CN105669798A

CN105669798A - Macrolide compound

Info

Publication number: CN105669798A
Application number: CN201511027811.1A
Authority: CN
Inventors: 刘兴金; 张许科
Original assignee: Pulaike Biological Engineering Co Ltd
Current assignee: Pulaike Biological Engineering Co Ltd
Priority date: 2013-08-23
Filing date: 2013-08-23
Publication date: 2016-06-15
Anticipated expiration: 2033-08-23
Also published as: CN105669798B

Abstract

The invention relates to a macrolide compound represented by formula I, and a pharmaceutically acceptable salt thereof. The compound is an antiseptic, and can be used to treat various bacteria and protozoa infection. The invention also relates to a preparation method and a medicinal composition of the compound.

Description

A kind of macrolides compound

The application is the divisional application of the Chinese invention patent application of the same name that application number is 201310373556.0 that on August 23rd, 2013 submits to.

Technical field

The invention belongs to pharmaceutical technology field, relate to new 4 "-9-deoxidation-8A-azepine-(8A-alkyl)-8A-a-homoerythromycin A derivatives of-replacement; and optically active body, pharmaceutically acceptable salt, comprise their preparation method and the pharmaceutical composition of described compound. The invention still further relates to this derivant for preparing treatment and/or pre-bacteriological protection infection, protozoal infections class disease.

Background technology

Macrolide is as the important anti-infection drug of a class, because its antibacterial activity is good, without anaphylaxis, side effect is little, safety is high, through the development of 50 years, it has also become clinical practice is only second to the second largest class anti-infectives of beta-lactam antibiotic, has consequence on clinical treatment. Erythromycin is as first generation macrocyclic lactone antibiotic, once the infection that treatment staphylococcus aureus, streptococcus pneumoniae, Streptococcus hemolyticus and mycoplasma pneumoniae etc. cause it was widely used in, the person that is particularly suited for penicillin anaphylaxis, then owing to acid medium unstability causing its application be restricted. The second filial generation macrocyclic lactone antibiotic that azithromycin is representative solves this problem in that, and has had in drug effect and pharmacokinetics and significantly improve. Azithromycin (9-deoxidation-9A-methyl-9A-azepine-a-homoerythromycin A) is first 15 ring macrocyclic lactone antibiotic that Bright (US Patent No. 4474768) and Kobrehe (US Patent No. 4517367) etc. find. It is that erythromycin introduces a nitrogen-atoms on oximate, Beckmann rearrangement and lactonic ring, is then passed through reduction, methylates and obtain a special macrocyclic lactone antibiotic of class. Its outstanding feature is: acid medium is stable, and tissue infiltration model, plasma half-life length, clinical indication are wide, evident in efficacy and untoward reaction is few. Particularly azithromycin has antimicrobial spectrum widely, has suppression gram negative bacilli such as hemophilus influenza etc. and has good antibacterial activity, compensate for macrocyclic lactone antibiotic deficiency in anti-gram-negative bacteria.

Tulathromycin (Tulathromycin) it be with dihydro homoerythromycin for initiation material, first to 2 ' positions protect, then to its 4 " position aoxidizes, cyclization, through reduction elimination 2 ' position protection, be then passed through amination and become salt to obtain Tulathromycin. It is a kind of fresh market and the Macrolide semisynthetic antibiotics for animal specific. The Ministry of Agriculture of China allowed Tulathromycin to use in animal productiong in 2008 in No. 957 bulletin first. Tulathromycin is mainly used in the respiratory system disease of Actinobacillus, mycoplasma, pasteurellosis bacillus, pig that secondary haemophilus causes, cattle.Have that consumption is few, the many merits such as single administration, low-residual and animal specific.

But, along with widely using antibiotic, particularly lasting, improper use, all creates drug resistance to now widely used macrolide antibiotic such as azithromycin, Tulathromycin etc., brings extreme difficulties to clinical treatment. And acute toxicity test proves that Tulathromycin oral toxicity is bigger.

Summary of the invention

In consideration of it, present invention is primarily targeted at the macrolides compound and pharmaceutically acceptable salt thereof that provide a kind of following general structure I,

Wherein, R ＇ is H or C₁～C₆Alkyl;

R₁Selected from H, hydroxyl, methoxyl group, propargyl, aryl and azacyclo-;

R₂For hydroxyl;

R₃For-CH₂R, wherein R be H containing or without heteroatomic organic group, described hetero atom is selected from O, N, S and halogen;

R₄Selected from H, acetyl group and benzyloxycarbonyl group.

In compound of the present invention, it is preferable that R₃For-CH₂NR₂₀R₃₀Or-CH₂SR₄₀, wherein R₂₀、R₃₀And R₄₀All independently be H or contain or without heteroatomic organic group, described hetero atom is selected from O, N, S and halogen and R₂₀And R₃₀Between selectively key be linked to be ring.

In compound of the present invention, it is preferable that R₃For-CH₂NHR₅₀, and R₅₀For being selected from containing or without heteroatomic organic group, described hetero atom is selected from O, N, S and halogen. It is further preferred that R₅₀For selected from n-pro-pyl, normal-butyl, cyclopropyl, ethyl, isopropyl, isobutyl group, the tert-butyl group, Cvclopropvlmethvl, 2-methoxy ethyl, cyclopenta, 2,4-difluorobenzyl, 3-methoxy-benzyl, n-pentyl, 2-Methyl-pyrazin-5-base-methyl, 3-methoxy-propyl, cyclohexyl methyl, 4-methoxyphenethyl.

Preferred R in the present invention₃For-CH₂NR₂₀R₃₀, and R₂₀And R₃₀It is each independently C₁～C₆Alkyl. More preferably R₂₀And R₃₀It is each independently methyl or ethyl.

In a specific embodiment of the present invention, described R₃Middle R is nitrogen-containing heterocycle compound, and wherein nitrogen element and R₃The carbon of methylene is joined directly together. Preferred R₃Middle R is morpholine, piperidines or piperazine.

In the preferred present invention, R₂₀And R₃₀Collectively form 4～10 yuan of monocycles or R₂₀And R₃₀Collectively form by 1 or 2 optionally substituted 5～10 yuan of hetero-aromatic ring of alkyl.

In the present invention, it is preferred to R₂₀And R₃₀In one be H, another is the organic group containing phenyl or benzyl.

It is further preferred that heretofore described compound is the one in following compound:

1), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylcarbamic) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

2), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(butylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

3), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(diethylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

4), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(phenyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

5), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(morpholine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

6), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclopropylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

7), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(pyrrole radicals) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

8), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-fluorobenzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

9), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(imidazoles) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

10), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(ethylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

11), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(isopropylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

12), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(isobutylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

13), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[tert-butylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

14), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[piperidine methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

15), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(Cyclopropyl-methyl-amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

16), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-methoxYbenzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

17), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-chlorobenzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

18), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-picolyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

19), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[((3-ethoxycarbonyl propyl) amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

20), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-methoxy ethyl) amino-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

21), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[2-methoxybenzyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

22), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(2-[(N-methyl) amino]-ethyl) amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

23), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(clopentylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

24), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[2,4-difluorobenzyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

25), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(6-chloro-pyridazine-3-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

26), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-3-phenyl) propyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

27), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[3-methoxybenzyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

28), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[2,2,2-trifluoroacetyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

29), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[[(the chloro-pyridin-4-yl-amino of 2-)-methyl]-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

30), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[[(4-formyl-benzyl-amino)-methyl]-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

31), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[propargyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

32), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[butanoic acid base-2-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

33), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[butanoic acid base-4-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

34), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-hydroxy-propyNamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

35), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[n-pentyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

36), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(morpholine-4-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

37), 3-({ (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-6-[-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl--1-oxa--7-azacyclo-pentadecane-15-ketone-13-base-oxygen]-3-hydroxyl-4-methoxyl group-2,4-dimethyl-tetrahydro pyrans-3-base-methyl }-amino)-butanoic acid;

38), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methylol-propylcarbamic)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

39), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-hydroxyl-2-phenyi-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

40), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-dimethoxy-butylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

41), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,4-dichloro-benzylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

42), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methyl-4-dimethrlaminobutyl amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

43), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(3-Cyclohexylamino) the third amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

44), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(4-methanesulfonylphenYl ethylamino) the third amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

45), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-but-1-ene-3-alkynes-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

46), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-butvl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

47), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(2-pyridin-4-yl-ethyl ammonia)-methyl]]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

48), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C--{ [(5-Methyl-pyrazin-2-base-methyl)-ammonia]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

49), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(3-methoxy-propvl-ammonia)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

50), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(Cyclohexyl-methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

51), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-fluoro-phenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

52), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-morpholine-propyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

53), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(furfuryl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

54), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-aminobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

55), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(phenylhydrazino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

56), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-{ [2-(1H-indol-3-yl)-ethylamino]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

57), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-chloropropyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

58), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,5-Dimethoxyphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

59), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(thiophenecarboxylate base-2-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

60), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-methyl furfuryl amine base)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

61), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the fluoro-phenylhydrazine of 4-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

62), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(benzyloxy-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

63), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(p-methoxyphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

64), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,4-3,5-dimethylphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

65), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-fluorine pyridine-2 amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

66), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-pyrroles-ethyl base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

67), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-pyridin-4-yl-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

68), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-luorobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

69), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-piperidin-4-yl-Methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

70), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-o-tolyl-amino of 5-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

71), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-fluoro-phenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

72), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the fluoro-5-aminomethyl phenyl-amino of 2-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

73), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-phenyl-amino of 2-methyl-4-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

74), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-methyl-butvl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

75), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(quinoline-6-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

76), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1,2,2-trimethyl-propyl amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

77), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(n-pro-pyl-amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

78), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(normal-butyl-amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

79), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(pentyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

80), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(diethylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

81), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(phenyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

82), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(morpholine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

83), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-{ [(5-amino-1,3,3-trimethyl cyclohex ylmethyl)-amino]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

84), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[piperonyl amino-methyl)]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-, (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

85), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-fluorobenzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

86), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1,2,3-triazole) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

87), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(ethylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-, 1-oxa--7-azacyclo-pentadecane-15-ketone;

88), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(isopropylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

89), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(isobutylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

90), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-chlorphenylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

91), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(tert-butylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

92), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(n-hexyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

93), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-trifluoromethyl benzyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

94), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(Cyclopropyl-methyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

95), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-Methoxy-benzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

96), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(4-Nitro-benzyl) amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

97), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[the chloro-benzyl-amino of 4-]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

98), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-pyridyl-methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

99), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(3-ethyoxyl-propyl group)-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

100), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-methoxy ethyl)-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

101), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-methyl-2-hydroxy-ethyl) amino-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

102), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-methyoxy-benzyl)-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

103), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclopenta-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

104), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,4-difluorobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

105), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(6-chloro-pyridazine-3-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

106), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-hydroxy-butyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

107), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methyl-3-phenyl-propylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

108), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-Methoxy-benzylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

109), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[piperazinyl-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

110), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[trifluoroacetamido]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

111), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[[(the chloro-pyridin-4-yl-amino of 2-)-methyl]-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

112), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[4-formyl benzylamino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

113), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[propargyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

114), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[1-butanoic acid base 2-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

115), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[1-butanoic acid base 4-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

116), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[diethylene glycol base-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

117), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-hydroxyl-1-ethoxy-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

118), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-hydroxy-propyNamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

119), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[n-pentyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

120), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(morpholine-4-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

121), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-amino-butyric acid base)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

122), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methylol-propylcarbamic)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

123), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-hydroxyl-2-phenyi-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

124), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,4-difluorophenyl methylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

125), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,5-difluorophenyl methylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

126), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-methoxyethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

127), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methyl-4-diethylamino butylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

128), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[4-sulfoamido-phenylethylamino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

129), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-but-1-ene-3-alkynes-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

130), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-butvl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

131), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(2-pyridin-4-yl-ethylamino)-methyl]]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

132), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-{ [(5-Methyl-pyrazin-2-base-methyl)-amino]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

133), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(Cyclohexyl-methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

134), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-fluoro-phenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

135), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-morpholine-propyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

136), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-phenyl methyl-amino of 2-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

137), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-furan-Methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

138), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-aminobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

139), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(phenylhydrazino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

140), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-{ [2-(1H-indol-3-yl)-ethylamino]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

141), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-chlorine-propyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

142), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,5-Dimethoxyphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

143), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-methyl-ribofuranosyl-2-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

144), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the fluoro-phenylhydrazino of 4-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

145), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(benzyloxy-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

146), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(p-methoxyphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

147), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,4-3,5-dimethylphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

148), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(to fluoro thiophenol)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

149), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-fluorine pyridine-2-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

150), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(diethyl-4-methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

151), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-morpholine-propyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

152), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-pyrroles-ethyl base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

153), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-pyridin-4-yl-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

154), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-luorobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

155), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-piperidin-4-yl-Methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

156), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-phenyl-amino of 2-methyl-4-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

157), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-methyl-butvl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

158), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4,6-Dichloro-pyrimidin-2-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

159), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclo-heptylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

160), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-(morpholine-methyl)-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

161), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4,4-dimethoxy-butylamino)-methyl]--α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

162), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-(piperidin-4-yl-amino-methyl)-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

163), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-pyridin-3-yl-amino of 6-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

164), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-(nafoxidine-methyl)-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

165), (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-sulfydryl-1H-[1,2,4] triazole-3-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

166), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-amino-5-chloropyridine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

167), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-ethyl dimethylamine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

168), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(diallylamine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

169), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,2,2-trifluoroacetamide) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

170), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-amino-2 chloropyridine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

171), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(Benzoylamide) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

172), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-trifluoromethyl benzylamine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

173), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(m-bromoaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

174), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(m-Anisidine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

175), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(paraiodoaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

176), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,4-dinitroaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

177), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,4-dimethylaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

178), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(two (trifluoromethyl) aniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

179), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,4-dichloroaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

180), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-chloroaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

181), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(allopurinol base) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

182), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1,2,4-triazol radical) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

183), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-methylimidazole base) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

184), 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-methyl-2 hydroxy ethylamine base) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone.

The present invention also provides for the pharmaceutically acceptable salt of a kind of described compound, preferably, described salt generates with acid through described compound, and described acid is preferably one or more in hydrochloric acid, oxalic acid, maleic acid, fumaric acid, citric acid, malic acid, isethionic acid, tartaric acid, methanesulfonic acid, ethyl sulfonic acid, hydrobromic acid, sulphuric acid, phosphoric acid, acetic acid, propanoic acid, lactic acid, trifluoroacetic acid, benzoic acid and p-methyl benzenesulfonic acid.

The present invention also provide for a kind of for treat mammal, fowl, fish antibacterial infect or the pharmaceutical composition of protozoal infections, it includes the above-claimed cpd of therapeutically effective amount or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier.

The present invention also provides for above-claimed cpd or its pharmaceutically acceptable salt for preparing the purposes of the medicine of antibacterial infection or the protozoal infections treating mammal, fish or fowl.

Following synthetic route describes the generalformula?compound of the present invention, relate to all of raw material be all by the method described in these signal formulas, prepared by the method that organic chemistry filed is well-known to the ordinarily skilled artisan or be purchased. The all titles compound of the present invention is all prepared by the method described in these signal formulas, and these methods are that organic chemistry filed is well-known to the ordinarily skilled artisan.

The generalformula?compound of the present invention, can be prepared according to following route.

The preparation method of the present invention:

Initial compounds 222 can according to bibliographical information well known to those skilled in the art (one-step synthesis method 9-deoxidation-8a-azepine-8a-homoerythromycin A, synthesis chemistry, 2011,18,265-268 pages) and Chinese patent CN1425022A described in synthetic method prepare.

In compound 222 in embodiment, C-2 ' hydroxyl is optionally protected by processing formula 222 compound with the acetic anhydride of equivalent under the outside alkali existent condition of nothing in dichloromethane, obtains wherein R₄It it is formula 223 compound of acetyl group. Available methanol processes formula 23 compound at 23-65 DEG C and removes Acetyl Protecting Groups in 10-48 hour. The hydroxyl of C-2 ' it be also possible to use other hydroxyl protecting group well known to those skilled in the art, as benzyloxycarbonyl group (Cbz) is protected, period C-4 " hydroxyl also can be protected, but do not affect subsequent experimental. C-2 ' hydroxyl can pass through to process formula 222 compound in oxolane and water with benzyl chloroformate and use Cbz selectivity protected in a step. Cbz group can use the catalytic hydrogenation of routine to remove, it is possible to use well known in the art in suitable organic solvent in about room temperature to the temperature range of about 100 DEG C reaction 2h～5 day can remove. In the following description, C-2 ' and C-4 " hydroxyl be that the appropriate format thought with those skilled in the art is protected or deprotection.

The C-4 of mutual-through type compound 223 " hydroxyl aoxidize. Concentrate C-4 " in the problem of oxidation of position hydroxyl the synthesis focus of parent nucleus. By method well known to those skilled in the art, being described in JournalofAnti-biotics including one or more, the method in 1988,1029-1047 pages, " hydroxyl oxidize is corresponding ketone to the C-4 by formula 223. Such as, the ketone of formula 224 can be prepared with dimethyl sulfoxide and suitable activator. The reaction condition being conventionally used for oxidation includes: as: a) Corey-kim oxidation: J.Med.Chem, 2001,44 (24): 4137～4156; B) Jone ' s reagent: Bioorg.Med.Chem.Lett, 2006,16 (3): 569～572.; C) Dess-martin ' s reagent: US2004/0254126; D) the Pfitzner-maffat oxidation improved: J.Med.Chem, 1998,41 (21): 4080～4100; E) Moffatt oxidation, uses the reaction under pyridinium trifluoroacetate salt exists of N-ethyl-N '-(N, N-dimethylaminopropyl) carbodiimide and dimethyl sulfoxide; Or f) Swem oxidation, its mesoxalic acid chlorine and dimethyl sulfoxide react in dichloromethane, are subsequently added into triethylamine or trifluoroacetic anhydride and dimethyl sulfoxide and react in dichloromethane, add triethylamine etc.

In general formula compound 223, method for oxidation is preferred: dimethyl sulfoxide and trifluoroacetic anhydride and triethylamine aoxidize. At-78 DEG C～50 DEG C, it is preferable that-78 DEG C～-60 DEG C, the desaccharide thing after protection is dissolved in suitable solvent; solvent for use is: dichloromethane, acetone, ethyl acetate; isopropyl acetate etc.; preferred dichloromethane, then adds trifluoroacetic anhydride, it is preferable that dropping; reaction 0～3h; take triethylamine dropping, react 0～3h, react complete process and namely obtain oxide general formula compound 224.

