HRP20140116T1 - Derivati retinala i postupci za njihovu upotrebu u lijeäśenju poremeä†aja vida - Google Patents
Derivati retinala i postupci za njihovu upotrebu u lijeäśenju poremeä†aja vida Download PDFInfo
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- HRP20140116T1 HRP20140116T1 HRP20140116TT HRP20140116T HRP20140116T1 HR P20140116 T1 HRP20140116 T1 HR P20140116T1 HR P20140116T T HRP20140116T T HR P20140116TT HR P20140116 T HRP20140116 T HR P20140116T HR P20140116 T1 HRP20140116 T1 HR P20140116T1
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- retinyl
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- 150000003726 retinal derivatives Chemical class 0.000 title claims 15
- 208000013521 Visual disease Diseases 0.000 title 1
- 208000029257 vision disease Diseases 0.000 title 1
- 201000003533 Leber congenital amaurosis Diseases 0.000 claims 8
- NCYCYZXNIZJOKI-IOUUIBBYSA-N 11-cis-retinal Chemical compound O=C/C=C(\C)/C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-IOUUIBBYSA-N 0.000 claims 7
- NCYCYZXNIZJOKI-HPNHMNAASA-N 11Z-retinal Natural products CC(=C/C=O)C=C/C=C(C)/C=C/C1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-HPNHMNAASA-N 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 6
- 230000007812 deficiency Effects 0.000 claims 5
- 150000002148 esters Chemical group 0.000 claims 5
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 206010064930 age-related macular degeneration Diseases 0.000 claims 4
- 229940102223 injectable solution Drugs 0.000 claims 4
- 108091008695 photoreceptors Proteins 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- WWDMJSSVVPXVSV-YCNIQYBTSA-N retinyl ester Chemical compound CC1CCCC(C)(C)C1\C=C\C(\C)=C\C=C\C(\C)=C\C(O)=O WWDMJSSVVPXVSV-YCNIQYBTSA-N 0.000 claims 3
- QGNJRVVDBSJHIZ-AQDFTDIISA-N (2e,4e,6z,8e)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-en-1-yl)nona-2,4,6,8-tetraen-1-yl acetate Chemical group CC(=O)OC\C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C QGNJRVVDBSJHIZ-AQDFTDIISA-N 0.000 claims 2
- NCYCYZXNIZJOKI-MKOSUFFBSA-N 9-cis-retinal Chemical class O=C/C=C(\C)/C=C/C=C(/C)\C=C\C1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-MKOSUFFBSA-N 0.000 claims 2
- 201000004569 Blindness Diseases 0.000 claims 2
- 208000003492 Fundus albipunctatus Diseases 0.000 claims 2
- 206010038910 Retinitis Diseases 0.000 claims 2
- 208000006623 congenital stationary night blindness Diseases 0.000 claims 2
- 239000003889 eye drop Substances 0.000 claims 2
- 229940012356 eye drops Drugs 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 229940049920 malate Drugs 0.000 claims 2
- 150000002763 monocarboxylic acids Chemical class 0.000 claims 2
- 230000004297 night vision Effects 0.000 claims 2
- 230000035945 sensitivity Effects 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- KPGXRSRHYNQIFN-UHFFFAOYSA-L 2-oxoglutarate(2-) Chemical compound [O-]C(=O)CCC(=O)C([O-])=O KPGXRSRHYNQIFN-UHFFFAOYSA-L 0.000 claims 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 1
- KHPXUQMNIQBQEV-UHFFFAOYSA-N oxaloacetic acid Chemical compound OC(=O)CC(=O)C(O)=O KHPXUQMNIQBQEV-UHFFFAOYSA-N 0.000 claims 1
- 229920005646 polycarboxylate Polymers 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/225—Polycarboxylic acids
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61P27/00—Drugs for disorders of the senses
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- C07C403/06—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms
- C07C403/10—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms by etherified hydroxy groups
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- C07C403/06—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms
- C07C403/12—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms by esterified hydroxy groups
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- C07C403/14—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by doubly-bound oxygen atoms
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- C07C403/20—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by carboxyl groups or halides, anhydrides, or (thio)esters thereof
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Claims (34)
1. Derivat 9-cis-retinala čija je struktura predstavljena Formulom I,
[image]
naznačen time, da A predstavlja CH2OR, a R tvori retinil ester namijenjen liječenju endogena deficijencija 11-cis-retinala kod ljudskog subjekta.
