公开(公告)号：WO2009049242A1

公开(公告)日：2009-04-16

申请号：PCT/US2008/079628

申请日：2008-10-10

Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY (SIOC), CAS CHINESE ACADEMY OF SCIENCES ,  YUAN, Junying ,  MA, Dawei ,  ZHANG, Lihong

Inventor： YUAN, Junying ,  MA, Dawei ,  ZHANG, Lihong

IPC: A01N43/40 ,  A61K9/00 ,  A61K31/445

CPC classification number: C07D211/44 ,  A61K31/445 ,  C07D211/82 ,  C07D401/12 ,  C07D491/22

Abstract: This invention pertains to a class of autophagy inducing compounds that treat diseases caused by misfolded protein aggregates and a screening method for identifying these compounds.

Abstract translation: 本发明涉及治疗由错误折叠的蛋白质聚集体引起的疾病的一类自噬诱导化合物和用于鉴定这些化合物的筛选方法。

公开(公告)号：WO02088101A3

公开(公告)日：2003-01-03

申请号：PCT/US0213741

申请日：2002-04-29

Applicant: VERTEX PHARMA ,  BHISETTI GOVINDA R ,  SAUNDERS JEFFREY O ,  MURCKO MARK A ,  LEPRE CHRISTOPHER A ,  BRITT SHAWN D ,  COME JON H ,  DENINGER DAVID D ,  WANG TIANSHANG

Inventor： BHISETTI GOVINDA R ,  SAUNDERS JEFFREY O ,  MURCKO MARK A ,  LEPRE CHRISTOPHER A ,  BRITT SHAWN D ,  COME JON H ,  DENINGER DAVID D ,  WANG TIANSHANG

IPC: A61K31/4409 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/47 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61P25/28 ,  C07D211/70 ,  C07D211/72 ,  C07D211/74 ,  C07D211/82 ,  C07D213/75 ,  C07D217/26 ,  C07D239/48 ,  C07D241/04 ,  C07D243/08 ,  C07D295/12 ,  C07D295/135 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D405/10 ,  C07D405/14 ,  C07D487/04 ,  C07D215/48

CPC classification number: C07D213/75 ,  C07D211/70 ,  C07D211/74 ,  C07D211/82 ,  C07D217/26 ,  C07D239/48 ,  C07D241/04 ,  C07D243/08 ,  C07D295/135 ,  C07D401/04 ,  C07D401/12 ,  C07D405/10 ,  C07D405/14 ,  C07D487/04

Abstract: The present invention relates to inhibitors of aspartic proteinases, particularly, BACE. The present invention also relates to compositions thereof and methods therewith for inhibiting BACE activity in a mammal, and for treating Alzheimer's Disease and other BACE-mediated diseases.

Abstract translation: 本发明涉及天冬氨酸蛋白酶抑制剂，特别是BACE。 本发明还涉及其组合物及其用于抑制哺乳动物中BACE活性的方法，以及用于治疗阿尔茨海默病和其它BACE介导的疾病。

公开(公告)号：WO1997015324A1

公开(公告)日：1997-05-01

申请号：PCT/US1996017240

申请日：1996-10-25

Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA ,  THIELE, Geoffrey, M. ,  McDONALD, Thomas, L. ,  TUMA, Dean, J. ,  KLASSEN, Lynell, W. ,  SORRELL, Michael, F.

Inventor： BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA

IPC: A61K39/00

CPC classification number: C07D211/82 ,  A61K39/385 ,  A61K2039/55511 ,  A61K2039/6012 ,  G01N33/533

Abstract: A high fluorescence specific immune enhancing factor and methods of its use are described. The factor comprises a malondialdehyde-acetaldehyde adduct which can be detected in the picomolar range. The specific immunoenhancing factor allowing for a shorter time course for the production of antibody and of higher titer antibodies without the need for adjuvant. The factor may further be used as a general fluorescent label for immunological techniques and can be used to visualize protein interactions and to monitor protein purification procedures.

Abstract translation: 描述了高荧光特异性免疫增强因子及其使用方法。 该因子包括可在皮摩尔范围内检测的丙二醛 - 乙醛加合物。 特异性免疫增强因子允许用于生产抗体和更高滴度抗体的较短时间，而不需要佐剂。 该因子可进一步用作免疫学技术的一般荧光标记，并且可用于显现蛋白质相互作用并监测蛋白质纯化程序。

公开(公告)号：WO1996033972A1

公开(公告)日：1996-10-31

申请号：PCT/US1996005956

申请日：1996-04-29

Applicant: GLAXO GROUP LIMITED ,  GORDEEV, Mikhail, F. ,  PATEL, Dinesh, V.

Inventor： GLAXO GROUP LIMITED

IPC: C07D211/02

CPC classification number: C07D213/80 ,  C07B2200/11 ,  C07D211/82 ,  C07D211/90 ,  C07D233/78 ,  C07D239/22 ,  C07D239/42 ,  C07D401/04 ,  C07D409/04 ,  C07D409/14 ,  C07D471/04 ,  C40B40/04 ,  C40B50/14

Abstract: Disclosed are methods for synthesizing very large collections of diverse dihydropyridine, dihydropyrimidine, pyridine or pyrimidine compounds on solid supports. Also disclosed are methods for identifying and isolating dihydropyridine and dihydropyrimidine compounds with useful and diverse activities from such collections including the incorporation of identification tags in such collections to facilitate identification of compounds with desired properties.

