公开(公告)号：US11913884B2

公开(公告)日：2024-02-27

申请号：US16798992

申请日：2020-02-24

Applicant: William Marsh Rice University

Inventor： Han Xiao ,  Juan Tang

IPC: G01N21/64 ,  C07D265/34 ,  C07D209/32 ,  C07D401/04 ,  B82Y15/00 ,  A61K49/00

CPC classification number: G01N21/6486 ,  C07D209/32 ,  C07D265/34 ,  C07D401/04 ,  G01N21/6428 ,  A61K49/0028 ,  B82Y15/00

Abstract: Disclosed herein are photoactivable fluorophores comprising one or more thiocarbonyl groups as well as conjugates and compositions thereof. The present disclosure also provides methods of preparing photoactivatable fluorophores as well as methods of imaging using the photoactivatable fluorophores, conjugates, and compositions of the present disclosure.

公开(公告)号：US20230212119A1

公开(公告)日：2023-07-06

申请号：US18173717

申请日：2023-02-23

Applicant: Terran Biosciences Inc.

Inventor： Matthew Alexander James DUNCTON ,  Sam CLARK

IPC: C07D209/32 ,  C07D209/14 ,  C07D209/12

CPC classification number: C07D209/32 ,  C07D209/14 ,  C07D209/12

Abstract: Described herein are compounds that are derivatives of DMT or 5-MeO-DMT and can be metabolically converted to N,N-dimethyltryptamine or analogs thereof upon administration to a subject. In certain embodiments, the compounds described herein are useful for the treatment of conditions associated with a neurological disease.

公开(公告)号：US11220507B2

公开(公告)日：2022-01-11

申请号：US16770811

申请日：2017-12-15

Applicant: Advitech Advisory and Technologies SA

Inventor： Brent Christopher Beck ,  Joe B. Perales ,  Jason D. Speake ,  Ilaria Ferrando

IPC: C07D487/06 ,  C07D209/14 ,  C07D403/08 ,  C07D209/32 ,  C07C243/22 ,  C07D487/04 ,  C07D209/48 ,  C07D403/06

Abstract: The present invention relates to a process for the preparation of rucaparib; the invention also refers to novel intermediates of synthesis as well as their use in the preparation of i.a. rucaparib.

公开(公告)号：US10961396B2

公开(公告)日：2021-03-30

申请号：US16155017

申请日：2018-10-09

Applicant: LANXESS Deutschland GmbH

Inventor： Frank Linke ,  Stephan Michaelis ,  Hans-Ulrich Borst

IPC: C07D209/32 ,  C08J3/12 ,  C08J3/20 ,  C08K5/00 ,  C08K5/3417 ,  C08L77/02 ,  C08L77/06 ,  C09B23/01 ,  C09B23/10 ,  D01F1/04 ,  D01F6/60

Abstract: The present invention relates to novel methine dyes, methods for the preparation thereof and use thereof for dyeing plastics, especially polyamides, so as to obtain yellow to orange colourings with improved light fastness and improved thermal stability.

公开(公告)号：US10221129B2

公开(公告)日：2019-03-05

申请号：US15565690

申请日：2016-04-22

Applicant: ViiV HEALTHCARE UK (NO.5) LIMITED

Inventor： John A. Bender ,  Robert G. Gentles ,  Annapurna Pendri ,  Alan Xiangdong Wang ,  Nicholas A. Meanwell ,  Brett R. Beno ,  Robert A. Fridell ,  Makonen Belema ,  Van N. Nguyen ,  Zhong Yang ,  Gan Wang ,  Selvakumar Kumaravel ,  Srinivasan Thangathirupathy ,  Rajesh Onkardas Bora ,  Shilpa Maheshwarappa Holehatti ,  Mallikarjuna Rao Mettu ,  Manoranjan Panda

IPC: C07C307/06 ,  C07C307/10 ,  C07C311/08 ,  A61P31/18 ,  A61K31/65 ,  C07D215/12 ,  C07D215/38 ,  C07D217/08 ,  C07D217/22 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D333/72 ,  C07D235/08 ,  C07D241/04 ,  C07D417/12 ,  C07D417/14 ,  C07D249/12 ,  C07D471/04 ,  C07D261/08 ,  C07D263/32 ,  C07D205/04 ,  C07D207/325 ,  C07D277/28 ,  C07D498/04 ,  C07D209/08 ,  C07D277/62 ,  C07D209/30 ,  C07D209/32 ,  C07D209/86 ,  C07D295/185 ,  C07D211/96 ,  C07D295/26 ,  C07D213/42

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:

公开(公告)号：US09849109B2

公开(公告)日：2017-12-26

申请号：US14628970

申请日：2015-02-23

Applicant: Amira Pharmaceuticals, Inc.

Inventor： Jeffrey Roger Roppe ,  Timothy Andrew Parr ,  Nicholas Simon Stock ,  Deborah Volkots ,  John Howard Hutchinson

IPC: C07D209/36 ,  C07D209/30 ,  A61K31/404 ,  C07D209/08 ,  C07D209/12 ,  C07D209/32 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D409/04 ,  C07D417/04 ,  C07D401/10 ,  C07D403/12 ,  C07F5/02 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  A61K31/69

CPC classification number: A61K31/404 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  A61K31/69 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D209/32 ,  C07D209/36 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D403/12 ,  C07D409/04 ,  C07D417/04 ,  C07F5/025

Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.