2. Derivat retinala za upotrebu u skladu s patentnim zahtjevom 1, koji je 9-cis-retinil ester, naznačen time, da esterski supstituent sadržava karboksilatni radikal C1-C10 monokarboksilne kiseline ili C2-C22 polikarboksilne kiseline.
3. Derivat retinala za upotrebu u skladu s patentnim zahtjevom 2, naznačen time, da je to 9-cis-retinil ester C3-C22 polikarboksilata.
4. Derivat retinala za upotrebu u skladu s patentnim zahtjevom 2, naznačen time, da je to 9-cis-retinil ester C1-C10 monokarboksilata.
5. Derivat retinala za upotrebu u skladu s patentnim zahtjevom 3, naznačen time, da je 9-cis-retinil ester 9-cis-retinil sukcinat, 9-cis-retinil citrat, 9-cis-retinil ketoglutarat, 9-cis-retinil fumarat, 9-cis-retinil malat ili 9-cis-retinil oksaloacetat.
6. Derivat retinala za upotrebu u skladu s patentnim zahtjevom 4, naznačen time, da je 9-cis-retinil ester 9-cis-retinil acetat.
7. Derivat retinala za upotrebu u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time, da se upotrebljava za ponovnu uspostavu fotoreceptorske funkcije kod navedenog ljudskog subjekta.
8. Derivat retinala za upotrebu u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time, da se upotrebljava za usporavanja gubitka fotoreceptorske funkcije kod navedenog ljudskog subjekta.
9. Derivat retinala za upotrebu u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time, da je navedena endogena deficijencija 11-cis-retinala povezana sa senilnom makularnom degeneracijom, Leberovom kongenitalnom amaurozom (LCA), retinitis punctata albesciens, kongenitalnim stacionarnim noćnim sljepilom ili fundus albipunctatus.
10. Derivat retinala za upotrebu u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time, da se upotrebljava za zadovoljavanje potrebe za endogenim 11-cis-retinalom kod navedenog ljudskog subjekta.
11. Derivat retinala za upotrebu u skladu s bilo kojim od patentnih zahtjeva 1-6, za liječenje gubitka noćnog vida ili gubitka kontrastne osjetljivosti, naznačen time, da je navedeni ljudski subjekt ljudski subjekt starije dobi.
12. Derivat retinala za upotrebu u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time, da se upotrebljava za liječenje makularne degeneracije povezane sa starenjem.
13. Derivat retinala za upotrebu u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time, da se upotrebljava za liječenje Leberove kongenitalne amauroze (LCA).
14. Farmaceutski pripravak za upotrebu u liječenju endogene deficijencije 11-cis-retinala kod ljudskog subjekta, naznačen time, da taj pripravak sadržava derivat retinala za upotrebu u skladu s bilo kojim od patentnih zahtjeva 1 do 13 i farmaceutski prihvatljiv vehikul.
15. Farmaceutski pripravak za upotrebu u skladu s patentnim zahtjevom 14, naznačen time, da je spravljen u obliku oftalmološkog pripravka u oftalmološki prihvatljivom vehikulu za lokalnu primjenu na oku ili intraokularnom injekcijom.
16. Farmaceutski pripravak za upotrebu u skladu s patentnim zahtjevom 14, naznačena time, da je farmaceutski pripravak spravljen za primjenu u obliku kapljica za oči, u obliku intraokularne injektibilne otopine ili u obliku periokularne injektibilne otopine.
17. Upotreba derivata 9-cis-retinala čija je struktura predstavljena Formulom I,
[image]
pri čemu A predstavlja CH2OR, a R tvori retinil ester, naznačena time, da je to upotreba za pripravu lijeka za liječenje endogene deficijencije 11-cis- retinala kod ljudskog subjekta.
18. Upotreba iz patentnog zahtjeva 17, naznačena time, da je derivat retinala 9-cis-retinil ester, pri čemu esterski supstituent sadržava karboksilatni radikal C1-C10 monokarboksilne kiseline ili C2-C22 polikarboksilne kiseline.
19. Upotreba iz patentnog zahtjeva 17 ili 18, naznačena time, da se upotrebljava za ponovnu uspostavu fotoreceptorske funkcije kod navedenog ljudskog subjekta.
20. Upotreba iz patentnog zahtjeva 17 ili 18, naznačena time, da se upotrebljava za usporavanja gubitka fotoreceptorske funkcije kod navedenog ljudskog subjekta.
