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AR078887A1 - Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina y composiciones farmaceuticas que los contienen. - Google Patents

Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina y composiciones farmaceuticas que los contienen.

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Publication number
AR078887A1
AR078887A1 ARP100104083A ARP100104083A AR078887A1 AR 078887 A1 AR078887 A1 AR 078887A1 AR P100104083 A ARP100104083 A AR P100104083A AR P100104083 A ARP100104083 A AR P100104083A AR 078887 A1 AR078887 A1 AR 078887A1
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AR
Argentina
Prior art keywords
oxo
dihydro
group
alkyl
optionally
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ARP100104083A
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English (en)
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Boehringer Ingelheim Int
Vitae Pharmaceuticals Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41683136&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR078887(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int, Vitae Pharmaceuticals Inc filed Critical Boehringer Ingelheim Int
Publication of AR078887A1 publication Critical patent/AR078887A1/es

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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
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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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    • C07D401/06—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 only aliphatic carbon atoms
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    • 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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    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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  • Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

En particular, los compuestos son inhibidores de 11beta-hidroxiesteroide deshidrogenasa (HSD) 1 y por lo tanto son adecuados para el tratamiento y prevencion de enfermedades que pueden influenciarse por la inhibicion de esta enzima, tal como enfermedades metabolicas, en particular diabetes tipo 2, obesidad y dislipidemia. Reivindicacion 1: Los compuestos de formula (1) en la que R1 se selecciona entre el grupo R1a que consiste en fenilo, naftilo, pirrolilo, furanilo, tienilo, piridilo, indolilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo, en el que en el grupo pirrolilo, furanilo, tienilo y piridilo, opcionalmente 1 o 2 grupos CH pueden estar reemplazados con N y en el que en el grupo indolilo, benzofuranilo, benzotiofenilo, quinolinilo e isoquinolinilo, de 1 a 3 grupos CH pueden estar reemplazados opcionalmente con N, 2-oxo-1,2-dihidro-piridinilo, 4-oxo-1,4-dihidro-piridinilo, 3-oxo-2,3-dihidro-piridazinilo, 3,6-dioxo-1,2,3,6-tetrahidro-piridazinilo, 2-oxo-1,2-dihidro-pirimidinilo, 4-oxo-3,4-dihidro-pirimidinilo, 1,2,3,4-tetrahidro-2,4-dioxo-pirimidinilo, 2-oxo-1,2-dihidro-pirazinilo, 2,3-dioxo-1,2,3,4-tetrahidro-pirazinilo, indanilo, 1-oxo-indanilo, 2,3-dihidro-indolilo, 2,3-dihidro-isoindolilo, 2-oxo-2,3-dihidro-indolilo, 1-oxo-2,3-dihidro-isoindolilo, 2,3-dihidrobenzofuranilo, 2-oxo-2,3-dihidro-benzoimidazolilo, 2-oxo-2,3-dihidro-benzoxazolilo, benzo[1,3]dioxolilo, 2-oxo-benzo[1,3]dioxolilo, 1,2,3,4-tetrahidro-naftilo, 1,2,3,4-tetrahidro-quinolinilo, 2-oxo-1,2,3,4-tetrahidro-quinolinilo, 2-oxo-1,2-dihidro-quinolinilo, 4-oxo-1,4-dihidro-quinolinilo, 1,2,3,4-tetrahidro-isoquinolinilo, 1-oxo-1,2,3,4-tetrahidro-isoquinolinilo, 1-oxo-1,2-dihidro-isoquinolinilo, 4-oxo-1,4-dihidro-cinnolinilo, 2-oxo-1,2-dihidro-quinazolinilo, 4-oxo-1,4-dihidro-quinazolinilo, 2,4-dioxo-1,2,3,4-tetrahidro-quinazolinilo, 2-oxo-1,2-dihidro-quinoxalinilo, 3-oxo-1,2,3,4-tetrahidro-quinoxalinilo, 2,3-dioxo-1,2,3,4-tetrahidro-quinoxalinilo, 1-oxo-1,2-dihidro-ftalazinilo, 