公开(公告)号：US10196358B2

公开(公告)日：2019-02-05

申请号：US15671428

申请日：2017-08-08

申请人： Ono Pharmaceutical Co., Ltd.

发明人： Kentaro Yashiro ,  Daisuke Wakamatsu ,  Tetsuji Saito

IPC分类号： C07D213/61 ,  A61K31/44 ,  A61K31/17 ,  A61K31/341 ,  A61K31/351 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/417 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/435 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/505 ,  C07D213/74 ,  C07D309/04 ,  C07C275/32 ,  C07C275/40 ,  C07D333/20 ,  C07D333/28 ,  C07D233/64 ,  C07D239/26 ,  C07D413/06 ,  C07D241/12 ,  C07C233/26 ,  C07C233/29 ,  C07D271/06 ,  C07D277/28 ,  C07D209/30 ,  C07D213/40 ,  C07D307/52

摘要： The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.

公开(公告)号：US20180291046A1

公开(公告)日：2018-10-11

申请号：US16006520

申请日：2018-06-12

申请人： Achillion Pharmaceuticals, Inc.

发明人： Jason Allan Wiles ,  Godwin Pais ,  Akihiro Hashimoto ,  Venkat Rao Gadhachanda ,  Qiuping Wang ,  Dawei Chen ,  Xiangzhu Wang ,  Atul Agarwal ,  Milind Deshpande ,  Avinash S. Phadke

IPC分类号： C07F9/572 ,  C07D417/06 ,  C07F7/08 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  C07D209/42 ,  C07D471/08 ,  C07D209/30 ,  C07D209/44 ,  C07D209/88 ,  C07D209/12 ,  A61K31/519 ,  A61K31/501 ,  A61K9/00 ,  A61K31/4045 ,  A61K31/444 ,  A61K31/675 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/549 ,  A61K31/55 ,  A61K31/683 ,  C07F9/6558 ,  C07F9/6561 ,  C07D513/04 ,  C07B59/00 ,  C07D209/14 ,  C07D209/40 ,  C07D405/12 ,  C07D417/12 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D413/06 ,  C07D403/08 ,  C07D405/14 ,  C07D487/04 ,  C07D413/14 ,  C07D417/14 ,  C07D403/06 ,  C07F5/02 ,  C07D471/04

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an alkyne (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

公开(公告)号：US10086085B2

公开(公告)日：2018-10-02

申请号：US14605697

申请日：2015-01-26

申请人： Pfizer Inc.

发明人： Andreas Maderna ,  Matthew David Doroski ,  Zecheng Chen ,  Hud Lawrence Risley ,  Jeffrey Michael Casavant ,  Christopher John O'Donnell ,  Alexander M. Porte ,  Chakrapani Subramanyam

IPC分类号： C07D487/04 ,  C07D487/06 ,  C07D209/30 ,  A61K31/404 ,  A61K31/407 ,  A61K47/48 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/675 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07F9/6561 ,  C07H17/02 ,  C07K5/06 ,  C07K5/08 ,  C07K9/00 ,  A61K47/68

摘要： Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.

公开(公告)号：US20180155286A1

公开(公告)日：2018-06-07

申请号：US15798545

申请日：2017-10-31

申请人： New Mexico Tech Research Foundation

发明人： Snezna ROGELJ ,  Liliya FROLOVA ,  Alexander KORNIENKO ,  Leslie D. EDWARDS ,  Cody CHAMPION ,  Kailee ZINGLER ,  Danielle Nicole Turner

IPC分类号： C07D209/42 ,  C07D209/40 ,  A61K31/404 ,  C07D209/30 ,  C07D209/10 ,  A61K41/00 ,  A61K38/14 ,  A61K38/12 ,  A61K31/7048 ,  A61K31/7036 ,  A61K31/655 ,  A61K31/65 ,  A61K31/496 ,  A61K31/431 ,  A61K31/43 ,  C07D209/36

CPC分类号： C07D209/42 ,  A61K31/404 ,  A61K31/43 ,  A61K31/431 ,  A61K31/496 ,  A61K31/65 ,  A61K31/655 ,  A61K31/7036 ,  A61K31/7048 ,  A61K38/12 ,  A61K38/14 ,  A61K41/0057 ,  A61P31/00 ,  C07D209/10 ,  C07D209/30 ,  C07D209/36 ,  C07D209/40 ,  Y02A50/473 ,  A61K2300/00

摘要： The present disclosure describes a method to treat conditions, including bacterial infections and cancer, using a photosensitive compound that, upon exposure to white light, can be activated. The photosensitive compound can also interact synergistically with antibiotics used concomitantly to kill drug-resistant bacteria. The photosensitive compounds can also be used to inhibit the proliferation of cancer cells.

