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AR083724A1 - AZAESPIROHEXANONAS INHIBIDORAS DE LA 11b-HSD1 (11-b-HIDROXIESTEROIDE DESHIDROGENASA) UTILES PARA TRATAR DIABETES Y OTROS TRASTORNOS METABOLICOS, Y COMPOSICIONES FARMACEUTICAS QUE LAS CONTIENEN - Google Patents

AZAESPIROHEXANONAS INHIBIDORAS DE LA 11b-HSD1 (11-b-HIDROXIESTEROIDE DESHIDROGENASA) UTILES PARA TRATAR DIABETES Y OTROS TRASTORNOS METABOLICOS, Y COMPOSICIONES FARMACEUTICAS QUE LAS CONTIENEN

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Publication number
AR083724A1
AR083724A1 ARP110102223A ARP110102223A AR083724A1 AR 083724 A1 AR083724 A1 AR 083724A1 AR P110102223 A ARP110102223 A AR P110102223A AR P110102223 A ARP110102223 A AR P110102223A AR 083724 A1 AR083724 A1 AR 083724A1
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cycloalkyl
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Frank Himmelsbach
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Boehringer Ingelheim Int
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    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
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    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

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Abstract

Reivindicación 1: Compuestos caracterizados porque tienen la fórmula (1), en la que R1 se selecciona del grupo R1a que consiste en H, alquil C1-6-, cicloalquil C3-6-, alquenil C2-6- y alquinil C2-6-, en el que un grupo -CH2- del grupo alquil C1-6- o grupo cicloalquil C3-6 anteriormente mencionados está sustituido opcionalmente por -O-, y en el que los grupos alquil C1-6-, alquenil C2-6-, alquinil C2-6- y cicloalquil C3-6- anteriormente mencionados pueden estar sustituidos opcionalmente con uno a tres F; R2 se selecciona del grupo R2a que consiste en: H y alquil C1-4-, en el que el grupo alquil C1-4- anteriormente mencionado puede estar sustituido opcionalmente con uno a tres F, o, R1a y R2a forman juntos un puente alquileno C2-5, en el que, en caso de que el grupo alquileno anteriormente mencionado contenga más de 2 grupos -CH2-, un grupo -CH2- puede estar sustituido opcionalmente por -O-; R3 se selecciona del grupo R3a que consiste en el grupo de formulas (2), H, F, fenilo, naftilo, pirrolilo, furanilo, tienilo, tetrazolilo, piridilo, indolilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo, en los que en el grupo pirrolilo, furanilo, tienilo, y piridilo 1 ó 2 grupos CH pueden estar sustituidos opcionalmente por N, y en los que en el grupo indolilo, benzofuranilo, benzotiofenilo, quinolinilo, e isoquinolinilo 1 a 3 grupos CH pueden estar sustituidos opcionalmente por N, y en los que todos los grupos anteriormente mencionados pueden estar sustituidos opcionalmente con uno o dos R10 que pueden ser idénticos o diferentes; R4 se selecciona independientemente entre sí del grupo R4a que consiste en H, halógeno, alquil C1-6, cicloalquil C3-6-, HO-, alquil C1-4-O-, HO-alquil C2-4-O-, H3CO-alquil C2-4-O-, NC-alquil C1-4-O-, cicloalquil C3-6-O-, tetrahidrofuranilo, tetrahidrofuranil-O-, tetrahidropiranil-, tetrahidropiranil-O-, NC-, HOOC-, alquil C1-4-OC(O)-, (R6)2N-C(O)-, alquil C1-4-S-, alquil C1-4-S(O)- y alquil C1-4-S(O)2-, en los que los grupos alquil C1-6-, alquil C1-4-O- y cicloalquil C3-6- anteriormente mencionados pueden estar sustituidos opcionalmente con uno a tres F, y en los que los grupos alquil C1-6- y cicloalquil C3-6- anteriormente mencionados pueden estar monosustituidos opcionalmente con HO-, H3CO-, NC-, HOOC-, alquil C1-4-OC(O)-, (R6)2N-C(O)-, alquil C1-4-S-, alquil C1-4-S(O)- o alquil C1-4-S(O)2-, y en los que dos de los grupos R4a anteriormente mencionados, con tal de que estén unidos a átomos de carbono adyacentes del anillo fenilo en la fórmula (1), pueden formar juntos un puente alquileno C3-5, en los que uno o dos grupos -CH2- del puente alquileno C3-5 anteriormente mencionado pueden estar sustituidos opcionalmente por cualquiera de los grupos seleccionados de -N(RN)-, -O-, y -C(O)-, y que pueden estar sustituidos opcionalmente con uno o dos grupos seleccionados independientemente de F y H3C-, y en los que dos de los grupos R4a anteriormente mencionados, con tal de que estén unidos a átomos de carbono adyacentes del anillo fenilo en la fórmula (1), pueden formar junto con los átomos de carbono a los que están unidos un anillo