公开(公告)号：US20240217979A1

公开(公告)日：2024-07-04

申请号：US18287844

申请日：2022-04-21

申请人： Emory University

发明人： Dennis C. Liotta ,  Stephen F. Traynelis ,  David S. Menaldino ,  Peipei Ma

IPC分类号： C07D487/04 ,  A61K31/415 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5025 ,  A61K31/519 ,  C07D231/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

CPC分类号： C07D487/04 ,  A61K31/415 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5025 ,  A61K31/519 ,  C07D231/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

摘要： Compounds that selectively inhibit the GluN2 subunits of NMDA receptors are disclosed. In general, the compounds have superior activity against GluN2C/D subunit(s) over GluN2A/B subunit(s). Optionally, the compounds have a structure of Formulas (I), (II), (III), or other formulas disclosed herein, enantiomers or diastereomers thereof, or pharmaceutically acceptable salts thereof. Pharmaceutical formulations containing one or more of the compounds are also disclosed. Additionally, methods of treating a neurological condition or disorder using the compounds or their pharmaceutical formulations thereof are disclosed. Exemplary neurological conditions or disorders include Parkinson's disease, dystonia and related motor disorders, depression, neuropsychiatric indications, stoke, hypoxia, traumatic brain injury, acute injuries involving the white matter, Alzheimer's disease, compulsivity and related disorders, and epilepsy.

公开(公告)号：US11939297B2

公开(公告)日：2024-03-26

申请号：US18108264

申请日：2023-02-10

申请人： The USA, as represented by the Secretary, Department of Health and Human Services

发明人： George Kunos ,  Malliga Iyer ,  Resat Cinar ,  Kenner C. Rice

IPC分类号： C07D231/06 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D231/06 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.

公开(公告)号：US11820763B2

公开(公告)日：2023-11-21

申请号：US17375635

申请日：2021-07-14

申请人： Lead High Technology (QingDao) Co., Ltd

发明人： Dayong Shi ,  Xiangqian Li ,  Xin Wang ,  Jinbo Yang

IPC分类号： C07D231/06 ,  C07D417/04 ,  A61P31/14

CPC分类号： C07D417/04 ,  A61P31/14 ,  C07D231/06

摘要： The present invention relates to a compound, and in particular to a bromophenol-pyrazoline compound and a synthesis method and use thereof. The bromophenol-pyrazoline compound is represented by a general structural formula below:




The bromophenol-pyrazoline compound provided in the present invention has efficient inhibitory activity against the main protease Mpro, and interferes with the replication of coronavirus in cells, indicating that the compound has the effect of treating coronavirus pneumonia and thus has a broad prospect of application in the preparation of drugs for treating coronavirus pneumonia.

公开(公告)号：US11753381B2

公开(公告)日：2023-09-12

申请号：US17033104

申请日：2020-09-25

申请人： Board of Regents, The University of Texas System

发明人： Richard T. Lewis ,  Matthew Michael Hamilton ,  William J. Ray ,  Fernando Alvarez ,  Dana E. Pfaffinger ,  Naphtali Reyna ,  Jason Cross ,  Suyambu Kesava Vijayan Ramaswamy

IPC分类号： C07D231/06 ,  A61K31/4965 ,  A61K31/415 ,  A61K31/416 ,  C07D231/56 ,  C07D403/12 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  A61K31/4439 ,  C07D471/04 ,  A61K31/437 ,  C07D403/08 ,  A61K31/4155 ,  C07D413/08 ,  A61K31/4245 ,  A61K31/4184 ,  C07D207/10 ,  A61K31/40 ,  A61K31/4015 ,  C07D401/12 ,  C07D403/14 ,  A61K31/497 ,  A61K31/4192 ,  C07D487/04 ,  A61K31/4985 ,  C07D417/14 ,  A61K31/427 ,  C07D241/24 ,  A61K45/06

CPC分类号： C07D231/06 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/4965 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/10 ,  C07D231/56 ,  C07D241/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D413/08 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.

公开(公告)号：US11672779B2

公开(公告)日：2023-06-13

申请号：US17095399

申请日：2020-11-11

申请人： UNM Rainforest Innovations

发明人： Angela Wandinger-Ness ,  Laurie Hudson ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea

IPC分类号： A61K31/407 ,  A61K31/415 ,  C07D231/06 ,  A61K45/06 ,  A61K31/403 ,  C12Q1/6886 ,  G01N33/573

CPC分类号： A61K31/407 ,  A61K31/403 ,  A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  C12Q1/6886 ,  G01N33/573 ,  C12Q2600/106 ,  C12Q2600/158 ,  Y02A50/30 ,  A61K31/415 ,  A61K2300/00

摘要： The present invention relates to molecules which function as modulators (i.e., inhibitors and agonists) of the Ras-homologous (Rho) family of small GTPases (e.g. Rac, Cdc42 and Rho GTPases) and their use to treat diseases, including cancers (including solid tumors-medulloblastoma, ovarian, breast, head and neck, testicular, prostate among others and hematologic malignancies-B cell lymphoma, where these GTPases are overexpressed or hyperactivated), sporadic and genetic diseases where activation of Rho GTPases plays a pivotal role (Menkes disease, rheumatoid arthritis, atherosclerosis, diabetes (type I), Huntington's disease and Alzheimer's disease) which are mediated through these proteins. Compounds according to the present invention may also be used as a therapy for the treatment of Entamoeba spp. or Acanthamoeba spp. infections, especially including Entamoeba histolytica.

