DK2521447T3 - Fedtsyrefumarater og deres anvendelser - Google Patents

Fedtsyrefumarater og deres anvendelser Download PDF

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Publication number
DK2521447T3
DK2521447T3 DK11732212.3T DK11732212T DK2521447T3 DK 2521447 T3 DK2521447 T3 DK 2521447T3 DK 11732212 T DK11732212 T DK 11732212T DK 2521447 T3 DK2521447 T3 DK 2521447T3
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oxobut
docosa
enamido
methyl
enoate
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DK11732212.3T
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English (en)
Inventor
Chi B Vu
Jean E Bemis
Michael R Jirousek
Jill C Milne
Jesse J Smith
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Catabasis Pharmaceuticals Inc
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    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/76—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
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Claims (19)

1. Forbindelse, der har formlen IA, IB, eller IC:
IC eller et farmaceutisk acceptabelt salt, hydrat, solvat, en enantiomer eller en stereoisomer deraf; hvori hvert \N<\ og W2 er uafhængigt nul, O, S, NH eller NR, eller \N^ og W2 kan tages sammen for at danne en eventuelt substitueret imidazolidin- eller piperazin-gruppe; hvert a, b, c og d er uafhængigt -H, -D, -CH3, -OCH3, -OCH2CH3, -C(0)-0R eller benzyl, eller to af a, b, c og d kan tages sammen med det enkelte carbon, hvortil de er bundet, for at danne en cycloalkyl eller heterocyklisk gruppe; hvert n, o, p og q er uafhængigt 0, 1 eller 2; hvert L er uafhængigt nul, -O-, -C(O)-, -S-, -S(O)-, -S(0)2-, -S-S-, -(CrCe-alkyl)-, -(C3-C6-cycloalkyl)-, en heterocyklisk gruppe, en heteroaryl,
hvor repræsentationen af L ikke er begrænset retningsbestemt fra venstre mod højre som vist, snarere kan enten venstre side eller højre side af L være bundet til Wrsiden af forbindelsen af formel IA, IB, eller IC; hvert R6 er uafhængigt -H, -D, -CrC4-alkyl, halogen, cyano, oxo, thiooxo, -OH, -C(0)CrC4-alkyl, -O-aryl, -O-benzyl, -0C(0)Ci-C4-alkyl, -C2-C3-alken, -C2-C3-alkyn, -NH2, -NH(CrC3-alkyl), -N(CrC3-alkyl)2, -NH-(C(0)CrC3-alkyl), -N(C(0)CrC3-alkyl)2, -SH, -S (CrC3-alkyl), -S(O) CrC3-alkyl eller -S(0)2CrC3-alkyl; hvert g er uafhængigt 2, 3 eller 4; hvert h er uafhængigt 1,2,3 eller 4; hvert m er uafhængigt 0, 1, 2 eller 3; hvis m er mere end 1, så kan L være ens eller forskellige; hvert ith er uafhængigt 0, 1, 2 eller 3; k er 0, 1,2 eller 3; z er 1, 2 eller 3; hvert R4 er uafhængigt H eller eventuelt substitueret CrC6-alkyl, hvor en methylen-enhed af CrC6-alkyl kan eventuelt være substitueret for enten O eller NR og i NR4R4, begge R4, når de sammen med nitrogenet, hvortil de er bundet, kan danne en heterocyklisk ring, der er valgt fra gruppen bestående af pyrrolidin, piperidin, morpholin, piperazin og pyrrol; hvert R3 er uafhængigt H eller -CrC6-alkyl; hvert R5 er uafhængigt e, H eller ligekædet eller forgrenet CrC^-alkyl, der eventuelt kan være substitueret med OH, NH2, C02R, CONH2, phenyl, C6H4OH, imidazol eller arginin; hvert e er uafhængigt H eller en hvilken som helst af sidekæderne af de naturligt forekommende aminosyrer; hvert R er uafhængigt -H, -CrCs-alkyl eller ligekædet eller forgrenet Ci-C4-alkyl, der eventuelt er substitueret med OH eller halogen.