Formula 225 compound can obtain by two kinds of methods.

In first method (method A), with (CH₃)₃S(O)X₂, wherein X₂It is halogen ,-BF₄, or-PF₆, wherein halogen is preferably iodine, at alkali such as potassium tert-butoxide, sodium tert-butoxide, Sodium ethylate, sodium hydride, 1,1,3,3-tetramethyl guanidine, 1,8-diazabicyclo [5.4.0] 11-7-alkene, 1,5-diazabicyclo [4.3.0]-5-in ninth of the ten Heavenly Stems alkene, potassium ethoxide, or Feldalat NM, under preferably existing containing soda such as sodium hydride, solvent is oxolane such as, ether solvents, N, dinethylformamide, or dimethyl sulfoxide, or in the mixture of two or more aforementioned solvents, process in the temperature range of 0 DEG C～about 60 DEG C, formula 225 compound can be obtained.

In second method (method B), with (CH₃)₃SX₂, wherein X₂It is halogen ,-BF4, or-PF₆, it will be preferred that-BF₄, at alkali such as potassium tert-butoxide, sodium tert-butoxide, Sodium ethylate, sodium hydride, 1, 1, 3, 3-tetramethyl guanidine, 1, 8-diazabicyclo [5.4.0] 11-7-alkene, 1, 5-diazabicyclo [4.3.0]-5-in ninth of the ten Heavenly Stems alkene, potassium ethoxide, hexamethyldisiloxane potassium ((KHMDS) (potassiumhexamethyldisilazide), or Feldalat NM, under preferred KHMDS exists, at solvent such as oxolane, ether solvents, N, dinethylformamide, or dimethyl sulfoxide, or in two or more aforementioned molten other mixture, formula 224 compound is processed in the temperature range of-78 DEG C～about 60 DEG C, formula 225 compound can be obtained.

Term " halogen " in the present invention, except as otherwise noted, including fluorine, chlorine, bromine or iodine.

Term " alkyl " in the present invention, except as otherwise noted, including having straight chain, the saturated monovalent hydrocarbon residue of ring-type or side chain or their mixing. It should be understood that when referring to annulus, described alkyl at least exists 3 carbon atoms. This kind of annulus includes cyclopropyl, cyclobutyl and cyclopenta.

Term " alkoxyl " in the present invention, except as otherwise noted, including-O-alkyl, wherein alkyl is as defined above.

Term " aryl " in the present invention, except as otherwise noted, including by removing the hydrogen organic residue derived from aromatic hydrocarbon, such as phenyl or naphthyl.

Term " 5-10 person's heteroaryl " in the present invention, except as otherwise noted, including containing one or more heteroatomic fragrant heterocyclic radicals being respectively selected from O, S and N, wherein each heterocyclic radical has 5-10 atom in ring system. The example of suitable 5-10 person's heteroaryl includes pyridine radicals, furyl, thienyl, pyrazolyl, (1,2,3)-and (1,2,4)-triazolyl, pyrazinyl, tetrazole radical, furyl, thienyl, isoxazole base, azoles base pyrrole radicals and thiazolyl.

The compound of the present invention can contain asymmetric carbon atom and therefore there is different enantiomer and diastereomer form. Methods known in the art can be used, according to the difference on respective physical chemistry, non-enantiomer mixture is divided into single diastereomer, for instance, with chromatograph or fractional crystallization. Can pass through by mixture of enantiomers with suitable optically active compound (such as, alcohol) reaction be converted into non-enantiomer mixture, then separate diastereomer and convert (such as, hydrolysis) each diastereomer and obtain enantiomer pure accordingly. Use all these isomers, including non-enantiomer mixture and pure enantiomer, be all the part of the present invention.

Preferably, the human diseases that antibacterial of the present invention infects and the disease of protozoal infections and these infection causes, including: the pneumonia that caused by pathogenic streptococcus, hemophilus influenza, catarrhalis, staphylococcus aureus, legionella, Actinobacillus, mycoplasma, chlamydia infection, tracheobronchitis, otitis media, sinusitis, tonsillitis, pharyngitis, nephritis; By pathogenic staphylococcus, streptococcus, the microbial heating of rod-like stem, Skin and soft tissue infection, abscess, osteomyelitis; The genitourinary system such as the urethritis that caused by pathogenic staphylococcus, enterococcus, chlamydia, spirillum, mycoplasma, Neisserial infection, cervicitis, gonorrhoea infection, sexually transmitted disease (STD); The Lyme disease caused is infected by B. burgdorferi; The conjunctivitis infected by chlamydia trachomatis, Diplococcus gonorrhoeae, staphylococcus aureus, streptococcus pneumoniae, streptococcus pyogenes, Haemophilus influenzae, or Listeria, keratitis and dacryocystisis; The gastroenteritis that caused by C. jejuni infec-tion or by the ulcer of helicobacter pylori infections; The enteric protozoal infection caused is infected by Crytosporiduumspp;The odontogenic infection infected by viridans streptococci; The intractable cough infected by Bordetella pertussis; By the para-infectious gas gangrene of bacillus perfringens or bacteroid; Arteriosclerosis by helicobacter pylori or infection involving chlamydia pneumoniae.

Preferably, the animal bacterial infection being treated and preventing of the present invention and protozoal infections and relate to the disease of these infection and include following disease: by pasteurella haemolytica, pasteurella multocida, Mycoplasma bovis, or the cattle respiratory system disease that Bordetella infection causes; The Intestinum Bovis seu Bubali tract disease caused is infected by escherichia coli or protozoa (such as coccidiosis); The bovine mastitis caused by staphylococcus aureus, streptococcus uberis, streptococcus agalactiae, streptococcus dysgalactiae, klebsiella, corynebacterium, enterococcal infection; The cattle that caused by coli-infection, pig metritis; The cattle infectious conjunctivitis infected by cattle Mohs bacterium; The cow premature birth and abortion caused is infected by protozoacide (i.e. nesporium); The porcine respiratory disease caused by Actinobacillus, pasteurella multocida, haemophilus, Mycoplasma Infections; The bloodprotozoonoses caused is infected by protozoacide (such as toxoplasma, Eperythrozoon); The Intestinum Sus domestica tract disease caused by escherichia coli, Salmonella, spirochaete infection; Pig septicemia, scytitis, arthroncus necrosis and the suppuration caused by bacillus rhusiopathiae suis, Streptococcus suis, infection due to Bacillus anthracis; The cat that caused by coli-infection, Canis familiaris L. urinary tract infection; By staphylococcus epidermidis, Staphylococcus intermedius, cat that coagulase staphylococcus or Pasteurella multocida Infection cause, Canis familiaris L. Skin and soft tissue infection; By alcaligenes, Bacteroides, fusobacterium, enterobacteria, Eubacterium, peptostreptococcus, the microbial Canis familiaris L. of Detection of Porphyromonas, Prevost, cat tooth or oral cavity infection etc.; The fowl intestinal tract disease caused is infected by escherichia coli, Salmonella, clostridieum welchii; The fowl septicemia, skin soft tissue and the internal organs organa parenchymatosum that are caused by escherichia coli, pasteurellosis bacillus, staphylococcus, streptococcal infection and mucosal inflammation; The protozoacide caused by protozoa (such as coccidiosis, leucocyte protozoon); The respiratory system disease caused by mycoplasma, haemophilus, escherichia coli.

The therapeutic dose of effective dose of the present invention, single-dose is 2-50mg/kg.

" pharmaceutically acceptable salt " of the present invention, except as otherwise noted, including the salt of the acid that may be present in the compounds of this invention or base. the compounds of this invention of alkalescence can form salt with various inorganic and organic acid in nature. can be used for preparing the pharmaceutically acceptable acid of alkali compounds of the present invention, including mineral acid or organic acid, formates such as the present invention, acetate, propionate, lactate, citrate, tartrate, oxalates, malate, hydrochlorate, sulfate, nitrate, disulfate, phosphate, acid phosphate, nicotinate, Salicylate, pantothenate, Ascorbate, succinate, maleate, gentisate, fumarate, gluconate, glucosaccharic acid salt, saccharate, benzoate, glutamate, Glu, mesylate, esilate, benzene sulfonate, tosilate and each seed amino acid. the compounds of this invention being acid in nature can form basic salt with various pharmaceutically acceptable cationes. these salt include alkali and alkaline earth metal ions, such as calcium, magnesium, sodium, potassium etc.

The present invention for treating mammal, fowl, fish antibacterial infect or the pharmaceutical composition of protozoal infections, including containing the compound of formula I or pharmaceutically acceptable salt as active component, with pharmaceutically acceptable carrier.Described pharmaceutically acceptable carrier refers to and any can be used for the diluent of pharmaceutical field, adjuvant.

The dosage form of the pharmaceutical composition of the present invention is oral formulations, injection, external preparation.

Preferably, the oral formulations of the present invention is powder, tablet, capsule, granule, solution, suspensoid. Injection is injectable powder, Emulsion, suspensoid, solution; External preparation is ointment, drop.