公开(公告)号：US09845317B2

公开(公告)日：2017-12-19

申请号：US15142418

申请日：2016-04-29

申请人： The Board of Trustees of the University of Illinois

发明人： Martin D. Burke ,  David M. Knapp ,  Eric P. Gillis

IPC分类号： C07F5/02 ,  C07F5/04 ,  C07D413/04 ,  C07C1/32 ,  C07C41/30 ,  C07D207/325 ,  C07D213/73 ,  C07D241/42 ,  C07D263/56 ,  C07D307/42 ,  C07D401/04 ,  C07D405/12 ,  C07D409/04 ,  C07B61/00 ,  C07D207/333 ,  C07D209/12 ,  C07D307/36 ,  C07D307/80 ,  C07D333/16 ,  C07D405/04 ,  C07D207/34 ,  C07D209/30 ,  C07D213/16 ,  C07D213/50 ,  C07D213/57

CPC分类号： C07D413/04 ,  C07B61/00 ,  C07C1/321 ,  C07C41/30 ,  C07C2527/173 ,  C07C2531/12 ,  C07C2531/24 ,  C07C2601/02 ,  C07D207/325 ,  C07D207/333 ,  C07D207/34 ,  C07D209/12 ,  C07D209/30 ,  C07D213/16 ,  C07D213/50 ,  C07D213/57 ,  C07D213/73 ,  C07D241/42 ,  C07D263/56 ,  C07D307/36 ,  C07D307/42 ,  C07D307/80 ,  C07D333/16 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  Y02P20/55 ,  C07C15/46 ,  C07C15/58 ,  C07C13/28 ,  C07C43/2055

摘要： A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T  (I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.

公开(公告)号：US09708267B2

公开(公告)日：2017-07-18

申请号：US14643107

申请日：2015-03-10

申请人： The United States of America, as represented by the Secretary, Department of Health and Human Services

发明人： Matthew B. Boxer ,  Min Shen ,  Douglas S. Auld ,  Craig J. Thomas ,  Martin J. Walsh

IPC分类号： C07D215/227 ,  C07D209/30 ,  C07D215/36 ,  C07D223/16 ,  C07D265/36 ,  C07D209/12 ,  C07D209/34 ,  C07D235/26

CPC分类号： C07D215/227 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D215/36 ,  C07D223/16 ,  C07D235/26 ,  C07D265/36

摘要： Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2(I).

公开(公告)号：US09670142B2

公开(公告)日：2017-06-06

申请号：US14898491

申请日：2014-05-09

申请人： Merck Patent GmbH

发明人： Christos Tsaklakidis ,  Wolfgang Staehle ,  Birgitta Leuthner ,  Paul Czodrowski ,  Thomas Fuchss

IPC分类号： C07C233/79 ,  C07D413/14 ,  C07D309/04 ,  C07D215/12 ,  C07D317/50 ,  C07D319/18 ,  C07D231/12 ,  C07D231/56 ,  C07D233/26 ,  C07D401/04 ,  C07D235/06 ,  C07D235/18 ,  C07D235/26 ,  C07D403/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D249/18 ,  C07D471/04 ,  C07D487/04 ,  C07D263/57 ,  C07D498/04 ,  C07D209/08 ,  C07D209/14 ,  C07D277/62 ,  C07D277/66 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D213/56 ,  C07C255/57 ,  C07C235/42 ,  A61K31/166 ,  A61K31/277 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/451 ,  A61K31/501 ,  A61K31/519 ,  C07C231/10 ,  C07C253/30 ,  C07C255/60 ,  C07D233/58

