HRP20100064T1 - Postupci za poboljšanje bioraspoloživosti inhibitora renina - Google Patents

Postupci za poboljšanje bioraspoloživosti inhibitora renina Download PDF

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HRP20100064T1
HRP20100064T1 HR20100064T HRP20100064T HRP20100064T1 HR P20100064 T1 HRP20100064 T1 HR P20100064T1 HR 20100064 T HR20100064 T HR 20100064T HR P20100064 T HRP20100064 T HR P20100064T HR P20100064 T1 HRP20100064 T1 HR P20100064T1
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hydroxy
amino
inhibitor
aryl
alkanoic acid
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P. Camenisch Gian
Gross Gerhard
Ottinger Isabel
Wasmuth Daniel
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Novartis Ag
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    • A61K31/00Medicinal preparations containing organic active ingredients
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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Abstract

Uporaba kombinacije inhibitora renina i inhibitora istjecanja proteina, pri čemu je inhibitor renina derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ili njegova farmaceutski prihvatljiva sol, naznačena time, da se koristi za pripravu lijeka, pri čemu inhibitor istjecanja proteina poboljšava bioraspoloživost inhibitora renina, tepri čemu inhibitor istjecanja proteina je inhibitor MDR1. Patent sadrži još 29 patentnih zahtjeva.

Claims (30)

