HRP20090581T1 - Spojevi i postupci za liječenje dislipidemije - Google Patents

Spojevi i postupci za liječenje dislipidemije Download PDF

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HRP20090581T1
HRP20090581T1 HR20090581T HRP20090581T HRP20090581T1 HR P20090581 T1 HRP20090581 T1 HR P20090581T1 HR 20090581 T HR20090581 T HR 20090581T HR P20090581 T HRP20090581 T HR P20090581T HR P20090581 T1 HRP20090581 T1 HR P20090581T1
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alkyl
cycloalkyl
alkylaryl
bistrifluoromethylbenzyl
alkylheterocycle
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Cao Guoqing
Maria Escribano Ana
Carmen Fernandez Maria
Fields Todd
Linn Gernert Douglas
Lawrence Cioffi Christopher
Jason Herr Robert
Bryan Mantlo Nathan
Maria Martin De La Nava Eva
Isabel Mateo Herranz Ana
Ray Mayhugh Daniel
Wang Xiaodong
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Eli Lilly And Company
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    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • C07—ORGANIC CHEMISTRY
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    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
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    • C07D223/32—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems containing carbocyclic rings other than six-membered
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Abstract

Spoj formule Igdjen je 0, 1, 2 ili 3; m je 0, 1, 2 ili 3; p je 1 ili 2; q je 0, 1, 2 ili 3; Y je veza, C=O ili S(O)t; gdje t je 0, 1 ili 2; R1 se bira iz skupine koju čine hidroksi, C1-C6 alkil, aril, C2-C6 alkenil, C1-C6 halogenalkil, C1-C6 alkilheterocikl, C3-C8 cikloalkil, C1-C6 alkilcikloalkil; C1-C6 alkilaril, heterociklil, C2-C6 alkilalkohol, C1-C6 alkoksi, ariloksi, -OC2-C6 alkenil, -OC1-C6 halogenalkil, -OC1-C6 alkilheterocikl, -OC3-C8 cikloalkil, -OC1-C6 alkilcikloalkil, -NR7R8 i -OC1-C6 alkilaril, -O-heterocikl, te -OC1-C6 alkilheterocikl; uz uvjet da R1 nije hidroksi kada Y je S(O)t, CO ili kada n i y su oba 0; te gdje svaka od cikloalkilne, arilne i heterocikličke skupine je izborno supstituirana s 1 do 3 skupine, koje se neovisno bira između okso, hidroksi, halogena, C1-C6 alkila, C2-C6 alkena, C2-C6 alkinila, C1-C6 alkoksi, C1-C6 halogenalkila, C1-C6 alkilalkohola, CONR11R12, NR11SO2R12, NR11COR12, C0-C3 alkilNR11R12, C1-C3 alkilCOR11C0-C6 alkilCOOR11, cijano, C1-C6 alkilcikloalkila, fenila, -OC1-C6 alkilcikloalkila, -OC1-C6 alkilarila, -OC1-C6 alkilheterocikla, te C1-C6 alkilarila; R2 je vezan samo na atome ugljika i skupina je koju se neovisno bira između vodika, hidroksi, halogena, C1-C6 alkila, C2-C6 alkena, C2-C6 alkinila, C1-C6 alkoksi, C1-C6 halogenalkila, CONR11R12, NR11SO2R12, NR11COR12, C0-C6 alkilNR11R12, C0-C6 alkilCOR11, C0-C6 alkilCOOR11, cijano, nitro, C0-C6 alkilcikloalkila, fenila, C0-C6 alkilaril-heterociklila, C3-C8 cikloalkila, te C1-C6 halogenalkila; R4 je skupina prikazana formulom -NR9R10;R5 se bira iz skupine koju čine vodik, hidroksi, halogen, C1-C6 halogenalkil, C3-C8 cikloalkil, C1-C6 alkilaril, C1-C6 alkilheterocikl, aril, heterocikl, cijano, nitro, C1-C6 alkil, C2-C6 alkenil C1-C6 alkoksi, ariloksi, -OC2-C6 alkenil, -OC1-C6 halogenalkil, -C0-C6 alkilNR7R8, C0-C6 atkilCOR7, C0-C6 atkilCO2R7, C0-C6 alkilCONR7R8, CONR7SO2R8, NR7SO2R8, NR7COR8, N=CR7R8, OCONR7R8, S(O)2R7, SO2NR7R8, C1-C6 alkilalkohol, -OC1-C6 alkilheterocikl, te -OC1-C6 alkilaril, gdje svaka od alkilne, cikloalkilne, arilne i heterocikličke skupine je izborno supstituirana s okso, alkiloksi, ariloksi; te gdje se bilo koje dvije skupine R5 može kombinirati kako bi se dobilo izborno supstituirani 5- do 7- člani karbociklički ili heterociklički, zasićeni ili nezasićeni prsten, kondenziran s prstenom A na kojeg su vezane; R6 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C2-C6 alkenil, hidroksi, COR7, C1-C6 alkoksi, ariloksi, -OC2-C6 alkenil, -OC1-C6 halogenalkil, C1-C6 alkilNR11R12, C3-C8 cikloalkil, heterocikl, aril, te C1-C6 alkilcikloalkil; svakog R7 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, -OC1-C6 alkil, C1-C6 halogenalkil, -O-aril, -OC3-C8 cikloalkil, - O-heterocikl, -NR11R12, -C1-C6 alkilcikloalkil, -OC1-C6 alkilcikloalkil, -OC1-C6 alkilheterocikl, C1-C6 alkilheterocikl, -OC1-C6 alkilaril, C3-C8 cikloalkil, heterocikl, aril, te C1-C6 alkilaril, gdje svaka alkilna, cikloalkilna, het

Claims (22)

1. Spoj formule I [image] gdje n je 0, 1, 2 ili 3; m je 0, 1, 2 ili 3; p je 1 ili 2; q je 0, 1, 2 ili 3; Y je veza, C=O ili S(O)t; gdje t je 0, 1 ili 2; R1 se bira iz skupine koju čine hidroksi, C1-C6 alkil, aril, C2-C6 alkenil, C1-C6 halogenalkil, C1-C6 alkilheterocikl, C3-C8 cikloalkil, C1-C6 alkilcikloalkil; C1-C6 alkilaril, heterociklil, C2-C6 alkilalkohol, C1-C6 alkoksi, ariloksi, -OC2-C6 alkenil, -OC1-C6 halogenalkil, -OC1-C6 alkilheterocikl, -OC3-C8 cikloalkil, -OC1-C6 alkilcikloalkil, -NR7R8 i -OC1-C6 alkilaril, -O-heterocikl, te -OC1-C6 alkilheterocikl; uz uvjet da R1 nije hidroksi kada Y je S(O)t, CO ili kada n i y su oba 0; te gdje svaka od cikloalkilne, arilne i heterocikličke skupine je izborno supstituirana s 1 do 3 skupine, koje se neovisno bira između okso, hidroksi, halogena, C1-C6 alkila, C2-C6 alkena, C2-C6 alkinila, C1-C6 alkoksi, C1-C6 halogenalkila, C1-C6 alkilalkohola, CONR11R12, NR11SO2R12, NR11COR12, C0-C3 alkilNR11R12, C1-C3 alkilCOR11C0-C6 alkilCOOR11, cijano, C1-C6 alkilcikloalkila, fenila, -OC1-C6 alkilcikloalkila, -OC1-C6 alkilarila, -OC1-C6 alkilheterocikla, te C1-C6 alkilarila; R2 je vezan samo na atome ugljika i skupina je koju se neovisno bira između vodika, hidroksi, halogena, C1-C6 alkila, C2-C6 alkena, C2-C6 alkinila, C1-C6 alkoksi, C1-C6 halogenalkila, CONR11R12, NR11SO2R12, NR11COR12, C0-C6 alkilNR11R12, C0-C6 alkilCOR11, C0-C6 alkilCOOR11, cijano, nitro, C0-C6 alkilcikloalkila, fenila, C0-C6 alkilaril-heterociklila, C3-C8 cikloalkila, te C1-C6 halogenalkila; R4 je skupina prikazana formulom -NR9R10; R5 se bira iz skupine koju čine vodik, hidroksi, halogen, C1-C6 