SA520420426B1 - مركبات ترابطية تستهدف إنتجرين واستخداماتها - Google Patents
مركبات ترابطية تستهدف إنتجرين واستخداماتهاInfo
- Publication number
- SA520420426B1 SA520420426B1 SA520420426A SA520420426A SA520420426B1 SA 520420426 B1 SA520420426 B1 SA 520420426B1 SA 520420426 A SA520420426 A SA 520420426A SA 520420426 A SA520420426 A SA 520420426A SA 520420426 B1 SA520420426 B1 SA 520420426B1
- Authority
- SA
- Saudi Arabia
- Prior art keywords
- beta
- integrin
- integrin alpha
- alpha
- compounds
- Prior art date
Links
- 239000003446 ligand Substances 0.000 title abstract 3
- 101000713585 Homo sapiens Tubulin beta-4A chain Proteins 0.000 abstract 3
- 108010047852 Integrin alphaVbeta3 Proteins 0.000 abstract 3
- 102100036788 Tubulin beta-4A chain Human genes 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102100022337 Integrin alpha-V Human genes 0.000 abstract 2
- 108010040765 Integrin alphaV Proteins 0.000 abstract 2
- 210000004027 cell Anatomy 0.000 abstract 2
- 108010044426 integrins Proteins 0.000 abstract 2
- 102000006495 integrins Human genes 0.000 abstract 2
- 108091034117 Oligonucleotide Proteins 0.000 abstract 1
- 108091030071 RNAI Proteins 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 230000021615 conjugation Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000009368 gene silencing by RNA Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 210000002966 serum Anatomy 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
- 210000004881 tumor cell Anatomy 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
- A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/70546—Integrin superfamily
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/70546—Integrin superfamily
- C07K14/70557—Integrin beta3-subunit-containing molecules, e.g. CD41, CD51, CD61
-
- 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
- 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
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/14—Type of nucleic acid interfering nucleic acids [NA]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Wood Science & Technology (AREA)
- Toxicology (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Cell Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physics & Mathematics (AREA)
- Plant Pathology (AREA)
- Microbiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862663763P | 2018-04-27 | 2018-04-27 | |
| US201962790372P | 2019-01-09 | 2019-01-09 | |
| PCT/US2019/029393 WO2019210200A1 (en) | 2018-04-27 | 2019-04-26 | Integrin targeting ligands and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SA520420426B1 true SA520420426B1 (ar) | 2024-11-19 |
Family
ID=68294255
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SA520420426A SA520420426B1 (ar) | 2018-04-27 | 2020-10-27 | مركبات ترابطية تستهدف إنتجرين واستخداماتها |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20210093725A1 (enExample) |
| EP (2) | EP4435000A3 (enExample) |
| JP (2) | JP7704529B2 (enExample) |
| KR (1) | KR102787533B1 (enExample) |
| CN (2) | CN112074290B (enExample) |
| AU (1) | AU2019260738B2 (enExample) |
| BR (1) | BR112020021949A2 (enExample) |
| CA (1) | CA3097656A1 (enExample) |
| DK (1) | DK3784269T3 (enExample) |
| ES (1) | ES2983950T3 (enExample) |
| FI (1) | FI3784269T3 (enExample) |
| HR (1) | HRP20240907T1 (enExample) |
| IL (2) | IL309955A (enExample) |
| JO (1) | JOP20200266A1 (enExample) |
| MX (1) | MX2020011290A (enExample) |
| SA (1) | SA520420426B1 (enExample) |
| SG (1) | SG11202009734VA (enExample) |
| SI (1) | SI3784269T1 (enExample) |
| TW (1) | TW202014206A (enExample) |
| WO (1) | WO2019210200A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3120580A1 (en) | 2019-01-09 | 2020-07-16 | Arrowhead Pharmaceuticals, Inc. | Rnai agents for inhibiting expression of hif-2 alpha (epas1), compositions thereof, and methods of use |
| WO2022056266A2 (en) * | 2020-09-11 | 2022-03-17 | Arrowhead Pharmaceuticals, Inc. | Rnai agents for inhibiting expression of dux4, compositions thereof, and methods of use |
| US20240409927A1 (en) * | 2021-07-07 | 2024-12-12 | Alnylam Pharmaceuticals, Inc. | Integrin targeting ligands for ocular delivery of rnai compounds |
| WO2024260259A1 (zh) * | 2023-06-19 | 2024-12-26 | 广东众生睿创生物科技有限公司 | 一种整合素配体及其用途 |
| WO2025252118A1 (zh) * | 2024-06-06 | 2025-12-11 | 苏州瑞博生物技术股份有限公司 | 整联蛋白αvβ6特异性配体化合物、缀合物、药物组合物及其用途 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| US6017926A (en) * | 1997-12-17 | 2000-01-25 | Merck & Co., Inc. | Integrin receptor antagonists |
