Derivatives of 1,3-propane diol and their use as biologically active substances

 

The invention relates to new compounds with the structure associated 1,3-propane diol, having the ability to penetrate lipid barriers, formula 1, where R1denotes an acyl group or a group of fatty alcohol, derived from C12-30preferably C16-30the fatty acids preferably with two or more double bonds in the CIS - or TRANS-position, and R2denotes hydrogen, acyl group or the group of fatty alcohol, which is the same or different from that specified for R1or is a biologically active residue that is different from the rest of Niacin, the chemical structure of which allows you to connect with 1,3-propane diol through the available carboxyl, alcohol or amino group. Connection with the structure associated 1,3-propane diol, having the ability to penetrate lipid barriers, formula 1, where R1denotes an acyl group or a group of fatty alcohol, derived from C12-30preferably16-30the fatty acids preferably with two or more double bonds in the CIS - or TRANS-position, and R2denotes hydrogen, acyl group or the group of fatty alcohol, which is the same or different from that specified for R1or alabastine with 1,3-propane diol through the available carboxyl, alcohol or amino group, in which between the group R1and/or R2and the rest of 1,3-propane diol included phosphate, succinate or other bifunctional acid group, in particular, when R2is a biologically active rest with a hydroxyl or amino functional groups. Drug therapy for transfer of a drug or other active substance through the lipid membranes in the body, or having the effect, of additional or complementary, or synergistic with R1containing as active agent a compound of formula 1. The technical result - new compounds with the ability to penetrate lipid barriers. 7 C. and 8 C.p. f-crystals.

Description text in facsimile form (see graphic part).

Claims

1. Connection with the structure associated 1,3-propane diol, having the ability to penetrate lipid barriers:where R1denotes an acyl group or a group of fatty alcohol, derived from C12-C30preferably16-C30fatty acids regroup or group of fatty alcohol, which is the same or different from that specified for R1or is a biologically active residue that is different from the rest of Niacin, the chemical structure of which allows you to connect with 1,3-propane diol through the available carboxyl, alcohol or amino group.

2. Connection with the structure associated 1,3-propane diol, having the ability to penetrate lipid barriers:where R1denotes an acyl group or a group of fatty alcohol, derived from C12-C30preferably16-C30fatty acids, preferably with two or more double bonds in the CIS - or TRANS-position; R2denotes hydrogen, acyl group or the group of fatty alcohol, which is the same or different from that specified for R1or is a biologically active residue that is different from the rest of Niacin, the chemical structure of which allows you to connect with 1,3-propane diol through the available carboxyl, alcohol or amino group, in which between the group R1and/or R2and the rest of 1,3-propane diol included phosphate, succinate or other bifunctional acid group, in particular, when R2is a biologically active OS the lot is an essential fatty acid of the number of n-6 or n-3, or oleic acid, or columbinus acid, or prinarovie acid, or conjugated linoleic acid.

4. Connection on p. 3, in which the fatty acid is gamma-linolenic acid, di-Homo-gamma-linolenic acid, arachidonic acid, atenolol acid, stearidonic acid, eicosapentaenoic acid, docosapentaenoic acid n-3, docosahexaenoic acid or conjugated linoleic acid.

5. Connection PP. 1-3 or 4, in which R2a drug or other active substance, for which you want to penetrate the lipid membranes in the body to provide the necessary action within the cell or move to the cell in which it must act, or to pass through the skin, the blood-brain or other barriers.

6. Connection PP. 1-3 or 4, in which regardless of the need to penetrate through the lipid membrane R2a drug, vitamin, amino acid, antioxidant or another active substance which is required to provide additive, complementary, or synergistic action with R1.

7. Drug therapy for transferring the medicament is optional, or complementary, or synergistic with R1, wherein the active agent comprises a compound according to any one of the preceding paragraphs. 1-4.

8. Compounds according to any one of paragraphs. 1-4 as such, except for compounds in which R1and R2represent the remains of saturated fatty acids, and compounds in which R1and R2have the same values and are derived from oleic acid, linoleic acid or alpha-linolenic acid.

9. Compounds according to any one of paragraphs. 1-6 to obtain preparations for skin care or hair care or treatment of skin diseases.

10. Compounds according to any one of paragraphs. 1-6 to obtain food, food additives or feed additives.

11. Derivatives of 1,3-propane diol containing two fatty acids, one of which fatty acid is gamma-linolenic acid or di-Homo-gamma-linolenic acid, and other gamma-linolenic acid, di-Homo-gamma-linolenic acid, stearidonic acid, eicosapentaenoic acid, docosahexaenoic acid, conjugated linoleic acid or columbinus acid intended for use in therapy.

12. Derivatives of 1,3-propane diol containing two fatty ka-linolenic acid, docosahexaenoic acid, di-Homo-gamma-linolenic acid or eicosapentaenoic acid, intended for use in therapy.

