公开(公告)号：US20240327408A1

公开(公告)日：2024-10-03

申请号：US18579501

申请日：2022-07-14

Applicant: CHINA PHARMACEUTICAL UNIVERSITY

Inventor： Haiying SUN ,  Yibei XIAO ,  Yuantao FU ,  Rongliang TAN ,  Guangjun XIE ,  Jinxin JIANG ,  Yinan YUAN

IPC: C07D471/14 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/519 ,  A61P35/02 ,  C07D471/04 ,  C07D491/147 ,  C07D495/14 ,  C07D513/14

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/519 ,  A61P35/02 ,  C07D471/04 ,  C07D491/147 ,  C07D495/14 ,  C07D513/14

Abstract: The present invention is related to compounds of formula I containing a tetrahydronaphthyridinone or tetrahydropyridopyrimidinone skeleton and preparation methods therefor. It has been experimentally verified that the compounds containing a tetrahydronaphthyridinone or tetrahydropyridopyrimidinone skeleton have significant agonistic effects on caseinolytic protease P (ClpP), and can be applied in the treatment of various cancers.

公开(公告)号：US12101998B2

公开(公告)日：2024-09-24

申请号：US17281414

申请日：2019-10-31

Applicant: LT MATERIALS CO., LTD.

Inventor： Min-Ji Park ,  Yun-Ji Lee ,  Won-Jang Jeong

IPC: H10K85/60 ,  C07D491/147 ,  C07D495/14 ,  C07D519/00 ,  C09K11/06 ,  H10K50/11 ,  H10K50/15 ,  H10K50/16 ,  H10K50/17 ,  H10K50/18 ,  H10K101/10

CPC classification number: H10K85/654 ,  C07D491/147 ,  C07D495/14 ,  C07D519/00 ,  C09K11/06 ,  H10K85/615 ,  H10K85/626 ,  H10K85/657 ,  H10K85/6572 ,  C09K2211/1018 ,  H10K50/11 ,  H10K50/15 ,  H10K50/16 ,  H10K50/17 ,  H10K50/171 ,  H10K50/18 ,  H10K2101/10

Abstract: The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same.

公开(公告)号：US20240299366A1

公开(公告)日：2024-09-12

申请号：US18456718

申请日：2023-08-28

Applicant: Arvinas Operations, Inc.

Inventor： Andrew P. CREW ,  Craig M. Crews ,  Hanqing Dong ,  Jing Wang ,  Yimin Qian ,  Meizhong Jin

IPC: A61K31/426 ,  A61K31/454 ,  A61K31/505 ,  A61K31/551 ,  A61K45/06 ,  A61K47/54 ,  A61K47/66 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/14 ,  C07D498/14 ,  C07K14/47 ,  C07K14/72 ,  C12N9/12 ,  C12N9/18 ,  C12Q1/25

CPC classification number: A61K31/426 ,  A61K31/454 ,  A61K31/505 ,  A61K31/551 ,  A61K45/06 ,  A61K47/545 ,  A61K47/555 ,  A61K47/66 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/14 ,  C07D498/14 ,  C07K14/4705 ,  C07K14/721 ,  C12N9/12 ,  C12N9/18 ,  C12Q1/25 ,  C12Y207/11001 ,  C12Y301/01031 ,  G01N2333/9015 ,  G01N2500/02

Abstract: The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.

公开(公告)号：US20240294543A1

公开(公告)日：2024-09-05

申请号：US18626665

申请日：2024-04-04

Applicant: Hoffmann-La Roche Inc.

Inventor： Bjoern BARTELS ,  Giuseppe CECERE ,  Guido GALLEY ,  Luca GOBBI ,  Martin GOEBEL ,  Maria-Clemencia HERNANDEZ ,  Andrés Miguel OLIVARES MORALES ,  Hasane RATNI ,  Michael REUTLINGER ,  Valerie RUNTZ-SCHMITT

IPC: C07D495/14 ,  A61K31/551 ,  C07D495/22

CPC classification number: C07D495/14 ,  A61K31/551 ,  C07D495/22

Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein.




Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

公开(公告)号：US12049470B2

公开(公告)日：2024-07-30

申请号：US17587555

申请日：2022-01-28

Applicant: Celgene Corporation

Inventor： Alexander L. Ruchelman ,  John R. Coombs ,  Keming Zhu ,  Daniel Lim ,  Candice Lee Joe ,  David T. George ,  Bin Zheng ,  Dong Lin

IPC: C07D215/227 ,  C07C255/50 ,  C07D215/58 ,  C07D495/04 ,  C07D495/14

CPC classification number: C07D495/14 ,  C07C255/50 ,  C07D215/58 ,  C07D495/04

Abstract: The present disclosure provides novel synthetic intermediates useful in the synthesis of MK2 kinase inhibitors.

