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    Lincomycin 3-nucleotides and the salts thereof
    5.
    发明授权
    Lincomycin 3-nucleotides and the salts thereof 失效
    LINCOMYCIN 3核和它的销售

    公开(公告)号：US3671647A

    公开(公告)日：1972-06-20

    申请号：US3671647D

    申请日：1971-03-24

    Applicant: UPJOHN CO

    Inventor： ARGOUDELIS ALEXANDER D ,  COATS JOHN H

    IPC: C07H15/16 ,  C07H19/04 ,  C07C47/18

    CPC classification number: C07H19/04 ,  C07H15/16 ,  Y10S435/886

    Abstract: This invention relates to novel antibacterial compounds and to processes for preparing them. It is particularly directed to novel 3-nucleotides of lincomycin, and of analogs thereof, and of celesticetins. The compounds of the invention can be shown by the following formula:

    WHEREIN Y is -SR wherein R is alkyl of one to six carbon atoms, inclusive, , OR -S-CH2-CH2-OH, R1 is H, or cis or trans lower-alkyl of from one to eight carbon atoms, inclusive; R2 is H, CH3, or C2H5; X is OH, chlorine, bromine, iodine or -OR3 wherein R3 is alkyl of one to six carbon atoms, inclusive, each in the (R) or (S) configuration; and Z is a nucleoside -5''- phosphate group wherein said nucleoside can be adenosine, guanosine, cytidine or uridine; and salts thereof. Examples of alkyl of from one to eight carbon atoms are methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, and octyl and isomers thereof.

    Abstract translation: 本发明涉及新的抗菌化合物及其制备方法。 特别涉及林可霉素及其类似物和celesticetins的新型3-核苷酸。 本发明的化合物可用下式表示：

    Antibiotic armentomycin and a process for producing the same
    8.
    发明授权
    Antibiotic armentomycin and a process for producing the same 失效
    抗生素弓形体霉素及其制备方法

    公开(公告)号：US3342681A

    公开(公告)日：1967-09-19

    申请号：US44861165

    申请日：1965-04-16

    Applicant: UPJOHN CO

    Inventor： ARGOUDELIS ALEXANDER D ,  HERR ROSS R ,  MASON DONALD J

    IPC: A01N63/02 ,  C07G11/00 ,  C12P13/04 ,  G03F7/34

    CPC classification number: A61K31/70 ,  C10M1/08 ,  C10M2215/04 ,  C10M2215/26 ,  C10N2240/401 ,  C10N2250/121 ,  C12P13/04 ,  Y10S435/886

    Abstract: 1,131,079. Armentomycin. UPJOHN CO. 25 March, 1966 [16 April, 1965], No. 13338/66. Heading C2A. [Also in Divisions A5, C5 and D2] The invention relates to the new antibiotic, armentomycin, which inhibits the growth of Gram-negative bacteria and has the following properties: Empirical formula, C 4 H 7 Cl 2 NO 2 ; an analysis, C-28À39%, H-4À44%, N-9À09%, Cl-40À60%, and O-17À48%; a calculated mol. wt. of 172; an equivalent weight of 168 by KOH titration and 174 by perchloric acid titration; an optical rotation [α] 25 D = +6À7‹ (C. 0À74 in water) and [α] 25 D = 26À240 (C. 0À74 in water at pH 1À0); a pKa of 8À28; no U.V. maxima between 220 and 400 mÁ; an I.R. spectrum as in Fig. 1 above; and is soluble in water, methanol and ethanol, and insoluble in methylene chloride, acetone and non-polar solvents. Armentomycin is amphoteric and forms acid addition salts and salts with bases. Salts include those with physiologically active bases, e.g. theophylline, theobromine, caffeine, antihistamine bases, nicotinamide, nicotinic acid hydrazide, adrenalin, ephedrine, and choline, and also with sodium, potassium and calcium. The antibiotic is produced by aerobic submerged cultivation of the new microorganism, Streptomyces armentosus var. armentosus, NRRL.3176, in aqueous nutrient medium containing sources of assimilable carbon and nitrogen. H may be isolated from the fermentation broth by, e.g. solvent extraction, liquidliquid distribution, adsorption on ion-exchange resins or surface-active agents, and purified by crystallization from mixed solvents.

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