JP2010539950A5 - - Google Patents
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- JP2010539950A5 JP2010539950A5 JP2010527254A JP2010527254A JP2010539950A5 JP 2010539950 A5 JP2010539950 A5 JP 2010539950A5 JP 2010527254 A JP2010527254 A JP 2010527254A JP 2010527254 A JP2010527254 A JP 2010527254A JP 2010539950 A5 JP2010539950 A5 JP 2010539950A5
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- 150000001875 compounds Chemical class 0.000 claims description 124
- 108091034117 Oligonucleotide Proteins 0.000 claims description 91
- 239000002777 nucleoside Substances 0.000 claims description 66
- 125000003835 nucleoside group Chemical group 0.000 claims description 46
- 230000000295 complement effect Effects 0.000 claims description 41
- 239000000203 mixture Substances 0.000 claims description 25
- 208000008589 Obesity Diseases 0.000 claims description 19
- 239000003472 antidiabetic agent Substances 0.000 claims description 19
- 229940126904 hypoglycaemic agent Drugs 0.000 claims description 19
- 150000007523 nucleic acids Chemical class 0.000 claims description 19
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 19
- 235000020824 obesity Nutrition 0.000 claims description 19
- 239000000883 anti-obesity agent Substances 0.000 claims description 17
- 229940125710 antiobesity agent Drugs 0.000 claims description 17
- 206010012601 diabetes mellitus Diseases 0.000 claims description 16
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims description 15
- 210000001789 adipocyte Anatomy 0.000 claims description 14
- 210000000577 adipose tissue Anatomy 0.000 claims description 14
- 206010022489 Insulin Resistance Diseases 0.000 claims description 13
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 13
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 13
- 238000007911 parenteral administration Methods 0.000 claims description 12
- 239000000164 antipsychotic agent Substances 0.000 claims description 11
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims description 10
- 102000055699 human FGFR4 Human genes 0.000 claims description 10
- 108020004707 nucleic acids Proteins 0.000 claims description 9
- 102000039446 nucleic acids Human genes 0.000 claims description 9
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 9
- 230000001225 therapeutic effect Effects 0.000 claims description 8
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 7
- 241001465754 Metazoa Species 0.000 claims description 7
- 230000037396 body weight Effects 0.000 claims description 7
- 239000008103 glucose Substances 0.000 claims description 7
- 238000001990 intravenous administration Methods 0.000 claims description 7
- 230000037323 metabolic rate Effects 0.000 claims description 7
- 238000007920 subcutaneous administration Methods 0.000 claims description 7
- LRSASMSXMSNRBT-UHFFFAOYSA-N 5-methylcytosine Chemical compound CC1=CNC(=O)N=C1N LRSASMSXMSNRBT-UHFFFAOYSA-N 0.000 claims description 6
- 108091028043 Nucleic acid sequence Proteins 0.000 claims description 6
- 125000002619 bicyclic group Chemical group 0.000 claims description 5
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 230000004663 cell proliferation Effects 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 239000003337 fertilizer Substances 0.000 claims 1
- -1 thio benzoate nucleoside Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 description 75
- 239000002773 nucleotide Substances 0.000 description 22
- 125000003729 nucleotide group Chemical group 0.000 description 22
- 108020005345 3' Untranslated Regions Proteins 0.000 description 20
- 108091081024 Start codon Proteins 0.000 description 20
- 108020003589 5' Untranslated Regions Proteins 0.000 description 10
- 108091026890 Coding region Proteins 0.000 description 10
- 230000035755 proliferation Effects 0.000 description 6
- 230000003247 decreasing effect Effects 0.000 description 5
- 230000001934 delay Effects 0.000 description 5
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 description 1
