AR081905A1 - Compuestos de picolinamida y de pirimidina-4-carboxamida, proceso para prepararlos y composicion farmaceutica que los comprende - Google Patents
Compuestos de picolinamida y de pirimidina-4-carboxamida, proceso para prepararlos y composicion farmaceutica que los comprendeInfo
- Publication number
- AR081905A1 AR081905A1 ARP110101580A AR081905A1 AR 081905 A1 AR081905 A1 AR 081905A1 AR P110101580 A ARP110101580 A AR P110101580A AR 081905 A1 AR081905 A1 AR 081905A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- integer
- heterocycle
- alkoxy
- Prior art date
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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Abstract
Uso médico de dichos compuestos como agentes para prevenir, regular o tratar enfermedades relacionadas con la regulación de los glucocorticoides, mediante el uso de la actividad de inhibición selectiva de los compuestos sobre las enzimas 11b-HSD1. Los compuestos de picolinamida y de pirimidina-4-carboxamida de la presente solicitud son inhibidores selectivos de las enzimas 11b-HSD1 de origen humano, por lo que son útiles como agentes para prevenir, regular o tratar aquellas enfermedades relacionadas con la regulación de los glucocorticoides en las que participan las enzimas 11b-HSD1 de origen humano, por ejemplo, los síndromes metabólicos, tales como la diabetes tipo 1 o tipo 2, las complicaciones posteriores a la diabetes, la diabetes autoinmune latente en adultos (LADA), los síndromes de tolerancia a la insulina, la obesidad, la tolerancia alterada a la glucosa (IGT), la glucosa alterada en ayunas (IFG), la tolerancia dañada a la glucosa, la dislipidemia, la aterosclerosis, la hipertensión, etcétera.Reivindicación 1: Un compuesto amida representado por la fórmula (1), o una sal aceptable farmacéuticamente, solvato, hidrato, prodroga, racemato o estereoisómero del mismo, [en la fórmula (1), X representa N o CR, e Y representa N o CH, siempre que X e Y no sean carbono al mismo tiempo; Z representa N o CH; R1 y R2 representan en forma independiente hidrógeno, alquilo C1-10, cicloalquilo C3-10, norbornilo, adamantilo, noradamantilo, arilo C6-20, arilo C6-20-alquilo C1-10, o heteroarilo C3-20, o R1 y R2 pueden estar unidos entre sí, junto con los átomos de nitrógeno a los cuales están unidos, para formar heterociclo C1-10, biheterociclo o heterociclo fusionado saturado o insaturado, siempre que R1 y R2 no sean ambos hidrógeno al mismo tiempo; L representa una unión simple, -O-, -NR11-, -CO-, -SO2-, -(CR21R22)-(CH2)c- (c representa un entero entre 0 y 5), -CO(CR21R22)d- (d representa un entero entre 1 y 6), cicloalquileno C3-10, arileno C6-20 o heteroarileno C3-20; R21 y R22 representan en forma independiente hidrógeno o alquilo C1-10, o R21 y R22 pueden estar unidos a través de alquileno o alquenileno para formar un anillo cicloalifático o un anillo aromático; R y R3 representan en forma independiente hidrógeno, alquilo C1-10, cicloalquilo C3-10, alcoxi C1-10, halógeno, hidroxi, ciano, -NR31R32, nitro, -CONH2, -CO2R33, -SO3H, -SO2NR34R35, -SO2R36, -O(CH2)aCO2H (a representa un entero entre 1 y 3), -O(CH2)bCONH2 (b representa un entero entre 1 y 3), -NH(CO)R37, -NH(SO2)R38, heterociclo de entre 5 y 7 miembros, arilo C6-20 o heteroarilo C3-20; R4 y