公开(公告)号：US20240327334A1

公开(公告)日：2024-10-03

申请号：US18390287

申请日：2023-12-20

申请人： Enanta Pharmaceuticals, Inc.

发明人： Xuri GAO ,  Bin WANG ,  Hui CAO ,  Jiajun ZHANG ,  Yuk Ming SIU ,  Jiang LONG ,  Wei LI ,  Matthew C. RHODES ,  Xuechao XING ,  Jianming YU ,  Scott MITCHELL ,  Yat Sun OR

IPC分类号： C07C233/56 ,  A61K31/166 ,  A61K31/277 ,  A61K31/337 ,  A61K31/365 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/662 ,  A61P31/14 ,  C07C243/30 ,  C07C255/46 ,  C07C255/66 ,  C07D205/04 ,  C07D207/16 ,  C07D209/52 ,  C07D209/56 ,  C07D213/40 ,  C07D215/12 ,  C07D231/08 ,  C07D231/12 ,  C07D231/56 ,  C07D239/26 ,  C07D241/12 ,  C07D249/06 ,  C07D263/32 ,  C07D263/34 ,  C07D265/02 ,  C07D277/28 ,  C07D295/185 ,  C07D305/08 ,  C07D307/58 ,  C07D333/20 ,  C07D333/24 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14 ,  C07F9/40

CPC分类号： C07C233/56 ,  A61K31/166 ,  A61K31/277 ,  A61K31/337 ,  A61K31/365 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/662 ,  A61P31/14 ,  C07C243/30 ,  C07C255/46 ,  C07C255/66 ,  C07D205/04 ,  C07D207/16 ,  C07D209/52 ,  C07D209/56 ,  C07D213/40 ,  C07D215/12 ,  C07D231/08 ,  C07D231/12 ,  C07D231/56 ,  C07D239/26 ,  C07D241/12 ,  C07D249/06 ,  C07D263/32 ,  C07D263/34 ,  C07D265/02 ,  C07D277/28 ,  C07D295/185 ,  C07D305/08 ,  C07D307/58 ,  C07D333/20 ,  C07D333/24 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14 ,  C07F9/4015

摘要： The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof:




which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240301417A1

公开(公告)日：2024-09-12

申请号：US18570892

申请日：2022-06-15

申请人： Sanford Burnham Prebys Medical Discovery Institute

发明人： Cynthia LEBEAUPIN ,  Randal J. KAUFMAN ,  Clementine DRUELLE

IPC分类号： C12N15/113 ,  A61K31/421 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K49/00 ,  A61P35/00

CPC分类号： C12N15/113 ,  A61K31/421 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K49/0008 ,  A61P35/00 ,  C12N2310/11 ,  C12N2310/351

摘要： Described herein are compositions and methods useful for detecting and treating pathologies associated with ATF in hepatocytes. A method of detecting a condition, a method of inhibiting a protein, a method of inhibiting a gene, and a method of treatment are disclosed herein. The present disclosure includes, but is not limited to, the development and testing of Atf6-specific short, synthetic, single-stranded antisense oligodeoxynucleotides (ASOs) in vitro and in vivo and future screening for ATF6 inhibitors.

公开(公告)号：US20240238374A1

公开(公告)日：2024-07-18

申请号：US18561769

申请日：2022-05-20

申请人： ENERGESIS PHARMACEUTICALS, INC.

发明人： OLIVIER D. BOSS ,  BRIAN FREEMAN

IPC分类号： A61K38/18 ,  A61K31/195 ,  A61K31/421 ,  A61K45/06 ,  A61P3/04 ,  A61P3/10

CPC分类号： A61K38/1825 ,  A61K31/195 ,  A61K31/421 ,  A61K45/06 ,  A61P3/04 ,  A61P3/10

摘要： This disclosure features compositions and methods for the treatment of metabolic disorders such as diabetes and obesity.

公开(公告)号：US20240197687A1

公开(公告)日：2024-06-20

申请号：US18215170

申请日：2023-06-28

申请人： Primus Pharmaceuticals, Inc.

