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21. 发明申请

WO1997028134A1 PROCESS FOR PREPARING QUINAZOLONES 审中-公开
标题翻译：制备喹喔啉的方法
公开(公告)号：WO1997028134A1
公开(公告)日：1997-08-07
申请号：PCT/US1997001861
申请日：1997-01-30
申请人： HOECHST CELANESE CORPORATION
发明人： HOECHST CELANESE CORPORATION , BHATTACHARYA, Apurba , ALLEN, Diane, E.
IPC分类号： C07D239/90
CPC分类号： C07D239/90 , C07D239/70
摘要： The present invention provides a process for preparing a quinazolone which comprises the steps of (a) dehydrating a N-acyl beta amino acid in the presence of a dehydration agent and an organic solvent for a sufficient period of time and under suitable temperature and pressure conditions to form an oxazone, (b) adding a carboxylic acid and a primary amine salt of a carboxylic acid to said oxazone to form a mixture, (c) distilling azeotropically said mixture for a suitable period of time and under suitable temperature and pressure conditions to substantially remove said dehydration agent and said organic solvent, and (d) heating the product of step (c) for a sufficient period of time and under suitable temperature and pressure conditions to form said quinazolone.
摘要翻译：本发明提供一种制备喹唑酮的方法，该方法包括以下步骤：（a）在脱水剂和有机溶剂存在下，在适当的温度和压力条件下脱水N-酰基β氨基酸（b）向所述恶唑酮中加入羧酸和羧酸伯胺盐以形成混合物，（c）将共沸蒸馏所述混合物一段适当的时间和温度和压力条件下，向基本上除去所述脱水剂和所述有机溶剂，和（d）在合适的温度和压力条件下加热步骤（c）的产物足够的时间以形成所述喹唑啉酮。

22. 发明申请

WO1997008153A1 PROCESS FOR PRODUCING QUINAZOLIN-4-ONE DERIVATIVES 审中-公开
标题翻译：制备喹唑啉-4-酮衍生物的方法
公开(公告)号：WO1997008153A1
公开(公告)日：1997-03-06
申请号：PCT/JP1996002388
申请日：1996-08-26
申请人： OTSUKA PHARMACEUTICAL FACTORY, INC. , MIYATA, Kazuyoshi , KUROGI, Yasuhisa , SAKAI, Yasuhiro , TSUDA, Yoshihiko
发明人： OTSUKA PHARMACEUTICAL FACTORY, INC.
IPC分类号： C07D239/90
CPC分类号： C07D239/91 , C07D239/90 , C07F9/6512 , C07F9/65128
摘要： A novel process comprising cyclizing a compound represented by general formula (1), wherein R , R , R and R are the same or different and each represents hydrogen, lower alkyl, etc.; R represents phenyl, etc.; and R represents lower alkyl, etc., by treating with a halogenated trialkylsilane in the presence of a base to thereby give a series of quinazolin-4-one derivatives represented by general formula (2), wherein R , R , R , R , R and R are each as defined above, which are useful as drugs and intermediates in the synthesis thereof in a high yield while suppressing the formation of by-products.
摘要翻译：一种包括使由通式（1）表示的化合物环化的新方法，其中R 1，R 2，R 3和R 4相同或不同，各自表示氢，低级烷基等。 ; R 5表示苯基等; 和R 6代表低级烷基等，通过在碱的存在下用卤代三烷基硅烷处理，得到一系列由通式（2）表示的喹唑啉-4-酮衍生物，其中R 1， R 2，R 3，R 4，R 5和R 6各自如上所定义，它们可以作为药物和中间体以高产率合成，同时抑制副产品。

23. 发明申请

WO2022209428A1 ＲＮＡの高次構造解析方法审中-公开
公开(公告)号：WO2022209428A1
公开(公告)日：2022-10-06
申请号：PCT/JP2022/007117
申请日：2022-02-22
申请人：株式会社イクスフォレストセラピューティクス
发明人：小松　リチャード　馨 , 宮下　映見 , 鬼塚　和光 , 永次　史
IPC分类号： C12Q1/68 , C07D239/90 , C12N15/09 , C12Q1/6806 , C12Q1/6869 , G16B15/10
摘要：本開示は、非ワトソンクリック塩基対型高次構造も含めた、より広範な種類のＲＮＡ高次構造を、効率的に検出する技術を提供する。本開示のＲＮＡの高次構造解析方法は、標的結合部分ＳｍとＲＮＡ修飾部分ＹとがリンカーＬで連結された化合物を用意し、この化合物と１又は複数のＲＮＡとを接触させる工程と、この化合物と接触したＲＮＡの塩基配列を決定する工程と、決定された塩基配列に基づいて、標的結合部分と相互作用するＲＮＡ上の位置及び／又は領域を決定する工程と、を含む。

