ES2574014T3 - Derivado de piperidina novedoso - Google Patents

Derivado de piperidina novedoso Download PDF

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ES2574014T3
ES2574014T3 ES06747135.9T ES06747135T ES2574014T3 ES 2574014 T3 ES2574014 T3 ES 2574014T3 ES 06747135 T ES06747135 T ES 06747135T ES 2574014 T3 ES2574014 T3 ES 2574014T3
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usp
inhibitors
compounds disclosed
srcard7799
mmol
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Shiho Ishikawa
Nagaaki Sato
Tsuyoshi Nagase
Shigeru Tokita
Toshihiro Wada
Hidekazu Takahashi
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MSD KK
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MSD KK
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    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
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Abstract

El compuesto 4-(2-metoxipirimidin-5-il)-9-(4-{3-[(2R)-2-metilpirrolidin-1-il]propoxi}fenil)-1-oxa-4,9-diazaespiro- [5,5]undecan-3-ona, o una sal farmacéuticamente aceptable del mismo.

Description

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65
y otros compuestos desvelados en el documento USP 5.739.106; 16) CNTF (factores neurotróficos ciliares) tales como GI181771 (GlaxoSmith Kline), SR146131 (Sanofi Synthelabo), butabindida, PD170.292, PS149164 (Pfizer); 17) derivados de CNTF tales como axokina (Regeneron), y otros compuestos desvelados en los documentos WO 94/09134, WO 98/22128, WO 99/43813; 18) agonistas de GHS (receptor de secreción de la hormona de crecimiento) tales como NN703, hexarelina, MK0677, SM130686, CP424.391, L692.429, L163.255, y compuestos desvelados en los documentos USP 6.358.951, solicitud de patente de Estados Unidos Nº 2002/049196, nº 2002/022637, WO 01/56592, WO 02/32888; 19) agonistas de 5HT2c (receptor de serotonina 2c) tales como BVT933, DPCA37215, IK264, PNU22394, WAY161503, R1065, YM348, y otros compuestos desvelados en los documentos USP 3.914.250, WO 02/36596, WO 02/48124, WO 02/10169, WO 01/66548, WO 02/44152, WO 02/51844, WO 02/40456 y WO 02/40457; 20) agonistas de Mc3r (receptor de melanocortina 3); 21) agonistas del receptor Mc4r (receptor de melanocortina 4) tales como CHIR86036 (Chiron), ME10142, ME10145 (Melacure) y otros compuestos desvelados en los documentos WO99/64002, WO00/74679, WO01/991752, WO01/74844, WO01/70708, WO01/70337, WO01/91752, WO02/059095, WO02/059107, WO02/059108, WO02/059117, WO02/12166, WO02/11715, WO02/12178, WO02/15909, WO02/068387, WO02/068388, WO02/067869, WO03/007949 y WO03/009847; 22) inhibidores de la recaptación de monoaminas tales como sibutramina (Meridia®/Reductil®) y sus sales, y otros derivados desvelados en los documentos USP 4.746.680, USP 4.806.570, USP 5.436.272, solicitud de patente de Estados Unidos Nº 2002/0006964, WO 01/27068 y WO 01/62341; 23) inhibidores de la recaptación de serotonina tales como dexflenfuramina, fluoxetina y otros compuestos desvelados en los documentos USP 6.365.633, WO 01/27060 y WO 01/162341; 24) agonistas de GLP1 (peptido 1 similar a glucagón); 25) topiramato (Topimax®); 26) compuesto 57 de Phytopharm (por ejemplo, CP644.673); 27) inhibidores de ACC2 (acetil CoA carboxilasa2); 28) agonistas de β3 (receptor 3 de adrenalina) tales como AD9677/TAK677 (DaiNippon Pharmaceutical/Takeda Chemical), CL316.243, SB418790, BRL37344, L796568, BMS196085, BRL35135A, CGP12177A, BTA243, W427353, trecadrina, Zeneca D7114, SR59119A, y otros compuestos desvelados en los documentos USP 5.705.515, USP 5.451.677, WO 01/74782 y WO 02/32897; 29) inhibidores de DGAT1 (diacilglicerol aciltransferasa1); 