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1. 发明申请

WO2016034126A1 ANTI-TUMOR COMPOUND AND MEDICAL USE THEREOF 审中-公开
标题翻译：抗肿瘤化合物及其医疗用途
公开(公告)号：WO2016034126A1
公开(公告)日：2016-03-10
申请号：PCT/CN2015/088842
申请日：2015-09-02
申请人： TIANJIN CANCER INSTITUTE
发明人： ZHANG, Ning , WANG, Yinsong , ZHOU, Ping , GUO, Hua , LUO, Yi , HAO, Xishan , GENG, Hua
IPC分类号： C07C233/87 , C07C231/02 , C07C69/78 , C07C65/03 , C07C63/06 , A61K31/24 , A61K31/198 , A61K31/192 , A61P35/04 , A61P35/00
CPC分类号： A61K31/337 , A61K31/192 , A61K45/06 , A61K2300/00 , C07C205/59 , C07C229/60 , C07C231/00 , C07C233/87
摘要： A compound of formula (I) is disclosed, which has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro , and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc.
摘要翻译：公开了具有低毒性的式（I）化合物，可以显着抑制体外肿瘤细胞的迁移和侵袭，并且可以在低浓度的小鼠体内抑制肿瘤转移，同时对细胞毒性抗体显示显着的敏化作用肿瘤药如紫杉醇等

2. 发明申请

WO2015111085A8 PROCESSES FOR THE PREPARATION OF ELTROMBOPAG AND PHARMACEUTICALLY ACCEPTABLE SALTS, SOLVATES AND INTERMEDIATES THEREOF 审中-公开
公开(公告)号：WO2015111085A8
公开(公告)日：2015-09-03
申请号：PCT/IN2015000052
申请日：2015-01-27
申请人： CADILA HEALTHCARE LTD
发明人： DESAI SANJAY JAGDISH , DWIVEDI SHRI PRAKASH DHAR , PARIHAR JAYPRAKASH AJITSINGH , RUPAPARA MAHESH LALJIBHAI , KESHAVALA DHARMENDRA MOHANBHAI
CPC分类号： C07D231/46 , C07C201/08 , C07C201/12 , C07C227/04 , C07C205/26 , C07C205/37 , C07C205/59 , C07C229/52
摘要： The present invention provides the processes for the preparation of eltrombopag of Formula (I) or its pharmaceutically acceptable salts. The invention also provides crystalline forms of eltrombopag.

3. 发明申请

WO2014177517A1 PREPARATION PROCESS OF AN AGONIST OF THE THROMBOPOIETIN RECEPTOR 审中-公开
标题翻译：血小板生成素受体激动剂的制备方法
公开(公告)号：WO2014177517A1
公开(公告)日：2014-11-06
申请号：PCT/EP2014/058610
申请日：2014-04-28
申请人： ESTEVE QUÍMICA, S.A. , GALCHIMIA, S.A.
发明人： BARTRA SANMARTÍ, Martí , SOLSONA ROCABERT, Joan Gabriel , CRUCES COLADO, Jacobo , ENJO BABIO, Juan , PAMPÍN CASAL, María Begoña
IPC分类号： C07C205/59 , C07C201/12 , C07D231/22 , C07C227/04 , C07C249/16
CPC分类号： C07C201/12 , C07C205/59 , C07C227/04 , C07C249/16 , C07D231/22 , C07C229/70 , C07C251/76
摘要： It relates to a preparation process of 2'-(benzyloxy)-3'-nitro-1,1'-biphenyl-3- carboxylic acid or a salt thereof comprising reacting 2-(benzyloxy)-1-bromo- 3-nitrobenzene with a either 3-carboxyphenylboronic acid or a salt thereof or a (C 1 -C 4 )-alkyl ester thereof in the presence of Pd(OAc) 2 , tricydohexylphosphine, a base, an appropriate solvent, and at an appropriate temperature; if appropriate, submitting the compound thus obtained to a hydrolysis reaction; and isolating the compound thus obtained in form of a salt of compound of formula (VI) or in form of the free acid by adding an acid. It also comprises the further preparation to eltrombopag or its salts from the new intermediate thus obtained by subsequent reduction of the nitro group and deprotection of the phenol, conversion of the amine intermediate obtained in a diazonium derivative, and either (1) subsequent reaction with ethyl acetoacetate and with (3,4-dimethylphenyl)hydrazine or a salt thereof, occurring the pyrazole ring formation by intermolecular cyclization, or (2) introduction of the pyrazole ring by reaction with 1-(3,4-dimethylphenyl)-3-methyl-3-pyrazolin-5-one.
摘要翻译：本发明涉及2' - （苄氧基）-3'-硝基-1,1'-联苯-3-甲酸或其盐的制备方法，其包括使2-（苄氧基）-1-溴-3-硝基苯与在Pd（OAc）2，三羟基己基膦，碱，适当的溶剂和适当的温度存在下，3-羧基苯基硼酸或其盐或其（C 1 -C 4） - 烷基酯; 如果合适，将由此获得的化合物提交至水解反应; 并通过添加酸分离由式（VI）化合物的盐形成的化合物或游离酸形式的化合物。它还包括通过随后还原硝基和脱保护苯酚得到的新中间体进一步制备埃曲波帕或其盐，以及在重氮衍生物中获得的胺中间体的转化，以及（1）随后的反应与乙基乙酰乙酸酯和（3,4-二甲基苯基）肼或其盐，通过分子间环化形成吡唑环，或（2）通过与1-（3,4-二甲基苯基）-3-甲基 -3-吡唑啉-5-酮。