24. 发明申请

WO2021116050A1 NEW BRAF INHIBITORS AS PARADOX BREAKERS 审中-公开
公开(公告)号：WO2021116050A1
公开(公告)日：2021-06-17
申请号：PCT/EP2020/084969
申请日：2020-12-08
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , HEWINGS, David Stephen , HUNZIKER, Daniel , KRUMMENACHER, Daniela , PETTAZZONI, Piergiorgio Francesco Tommaso , WICHMANN, Juergen
IPC分类号： C07D239/90 , C07D403/12 , A61P35/00 , A61K31/517
摘要： The invention provides a novel compound having the general formula (I) (I) wherein R1-R3 and X are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

25. 发明申请

WO2017162510A1 SUBSTITUTED QUINAZOLINONE COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：取代的喹唑啉酮类化合物治疗增殖性疾病
公开(公告)号：WO2017162510A1
公开(公告)日：2017-09-28
申请号：PCT/EP2017/056229
申请日：2017-03-16
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： INCE, Stuart, James , HARTUNG, Ingo , HILLIG, Roman , FANGHÄNEL, Jörg , BRIEM, Hans , LIENAU, Philip , DENNER, Philip , NGUYEN, Duy , HUSEMANN, Manfred , BÖMER, Ulf
IPC分类号： C07D403/04 , C07D403/14 , C07D239/90 , C07D491/056 , A61K31/517 , A61P35/00 , A61P37/00
摘要： The present invention relates to substituted quinazolinone compounds of general formula (I) : in which R 1 , R 2 , R3, R 4 , R5, R6, R7, and R8 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
摘要翻译：本发明涉及通式（I）的取代的喹唑啉酮化合物：其中R 1，R 2，R 3，R

26. 发明申请

WO2015168079A1 PYRIMIDINE OR PYRIDINE DERIVATIVES USEFUL AS PI3K INHIBITORS 审中-公开
标题翻译：可用作PI3K抑制剂的吡嗪或吡啶衍生物
公开(公告)号：WO2015168079A1
公开(公告)日：2015-11-05
申请号：PCT/US2015/027926
申请日：2015-04-28
申请人： INFINITY PHARMACEUTICALS, INC.
发明人： CASTRO, Alfredo, C. , EVANS, Catherine, A.
IPC分类号： C07D403/12 , C07D401/12 , C07D403/04 , C07D405/04 , C07D239/90 , A61K31/517 , A61P35/00 , A61P29/00 , A61P37/00
CPC分类号： C07D403/12 , C07D239/90 , C07D401/12 , C07D403/04 , C07D405/04
摘要： Compounds (I) and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
摘要翻译：本文描述了调节激酶活性（包括PI3激酶活性）的化合物（I）和药物组合物以及与激酶活性（包括P13激酶活性）相关的疾病和病症的化合物，药物组合物和治疗方法。

27. 发明申请

WO2014009872A1 TETRAHYDROQUINAZOLINONE DERIVATIVES AS PARP INHIBITORS 审中-公开
标题翻译：四氢嘧啶酮衍生物作为PARP抑制剂
公开(公告)号：WO2014009872A1
公开(公告)日：2014-01-16
申请号：PCT/IB2013/055618
申请日：2013-07-09
申请人： LUPIN LIMITED
发明人： JANA, Gourhari , KURHADE, Sanjay, Pralhad , JAGDALE, Arun, Rangnath , KUKREJA, Gagan , SINHA, Neelima , PALLE, Venkata, P. , KAMBOJ, Rajender, Kumar
IPC分类号： C07D239/90 , C07D239/88 , A61K31/517 , A61P35/00
CPC分类号： C07D487/08 , A61K31/517 , A61K31/527 , A61K45/06 , C07D239/88 , C07D239/90 , C07D239/91 , C07D401/12
摘要： Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R 1 -R 6 , R 7a-d , R 8a-d , A, M, n, and p are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PARP enzyme of a subject.
摘要翻译：公开了式（I）化合物，其互变异构形式，立体异构体及其药学上可接受的盐，其中R 1 -R 6，R 7a，R d，R 8a，d，A，M，n和p如说明书中所定义，包括化合物，互变异构体，立体异构体或其盐的组合物，以及治疗或预防疾病或病症例如癌症的方法，其可通过抑制受试者的PARP酶来治疗或预防。

