RU2018113709A - Модуляторы экспрессии kras - Google Patents
Модуляторы экспрессии kras Download PDFInfo
- Publication number
- RU2018113709A RU2018113709A RU2018113709A RU2018113709A RU2018113709A RU 2018113709 A RU2018113709 A RU 2018113709A RU 2018113709 A RU2018113709 A RU 2018113709A RU 2018113709 A RU2018113709 A RU 2018113709A RU 2018113709 A RU2018113709 A RU 2018113709A
- Authority
- RU
- Russia
- Prior art keywords
- cancer
- compound
- segment
- linked nucleosides
- modified oligonucleotide
- Prior art date
Links
- 239000002777 nucleoside Substances 0.000 claims 60
- 150000001875 compounds Chemical class 0.000 claims 50
- 108091034117 Oligonucleotide Proteins 0.000 claims 31
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 31
- 125000003835 nucleoside group Chemical group 0.000 claims 28
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 claims 12
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 8
- LRSASMSXMSNRBT-UHFFFAOYSA-N 5-methylcytosine Chemical group CC1=CNC(=O)N=C1N LRSASMSXMSNRBT-UHFFFAOYSA-N 0.000 claims 7
- 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 claims 7
- 206010009944 Colon cancer Diseases 0.000 claims 6
- 229940104302 cytosine Drugs 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 208000003019 Neurofibromatosis 1 Diseases 0.000 claims 4
- 208000029742 colonic neoplasm Diseases 0.000 claims 4
- 201000009020 malignant peripheral nerve sheath tumor Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 208000029974 neurofibrosarcoma Diseases 0.000 claims 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 4
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 4
- 208000024834 Neurofibromatosis type 1 Diseases 0.000 claims 3
- 230000000295 complement effect Effects 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 108091032973 (ribonucleotides)n+m Proteins 0.000 claims 2
- 102000040650 (ribonucleotides)n+m Human genes 0.000 claims 2
- ABEXEQSGABRUHS-UHFFFAOYSA-N 16-methylheptadecyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC(C)C ABEXEQSGABRUHS-UHFFFAOYSA-N 0.000 claims 2
- 206010004593 Bile duct cancer Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 102100030708 GTPase KRas Human genes 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 2
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 claims 2
- 241000764238 Isis Species 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010027476 Metastases Diseases 0.000 claims 2
- 201000004404 Neurofibroma Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 238000005417 image-selected in vivo spectroscopy Methods 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000012739 integrated shape imaging system Methods 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 230000009401 metastasis Effects 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 208000025113 myeloid leukemia Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 210000000578 peripheral nerve Anatomy 0.000 claims 2
- 201000002314 small intestine cancer Diseases 0.000 claims 2
- 159000000000 sodium salts Chemical group 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 108091028664 Ribonucleotide Proteins 0.000 claims 1
- 206010042674 Swelling Diseases 0.000 claims 1
- 239000005547 deoxyribonucleotide Substances 0.000 claims 1
- 125000002637 deoxyribonucleotide group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- -1 methoxyethyl nucleoside Chemical class 0.000 claims 1
- 125000005642 phosphothioate group Chemical group 0.000 claims 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical group [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 239000002336 ribonucleotide Substances 0.000 claims 1
- 125000002652 ribonucleotide group Chemical group 0.000 claims 1
- 230000008961 swelling Effects 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
- C07H21/04—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
-
- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
-
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- A61K31/7088—Compounds having three or more nucleosides or nucleotides
- A61K31/713—Double-stranded nucleic acids or oligonucleotides
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12N2310/31—Chemical structure of the backbone
- C12N2310/315—Phosphorothioates
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/32—Chemical structure of the sugar
