公开(公告)号：US11986442B2

公开(公告)日：2024-05-21

申请号：US17339620

申请日：2021-06-04

申请人： The Regents of the University of California

发明人： Muhammad Hagras ,  Alexei Stuchebrukhov

IPC分类号： A61K31/047 ,  A61K31/05 ,  A61K31/09 ,  A61K31/12 ,  A61K31/122 ,  A61K31/192 ,  A61K31/196 ,  A61K31/351 ,  A61K31/353 ,  A61K31/404 ,  A61K31/416 ,  A61K31/5513 ,  A61P35/00 ,  C07C35/42 ,  C07C43/295 ,  C07C49/577 ,  C07C205/45 ,  C07C271/58 ,  C07C317/44 ,  C07D243/24 ,  C07D309/14 ,  C07D407/04 ,  C07D493/04

CPC分类号： A61K31/047 ,  A61K31/05 ,  A61K31/09 ,  A61K31/12 ,  A61K31/122 ,  A61K31/192 ,  A61K31/196 ,  A61K31/351 ,  A61K31/353 ,  A61K31/404 ,  A61K31/416 ,  A61K31/5513 ,  A61P35/00 ,  C07C35/42 ,  C07C43/295 ,  C07C49/577 ,  C07C205/45 ,  C07C271/58 ,  C07C317/44 ,  C07D243/24 ,  C07D309/14 ,  C07D407/04 ,  C07D493/04

摘要： The present invention provides methods for inhibiting respiratory complex III in a cell. The present invention also provides methods for treating cancer in a subject.

公开(公告)号：US20210309617A1

公开(公告)日：2021-10-07

申请号：US17339620

申请日：2021-06-04

申请人： The Regents of the University of California

发明人： Muhammad Hagras ,  Alexei Stuchebrukhov

IPC分类号： C07D243/24 ,  C07C205/45 ,  C07C49/577 ,  C07C317/44 ,  C07C43/295 ,  C07C35/42 ,  C07C271/58 ,  C07D309/14 ,  C07D493/04 ,  C07D407/04

摘要： The present invention provides methods for inhibiting respiratory complex III in a cell. The present invention also provides methods for treating cancer in a subject.

公开(公告)号：US20190047932A1

公开(公告)日：2019-02-14

申请号：US16107532

申请日：2018-08-21

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

发明人： Jane B. Neckers ,  Yeong Sang Kim ,  Sunmin Lee ,  Vineet Kumar ,  Sanjay V. Malhotra

IPC分类号： C07C49/796 ,  C07C49/84 ,  C07C49/813 ,  C07C49/80 ,  A61K45/06 ,  A61K31/12 ,  C07C255/56 ,  C07C205/45 ,  A61K31/275

摘要： Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.

公开(公告)号：US20180222873A1

公开(公告)日：2018-08-09

申请号：US15946601

申请日：2018-04-05

申请人： E.I. DU PONT DE NEMOURS AND COMPANY

发明人： Gary David Annis

IPC分类号： C07D261/04 ,  C07C17/35 ,  C07C45/45 ,  C07C45/70 ,  C07C49/80 ,  C07C49/813 ,  C07C67/343 ,  C07C205/45 ,  C07C209/74 ,  C07C231/12 ,  C07C231/14 ,  C07C235/84 ,  C07D213/40 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D249/08 ,  C07D249/10 ,  C07D277/28

CPC分类号： C07D261/04 ,  C07C17/35 ,  C07C25/13 ,  C07C45/455 ,  C07C45/70 ,  C07C49/80 ,  C07C49/813 ,  C07C67/343 ,  C07C205/45 ,  C07C209/74 ,  C07C231/12 ,  C07C231/14 ,  C07C235/84 ,  C07D213/40 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D249/08 ,  C07D249/10 ,  C07D277/28 ,  C07C69/94 ,  C07C69/76 ,  C07C211/56

摘要： Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is OR11 or NR12R13, and R11, R12 and R13 are as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.