30) inhibidores de DGAT2 (diacilglicerol aciltransferasa2); 31) inhibidores de FAS (ácido graso sintasa) tales como cerulenina, C75; 32) inhibidores de PDE (fosfodiesterasa) tales como teofilina, pentoxifilina, zaprinast, sildenafilo, amrinona, milrinona, cilastamida, rolipram y cilomilast; 33) agonistas de la hormona β del tiroides tales como KB2611 (KaroBio BMS), y otros compuestos desvelados en los documentos WO 02/15845, JPA 2000256190; 34) activadores 1, 2 o 3 de UCP (proteína de desacoplamiento) tales como ácido fitánico, ácido 4[(E)2(5,6,7,8tetrahidro5,5,8,8tetrametil2naftalenil1propenil]benzoico (TTNPB), ácido retinoico y otros compuestos desvelados en el documento WO 99/00123; 35) acilestrógenos tal como oleilestrona (desvelados en del MarGrasa, M. y col, Obesity Research, 9: 2029 (2001)), 36) antagonistas de glucocorticoides; 37) inhibidores de 11β HSD1 (11βhidroesteroide deshidrogenasa1) tales como BVT3498, BVT2733, y otros compuestos desvelados en los documentos WO 01/90091, WO 01/90090, WO 01/90092; 38) inhibidores de SCD1 (estearoilCoA desaturasa1); 39) inhibidores de DPIV (dipeptidil peptidasaIV) tales como isoleucina tiazolidina, valina pirrolidida, NVPDPP728, AF237, P93/01, TSL225, TMC2A/2B/2C, FE999011, P9310/K364, VIP0177, SDZ274444, y otros compuestos desvelados en los documentos WO03/004498, WO03/004496, EP1258476, WO02/083128, WO02/062764, WO03/000250, WO03/002530, WO03/002531, WO03/002553, WO03/002593, WO03/000180 y WO03/000181; 40) inhibidores de lipasa tales como tetrahidroliptatina (Orlisat/Xenical®), Triton WR1339, RHC80267, lipstatina, saponina del té, fosfato de dietilumbilferilo, FL386, WAY121898, BayN3176, valilactona, esteracina, ebelactona A, ebalactona B, RHC80267, y otros compuestos desvelados en los documentos WO 01/77094, USP 4.598.089, USP 4.452.813, USP 5.512.565, USP 5.391.571, USP 5.602.151, USP 4.405.644, USP 4.189.438, y USP 4.242.453; 41) inhibidores del transportador de ácidos grasos; 42) inhibidores del transportador de dicarboxilato; 43) inhibidores del transportador de glucosa; 44) inhibidores del transportador de fosfato; 45) antagonistas de melanocortina tales como melanotán II, y otros compuestos desvelados en los documentos WO 99/64002 y WO 00/746799; 46) antagonistas de la hormona concentradora de melanina; 47) antagonistas de galanina; 48) agonistas de CCK;
16
imagen15
Hz: hertzio
Ejemplo 1: (referencia)
5 Producción de 1'[4(3peridin1ilpropoxi)fenil]3Hespiro[2benzofuran1,4'piperidina]
Se mezclaron 3Hespiro[2benzofuran1,4'piperidina] (131 mg, 0,695 mmol), 1[3(4yodofenoxi)propil]piperidina (200 mg, 0,58 mmol) preparada en el Ejemplo de Referencia (2), tercbutóxido sódico (78 mg, 0,812 mmol), Pd2(dba)3 (5 mg, 0,0058 mmol), 9,9dimetil4,5bis(difenilfosfino)xanteno (7 mg, 0,0116 mmol) y se agitaron durante
10 una noche en 1,4dioxano en una atmósfera de nitrógeno a 60 ºC. La solución de reacción se filtró bajo succión a través de Celite, se diluyó con acetato de etilo, se lavó con agua y una solución salina saturada en este orden, y la capa orgánica se secó con sulfato sódico. El disolvente se retiró por evaporación a presión reducida, y el residuo resultante se purificó a través de cromatografía preparativa de capa fina (eluato: cloroformo/metanol = 10/1) para obtener el compuesto del título en forma de un sólido incoloro (60,5 mg, 26 %).
15 1H RMN (400 MHz, CDCl3) δ: 1,43 (2H, s a), 1,561,61 (4H, m), 1,87 (2H, d, J = 12,0 Hz), 1,921,99 (2H, m), 2,082,16 (2H, m), 2,392,48 (6H, m), 3,10 (2H, t, J = 12,4 Hz), 3,43 (2H, d, J = 11,2 Hz), 3,96 (2H, t, (J=6,4 Hz), 5,09 (2H, s), 6,83 (2H, d, J = 8,8 Hz), 6,96 (2H, d, J = 8,8 Hz), 7,137,15 (1H, m), 7,217,28 (3H, m)
