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AR069545A1 - Derivados de aril y heteroarilcarbonilo de benzomorfanos y estructuras relacionadas, composiciones farmaceuticas que contienen dichos compuestos, obtencion de las mismas, su uso en el tratamiento de enfermedades mediadas por la inhibicion de la enzima 11beta-hidroxiesteroide deshidrogenasa (hsd) 1 y - Google Patents

Derivados de aril y heteroarilcarbonilo de benzomorfanos y estructuras relacionadas, composiciones farmaceuticas que contienen dichos compuestos, obtencion de las mismas, su uso en el tratamiento de enfermedades mediadas por la inhibicion de la enzima 11beta-hidroxiesteroide deshidrogenasa (hsd) 1 y

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Publication number
AR069545A1
AR069545A1 ARP080104991A ARP080104991A AR069545A1 AR 069545 A1 AR069545 A1 AR 069545A1 AR P080104991 A ARP080104991 A AR P080104991A AR P080104991 A ARP080104991 A AR P080104991A AR 069545 A1 AR069545 A1 AR 069545A1
Authority
AR
Argentina
Prior art keywords
oxo
alkyl
piperazin
3alkyl
dihydro
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Suspension/Interruption
Application number
ARP080104991A
Other languages
English (en)
Inventor
Frank Himmelsbach
Bradford S Hamilton
Matthias Zentgraf
Herbert Nar
Annette Schuler-Metz
Armin Heckel
Matthias Eckhardt
Joerg Kley
Thorsten Lehmann-Linz
Stefan Peters
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH Co KG
Original Assignee
Boehringer Ingelheim Pharma GmbH Co KG
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Filing date
Publication date
Application filed by Boehringer Ingelheim Pharma GmbH Co KG filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of AR069545A1 publication Critical patent/AR069545A1/es
Suspension/Interruption legal-status Critical Current

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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
    • C07D221/22—Bridged ring systems
    • C07D221/26—Benzomorphans
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
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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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    • C07D401/14—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 three or more hetero rings
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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
    • C07D403/06—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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D405/00—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
    • C07D405/02—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
    • C07D405/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
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    • C07D417/02—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
    • 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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    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen 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
    • C07D471/08—Bridged systems
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    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

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  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (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