4. 发明申请

WO2004096750A1 ３－ニトロ－４－アルコキシ安息香酸の製造方法审中-公开
标题翻译：生产3-硝基-4-羟基苯甲酸的方法
公开(公告)号：WO2004096750A1
公开(公告)日：2004-11-11
申请号：PCT/JP2004/006055
申请日：2004-04-27
申请人：株式会社上野製薬応用研究所 , 上野隆三 , 北山雅也 , 若森浩之
发明人：上野隆三 , 北山雅也 , 若森浩之
IPC分类号： C07C201/08
CPC分类号： C07C201/08 , C07C205/59
摘要：　４−アルコキシ安息香酸および４−アルコキシ安息香酸に対して８重量倍以上の濃度４０～８０％の硝酸を含む混合物を、３０～１００℃の温度下で反応させる工程を含む、３−ニトロ−４−アルコキシ安息香酸の製造方法を提供する。
摘要翻译：一种制备3-硝基-4-烷氧基苯甲酸的方法，其包括在30-100℃的温度下使包含浓度为40-80％的4-烷氧基苯甲酸和硝酸的混合物，硝酸酸的含量为4-烷氧基苯甲酸的量的至少8倍。

5. 发明申请

WO1998003452A1 POLYMERS AS A SUPPORT FOR COMBINATORIAL SYNTHESIS 审中-公开
标题翻译：聚合物作为组合合成的支持
公开(公告)号：WO1998003452A1
公开(公告)日：1998-01-29
申请号：PCT/US1997012694
申请日：1997-07-18
申请人： THE PROCTER & GAMBLE COMPANY , PAN, Yong
发明人： THE PROCTER & GAMBLE COMPANY
IPC分类号： C07B61/00
CPC分类号： C07C201/12 , B01J2219/00599 , C40B50/08 , C07C205/58 , C07C205/59
摘要： "Three-dimensional" polymers of very small size can be used in the context of synthesis. These polymers provide simple isolation routes by avoiding the need for workup following the reactions, pre-workup characterization, high yield, high capacity and reusability. Of equal importance, these polymers provide a more efficient route to combinatorial synthesis of small molecules. This provides greatly enhanced efficiency for making and screening molecules for physical/biological properties.
摘要翻译：非常小尺寸的“三维”聚合物可以在合成的背景下使用。这些聚合物通过避免对反应后的后处理，预处理表征，高产率，高容量和可再利用性提供简单的隔离途径。同样重要的是，这些聚合物提供了一种更有效的组合小分子合成途径。这为制备和筛选分子的物理/生物学特性提供了极大的提高的效率。

