DK2807183T3 - Syntetiske apelin-mimetika til behandlingen af hjerteinsufficiens - Google Patents

Syntetiske apelin-mimetika til behandlingen af hjerteinsufficiens Download PDF

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DK2807183T3
DK2807183T3 DK13711953.3T DK13711953T DK2807183T3 DK 2807183 T3 DK2807183 T3 DK 2807183T3 DK 13711953 T DK13711953 T DK 13711953T DK 2807183 T3 DK2807183 T3 DK 2807183T3
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nle
polypeptide
rprlc
salt
amide
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Andrei Golosov
Philipp Grosche
Qi-Ying Hu
Hidetomo Imase
David Thomas Parker
Kayo Yasoshima
Frédéric Zecri
Hongjuan Zhao
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Novartis Ag
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    • A61M16/00—Devices for influencing the respiratory system of patients by gas treatment, e.g. ventilators; Tracheal tubes
    • A61M16/08—Bellows; Connecting tubes ; Water traps; Patient circuits
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
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    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
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    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C07K7/60—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation occurring through the 4-amino group of 2,4-diamino-butanoic acid
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    • A61M16/00—Devices for influencing the respiratory system of patients by gas treatment, e.g. ventilators; Tracheal tubes
    • A61M16/0003—Accessories therefor, e.g. sensors, vibrators, negative pressure
    • A61M2016/0027—Accessories therefor, e.g. sensors, vibrators, negative pressure pressure meter
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    • A61M16/00—Devices for influencing the respiratory system of patients by gas treatment, e.g. ventilators; Tracheal tubes
    • A61M16/0003—Accessories therefor, e.g. sensors, vibrators, negative pressure
    • A61M2016/003—Accessories therefor, e.g. sensors, vibrators, negative pressure with a flowmeter
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    • A61M2205/50—General characteristics of the apparatus with microprocessors or computers
    • A61M2205/502—User interfaces, e.g. screens or keyboards

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Claims (20)

