公开(公告)号：US11912679B2

公开(公告)日：2024-02-27

申请号：US18372771

申请日：2023-09-26

Applicant: Astellas Pharma, Inc. ,  Mitobridge, Inc.

Inventor： Junko Maeda ,  Ikumi Kuriwaki ,  Kai Kitamura ,  Yumi Yamashita ,  Kenichi Kakefuda ,  Akio Kamikawa ,  Kenji Negoro ,  Wataru Hamaguchi ,  Ryushi Seo ,  Jeffrey Ciavarri

IPC: C07C233/69 ,  C07C233/22 ,  C07C233/81 ,  C07C235/42 ,  C07C237/42 ,  C07C311/13 ,  C07C311/46 ,  C07D205/04 ,  C07D207/12 ,  C07D207/16 ,  C07D207/273 ,  C07D209/08 ,  C07D211/48 ,  C07D211/62 ,  C07D213/56 ,  C07D213/75 ,  C07D231/12 ,  C07D231/40 ,  C07D239/26 ,  C07D279/12 ,  C07D295/155 ,  C07D295/16 ,  C07D295/195 ,  C07D305/08 ,  C07D307/22 ,  C07D309/14 ,  C07D333/48 ,  C07D401/06 ,  C07D403/06 ,  C07D403/10 ,  C07D405/10 ,  C07D487/10

CPC classification number: C07D295/16 ,  C07C233/22 ,  C07C233/69 ,  C07C233/81 ,  C07C235/42 ,  C07C237/42 ,  C07C311/13 ,  C07C311/46 ,  C07D205/04 ,  C07D207/12 ,  C07D207/16 ,  C07D207/273 ,  C07D209/08 ,  C07D211/48 ,  C07D211/62 ,  C07D213/56 ,  C07D213/75 ,  C07D231/12 ,  C07D231/40 ,  C07D239/26 ,  C07D279/12 ,  C07D295/155 ,  C07D295/195 ,  C07D305/08 ,  C07D307/22 ,  C07D309/14 ,  C07D333/48 ,  C07D401/06 ,  C07D403/06 ,  C07D403/10 ,  C07D405/10 ,  C07D487/10

Abstract: [Problem] A compound which is useful as a STING inhibitor is provided.
[Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.

公开(公告)号：US20230165974A1

公开(公告)日：2023-06-01

申请号：US17997376

申请日：2021-04-28

Applicant: MEDIMMUNE, LLC

Inventor： Ronald James CHRISTIE ,  Morgan Audrey URELLO

IPC: A61K48/00 ,  C07D213/82 ,  C07D279/12 ,  C07D295/15 ,  A61K47/69 ,  A61K47/64

CPC classification number: A61K48/0041 ,  C07D213/82 ,  C07D279/12 ,  C07D295/15 ,  A61K47/6935 ,  A61K47/6455

Abstract: The invention relates to modified lysines of the formula (I). The invention further relates to polypeptides comprising one or more modified lysine residues, pharmaceutical delivery systems comprising these polypeptides, pharmaceutical compositions containing them, and to their use in therapy.

公开(公告)号：US11661580B2

公开(公告)日：2023-05-30

申请号：US17006338

申请日：2020-08-28

Applicant: Cassava Science, Inc.

Inventor： Hoau-Yan Wang ,  Lindsay Burns Barbier

IPC: C12N5/079 ,  C07D265/30 ,  C07D211/14 ,  C07D277/04 ,  C07D295/088 ,  C07D205/04 ,  C07D491/056 ,  C07D498/10 ,  C07D217/04 ,  C07D471/10 ,  C07D491/04 ,  C07D207/08 ,  C07D265/36 ,  C07D277/02 ,  C07D279/12 ,  C07D295/08 ,  C07D211/74 ,  G01N33/50 ,  G01N33/68 ,  G01N33/94

CPC classification number: C12N5/0622 ,  C07D205/04 ,  C07D207/08 ,  C07D211/14 ,  C07D211/74 ,  C07D217/04 ,  C07D265/30 ,  C07D265/36 ,  C07D277/02 ,  C07D277/04 ,  C07D279/12 ,  C07D295/08 ,  C07D295/088 ,  C07D471/10 ,  C07D491/04 ,  C07D491/056 ,  C07D498/10 ,  G01N33/50 ,  G01N33/6896 ,  G01N33/94 ,  G01N2333/70571 ,  G01N2800/2821 ,  G01N2800/52

Abstract: A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

公开(公告)号：US20220251036A1

公开(公告)日：2022-08-11

申请号：US17629543

申请日：2020-07-24

Applicant: PHARMAXIS LTD.

Inventor： Dieter Wolfgang HAMPRECHT ,  Alison Dorothy FINDLAY ,  Craig Ivan TURNER ,  Mandar DEODHAR ,  Angelique Elsa GRECO ,  Wolfgang JAROLIMEK ,  Wenbin ZHOU

IPC: C07C317/32 ,  C07C317/28 ,  C07C317/20 ,  C07D279/12 ,  C07D215/36 ,  C07C317/36 ,  C07B59/00 ,  C07B45/04 ,  C07D209/48 ,  C07D295/116 ,  C07D307/64 ,  C07D333/34

Abstract: The present invention relates to methods for preparing a variety of difluorohaloallylamine derivatives. The present invention also relates to novel difluorohaloallylamine derivatives that are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for the treatment of a variety of indications, e.g., fibrosis, cancer and/or scarring in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as uses thereof.

