"> N-(3-(1'-3
    1.
    发明授权
    N-(3-(1'-3"-Oxapentamethyleneamino-ethylideneamino)-2,4,6-triio dobenzoyl)-.beta.-amino-.alpha.-methylpropionitrile 失效
    N-(3-(1'-3“ - 亚氧杂亚氨基 - 亚乙基氨基)-2,4,6-三碘苯甲酰基)-β-氨基-α-甲基丙腈

    公开(公告)号:US4308383A

    公开(公告)日:1981-12-29

    申请号:US218741

    申请日:1980-12-22

    CPC分类号: C07D295/195 C07C255/00

    摘要: The present invention relates to the novel compound N-[3-(1'-3"-Oxapentamethyleneamino-ethylideneamino)-2,4,6-triiodobenzoyl]-.beta.-amino-.alpha.-methylpropionitrile which due to the sparing solubility in water, can be purified readily in a simple manner and can be used for the preparation of the known active compound for agents for peroral rapid cholecystography N-[3-(1'-3"-oxapentamethyleneamino-ethylideneamino)-2,4,6-triiodobenzoyl]-.beta.-amino-.alpha.-methyl propionic acid.

    摘要翻译: 本发明涉及新型化合物N- [3-(1'-3“ - 亚氧杂亚戊基氨基 - 亚乙基氨基)-2,4,6-三碘苯甲酰基]-β-氨基-α-甲基丙腈,其由于在 水可以以简单的方式容易地纯化,并且可以用于制备用于口腔快速胆囊造影剂N- [3-(1'-3“ - 氧杂亚戊基亚氨基 - 亚乙基氨基)-2,4, 6-三碘苯甲酰基]-β-氨基-α-甲基丙酸。

    "> N-[3-(1'-3
    2.
    发明授权
    N-[3-(1'-3"-O xapentamethylene-amino-ethylideneamino)-2,4,6-triiodobenzoyl]-.beta.-amin o-.alpha.- methylpropionitrile in process to make corresponding acid 失效
    N- [3-(1'-3“ - 亚氧杂亚麻基 - 氨基 - 亚乙基氨基)-2,4,6-三碘苯甲酰基]-β-氨基-α-甲基丙腈在制备相应的酸

    公开(公告)号:US4375543A

    公开(公告)日:1983-03-01

    申请号:US288200

    申请日:1981-07-29

    CPC分类号: C07D295/195 C07C255/00

    摘要: The present invention relates to the novel compound N-[3-(1'-3"-Oxapentamethyleneamino-ethylideneamino)-2,4,6-triiodobenzoyl]-.beta.-amino-.alpha.methylpropionitrile which due to the sparing solubility in water, can be purified readily in a simple manner and can be used for the preparation of the known active compound for agents for peroral rapid cholecystography N-[3-(1'-3"-oxapentamethyleneamino-ethylideneamino)-2,4,6-triiodobenzoyl]-.beta.-amino-.alpha.-methyl propionic acid.

    摘要翻译: 本发明涉及新型化合物N- [3-(1'-3“ - 亚氧杂亚戊基氨基 - 亚乙基氨基)-2,4,6-三碘苯甲酰基]-β-氨基-α甲基丙腈,其由于在水中的保留溶解度 可以以简单的方式容易地纯化,并且可以用于制备用于口腔快速胆囊造影剂的已知活性化合物N- [3-(1'-3“ - 氧杂亚戊基亚氨基 - 亚乙基氨基)-2,4,6 三碘苯甲酰基]-β-氨基-α-甲基丙酸。

    Crystalline forms of tigecycline hydrochloride
    5.
    发明授权
    Crystalline forms of tigecycline hydrochloride 有权
    盐酸替加环素的结晶形式

    公开(公告)号:US08252946B2

    公开(公告)日:2012-08-28

    申请号:US12742706

    申请日:2008-11-12

    IPC分类号: C07C237/26

    摘要: The present invention relates to crystalline forms A and B of Tigecycline hydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline forms A and B of Tigecycline hydrochloride as intermediates for the formulation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form A of Tigecycline hydrochloride in an effective amount and to the use of crystalline form A of Tigecycline hydrochloride as anti-infective medicament.

    摘要翻译: 本发明涉及盐酸替加环素的结晶形式A和B及其制备方法。 此外,本发明涉及盐酸替加环素的结晶形式A和B在制备抗感染药物中的用途。 此外,本发明涉及包含有效量的盐酸替加环素的结晶形式A和使用盐酸替加环素的结晶形式A作为抗感染药物的药物组合物。

    CRYSTALLINE FORM C OF TIGECYCLINE DIHYDROCHLORIDE AND METHODS FOR ITS PREPARATION
    6.
    发明申请
    CRYSTALLINE FORM C OF TIGECYCLINE DIHYDROCHLORIDE AND METHODS FOR ITS PREPARATION 有权
    二乙基二氯化锆的结晶形式及其制备方法

    公开(公告)号:US20120022025A1

    公开(公告)日:2012-01-26

    申请号:US13133164

    申请日:2009-12-18

    CPC分类号: C07C237/26 C07C2603/46

    摘要: The present invention relates to crystalline form C of Tigecycline dihydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline form C of Tigecycline dihydrochloride as an intermediate for the preparation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form C of Tigecycline dihydrochloride in an effective amount and to the use of crystalline form C of Tigecycline dihydrochloride as an anti-infective medicament.

