medicinal product for use as a cardioprotector.  8. Pharmaceutical composition having inhibitory platelet aggregation activity, containing a compound according to any one of claims 1 to 3 and a pharmaceutically acceptable carrier or diluent.  9. The composition of claim 8, which is an anti-thrombotic composition.  10. The composition of claim 8, which is an antihypertensive composition.  11. The composition of claim 8, which is a cardioprotective composition.