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.Info
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- 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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- 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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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
- C07D221/06—Ring systems of three rings
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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
- C07D221/06—Ring systems of three rings
- C07D221/16—Ring systems of three rings containing carbocyclic rings other than six-membered
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D401/00—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
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
- C07D401/06—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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- C—CHEMISTRY; METALLURGY
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- C07D401/00—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
- 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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- C07D401/00—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
- 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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- 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
- C07D405/04—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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- 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
- C07D405/14—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 three or more hetero rings
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- C07D417/00—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
- 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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- 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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- 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
- C07D498/04—Ortho-condensed systems
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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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EP09175233 | 2009-11-06 |
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AR078887A1 true AR078887A1 (es) | 2011-12-07 |
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ARP100104083A AR078887A1 (es) | 2009-11-06 | 2010-11-04 | Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina y composiciones farmaceuticas que los contienen. |
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EP (1) | EP2496559B1 (es) |
JP (1) | JP5796015B2 (es) |
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CN (2) | CN102666491B (es) |
AP (1) | AP2012006248A0 (es) |
AR (1) | AR078887A1 (es) |
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CN102119160B (zh) | 2008-07-25 | 2014-11-05 | 贝林格尔·英格海姆国际有限公司 | 11β-羟基类固醇脱氢酶1的环状抑制剂 |
WO2010010157A2 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1 |
EP2350068B1 (en) | 2008-10-23 | 2017-08-30 | Boehringer Ingelheim International GmbH | Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use |
WO2010089303A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | CYCLIC INHIBITORS OF 11 β-HYDROXYSTEROID DEHYDROGENASE 1 |
MA33216B1 (fr) | 2009-04-30 | 2012-04-02 | Boehringer Ingelheim Int | Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1 |
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JP5860042B2 (ja) | 2010-06-16 | 2016-02-16 | 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 | 置換5、6及び7員複素環、そのような化合物を含有する医薬及びそれらの使用 |
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JP2013540801A (ja) | 2010-11-02 | 2013-11-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 代謝異常の治療のための組合せ医薬 |
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EA201401231A1 (ru) * | 2012-05-09 | 2015-08-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Фармацевтические комбинации, предназначенные для лечения метаболических нарушений |
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CN109045035B (zh) * | 2018-07-19 | 2020-07-28 | 广西科技大学 | 7-(2,2-二甲基-3-丁烯酰胺基)-八氢苯喹啉乙酸酯在制备治疗肝病药物的应用 |
CN118251396A (zh) * | 2021-11-19 | 2024-06-25 | 豪夫迈·罗氏有限公司 | 2'-(7,7-二甲基-1'H,7H-螺[呋喃并[3,4-b]吡啶-5,4'-哌啶]-1'-基)-1,3-二氢-4'H-螺[茚-2,5'-[1,3]噁唑]-4'-酮的合成及其结晶形式 |
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