AR077280A1 - Pirimidinonas como inhibidores de pi3k, y composiciones farmaceuticas que los comprenden - Google Patents
Pirimidinonas como inhibidores de pi3k, y composiciones farmaceuticas que los comprendenInfo
- Publication number
- AR077280A1 AR077280A1 ARP100102306A ARP100102306A AR077280A1 AR 077280 A1 AR077280 A1 AR 077280A1 AR P100102306 A ARP100102306 A AR P100102306A AR P100102306 A ARP100102306 A AR P100102306A AR 077280 A1 AR077280 A1 AR 077280A1
- Authority
- AR
- Argentina
- Prior art keywords
- nrc5rd5
- alkyl
- nrc1rd1
- nrc5c
- heterocycloalkyl
- Prior art date
Links
- 239000012828 PI3K inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 21
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 20
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 19
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 19
- 125000001072 heteroaryl group Chemical group 0.000 abstract 19
- 125000005843 halogen group Chemical group 0.000 abstract 16
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 15
- 125000003118 aryl group Chemical group 0.000 abstract 14
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 13
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 13
- 125000001424 substituent group Chemical group 0.000 abstract 13
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 11
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 10
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 9
- 125000005311 halosulfanyl group Chemical group 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 229910052799 carbon Inorganic materials 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 102100038417 Cytoplasmic FMR1-interacting protein 1 Human genes 0.000 abstract 3
- 101710181791 Cytoplasmic FMR1-interacting protein 1 Proteins 0.000 abstract 3
- 108091007960 PI3Ks Proteins 0.000 abstract 3
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 abstract 3
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 101100310920 Caenorhabditis elegans sra-2 gene Proteins 0.000 abstract 2
- 101100310926 Caenorhabditis elegans sra-3 gene Proteins 0.000 abstract 2
- 101100150278 Caenorhabditis elegans srb-5 gene Proteins 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- -1 C1- alkyl 6 Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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Abstract
Pirimidinonas que modulan la actividad de fosfoinosítido 3-quinasas (PI3Ks) que son utiles en el tratamiento de enfermedades relacionadas con la actividad de PI3Ks que incluyen, por ejemplo, trastornos inflamatorios, trastornos de base inmune, cáncer, y otras enfermedades. Reivindicacion 1: Un compuesto caracterizado porque es de formula (1) o (2) o una sal aceptable farmacéuticamente del mismo, donde A es alquilo C1-10, arilo, heteroarilo, cicloalquilo, o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, y S(O)2NRcRd; donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, o heterocicloalquilo está opcionalmente sustituido con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, y S(O)2NRcRd; L se encuentra ausente o es (CR7aR7b)m, (CR7aR7b)pO(CR7aR7b)q, (CR7aR7b)pS(CR7aR7)q, (CR7aR7b)S(O)(CR7aR7b)q, (CR7aR7b)pS(O)2(CR7aR7b)q, (CR7aR7b)pN R7c(CR7aR7b)q, (CR7aR7b)pNR7cC(O)NR7c(CR7aR7b)q, (CR7aR7b)pNR7cC(O)O(CR7aR7b)q, (CR7aR7b)pNR7cC(=NR7d)NR7c(CR7aR7b)q, o (CR7aR7)pNR7cS(O)2(CR7aR7b)q; W es N o CR3; X es N o CR4; Y es N o CR5; Z es N o CR6; G es O, S, o NRN; R1 es ORA, SRA, S(O)RA, S(O)2RA, NRARB, NRcC(O)NRARB, NRcC(O)ORA, NRcC(=NRE)NRARB, N RcS(O)2RA, NRcS(O)2NRcRA, heterocicloalquilo, o heteroarilo, donde dicho heterocicloalquilo o heteroarilo está opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados en forma independiente entre -(alquil C1-4)r-Cy1, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, y S(O)2NRc1Rd1; R2a y R2b se seleccionan en forma independiente entre H, halo, OH, CN, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, y heterocicloalquilalquilo, donde dicho alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe)NRc2Rd2, NRc2C(=NRe)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, y S(O)2NRc2Rd2; o R2a y R2b junto con el átomo de carbono al cual se encuentran unidos forman un anillo cicloalquilo de 3, 4, 5, 6 o 7 miembros o un anillo heterocicloalquilo de 3, 4, 5, 6, o 7 miembros, cada uno opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe)NRc2Rd2, NRc2C(=NRe)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, y S(O)2NRc2Rd2; R3, R4, R5, y R6 se seleccionan en forma independiente entre H, halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, NRc3Rd3, NRc3C(O)Rb3, N Rc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)2NRc3Rd3, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, o heterocicloalquilalquilo, donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre alquilo C1-6, haloalquilo C1-6, halo, CN, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(=NRe)NRc3Rd3, NRc3C(=NRe)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, y S(O)2NRc3Rd3; R7a y R7b se seleccionan en forma independiente entre H, halo, o alquilo C1-4; R7c es H o alquilo C1-4; R7d es H, CN, NO2, ORa5, SRb5, S(O)2Rb5, C(O)Rb5, S(O)2NRc5Rd5, C(O)NRc5Rd5; RA es heteroarilo, heterocicloalquilo, heteroarilalquilo, o heterocicloalquilalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre -(alquil C1-4)r-Cy1, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, y S(O)2NRc1Rd1; RB y Rc se seleccionan en forma independiente entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, y heterocicloalquilalquilo, donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, y S(O)2NRc5Rd5; RE es H, CN, NO2, ORa5, SRb5, S(O)2Rb5, C(O)Rb5, S(O)2NRc5Rd5, o C(O)NRc5Rd5; RN es H o alquilo C1-4; Cy1 es arilo, heteroarilo, cicloalquilo, o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, y S(O)2NRc1Rd1; Ra, Rb, Rc, y Rd se seleccionan en forma independiente entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, y heterocicloalquilalquilo, donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, y S(O)2NRc5Rd5; o Rc y Rd junto con el átomo de N al cual están unidos forman un grupo heterocicloalquilo o heteroarilo de 3, 4, 5, 6 o 7 miembros, cada uno opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados en forma independiente entre alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, y S(O)2NRc5Rd5; Ra1, Rb1, Rc1, y Rd1 se seleccionan en forma independiente entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, y heterocicloalquilalquilo, donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, y S(O)2NRc5Rd5, o Rc1 y Rd1 junto con el átomo de N al cual están unidos forman un grupo heterocicloalquilo o heteroarilo de 3, 4, 5, 6 o 7 miembros, cada uno opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados en forma independiente entre alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, y S(O)2NRc5Rd5; Ra2, Rb2, Rc2, y Rd2 se seleccionan en forma independiente entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6,
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