公开(公告)号：US11964971B2

公开(公告)日：2024-04-23

申请号：US17388100

申请日：2021-07-29

Applicant: Skyhawk Therapeutics, Inc.

Inventor： Michael Luzzio ,  Brian Lucas ,  Tiansheng Wang ,  Jun Feng

IPC: C07D451/14 ,  C07D451/06 ,  C07D498/08 ,  C07D519/00

CPC classification number: C07D451/14 ,  C07D451/06 ,  C07D498/08 ,  C07D519/00

Abstract: Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, pharmaceutical compositions comprising the same, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.

公开(公告)号：US11945801B2

公开(公告)日：2024-04-02

申请号：US17311121

申请日：2019-12-09

Applicant: Heptares Therapeutics Limited

Inventor： Giles Albert Brown ,  Barry John Teobald ,  Benjamin Gerald Tehan

IPC: C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D451/02 ,  C07D451/04 ,  C07D451/14

CPC classification number: C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D451/02 ,  C07D451/04 ,  C07D451/14

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where X1; X2; R1 and R4 are as defined herein.

公开(公告)号：US11773090B2

公开(公告)日：2023-10-03

申请号：US17024085

申请日：2020-09-17

Applicant: Heptares Therapeutics Limited

Inventor： Giles Albert Brown ,  Barry John Teobald ,  Benjamin Gerald Tehan

IPC: C07D451/14 ,  A61P25/28

CPC classification number: C07D451/14 ,  A61P25/28

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula




where Y, R1, R2 and R4 are as defined herein.

公开(公告)号：US20230257365A1

公开(公告)日：2023-08-17

申请号：US18012369

申请日：2021-07-09

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng Wang ,  Xin Han ,  Weiguo Xiang ,  Chong Qin ,  Tianfeng Xu ,  Lijie Zhao

IPC: C07D401/14 ,  C07D451/06 ,  C07D451/14 ,  C07D519/00 ,  C07D487/04 ,  C07D487/10 ,  C07D471/04 ,  C07D491/08

CPC classification number: C07D401/14 ,  C07D451/06 ,  C07D451/14 ,  C07D519/00 ,  C07D487/04 ,  C07D487/10 ,  C07D471/04 ,  C07D491/08

Abstract: The present disclosure provides compounds represented by Formula I: A-L-B1 I, and the salts or solvates thereof, wherein A, L, and B1 are as defined in the specification. Compounds having Formula I are androgen receptor degraders useful for the treatment of cancer and other diseases.

公开(公告)号：US20180318270A1

公开(公告)日：2018-11-08

申请号：US16037001

申请日：2018-07-17

Applicant: Astraea Therapeutics, LLC

Inventor： Nurulain Zaveri ,  Faming Jiang ,  Lawrence Toll

IPC: A61K31/439 ,  C07D519/00 ,  C07D451/14

CPC classification number: A61K31/439 ,  C07D451/14 ,  C07D519/00

Abstract: Provided herein are novel and selective high affinity α3β4 nicotinic acetycholine receptor ligands and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, drug addiction or pain using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of selectively antagonizing receptors such as, for example, the α3β4 nicotinic acetycholine receptor using the compounds and compositions disclosed herein.

公开(公告)号：US20180002327A1

公开(公告)日：2018-01-04

申请号：US15701842

申请日：2017-09-12

Applicant: Merck Patent GmbH

Inventor： Catherine JORAND-LEBRUN ,  Reinaldo JONES ,  Annie Cho WON ,  Ngan NGUYEN ,  Theresa L. JOHNSON ,  Lizbeth Celeste DESELM ,  Kausik PANDA

IPC: C07D451/04 ,  C07D451/14 ,  C07D417/14 ,  C07D413/14 ,  C07D405/14 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04 ,  C07D401/12

CPC classification number: C07D451/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/14 ,  C07D487/04

Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.

公开(公告)号：US20170312280A1

公开(公告)日：2017-11-02

申请号：US15498803

申请日：2017-04-27

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Jennifer Kozak ,  Melissa Fleury ,  Paul R. Fatheree ,  Anne-Marie Beausoleil ,  Dante D. Podesto ,  Xiaojun Huang

IPC: A61K31/519 ,  C07D211/00 ,  C07D211/06 ,  C07D487/04

CPC classification number: A61K31/519 ,  C07D211/00 ,  C07D211/06 ,  C07D451/04 ,  C07D451/14 ,  C07D487/04

Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.

