公开(公告)号：WO2011127255A1

公开(公告)日：2011-10-13

申请号：PCT/US2011/031540

申请日：2011-04-07

申请人： MERCK SHARP & DOHME CORP. ,  THE TRUSTEES OF PRINCETON UNIVERSITY ,  BURKE, Paul, A. ,  GINDY, Marian, E. ,  KUMAR, Varun ,  MATHRE, David, J. ,  PRUD'HOMME, Robert, K.

发明人： BURKE, Paul, A. ,  GINDY, Marian, E. ,  KUMAR, Varun ,  MATHRE, David, J. ,  PRUD'HOMME, Robert, K.

IPC分类号： A61K9/127

CPC分类号： A61K9/1271 ,  A61K9/127 ,  A61K9/1272 ,  A61K9/1277 ,  A61K48/00

摘要： The present invention provides a process for producing lipid nanoparticles encapsulating therapeutic products, said process comprising: a) providing one or more aqueous solutions in one or more reservoirs; b) providing one or more organic solutions in one or more reservoirs, wherein one or more of the organic solutions contains a lipid and wherein one or more of the aqueous solutions and/or one or more of the organic solutions includes therapeutic products; c) mixing said one or more aqueous solutions with said one or more organic solutions in a first mixing region, wherein said first mixing region is a Multi-Inlet Vortex Mixer (MIVM), wherein said one or more aqueous solutions and said one or more organic solutions are introduced tangentially into a mixing chamber within the MIVM so as to substantially instantaneously produce a lipid nanoparticle solution containing lipid nanoparticles encapsulating therapeutic products.

摘要翻译： 本发明提供了一种制备包封治疗产品的脂质纳米颗粒的方法，所述方法包括：a）在一个或多个储存器中提供一种或多种水溶液; b）在一个或多个储存器中提供一种或多种有机溶液，其中一种或多种有机溶液含有脂质，并且其中一种或多种水溶液和/或一种或多种有机溶液包括治疗产品; c）在第一混合区域中将所述一种或多种水溶液与所述一种或多种有机溶液混合，其中所述第一混合区域是多入口涡旋混合器（MIVM），其中所述一种或多种水溶液和所述一种或多种 将有机溶液切向引入MIVM内的混合室中，从而基本上瞬时产生含有包封治疗产品的脂质纳米颗粒的脂质纳米颗粒溶液。

公开(公告)号：WO2021163002A1

公开(公告)日：2021-08-19

申请号：PCT/US2021/017157

申请日：2021-02-09

申请人： MERCK SHARP & DOHME CORP. ,  GINDY, Marian, E. ,  BILELLO, John, P. ,  ESPESETH, Amy, S. ,  BETT, Andrew, J. ,  FU, Tong-Ming

发明人： GINDY, Marian, E. ,  BILELLO, John, P. ,  ESPESETH, Amy, S. ,  BETT, Andrew, J. ,  FU, Tong-Ming

IPC分类号： A61K39/12 ,  A61P31/20

摘要： The present disclosure provides, among other things, a pharmaceutical composition that includes a lipid nanoparticle adjuvant and an anti-human papillomavirus (HPV) comprising HPV virus-like particles (VLPs) of at least one type of human papillomavirus (HPV) selected from the group consisting of HPV types: 6, 11, 16, 18, 26, 31, 33, 35, 39, 45, 51, 52, 53, 55, 56, 58, 59, 66, 68, 73, and 82.

公开(公告)号：WO2017192470A1

公开(公告)日：2017-11-09

申请号：PCT/US2017/030484

申请日：2017-05-02

申请人： MERCK SHARP & DOHME CORP. ,  GINDY, Marian, E. ,  CASIMIRO, Danilo, R. ,  KAUFMAN, David, R. ,  PHAN, Uyen Truong

发明人： GINDY, Marian, E. ,  CASIMIRO, Danilo, R. ,  KAUFMAN, David, R. ,  PHAN, Uyen Truong

IPC分类号： A61K39/00

CPC分类号： C07K16/244 ,  A61K9/0019 ,  A61K9/1272 ,  A61K9/5123 ,  A61K9/5146 ,  A61K39/3955 ,  A61K2039/505 ,  A61K2039/55561 ,  C12N15/117 ,  C12N2310/17 ,  C12N2310/315 ,  C12N2320/31 ,  C12N2320/32 ,  A61K2300/00

摘要： The present invention is directed to a composition comprising: a) a lipid nanoparticle (LNP) comprising one or more cationic lipids and a poly(ethyleneglycol)-lipid (PEG-lipid); b) a Toll-like receptor 9 (TLR9) agonist CpG oligonucleotide; and c) an anti-IL-10 antibody or antigen binding fragment thereof. The present invention is also directed to methods of treating cancer in the subject by co-administering to the subject 1) an effective amount of a composition comprising the LNP of the invention and TLR9 agonist; and 2) an anti-IL-10 antibody or antigen binding fragment thereof.