6. 发明申请

WO1997027846A1 BIPHENYL COMPOUNDS AND USE THEREOF AS OESTROGENIC AGENTS 审中-公开
标题翻译：联苯化合物及其作为致癌剂的用途
公开(公告)号：WO1997027846A1
公开(公告)日：1997-08-07
申请号：PCT/FR1997000183
申请日：1997-01-30
申请人： ROUSSEL UCLAF , LESUISSE, Dominique , TEUTSCH, Jean-Georges
发明人： ROUSSEL UCLAF
IPC分类号： A61K31/055
CPC分类号： C07C217/20 , C07C39/15 , C07C39/24 , C07C39/367 , C07C39/373 , C07C43/23 , C07C45/00 , C07C45/59 , C07C45/67 , C07C45/673 , C07C45/68 , C07C47/57 , C07C47/575 , C07C49/83 , C07C205/20 , C07C205/26 , C07C205/58 , C07C205/59 , C07C215/54 , C07C215/78
摘要： Compounds of formula (I), wherein R5 is an [A]-CH3, -[A]-C(OH)ZZ' or -[A]-C(O)Z" grouping where -[A]- is an alkylene, alkenylene or alkynylene radical or a single bond, and Z, Z' and Z" are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl radical; and R1, R2, R3, R4, R6, R7 and R8 are as defined in the description; the use thereof as a drug, pharmaceutical compositions containing same, a preparation method therefor, and intermediates of said method, are disclosed.
摘要翻译：式（I）化合物，其中R 5是[A] -CH 3， - [A] -C（OH）ZZ'或 - [A] -C（O）Z“基团，其中 - [A] 亚烯基或亚炔基或单键，Z，Z'和Z“为氢原子或任选取代的烷基，烯基，炔基或芳基; 并且R1，R2，R3，R4，R6，R7和R8如说明书中所定义; 公开了其作为药物的用途，含有它们的药物组合物，其制备方法和所述方法的中间体。

7. 发明申请

WO1997016569A1 LAWN ASSAY FOR COMPOUNDS THAT AFFECT ENZYME ACTIVITY OR BIND TO TARGET MOLECULES 审中-公开
标题翻译：影响酶活性或结合靶向分子的化合物的法分析
公开(公告)号：WO1997016569A1
公开(公告)日：1997-05-09
申请号：PCT/US1996017702
申请日：1996-10-24
申请人： PHARMACOPEIA, INC.
发明人： PHARMACOPEIA, INC. , CHELSKY, Daniel , BURBAUM, Jonathan, J.
IPC分类号： C12Q01/68
CPC分类号： C07C205/59 , C07B2200/11 , C07D311/08 , C07D311/22 , C07D311/96 , C07D491/10 , C07D493/10 , C07D495/10 , C12Q1/00 , C40B40/00 , G01N33/573
摘要： A lawn assay is described for determining compounds that affect enzyme activity or that bind to target molecules. Compounds to be screened are cleaved, and diffused from solid supports into a colloidal matrix. Enzymatic catalysis or binding to target molecules by the compounds is carried out in the matrix. Active compounds are found by monitoring a photometrically detectable change in a substrate, coenzyme, or cofactor involved in the enzymatic reaction, or in a labeled ligand bound to the target molecule, that produces a zone of activity associated with the compounds.
摘要翻译：描述了用于确定影响酶活性或结合靶分子的化合物的草坪测定。待筛选的化合物被切割，并从固体载体扩散到胶体基质中。通过化合物的酶催化或与靶分子的结合在基质中进行。通过监测参与酶反应的底物，辅酶或辅因子或与靶分子结合的标记配体中的光学上可检测的变化，发现活性化合物，其产生与化合物相关的活性区。