发明人： Francesco Squadrito ,  James C. Lukban ,  Ryan E. Hartung ,  Garrett A. Campbell

IPC分类号： A61K31/421 ,  A61K9/20 ,  A61P25/02 ,  A61P29/00

CPC分类号： A61K31/421 ,  A61K9/2018 ,  A61P25/02 ,  A61P29/00

摘要： A method of neuroinflammation and conditions associated therewith including chronic and acute conditions as well as specific and non-specific conditions. Oral dosage forms containing 640 mg micronized and non-micronized particulate metaxalone and excipients including alginic acid and propylene glycol alginate. The method includes inhibiting the monoamine oxidase A (MAO-A) enzyme as well as restoring/upregulating/increasing IL-13 and PGC-1α. The treated conditions, among others, include diabetic neuropathy, fibromyalgia, back pain, chronic pain induced depression, restless leg syndrome, anxiety, mood disorder, peripheral neuropathy, and herpetic neuralgia. The method further includes inducing or restoring homeostasis, restoring oxidative homeostasis, restoring basal phenotype from a neuroinflammatory state and improving neuroplasticity.

公开(公告)号：US11992560B2

公开(公告)日：2024-05-28

申请号：US17251601

申请日：2018-06-14

申请人： ALMA MATER STUDIORUM—UNIVERSITÀ DI BOLOGNA

发明人： Laura Calza ,  Luciana Giardino ,  Maria Letizia Focarete ,  Chiara Gualandi ,  Maria-Laura Bolognesi ,  Nadia Passerini ,  Giampiero Pagliuca ,  Teresa Gazzotti ,  Elisa Zironi

IPC分类号： A61K9/70 ,  A61K9/00 ,  A61K31/12 ,  A61K31/19 ,  A61K31/192 ,  A61K31/196 ,  A61K31/197 ,  A61K31/198 ,  A61K31/40 ,  A61K31/405 ,  A61K31/407 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4418 ,  A61K31/5415 ,  A61K31/5575 ,  A61K31/603 ,  A61K31/704 ,  A61P25/28

CPC分类号： A61K9/70 ,  A61K9/0024 ,  A61K31/12 ,  A61K31/19 ,  A61K31/192 ,  A61K31/196 ,  A61K31/197 ,  A61K31/198 ,  A61K31/40 ,  A61K31/405 ,  A61K31/407 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4418 ,  A61K31/5415 ,  A61K31/5575 ,  A61K31/603 ,  A61K31/704 ,  A61P25/28

摘要： The present invention relates to electro spun fibers for a local release in the central nervous system of an anti-inflammatory and a promyelinating agent over a defined time-window, in order to limit secondary neurodegeneration triggered by the glutamate release and supported by on-going inflammation. The combined treatment aimed to reduce inflammation and improve remyelination in the very early stage of the pathology improving the chronic clinical outcome of the lesion. In particular the present invention relates to electrospun polymeric fibers, wherein said fibers are loaded with 3,3,5-Triiodo-L-thyronine (T3) and Ibuprofen.

公开(公告)号：US20240150304A1

公开(公告)日：2024-05-09

申请号：US18221353

申请日：2023-07-12

申请人： iCeutica Inc.

发明人： H. William Bosch

IPC分类号： C07D263/24 ,  A61K9/14 ,  A61K31/421

CPC分类号： C07D263/24 ,  A61K9/145 ,  A61K31/421 ,  A61K9/20

摘要： Dosage forms of metaxalone containing submicron particles of metaxalone and uses thereof are described. The submicron dosage forms have improved bioavailability compared to certain conventional metaxalone dosage forms.

公开(公告)号：US11813304B2

公开(公告)日：2023-11-14

申请号：US16512210

申请日：2019-07-15

申请人： Ardelyx, Inc.

发明人： Dominique Charmot ,  Jason G. Lewis ,  Jeffrey W. Jacobs ,  Ingrid Langsetmo ,  Christopher Carreras

IPC分类号： A61K38/10 ,  A61K31/00 ,  A61K38/16 ,  A61K31/195 ,  A61K31/27 ,  A61K31/352 ,  A61K31/353 ,  A61K31/382 ,  A61K31/4045 ,  A61K31/421 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/475 ,  A61K31/506 ,  A61K31/7072 ,  A61K33/26 ,  A61K45/06 ,  G01N33/50 ,  G01N33/84

CPC分类号： A61K38/10 ,  A61K31/00 ,  A61K31/195 ,  A61K31/27 ,  A61K31/352 ,  A61K31/353 ,  A61K31/382 ,  A61K31/4045 ,  A61K31/421 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/475 ,  A61K31/506 ,  A61K31/7072 ,  A61K33/26 ,  A61K38/16 ,  A61K45/06 ,  G01N33/5038 ,  G01N33/5044 ,  G01N33/84 ,  A61K31/00 ,  A61K2300/00 ,  A61K38/10 ,  A61K2300/00 ,  A61K38/16 ,  A61K2300/00

摘要： Provided are non-NHE3-binding agents having activity as phosphate transport/uptake inhibitors in the gastrointestinal tract, including in the small intestine, methods for their use as therapeutic or prophylactic agents, and related methods of drug discovery.

