AR080357A1 - Derivados de fumaratos de acidos grasos, composiciones farmaceuticas y sus usos - Google Patents

Derivados de fumaratos de acidos grasos, composiciones farmaceuticas y sus usos

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Publication number
AR080357A1
AR080357A1 ARP110100061A ARP110100061A AR080357A1 AR 080357 A1 AR080357 A1 AR 080357A1 AR P110100061 A ARP110100061 A AR P110100061A AR P110100061 A ARP110100061 A AR P110100061A AR 080357 A1 AR080357 A1 AR 080357A1
Authority
AR
Argentina
Prior art keywords
alkyl
independently
null
optionally substituted
compound
Prior art date
Application number
ARP110100061A
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English (en)
Original Assignee
Catabasis Pharmaceuticals Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44258993&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR080357(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Catabasis Pharmaceuticals Inc filed Critical Catabasis Pharmaceuticals Inc
Publication of AR080357A1 publication Critical patent/AR080357A1/es

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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
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    • C07—ORGANIC CHEMISTRY
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    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/76—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
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Abstract

Derivados de fumaratos de ácidos grasos; composiciones que comprenden cantidades eficaces de un derivado de fumarato de ácido graso; y métodos para tratar o prevenir el cáncer, un trastorno metabolico o un trastorno neurodegenerativo, que comprende administrar una cantidad eficaz de un derivado de fumarato de ácido graso. Reivindicacion 2: Un compuesto caracterizado porque es de formula (1) o una sal aceptable farmacéuticamente, hidrato, solvato, prodroga, enantiomero, o estereoisomero del mismo; donde cada W1 y W2 es en forma independiente nulo, O, S, NH, o NR, o W1 y W2 pueden tomarse juntos para formar un grupo imidazolidina o piperazina opcionalmente sustituido; cada a, b, c, y d, es en forma independiente -H, -D, -CH3, -OCH3, -OCH2CH3, -C(O)O, -O-Z, o bencilo, o dos de a, b, c, y d pueden tomarse juntos, junto con el unico carbono al que están unidos, para formar un cicloalquilo o heterociclo; cada n, o, p, q, es en forma independiente 0, 1 o 2; cada L es en forma independiente nulo, -O-, -C(O)-,-S-, -S(O)-, -S(O)2-, -S-S-, -alquil C1-6-, -cicloalquil C3-6-, un heterociclo, un heteroarilo, una de los compuestos del grupo de formulas (2) donde la representacion de L no constituye una limitacion direccional de izquierda a derecha como se ilustra, sino que el lado derecho o el lado izquierdo de L puede estar unido al lado W1 del compuesto de formula (1); cada R6 es en forma independiente -H, -D, alquilo C1-4, -halogeno, ciano, oxo, tiooxo, -OH, -C(O)alquilo C1-4, -O-arilo, -O-bencilo, -OC(O)alquilo C1-4, alqueno C1-3, alquino C1-3, -C(O)alquilo C1-4, -NH2, -NH(alquilo C1-3), -N(alquil C1-3)2, -NH(C(O)alquilo C1-3), -N(C(O)alquil C1-3)2, -SH, -S(alquilo C1-3), -S(O)alquilo C1-3, -S(O)2alquilo C1-3; cada g es en forma independiente 2, 3 o 4; cada h es en forma independiente 1, 2, o 4; cada m y m' es en forma independiente 0, 1, 2, o 3; si m es mayor a 1, luego L o L' pueden ser iguales o diferentes; cada m1 es en forma independiente 0, 1, 2 o 3; k es 0, 1, 2, o 3; z es 1, 2, o 3; cada R4 es en forma independiente H o alquilo C1-6 opcionalmente sustituido, donde una unidad metileno del alquilo C1-6 puede reemplazarse opcionalmente por O o NR, y en NR4R4, ambos R4 cuando se toman junto con el nitrogeno al cual están unidos pueden formar un anillo heterocíclico como por ejemplo una pirrolidina, piperidina, morfolina, piperazina o pirrol; cada Z es en forma independiente H, o un resto de las formulas (3), (4) o (5) con las siguientes condiciones se encuentra presente al menos un resto (3) o (4) o en el compuesto; cada t es en forma independiente 0 o 1; cada r es en forma independiente 2, 3, o 7; cada s es en forma independiente 3, 5, o 6; cada v es en forma independiente 1, 2, o 6; cada R1 y R2 es en forma independiente -H, -O, alquilo C1-4, -halogeno, -OH, -C(O)alquilo C1-4, -O-arilo, -O-bencilo, -OC(O)alquilo C1-4, -alqueno C1-3, alquino C1-3, -C(O)alquilo C1-4, -NH2, -NH(alquilo C1-3), -N(alquil C1-3)2, -NH(C(O)alquilo C1-3), -N(C(O)alquil C1-3)2, -SH, -S(alquilo C1-3), -S(O)alquilo C1-3, -S(O)2alquilo C1-3; cada R3 es en forma independiente H, -alquilo C1-6 o -C(CH2OH)2; cada R5 es en forma independiente e, H o alquilo C1-10 de cadena lineal o ramificada que puede estar opcionalmente sustituido con OH, NH2, CO2R, CONH2, fenilo, C6H4OH, imidazol o arginina; cada e es en forma independiente H o cualquiera de las cadenas laterales de los aminoácidos naturales; cada R es en forma independiente -H, -alquilo C1-3, o alquilo C1-4 de cadena lineal o ramificada opcionalmente sustituido con OH, o halogeno; con las siguientes condiciones cuando cada uno de m, n, o, p, y q es 0, W1 y W2 son cada uno nulo, y Z es un resto (3) o (5) luego t debe ser 0; cuando cada uno de m, n, o, p, y q es 0, y W1 y W2 son cada uno nulo, luego Z no debe ser un resto (4). Reivindicacion 13: Una composicion farmacéutica caracterizada porque comprende un compuesto de formula 1, 1A, 1B, 1C o 2 y un vehículo farmacéuticamente aceptable. Reivindicacion 16: El método de la reivindicacion 15, caracterizado porque el trastorno metabolico es la diabetes tipo II, la enfermedad cardiovascular con resistencia a la insulina, la arritmia, la aterosclerosis, la enfermedad de la arteria coronaria, la hipertrigliceridemia, la dislipidemia, la retinopatía, la neuropatía, el edema macular, la nefropatía diabética, la nefropatía asociada a la lgA, la enfermedad renal cronica (CKD) y las enfermedades inflamatorias del rinon, que incluyen las complicaciones urémicas, la glomerulonefritis y la nefrosis.
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