ES2536415T3 - Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK - Google Patents
Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK Download PDFInfo
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- ES2536415T3 ES2536415T3 ES11793604.7T ES11793604T ES2536415T3 ES 2536415 T3 ES2536415 T3 ES 2536415T3 ES 11793604 T ES11793604 T ES 11793604T ES 2536415 T3 ES2536415 T3 ES 2536415T3
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- pyrimidin
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- C07—ORGANIC CHEMISTRY
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Abstract
Un compuesto de fórmula I:**Fórmula** o una sal farmacéuticamente aceptable del mismo; en la que : X es CH o N; Y es H, ciano, halógeno, alquilo C1-3 o haloalquilo C1-3; Z es CR4 o N; L es O o S; R1, R2, R3 y R4 son cada uno independientemente H, hidroxi, halógeno, alquilo C1-3 o haloalquilo C1-3; cada R5 es independientemente hidroxi, alcoxi C1-4, flúor, alquilo C1-4, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4 o fluoroalquilo C1-4; A es alquilo C1-6, cicloalquilo C3-10, heterocicloalquilo C2-10, arilo C6-10 o heteroarilo C1-10; cada uno opcionalmente sustituido con p sustituyentes R7 30 independientemente seleccionados; en la que p es 1, 2, 3, 4 ó 5; cada R7 está seleccionado independientemente de halógeno, ciano, nitro, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10, heteroaril C1-10-alquilo C1-4, -ORa, -SRa, -S(>=O)Rb, -S(>=O)2Rb, -S(>=O)2NReRf, -C(>=O)Rb, -C(>=O)ORa, -C(>=O)NReRf, -OC(>=O)Rb, - OC(>=O)NReRf, -NReRf, -NRcC(>=O)Rd, -NRcC(>=O)ORd, -NRcS(>=O)2Rd y -NRcS(>=O)2NReRf; en el que dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rg independientemente seleccionados; cada Ra, Rc, Rd, Re y Rf está seleccionado independientemente de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2- 6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10- alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4; en los que dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rg independientemente seleccionados; cada Rb está seleccionado independientemente de alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10-alquilo C1-4, arilo C6- 10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4; en el que dicho alquilo C1-6, alquenilo C2- 6, alquinilo C2-6, cicloalquilo C3-10, cicloalquil C3-10-alquilo C1-4, heterocicloalquilo C2-10, heterocicloalquil C2-10- alquilo C1-4, arilo C6-10, aril C6-10-alquilo C1-4, heteroarilo C1-10 y heteroaril C1-10-alquilo C1-4 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rg independientemente seleccionados; cada Rg está seleccionado independientemente de halógeno, ciano, nitro, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7, heteroaril C1-7-alquilo C1-3, -ORa1, -SRa1, -S(>=O)Rb1, - S(>=O)2Rb1, -S(>=O)2NRe1Rf1, -C(>=O)Rb1, -C(>=O)ORa1, -C(>=O)NRe1Rf1, -OC(>=O)Rb1, -OC(>=O)NRe1Rf1, -NRe1Rf1, - NRc1C(>=O)Rd1, -NRc1C(>=O)ORd1, -NRc1S(>=O)2Rd1 y -NRc1S(>=O)2NRe1Rf1; en el que dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7- alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rh independientemente seleccionados; cada Ra1, Rc1, Rd1, Re1 y Rf1 está seleccionado independientemente de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7- alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3; en los que dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rh 65 independientemente seleccionados; cada Rb1 está seleccionado independientemente de alquilo C1-6, haloalquilo C1-6, alquenilo cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3; en el que dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, heteroarilo C1-7 y heteroaril C1-7-alquilo C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos Rh independientemente 5 seleccionados; cada Rh está seleccionado independientemente de ciano, halógeno, hidroxi, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquil C1-4-amino, di-alquil C1-4-amino, tio, alquiltio C1-6, alquil C1-6-sulfinilo, alquil C1- 6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6- carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; m es 0, 1 ó 2; n es 0, 1, 2, 3 ó 4; y r es 1, 2 ó 3.