公开(公告)号：US09073855B2

公开(公告)日：2015-07-07

申请号：US13839060

申请日：2013-03-15

Applicant: AbbVie Inc.

Inventor： George A. Doherty ,  Steven W. Elmore ,  Lisa Hasvold ,  Laura Hexamer ,  Robert A. Mantei ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Todd M. Hansen

IPC: C07D401/10 ,  C07D213/62 ,  C07D307/02 ,  C07D215/14 ,  C07D209/32 ,  C07D211/96 ,  C07D213/64 ,  C07D215/20 ,  C07D217/16 ,  C07D231/56 ,  C07D235/26 ,  C07D249/04 ,  C07D295/125 ,  C07D295/14 ,  C07D309/14 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D295/13 ,  C07D309/08 ,  C07D487/04 ,  C07D209/20 ,  C07D295/155 ,  C07D309/32

CPC classification number: C07D215/14 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/20 ,  C07D209/32 ,  C07D211/96 ,  C07D213/64 ,  C07D215/20 ,  C07D217/16 ,  C07D231/56 ,  C07D235/26 ,  C07D249/04 ,  C07D295/125 ,  C07D295/13 ,  C07D295/14 ,  C07D295/155 ,  C07D309/08 ,  C07D309/14 ,  C07D309/32 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.

Abstract translation: 公开了抑制抗凋亡Bcl-2或Bcl-xL蛋白的活性的化合物，含有该化合物的组合物和治疗疾病的方法，其中表达抗凋亡Bcl-2蛋白。

公开(公告)号：US08889729B2

公开(公告)日：2014-11-18

申请号：US12794746

申请日：2010-06-06

Applicant: Ehud Gazit ,  Tomer Cohen

Inventor： Ehud Gazit ,  Tomer Cohen

IPC: A61K31/405 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/403 ,  C07D209/12 ,  A61K31/404 ,  C07D209/32

CPC classification number: C07D209/12 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4164 ,  C07D209/32

Abstract: Indole derivatives, compositions including same, and methods utilizing same for the treatment of amyloid associated diseases, such as type II diabetes mellitus, Alzheimer's dementia or diseases, systemic and localized amyloidosis, and prion-related encephalopathies are provided.

Abstract translation: 提供了吲哚衍生物，包含其的组合物及其用于治疗淀粉样蛋白相关疾病如II型糖尿病，阿尔茨海默氏痴呆或疾病，全身和局部淀粉样变性病和朊病毒相关性脑病的方法。

公开(公告)号：US20130281366A1

公开(公告)日：2013-10-24

申请号：US13976598

申请日：2011-12-26

Applicant: Harikishore Pingali ,  Pankaj Makadia ,  Vrajesh Pankaj ,  Sairam Kalapatapu, V.V.M. ,  Mukul R. JAIN

Inventor： Harikishore Pingali ,  Pankaj Makadia ,  Vrajesh Pankaj ,  Sairam Kalapatapu, V.V.M. ,  Mukul R. JAIN

IPC: C07D405/12 ,  A61K31/351 ,  A61K31/4433 ,  A61K31/404 ,  A61K31/5377 ,  A61K31/541 ,  C07D409/12 ,  A61K31/381 ,  A61K31/506 ,  C07D413/12 ,  A61K31/422 ,  A61K31/4155 ,  A61K31/4709 ,  A61K45/06 ,  C07D213/64 ,  C07D263/38 ,  C07D215/06 ,  C07D239/28 ,  C07D209/32 ,  C07D309/04

CPC classification number: C07D309/04 ,  A61K31/137 ,  A61K31/351 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/4433 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D209/32 ,  C07D213/64 ,  C07D215/06 ,  C07D239/28 ,  C07D263/38 ,  C07D309/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.

Abstract translation: 本发明涉及通式（I）的化合物，其互变异构形式，其立体异构体，其药学上可接受的盐，含有它们的药物组合物，其制备方法，这些化合物在医药中的用途以及参与其制备的中间体。 本发明涉及可用于治疗疾病如高脂血症的化合物，并且还对胆固醇具有有益作用。

公开(公告)号：US20100197676A1

公开(公告)日：2010-08-05

申请号：US12752396

申请日：2010-04-01

Applicant: Yoshiaki Isshiki ,  Yasunori Kohchi ,  Eisaku Mizuguchi ,  Hitoshi Iikura ,  Yasuaki Matsubara ,  Shinji Tsujii ,  Nobuo Shimma ,  Masanori Miwa ,  Satoshi Aida ,  Masami Kohchi ,  Takeshi Murata ,  Kosuke Aso

Inventor： Yoshiaki Isshiki ,  Yasunori Kohchi ,  Eisaku Mizuguchi ,  Hitoshi Iikura ,  Yasuaki Matsubara ,  Shinji Tsujii ,  Nobuo Shimma ,  Masanori Miwa ,  Satoshi Aida ,  Masami Kohchi ,  Takeshi Murata ,  Kosuke Aso

IPC: A61K31/539 ,  A61P19/02 ,  A61K31/16 ,  C07C259/00 ,  C07D209/32 ,  A61K31/4035 ,  C07D265/02 ,  A61K31/535 ,  C07D273/01

CPC classification number: C07C259/10 ,  C07C317/18 ,  C07C323/12 ,  C07D207/27 ,  C07D211/76 ,  C07D239/10 ,  C07D261/04 ,  C07D263/22 ,  C07D265/02 ,  C07D265/32 ,  C07D273/00

Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].

Abstract translation: 本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。 本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。