HRP20211410T1 - Pripravci i postupci za inhibiciju ekspresije gena lpa - Google Patents
Pripravci i postupci za inhibiciju ekspresije gena lpa Download PDFInfo
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- HRP20211410T1 HRP20211410T1 HRP20211410TT HRP20211410T HRP20211410T1 HR P20211410 T1 HRP20211410 T1 HR P20211410T1 HR P20211410T T HRP20211410T T HR P20211410TT HR P20211410 T HRP20211410 T HR P20211410T HR P20211410 T1 HRP20211410 T1 HR P20211410T1
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- 230000014509 gene expression Effects 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 102000057248 Lipoprotein(a) Human genes 0.000 claims 28
- 108010033266 Lipoprotein(a) Proteins 0.000 claims 28
- 238000012228 RNA interference-mediated gene silencing Methods 0.000 claims 28
- 230000009368 gene silencing by RNA Effects 0.000 claims 28
- 239000003795 chemical substances by application Substances 0.000 claims 27
- 230000000692 anti-sense effect Effects 0.000 claims 26
- 125000003729 nucleotide group Chemical group 0.000 claims 22
- 108091081021 Sense strand Proteins 0.000 claims 13
- 239000002773 nucleotide Substances 0.000 claims 6
- 230000008685 targeting Effects 0.000 claims 3
- BXJSAMKIFDDLGI-UHFFFAOYSA-N 2-(dimethylamino)-N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]benzamide Chemical compound COc1ccc(cc1S(=O)(=O)Nc1cccc(NCCNC(=O)c2ccccc2N(C)C)c1)-c1cccc(c1)C(=O)N(C)C BXJSAMKIFDDLGI-UHFFFAOYSA-N 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 2
- 102000005427 Asialoglycoprotein Receptor Human genes 0.000 claims 2
- 108010006523 asialoglycoprotein receptor Proteins 0.000 claims 2
- 208000026106 cerebrovascular disease Diseases 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 208000035657 Abasia Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 208000003017 Aortic Valve Stenosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 101100239890 Candida albicans (strain SC5314 / ATCC MYA-2876) NAG4 gene Proteins 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 101001024442 Cellulomonas fimi Beta-N-acetylglucosaminidase/beta-glucosidase Proteins 0.000 claims 1
- 208000002251 Dissecting Aneurysm Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 206010022680 Intestinal ischaemia Diseases 0.000 claims 1
- 208000004535 Mesenteric Ischemia Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000004531 Renal Artery Obstruction Diseases 0.000 claims 1
- 206010038378 Renal artery stenosis Diseases 0.000 claims 1
- 201000007527 Retinal artery occlusion Diseases 0.000 claims 1
- 208000007718 Stable Angina Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 206010002895 aortic dissection Diseases 0.000 claims 1
- 206010002906 aortic stenosis Diseases 0.000 claims 1
- 201000002064 aortic valve insufficiency Diseases 0.000 claims 1
- 230000000295 complement effect Effects 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 229930182830 galactose Natural products 0.000 claims 1
- 125000001921 locked nucleotide group Chemical group 0.000 claims 1
- 210000001363 mesenteric artery superior Anatomy 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- RHLMXWCISNJNDH-UHFFFAOYSA-N n-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]-3-methylbenzamide Chemical compound COC1=CC=C(C=2C=C(C=CC=2)C(=O)N(C)C)C=C1S(=O)(=O)NC(C=1)=CC=CC=1NCCNC(=O)C1=CC=CC(C)=C1 RHLMXWCISNJNDH-UHFFFAOYSA-N 0.000 claims 1
- 208000030613 peripheral artery disease Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 1
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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
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- 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
- C12N15/1137—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 enzymes
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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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C12N2310/00—Structure or type of the nucleic acid
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Claims (21)
1. LPA (Lipoprotein(a)) RNA interferencijsko (RNAi) sredstvo koje sadrži smisleni lanac i protusmisleni lanac, naznačeno time što protusmisleni lanac sadrži sekvencu bilo koje od SEQ ID NO:1280, SEQ ID NO:1282, SEQ ID NO:1246, SEQ ID NO:1242, SEQ ID NO:1244, ili SEQ ID NO:1254, i pri čemu smisleni lanac sadrži sekvencu koja je komplementarna sa sekvencom protusmislenog lanca.
2. LPA RNAi sredstvo prema patentnom zahtjevu 1, naznačeno time što su smisleni lanac i protusmisleni lanac svaki dužine 19 do 26 nukleotida.
3. LPA RNAi sredstvo prema patentnom zahtjevu 2, naznačeno time što su smisleni lanac i protusmisleni lanac svaki dužine 21 nukleotida.
4. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 3, naznačeno time što LPA RNAi sredstvo sadrži jedno ili dva izbočenja.
