AR056763A1 - Aminopirimidinas sustituidas con tiazol o pirazol,utiles como agentes anticancer y composiciones farmaceuticas que las contienen. - Google Patents

Aminopirimidinas sustituidas con tiazol o pirazol,utiles como agentes anticancer y composiciones farmaceuticas que las contienen.

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Publication number
AR056763A1
AR056763A1 ARP060104841A ARP060104841A AR056763A1 AR 056763 A1 AR056763 A1 AR 056763A1 AR P060104841 A ARP060104841 A AR P060104841A AR P060104841 A ARP060104841 A AR P060104841A AR 056763 A1 AR056763 A1 AR 056763A1
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ring
aliphatic
con
so2n
optionally substituted
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Vertex Pharma
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • A61P35/00—Antineoplastic agents
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    • A—HUMAN NECESSITIES
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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
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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
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    • 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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    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/14—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 three or more hetero rings

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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) o una de sus sales farmacéuticamente aceptables, en donde: Ht es tiazol, o pirazol, en donde cada anillo está opcional e independientemente sustituido con R2 y R2'; Q es -O-, -NR'-, -S- o -C(R')2-; Rx es H, alifático C1-6, NO2, CN, halo, NH2, N(alifático C1-4), N(alifático C1-4)2, O(alifático C1-4), OH o -N(C=O)(alifático C1-4); en donde dicho alifático está opcionalmente sustituido con 1-3 fluoro; Ry es T2-R10 o L-Z-R10; R1 es T3-(anillo D); anillo D es un anillo arilo o heteroarilo monocíclico de 5-7 miembros, en donde dicho heteroarilo tiene 1-4 heteroátomos del anillo seleccionados de O, N y S; anillo D puede estar opcionalmente fusionado con el anillo D'; anillo D' es un anillo de 5- 8 miembros, aromático, parcialmente saturado o totalmente insaturado que contiene 0-4 heteroátomos del anillo seleccionados de N, O o S; cada C del anillo sustituible del anillo D y anillo D' está sustituido, de modo independiente, con oxo, T4-R5 o V-Z-R5; cada N del anillo sustituible del anillo D y anillo D' está sustituido, de modo independiente, con -R4; cada T, T3 y T4 es, de modo independiente, una cadena alquilideno C1-4 o está ausente; Z es una cadena alquilideno C1-4 o está ausente; L es -O-, -S-, -SO-, -SO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, -CO-, -CO2-, -N(R6)CO-, -N(R6)C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2N(R6)-, -N(R6)N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)- , -C(R6)2N(R6)C(O)-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)- o -C(R6)2N(R6)CON(R6)-; T2 está, de modo independiente, ausente o es una cadena alquilideno C1-10 en donde hasta seis unidades C de la cadena alquilideno están opcionalmente reemplazadas por -O-, -C(=O)-, -S(O)-, -S(O)2-, -S- o -N(R4)-; T2 está opcionalmente sustituido con 0-6 grupos JT; R2 y R2' son, de modo independiente, -R, -T-W-R6 o R8 o R2 y R2' se toman juntos con sus átomos intervinientes para formar un anillo fusionado, de 5-8 miembros, insaturado o parcialmente insaturado con 0-3 heteroátomos del anillo seleccionados de N, O o S, en donde cada C del anillo sustituible de dicho anillo fusionado formado por R2 y R2' está sustituido, de modo independiente, con halo, oxo, -CN, -NO2, -R7 o -V-R6 y cada N del anillo sustituible de dicho anillo formado por R2 y R2' está sustituido, de modo independiente, con R4; R5 es -R, -halo, -OR, -C(=O)R, -CO2R, -COCOR, COCH2COR, -NO2, -CN, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R7)2, -SO2N(R7)2, -OC(=O)R, -N(R7)COR, -N(R7)CO2(alifático C1-6), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R7)CON(R7)2, -N(R7)SO2N(R7)2, -N(R4)SO2R o -OC(=O)N(R7)2; cada R es H, un grupo alifático C1-10, un anillo arilo C6-10, un anillo heteroarilo con 5-10 átomos del anillo o un anillo heterociclilo con 4-10 átomos del anillo, donde el anillo heteroarilo o heterociclilo tiene 1-4 heteroátomos del anillo seleccionados de N, O o S, el grupo alifático y cada R está opcionalmente sustituido con 0-6 R9; cada R4 es -R7,-COR7, -CO2(alifático C1-6 opcionalmente sustituido), -CON(R7)2 o -SO2R7; V es -O-, -S-, -SO-, -SO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, -CO-, -CO2-, -N(R6)CO-, - N(R6)C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2N(R6)-, -N(R6)N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -C(R6)2N(R6)C(O)-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)=N-O-, - C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)- o -C(R6)2N(R6)CON(R6)-; W es -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -CO-, -CO2-, -C(R6)2OC(O)-, -C(R6)2OC(O)N(R6)-, -C(R6)2N(R6)CO-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)- , -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)- -C(R6)2N(R6)CON(R6)- o -CON(R6)-; cada R6 es, de modo independiente, H o alifático C1-6 opcionalmente sustituido con 0-3 J6; o dos grupos R6 en el mismo átomo de N se toman juntos con el átomo de N para formar un anillo heterociclilo o heteroarilo de 4-8 miembros; en donde dicho anillo heterociclilo o heteroarilo está opcionalmente sustituido con 0-4 J6; cada R7 es, de modo independiente, H; alifático C1-6; un heteroarilo de 5 miembros que contiene 0-4 heteroátomos seleccionados de O, N o S; o fenilo, cada R7 está opcionalmente sustituido con 0-3 J7; o dos R7 en el mismo N se toman juntos con el N para formar un anillo heterociclilo o heteroarilo opcionalmente sustituido de 4-8 miembros; en donde dicho anillo heterociclilo o heteroarilo está opcionalmente sustituido con 0-4 J7; cada R8 es halogeno, -CN o -NO2; cada R9 es -R', -halo, -OR', -C(=O)R', -CO2R', -COCOR', COCH2COR', -NO2, -CN, -S(O)R', -S(O)2R', -SR', -N(R')2, - CON(R')2, -SO2N(R')2, -OC(=O)R', -N(R')COR', -N(R')CO2(alifático C1-6), -N(R')N(R')2, --N(R')CON(R')2, -N(R')SO2N(R')2, -N(R')SO2R', -OC(=O)N(R')2; =N-OR' o =O; cada R10 es un anillo heterocíclico de 4 miembros que contiene un heteroátomo seleccionado de O, NR11 y S; cada R10 está opcionalmente sustituido con 0-6 ocurrencias de J; cada J y JT es, de modo independiente, -R, -halo, -OR, -C(=O)R, -CO2R, -COCOR, COCH2COR, -NO2, -CN, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R7)2, -SO2N(R7)2, - OC(=O)R, -N(R7)COR, -N(R7)CO2(alifático C1-6), -N(R4)N(R4)2, =NN(R4)2, =N-OR, =NR, =O, -N(R7)CON(R7)2, -N(R7)SO2N(R7)2, -N(R4)SO2R, -OC(=O)N(R7)2 o -OP(=O)(ORö)2; o cada J6 y J7 es, de modo independiente, NH2, NH(alifático C1-4), N(alifático C1-4)2, halogeno, alifático C1-4, OH, O(alifático C1-4), NO2, CN, CO2H, CO2(alifático C1-4), O(haloalifático C1-4) o haloalifático C1-4; 2 grupos J o JT, en el mismo átomo o en átomos diferentes, junto con los átomos a los que cada grupo J o JT están unidos, forman un anillo de 3-8 miembros saturado, parcialmente saturado o insaturado con 0-2 heteroátomos seleccionados de O, N o S; en donde 1-4 átomos de H en el anillo formado por los 2 grupos J o JT está opcionalmente reemplazado con halo, alquilo C1-3 o -O(alquilo C1-3); en donde dicho alquilo C1-3 está opcionalmente sustituido con 1-3 F; o dos átomos de H en el mismo átomo en el anillo formado por los 2 grupos J o JT están opcionalmente reemplazados con oxo; cada R11 es -R7, -CR7, - CO2(alifático C1-6 opcionalmente sustituido), -CON(R7)2 o -SO2R7; cada R' es, de modo independiente, H o un grupo alifático C1-6 opcionalmente sustituido con 0-4 ocurrencias de NH2, NH(alifático C1-4), N(alifático C1-4)2, halogeno, alifático C1-4, OH, O(alifático C1-4), NO2, CN, CO2H, CO2(alifático C1-4), CONH2, CONH(alifático C1-4), CON(alifático C1-4)2, O(haloalifático C1-4) o haloalifático C1-4; o dos R', junto con los átomos a los que están unidos, forman =O, un carbociclilo o heterociclilo opcionalmente sustituido de 3-6 miembros; cada Rö es, de modo independiente, H o alquilo C1-2.
ARP060104841A 2005-11-03 2006-11-03 Aminopirimidinas sustituidas con tiazol o pirazol,utiles como agentes anticancer y composiciones farmaceuticas que las contienen. AR056763A1 (es)

