公开(公告)号：US09758473B2

公开(公告)日：2017-09-12

申请号：US14875416

申请日：2015-10-05

Applicant: Cortexyme, Inc.

Inventor： Andrei Konradi ,  Stephen S. Dominy ,  Casey Crawford Lynch ,  Craig Coburn ,  Joseph Vacca

IPC: C07C247/16 ,  C07C233/62 ,  C07C233/78 ,  C07D417/12 ,  C07D277/64 ,  C07D409/12 ,  C07D213/50

CPC classification number: C07D417/12 ,  C07B2200/07 ,  C07C233/62 ,  C07C233/78 ,  C07C247/16 ,  C07C247/18 ,  C07C2601/08 ,  C07D213/50 ,  C07D213/53 ,  C07D277/24 ,  C07D277/28 ,  C07D277/64 ,  C07D409/12

Abstract: The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

公开(公告)号：US09108943B2

公开(公告)日：2015-08-18

申请号：US14308094

申请日：2014-06-18

Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS

Inventor： Pavel Petukhov

IPC: C07D333/24 ,  C07C247/16 ,  C07C247/18

CPC classification number: C07D333/24 ,  C07C247/16 ,  C07C247/18

Abstract: The design, modeling, synthesis, biological evaluation, and photoaffinity labeling studies of a series of photoreactive potent and selective HDACs 1 and 2 benzamide based probes are disclosed herein.

Abstract translation: 本文公开了一系列光反应性有效和选择性HDAC 1和2苯甲酰胺基探针的设计，建模，合成，生物学评估和光亲和标记研究。

公开(公告)号：US20150079519A1

公开(公告)日：2015-03-19

申请号：US14391170

申请日：2013-02-28

Applicant: TOYO GOSEI CO., LTD.

Inventor： Toru Shibuya

IPC: G03F7/038 ,  C08F116/06 ,  C07D233/60 ,  C07D263/38 ,  C07C247/16

CPC classification number: G03F7/012 ,  C07C233/83 ,  C07C247/16 ,  C07C247/18 ,  C07D233/60 ,  C07D233/61 ,  C07D263/38 ,  C07D263/42 ,  C07D295/14 ,  C08F116/06 ,  G03F7/008 ,  G03F7/0125 ,  G03F7/0388

Abstract: A photosensitive compound represented by formula (1) or formula (2). (Chemical formula 1) (In formula (1) and formula (2), n is an integer of 1-3; R1 is a linear or branched alkyl group having 1-6 carbon atoms or an alkylene group having 2-6 carbon atoms formed from two R1 together; R2 is —NR3R4; R3 and R4 are each independently a linear or branched alkyl group or alkenyl group having 1-6 carbon atoms, a linear or branched alkylene group having 2-6 carbon atoms formed by R3 and R4 together, or a linear or branched alkylene group or alkenylene group having 3-8 carbon atoms optionally containing an oxygen atom or nitrogen atom.)

Abstract translation: 由式（1）或式（2）表示的光敏化合物。 （化学式1）（式（1）和式（2）中，n为1〜3的整数，R 1为碳原子数1〜6的直链或支链烷基或碳原子数2〜6的亚烷基 由两个R 1一起形成; R 2是-NR 3 R 4; R 3和R 4各自独立地是具有1-6个碳原子的直链或支链烷基或烯基，由R3和R4形成的具有2-6个碳原子的直链或支链亚烷基 一起或具有任选含有氧原子或氮原子的具有3-8个碳原子的直链或支链亚烷基或亚烯基）

公开(公告)号：US20120237444A1

公开(公告)日：2012-09-20

申请号：US13510656

申请日：2010-12-10

Applicant: Michelle Avory

Inventor： Michelle Avory

IPC: C07K7/56 ,  B01L3/00 ,  A61K51/08

CPC classification number: A61K51/08 ,  C07B59/002 ,  C07B2200/05 ,  C07C247/16 ,  C07C291/06 ,  C07D231/12 ,  C07D249/06 ,  C07D261/08 ,  C07K1/13 ,  C07K5/0817 ,  G01N2800/52

Abstract: The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using the radioiodinated BTMs.