1. Uporaba kombinacije inhibitora renina i inhibitora istjecanja proteina, pri čemu je inhibitor renina derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ili njegova farmaceutski prihvatljiva sol, naznačena time, da se koristi za pripravu lijeka, pri čemu inhibitor istjecanja proteina poboljšava bioraspoloživost inhibitora renina, te pri čemu inhibitor istjecanja proteina je inhibitor MDR1.
2. Uporaba u skladu sa zahtjevom 1, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ima formulu [image] gdje R1 je C1-4alkoksi-C1-4alkoksi ili C1-4alkoksi-C1-4alkil; R2 je C1-4alkil ili C1-4alkoksi; te R3 i R4 su neovisno razgranati C1-4alkil; ili je njegova farmaceutski prihvatljiva sol.
3. Uporaba u skladu sa zahtjevom 2, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je spoj formule (I) gdje R1 je 3-metoksipropoksi; R2 je metoksi; te R3 i R4 su izopropil; ili je njegova farmaceutski prihvatljiva sol.
4. Uporaba u skladu sa zahtjevom 3, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je (2S, 4S, 5S, 7S)-5-amino-4-hidroksi-2-izopropil-7-[4-metoksi-3-(3-metoksi-propoksi)-benzil]-8-metil-nonanoične kiseline (2-karbamoil-2-metil-propil)-amid hemifumarat.
5. Uporaba u skladu s bilo kojim zahtjevom 1 do 4, naznačena time, da MDR1 inhibitor je PSC833.
6. Uporaba kombinacije inhibitora renina i inhibitora istjecanja proteina, pri čemu inhibitor istjecanja proteina je PSC833, naznačena time, da se koristi pripravu lijeka, pri čemu inhibitor istjecanja proteina poboljšava bioraspoloživost inhibitora renina.
7. Uporaba u skladu sa zahtjevom 6, naznačena time, da inhibitor renina je derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline, ili je njegova farmaceutski prihvatljiva sol.
8. Uporaba u skladu sa zahtjevom 7, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ima formulu [image] gdje R1 je C1-4alkoksi-C1-4alkoksi ili C1-4alkoksi-C1-4alkil; R2 je C1-4alkil ili C1-4alkoksi; te R3 i R4 su neovisno razgranati C1-4alkil; ili je njegova farmaceutski prihvatljiva sol.
9. Uporaba u skladu sa zahtjevom 8, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je spoj formule (I) gdje R1 je 3-metoksipropoksi; R2 je metoksi; te R3 i R4 su izopropil; ili je njegova farmaceutski prihvatljiva sol.
10. Uporaba u skladu sa zahtjevom 9, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je (2S, 4S, 5S, 7S)-5-amino-4-hidroksi-2-izopropil-7-[4-metoksi-3-(3-metoksi-propoksi)-benzil]-8-metil-nonanoične kiseline (2-karbamoil-2-metil-propil)-amid hemifumarat.
11. Farmaceutski pripravak, naznačen time, da sadrži terapeutski učinkovitu količinu inhibitora renina u kombinaciji s inhibitorom istjecanja proteina, pri čemu je navedeni inhibitor istjecanja proteina prisutan u količini takvoj da se nakon primjene bioraspoloživost inhibitora renina poboljša najmanje 5%, pri čemu inhibitor renina je derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ili je to njegova farmaceutski prihvatljiva sol, te pri čemu inhibitor istjecanja proteina je MDR1 inhibitor.
12. Farmaceutski pripravak u skladu sa zahtjevom 11, naznačen time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ima formulu [image] gdje R1 je C1-4alkoksi-C1-4alkoksi ili C1-4alkoksi-C1-4alkil; R2 je C1-4alkil ili C1-4alkoksi; te R3 i R4 su neovisno razgranati C1-4alkil; ili je njegova farmaceutski prihvatljiva sol.
13. Farmaceutski pripravak u skladu sa zahtjevom 12, naznačen time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je spoj formule (I) gdje R1 je 3-metoksipropoksi; R2 je metoksi; te R3 i R4 su izopropil; ili je njegova farmaceutski prihvatljiva sol.
14. Farmaceutski pripravak u skladu sa zahtjevom 13, naznačen time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je (2S, 4S, 5S, 7S)-5-amino-4-hidroksi-2-izopropil-7-[4-metoksi-3-(3-metoksi-propoksi)-benzil]-8-metil-nonanoične kiseline (2-karbamoil-2-metil-propil)-amid hemifumarat.
15. Farmaceutski pripravak u skladu s bilo kojim zahtjevom 11 do 14, naznačen time, da MDR1 inhibitor je PSC833.
16. Farmaceutski pripravak, naznačen time, da sadrži terapeutski učinkovitu količinu inhibitora renina u kombinaciji s inhibitorom istjecanja proteina, pri čemu je navedeni inhibitor istjecanja proteina prisutan u količini takvoj da se nakon primjene bioraspoloživost inhibitora renina poboljša najmanje 5%, pri čemu inhibitor istjecanja proteina je PSC833.
17. Farmaceutski pripravak u skladu sa zahtjevom 16, naznačen time, da inhibitor renina je derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ili je njegova farmaceutski prihvatljiva sol.
18. Farmaceutski pripravak u skladu sa zahtjevom 17, naznačen time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ima formulu [image] gdje R1 je C1-4alkoksi-C1-4alkoksi ili C1-4alkoksi-C1-4alkil; R2 je C1-4alkil ili C1-4alkoksi; te R3 i R4 su neovisno razgranati C1-4alkil; ili je njegova farmaceutski prihvatljiva sol.
19. Farmaceutski pripravak u skladu sa zahtjevom 18, naznačen time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je spoj formule (I) gdje R1 je 3-metoksipropoksi; R2 je metoksi; te R3 i R4 su izopropil; ili je njegova farmaceutski prihvatljiva sol.
20. Farmaceutski pripravak u skladu sa zahtjevom 19, naznačen time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je (2S, 4S, 5S, 7S)-5-amino-4-hidroksi-2-izopropil-7-[4-metoksi-3-(3-metoksi-propoksi)-benzil]-8-metil-nonanoične kiseline (2-karbamoil-2-metil-propil)-amid hemifumarat.
21. Uporaba inhibitora istjecanja proteina u poboljšanju bioraspoloživosti inhibitora renina, naznačena time, da inhibitor renina je derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ili njegova farmaceutski prihvatljiva sol, te pri čemu inhibitor istjecanja proteina je inhibitor MDR1.
22. Uporaba u skladu sa zahtjevom 21, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ima formulu [image] gdje R1 je C1-4alkoksi-C1-4alkoksi ili C1-4alkoksi-C1-4alkil; R2 je C1-4alkil ili C1-4alkoksi; te R3 i R4 su neovisno razgranati C1-4alkil; ili je njegova farmaceutski prihvatljiva sol.
23. Uporaba u skladu sa zahtjevom 22, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je spoj formule (I) gdje R1 je 3-metoksipropoksi; R2 je metoksi; te R3 i R4 su izopropil; ili je njegova farmaceutski prihvatljiva sol.
24. Uporaba u skladu sa zahtjevom 23, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je (2S, 4S, 5S, 7S)-5-amino-4-hidroksi-2-izopropil-7-[4-metoksi-3-(3-metoksi-propoksi)-benzil]-8-metil-nonanoične kiseline (2-karbamoil-2-metil-propil)-amid hemifumarat.
25. Uporaba u skladu s bilo kojim zahtjevom 21 do 24, naznačena time, da MDR1 inhibitor je PSC833.
26. Uporaba inhibitora istjecanja proteina u poboljšanju bioraspoloživosti inhibitora renina ili njegove farmaceutski prihvatljive soli, naznačena time, da inhibitor istjecanja proteina je PSC833.
27. Uporaba u skladu sa zahtjevom 26, naznačena time, da inhibitor renina je derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline, ili je njegova farmaceutski prihvatljiva sol.
28. Uporaba u skladu sa zahtjevom 27, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline ima formulu [image] gdje R1 je C1-4alkoksi-C1-4alkoksi ili C1-4alkoksi-C1-4alkil; R2 je C1-4alkil ili C1-4alkoksi; te R3 i R4 su neovisno razgranati C1-4alkil; ili je njegova farmaceutski prihvatljiva sol.
29. Uporaba u skladu sa zahtjevom 28, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je spoj formule (I) gdje R1 je 3-metoksipropoksi; R2 je metoksi; te R3 i R4 su izopropil; ili je njegova farmaceutski prihvatljiva sol.
30. Uporaba u skladu sa zahtjevom 29, naznačena time, da derivat amida δ-amino-γ-hidroksi-ω-aril-alkanoične kiseline je (2S, 4S, 5S, 7S)-5-amino-4-hidroksi-2-izopropil-7-[4-metoksi-3-(3-metoksi-propoksi)-benzil]-8-metil-nonanoične kiseline (2-karbamoil-2-metil-propil)-amid hemifumarat.
HR20100064T 2004-08-03 2010-02-02 Postupci za poboljšanje bioraspoloživosti inhibitora renina HRP20100064T1 (hr)

