公开(公告)号：US20230114472A1

公开(公告)日：2023-04-13

申请号：US17702718

申请日：2022-03-23

Applicant: Denali Therapeutics Inc.

Inventor： Robert A. Craig, II ,  Javier de Vicente Fidalgo ,  Anthony A. Estrada ,  Jianwen A. Feng ,  Brian M. Fox ,  Maksim Osipov ,  Arun Thottumkara

IPC: C07D413/04 ,  C07D271/113 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D493/08

Abstract: The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or prodrug thereof, and methods of making and using thereof.

公开(公告)号：US11617733B2

公开(公告)日：2023-04-04

申请号：US17149327

申请日：2021-01-14

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Tohru Kambe ,  Toru Maruyama ,  Shinsaku Yamane ,  Satoshi Nakayama ,  Kousuke Tani

IPC: A61K31/335 ,  A61K31/4427 ,  A61K31/558 ,  C07D401/06 ,  C07D313/06 ,  C07D417/04 ,  C07D407/12 ,  C07D405/06 ,  A61K9/00

Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

公开(公告)号：US20230096085A1

公开(公告)日：2023-03-30

申请号：US17795670

申请日：2020-12-16

Applicant: UNIMATEC CO., LTD.

Inventor： Junya SEINO ,  Rie AOTSU ,  Keisuke KOKIN

IPC: C07D403/04 ,  C07D401/04 ,  C07D471/04 ,  C07D417/04 ,  C07D405/04

Abstract: A fluorine-containing pyrimidine compound represented by the following formula (1): wherein in the general formula (1) above, R represents a hydrocarbon group having 1 to 12 carbon atoms, and a ring Z represents a fused heterocyclic ring containing a heteroatom.

公开(公告)号：US20230077316A1

公开(公告)日：2023-03-09

申请号：US17452011

申请日：2021-10-22

Applicant: Nimbus Clotho, Inc.

Inventor： Kevin D. KREUTTER ,  Lewis Whitehead ,  Angela V. West ,  Steven K. Albanese ,  Andreas Verras ,  Shaughnessy Robinson ,  Neelu Kaila ,  Sebastien Campos ,  Kevin Demarco

IPC: C07D417/14 ,  C07D277/52 ,  C07D417/12 ,  C07D401/14 ,  C07D401/04 ,  C07D401/12 ,  C07D413/14 ,  C07D241/18 ,  C07D417/04 ,  C07D471/04 ,  C07D403/14 ,  C07D498/08

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CPTS1, and the treatment of CPTS1-mediated disorders.

公开(公告)号：US11597708B2

公开(公告)日：2023-03-07

申请号：US16501272

申请日：2017-09-12

Applicant: HSF Pharmaceuticals SA

Inventor： Nuria Vilaboa ,  Richard W Voellmy

IPC: C07D277/46 ,  A61P35/00 ,  C07D213/75 ,  C07D215/42 ,  C07D231/40 ,  C07D261/14 ,  C07D263/48 ,  C07D277/56 ,  C07D277/82 ,  C07D285/135 ,  C07D333/36 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: The present disclosure relates to a class of mammalian heat shock factor (HSF) inhibitors, to pharmaceutical compositions comprising these inhibitors as well as to methods for using the inhibitors. The inhibitors inhibit stress-induced expression from heat shock gene promoters. Furthermore, the inhibitors are cytotoxic to a variety of human cancer cells types.