公开(公告)号：US11760754B2

公开(公告)日：2023-09-19

申请号：US16761210

申请日：2018-11-02

申请人： UNIVERSITÉ DE MONTRÉAL

发明人： Yves Gareau ,  Stéphane Gingras ,  Yves Chantigny ,  Gaoqiang Yang ,  Guy Sauvageau ,  Irène Baccelli ,  Anne Marinier

IPC分类号： C07D413/12 ,  C07D263/32 ,  C07D263/34 ,  C07D417/12 ,  A61K31/421 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  A61P35/02 ,  C07D249/04 ,  C07D277/24 ,  G01N33/50

CPC分类号： C07D417/12 ,  C07D249/04 ,  C07D263/32 ,  C07D263/34 ,  C07D277/24 ,  C07D413/12 ,  G01N33/5011

摘要： Heterocyclic compounds of Formula (I) and pharmaceutically acceptable salt thereof are disclosed. The use of such heterocyclic compounds and pharmaceutically acceptable salt thereof for the treatment of cancers, and more particularly cancers sensitive to mitochondrial activity inhibition and increased reactive oxygen species (ROS) levels, is also disclosed. Such cancers include acute myeloid leukemia (AML), preferably AML characterized by certain features, such as high level of expression of one or more Homeobox (HOX)-network genes, high and/or low expression of specific genes, the presence of one or more cytogenetic or molecular risk factors such as intermediate cytogenetic risk, Normal Karyotype (A/K), mutated NPM1, mutated CEBPA, mutated FLT3, mutated DNMT3A, mutated TET2, mutated IDH1, mutated IDH2, mutated RUNX1, mutated WT1, mutated SRSF2, intermediate cytogenetic risk with abnormal karyotype (intern(abnK)), trisomy 8 (+8) and/or abnormal chromosome (5/7), and/or a high leukemic stem cell (LSC) frequency.

公开(公告)号：US11752115B2

公开(公告)日：2023-09-12

申请号：US16014607

申请日：2018-06-21

申请人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS

发明人： Graziano Pinna ,  Andrea Locci

IPC分类号： A61K31/16 ,  A61P25/22 ,  A61P25/24 ,  A61K31/216 ,  A61K31/505 ,  A61K31/402 ,  A61K31/403 ,  A61K31/421 ,  A61K31/422 ,  A61K31/045 ,  A61K31/192

CPC分类号： A61K31/16 ,  A61P25/22 ,  A61P25/24 ,  A61K31/045 ,  A61K31/192 ,  A61K31/216 ,  A61K31/402 ,  A61K31/403 ,  A61K31/421 ,  A61K31/422 ,  A61K31/505 ,  A61K2300/00

摘要： Described herein are PPARα agonists, including, but not limited to, endocannabinoids that can be used for treatment of a neuropsychiatric disorder and/or symptom thereof. Also described herein are pharmaceutical formulations containing an effective amount of a PPARα agonists, including but not limited to endocannabinoids, where the effective amount is effective for treating a neuropsychiatric disorder and/or symptom thereof. Also described herein are methods of treating a neuropsychiatric disorder and/or a symptom thereof in a subject in need thereof.

公开(公告)号：US11723897B2

公开(公告)日：2023-08-15

申请号：US17070769

申请日：2020-10-14

申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education

发明人： Bruce A. Freeman ,  Francisco J. Schopfer

IPC分类号： A61K31/426 ,  A61K31/231 ,  A61K31/232 ,  A61K31/12 ,  A61K31/4166 ,  A61K31/4192 ,  A61K31/421

CPC分类号： A61K31/426 ,  A61K31/12 ,  A61K31/231 ,  A61K31/232 ,  A61K31/4166 ,  A61K31/4192 ,  A61K31/421 ,  Y02A50/30

摘要： Compounds of formula I and their metabolites are potent mediators of an inflammatory response:




where a, b, c, d, e, f, V, W, X, Y, Ra, Ra′, Rb, Rb′, Rc, and Rc′ are defined herein. In particular, the compounds of the invention are candidate therapeutics for treating inflammatory conditions.