公开(公告)号：US20250051320A1

公开(公告)日：2025-02-13

申请号：US18583347

申请日：2024-02-21

Applicant: Kymera Therapeutics, Inc.

Inventor： Nello MAINOLFI ,  Nan JI ,  Arthur F. KLUGE

IPC: C07D417/04 ,  C07D211/88 ,  C07D239/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.

公开(公告)号：US20240261416A1

公开(公告)日：2024-08-08

申请号：US18426920

申请日：2024-01-30

Applicant: Wisconsin Alumni Research Foundation

Inventor： Weiping Tang ,  Haibo Xie ,  Yunxiang Wu ,  Junzhuo Liao ,  Chunrong Li ,  Ira Tandon ,  Hua Tang

IPC: A61K47/55 ,  C07D239/22 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

CPC classification number: A61K47/55 ,  C07D239/22 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

Abstract: Provided herein are achiral cereblon (CRBN) ligands based on phenyl dihydrouracil that have optimal binding to CRBN without having chiral carbons. Also provided herein are the proteolysis targeting chimeras (PROTACs) comprising the CRBN ligands and a protein binder, pharmaceutical compositions containing the PROTACs, and methods of treating diseases using the PROTACs.

公开(公告)号：US20230234950A1

公开(公告)日：2023-07-27

申请号：US18059232

申请日：2022-11-28

Applicant: Kymera Therapeutics, Inc.

Inventor： Nello MAINOLFI ,  Nan JI ,  Arthur F. KLUGE

IPC: C07D417/04 ,  C07D211/88 ,  C07D239/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D417/04 ,  C07D211/88 ,  C07D239/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.

公开(公告)号：US20230227414A1

公开(公告)日：2023-07-20

申请号：US18187211

申请日：2023-03-21

Applicant: GlaxoSmithKline LLC

Inventor： Kevin J. DUFFY ,  Duke M. FITCH ,  Jian JIN ,  Ronggang LIU ,  Antony N. SHAW ,  Kenneth WIGGALL

IPC: C07D239/60 ,  A61K31/515 ,  C07D239/54 ,  C07D239/62 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D417/10 ,  C07D239/22

CPC classification number: C07D239/60 ,  A61K31/515 ,  C07D239/54 ,  C07D239/62 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D417/10 ,  C07D239/22

Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I)




which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

公开(公告)号：US11643397B2

公开(公告)日：2023-05-09

申请号：US17383554

申请日：2021-07-23

Applicant: GlaxoSmithKline LLC

Inventor： Kevin J. Duffy ,  Duke M. Fitch ,  Jian Jin ,  Ronggang Liu ,  Antony N. Shaw ,  Kenneth Wiggall

IPC: C07D239/54 ,  C07D239/60 ,  A61K31/515 ,  C07D239/62 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D417/10 ,  C07D239/22

CPC classification number: C07D239/60 ,  A61K31/515 ,  C07D239/22 ,  C07D239/54 ,  C07D239/62 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D417/10

Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I)




which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

公开(公告)号：US20220356175A1

公开(公告)日：2022-11-10

申请号：US17259370

申请日：2019-07-09

Applicant: ABIVAX ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  UNIVERSITE DE MONTPELLIER ,  INSTITUT CURIE

Inventor： Didier SCHERRER ,  Jamal TAZI ,  Florence MAHUTEAU-BETZER ,  Romain NAJMAN ,  Julien SANTO ,  Cécile APOLIT

IPC: C07D413/12 ,  C07D239/16 ,  C07D405/12 ,  C07D239/22 ,  C07D403/12 ,  C07D401/12

Abstract: A compound of formula (Ic) wherein X2 represents a —CO—NRk— group, wherein Rk represents a hydrogen atom or a methyl group, a —NH—CO—NH— group, a —OCH2— group, a —CH(OH)— group, a —NH—CO— group, a —O— group, a —O—(CH2)s—O—, a —CO— group, a —SO2— group, a divalent 5-membered heteroaromatic ring comprising 1, 2, 3 or 4 heteroatoms, —a NH—SO2— or a —SO2—NH— group; Y2 represents a hydrogen atom, a halogen atom, a hydroxyl group, a (C1-C4)alkoxy group, a a group, a group, a morpholinyl group, optionally substituted by a (C1-C4)alkyl group, a piperazinyl group, a piperidinyl group, or a —CR1R2R3 group, or any of its pharmaceutically acceptable salt.

公开(公告)号：US20220340551A1

公开(公告)日：2022-10-27

申请号：US17647582

申请日：2022-01-10

Applicant: Cellix Bio Private Limited

Inventor： Mahesh Kandula

IPC: C07D405/14 ,  A61P1/02 ,  C07C211/03 ,  C07C211/21 ,  C07D233/60 ,  C07D233/62 ,  C07D239/22 ,  C07D403/06 ,  C07D233/64

Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX or Formula X and, the methods for the treatment of fungal infections may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of fungal infections.

公开(公告)号：US11124485B2

公开(公告)日：2021-09-21

申请号：US16773411

申请日：2020-01-27

Applicant: CV6 Therapeutics (NI) Limited

Inventor： Mark Spyvee ,  Pravin S. Shirude

IPC: A61K31/513 ,  C07D239/22 ,  C07D211/88 ,  C07D207/404 ,  A61P35/00

Abstract: Provided herein are dUTPase inhibitors of Formula (I), compositions comprising such compounds and methods of using such compounds and compositions

公开(公告)号：US20210130300A1

公开(公告)日：2021-05-06

申请号：US16902935

申请日：2020-06-16

Applicant: Japan Tobacco Inc.

Inventor： Masahiro YOKOTA ,  Taku IKENOGAMI ,  Eiichi WATANABE ,  Noriyoshi SEKI ,  Takayuki SAKAI ,  Shingo FUJIOKA ,  Makoto SHIOZAKI ,  Katsunori SUWA ,  Yosuke OGOSHI ,  Masato NOGUCHI ,  Katsuya MAEDA

IPC: C07D239/22 ,  A61K31/505 ,  A61K31/506 ,  A61K31/695 ,  C07D403/04 ,  C07D405/04 ,  C07F7/12 ,  C07D405/10 ,  C07D413/04 ,  C07F7/08 ,  A61P25/00 ,  A61P27/00 ,  A61P3/00 ,  A61P29/00 ,  A61P37/00 ,  A61P17/00 ,  A61P43/00 ,  C07D401/04

Abstract: A compound of Formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is defined as in the specification.

公开(公告)号：US20200255385A1

公开(公告)日：2020-08-13

申请号：US16789687

申请日：2020-05-04

Applicant: CV6 Therapeutics (NI) Limited

Inventor： Mark Spyvee ,  Pravin S. Shirude

IPC: C07D233/74 ,  C07D277/34 ,  C07D263/44 ,  C07D251/10 ,  C07D249/12 ,  C07D241/08 ,  C07D239/22 ,  C07D233/46 ,  C07D207/404 ,  C07D207/36 ,  C07D487/04 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  A61P35/00 ,  C07D207/40 ,  C07D211/88 ,  A61K31/4015 ,  C07F9/6506

Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.