Abstract translation: 公开了在固体支持物上合成非常大量不同的二氢吡啶，二氢嘧啶，吡啶或嘧啶化合物的方法。 还公开了用于鉴定和分离二氢吡啶和二氢嘧啶化合物的方法，其具有来自这些收集物的有用和多种活性，包括在这种收集物中掺入鉴定标签以促进鉴定具有所需性质的化合物。

公开(公告)号：WO2017088031A1

公开(公告)日：2017-06-01

申请号：PCT/AU2016/051162

申请日：2016-11-28

Applicant: COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION

Inventor： RYAN, John ,  YORK, Mark

IPC: C07D211/70 ,  C07D211/78 ,  C07D211/80 ,  C07D213/50 ,  C07D241/04 ,  C07D241/08 ,  C09D5/32 ,  A61K8/40

CPC classification number: C07D211/70 ,  A61K8/4926 ,  A61Q17/04 ,  C07C49/543 ,  C07C49/792 ,  C07C49/807 ,  C07D211/82 ,  C07D401/10 ,  C09D5/32 ,  C09K15/30

Abstract: The present invention describes compounds and uses thereof in applications relating to absorption of electromagnetic energy. Preferred compounds are double bond-containing cyclic compounds capable of absorbing electromagnetic radiation energy and having improved photostability due to the presence and location of one or more fluorine groups in relation to the double bond of the ring.

Abstract translation: 本发明描述了化合物及其在涉及电磁能量吸收的应用中的用途。 优选的化合物是能够吸收电磁辐射能并且由于一个或多个氟基团相对于环的双键的存在和位置而具有改进的光稳定性的含双键环状化合物。

公开(公告)号：WO2016210190A1

公开(公告)日：2016-12-29

申请号：PCT/US2016/039114

申请日：2016-06-23

Applicant: NITTO DENKO CORPORATION ,  YING, Wenbin

Inventor： YING, Wenbin ,  ADAMI, Roger ,  BAI, Hao ,  GAUDETTE, John ,  MAJETI, Bharat ,  NUKUI, Seiji ,  TSANG, Kwok Yin ,  WANG, Hai ,  YING, Haiqing

IPC: A61K47/16 ,  A61K47/18 ,  A61K47/22

CPC classification number: C07C271/16 ,  A61K31/7105 ,  A61K31/713 ,  A61K47/16 ,  A61K47/22 ,  A61K47/24 ,  C07C237/08 ,  C07C237/16 ,  C07C237/50 ,  C07D205/04 ,  C07D207/09 ,  C07D207/12 ,  C07D211/74 ,  C07D211/82 ,  C07D211/86 ,  C07F9/06 ,  C07F9/106 ,  A61K2300/00

Abstract: This invention includes ionizable compounds, and compositions and methods of use thereof. The ionizable compounds can be used for making nanoparticle compositions for use in biopharmaceuticals and therapeutics. More particularly, this invention relates to compounds, compositions and methods for providing nanoparticles to encapsulate active agents, to deliver and distribute the active agents to cells, tissues, organs, and subjects.

Abstract translation: 本发明包括可离子化的化合物及其组合物及其使用方法。 可电离化合物可用于制备用于生物药物和治疗剂的纳米颗粒组合物。 更具体地说，本发明涉及提供纳米颗粒以包封活性剂，将活性剂递送和分配到细胞，组织，器官和受试者中的化合物，组合物和方法。

公开(公告)号：WO2016138648A1

公开(公告)日：2016-09-09

申请号：PCT/CN2015/073647

申请日：2015-03-04

Applicant: NOVARTIS AG ,  KAPFERER, Tobias ,  GONG, Baoqing ,  DAVIS, Mark Clinton ,  ZHENG, Xuchun ,  HAR, Denis

Inventor： KAPFERER, Tobias ,  GONG, Baoqing ,  DAVIS, Mark Clinton ,  ZHENG, Xuchun ,  HAR, Denis

IPC: C07D401/12 ,  C07D211/22 ,  C07D211/26 ,  C07D239/26

CPC classification number: C07D211/28 ,  C07D211/80 ,  C07D211/82 ,  C07D239/42

Abstract: The present disclosure relates to a method of synthesizing 5-chloro-N2- (2-isopropoxy-5-methyl-4- (piperidin-4-yl) phenyl) -N4- [2- (propane-2-sulfonyl) -phenyl] -pyrimidine-2, 4-diamine (ceritinib) and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing ceritinib.

