JOP20200266A1 - مركبات ترابطية تستهدف إنتجرين واستخداماتها - Google Patents
مركبات ترابطية تستهدف إنتجرين واستخداماتهاInfo
- Publication number
- JOP20200266A1 JOP20200266A1 JOP/2020/0266A JOP20200266A JOP20200266A1 JO P20200266 A1 JOP20200266 A1 JO P20200266A1 JO P20200266 A JOP20200266 A JO P20200266A JO P20200266 A1 JOP20200266 A1 JO P20200266A1
- Authority
- JO
- Jordan
- Prior art keywords
- integrin
- targeting ligands
- compounds
- cargo molecules
- integrin targeting
- Prior art date
Links
- 102000006495 integrins Human genes 0.000 title abstract 7
- 108010044426 integrins Proteins 0.000 title abstract 7
- 239000003446 ligand Substances 0.000 title abstract 4
- 230000008685 targeting Effects 0.000 title abstract 3
- CTCHDPAJHVDPRN-UHFFFAOYSA-N integrin Chemical compound C=1C(OC)=CC(O)=C(C(C=2CC=C(C)C)=O)C=1OC=2C1=CC=C(O)C=C1O CTCHDPAJHVDPRN-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 210000004027 cell Anatomy 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
-
- 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
- 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
-
- 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
- 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
- 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 N.A.
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Biomedical Technology (AREA)
- Biotechnology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Wood Science & Technology (AREA)
- General Engineering & Computer Science (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Toxicology (AREA)
- Cell Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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)
Abstract
يتعلق الاختراع الحالي بوصف مركبات لها ألفة لمركبات إنتجرين وتخليق تلك المركبات واستخدام تلك المركبات في شكل مركبات ترابطية لتسهيل توصيل جزيئات حمولة إلى خلايا تعبر عن مركبات إنتجرين. يتعلق الاختراع بوصف مركبات ترابطية تستهدف إنتجرين التي لها ثبات خاص بالمصل وألفة خاصة بإنتجرين ?v?3 و/أو إنتجرين ?v?5 وهي مناسبة للترافق مع جزيئات الحمولة مثل العوامل العلاجية المعتمدة على الأوليجيونيوكليوتيد (مثل عوامل RNAi) لتسهيل توصيل جزيئات الحمولة إلى الخلايا والأنسجة مثل خلايا الورم التي تعبر عن ?v?3 أو إنتجرين ?v?5 أو كل من إنتجرين ?v?3 وإنتجرين ?v?5. وتم أيضاً وصف التركيبات التي تشتمل على المركبات الترابطية التي تستهدف إنتجرين وطرق استخدامها.
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 |
---|---|
JOP20200266A1 true JOP20200266A1 (ar) | 2020-10-21 |
Family
ID=68294255
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JOP/2020/0266A JOP20200266A1 (ar) | 2018-04-27 | 2019-04-26 | مركبات ترابطية تستهدف إنتجرين واستخداماتها |
Country Status (14)
Country | Link |
---|---|
US (1) | US20210093725A1 (ar) |
EP (1) | EP3784269B1 (ar) |
JP (1) | JP2021522269A (ar) |
KR (1) | KR20210005145A (ar) |
CN (1) | CN112074290A (ar) |
AU (1) | AU2019260738A1 (ar) |
BR (1) | BR112020021949A2 (ar) |
CA (1) | CA3097656A1 (ar) |
IL (2) | IL309955A (ar) |
JO (1) | JOP20200266A1 (ar) |
MX (1) | MX2020011290A (ar) |
SG (1) | SG11202009734VA (ar) |
TW (1) | TW202014206A (ar) |
WO (1) | WO2019210200A1 (ar) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP4367246A2 (en) * | 2021-07-07 | 2024-05-15 | Alnylam Pharmaceuticals, Inc. | Integrin targeting ligands for ocular delivery of rnai compounds |
