AR076936A1 - Inhibidores de carbamato y urea de la 11 beta hidroxiesteroide deshidrogenasa 1 - Google Patents

Inhibidores de carbamato y urea de la 11 beta hidroxiesteroide deshidrogenasa 1

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AR076936A1
AR076936A1 ARP100101907A ARP100101907A AR076936A1 AR 076936 A1 AR076936 A1 AR 076936A1 AR P100101907 A ARP100101907 A AR P100101907A AR P100101907 A ARP100101907 A AR P100101907A AR 076936 A1 AR076936 A1 AR 076936A1
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Argentina
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optionally substituted
heterocyclyl
cycloalkyl
alkyl
heteroaryl
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ARP100101907A
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Vitae Pharmaceuticals Inc
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
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    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
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    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D471/04—Ortho-condensed systems

Abstract

Compuestos que son utiles para el tratamiento terapéutico de enfermedades asociadas con la modulacion o inhibicion de 11beta-HSD1 en mamíferos, también se refiere a composiciones farmacéuticas de los compuestos y a métodos para su uso en la reduccion o control de la produccion de cortisol en una célula o la inhibicion de la conversion de cortisona en cortisol en una célula. Reivindicacion 1: Un compuesto de formula 1 en la que Cy es bicicloalquilo C7-1) o tricicloalquilo C9-12, en el que 1-2 átomos de carbono están opcionalmente reemplazados con un heteroátomo seleccionado independientemente entre N y O, y que está opcionalmente sustituido con 1-3 grupos seleccionados independientemente entre halogeno, nitro, ciano, alquilo C1-3, haloalquilo C1-3, hidroxialquilo C1-3, OR4, haloalcoxi C1-3, N(R4)2, (CH2)xC(=NOH)NH2, (CH2)xNR4CON(R4)2, (CH2)xCON(R4)2, (CH2)xCO2R4, (CH2)xSO2N(R4)2, (CH2)xSO2R4, (CH2)xNR4COR4, (CH2)xNR4CO2R4, (CH2)xNR4SO2R4, (CH2)xOC(=O)N(R4)2, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido y cicloalquilo opcionalmente sustituido, donde el arilo, heteroarilo, heterociclilo y cicloalquilo están opcionalmente sustituidos con uno a tres grupos representados por R7; B es arilo, heterociclilo o heteroarilo, cada uno opcionalmente sustituido con 1-4 grupos representados por R6; R3 es alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilalquilo C0-3, heterociclilalquilo C0-3, arilalquilo C0-3, heteroarilalquilo C0-3 o (CH2)xCO2R4, cada uno opcionalmente sustituido con 1-4 grupos seleccionados independientemente entre halogeno, nitro, ciano, alquilo C1-3, haloalquilo C1-3, haloalcoxi C1-3, hidroxialquilo C1-3, OR4, N(R4)2, (CH2)xC(=NOH)NH2, (CH2)xNR4CON(R4)2, (CH2)xCON(R4)2, (CH2)xCO2R4, (CH2)xSO2N(R4)2, (CH2)xSO2R4, (CH2)xNR4COR4, (CH2)xNR4CO2R4, (CH2)xNR4SO2R4, (CH2)xOC(=O)N(R4)2, (CH2)xOR4, (CH2)xO(CH2)xCO2R4, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido y cicloalquilo opcionalmente sustituido, donde el arilo, heteroarilo, heterociclilo y cicloalquilo están opcionalmente sustituidos con uno a tres grupos representados por R7, donde el alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, heterociclilo, heteroarilo, cicloalquilalquilo C0-3, heterociclilalquilo C0-3, la porcion del alquilo arilalquilo C0-3 y heteroarilalquilo C0-3 están opcionalmente sustituidos adicionalmente con oxo; cada R4 es independientemente (a) hidrogeno; o (b) alquilo C1-10 o arilalquilo C0-3, cada uno opcionalmente sustituido con 1-4 grupos seleccionados entre halogeno, alcoxi C1-3, alquilo C1-3, haloalquilo C1-3, haloalcoxi C1-3, ciano y nitro; cada R6 se selecciona independientemente entre halogeno, nitro, ciano, alquilo C1-3, cicloalquilo C3-6, haloalquilo C1-3, hidroxialquilo C1-3, oxo, OR4, haloalcoxi C1-3, (CH2)xN(R4)2, (CH2)xC(=NOH)NH2, (CH2)xNR4CON(R4)2, (CH2)xCON(R4)2, (CH2)xCO2R4, (CH2)xSO2N(R4)2, (CH2)xSO2R4, (CH2)xNR4COR4, (CH2)xNR4CO2R4, (CH2)xNR4SO2R4, (CH2)xOC(=O)N(R4)2, (CH2)xOR4, (CH2)xO(CH2)xCO2R4, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido y cicloalquilo opcionalmente sustituido, donde el arilo, heteroarilo, heterociclilo y cicloalquilo están opcionalmente sustituidos adicionalmente con uno a tres grupos representados por R7; R7 es halogeno, nitro, ciano, alquilo C1-3, haloalquilo C1-3, cicloalquilo C3-6, alcoxi C1-3, haloalcoxi C1-3, N(R4)2 o CON(R4)2, con la condicion de que R7 también incluya oxo cuando el heteroarilo, heterociclilo y cicloalquilo estén sustituidos con R7; x es 0, 1, 2 o 3; A' es un enlace, CH2, o -AO-, donde O está conectado a B; A es un enlace o CH2; m es 0 ,1, 2 0 3; y n es 1, 2 o 3; o una sal farmacéuticamente aceptable del mismo. Con la condicion de que el compuesto de formula 1 no es como en formula (2) o (3), o una sal farmacéuticamente aceptable del mismo.
ARP100101907A 2009-06-02 2010-05-31 Inhibidores de carbamato y urea de la 11 beta hidroxiesteroide deshidrogenasa 1 AR076936A1 (es)

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EP (1) EP2438043A1 (es)
JP (1) JP5850459B2 (es)
AR (1) AR076936A1 (es)
TW (1) TW201103910A (es)
WO (1) WO2010141424A1 (es)

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AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
EP2229368A1 (en) 2007-12-11 2010-09-22 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11beta-hydroxysteroid dehydrogenase 1
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
EP2252601B1 (en) 2008-01-24 2012-12-19 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5730021B2 (ja) 2008-02-15 2015-06-03 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤としてのシクロアルキルラクタム誘導体
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JP5538365B2 (ja) 2008-05-01 2014-07-02 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
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CN102105454A (zh) 2008-07-25 2011-06-22 贝林格尔.英格海姆国际有限公司 合成1型11β-羟基类固醇脱氢酶的抑制剂
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