NOVEL SYNTHETIC METHODS FOR NON-IONIC RADIOGRAPHIC CONTRAST MEDIA
    2.
    发明申请
    NOVEL SYNTHETIC METHODS FOR NON-IONIC RADIOGRAPHIC CONTRAST MEDIA 审中-公开
    非离子放射对比介质的新型合成方法

    公开(公告)号:WO1985001727A1

    公开(公告)日:1985-04-25

    申请号:PCT/US1984001657

    申请日:1984-10-12

    CPC classification number: A61K49/04 C07C233/00 Y02P20/55

    Abstract: Methods for substituting aromatic carboxylic acids and derivatives thereof and amino substituted aromatic carboxylic acids and derivatives thereof, by forming imides and imide-amides, respectively, by acylation with aliphatic carboxylic acids, substituting at least one nitrogen atom under mild basic conditions with an aliphatic compound having as alkylating agent a displaceable functionality and removing undesired acyl group, as appropriate.

    Abstract translation: 通过分别通过用脂族羧酸酰化形成酰亚胺和酰亚胺,在温和的碱性条件下用脂族化合物代替至少一个氮原子来代替芳族羧酸及其衍生物和氨基取代的芳族羧酸及其衍生物的方法 作为烷基化剂具有可置换的官能团,并酌情除去不需要的酰基。

    A PROCESS FOR THE PREPARATION OF N,N'-DIACETYLETHYLENE DIAMINE
    3.
    发明申请
    A PROCESS FOR THE PREPARATION OF N,N'-DIACETYLETHYLENE DIAMINE 审中-公开
    一种制备N,N'-二乙基乙烯二胺的方法

    公开(公告)号:WO1988005041A1

    公开(公告)日:1988-07-14

    申请号:PCT/DK1988000003

    申请日:1988-01-11

    Inventor: A/S CHEMINOVA

    CPC classification number: C07C233/00

    Abstract: In a process for preparing N,N'-diacetylethylene diamine by mixing ethylene diamine with the stoichiometric amount of acetic acid, a greater or smaller part of which may be aqueous, and distilling off any water originating from the use of aqueous acetic acid, and then dehydrating the ethylene diamine diacetate salt at a temperature of from 140 DEG C to 150 DEG C while using an auxiliary agent for distilling off water, as said auxiliary agent use is made of an organic solvent forming with water an azeotropic mixture having a boiling point preferably lying between 80 DEG C and 200 DEG C.

    Abstract translation: 在通过将乙二胺与化学计量的乙酸混合制备N,N'-二乙烯基乙二胺的方法中,其中大部分或更少部分可以是含水的,并且蒸馏出任何使用乙酸水溶液的水,以及 然后在140℃至150℃的温度下使乙二胺二乙酸盐脱水,同时使用蒸馏水的辅助剂,因为所述助剂使用由水形成的有机溶剂,具有沸点的共沸混合物 优选在80℃和200℃之间。

    NON-IONIC POLYOL CONTRAST MEDIA FROM IONIC CONTRAST MEDIA
    4.
    发明申请
    NON-IONIC POLYOL CONTRAST MEDIA FROM IONIC CONTRAST MEDIA 审中-公开
    离子对比介质的非离子聚对苯二甲酸乙二醇酯介质

    公开(公告)号:WO1987000757A1

    公开(公告)日:1987-02-12

    申请号:PCT/US1986001590

    申请日:1986-08-01

    CPC classification number: C07C233/00 A61K49/04 C07C233/16

    Abstract: Novel non-ionic contrast media are efficiently prepared from generally available ionic contrast media or non-iodinated precursors. Particularly, polyhydroxyhalo-hydrocarbons are employed with a triiodo-substituted acylamido benzoic acids in aqueous weakly basic media to selectively substitute the amido nitrogen, followed by activation of the carboxyl group for amide formation.