| US6048861A (en) * | 1997-12-17 | 2000-04-11 | Merck & Co., Inc. | Integrin receptor antagonists |
| IL136495A0 (en) | 1997-12-17 | 2001-06-14 | Merck & Co Inc | Integrin receptor antagonists |
| US20040224986A1 (en) * | 2002-08-16 | 2004-11-11 | Bart De Corte | Piperidinyl targeting compounds that selectively bind integrins |
| AU2009223235B2 (en) * | 2008-03-14 | 2014-09-11 | Merck Sharp & Dohme Corp. | Integrin targeting agents and in-vivo and in-vitro imaging methods using the same |
| MX2014008373A (es) | 2012-01-27 | 2014-09-26 | Hoffmann La Roche | Conjugados antagonistas de integrina para suministro dirigido a celulas que expresan alfa-v-beta-3. |
| CA2895430C (en) | 2013-01-28 | 2021-11-23 | Janssen Sciences Ireland Uc | Quinoxalinones and dihydroquinoxalinones as respiratory syncytial virus antiviral agents |
| SG11201506805QA (en) | 2013-02-28 | 2015-09-29 | Arrowhead Res Corp | Organic compositions to treat epas1-related diseases |
| KR20160035081A (ko) | 2013-08-07 | 2016-03-30 | 애로우헤드 리서치 코오포레이션 | 생체 내에서 RNAi 유발제를 종양 세포로 전달하기 위한 폴리콘주게이트 |
| EP3925959A1 (en) * | 2015-02-19 | 2021-12-22 | OcuTerra Therapeutics, Inc. | Fluorinated derivatives of 3-(2-oxo-3-(3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl)imidazolidin-1-yl)propanoic acid and uses thereof |
| WO2016172710A2 (en) * | 2015-04-24 | 2016-10-27 | Cornell University | Methods and reagents for determination and treatment of organotropic metastasis |
| EP3288555A1 (en) * | 2015-04-30 | 2018-03-07 | SciFluor Life Sciences, Inc. | Tetrahydronaphthyridinyl propionic acid derivatives and uses thereof |
| TWI761305B (zh) | 2015-05-29 | 2022-04-21 | 美商愛羅海德製藥公司 | 抑制Ｈｉｆ２α基因表現之組合物及方法 |
-
2019
- 2019-04-26 IL IL309955A patent/IL309955A/en unknown
- 2019-04-26 FI FIEP19794009.1T patent/FI3784269T3/fi active
- 2019-04-26 MX MX2020011290A patent/MX2020011290A/es unknown
- 2019-04-26 BR BR112020021949-5A patent/BR112020021949A2/pt unknown
- 2019-04-26 EP EP24179088.0A patent/EP4435000A3/en active Pending
- 2019-04-26 US US17/050,042 patent/US20210093725A1/en active Pending
- 2019-04-26 HR HRP20240907TT patent/HRP20240907T1/hr unknown
- 2019-04-26 SI SI201930780T patent/SI3784269T1/sl unknown
- 2019-04-26 AU AU2019260738A patent/AU2019260738B2/en active Active
- 2019-04-26 EP EP19794009.1A patent/EP3784269B1/en active Active
- 2019-04-26 DK DK19794009.1T patent/DK3784269T3/da active
- 2019-04-26 ES ES19794009T patent/ES2983950T3/es active Active
- 2019-04-26 WO PCT/US2019/029393 patent/WO2019210200A1/en not_active Ceased
- 2019-04-26 CA CA3097656A patent/CA3097656A1/en active Pending
- 2019-04-26 JP JP2020560257A patent/JP7704529B2/ja active Active
- 2019-04-26 SG SG11202009734VA patent/SG11202009734VA/en unknown
- 2019-04-26 JO JOP/2020/0266A patent/JOP20200266A1/ar unknown
- 2019-04-26 IL IL278304A patent/IL278304B2/en unknown
- 2019-04-26 CN CN201980028704.0A patent/CN112074290B/zh active Active
- 2019-04-26 KR KR1020207033772A patent/KR102787533B1/ko active Active
- 2019-04-26 CN CN202411099363.5A patent/CN118994152A/zh active Pending
- 2019-04-29 TW TW108114935A patent/TW202014206A/zh unknown
-
2020
- 2020-10-27 SA SA520420426A patent/SA520420426B1/ar unknown
-
2024
- 2024-12-27 JP JP2024232254A patent/JP2025060958A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| IL309955A (en) | 2024-03-01 |
| IL278304B1 (en) | 2024-02-01 |
| SG11202009734VA (en) | 2020-11-27 |
| KR20210005145A (ko) | 2021-01-13 |
| KR102787533B1 (ko) | 2025-03-31 |
| HRP20240907T1 (hr) | 2024-10-25 |
| AU2019260738B2 (en) | 2025-01-30 |
| FI3784269T3 (fi) | 2024-07-03 |
| CA3097656A1 (en) | 2019-10-31 |
| CN112074290B (zh) | 2024-09-10 |
| ES2983950T3 (es) | 2024-10-28 |
| JP7704529B2 (ja) | 2025-07-08 |
| JP2025060958A (ja) | 2025-04-10 |
| EP4435000A2 (en) | 2024-09-25 |
| BR112020021949A2 (pt) | 2021-01-26 |
| DK3784269T3 (da) | 2024-07-08 |
| JP2021522269A (ja) | 2021-08-30 |
| US20210093725A1 (en) | 2021-04-01 |
| TW202014206A (zh) | 2020-04-16 |
| SI3784269T1 (sl) | 2024-08-30 |
| EP3784269A4 (en) | 2022-03-23 |
| CN112074290A (zh) | 2020-12-11 |
| EP4435000A3 (en) | 2025-02-19 |
| EP3784269B1 (en) | 2024-06-05 |
| AU2019260738A1 (en) | 2020-10-15 |
| JOP20200266A1 (ar) | 2020-10-21 |
| WO2019210200A1 (en) | 2019-10-31 |
| IL278304A (enExample) | 2020-12-31 |
| MX2020011290A (es) | 2020-11-13 |
| CN118994152A (zh) | 2024-11-22 |
| IL278304B2 (en) | 2024-06-01 |
| EP3784269A1 (en) | 2021-03-03 |
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