1,4-dioxo-1,2,3,4-tetrahidro-ftalazinilo, cromanilo, coumarinilo, 2,3-dihidro-benzo[1,4]dioxin-ilo, 3-oxo-3,4-dihidro-benzo[1,4]oxazinilo, tetrazolilo, 2-oxo-2,3-dihidro-benzotiazolilo, e imidazo[1,2-a]piridinilo, en el que los miembros del grupo R1a están acoplados al grupo carbonitrilo en formula (1) mediante un átomo de carbono aromático y en el que los miembros del grupo R1a pueden estar opcionalmente sustituido con un R5, de uno a 3 R6 iguales y/o diferentes, y/o un R7, con la condicion de que en el caso de que R1 sea un grupo fenilo, los sustituyentes R5, R6 y/o R7 no estén acoplados con los átomos de carbono adyacentes al átomo de carbono que está acoplado con el grupo carbonitrilo en la formula (1); R2 se selecciona entre el grupo R2a que consiste en hidrogeno, halogeno, (het)arilo, ciano, nitro, amino, hidroxi, alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, y alquinilo C2-6, en el que en cada grupo alquil C1-6, cicloalquil C3-6, alquenil C2-6 o alquinil C2-6, un grupo CH2 puede estar opcionalmente reemplazado por CO o SO2, un grupo CH2 opcionalmente por O o NRN y un grupo CH opcionalmente por N y en el que cada uno de estos grupos puede estar opcionalmente mono- o polifluorado y opcionalmente mono- o independientemente de los otros disustituido con cloro, alquilo C1-3, ciano, (het)arilo, amino, alquilamino C1-3, di-(alquil C1-3)-amino, hidroxi, alquiloxi C1-3, (het)ariloxi, alquilsulfanilo C1-3, alquilsulfinilo C1-3 o cicloalquilo C3-6, en los que uno o dos grupos CH2 del grupo cicloalquilo C3-6 puede estar opcionalmente reemplazado independientemente de los otros con carbonilo, O o NRN y un grupo CH opcionalmente con N, y que puede estar independientemente mono- o independientemente disustituido con fluor o alquilo C1-3; R3, R4 se seleccionan, independientemente entre sí, entre el grupo R3/4a que consiste en hidrogeno, halogeno, alquilo C1-3, trifluorometilo, hidroxi, alquiloxi C1-3 y ciano o R3/4a representa R3 y R4 que están enlazados a átomos de carbono adyacentes y se unen para formar un grupo metilenodioxi, etilenodioxi o alquileno C3-5, cada uno de los cuales puede estar opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre fluor y metilo o, junto con los átomos de carbono a los que están acoplados, forman un anillo benzo, pirido, pirimido, pirazino, piridazino, pirazolo, imidazo, triazolo, oxazolo, tiazolo, isoxazolo o isotiazolo, cada uno de los cuales puede estar opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halogeno, alquilo C1-3, trifluorometilo, amino, alquilamino C1-3, di-(alquil C1-3)amino, hidroxi y alquiloxi C1-3; R5 se selecciona entre el grupo R5a que consiste en halogeno, (het)arilo, ciano, nitro, amino, hidroxi, alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6 y alquinilo C2-6, en el que en cada grupo, un grupo CH2 puede estar opcionalmente reemplazado con CO o SO2, un grupo CH2 opcionalmente con O o NRN y un grupo CH opcionalmente con N, y en el que cada uno de esos grupos puede estar opcionalmente mono- o polifluorado y opcionalmente mono- o disustituido independientemente de los otros con cloro, alquilo C1-3, ciano, (het)arilo, amino, alquilamino C1-3, di-(alquil C1-3)-amino, hidroxi, alquiloxi C1-3, (het)ariloxi, alquilsulfanilo C1-3, alquilsulfinilo C1-3 o cicloalquilo C3-6, en el que uno o dos grupos CH2 del grupo cicloalquilo C3-6 puede estar opcionalmente reemplazado independientemente de los otros con carbonilo, O o NRN y un grupo CH opcionalmente con N, y que puede estar opcionalmente mono- o independientemente disustituido con fluor o alquilo C1-3; R6, R7 se seleccionan, independientemente entre sí, entre el grupo R6/7a que consiste en halogeno, alquilo C1-3, alquinilo C2-3, trifluorometilo, hidroxi, alquiloxi C1-3 y ciano y/o R6/7a representa un R6 combinado con R7, que están unido a átomos de carbono adyacentes, que forman un grupo metilenodioxi, difluorometilenodioxi, etilenodioxi, alquileno C3-5, o forman, junto