MX2021008261A - Agentes de rnai para inhibir la expresion de hif-2 a (epas1), composiciones de estos y metodos de uso. - Google Patents
Agentes de rnai para inhibir la expresion de hif-2 a (epas1), composiciones de estos y metodos de uso.Info
- Publication number
- MX2021008261A MX2021008261A MX2021008261A MX2021008261A MX2021008261A MX 2021008261 A MX2021008261 A MX 2021008261A MX 2021008261 A MX2021008261 A MX 2021008261A MX 2021008261 A MX2021008261 A MX 2021008261A MX 2021008261 A MX2021008261 A MX 2021008261A
- Authority
- MX
- Mexico
- Prior art keywords
- alpha
- hif
- rnai agents
- methods
- compositions
- Prior art date
Links
- 108091030071 RNAI Proteins 0.000 title abstract 7
- 230000014509 gene expression Effects 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title 1
- 108010018033 endothelial PAS domain-containing protein 1 Proteins 0.000 abstract 7
- 239000003795 chemical substances by application Substances 0.000 abstract 6
- 230000009368 gene silencing by RNA Effects 0.000 abstract 6
- 208000030808 Clear cell renal carcinoma Diseases 0.000 abstract 3
- 208000006265 Renal cell carcinoma Diseases 0.000 abstract 3
- 206010073251 clear cell renal cell carcinoma Diseases 0.000 abstract 3
- 201000011330 nonpapillary renal cell carcinoma Diseases 0.000 abstract 3
- 102000006495 integrins Human genes 0.000 abstract 2
- 108010044426 integrins Proteins 0.000 abstract 2
- 102100036448 Endothelial PAS domain-containing protein 1 Human genes 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 239000003623 enhancer Substances 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000008685 targeting Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K48/00—Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
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- 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
- C12N15/1138—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 against receptors or cell surface proteins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/713—Double-stranded nucleic acids or oligonucleotides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/40—2,5-Pyrrolidine-diones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- 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
- C12N15/1135—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 against oncogenes or tumor suppressor genes
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01K—ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
- A01K2207/00—Modified animals
- A01K2207/12—Animals modified by administration of exogenous cells
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01K—ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
- A01K2227/00—Animals characterised by species
- A01K2227/10—Mammal
- A01K2227/105—Murine
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01K—ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
- A01K2267/00—Animals characterised by purpose
- A01K2267/03—Animal model, e.g. for test or diseases
- A01K2267/0331—Animal model for proliferative diseases
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/14—Type of nucleic acid interfering N.A.
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- 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
- C12N2310/33—Chemical structure of the base
- C12N2310/333—Modified A
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/34—Spatial arrangement of the modifications
- C12N2310/343—Spatial arrangement of the modifications having patterns, e.g. ==--==--==--
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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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- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
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- C12N2310/3515—Lipophilic moiety, e.g. cholesterol
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- C12N2320/30—Special therapeutic applications
- C12N2320/34—Allele or polymorphism specific uses
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Genetics & Genomics (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Wood Science & Technology (AREA)
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- Plant Pathology (AREA)
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- Physics & Mathematics (AREA)
- Microbiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
