公开(公告)号：US06350780B1

公开(公告)日：2002-02-26

申请号：US09286147

申请日：1999-04-05

申请人： Michael E. Garst ,  Joseph S. Adorante

发明人： Michael E. Garst ,  Joseph S. Adorante

IPC分类号： A61K31235

CPC分类号： A61K31/00 ,  A61K31/198 ,  A61K31/216 ,  A61K31/222 ,  A61K31/23 ,  A61K47/555 ,  Y10S514/912

摘要： Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains as the active ingredient one or more compounds having calcium chelating activity. Examples of calcium chelating agents utilized in the pharmaceutical composition and method of treatment are: and lower alkyl and alkoxyalkyl esters thereof. Also disclosed are methods and compositions for delivering a drug within the cytoplasm of a cell having cell surface acetylcholinesterase or acetylcholinesterase receptors, wherein the compositions comprise an apolar prodrug joined to an acetylcholine ester or psuedoacetylcholine group.

摘要翻译： 公开了药物组合物和方法，用于通过向哺乳动物眼睛施用含有作为活性成分的一种或多种具有钙螯合活性的化合物的本发明的药物组合物来治疗哺乳动物眼中的青光眼和/或高眼压症。 用于药物组合物和治疗方法的钙螯合剂的实例是：及其低级烷基和烷氧基烷基酯。 还公开了用于在具有细胞表面乙酰胆碱酯酶或乙酰胆碱酯酶受体的细胞的细胞质内输送药物的方法和组合物，其中所述组合物包含与乙酰胆碱酯或伪乙酰胆碱基团连接的非极性前药。

公开(公告)号：US12083108B2

公开(公告)日：2024-09-10

申请号：US17752683

申请日：2022-05-24

申请人： CHDI Foundation, Inc.

发明人： Celia Dominguez ,  Jonathan Bard ,  Matthew R. Lee ,  Longbin Liu ,  Michael Edward Prime ,  Samuel Coe

IPC分类号： A61K31/454 ,  A61K31/165 ,  A61K31/427 ,  A61K47/54

CPC分类号： A61K31/454 ,  A61K31/165 ,  A61K31/427 ,  A61K47/555

摘要： The present disclosure relates generally to compounds that simultaneously bind both mutant huntingtin protein (mHTT) and an ubiquitin E3 ligase and their use as therapeutic agents, for example, in treating diseases, such as neurodegenerative disorders caused by aggregation of mHTT.

公开(公告)号：US20240091204A1

公开(公告)日：2024-03-21

申请号：US18309867

申请日：2023-09-18

申请人： Arvinas Operations, Inc.

发明人： Andrew P. Crew ,  Hanqing Dong ,  Michael Berlin ,  Steven M. Sparks

IPC分类号： A61K31/427 ,  A61K31/4035 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/541 ,  A61K47/54

CPC分类号： A61K31/427 ,  A61K31/4035 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/541 ,  A61K47/555

摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of α-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US11788089B2

公开(公告)日：2023-10-17

申请号：US16876271

申请日：2020-05-18

申请人： The General Hospital Corporation

发明人： Arthur M. Krieg ,  Romesh R. Subramanian ,  James McSwiggen ,  Jeannie T. Lee

IPC分类号： C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  A61K47/61 ,  A61K47/64 ,  A61K31/7115 ,  A61K31/712 ,  A61K31/7125 ,  C07H21/00 ,  A61K47/54

CPC分类号： C12N15/113 ,  A61K31/712 ,  A61K31/7115 ,  A61K31/7125 ,  A61K47/555 ,  A61K47/61 ,  A61K47/64 ,  A61K47/6455 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/321 ,  C12N2310/3231 ,  C12N2310/321 ,  C12N2310/3521

摘要： Aspects of the invention provide single stranded oligonucleotides for activating or enhancing expression of MECP2. Further aspects provide compositions and kits comprising single stranded oligonucleotides for activating or enhancing expression of MECP2. Methods for modulating expression of MECP2 using the single stranded oligonucleotides are also provided. Further aspects of the invention provide methods for selecting a candidate oligonucleotide for activating or enhancing expression of MECP2.

公开(公告)号：US20230248721A1

公开(公告)日：2023-08-10

申请号：US18091145

申请日：2022-12-29

申请人： Children's Medical Center Corporation

发明人： Debra Auguste ,  Marsha A. Moses ,  Peng Guo

IPC分类号： A61K31/4965 ,  A61K31/191 ,  A61K31/4365 ,  G01N33/574 ,  A61K9/14 ,  A61K31/429 ,  C12Q1/6886 ,  A61K47/54

CPC分类号： A61K31/4965 ,  A61K9/14 ,  A61K31/191 ,  A61K31/429 ,  A61K31/4365 ,  A61K47/555 ,  C12Q1/6886 ,  G01N33/57415 ,  A61K2121/00 ,  C12Q2600/158 ,  G01N2333/70525

摘要： A method of detecting triple negative breast cancer (TNBC) is provided. Overexpression of ICAM-1 is linked to an increased risk of TNBC. A composition of matter is also provided that binds an anti-ICAM~1 antibody to a nanoparticle. The composition may be used as an imaging agent and/or a therapeutic targeting agent. A therapeutically active molecule may be bound to the composition to provide targeted therapy.