Compuestos de formula (1) que poseen actividad farmacologica, particularmente los compuestos son inhibidores de la 11b-hidroxiesteroide deshidrogenasa (HSD 1) y por lo tanto son adecuados para el tratamiento y prevencion de enfermedades que pueden estar influenciadas por la inhibicion de esta enzima, tales como enfermedades metabolicas, en particular diabetes de tipo 2, obesidad y dislipidemia. Composiciones farmacéuticas que las contienen y obtencion de las mismas. Reivindicacion 1: Los compuestos caracterizados porque tienen la formula (1) en la que R1 representa arilo o heteroarilo, mientras que por arilo se entiende fenilo o naftilo y por heteroarilo se entiende pirrolilo, furanilo, tienilo, piridilo, indolilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo, o pirrolilo, furanilo, tienilo, piridilo donde 1 o 2 CH se reemplazan por N, o indolilo, benzofuranilo, benzotiotenilo, quinolinilo, o isoquinolinilo, donde 1 a 3 CH se reemplazan por N, o 1,2-dihidro-2-oxo-piridinilo, 1,4-dihidro-4-oxo-piridinilo, 2,3-dihidro-3-oxo-piridazinilo, 1,2,3,6-tetrahidro-3,6-dioxo-piridazinilo, 1,2-dihidro-2-oxo-pirimidinilo, 3,4-dihidro-4-oxo-pirimidinilo, 1,2,3,4-tetrahidro-2,4-dioxo-pirimidinilo, 1,2-dihidro-2-oxo-pirazinilo, 1,2,3,4-tetrahidro-2,3-dioxo-pirazinilo, indanilo, 1-oxo-indanilo, 2,3-dihidro-indolilo, 2,3-dihidro-1H-isoindolilo, 2,3-dihidro-2-oxo-indolilo, 2,3-dihidro-1-oxo-isoindolilo, 2,3-dihidrobenzo-furanilo, 2,3-dihidro-2-oxo-1H-bencimidazolilo, 2,3-dihidro-2-oxo-benzoxazolilo, benzo[1,3]dioxolilo, 2-oxo-benzo[1,3]dioxolilo, 1,2,3,4-tetrahidro-naftilo, 1,2,3,4-tetrahidro-quinolinilo, 1,2,3,4-tetrahidro-2-oxo-quinolinilo, 1,2-dihidro-2-oxo-quinolinilo, 1,4-dihidro-4-oxo-quinolinilo, 1,2,3,4-tetrahidro-isoquinolinilo, 1,2,3,4-tetrahidro-1-oxo-isoquinolinilo, 1,2-dihidro-1-oxo-isoquinolinilo, 1,4-dihidro-4-oxo-cinnolinilo, 1,2-dihidro-2-oxo-quinazolinilo, 1,4-dihidro-4-oxo-quinazolinilo, 1,2,3,4-tetrahidro-2,4-dioxo-quinazolinilo, 1,2-dihidro-2-oxoquinoxalinilo, 1,2,3,4-tetrahidro-3-oxo-quinoxalinilo, 1,2,3,4-tetrahidro-2,3-dioxo-quinoxalinilo, 1,2-dihidro-1-oxo-ftalazinilo, 1,2,3,4-tetrahidro-1,4-dioxo-ftalazinilo, cromanilo, coumarinilo, 2,3-dihidro-benzo[1,4]dioxin-ilo o 3,4-dihidro-3-oxo-2H-benzo[1,4]oxazinilo, donde los anillos arilo o heteroarilo mencionados anteriormente están opcionalmente sustituidos con un R4, uno a cuatro R5 iguales o diferentes, y un R6, y todos los anillos heteroarilo están unidos al grupo carbonilo mediante un átomo de carbono; R2 y R3 junto con el doble enlace al que están unidos representan un anillo benzo opcionalmente sustituido con R7, R8 y R9, un anillo pirido opcionalmente sustituido con R7, R8 y R9, un anillo pirrolo, furo, tieno, piridazino, pirimido o pirazino opcionalmente sustituido con dos sustituyentes seleccionados entre R7, R8 y R9, un anillo pirazolo, imidazo, oxazolo, tiazolo, isoxazolo o isotiazolo opcionalmente sustituido con R7, o un anillo 1,2,3-triazolo opcionalmente sustituido con alquilo C1-4 o con fenilo que está adicionalmente opcionalmente sustituido con uno a tres R10; R4 representa fluor, cloro, bromo, yodo, alquilo C, alquenilo C2-4, alquinilo C2-6, hidroxi, alquiloxi C1-4, nitro, amino, alquilamino C1-3, di-(alquil C1-3)amino, pirrolidin-1-ilo, 2-oxo-pirrolidin-1-ilo, piperidin-1-ilo, 2-oxo-piperidin-1-ilo, morfolin-4-ilo, 3-oxo-morfolin-4-ilo, piperazin-1-ilo, 2-oxo-piperazin-1-ilo, 3-oxo-piperazin-1-ilo, 4-(alquil C1-3)-piperazin-1-ilo, 4-(alquilcarbonil C1-4)-piperazin-1-ilo, 