公开(公告)号：US20230210808A1

公开(公告)日：2023-07-06

申请号：US18120484

申请日：2023-03-13

申请人： Janssen Pharmaceutica NV

发明人： Gee-Hong Kuo ,  Rui Zhang ,  Aihua Wang ,  Alan R. DeAngelis

IPC分类号： A61K31/277 ,  A61K31/192 ,  C07C59/68 ,  C07C59/70 ,  C07C317/22 ,  C07C323/60 ,  C07C323/62 ,  C07D333/16 ,  C07D333/28 ,  C07C323/20

CPC分类号： A61K31/277 ,  A61K31/192 ,  C07C59/68 ,  C07C59/70 ,  C07C317/22 ,  C07C323/60 ,  C07C323/62 ,  C07D333/16 ,  C07D333/28 ,  C07C323/20

摘要： The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.

公开(公告)号：US20230151060A1

公开(公告)日：2023-05-18

申请号：US17773733

申请日：2020-11-05

申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA

发明人： Mikimasa TANADA ,  Koji TAKANO ,  Atsushi MATSUO ,  Minoru TAMIYA ,  Aya CHIYODA ,  Toshiya ITO ,  Takeo IIDA

IPC分类号： C07K7/64 ,  C07D211/38 ,  C07C271/22 ,  C07D213/55 ,  C07D213/65 ,  C07D213/64 ,  C07D213/61 ,  C07D205/04 ,  C07C323/09 ,  C07F5/02 ,  C07D309/12 ,  C07C317/04 ,  C07D409/12 ,  C07D333/28 ,  C07D295/15

CPC分类号： C07K7/64 ,  C07D211/38 ,  C07C271/22 ,  C07D213/55 ,  C07D213/65 ,  C07D213/64 ,  C07D213/61 ,  C07D205/04 ,  C07C323/09 ,  C07F5/025 ,  C07D309/12 ,  C07C317/04 ,  C07D409/12 ,  C07D333/28 ,  C07D295/15 ,  A61K38/00

摘要： The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.

公开(公告)号：US20230086179A1

公开(公告)日：2023-03-23

申请号：US16472118

申请日：2017-12-18

申请人： Bayer Pharma Aktiengesellschaft

发明人： Stefan BAEURLE ,  Adam James DAVENPORT ,  Christopher STIMSON ,  Jens NAGEL ,  Nicole SCHMIDT ,  Andrea ROTGERI ,  Ina GROETICKE ,  Alexandra RAUSCH ,  Juergen KLAR ,  Thomas DYRKS

IPC分类号： C07D333/28 ,  C07D213/56 ,  C07D231/12 ,  C07D231/56 ,  C07D495/04 ,  C07D333/38 ,  C07D233/64 ,  C07D405/04 ,  C07D277/56 ,  C07D241/12 ,  C07D333/58 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00 ,  A61P19/02 ,  A61P13/10

摘要： The present invention relates to carboxylic acid aromatic amides compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease as a sole agent or in combination with other active ingredients.

公开(公告)号：US20220112153A1

公开(公告)日：2022-04-14

申请号：US17426187

申请日：2019-10-10

申请人： University of Padova ,  MGGM LLC ,  Institute for Research in Biomedicine

发明人： Paolo L. Manfredi ,  Charles E. Inturrisi ,  Andrea Mattarei ,  Sara De Martin ,  Jacopo Sgrignani ,  Andrea Cavalli

IPC分类号： C07C225/16 ,  C07D207/09 ,  C07D209/14 ,  C07D233/64 ,  C07C229/34 ,  C07D295/135 ,  C07C323/29 ,  C07C225/18 ,  C07D319/06 ,  C07D317/58 ,  C07D333/28

摘要： Aspects of the present invention are directed to structurally modified opioids (SMOs) that result in improved modulating activity at the NMDAR and improved PK and PD parameters over existing drugs with NMDAR modulating activity. The structural modifications of an opioid or opioid enantiomer that result in the SMOs can be obtained by starting the synthetic process de novo; by modifying the synthetic process for the opioid at any intermediate step during the synthesis of the racemate or of one enantiomer; or by modifying the structure of the opioid or opioid enantiomer after the synthesis. The nitric acid ester substitutions are of particular relevance, especially when associated to deuterated substitutions and/or halogen substitutions.

