DK2442644T3 - Opsin-bindende ligander, sammensætninger og fremgangsmåder til anvendelse - Google Patents
Opsin-bindende ligander, sammensætninger og fremgangsmåder til anvendelse Download PDFInfo
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- DK2442644T3 DK2442644T3 DK10789866.0T DK10789866T DK2442644T3 DK 2442644 T3 DK2442644 T3 DK 2442644T3 DK 10789866 T DK10789866 T DK 10789866T DK 2442644 T3 DK2442644 T3 DK 2442644T3
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- compound
- trimethylcyclohex
- opsin
- acryloyl
- enyl
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Claims (12)
1. Forbindelse med strukturen med formel I A-B-Q-V Formel I hvor A er:
B er -CH=CH-, -CH2-N(R22)- eller -CH2-CH2-, Q er -C(O)- eller -CH2-; V er
hvor b er 1 eller 2 og a er 1 eller 2; Y er NR22, N-Q-U, CR22R23, oxygen, S(0)„, N-C(S)-NR22R23; N-(C=N-CN)-NR22R23, N-(C=N-S02CH3)-NR22R23, C=NOR22, C=N-NR22R23 eller C-Q-U, n er 0, 1 eller 2; U er NR22R23, lavere alkyl, haloalkyl, OR22 eller hydrogen; X er hydrogen, alkyl eller -C^CR9; W er -OR22, -NR22R23, -N(R22)-C(0)-NR22R23, -0-C(0)-NR22R23, -N(R22)-C(S)-NR22R23, -0-C(S)-NR22R23, -S-C(0)-NR22R23, -N(R22)-(C=N-CN)-NR22R23, -N(R22)-(C=N-S02Me)-NR22R23, eller -C(0)N(R9)N(R14)(R16); hvor p er 0 eller 1; R14 og R16 er hver uafhængigt hydrogen, eller -CH3; R1 og R2 er uafhængigt -CHs eller -CH2CH3; R3 er hydrogen, -CH3 eller -CH2CH3; Ra, og Rb, er hver uafhængigt hydrogen, deutero eller -CH3; Rc, og Rd, er hver uafhængigt hydrogen, alkoxy, lavere alkyl eller alkenyl; R9 er hydrogen, eller -CH3; R22 og R23 er hver uafhængigt hydrogen; eller lavere alkyl; R24 og R25 er hver uafhængigt hydrogen eller -CH3; R26 er NR22R23 eller alkoxy; og hvor R1 og R2 taget sammen eller Ra og Rb taget sammen med det carbonatom til hvilket de er bundet er cyclopropyl; R24 og R25 taget sammen med det carbonatom til hvilket de er bundet er cyclopropyl: R24 og R25 taget sammen er oxo; herunder farmaceutisk acceptable salte, solvater og hydrater deraf; og hvor lavere alkyl er er en forgrenet eller ligekædet acyklisk alkylgruppe omfattende et til ti carbonatomer; haloalkyl er en lavere alkylgruppe, en alkenylgruppe, en alkynylgruppe, en brodannet cycloalkylgruppe, en cycloalkylgruppe til hvilke er vedhæftet én eller flere halogener; alkoxy er R50O-, hvor Rso er en alkylgruppe; alkyl er en ubrudt ikke-cyklisk kæde af carbonatomer der kan være forgrenede, uforgrenede, substituerede eller andre kemiske grupper såsom lavere alkyl, hydroxyl, ester, amidyl, oxo, carboxyl, carboxamido, halo, cyano, nitrat, nitrit, thionitrat, thionitrit, sulfhydryl og amino, eller usubstituerede; alkenyl er et forgrenet eller ligekædet C2-C10 carbonhydrid der kan omfatte én eller flere carbon-carbon-dobbeltbindinger; alkynyl er et umættet acyklisk C2-C10 carbonhydrid der kan indeholde én eller flere carbon-carbon-tredobbelte bindinger; cycloalkyl er er et mættet eller umættet cyklisk carbonhydrid omfattende fra 3 til 10 carbonatomer; heterocyklisk ring er en mættet eller umættet cyklisk eller polycyklisk carbonhydridgruppe med 2 til 12 carbonatomer hvor 1 til 4 carbonatomer er erstattet af ét eller flere nitrogen-, oxygen- og/eller svovlatomer.
