公开(公告)号：USRE50083E1

公开(公告)日：2024-08-20

申请号：US17707795

申请日：2022-03-29

申请人： Jiangsu Atom Bioscience and Pharmaceutical Co., Ltd.

发明人： Dongfang Shi ,  Changjin Fu ,  Xi Cheng ,  Jianghua Zhu ,  Jie Gu

IPC分类号： C07D487/04 ,  A61P3/00 ,  C07D307/80 ,  C07D471/04 ,  C07D491/048 ,  C07D513/04

CPC分类号： C07D487/04 ,  A61P3/00 ,  C07D307/80 ,  C07D471/04 ,  C07D491/048 ,  C07D513/04

摘要： Disclosed are a class of URAT1 inhibitor compounds and the use of such compounds. These compounds are compounds represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on hURAT1-transported uric acid in HEK293 transfected cells, and show that such compounds have a good potential for application in the treatment of hyperuricemia or gout.

公开(公告)号：US20240158379A1

公开(公告)日：2024-05-16

申请号：US17721178

申请日：2022-04-14

申请人： OLIGOMERIX INC.

发明人： Eliot J. Davidowitz ,  James G. Moe ,  Allen B. Reitz ,  Haiyan Bian ,  Charles Gluchowski ,  James Hendrix ,  Albert S. Yehaskel ,  Mark E. McDonnell ,  H. Marie Loughran

IPC分类号： C07D409/14 ,  C07D307/80 ,  C07D405/14

CPC分类号： C07D409/14 ,  C07D307/80 ,  C07D405/14

摘要： Novel benzofurans, benzothiophenes and indoles useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.

公开(公告)号：US20230373900A1

公开(公告)日：2023-11-23

申请号：US18198423

申请日：2023-05-17

申请人： FUNDACIÓ INSTITUT CATALÀ D'INVESTIGACIÓ QUÍMICA

发明人： Marcos GARCÍA SUERO ,  Hangfei TU ,  Aliénor JEANDIN

IPC分类号： C07C69/743 ,  C07D209/08 ,  C07D209/38 ,  C07D333/24 ,  C07D307/80 ,  C07D213/69 ,  C07D223/24 ,  C07D495/04 ,  C07D295/088 ,  C07J51/00 ,  C07D405/12 ,  C07D239/04 ,  C07F5/02 ,  C07D213/64 ,  C07C67/00 ,  C07D207/22 ,  C07D209/26 ,  C07C233/15 ,  C07C231/12

CPC分类号： C07C69/743 ,  C07D209/08 ,  C07D209/38 ,  C07D333/24 ,  C07D307/80 ,  C07D213/69 ,  C07D223/24 ,  C07D495/04 ,  C07D295/088 ,  C07J51/00 ,  C07D405/12 ,  C07D239/04 ,  C07F5/022 ,  C07D213/64 ,  C07C67/00 ,  C07D207/22 ,  C07D209/26 ,  C07C233/15 ,  C07C231/12 ,  C07C2601/02

摘要： The present invention relates to a cyclopropenium salt bearing an electron withdrawing group suitable for use as a reagent in cyclopropenylation reactions of formula (I). The invention also relates to a process for their preparation, the use thereof as cyclopropenylation reagent, to an electrophilic aromatic substitution process of cyclopropenylation, and to a process for cyclopropenylation of organometallic substrates using said reagents.

公开(公告)号：US20180369190A1

公开(公告)日：2018-12-27

申请号：US16063622

申请日：2016-12-22

申请人： MCMASTER UNIVERSITY

发明人： Sukhbinder Dhesy-Thind ,  Katarzyna J. Jerzak ,  Anita Bane ,  Jessica G. Cockburn ,  John A. Hassell

IPC分类号： A61K31/343 ,  A61P5/14 ,  A61K31/12 ,  C07C49/215 ,  A61K31/192 ,  C07C59/68 ,  C07D307/80 ,  A61K45/06

CPC分类号： A61K31/343 ,  A61K31/12 ,  A61K31/192 ,  A61K45/06 ,  A61P5/14 ,  A61P35/00 ,  C07C49/215 ,  C07C59/68 ,  C07D307/80

摘要： Two isoforms of thyroid receptor alpha (THRα1 and THRα2) have been found to be associated with the growth of cancer. Use of inhibitors of THRα1 (Formula I) and/or agonists of THRα2 (Formula II) in the treatment of such cancers is disclosed. Treatment of other disorders associated with such receptors is also contemplated, as is the use of diagnostic methods for predicting therapeutic outcomes based on the levels of expression of THRα1 and THRaα2 in a tissue sample.

公开(公告)号：US20180346433A1

公开(公告)日：2018-12-06

申请号：US15774638

申请日：2016-11-10

申请人： WARNER BABCOCK INSTITUTE FOR GREEN CHEMISTRY

发明人： John C. Warner ,  Srinivasa R. Cheruku ,  Jeffery A. Gladding

IPC分类号： C07D307/80 ,  C07D307/81

CPC分类号： C07D307/80 ,  A61K31/343 ,  C07D307/81

摘要： The present application discloses 2-phenyl benzofuran derivative compounds and compositions, and methods for treating ocular diseases, neurological disorders and protein aggregation-related disorders in patients using the compounds and compositions as disclosed herein.