公开(公告)号：US10730848B2

公开(公告)日：2020-08-04

申请号：US14801247

申请日：2015-07-16

申请人： The Regents of the University of California

发明人： Eugene Gillespie ,  Robert Damoiseaux ,  Chi-Lee Charlie Ho ,  Brian T. Chamberlain ,  Michael E. Jung ,  Kenneth A. Bradley

IPC分类号： C07D333/28 ,  C07C281/14 ,  C07C335/26 ,  C07D213/53 ,  C07D307/56 ,  C07C281/18 ,  C07C337/08 ,  C07D231/12 ,  C07C243/22 ,  C07C311/08 ,  C07D307/52 ,  C07D333/22

摘要： Disclosed herein inter alia are compositions and methods useful in the treatment of infectious diseases and exposure to toxins.

公开(公告)号：US20200157050A1

公开(公告)日：2020-05-21

申请号：US16752076

申请日：2020-01-24

申请人： Ono Pharmaceutical Co., Ltd.

发明人： Kentaro YASHIRO ,  Daisuke WAKAMATSU ,  Tetsuji SAITO

IPC分类号： C07D213/61 ,  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：US10131659B2

公开(公告)日：2018-11-20

申请号：US15302566

申请日：2015-04-06

申请人： THE UNITED STATES OF AMERICA as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  STARKS ASSOCIATES INC.

发明人： James Halpern Doroshow ,  Prabhakar Risbood ,  Jiamo Lu ,  Krishnendu Roy ,  Charles T. Kane, Jr. ,  Md Tafazzal Hossain

IPC分类号： C07D471/04 ,  C07D347/00 ,  C07C233/15 ,  C07C205/12 ,  C07C43/225 ,  C07D409/14 ,  C07D409/12 ,  C07D333/28 ,  A61K31/381 ,  A61K31/4745

摘要： Disclosed herein are novel iodonium analogs having anticancer and anti-inflammatory activity.

公开(公告)号：US20180319741A1

公开(公告)日：2018-11-08

申请号：US16037396

申请日：2018-07-17

申请人： ELANCO Tiergesundheit AG

发明人： Noelle Gauvry ,  Chouaib Tahtaoui

IPC分类号： C07C311/08 ,  C07F7/08 ,  C07D237/26 ,  C07D487/04 ,  C07D215/06 ,  C07D209/08 ,  C07D317/66 ,  C07D275/03 ,  C07D263/50 ,  C07D277/54 ,  C07D277/46 ,  C07D333/78 ,  C07D285/135 ,  C07D277/56 ,  C07D277/60 ,  C07D277/64 ,  C07D249/08 ,  C07D309/06 ,  C07C311/14 ,  C07C311/21 ,  C07D333/28 ,  C07D213/84 ,  C07D277/30 ,  C07D239/26 ,  C07D239/30 ,  C07D213/56 ,  C07D231/56 ,  C07D213/61 ,  C07D231/12 ,  C07D333/24 ,  C07D295/155 ,  C07F5/02

CPC分类号： C07C311/08 ,  C07C235/56 ,  C07C307/10 ,  C07C311/09 ,  C07C311/10 ,  C07C311/14 ,  C07C311/21 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/40 ,  C07C2602/42 ,  C07D209/08 ,  C07D213/26 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/84 ,  C07D215/06 ,  C07D231/12 ,  C07D231/20 ,  C07D231/56 ,  C07D237/26 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D249/08 ,  C07D249/12 ,  C07D263/50 ,  C07D275/03 ,  C07D277/30 ,  C07D277/46 ,  C07D277/54 ,  C07D277/56 ,  C07D277/60 ,  C07D277/62 ,  C07D277/64 ,  C07D279/12 ,  C07D285/135 ,  C07D295/155 ,  C07D295/185 ,  C07D295/26 ,  C07D309/06 ,  C07D317/66 ,  C07D333/24 ,  C07D333/28 ,  C07D333/78 ,  C07D487/04 ,  C07F5/025 ,  C07F7/081 ,  C07F7/0812