Carrier in pharmaceutical composition of the present invention refers to auxiliary element necessary to pharmaceutical field composition preparation, including: diluent, cosolvent, antioxidant, correctives, preservative, excipient, coagulating agent.

Detailed description of the invention

The method examples further illustrating the present invention of following offer and intermediate. But the invention is not restricted to the scope of following embodiment.

It is the route of the embodiment of the present invention 1～80 below:

Embodiment 1

Unlatching cryostat arranges temperature and is-12 DEG C; 1.0L three-necked bottle takes dichloromethane 500mL with 1L graduated cylinder add, it is placed in cryostat and stirs cooling, take 50g (0.068mol) compound 2 by counter balance and join in reaction bulb, take dichloromethane 300mL with 1L graduated cylinder and add in reaction bulb, stirring and dissolving, cooling; It is cooled to interior temperature 0～5 DEG C, keeps reacting liquid temperature 0～5 DEG C, be slowly added dropwise benzyl chloroformate 11.98mL and the mixed solution of dichloromethane 60mL, drip and finish, insulation reaction 1 hour; Adopt thin layer chromatography monitoring reaction process (developing solvent: methylene chloride/methanol=10:1 adds two ammonia). Reaction is finished, to reactant liquor in temperature≤50 DEG C, and vacuum≤-0.086Mpa concentrating under reduced pressure, it is concentrated into about 300mL compound 3;

TLCRf=0.42 (dichloromethane: methanol=7:1)

ESI/MS:m/z869 [M+H]⁺。

Embodiment 2

Opening cryogenic refrigeration equipment, temperature regulating, to-75 DEG C, is cooled to-70～-60 DEG C; Embodiment 1 being concentrated gained be about 300mL compound 3 liquid and be transferred in 1.0L tri-neck reaction bulb, under room temperature, (25～30 DEG C) add dimethyl sulfoxide 106.46mL (117.11g, 1.498mol); Finish dimethyl sulfoxide, reaction bulb is placed in cryostat stirring and is cooled to-70～60 DEG C, take trifluoroacetic anhydride 21.55mL (0.152mol, 31.865g) and control rate of addition to maintain reacting liquid temperature at-65～-60 DEG C, slowly drip and finish, insulation reaction 0.5 hour; Then keep reacting liquid temperature to be slowly dropped into triethylamine 47.3mL (0.339mol, 34.35g) at-65～-60 DEG C, drip off insulated and stirred 0.5 hour; Reaction is finished, and reactant liquor rises to room temperature. The reactant liquor rising to room temperature (20 DEG C～30 DEG C) is proceeded in 2.0L separatory funnel, adds purified water 350mL, extract, discard water layer, obtain organic layer; Organic layer extracts once with saturated sodium bicarbonate solution 250mL again, extracts and gets organic layer, discards water layer, and organic layer extracts with purified water 350mL again, discards water layer, obtains organic layer. Organic layer is transferred in 1.0L beaker addition anhydrous magnesium sulfate 20g, stir 20 minutes to dry and dewater, after filter magnesium sulfate, obtain light yellow filtrate. Light yellow filtrate to dry gained, in temperature≤60 DEG C, vacuum≤-0.086Mpa concentrating under reduced pressure, after being concentrated into about 125mL, adds isopropanol 135mL, it is again concentrated to 135mL, final concentration gained liquid is proceeded in 1.0L three-necked bottle, adds t-butyl methyl ether 700mL, under room temperature, be slowly added dropwise trifluoroacetic acid 11.2mL (0.1497mol, 17.07g), finish stirring and crystallizing under room temperature. Sucking filtration, filter cake is agitator treating 30min in normal heptane (200mL × 2), filter cake 30 DEG C, forced air drying.Obtain 8.2g compound 4. Yield: 82.2%; HPLC measures purity: 91%. (application HPLC-WatersSymmetryC8,15cm × 3.9mmI.D. post, with methanol: ammonium acetate (25:75) for mobile phase, flow velocity 2.0mL/min, retention time 5.07min)

TLCRf=0.39 (dichloromethane: methanol=7:1)

ESI/MS:m/z867 [M+H]⁺。

Embodiment 3

3.0L beaker adds the compound 4 that 50g (0.0456mol) embodiment 2 obtains, dichloromethane 80ml, after stirring and evenly mixing, the solution dry 20min of anhydrous magnesium sulfate 15g, sucking filtration, filtrate is again with anhydrous magnesium sulfate 7g redrying 20min, sucking filtration, filtering residue washed with dichloromethane, filtrate adds dichloromethane to 160ml, and (filtrate is surveyed moisture and be should be less than 0.3%) is standby. Opening cryogenic refrigeration equipment, temperature regulating is to-8 DEG C; (anhydrous magnesium sulfate dries 30min to add oxolane in 1.0L three-necked bottle, sucking filtration) 170mL, it is placed in cryostat stirring and is cooled to-5～0 DEG C, it is added thereto to trimethyl sulfur bromide 20g (0.1273mol), temperature control adds potassium tert-butoxide 20g (0.1786mol), logical nitrogen gas stirring reaction 15min after utilizing water circulating pump evacuation. Regulate cryogenic refrigeration device temperature to-75 DEG C, by interior temperature drop to-65～-60 DEG C; Dried for deacidification solution being added dropwise to reaction bulb, keeps reacting liquid temperature-65～-60 DEG C, be slowly added dropwise, start simultaneously at timing, drip and finish, insulation reaction was to 3 hours; Adopt thin layer chromatography monitoring reaction process (developing solvent: methylene chloride/methanol=10:1 adds two ammonia). Reaction is finished, and adds the 120ml aqueous solution of 21.5g ammonium chloride (0.405mol) in reactant liquor, is warming up to 5～10 DEG C of stirring 15min, stratification, and water layer with 200ml dichloromethane extraction once, merges organic facies; Organic layer washes with water four times mutually, each 100ml; Organic layer is evaporated to no longer distillation; Replacing with methanol 200ml and residual solvent is evaporated off, after replacing twice, concentration obtains compound 5.

TLCR_f=0.55 (dichloromethane: methanol=8:1)

ESI/MS:m/z881 [M+H]⁺。

Embodiment 4

The compound 5 methanol 350ml solution transfer that embodiment 3 prepares, to the three-necked bottle of 1.0L, adds palladium carbon 16g, formic acid ammonia 14.2g (0.2246mol); It is incubated 50 DEG C of reaction 2h; Adopt thin layer chromatography monitoring reaction process (developing solvent: methylene chloride/methanol=10:1 adds two ammonia). Reaction is finished, and reactant liquor is cooled to less than 30 DEG C, sucking filtration, and filtrate reduced in volume is about 200ml extremely, the airtight preservation of filter cake water seal; Concentrated solution is slowly added dropwise in 550ml water, drips in 20 minutes, stirring and crystallizing 1h. Sucking filtration, filter cake methanol-water (1:3) washs, and obtains filter cake; Dry cake obtains compound 6 (application WATERSACQUITYUPLCBEHC18 chromatographic column (2.1 × 50mm, 1.7 μm); Mobile phase is acetonitrile-0.01moL/L ammonium acetate (55:45); Flow velocity 0.20mL/min, retention time 2.77min; Detection wavelength 210nm; Column temperature 40 DEG C, sample size 2.5 μ l. )

TLCR_f=0.45 (dichloromethane: methanol=7:1)

ESI/MS:m/z747 [M+H]⁺。

Embodiment 5

The logical method 1 of preparation

(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclopropylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12, the preparation of 14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone

In 50mL round-bottomed flask, just compound 6 (0.5g, 0.6698mmol), potassium iodide (1.11g, 0.698mmol) with cyclopropylamine (2.43mL, 2.00g, 35mmoL) 50 DEG C of concussion dissolvings, insulation reaction in isopropanol (5mL), TLC detects reaction process, reaction is finished, concentration, and residue is dissolved in water (50mL) and ethyl acetate (100mL).After stratification, water-bearing layer ethyl acetate (3 × 50mL) is washed. merging organic facies, with saturated sodium bicarbonate aqueous solution (50mL), saline (40mL) washing, dry with anhydrous sodium sulfate, filter, filter vacuum concentrates to obtain crude product. silica gel chromatography, with methanol: dichloromethane: ammonia (4:95.6:0.4 to 6:93.5:0.4) eluting, obtain 0.38g title compound (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2, 6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclopropylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3, 4, 10-trihydroxy-3, 5, 8, 10, 12, 14-vegolysen 1-[[3, 4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone.

TLCR_f=0.47 (dichloromethane: methanol=5:1)

ESI/MS:m/z805 [M+H]⁺。

The logical method 2 of preparation

(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(butylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12, the preparation of 14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone

By compound 6 (0.5g, 0.6698mmol), tetrabutylammonium iodide (0.74,2.0mmoL) dissolve 50 DEG C of concussions with the n-butylamine (0.395mL, 0.2938,4mmoL) solution in methanol (5mL), insulation reaction, TLC detects reaction process. reaction is finished, concentration, and residue is dissolved in water (20mL) and ethyl acetate (20mL). after stratification, water-bearing layer ethyl acetate (3 × 20mL) is washed. merging organic extract saline (40mL) to wash, dry with anhydrous sodium sulfate, filter, filter vacuum concentrates, and obtains crude product. silica gel chromatography, with methanol: dichloromethane: ammonia (4:95.6:0.4 to 6:93.5:0.4) eluting, obtain 0.0888g title compound (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2, 6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(butylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3, 4, 10-trihydroxy-3, 5, 8, 10, 12, 14-vegolysen 1-[[3, 4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone.

TLCR_f=0.47 (dichloromethane: methanol=5:1)

ESI/MS:m/z819 [M+H]⁺。

The logical method 3 of preparation

(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylcarbamic) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12, the preparation of 14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone

By compound 6 (0.5g, 0.6694mmol) dissolve with n-propylamine (0.5g) 50 DEG C of concussions in isopropanol (10mL), insulation reaction 48h, TLC detects reaction process, reaction is finished, concentration, is added by condensate residue in saturated sodium bicarbonate solution (50mL) and dichloromethane (80mL), shaking uniform stratification, organic facies dichloromethane use water (3 × 50m1) is washed. Merge organic facies, use MgSO₄Dry and vacuum is concentrated into dry, it is then dissolved in dichloromethane, loading and GF254 silica gel plate, TLC separation is carried out in hexamethylene/diethylamine=4/1 or methylene chloride/methanol/ammonia=4/1/0.01, scraping respective color band, upper prop, then post is rushed with methylene chloride/methanol/ammonia=4/1/0.01, mobile phase is evaporated to 0.16 gram of (2R of sterling of dry aminate in 50 DEG C, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2, 6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylcarbamic) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3, 4, 10-trihydroxy-3, 5, 8, 10, 12, 14-vegolysen 1-[[3, 4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone.

TLCR_f=0.47 (dichloromethane: methanol=5:1)

ESI/MS:m/z807 [M+H]⁺。

The compound of embodiment 5-80 has the structure of following formula 1.

In embodiment 5～80, R is the group described in table 1, and nitrogen element or the element sulphur in R is directly connected in R₃In methylene on. And R ' is H in embodiment 5～80. According to the logical method 1 of above-described embodiment 5 preparation, the logical method 2 of preparation, the lower example embodiment 6-80 of the logical method 3 method preparation of preparation, the concrete response time is listed in table. In table, structure, productivity and mass spectrum (" MassSpec ") data are the data of finalization compound.

Table 1

It is respective compound during n-pro-pyl and preparation thereof that following example relate to R ＇ in formula I:

Embodiment 81

Add methylene chloride 600mL in 2L three-necked bottle, it is placed in cryostat and stirs cooling, the compound 11 prepared by the method in CN102239174A weighs 30g (0.3861mol) and joins stirring and dissolving in reaction bulb, it is cooled to 0～5 DEG C, keep reacting liquid temperature 0-5 DEG C, it is slowly added dropwise benzyl chloroformate 6.8mL (0.424mol, 82.32g) and the mixed solution of dichloromethane 30mL, drip and finish, 0～5 DEG C is reacted 1 hour, rear concentrating under reduced pressure reactant liquor, temperature≤50 DEG C, vacuum≤-0.086Mpa, concentrates to obtain compound 7 concentrated solution 180mL. Move in 2L tri-neck reaction bulb, under room temperature, (25～30 DEG C) add dimethyl sulfoxide 60.6mL (66.6g, 8.532mol), finish, reaction bulb is placed in cryostat stirring and is cooled to-70～-60 DEG C, take trifluoroacetic anhydride 12.18mL (0.864mol, 181.32g) and control rate of addition to maintain reacting liquid temperature at-65～-60 DEG C, slowly drip and finish, insulation reaction 0.5 hour; Then keep reacting liquid temperature to be slowly dropped into triethylamine 26.88mL (1.932mol, 195.3g) at-65～-60 DEG C, drip off insulated and stirred 0.5 hour.

Reaction is finished, and reactant liquor rises to room temperature. Then it is proceeded in 2L separatory funnel, add purified water 210mL, extract to obtain organic layer, discard water layer, organic layer extracts once with saturated sodium bicarbonate solution 150mL again, extracts and gets organic layer, discards water layer, organic layer extracts with purified water 200mL again, discards water layer, obtains organic layer.

Organic layer is transferred in 1.0L beaker addition anhydrous magnesium sulfate 120g, stir 20 minutes to dry and dewater, after filter magnesium sulfate, obtain light yellow filtrate. Light yellow filtrate, in temperature≤60 DEG C, vacuum≤-0.086Mpa concentrating under reduced pressure, it is concentrated into and dry obtains compound 8.

TLCRf=0.60 (dichloromethane: methanol=7:1)

ESI/MS:m/z909 [M+H]⁺。

Embodiment 82

1.0L three-necked bottle adds oxolane 170mL, is placed in cryostat and stirs is cooled to-5～0 DEG C, be added thereto to trimethyl sulfur bromide (0.12256mol, 19.25g), temperature control adds potassium tert-butoxide (0.17156mol, 19.25g), logical nitrogen gas stirring reaction 15min. Then dropping interior temperature to-70 DEG C, the dichloromethane solution dropping that embodiment 81 prepares compound 8 is come in, and timing, temperature control-65～-60 DEG C dropping, dropwises logical nitrogen and continues to react to 3h.

20.85g ammonium chloride (0.39mol is added in reactant liquor, 20.85g) 120ml aqueous solution, it is warming up to 5～10 DEG C of stirring 15min, stratification, water layer is with 200ml dichloromethane extraction once, dichloromethane layer washes with water after merging with organic layer four times, each 200ml, washes complete organic layer and is evaporated to and no longer has distillation.Then replace with methanol 200ml and residual solvent is evaporated off, after replacing twice, concentrate to obtain compound 9.

TLCRf=0.58 (dichloromethane: methanol=7:1)

ESI/MS:m/z923 [M+H]⁺。

Embodiment 83

Dissolve embodiment 82 with 170ml methanol and prepare compound 9, it is added thereto to palladium carbon 16g, formic acid ammonia 13.63g (0.2164mol, 13.63g), 50 DEG C of insulation reaction 2h, cooling sucking filtration, the airtight preservation of filter cake water seal, filtrate reduced in volume is about 80ml extremely, then it is slowly added dropwise in 250ml water, dripping in 20min, the sodium hydroxide solution with 10% adjusts pH to 10.5 ± 0.5, stirring and crystallizing 1h. Sucking filtration, filter cake methanol-water (1:3) washs, and 40 DEG C of forced air dryings obtain compound 10.

TLCRf=0.33 (dichloromethane: methanol=7:1)

ESI/MS:m/z789 [M+H]⁺。

Embodiment 84

The logical method a of preparation

(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclopropylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12, the preparation of 14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone

In 50mL round-bottomed flask, just embodiment 83 prepares compound 10 (0.5g, 0.6698mmol), potassium iodide (1.11g, 0.698mmol) with cyclopropylamine (2.43mL, 2.00g, 35mmoL) 50 DEG C of concussion dissolvings, insulation reaction in isopropanol (5mL), TLC detects reaction process, reaction is finished, concentration, and residue is dissolved in water (50mL) and ethyl acetate (100mL). After stratification, water-bearing layer ethyl acetate (3 × 50mL) is washed. Merging organic facies, with saturated sodium bicarbonate aqueous solution (50mL), saline (40mL) washing, dry with anhydrous sodium sulfate, filter, filter vacuum concentrates to obtain crude product. Silica gel chromatography, with methanol: dichloromethane: ammonia (4:95.6:0.4 to 6:93.5:0.4) eluting, obtains 0.38g title compound.

TLCR_f=0.47 (dichloromethane: methanol=5:1)

ESI/MS:m/z846 [M+H]⁺。

The logical method b of preparation

(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(n-butylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-

The preparation of [[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone

Embodiment 83 is prepared compound 10 (0.5g, 0.6698mmol), tetrabutylammonium iodide (0.74,2.0mmoL) with n-butylamine (0.395mL, 0.2938,4mmoL) solution in methanol (5mL) dissolves 50 DEG C of concussions, and insulation reaction, TLC detects reaction process. Reaction is finished, concentration, and residue is dissolved in water (20mL) and ethyl acetate (20mL). After stratification, water-bearing layer ethyl acetate (3 × 20mL) is washed. Merging organic extract saline (40mL) to wash, dry with anhydrous sodium sulfate, filter, filter vacuum concentrates, and obtains crude product. Silica gel chromatography, with methanol: dichloromethane: ammonia (4:95.6:0.4 to 6:93.5:0.4) eluting, obtains 0.0888g title compound.

TLCR_f=0.47 (dichloromethane: methanol=5:1)

ESI/MS:m/z862 [M+H]⁺。

The logical method c of preparation

(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(n-pro-pyl amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12, the preparation of 14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone

Embodiment 83 is prepared compound 10 (0.5g, 0.6694mmol) with n-propylamine (0.5g, 25n1mmo1) in isopropanol (10mL), 50 DEG C of concussions are dissolved, insulation reaction 72h, TLC detect reaction process, and reaction is finished, concentration, being added by condensate residue in saturated sodium bicarbonate solution (50mL) and dichloromethane (80mL), shake uniform stratification, organic facies dichloromethane use water (3 × 50m1) is washed.Merge organic facies, use MgSO₄Dry and vacuum is concentrated into dry, it is then dissolved in dichloromethane, loading and GF254 silica gel plate, TLC separation is carried out in hexamethylene/diethylamine=4/1 or methylene chloride/methanol/ammonia=4/1/0.01, scraping respective color band, upper prop, then rushes post with methylene chloride/methanol/ammonia=4/1/0.01, and mobile phase is in the title compound of 50 DEG C of sterlings 0.16 gram being evaporated to dry aminate.