5. LPA RNAi sredstvo prema patentnom zahtjevu 4, naznačeno time što LPA RNAi sredstvo sadrži izbočenje na 3' kraju protusmislenog lanca i izbočenje na 3' kraju smislenog lanca.
6. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 3, naznačeno time što LPA RNAi sredstvo sadrži jedan ili dva tupa kraja.
7. LPA RNAi sredstvo prema patentnom zahtjevu 6, naznačeno time što LPA RNAi sredstvo sadrži dva tupa kraja.
8. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 7, naznačeno time što smisleni lanac, protusmisleni lanac, ili oba smisleni i protusmisleni lanac sadrže jedan ili više modificiranih nukleotida.
9. LPA RNAi sredstvo prema patentnom zahtjevu 8, naznačeno time što su jedan ili više modificiranih nukleotida neovisno odabrani od 2'-modificiranog nukleotida, zaključanog nukleotida, abazičnog nukleotida, invertiranog deoksinukleotida, morfolino nukleotida, mimetika 2',3'-seko nukleotida, ili nukleotida koji sadrži neprirodnu bazu.
10. LPA RNAi sredstvo prema patentnom zahtjevu 9, naznačeno time što 2'-modificirani nukleotid je 2'-O-metil nukleotid, 2'-deoksi-2'-fluoro nukleotid, 2'-deoksinukleotid, 2'-metoksietil nukleotid, 2'-amino nukleotid, ili 2'-alkil nukleotid.
11. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 10, naznačeno time što LPA RNAi sredstvo sadrži jednu ili više fosforotioatnih intemukleozidnih veza.
12. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 11, naznačeno time što LPA RNAi sredstvo nadalje sadrži ciljajuću skupinu, pri čemu ciljajuća skupina sadrži ligand receptora asialoglikoproteina.
13. LPA RNAi sredstvo prema patentnom zahtjevu 12, naznačeno time što ligand receptora asialoglikoproteina sadrži klaster galaktoze odabran od (C11-PEG3-NAG3), (C6-PEG4-NAG3), (NAG3), (NAG4), (NAG3-AA2), (NAG3-Palm), (NAG13), (NAG18), (NAG24), (NAG25), (NAG25)s, (NAG26), (NAG27), (NAG28), (NAG29), (NAG30), (NAG30)s, (NAG31), (NAG31s), (NAG32), (NAG33), (NAG34), (NAG35), (NAG36), i (NAG37).
14. LPA RNAi sredstvo prema patentnom zahtjevu 12 ili 13, naznačeno time što je ciljajuća skupina konjugirana na 5' kraj smislenog lanca ili 3' kraj smislenog lanca.
15. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 14, naznačeno time što:
a) protusmisleni lanac sadrži sekvencu SEQ ID NO:1280 i smisleni lanac sadrži sekvencu SEQ ID NO:1284;
b) protusmisleni lanac sadrži sekvencu SEQ ID NO:1246 i smisleni lanac sadrži sekvencu SEQ ID NO:1247;
c) protusmisleni lanac sadrži sekvencu SEQ ID NO:1242 i smisleni lanac sadrži sekvencu SEQ ID NO:1243;
d) protusmisleni lanac sadrži sekvencu SEQ ID NO:1244 i smisleni lanac sadrži sekvencu SEQ ID NO:1245;
e) protusmisleni lanac sadrži sekvencu SEQ ID NO:1254 i smisleni lanac sadrži sekvencu SEQ ID NO:1255;
f) protusmisleni lanac sadrži sekvencu SEQ ID NO:1280 i smisleni lanac sadrži sekvencu SEQ ID NO:1260; ili
g) protusmisleni lanac sadrži sekvencu SEQ ID NO:1282 i smisleni lanac sadrži sekvencu SEQ ID NO:1259.
16. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 15, naznačeno time što:
a) protusmisleni lanac sadrži sekvencu SEQ ID NO:188 i smisleni lanac sadrži sekvencu SEQ ID NO:384;
b) protusmisleni lanac sadrži sekvencu SEQ ID NO:156 i smisleni lanac sadrži sekvencu SEQ ID NO:310;
c) protusmisleni lanac sadrži sekvencu SEQ ID NO:164 i smisleni lanac sadrži sekvencu SEQ ID NO:357;
d) protusmisleni lanac sadrži sekvencu SEQ ID NO:164 i smisleni lanac sadrži sekvencu SEQ ID NO:376; ili
e) protusmisleni lanac sadrži sekvencu SEQ ID NO:164 i smisleni lanac sadrži sekvencu SEQ ID NO:384.
17. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 16, naznačeno time što:
a) protusmisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 790 i smisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 1189;
b) protusmisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 637 i smisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 1132;
c) protusmisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 709 i smisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 1135;
d) protusmisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 787 i smisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 1191; ili
e) protusmisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 788 i smisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 1189.