公开(公告)号：US09732105B2

公开(公告)日：2017-08-15

申请号：US14941466

申请日：2015-11-13

Applicant: University of Pittsburgh—of the Commonwealth System of Higher Education

Inventor： Peter Wipf ,  Marie-Celine Frantz

IPC: C07D451/14 ,  C07F5/02 ,  C07D211/94 ,  C07D471/08 ,  C07D295/24 ,  C07F9/59 ,  C07D209/46 ,  C07D453/02

CPC classification number: C07F9/59 ,  C07D209/46 ,  C07D211/94 ,  C07D295/24 ,  C07D451/14 ,  C07D453/02 ,  C07D471/08 ,  C07F5/022

Abstract: A compound having a structure of:

公开(公告)号：US09550798B2

公开(公告)日：2017-01-24

申请号：US14417293

申请日：2013-07-26

Applicant: BIOGEN MA INC.

Inventor： Kevin Guckian ,  Gnanasambandam Kumaravel ,  Bin Ma ,  Sha Mi ,  Hairuo Peng ,  Zhaohui Shao ,  Lihong Sun ,  Arthur Taveras ,  Zhili Xin ,  Lei Zhang

IPC: C07C229/48 ,  C07D223/06 ,  C07D221/22 ,  C07D209/52 ,  C07D211/62 ,  C07D295/096 ,  A61K31/5375 ,  A61K31/439 ,  A61K31/46 ,  A61K31/445 ,  A61K31/196 ,  A61K31/136 ,  C07F7/08 ,  A61K45/06 ,  A61K31/195 ,  A61K31/41 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5513 ,  C07D215/38 ,  C07D217/22 ,  C07D401/04 ,  C07D471/08 ,  C07C217/58 ,  C07C229/46 ,  C07C233/61 ,  C07C235/66 ,  A61K31/397 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/695 ,  C07C211/38 ,  C07D205/04 ,  C07D213/74 ,  C07D215/20 ,  C07D401/06

CPC classification number: C07F7/081 ,  A61K31/195 ,  A61K31/196 ,  A61K31/397 ,  A61K31/403 ,  A61K31/41 ,  A61K31/439 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/695 ,  A61K45/06 ,  C07C211/38 ,  C07C217/58 ,  C07C229/46 ,  C07C229/50 ,  C07C233/60 ,  C07C233/61 ,  C07C235/66 ,  C07C2102/10 ,  C07C2102/42 ,  C07C2102/44 ,  C07C2102/50 ,  C07C2103/62 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2602/46 ,  C07C2602/50 ,  C07C2603/62 ,  C07C2603/74 ,  C07D205/04 ,  C07D209/52 ,  C07D211/14 ,  C07D213/74 ,  C07D215/12 ,  C07D215/20 ,  C07D215/38 ,  C07D217/22 ,  C07D239/42 ,  C07D241/20 ,  C07D295/096 ,  C07D401/04 ,  C07D401/06 ,  C07D451/02 ,  C07D451/14 ,  C07D471/08 ,  C07D491/107 ,  C07F7/0805 ,  A61K2300/00

Abstract: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

Abstract translation: 式（I）化合物可以调节一种或多种SIP受体的活性和/或自分泌素（ATX）的活性。

公开(公告)号：US20160200726A1

公开(公告)日：2016-07-14

申请号：US14913736

申请日：2014-08-14

Applicant: NIPPON SODA CO., LTD.

Inventor： Masaya AKASHI ,  Tsutomu INOUE ,  Hirohito OOOKA

IPC: C07D471/08

CPC classification number: C07D471/08 ,  B01J31/1805 ,  B01J31/1815 ,  B01J31/189 ,  B01J31/24 ,  B01J31/2409 ,  B01J31/2447 ,  B01J2231/643 ,  B01J2531/821 ,  C07B53/00 ,  C07D451/14

Abstract: A 9-azabicyclo[3.3.1]nonan-3-one derivative is reacted with a hydrogen in the presence of a catalyst composed of a ruthenium complex to obtain, at a low cost, an endo-9-azabicyclo[3.3.1]nonan-3-ol derivative useful as a production intermediate for agrochemical agents or medicines.

Abstract translation: 在由钌络合物组成的催化剂存在下，将9-氮杂双环[3.3.1]壬-3-酮衍生物与氢气反应，以低成本获得内-9-氮杂双环[3.3.1] 壬烷-3-醇衍生物，可用作农药或药物的生产中间体。