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    SULFUR (VI) FLUORIDE COMPOUNDS AND THEIR USE IN CLICK-REACTION
    73.
    发明公开
    SULFUR (VI) FLUORIDE COMPOUNDS AND THEIR USE IN CLICK-REACTION 审中-实审

    公开(公告)号：EP4295841A3

    公开(公告)日：2024-03-13

    申请号：EP23191114.0

    申请日：2015-06-05

    Applicant: The Scripps Research Institute

    Inventor： DONG, Jiajia ,  SHARPLESS, K. Barry ,  KELLY, Jeffery W. ,  BARANCZAK, Aleksandra ,  CHEN, Wentao

    IPC: C07C201/00 ,  A61K31/10 ,  A61K31/16 ,  C07K1/00

    Abstract: This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X 1 is a covalent bond or -CH 2 CH 2 -, X 2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

    MANUFACTURING PROCESS FOR NO-DONATING COMPOUNDS SUCH AS NO-DONATING DICLOFENAC
    75.
    发明公开
    MANUFACTURING PROCESS FOR NO-DONATING COMPOUNDS SUCH AS NO-DONATING DICLOFENAC 审中-公开
    用于免疫化合物的制造方法，如免疫供体双氯芬酸

    公开(公告)号：EP1558559A1

    公开(公告)日：2005-08-03

    申请号：EP03797782.4

    申请日：2003-09-18

    Applicant: NicOx S.A.

    Inventor： ANDERSSON, Johan ,  BELLI, Aldo ,  CANNATA, Vincenzo ,  HEDBERG, Martin ,  PALMGREN, Andreas ,  SCHULDEI, Sigrid ,  STRÖM, Marika ,  VILLA, Marco

    IPC: C07C201/00 ,  C07C309/63 ,  A61K31/216 ,  A61P29/00 ,  C07C211/55

    CPC classification number: C07C303/28 ,  A61K31/216 ,  C07C67/08 ,  C07C201/02 ,  C07C203/04 ,  C07C227/16 ,  C07C227/20 ,  C07C229/42 ,  C07C309/66 ,  C07C69/738

    Abstract: The present invention relates to a new process for the preparation of NO-donating compounds using a sulfonated intermediate. The invention relates to new intermediates prepared therein suitable for large scale manufacturing of NO-donating compounds. The invention further relates to the use of the new intermediates for the manufacturing of pharmaceutically active NO-donating compounds.The invention further relates to a substantially crystalline form of NO-donating NSAIDs, especially 2-[2-(nitrooxy)ethoxy]ethyl {2-[(2,6-dichlorophenyl)amino]phenyl}acetate, the preparation thereof and to pharmaceutical formulations containing said crystalline form and to the use of said crystalline form in the preparation of a medicament.

    Abstract translation: 本发明涉及使用磺化中间体制备NO供体化合物的新方法。 本发明涉及适用于大规模生产NO供体化合物的新中间体。 本发明进一步涉及该新中间体在制备药学活性NO供体化合物中的用途。本发明还涉及NO供体非甾体抗炎药的基本结晶形式，尤其是2- [2-（硝基氧基）乙氧基]乙基{ 2 - [（2,6-二氯苯基）氨基]苯基}乙酸乙酯，其制备方法和含有所述结晶形式的药物制剂以及所述结晶形式在制备药物中的用途。

    A PROCESS FOR THE PREPARATION OF CYCLOBUTENE-SUBSTITUTED AROMATIC HYDROCARBONS.
    79.
    发明公开
    A PROCESS FOR THE PREPARATION OF CYCLOBUTENE-SUBSTITUTED AROMATIC HYDROCARBONS. 失效
    VERFAHREN ZUR HERSTELLUNG ZYKLOBUTENSUBSTITUIERTER AROMATISCHER KOHLENWASSERSTOFFE。

    公开(公告)号：EP0182872A4

    公开(公告)日：1986-08-21

    申请号：EP85902848

    申请日：1985-05-20

    Applicant: DOW CHEMICAL CO

    Inventor： SO YING-HUNG

    IPC: C07C43/21 ,  C07B31/00 ,  C07B37/10 ,  C07C1/00 ,  C07C1/26 ,  C07C13/44 ,  C07C17/00 ,  C07C17/25 ,  C07C25/18 ,  C07C27/00 ,  C07C37/00 ,  C07C39/17 ,  C07C41/00 ,  C07C41/24 ,  C07C51/00 ,  C07C51/347 ,  C07C63/34 ,  C07C67/00 ,  C07C67/28 ,  C07C67/30 ,  C07C69/035 ,  C07C69/76 ,  C07C201/00 ,  C07C231/00 ,  C07C231/12 ,  C07C233/65 ,  C07C253/00 ,  C07C51/09

    CPC classification number: C07C69/76

    Abstract: Process for the preparation of an aromatic hydrocarbon with a cyclobutene ring fused to the aromatic hydrocarbon which comprises, dissolving an ortho-alkyl halomethyl aromatic hydrocarbon in an inert solvent and pyrolyzing the solution of ortho-alkyl halomethyl aromatic hydrocarbon in the inert solvent under conditions such that the ortho-alkyl and the halomethyl substituents form a cyclobutene ring thereby forming an aromatic hydrocarbon having a fused cyclobutene ring. The ortho-alkyl group has the structural formula (R')2-CH-, wherein R' is separately in each occurance hydrogen or a C1-20 alkyl. The aromatic hydrocarbons with a cyclobutene ring fused to the aromatic hydrocarbon are useful in the preparation of monomers, which are then useful in the preparation of high performance polymers.

    Abstract translation: 制备具有与芳族烃稠合的环丁烯环的芳烃的方法，包括将邻烷基卤代甲基芳烃溶解在惰性溶剂中，并在惰性溶剂中将邻烷基卤甲基芳烃的溶液在惰性溶剂中热解 邻位烷基和卤代甲基取代基形成环丁烯环，从而形成具有稠合的环丁烯环的芳烃。 邻烷基具有结构式（R'）2 -CH-，其中R'分别在每个出现的氢或C1-20烷基中。 具有与芳族烃稠合的环丁烯环的芳族烃可用于制备单体，其然后可用于制备高性能聚合物。

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