摘要翻译： 本发明涉及一种组合物，其包含：a）包含一种或多种阳离子脂质和聚（乙二醇） - 脂质（PEG-脂质）的脂质纳米颗粒（LNP）; b）Toll样受体9（TLR9）激动剂CpG寡核苷酸; 和c）抗IL-10抗体或其抗原结合片段。 本发明还涉及通过向受试者共施用1）有效量的包含本发明的LNP和TLR9激动剂的组合物来治疗受试者的癌症的方法; 和2）抗IL-10抗体或其抗原结合片段。

公开(公告)号：WO2022119883A2

公开(公告)日：2022-06-09

申请号：PCT/US2021/061336

申请日：2021-12-01

申请人： MERCK SHARP & DOHME CORP. ,  GINDY, Marian, E. ,  BETT, Andrew ,  RAHEEM, Izzat Tiedje ,  KIM, Ronald, M.

发明人： GINDY, Marian, E. ,  BETT, Andrew ,  RAHEEM, Izzat Tiedje ,  KIM, Ronald, M.

IPC分类号： C07C323/25 ,  A61K47/18 ,  A61K47/20 ,  A61K31/7088 ,  A61K31/7105 ,  A61K47/543 ,  A61K47/6929 ,  A61K9/513

摘要： The present disclosure provides, among other things, lipid nanoparticle formulations that include monoester cationic lipids. The present invention also provides compositions that include monoester cationic lipid nanoparticles and nucleic acids. The present disclosure also provides lipid nanoparticles encapsulating agents. The present disclosure further provides methods of producing lipid nanoparticles with encapsulated nucleic acids.

公开(公告)号：WO2012018754A3

公开(公告)日：2012-02-09

申请号：PCT/US2011/046178

申请日：2011-08-02

申请人： MERCK SHARP & DOHME CORP. ,  BROWN, Duncan ,  CUNNINGHAM, James, J. ,  GINDY, Marian ,  PICKERING, Victoria ,  STANTON, Matthew, G. ,  STIRDIVANT, Steven, M. ,  STRAPPS, Walter

发明人： BROWN, Duncan ,  CUNNINGHAM, James, J. ,  GINDY, Marian ,  PICKERING, Victoria ,  STANTON, Matthew, G. ,  STIRDIVANT, Steven, M. ,  STRAPPS, Walter

IPC分类号： C12N15/11

摘要： The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of CTNNB1 gene expression and/or activity, and/or modulate a beta-catenin gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against CTNNB1 gene expression.

公开(公告)号：WO2009061406A1

公开(公告)日：2009-05-14

申请号：PCT/US2008/012485

申请日：2008-11-05

申请人： THE TRUSTEES OF PRINCETON UNIVERSITY ,  PRUD'HOMME, Robert, K. ,  GINDY, Marian ,  UNGUN, Baris ,  BUDIJONO, Stephanie ,  LIU, Ying

发明人： PRUD'HOMME, Robert, K. ,  GINDY, Marian ,  UNGUN, Baris ,  BUDIJONO, Stephanie ,  LIU, Ying

IPC分类号： A61N5/06 ,  A61B18/18

CPC分类号： A61K9/0009

摘要： Embodiments of the invention include nanoparticulate products of a flash nanoprecipitation process, the products comprising, in combination, pre-formed nanoparticles having properties of an upconversion phosphor and a hydrophobic organic compound having the properties of a photosensitizer, and a method of photodynamic therapy comprising the use of the nanoparticulate products is described.

摘要翻译： 本发明的实施方案包括快速纳米颗粒沉积方法的纳米颗粒产物，该组合物包含具有上转换荧光体和具有光敏剂性质的疏水性有机化合物的特性的预形成纳米颗粒，以及包含 描述了纳米颗粒产品的使用。

公开(公告)号：WO2015130584A2

公开(公告)日：2015-09-03

申请号：PCT/US2015/017007

申请日：2015-02-23

申请人： MERCK SHARP & DOHME CORP. ,  GINDY, Marian ,  CASIMIRO, Danilo, R. ,  BETT, Andrew ,  TER MEULEN, Jan, H.

发明人： GINDY, Marian ,  CASIMIRO, Danilo, R. ,  BETT, Andrew ,  TER MEULEN, Jan, H.