TLCR_f=0.47 (dichloromethane: methanol=5:1)

ESI/MS:m/z848 [M+H]⁺。

The compound of embodiment 85-187 has the structure of following formula 1, and wherein substituent R is as listed in table 2. According to the logical method a of above-described embodiment 84 preparation, the logical method b of preparation, the lower example embodiment 85-187 of the logical method c method preparation of preparation, the concrete response time is listed in table. In table, structure, productivity and mass spectrum (" MassSpec ") data are the data of finalization compound.

In embodiment 84～187, R is the group described in table 2, and nitrogen element or the element sulphur in R is directly connected in R₃In methylene on. R ' is n-pro-pyl in embodiment 84～187.

Table 2

Although describing the present invention according to detailed description of the invention, but those skilled in the art obviously understand some being changed and equivalent, they are included within the scope of the invention.

Table 3 provides the structural formula of part of compounds in table 1 and table 2.

Table 3

Embodiment 188: the conventional bacterial strain extracorporeal sensitivity of test chamber is measured by the compounds of this invention

According to U.S. NCCLS antimicrobial agents sensitivity experiments operation standard, the enforcement 5 of preparation is prepared compound to embodiment 187 and carry out Determination of Antibacterial Activity, medicine prepared by this operation employing micro-broth dilution method embodiment MIC (minimal inhibitory concentration) to strains.

1. bacterial strain

Staphylococcus aureus CVCC26003, adenitis equorum streptococcus CVCC556, Actinobacillus pleuropneumoniae CVCC262, haemophilus parasuis infection, pasteurella multocida CVCC399, above bacterial strain is purchased from China Veterinary Drugs Supervisory Inst..

2. trial drug (comparison)

Gamithromycin, content 95.2%, prepare with reference to CN102239174A method;

Tulathromycin, content 96.4%, prepare with reference to CN1530370A method;

3. test equipment

Clean bench, model: SuZhou Antai Air Tech Co., Ltd. of SW-CJ-2FD, Su Jing group; Electro-heating standing-temperature cultivator, model: DNP-9272BS-III, Shanghai new talent medical apparatus and instruments Manufacturing Co., Ltd; Nucleic acid-protein analyzer, model: 6132, Germany eppendorf; Double-range electronic balance, model: ABC-265, METTLERTOLEDO; MHA, lot number: 20120921, Qingdao GaoKeYuan Hai Bo Bioisystech Co., Ltd; MHB, lot number: 20120229, Qingdao GaoKeYuan Hai Bo Bioisystech Co., Ltd; New-born calf serum, lot number 20120824, Wei Kesheng bio tech ltd, the Inner Mongol; Plastic culture dish, Yangzhou brilliance medical apparatus and instruments factory; 96 road liquor removing workstations, METTLERTOLEDO; Single track pipettor, multichannel pipettor, Germany eppendorf.

4. test method

The preparation of 4.1 culture medium

4.1.1 staphylococcus aureus 26003 used medium

Fluid medium: CAMHB:MHB adds CaCl in (illustrating to prepare by finished product)₂And MgCl₂, make Ca²⁺Final concentration of 20mg/L and Mg in the medium²⁺Final concentration of 10mg/L in the medium.

Solid medium: MHA, illustrates to prepare by finished product.

4.1.2 all the other four kinds of bacterium used mediums

Fluid medium: CAMHB+10% calf serum+0.005%NAD+.

Solid medium: MHA+10% calf serum+0.005%NAD+.

4.2 strain recoveries

Taking out strain from-20 DEG C of refrigerators to recover, inoculating loop takes ring line on corresponding solid medium; Postvaccinal culture medium is placed in constant incubator, cultivates 20h, picking monoclonal from well-grown flat board, solid medium is rule, postvaccinal culture medium is placed in constant incubator for 35 DEG C, cultivate 20h for 35 DEG C.

The dilution of 4.3 compounds

5～embodiment 80 and embodiment 84～187 will be implemented it will be configured to by compound the concentration of 8.8mg/ml with 100%DMSO, take 96 orifice plates, 2-11 hole adds 100 μ lDMSO, 1st hole adds the drug solution 200 μ l prepared, 100 μ l medicinal liquids are drawn to the 2nd hole from the 1st hole, carry out doubling dilution to the 11st hole, be diluted to 11 gradients, prepare motherboard compound. Drawing, with 12 road pipettors, the medicine that 3 μ l doubling dilutions are good from motherboard compound, join in the 1-11 hole of new disposable 96 well culture plates, the 12nd hole is control wells, and it is parallel that each medicine is 2 rows, and the compound plate after transfer is standby.

4.4 bacterium solution preparations

From 4.2, in the flat board of preparation, picking colonies typical, to normal saline, regulates OD₆₀₀Value, between 0.14-0.15, records dilution ratio, and by required for test bacterium solution by this dilution proportion, bacteria suspension and fluid medium are diluted in the ratio of 1:200 afterwards, standby.

4.5 test operations

Taking the compound plate in 4.3, by adding medicine and bacterium solution shown in table 4, every kind of medicine two row, every block of plate does a kind of bacterium. Obtained experimental result is in Table 5. Part once not can determine that the compound of MIC selects diluted concentration to further determine that again.

Table 496 orifice plate additive signal chart

cmd

1

2

3

4

5

6

7

8

9

10

11

12

A

○

■

B

○

■

C

○

■

D

○

■

E

○

▲

F

○

▲

G

○

▲

H

○

▲

Zero represents 3 μ l compound+100 μ l bacterium solution; ■ represents that positive control, hole include 100 μ l bacterium solution; ▲ represent negative control,

Hole includes 100 μ l culture medium.

The MIC value (ug/ml) of table 5 compound

Antibacterial activity in vivo uses conventional animal experimental technique well known to those skilled in the art to detect, and laboratory animal is BALB/c mouse.

Test material: streptococcus pneumoniae reference culture, is numbered CMCC31203, is purchased from Chinese medicine antibacterial preservation administrative center. Tulathromycin, prepares with reference to CN1530370A method.

Trial drug: compound (syzx-1 prepared by 5 three logical methods of the embodiment of the present invention, syzx-2, syzx-6), embodiment 6 (syzx-3), embodiment 8 (syzx-5), embodiment 12 (syzx-10), embodiment 13 (syzx-11), embodiment 14 (syzx-12), embodiment 15 (syzx-14), embodiment 16 (syzx-15), embodiment 17 (syzx-17), the logical method C (syzx-101) of embodiment 84 preparation, embodiment 26 (syzx-30), embodiment 30 (syzx-35), embodiment 38 (syzx-47) embodiment 45 (syzx-58), 52 (syzx-65), embodiment 53 (syzx-66) embodiment 54 (syzx-67), embodiment 170 (syzx-213) prepares the compound of gained, compare with Tulathromycin simultaneously. test front dehydrated alcohol by medicine dissolution, supply with distilled water volume required and after filling and releasing mixing, be configured to the liquid that concentration is 1mg/mL.

The mice 350 in test method: 5-6 week, selects the body weight carrying out between 18-20g point cage, 10, every cage, raises 72h, observe and normally can enter test. Before experiment, streptococcus pneumoniae blood plate is cultivated 24h, add 37 DEG C of shaken cultivation (120r/min) 20h Zengjing Granule in the aseptic meat soup containing serum, carry out count plate.It is diluted to 5 × 10 with sterile saline⁸Cfu/mL, mouse peritoneal injection carries out counteracting toxic substances, every 0.5mL. Counteracting toxic substances the 2nd day, take compound and control drug prepared by above-described embodiment, it is administered by 5mg/kg body weight cervical region subcutaneous injection, successive administration 3 days, sets blank composition of medicine matched group simultaneously, it is not administered after drug control group counteracting toxic substances, drug control group presses 10mg/kg body weight injection Tulathromycin, and after counteracting toxic substances, administration, every day observes animal, record the death toll of each group, observe to the 7th day. Table 6 is the general formula compound of the present invention impact on streptococcus pneumoniae mouse survival rate.

1, result of the test

The internal antibacterial tests result of table 6 part of compounds

2, result

Showing to give the compound of present configuration formula by 5mg/kg body weight from table 6 result, to reduce the mouse infection that streptococcus pneumoniae causes dead, compared with matched group, it is possible to significantly improves the survival rate of test group mice after counteracting toxic substances, shows obvious antibacterial activity in vivo.

Embodiment 189: the acute toxicity test of compound Syzx-24

1, experiment material

1.1 for reagent product

Nomenclature of drug: the compound of lot number Syzx-24, Tulathromycin, content 96.4%, prepare with reference to CN1530370A method.

1.2 animal subjects

Balb/c mice, body weight 16.0-19.0g, male and female half and half. Mice male and female sub-cage rearing before test, observes 3 days, and the mice 12 (male and female half and half) selecting bouncing is used for testing, and before administration, water 14h (some 6 pm the night before last to the next morning 8) is can't help in fasting.

1.3 test articles for use

Mouse stomach device, 1ml disposable syringe, 50mL, 100ml beaker, independent air-feeding Mus isolation cage tool (IVC), ophthalmologic operation is cut, tweezers, medical tray, the basic fuchsin dye liquor of 0.5%, medical rubber glove, analytical balance, electronic balance.