Description
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4-[4-(3-{[ciclopropil(metil)amino]metil}-5-fluorofenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1Hpirazol-1-il]butanonitrilo; 4-{4-[3-(azetidin-1-ilmetil)-5-fluorofenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-((4-{3-[(ciclobutilamino)metil]-5-fluorofenoxi}piperidin-1-il)-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-{4-[3-fluoro-5-(pirrolidin-1-ilmetil)fenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-{4-[3-fluoro-5-(piperidin-1-ilmetil)fenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-{4-[3-fluoro-5-(morfolin-4-ilmetil)fenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-((4-{3-[(3,3-difluoropirrolidin-1-il)metil]-5-fluorofenoxi}piperidin-1-il)-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1Hpirazol-1-il]butanonitrilo; 4-[4-(3-fluoro-5-{[2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-[4-(3-fluoro-5-{[(2-metoxietil)amino]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 3-[((1-{3-ciano-2-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]propil}-3-fluoropiperidin-4-il)oxi]-5fluorobenzonitrilo; y 4-[3-fluoro-4-(3-fluoro-5-{[2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1Hpirazol-1-il]butanonitrilo;
o una sal farmacéutica de cualquiera de los anteriormente mencionados.
En algunas realizaciones, el compuesto se selecciona de:
4-[4-(3-fluoro-5-{[(2R)-2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1Hpirazol-1-il]butanonitrilo; 4-[4-(3-fluoro-5-{[(2S)-2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1Hpirazol-1-il]butanonitrilo; 4-[3-fluoro-4-(3-fluoro-5-{[(2R)-2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)1H-pirazol-1-il]butanonitrilo; y 4-[3-fluoro-4-(3-fluoro-5-{[(2S)-2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)1H-pirazol-1-il]butanonitrilo;
o una sal farmacéutica de cualquiera de los anteriormente mencionados.
En algunas realizaciones, el compuesto es el enantiómero (R), o una sal farmacéuticamente aceptable del mismo.
En algunas realizaciones, el compuesto es el enantiómero (S), o una sal farmacéuticamente aceptable del mismo.
Se aprecia que ciertas características de la invención, que se describen, por claridad, en el contexto de realizaciones separadas, también pueden proporcionarse en combinación en una única realización. En cambio, diversas características de la invención que se describen, por brevedad, en el contexto de una única realización, también pueden proporcionarse por separado o en cualquier subcombinación adecuada.
En diversos sitios en la presente memoria descriptiva se describen sustituyentes de enlace divalente. Se pretende específicamente que cada sustituyente de enlace divalente incluya tanto las formas tanto hacia adelante como hacia detrás del sustituyente de enlace. Por ejemplo, -NR(CR'R")n-incluye tanto -NR(CR'R")n-como -(CR'R")nNR-. Si la estructura requiere claramente un grupo de enlace, se entiende que las variables de Markush enumeradas para ese grupo son grupos de enlace.
El término “de n miembros” si n es un número entero normalmente describe el número de átomos formadores de anillo en un resto en el que el número de átomos formadores de anillo es n. Por ejemplo, piperidinilo es un ejemplo de un anillo de heterocicloalquilo de 6 miembros, pirazolilo es un ejemplo de un anillo de heteroarilo de 5 miembros, piridilo es un ejemplo de un anillo de heteroarilo de 6 miembros y 1,2,3,4-tetrahidro-naftaleno es un ejemplo de un grupo cicloalquilo de 10 miembros.
Para compuestos de la invención en los que una variable aparece más de una vez, cada variable puede ser un resto diferente independientemente seleccionado del grupo que define la variable. Por ejemplo, si se describe una estructura que tiene dos grupos R que están simultáneamente presentes sobre el mismo compuesto, los dos grupos R pueden representan restos diferentes independientemente seleccionados del grupo definido para R. En otro ejemplo, si un sustituyente opcionalmente múltiple se designa en la forma:
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tiene 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “aminosulfonilo”, empleado solo o en combinación con otros términos, se refiere a un grupo de fórmula -S(O)2NH2.
Como se usa en el presente documento, el término “alquil Cn-m-aminosulfonilo” se refiere a un grupo de fórmula S(O)2NH(alquilo), en el que el grupo alquilo tiene n a m átomos de carbono. En algunas realizaciones, el grupo alquilo tiene 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “di(alquil Cn-m)aminosulfonilo” se refiere a un grupo de fórmula S(O)2N(alquilo)2, en el que cada grupo alquilo tiene independientemente n a m átomos de carbono. En algunas realizaciones, cada grupo alquilo tiene, independientemente, 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “aminosulfonilamino” se refiere a un grupo de fórmula -NHS(O)2NH2.