公开(公告)号：US09957258B2

公开(公告)日：2018-05-01

申请号：US14917508

申请日：2014-09-08

申请人： BASF SE

发明人： Kazuhiko Kunimoto ,  Hisatoshi Kura ,  Hiroshi Yamamoto ,  Yumiko Nakagawa ,  Toshikage Asakura ,  Kaori Sameshima

IPC分类号： G03F7/031 ,  C07D409/06 ,  C07D209/12 ,  C07D307/56 ,  C07D307/80 ,  C07D307/92 ,  C07D307/83 ,  C07D307/86 ,  C07D307/91 ,  C07D333/56 ,  C07D407/12 ,  G02B5/20 ,  G02B5/22 ,  G03F7/00 ,  G03F7/20 ,  G03F7/32

CPC分类号： C07D409/06 ,  C07D209/12 ,  C07D307/56 ,  C07D307/80 ,  C07D307/83 ,  C07D307/86 ,  C07D307/91 ,  C07D307/92 ,  C07D333/56 ,  C07D407/12 ,  G02B5/201 ,  G02B5/223 ,  G03F7/0007 ,  G03F7/031 ,  G03F7/20 ,  G03F7/32

摘要： Disclosed are oxime ester compounds which have specific benzo (unsaturated 5-membered ring)-carbonyl group and their use as photoinitiators in photopolymerizable compositions, in particular in photoresist formulations for display applications, e.g. liquid crystal display (LCD), organic light emitting diode (OLED) and touch panel.

公开(公告)号：US09890132B2

公开(公告)日：2018-02-13

申请号：US14914378

申请日：2014-08-25

申请人： COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

发明人： Chepuri Venkata Ramana ,  Yadagiri Kommagalla ,  Kolluru Srinivas

IPC分类号： C07D307/80

CPC分类号： C07D307/80

摘要： Disclosed herein an efficient process for synthesis of benzofuran analogs having anti-inflammatory activity which comprises, Ru-catalyzed branched and linear selective alkylation of aroylbenzofurans formula-I with alpha, beta unsaturated esters of formula-II via C—H activation in presence of base, additives and organic solvent at suitable temperature to give high yield of desired linear alkylated benzofuran compounds of formula-III or branched alkylated benzofuran compounds of formula-IV or mixture thereof.

公开(公告)号：US20170369417A1

公开(公告)日：2017-12-28

申请号：US15694982

申请日：2017-09-04

申请人： Emory University

发明人： Huw M. L. Davies ,  Spandan Chennamadhavuni ,  Andrei Bakin

IPC分类号： C07C69/73 ,  A61K31/194 ,  C07D317/60 ,  C07D307/80 ,  C07D307/79 ,  C07D209/34 ,  C07D209/26 ,  C07D209/24 ,  C07C259/06 ,  C07C205/56 ,  C07C201/12 ,  C07C69/738 ,  C07C69/736 ,  C07C69/734 ,  C07C69/732 ,  C07C69/65 ,  C07C69/618 ,  C07C69/604 ,  C07C67/31 ,  C07C57/42 ,  C07C51/00 ,  A61K31/405 ,  A61K31/36 ,  A61K31/357 ,  A61K31/343 ,  A61K31/216 ,  C07D317/68 ,  C07D319/18

CPC分类号： C07C69/73 ,  A61K31/194 ,  A61K31/216 ,  A61K31/343 ,  A61K31/357 ,  A61K31/36 ,  A61K31/405 ,  C07C51/00 ,  C07C57/42 ,  C07C67/31 ,  C07C69/604 ,  C07C69/618 ,  C07C69/65 ,  C07C69/732 ,  C07C69/734 ,  C07C69/736 ,  C07C69/738 ,  C07C201/12 ,  C07C205/56 ,  C07C259/06 ,  C07D209/24 ,  C07D209/26 ,  C07D209/34 ,  C07D307/79 ,  C07D307/80 ,  C07D317/60 ,  C07D317/68 ,  C07D319/18

摘要： The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I, pharmaceutical compositions having a compound of formula I, and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula I to a subject in need thereof.

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：US09822058B2

公开(公告)日：2017-11-21

申请号：US14390190

申请日：2013-03-13

申请人： CHDI FOUNDATION, INC.

发明人： Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Michael Prime ,  William Leonard Mitchell ,  Peter Johnson ,  Naomi Went

IPC分类号： C07C62/38 ,  C07D307/94 ,  C07D309/10 ,  C07D215/18 ,  C07D311/58 ,  C07D317/46 ,  C07D317/60 ,  C07D319/18 ,  C07D233/64 ,  C07D235/26 ,  C07D403/10 ,  C07D405/08 ,  C07D405/10 ,  C07D405/12 ,  C07C317/44 ,  C07D413/08 ,  C07D413/10 ,  C07C323/62 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07D257/04 ,  C07D203/08 ,  C07D263/58 ,  C07C235/82 ,  C07D207/08 ,  C07D271/07 ,  C07D207/337 ,  C07D295/155 ,  C07D305/06 ,  C07D305/08 ,  C07D307/54 ,  C07D307/80 ,  C07C69/757 ,  C07D203/10 ,  C07D307/79 ,  C07D413/12 ,  C07H15/20

CPC分类号： C07C62/38 ,  C07C69/757 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07C235/82 ,  C07C317/44 ,  C07C323/62 ,  C07C2601/02 ,  C07C2602/50 ,  C07D203/08 ,  C07D203/10 ,  C07D207/08 ,  C07D207/337 ,  C07D215/18 ,  C07D233/64 ,  C07D235/26 ,  C07D257/04 ,  C07D263/58 ,  C07D271/07 ,  C07D295/155 ,  C07D305/06 ,  C07D305/08 ,  C07D307/54 ,  C07D307/79 ,  C07D307/80 ,  C07D307/94 ,  C07D309/10 ,  C07D311/58 ,  C07D317/46 ,  C07D317/60 ,  C07D319/18 ,  C07D403/10 ,  C07D405/08 ,  C07D405/10 ,  C07D405/12 ,  C07D413/08 ,  C07D413/10 ,  C07D413/12 ,  C07H15/20

摘要： Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.