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US59870004P 2004-08-03 2004-08-03
PCT/EP2005/008369 WO2006013094A1 (en) 2004-08-03 2005-08-02 Methods for improving bioavailability of a renin inhibitor

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US (1) US7709532B2 (hr)
EP (2) EP1776099B1 (hr)
JP (1) JP5134366B2 (hr)
KR (1) KR20070040384A (hr)
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AR (1) AR050043A1 (hr)
AT (1) ATE449601T1 (hr)
AU (1) AU2005268844B2 (hr)
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EC (1) ECSP077169A (hr)
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HR (1) HRP20100064T1 (hr)
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PT (1) PT1776099E (hr)
RU (1) RU2404758C2 (hr)
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EP1927350A1 (en) * 2006-11-24 2008-06-04 Novartis AG Methods for improving bioavailability of a renin inhibitor
CA2769392A1 (en) 2009-07-31 2011-02-03 Sandoz Ag Method for the preparation of w-amino-alkaneamides and w-amino-alkanethioamides as well as intermediates of this method
WO2012010651A2 (en) 2010-07-23 2012-01-26 Sandoz Ag Method for the preparation of omega-amino-alkaneamides and omega-amino-alkanethioamides as well as intermediates of this method
WO2014168255A1 (ja) * 2013-04-12 2014-10-16 国立大学法人京都大学 巨核球の成熟化促進物質
WO2015035218A1 (en) * 2013-09-05 2015-03-12 Howard University Method of increasing the bioavailability of an hiv drug
JP6029621B2 (ja) * 2014-07-14 2016-11-24 ヤマサ醤油株式会社 血漿レニン活性の測定法

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AU2005268844A1 (en) 2006-02-09
MX2007001339A (es) 2007-03-27
CN1993116B (zh) 2011-04-13
ZA200610639B (en) 2008-05-28
AU2005268844B2 (en) 2009-03-05
IL180678A (en) 2011-04-28
PE20060416A1 (es) 2006-06-09
RU2404758C2 (ru) 2010-11-27
MA28821B1 (fr) 2007-08-01
CA2572743C (en) 2012-12-04
CA2572743A1 (en) 2006-02-09
DK1776099T3 (da) 2010-03-01
AR050043A1 (es) 2006-09-20
JP2008508340A (ja) 2008-03-21
DE602005017905D1 (de) 2010-01-07
BRPI0514021A (pt) 2008-05-27
SI1776099T1 (sl) 2010-03-31
US7709532B2 (en) 2010-05-04
US20080108703A1 (en) 2008-05-08
PT1776099E (pt) 2010-01-06
PL1776099T3 (pl) 2010-05-31
WO2006013094A1 (en) 2006-02-09
IL180678A0 (en) 2008-03-20
EP2191823A1 (en) 2010-06-02
CN1993116A (zh) 2007-07-04
KR20070040384A (ko) 2007-04-16
EP1776099A1 (en) 2007-04-25
ECSP077169A (es) 2007-02-28
RU2007107850A (ru) 2008-09-10
JP5134366B2 (ja) 2013-01-30
TNSN07038A1 (en) 2008-06-02
NZ552903A (en) 2010-09-30
ATE449601T1 (de) 2009-12-15
NO20071142L (no) 2007-04-26
MY142180A (en) 2010-10-15
EP1776099B1 (en) 2009-11-25
CY1109826T1 (el) 2014-09-10
ES2335597T3 (es) 2010-03-30

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