公开(公告)号：US09938248B2

公开(公告)日：2018-04-10

申请号：US15798330

申请日：2017-10-30

申请人： E.I. DU PONT DE NEMOURS AND COMPANY

发明人： Gary David Annis

IPC分类号： C07C25/06 ,  C07D261/04 ,  C07C209/74 ,  C07C45/70 ,  C07D231/16 ,  C07C49/813 ,  C07C231/14 ,  C07D231/12 ,  C07D231/14 ,  C07C49/80 ,  C07C45/45 ,  C07C205/45 ,  C07C231/12 ,  C07D213/40 ,  C07D249/08 ,  C07C17/35 ,  C07D277/28 ,  C07C67/343 ,  C07C235/84 ,  C07D249/10

CPC分类号： C07D261/04 ,  C07C17/35 ,  C07C25/13 ,  C07C45/455 ,  C07C45/70 ,  C07C49/80 ,  C07C49/813 ,  C07C67/343 ,  C07C205/45 ,  C07C209/74 ,  C07C231/12 ,  C07C231/14 ,  C07C235/84 ,  C07D213/40 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D249/08 ,  C07D249/10 ,  C07D277/28 ,  C07C69/94 ,  C07C69/76 ,  C07C211/56

摘要： Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is OR11 or NR12R13, and R11, R12 and R13 are as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.

公开(公告)号：US20180057468A1

公开(公告)日：2018-03-01

申请号：US15798330

申请日：2017-10-30

申请人： E.I. DU PONT DE NEMOURS AND COMPANY

发明人： Gary David Annis

IPC分类号： C07D261/04 ,  C07D277/28 ,  C07C17/35 ,  C07D249/08 ,  C07D231/16 ,  C07D231/14 ,  C07D231/12 ,  C07D213/40 ,  C07C235/84 ,  C07C231/14 ,  C07C231/12 ,  C07C209/74 ,  C07C205/45 ,  C07C67/343 ,  C07C49/813 ,  C07C49/80 ,  C07C45/70 ,  C07C45/45 ,  C07D249/10

CPC分类号： C07D261/04 ,  C07C17/35 ,  C07C25/13 ,  C07C45/455 ,  C07C45/70 ,  C07C49/80 ,  C07C49/813 ,  C07C67/343 ,  C07C205/45 ,  C07C209/74 ,  C07C231/12 ,  C07C231/14 ,  C07C235/84 ,  C07D213/40 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D249/08 ,  C07D249/10 ,  C07D277/28 ,  C07C69/94 ,  C07C69/76 ,  C07C211/56

摘要： Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is OR11 or NR12R13, and R11, R12 and R13 are as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.

公开(公告)号：US20170217865A1

公开(公告)日：2017-08-03

申请号：US15515271

申请日：2015-10-07

申请人： SYNGENTA PARTICIPATIONS AG

发明人： Denis GRIBKOV

IPC分类号： C07C45/63 ,  C07C201/08 ,  C07C205/45 ,  C07C45/46

CPC分类号： C07C45/63 ,  C07C45/46 ,  C07C201/08 ,  C07C201/12 ,  C07C205/45 ,  C07C49/80

摘要： A process for the preparation of a compound of formula (I) wherein R1 is hydrogen, fluoro or chloro; which process comprises: a) reacting a compound of formula (II) wherein R1 is hydrogen, fluoro or chloro; with a nitration agent to the compound of formula (III) wherein R1 is hydrogen, fluoro or chloro; b) reacting the compound of formula (III) with trichloroisocyanuric acid in the presence of sulfuric acid or fuming sulfuric acid to the compound of formula (IV) wherein R1 is hydrogen, fluoro or chloro; and c) reacting the compound of formula (III) with chlorine gas at a temperature from 180° C. to 250° C. to the compound of formula (I).

公开(公告)号：US09034439B2

公开(公告)日：2015-05-19

申请号：US13539520

申请日：2012-07-02

申请人： Tahsin J. Chow ,  Chung-Chih Wu ,  Ta-Hsien Chuang ,  Hsing-Hung Hsieh ,  Hsin-Hui Huang

发明人： Tahsin J. Chow ,  Chung-Chih Wu ,  Ta-Hsien Chuang ,  Hsing-Hung Hsieh ,  Hsin-Hui Huang

IPC分类号： C07C25/22 ,  C07C49/665 ,  C07C49/683 ,  C07C49/753 ,  C07D333/08 ,  C07C205/45 ,  C07C255/56 ,  B05D1/32 ,  B05D3/02 ,  B05D3/06 ,  H01L51/00

CPC分类号： C07C25/22 ,  B05D1/327 ,  B05D3/0254 ,  B05D3/06 ,  C07C49/665 ,  C07C49/683 ,  C07C49/753 ,  C07C205/45 ,  C07C255/56 ,  C07C2603/86 ,  C07C2603/90 ,  C07D333/08 ,  H01L51/0003 ,  H01L51/0055 ,  H01L51/0068 ,  Y02E10/549

摘要： The present disclosure relates to methods and systems for synthesis of bridged-hydropentacene, hydroanthracene and hydrotetracene from the precursor compounds pentacene derivatives, tetracene derivatives, and anthracene derivatives. The invention further relates to methods and systems for forming thin films for use in electrically conductive assemblies, such as semiconductors or photovoltaic devices.