Abstract translation: 本公开内容涉及合成5-氯-N2-（2-异丙氧基-5-甲基-4-（哌啶-4-基）苯基）-N4- [2-（丙烷-2-磺酰基） - 苯基 ] - 嘧啶-2,4-二胺（ceritinib）和/或其中间体，它们作为药物和药物组合物的用途以及中间体用于制备ceritinib的用途。

公开(公告)号：WO2012134822A1

公开(公告)日：2012-10-04

申请号：PCT/US2012/029206

申请日：2012-03-15

Applicant: MEMORIAL SLOAN-KETTERING CANCER CENTER ,  DJABALLAH, Hakim ,  WU, Hao ,  FELDMAN, Taya ,  JIANG, Xuejun

Inventor： DJABALLAH, Hakim ,  WU, Hao ,  FELDMAN, Taya ,  JIANG, Xuejun

IPC: A01N55/02

CPC classification number: C07D211/82 ,  A61K31/44 ,  A61K31/555 ,  A61K45/06 ,  C07F1/08 ,  A61K2300/00

Abstract: The invention provides a method for the use of a group of compounds as allosteric reversible caspase inhibitors. This invention is in the field of medicinal chemistry and relates to novel compounds, and pharmaceutical compositions and methods of use thereof that inhibit caspases and/or tumor necrosis factor alpha (TNFa) that mediate cell apoptosis and inflammation and inhibit pathophysiologic effects of excessive amounts of TNFa. The invention also relates to methods of using the compounds and pharmaceutical compositions of this invention to treat diseases where caspase and/or TNFa activity is implicated. The present invention also relates to methods for the use of allosteric, reversible pan-caspase inhibitors with pyridinyl, copper-containing molecules with a multi-ring structure.

Abstract translation: 本发明提供使用一组化合物作为变构可逆半胱天冬酶抑制剂的方法。 本发明涉及药物化学领域，涉及新型化合物及其抑制胱天蛋白酶和/或介导细胞凋亡和炎症的肿瘤坏死因子α（TNFa）的用途的药物组合物及其使用方法，并抑制过量药物的病理生理作用 TNFα的。 本发明还涉及使用本发明化合物和药物组合物治疗涉及半胱天冬酶和/或TNFα活性的疾病的方法。 本发明还涉及使用具有吡啶基的变构的可逆泛胱天蛋白酶抑制剂与具有多环结构的含铜分子的方法。

公开(公告)号：WO2016101887A1

公开(公告)日：2016-06-30

申请号：PCT/CN2015/098385

申请日：2015-12-23

Applicant: NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING

Inventor： ZHANG, Zhiyuan ,  WANG, Xiaodong ,  SU, Yaning ,  RUAN, Hanying ,  REN, Yan

IPC: C07D205/04 ,  C07D207/12 ,  C07D211/70 ,  C07D263/04 ,  C07D265/30 ,  C07D405/06 ,  C07D417/06 ,  A61K31/397 ,  A61K31/40 ,  A61K31/421 ,  A61P43/00

CPC classification number: A61K31/165 ,  A61K31/10 ,  A61K31/167 ,  C07C233/01 ,  C07C235/38 ,  C07D203/18 ,  C07D205/04 ,  C07D205/08 ,  C07D207/06 ,  C07D207/08 ,  C07D207/12 ,  C07D207/20 ,  C07D207/24 ,  C07D207/27 ,  C07D207/333 ,  C07D211/16 ,  C07D211/70 ,  C07D211/82 ,  C07D231/02 ,  C07D231/04 ,  C07D231/08 ,  C07D233/38 ,  C07D241/04 ,  C07D261/02 ,  C07D263/04 ,  C07D263/22 ,  C07D265/30 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04

Abstract: The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Abstract translation: 本发明提供抑制细胞坏死和/或人受体相互作用蛋白1激酶（RIP1）的酰胺，包括相应的磺酰胺及其药学上可接受的盐，氢化物和立体异构体。 这些化合物用于药物组合物，以及制备和使用的方法，包括用有效量的化合物或组合物治疗有需要的人，并检测由此导致的人的健康或状况的改善。

公开(公告)号：WO2006134606A1

公开(公告)日：2006-12-21

申请号：PCT/IN2005/000198

申请日：2005-06-15

Applicant: HETERO DRUGS LIMITED ,  PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  SATISH KUMAR, Dandamudi

Inventor： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  SATISH KUMAR, Dandamudi

IPC: C07D211/02 ,  C07D211/90

CPC classification number: C07D211/90 ,  C07D211/82

Abstract: The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of triethyl amine in methylene chloride to give 2,N-dimethyl-2-(trimethylsilyloxy)-N-(3,3-diphenylpropyl)-1-propanamine, which is then reacted with 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carbonyl chloride for 2 hours and crystallized to obtain lercanidipine hydrochloride.

Abstract translation: 本发明提供了使用新型中间体制备氯卡地平或药学上可接受的盐的新方法。 因此，在三氯甲烷存在下，将二，N-二甲基-N-（3,3-二苯基丙基）-1-氨基-2-丙醇与三甲基甲硅烷基氯反应，得到2，N-二甲基-2-（三甲基甲硅烷氧基 ）-N-（3,3-二苯基丙基）-1-丙胺，然后与2,6-二甲基-5-甲氧羰基-4-（3-硝基苯基）-1,4-二氢吡啶-3-羰基氯反应 2小时结晶，得到盐酸氯卡地平。