21. Upotreba iz patentnog zahtjeva 17 ili 18, naznačena time, da je deficijencija endogenog 11-cis-retinala povezana sa senilnom makularnom degeneracijom, Leberovom kongenitalnim amaurozom (LCA), retinitis punctata albesciens, kongenitalnim stacionarnim noćnim sljepilom ili fundus albipunctatus.
22. Upotreba iz patentnog zahtjeva 17 ili 18, naznačena time, da se upotrebljava za liječenje Leberove kongenitalne amauroze (LCA).
23. Upotreba iz patentnog zahtjeva 17 ili 18, naznačena time, da se upotrebljava za liječenje makularne degeneracije povezane sa starenjem.
24. Upotreba iz patentnog zahtjeva 17 ili 18, naznačena time, da se upotrebljava za zadovoljavanje potrebe za endogenim 11-cis-retinalom kod navedenog ljudskog subjekta.
25. Upotreba iz patentnog zahtjeva 17 ili 18 za liječenje gubitka noćnog vida ili gubitka kontrastne osjetljivosti, naznačen time, da je navedeni ljudski subjekt ljudski subjekt starije dobi.
26. Upotreba iz bilo kojeg patentnog zahtjeva 17 do 25, naznačena time, da je retinil ester 9-cis-retinil acetate.
27. Upotreba iz bilo kojeg patentnog zahtjeva 17 do 25, naznačena time, da esterski supstituent sadržava karboksilatni radikal C2-C22 polikarboksilne kiseline.
28. Upotreba iz patentnog zahtjeva 27, naznačena time, da je esterski supstituent odabran iz skupine koju čine sukcinat, citrat, ketoglutarat, fumarat, malat i oksaloacetat.
29. Upotreba iz bilo kojeg patentnog zahtjeva 17 do 25, naznačena time, da je ester 9-cis-retinil ester C1-C10 monokarboksilata.
30. Upotreba iz bilo kojeg patentnog zahtjeva 17 do 29, naznačena time, da je lijek farmaceutski pripravak.
31. Upotreba iz patentnog zahtjeva 26, naznačena time, da je lijek namijenjen za lokalnu primjenu na oku.
32. Upotreba iz patentnog zahtjeva 26, naznačena time, da je lijek namijenjen za lokalnu primjenu u obliku kapljica za oči, u obliku intraokularne injektibilne otopine ili u obliku periokularne injektibilne otopine.
33. Upotreba iz patentnog zahtjeva 26, naznačena time, da je lijek namijenjen za peroralnu primjenu kod subjekta.
34. Upotreba iz patentnog zahtjeva 25, naznačena time, da je lijek namijenjen za profilaktičku primjenu kod subjekta.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US58088904P | 2004-06-18 | 2004-06-18 | |
PCT/US2005/021812 WO2006002097A2 (en) | 2004-06-18 | 2005-06-20 | Retinal derivatives and methods for the use thereof for the treatment of visual disorders |
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HRP20140116T1 true HRP20140116T1 (hr) | 2014-03-28 |
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HRP20140116TT HRP20140116T1 (hr) | 2004-06-18 | 2014-02-06 | Derivati retinala i postupci za njihovu upotrebu u lijeäśenju poremeä†aja vida |
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US (8) | US7951841B2 (hr) |
EP (5) | EP2397130B1 (hr) |
JP (2) | JP5166026B2 (hr) |
KR (4) | KR101490145B1 (hr) |
CN (2) | CN1988898B (hr) |
AU (1) | AU2005257997B2 (hr) |
BR (1) | BRPI0511396B1 (hr) |
CA (2) | CA2571049C (hr) |
CY (2) | CY1114873T1 (hr) |
DK (2) | DK2397133T3 (hr) |
ES (4) | ES2644981T3 (hr) |
HK (1) | HK1098696A1 (hr) |
HR (1) | HRP20140116T1 (hr) |
HU (1) | HUE036596T2 (hr) |
IL (4) | IL180078A (hr) |
IN (1) | IN2012DN09335A (hr) |
LT (1) | LT2397133T (hr) |
MX (2) | MX359668B (hr) |
NO (1) | NO339969B1 (hr) |
NZ (2) | NZ552080A (hr) |
PL (2) | PL1765322T3 (hr) |
PT (2) | PT1765322E (hr) |
RS (1) | RS53178B (hr) |
RU (2) | RU2408578C2 (hr) |
SI (2) | SI1765322T1 (hr) |
WO (1) | WO2006002097A2 (hr) |
ZA (1) | ZA200700368B (hr) |
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