JP2018528781A5 - - Google Patents
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- JP2018528781A5 JP2018528781A5 JP2018515292A JP2018515292A JP2018528781A5 JP 2018528781 A5 JP2018528781 A5 JP 2018528781A5 JP 2018515292 A JP2018515292 A JP 2018515292A JP 2018515292 A JP2018515292 A JP 2018515292A JP 2018528781 A5 JP2018528781 A5 JP 2018528781A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- modified oligonucleotide
- nucleosides
- wing segment
- bound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 239000002777 nucleoside Substances 0.000 claims description 100
- 150000001875 compounds Chemical class 0.000 claims description 64
- 125000003835 nucleoside group Chemical group 0.000 claims description 63
- 108091034117 Oligonucleotide Proteins 0.000 claims description 62
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 30
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 claims description 18
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 235000000346 sugar Nutrition 0.000 claims description 13
- 206010009944 Colon cancer Diseases 0.000 claims description 12
- 208000031839 Peripheral nerve sheath tumour malignant Diseases 0.000 claims description 12
- 201000009020 malignant peripheral nerve sheath tumor Diseases 0.000 claims description 12
- 208000029974 neurofibrosarcoma Diseases 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 11
- LRSASMSXMSNRBT-UHFFFAOYSA-N 5-methylcytosine Chemical group CC1=CNC(=O)N=C1N LRSASMSXMSNRBT-UHFFFAOYSA-N 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 229940104302 cytosine Drugs 0.000 claims description 9
- 208000003019 Neurofibromatosis 1 Diseases 0.000 claims description 8
- 208000024834 Neurofibromatosis type 1 Diseases 0.000 claims description 8
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 8
- 208000029742 colonic neoplasm Diseases 0.000 claims description 8
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 8
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 8
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims description 8
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 8
- 206010005003 Bladder cancer Diseases 0.000 claims description 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 206010014733 Endometrial cancer Diseases 0.000 claims description 4
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 4
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 4
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010025323 Lymphomas Diseases 0.000 claims description 4
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 4
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 4
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 4
- 201000009036 biliary tract cancer Diseases 0.000 claims description 4
- 208000020790 biliary tract neoplasm Diseases 0.000 claims description 4
- 201000010881 cervical cancer Diseases 0.000 claims description 4
- 230000000295 complement effect Effects 0.000 claims description 4
- 201000004101 esophageal cancer Diseases 0.000 claims description 4
- 206010017758 gastric cancer Diseases 0.000 claims description 4
- 208000005017 glioblastoma Diseases 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 201000007270 liver cancer Diseases 0.000 claims description 4
- 208000014018 liver neoplasm Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 208000025113 myeloid leukemia Diseases 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 159000000000 sodium salts Chemical group 0.000 claims description 4
- 201000011549 stomach cancer Diseases 0.000 claims description 4