4-(cicloalquilcarbonil C3-6)-piperazin-1-ilo, 4-(alquiloxicarbonil C1-4)-piperazin-1-ilo, 4-(alquilsulfonil C1-4)-piperazin-1-ilo, 2-oxo-4-(alquil C1-3)-piperazin-1-ilo, 3-oxo-4-(alquil C1-3)-piperazin-1-ilo, alquil C1-3carbonilamino, (het)aril-carbonilamino, (het)aril-alquil C1-3-carbonilamino, alquiloxi C1-3-carbonilamino, aminocarbonilamino, alquil C1-3-aminocarbonilamino, di-(alquil C1-3)aminocarbonilamino, pirrolidin-1-il-carbonilamino, piperidin-1-il-carbonilamino, morfolin-4-il-carbonilamino, piperazin-1-il-carbonilamino, 4-(alquil C1-3)-piperazin-1-il-carbonilamino, alquil C1-3 sulfonilamino, aminosulfonilamino, alquilamino C1-3-sulfonilamino, di-(alquil C1-3)amino-sulfonilamino, pirrolidin-1-il-sulfonilamino, piperidin-1-il-sulfonilamino, morfolin-4-il-sulfonilamino, piperazin-1-il-sulfonilamino, 4-(alquil C1-3)-piperazin-1-il-sulfonilamino, (alquiloxi C1-3-carbonilamino)carbonilamino, (het)arilsulfonilamino, (het)aril-alquil C1-3-sulfonilamino, N-(alquil C1-3)-alquil C1-3-carbonilamino, N-(alquil C1-3)-(het)arilcarbonilamino, N(alquil C1-3)-(het)aril-alquil C1-3-carbonilamino, N-(alquil C1-3)-alquiloxi C1-3 carbonilamino, N-(aminocarbonil)-alquilamino C1-3, N-(alquil C1-3-aminocarbonil-alquilamino C1-3, N-[di-(alquil C1-3)aminocarbonil]-alquilamino C1-3, N-(alquil C1-3)-alquil C1-3-sulfonilamino, N-(alquil C1-3)-(het)arilsulfonilamino, N-(alquil C1-3)-(het)aril-alquil C1-3-sulfonilamino, oxo-imidazolidin-1-ilo, 2,4-dioxo-imidazolidin-1-ilo, 2,5-dioxo-imidazolidin-1-ilo, 2-oxo-hexahidropirimidin-1-ilo, donde el átomo de nitrogeno de la posicion 3 de los grupos mencionados anteriormente está opcionalmente sustituido con metilo o etilo, ciano, carboxi, alquiloxi C1-3-carbonilo, aminocarbonilo, alquil C1-3-aminocarbonilo, di-(alquil C1-3)-aminocarbonilo, pirrolidin-1-il-carbonilo, piperidin1-il-carbonilo, morfolin-4-il-carbonilo, piperazin-1-il-carbonilo, 4-(alquil C1-3)-piperazin-1-il-carbonilo, (het)arilaminocarbonilo, N-(alquil C1-3)-(het)arilaminocarbonilo, (het)aril-alquilaminocarbonilo C1-3, N-(alquil C1-3)-(het)aril-alquilaminocarbonilo C1-3, alquil C1-3-carbonilo, (het)aril-carbonilo, carboxi-alquilo C1-3, alquiloxi C1-3-carbonil-alquilo C1-3, ciano-alquilo C1-3, aminocarbonil-alquilo C1-3, alquil C1-3-aminocarbonil-alquilo C1-3, di-(alquil C1-3)-aminocarbonil-alquilo C1-3, pirrolidin-1-il-carbonil-alquilo C1-3, piperidin-1-il-carbonil-alquilo C1-3, morfolin-4-il-carbonil-alquilo C1-3, piperazin-1-il-carbonil-alquilo C1-3, 4-(alquil C1-3)-piperazin-1-il-carbonil-alquilo C1-3, carboxi-alquiloxi C1-3, alquiloxi C1-3-carbonil-alquiloxi C1-3, ciano-alquiloxi C1-3, aminocarbonil-alquiloxi C1-3, alquil C1-3-aminocarbonil-alquiloxi C1-3, di-(alquil C1-3)-aminocarbonil-alquiloxi C1-3, pirrolidin-1-il-carbonil-alquiloxi C1-3, piperidin-1-il-carbonil-alquiloxi C1-3, morfolin-4-iI-carbonil-alquiloxi C1-3, piperazin-1-il-carbonil-alquiloxi C1-3, 4-(alquil C1-3)-piperazin-1-il-carbonil-alquiloxi C1-3, hidroxi-alquilo C1-3, alquiloxi C1-3-alquilo C1-3, amino-alquilo C1-3, alquilamino C1-3-alquilo C1-3, di-(alquil C1-3)-amino-alquilo C1-3, pirrolidin-1-il-alquilo C1-3, 2-oxo-pirrolidin-1-il-alquilo C1-3, piperidin-1-il-alquilo C1-3, 2-oxo-piperidin-1-il-alquilo C1-3, morfolin-4-il-alquilo C1-3, 3-oxo-morfolin-4-il-alquilo C1-3, piperazin-1-il-alquilo C1-3, 2-oxo-piperazin-1-il-alquilo C1-3, 3-oxo-piperazin-1-il-alquilo C1-3, 4-(alquil C1-3)-piperazin-1-il-alquilo C1-3, 2-oxo-4-(alquil