1. Polypeptid med følgende formel II:
hvor XI er fraværende, pE, R, Q eller Isn; X5 er L eller Cha; X7 er H, Aib, F, K(Lauroyl) eller K(Palmitoyl); X8 er K, F eller 4-amino-lsn; X9 er G eller Aib; XII er Nle eller Cha; X13 er fraværende eller er F, f, K(Lauroyl), K(Palmitoyl); X6 og X12 er uafhængigt en naturlig eller unaturlig aminosyre valgt blandt C, c, hC, D-hC, hvor sidekæden af X6 og X12 er forbundet indbyrdes via en kovalent binding, under dannelse af et disulfid; og hvor N-terminus og C-terminus eventuelt danner en ring sammen med 1,2, 3 eller 4 glycinaminosyrer; eller en amid, en ester eller et salt af polypeptidet; hvor Nle er L-norleucin; D-hC er D-homocystein; hC er L-homocystein; Aib er a-aminoisosmørsyre; Cha er (S)-3-cyclohexylalanin; Isn er isonipecotinoyl; og pE er L-pyroglutaminsyre.
2. Polypeptid ifølge krav 1 med formlen III:
eller en amid, en ester eller et salt af polypeptidet.
3. Polypeptid ifølge krav 1 med formlen IV:
eller en amid, en ester eller et salt af polypeptidet.
4. Polypeptid ifølge ethvert af kravene 1 til 3 med formlen V:
eller en amid, en ester eller et salt af polypeptidet.
5. Polypeptid ifølge ethvert af kravene 1 til 4, hvor X1 er pE; eller en amid, en ester eller et salt af polypeptidet.
6. Polypeptid ifølge ethvert af kravene 1 til 4, hvor X13 er F; eller en amid, en ester eller et salt af polypeptidet.
7. Polypeptid ifølge ethvert af kravene 1 til 6, hvor X5 er L; eller en amid, en ester eller et salt af polypeptidet.
8. Polypeptid ifølge ethvert af kravene 1 til 7, hvor X7 er H; eller en amid, en ester eller et salt af polypeptidet.
9. Polypeptid ifølge ethvert af kravene 1 til 8, hvor X11 er Nle, eller en amid, en ester eller et salt af polypeptidet.
10. Polypeptid ifølge krav 1, valgt blandt: pE-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, pE-R-P-R-L-C*-Aib-K-G-P-Nle-C*-F-OH, pE-R-P-R-L-C*-Aib-K-G-P-Nle-C*-f-OH, H-lsn-R-P-R-L-C*-Aib-K-G-P-Nle-C*-f-OH, pE-R-P-R-L-C*-H-K-G-P-Nle-C*-phenethylamin, pE-R-P-R-L-C*-H-K-G-P-Nle-C*-f-OH, pE-R-P-R-Cha-C*-H-K-G-P-Cha-C*-F-OH, pE-R-P-R-L-C*-F-K-G-P-Nle-C*-F-OH, /-/-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, /-/-R-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, H-|Sn-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, pE-R-P-R-L-C*-H-F-G-P-Nle-C*-phenethylamin, pE-R-P-R-L-C*-H-K-Aib-P-Nle-C*-F-OH, pE-R-P-R-L-C*-H-(4-NH-lsn)-G-P-Nle-C*-F-0H, pE-R-P-R-L-C*-H-K-G-P-Nle-C*-K(palmitoyl)-OH, pE-R-P-R-L-C*-K(palmitoyl)-K-G-P-Nle-C*-F-OH, palmitoyl-020c-Q-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, lauroyl-020c-Q-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, pE-R-P-R-L-C*-H-K-G-P-Nle-C*-K(lauroyl)-OH, pE-R-P-R-L-C*-K(lauroyl)-K-G-P-Nle-C*-F-OH, pE-R-P-R-L-C*-H-K-G-P-Nle-C*-NH2; pE-R-P-R-L-C*-H-K-G-P-Nle-C*-F-NH2; pE-R-P-R-L-C*-H-K-G-P-Nle-C*-0/-/; pE-R-P-R-L-C*-H-K-G-P-Nle-/7C*-F-0H; pE-R-P-R-L-rtC*-H-K-G-P-Nle-/7C*-F-0H; pE-R-P-R-L-c*-H-K-G-P-Nle-C*-F-OH; pE-R-P-R-L-C*-H-K-G-P-Nle-(D-/7C)*-F-0H; pE-R-P-R-L-(D-hC)*-H-K-G-P-Nle-(D-hC)*-F-OH; myristoyl020c020cQ-R-P-R-L-C*-H-K-G-P-Nle-C*-f-OH; myristoyl020c020c020cQ-R-P-R-L-C*-H-K-G-P-Nle-C*-f-0/-/; myristoyl020c020c020c020cQ-R-P-R-L-C*-H-K-G-P-Nle-C-f-OH; pE-R-P-R-L-C*H-K-G-P-Nle-c*-F-OH; pE-R-P-R-L-c*-H-K-G-P-Nle-c*-F-OH; og pE-R-P-R-L-C*-H-K(Myr)-G-P-Nle-C*-F-OH. hvor de to aminosyrer mærkede med repræsenterer aminosyrerne, som danner et disulfid via deres sidekæde; eller en amid, en ester eller et salt af polypeptidet.
11. Polypeptid ifølge krav 10 valgt blandt: pE-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, pE-R-P-R-L-C*-Aib-K-G-P-Nle-C*-F-OH, pE-R-P-R-L-C*-Aib-K-G-P-Nle-C*-f-OH, H-lsn-R-P-R-L-C*-Aib-K-G-P-Nle-C*-f-OH, pE-R-P-R-L-C*-H-K-G-P-Nle-C*-phenethylamin, pE-R-P-R-L-C*-H-K-G-P-Nle-C*-f-OH, pE-R-P-R-Cha-C*-H-K-G-P-Cha-C*-F-OH, pE-R-P-R-L-C*-F-K-G-P-Nle-C*-F-OH, H-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, H-R-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, H-lsn-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH, og pE-R-P-R-L-C*-H-F-G-P-Nle-C*-phenethylamin; hvor sidekæderne af de to cysteinaminosyrer C* sammen danner en disulfidbinding; eller en amid, en ester eller et salt af polypeptidet.
12. Polypeptid ifølge krav 11, som er pE-R-P-R-L-C*-H-K-G-P-Nle-C*-F-OH; hvor sidekæderne af de to cysteinaminosyrer C* sammen danner en disulfidbinding; eller en amid, en ester eller et salt af polypeptidet.
13. Polypeptid ifølge krav 12 eller et salt af polypeptidet.
14. Polypeptid ifølge krav 12 i acetatsaltform.
15. Polypeptid ifølge ethvert af kravene 1 til 14 til anvendelse som et lægemiddel.
16. Polypeptid ifølge ethvert af kravene 1 til 14 til anvendelse ved behandlingen eller forebyggelsen af en sygdom eller lidelse, som reagerer på agonismen af APJ receptoren.
17. Polypeptid ifølge ethvert af kravene 1 til 14 til anvendelse ved behandlingen af akut dekompenseret hjerteinsufficiens (ADHF), kronisk hjertesvigt, pulmonær hypertension, atrial flimmer, Brugada syndrom, ventrikulær tachycardi, atherosclerose, hypertension, restenose, iskæmisk kardiovaskulær lidelse, kardiomyopati, kardial fibrose, arrhythmi, vandretention, diabetes (inkl. svangerskabsdiabetes), obesitas, perifer arteriel lidelse, cerebrovaskulære tilfælde, transiente iskæmiske anfald, traumatiske hjerneskader, amyotrofisk lateral sclerose, forbrændinger (inkl. solskoldning) eller præeclampsi.
18. Kombination omfattende en terapeutisk effektiv mængde af et polypeptid ifølge ethvert af kravene 1 til 14, og ét eller flere terapeutisk aktive co-agenser.
19. Kombination ifølge krav 18, hvorco-agens er valgt blandt inotroper, beta adrener-ge receptor-blokere, HMG-Co-A-reduktaseinhibitorer, angiotensin II receptor antagonister, angiotensin konverterende enzym (ACE)-inhibitorer, calciumkanalblokere (CCB), endothelin-antagonister, renin-inhibitorer, diuretika, ApoA-l mimetika, anti-diabetiske midler, obesitas-reducerende agenser, aldosteronreceptorblokere, endo-thelinreceptorblokere, aldosteron-syntaseinhibitorer (ASI), en CETP inhibitor, anti-koagulanser, relaxin, BNP (nesiritid) og/eller en NEP-inhibitor.
20. Farmaceutisk sammensætning omfattende en terapeutisk effektiv mængde af et polypeptid ifølge ethvert af kravene 1 til 14 og ét eller flere farmaceutisk acceptable bærestoffer.
DK13711953.3T 2012-01-27 2013-01-25 Syntetiske apelin-mimetika til behandlingen af hjerteinsufficiens DK2807183T3 (da)

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US201261591557P 2012-01-27 2012-01-27
US201261717760P 2012-10-24 2012-10-24
US201261731697P 2012-11-30 2012-11-30
PCT/IB2013/050666 WO2013111110A2 (en) 2012-01-27 2013-01-25 Synthetic apelin mimetics for the treatment of heart failure

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