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 4
- 125000002619 bicyclic group Chemical group 0.000 claims description 3
- -1 bicyclic sugars Chemical class 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 208000005016 Intestinal Neoplasms Diseases 0.000 claims 2
- 208000009905 Neurofibromatoses Diseases 0.000 claims 2
- 230000002489 hematologic effect Effects 0.000 claims 2
- 201000002313 intestinal cancer Diseases 0.000 claims 2
- 201000004931 neurofibromatosis Diseases 0.000 claims 2
- 150000007523 nucleic acids Chemical class 0.000 claims 2
- 108091028043 Nucleic acid sequence Proteins 0.000 claims 1
- 125000000129 anionic group Chemical group 0.000 claims 1
- 108020004707 nucleic acids Proteins 0.000 claims 1
- 102000039446 nucleic acids Human genes 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- IHLOTZVBEUFDMD-UUOKFMHZSA-N 7-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-2,2-dioxo-1h-imidazo[4,5-c][1,2,6]thiadiazin-4-one Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(NS(=O)(=O)NC2=O)=C2N=C1 IHLOTZVBEUFDMD-UUOKFMHZSA-N 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 2
- 102000040650 (ribonucleotides)n+m Human genes 0.000 description 2
- ABEXEQSGABRUHS-UHFFFAOYSA-N 16-methylheptadecyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC(C)C ABEXEQSGABRUHS-UHFFFAOYSA-N 0.000 description 2
- 102100030708 GTPase KRas Human genes 0.000 description 2
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 description 2
- 241000764238 Isis Species 0.000 description 2
- 206010027476 Metastases Diseases 0.000 description 2
- 201000004404 Neurofibroma Diseases 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 201000005787 hematologic cancer Diseases 0.000 description 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 description 2
- 238000005417 image-selected in vivo spectroscopy Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 238000012739 integrated shape imaging system Methods 0.000 description 2
- 230000009401 metastasis Effects 0.000 description 2
- 201000002314 small intestine cancer Diseases 0.000 description 2
- HWPZZUQOWRWFDB-UHFFFAOYSA-N 1-methylcytosine Chemical compound CN1C=CC(N)=NC1=O HWPZZUQOWRWFDB-UHFFFAOYSA-N 0.000 description 1
- 101710163270 Nuclease Proteins 0.000 description 1
- 108091028664 Ribonucleotide Proteins 0.000 description 1
- 239000005547 deoxyribonucleotide Substances 0.000 description 1
- 125000002637 deoxyribonucleotide group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 239000002773 nucleotide Substances 0.000 description 1
- 125000003729 nucleotide group Chemical group 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 239000002336 ribonucleotide Substances 0.000 description 1
- 125000002652 ribonucleotide group Chemical group 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562232120P | 2015-09-24 | 2015-09-24 | |
| US62/232,120 | 2015-09-24 | ||
| PCT/US2016/053334 WO2017053722A1 (en) | 2015-09-24 | 2016-09-23 | Modulators of kras expression |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018528781A JP2018528781A (ja) | 2018-10-04 |
| JP2018528781A5 true JP2018528781A5 (enExample) | 2020-11-12 |
| JP6877414B2 JP6877414B2 (ja) | 2021-05-26 |
Family
ID=58387506
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018515292A Expired - Fee Related JP6877414B2 (ja) | 2015-09-24 | 2016-09-23 | Ｋｒａｓ発現のモジュレーター |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20180273577A1 (enExample) |
| EP (1) | EP3353328A4 (enExample) |
| JP (1) | JP6877414B2 (enExample) |