C1-3)-piperazin-1-il-alquilo C1-3, 3-oxo-4-(alquil C1-3)-piperazin-1-iI-alquilo C1-3, alquilcarbonilamino C1-3-alquilo C1-3, arilcarbonilarnino-alquilo C1-3, hidroxi-alquiloxi C1-3, alquiloxi C1-3-alquiloxi C1-3, alquilsulfanil C1-3-alquiloxi C1-3, alquilsulfinil C1-3-alquiloxi C1-3, alquilsulfonil C1-3-alquiloxi C1-3, amino-alquiloxi C1-3, alquilamino C1-3-alquiloxi C1-3, di-(alquil C1-3)-amino-alquiloxi C1-3, pirrolidin-1-il-alquiloxi C1-3, 2-oxo-pirrolidin-1-il-alquiloxi C1-3, piperidin-1-il-alquiloxi C1-3, 2-oxo-piperidin-1-il-alquiloxi C1-3, morfolin-4-il-alquiloxi C1-3, 3-oxo-morfolin-4-il-alquiloxi C1-3, piperazin-1-il-alquiloxi C1-3, 2-oxo-piperazin-1-iI-alquiloxi C1-3, 3-oxo-piperazin-1-il-alquiloxi C1-3, 4-(alquil C1-3)-piperazin-1-il-alquiloxi C1-3, 2-oxo-4-(alquil C1-3)-piperazin-1-il-alquiloxi C1-3, 3-oxo-4-(alquil C1-3)-piperazin-1-il-alquiloxi C1-3, alquilsulfanilo C1-3, alquilsulfinilo C1-3, alquilsulfonilo C1-3, alquilsulfoniloxi C1-3, (het)arilsulfonilo, (het)arilsulfoniloxi, trifluorometilsulfanilo, trifluorometilsulfinilo, trifluorometilsulfonilo, aminosulfonilo, alquil C1-3-aminosuIfoniIo, di-(alquil C1-3)-aminosulfonilo, pirrolidin1-il-sulfonilo, piperidin-1-il-sulfonilo, morfolin-4-il-sulfonilo, piperazin-1-il-sulfonilo, 4-(alquil C1-3)-piperazin-1-il-sulfonilo, difluorometilo, trifluorometilo, difluorometoxi, trifluorometoxi, 2,2,2-trifluoro-1-hidroxietilo, 2,2,2-trifluoro-1-hidroxi-1-metiletilo, 2,2,2-trifluoro-1-hidroxi-1-(trifluorometil)etilo, cicloalquilo C3-6, cicloalquiloxi C3-6, cicloalquil C3-6-alquilo C1-3, cicloalquil C3-6-alquiloxi C1-3, (het)arilo, (het)ariloxi, (het)aril-alquilo C1-3, (het)aril-alquiloxi C1-3, (het)ariloxialquilo C1-3, o tetrahidrofurano-3-il-oxi, tetrahidropiran-3-iI-oxi, tetrahidropiran-4-il-oxi, tetrahidrofuranil-alquiloxi C1-3, tetrahidropiranil-alquiloxi C1-3, donde los restos azetidin-1-ilo, pirrolidin-1-ilo y piperidin-1-ilo mencionados anteriormente están opcionalmente sustituidos con uno o dos grupos seleccionados entre metilo, etilo, metoximetilo, hidroxi o metoxi, y donde los restos piperazin-1-ilo y morfolin-4-ilo mencionados anteriormente están opcionalmente sustituidos con uno o dos grupos seleccionados entre metilo, etilo o metoximetilo, y donde el resto (het)arilo mencionado anteriormente es fenilo, naftilo, pirrolilo, furanilo, tienilo, tetrazolilo, piridilo, indolilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo, o pirrolilo, furanilo, tienilo, piridilo donde 1 o 2 CH se reemplazan por N, o indolilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo donde 1 a 3 CH se reemplazan por N, o 1,2-dihidro-2-oxo-piridinilo, 1,4-dihidro-4-oxo-piridinilo, 2,3-dihidro-3-oxo-piridazinilo, 1,2,3,6-tetrahidro-3,6-dioxo-piridazinilo, 1,2-dihidro-2-oxo-pirimidinilo, 3,4-dihidro-4-oxo-pirimidinilo, 1,2,3,4-tetrahidro-2,4-dioxo-pirimidinilo, 1,2-dihidro-2-oxo-pirazinilo, 1,2,3,4-tetrahidro-2,3-dioxo-pirazinilo, 2,3-dihidro-2-oxo-indolilo, 2,3-dihidrobenzofuranilo, 2,3-dihidro-2-oxo-1H-bencimidazolilo, 2,
ARP080104991A 2007-11-16 2008-11-14 Derivados de aril y heteroarilcarbonilo de benzomorfanos y estructuras relacionadas, composiciones farmaceuticas que contienen dichos compuestos, obtencion de las mismas, su uso en el tratamiento de enfermedades mediadas por la inhibicion de la enzima 11beta-hidroxiesteroide deshidrogenasa (hsd) 1 y Suspension/Interruption AR069545A1 (es)

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