摘要翻译： 本公开内容涉及从前体化合物并五苯衍生物，并四苯衍生物和蒽衍生物合成桥联 - 水合氢，氢蒽和氢化四苯的方法和系统。 本发明还涉及用于形成用于诸如半导体或光伏器件的导电组件中的薄膜的方法和系统。

公开(公告)号：US20130079396A1

公开(公告)日：2013-03-28

申请号：US13623161

申请日：2012-09-20

申请人： Council of Scientific and Industrial Research

发明人： Arvind Singh Negi ,  Ayyampudur Palanisamy Prakasham ,  Ajit Kumar Saxena ,  Suaib Luqman ,  Debabrata Chanda ,  Tandeep Kaur ,  Atul Gupta

IPC分类号： C07C49/755 ,  C07C201/12 ,  C07C45/72 ,  C07D317/54 ,  C07C205/45

CPC分类号： C07C49/755 ,  C07C45/72 ,  C07C45/74 ,  C07C201/12 ,  C07C205/45 ,  C07C2102/08 ,  C07C2602/08 ,  C07D317/54

摘要： The present invention relates to benzylidene indanones of general formula 1. The compounds exhibited tubulin polymerisation inhibition. A series of compounds 2-benzylidene 3-(3,4,5-trimethoxyphenyl) indanones having general formulae 1 were synthesized from gallic acid through a chemical process. 2-(3,4-Methylenedioxybenzylidine), 3-(3,4,5-trimethoxyphenyl), 4,5,6-trimethoxyindanone (8), a representative compound of this series possessing the molecular formulae C29H28O9, was synthesized from gallic acid and exhibits potent anticancer activity. Compound 8 was evaluated for acute oral activity in Swiss albino mice and found to be safe up to 300 mg/kg body weight. The anticancer activity of the compounds has been determined, in order to obtain new potent and cost effective molecules using an in vitro cytotoxicity assay.

摘要翻译： 本发明涉及通式1的亚苄基茚满酮。该化合物表现出微管蛋白聚合抑制作用。 通过化学方法由没食子酸合成一系列化合物，具有通式1的2-亚苄基3-（3,4,5-三甲氧基苯基）茚满酮。 2-（3,4-亚甲基二氧基亚苄基），3-（3,4,5-三甲氧基苯基），4,5,6-三甲氧基茚满酮（8），具有分子式C29H28O9的该系列的代表性化合物，由没食子酸 并具有很强的抗癌活性。 评估化合物8在瑞士白化病小鼠中的急性口服活性，发现其安全性高达300mg / kg体重。 已经确定了化合物的抗癌活性，以便使用体外细胞毒性测定来获得新的有效和成本有效的分子。

公开(公告)号：US20120004424A1

公开(公告)日：2012-01-05

申请号：US12782706

申请日：2010-05-18

申请人： GUOFU ZHONG ,  BIN TAN ,  XUAN ZHANG ,  PEI JUAN CHUA

发明人： GUOFU ZHONG ,  BIN TAN ,  XUAN ZHANG ,  PEI JUAN CHUA

IPC分类号： C07C205/45 ,  C07D307/46 ,  C07D333/22

CPC分类号： C07D333/22 ,  C07C201/12 ,  C07D307/46 ,  C07D401/06 ,  C07C205/45

摘要： Disclosed is a process of carrying out a Michael reaction with recovery of the catalyst, where a compound of formula (1): is reacted with a compound of formula (2): in the presence of a catalyst of formula (4): where the compounds of formulae (1) and (2) undergo a Michael reaction.

摘要翻译： 公开了一种通过回收催化剂进行迈克尔反应的方法，其中式（1）化合物与式（2）化合物在式（4）的催化剂存在下反应：其中 式（1）和（2）的化合物经历迈克尔反应。