R5 representan en forma independiente hidrógeno, alquilo C1-10, cicloalquilo C3-10, alcoxi C1-10, halógeno, hidroxi, ciano, amino, nitro, -CONH2 o -CO2R12, e incluyen todos los isómeros y compuestos racémicos de los mismos, o R4 y R5 pueden estar sustituidos con átomos de carbono adyacentes para formar carbociclo C1-10, heterociclo, bicarbociclo, biheterociclo, carbociclo fusionado, o heterociclo fusionado saturado o insaturado, o pueden estar unidos a R3 para carbociclo saturado o insaturado; R6 y R7 representan en forma independiente hidrógeno, alquilo C1-10, cicloalquilo C3-10, alcoxi C1-10, halógeno, hidroxi, ciano, amino, nitro, -CONH2 o -CO2R12; el cicloalquileno, arileno o heteroarileno de L; el alquilo, cicloalquilo, norbornilo, adamantilo, noradamantilo, arilo, aralquilo o heteroarilo de R1 y R2; el heterociclo, biheterociclo o heterociclo fusionado saturado o insaturado formado por la unión de R1 y R2; el alquilo, cicloalquilo, alcoxi, heterociclo, arilo o heteroarilo de R y R3; el alquilo, cicloalquilo o alcoxi de R4 y R5; el carbociclo, heterociclo, bicarbociclo, biheterociclo, carbociclo fusionado o heterociclo fusionado saturado o insaturado formado por la sustitución de R4 y R5 con átomos de carbono adyacentes; y el alquilo, cicloalquilo o alcoxi de R6 y R7 puede estar adicionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en alquilo C1-10, cicloalquilo C3-10, alcoxi C1-10, haloalquilo C1-10, haloalcoxi C1-10, halógeno, hidroxi, ciano, -NR41R42, nitro, -CO2R43, -CONH2, -SO3H, -SO2NR44R45, -SO2(CH2)cNR44R45 (c representa un entero entre 1 y 3), -SO2R46, -O(CH2)cCO2H (c representa un entero entre 1 y 3), -O(CH2)dCONH2 (d representa un entero entre 1 y 3), -NH(CO)R47, -NH(SO2)R48, arilo C6-20 y heteroarilo C3-20; R11, R12, R31, R32, R33, R34, R35, R36, R37, R38, R41, R42, R43, R44, R45, R46, R47 y R48 representan en forma independiente hidrógeno, alquilo C1-10, cicloalquilo C3-10 o arilo C6-20; y m y n representan en forma independiente un entero entre 0 y 3, siempre que m + n represente un entero mayor o igual a 2].
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KR20100043168 | 2010-05-07 | ||
KR20110037758A KR20110123657A (ko) | 2010-05-07 | 2011-04-22 | 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물 |
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BR112012028527A2 (pt) | 2020-08-25 |
MX336376B (es) | 2016-01-15 |
EP2566859A4 (en) | 2014-07-30 |
BR112012028527B1 (pt) | 2021-10-05 |
CA2798360C (en) | 2018-10-30 |
CN103025721A (zh) | 2013-04-03 |
RU2566827C2 (ru) | 2015-10-27 |
WO2011139107A3 (en) | 2012-05-18 |
BR112012028527B8 (pt) | 2021-10-26 |
JP5837573B2 (ja) | 2015-12-24 |
AU2011249167B2 (en) | 2016-02-25 |
KR20110123657A (ko) | 2011-11-15 |
CN103025721B (zh) | 2015-06-17 |
TW201144294A (en) | 2011-12-16 |
TWI491603B (zh) | 2015-07-11 |
ZA201208198B (en) | 2014-01-29 |
AU2011249167A1 (en) | 2012-11-29 |
US9096571B2 (en) | 2015-08-04 |
SA111320433B1 (ar) | 2015-06-10 |
EP2566859A2 (en) | 2013-03-13 |
JP2013525479A (ja) | 2013-06-20 |
WO2011139107A2 (en) | 2011-11-10 |
EP2566859B1 (en) | 2016-12-21 |
MX2012012972A (es) | 2013-02-26 |
US20130210811A1 (en) | 2013-08-15 |
RU2012152639A (ru) | 2014-06-20 |
CA2798360A1 (en) | 2011-11-10 |
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