benzo, pirido, pirimido, pirazino, piridazino, pirazolo, imidazo, triazolo, oxazolo, tiazolo, isoxazolo, o isotiazolo, en los que cada uno de los anillos benzo, pirido, pirimido, pirazino, piridazino, pirazolo, imidazo, triazolo, oxazolo, tiazolo, isoxazolo, o isotiazolo anteriormente mencionados pueden estar sustituidos opcionalmente con uno o dos sustituyentes seleccionados independientemente entre sí de halógeno, alquil C1-4, FH2C-, F2HC-, F3C-, H2N-, alquil C1-4-NH-, (alquil C1-4)2N-, HO-, alquil C1-4-O-, FH2CO-, F2HCO-, F3CO- y NC-; A se selecciona del grupo Aa que consiste en un resto de formula (3) y -(CH2)4-6-, en el que un grupo -CH2-CH2- puede estar sustituido opcionalmente por un grupo -CH=CH-, y en el que los grupos anteriormente mencionados pueden estar sustituidos opcionalmente con uno a cuatro R5; R5 se selecciona independientemente entre sí del grupo R5a que consiste en halógeno, NC-, (R6)2N-, HO-, O=, alquil C1-6-, cicloalquil C3-6-, alquenil C2-6, alquinil C2-6-, HOOC-, alquil C1-4-OC(O)-, (R6)2N-C(O)-, alquil C1-4-S-, alquil C1-4-S(O)- y alquil C1-4-S(O)2-, en los que los grupos alquil C1-6- y cicloalquil C3-6-, alquenil C2-6- y alquinil C2-6 pueden estar sustituidos opcionalmente independientemente entre sí por uno a tres F y/o un sustituyente seleccionado del grupo que consiste en F, Cl, NC-, (R6)2N-, HO-, O=, alquil C1-4-, HOOC-, alquil C1-4-OC(O)-, (R6)2N-C(O)-, alquil C1-4-S-, alquil C1-4-S(O)- y alquil C1-4-S(O)2-, y en los que dos de los grupos R5a anteriormente mencionados pueden formar juntos un puente alquileno -(CH2)4-6-, en el que el puente alquileno -(CH2)4-6- anteriormente mencionado puede estar sustituido opcionalmente con uno o dos grupos seleccionados independientemente entre si del grupo que consiste en F, H3C-, HO-, y H3C-O-, y en el que uno o dos grupos -CH2- de dicho puente alquileno (CH2)4-6 pueden estar sustituidos opcionalmente por -O-; R6 se selecciona independientemente entre sí del grupo R6a que consiste en H y alquil C1-4; R7 se selecciona del grupo R7a que consiste en H, halógeno, alquil C1-4, F3C-, HO-, alquil C1-4-O-, NC-, o el grupo R7a anteriormente mencionado puede formar junto con R1 un puente -alquileno (CH2)2-4, en el que el puente -alquileno (CH2)2-4 anteriormente mencionado puede estar sustituido opcionalmente con uno o dos grupos seleccionados independientemente entre sí del grupo que consiste en F, H3C-, HO-, y H3C-O-, y en el que un grupo -CH2- puede estar sustituido opcionalmente por -O-; R10 se selecciona independientemente entre sí del grupo R10a que consiste en halógeno, alquil C1-4, cicloalquil C3-6-, FH2C, F2HC-, F3C-, NC-, H2N-C(O)-, alquil C1-4-NH-C(O)-, (alquil C1-4)2N-C(O)-, HO2C-, alquil C1-4-O-C(O)-, O2N-, H2N-, alquil C1-4-NH-, (alquil C1-4)2N-, H3CC(O)NH-, H3C-S(O)2-NH-, HO-, alquil C1-4-O-, FH2CO-, F2HC-O-, F3C-O-, H3C-S-, H3C-S(O)-, H3C-S(O)2-, en los que los grupos alquil C1-4- y cicloalquil C3-6- anteriormente mencionados pueden estar sustituidos opcionalmente con 1 ó 2 grupos seleccionados independientemente entre sí del grupo que consiste en F, H3C-, H3C-O-, -NC-, H2N-C(O)-, alquil C1-4-NH-C(O)-, (alquil C1-4)2N-C(O)- y HO-; Z se selecciona del grupo Za que consiste en -CH2-, -N(R6)- y -O-; RN se selecciona independientemente entre sí del grupo RNa que consiste en H, alquil C1-6-, cicloalquil C3-6-, alquenil C3-6-, alquinil C3-6-, alquil C1-4-C(O)-, cicloalquil C3-6-C(O)-, H2N-C(O)-, alquil C1-4-NH-C(O)-, (alquil C1-4)2N-C(O)-, alquil C1-4-O-C(O)-, alquil C1-4-S(O)2-, cicloalquil C3-6-S(O)2-, en los que los grupos alquil C1-6-, alquenil C3-6- y alquinil C3-6- anteriormente mencionados pueden estar opcionalmente mono- di- o trisustituidos con flúor; m significa 0, 1, 2 ó 3; o una sal de los mismos.
ARP110102223A 2010-06-25 2011-06-24 AZAESPIROHEXANONAS INHIBIDORAS DE LA 11b-HSD1 (11-b-HIDROXIESTEROIDE DESHIDROGENASA) UTILES PARA TRATAR DIABETES Y OTROS TRASTORNOS METABOLICOS, Y COMPOSICIONES FARMACEUTICAS QUE LAS CONTIENEN AR083724A1 (es)

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EP10167325 2010-06-25
EP10167958 2010-06-30

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AR083724A1 true AR083724A1 (es) 2013-03-20

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US (1) US8765744B2 (es)
EP (1) EP2585444B1 (es)
JP (1) JP5813106B2 (es)
AR (1) AR083724A1 (es)
TW (1) TW201213313A (es)
WO (1) WO2011161128A1 (es)

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