AR031613A1 - Derivados de piridina, un medicamento, una composicion farmaceutica, un inhibidor de la quinasa betaikappab, un medicamento anti-inflamatorio, un inmunosupresor, un medicamento para la isquemia, un medicamento anti-tumoral y el uso de dichos derivados para la preparacion de un medicamento - Google Patents
Derivados de piridina, un medicamento, una composicion farmaceutica, un inhibidor de la quinasa betaikappab, un medicamento anti-inflamatorio, un inmunosupresor, un medicamento para la isquemia, un medicamento anti-tumoral y el uso de dichos derivados para la preparacion de un medicamentoInfo
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- AR031613A1 AR031613A1 ARP010104446A ARP010104446A AR031613A1 AR 031613 A1 AR031613 A1 AR 031613A1 AR P010104446 A ARP010104446 A AR P010104446A AR P010104446 A ARP010104446 A AR P010104446A AR 031613 A1 AR031613 A1 AR 031613A1
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- alkyl
- amino
- hydrogen
- alkanoyl
- aminocarbonyl
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Abstract
Derivados de piridina, que comprenden un derivado de formula (1), en la que: R1 representa un resto de formula (2), (3) o (4), en la que R11 es hidrogeno, alquilo C1-6, halogeno, hidroxi, alcoxi C1-12, nitro, amino, alquil C1-6-sulfonilamino, alcoxi C1-6-carbonilo, alquil C1-6-amino, di(alquil C1-6)amino, alcanoil C1-6-amino, fenilalquil C1-6-amino, fenilsulfonilamino o -O-(CH2)n-R111, en la que n representa un numero entero seleccionado entre 0 y 6, y R111 es alquenilo C2-6, benzoilo, difenilmetilo, di(alquil C1-6)amino, alcanoilo C1-6alcoxi C1-6carbonilo, o un anillo saturado o insaturado de 3-10 miembros que presenta de 0-3 heteroátomos seleccionados del grupo constituido por S, O y N como heteroátomos y está opcionalmente sustituido por alquilo C1-6, mono o dihalogeno, alquilo C1-6 sustituido con halogeno, nitro, ciano, alcoxi C1-6-carbonilo, fenilo, hidroxi, amino, alquil C1-6-amino, di(alquilC1-6)amino, alcanoil C1-6-amino, alcoxi C1-6 o carbamoilo; R2 representa hidrogeno o halogeno; R3 representa hidrogeno o 1,2,3,4-tetrahidropiridina, CR31R32R33, en la que R31 es hidrogeno o alquilo C1-6, R32 es hidrogeno, alfa-aminobencilo, alquilo C1-6 opcionalmente sustituido por uno o dos sustituyentes seleccionados del grupo constituido por hidroxi, amino, fenilo sustituido con amino, fenilo, fenilo sustituido con halogeno y fenilo sustituido con alcoxi C1-6, o un anillo saturado de 5-8 miembros que presenta de 0-3 heteroátomos seleccionados entre el grupo constituido por S, O y N como heteroátomos y opcionalmente sustituidos por alquilo C1-6, y R33 es hidrogeno, amino, alcoxi C1-6-carbonilamino, alquenil C2-6-oxicarbonilamino, piperidinalquil C1-6-carbonilamino, piperidinialquil C1-6-carbonilamino, o R32 y R33 pueden formar, junto con el átomo de carbono adyacente un anillo saturado de 5-8 miembros que presente de 0-3 heteroátomos seleccionados del grupo constituido por N, O y S como heteroátomos, cuyo anillo está opcionalmente sustituido con fenilalquilo C1-6, fenilalquilo C1-6 sustituido con alcoxi C1-6, alquilo C1-6, amino, ciano, hidroxi, carbamoilo, carboxi, alquil C1-6-amino, alcoxi C1-6-carbonilo, di(alquilo C1-6)amino, bencilamino, alquil C1-6-sulfonilo, piperidinalquil C1-6-carbonilo u opcionalmente fusionado por benceno; o -NR34R35, en la que R34 es hidrogeno o alquilo C1-6, y R35 es hidrogeno, un anillo saturado de 5-8 miembros que presenta de 0-3 heteroátomos seleccionados del grupo constituido por N, O, y S como heteroátomos, o -(CH2)m-NR351R352 (m representa cualquier numero entero de 1 a 6), en la que R351representa hidrogeno o alquilo C1-6, y R352 representa hidrogeno, alquilo C1-6, alcanoilo C1-6, fenilo sustituido con alquilo C1-6, benzoilo, alcanoilo C1-6, fenilaminocarbonilo, fenilsulfonilo, o R34 y R35 pueden formar, junto con el átomo de N adyacente, un anillo heterocíclico saturado de 5-8 miembros, y el mencionado anillo puede contener opcionalmente NH, átomos de S u O distintos del átomo de N adyacente y opcionalmente sustituido por carbamoilo, amino o alquilo C1-6; R4 representa hidroxicarbonilo, alcanoilo C1-6, carbamoilo, ciano, nitro, carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbamoilo, alquil C1-6-amino, heteroaril(hidroxi)metilo de 5-10 miembros, heteroarilalquilo C1-6 de 5-10 miembros