DK2089417T3 - Fremgangsmåder, forbindelser, sammensætninger og vehikler til afgivelse af 3-amion-1-propansulfonsyre - Google Patents

Fremgangsmåder, forbindelser, sammensætninger og vehikler til afgivelse af 3-amion-1-propansulfonsyre Download PDF

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DK2089417T3
DK2089417T3 DK07875176.5T DK07875176T DK2089417T3 DK 2089417 T3 DK2089417 T3 DK 2089417T3 DK 07875176 T DK07875176 T DK 07875176T DK 2089417 T3 DK2089417 T3 DK 2089417T3
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compound
3aps
compounds
acid
disease
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DK07875176.5T
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Xianqi Kong
Mohamed Atfani
Benoit Bachand
Abderrahim Bouzide
Stephane Ciblat
Sophie Levesque
David Migneault
Xinfu Wu
Daniel Delorme
Isabelle Valade
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Bhi Ltd Partnership
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    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/13—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
    • C07C309/14—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton containing amino groups bound to the carbon skeleton
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Claims (15)

1. Forbindelse med formlen IV eller et farmaceutisk acceptabelt salt eller solvat deraf:
(IV) hvor: aa1 er en naturlig eller ikke-naturlig aminosyrerest; aa2 er en naturlig eller ikke-naturlig aminosyrerest eller er fraværende; hvor aa1 og aa2, begge uafhængigt af hinanden, er aminosyrerester med formlen VI:
(VI) hvor: R1 er udvalgt fra gruppen bestående af en substitueret eller ikke-substitueret gruppe udvalgt fra Ci-C^alkyl, C2-Ci2alkenyl, C2-Ci2alkynyl, C3-Ci5cycloalkyl; R2 er hydrogen R3 er hydrogen; eller R3 er en binding mellem to aminosyrerester, når to aminosyrerester er til stede; R4 er udvalgt fra gruppen bestående af H og en substitueret eller ikke-substitueret gruppe udvalgt fra Ci-C5alkyl, C2-C5alkenyl, C2-C5alkynyl; og n er 1, 2 eller 3; hvor begrebet substitueret, når det er forbundet med en hvilken som hlest af de foregående grupper, henviser til en gruppe, der er substitueret ved én eller flere positioner med substituenter, der er udvalgt fra amino, der er udvalgt fra enkel amino, mono og dial-kylamino, mono- og diarylamino, og alkylarylamino, acylamino, indbefattende carbamoyl, og ureido, aminocarbonyl, mono- og dialkylaminocarbonyl, cyano, azido, halogen, hydroxyl, nitro, trifluormethyl, Ci-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, cycloalkyl, heterocycloal-kyl, aryl, heteroaryl, Ci-C6alkoxy, aryloxy, benzyloxy, benzyl, guanidin, imino, og formyl; forudsat, at når R2 er H og R3 er H eller en binding, så er R1 ikke en —CH2-phenylgruppe.
2. Forbindelse ifølge krav 1, hvor forbindelsen er en forbindelse med formlen V eller et farmaceutisk acceptabelt salt eller solvat deraf:
(V) hvor: aa1 er en naturlig eller ikke-naturlig aminosyre som defineret i krav 1.
3. Forbindelse ifølge krav 2, hvor aa1 er udvalgt fra aminosyrerester af valin, lysin, leucin, serin, alanin, isoleucin, histidin og O-benzylserin.
4. Forbindelse ifølge krav 1 eller 2, hvor forbindelsen er udvalgt fra gruppen bestående af:
eller et farmaceutisk acceptabelt salt eller solvat deraf.
5. Forbindelse ifølge krav 4, hvor forbindelsen er udvalgt fra:
og farmaceutisk acceptabelt salt eller solvater deraf.
6. Forbindelse ifølge krav 5, hvor forbindelsen er:
eller et farmaceutisk acceptabelt salt eller solvat deraf.
7. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 1 til 6 sammen med et farmaceutisk acceptabelt bærestof.
8. Prodrug af 3-amino-l-propansulfonsyre, hvor prodrug'en er en forbindelse ifølge et hvilket som helst af kravene 1 til 6.
9. Forbindelse ifølge et hvilket som helst af kravene 1 til 6 til anvendelse ved behandling eller forebyggelse af en sygdom eller tilstand, der er udvalgt fra Alzheimers sygdom, mild kognitiv nedsættelse, Downs syndrom, Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-Type, cerebral amyloid angiopati, Parkinsons sygdom, en degenerativ demens, en demens af blandet vaskulær og degenerativ oprindelse, demens forbundet med Parkinsons sygdom, demens forbundet med progressiv supranuklear lammelse, demens forbundet med kortikal basal degeneration eller diffus Lewy body-type af Alzheimers sygdom.
10. Forbindelse til anvendelse ifølge krav 9, hvor sygdommen eller tilstanden er udvalgt fra Alzheimers sygdom, mild kognitiv nedsættelse, cerebral amyloid angiopati og degenerativ demens.
11. Forbindelse til anvendelse ifølge krav 10, hvor sygdommen eller tilstanden er Alzheimers sygdom.
12. Forbindelse ifølge et hvilket som helst af kravene 1 til 6 til anvendelse ved tilvejebringelse af neurobeskyttelse til et individ med en amyloid-p-relateret sygdom.
13. Forbindelse ifølge et hvilket som helst af kravene 1 til 5 til anvendelse ved afgivelse af 3-amino-l-propansulfonsyre (3APS) ved etablering af kontakt mellem forbindelsen og et enzym, der metaboliserer forbindelsen til 3APS In vitro eller In vivo.
14. Forbindelse ifølge krav 13, hvor 3APS afgives, når forbindelsen bringes i kontakt med plasma, blod og/eller hjerneceller.
15. Forbindelse ifølge et hvilket som helst af kravene 1 til 5 til anvendelse ved hæmning af nervecelledød.
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