公开(公告)号：US20240092765A1

公开(公告)日：2024-03-21

申请号：US18348114

申请日：2023-07-06

申请人： Insilico Medicine IP Limited

发明人： Aleksandr Aliper ,  Vladimir Aladinskiy ,  Aleksandrs Zavoronkovs

IPC分类号： C07D405/04 ,  A61K31/4164 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/048

CPC分类号： C07D405/04 ,  A61K31/4164 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/048

摘要： A method of inhibiting TNIK and/or MAP4K4 kinase can include: contacting the kinase with a compound of Formula A,






wherein: ring 1 is an aromatic ring with or without hetero atoms; ring 2 is a hetero aromatic ring; ring 3 includes at least one hetero aromatic ring and optionally at least one cycloaliphatic ring fused with the at least one hetero aromatic ring; ring 4 is an aromatic ring with or without hetero atoms; Y is a bond or a linker; Y1 is a linker; each n is independently 0, 1, or 2; each o is independently 0. 1, 2, 3, 4, or 5; each R1, R6, R11, and R12 is independently a substituent; and RA is a ring structure, straight aliphatics, or branched aliphatics, which can be substituted or unsubstituted, any with or without hetero atoms.

公开(公告)号：US20240092756A1

公开(公告)日：2024-03-21

申请号：US18253712

申请日：2021-11-18

申请人： 2692372 ONTARIO, INC. ,  DUNAD THERAPEUTICS LTD.

发明人： Patrick T. GUNNING ,  Jeff OMEARA ,  Siawash AHMAR ,  Graham L. SIMPSON ,  Peter HUNT ,  David Alexander ROSA ,  Ji Sung PARK

IPC分类号： C07D401/12 ,  C07D215/12 ,  C07D215/42 ,  C07D401/04 ,  C07D471/14

CPC分类号： C07D401/12 ,  C07D215/12 ,  C07D215/42 ,  C07D401/04 ,  C07D471/14 ,  C07B2200/09

摘要： Provided herein are compounds binding to KRAS protein or a mutant thereof, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

公开(公告)号：US11932620B1

公开(公告)日：2024-03-19

申请号：US18386411

申请日：2023-11-02

申请人： KING FAISAL UNIVERSITY

发明人： Hany Mohamed Abd El-Lateef Ahmed ,  Mai Mostafa Khalaf Ali ,  Antar Ahmed Abdelhamid Ahmed

IPC分类号： A61P31/10 ,  A61P31/04 ,  C07D401/04

CPC分类号： C07D401/04 ,  A61P31/04 ,  A61P31/10

摘要： An ethyl 2-[9-(6-fluoro-2-hydroxyquinolin-3-yl)-1,8-dioxo-3,4,9,10-tetrahydroacridine-10-yl]-acetate compound, its synthesis, and its use as an antimicrobial agent.

公开(公告)号：US11926612B2

公开(公告)日：2024-03-12

申请号：US16341597

申请日：2017-10-11

申请人： Research Triangle Institute

发明人： Scott P. Runyon ,  Rangan Maitra ,  Sanju Narayanan ,  Kenneth S. Rehder

IPC分类号： C07D233/90 ,  C07D249/10 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14

CPC分类号： C07D401/12 ,  C07D233/90 ,  C07D249/10 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14

摘要： This disclosure is directed to agonists of the apelin receptor (APJ) with heterocyclic cores and uses of such agonists.

公开(公告)号：US11926609B1

公开(公告)日：2024-03-12

申请号：US18379964

申请日：2023-10-13

申请人： KING FAISAL UNIVERSITY

发明人： Mai Mostafa Khalaf Ali ,  Hany Mohamed Abd Al-Lateef Ahmed ,  Antar Ahmed Abdelhamid Ahmed ,  Amer A. Amer

IPC分类号： C07D401/04 ,  A61P31/04 ,  A61P31/10

CPC分类号： C07D401/04 ,  A61P31/04 ,  A61P31/10

摘要： A 6′-(3-chlorophenyl)-2′-ethoxy-3,4′-bipyridine-3′-carbonitrile compound, its synthesis, and its use as an antimicrobial agent.

公开(公告)号：US20240067656A1

公开(公告)日：2024-02-29

申请号：US18490700

申请日：2023-10-19

申请人： The Regents of the University of California

发明人： Jonathan Ostrem ,  Ulf Peters ,  Kevan M. Shokat

IPC分类号： C07D495/04 ,  A61K38/17 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/185 ,  C07D295/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886

CPC分类号： C07D495/04 ,  A61K38/1709 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/185 ,  C07D295/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Y306/05002 ,  G01N2500/04

摘要： K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

公开(公告)号：US20240067623A1

公开(公告)日：2024-02-29

申请号：US18250664

申请日：2021-11-02

申请人： Bayer Aktiengesellschaft

发明人： Thomas MÜLLER ,  Estella BUSCATO ARSEQUELL ,  Hendrik HELMKE ,  Harald JAKOBI ,  Michael Gerhard HOFFMANN ,  Jan DITTGEN

IPC分类号： C07D401/04 ,  C07D405/14 ,  A01N25/32 ,  A01P13/00

CPC分类号： C07D401/04 ,  C07D405/14 ,  A01N25/32 ,  A01P13/00

摘要： [1-Pheny1)-5-(heteroaryl)-1H-pyrazol-3-yl)oxy] acetic acid derivatives and salts thereof, crop protection compositions comprising them, processes for preparing them, use thereof and plant protection compositions.
The present invention relates to crop protection compounds and to compositions which comprise specific compounds as safeners for reducing phytotoxic effects of agrochemicals, especially herbicides.
The invention relates more particularly to certain [1-(phenyl)-5-(heteroaryl)-1H-pyrazol-3-yl)oxy]acetic acid derivatives of the general formula (I)






and their salts, to processes for preparing them and to their use as plant protection compounds (safeners).

公开(公告)号：US20240051935A1

公开(公告)日：2024-02-15

申请号：US18256647

申请日：2021-12-09

申请人： BAYER AKTIENGESELLSCHAFT

发明人： Alexandros VAKALOPOULOS ,  Marie-Pierre COLLIN-KRÖPELIN ,  Nuria ORTEGA HERNANDEZ ,  Andre DIESKAU ,  Melissa BOULTADAKIS-ARAPINIS ,  Lisa CANDISH ,  Timo STELLFELD ,  Ilka MATHAR ,  Lucas Hudson HOFMEISTER ,  Peter SANDNER ,  Frank WUNDER ,  Lisa DIETZ ,  Robert Alan WEBSTER ,  Carsten SCHMECK ,  Thomas MONDRITZKI

IPC分类号： C07D401/04 ,  A61P9/12 ,  A61P9/00

CPC分类号： C07D401/04 ,  A61P9/12 ,  A61P9/00

摘要： The invention relates to substituted pyrazolo piperidine carboxylic acids, their salts and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and cardiac diseases, preferably heart failure with reduced and preserved ejection fraction (HFrEF, HFmrEF and HFpEF), hypertension (HTN), peripheral arterial diseases (PAD, PAOD), cardio-renal and kidney diseases, preferably chronic and diabetic kidney disease (CKD and DKD), cardiopulmonary and lung diseases, preferable pulmonary hypertension (PH), and other diseases, preferably neurodegenerative diseases and different forms of dementias, fibrotic diseases, systemic sclerosis (SSc), sickle cell disease (SCD), wound healing disorders such as diabetic foot ulcer (DFU).

公开(公告)号：US11897862B2

公开(公告)日：2024-02-13

申请号：US18297316

申请日：2023-04-07

申请人： Gilead Sciences, Inc.

发明人： Gayatri Balan ,  Peter A. Blomgren ,  Chen Chen ,  Julian A. Codelli ,  Zhimin Du ,  Musong Kim ,  Dorothée Saddier Axe ,  Gregg M. Schwarzwalder ,  Rhiannon Thomas-Tran ,  Michael T. Tudesco ,  Chandrasekar Venkataramani ,  William J. Watkins ,  Brian M. Weist ,  Suet C. Yeung ,  Helen Yu

IPC分类号： C07D401/04

CPC分类号： C07D401/04 ,  C07B2200/05 ,  C07D401/04 ,  C07B2200/05

摘要： The present disclosure relates generally to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios) and/or IKZF4 (Eos). The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding and degradation of an IKZF protein, such as IKZF2 and/or IKZF4, including cancer.

公开(公告)号：US20240043405A1

公开(公告)日：2024-02-08

申请号：US17906938

申请日：2021-03-22

申请人： Dana-Farber Cancer Institute, Inc.

发明人： John M. Hatcher

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  A61K45/06

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  A61K45/06

摘要： The disclosure relates to compounds that act as irreversible inhibitors interleukin 1 (IL-1) receptor-associated kinases (IRAKs); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.