公开(公告)号：US20230060122A9

公开(公告)日：2023-02-23

申请号：US17172314

申请日：2021-02-10

Applicant: Wisconsin Alumni Research Foundation

Inventor： Robert Todd Striker ,  Nathan Joseph Wlodarchak ,  John Bruce Feltenberger ,  Jennifer Golden

IPC: C07D401/04 ,  C07D239/42 ,  C07D417/04 ,  C07D277/28 ,  A61K31/506 ,  A61K45/06 ,  A61K31/496 ,  A61P31/06

Abstract: Biochemically active PASTA kinase inhibitors which exploit subtle structural differences between human kinases and bacterial PASTA kinases to improve specificity and inhibitor activity. The disclosed kinase inhibitors have the general formula: wherein: R1=Me, Et, n-Pr, —CH2CH2OH, —CH2CH2OP(O)(OH)2, —CH2CH2NMe2; R2=H, Me, Et, o-Pr, i-Pr, CF3, Cl, OMe; R3=H, Me, NHMe, NHBn, Cl, NO2OMe, F, CN; and Ar=

公开(公告)号：US20230056253A1

公开(公告)日：2023-02-23

申请号：US17354203

申请日：2021-06-22

Applicant: PMV Pharmaceuticals, Inc.

Inventor： Binh VU ,  Romyr DOMINIQUE ,  Hongju LI ,  Bruce FAHR ,  Yi CHEN

IPC: C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D209/34 ,  C07D409/04 ,  C07D413/04 ,  C07D471/04 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14

Abstract: Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

公开(公告)号：US11584765B2

公开(公告)日：2023-02-21

申请号：US16885604

申请日：2020-05-28

Applicant: Ecstasy LLC

Inventor： Xiaodong Wang ,  Hua Zhong

IPC: C07D205/04 ,  C07D409/04 ,  C07D211/12 ,  C07D211/34 ,  C07D223/04 ,  C07D223/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07F5/02 ,  C07D475/00 ,  C07D211/14 ,  C07D207/09 ,  C07D417/06 ,  C07D417/10 ,  C07D409/06 ,  C07D451/02 ,  C07D473/00 ,  C07D471/08 ,  C07D513/04

Abstract: The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

公开(公告)号：US20230043159A1

公开(公告)日：2023-02-09

申请号：US17282176

申请日：2019-10-02

Applicant: DISC MEDICINE, INC.

Inventor： Srikanth Venkatraman ,  Subhendu Mukherjee ,  Rajeev Goswami ,  Venkateshwar Rao Gummadi ,  A. Bharathi Raja ,  Martuza Hadianawala

IPC: C07D471/04 ,  C07D401/12 ,  C07D403/12 ,  C07D401/14 ,  C07D209/42 ,  C07D403/14 ,  C07D413/10 ,  C07D417/12 ,  C07D409/12 ,  C07D413/14 ,  C07D409/06 ,  C07D405/12 ,  C07D233/28 ,  C07D417/04 ,  C07D413/04 ,  C07D401/06 ,  C07D471/08

Abstract: The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

公开(公告)号：US20230041523A1

公开(公告)日：2023-02-09

申请号：US17610758

申请日：2020-05-14

Applicant: The Scripps Research Institute

Inventor： Corinne Lasmézas ,  Minghai Zhou ,  Thomas D. Bannister

IPC: C07D487/04 ,  C07D401/06 ,  C07D405/14 ,  C07D471/04 ,  C07D417/04 ,  C07D277/42 ,  C07D513/04 ,  C07D311/30 ,  C07H17/07 ,  C07D217/10 ,  C07D217/04 ,  C07D401/14 ,  C07D413/14

Abstract: Compounds described herein may be used for the treatment of neurodegenerative diseases linked to protein misfolding, including prion diseases, Alzheimer's disease, Parkinson's disease (PD) and amyotrophic lateral sclerosis (ALS), and also other neurodegenerative, degenerative, metabolic and ischemic conditions. Indeed, NAD metabolism impairment is also a critical feature in brain ischemia/reperfusion injury, Wallerian degeneration, kidney failure, multiple sclerosis, aging, and metabolic disorders such as diabetes mellitus. Therapies that elevate or stabilize NAD levels may thus have broad potential for treating many severely debilitating neurological and metabolic conditions. Evidence is provided herein with compounds from 8 lead series for NAD restoring properties and for therapeutic efficacy in cellular and/or animal models of prion disease, PD and ALS.