Family Cites Families (12)
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 |
KR20010033248A (ko) * | 1997-12-17 | 2001-04-25 | 폴락 돈나 엘. | 인테그린 수용체 길항제 |
US6017926A (en) * | 1997-12-17 | 2000-01-25 | Merck & Co., Inc. | Integrin receptor antagonists |
US20040224986A1 (en) * | 2002-08-16 | 2004-11-11 | Bart De Corte | Piperidinyl targeting compounds that selectively bind integrins |
JP5586485B2 (ja) * | 2008-03-14 | 2014-09-10 | ビセン メディカル, インコーポレイテッド | インテグリン標的化剤およびそれらを用いるinvivoおよびinvitroでの画像化方法 |
CA2856619A1 (en) * | 2012-01-27 | 2013-08-01 | Robert Alan Goodnow, Jr. | Integrin antagonist conjugates for targeted delivery to cells expressing alpha-v-beta-3 |
SG11201506805QA (en) * | 2013-02-28 | 2015-09-29 | Arrowhead Res Corp | Organic compositions to treat epas1-related diseases |
EP3030244B1 (en) | 2013-08-07 | 2021-04-21 | Arrowhead Pharmaceuticals, Inc. | Polyconjugates for delivery of rnai triggers to tumor cells in vivo |
KR102647026B1 (ko) * | 2015-02-19 | 2024-03-12 | 사이플루어 라이프 사이언시즈, 인크 | 플루오르화 테트라히드로나프티리디닐 노난산 유도체 및 이의 용도 |
US11971402B2 (en) * | 2015-04-24 | 2024-04-30 | Cornell University | Methods and reagents for determination and treatment of organotropic metastasis |
WO2016176532A1 (en) * | 2015-04-30 | 2016-11-03 | Scifluor Life Sciences, Inc. | Tetrahydronaphthyridinyl propionic acid derivatives and uses thereof |
CN114601845A (zh) | 2015-05-29 | 2022-06-10 | 箭头药业股份有限公司 | 抑制Hif2α基因表达的组合物及方法 |
-
2019
- 2019-04-26 WO PCT/US2019/029393 patent/WO2019210200A1/en active Application Filing
- 2019-04-26 KR KR1020207033772A patent/KR20210005145A/ko not_active Application Discontinuation
- 2019-04-26 SG SG11202009734VA patent/SG11202009734VA/en unknown
- 2019-04-26 MX MX2020011290A patent/MX2020011290A/es unknown
- 2019-04-26 IL IL309955A patent/IL309955A/en unknown
- 2019-04-26 CN CN201980028704.0A patent/CN112074290A/zh active Pending
- 2019-04-26 BR BR112020021949-5A patent/BR112020021949A2/pt unknown
- 2019-04-26 CA CA3097656A patent/CA3097656A1/en active Pending
- 2019-04-26 US US17/050,042 patent/US20210093725A1/en active Pending
- 2019-04-26 JP JP2020560257A patent/JP2021522269A/ja active Pending
- 2019-04-26 JO JOP/2020/0266A patent/JOP20200266A1/ar unknown
- 2019-04-26 AU AU2019260738A patent/AU2019260738A1/en active Pending
- 2019-04-26 EP EP19794009.1A patent/EP3784269B1/en active Active
- 2019-04-26 IL IL278304A patent/IL278304B2/en unknown
- 2019-04-29 TW TW108114935A patent/TW202014206A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
JP2021522269A (ja) | 2021-08-30 |
TW202014206A (zh) | 2020-04-16 |
BR112020021949A2 (pt) | 2021-01-26 |
IL278304A (ar) | 2020-12-31 |
EP3784269A4 (en) | 2022-03-23 |
MX2020011290A (es) | 2020-11-13 |
CN112074290A (zh) | 2020-12-11 |
IL278304B1 (en) | 2024-02-01 |
EP3784269B1 (en) | 2024-06-05 |
US20210093725A1 (en) | 2021-04-01 |
IL278304B2 (en) | 2024-06-01 |
KR20210005145A (ko) | 2021-01-13 |
IL309955A (en) | 2024-03-01 |
AU2019260738A1 (en) | 2020-10-15 |
EP3784269A1 (en) | 2021-03-03 |
CA3097656A1 (en) | 2019-10-31 |
WO2019210200A1 (en) | 2019-10-31 |
SG11202009734VA (en) | 2020-11-27 |
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