摘要： The present invention relates to a new compound of formula (I) wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endoparasites, in and on vertebrates.

公开(公告)号：US20180215745A1

公开(公告)日：2018-08-02

申请号：US15851434

申请日：2017-12-21

申请人： CHDI Foundation, Inc.

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

IPC分类号： C07D413/12 ,  C07D231/56 ,  C07D215/18 ,  C07D333/06 ,  C07D241/42 ,  C07D277/24 ,  C07D277/64 ,  C07D213/46 ,  C07D307/79 ,  C07D263/56 ,  C07D261/20 ,  C07D239/74 ,  C07D237/28 ,  C07D235/08 ,  C07D217/02 ,  C07D209/08 ,  C07D407/12 ,  C07D333/28 ,  C07D333/10 ,  C07D319/18

CPC分类号： C07D413/12 ,  A61K31/343 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/47 ,  A61K31/502 ,  A61K31/517 ,  C07D209/08 ,  C07D213/46 ,  C07D215/18 ,  C07D217/02 ,  C07D231/56 ,  C07D235/08 ,  C07D237/28 ,  C07D239/74 ,  C07D241/42 ,  C07D261/20 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D307/79 ,  C07D319/18 ,  C07D333/06 ,  C07D333/10 ,  C07D333/28 ,  C07D407/12

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.

公开(公告)号：US10035760B2

公开(公告)日：2018-07-31

申请号：US15031352

申请日：2014-10-23

申请人： VIIV HEALTHCARE UK (NO. 5) LIMITED

发明人： Annapurna Pendri ,  Guo Li ,  John A. Bender ,  Zhong Yang ,  Alan Xiangdong Wang ,  Brett R. Beno ,  Robert A. Fridell ,  Makonen Belema ,  Nicholas A. Meanwell ,  Robert G. Gentles

IPC分类号： A61K31/36 ,  A61K31/357 ,  A61K31/64 ,  A61K31/17 ,  A61K31/18 ,  C07C275/28 ,  C07C275/26 ,  C07C275/18 ,  C07C275/24 ,  C07C275/22 ,  C07C311/62 ,  C07C311/59 ,  C07C311/58 ,  C07C311/56 ,  C07C311/55 ,  C07D317/66 ,  C07D317/62 ,  C07D205/04 ,  C07D209/08 ,  C07D209/10 ,  C07D213/56 ,  C07D215/08 ,  C07D231/12 ,  C07D249/08 ,  C07D261/08 ,  C07D265/36 ,  C07D271/06 ,  C07D277/82 ,  C07D307/38 ,  C07D317/46 ,  C07D333/18 ,  C07D333/28 ,  C07D333/54 ,  C07D401/04 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D491/08 ,  C07D495/04

CPC分类号： C07C311/58 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D205/04 ,  C07D209/08 ,  C07D209/10 ,  C07D213/56 ,  C07D215/08 ,  C07D231/12 ,  C07D249/08 ,  C07D261/08 ,  C07D265/36 ,  C07D271/06 ,  C07D277/82 ,  C07D307/38 ,  C07D317/46 ,  C07D317/66 ,  C07D333/18 ,  C07D333/28 ,  C07D333/54 ,  C07D401/04 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D491/08 ,  C07D495/04

摘要： Compounds of Formula I with activity against HIV, including pharmaceutical compositions and methods for using these compounds in treating human immunodeficiency virus (HIV) infection, are set forth: