AR073099A2 - Analogos de ghrelina - Google Patents

Analogos de ghrelina

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Publication number
AR073099A2
AR073099A2 ARP090103204A ARP090103204A AR073099A2 AR 073099 A2 AR073099 A2 AR 073099A2 AR P090103204 A ARP090103204 A AR P090103204A AR P090103204 A ARP090103204 A AR P090103204A AR 073099 A2 AR073099 A2 AR 073099A2
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dab
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Sod Conseils Rech Applic
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    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/60—Growth-hormone releasing factors (GH-RF) (Somatoliberin)
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Abstract

Análogos de GHrelina, junto con usos terapéuticos y no terapéuticos de los mismos. Reivindicacion 1: Un compuesto conforme a la formula: (R2R3)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-R1 o una sal farmacéuticamente aceptable del mismo, en donde: A1 es Gly, Aib, Ala, b-Ala, o Acc; A2 es Ser, Aib, Act, Ala, Acc, Abu, Act, Ava, Thr, o Val; A3 es Ser, Ser(C(O)-R4), Asp(O-R8), Asp(NH-R9), Cys(S-R14), Dap(S(O)2-R10), Dab(S(O)2-R11), Glu(O-R6), Glu(NH-R7), Thr, Thr(C(O)-R5), o HN-CH((CH2)n-N(R12R13))-C(O); A4 es Phe, Acc, Aic, Cha, 2Fua, 1Nal, 2Nal, 2Pal, 4Pal, hPhe, (X1,X2,X3,X4,X5)Phe, Taz, 2Thi, 3Thi, Trp, o Tyr; A5 es Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, o Val; A6 es Ser, Abu, Acc, Act, Aib, Ala, Gly, Thr, o Val; A7 es Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, o eliminado; A8 es Glu, Acc, Aib, Arg, Asn, Asp, Dap, Gln, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A9 es His, Apc, Aib, Acc, 2Fua, 2Pal, 3pal, 4Pal, Taz, 2Thi, 3Thi, (X1,X2,X3,X4,X5-)Phe o eliminado; A10 es Gln, Acc, Aib, ASn, ASp, Glu, o eliminado; A11 es Arg, Apc, hArg, Dab, Dap, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A12 es Val, Abu, Acc, Aib, Ala, Cha, Nva, Gly, Ile, Leu, Nle, Tle, Cha, o eliminado; A13 es Gln, Acc, Aib, Asn, Asp, Glu, o eliminado; A14 es Gln, Acc, Aib, Asn, Asp, Glu, o eliminado; A15 es Arg, hArg, Acc, Aib, Apc, Dab, Dap, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A16 es Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A17 es Glu, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A18 es Ser, Abu, Acc, Act, Aib, Ala, Thr, Val, o eliminado; A19 es Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A20 es Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A21 es Pro, Dhp, Dmt, Inc, 3Hyp, 4Hyp, Ktp, Oic, Pip, Thz, Tic, o eliminado; A22 es Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, o eliminado; A23 es Abu, Acc, Act, Aib, Ala, Apc, Gly, Nva, Val, o eliminado; A24 es Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A25 es Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, Val, o eliminado; A26 es Gln, Aib, Asn, Asp, Glu, o eliminado; A27 es Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, o eliminado; A28 es Acc, Aib, Apc, Arg, hArg, Dab, Dap, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; R1 es -OH, -NH2, -alcoxi C1-30, o NH-X6-CH2-Z0, en donde X6 es un alquilo C1-12, alquenilo C2-12, y Z0 es -H, -OH, -CO2H o -C(O)-NH2; R2 y R3 son, cada uno en forma independiente para cada aparicion, H, alquilo C1-20 o acilo C1-20; R4, R5, R6, R7, R8, R9, R10, R11 y R14 son, cada uno en forma independiente para cada aparicion, alquilo C1-40, alquenilo (C2-40, alquilo C1-40 sustituido, alquenilo C2-40 sustituido, alquilarilo, alquilarilo sustituido, arilo o arilo sustituido; R12 y R13 son, cada uno en forma independiente para cada aparicion, H, alquilo C1-40, acilo C1-40, alquilsulfonilo C1-30, o -C(NH)-NH2, en donde cuando R12 es acilo C1-40, alquilsulfonilo C1-30, o -C(NH)-NH2, entonces R13 es H o alquilo C1-40; n es, en forma independientemente para cada aparicion, 1, 2, 3, 4, o 5; X1, X2, X3, X4 y X5 son, cada uno en forma independiente para cada aparicion, H, F, Cl, Br, I, alquilo C1-10, alquilo C1-10 sustituido, arilo, arilo sustituido, OH, NH2, NO2, o CN; siempre que el péptido contenga por lo menos un aminoácido seleccionado entre los grupos que consisten en: A2 es Aib, Acc, o Act; A3 es Dap(S(O)2-R10), Dab(S(O)2-R11), Glu(NH-Hexil), o Cys(S-Decil); A5 es Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, o Val; A6 es Abu, Acc, Act, Aib, Ala, Gly, Thr o Val; A7 es Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz o Tic; A8 es Acc, Aib, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, o HN-CH((CH2)n-N(R12R13))-C(O); A9 es Aib, Acc, Apc, 2Fua, 2Pal, 3Pal, 4Pal, Taz, 2Thi, 3Thi, o (X1,X2,X3,X4,X5-)Phe; y A10 es Acc, Aib, Asn, Asp, o Glu; y además, siempre que el péptido no sea (Lys8)hGHrelina(1-8)-NH2 o (Arg8)hGHrelina(1-8)-NH2.
ARP090103204A 2002-07-23 2009-08-20 Analogos de ghrelina AR073099A2 (es)

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KR20050026503A (ko) 2005-03-15
CA2491946A1 (en) 2004-01-29
MXPA05000908A (es) 2005-07-22
JP2006515271A (ja) 2006-05-25
US9133261B2 (en) 2015-09-15
EP1578778A2 (en) 2005-09-28
US20050272648A1 (en) 2005-12-08
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EP1578778B1 (en) 2011-01-26
NO20050083L (no) 2005-03-23
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