公开(公告)号：US20220227792A1

公开(公告)日：2022-07-21

申请号：US17616559

申请日：2020-06-15

Applicant: LOYOLA UNIVERSITY OF CHICAGO

Inventor： Daniel Paul Becker ,  Sebastian Flieger ,  Isaac Schwarz

IPC: C07F5/02 ,  C07D401/12 ,  C07D279/12 ,  C07D213/42 ,  C07D265/30

Abstract: Disclosed herein are novel carborane hydroxamic acid matrix metalloproteinase (“MMP”) agents bearing borane-containing moieties and methods for their use in treating or preventing a disease, such as cancer and rheumatoid arthritis. In particular, disclosed herein are compounds of Formula (I) and (II) and pharmaceutically acceptable salt thereof: wherein the substituents are as described.

公开(公告)号：US10964966B2

公开(公告)日：2021-03-30

申请号：US16469766

申请日：2017-12-15

Applicant: LOCKHEED MARTIN ENERGY, LLC

Inventor： Zachariah M. Norman ,  Matthew Millard ,  Emily Grace Nelson ,  Scott Thomas Humbarger

IPC: H01M4/36 ,  H01M8/18 ,  C07D209/04 ,  C07D209/46 ,  C07D221/00 ,  C07D279/12 ,  C07F1/00 ,  C07F3/00 ,  H01M4/60

Abstract: Flow batteries can include a first half-cell containing a first aqueous electrolyte solution, a second half-cell containing a second aqueous electrolyte solution, and a separator disposed between the first half-cell and the second half-cell. The first aqueous electrolyte solution contains a first redox-active material, and the second aqueous electrolyte solution contains a second redox-active material. At least one of the first redox-active material and the second redox-active material is a nitroxide compound or a salt thereof. Particular nitroxide compounds can include a doubly bonded oxygen contained in a ring bearing the nitroxide group, a doubly bonded oxygen appended to a ring bearing the nitroxide group, sulfate or phosphate groups appended to a ring bearing the nitroxide group, various heterocyclic rings bearing the nitroxide group, or acyclic nitroxide compounds.

公开(公告)号：US20200283397A1

公开(公告)日：2020-09-10

申请号：US16672083

申请日：2019-11-01

Applicant: Imago Biosciences, Inc.

Inventor： Hugh Y. RIENHOFF, JR. ,  John M. MCCALL ,  Michael CLARE ,  Cassandra CELATKA ,  Amy E. TAPPER

IPC: C07D249/06 ,  C07C309/30 ,  A61K9/00 ,  A61K31/496 ,  C07D239/26 ,  A61K31/506 ,  C07D295/192 ,  A61K31/495 ,  C07D279/12 ,  A61K31/54 ,  C07D205/04 ,  A61K31/397 ,  C07D295/26 ,  C07D215/54 ,  C07C53/18 ,  C07D231/12 ,  C07D263/32 ,  A61K31/541 ,  C07B59/00 ,  C07D403/12 ,  A61K31/4192 ,  C07D401/12 ,  A61K31/454 ,  C07D249/08 ,  A61K31/4196 ,  C07D211/66 ,  A61K31/445 ,  C07D239/42 ,  C07D491/107 ,  C07D413/12 ,  A61K31/5377 ,  C07D498/08 ,  A61K31/5383 ,  C07D471/10 ,  A61K31/435 ,  C07D401/04 ,  A61K31/41 ,  C07D487/04 ,  A61K31/4162 ,  C07D487/08 ,  A61K31/4995 ,  A61K31/551 ,  C07D237/08 ,  A61K31/501 ,  A61K9/16 ,  A61K9/48 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00

Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

公开(公告)号：US10533001B2

公开(公告)日：2020-01-14

申请号：US15828154

申请日：2017-11-30

Applicant: PORTOLA PHARMACEUTICALS, INC.

Inventor： Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Yonghong Song ,  Qing Xu ,  Wolin Huang ,  Chandrasekar Venkataramani ,  Jack W. Rose ,  Anjali Pandey

IPC: C07D239/28 ,  C07D403/02 ,  C07D413/02 ,  C07D279/12 ,  A61K31/506 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/541 ,  C07D417/12 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5355 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention is directed to topical pharmaceutical compositions of Formula (If) or pharmaceutically acceptable salt thereof, which act as inhibitors of syk and/or JAK kinase activity. The described topical pharmaceutical compositions are useful in preventing or treating a number of conditions mediated at least in part by syk and/or JAK kinase activity.

公开(公告)号：US10464889B2

公开(公告)日：2019-11-05

申请号：US16037396

申请日：2018-07-17

Applicant: ELANCO Tiergesundheit AG

Inventor： Noelle Gauvry ,  Chouaib Tahtaoui

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

Abstract: 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：US20190300477A1

公开(公告)日：2019-10-03

申请号：US16446331

申请日：2019-06-19

Applicant: Global Blood Therapeutics, Inc.

Inventor： Qing Xu ,  Zhe Li

IPC: C07D207/08 ,  C07D401/06 ,  C07D335/02 ,  C07D401/12 ,  C07D211/16 ,  C07C271/16 ,  C07D207/34 ,  C07D211/22 ,  C07D211/60 ,  C07D211/78 ,  C07D213/81 ,  C07D241/04 ,  C07D265/30 ,  C07D279/12 ,  C07D309/08 ,  C07D309/28 ,  C07D333/38 ,  C07D207/48 ,  C07D403/06

Abstract: Provided herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.