New derivatives of fatty acids

 

The invention relates to new derivatives of fatty acids, which drugs or agrochemicals, with improved performance as it relates to lipophilic derivative of biologically active compounds of the General formula CH3-(CH2)7-CH=CH-(CH2)n-X -, where n is an integer of 7 or 9; X is selected from the group comprising-COO-, -CONH-, -CH2O-, -CH2S-, -CH2O-CO-, -CH2NHCO-, -COS-; lipophilic group SN3-(CH2)7-CH=CH-(CH2)n-X - is CIS - or transconfiguration; And is a fragment of a molecule of biologically active compounds (BAC), non-nucleoside and nucleoside derivative and containing in its structure at least one of functional groups selected from a) alcohol, b) simple broadcast) phenol, (d) amino, (e) thiol, (f) carboxylic acids and (g) of ester carboxylic acid, provided that no connection specified in paragraph 1 of the claims. 23 C.p. f-crystals, 13 ill., 3 table.

Description text in facsimile form (see graphic part).

Claims

1. Lipophilic derivative of a biologically active with the mu number 7 or 9;

X is selected from the group comprising-COO-,-CONH-,-CH2O-, -CH2S-, -CH2O-CO-, -CH2NHCO-, -COS-;

lipophilic group SN3-(CH2)7-CH=CH-(CH2)n-X - is CIS - or TRANS-configuration;

And is a fragment of a molecule of biologically active compounds (BAC), non-nucleoside and nucleoside derivative and containing in its structure at least one of functional groups selected from: a) alcohol, b) simple broadcast) phenol, (d) amino, (e) thiol, (f) carboxylic acids and (g) of ester carboxylic acids, provided that excluded:

3-oleate 22, 23-binangonan-5-OIC acid,

2-(3-oleolux-androst-5-enyl)propanol,

2-(3-oleolux-androst-5-ene-17-Il) propylenecarbonate bis(2-chloroethyl)amine,

methyl 3-oleoleole-5-at,

3-oleoleole-5-OIC acid,

4-(3-oleolux-androst-5-ene-17-yl)-pentanol,

4-(3-oleolux-androst-5-ene-17-yl)-pentyloxybenzoyl bis(2-chloroethyl)amine,

(Z)-N-(4,6-dimethoxy-5-pyrimidinyl)-9-octadecenamide,

(Z)-N-(4,6-diethoxy-5-casinol]glycine,

N-[N-[3-(9-octadecanoyloxy)-11-eicosenoic]glycyl]-L-phenylalanine,

N-[N-[3-(9-octadecanoyloxy)-11-eicosenoic]glycyl]-L-serine,

N-((4-(2-aminoethoxy)-3-methoxyphenyl)-methyl)-9Z-octadecenamide,

N-((4-(2-aminoethoxy)-3-hydroxyphenyl)-methyl)-9Z-octadecenamide,

N-((4-(2-aminoethoxy)-phenyl)-methyl)-9Z-octadecenamide,

N-((4-(2-methyl-2-aminopropoxy)-3-methoxyphenyl)-methyl)-9Z-octadecenamide,

N-((4-(2-(S)-amino-3-methylbutoxy)-3-methoxyphenyl)-methyl)-9Z-octadecenamide,

N-((4-(2-carboxy)-2-aminoethoxy)-3-methoxyphenyl)-methyl)-9Z-octadecenamide,

N-((4-(2-amino-3-hydroxypropoxy)-3-methoxyphenyl)-methyl)-9Z-octadecenamide,

N-(9Z-octadecenyl)-4-(2-aminoethoxy)-3-methoxyphenylacetamide,

N-((4-amino-N'-(2-amino-ethyl)-3-methoxyphenyl)-methyl)-9Z-octadecenamide,

N-(9Z-octadecenyl)-4-(amino-N'-(2-amino-ethyl))-3-methoxyphenyl the ndimethylacetamide,

N-(9Z-octadecenyl)-4-(2-aminoethoxy)-3-methoxybenzylamine

2. Lipophilic derivative of p. 1, where these biologically active compounds selected from the group including: 1) adrenocorticosteroid (ACU), 2) non-steroidal anti-inflammatory drugs (NSAIDs), 3) antineoplastic agents (PIC), 4) antimicrobial agents (AMA), 5) antiparasitic funds (PPP) and 6) cardiovascular drugs.

3. Lipophilic production is x at least one functional group, selected from: (a) alcohol, b) simple broadcast) phenol, (d) amino.

4. Lipophilic derivative of p. 3, where adrenocorticosteroid selected from betamethasone, cortisone, dexamethasone, fluoqinolona, fludrocortisone, hydrocortisone, methylprednisolone, prednisolone, triamcinolone, eprazinone, paramethasone, prednisone, beclomethasone and ortsiprenalina.

5. Lipophilic derivative under item 3 or 4, where adrenocorticosteroid selected from prednisolone and betamethasone.

6. Lipophilic derivative of p. 5, representing 1117th, 21-trihydroxypregn-1,4-diene-3, 20-dione-21-elaidate or 9-fluoro-11,17,21 trihydroxy-16-methyl-pregna-1,4-diene-3, 20-dione-21-elaidate.

7. Lipophilic derivative of p. 2, where the biologically active compound selected from group 2) nonsteroidal anti-inflammatory drugs (NSAIDs), containing in its molecule at least one functional group selected from: a) alcohol, b) simple broadcast) phenol, (d) amino, (e) thiol, (f) carboxylic acids and (g) of ester carboxylic acid.

8. Lipophilic derivative of p. 7, where the non-steroidal anti-inflammatory drugs (NSAID) selected from acemetacin, al is she, butibufen, cuprofen, cinmetacin, clidanac, cloretazine, coripata, diclofenac, diflunisal, etodolac, etofenamate, felonica, fenbufen, fenclofenac, vinklarek, fendosal, fenoprofen, fentiazac, flufenamic acid, flurbiprofen, glafenine, ibufenac, ibuprofen, indometacin, softalk, isoxepac, Ketoprofen, Ketorolac, lonazolac, meclofenamic acid, methanomonas acid, medicinova acid, nabumetone, naproxen, niflumova acid, exametazime, oxaprozin, pyrazole, piroxicam, proteinwas acid, salicylic acid, sulindaka, surgana, tenidap, tenoxicam, tiaramide, tinoridine, tolfenamic acid, tolmetin and Comerica.

9. Lipophilic derivative of p. 8, wherein the non-steroidal anti-inflammatory drugs are selected from diclofenac, indometacin, naproxen and piroxicam.

10. Lipophilic derivative of p. 7, selected from the following compounds:

CIS-9'-octadecenoyl ester (2-(2,6-dichlorophenyl) amino)-benzooxazol acid,

(CIS-9'-octadecenyl)amide 1-(p-chlorbenzoyl)-5-methoxy-2-methylindol-3-acetic acid,

(CIS-9'-octadecenyl)amide S(+)-2-(6-methoxy-2-naphthyl) propionic acid,

CIS-9'-octadecenoyl ester of S(+)-2-(6-methoxy-2-dioxide,

4-O-(CIS-11'-eicosanol)-2-methyl-N-(2-pyridyl)-2H-1,2-benzothiazin-3-carboxamide-1,1-dioxide,

(CIS-9'-octadecenoyl)ester 2-hydroxybenzoic acid,

2-(CIS-9'-octadecenoic)ethylbenzoic,

2-(CIS-9'-octadecenoic)benzoic acid,

ethyl ester of S(+)-2-(6-[CIS-9'-octadecenoic]-2-naphthyl) propionic acid,

S(+)-2-(6-[CIS-9'-octadecenoic]-2-naphthyl)propionic acid.

11. Lipophilic derivative of p. 2, where these biologically active compounds selected from the group including antitumor agents (PIC) containing in its molecule at least one functional group selected from: a) alcohol, b) simple broadcast) phenol, (d) amino, (e) thiol, (f) carboxylic acids and (g) of ester carboxylic acid.

12. Lipophilic derivative according to p. 11, where these anti-cancer agents selected from megestrol, medroxyprogesterone, hexestrol, trilostane, aminoglutethimide, epitiostanol, calusterone, 2-acylhydrazides podophylline acid, pirarubicin, doxorubicin, daunorubicin, Taxol, mopidamol, mitoxantrone, lonidamine, etoposide, eflornithine, defoamed, trimetrexate, methotrexate, neopterin, Tg, miamidian, mercaptopurine, dacarbazine, nimustine, PI is proizvodnje on p. 11, where these anti-cancer agents selected from hlorambuzila, melphalan and Taxol.

14. Lipophilic derivative according to p. 11, where these anti-cancer agents selected from the group including:

chlorambucil-alerby ester, mefenamic elaidic acid, Taxol-2'-elaidate, daunorubicine elaidic acid, doxorubicine elaidic acid, daunorubicin-olycarbonate, doxorubicin-olycarbonate.

15. Lipophilic derivative of p. 2, where these biologically active compounds selected from antimicrobic agents containing in its molecule at least one functional group selected from: a) alcohol, b) simple broadcast) phenol, (a) amino, (e) thiol, (f) carboxylic acids and (g) of ester carboxylic acid.

16. Lipophilic derivative according to p. 15, where these antimicrobial agents selected from oxacillin, ampicillin, amoxicillin, cephalexin, tsefalotina, cyclosporine, doxycycline, chloramphenicol, p-aminosalicylic acid, ethambutol, ciprofloxacin, enrofloxacin, difloxacin and danofloxacin.

17. Lipophilic derivative according to p. 16, where these antimicrobial agents are selected from p-aminosalicylic acid, chloramphenicol, oxacillin and amusa complex laidlawii ester of p-aminosalicylic acid, 4-(Luidmila)salicylic acid, chloramphenicolbuy ester elaidic acid, alerby ester oxacillin and ampicillin, ampicilline elaidic acid.

19. Lipophilic derivative of p. 2, where these biologically active compounds selected from anti-parasite substances (PPP) containing in its molecule at least one functional group selected from: a) alcohol, b) simple broadcast) phenol, (d) amino, (e) thiol, (f) carboxylic acids and (g) of ester carboxylic acid.

20. Lipophilic derivative according to p. 19, where these antiparasitic funds (PPP) selected from amodiaquine, hydroxychloroquine, mefloquine, mepacrine, decoquinate, zoalene, the compounds of the formula

and compounds of the formula

21. Lipophilic derivative according to p. 19, which represents 7-chloro-4-[4-[ethyl(2-laideronnette)-amino]]methylbutyl-amino]hinolan.

22. Lipophilic derivative of p. 2, where these biologically active compounds selected from cardiovascular drugs, containing in its molecule at least one functional group selected from: a) alcohol, b) simple broadcast) phenol, (d) amino, (e) thiol, (f) the carb is Dechen-vascular equipment selected from captopril, enalapril, bunitrolol, seloken, labetalola.

24. Lipophilic derivative according to p. 22, representing a 3(-acetonylbenzyl)-4-Baidaratskaya.

 

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