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ARP060104841A AR056763A1 (es) 2005-11-03 2006-11-03 Aminopirimidinas sustituidas con tiazol o pirazol,utiles como agentes anticancer y composiciones farmaceuticas que las contienen.
ARP060104842A AR057874A1 (es) 2005-11-03 2006-11-03 Aminopirimidinas utiles como inhibidores de quinasa
ARP060104843A AR056764A1 (es) 2005-11-03 2006-11-03 Aminopirimidinas utiles como inhibidores de quinasa

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ARP060104843A AR056764A1 (es) 2005-11-03 2006-11-03 Aminopirimidinas utiles como inhibidores de quinasa

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US (7) US7820685B2 (es)
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JP (5) JP5249771B2 (es)
KR (3) KR20080067693A (es)
CN (3) CN101316843B (es)
AR (3) AR056763A1 (es)
AU (3) AU2006311830B2 (es)
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CA (3) CA2627830A1 (es)
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SG (2) SG166827A1 (es)
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HUP0302173A2 (hu) 2000-09-15 2003-09-29 Vertex Pharmaceuticals Incorporated Protein kináz inhibitorokként alkalmazható pirazolvegyületek
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
WO2004072029A2 (en) 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
PT1853588E (pt) * 2005-02-16 2008-08-25 Astrazeneca Ab Compostos químicos
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CA2685876A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
CA2694381A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247595A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
CN101687852A (zh) * 2007-05-24 2010-03-31 沃泰克斯药物股份有限公司 可用作激酶抑制剂的噻唑类和吡唑类化合物
NZ624460A (en) 2009-03-20 2015-12-24 Vertex Pharma Process for making modulators of cystic fibrosis transmembrane conductance regulator

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