18. LPA RNAi sredstvo prema patentnom zahtjevu 17, naznačeno time što protusmisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 790 i smisleni lanac sadrži sekvencu modificiranih nukleotida prema SEQ ID NO: 1189.
19. Farmaceutski pripravak naznačen time što sadrži LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 18 i farmaceutski prihvatljivu pomoćnu tvar.
20. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 18 naznačeno time što je za upotrebu u liječenju kardiovaskularne bolesti kod subjekta kojem je to potrebno.
21. LPA RNAi sredstvo prema bilo kojem od patentnih zahtjeva 1 do 18 naznačeno time što je za upotrebu u liječenju Bergerove bolesti, bolesti perifernih arterija, koronarne arterijske bolesti, metaboličkog sindroma, akutnog koronarnog sindroma, stenoze aortne valvule, regurgitacije aortne valvule, disekcije aorte, okluzije retinalne arterije, cerebrovaskularne bolesti, mezenterične ishemije, začepljenja gornje mezenterične arterije, stenoze bubrežne arterije, stabilne/nestabilne angine pektoris, akutnog koronarnog sindroma, heterozigotne ili homozigotne nasljedne hiperkolesterolemije, hiperapobetalipoproteinemije, cerebrovaskularne ateroskleroze, cerebrovaskularne bolesti, ili venske tromboze kod subjekta kojem je to potrebno.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562235816P | 2015-10-01 | 2015-10-01 | |
| US201662346304P | 2016-06-06 | 2016-06-06 | |
| US201662383221P | 2016-09-02 | 2016-09-02 | |
| EP16852695.2A EP3356529B1 (en) | 2015-10-01 | 2016-09-30 | Compositions and methods for inhibiting gene expression of lpa |
| PCT/US2016/054729 WO2017059223A2 (en) | 2015-10-01 | 2016-09-30 | Compositions and methods for inhibiting gene expression of lpa |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211410T1 true HRP20211410T1 (hr) | 2021-12-24 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211410TT HRP20211410T1 (hr) | 2015-10-01 | 2016-09-30 | Pripravci i postupci za inhibiciju ekspresije gena lpa |
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| Country | Link |
|---|---|
| US (3) | US9932586B2 (hr) |
| EP (2) | EP4029941A1 (hr) |
| JP (4) | JP6991966B2 (hr) |
| KR (1) | KR20180052703A (hr) |
| CN (1) | CN108368506A (hr) |
| AU (2) | AU2016331084B2 (hr) |
| BR (1) | BR112018006489A2 (hr) |
| CA (1) | CA3000397A1 (hr) |
| CL (1) | CL2018000803A1 (hr) |
| CO (1) | CO2018003678A2 (hr) |
| CR (1) | CR20180231A (hr) |
| CY (1) | CY1125263T1 (hr) |
| DK (1) | DK3356529T3 (hr) |
| EA (1) | EA038478B1 (hr) |
| ES (1) | ES2896298T3 (hr) |
| HK (1) | HK1259063A1 (hr) |
| HR (1) | HRP20211410T1 (hr) |
| HU (1) | HUE055942T2 (hr) |
| IL (3) | IL300438A (hr) |
| JO (2) | JOP20210043A1 (hr) |
| LT (1) | LT3356529T (hr) |
| MA (1) | MA43347B1 (hr) |
| MX (2) | MX2018003833A (hr) |
| MY (1) | MY195796A (hr) |
| PE (1) | PE20181139A1 (hr) |
| PH (1) | PH12018500713A1 (hr) |
| PL (1) | PL3356529T3 (hr) |
| PT (1) | PT3356529T (hr) |
| RS (1) | RS62523B1 (hr) |
| SG (1) | SG10202008530TA (hr) |
| SI (1) | SI3356529T1 (hr) |
| TN (1) | TN2018000094A1 (hr) |
| TW (2) | TWI784934B (hr) |
| UA (1) | UA121998C2 (hr) |
| UY (1) | UY36926A (hr) |
| WO (1) | WO2017059223A2 (hr) |
| ZA (1) | ZA202106265B (hr) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7718133B2 (en) | 2003-10-09 | 2010-05-18 | 3M Innovative Properties Company | Multilayer processing devices and methods |
| AU2017229469B2 (en) * | 2016-03-07 | 2023-02-23 | Arrowhead Pharmaceuticals, Inc. | Targeting ligands for therapeutic compounds |
| BR112019004178A2 (pt) * | 2016-09-02 | 2019-05-28 | Arrowhead Pharmaceuticals Inc | ligantes de alvejamento |
| RS63836B1 (sr) | 2017-04-05 | 2023-01-31 | Silence Therapeutics Gmbh | Proizvodi i sastavi |
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