| KR (1) | KR20180051626A (enExample) |
| CN (1) | CN108513588A (enExample) |
| AR (1) | AR106135A1 (enExample) |
| AU (2) | AU2016326619B2 (enExample) |
| BR (1) | BR112018004620A2 (enExample) |
| CA (1) | CA2998382A1 (enExample) |
| CL (1) | CL2018000429A1 (enExample) |
| CO (1) | CO2018003168A2 (enExample) |
| HK (2) | HK1255699A1 (enExample) |
| IL (1) | IL258013A (enExample) |
| MX (1) | MX2018003472A (enExample) |
| RU (1) | RU2018113709A (enExample) |
| SG (1) | SG10201913209WA (enExample) |
| TW (1) | TW201723176A (enExample) |
| WO (1) | WO2017053722A1 (enExample) |
| ZA (1) | ZA201802663B (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015004111A2 (pt) | 2012-09-25 | 2017-07-04 | Hoffmann La Roche | novos derivados bicíclicos |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| KR20160087900A (ko) | 2013-11-26 | 2016-07-22 | 에프. 호프만-라 로슈 아게 | 신규한 옥타하이드로-사이클로부타[1,2-c；3,4-c'']다이피롤-2-일 |
| SI3122750T1 (sl) | 2014-03-26 | 2019-12-31 | F. Hoffmann-La Roche Ag | Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA) |
| KR20160128428A (ko) | 2014-03-26 | 2016-11-07 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 및 리소포스파티드산(lpa) 생성 억제제로서의 축합형 [1,4]다이아제핀 화합물 |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| JP6886967B2 (ja) | 2015-09-04 | 2021-06-16 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | フェノキシメチル誘導体 |
| CN107635995B (zh) | 2015-09-24 | 2022-08-19 | 豪夫迈·罗氏有限公司 | 作为atx抑制剂的二环化合物 |
| AU2016328365B2 (en) | 2015-09-24 | 2020-04-23 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
| RU2018112230A (ru) | 2015-09-24 | 2019-10-30 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов atx |
| JP6877413B2 (ja) | 2015-09-24 | 2021-05-26 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 二重ａｔｘ／ｃａ阻害剤としての新規な二環式化合物 |
| US11180759B2 (en) * | 2016-01-19 | 2021-11-23 | The University Of North Carolina At Chapel Hill | Methods and compositions using RNA interference and antisense oligonucleotides for inhibition of KRAS |
| SG11201810171SA (en) | 2016-05-18 | 2018-12-28 | Mirati Therapeutics Inc | Kras g12c inhibitors |
| WO2018146316A1 (en) * | 2017-02-13 | 2018-08-16 | Astrazeneca Ab | Combination of a mapk pathway inhibitor and an antisense compound targeted to kras |
| US11261440B2 (en) | 2017-02-21 | 2022-03-01 | Osaka University | Antisense oligonucleic acid |
| WO2018167113A1 (en) | 2017-03-16 | 2018-09-20 | F. Hoffmann-La Roche Ag | New bicyclic compounds as atx inhibitors |
| EP3596059B1 (en) | 2017-03-16 | 2024-04-24 | F. Hoffmann-La Roche AG | Heterocyclic compounds useful as dual atx/ca inhibitors |
| PT3710439T (pt) | 2017-11-15 | 2023-05-15 | Array Biopharma Inc | Inibidores de kras g12c |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| AU2019218987B2 (en) | 2018-02-12 | 2025-04-24 | Ionis Pharmaceuticals, Inc. | Modified compounds and uses thereof |
| EP3752615B1 (en) | 2018-02-12 | 2025-08-27 | Lonza Sales AG | Methods and compositions for macrophage polarization |
| TWI840345B (zh) * | 2018-03-02 | 2024-05-01 | 美商Ionis製藥公司 | Irf4表現之調節劑 |
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| IL316397A (en) | 2018-05-22 | 2024-12-01 | Ionis Pharmaceuticals Inc | Modulators of APOL1 expression |
| JP7473113B2 (ja) * | 2018-07-31 | 2024-04-23 | 国立大学法人大阪大学 | オリゴヌクレオチドを含有する小細胞肺癌治療薬 |
| CA3111980A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| IL281344B2 (en) | 2018-09-10 | 2025-09-01 | Mirati Therapeutics Inc | Combination of adagrasib and cetuximab for cancer treatment |
