公开(公告)号：US20240140911A1

公开(公告)日：2024-05-02

申请号：US18542913

申请日：2023-12-18

申请人： Arena Pharmaceuticals, Inc.

发明人： Anthony C. Blackburn ,  Ryan O. Castro ,  Mark Allen Hadd ,  You-An Ma ,  Antonio Garrido Montalban ,  Jaimie Karyn Rueter ,  Lee Alani Selvey ,  Sagar Raj Shakya ,  Marlon Carlos

IPC分类号： C07D209/94 ,  C07C279/12

CPC分类号： C07D209/94 ,  C07C279/12 ,  C07B2200/13

摘要： The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

公开(公告)号：US20240000732A1

公开(公告)日：2024-01-04

申请号：US17854360

申请日：2022-06-30

申请人： JOONG HO MOON ,  MICHELLE MIRANDA

发明人： JOONG HO MOON ,  MICHELLE MIRANDA

IPC分类号： A61K31/17 ,  C07D295/215 ,  C07C279/12 ,  A61K31/496 ,  A61K31/498 ,  A61K31/47 ,  A61K31/277 ,  A61K31/5377 ,  A61K31/4409 ,  A61K31/4965 ,  A61K31/133 ,  A61P31/06 ,  C08G65/00 ,  C08G71/02

CPC分类号： A61K31/17 ,  C07D295/215 ,  C07C279/12 ,  A61K31/496 ,  A61K31/498 ,  A61K31/47 ,  A61K31/277 ,  A61K31/5377 ,  A61K31/4409 ,  A61K31/4965 ,  A61K31/133 ,  A61P31/06 ,  C08G65/00 ,  C08G71/02 ,  C07C2601/16

摘要： The subject invention provides oligo(carbamoylated guanidine)s (OCGs) having fast and selective mycobactericidal effects via disruption of the mycobacterial membrane potential. OCGs also potentiates bedaquiline, an oxidative phosphorylation-targeting anti-TB drug. The combination of OCG and anti-TB drug can be used as an effective therapy for treating tuberculosis.

公开(公告)号：US11660350B2

公开(公告)日：2023-05-30

申请号：US15508651

申请日：2015-09-04

申请人： UNIVERSITY OF LINCOLN

发明人： Ishwar Singh ,  Edward Taylor

IPC分类号： A61K47/64 ,  C07C277/08 ,  A61K38/14 ,  C07C271/20 ,  C07C279/12 ,  A61K38/16 ,  C07H13/00 ,  A61K47/59 ,  A61P31/04 ,  A61K31/7034 ,  A61K31/7056

CPC分类号： A61K47/64 ,  A61K31/7034 ,  A61K31/7056 ,  A61K38/14 ,  A61K38/164 ,  A61K47/59 ,  A61P31/04 ,  C07C271/20 ,  C07C277/08 ,  C07C279/12 ,  C07H13/00 ,  C07C277/08 ,  C07C279/12

摘要： The invention provides a combination of an antibacterial agent (in particular vancomycin or moenomycin) and a delivery agent, in which the delivery agent is bonded, or capable of binding, to the antibacterial agent, and in which the delivery agent is capable of binding to one or more structures on a bacterial cell membrane. The invention further provides the use of such combinations in treating or preventing bacterial infections.

公开(公告)号：US11465989B2

公开(公告)日：2022-10-11

申请号：US15304798

申请日：2015-04-17

申请人： IMMUNOMET THERAPEUTICS INC.

发明人： Sung Wuk Kim ,  Hong Woo Kim ,  Sang Hee Yoo ,  Ji Sun Lee ,  Hye Jin Heo ,  Hong Bum Lee ,  Ji Ae Kook ,  Young Woo Lee ,  Mi Jeong Kim ,  Woong Cho

IPC分类号： C07D295/13 ,  C07D213/38 ,  C07D213/40 ,  C07D333/20 ,  C07D333/16 ,  C07D249/14 ,  C07D251/18 ,  C07D251/48 ,  C07D211/14 ,  C07D211/54 ,  C07D209/44 ,  C07D209/40 ,  C07D233/88 ,  C07D233/91 ,  C07D207/46 ,  C07D279/08 ,  C07D203/12 ,  C07D239/42 ,  C07D263/48 ,  C07D319/18 ,  C07D317/58 ,  C07D277/46 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P3/06 ,  A61P5/50 ,  A61P13/00 ,  A61P21/00 ,  A61P35/00 ,  A61P35/04 ,  A61P9/00 ,  A61P19/10 ,  A61P1/16 ,  A61P15/00 ,  C07C279/16 ,  C07C311/47 ,  C07C311/49 ,  C07C279/12 ,  C07C279/26 ,  C07C279/24 ,  C07C279/08 ,  C07C279/04 ,  C07C279/06 ,  C07D403/12 ,  C07D207/16

摘要： The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.