- 101710182387 Fibroblast growth factor receptor 4 Proteins 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 230000000692 anti-sense effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- VAAUVRVFOQPIGI-SPQHTLEESA-N ceftriaxone Chemical compound S([C@@H]1[C@@H](C(N1C=1C(O)=O)=O)NC(=O)\C(=N/OC)C=2N=C(N)SC=2)CC=1CSC1=NC(=O)C(=O)NN1C VAAUVRVFOQPIGI-SPQHTLEESA-N 0.000 description 1
- 229960004755 ceftriaxone Drugs 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229940104302 cytosine Drugs 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97678207P | 2007-10-01 | 2007-10-01 | |
| US60/976,782 | 2007-10-01 | ||
| PCT/US2008/078497 WO2009046141A2 (en) | 2007-10-01 | 2008-10-01 | Antisense modulation of fibroblast growth factor receptor 4 expression |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010539950A JP2010539950A (ja) | 2010-12-24 |
| JP2010539950A5 true JP2010539950A5 (cg-RX-API-DMAC7.html) | 2011-11-24 |
| JP5792955B2 JP5792955B2 (ja) | 2015-10-14 |
Family
ID=40526946
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010527254A Expired - Fee Related JP5792955B2 (ja) | 2007-10-01 | 2008-10-01 | 線維芽細胞増殖因子受容体４発現のアンチセンスモジュレーション |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US8486904B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2215102B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5792955B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR101660989B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN101883777B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2008308691B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BRPI0817527A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2701128A1 (cg-RX-API-DMAC7.html) |
| IL (1) | IL204796A (cg-RX-API-DMAC7.html) |
| MX (1) | MX2010003606A (cg-RX-API-DMAC7.html) |
| NZ (1) | NZ584827A (cg-RX-API-DMAC7.html) |
| RU (1) | RU2501803C2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2009046141A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009046141A2 (en) | 2007-10-01 | 2009-04-09 | Isis Pharmaceuticals, Inc. | Antisense modulation of fibroblast growth factor receptor 4 expression |
| AU2009323766B2 (en) | 2008-12-02 | 2016-10-06 | Wave Life Sciences Ltd. | Method for the synthesis of phosphorus atom modified nucleic acids |
| BRPI1015236A2 (pt) * | 2009-04-15 | 2019-09-24 | Isis Pharmaceuticals Inc | métodos para modular uma resposta inflamatória, apra melhorar uma doença, distúrbio ou condição inflamatórios em um animal, para tratar um animal em risco para uma doença, distúrbio ou condição inflamatórios, para inibir a expressão de fator xi em um animal, para reduzir o risco de doença, distúrbio ou condição inflamatórios, em um animal, para tratar um animal em risco para uma doença inflamatória, e para tratar um animal tendo uma doença inflamatória, e, uso de um composto marcado para fator xi |
| SG177564A1 (en) | 2009-07-06 | 2012-02-28 | Ontorii Inc | Novel nucleic acid prodrugs and methods of use thereof |
| EP2620428B1 (en) | 2010-09-24 | 2019-05-22 | Wave Life Sciences Ltd. | Asymmetric auxiliary group |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| AU2012242642A1 (en) | 2011-04-13 | 2013-05-02 | Ionis Pharmaceuticals, Inc. | Antisense modulation of PTP1B expression |
| AU2012271357A1 (en) * | 2011-06-16 | 2013-05-02 | Ionis Pharmaceuticals, Inc. | Antisense modulation of fibroblast growth factor receptor 4 expression |
| US9605019B2 (en) | 2011-07-19 | 2017-03-28 | Wave Life Sciences Ltd. | Methods for the synthesis of functionalized nucleic acids |
| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| CN102337247B (zh) * | 2011-09-13 | 2013-07-10 | 西安交通大学 | 一种fgfr4高表达的重组hek293细胞及其应用 |
| EP3495367B1 (en) | 2012-06-13 | 2020-09-30 | Incyte Holdings Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| JP6268157B2 (ja) | 2012-07-13 | 2018-01-24 | 株式会社Ｗａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｊａｐａｎ | 不斉補助基 |
| SG10201912895PA (en) | 2012-07-13 | 2020-02-27 | Wave Life Sciences Ltd | Chiral control |
