公开(公告)号：WO9628420A3

公开(公告)日：1996-12-12

申请号：PCT/GB9600552

申请日：1996-03-08

Applicant: NYCOMED SALUTAR INC ,  UNIV IOWA RES FOUND ,  COCKBAIN JULIAN ,  MESSERLE LOUIS ,  AMARASINGHE GANDARA ,  FELLMANN JERE DOUGLAS ,  GARRITY MARTHA ,  VARADARAJAN JOHN ,  VASILEVSKIS JANIS

Inventor： MESSERLE LOUIS ,  AMARASINGHE GANDARA ,  FELLMANN JERE DOUGLAS ,  GARRITY MARTHA ,  VARADARAJAN JOHN ,  VASILEVSKIS JANIS

IPC: A61K49/00 ,  A61K49/06 ,  C07C303/44 ,  C07C305/06 ,  C07D203/08 ,  C07D255/00 ,  C07D257/02 ,  C07D259/00 ,  C07C305/04

CPC classification number: C07D203/08 ,  A61K49/0002 ,  A61K49/06 ,  C07C303/44 ,  C07D255/00 ,  C07D257/02 ,  C07D259/00 ,  C07C305/06

Abstract: Aziridines may be subjected to a cyclooligomerization reaction to produce polyazacycloalkane compounds useful for example in the preparation of chelating agents for use in diagnostic imaging contrast agents. N-benzyl-aziridine in particular is useful as it can be cyclotetramerized and debenzylated to yield cyclen, a key intermediate in chelating agent preparation. The invention provides a particularly attractive route to production of N-benzyl and other N-arylmethyl aziridines of formula (I), (where each R1 independently is hydrogen or a group Ar and Ar is an optionally substituted phenyl group), said process comprising reacting a purified N-arylmethylethanolamine-sulphonate ester with a base. N-arylmethyl-ethanolamine sulphonate ester of the formula: R'NHCH2CH2OSO3H, wherein the N-arylmethyl group R' is an N-(bisarylmethyl) or N-(triarylmethyl) group, as intermediates. In a further aspect the invention provides compounds of formula (II), where Ar and R1 are as hereinbefore defined and at least two differing ArCHR1 moieties are present.

Abstract translation: 氮杂环丁烷可以被喷射到环烯化反应中以产生用于例如制备用于诊断成像造影剂的螯合剂的多氮杂环烷烃化合物。 特别是N-苄基 - 氮丙啶是有用的，因为它可以进行环化聚合和脱苄基化，以产生螯合剂，螯合剂制备中的关键中间体。 本发明提供了生产式（I）的N-苄基和其它N-芳基甲基氮丙啶的特别有吸引力的途径，其中每个R 1独立地为氢或基团AR，Ar为任选取代的苯基。 该方法包括使纯化的N-芳基甲基乙醇胺 - 磺酸酯磺酸酯与碱反应。 作为中间体，式R'NHCH2CH2OSO3H的N-芳基甲基 - 乙醇胺磺酸酯，其中N-芳基甲基R'是N-（二芳基甲基）或N-（三芳基甲基）基团。 在另一方面，本发明提供式（II）的化合物，其中Ar和R 1如上所定义，并且存在至少两个不同的ArCHR 21部分。

公开(公告)号：WO0206287A9

公开(公告)日：2002-07-18

申请号：PCT/US0122491

申请日：2001-07-17

Applicant: CALIFORNIA INST OF TECHN ,  HUBIN TIMOTHY J ,  MEADE THOMAS J

Inventor： HUBIN TIMOTHY J ,  MEADE THOMAS J

IPC: A61K49/10 ,  C07D487/08 ,  A61K49/06 ,  C07D255/00

CPC classification number: C07D487/08 ,  A61K49/106

Abstract: The invention relates to novel magnetic resonance imaging contrast agents.

Abstract translation: 本发明涉及新型磁共振成像造影剂。

公开(公告)号：WO2021043260A1

公开(公告)日：2021-03-11

申请号：PCT/CN2020/113474

申请日：2020-09-04

Applicant: 湖北生物医药产业技术研究院有限公司 ,  人福医药集团股份公司

Inventor： 张学军 ,  李莉娥 ,  沈洁 ,  魏文军 ,  雷四军 ,  丁肖华 ,  臧杨 ,  孙红娜 ,  付强强

IPC: C07D255/00 ,  C07D255/02 ,  C07D401/02 ,  C07D401/12 ,  C07D403/12 ,  A61K31/506 ,  A61P35/00 ,  A61P19/02

Abstract: 嘧啶类化合物，更具体地，涉及嘧啶类化合物及其制备方法，以及其在制备药物中的用途。提供一种式(I)所示化合物，或者式(I)所示化合物的互变异构体、立体异构体、水合物、溶剂化物、药学可接受的盐或前药。该化合物对ATX酶有明显的抑制作用，且表现出优良的肝代谢稳定性，在人体内代谢更慢，暴露量更高。