    摘要翻译: 本发明涉及替加环素二盐酸盐的结晶形式C及其制备方法。 此外,本发明涉及替加环素二盐酸盐的结晶形式C作为制备抗感染药物的中间体的用途。 此外,本发明涉及有效量的包含替加环素二盐酸盐的结晶形式C的药物组合物和使用替加环素二盐酸盐的结晶形式C作为抗感染药物。

    CRYSTALLINE FORM OF AN ORGANIC COMPOUND
    7.
    发明申请
    CRYSTALLINE FORM OF AN ORGANIC COMPOUND 有权
    有机化合物的结晶形式

    公开(公告)号:US20110306764A1

    公开(公告)日:2011-12-15

    申请号:US13139863

    申请日:2009-12-18

    IPC分类号: C07D239/545

    CPC分类号: C07D401/04

    摘要: The present invention is directed to a crystalline form of 2-[6-[3(R)-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]-benzonitrile, a process for the preparation of said crystalline form and the use thereof in the manufacture of a pharmaceutical composition.

    摘要翻译: 本发明涉及2- [6- [3(R) - 氨基哌啶-1-基] -3-甲基-2,4-二氧代-1,2,3,4-四氢嘧啶-1-基 甲基] - 苄腈,制备所述结晶形式的方法及其在制备药物组合物中的用途。

    Process for the production of 3-vinyl cephalosporins
    9.
    发明授权
    Process for the production of 3-vinyl cephalosporins 失效
    生产3-乙烯基头孢菌素的方法

    公开(公告)号:US06414140B2

    公开(公告)日:2002-07-02

    申请号:US09792800

    申请日:2001-02-23

    IPC分类号: C07D50122

    CPC分类号: C07D501/00

    摘要: A process for the production of a 3-vinylcephalosporin compound of formula I wherein R1 and R2 denote hydrogen or an organic group by a Wittig reaction reacting first a compound of formula II with a compound of formula P(R4)3 or P(OR4)3 to produce a compound of formula III and secondly reacting the compound of formula III with a weak base of formula or of formula R10—COO−W+ wherein R5 is hydrogen, alkly or aryl and R6 and R7 are each an activated group of formula —COOR8, —CN, —SO2R8, —COR8 or —CON(R8)2; or R5 and R8 are each aryl and R7 is an activated group of formula —COOR8, —CN, —SO2R8, —COR8 or —CON(R8)2, W+ is an alkali metal cation and R10 is alkyl or aryl to produce a compound of formula IV and finally reacting a compound of formula IV with a compound of formula V to produce a compound of formula I.

    摘要翻译: 制备式I的3-乙酰头孢菌素化合物的方法,其中R1和R2通过维蒂希反应表示氢或有机基团,首先将式II化合物与式P(R4)3或P(OR4)3的化合物反应至 制备式III化合物,其次使式III化合物与式R 10 -COO-W +的弱碱反应,其中R 5是氢,烷基或芳基,R 6和R 7各自是式-COOR 8,-CN的活化基团 ,-SO 2 R 8,-COR 8或-CON(R 8)2; 或R 5和R 8各自为芳基,R 7为式-COOR 8,-CN,-SO 2 R 8,-COR 8或-CON(R 8)2的活化基团,W +为碱金属阳离子,R 10为烷基或芳基, 然后最终使式Ⅳ化合物与式Ⅴ化合物反应,生成式Ⅰ化合物。

    Cephalosporin synthesis
    10.
    发明授权
    Cephalosporin synthesis 失效
    头孢菌素合成

    公开(公告)号:US6063917A

    公开(公告)日:2000-05-16

    申请号:US164055

    申请日:1998-09-30

    摘要: A process for the production of a compound of formula ##STR1## wherein R.sup.a denotes hydrogen or silyl;R.sup.b denotes a group of formula --OR.sup.e, whereinR.sup.e denotes hydrogen or alkyl; andR.sup.c and R.sup.d together denote a bond;in free form or in salt form,which process comprises the step of spitting, in the presence of ozone, the double bond in position 3 of the ring structure of a compound of formula III ##STR2## wherein R.sub.2 and R.sub.3 are the same or different and independently of each other denote hydrogen or an organic group, and X.sup.- denotes the anion of an inorganic or organic acid and optionally silylating the amine group in position 7 of the ring system.

    摘要翻译: 制备下式化合物的方法其中R a表示氢或甲硅烷基; Rb表示式-OR的基团,其中Re表示氢或烷基; Rc和Rd一起表示键; 游离形式或盐形式,该方法包括在臭氧存在下吐出式III化合物的环结构位置3上的双键的步骤,其中R2和R3相同或不同并且独立地 彼此表示氢或有机基团,X表示无机或有机酸的阴离子,并且任选地使环系的位置7中的胺基甲硅烷基化。