公开(公告)号：US09951333B2

公开(公告)日：2018-04-24

申请号：US15618892

申请日：2017-06-09

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Charlotte Albaek Thrue ,  Majken Westergaard ,  Christoph Rosenbohm

IPC分类号： C12N15/11 ,  A61K48/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  A61K31/7088 ,  C07H21/00 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

公开(公告)号：US09938527B2

公开(公告)日：2018-04-10

申请号：US15243646

申请日：2016-08-22

申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S

发明人： Majken Westergaard ,  Charlotte Albaek Thrue ,  Frank Rasmussen ,  Henrik Frydenlund Hansen

IPC分类号： C12N15/113 ,  C07H21/04 ,  A61K45/06 ,  A61N5/10 ,  A61K31/7088 ,  C12N15/11

CPC分类号： C12N15/113 ,  A61K31/7088 ,  A61K45/06 ,  A61N5/10 ,  C07H21/04 ,  C12N15/111 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2320/30

摘要： The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5′-(Tx)GxGxcsasasgscsastscscsTxGxT-3′ and 5′-(Gx)TxTxascstsgscscststscsTxTxA-3′, wherein capital letters designate a beta-D-oxy-LNA nucleotide analog, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analog or a 2-deoxynucleotide, subscript “s” designates a phosphorothioate link between neighboring nucleotides/LNA nucleotide analogs, and subscript “x” designates either a phosphorothioate link or a phosphorodiester link between neighboring nucleotides/LNA nucleotide analogs, and wherein the sequence is optionally extended by up to five 2-deoxynucleotide units. The LNA oligonucleotides are useful for modulating the expression of hypoxia-inducible factor-1a (HIF-1a), e.g. in the treatment of cancer diseases, inhibiting angiogenesis, inducing apoptosis, preventing cellular proliferation, or treating an angiogenic disease, e.g. diabetic retinopathy, macular degeneration (ARMD), psoriasis, rheumatoid arthritis and other inflammatory diseases.

公开(公告)号：US20170342413A1

公开(公告)日：2017-11-30

申请号：US15619134

申请日：2017-06-09

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Christoph Rosenbohm ,  Charlotte Albaek Thrue ,  Majken Westergaard

IPC分类号： C12N15/113 ,  C07H19/06 ,  C07H19/16 ,  C12N15/11 ,  C07H21/02 ,  C07H21/04 ,  A61K31/7088 ,  C07H19/04 ,  C07H21/00

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

公开(公告)号：US20160168576A1

公开(公告)日：2016-06-16

申请号：US14882369

申请日：2015-10-13

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Christoph Rosenbohm ,  Charlotte Albaek Thrue ,  Majken Westergaard

IPC分类号： C12N15/113

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

公开(公告)号：US20180237777A1

公开(公告)日：2018-08-23

申请号：US15863635

申请日：2018-01-05

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Christoph Rosenbohm ,  Charlotte Albaek Thrue ,  Majken Westergaard

IPC分类号： C12N15/113 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  A61K31/7088 ,  C12N15/11

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

公开(公告)号：US09994850B2

公开(公告)日：2018-06-12

申请号：US15619134

申请日：2017-06-09

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Christoph Rosenbohm ,  Charlotte Albaek Thrue ,  Majken Westergaard

IPC分类号： A61K31/712 ,  A61K48/00 ,  C12N15/113 ,  A61K31/7088 ,  C07H21/00 ,  C12N15/11 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/02 ,  C07H21/04

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

公开(公告)号：US09890383B2

公开(公告)日：2018-02-13

申请号：US15618650

申请日：2017-06-09

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Christoph Rosenbohm ,  Charlotte Albaek Thrue ,  Majken Westergaard

IPC分类号： C12N15/11 ,  C07H21/02 ,  A61K48/00 ,  C12N15/113 ,  C07H21/04 ,  C07H19/06 ,  C07H19/16 ,  C07H19/04 ,  A61K31/7088 ,  C07H21/00

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

公开(公告)号：US20180237778A1

公开(公告)日：2018-08-23

申请号：US15863667

申请日：2018-01-05

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Christoph Rosenbohm ,  Charlotte Albaek Thrue ,  Majken Westergaard

IPC分类号： C12N15/113 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  A61K31/7088 ,  C12N15/11

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

公开(公告)号：US20170342412A1

公开(公告)日：2017-11-30

申请号：US15618892

申请日：2017-06-09

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Christoph Rosenbohm ,  Charlotte Albaek Thrue ,  Majken Westergaard

IPC分类号： C12N15/113 ,  C07H19/06 ,  C07H19/16 ,  C12N15/11 ,  C07H21/02 ,  C07H21/04 ,  A61K31/7088 ,  C07H19/04 ,  C07H21/00

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

公开(公告)号：US09708614B2

公开(公告)日：2017-07-18

申请号：US15237307

申请日：2016-08-15

申请人： Roche Innovation Center Copenhagen A/S

发明人： Signe M. Christensen ,  Nikolaj Dam Mikkelsen ,  Miriam Frieden ,  Henrik Frydenlund Hansen ,  Troels Koch ,  Daniel Sejer Pedersen ,  Christoph Rosenbohm ,  Charlotte Albaek Thrue ,  Majken Westergaard

IPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H21/00 ,  C07H21/04 ,  C07H21/02 ,  C12N15/11 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16

CPC分类号： C12N15/113 ,  A61K31/7088 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2320/30 ,  C12N2320/51

摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.