con los átomos de carbono a los que están acoplados, un anillo pirazolo, imidazo, oxazolo, isoxazolo, tiazolo o isotiazolo, cada uno de los cuales puede estar opcionalmente mono- o disustituido independientemente de los otros con alquilo C1-3, trifluorometilo, amino, alquilamino C1-3, di-(alquil C1-3)amino, hidroxi, alquiloxi C1-3; RN se selecciona, independientemente entre sí, entre el grupo RNa que consiste en hidrogeno, alquilo C1-6, cicloalquilo C3-6, alquenilo C3-6, alquinilo C3-6, (het)arilo, alquilcarbonilo C1-4, (het)arilcarbonilo, alquilaminocarbonilo C1-4, di-(alquil C1-3)-aminocarbonilo, (het)arilaminocarbonilo, alquiloxicarbonilo C1-4, alquilsulfonilo C1-4 y (het)arilsulfonilo, en el que cada grupo alquilo, alquenilo y alquinilo puede estar opcionalmente mono- o polisustituido con fluor y opcionalmente monosustituido con (het)arilo, ciano, aminocarbonilo, alquilaminocarbonilo C1-3, di-(alquil C1-3)aminocarbonilo, carboxi, alquiloxicarbonilo C1-4, amino, alquilamino C1-4, di-(alquil C1-3)amino, alquilcarbonilamino C1-4, hidroxi, alquiloxi C1-4, alquilsulfanilo C1-4, alquilsulfinilo C1-4, o alquilsulfonilo C1-4; (het)arilo se selecciona, independientemente entre sí, entre el grupo HAa que consiste en fenilo, naftilo, pirrolilo, furanilo, tienilo, piridilo, indolilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo, en el que en el grupo pirrolilo, furanilo, tienilo y piridilo, opcionalmente 1 o 2 grupos CH pueden estar reemplazados con N, y en el que en el grupo indolilo, benzofuranilo, benzotiofenilo, quinolinilo e isoquinolinilo, de 1 a 3 grupos CH pueden estar reemplazados opcionalmente con N, 2-oxo-1,2-dihidro-piridinilo, 4-oxo-1,4-dihidro-piridinilo, 3-oxo-2,3-dihidro-piridazinilo, 3,6-dioxo-1,2,3,6-tetrahidro-piridazinilo, 2-oxo-1,2-dihidro- pirimidinilo, 4-oxo-3,4-dihidro-pirimidinilo, 2,4-dioxo-1,2,3,4-tetrahidro-pirimidinilo, 2-oxo-1,2-dihidro-pirazinilo, 2,3-dioxo-1,2,3,4-tetrahidro- pirazinilo, 2-oxo-2,3-dihidro-indolilo, 2,3-dihidrobenzo-furanilo, 2-oxo-2,3-dihidro-benzoimidazolilo, 2-oxo-2,3-dihidro-benzoxazolilo, 2-oxo-1,2- dihidro-quinolinilo, 4-oxo-1,4-dihidro-quinolinilo, 1-oxo-1,2-dihidro-isoquinolinilo, 4-oxo-1,4-dihidro-cinnolinilo, 2-oxo-1,2-dihidro-quinazolinilo, 4-oxo-1,4-dihidro-quinazolinilo, 2,4-dioxo-1,2,3,4-tetrahidro-quinazolinilo, 2-oxo-1,2-dihidro-quinoxalinilo, 3-oxo-1,2,3,4-tetrahidro-quinoxalinilo, 2,3-dioxo-1,2,3,4-tetrahidro-quinoxalinilo, 1-oxo-1,2-dihidro-ftalazinilo, 1,4-dioxo-1,2,3,4-tetrahidro-ftalazinilo, cromanilo, coumarinilo, 2,3-dihidro-benzo[1,4jdioxinilo, 3-oxo-3,4-dihidro-benzo[1,4]oxazinilo y tetrazolilo, y en el que los grupos (het)arilo mencionados anteriormente pueden estar opcionalmente sustituidos con uno a tres R10 que pueden ser iguales o diferentes; R10 se selecciona, independientemente entre sí, entre el grupo R10a que consiste en halogeno, alquilo C1-3, difluorometilo, trifluorometilo, ciano, aminocarbonilo, alquilaminocarbonilo C1-3, di-(alquil C1-3)-aminocarbonilo carboxi, alquiloxicarbonilo C1-4, nitro, amino, alquilamino C1-3, di-(alquil C1-3)amino, acetilamino, metilsulfonilamino, hidroxi, alquiloxi C1-3, difluorometoxi, trifluorometoxi, metilsulfanilo, metilsulfinilo, metilsulfonilo, aminosulfonilo y fenilo, en el que el grupo fenilo puede estar opcionalmente sustituido con 1 o 2 sustituyentes independientemente seleccionados de los otros entre fluor, metilo, metoxi, ciano e hidroxi; m representa 0 o 1; y en el que la parte alifática de la estructura de nucleo tricíclico de formula general (1) está sustituida con uno o dos grupos iguales o diferentes R8 se selecciona, independientemente entre sí, entre el grupo R8a que consiste en hidrogeno, metilo y etilo; los tautomeros de los mismos, los estereoisomeros de los mismos, las mezclas de los mismos y las sales de los mismos, aunque los siguientes compuestos de formulas (2) a (4) están excluidos.
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