CPC分类号： C07C233/79 ,  A61K31/166 ,  A61K31/277 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/451 ,  A61K31/501 ,  A61K31/519 ,  C07C231/10 ,  C07C235/42 ,  C07C253/30 ,  C07C255/57 ,  C07C255/60 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D213/56 ,  C07D215/12 ,  C07D231/12 ,  C07D231/56 ,  C07D233/26 ,  C07D233/58 ,  C07D235/06 ,  C07D235/18 ,  C07D235/26 ,  C07D249/18 ,  C07D263/57 ,  C07D277/62 ,  C07D277/66 ,  C07D309/04 ,  C07D317/50 ,  C07D319/18 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： Compounds of the formula I in which R1, R4, R6, R, X1, X2, X3, X4, q and W have the meanings indicated in claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

公开(公告)号：US09598364B2

公开(公告)日：2017-03-21

申请号：US14468408

申请日：2014-08-26

申请人： Taipei Medical University ,  Ohio State University ,  National Taiwan University

发明人： Ching-Shih Chen ,  Jing-Ping Liou ,  Hsing-Jin Liu ,  Kuo-Sheng Hung ,  Pei-Wen Shan ,  Wen-Ta Chiu ,  Che-Ming Teng

IPC分类号： C07D209/08 ,  C07D209/12 ,  C07D209/40 ,  C07D209/18 ,  C07D209/30

CPC分类号： C07D209/08 ,  C07D209/12 ,  C07D209/18 ,  C07D209/30 ,  C07D209/40

摘要： Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.

公开(公告)号：US20170029372A1

公开(公告)日：2017-02-02

申请号：US15302363

申请日：2015-04-09

申请人： THE UNIVERSITY OF BRITISH COLUMBIA ,  SIMON FRASER UNIVERSITY

发明人： Paul RENNIE ,  Artem TCHERKASSOV ,  Robert N. YOUNG ,  Christophe M. ANDRE

IPC分类号： C07D209/14 ,  C07D231/56 ,  C07D471/04 ,  C07D405/14 ,  C07D235/30 ,  C07D209/30 ,  C07D209/08 ,  C07D209/42 ,  C07D405/12 ,  C07D235/18 ,  C07D413/04 ,  C07D401/06 ,  C07D417/04 ,  C07C243/22 ,  C07D403/04 ,  C07D401/04 ,  C07D209/10 ,  C07D417/10 ,  C07D413/10 ,  C07D401/10 ,  C07D417/14 ,  C07D403/14 ,  C07D209/34 ,  C07D277/82

CPC分类号： C07D209/14 ,  C07C243/22 ,  C07D209/08 ,  C07D209/10 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D231/56 ,  C07D235/18 ,  C07D235/30 ,  C07D277/82 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04

摘要： This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.

摘要翻译： 本发明提供具有以下结构的化合物：还提供了用于治疗各种适应症的这些化合物的用途，包括前列腺癌以及涉及这些化合物的治疗方法。

公开(公告)号：US09472769B2

公开(公告)日：2016-10-18

申请号：US14543538

申请日：2014-11-17

申请人： UDC Ireland Limited

发明人： Kazunari M. Yagi ,  Ryo Nishio

IPC分类号： H01L29/08 ,  H01L51/00 ,  C07D209/08 ,  C07D209/40 ,  C09K11/06 ,  H01L51/50 ,  C07D209/12 ,  C07D209/30 ,  C07D401/14 ,  C07D471/04 ,  C07F7/08 ,  C07F7/10 ,  C07F15/00

CPC分类号： H01L51/0072 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D209/40 ,  C07D401/14 ,  C07D471/04 ,  C07F7/0814 ,  C07F7/10 ,  C07F15/0033 ,  C07F15/0086 ,  C09K11/06 ,  C09K2211/1022 ,  C09K2211/1029 ,  C09K2211/185 ,  H01L51/0052 ,  H01L51/0058 ,  H01L51/0061 ,  H01L51/0067 ,  H01L51/0085 ,  H01L51/0087 ,  H01L51/0094 ,  H01L51/5012 ,  H01L51/5036 ,  H01L2251/552

摘要： An organic electroluminescent device is provided and includes: a pair of electrodes; and at least one organic layer between the pair of electrodes, the at least one organic layer including a light-emitting layer. The at least one organic layer contains an indole compound represented by formula (1): in which Ind101 represents a substituted or unsubstituted indole ring, L101 represents a linking group, Ind101 and L101 are connected to each other at 2- or 3-position of Ind101, and n101 represents an integer of 2 or more.