公开(公告)号：WO2019118313A1

公开(公告)日：2019-06-20

申请号：PCT/US2018/064649

申请日：2018-12-10

Applicant: MERCK SHARP & DOHME CORP. ,  ALI, Amjad ,  LIM, Yeon-Hee ,  GALLO-ETIENNE, Gioconda, V. ,  KELLY, Joseph, Michael ,  BERLIN, Michael ,  TING, Pauline ,  TAGAT, Jayaram, R. ,  XIAO, Dong ,  KUANG, Rongze ,  WU, Heping ,  WANG, Hongwu

Inventor： ALI, Amjad ,  LIM, Yeon-Hee ,  GALLO-ETIENNE, Gioconda, V. ,  KELLY, Joseph, Michael ,  BERLIN, Michael ,  TING, Pauline ,  TAGAT, Jayaram, R. ,  XIAO, Dong ,  KUANG, Rongze ,  WU, Heping ,  WANG, Hongwu

IPC: A61K31/4188 ,  A61K31/505 ,  A61K31/519 ,  C07D247/00 ,  C07D247/02 ,  C07D255/00

Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: "Z" and R1 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：WO2022037650A1

公开(公告)日：2022-02-24

申请号：PCT/CN2021/113538

申请日：2021-08-19

Applicant: BEIJING INNOCARE PHARMA TECH CO., LTD.

Inventor： CHEN, Xiangyang ,  PANG, Yucheng

IPC: C07D253/00 ,  C07D255/00 ,  C07D487/04 ,  A61P19/08 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00 ,  A61K31/41 ,  A61K31/53

Abstract: Provided herein are bridged bicyclic Compounds A and B or their pharmaceutically acceptable salts, which are as inhibitors of Bruton's tyrosine kinase (BTK) and its C481 mutant. Also provided are methods for preparing Compounds A and B or their pharmaceutically acceptable salts thereof. Compounds A and B can be used to treat and/or prevent related diseases mediated by BTK or its C481 mutant, especially cancer and autoimmune diseases.

公开(公告)号：WO2021226161A1

公开(公告)日：2021-11-11

申请号：PCT/US2021/030766

申请日：2021-05-05

Applicant: BIOHAVEN THERAPEUTICS LTD.

Inventor： PENDRI, Yadagiri R. ,  KATHAM, Srinivasa ,  MENDE, Sreenivas ,  KEDAS, Chendrasekhar ,  KANDIYALA, Srinivasa ,  CHILAKALA, Dhanaraj

IPC: A61K31/513 ,  A61K31/519 ,  A61P25/28 ,  C07D239/70 ,  C07D239/95 ,  C07D255/00

Abstract: An improved process for preparing verdiperstat is disclosed. The process includes the steps of reacting a compound having formula or a salt thereof, wherein R is the same or different and is each independently a C1-C5 alkyl with 3-(dimethylamino)acrylonitrile to obtain a compound having formula; and converting the compound having formula to verdiperstat.

公开(公告)号：WO2008123779A1

公开(公告)日：2008-10-16

申请号：PCT/NO2008/000122

申请日：2008-04-03

Applicant: GE HEALTHCARE AS ,  MORISSON-IVESON, Véronique

Inventor： MORISSON-IVESON, Véronique

IPC: C07D239/04 ,  C07D255/00 ,  A61K49/04

CPC classification number: C07D239/04 ,  A61K49/04 ,  C07D255/00

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing a saturated triaza cyclic central moiety containing carbonyl functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract translation: 本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。 更具体地说，含碘化合物是含有含有羰基官能团的饱和三氮杂环状中心部分的化合物，其允许与其结合的三个碘化苯基的排列。 本发明还涉及这种诊断组合物作为造影剂在诊断成像中的用途，特别是在X射线成像中以及含有这种化合物的造影剂的用途。

公开(公告)号：WO99057104A1

公开(公告)日：1999-11-11

申请号：PCT/US1999/009167

申请日：1999-04-27

IPC: C06B25/34 ,  C07D487/02 ,  C07D255/00 ,  C07D487/00

CPC classification number: C07D487/02 ,  C06B25/34

Abstract: Processes and compositions for nitration of N-substituted isowurtzitane compounds with concentrated nitric acid at elevated temperatures to form HNIW and recovery thereof with high yields and purities. Polymorphic conversions to the epsilon HNIW crystalform at quantitative yields are also described.

Abstract translation: 在高温下用浓硝酸硝化N-取代的异烟酸烷基酯化合物以形成HNIW并以高产率和纯度回收的方法和组合物。 还描述了以定量产率向εHNIW晶体形式的多晶型转化。