2. Forbindelsen ifølge krav 1, hvor forbindelsen er af formel IA:
3. Forbindelsen ifølge krav 1, hvor forbindelsen er af Formel IB:
4. Forbindelsen ifølge krav 1, hvor forbindelsen er af Formel IC:
5. Forbindelse ifølge krav 1,2, 3 eller 4, hvor W^ og W2 er hver NH.
6. Forbindelse ifølge krav 1, 2, 3 eller 4, hvor mindst to af n, o, p og q hver især er 1.
7. Forbindelse ifølge krav 1,2,3 eller 4, hvor to af n, o, p og q hver især er 1, og de to andre er hver 0.
8. Forbindelse ifølge krav 1,2, 3 eller 4, hvor m er 0.
9. Forbindelse ifølge krav 1,2,3 eller 4, hvor m er 1.
10. Forbindelse ifølge krav 1, 2, 3 eller 4, hvor L er valgt fra gruppen, der består af -O-, -N(R4)-,
11. Forbindelse ifølge Krav 1,2, 3 eller 4, hvor R3 er CFI3.
12. Forbindelse ifølge krav 1,2, 3 eller 4, hvor Wi og W2 er hver NH, m er 0, n og o er hver 1, og p og q er hver 0.
13. Forbindelse ifølge krav 1, hvor forbindelsen er valgt fra gruppen, der består af: (E)-methyl-4-(2-(4Z,7Z, 10Z, 13Z, 16Z, 19Z)-docosa-4,7,10,13,16,19-hexaenamidoethylamino)-4-oxobut-2-enoat (1-1), (E)-methyl-4-(2-(5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamidoethylamino)-4-oxobut-2-enoat (I-2), (E)-methyl-4-(2-(2-(4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamidoethoxy)ethylamino)-4-oxobut-2-enoat (I-3), (S)-6-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamido)-2-((E)-4-methoxy-40xobut-2-enamido)hexansyre (I-7), (S)-6-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamido)-2-((E)-4- methoxy-4-oxo-but-2-amido)hexansyre (1-71), (S)-1,3-dihydroxypropan-2-yl-6-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa- 4,7,10,13,16,19-hexaenamido)-2-(E)-4-methoxy-4-oxo-but-2-enannido)hexanoat (I-8), (S)-1,3-dihydroxypropan-2-yl-6-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamido)-2-((E)-4-methoxy-4-oxo-but-2-enamido)hexanoat (I-96), (S)-2-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamido)-6-((E)-4-methoxy-40xobut-2-enamido)hexansyre (1-10), (S)-2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamido)-6-((E)-4-methoxy-4-oxo-but-2-amido)hexansyre (I-72), (S)-1,3-dihydroxypropan-2-yl-2-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa- 4.7.10.13.16.19- hexaenamido)-6-(E)-4-methoxy-4-oxo-but-2-enamido)hexanoat (1-11), (S)-1,3-dihydroxypropan-2-yl-2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamido)-6-((E)-4-methoxy-4-oxo-but-2-enamido)hexanoat (1-97), (E)-methyl-4-(2-(2-(4Z,7Z, 10Z, 13Z, 16Z, 19Z)-docosa-4,7,10,13,16,19-hexaenamidoethylamino)ethylannino)-4-oxobut-2-enoat (I-24), (E)-methyl-4-(2-(2-(5Z,8Z, 11Z, 14Z, 17Z)-icosa-5,8,11,14,17-pentaenamidoethylamino)ethylannino)-4-oxobut-2-enoat (I-73), (E)-methyl-4-(2-((2-(4Z,7Z, 10Z, 13Z, 16Z, 19Z)-docosa-4,7,10,13,16,19-hexaenamidoethyl)(methyl)amino)ethylannino)-4-oxobut-2-enoat (I-4), (E)-methyl-4-(2-((2-(5Z,8Z,11Z, 14Z, 17Z)-icosa-5,8,11,14,17-pentaenamidoethyl)(methyl)amino)ethylannino)-4-oxobut-2-enoat (I-74), (S)-5-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamido)-2-((E)-4-methoxy-40xobut-2-enamido)pentansyre (I-80), (S)-2-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamido)-5-((E)-4-methoxy-40xobut-2-enamido)pentansyre (1-81), (S)-1,3-dihydroxypropan-2-yl-5-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa- 4.7.10.13.16.19- hexaenamido)-2-(E)-4-methoxy-4-oxo-but-2-enamido)pentanoat (I-82), (S)-1,3-dihydroxypropan-2-yl-2-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa- 4.7.10.13.16.19- hexaenamido)-5-((E)-4-methoxy-4-oxo-but-2-enamido)pentanoat (I-83); (S)-5-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamido)-2-((E)-4-methoxy-4-oxo-but-2-amido)pentansyre (I-84), (S)-2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamido)-5-((E)-4-methoxy-4-oxo-but-2-amido)pentansyre (I-85), (S)-1,3-dihydroxypropan-2-yl-5-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamido)-2-((E)-4-methoxy-4-oxo-but-2-enamido)pentanoat (I-86), (S)-1,3-dihydroxypropan-2-yl-2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamido)-5-((E)-4-methoxy-4-oxo-but-2-enamido)pentanoat (I-87), (E)-ethyl-4-(2-(4Z,7Z, 10Z, 13Z, 16Z, 19Z)-docosa-4,7,10,13,16,19-hexaenamidoethylamino)-4-oxobut-2-enoat (I-66), (E)-ethyl-4-(2-(5Z,8Z, 11Z, 14Z, 17Z)-icosa-5,8,11,14,17-pentaenamidoethylamino)-4-oxobut-2-enoat (I-75), (S)-6-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamido)-2-((E)-4-ethoxy-4-oxobut-2-enamido)hexansyre (I-69), (S)-2-((E)-4-ethoxy-4-oxobut-2-enamido)-6-((5Z,8Z,11 Z,14Z,17Z)-icosa- 5.8.11.14.17- pentaenamido)hexansyre (I-76), (S)-1,3-dihydroxypropan-2-yl-6-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa- 4.7.10.13.16.19- hexaenamido)-2-(E)-4-ethoxy-4-oxobut-2-enamido)hexanoat (I-98), (S)-1,3-dihydroxypropan-2-yl-2-((E)-4-ethoxy-4-oxobut-2-enamido)-6-((5Z,8Z,11 Z,14Z,17Z)5,8,11,14,17-pentaenamido)hexanoat (I-99), (S)-2-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamido)-6-((E)-4-ethoxy-40xobut-2-enamido)hexansyre (I-70), (S)-6-((E)-4-ethoxy-4-oxobut-2-enamido)-2-((5Z,8Z,11 Z,14Z,17Z)-icosa- 5.8.11.14.17- pentaenamido)hexansyre (I-77), (S)-1,3-dihydroxypropan-2-yl-2-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa- 4.7.10.13.16.19- hexaenamido)-6-(E)-4-ethoxy-4-oxobut-2-enamido)hexanoat (I- 100), (S)-1,3-dihydroxypropan-2-yl-6-((E)-4-ethoxy-4-oxobut-2-enamido)-2-((5Z,8Z,11 Z,14Z,17Z)5,8,11,14,17-pentaenamido)hexanoat (1-101), (E)-ethyl-4-(2-(2-(4Z,7Z, 10Z, 13Z, 16Z, 19Z)-docosa-4,7,10,13,16,19-hexaenamidoethylamino)ethylannino)-4-oxobut-2-enoat (I-68), (E)-ethyl-4-(2-(2-(5Z,8Z, 11Z, 14Z, 17Z)-icosa-5,8,11,14,17-pentaenamidoethylamino)ethylannino)-4-oxobut-2-enoat (I-79), (E)-ethyl-4-(2-((2-(4Z,7Z, 10Z, 13Z, 16Z, 19Z)-docosa-4,7,10,13,16,19-hexaenamidoethyl)(methyl)annino)ethylannino)-4-oxobut-2-enoat (I-67), (E)-ethyl-4-(2-((2-(5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenamidoethyl)(methyl)annino)ethylannino)-4-oxobut-2-enoat (I-78), (S)-5-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamido)-2-((E)-4-ethoxy-40xobut-2-enamido)pentansyre (I-88), (S)-2-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenamido)-5-((E)-4-ethoxy-40xobut-2-enamido)pentansyre (I-89), (S)-1,3-dihydroxypropan-2-yl-5-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa- 4.7.10.13.16.19- hexaenamido)-2-(E)-4-ethoxy-4-oxobut-2-enannido)pentanoat (I-90), (S)-1,3-dihydroxypropan-2-yl-2-((4Z,7Z,10Z,13Z,16Z,19Z)-docosa- 4.7.10.13.16.19- hexaenamido)-5-((E)-4-ethoxy-4-oxobut-2-enamido)pentanoat (1-91), (S)-2-((E)-4-ethoxy-4-oxobut-2-enamido)-5-((5Z,8Z,11 Z,14Z,17Z)-icosa- 5.8.11.14.17- pentaenamido)pentansyre (I-92), (S)-5-((E)-4-ethoxy-4-oxobut-2-enamido)-2-((5Z,8Z,11 Z,14Z,17Z)-icosa- 5.8.11.14.17- pentaenamido)pentansyre (I-93), (S)-1,3-dihydroxypropan-2-yl-2-((E)-4-ethoxy-4-oxobut-2-enamido)-5-((5Z,8Z,11Z,14Z,17Z)5,8,11,14,17-pentaenamido)pentanoat (I-94), og (S)-1,3-dihydroxypropan-2-yl-5-((E)-4-ethoxy-4-oxobut-2-enamido)-2-((5Z,8Z,11 Z,14Z,17Z)5,8,11,14,17-pentaenamido)pentanoat (I-95).
14. Forbindelse ifølge krav 1 eller 2, hvor forbindelsen er
(E)-methyl-4-(2-(4Z,7Z, 10Z, 13Z, 16Z, 19Z)-docosa-4,7,10,13,16,19-hexaenamidoethylamino)-4-oxobut-2-enoat (1-1).
15. Farmaceutisk sammensætning, der omfatter en forbindelse ifølge et hvilket som helst af kravene 1-14 og en farmaceutisk acceptabel bærer.
16. Forbindelse ifølge et hvilket som helst af kravene 1-14 eller en farmaceutisk sammensætning ifølge krav 15 til anvendelse til behandling afen neurodegenerativ sygdom, en inflammation eller en inflammatorisk sygdom.
17. Forbindelse eller farmaceutisk sammensætning til anvendelse ifølge krav 16, hvor den inflammatoriske sygdom er forbundet med en metabolisk lidelse, der er valgt fra gruppen, der består af type-ll-diabetes, insulinresistens, kardiovaskulær sygdom, arytmi, aterosklerose, koronararteriesygdom, hypertriglyceridæmi, dyslipidæmi, retinopati, neuropati, makulært ødem, diabetisk nefropati, IgA-nefropati, kronisk nyresygdom (CKD), inflammatoriske sygdomme i nyrerne inklusive uremiske komplikationer, glomerulonefritis og nefrose.
18. Forbindelse eller farmaceutisk sammensætning til anvendelse ifølge krav 16, hvor den inflammatoriske sygdom er cystisk fibrose, astma, sclerodermatitis, psoriasis, arthritis, reumatoid arthritis, inflammatorisk tarmsygdom, ileitis, ulcerøs colitis, Barrett's syndrom, Crohns sygdom eller eksem, og den neurodegenerativ sygdom er multipel sklerose, Parkinsons sygdom, Fluntingtons sygdom, amyotrofisk lateralsklerose (ALS) eller Alzheimers sygdom.
19. Forbindelse ifølge et hvilket som helst af kravene 1-14 eller en farmaceutisk sammensætning ifølge krav 15 til anvendelse ved behandling af Duchennes muskeldystrofi.
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