公开(公告)号：US20220363644A1

公开(公告)日：2022-11-17

申请号：US17869819

申请日：2022-07-21

申请人： Shandong Linghai Biotechnology Co., Ltd.

发明人： Dayong Shi ,  Xiangqian Li ,  Xin Wang ,  Feng Xu

IPC分类号： C07D231/06 ,  A61P31/14

摘要： The present invention belongs to the field of medical technology, and specifically relates to use of bromophenol-pyrazoline compounds for the treatment of feline coronavirus diseases. Studies carried out for the present invention revealed that bromophenol-pyrazoline compounds could inhibit activity of feline infectious peritonitis virus main protease (FIPV Mpro) and interfere with replication of feline infectious peritonitis virus (FIPV) in cells. In a clinical trial, the bromophenol-pyrazoline compounds can treat infectious peritonitis in cats naturally infected with the FIPV, greatly improve survival rate of cats, and can be used to prepare drugs for treating feline infectious peritonitis.

公开(公告)号：US11485710B2

公开(公告)日：2022-11-01

申请号：US17156478

申请日：2021-01-22

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： Niall Andrew Anderson ,  Deepak Bandyopadhyay ,  Alain Claude-Marie Daugan ,  Frederic G. Donche ,  Patrick M. Eidam ,  Nicolas Eric Faucher ,  Nicolas S. George ,  Philip Anthony Harris ,  Jae U. Jeong ,  Bryan W. King ,  Clark A. Sehon ,  Gemma Victoria White ,  David Duff Wisnoski

IPC分类号： A61K31/415 ,  C07D231/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/14 ,  C07D417/14 ,  C07D403/04 ,  C07D487/04 ,  A61P21/00 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  C07D403/06 ,  C07D409/06 ,  C07D413/04

摘要： Disclosed are compounds having the formula: wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.

公开(公告)号：US11325898B2

公开(公告)日：2022-05-10

申请号：US17112980

申请日：2020-12-04

申请人： Board of Regents, The University of Texas System

发明人： Jef De Brabander ,  Qiren Liang ,  Beth Levine ,  Wei-Chung Chiang

IPC分类号： C07D405/04 ,  C07D405/14 ,  C07D231/06 ,  C07D403/04 ,  C07D231/12 ,  C07D401/04 ,  C07D413/10 ,  C07D413/04 ,  C07D409/04 ,  C07D405/06 ,  C07D417/04 ,  C07D405/12

摘要： Small molecule disruptors of Beclin-1/Bcl-2 protein-protein interactions induce autophagy and hence are useful for treating a variety of indications where stimulation of autophagy is therapeutically useful, including cancer, infection immunity, neurodegeneration, longevity.

公开(公告)号：US20210253532A1

公开(公告)日：2021-08-19

申请号：US17156478

申请日：2021-01-22

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： Niall Andrew Anderson ,  Deepak Bandyopadhyay ,  Alain Claude-Marie Daugan ,  Frederic G. Donche ,  Patrick M. Eidam ,  Nicolas Eric Faucher ,  Nicolas S. George ,  Philip Anthony Harris ,  Jae U. Jeong ,  Bryan W. King ,  Clark A. Sehon ,  Gemma Victoria White ,  David Duff Wisnoski

IPC分类号： C07D231/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/14 ,  C07D417/14 ,  C07D403/04 ,  C07D487/04 ,  A61P21/00 ,  A61K31/415 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  C07D403/06 ,  C07D409/06 ,  C07D413/04

摘要： Disclosed are compounds having the formula: wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.

公开(公告)号：US10899716B2

公开(公告)日：2021-01-26

申请号：US16778206

申请日：2020-01-31

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Niall Andrew Anderson ,  Deepak Bandyopadhyay ,  Alain Claude-Marie Daugan ,  Frederic G. Donche ,  Patrick M. Eidam ,  Nicolas Eric Faucher ,  Nicolas S. George ,  Philip Anthony Harris ,  Jae U. Jeong ,  Bryan W. King ,  Clark A. Sehon ,  Gemma Victoria White ,  David Duff Wisnoski

IPC分类号： A61K31/4439 ,  C07D401/06 ,  C07D231/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/14 ,  C07D417/14 ,  C07D403/04 ,  C07D487/04 ,  A61P21/00 ,  A61K31/415 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  C07D403/06 ,  C07D409/06 ,  C07D413/04

摘要： Disclosed are compounds having the formula: wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.