公开(公告)号：US20240246993A1

公开(公告)日：2024-07-25

申请号：US18600852

申请日：2024-03-11

Applicant: Prelude Therapeutics Incorporated

Inventor： Jincong Zhuo ,  Xiaowei Wu ,  Katarina Rohlfing ,  Andrew Combs

IPC: C07D495/14 ,  A61K45/06 ,  A61P15/08 ,  A61P35/00 ,  C07D498/14

CPC classification number: C07D495/14 ,  A61K45/06 ,  A61P15/08 ,  A61P35/00 ,  C07D498/14 ,  C07B2200/05

Abstract: The disclosure is directed to compounds of Formula I




pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.

公开(公告)号：US20240199634A1

公开(公告)日：2024-06-20

申请号：US18282318

申请日：2022-03-17

Applicant: SCHRÖDINGER, INC.

Inventor： Sayan MONDAL ,  Haifeng TANG ,  Xianhai HUANG ,  Adam Marc LEVINSON ,  Leah FRYE ,  Sathesh BHAT ,  Pieter Harm BOS ,  Zef KONST ,  Phani GHANAKOTA ,  Jeremy Robert GREENWOOD

IPC: C07D495/04 ,  A61K31/4365 ,  A61K31/4375 ,  A61K31/4743 ,  A61K31/5377 ,  C07D495/14

CPC classification number: C07D495/04 ,  A61K31/4365 ,  A61K31/4375 ,  A61K31/4743 ,  A61K31/5377 ,  C07D495/14

Abstract: The present application relates to compounds of Formula (I), as defined herein, and pharmaceutically acceptable salts thereof. The present application also describes pharmaceutical composition comprising a compound of Formula (I), and pharmaceutically acceptable salts thereof, and methods of using the compounds and compositions for inhibiting kinase activity, and for treating cancer.

公开(公告)号：US20240190890A1

公开(公告)日：2024-06-13

申请号：US18495004

申请日：2023-10-26

Applicant: Bristol-Myers Squibb Company ,  Celgene Corporation

Inventor： Xirui Hu ,  Lixin Qiao ,  Boris Seletsky ,  Matthew Patton ,  Min Cao ,  Farid van der Mei ,  Guobin Miao ,  Ivar McDonald ,  Carolyn Dzierba

IPC: C07D495/14

CPC classification number: C07D495/14

Abstract: The present invention provides compounds, compositions thereof, and methods of using the MK2 inhibitors of the Formula:

公开(公告)号：US20240190889A1

公开(公告)日：2024-06-13

申请号：US18429832

申请日：2024-02-01

Applicant: Hoffmann-La Roche Inc.

Inventor： Giuseppe CECERE ,  Luca GOBBI ,  Maria-Clemencia HERNANDEZ ,  Andreas KOBLET ,  Andres Miguel OLIVARES MORALES ,  Valerie RUNTZ-SCHMITT ,  Nicolas ZORN

IPC: C07D495/14 ,  A61K31/551

CPC classification number: C07D495/14 ,  A61K31/551

Abstract: The invention provides heterocyclic compounds having the general formula (1), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein.




Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders. release wednesday

公开(公告)号：US20240141199A1

公开(公告)日：2024-05-02

申请号：US18267877

申请日：2021-12-14

Applicant: Sumitomo Chemical Company, Limited

Inventor： Eiji YOSHIKAWA ,  Takayuki OKACHI ,  Yoshiaki TSUBATA ,  Takahiro SATO

IPC: C09D151/00 ,  C07D495/04 ,  C07D495/14 ,  C07F7/18

CPC classification number: C09D151/006 ,  C07D495/04 ,  C07D495/14 ,  C07F7/1804

Abstract: A compound having formula (1) has excellent heat resistance.




In formula (1), X represents a divalent polycyclic condensed ring group having two or more thiophene rings and having an sp3 carbon atom as a constituent element. R1 and R2 each represent an alkyl group, R3 represents an alkyl group, k represents an integer of 0 to 4, and A represents a group having formula (a1), (a2), or (b1):




R4, R5, R6, R7, R8, and R9 each represent an alkyl group, E1 and E2 each represent —C(R10)(R11)—, —C(O)—, —O—, or —NR12—. R10 and R11 each represent an alkyl group, R12 represents an alkyl group, m and n each represent 0 or 1, where m+n=1.