ES2318577T3 - Derivados de cicloalquil lactama como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1'. - Google Patents

Derivados de cicloalquil lactama como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1'. Download PDF

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ES2318577T3
ES2318577T3 ES05819201T ES05819201T ES2318577T3 ES 2318577 T3 ES2318577 T3 ES 2318577T3 ES 05819201 T ES05819201 T ES 05819201T ES 05819201 T ES05819201 T ES 05819201T ES 2318577 T3 ES2318577 T3 ES 2318577T3
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lactama
cyclalkyl
inhibitors
beta
derivatives
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Thomas D. Aicher
Mark Joseph Chicarelli
Ronald Jay Hinklin
Hongqi Tian
Owen Brendan Wallace
Zhaogen Chen
Thomas Edward Mabry
Jefferson Ray Mccowan
Nancy June Snyder
Leonard Larry Junior Winneroski
John Gordon Allen
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Eli Lilly and Co
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    • C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
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    • C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
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    • C07—ORGANIC CHEMISTRY
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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
    • C07D401/10—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 carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

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Abstract

Un compuesto representado estructuralmente por la fórmula (I): ** ver fórmula** o una sal farmacéuticamente aceptable del mismo, en la que G 1 es metileno o etileno; L es grupo de engarce divalente seleccionado entre alquileno C 1-C 4, -S-, -CH(OH)-, y -O-; R 1 es hidrógeno, hidroxi, -alquilo (C1-C4) (opcionalmente sustituido con de uno a tres halógenos), -alcoxi (C1- C6) (opcionalmente sustituido con de uno a tres halógenos), o -CH2OR 7 , en la que R 7 es hidrógeno o -alquilo (C1-C4) (opcionalmente sustituido con de uno a tres halógenos); R 1a es hidrógeno o -CH3 (opcionalmente sustituido con de uno a tres halógenos); R 2 es ** ver fórmula** en las que la línea discontinua representa el punto de unión a la posición R 2 en la fórmula I; en la que X es hidrógeno, hidroxi, -O-CH3, -CH2OH, o -O-C(O)-fenil-NO2; en la que Y es hidrógeno o metilo, con la condición de que al menos uno de X e Y no sea hidrógeno; en la que opcionalmente X e Y junto con el carbono al que están unidos forman carbonilo; en la que R 8 es independientemente hidrógeno, hidroxi, o -alquilo (C1-C4); R 9 es independientemente hidrógeno, hidroxi, -alquilo (C1-C4), o fenilo; R 10 es independientemente en cada aparición hidrógeno, hidroxi, o -alquilo (C1-C4); y G 2 es metileno, etileno, o 1-propileno; R 3 es hidrógeno, hidroxilo (con la condición de que cuando L es -S- o -CH(OH)- entonces R 3 no puede ser hidroxi), o -alquilo (C1-C4) (opcionalmente sustituido con de uno a tres halógenos); cada uno de R 4 y R 5 es independientemente hidrógeno, hidroxi, -C(O)OH, -alquilo (C1-C4) (opcionalmente sustituido con de uno a tres halógenos), -alcoxi (C1- C6) (opcionalmente sustituido con de uno a tres halógenos), halógeno, ciano, -CF3, -OCF3, -alquil (C1-C4)-C(O)OH, -alquil (C 1-C 4)-C(O)Oalquil (C 1-C 4), o -alquil (C 1-C 4)-OH; R 5a y R 5b son independientemente hidrógeno o halógeno; R 6 es hidrógeno, hidroxi, -alquilo (C1-C4) (opcionalmente sustituido con de uno a tres halógenos), -alcoxi (C1- C6) (opcionalmente sustituido con de uno a tres halógenos), -O-alquinilo (C2-C6), halógeno, ciano, -NH2, -CF3, -SCF3, -C(O) Oalquil (C1-C4), -cicloalquilo (C3-C8), -O-SO2-alquilo (C1-C4), -O-SO2-CF3, -O-fenilo, -O-alquil (C1- C 4)-fenilo, -O-fenil-C(O)O-alquilo (C 1-C 4), -O-alquil (C 1-C 4)-fenil-C(O)O-alquilo (C 1-C 4), -NH-fenilo, -CH 2-fenilo, -O-(C 1-C 4) alquil-piridinilo, Ar 1 , Het 1 , Ar 2 , Het 2 , -C(O)alquilo (C 1-C 4), -C(O)-Ar 2 , -C(O)-Het 2 , -NHSO 2-alquilo (C 1- C4), -NHSO2-fenil(R 19 )(R 19 ), -alquil (C1-C4)-C(O)N(R 11 )(R 12 ), o alquil (C1-C4)-N(R 13 )(R 14 ); en la que cada uno de R 11 y R 12 es independientemente hidrógeno o -alquilo (C1-C4), o R 11 y R 12 tomados junto con el nitrógeno al que están unidos forman piperidinilo, piperazinilo, o pirrolidinilo (donde opcionalmente el anillo de piperidinilo, piperazinilo, o pirrolidinilo está sustituido una vez con -alquilo (C 1-C 4)); en la que cada uno de R 13 y R 14 es independientemente hidrógeno o -alquil (C 1-C 4) (opcionalmente sustituido con de uno a tres halógenos), o R 13 y R 14 tomados junto con el nitrógeno al que están unidos forman piperidinilo, pirrolidinilo, o piperazinilo; con la condición de que cuando L es -O- o -S-, entonces R 6 no es hidrógeno; Ar 1 es fenilo o naftilo; Ar 2 es Ar 1 opcional e independientemente sustituido de una a tres veces con halógeno, hidroxi, -C(O)OH, -alcoxi (C1-C6), ciano, -CF3, -alquilo (C1-C4), -alquil (C1-C4)-C(O)OH, -Oalquil (C1-C4)-C(O)OH, -alquil (C1-C4)- N(R 15 )(R 16 ), -O-alquil (C 1-C 4)-N(R 15 )(R 16 ), -O-alquil (C 1-C 4)-C(O)O-alquilo (C 1-C 4), -O-alquil (C 1-C 4)-piperidinilo, imidazolilo, piridinilo, o -alquil (C 1-C 4)-imidazolilo; en la que cada uno de R 15 y R 16 es independientemente hidrógeno o -alquilo (C1-C4), o R 15 y R 16 tomados junto con el nitrógeno al que están unidos forman piperidinilo, pirrolidinilo, morfolinilo, o imidazolilo; Het 1 es independientemente imidazolilo, oxadiazolilo, pirazolilo, pirrolilo, tetrazolilo, tiadiazolilo, triazolilo, pirrolidinilo, morfolinilo, piridinilo, piperidinilo, pirimidinilo, pirazinilo, piperazinilo, piridazinilo, furanilo, tiofenilo, tiazolilo, oxazolilo, isoxazolilo, isotiazolilo, indolilo, isoindolilo, indolinilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo, quinoxalinilo, quinazolinilo, o ftalazinilo; Het 2 es Het 1 opcional e independientemente sustituido de una a tres veces con halógeno, hidroxi, -alcoxi (C1-C6) (opcionalmente sustituido con de uno a tres halógenos), -C(O)OH, -NH2, ciano, -CF3, -alquilo (C1-C4) (opcionalmente sustituido con de uno a tres halógenos), -alquil (C1-C4)-C(O)OH, -Oalquil (C1-C4)-C(O)OH, -C(O)O-alquilo (C1-C4), -alquil (C 1-C 4)-N(R 17 )(R 18 ), -Oalquil (C 1-C 4)-N(R 17 )(R 18 ), imidazolilo, piridinilo, o -alquil (C 1-C 4)-imidazolilo; en la que cada uno de R 17 y R 18 es independientemente hidrógeno o -alquilo (C 1-C 4) (opcionalmente sustituido con de uno a tres halógenos), o R 17 y R 18 tomados junto con el nitrógeno al que están unidos forman piperidinilo o pirrolidinilo; R 19 es hidrógeno, halógeno, o -alquilo (C1-C4) (opcionalmente sustituido con de uno a tres halógenos); y R 20 es hidroxi, -alquilo (C 1-C 4) (opcionalmente sustituido con de uno a tres halógenos), -CH 2OH, o fenilo; con la condición de que un compuesto de fórmula (I) no sea 1-ciclohexil-3-fenoxi-pirrolidin-2-ona o 1-ciclohexil-3-fenilsulfanil-pirrolidin-2-ona.
ES05819201T 2004-10-29 2005-10-26 Derivados de cicloalquil lactama como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1'. Expired - Lifetime ES2318577T3 (es)

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US20080275043A1 (en) 2008-11-06
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US7713979B2 (en) 2010-05-11
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