| EP3849537B1 (en) | 2018-09-10 | 2024-10-23 | Mirati Therapeutics, Inc. | Combination therapies |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| TW202028222A (zh) * | 2018-11-14 | 2020-08-01 | 美商Ionis製藥公司 | Foxp3表現之調節劑 |
| CA3112129A1 (en) | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| TW202214854A (zh) | 2019-01-31 | 2022-04-16 | 美商Ionis製藥公司 | Yap1表現之調節劑 |
| EP4013872A1 (en) * | 2019-08-14 | 2022-06-22 | Codiak BioSciences, Inc. | Extracellular vesicles with antisense oligonucleotides targeting kras |
| AU2020337938B2 (en) | 2019-08-29 | 2025-09-25 | Array Biopharma Inc. | KRas G12D inhibitors |
| MX2022003537A (es) | 2019-09-24 | 2022-07-11 | Mirati Therapeutics Inc | Terapias de combinacion. |
| CN110981943B (zh) * | 2019-12-02 | 2021-08-03 | 清华大学 | 多肽及其在制备药物中的用途和药物 |
| EP4076418A4 (en) | 2019-12-20 | 2024-01-24 | Mirati Therapeutics, Inc. | Sos1 inhibitors |
| JP7427227B2 (ja) * | 2020-01-21 | 2024-02-05 | 学校法人産業医科大学 | 腫瘍細胞の生存を低下させるｋｒａｓアンチセンスオリゴヌクレオチド及びその用途 |
| AU2021340716A1 (en) | 2020-09-11 | 2023-03-30 | Mirati Therapeutics, Inc. | Crystalline forms of a KRas G12C inhibitor |
| AU2021401232A1 (en) | 2020-12-15 | 2023-06-22 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| KR102574252B1 (ko) * | 2020-12-15 | 2023-09-07 | 주식회사 시선테라퓨틱스 | 펩티드 핵산 복합체를 유효성분으로 함유하는 췌장암 예방 또는 치료용 조성물 |
| US11999753B2 (en) | 2020-12-16 | 2024-06-04 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-KRas inhibitors |
| US20240191233A1 (en) * | 2021-02-18 | 2024-06-13 | Ionis Pharmaceuticals, Inc. | Compounds and methods for reducing nlrp3 expression |
| JP2024532477A (ja) * | 2021-09-02 | 2024-09-05 | モレキュラー アクシオム エルエルシー | Ｋｒａｓ発現を調節するための組成物及び方法 |
| WO2024155770A2 (en) * | 2023-01-18 | 2024-07-25 | Molecular Axiom, Llc | Compositions for modulating kras expression and uses thereof |
| CN119639745B (zh) * | 2024-12-12 | 2025-11-25 | 制能(北京)生物科技有限公司 | 一种靶向kras基因的反义核酸及其药物制剂和应用 |
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-
2016
- 2016-09-23 SG SG10201913209WA patent/SG10201913209WA/en unknown
- 2016-09-23 HK HK18114849.4A patent/HK1255699A1/zh unknown
- 2016-09-23 HK HK18111182.5A patent/HK1251624A1/zh unknown
- 2016-09-23 TW TW105130913A patent/TW201723176A/zh unknown
- 2016-09-23 KR KR1020187010307A patent/KR20180051626A/ko not_active Withdrawn
- 2016-09-23 EP EP16849701.4A patent/EP3353328A4/en not_active Withdrawn
- 2016-09-23 RU RU2018113709A patent/RU2018113709A/ru not_active Application Discontinuation
- 2016-09-23 JP JP2018515292A patent/JP6877414B2/ja not_active Expired - Fee Related
- 2016-09-23 AU AU2016326619A patent/AU2016326619B2/en not_active Ceased
- 2016-09-23 CN CN201680053233.5A patent/CN108513588A/zh active Pending
- 2016-09-23 BR BR112018004620-5A patent/BR112018004620A2/pt active Search and Examination
- 2016-09-23 US US15/762,616 patent/US20180273577A1/en not_active Abandoned
- 2016-09-23 WO PCT/US2016/053334 patent/WO2017053722A1/en not_active Ceased
- 2016-09-23 MX MX2018003472A patent/MX2018003472A/es unknown
- 2016-09-23 CA CA2998382A patent/CA2998382A1/en not_active Abandoned
- 2016-09-23 AR ARP160102916A patent/AR106135A1/es unknown
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2018
- 2018-02-16 CL CL2018000429A patent/CL2018000429A1/es unknown
- 2018-03-11 IL IL258013A patent/IL258013A/en unknown
- 2018-03-23 CO CONC2018/0003168A patent/CO2018003168A2/es unknown
- 2018-04-20 ZA ZA2018/02663A patent/ZA201802663B/en unknown
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2020
- 2020-10-28 AU AU2020260436A patent/AU2020260436A1/en not_active Abandoned
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