Ejemplo 3: (referencia)
20 Producción de 4(4fluorofenil)9[4(3[(3S)3metilpiperidin1il]propoxi)fenil]1oxa4,9diazaespiro[5,5]undecan3ona
Se mezclaron 9(4{3[(3S)3metilpiperidin1il]propoxi}fenil)1oxa4,9diazaespiro[5,5]undecan3ona (100 mg,
25 0,25 mmol) obtenida en el Ejemplo de Referencia 121, 1bromo4fluorobenceno (52 mg, 0,25 mmol), fosfato potásico (110 mg, 0,50 mmol), yoduro de cobre (23 mg, 0,125 mmol), N,N'dimetildiaminoetano (22 mg, 0,25 mmol) en 1,4dioxano, y se agitaron durante una noche con calentamiento en un tubo cerrado herméticamente a 110 ºC. La solución de reacción se diluyó con acetato de etilo, se lavó con agua y una solución salina saturada en este orden, y la capa orgánica se secó con sulfato sódico. El disolvente se concentró a presión reducida, y el residuo se purificó a
30 través de HPLC preparativa de fase inversa (líquido A, TFA al 0,1 %/agua; líquido B, TFA al 0,1 %/acetonitrilo; A/B = 90/10 a 50/50; elución de gradiente de concentración lineal de 8 minutos; caudal, 40 ml/min) para recoger una fracción que contenía el producto pretendido. Después, el disolvente se concentró a presión reducida, y el residuo se neutralizó con una solución acuosa 2 N de hidróxido sódico añadida al mismo. Éste se extrajo mediante la adición de acetato de etilo al mismo, y la capa orgánica se lavó con una solución salina saturada y se secó con sulfato sódico.
35 El disolvente se retiró por evaporación a presión reducida para obtener el compuesto del título en forma de un sólido de color pardo pálido (83,7 mg, 68 %). 1H RMN (400 MHz, CDCl3) δ: 0,86 (3H, d, J = 6,3 Hz), 1,531,72 (6H, m), 1,821,90 (3H, m), 1,932,00 (2H, m), 2,13 (2H, d, J = 12,9 Hz), 2,462,50 (2H, m), 2,832,90 (2H, m), 3,07 (2H, t, J = 10,6 Hz), 3,27 (2H, d, J = 12,5 Hz), 3,60 (2H, s), 3,96 (2H, t, J = 6,3 Hz), 4,35 (2H, s), 6,84 (2H, d, J = 9,0 Hz), 6,92 (2H, d, J = 9,0 Hz), 7,11 (2H, t, J = 8,6
40 Hz), 7,267,28 (2H, m)
Ejemplo 38 (referencia):
Producción de 4fenil9[4(3piperidin1ilpropoxi)fenil]1oxa4,9diazaespiro[55]undecan3ona
45 El compuesto del título se obtuvo en forma de un sólido de color blanco, de acuerdo con el mismo método que en el Ejemplo 3 o de acuerdo con un método similar a éste pero usando 9[4(3piperidin1ilpropoxi)fenil]1oxa4,9diazaespiro[5,5]undecan3ona obtenida en el Ejemplo de Referencia 12, y bromobenceno en lugar de 1bromo4fluorobenceno.
50 1H RMN (400 MHz, CDCl3) δ: 1,43 (2H, m), 1,561,60 (4H, m), 1,841,99 (4H, m), 2,13 (2H, d, J = 13,2 Hz), 2,402,48 (6H, m), 3,053,10 (2H, m), 3,26 (2H, d, J = 12,4 Hz), 3,64 (2H, s), 3,96 (2H, t, J = 6,4 Hz), 4,36 (2H, s), 6,84 (2H, d, J = 9,2 Hz), 6,93 (2H, d, J = 9,2 Hz), 7,287,31 (3H, m), 7,417,45 (2H, m)
Ejemplo 381:
55 Producción de 4(2metoxipirimidin5il)9(4{3[(2R)2metilpirrolidin1il]propoxi}fenil)1oxa4,9diazaespiro[5,5]undecan3ona
El compuesto del título se obtuvo en forma de un sólido de color amarillo pálido, de acuerdo con el mismo método
60 que en el Ejemplo 3 o de acuerdo con un método similar a éste pero usando 9(4{3[(2R)2metilpirrolidin1il]propoxi}fenil)1oxa4,9diazaespiro[5,5]undecan3ona obtenida en el Ejemplo de Referencia 124, y 5yodo2metoxipirimidina en lugar de 1bromo4fluorobenceno. 1H RMN (400 MHz, CDCl3) δ: 1,10 (3H, d, J = 6,3 Hz), 1,381,48 (1H, m), 1,572,01 (7H, m), 2,092,23 (4H, m), 2,272,33 (1H, m), 2,943,01 (1H, m), 3,033,09 (2H, m), 3,163,21 (1H, m), 3,263,31 (2H, m), 3,63 (2H, s), 3,944,01 (2H,
65 m), 4,03 (3H, s), 4,37 (2H, s), 6,85 (2H, d, J = 9,3 Hz), 6,93 (2H, d, J = 9,3 Hz), 8,53 (2H, s)
18
imagen16
imagen17
imagen18
imagen19
imagen20

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