o metilo sustituido por hidroxi y un anillo cíclico saturado de 5-7 miembros, alquilo C1-6 opcionalmente sustituido por un sustituyente seleccionado del grupo constituido por hidroxi, alcoxi C1-6, alquilo C1-6-sulfonilamino, alquil C1-6-carbonilamino, arilo C5-10, aril C5-10-sulfonilo, aril C5-10-sulfanilo, aril C5-10-oxi, imidazolilo o pirrolidinoxi sustituido con dioxo, -(CH2)pNHCOR41, -(CH2)pNCH(=S)R41, en las que p representa cualquier numero entero de 1 a 6 y R41 representa alcoxi C1-6, amino, fenilamino, alquilo C1-6, alquil C1-6-amino, di(alquil C1-6)amino, cicloalquil C3-10-amino; R3 y R4 pueden formar junto con los átomos de carbono en el anillo de piridina, monocicloalquilo o bicicloalquilo de 4-10 miembros opcionalmente interrumpidos por NH y opcionalmente sustituidos por bencilo, =NH o =O; R5 representa NR51R52, en la que R51 es hidrogeno o alquilo C1-6; R52 es hidrogeno, alquilo C1-6, fenilo, bencilo, alcanoilo o NR51R52 puede formar un anillo saturado de 5-6 miembros que contienen opcionalmente NH u O como otro heteroátomo distinto al átomo de N adyacente; o R4 y R5 pueden formar, -R40-CO-NH-, -R40-SO2-NH-, -R40-C(=S)-NH-, -R40-CH2-NH-, en las que el mencionado R40 representa -CHR401-O-, -CH2-NR401, -CO-NR401, CH2CHR401, -CH=CR401 (en las cuales R401 es alcanoilo C1-6, alquilo C1-6, fenilo, alquil C1-6-sulfonilo, cicloalquil C3-8-aminocarbonilo, hidrogeno, halogeno, nitro, amino, ciano, benzoilamino, fenilsulfonilo, carbamoilo, hidroxicarbonilo, alcoxi C1-6-carbonilo, alquil C1-12-aminicarbonilo, alquil C1-6-aminocarbonilo sustituido con halogeno, alcanoil C1-6-amino, di(alquil C1-6)aminocarbonilo, di(alquil C1-6)aminoalquil C1-6-aminocarbonilo, hidroindenilaminocarbonilo, difenilmetilaminocarbonilo, pirrolidincarbonilo, alcoxi C1-6-alquil C1-6-aminocarbonilo, morfolincarbonilo, piperazinacarbonilo, fenilalquil C1-6-aminocarbonilo, hidroxicarbonilalquil C1-6-aminocarbonilo, cicloalquil C3-8-aminocarbonilo, cicloalquil C3-8-alquil C1-6-aminocarbonilo, hidroxialquil C1-6-aminocarbonilo, carboxietilaminocarbonilo, alquil C1-6-sulfonilaminocarbonilo), -CR41=N-NH- (donde R41 es hidrogeno, amino o alcanoil C1-6-amino), -CR42=N-C=N- (donde R42 es hidrogeno o amino); o una sal del mismo; un medicamento, una composicion farmacéutica, un inhibidor de la quinasa betaIkappaB, un medicamento anti-inflamatorio, un inmunosupresor, un medicamento para la isquemia, un medicamento anti-tumoral y el uso de dichos derivados para la preparacion de un medicamento.
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MA43373A (fr) | 2015-12-04 | 2018-10-10 | Global Blood Therapeutics Inc | Régimes posologiques pour 2-hydroxy-6-((2- (1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)méthoxy)benzaldéhyde |
AR108435A1 (es) | 2016-05-12 | 2018-08-22 | Global Blood Therapeutics Inc | Proceso para sintetizar 2-hidroxi-6-((2-(1-isopropil-1h-pirazol-5-il)-piridin-3-il)metoxi)benzaldehído |
EA036446B1 (ru) | 2016-06-14 | 2020-11-11 | Новартис Аг | Соединения и композиции для подавления активности shp2 |
KR20190024983A (ko) | 2016-06-29 | 2019-03-08 | 오토노미, 인코포레이티드 | 트리글리세라이드 귀 제제 및 이의 용도 |
TWI778983B (zh) | 2016-10-12 | 2022-10-01 | 美商全球血液治療公司 | 包含2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)吡啶-3-基)甲氧基)-苯甲醛之片劑 |
CN107417605A (zh) * | 2017-08-02 | 2017-12-01 | 江苏艾立康药业股份有限公司 | 作用于脯氨酰羟化酶的吡啶衍生化合物 |
RU2669348C1 (ru) * | 2017-11-15 | 2018-10-10 | Федеральное государственное автономное образовательное учреждение высшего образования "Белгородский государственный национальный исследовательский университет" (НИУ "БелГУ") | Способ ингибирования нуклеарного фактора каппа В с использованием 2-этил-6-метил-3-гидроксипиридиния L-2,6-диаминогексаноата в культуре клеток |
WO2019173653A1 (en) | 2018-03-07 | 2019-09-12 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
WO2020072377A1 (en) | 2018-10-01 | 2020-04-09 | Global Blood Therapeutics, Inc. | Modulators of hemoglobin for the treatment of sickle cell disease |
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US4003908A (en) * | 1976-03-11 | 1977-01-18 | E. R. Squibb & Sons, Inc. | Derivatives of imidazo(4,5-b)pyridines |
PE20010635A1 (es) * | 1999-10-08 | 2001-08-15 | Smithkline Beecham Corp | Inhibidores de fab i utiles para el tratamiento de infecciones bacterianas |
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