| JP6246121B2 (ja) | 2012-07-13 | 2017-12-13 | 株式会社新日本科学 | キラル核酸アジュバント |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| AR092982A1 (es) * | 2012-10-11 | 2015-05-13 | Isis Pharmaceuticals Inc | Modulacion de la expresion de receptores androgenicos |
| ES2724853T3 (es) | 2012-11-15 | 2019-09-16 | Roche Innovation Ct Copenhagen As | Conjugados de oligonucleótidos |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| MY177989A (en) | 2013-01-30 | 2020-09-28 | Hoffmann La Roche | Lna oligonucleotide carbohydrate conjugates |
| DK2986610T5 (en) | 2013-04-19 | 2018-12-10 | Incyte Holdings Corp | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
| KR102138781B1 (ko) * | 2013-05-01 | 2020-07-28 | 아이오니스 파마수티컬즈, 인코포레이티드 | 아포지질단백질 c-iii 발현을 조절하는 조성물 및 방법 |
| EP3095460A4 (en) | 2014-01-15 | 2017-08-23 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having anti-allergic activity, and anti-allergic agent |
| JPWO2015108048A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 抗腫瘍作用を有するキラル核酸アジュバンド及び抗腫瘍剤 |
| JPWO2015108047A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 免疫誘導活性を有するキラル核酸アジュバンド及び免疫誘導活性剤 |
| PT3094728T (pt) | 2014-01-16 | 2022-05-19 | Wave Life Sciences Ltd | Desenho quiral |
| US10006027B2 (en) | 2014-03-19 | 2018-06-26 | Ionis Pharmaceuticals, Inc. | Methods for modulating Ataxin 2 expression |
| HRP20211397T1 (hr) | 2014-03-19 | 2021-12-10 | Ionis Pharmaceuticals, Inc. | Pripravci za modulaciju ekspresije ataksina 2 |
| US9994855B2 (en) | 2014-05-01 | 2018-06-12 | Ionis Pharmaceuticals, Inc. | Compositions and methods for modulating growth hormone receptor expression |
| WO2015179693A1 (en) | 2014-05-22 | 2015-11-26 | Isis Pharmaceuticals, Inc. | Conjugated antisense compounds and their use |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| CN109477106B (zh) * | 2015-07-10 | 2022-10-04 | Ionis制药公司 | 二酰基甘油酰基转移酶2(dgat2)的调节剂 |
| CA3006015A1 (en) | 2015-12-31 | 2017-07-06 | Ionis Pharmaceuticals, Inc. | Methods for reducing ataxin-2 expression |
| US11400161B2 (en) | 2016-10-06 | 2022-08-02 | Ionis Pharmaceuticals, Inc. | Method of conjugating oligomeric compounds |
| JP2019535839A (ja) | 2016-11-29 | 2019-12-12 | ピュアテック ヘルス エルエルシー | 治療剤の送達のためのエクソソーム |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| US11466004B2 (en) | 2018-05-04 | 2022-10-11 | Incyte Corporation | Solid forms of an FGFR inhibitor and processes for preparing the same |
| CN112566912A (zh) | 2018-05-04 | 2021-03-26 | 因赛特公司 | Fgfr抑制剂的盐 |
| CA3106986A1 (en) | 2018-07-25 | 2020-01-30 | Ionis Pharmaceuticals, Inc. | Compounds and methods for reducing atxn2 expression |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEAP202415945A (en) | 2019-10-14 | 2024-04-25 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CN112759593A (zh) | 2019-11-01 | 2021-05-07 | 北京伯汇生物技术有限公司 | 桥环并醛基吡啶衍生物及其应用 |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式ヘテロ環 |
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-
2008
- 2008-10-01 WO PCT/US2008/078497 patent/WO2009046141A2/en not_active Ceased
- 2008-10-01 CA CA2701128A patent/CA2701128A1/en not_active Abandoned
- 2008-10-01 JP JP2010527254A patent/JP5792955B2/ja not_active Expired - Fee Related
- 2008-10-01 AU AU2008308691A patent/AU2008308691B2/en not_active Ceased
- 2008-10-01 US US12/681,360 patent/US8486904B2/en not_active Expired - Fee Related
- 2008-10-01 EP EP08835484.0A patent/EP2215102B1/en not_active Not-in-force
- 2008-10-01 CN CN200880118757.3A patent/CN101883777B/zh not_active Expired - Fee Related
- 2008-10-01 RU RU2010116994/10A patent/RU2501803C2/ru not_active IP Right Cessation
- 2008-10-01 NZ NZ584827A patent/NZ584827A/xx not_active IP Right Cessation
- 2008-10-01 MX MX2010003606A patent/MX2010003606A/es active IP Right Grant
- 2008-10-01 BR BRPI0817527A patent/BRPI0817527A2/pt not_active IP Right Cessation
- 2008-10-01 KR KR1020107009236A patent/KR101660989B1/ko not_active Expired - Fee Related
-
2010
- 2010-03-28 IL IL204796A patent/IL204796A/en not_active IP Right Cessation
-
2013
- 2013-06-12 US US13/915,855 patent/US8895529B2/en not_active Expired - Fee Related