公开(公告)号：US12065459B2

公开(公告)日：2024-08-20

申请号：US16672114

申请日：2019-11-01

申请人： Achillion Pharmaceuticals, Inc.

发明人： Jason Allan Wiles ,  Venkat Rao Gadhachanda ,  Qiuping Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Dawei Chen ,  Xiangzhu Wang ,  Atul Agarwal ,  Milind Deshpande ,  Avinash S. Phadke

IPC分类号： C07F9/572 ,  A61K9/00 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/00 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F7/08 ,  C07F9/6558 ,  C07F9/6561

CPC分类号： C07F9/5728 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/002 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/025 ,  C07F5/027 ,  C07F7/0812 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65616 ,  C07B2200/05

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

公开(公告)号：US20240132948A1

公开(公告)日：2024-04-25

申请号：US18183418

申请日：2023-03-14

申请人： Pacific Biosciences of California, Inc.

发明人： Stephen YUE ,  Gene SHEN ,  Wei-Chuan (David) SUN

IPC分类号： C12Q1/6869 ,  C07D209/14 ,  C07D401/14 ,  C07D405/14 ,  C07H19/10 ,  C07K5/09 ,  C07K5/11 ,  C09B23/01 ,  C09B23/06 ,  C09B23/08 ,  C09B23/10 ,  C09B23/16 ,  C12Q1/6844 ,  C12Q1/6876 ,  G01N33/52 ,  G01N33/58

CPC分类号： C12Q1/6869 ,  C07D209/14 ,  C07D401/14 ,  C07D405/14 ,  C07H19/10 ,  C07K5/0815 ,  C07K5/1019 ,  C09B23/0025 ,  C09B23/0033 ,  C09B23/0066 ,  C09B23/06 ,  C09B23/083 ,  C09B23/105 ,  C09B23/164 ,  C12Q1/6844 ,  C12Q1/6876 ,  G01N33/52 ,  G01N33/582 ,  G01N2333/9126

摘要： The invention provides a novel class of cyanine dyes that are functionalized with sulfonic acid groups and a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.

公开(公告)号：US11939292B1

公开(公告)日：2024-03-26

申请号：US18386021

申请日：2023-11-01

申请人： Mydecine Innovations Group Inc.

发明人： Denton W. Hoyer ,  Robert F. Roscow

IPC分类号： C07D209/14 ,  C07D209/12 ,  C07D209/16 ,  C07D471/04

CPC分类号： C07D209/14 ,  C07D209/12 ,  C07D209/16 ,  C07D471/04

摘要： The present invention is directed to novel chemical compositions of matter and their methods of synthesis, and in particular novel analogs of Psilocin having enhanced physical and pharmacokinetic characteristics.

公开(公告)号：US11814373B2

公开(公告)日：2023-11-14

申请号：US17028720

申请日：2020-09-22

申请人： PMV Pharmaceuticals, Inc.

发明人： Binh Vu ,  Romyr Dominique ,  Hongju Li ,  Bruce Fahr ,  Andrew Good

IPC分类号： C07D405/14 ,  C07D209/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D491/107 ,  C07F7/08 ,  C07H15/26

CPC分类号： C07D405/14 ,  C07D209/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D491/107 ,  C07F7/0812 ,  C07H15/26

摘要： Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention 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：US20230322672A1

公开(公告)日：2023-10-12

申请号：US18043146

申请日：2021-08-30

申请人： VIEWPOINT THERAPEUTICS, INC.

发明人： Michael S. LOPEZ ,  Bryan M. DUNYAK

IPC分类号： C07D209/14 ,  A61P27/10 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04 ,  C07D401/12 ,  C07D491/048 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14

CPC分类号： C07D209/14 ,  A61P27/10 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04 ,  C07D401/12 ,  C07D491/048 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14

摘要： The present disclosure is directed to compounds, compositions, formulations and methods of use thereof in the treatment and prevention of ocular conditions including cataract and presbyopia.

公开(公告)号：US11773062B2

公开(公告)日：2023-10-03

申请号：US17208583

申请日：2021-03-22

申请人： Small Pharma Ltd.

发明人： Peter Rands ,  Ellen James ,  Tiffanie Benway

IPC分类号： C07D209/14

CPC分类号： C07D209/14 ,  C07B2200/05

摘要： Described herein are compounds of formula (I) as defined herein, which comprise a greater proportion of deuterium to protium than naturally found in hydrogen; and compositions, including pharmaceutical compositions, comprising these compounds and optionally analogous compounds of formula (I), which are not deuterium-enriched. These compounds and compositions are of use in therapy, in particular in the treatment of psychiatric or neurological disorders. Varying the amounts of the different compounds within the compositions of the invention allows tailoring of the compositions' therapeutic effects. A particularly efficient synthetic method which enables compounds of formula (I) and related compounds of formula (I′) is also provided.