halogenalkil, C3-C8 cikloalkil, C1-C6 alkilaril, C1-C6 alkilheterocikl, aril, heterocikl, cijano, nitro, C1-C6 alkil, C2-C6 alkenil C1-C6 alkoksi, ariloksi, -OC2-C6 alkenil, -OC1-C6 halogenalkil, -C0-C6 alkilNR7R8, C0-C6 atkilCOR7, C0-C6 atkilCO2R7, C0-C6 alkilCONR7R8, CONR7SO2R8, NR7SO2R8, NR7COR8, N=CR7R8, OCONR7R8, S(O)2R7, SO2NR7R8, C1-C6 alkilalkohol, -OC1-C6 alkilheterocikl, te -OC1-C6 alkilaril, gdje svaka od alkilne, cikloalkilne, arilne i heterocikličke skupine je izborno supstituirana s okso, alkiloksi, ariloksi; te gdje se bilo koje dvije skupine R5 može kombinirati kako bi se dobilo izborno supstituirani 5- do 7- člani karbociklički ili heterociklički, zasićeni ili nezasićeni prsten, kondenziran s prstenom A na kojeg su vezane; R6 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C2-C6 alkenil, hidroksi, COR7, C1-C6 alkoksi, ariloksi, -OC2-C6 alkenil, -OC1-C6 halogenalkil, C1-C6 alkilNR11R12, C3-C8 cikloalkil, heterocikl, aril, te C1-C6 alkilcikloalkil; svakog R7 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, -OC1-C6 alkil, C1-C6 halogenalkil, -O-aril, -OC3-C8 cikloalkil, - O-heterocikl, -NR11R12, -C1-C6 alkilcikloalkil, -OC1-C6 alkilcikloalkil, -OC1-C6 alkilheterocikl, C1-C6 alkilheterocikl, -OC1-C6 alkilaril, C3-C8 cikloalkil, heterocikl, aril, te C1-C6 alkilaril, gdje svaka alkilna, cikloalkilna, heterociklička ili arilna skupina je izborno supstituirana s 1-3 skupine, koje se neovisno bira između hidroksi, halogena, okso, C1-C6 alkila, C1-C6 alkoksi, SO2R11, SO2NR11R12, C1-C6 alkilSO2NR11R12, COOR11, C1-C6 halogenalkila, te NR11R12, ili R11 i R12 se kombinira kako bi se dobilo heterociklički prsten s dušikom, koji još sadrži 0, 1 ili 2 dodatna heteroatoma, koje se bira između kisika, dušika i sumpora, gdje heterocikl s dušikom je izborno supstituiran s okso ili C1-C6 alkilom; svakog R8 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, -OC1-C6 alkil, C1-C6 halogenalkil, -O-aril, -OC3-C8 cikloalkil, -O-heterocikl, -NR11R12, -C1-C6 alkilcikloalkil, -OC1-C6 alkilcikloalkil, -OC1-C6 alkilheterocikl, C1-C6 alkilheterocikl, -OC1-C6 alkilaril, C3-C8 cikloalkil, heterocikl, aril, te C1-C6 alkilaril, gdje svaka alkilna, cikloalkilna, heterociklička ili arilna skupina je izborno supstituirana s 1-3 skupine, koje se neovisno bira između hidroksi, halogena, C1-C6 alkila, C1-C6 alkoksi, C1-C6 halogenalkila, te NR11R12, ili R11 i R12 se kombinira kako bi se dobilo heterociklički prsten s dušikom, koji još sadrži 0, 1, ili 2 dodatna heteroatoma, koje se bira između kisika, dušika i sumpora, gdje heterocikl s dušikom je izborno supstituiran s okso ili C1-C6 alkilom; R9 je COR7 ili S(O)tR7, gdje R7 je definiran kako gore; R10 se bira iz skupine koju čine aril, C1-C6 alkilaril, C2-C6 alkenilaril, C2-C6 alkinilaril, C1-C6 alkilheterocikl, C2-C6 alkenilheterocikl, C1-C6 alkilcikloalkil, C1-C6 alkil-O-C1-C6 alkilaril, te gdje svaka cikloalkilna, arilna ili heterociklička skupina je izborno supstituirana s 1-3 skupine, koje se neovisno