AR068014A1 - Derivados de pirimidin-2-il-amina, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de la cinasa. - Google Patents

Derivados de pirimidin-2-il-amina, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de la cinasa.

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Publication number
AR068014A1
AR068014A1 ARP080103671A ARP080103671A AR068014A1 AR 068014 A1 AR068014 A1 AR 068014A1 AR P080103671 A ARP080103671 A AR P080103671A AR P080103671 A ARP080103671 A AR P080103671A AR 068014 A1 AR068014 A1 AR 068014A1
Authority
AR
Argentina
Prior art keywords
carbon atoms
optionally substituted
alkyl
halogen
nr7r8
Prior art date
Application number
ARP080103671A
Other languages
English (en)
Original Assignee
Irm Llc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39929716&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR068014(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Irm Llc filed Critical Irm Llc
Publication of AR068014A1 publication Critical patent/AR068014A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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Abstract

Compuestos y composiciones farmacéuticas los cuales son utiles como inhibidores de cinasa de proteína, así como la utilizacion de tales compuestos con el fin de tratar, disminuir, o prevenir una condicion asociada con una actividad de cinasa anormal o mal regulada. En algunas modalidades, se proporciona el uso en la fabricacion de medicamentos que utilizan tales compuestos con el fin de tratar, disminuir, o prevenir enfermedades o trastornos que involucren una activacion anormal de las cinasas c-kit, PDGFRalfa, PDGFRbeta, CSF1R, Abl BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFbeta, SRC, EGFR trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2beta, BRK, Fms, KDR, c-raf o b-raf. Reivindicacion 1: Un compuesto de la formula (1): o una sal farmacéuticamente aceptable del mismo: R1 es un halo-alquilo que tiene de 1 a 6 átomos de fluor; R2 es alquilo de 1 a 6 átomos de carbono alquenilo de 2 a 6 átomos de carbono o alquinilo de 2 a 6 átomos de carbono, cada uno de los cuales puede estar opcionalmente sustituido con grupos halogeno, amino o hidroxilo; halogeno, ciano, nitro, (CR2)kOR7, (CR2)kO(CR2)1-4R7, (CR2)kSR7, (CR2)kNR9R10, (CR2)kC(O)O0-1R7, OC(O)R7, (CR2)kC(S)R7, (CR2)kC(O)NR9R10, (CR2)kC(O)NR(CR2)0-6C(O)O0-1R7, (CR2)kNRC(O)O0-1R7, (CR2)kS(O)1-2NR9R10, (CR2)kS(O)1-2R8, (CR2)kNRS(O)1-2R8 o (CR2)kR6; o cualesquiera dos grupos R2 adyacentes pueden formar juntos un anillo de arilo o heteroarilo carbocíclico, heterocíclico, de 5 a 8 miembros, opcionalmente sustituido; R3 es -L-NR4R5, -X-NR-C(O)R8 o -X-NR-C(O)NR4R5 en donde L es -X-C(O), -X-OC(O), -(CR2)j, -SO0-2(CR2)j, -O(CR2)1-4, o resto de formula 2; y X es (CR2)j o [C(R)-(CR2OR)]; R4, R5, R9 y R10 son independientemente H; alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono o alquinilo de 2 a 6 átomos de carbono, cada uno de los cuales puede estar opcionalmente sustituido con halogeno, amino, hidroxilo, alcoxilo, ciano, carboxilo o R6 (CR2)kCN, (CR2)1-6NR7R8, (CR2)1-6OR7, (CR2)kC(O)O0-1R7, (CR2)kC(O)NR7R8 o (CR2)k-R6; R6 es un cicloalquilo de 3 a 7 átomos de carbono opcionalmente sustituido, arilo de 6 átomos de carbono, o un anillo de heteroarilo de 5 a 6 miembros o heterocíclico de 5 a 7 miembros; R7 y R8 son independientemente (CR2)k-R6 o alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono o alquinilo de 2 a 6 átomos de carbono, cada uno de los cuales puede estar opcionalmente sustituido con halogeno, amino, amido, hidroxilo, alcoxilo, ciano, carboxilo o R6; o R7 es H; de una manera alternativa, R4 y R5 junto con N en cada NR4R5, R7 y R8 junto con N en NR7R8, o R9 y R10 junto con N en NR9R10 pueden formar un anillo heterocíclico de 4 a 7 miembros opcionalmente sustituido con 1 a 3 grupos R11; R11 es R8, (CR2)k-OR7, CO2R7, (CR2)k-C(O)-(CR2)k-R8, (CR2)kC(O)NR7R8, (CR2)kC(O)NR(CR2)0-6C(O)O0-1R7, (CR2)kNRC(O)O0-1R7, (CR2)kS(O)1-2NR7R8, (CR2)kS(O)1-2R8 o (CR2)kNRS(O)1-2R8; cada R es H o alquilo de 1 a 6 átomos de carbono; cada k es de 0 a 6; y j y m son independientemente de 0 a 4; en el entendido de que R1 no es trifluoro-metoxilo cuando R3 es C(O)NH2, C(O)NR12R13 o SO2NH(CH2)2-3NR14R15 en donde R12 y R13 forman juntos piperazinilo, y R14 y R15 forman juntos morfolinilo.
ARP080103671A 2007-08-22 2008-08-22 Derivados de pirimidin-2-il-amina, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de la cinasa. AR068014A1 (es)

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