AR071354A1 - Composicion farmaceutica que comprende derivados de 5-(3-(etilsulfonil)fenil)-3,8-dimetil-n-(1-metilpiperidin-4-il)-9h-pirido [2,3-b]indol-7-carboxamida y una b ciclodextrina para mejorar su solubilidad - Google Patents

Composicion farmaceutica que comprende derivados de 5-(3-(etilsulfonil)fenil)-3,8-dimetil-n-(1-metilpiperidin-4-il)-9h-pirido [2,3-b]indol-7-carboxamida y una b ciclodextrina para mejorar su solubilidad

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Publication number
AR071354A1
AR071354A1 ARP090100683A ARP090100683A AR071354A1 AR 071354 A1 AR071354 A1 AR 071354A1 AR P090100683 A ARP090100683 A AR P090100683A AR P090100683 A ARP090100683 A AR P090100683A AR 071354 A1 AR071354 A1 AR 071354A1
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Argentina
Prior art keywords
alkyl
substituted
group
cycloalkyl
absent
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ARP090100683A
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English (en)
Inventor
Ronald J Christopher
Tomomichi Futo
Shinichiro Nakai
Bumsup Lee
Jong Rinaldo Laurentius De
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Takeda Pharmaceutical
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Application filed by Takeda Pharmaceutical filed Critical Takeda Pharmaceutical
Publication of AR071354A1 publication Critical patent/AR071354A1/es

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    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
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    • A61K31/716—Glucans
    • A61K31/724—Cyclodextrins
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
    • A61K47/6951—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
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Abstract

Reivindicacion 1: Una composicion farmacéutica que comprende: i) un compuesto caracterizado por la formula (1) donde Z, Z1, Z2, Z3, Z4 y Z5 se seleccionan cada uno en forma independiente del grupo que consiste en C y N; R1 es -Y1-R12, o R1 está ausente cuando Z1 es N; R2 es -Y2-R13, o R2 está ausente cuando Z2 es N, o R1 y R2 se toman en conjunto para formar un anillo sustituido o no sustituido; Y1, Y2 e Y3 están independientemente ausentes o son un conector que provee una separacion de 1 o 2 átomos entre R12, R13 o R14 y el anillo al que Y1, Y2 o Y3 están unidos, donde los átomos del conector que provee la separacion se seleccionan del grupo que consiste en carbono, oxígeno, nitrogeno y azufre; R4 se seleccionan del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi, carbonilo, amino, alquilamino C1-5, alquilo C1-5, haloalquilo C1-5, carbonilalquilo C1-3, sulfonilalquilo C1-3, aminoalquilo C1-5, arilalquilo C1-5 , heteroarilalquilo C1-5, cicloalquilo C3-6 y heterocicloalquilo C3-6, sustituido o no sustituido, con la condicion de que R4 esté ausente cuando el átomo al que esté unido sea N; R5 y R6 se seleccionan en forma independiente del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, aminoalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12, alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo, heteroarilo, bicicloarilo C9-12 y heterobicicloarilo C4-12, sustituido o no sustituido, con la condicion de que cada uno de R5 y R6 esté ausente cuando el átomo al que esté unido sea N; R7 se selecciona del grupo que consiste en hidrogeno, halo, hidroxi, alcoxi, amino y alquilo C1-5, sustituido o no sustituido, con la condicion de que R7 esté ausente cuando el átomo al que esté unido sea N; R12 y R13 se seleccionan en forma independiente del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, aminoalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo, heteroarilo, bicicloarilo C9-12 y heterobicicloarilo C4-12, sustituido o no sustituido, o R12 y R13 se toman en conjunto para formar un anillo sustituido o no sustituido; y R14 se selecciona del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, aminoalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo, heteroarilo, bicicloarilo C9-12 y heterobicicloarilo C4-12, sustituido o no sustituido; con la condicion de que (a) -Y3-R14 no sea H cuando Z, Z1, Z2, Z3 y Z5 son C; R5 sea un grupo amino sustituido; y R2 sea metoxi o R7 sea metilo o amino; y (b) R14 no sea 3-clorofenilo cuando R1, R5, R6 y R7, son H; Z y Z2 sean N; R2 y R4 estén ausentes; Z1, Z3, Z4 y Z5 sean C; e Y3 sea NH; una sal del mismo o un profármaco del mismo; ii) al menos un derivado de ciclodextrina; y iii) agua. Reivindicacion 12: La composicion de la reivindicacion 1, caracterizado porque es un agente para prevenir o tratar cáncer, inflamacion, enfermedades intestinales inflamatorias, psoriasis, rechazo al transplante, esclerosis lateral amiotrofica, degeneracion corticobasal, síndrome de Down, enfermedad de Huntington, enfermedad de Parkinson, parkisonismo postencefalítico, parálisis supranuclear progresiva, enfermedad de Pick, enfermedad de Niemann-Pick, apoplejía, traumas en la cabeza y otras enfermedades neurodegenerativas cronicas, trastorno bipolar, trastornos afectivos, depresion, esquizofrenia, trastornos cognitivos, pérdida del cabello, medicacion anticonceptiva, deficiencia cognitiva leve, deficiencia de la memoria asociada con la edad, deterioro cognitivo asociado con la edad, deficiencia cognitiva sin demencia, deterioro cognitivo leve, deterioro neurocognitivo leve, amnesia a edad avanzada, deficiencia de la memoria, deficiencia cognitiva, alopecia androgenética, enfermedades relacionadas con demencia, enfermedad de Alzheimer, afecciones asociadas con quinasas. Reivindicacion 14: Una composicion farmacéutica caracterizado porque comprende: i) 5-(3-(etilsulfonil)fenil)-3,8-dimetil-N-(1-metilpiperidin-4-il)-9H-pirido[2,3-b]indol-7-carboxamida o una sal de la misma, ii) sulfobutil éter-b-ciclodextrina o una sal de la misma, iii) agua y iv) ácido cítrico, que es una composicion farmacéutica, que tiene un pH de aproximadamente 2 a aproximadamente 4.
ARP090100683A 2008-02-28 2009-02-27 Composicion farmaceutica que comprende derivados de 5-(3-(etilsulfonil)fenil)-3,8-dimetil-n-(1-metilpiperidin-4-il)-9h-pirido [2,3-b]indol-7-carboxamida y una b ciclodextrina para mejorar su solubilidad AR071354A1 (es)