2, test method

2.1 experimental animals and packet

Test sets 3 groups, and often 4 animals (male and female half and half) of group, organize respectively Tulathromycin group, Syzx-24 group and solvent control group for 3. Each treated animal dyes with the basic fuchsin of 0.5% and makes marks, Tulathromycin group echo position: upper left shoulder (female), left rib (female), right upper shoulder (hero), right rib (hero); Syzx-24 group echo position: left hind (female), cervical region (female), right hind (hero), cervical region (hero); Solvent control group echo position: be unstained.

Administration group press 2000mg/kg.d-1 dosed administration (bibliographical information Tulathromycin to its mouse oral contaminate after minimum lethal dose more than 2000mg/kg.d-1).

2.2 medicine preparations

Take sodium carboxymethyl cellulose 0.2g to add in 40ml purified water, place 80 DEG C of stirring and dissolving, be made into 0.5% carboxymethylcellulose sodium solution, as the solvent of compounding pharmaceutical. For reagent thing according to dosage, 0.5% carboxymethylcellulose sodium solution will be added and is made into the suspension of 170mg/ml, add the carboxymethylcellulose sodium solution of equal-volume 0.5%, cross 100 mesh sieves, be configured to the suspension of 85mg/ml.

2.3 medications

By 2000mg/kg.d-1, medicine being made into the suspension that concentration is 85mg/ml, once, every mice 0.47ml/20g, concrete packet and medication are in Table 7 for gastric infusion.

Table 7 experimental animal is grouped

Conventional after administration raise, observed and recorded be administered latter 6 hours in animal poisoning symptom and death condition. Continuous observation 30 minutes after administration, observe 1 time on the 1st～4 hour again, observe later every day 1 time until animal recovers normal, record the toxic reaction and death toll that occur, and dead animal is dissected at any time, observes its heart, liver, spleen, lung, kidney, gastrointestinal organ.

3, result of the test and analysis

After 3.1 contamination 6h, mortality rate compares, and table 8 is each group of death condition and mortality rate.

Table 8 animal dead result

Group	Dead animal number/animal number	Mortality rate
			Tulathromycin group	3/4 (2 female, 1 heros)	75%
Syzx-24 group	0/4	0%
			Solvent control group	0/4	0%

Acute toxicity test shows that toxicity of compound that the present invention obtains is significantly lower than Tulathromycin.

Embodiment 190: the acute toxicity test of the oral administration of part of compounds of the present invention

1, test material

1.1, appliance material: 1ml disposable plastic asepsis injector, minor operation are cut, disposable rubber gloves, WKZ-4 type pulverizer, mortar, graduated cylinder, beaker, TIANYIJA2003 electronic balance, medical tray, picric acid dyestuff, medical rubber glove, mouse stomach device (No. 12), sodium carboxymethyl cellulose (Tianjin Ke Miou reagent company limited) etc.

1.2, for reagent product: compound (syzx-1 prepared by 5 three logical methods of embodiment, syzx-2, syzx-6), embodiment 6 (syzx-3), embodiment 8 (syzx-5), embodiment 12 (syzx-10), embodiment 13 (syzx-11), embodiment 14 (syzx-12), embodiment 15 (syzx-14), embodiment 16 (syzx-15), embodiment 17 (syzx-17), embodiment 45 (syzx-58), the logical method C (syzx-101) of embodiment 84 preparation, embodiment 170 (syzx-213).

Medicine solvent: the carboxymethylcellulose sodium solution of 0.2%.

1.3, experimental animal: Kunming mouse, SPF level, male and female half and half, body weight 18-22g, purchased from Henan Province's Experimental Animal Center, credit number: SCXK (Henan) 2010-0002. Use mice IVC independent air-feeding isolation cage tool, male and female sub-cage rearing. Rearing conditions: sterilizing complete feed is fed, free choice feeding and drinking-water, room temperature 20～24 DEG C, relative humidity 40～60%.

2 test methods

The preparation of 2.1 medicines

2.1.10.2% carboxymethylcellulose sodium solution preparation: taking 0.2g sodium carboxymethyl cellulose, be dissolved in 100ml purified water, placement overnight makes swelling, stirs, standby.

2.1.2 take bright embodiment mortar to grind, cross 100 mesh sieves, standby.

2.2 test methods

LD is determined by trial test repeatedly₀～LD₁₀₀Interval range, and the packet complied with, it is determined that compare between group.

The mice 60 of 18-22g is selected in every kind of medicine formal test, male and female is separated, weighs, and the mice (such as 18.0-18.9g, 19.0-19.9g etc.) of same body weight section puts into a cage, labelling. Male and female mice is randomly divided into 6 groups by body weight level, makes the mice of different sexes and body weight be uniformly distributed in each group, often group 10, male and female half and half. First medicine is configured with the carboxymethylcellulose sodium solution of 0.2% by the drug level set before contamination, the dosage gavage of 0.2ml/10g body weight 1 time, fasting 12～16h before gavage, can't help water, in detail the general health situation of observed and recorded mice, poisoning manifestations and death process immediately after gavage, dead mice is substantially analysed in time, Continuous Observation 7 days.

Per os LD is calculated according to improvement karber's method₅₀And 95% fiducial limit (FL). Formula is as follows:

LD₅₀=lg^-1[X_m-i(∑p-0.5)]

S_{x 50} = i \sqrt{Σ \frac{p q}{n}}

95% fiducial limit: FL=lg^-1(lgLD₅₀±1.96×S_x50)

In formula: X_mThe logarithm value of maximal dose;

The logarithm of i adjacent doses ratio;

P respectively organizes the mortality rate (with fractional representation) of dosage;

Q respectively organizes the survival rate of dosage, q=1-p;

∑ p respectively organizes mortality rate sum;

The each treated animal number of n;

P_mMost high mortality;

P_nMinimum mortality;

S_x50——lgLD₅₀Standard error.

3, result of the test

The Oral Acute Toxicity result of the test of table 9 part of compounds of the present invention

According to chemicals acute toxicity LD in veterinary drug acute toxicity guideline₅₀Dose fractionation standard, LD₅₀Between 501～5000mg/kg, it is determined that for low toxicity, although be all low toxicity, but the toxicity of compound that substantially prepared by the embodiment of the present invention is lower.Those of skill in the art would appreciate that LD₅₀When being worth more high, toxicity is more little.

The foregoing is only presently preferred embodiments of the present invention, not in order to limit the present invention, all within the spirit and principles in the present invention, any amendment of making, equivalent replacement, improvement etc., should be included within protection scope of the present invention.

Claims

1. a macrolides compound, the general structure of wherein said macrolides compound is such as shown in formula I,

Wherein, R ＇ is H or C₁～C₆Alkyl;

R₁Selected from H, hydroxyl, methoxyl group, propargyl, aryl and azacyclo-;

R₂For hydroxyl;

R₄Selected from H, acetyl group and benzyloxycarbonyl group.

2. compound according to claim 1, it is characterised in that R₃For-CH₂NR₂₀R₃₀Or-CH₂SR₄₀, wherein R₂₀、R₃₀And R₄₀All independently be H or contain or without heteroatomic organic group, described hetero atom is selected from O, N, S and halogen and R₂₀And R₃₀Between selectively key be linked to be ring.

3. compound according to claim 1, it is characterised in that R₃For-CH₂NHR₅₀, and R₅₀For being selected from containing or without heteroatomic organic group, described hetero atom is selected from O, N, S and halogen.

4. compound according to claim 3, it is characterised in that R₅₀For selected from n-pro-pyl, normal-butyl, cyclopropyl, ethyl, isopropyl, isobutyl group, the tert-butyl group, Cvclopropvlmethvl, 2-methoxy ethyl, cyclopenta, 2,4-difluorobenzyl, 3-methoxy-benzyl, n-pentyl, 2-Methyl-pyrazin-5-base-methyl, 3-methoxy-propyl, cyclohexyl methyl, 4-methoxyphenethyl.

5. compound according to claim 2, it is characterised in that R₃For-CH₂NR₂₀R₃₀, and R₂₀And R₃₀It is each independently C₁～C₆Alkyl.

6. compound according to claim 5, it is characterised in that R₂₀And R₃₀It is each independently methyl or ethyl.

7. compound according to claim 1, it is characterised in that described R₃Middle R is nitrogen-containing heterocycle compound, and wherein nitrogen element and R₃In the carbon of methylene be joined directly together.

8. compound according to claim 7, it is characterised in that R₃Middle R is morpholine, piperidines or piperazine.

9. compound according to claim 2, it is characterised in that R₂₀And R₃₀Collectively form 4～10 yuan of monocycles or R₂₀And R₃₀Collectively form by 1 or 2 optionally substituted 5～10 yuan of hetero-aromatic ring of alkyl.

10. compound according to claim 2, it is characterised in that R₂₀And R₃₀In one be H, another is the organic group containing phenyl or benzyl.