8. 发明申请

WO1994019316A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO1994019316A1
公开(公告)日：1994-09-01
申请号：PCT/SE1994000153
申请日：1994-02-24
申请人： AKTIEBOLAGET ASTRA , THE UNIVERSITY OF MARYLAND , CORNELL RESEARCH FOUNDATION INC. , BJÖRK, Susanna, Karin, Maria , CARPENTIER, Barry, K. , GOTTHAMMAR, Kristina, Brigitta , LINDERBERG, Mat, Torbjörn , LUTHMAN, Per, Johan , PERSSON, Kerstin, Margareta, Irma , SCHWARCZ, Robert
发明人： AKTIEBOLAGET ASTRA , THE UNIVERSITY OF MARYLAND , CORNELL RESEARCH FOUNDATION INC.
IPC分类号： C07C229/64
CPC分类号： C07D333/20 , C07C45/27 , C07C47/277 , C07C205/37 , C07C205/59 , C07C205/60 , C07C229/64
摘要： The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of general formula (I) wherein R and R are the same or different and selected from H, alkyl, aryl and arylalkyl; X and Y are the same or different and selected from alkoxy, aryloxy, alkyl, alkylthio, arylthio, fluoroalkyl, halogen, cyano, OSO2CH3, OSO2CF3, OCF3 and SCF3 with the proviso that the compound of formula (I) wherein R and R = H, X = Br and Y = Me is excluded; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxyanthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.
摘要翻译：本发明涉及通式（I）的3-羟基邻氨基苯甲酸的新型衍生物，其中R 1和R 2相同或不同并且选自H，烷基，芳基和芳基烷基; X和Y相同或不同，并且选自烷氧基，芳氧基，烷基，烷硫基，芳硫基，氟烷基，卤素，氰基，OSO 2 CH 3，OSO 2 CF 3，OCF 3和SCF 3，条件是其中R 1，和R 2 = H，X = Br和Y = Me; 或其药学上可接受的盐，其制备方法和中间体，新型药物组合物及其用于抑制负责内源性神经毒素喹啉酸QUIN的3-羟基邻氨基苯甲酸酶加氧酶3-HAO的用途。

9. 发明申请

WO2015111085A3 PROCESSES FOR THE PREPARATION OF ELTROMBOPAG AND PHARMACEUTICALLY ACCEPTABLE SALTS, SOLVATES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备药物缓释剂和药物可接受的盐，溶剂和中间体的方法
公开(公告)号：WO2015111085A3
公开(公告)日：2015-11-12
申请号：PCT/IN2015000052
申请日：2015-01-27
申请人： CADILA HEALTHCARE LTD
发明人： DESAI SANJAY JAGDISH , DWIVEDI SHRI PRAKASH DHAR , PARIHAR JAYPRAKASH AJITSINGH , RUPAPARA MAHESH LALJIBHAI , KESHAVALA DHARMENDRA MOHANBHAI
IPC分类号： C07D231/48 , A61K31/4152 , A61P7/02 , C07C227/04
CPC分类号： C07D231/46 , C07C201/08 , C07C201/12 , C07C227/04 , C07C205/26 , C07C205/37 , C07C205/59 , C07C229/52
摘要： The present invention provides the processes for the preparation of eltrombopag of Formula (I) or its pharmaceutically acceptable salts. The invention also provides crystalline forms of eltrombopag.
摘要翻译：本发明提供了用于制备式（I）的艾曲波帕或其药学上可接受的盐的方法。本发明还提供了eltrombopag的结晶形式。

10. 发明申请

WO2015111085A2 PROCESSES FOR THE PREPARATION OF ELTROMBOPAG AND PHARMACEUTICALLY ACCEPTABLE SALTS, SOLVATES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备高效液相色谱法和药物可接受的盐，溶剂及其中间体的方法
公开(公告)号：WO2015111085A2
公开(公告)日：2015-07-30
申请号：PCT/IN2015/000052
申请日：2015-01-27
申请人： CADILA HEALTHCARE LIMITED
发明人： DESAI, Sanjay Jagdish , DWIVEDI, Shri Prakash Dhar , RUPAPARA, Mahesh Laljibhai , KESHAVALA, Dharmendra Mohanbhai
CPC分类号： C07D231/46 , C07C201/08 , C07C201/12 , C07C227/04 , C07C205/26 , C07C205/37 , C07C205/59 , C07C229/52
摘要： The present invention provides the processes for the preparation of eltrombopag of Formula (I) or its pharmaceutically acceptable salts. The invention also provides crystalline forms of eltrombopag.
摘要翻译：本发明提供制备式（I）的埃曲波帕或其药学上可接受的盐的方法。本发明还提供了埃曲波帕的结晶形式。

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