Abstract translation: 本发明提供了用放射性碘标记生物靶向分子（BTM）的新方法。 还提供了使用该方法制备的新型放射性碘化BTM，以及包含这种放射性碘化BTM的放射性药物组合物。 本发明还提供了可用于该方法的放射性碘化中间体，以及使用放射性碘化BTM的体内成像方法。

公开(公告)号：US20090004402A1

公开(公告)日：2009-01-01

申请号：US11994565

申请日：2006-07-04

Applicant: Peter Kian-Hoon Ho ,  Lay-Lay Chua ,  Siong-Hee Khong ,  Sankaran Sivaramakrishnan ,  Perq-Jon Chia

Inventor： Peter Kian-Hoon Ho ,  Lay-Lay Chua ,  Siong-Hee Khong ,  Sankaran Sivaramakrishnan ,  Perq-Jon Chia

IPC: C08J7/04 ,  C07C247/16 ,  C08F273/00 ,  C08F277/00

CPC classification number: C07C247/16 ,  C07C247/18 ,  G03F7/038

Abstract: There is provided a class of crosslinking compound, said compound comprising (i) one or more fluorinated aromatic group; and (ii) one or more ionisable group, wherein the crosslinking compound is soluble in at least one polar solvent. Methods of preparing the crosslinking compounds are also disclosed. There is further provided devices obtainable from the methods of preparing the crosslinking compounds.

Abstract translation: 提供一类交联化合物，所述化合物包含（i）一种或多种氟化芳族基团; 和（ii）一种或多种可离子化基团，其中所述交联化合物可溶于至少一种极性溶剂。 还公开了制备交联化合物的方法。 进一步提供可从制备交联化合物的方法获得的装置。

公开(公告)号：US20060284166A1

公开(公告)日：2006-12-21

申请号：US10556404

申请日：2004-05-12

Applicant: Lay-Lay Chua ,  Peter Ho ,  Henning Sirringhaus ,  Richard Friend

Inventor： Lay-Lay Chua ,  Peter Ho ,  Henning Sirringhaus ,  Richard Friend

IPC: H01L29/08 ,  H01L51/40

CPC classification number: H01L51/0002 ,  C07C247/16 ,  G03C1/695 ,  H01L51/0003 ,  H01L51/0035 ,  H01L51/0037 ,  H01L51/0038 ,  H01L51/0039 ,  H01L51/0043 ,  H01L51/0059 ,  H01L51/052

Abstract: A transistor including a semiconductive layer; and a gate dielectric layer comprising an insulating polymer, characterised in that the insulating polymer is crosslinked and comprises one or more units having a low cohesive-energy-density and one or more crosslinking groups and the insulating polymer includes substantially no residual —OH leaving groups.

Abstract translation: 一种包括半导体层的晶体管; 以及包含绝缘聚合物的栅极电介质层，其特征在于，所述绝缘聚合物是交联的并且包含具有低内聚能量密度和一个或多个交联基团的一个或多个单元，并且所述绝缘聚合物基本上不包括残余的-OH离去基团 。

公开(公告)号：US06768027B2

公开(公告)日：2004-07-27

申请号：US10400838

申请日：2003-03-27

Applicant: Mineko Takeda

Inventor： Mineko Takeda

IPC: C07C4752

CPC classification number: C07C247/16

Abstract: The invention provides a novel azidocinnamaldehyde compound which, when used as an intermediate for providing a photosensitive moiety of a photoresist, introduces a photosensitive moiety having high sensitivity and attaining high contrast between the exposed portion and the unexposed portion, and which per se can serve as a photosensitive moiety. The azidocinnamaldehyde compound is represented by formula(I): wherein R represents a lower alkyl group and Y represents hydrogen or a sulfonate salt group.

