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公开(公告)号：US10175229B2
公开(公告)日：2019-01-08
申请号：US15301256
申请日：2015-03-30
申请人： NAGASAKI UNIVERSITY
发明人： Yoshimasa Tanaka , Yuki Sakai , Satoshi Mizuta , Hiroshi Ueda
IPC分类号： C07D401/14 , G01N33/58 , G01N33/50 , G01N21/64 , C07D401/12 , C07D213/79
摘要： The present invention aims to provide a novel compound for measuring cellular cytotoxicity or cell proliferation capacity accurately with high reproducibility, conveniently and rapidly, and a measurement method of cellular cytotoxicity or cell proliferation capacity by using the compound. The present invention relates to a compound represented by the formula (I): wherein R1 is a substituent, R2 and R3 are each an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group, Y is a substituent, n is an integer of 0-3, Z is a single bond, —O—, —S—, —SO—, —SO2—, or —NR4— (R4 is a hydrogen atom or a substituent), and A is an optionally substituted C1-6 alkylene group) or a salt thereof.
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公开(公告)号：US10167246B2
公开(公告)日：2019-01-01
申请号：US15532957
申请日：2015-09-25
发明人： Yehua Su , Jieping Shi , Jianxin Lu , Tianhao Zhang , Xiaohua Yu , Guoping Cai , Bangchi Chen
IPC分类号： C07B41/08 , C07C53/08 , C07C201/12 , C07C205/11 , C07C205/56 , C07C205/58 , C07C253/30 , C07C255/41 , C07C315/04 , C07C317/44 , C07C51/285 , C07D213/60 , C07D213/79 , C07D213/803
摘要： A preparative method for carboxylic acids is disclosed in the present invention. The method is characterized in that: compounds (II) are reacted in the presence of hydrogen peroxide and base to produce target products (I), as represented by the following reaction scheme: wherein R1 is aryl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, benzothienyl, benzofuranyl, quinolinyl, isoquinolinyl, thiadiazolyl, C1-6 alkyl, C3-6 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl and hydrogen; R2 is alkoxycarbonyl, alkylaminocarbonyl, aminocarbonyl, alkylthiolcarbonyl, cyano, sulfonyl, sulfinyl, carbonyl, aldehyde, carboxyl, nitro, alkyl and hydrogen; R3 is alkoxycarbonyl, alkyl amido carbonyl, aminocarbonyl, cyano, sulfonyl, sulfinyl, carbonyl, carboxyl and nitro. The present invention has the following main benefits: cheap and readily available starting materials, safe processes, high yield, good quality, which facilitates industrial production.
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公开(公告)号：US20180369386A1
公开(公告)日：2018-12-27
申请号：US16115883
申请日：2018-08-29
申请人： Novartis AG
发明人： Jeremy Lee Baryza , Rohan Eric John Beckwith , Keith Bowman , Crystal Byers , Tanzina Fazal , Gabriel Grant Gamber , Cameron Chuck-Munn Lee , Ritesh Bhanudasji Tichkule , Chandra Vargeese , Shuangxi Wang , Laura West , Thomas Zabawa , Junping Zhao
IPC分类号： A61K47/18 , C07C229/14 , A61K9/127 , A61K9/51 , C12N15/113 , C07D317/28 , C07D295/096 , C07D213/79 , C07D213/69 , C07D205/04 , C07C235/42 , A61K9/00 , C07C229/12 , C07C219/06 , C07C217/58 , A61K47/22 , A61K38/22 , A61K31/713 , A61K48/00
摘要： This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
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公开(公告)号：US20180251458A1
公开(公告)日：2018-09-06
申请号：US15971749
申请日：2018-05-04
IPC分类号： C07D417/14 , C07D405/12 , C07D409/12 , C07D417/12 , C07D413/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D213/79 , C07D401/12 , C07D403/12
CPC分类号： C07D417/14 , A61P35/00 , C07D213/79 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
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25.发明申请公开(公告)号：US20180230102A1
公开(公告)日：2018-08-16
申请号：US15750205
申请日：2016-08-31
发明人： Xinye YANG , Changwei HUANG , Facheng MA , Ji ZHANG , Xiaojun WANG , Yingjun ZHANG
IPC分类号： C07D215/48 , A61K31/47 , C07D209/42 , A61K31/404 , C07D307/85 , A61K31/343 , C07C255/57 , A61K31/277 , C07D307/84 , C07D261/20 , A61K31/423 , C07D209/10 , C07D277/56 , A61K31/426 , C07D249/18 , A61K31/4192 , C07D231/56 , A61K31/416 , C07D317/68 , A61K31/36 , C07D307/83 , C07D209/08 , C07D213/79 , A61K31/4418 , C07D215/18 , C07D215/16 , C07D215/06 , C07D333/62 , A61K31/381 , C07D333/70 , C07D471/04 , A61K31/437 , C07D235/06 , A61K31/4184 , C07D263/56 , C07D277/64 , A61K31/428 , C07D487/04 , A61K31/519 , C07D405/04 , A61K31/443 , C07D237/30 , A61K31/502 , A61K45/06 , A61P13/02
CPC分类号： C07D215/48 , A61K31/277 , A61K31/33 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/42 , A61K31/423 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/44 , A61K31/4418 , A61K31/443 , A61K31/47 , A61K31/502 , A61K31/517 , A61K31/519 , A61K45/06 , A61P13/02 , C07C255/57 , C07C2602/06 , C07C2602/08 , C07D209/04 , C07D209/08 , C07D209/10 , C07D209/30 , C07D209/42 , C07D213/79 , C07D215/02 , C07D215/06 , C07D215/16 , C07D215/18 , C07D231/56 , C07D235/06 , C07D235/08 , C07D237/28 , C07D237/30 , C07D249/18 , C07D261/20 , C07D263/54 , C07D263/56 , C07D277/56 , C07D277/64 , C07D291/08 , C07D307/79 , C07D307/82 , C07D307/83 , C07D307/84 , C07D307/85 , C07D317/64 , C07D317/68 , C07D333/54 , C07D333/62 , C07D333/70 , C07D405/04 , C07D471/04 , C07D487/04
摘要： Carboxy-substituted (hetero)aryl derivatives, pharmaceutical compositions comprising these compounds, and methods of preparing such compounds and compositions are provided. The compounds or compositions are useful in inhibiting xanthine oxidase and urate anion transporter 1, and also can be used in the treatment or prevention of diseases associated with high blood uric acid level in mammals, especially humans.