公开(公告)号：US11707452B2

公开(公告)日：2023-07-25

申请号：US16545983

申请日：2019-08-20

申请人： Arvinas Operations, Inc.

发明人： Andrew P. Crew ,  Hanqing Dong ,  Michael Berlin ,  Steven M. Sparks

IPC分类号： A61K31/427 ,  A61K47/54 ,  A61K31/4035 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/541

CPC分类号： A61K31/427 ,  A61K31/4035 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/541 ,  A61K47/555

摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of α-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20190192687A1

公开(公告)日：2019-06-27

申请号：US16076878

申请日：2017-02-13

申请人： The United States of America, as represented by the Secretary, Dept. of Health and Human Service

发明人： Bruce Allen Shapiro ,  Kirill Andreevich Afonin ,  Mathias D. Viard ,  Eckart H.U. Bindewald ,  Lorena Parlea

IPC分类号： A61K47/69 ,  C12N15/113

CPC分类号： A61K47/6929 ,  A61K47/555 ,  A61K47/6925 ,  B82Y5/00 ,  C12N15/111 ,  C12N15/113 ,  C12N15/87 ,  C12N2310/14 ,  C12N2310/351 ,  C12N2310/50 ,  C12N2320/50 ,  C12N2330/50

摘要： The invention discloses the use of single-stranded RNA toeholds of different lengths to promote the re-association of various RNA-DNA hybrids, which results in activation of multiple split functionalities inside human cells. Previously designed RNA/DNA nanoparticles employed single-stranded DNA toeholds to initiate re-association. The use of RNA toeholds is advantageous because of the simpler design rules, the shorter toeholds, and the smaller size of the resulting nanoparticles compared to the same hybrid nanoparticles with single-stranded DNA toeholds. Moreover, the co-transcriptional assemblies result in higher yields for hybrid nanoparticles with ssRNA toeholds.

公开(公告)号：US20180326031A1

公开(公告)日：2018-11-15

申请号：US15757854

申请日：2016-09-07

申请人： Becton, Dickinson and Company

发明人： Brian P. Dwyer

IPC分类号： A61K39/00 ,  C07F9/6584 ,  C12N5/16 ,  A61K47/54 ,  A61K47/68 ,  G01N33/94 ,  G01N33/531 ,  C07K16/06

CPC分类号： A61K39/0013 ,  A61K47/555 ,  A61K47/6843 ,  A61K47/6897 ,  C07F9/65846 ,  C07K16/065 ,  C12N5/163 ,  G01N33/531 ,  G01N33/94 ,  G01N33/9493

摘要： The present application relates to antibodies that bind to small molecules such as cyclophosphamide, ifosfamide, and analogs thereof, and immunological assays for determining the presence and/or quantifying the amount of cyclophosphamide and/or ifosfamide in a sample. By way of example, such immunological assays can be used for environmental testing.

公开(公告)号：US20180177918A1

公开(公告)日：2018-06-28

申请号：US15805412

申请日：2017-11-07

申请人： BAYLOR UNIVERSITY

发明人： Bob Kane ,  Babatope Akinbobuyi ,  Charles Chang ,  Bashoo Naziruddin

IPC分类号： A61L27/36 ,  C12N5/071 ,  A61L27/38 ,  A61L27/54 ,  A61K31/216 ,  A61K47/54 ,  A61P37/06 ,  A61P29/00 ,  A61K31/18

CPC分类号： A61L27/3683 ,  A61K31/18 ,  A61K31/216 ,  A61K47/54 ,  A61K47/545 ,  A61K47/555 ,  A61L27/3687 ,  A61L27/3695 ,  A61L27/3839 ,  A61L27/54 ,  A61L2300/41 ,  A61L2300/418 ,  A61L2300/426 ,  A61L2400/16 ,  A61P29/00 ,  A61P37/06 ,  C12N5/0006 ,  C12N5/0676

摘要： Methods for the ex vivo modification of the surfaces of viable tissue result in tissue modifications that are stable and/or result in the controlled release of active compounds, and are expected to provide effective protection for transplanted tissue subsequent to transplant.

公开(公告)号：US20170320914A1

公开(公告)日：2017-11-09

申请号：US15528732

申请日：2015-11-23

申请人： Nicolai Vladimirovich BOVIN ,  Stephen Micheal HENRY ,  Elena KORCHAGINA ,  Igor Leonidovich RODIONOV ,  Alexander Borisovich TUZIKOV

发明人： Nicolai Vladimirovich BOVIN ,  Stephen Micheal HENRY ,  Elena KORCHAGINA ,  Igor Leonidovich RODIONOV ,  Alexander Borisovich TUZIKOV

IPC分类号： C07K9/00

CPC分类号： C07K9/00 ,  A61K31/685 ,  A61K31/7004 ,  A61K31/7016 ,  A61K31/702 ,  A61K38/00 ,  A61K47/555 ,  C07K7/06 ,  C07K7/08 ,  C07K14/001

摘要： Water dispersible, multivalent ligand-lipid constructs that spontaneously and stably incorporate into membranes are disclosed.