公开(公告)号：US20210347949A1

公开(公告)日：2021-11-11

申请号：US17382452

申请日：2021-07-22

申请人： Alliance for Sustainable Energy, LLC

发明人： Tao DONG ,  Lieve M.L. LAURENS ,  Philip T. PIENKOS ,  Paris Fabian SPINELLI

IPC分类号： C08G71/04 ,  C07C269/04 ,  C07C271/16 ,  C07C271/20 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C279/12

摘要： The present disclosure relates to methods for producing polymers and resins, the method including a first reacting of at least a first diamine with a first carbonate-containing compound and a second carbonate-containing compound to produce at least one of the polymer or the resin, where the first reacting is according to each of R1, R2, R3, and R4 include at least one of a hydrogen atom, a methyl group, a saturated hydrocarbon chain, and/or an unsaturated hydrocarbon chain, and R comprises at least one of a carbon atom, a saturated hydrocarbon chain, and/or an unsaturated hydrocarbon chain.

公开(公告)号：US20210163399A1

公开(公告)日：2021-06-03

申请号：US17262082

申请日：2019-07-24

申请人： PROTECH Co., Ltd.

发明人： Yong Tae Kwon ,  Chang Hoon Ji ,  Srinivasrao Ganipisetti ,  Hee Yeon Kim ,  Su Ran Mun ,  Chan Hoon Jung ,  Eui Jung Jung ,  Ki Woon Sung

IPC分类号： C07C217/58 ,  C07C279/12 ,  C07C275/24 ,  C07C235/06 ,  C07C237/06 ,  A61P25/28

摘要： The present invention relates to a novel p62 ligand compound, a stereoisomer, hydrate, solvate or prodrug thereof, and a pharmaceutical or food composition for preventing or treating misfolded protein diseases comprising the same as an active ingredient. The p62 ligand compound according to the present invention can be usefully used as a pharmaceutical composition for the prevention, amelioration or treatment of various proteinopathies by activating selective autophagy in cells and thus selectively eliminating in vivo proteins, organelles and aggregates.

公开(公告)号：US10821096B1

公开(公告)日：2020-11-03

申请号：US16986863

申请日：2020-08-06

申请人： King Abdulaziz University

发明人： Moustafa E. El-Araby ,  Abdelsattar Mansour Omar ,  Mahmoud Abdelkhalek El-Faky ,  Sameh Hamdy Abdelmageed Soror ,  Maan Talaat Khayat ,  Hani Zakariah Asfour ,  Faida Hassan Bamane

IPC分类号： A61K31/4164 ,  A61K31/55 ,  C07D233/64 ,  C07D233/54 ,  C07C279/04 ,  C07C279/10 ,  C07C279/12 ,  C07D279/16 ,  A61P31/14

摘要： Imidazole-based compounds as hepatitis C virus (HCV) inhibitors. The compounds have an imidazole core that is disubstituted via amide links. Also described are a pharmaceutical composition incorporating the imidazole-based compound, a method of preparing these compounds, and a method for using the pharmaceutical composition in the treatment of HCV infection.

公开(公告)号：US10570088B2

公开(公告)日：2020-02-25

申请号：US15683739

申请日：2017-08-22

申请人： Human BioMolecular Research Foundation

发明人： John R. Cashman ,  Jaroslaw Kalisiak

IPC分类号： C07C251/40 ,  C07C279/12 ,  C07C257/12 ,  C07C257/14 ,  C07C257/18 ,  C07D239/06 ,  C07D249/04 ,  C07D233/24

摘要： The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.

公开(公告)号：US10442756B2

公开(公告)日：2019-10-15

申请号：US15846084

申请日：2017-12-18

申请人： ModernaTX, Inc.

发明人： Kerry E. Benenato ,  Mark Cornebise

IPC分类号： C07C229/12 ,  A61K9/127 ,  C07C271/20 ,  C07C279/12 ,  C07C279/28 ,  C07C279/32 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D207/27 ,  C07D277/38 ,  C07C275/14 ,  C07C279/24 ,  C07C311/05 ,  C07C229/16 ,  C07C335/08 ,  C07C233/36 ,  C07C233/72 ,  C07C263/20 ,  C07C235/10 ,  C07C255/24 ,  C07F9/09 ,  A61K9/16 ,  A61K38/18 ,  A61K48/00 ,  C07K14/505 ,  A61K9/00 ,  A61K47/54 ,  A61K47/69 ,  C07C227/16 ,  A61K9/51 ,  A61K31/7105 ,  A61K38/17 ,  C07C227/18

摘要： The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

公开(公告)号：US10414796B2

公开(公告)日：2019-09-17

申请号：US15537125

申请日：2015-12-14

申请人： Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional

发明人： Pablo Cruz Morales ,  Francisco Barona Gómez ,  Hilda Eréndira Ramos Aboites

IPC分类号： C12N15/70 ,  C07K5/065 ,  C07C279/12 ,  C12N15/63

摘要： The present invention describes a new peptide aldehyde produced naturally by Streptomyces lividans 66, which we have called livipeptin. Using genome mining of natural products, we predicted that SLI0883-5 genes encode an unprecedented biosynthetic system, unusually small (4.6 Kbp), which produces an acylated peptide aldehyde. Because of the chemical characteristics of the predicted compound, we postulated its anti-proteolytic activity, which we confirmed by identifying and purifying this compound through metabolic profiles of HPLC and MS of the mutated strain lacking these three genes and the wild strain. To this objective, we identified the conditions wherein these genes are strongly expressed. The livipeptin was purified and its inhibitory activity on the proteolytic activity of selected proteases was demonstrated in vitro. The design of an expression cassette for its heterologous expression is also described plus its use for heterologous protein production.