AR086481A1 - COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K), Y UN INHIBIDOR DE mTOR - Google Patents

COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K), Y UN INHIBIDOR DE mTOR

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Publication number
AR086481A1
AR086481A1 ARP120101389A ARP120101389A AR086481A1 AR 086481 A1 AR086481 A1 AR 086481A1 AR P120101389 A ARP120101389 A AR P120101389A AR P120101389 A ARP120101389 A AR P120101389A AR 086481 A1 AR086481 A1 AR 086481A1
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AR
Argentina
Prior art keywords
alkyl
substituted
substituents
deuterium
fluorine
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ARP120101389A
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English (en)
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Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR086481A1 publication Critical patent/AR086481A1/es

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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
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    • 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
    • A61K31/436—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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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Abstract

Combinación farmacéutica que comprende un compuesto inhibidor de cinasa de fosfatidil-inositol-3 (PI3K), el cual es un derivado de 2-carboxamida-cicloamino-urea, o una sal farmacéuticamente aceptable del mismo, y cuando menos un inhibidor del objetivo de rapamicina de mamífero (mTOR), o una sal farmacéuticamente aceptable del mismo. Composición farmacéutica, la cual comprende dicha combinación; y usos de esta combinación en el tratamiento de las enfermedades proliferativas, más específicamente de las enfermedades dependientes de la cinasa del objetivo de rapamicina de mamífero (mTOR).Reivindicación 1: Una combinación farmacéutica, la cual comprende: a) un compuesto de la fórmula (1), o una sal del mismo, en donde: A representa un heteroarilo seleccionado a partir del grupo de fórmulas (2); R1 representa uno de los siguientes sustituyentes: (i) alquilo C1-7 insustituido o sustituido, de preferencia sustituido, en donde los sustituyentes se seleccionan independientemente a partir de una o más, de preferencia de una a nueve de las siguientes fracciones: deuterio, flúor, o de una a dos de las siguientes fracciones: cicloalquilo C3-5; (ii) cicloalquilo C3-5 opcionalmente sustituido, en donde los sustituyentes se seleccionan independientemente a partir de una o más, de preferencia de una a cuatro de las siguientes fracciones: deuterio, alquilo C1-4 (de preferencia metilo), flúor, ciano, amino-carbonilo; (iii) fenilo opcionalmente sustituido, en donde los sustituyentes se seleccionan independientemente a partir de una o más, de preferencia de una a dos de las siguientes fracciones: deuterio, halógeno, ciano, alquilo C1-7, alquilo C1-7-amino, di-(alquilo C1-7)-amino, alquilo C1-7-amino-carbonilo, di-(alquilo C1-7)-amino-carbonilo, alcoxilo C1-7; (iv) amina opcionalmente mono- o di-sustituida; en donde los sustituyentes se seleccionan independientemente a partir de las siguientes fracciones: deuterio, alquilo C1-7 (que está insustituido o sustituido por uno o más sustituyentes seleccionados a partir del grupo de deuterio, flúor, cloro, hidroxilo), fenil-sulfonilo (que está insustituido o sustituido por uno o más, de preferencia uno de alquilo C1-7, alcoxilo C1-7, di-(alquilo C1-7)-amino-alcoxilo C1-7); (v) sulfonilo sustituido: en donde el sustituyente se selecciona a partir de las siguientes fracciones: alquilo C1-7 (que está insustituido o sustituido por uno o más sustituyentes seleccionados a partir del grupo de deuterio, flúor), pirrolidino (que está insustituido o sustituido por uno o más sustituyentes seleccionados a partir del grupo de deuterio, hidroxilo, oxo; en particular un oxo); (vi) flúor, cloro; R2 representa hidrógeno; R3 representa: (i) hidrógeno, (ii) flúor, cloro, (iii) metilo opcionalmente sustituido, en donde los sustituyentes se seleccionan independientemente a partir de una o más, de preferencia de una a tres de las siguientes fracciones: deuterio, flúor, cloro, dimetilamino; con la excepción de la 1-({5-[2-(terbutil)-pirimidin-4-il]-4-metil-tiazol-2-il}-amida) de 2-amida del ácido (S)-pirrolidin-1,2-dicarboxílico y b) cuando menos un inhibidor de mTOR. Reivindicación 2: La combinación farmacéutica de acuerdo con la reivindicación 1, en donde el compuesto de la fórmula (1) es la 1-({4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il}-amida) de 2-amida del ácido (S)-pirrolidin-1,2-dicarboxílico.
ARP120101389A 2011-04-25 2012-04-23 COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K), Y UN INHIBIDOR DE mTOR AR086481A1 (es)

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US201161478572P 2011-04-25 2011-04-25

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AR086481A1 true AR086481A1 (es) 2013-12-18

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ARP120101389A AR086481A1 (es) 2011-04-25 2012-04-23 COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K), Y UN INHIBIDOR DE mTOR

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US (3) US20140066474A1 (es)
EP (1) EP2701703A1 (es)
JP (2) JP6086902B2 (es)
KR (1) KR101925656B1 (es)
CN (1) CN103491955B (es)
AR (1) AR086481A1 (es)
AU (2) AU2012250010A1 (es)
BR (1) BR112013027486A2 (es)
CA (1) CA2833962A1 (es)
CL (1) CL2013003078A1 (es)
CO (1) CO6801759A2 (es)
EA (1) EA025948B1 (es)
EC (1) ECSP13012994A (es)
GT (1) GT201300263A (es)
IL (1) IL229008A (es)
MA (1) MA35038B1 (es)
MX (1) MX2013012385A (es)
NZ (1) NZ615593A (es)
PE (1) PE20140601A1 (es)
SG (1) SG193919A1 (es)
TN (1) TN2013000392A1 (es)
TW (1) TWI602567B (es)
UA (1) UA110961C2 (es)
WO (1) WO2012148846A1 (es)
ZA (1) ZA201306973B (es)

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RU2014122198A (ru) * 2011-11-02 2015-12-10 Новартис Аг Производные 2-карбоксамид циклоамино мочевины для применения в лечении vegf-зависимых заболеваний
CN105246482A (zh) * 2013-03-15 2016-01-13 因特利凯有限责任公司 激酶抑制剂的组合及其用途
EP3068435A1 (en) * 2013-11-13 2016-09-21 Novartis AG Mtor inhibitors for enhancing the immune response
KR20160110963A (ko) * 2014-02-11 2016-09-23 노파르티스 아게 암 치료를 위한 pi3k 억제제를 포함하는 제약 조합물
WO2015148626A1 (en) * 2014-03-26 2015-10-01 Millennium Pharmaceuticals, Inc. Treatment of fibrotic disorders
MX2017004359A (es) * 2014-10-03 2017-06-23 Novartis Ag Composiciones farmaceuticas que comprenden alpelisib.
US20160339030A1 (en) 2015-05-19 2016-11-24 University Of Maryland, Baltimore Treatment agents for inhibiting hiv and cancer in hiv infected patients
GB202010627D0 (en) * 2020-07-10 2020-08-26 Qbd (Qs-Ip) Ltd Blocking method

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