公开(公告)号：US11534434B2

公开(公告)日：2022-12-27

申请号：US17099214

申请日：2020-11-16

申请人： Karuna Therapeutics, Inc.

发明人： James A. Monn ,  Clifford Adam Schlecht ,  Dennis A. Bennett ,  Giorgio Attardo

IPC分类号： C07D417/04 ,  A61K31/4439 ,  A61K31/46

摘要： Provided herein are compounds comprising compounds of formula I and/or salts thereof; wherein at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is fluorine, and the remainder are independently chosen from hydrogen and fluorine; and R14, R15, R16, R17, R18, R19, R20, R21, R22, and R23 are independently chosen from hydrogen and deuterium; with the proviso that when R1, R2, and R3 are fluorine, then at least one of R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is fluorine or at least one of R14, R15, R16, R17, R18, R19, R20, R21, R22, and R23 is deuterium. Also provided are medicaments comprising these compounds and methods for treating central nervous system disorders with the compounds and medicaments described herein.

公开(公告)号：US11471413B2

公开(公告)日：2022-10-18

申请号：US17143904

申请日：2021-01-07

申请人： Karuna Therapeutics, Inc.

发明人： Aimesther Betancourt ,  Bruce Rehlaender ,  Roch Thibert

IPC分类号： A61K9/16 ,  A61K31/439 ,  A61K31/454 ,  A61K9/48 ,  A61K9/00

摘要： Provided herein is an oral pharmaceutical composition, comprising a plurality of xanomeline beads having a core comprising xanomeline or a salt thereof; and a plurality of trospium beads having a core comprising a salt of trospium.

公开(公告)号：US11104736B2

公开(公告)日：2021-08-31

申请号：US17119207

申请日：2020-12-11

申请人： Ensemble Group Holdings

发明人： Michael David Kuo

IPC分类号： A61K39/395 ,  C07K16/28 ,  A61P35/04 ,  A61K39/00

摘要： Provided herein is a method for treating cancer in a patient in need thereof, wherein said cancer has a tumor proportion score (TPS) for programmed death receptor-1 (PD-1) or programmed death-ligand-1 (PD-L1) of 50% or less and said patient is negative for lymphatic dysfunction, comprising administering a therapeutically effective amount of an antagonist for immune checkpoint inhibition.

公开(公告)号：US10933020B2

公开(公告)日：2021-03-02

申请号：US16585532

申请日：2019-09-27

申请人： Karuna Therapeutics, Inc.

发明人： Aimesther Betancourt ,  Bruce Rehlaender ,  Roch Thibert

IPC分类号： A61K9/00 ,  A61K9/16 ,  A61K31/439 ,  A61K31/454 ,  A61K9/48

摘要： Provided herein is an oral pharmaceutical composition, comprising a plurality of xanomeline beads having a core comprising xanomeline or a salt thereof, and a plurality of trospium beads having a core comprising a salt of trospium.

公开(公告)号：US11413359B2

公开(公告)日：2022-08-16

申请号：US17017135

申请日：2020-09-10

申请人： Washington University

发明人： Samuel Achilefu ,  Kexian Liang ,  Rui Tang

IPC分类号： A61K49/00 ,  C07K7/06 ,  G01N33/574 ,  A61K51/08 ,  A61K38/00

摘要： The present invention provides compounds that have motifs that target the compounds to cells that express integrins. In particular, the compounds have peptides with one or more RD motifs conjugated to an agent selected from an imaging agent and a targeting agent. The compounds may be used to detect, monitor and treat a variety of disorders mediated by integrins.