bira iz skupine koju čine hidroksi, okso, -SC1-C6 alkil, C1-C6 alkil, C1-C6 alkenil, C1-C6 alkinil, C1-C6 halogenalkil, halogen, C1-C6 alkoksi, ariloksi, C1-C6 alkeniloksi, C1-C6 halogenalkoksialkil, C0-C6 alkilNR11R12, -OC1-C6 alkilaril, nitro, cijano, C1-C6 halogenalkilalkohol, te C1-C6 alkilalkohol; R11 i R12 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C1-C6 alkenil, C3-C8 cikloalkil, heterocikl, aril, C1-C6 alkilaril, gdje svaka arilna, cikloalkilna i heterociklička skupina je izborno supstituirana s 1-3 skupine, koje se neovisno bira između halogena, C1-C6 alkilheterocikla, te C1-C6 halogenalkila, ili R11 i R12 se kombinira kako bi se dobilo heterociklički prsten s dušikom, koji može još sadržavati 0, 1 ili 2 dodatna heteroatoma, koje se bira između kisika, dušika ili sumpora, i izborno je supstituiran s okso, C1-C6 alkilom, COR7, te SO2R7; ili njegova farmaceutski prihvatljiva sol, solvat, enantiomer, racemat, dijastereomer ili smjesa njegovih dijastereomera.
2. Spoj u skladu s patentnim zahtjevom 1, gdje R1 se bira iz skupine koju čine C1-C6 alkoksi, C1-C6 alkilcikloalkil, C3-C8 cikloalkil, C1-C6 alkilheterocikl, ariloksi, -OC2-C6 alkenil, -OC1-C6 halogenalkil, -OC3-C8 cikloalkil, -OC1-C6 alkilaril, OC3-C8 heterocikl, te -OC1-C6 alkilheterocikl.
3. Spoj u skladu s patentnim zahtjevom 1, gdje R1 se bira iz skupine koju čine C1-C6 alkoksi, C1-C6 alkilcikloalkil, C3-C8 cikloalkil, C1-C6 alkilheterocikl, ariloksi, -OC2-C6 alkenil, -OC1-C6 haloalkil, -OC3-C8 cikloalkil, -OC1-C6 alkilaril, OC3-C8 heterocikl, te -OC1-C6 alkilheterocikl; R4 je skupina NR9R10, a R9 se bira između izborno supstituiranog heterocikla ili alkilheterocikla.
4. Spoj u skladu s patentnim zahtjevom 1, gdje R1 se bira iz skupine koju čine C1-C6 alkoksi, C1-C6 alkilcikloalkil, C1-C6 alkilheterocikl, C3-C8 cikloalkil, C1-C6 alkilaril, ariloksi, -OC2-C6 alkenil, -OC1-C6 haloalkil, -OC3-C8 cikloalkil, OC1-C6 heterocikl, -OC1-C6 alkilaril, te -OC1-C6 alkilheterocikl; R4 je skupina NR9R10, gdje R9 je COR7.
5. Spoj u skladu s patentnim zahtjevom 1, gdje n je 0; i je veza; a R1 je alkilaril, alkilheterocikl, alkilcikloalkil, gdje svaka od alkilne, arilne, cikloalkilne i heterociklne skupine je izborno supstituirana s 1, 2 ili 3 skupine, koje se neovisno bira između hidroksi, okso, -COOH, C1-C6 alkila, C1-C6 alkoksi, C1-C6 alkilcikloalkila, C1-C6 alkilarila, te -OC1-C6 alkilarila.
6. Spoj u skladu s patentnim zahtjevom 1, gdje p je 1.
7. Spoj u skladu s patentnim zahtjevom 1, gdje p je 2.
8. Spoj u skladu s patentnim zahtjevom 1, gdje p je 1 ili 2; n je 0 ili 1; m je 0, a q je 1-3.
9. Spoj u skladu s patentnim zahtjevom 1, gdje n i m su neovisno 0 ili 1; a q je 2 ili 3.
10. Spoj u skladu s patentnim zahtjevom 1 ili 3, gdje q je 2, a skupine R5 se kombinira kako bi se dobilo petero- ili 6- člani, izborno supstituirani, prsten, kondenziran s prstenom A, gdje navedeni kondenzirani prsten može imati 1, 2 ili 3 heteroatomske spojnice, koje se neovisno bira između kisika, ili N ili NH.