Como se usa en el presente documento, el término “alquil Cn-m-aminosulfonilamino” se refiere a un grupo de fórmula -NHS(O)2NH(alquilo), en el que el grupo alquilo tiene n a m átomos de carbono. En algunas realizaciones, el grupo alquilo tiene 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “di(alquil Cn-m)aminosulfonilamino” se refiere a un grupo de fórmula -NHS(O)2N(alquilo)2, en el que cada grupo alquilo tiene independientemente n a m átomos de carbono. En algunas realizaciones, cada grupo alquilo tiene, independientemente, 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “aminocarbonilamino” se refiere a un grupo de fórmula -NHC(O)NH2.
Como se usa en el presente documento, el término “alquil Cn-m-aminocarbonilamino” se refiere a un grupo de fórmula -NHC(O)NH(alquilo), en el que el grupo alquilo tiene n a m átomos de carbono. En algunas realizaciones, el grupo alquilo tiene 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “di(alquil Cn-m)aminocarbonilamino” se refiere a un grupo de fórmula -NHC(O)N(alquilo)2, en el que cada grupo alquilo tiene independientemente n a m átomos de carbono. En algunas realizaciones, cada grupo alquilo tiene, independientemente, 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “alquil Cn-m-carbamilo” se refiere a un grupo de fórmula -C(O)NH(alquilo), en el que el grupo alquilo tiene n a m átomos de carbono. En algunas realizaciones, el grupo alquilo tiene 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “di(alquil Cn-m)carbamilo” se refiere a un grupo de fórmula C(O)N(alquilo)2, en el que los dos grupos alquilo tienen cada uno, independientemente, n a m átomos de carbono. En algunas realizaciones, cada grupo alquilo tiene independientemente 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “tio” se refiere a un grupo de fórmula -SH.
Como se usa en el presente documento, el término “alquiltio Cn-m” se refiere a un grupo de fórmula -S-alquilo, en el que el grupo alquilo tiene n a m átomos de carbono. En algunas realizaciones, el grupo alquilo tiene 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “alquil Cn-m-sulfinilo” se refiere a un grupo de fórmula -S(O)alquilo, en el que el grupo alquilo tiene n a m átomos de carbono. En algunas realizaciones, el grupo alquilo tiene 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “alquil Cn-m-sulfonilo” se refiere a un grupo de fórmula -S(O)2alquilo, en el que el grupo alquilo tiene n a m átomos de carbono. En algunas realizaciones, el grupo alquilo tiene 1 a 6 ó 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “amino” se refiere a un grupo de fórmula -NH2.
Como se usa en el presente documento, el término “hidroxi-alquilo Cn-m” se refiere a un grupo de fórmula -alquilen-OH, en el que dicho grupo alquileno tiene n a m átomos de carbono. En algunas realizaciones, el grupo alquileno tiene 1 a 4 átomos de carbono.