2. Forbindelsen ifølge krav 1, hvor hver af R1, R2 og R3 er methyl, eller hvor hver af R24 er hydrogen, eller hvor Ra og Rb er hver uafhængigt hydrogen eller methyl, eller hvor Ra og Rb hver er methyl, eller hvor Rc og Rd hver er uafhængigt hydrogen eller lavere alkyl, eller hvor Rc og Rd hver er lavere alkyl eller hvor Rc og Rd hver er hydrogen; og hvor V er:
og hvor lavere alkyl er defineret i krav 1.
3. Forbindelsen ifølge krav 1, hvor V er:
eller hvor B er CH = CH, eller hvor Q er -C(O)-, eller hvor X er H, eller lavere alkyl eller -C=CR9, eller hvor X er H eller methyl, eller hvor Y er O eller N-C(0)-NR22R23; og hvor lavere alkyl er som defineret i krav 1.
4. Forbindelsen ifølge krav 1, hvor V er
og hvor Ra og Rb er hver uafhængigt hydrogen, deutero eller methyl, eller hvor Ra eller Rb hver er hydrogen, eller hvor Rc og Rd er hver uafhængigt hydrogen, alkoxy eller lavere alkyl, og hvor alkoxy og lavere alkyl er som defineret i krav 1.
5. Forbindelse ifølge krav 1, med strukturen
(E)-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)piperazin-l-carboxamid (forbindelse 33);
(S/E)-2-methyl-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)piperazin-l-carboxamid (forbindelse 52);
(E)-4-(3-(3,3-dideutero-2,6,6-trimethylcyclohex-l-en-l-yl)acryloyl)piperazin-l-carboxamid (forbindelse 63);
(±)-4-((E)-3-((l,6-ant/')-2,2,6-trimethylcyclohexyl)acryloyl)piperazin-l-carboxamid (forbindelse 71);
(-)-4-((E)-3-((lR, 6R)-2,2,6-trimethylcyclohexyl)acryloyl)piperazin-l-carboxamid (forbindelse 72);
(+)-4-((5)-3-((lS,6S)-2,2,6-trimethylcyclohexyl)acryloyl)piperazin-l-carboxamid (forbindelse 73); eller
4-(3-(( IR, 6S)-2,2,6-trimethylcyclohexyl)propanoyl)piperazin-l-carboxamid (forbindelse 80); herunder farmaceutisk acceptable salte, solvater og hydrater deraf.
6. Forbindelse ifølge krav 1, med strukturen
(E)-l-morpholino-3-(2,6,6-trimethylcyclohex-l-enyl)prop-2-en-l-on (forbindelse 6);
(E)-l-(l-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl) pyrrolidin-3-yl)urinstof (forbindelse 50); eller
(E)-2-ethynyl-4-(3-(2,6,6-trimethylcyclohex-l-en-l-yl)acryloyl)piperazin-l-carboxamid (forbindelse 106); herunder farmaceutisk acceptable salte, solvater og hydrater deraf. 7
7. Forbindelse ifølge krav 1, med strukturen
(E)-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)-l,4-diazepan-l-carboxamid (forbindelse 13);
(E)-/V-isopropyl-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)piperazin-l-carboxamid (forbindelse 37);
(R,E)-2-methyl-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)piperazin-l-carboxamid (forbindelse 53); eller
A/J-((2,6,6-trimethylcyclohex-l-en-l-yl)methyl)piperazin-l ,4-dicarboxamid (forbindelse 55); herunder farmaceutisk acceptable salte, solvater og hydrater deraf.
