AR066148A1 - Derivados puenteados de ciclohexeno bloqueadores del canal de calcio - Google Patents
Derivados puenteados de ciclohexeno bloqueadores del canal de calcioInfo
- Publication number
- AR066148A1 AR066148A1 ARP080101765A ARP080101765A AR066148A1 AR 066148 A1 AR066148 A1 AR 066148A1 AR P080101765 A ARP080101765 A AR P080101765A AR P080101765 A ARP080101765 A AR P080101765A AR 066148 A1 AR066148 A1 AR 066148A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- group
- substituted
- unsubstituted
- Prior art date
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- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/14—Radicals substituted by nitrogen atoms
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- C07C217/56—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
- C07C217/62—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
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- Anesthesiology (AREA)
Abstract
Reivindicacion 1: Un compuesto de formula (1) en el cual X representa un átomo de carbono, y R1a y R2a en conjunto forman un enlace; o X representa un átomo de carbono, R1a y R2a en conjunto forman un enlace, y R1 y R2 en conjunto forman el fragmento de formula (2) en donde el asterisco indica el punto de union de R2; o X representa un átomo de carbono, R1a representa hidrogeno o alcoxilo C1-4, y R2a representa hidrogeno; o X representa un átomo de carbono, R1 y R1a en conjunto forman un grupo 3H-benzofuran-2,2-diilo, y R2 y R2a ambos representan hidrogeno; o X representa un átomo de nitrogeno, R1a está ausente, y R2 y R2a ambos representan hidrogeno o y R2 y R2a en conjunto forman un grupo carbonilo; y R1 y R2, si no se indica de otra manera, representan de manera independiente hidrogeno; alquilo C1-5; arilo, que está no substituido, o de manera independientes, mono-, di-, o tri-substituido en donde los substituyentes se seleccionan de manera independiente desde el conjunto que consiste en alquilo C1-4, alcoxilo C1-4, halogeno, trifluorometilo, trifluorometoxilo, ciano, y cicloalquilo C3-6; o heteroarilo, que está no substituido, o de manera independientes, mono-, di-, o tri-substituido en donde los substituyentes se seleccionan de manera independiente desde el conjunto que consiste en alquilo C1-4, alcoxilo C1-4, halogeno, ciano, trifluorometilo, y trifluorometoxilo; con la condicion de que en el caso en que R2 represente arilo o heteroarilo, R1 no puede representar arilo o heteroarilo, en donde el arilo y el heteroarilo de manera independiente están no substituidos o substituidos tal como se define anteriormente; R3 representa hidrogeno, o -CO-R31; R31 representa alquilo C1-5, fluoroalquilo C1-5, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-3, alcoxilo C1-5, alcoxi C1-2-alquilo C1-3, o R32R33N-; R32 representa alquilo C1-5; R33 representa hidrogeno, o alquilo C1-5; n representa el entero 1, 2, 3 o 4; B representa un grupo -(CH2)m-, en donde m representa el entero 1, 2, 3, 4 o 5; o B en conjunto con R4 y el átomo de nitrogeno al cual B y R4 están unidos forman un anillo saturado de 4 a 6 miembros; A representa una cadena lineal alcan-diilo C1-3, en donde dicha cadena lineal alcan-diilo C1-3 está opcionalmente substituida con uno o más metilo; R4 representa hidrogeno; alquilo C1-5; alcoxi C1-2-alquilo C1-3; fluoroalquilo C1-3; cicloalquilo C3-6; cicloalquil C3-6-alquilo C1-3; o R4 en conjunto con B y el átomo de nitrogeno al cual R4 y B están unidos forman un anillo saturado de 4 a 6 miembros; W representa arilo, que está no substituido, mono-, di-, o tri-substituido (especialmente no substituido o di-substituido), en donde los substituyentes se seleccionan de manera independiente desde el conjunto que consiste, en alquilo C1-4, alcoxilo C1-4, halogeno, trifluorometilo, trifluorometoxilo, ciano, y cicloalquilo C3-6 (especialmente de alcoxilo C1-4); o W representa heteroarilo, que está no substituido, mono-, di-, o tri-substituido, en donde los substituyentes se seleccionan de manera independiente desde el conjunto que consiste en alquilo C1-4, alcoxilo C1-4, halogeno, ciano, trifluorometilo, y trifluorometoxilo; o W representa un grupo seleccionado de entre radicales del grupo de formulas (3) en donde R5 representa hidrogeno, o alquilo C1-5; R6 y R7 representan de manera independiente hidrogeno; alquilo C1-5; o fenilo, que está independientemente no substituido, mono-, o di-substituido, en donde cada substituyente es independientemente seleccionado desde el conjunto que consiste en alquilo, alcoxilo, halogeno y trifluorometilo; R8, R9 y R10 representan de manera independiente hidrogeno, halogeno, alquilo C1-5, hidroxilo, alcoxilo C1-5, -O-CO-alquilo C1-5, fluoroalquilo C1-3, fluoroalcoxilo C1-3, -COOH, -CO-alcoxilo C1-5, alcoxi C1-2-alcoxilo C1-4, o -NH-CO-alquilo C1-5; R11 representa hidrogeno, o alquilo C1-5; R12 representa alquilo C1-5, que está no substituido, mono-, o di-substituido, en donde cada substituyente es independientemente seleccionado desde el conjunto que consiste en hidroxilo y alcoxilo C1-2; o R12 representa un anillo saturado de cuatro a ocho miembros carbono que opcionalmente contiene dos átomos oxígeno en el anillo, en donde los dos átomos de oxígeno en el anillo no están adyacentes entre sí; o una sal de tal compuesto. Reivindicacion 16: Un compuesto de formula (1) de acuerdo con cualquiera de las reivindicaciones 1 a 12, o una sal farmacéuticamente aceptable del mismo, para el tratamiento o la prevencion de angina cronica estable, hipertension, isquemia (renal y cardiaca), arritmias cardiacas incluyendo fibrilacion del atrio, hipertrofia cardiaca, o falla congestiva del corazon.