Como se usa en el presente documento, el término “alcoxi Co-p-alquilo Cn-m ” se refiere a un grupo de fórmula alquilen-O-alquilo, en el que dicho grupo alquileno tiene n a m átomos de carbono y dicho grupo alquilo tiene o a p átomos de carbono. En algunas realizaciones, los grupos alquilo y alquileno tienen cada uno independientemente 1
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Claims (7)
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imagen1 imagen2 imagen3 imagen4 imagen5 51525354555653-[((1-{3-ciano-2-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]propil}piperidin-4-il)oxi]-5-fluoro-N-(2morfolin-4-iletil)benzamida; 4-{4-[3-fluoro-5-(piperidin-1-ilcarbonil)fenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-{4-[3-fluoro-5-(morfolin-4-ilcarbonil)fenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-((4-{3-[(3,3-difluoropirrolidin-1-il)carbonil]-5-fluorofenoxi}piperidin-1-il)-3-[4-(7H-pirrolo[2,3-d]pirimidin-4il)-1H-pirazol-1-il]butanonitrilo; 4-((4-{3-[(dimetilamino)metil]-5-fluorofenoxi}piperidin-1-il)-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-[4-(3-{[ciclopropil(metil)amino]metil}-5-fluorofenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1Hpirazol-1-il]butanonitrilo; 4-{4-[3-(azetidin-1-ilmetil)-5-fluorofenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-((4-{3-[(ciclobutilamino)metil]-5-fluorofenoxi}piperidin-1-il)-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol1-il]butanonitrilo; 4-{4-[3-fluoro-5-(pirrolidin-1-ilmetil)fenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-{4-[3-fluoro-5-(piperidin-1-ilmetil)fenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-{4-[3-fluoro-5-(morfolin-4-ilmetil)fenoxi]piperidin-1-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1il]butanonitrilo; 4-((4-{3-[(3,3-difluoropirrolidin-1-il)metil]-5-fluorofenoxi}piperidin-1-il)-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)1H-pirazol-1-il]butanonitrilo; 4-[4-(3-fluoro-5-{[2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1Hpirazol-1-il]butanonitrilo; 4-[4-(3-fluoro-5-{[(2-metoxietil)amino]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1Hpirazol-1-il]butanonitrilo; 3-[((1-{3-ciano-2-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]propil}-3-fluoropiperidin-4-il)oxi]-5fluorobenzonitrilo; y 4-[3-fluoro-4-(3-fluoro-5-{[2-metilpirrolidin-l-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)1H-pirazol-1-il]butanonitrilo;o una sal farmacéutica de cualquiera de los anteriormente mencionados; o b) seleccionado de:4-[4-(3-fluoro-5-{[(2R)-2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)1H-pirazol-1-il]butanonitrilo; 4-[4-(3-fluoro-5-{[(2S)-2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)1H-pirazol-1-il]butanonitrilo; 4-[3-fluoro-4-(3-fluoro-5-{[(2R)-2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3d]pirimidin-4-il)-1H-pirazol-1-il]butanonitrilo; y 4-[3-fluoro-4-(3-fluoro-5-{[(2S)-2-metilpirrolidin-1-il]metil}fenoxi)piperidin-1-il]-3-[4-(7H-pirrolo[2,3d]pirimidin-4-il)-1H-pirazol-1-il]butanonitrilo;o una sal farmacéutica de cualquiera de los anteriormente mencionados. -
- 16.
- El compuesto según una cualquiera de las reivindicaciones 1 a 15, en el que el compuesto es el enantiómero (R), o una sal farmacéuticamente aceptable del mismo.
-
- 17.
- El compuesto según una cualquiera de las reivindicaciones 1 a 15, en el que el compuesto es el enantiómero (S),
o una sal farmacéuticamente aceptable del mismo. -
- 18.
- Una composición que comprende un compuesto según una cualquiera de las reivindicaciones 1 a 17, o una sal farmacéuticamente aceptable del mismo, y al menos un vehículo farmacéuticamente aceptable.
-
- 19.
- Un compuesto según una cualquiera de las reivindicaciones 1 a 17, o una sal farmacéuticamente aceptable del mismo, para su uso en un método para modular una actividad de JAK1.
-
- 20.
- Un compuesto, o una sal farmacéuticamente aceptable del mismo, para su uso según la reivindicación 19, en el que dicho compuesto, o sal farmacéuticamente aceptable del mismo, es selectivo para JAK1 con respecto a JAK2.
-
- 21.
- Un compuesto según una cualquiera de las reivindicaciones 1 a 17, o una sal farmacéuticamente aceptable del mismo, para su uso en un método para tratar una enfermedad autoinmunitaria, un cáncer, un trastorno mieloproliferativo, una enfermedad inflamatoria, una enfermedad de resorción ósea o rechazo de trasplante de órgano en un paciente en necesidad del mismo.
54imagen6
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PCT/US2011/061351 WO2012068440A1 (en) | 2010-11-19 | 2011-11-18 | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
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CA2818545C (en) | 2019-04-16 |
JP5917544B2 (ja) | 2016-05-18 |
EP2640725B1 (en) | 2015-01-07 |
US9034884B2 (en) | 2015-05-19 |
US20120149682A1 (en) | 2012-06-14 |
EP2640725A1 (en) | 2013-09-25 |
HK1189877A1 (en) | 2014-06-20 |
CA2818545A1 (en) | 2012-05-24 |
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