- C12N2310/321—2'-O-R Modification
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/32—Chemical structure of the sugar
- C12N2310/323—Chemical structure of the sugar modified ring structure
- C12N2310/3231—Chemical structure of the sugar modified ring structure having an additional ring, e.g. LNA, ENA
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/33—Chemical structure of the base
- C12N2310/334—Modified C
- C12N2310/3341—5-Methylcytosine
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/34—Spatial arrangement of the modifications
- C12N2310/341—Gapmers, i.e. of the type ===---===
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/34—Spatial arrangement of the modifications
- C12N2310/346—Spatial arrangement of the modifications having a combination of backbone and sugar modifications
-
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/352—Nature of the modification linked to the nucleic acid via a carbon atom
- C12N2310/3525—MOE, methoxyethoxy
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- C12N2320/00—Applications; Uses
- C12N2320/50—Methods for regulating/modulating their activity
- C12N2320/51—Methods for regulating/modulating their activity modulating the chemical stability, e.g. nuclease-resistance
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- General Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Physics & Mathematics (AREA)
- Biophysics (AREA)
- Microbiology (AREA)
- Plant Pathology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Analytical Chemistry (AREA)
- Oncology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
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 (2)
| Publication Number | Publication Date |
|---|---|
| RU2018113709A true RU2018113709A (ru) | 2019-10-30 |
| RU2018113709A3 RU2018113709A3 (enExample) | 2020-05-29 |
Family
ID=58387506
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018113709A RU2018113709A (ru) | 2015-09-24 | 2016-09-23 | Модуляторы экспрессии kras |
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 (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR092645A1 (es) | 2012-09-25 | 2015-04-29 | Hoffmann La Roche | Derivados biciclicos inhibidores de autotaxina (atx) |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| PE20160845A1 (es) | 2013-11-26 | 2016-09-10 | Hoffmann La Roche | Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo |
| EP3122751B1 (en) | 2014-03-26 | 2019-10-30 | F.Hoffmann-La Roche Ag | Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| PL3122750T3 (pl) | 2014-03-26 | 2020-03-31 | F.Hoffmann-La Roche Ag | Związki bicykliczne jako inhibitory wytwarzania autotaksyny (ATX) i kwasu lizofosfatydowego (LPA) |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| UA123362C2 (uk) | 2015-09-04 | 2021-03-24 | Ф. Хоффманн-Ля Рош Аг | Феноксиметильні похідні |
| AU2016328437A1 (en) | 2015-09-24 | 2018-01-25 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| WO2017050791A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual atx/ca inhibitors |
| MX2018002217A (es) | 2015-09-24 | 2018-03-23 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de autotaxina (atx). |
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- 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
-
2020
- 2020-10-28 AU AU2020260436A patent/AU2020260436A1/en not_active Abandoned
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| EP3353328A1 (en) | 2018-08-01 |
| WO2017053722A1 (en) | 2017-03-30 |
| MX2018003472A (es) | 2018-07-06 |
| CA2998382A1 (en) | 2017-03-30 |
| AU2016326619B2 (en) | 2020-07-30 |
| AU2016326619A1 (en) | 2018-05-10 |
| CN108513588A (zh) | 2018-09-07 |
| SG10201913209WA (en) | 2020-02-27 |
| JP6877414B2 (ja) | 2021-05-26 |
| HK1251624A1 (zh) | 2019-02-01 |
| AU2020260436A1 (en) | 2020-11-26 |
| EP3353328A4 (en) | 2019-06-12 |
| CL2018000429A1 (es) | 2018-08-10 |
| JP2018528781A (ja) | 2018-10-04 |
| RU2018113709A3 (enExample) | 2020-05-29 |
| US20180273577A1 (en) | 2018-09-27 |
| IL258013A (en) | 2018-05-31 |
| ZA201802663B (en) | 2019-01-30 |
| HK1255699A1 (zh) | 2019-08-23 |
| BR112018004620A2 (pt) | 2018-09-25 |
| AR106135A1 (es) | 2017-12-13 |
| TW201723176A (zh) | 2017-07-01 |
| CO2018003168A2 (es) | 2018-06-20 |
| KR20180051626A (ko) | 2018-05-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20210224 |