La presente divulgación se refiere a agentes de RNAi, por ejemplo, agentes de RNAi bicatenarios, capaces de inhibir la expresión del gen HIF-2 a (EPAS1). También se divulgan composiciones farmacéuticas que incluyen agentes de RNAi de HIF-2 a y métodos de uso de estos. Los agentes de RNAi de HIF-2 a divulgados en el presente documento pueden unirse o conjugarse con ligandos de direccionamiento (tales como compuestos que tienen afinidad por integrinas, incluidas integrinas a-v-beta-3 y a-v-beta-5) y potenciadores farmacocinéticos (PK), para facilitar la administración a células y tejidos, incluidos tumores y células de carcinoma renal de células claras (ccRCC). La administración de composiciones que comprenden los agentes de RNAi de HIF-2 a in vivo proporciona la inhibición de la expresión del gen HIF-2 a. Los agentes de RNAi de HIF-2 a pueden utilizarse en métodos de tratamiento de diversas enfermedades y trastornos, incluido ccRCC.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201962790360P | 2019-01-09 | 2019-01-09 | |
US201962827564P | 2019-04-01 | 2019-04-01 | |
US201962839381P | 2019-04-26 | 2019-04-26 | |
PCT/US2020/012775 WO2020146521A2 (en) | 2019-01-09 | 2020-01-08 | Rnai agents for inhibiting expression of hif-2 alpha (epas1), compositions thereof, and methods of use |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2021008261A true MX2021008261A (es) | 2021-08-16 |
Family
ID=71520182
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2021008261A MX2021008261A (es) | 2019-01-09 | 2020-01-08 | Agentes de rnai para inhibir la expresion de hif-2 a (epas1), composiciones de estos y metodos de uso. |
Country Status (14)
Country | Link |
---|---|
US (1) | US20220204976A1 (es) |
EP (1) | EP3908288A4 (es) |
JP (1) | JP2022518384A (es) |
KR (1) | KR20210113273A (es) |
CN (1) | CN113613661A (es) |
AU (1) | AU2020207050A1 (es) |
BR (1) | BR112021013362A2 (es) |
CA (1) | CA3120580A1 (es) |
IL (1) | IL284696A (es) |
MX (1) | MX2021008261A (es) |
SG (1) | SG11202105577TA (es) |
TW (1) | TW202043470A (es) |
UY (1) | UY38539A (es) |
WO (1) | WO2020146521A2 (es) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN114053426A (zh) * | 2020-07-30 | 2022-02-18 | 成都科岭源医药技术有限公司 | 一种双药链接组装单元及双药靶向接头-药物偶联物 |
JP2023541427A (ja) * | 2020-09-11 | 2023-10-02 | アローヘッド ファーマシューティカルズ インコーポレイテッド | 骨格筋送達プラットフォーム及び使用方法 |
WO2022086882A1 (en) | 2020-10-21 | 2022-04-28 | Nikang Therapeutics, Inc. | Diagnostic and therapeutic methods for treatment of cancer with a hif-2(alpha) inhibitor |
CN115105607A (zh) * | 2021-03-22 | 2022-09-27 | 成都科岭源医药技术有限公司 | 一种用于adc的双药-接头的制备方法及其用途 |
CN113304274A (zh) * | 2021-04-23 | 2021-08-27 | 南开大学 | 缀合物及其制备方法和用途 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8685370B2 (en) * | 2008-03-14 | 2014-04-01 | Visen Medical, Inc. | Integrin targeting agents and in-vivo and in-vitro imaging methods using the same |
WO2009123764A2 (en) * | 2008-04-04 | 2009-10-08 | Calando Pharmaceuticals, Inc. | Compositions and use of epas1 inhibitors |
CA2902393C (en) * | 2013-02-28 | 2022-11-01 | Arrowhead Research Corporation | Organic compositions to treat epas1-related diseases |
MX2017014641A (es) * | 2015-05-29 | 2018-01-23 | Arrowhead Pharmaceuticals Inc | Composiciones y metodos para inhibir la expresion del gen de factor inducible por hipoxia alfa (hif2alfa). |
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2020
- 2020-01-08 US US17/420,460 patent/US20220204976A1/en active Pending
- 2020-01-08 EP EP20738972.7A patent/EP3908288A4/en active Pending
- 2020-01-08 JP JP2021540037A patent/JP2022518384A/ja active Pending
- 2020-01-08 MX MX2021008261A patent/MX2021008261A/es unknown
- 2020-01-08 KR KR1020217024646A patent/KR20210113273A/ko unknown
- 2020-01-08 AU AU2020207050A patent/AU2020207050A1/en not_active Abandoned
- 2020-01-08 CA CA3120580A patent/CA3120580A1/en active Pending
- 2020-01-08 BR BR112021013362A patent/BR112021013362A2/pt not_active Application Discontinuation
- 2020-01-08 SG SG11202105577TA patent/SG11202105577TA/en unknown
- 2020-01-08 WO PCT/US2020/012775 patent/WO2020146521A2/en unknown
- 2020-01-08 CN CN202080008795.4A patent/CN113613661A/zh active Pending
- 2020-01-09 TW TW109100806A patent/TW202043470A/zh unknown
- 2020-01-09 UY UY0001038539A patent/UY38539A/es unknown
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2021
- 2021-07-07 IL IL284696A patent/IL284696A/en unknown
Also Published As
Publication number | Publication date |
---|---|
WO2020146521A3 (en) | 2020-08-20 |
IL284696A (en) | 2021-08-31 |
EP3908288A2 (en) | 2021-11-17 |
CN113613661A (zh) | 2021-11-05 |
KR20210113273A (ko) | 2021-09-15 |
TW202043470A (zh) | 2020-12-01 |
UY38539A (es) | 2020-07-31 |
SG11202105577TA (en) | 2021-06-29 |
AU2020207050A1 (en) | 2021-06-17 |
CA3120580A1 (en) | 2020-07-16 |
WO2020146521A2 (en) | 2020-07-16 |
US20220204976A1 (en) | 2022-06-30 |
BR112021013362A2 (pt) | 2021-12-14 |
JP2022518384A (ja) | 2022-03-15 |
EP3908288A4 (en) | 2023-12-20 |
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