    Abstract translation: 新型非离子造影剂可从一般可获得的离子造影剂或非碘化前体有效制备。 特别地,多羟基卤代烃与三碘取代的酰基酰氨基苯甲酸在弱碱性介质中选择性地取代酰氨基氮,然后活化羧基以形成酰胺。

    PREPARATION OF 5-ACYLAMINO-2,4,6-TRIIODO- OR TRIBROMO-BENZOIC ACID DERIVATIVES
    6.
    发明申请
    PREPARATION OF 5-ACYLAMINO-2,4,6-TRIIODO- OR TRIBROMO-BENZOIC ACID DERIVATIVES 审中-公开
    5-亚氨基-2,4,6-三异丙基或三溴代苯甲酸衍生物的制备

    公开(公告)号:WO1988009328A1

    公开(公告)日:1988-12-01

    申请号:PCT/EP1988000453

    申请日:1988-05-20

    CPC classification number: C07C233/00 A61K49/04 C07C233/12

    Abstract: A process for the preparation of 5-acylamino-2,4,6-triiodo or tribromo-benzoic acid derivatives of formula (I), wherein X is I or Br, R is H or a variously substituted alkyl, or a group of formula (II), wherein X has the above meanings; Y is hydroxy, alkoxy, hydroxyalkoxy, alkylamino or hydroxyalkylamino; Z may be the same as COY or it is hydroxyalkylaminocarbonyl provided that at least one of the two acyl or R groups is hydroxy-substituted, which process comprises the rearrangement of the corresponding 5-(alkylaminocarbonyl-alkoxy)-2,4,6-triiodo or tribromo-benzoic acid derivatives, in the presence of bases.

    Abstract translation: 制备式(I)的5-酰基氨基-2,4,6-三碘代或三溴 - 苯甲酸衍生物的方法,其中X是I或Br,R是H或各种取代的烷基或式 (II),其中X具有上述含义; Y是羟基,烷氧基,羟基烷氧基,烷基氨基或羟烷基氨基; Z可以与COY相同,或者它是羟基烷基氨基羰基,条件是两个酰基或R基团中的至少一个是羟基取代的,该方法包括相应的5-(烷基氨基羰基 - 烷氧基)-2,4,6- 三碘或三溴 - 苯甲酸衍生物,在碱的存在下。

    ORALLY EFFECTIVE ION CHELATORS RELATED TO DEFEROXAMINE
    7.
    发明申请
    ORALLY EFFECTIVE ION CHELATORS RELATED TO DEFEROXAMINE 审中-公开
    与DEFEROXAMINE相关的ORALLY有效离子注射器

    公开(公告)号:WO1985003290A1

    公开(公告)日:1985-08-01

    申请号:PCT/US1985000104

    申请日:1985-01-24

    Applicant: ORAL-D

    CPC classification number: A61K31/295 C07C233/00

    Abstract: Compounds of general formula (I), wherein: R1 is acyl of the formula -C(=O)-R5; R2, R3, R4, R6, R7 and R8 are each selected from the group consisting of hydrogen and acyl of the formula: -C(=O)-R5, wherein R5 is selected from the group consisting of alkyls, substituted alkyls, alkenyls, substituted alkenyls, cycloalkyls, substituted cycloalkyls, arylalkylenes, substituted arylalkylenes, alkylenecycloalkyls, alkylene substituted cycloalkyls, alkynyls, substituted alkynyls, aryls and substituted aryls, wherein R2, R3 and R4 are selected such that at least one of R2, R3 and R4 is an acyl. When R2, R3 and R4 include one or more acyls that are not identical to the acyl of R1, these compounds of formula (I) are novel compounds. The invention also includes processes to produce the compounds of formula (I). Compounds of formula (I) complex and/or chelate tissue tri-valent ions, especially iron and aluminum (Fe+++, Al+++), when administered to a human being, and are therefore useful in therapy in the treatment of diseases in which tissue ion levels in the body have increased or toxic levels. These iron-related diseases include, for example, thalassemia major, sideroachrestic anemic, Blackfan-Diamond anemia, aplastic anemia, sickle cell anemia, hemolytic anemias and hemosiderosis brought about by multiple blood transfusions including treatment for the anemia accompanying conditions requiring kidney dialysis. Aluminum-related diseases or conditions include Alzheimer's disease, senile dementia and dialysis encephalopathy.

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