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US (1) | US8202885B2 (es) |
EP (1) | EP2152670B1 (es) |
JP (1) | JP4595040B2 (es) |
KR (1) | KR101114725B1 (es) |
CN (1) | CN101668742B (es) |
AR (1) | AR066148A1 (es) |
AU (1) | AU2008243860B2 (es) |
BR (1) | BRPI0810399B8 (es) |
CA (1) | CA2683866C (es) |
CL (1) | CL2008001205A1 (es) |
CY (1) | CY1115328T1 (es) |
DK (1) | DK2152670T3 (es) |
ES (1) | ES2449147T3 (es) |
HK (1) | HK1141296A1 (es) |
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AU2009239620A1 (en) * | 2008-04-25 | 2009-10-29 | Actelion Pharmaceuticals Ltd | Benzimidazole derivatives as calcium channel blockers |
WO2010046855A1 (en) * | 2008-10-22 | 2010-04-29 | Actelion Pharmaceuticals Ltd | Bridged tetrahydronaphthalene derivatives |
WO2010046857A1 (en) * | 2008-10-22 | 2010-04-29 | Actelion Pharmaceuticals Ltd | Salts of isobutyric acid (1 r*, 2r*, 4r* ) -2- (2-{ [3- (4, 7-dimeth0xy-1 h-benzoimidazol-2-yl) -propyl] -methyl-amino } -ethyl) -5-phenyl-bicyclo [2.2.2] oct-5- en- 2 -yl |
WO2010046729A2 (en) * | 2008-10-23 | 2010-04-29 | Actelion Pharmaceuticals Ltd | Tetrahydronaphthalene compounds |
US9096531B2 (en) * | 2010-05-24 | 2015-08-04 | Toa Eiyo Ltd. | Fused imidazole derivative |
ES2537610T3 (es) | 2010-06-11 | 2015-06-10 | Rhodes Technologies | Proceso para la N-desalquilación de aminas terciarias |
TWI551583B (zh) | 2010-10-20 | 2016-10-01 | 艾克泰聯製藥有限公司 | 雙環[2.2.2]辛-2-酮化合物之製備 |
MX2013004425A (es) | 2010-10-20 | 2013-07-17 | Actelion Pharmaceuticals Ltd | Preparacion diastereoselectiva de los compuestos de biciclo [2.2.2] octan-2-ona. |
CN102875474A (zh) * | 2012-10-23 | 2013-01-16 | 中国科学院广州生物医药与健康研究院 | 用于抗变异流感病毒的新型环烷胺类化合物 |
MY189770A (en) * | 2014-12-24 | 2022-03-04 | Lg Chemical Ltd | Biaryl derivative as gpr120 agonists |
CN114340670A (zh) | 2019-07-11 | 2022-04-12 | 普拉克西斯精密药物股份有限公司 | T-型钙通道调节剂的制剂及其使用方法 |
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HU184960B (en) * | 1981-07-20 | 1984-11-28 | Richter Gedeon Vegyeszet | Process for preparing new derivatives of 3,7-diazabicyclo/3.3.1/ nonane |
DK171349B1 (da) * | 1986-11-14 | 1996-09-16 | Hoffmann La Roche | Tetrahydronaphthalenderivater, fremgangsmåde til fremstilling deraf, lægemidler indeholdende forbindelserne samt anvendelse af forbindelserne til fremstilling af lægemidler |
CA2011461A1 (en) | 1989-03-20 | 1990-09-20 | Urs Hengartner | Tetrahydronaphthalene derivatives |
IL108432A (en) | 1993-01-29 | 1997-09-30 | Sankyo Co | DERIVATIVES OF 3, 5-DIHYDROXY-7- £1, 2, 6, 7, 8, 8a-HEXAHYDRO-2- METHYL-8- (SUBSTITUTED ALKANOYLOXY)-1-NAPHTHYL| HEPTANOIC ACID AND THEIR LACTONES, THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
US5489685A (en) | 1994-05-12 | 1996-02-06 | Merck & Co., Ltd. | Method of synthesizing furo[2,3-b]pyridine carboxylic acid esters |
US6268377B1 (en) * | 1998-09-28 | 2001-07-31 | Merck & Co., Inc. | Method for treating androgen-related conditions |
JP2005508949A (ja) * | 2001-10-10 | 2005-04-07 | アリックス セラピューティクス | 高血圧および狭心症の治療に有用なカルシウムチャネル遮断剤であるミベフラジルをベースとした化合物 |
AU2009239620A1 (en) | 2008-04-25 | 2009-10-29 | Actelion Pharmaceuticals Ltd | Benzimidazole derivatives as calcium channel blockers |
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