11. the compound according to any one in claim 1～10, it is characterised in that described compound is:

1) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylcarbamic) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

2) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(butylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

3) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(diethylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

4) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(phenyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

5) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(morpholine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

6) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclopropylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

7) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(pyrrole radicals) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

8) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-fluorobenzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

9) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(imidazoles) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

10) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(ethylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

11) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(isopropylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

12) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(isobutylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

13) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[tert-butylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

14) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[piperidine methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

15) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(Cyclopropyl-methyl-amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

16) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-methoxYbenzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

17) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-chlorobenzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

18) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-picolyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

19) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[((3-ethoxycarbonyl propyl) amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

20) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-methoxy ethyl) amino-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

21) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[2-methoxybenzyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

22) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(2-[(N-methyl) amino]-ethyl) amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

23) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(clopentylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

24) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[2,4-difluorobenzyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

25) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(6-chloro-pyridazine-3-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

26) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-3-phenyl) propyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

27) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[3-methoxybenzyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

28) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[2,2,2-trifluoroacetyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

29) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[[(the chloro-pyridin-4-yl-amino of 2-)-methyl]-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

30) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[[(4-formyl-benzyl-amino)-methyl]-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

31) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[propargyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

32) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[butanoic acid base-2-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

33) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[butanoic acid base-4-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

34) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-hydroxy-propyNamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

35) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[n-pentyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

36) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(morpholine-4-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

37) 3-({ (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-6-[-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl--1-oxa--7-azacyclo-pentadecane-15-ketone-13-base-oxygen]-3-hydroxyl-4-methoxyl group-2,4-dimethyl-tetrahydro pyrans-3-base-methyl }-amino)-butanoic acid;

38) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methylol-propylcarbamic)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

39) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-hydroxyl-2-phenyi-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

40) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-dimethoxy-butylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

41) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,4-dichloro-benzylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

42) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methyl-4-dimethrlaminobutyl amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

43) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(3-Cyclohexylamino) the third amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

44) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(4-methanesulfonylphenYl ethylamino) the third amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

45) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-but-1-ene-3-alkynes-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

46) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-butvl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

47) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(2-pyridin-4-yl-ethyl ammonia)-methyl]]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

48) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C--{ [(5-Methyl-pyrazin-2-base-methyl)-ammonia]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

49) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(3-methoxy-propvl-ammonia)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

50) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(Cyclohexyl-methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

51) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-fluoro-phenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

52) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-morpholine-propyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

53) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(furfuryl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

54) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-aminobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

55) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(phenylhydrazino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

56) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-{ [2-(1H-indol-3-yl)-ethylamino]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

57) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-chloropropyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

58) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,5-Dimethoxyphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

59) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(thiophenecarboxylate base-2-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

60) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-methyl furfuryl amine base)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

61) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the fluoro-phenylhydrazine of 4-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

62) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(benzyloxy-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

63) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(p-methoxyphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

64) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,4-3,5-dimethylphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

65) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-fluorine pyridine-2 amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

66) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-pyrroles-ethyl base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

67) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-pyridin-4-yl-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

68) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-luorobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

69) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-piperidin-4-yl-Methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

70) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-o-tolyl-amino of 5-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

71) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-fluoro-phenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

72) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the fluoro-5-aminomethyl phenyl-amino of 2-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

73) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-phenyl-amino of 2-methyl-4-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

74) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-methyl-butvl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

75) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(quinoline-6-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

76) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1,2,2-trimethyl-propyl amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

77) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(n-pro-pyl-amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

78) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(normal-butyl-amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

79) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(pentyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

80) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(diethylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

81) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(phenyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

82) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(morpholine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

83) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-{ [(5-amino-1,3,3-trimethyl cyclohex ylmethyl)-amino]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

84) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[piperonyl amino-methyl)]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-, (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

85) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-fluorobenzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

86) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1,2,3-triazole) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

87) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(ethylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-, 1-oxa--7-azacyclo-pentadecane-15-ketone;

88) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(isopropylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

89) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(isobutylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

90) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-chlorphenylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

91) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(tert-butylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

92) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(n-hexyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

93) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-trifluoromethyl benzyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

94) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(Cyclopropyl-methyl amino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

95) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-Methoxy-benzylamino) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

96) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(4-Nitro-benzyl) amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

97) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[the chloro-benzyl-amino of 4-]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

98) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-pyridyl-methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

99) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(3-ethyoxyl-propyl group)-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

100) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-methoxy ethyl)-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

101) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-methyl-2-hydroxy-ethyl) amino-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

102) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-methyoxy-benzyl)-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

103) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclopenta-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

104) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,4-difluorobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

105) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(6-chloro-pyridazine-3-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

106) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4-hydroxy-butyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

107) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methyl-3-phenyl-propylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

108) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-Methoxy-benzylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

109) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[piperazinyl-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

110) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[trifluoroacetamido]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

111) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[[(the chloro-pyridin-4-yl-amino of 2-)-methyl]-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

112) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[4-formyl benzylamino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

113) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[propargyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

114) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[1-butanoic acid base 2-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

115) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[1-butanoic acid base 4-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

116) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[diethylene glycol base-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

117) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-hydroxyl-1-ethoxy-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

118) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-hydroxy-propyNamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

119) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[n-pentyl-amino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

120) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(morpholine-4-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

121) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-amino-butyric acid base)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

122) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methylol-propylcarbamic)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

123) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-hydroxyl-2-phenyi-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

124) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,4-difluorophenyl methylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

125) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,5-difluorophenyl methylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

126) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-methoxyethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

127) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1-methyl-4-diethylamino butylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

128) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[4-sulfoamido-phenylethylamino]-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

129) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-but-1-ene-3-alkynes-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

130) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(1-methyl-butvl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

131) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(2-pyridin-4-yl-ethylamino)-methyl]]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

132) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-{ [(5-Methyl-pyrazin-2-base-methyl)-amino]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

133) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[[(Cyclohexyl-methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

134) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-fluoro-phenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-vegolysen 1-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

135) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-morpholine-propyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

136) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-phenyl methyl-amino of 2-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

137) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-furan-Methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

138) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-aminobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

139) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(phenylhydrazino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

140) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-{ [2-(1H-indol-3-yl)-ethylamino]-methyl }-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

141) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-chlorine-propyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

142) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,5-Dimethoxyphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

143) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-methyl-ribofuranosyl-2-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

144) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the fluoro-phenylhydrazino of 4-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

145) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(benzyloxy-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

146) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(p-methoxyphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

147) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3,4-3,5-dimethylphenyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

148) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(to fluoro thiophenol)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

149) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-fluorine pyridine-2-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

150) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(diethyl-4-methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

151) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-morpholine-propyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

152) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-pyrroles-ethyl base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

153) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-pyridin-4-yl-ethylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

154) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-luorobenzyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

155) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-piperidin-4-yl-Methyl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

156) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-phenyl-amino of 2-methyl-4-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

157) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-methyl-butvl-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

158) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4,6-Dichloro-pyrimidin-2-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

159) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(cyclo-heptylamino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

160) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-(morpholine-methyl)-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

161) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(4,4-dimethoxy-butylamino)-methyl]--α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

162) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-(piperidin-4-yl-amino-methyl)-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

163) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(the chloro-pyridin-3-yl-amino of 6-)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

164) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-(nafoxidine-methyl)-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

165) (2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(5-sulfydryl-1H-[1,2,4] triazole-3-base-amino)-methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[the 3,4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-1-oxa--7-azacyclo-pentadecane-15-ketone;

166) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-amino-5-chloropyridine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

167) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-ethyl dimethylamine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

168) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(diallylamine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

169) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,2,2-trifluoroacetamide) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

170) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-amino-2 chloropyridine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

171) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(Benzoylamide) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

172) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(3-trifluoromethyl benzylamine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

173) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(m-bromoaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

174) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(m-Anisidine) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

175) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(paraiodoaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

176) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,4-dinitroaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

177) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,4-dimethylaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

178) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(two (trifluoromethyl) aniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

179) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2,4-dichloroaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3,4, the 6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

180) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-chloroaniline) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

181) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(allopurinol base) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

182) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(1,2,4-triazol radical) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

183) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(2-methylimidazole base) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone;

184) 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(N-methyl-2 hydroxy ethylamine base) methyl]-α-L-ribopyranoside base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl group-11-[[3, the 4,6-tri-own xylopyranosyl of deoxidation-3-(dimethylamino)-β-D-] oxygen base]-(2R, 3S, 4R, 5S, 8R, 10R, 11R, 12S, 13S, 14R)-1-oxa--7-azacyclo-pentadecane-15-ketone.

12. the pharmaceutically acceptable salt of a compound as described in any one in claim 1～11.

13. pharmaceutically acceptable salt according to claim 12, it is characterized in that, described salt generates with acid through described compound, and described acid is preferably one or more in hydrochloric acid, oxalic acid, maleic acid, fumaric acid, citric acid, malic acid, isethionic acid, tartaric acid, methanesulfonic acid, ethyl sulfonic acid, hydrobromic acid, sulphuric acid, phosphoric acid, acetic acid, propanoic acid, lactic acid, trifluoroacetic acid, benzoic acid and p-methyl benzenesulfonic acid.

14. for treat mammal, fowl, fish antibacterial infect or the pharmaceutical composition of protozoal infections, it includes in the claim 1～11 of therapeutically effective amount compound described in any one or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier.

15. compound described in any one or its pharmaceutically acceptable salt are for preparing the purposes of the medicine of antibacterial infection or the protozoal infections treating mammal, fish or fowl in claim 1～11.