AR104529A2 - Ligandos del receptor de melanocortina modificados con hidantoína - Google Patents

Ligandos del receptor de melanocortina modificados con hidantoína

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AR104529A2
AR104529A2 ARP160101279A ARP160101279A AR104529A2 AR 104529 A2 AR104529 A2 AR 104529A2 AR P160101279 A ARP160101279 A AR P160101279A AR P160101279 A ARP160101279 A AR P160101279A AR 104529 A2 AR104529 A2 AR 104529A2
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Argentina
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cys
arg
trp
hydantoin
seq
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ARP160101279A
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Ipsen Pharma Sas
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Abstract

La presente se relaciona con ligandos peptídicos de los receptores de melanocortina, en particular el receptor de melanocortina 4, y como tales, son útiles en el tratamiento de trastornos sensibles a la activación de este receptor, como obesidad, diabetes mellitus y disfunción sexual. Reivindicación 1: Un compuesto representado por la fórmula (1) caracterizado porque, X¹ es un resto de fórmula (2); X² es un resto de fórmula (3); A¹ es Cys; A² es un Glu, D-Ala; A³ es His; A⁴ es D-2-Nal, D-Phe; A⁵ es Arg; A⁶ es Trp; A⁷ es Cys, Pen; R¹ es H, alquilo C₁₋₁₀ o alquilo C₁₋₁₀ sustituido; R² y R³ son cada uno, independientemente, H, alquilo C₁₋₁₀, heteroalquilo C₁₋₁₀ sustituido con NRᵃRᵇ o ciclohexilo donde Rᵃ y Rᵇ es hidrógeno o R² y R³ pueden unirse para formar un ciclohexilo; R⁴ es OH o NH₂; R⁵ y R⁶ son cada uno, independientemente, H, alquilo C₁₋₁₀, heteroalquilo C₁₋₁₀ sustituido con NRᵃRᵇ o ciclohexilo donde Rᵃ y Rᵇ es hidrógeno o R⁵ y R⁶ pueden unirse para formar ciclohexilo; R⁷ y R⁸ son cada uno, independientemente, H, alquilo C₁₋₁₀, heteroalquilo C₁₋₁₀ sustituido con NRᵃRᵇ o ciclohexilo donde Rᵃ y Rᵇ es hidrógeno; o R⁷ y R⁸ pueden unirse para formar un ciclohexilo; R⁹ es H; y n es 0, caracterizado en que son seleccionados del grupo que consiste en: Hidantoína (C(O)-(Arg-Gly))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 13); Hidantoína (C(O)-(Nle-Gly))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 14); Hidantoína (C(O)-(Gly-Gly))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 15); Hidantoína (C(O)-(Nle-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 16); Hidantoína (C(O)-(Gly-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 17); Hidantoína (C(O)-(Nle-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH₂ (SEQ ID Nº 18); Hidantoína (C(O)-(Gly-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH₂ (SEQ ID Nº 19); Hidantoína (C(O)-(Ala-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 20); Hidantoína (C(O)-(D-Ala-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 21); Hidantoína (C(O)-(Aib-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 22); Hidantoína (C(O)-(Val-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 23); Hidantoína (C(O)-(Ile-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 24); Hidantoína (C(O)-(Leu-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 25); Hidantoína (C(O)-(Gly-Gly))-ciclo(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 15); Hidantoína (C(O)-(Nle-Gly))-ciclo(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 14); Hidantoína (C(O)-(D-Arg-Gly))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 26); Hidantoína (C(O)-(D-Arg-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 27); Hidantoína (C(O)-(Arg-Gly))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 28); Hidantoína (C(O)-(D-Arg-Gly))-ciclo(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 27); Hidantoína (C(O)-(Arg-Gly))-ciclo(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 28); Hidantoína (C(O)-(Ala-Nle))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 29); Hidantoína (C(O)-(Val-Nle))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 30); Hidantoína (C(O)-(Gly-Nle))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 31); Hidantoína (C(O)-(A6c-Nle))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 32); Hidantoína (C(O)-(Gly-Nle))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 33); Hidantoína (C(O)-(Ala-Nle))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 34); Hidantoína (C(O)-(D-Ala-Nle))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 35); Hidantoína (C(O)-(Val-Nle))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 36); Hidantoína (C(O)-(Leu-Nle))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 37); Hidantoína (C(O)-(Cha-Nle))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 38); Hidantoína (C(O)-(Aib-Nle))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 39); Hidantoína (C(O)-(Gly-Arg))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 40); Hidantoína (C(O)-(Gly-Arg))-ciclo(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 40); Hidantoína (C(O)-(Gly-Arg))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 41); Hidantoína (C(O)-(Gly-Arg))-ciclo(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 41); Hidantoína (C(O)-(Gly-D-Arg))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 42); Hidantoína (C(O)-(Gly-D-Arg))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 42); Hidantoína (C(O)-(Gly-D-Arg))-ciclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 43); Hidantoína (C(O)-(Gly-D-Arg))-ciclo(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 43); o Hidantoína (C(O)-(Nle-Ala))-ciclo(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH₂ (SEQ ID Nº 44).
ARP160101279A 2007-05-25 2016-05-05 Ligandos del receptor de melanocortina modificados con hidantoína AR104529A2 (es)

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CN101987865B (zh) * 2009-07-29 2014-07-30 中国人民解放军军事医学科学院毒物药物研究所 含有乙内酰脲结构的促黄体生成素释放激素拮抗剂
CN102548399A (zh) * 2009-08-05 2012-07-04 益普生制药股份有限公司 黑皮质素治疗血脂异常的用途
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