28. 发明申请

WO2013154870A1 HISTONE DEACETYLASES (HDACS) INHIBITORS 审中-公开
标题翻译： HISTONE DEACETYLASES（HDACS）抑制剂
公开(公告)号：WO2013154870A1
公开(公告)日：2013-10-17
申请号：PCT/US2013/035004
申请日：2013-04-02
申请人： ANNJI PHARMACEUTICAL CO., LTD. , HEALTHBANKS USA INC.
发明人： CHERN, Ji-Wang , YU, Chao-Wu , CHANG, Pei-Teh
IPC分类号： C07D239/90
CPC分类号： A61K31/517 , C07D239/91 , C07D403/06
摘要： Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit are also disclosed. In an embodiment of the invention, the compound is (2E)-3-(2-ethyl-6-fluoro-3,4-dihydro-4-oxo-3-phenethylquina20lin-7-yl)-N-hydroxyacrylamide, or a salt thereof. In another embodiment of the invention, the compound is (2E)-3-(2-ethyl-7-f1uoro-3,4-dihydro-4-oxo-3-phenethylquinazolin-6-yl)-N-hydroxyacrylamide, (2E)-3-(7-chloro-2-ethyl-3,4-dihydro-4-oxo-3-phenethylquinazolin-6-yl)-N-hydroxyacrylamide, or a salt thereof. In another aspect the invention relates to a composition comprising a therapeutically effective amount of a compound as aforementioned, or a pharmaceutically acceptable salt, a solvate or hydrate, a prodrug, or a metabolite thereof, and a pharmaceutically acceptable carrier or vehicle.
摘要翻译：还公开了治疗HDAC的抑制提供益处的疾病和病症的方法。在本发明的一个实施方案中，化合物是（2E）-3-（2-乙基-6-氟-3,4-二氢-4-氧代-3-苯乙基喹唑啉-2-基）-N-羟基丙烯酰胺或的盐。在本发明的另一个实施方案中，化合物是（2E）-3-（2-乙基-7-氟-3,4-二氢-4-氧代-3-苯乙基喹唑啉-6-基）-N-羟基丙烯酰胺，（2E ）-3-（7-氯-2-乙基-3,4-二氢-4-氧代-3-苯乙基喹唑啉-6-基）-N-羟基丙烯酰胺或其盐。在另一方面，本发明涉及包含治疗有效量的如上所述的化合物或其药学上可接受的盐，溶剂合物或水合物，前药或代谢物，以及药学上可接受的载体或载体的组合物。

29. 发明申请

WO2009143049A1 BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS 审中-公开
标题翻译：双相异构体衍生物及其作为GPR119调节剂的用途
公开(公告)号：WO2009143049A1
公开(公告)日：2009-11-26
申请号：PCT/US2009/044323
申请日：2009-05-18
申请人： SCHERING CORPORATION , HARRIS, Joel, M. , NEELAMKAVIL, Santhosh, Francis , NEUSTADT, Bernard, R. , BOYLE, Craig, D. , LIU, Hong , HAO, Jinsong , STAMFORD, Andrew , CHACKALAMANNIL, Samuel , GREENLEE, William, J.
发明人： HARRIS, Joel, M. , NEELAMKAVIL, Santhosh, Francis , NEUSTADT, Bernard, R. , BOYLE, Craig, D. , LIU, Hong , HAO, Jinsong , STAMFORD, Andrew , CHACKALAMANNIL, Samuel , GREENLEE, William, J.
IPC分类号： C07D239/88 , C07D239/90 , C07D239/95 , C07D401/06 , C07D401/12 , C07D401/14 , C07D407/06 , C07D407/12 , C07D413/04 , C07D413/12 , C07D417/12 , A61K31/517 , A61P3/04 , A61P3/10 , A61P9/00
CPC分类号： C07D239/90 , C07D401/06 , C07D401/12 , C07D403/04 , C07D413/04 , C07D417/12 , C07D471/04
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.
摘要翻译：本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与 GPR1 19在患者体内的活动。

30. 发明申请

WO2008035359A2 OXIMINOPHENOXYALKANOIC ACID AND PHENYLALKANOIC ACID DERIVATIVES 审中-公开
标题翻译：亚硝基羟基烷酸和苯甲酸衍生物
公开(公告)号：WO2008035359A2
公开(公告)日：2008-03-27
申请号：PCT/IN2007000226
申请日：2007-06-05
申请人： CADILA HEALTHCARE LTD , LOHRAY BRAJ BHUSHAN , LOHRAY VIDYA BHUSHAN , PINGALI HARIKISHORE , PATEL PANKAJ RAMANBHAI
发明人： LOHRAY BRAJ BHUSHAN , LOHRAY VIDYA BHUSHAN , PINGALI HARIKISHORE , PATEL PANKAJ RAMANBHAI
IPC分类号： C07C251/48 , A61K31/15 , A61K31/216 , A61K31/517 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , C07C251/52 , C07D239/90
CPC分类号： C07D239/90 , C07C251/48 , C07C251/52 , C07C2601/08 , C07C2601/14 , C07D207/333 , C07D209/08 , C07D209/86 , C07D231/12 , C07D263/24 , C07D263/32 , C07D265/36 , C07D265/38 , C07D277/24 , C07D333/22
摘要： The present invention discloses oximinophenoxyalkanoic acid and phenylalkanoic acid of the general formula (I) their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.
摘要翻译：本发明公开了通式（I）的肟基苯氧基链烷酸和苯基链烷酸的互变异构形式，它们的立体异构体，其药学上可接受的盐，含有它们的药物组合物，其制备方法，这些化合物在医药中的用途以及涉及它们的中间体制备。

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