13. Derivatives of 1,3-propane diol containing two fatty acids, one of which fatty acid is eicosapentaenoic acid, and the other of eicosapentaenoic acid or docosahexaenoic acid, intended for use in therapy.

14. Derivatives of 1,3-propane diol, containing in one position fatty acid selected from gamma-linolenic acid, di-Homo-gamma-linolenic acid, arachidonic acid, stearidonic acid, conjugated linoleic acid, eicosapentaenoic acid or docosahexaenoic acid, and in another position of the tool selected from the following chemical structure which allows it to communicate with 1,3-propane diol through the available carboxyl, alcohol or amino group: (a) tryptophan; (b) phenylalanine; (c)arginine; (d) carnitine or a derivative of carnitine; (e) any other amino acid or its derivatives or aminolevulinate acid or its derivatives; (f) adenylosuccinate or its derivatives; (g) aspirin, salicylic acid, indomethacin, ibuprofen, or any non-steroidal anti-inflammatory securitiesin; (i) any anti-malarial or Antiprotozoal agent, in particular chloroquine, mepacrine, chinacan and mefloquine; (j) any antifungal drug, in particular metronidazole and antifungal imidazoles, nitroimidazoles and amphotericin; (k) any anti-inflammatory steroid, in particular hydrocortisone and betamethasone, beclomethasone and budesonide; (l) any gonadally steroid, in particular oestrogen, POCs and androgens; (m) any adrenal steroid, particularly dehydroepiandrosterone; (n) any retinoid, in particular, tretinoin and isotretinoin; (o) any anti-cancer agent; (p) any antipsychotic agent; (q) any antidepressant; (r) any tranquilizer; (s) any immunosuppressive agent, in particular cyclosporine and tacrolimus; (t) any proton pump inhibitor or H2 antagonist; (u) any diuretic; (v) any calcium antagonist; (w) any angiotensin-converting enzyme inhibitor or antagonist of angiotensin; (x) any beta-blocker; (y) any antiepileptic drug, particularly phenytoin, carbamazepine, valproate, ethosuximide, vigabatrin or lamotrigine; (z) any gipolipidemicheskie tool, in particular the fibrates and statins; (AA) any p is the based tool, used in radiology, including connection of diatrizoate, iodipamide, ioglycamide, iopanoic, opendylan, iothalamate, ioxaglate, metrizamide and their derivatives; (dd) any peptide or protein, including insulin, calcitonin or erythropoetin; (EE) any vitamin; (ff) any antioxidant; (gg) any porphyrin, chlorin or drug-based bacteriochlorin, in particular tetrakis(hydroxyproline) derivatives.

15. Derivatives of 1,3-propane diol under item 14, containing in one position fatty acid selected from gamma-linolenic acid, di-Homo-gamma-linolenic acid, arachidonic acid, stearidonic acid, conjugated linoleic acid, eicosapentaenoic acid or docosahexaenoic acid, and in another position - vitamin or antioxidant, chemical structure which allows it to communicate with 1,3-propane diol through the available carboxyl, alcohol or amino group, for use in food additives, food or nutrients.

Priority points and features: 01.05.1995 on PP. 1 and 2, where R1and R2groups derived from fatty acids with two or more CIS or TRANS double bonds, biologically active balance associated with 1,3-propandiol is Noah linoleic acid;
p. 14, where derivatives of 1,3-propane diol, containing in one position fatty acid selected from gamma-linolenic acid, di-Homo-gamma-linolenic acid, arachidonic acid, stearidonic acid, conjugated linoleic acid, eicosapentaenoic acid or docosahexaenoic acid, and in another position the drug (a), (C), amino acids (e), (g), (h), metronidazole (j), (k), (o), (p), (q) and b vitamins (In) (its);
p. 15, where derivatives of 1,3-propane diol, containing in one position fatty acid selected from gamma-linolenic acid, di-Homo-gamma-linolenic acid, arachidonic acid, stearidonic acid, conjugated linoleic acid, eicosapentaenoic acid or docosahexaenoic acid, and in another position of the b vitamin;
21.08.1995 under item 3, except conjugate linoleic acid;
p. 9 - for skin care;
PP. 10, 12 and 13;
15.03.1996 on PP. 1 and 2, except for the sign "is different from the rest of the Niacin";
p. 8, except signs, excluding the number of compounds;
p. 14, where derivatives of 1,3-propane diol, containing in one position fatty acid selected from gamma-linolenic acid, di-Homo-gamma-linolenic acid, arachidonic acid, stearidonic acids is drop - drug (b), derivatives of carnitine (d), chloroquine, mepacrine (i), (v), (cc), peptides (dd), (EE), (ff);
p. 15, except conjugate linoleic acid.

 

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< / BR>
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< / BR>
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