8. Sammensætning til anvendelse i inhibering af dannelsen eller akkumulering af en toksisk visuel cyklusprodukttilstand i et individ med risiko derfor eller afficeret dermed, omfattende en effektiv mængde af forbindelse ifølge krav 1, 5, 6 eller 7.
9. Sammensætningen til anvendelse ifølge krav 8, hvor inhiberingen foregår i en celle.
10. Sammensætningen til anvendelse ifølge krav 8, hvor det visuelle cyklusprodukt er lipofuscin eller N-retinyliden-N-retinylethanolamin (A2E).
11. Sammensætning til anvendelse i behandling eller forebyggelse af en ophthalmisk tilstand i et individ med risiko derfor eller afficeret dermed, omfattende en effektiv mængde afen forbindelse ifølge krav 1, 5, 6 eller 7.
12. Sammensætningen til anvendelse ifølge krav 11, hvor den ophthalmiske tilstand er valgt fra gruppen bestående af våd- eller tør-alders-relateret makulær degeneration (ARMD), retinitis pigmentosa (RP), en retinal- eller makulær dystrofi, Stargardt's sygdom, Sorsby's dystrofi, autosomal dominant drusen, Best's dystrofi, peripherin mutation associeret med makulær dystrofi, dominant form af Stargart's sygdom, North Carolina makulær dystrofi, let toksicitet, normal synstabs-relateret aldring og normal tab af nattesyn relateret til aldring.
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Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US26875709P | 2009-06-16 | 2009-06-16 | |
PCT/US2010/001739 WO2010147653A1 (en) | 2009-06-16 | 2010-06-16 | Opsin-binding ligands, compositions and methods of use |
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DK10789866.0T DK2442644T3 (da) | 2009-06-16 | 2010-06-16 | Opsin-bindende ligander, sammensætninger og fremgangsmåder til anvendelse |
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EP (2) | EP2442644B1 (da) |
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CN (1) | CN102480943A (da) |
AU (1) | AU2010260535B2 (da) |
CA (1) | CA2767895C (da) |
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EA (1) | EA021747B1 (da) |
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HR (1) | HRP20161477T1 (da) |
HU (1) | HUE031705T2 (da) |
IN (1) | IN2012DN00352A (da) |
LT (1) | LT2442644T (da) |
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PT (1) | PT2442644T (da) |
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SM (1) | SMT201600388B (da) |
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CA2767895A1 (en) | 2010-12-23 |
ZA201200226B (en) | 2013-06-26 |
EP2442644B1 (en) | 2016-08-10 |
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ES2610429T3 (es) | 2017-04-27 |
CA2767895C (en) | 2017-12-12 |
HUE031705T2 (en) | 2017-07-28 |
PL2442644T3 (pl) | 2017-02-28 |
KR20180099944A (ko) | 2018-09-05 |
HRP20161477T1 (hr) | 2016-12-16 |
US20170037018A1 (en) | 2017-02-09 |
EP2442644A4 (en) | 2013-05-22 |
KR101726358B1 (ko) | 2017-04-26 |
IN2012DN00352A (da) | 2015-08-21 |
CN102480943A (zh) | 2012-05-30 |
EP2442644A1 (en) | 2012-04-25 |
SI2442644T1 (sl) | 2017-01-31 |
WO2010147653A1 (en) | 2010-12-23 |
EP3100723A1 (en) | 2016-12-07 |
EA201270018A1 (ru) | 2012-07-30 |
CY1118221T1 (el) | 2017-06-28 |
KR101921288B1 (ko) | 2018-11-22 |
SMT201600388B (it) | 2017-03-08 |
PT2442644T (pt) | 2016-11-09 |
EP3100723B1 (en) | 2019-06-12 |
KR20170041282A (ko) | 2017-04-14 |
US20110003784A1 (en) | 2011-01-06 |
AU2010260535B2 (en) | 2015-08-20 |
LT2442644T (lt) | 2016-12-12 |
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