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公开(公告)号：US10045972B2
公开(公告)日：2018-08-14
申请号：US15389182
申请日：2016-12-22
申请人： BioTheryX, Inc.
IPC分类号： C07D213/79 , A61K31/4418
摘要： Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods for treating, preventing, or ameliorating one or more symptoms of an inflammatory, neurodegenerative, or immune-mediated disease (e.g., multiple sclerosis).
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公开(公告)号：US10011552B2
公开(公告)日：2018-07-03
申请号：US15032298
申请日：2014-06-19
IPC分类号： C07D213/08 , C07D213/79 , C07D213/803 , C07D215/08 , C07D215/18 , A01N33/08 , A01N37/00 , A01N37/40 , A01N39/04 , A01N43/40 , A01N43/42 , C07C51/41 , C07C51/42 , A01N25/12 , A01N37/10 , C07C51/47 , C07C59/68 , C07C65/21 , C07C213/08 , C07C215/08
CPC分类号： C07C51/412 , A01N25/12 , A01N33/08 , A01N37/10 , A01N37/40 , A01N39/04 , A01N43/40 , A01N43/42 , C07C51/42 , C07C51/47 , C07C59/68 , C07C65/21 , C07C213/08 , C07C215/08 , C07D213/79 , C07D213/803 , C07D215/18
摘要： A process for preparing a herbicidally active carboxylic acid salt is disclosed. The process comprises the steps of: i) combining a carboxylic acid with a high-boiling, water-immiscible organic solvent to obtain a solution or slurry; ii) treating the solution or slurry produced in step (i) with a base to form a carboxylic acid salt; iii) removing solvent from the mixture produced in step (ii) to obtain a carboxylic acid salt cake; and v) drying the cake obtained in step (iii). The process is particularly suitable for preparing a salt of dicamba.
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公开(公告)号：US09994561B2
公开(公告)日：2018-06-12
申请号：US15792570
申请日：2017-10-24
IPC分类号： C07D417/14 , C07D405/14 , C07D403/12 , C07D401/12 , C07D213/79 , C07D409/14 , C07D403/14 , C07D413/12 , C07D417/12 , C07D409/12 , C07D405/12
CPC分类号： C07D417/14 , A61P35/00 , C07D213/79 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
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公开(公告)号：US09944657B2
公开(公告)日：2018-04-17
申请号：US13589027
申请日：2012-08-17
申请人： Niko Meltola , Harri Takalo
发明人： Niko Meltola , Harri Takalo
IPC分类号： C07F5/00 , G01N21/64 , C07D213/79
CPC分类号： C07F5/003 , C07D213/79 , G01N21/6486
摘要： The present application discloses a luminescent lanthanide chelate of formula (I) with lanthanides such as europium, as well as the corresponding luminescence lanthanide chelating ligand. The application also discloses a detectable molecule comprising a biospecific binding reactant (such as an antibody) conjugated to the luminescent lanthanide chelate as well as a method of carrying out a biospecific binding assay, the use of such a detectable molecule in a specific bioaffinity based assay, the use of such a detectable molecule in a specific bioaffinity based binding assay utilizing time-resolved fluorometric determination of a specific luminescence, and a solid support material conjugated with the luminescent lanthanide chelate.
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公开(公告)号：US20180057455A1
公开(公告)日：2018-03-01
申请号：US15689115
申请日：2017-08-29
发明人： KAP-SUN YEUNG , Katharine A. Grant-Young , Juliang Zhu , Mark G. Saulnier , David B. Frennesson , David R. Langley , Piyasena Hewawasam , Tao Wang , Zhongxing Zhang , Zhaoxing Meng , Li-Qiang Sun , Eric Mull , Paul Michael Scola
IPC分类号： C07D207/12 , C07D211/66 , C07D207/16 , C07D403/12 , C07D401/12 , C07D207/14 , C07D211/22 , C07D213/38 , C07D401/14 , C07C237/06 , C07D295/088 , C07D205/04 , C07D213/85 , C07C217/18 , C07D213/73 , C07D405/12 , C07C255/24 , C07D413/14 , C07D405/14 , C07D213/79 , C07D231/12 , C07D239/26 , C07D277/28 , C07D211/90
CPC分类号： C07D207/12 , C07C217/18 , C07C217/28 , C07C217/58 , C07C229/14 , C07C235/08 , C07C237/04 , C07C237/06 , C07C255/24 , C07C255/25 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/66 , C07D211/90 , C07D213/38 , C07D213/42 , C07D213/55 , C07D213/73 , C07D213/79 , C07D213/85 , C07D231/12 , C07D239/26 , C07D277/28 , C07D295/088 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12
摘要： The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
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