Abstract translation: 本发明提供了一种新的叠氮肉桂醛化合物，当用作提供光致抗蚀剂的光敏部分的中间体时，引入具有高灵敏度并在曝光部分和未曝光部分之间获得高对比度的感光部分，其本身可以用作 感光部分。 叠氮肉桂醛化合物由式（I）表示：其中R表示低级烷基，Y表示氢或磺酸盐基团。

公开(公告)号：US06455701B1

公开(公告)日：2002-09-24

申请号：US09708972

申请日：2000-11-08

Applicant: Tae K. Song ,  Min Teng ,  Roshantha A. Chandraratna

Inventor： Tae K. Song ,  Min Teng ,  Roshantha A. Chandraratna

IPC: C07D21330

CPC classification number: C07D213/80 ,  C07C65/28 ,  C07C69/94 ,  C07C205/38 ,  C07C235/56 ,  C07C247/16

Abstract: Compounds of the formula Y3(R4)—X—Y1(R1R2)—Z—Y2(R2)—A—B where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.

Abstract translation: 符号具有本说明书中定义的含义的化合物具有类视黄醇，维生素A拮抗剂或类视黄醇反向激动剂型生物活性。

公开(公告)号：US06316455B1

公开(公告)日：2001-11-13

申请号：US09448485

申请日：1999-11-24

Applicant: Roger John Griffin ,  Alan Hilary Calvert ,  Nicola Jane Curtin ,  David Richard Newell ,  Bernard Thomas Golding

Inventor： Roger John Griffin ,  Alan Hilary Calvert ,  Nicola Jane Curtin ,  David Richard Newell ,  Bernard Thomas Golding

IPC: A61K31513

CPC classification number: C07D263/56 ,  C07C235/46 ,  C07C247/16 ,  C07C255/54 ,  C07D239/91 ,  C07D263/57 ,  C07D317/68 ,  C07D473/34 ,  C07D473/40

Abstract: A range of 3-oxybenzamide compounds and related quinazolinone compounds are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The coumpounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula X and Y together may form a bride —X—Y— that represents the grouping (a), (b) or (c) wherein R5 is H, alkyl, aryl or aralkyl.

Abstract translation: 公开了一系列3-氧基苯甲酰胺化合物和相关的喹唑啉酮化合物，其可以作为DNA修复酶聚（ADP-核糖）聚合酶或PARP酶（EC 2.4.2.30）的有效抑制剂，由此可以为 与DNA损伤性细胞毒性药物或放射治疗联合使用以增强后者的作用。 公开的专利文献包括3-苄氧基苯甲酰胺，其中5个或更多个亚甲基的链终止于卤素原子或嘌呤-9-基部分的某些苯并恶唑-4-甲酰胺化合物和某些喹唑啉酮化合物的3-氧代苯甲酰胺。 式X和Y一起可以形成代表（a），（b）或（c）的组合的新娘-X-Y-，其中R 5是H，烷基，芳基或芳烷基。

公开(公告)号：US06252096B1

公开(公告)日：2001-06-26

申请号：US09525753

申请日：2000-03-14

Applicant: Hans Peter Spielmann ,  Kareem Abdel Hassan Chehade

Inventor： Hans Peter Spielmann ,  Kareem Abdel Hassan Chehade

IPC: C07C24710

CPC classification number: C07C247/16 ,  C07C311/44

Abstract: The invention is directed to a novel compounds comprising 4-azidotetrafluoroaniline and the alkyl, acyl and sulfonamide derivatives thereof and to methods of making and using the same. The novel compounds are useful as a photoaffinity probe to study protein structure and function. Two methods for preparing 4-azidotetrafluoroaniline are disclosed, each employing a stable carbamate intermediate from which the 4-azidotetrafluoroaniline is derived.

Abstract translation: 本发明涉及包含4-叠氮四氟四苯胺及其烷基，酰基和磺酰胺衍生物的新化合物及其制备和使用方法。 新型化合物可用作光亲和性探针来研究蛋白质结构和功能。 公开了制备4-叠氮四氟苯胺的两种方法，每种方法使用得自4-叠氮四氟乙苯的稳定的氨基甲酸酯中间体。