公开(公告)号：US20230234963A1

公开(公告)日：2023-07-27

申请号：US17859505

申请日：2022-07-07

申请人： Nogra Pharma Limited

发明人： Francesca Viti ,  Salvatore Bellinvia ,  Salvatore Demartis

IPC分类号： C07D495/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07C233/29 ,  C07C233/73 ,  C07C235/38 ,  C07C235/46 ,  C07D209/08 ,  C07D209/14 ,  C07D209/86 ,  C07D209/94 ,  C07D213/75 ,  C07D235/30 ,  C07D277/64 ,  C07D277/82 ,  C07D333/36

CPC分类号： C07D495/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07C233/29 ,  C07C233/73 ,  C07C235/38 ,  C07C235/46 ,  C07D209/08 ,  C07D209/14 ,  C07D209/86 ,  C07D209/94 ,  C07D213/75 ,  C07D235/30 ,  C07D277/64 ,  C07D277/82 ,  C07D333/36

摘要： The present invention is generally directed towards compounds capable of binding the aryl hydrocarbon receptor and modulating its activity, methods of treating inflammatory conditions such as Crohn's disease using such compounds, and pharmaceutical compositions comprising such compounds. Also provided are methods of increasing levels of IL-22 in a subject and/or decreasing levels of IFN-γ in a subject.

公开(公告)号：US20230226062A1

公开(公告)日：2023-07-20

申请号：US17952460

申请日：2022-09-26

申请人： Incyte Corporation

发明人： Liangxing Wu ,  Ding-Quan Qian ,  Liang Lu ,  Neil Lajkiewicz ,  Leah C. Konkol ,  Zhenwu Li ,  Fenglei Zhang ,  Jingwei Li ,  Haisheng Wang ,  Meizhong Xu ,  Kaijiong Xiao ,  Wenqing Yao

IPC分类号： A61K31/519 ,  A61K31/4985 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/445 ,  A61K31/4375 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/429 ,  A61K31/426 ,  A61K31/4196 ,  A61K31/4162 ,  A61K31/4155 ,  A61K31/421 ,  A61K31/404 ,  A61K31/357 ,  A61K31/353 ,  A61K31/133 ,  A61P31/00 ,  A61P35/00 ,  A61K31/5025 ,  C07D513/04 ,  C07D217/04 ,  C07D211/60 ,  C07D403/06 ,  C07D209/44 ,  C07C215/28 ,  C07D495/04 ,  C07D401/06 ,  C07D211/56 ,  C07D217/02 ,  C07D213/74 ,  C07D209/14 ,  C07D311/04 ,  C07D401/12 ,  C07D211/58 ,  C07D471/10 ,  C07C215/08 ,  C07D487/04 ,  C07D295/02 ,  A61P37/00 ,  C07D213/38

CPC分类号： A61K31/519 ,  A61K31/4985 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/445 ,  A61K31/4375 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/429 ,  A61K31/426 ,  A61K31/4196 ,  A61K31/4162 ,  A61K31/4155 ,  A61K31/421 ,  A61K31/404 ,  A61K31/357 ,  A61K31/353 ,  A61K31/133 ,  A61P31/00 ,  A61P35/00 ,  A61K31/5025 ,  C07D513/04 ,  C07D217/04 ,  C07D211/60 ,  C07D403/06 ,  C07D209/44 ,  C07C215/28 ,  C07D495/04 ,  C07D401/06 ,  C07D211/56 ,  C07D217/02 ,  C07D213/74 ,  C07D209/14 ,  C07D311/04 ,  C07D401/12 ,  C07D211/58 ,  C07D471/10 ,  C07C215/08 ,  C07D487/04 ,  C07D295/02 ,  A61P37/00 ,  C07D213/38 ,  A61K2300/00

摘要： Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

公开(公告)号：US20220340522A1

公开(公告)日：2022-10-27

申请号：US17842367

申请日：2022-06-16

申请人： Janssen Pharmaceuticals, Inc. ,  Katholieke Universiteit Leuven

发明人： Jean-François Bonfanti ,  Bart Rudolf Romanie Kesteleyn ,  Dorothée Alice Marie-Eve Bardiot ,  Arnaud Didier M Marchand ,  Erwin Coesemans ,  Jérôme Michel Claude Fortin ,  Guillaume Jean Maurice Mercey ,  Pierre Jean-Marie Bernard Raboisson

IPC分类号： C07D209/14 ,  A61P31/14

摘要： The present invention concerns substituted indoline derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

公开(公告)号：US11407715B2

公开(公告)日：2022-08-09

申请号：US16612670

申请日：2018-05-18

申请人： JANSSEN PHARMACEUTICALS, INC. ,  KATHOLIEKE UNIVERSITEIT LEUVEN

发明人： Jean-François Bonfanti ,  Bart Rudolf Romanie Kesteleyn ,  Dorothée Alice Marie-Eve Bardiot ,  Arnaud Didier M Marchand ,  Erwin Coesemans ,  Jérôme Michel Claude Fortin ,  Guillaume Jean Maurice Mercey ,  Pierre Jean-Marie Bernard Raboisson

IPC分类号： C07D209/14 ,  A61P31/14 ,  A61K45/06

摘要： The present invention concerns substituted indoline derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.