IPC分类号： A61K39/12

CPC分类号： A61K39/39 ,  A61K9/5015 ,  A61K9/5031 ,  A61K31/451 ,  A61K31/80 ,  A61K39/12 ,  A61K39/292 ,  A61K2039/545 ,  A61K2039/55505 ,  A61K2039/55511 ,  A61K2039/55555 ,  A61K2039/55561 ,  A61K2039/55572 ,  A61K2039/55577 ,  C12N7/00 ,  C12N2730/10134 ,  C12N2730/10171 ,  C12N2770/24134 ,  C12N2770/24171 ,  Y02A50/386 ,  Y02A50/412

摘要： The instant invention provides for novel lipid nanoparticle (LNP) formulations, containing cationic lipids, for use as vaccine adjuvants and/or as antigen delivery systems. It is an object of the instant invention to provide LNP formulations that demonstrate enhancements in humoral and cellular immunogenicity of vaccine antigens, particularly subunit vaccine antigens, when utilized alone or in combination with immunostimulatory agents (e.g. small molecule or oligonucleotide TLR agonists). The instant invention further identifies physical and chemical properties of the LNP formulations that can be manipulated to enhance antigen efficiency and adjuvant tolerability in vivo.

摘要翻译： 本发明提供了用作疫苗佐剂和/或作为抗原递送系统的新型脂质纳米颗粒（LNP）制剂，其含有阳离子脂质。 本发明的目的是提供当单独使用或与免疫刺激剂（例如小分子或寡核苷酸TLR激动剂）组合使用时，证明疫苗抗原，特别是亚单位疫苗抗原的体液和细胞免疫原性增强的LNP制剂。 本发明进一步鉴定LNP制剂的物理和化学性质，其可被操作以增强体内抗原效率和佐剂耐受性。

公开(公告)号：WO2015094928A1

公开(公告)日：2015-06-25

申请号：PCT/US2014/069872

申请日：2014-12-12

申请人： MERCK SHARP & DOHME CORP. ,  SMITH, Michael Hughes ,  GINDY, Marian

发明人： SMITH, Michael Hughes ,  GINDY, Marian

IPC分类号： A61K31/519

CPC分类号： A61K9/1277 ,  A61K9/0019 ,  A61K9/127 ,  A61K9/1271 ,  A61K9/1273 ,  A61K9/5123 ,  A61K31/4375 ,  A61K47/14

摘要： Disclosed herein is a lipid nanoparticle (LNP) composition comprising (a) an Akt inhibitor; (b) DSPC; (c) cholesterol; and (d) PEG-DMG. Also disclosed herein is a method for preparing the lipid composition using a scalable tangential flow micro-mixing technology.

摘要翻译： 本文公开了一种脂质纳米颗粒（LNP）组合物，其包含（a）Akt抑制剂; （b）DSPC; （c）胆固醇; 和（d）PEG-DMG。 本文还公开了使用可伸缩切向流微混合技术制备脂质组合物的方法。

公开(公告)号：WO2022046578A1

公开(公告)日：2022-03-03

申请号：PCT/US2021/047046

申请日：2021-08-23

申请人： MERCK SHARP & DOHME CORP. ,  BARRETT, Stephanie Elizabeth ,  FORSTER, Seth, P. ,  GINDY, Marian, E.

发明人： BARRETT, Stephanie Elizabeth ,  FORSTER, Seth, P. ,  GINDY, Marian, E.

IPC分类号： A61K9/00 ,  A61K31/7076 ,  A61K47/20 ,  A61K47/34 ,  A61P31/18

摘要： This invention relates to novel injectable depot compositions for long-acting delivery of antiviral drugs. These compositions are useful for the treatment or prevention of human immunodeficiency virus (HIV) infection.

公开(公告)号：WO2018226512A1

公开(公告)日：2018-12-13

申请号：PCT/US2018/035520

申请日：2018-06-01

申请人： MERCK SHARP & DOHME CORP. ,  BARRETT, Stephanie Elizabeth ,  FORSTER, Seth, P. ,  GINDY, Marian, E. ,  GROBLER, Jay, A. ,  OLSEN, David Brian ,  TELLER, Ryan Stevenson

发明人： BARRETT, Stephanie Elizabeth ,  FORSTER, Seth, P. ,  GINDY, Marian, E. ,  GROBLER, Jay, A. ,  OLSEN, David Brian ,  TELLER, Ryan Stevenson

IPC分类号： A61P31/08 ,  A61P31/00 ,  A61P31/04 ,  A61P31/10

摘要： The present invention relates to long-acting implants useful for the treatment of bacterial infections, particularly mycobacterial infections. The invention also relates to methods of use of such long-acting implants for the treatment of mycobacterial infections such as those caused by Mycobacteria tuberculosis.