11. Spoj u skladu s patentnim zahtjevom 1, gdje R4 se bira iz skupine koju čine: [image] [image] [image]
12. Spoj u skladu s patentnim zahtjevom 1, kojeg se bira iz skupine koju čine: izopropilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-7-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[(3,5-bistrifluormetilbenzil)metoksikarbonilamino]-7-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, etilni ester 5-[(3,5-bistrifluormetilbenzil)metoksikarbonilamino]-7-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, etilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-7-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[(3,5-bistrifluormetilbenzil)metoksikarbonilamino]-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[(3,5-bistrifluormetilbenzil)metoksikarbonilamino]-7-brom-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, etilni ester 5-[(3,5-bistrifluormetilbenzil)metoksikarbonilamino]-7-brom-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, etilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-7-brom-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, etilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-7-metoksi-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-8-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-8-fluor-7-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-2-metil-7-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-4,4-dimetil-7-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 6-[acetil-(3,5-bistrifluormetilbenzil)amino]-8-trifluormetil-3,4,5,6-tetrahidro-2H-benzo[b]azocin-1-karboksilne kiseline, izopropilni ester 6-[acetil-(3,5-bistrifluormetilbenzil)amino]-9-trifluormetil-3,4,5,6-tetrahidro-2H-benzo[b]azocin-1-karboksilne kiseline, izopropilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-9-trifluormetil-3,4,5,6-tetrahidro-2H-benzo[b]azocin-1-karboksilne kiseline, izopropilni ester 4-[acetil-(3,5-bistrifluormetilbenzil)amino]-7-trifluormetil-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[acetil-(3,5-bistrifluormetilbenzil)amino]-8-klor-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, izopropilni ester 5-[(3,5-bistrifluormetilbenzil)metoksikarbonilamino]-8-klor-2,3,4,5-tetrahidrobenzo[b]azepin-1-karboksilne kiseline, ili njihove farmaceutski prihvatljive soli, solvati, enantiomeri, dijastereomeri ili njihove smjese.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, namijenjen upotrebu u terapiji.
14. Spoj formule I u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, solvat, enantiomer, racemat, dijastereomer, ili smjesa njegovih dijastereomera, namijenjen upotrebi u liječenju ili sprječavanju dislipidemije.
15. Spoj formule I u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, solvat, enantiomer, racemat, dijastereomer, ili smjesa njegovih dijastereomera, namijenjen upotrebi u liječenju kardiovaskularnih bolesti.
16. Spoj formule I u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, solvat, enantiomer, racemat, dijastereomer, ili smjesa njegovih dijastereomera, namijenjen upotrebi u liječenju ili sprječavanju ateroskleroze.
17. Spoj formule I u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, solvat, enantiomer, racemat, dijastereomer, ili smjesa njegovih dijastereomera, namijenjen smanjivanju razine LDL-kolesterola u plazmi kod sisavca.
18. Spoj formule I u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, solvat, enantiomer, racemat, dijastereomer, ili smjesa njegovih dijastereomera, namijenjen upotrebi u liječenju i/ili sprječavanju patoloških posljedica visokih razina LDL-kolesterola u plazmi kod sisavca.
19. Spoj formule I u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, solvat, enantiomer, racemat, dijastereomer, ili smjesa njegovih dijastereomera, namijenjen upotrebi u liječenju i/ili sprječavanju patoloških posljedica niskih razina HDL-kolesterola u plazmi kod sisavca.
20. Spoj formule I u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, solvat, enantiomer, racemat, dijastereomer, ili smjesa njegovih dijastereomera, namijenjen upotrebi u liječenju i/ili sprječavanju pretilosti.
21. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, namijenjen upotrebi u liječenju i/ili sprječavanju arterioskleroze kod sisavca.
22. Farmaceutska formulacija, koja sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, te podlogu, razrjeđivač i/ili pomoćnu tvar.
HR20090581T 2003-10-08 2009-10-30 Spojevi i postupci za liječenje dislipidemije HRP20090581T1 (hr)

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