公开(公告)号：US10695339B2

公开(公告)日：2020-06-30

申请号：US16444206

申请日：2019-06-18

申请人： PureTech Health LLC

发明人： Eric Elenko ,  Philip E. Murray, III ,  Andrew C. Miller

IPC分类号： A61K31/46 ,  A61K9/48 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/4725 ,  A61K31/44 ,  A61K31/438 ,  A61K31/222 ,  A61K31/138 ,  A61K31/4025 ,  A61K31/4178

摘要： The present disclosure provides a method of treating a central nervous system disorder in a patient in need thereof. The method comprises orally administering between 75 mg and 300 mg xanomeline salt and between 20 mg and 200 mg trospium chloride to the patient during a 24-hour period, the central nervous system disorder being selected from schizophrenia, Alzheimer's disease, Huntington's disease, Parkinson's disease, and Lewy Body dementia, wherein use of the trospium chloride alleviates a side effect associated with use of the xanomeline salt.

公开(公告)号：US10369143B2

公开(公告)日：2019-08-06

申请号：US16270206

申请日：2019-02-07

申请人： PureTech Health LLC

发明人： Eric Elenko ,  Philip E. Murray, III ,  Andrew C. Miller

IPC分类号： A61K31/46 ,  A61K9/48 ,  A61K31/4439 ,  A61K31/138 ,  A61K31/222 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/438 ,  A61K31/44 ,  A61K31/4725 ,  A61K45/06

摘要： Provided herein is a method of treating a central nervous system disorder in a patient in need thereof, wherein the central nervous system disorder is selected from schizophrenia, Alzheimer's disease, Huntington's disease, Parkinson's disease, and Lewy Body dementia. The method comprises orally administering an initial dose of between 75 mg and 300 mg xanomeline and an initial dose of between 20 mg and 200 mg trospium chloride to the patient during a 24-hour period. Provided that the patient tolerates said administration, an increased dose of trospium chloride and an increased dose of xanomeline are orally administering to the patient, wherein the increased dose of trospium chloride is greater than the initial dose of the trospium chloride, and wherein the increased dose of xanomeline is greater than the initial dose of the xanomeline.

公开(公告)号：US11452692B2

公开(公告)日：2022-09-27

申请号：US17649826

申请日：2022-02-03

申请人： Karuna Therapeutics, Inc.

发明人： Aimesther Betancourt ,  Bruce Rehlaender ,  Roch Thibert

IPC分类号： A61K9/16 ,  A61K31/439 ,  A61K31/454 ,  A61K9/48 ,  A61K9/00

摘要： Provided herein is an oral pharmaceutical composition, comprising a plurality of xanomeline beads having a core comprising xanomeline or a salt thereof; and a plurality of trospium beads having a core comprising a salt of trospium.

公开(公告)号：US11419345B2

公开(公告)日：2022-08-23

申请号：US16999380

申请日：2020-08-21

申请人： Allied Blending LP

发明人： Mostafa Galal ,  John Fannon

IPC分类号： A23C20/00 ,  A23C19/082

摘要： Disclosed herein are dry blends used in the process of making extended cheese products with improved meltability and firmness profiles.

公开(公告)号：US10966381B2

公开(公告)日：2021-04-06

申请号：US15024296

申请日：2014-09-24

申请人： STICHTING WAGENINGEN RESEARCH

发明人： Kimberly Boutilier ,  Gerrit Cornelis Angenent ,  Mercedes Soriano Castan ,  Li Hui

IPC分类号： A01H4/00 ,  A01H1/00 ,  A01H1/08 ,  A01N37/28

摘要： A switch to haploid embryogenesis is controlled by the activity of histone deacetylases (HDACs). Blocking HDAC activity with HDAC inhibitors (HDACi), e.g. trichostatin A (TSA), in Brassica napus, B. rapa, B. oleracea, Arabidopsis thaliana and Capsicum annuum male gametophytes leads to a large increase in the proportion of cells that undergo embryogenic growth. In B. napus, treatment with one specific HDACi (SAHA) improves the conversion (i.e. germination) of these embryos into seedlings. Existing methods of culturing microspores of angiosperm plants following stress to produce haploid embryos, haploid plants and double haploid plants can be improved by adding HDACi to the culture medium. Advantageously, species hitherto recalcitrant to haploid embryogenesis via microspore culture are rendered useful when using HDACi. Haploid and double haploid plants are of industrial application in the plant breeding programmes.