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US (1) US20100331357A1 (es)
EP (1) EP2252291A1 (es)
JP (1) JP2011513201A (es)
KR (1) KR20100129308A (es)
CN (1) CN102014901A (es)
AR (1) AR071354A1 (es)
AU (1) AU2009217969A1 (es)
BR (1) BRPI0908077A2 (es)
CA (1) CA2716720A1 (es)
CL (1) CL2009000453A1 (es)
CO (1) CO6290659A2 (es)
CR (1) CR11660A (es)
DO (1) DOP2010000262A (es)
EA (1) EA201071007A1 (es)
EC (1) ECSP10010505A (es)
IL (1) IL207734A0 (es)
MA (1) MA32165B1 (es)
MX (1) MX2010009513A (es)
PE (1) PE20091432A1 (es)
TW (1) TW200938544A (es)
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CN102827307B (zh) * 2011-06-17 2015-06-17 首都医科大学 β-环糊精修饰的四氢-β-咔啉羧酸衍生物及其制备方法和应用
CN103450371A (zh) * 2012-06-01 2013-12-18 首都医科大学 四氢-β-咔啉-3-甲酰基-二乙烯三胺-β-环糊精，其制备，抗血栓活性和应用
IN2015KN00075A (es) * 2012-07-12 2015-07-31 Sanofi Sa
WO2016022750A1 (en) * 2014-08-08 2016-02-11 Forsight Vision4, Inc. Stable and soluble formulations of receptor tyrosine kinase inhibitors, and methods of preparation thereof
JP2017155023A (ja) * 2016-03-04 2017-09-07 ジェイファーマ株式会社 Ｌａｔ１阻害活性を有する芳香族アミノ酸誘導体を含有する注射剤

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DE3346123A1 (de) * 1983-12-21 1985-06-27 Janssen Pharmaceutica, N.V., Beerse Pharmazeutische praeparate von in wasser schwerloeslichen oder instabilen arzneistoffen und verfahren zu ihrer herstellung
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WO2009107877A1 (en) 2009-09-03
TW200938544A (en) 2009-09-16
BRPI0908077A2 (pt) 2015-08-25
AU2009217969A1 (en) 2009-09-03
CN102014901A (zh) 2011-04-13
JP2011513201A (ja) 2011-04-28
CA2716720A1 (en) 2009-09-03
MX2010009513A (es) 2010-09-22
KR20100129308A (ko) 2010-12-08
EA201071007A1 (ru) 2011-04-29
ECSP10010505A (es) 2010-10-30
IL207734A0 (en) 2010-12-30
CL2009000453A1 (es) 2010-08-13
CR11660A (es) 2010-11-25
CO6290659A2 (es) 2011-06-20
PE20091432A1 (es) 2009-10-17
DOP2010000262A (es) 2010-09-30
US20100331357A1 (en) 2010-12-30
ZA201006224B (en) 2011-11-30

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