AR066958A1 - IMIDAZOPIRAZINS AS INHIBITORS OF PROTEIN QUINASA - Google Patents

IMIDAZOPIRAZINS AS INHIBITORS OF PROTEIN QUINASA

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Publication number
AR066958A1
AR066958A1 ARP080102481A ARP080102481A AR066958A1 AR 066958 A1 AR066958 A1 AR 066958A1 AR P080102481 A ARP080102481 A AR P080102481A AR P080102481 A ARP080102481 A AR P080102481A AR 066958 A1 AR066958 A1 AR 066958A1
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AR
Argentina
Prior art keywords
alkyl
heterocyclyl
alkylc
heteroaryl
aryl
Prior art date
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ARP080102481A
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Spanish (es)
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Schering Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40002934&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR066958(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of AR066958A1 publication Critical patent/AR066958A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Métodos de preparacion de dichos compuestos, composiciones farmacéuticas que incluyen uno o más de dichos compuestos, métodos de preparacion de formulaciones farmacéuticas que incluyen uno o más de dichos compuestos, y métodos de tratamiento, prevencion, inhibicion, o mejoramiento de una o más enfermedades asociadas con las proteínas o Aurora quinasas que utilizan dichos compuestos o composiciones farmacéuticas. Reivindicacion 1: Un compuesto de la formula 1: o una sal, solvato, éster o prodroga farmacéuticamente aceptable del mismo, en donde: R es H, CN, -NR5R6, cicloalquilo, cicloalquenilo, heterociclenilo, heteroarilo, -C(O)NR5R6, -N(R5)C(O)R6, heterociclilo, heteroarilo sustituido con (CH2)1-3NR5R6, alquilo no sustituido, o alquilo sustituido con uno o más restos los cuales pueden ser los mismos o diferentes, estando cada resto independientemente seleccionado del grupo integrado por -OR5, heterociclilo, -N(R5)C(O)N(R5R6), -N(R5)-C(O)OR6, -(CH2)13-N(R5R6) y -NR5R6; R1 es H, halo, arilo o heteroarilo, en donde cada uno de dichos arilo y heteroarilo pueden estar no sustituidos o sustituidos con uno o más restos los cuales pueden ser los mismos o diferentes estando cada resto independientemente seleccionado del grupo integrado por halo, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo, heterociclilo, -CH2OR5, -C(O)NR5R6, -C(O)OH, -C(O)NH2, -NR5R6 (en donde los R5 y R6, conjuntamente con el N de dicho -NR5R6, forman un anillo heterociclilo), -S(O)R5, -S(O2)R5, -CN, -CHO, -SR5, -C(O)OR5, -C(O)R5 y -OR5; R2 es H, halo, arilo, arilalquilo o heteroarilo, en donde cada uno de dichos arilo, arilalquilo y heteroarilo pueden estar no sustituidos u opcionalmente independientemente sustituidos con uno o más restos los cuales pueden ser los mismos o diferentes estando cada resto independientemente seleccionado del grupo integrado por halo, amida, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, -C(O)OH, -C(O)NH2, -NR5R6 (en donde los R5 y R6, conjuntamente con el N de dicho -NR5R6, forman un anillo heterociclilo), -CN, arilalquilo, -CH2OR5, -S(O)R5, -S(O2)R5, -CN, -CHO, -SR5, -C(O)OR5, -C(O)R5, heteroarilo y heterociclilo; R3 es heterociclil-(CR7R8)n-X, heterociclenil-(CR7R8)n-X, heteroaril-(CR7R8)n-X o aril-(CR7R8)n-X en donde cada uno de los restos heterociclil-, heterociclenil-, heteroaril- o aril- de dicho R3 pueden estar no sustituidos o sustituidos con uno o más restos, independientemente seleccionados del grupo integrado por -CONR5R6, -OR5 y alquilo, n es 1-6, X está seleccionado del grupo integrado por -NR5R6, -OR5, -SO-R5, -SR5, SO2R5, heteroarilo, heterociclilo y arilo, en donde dicho heteroarilo o arilo puede estar no sustituidos o sustituido con uno o más restos, independientemente seleccionados del grupo integrado por -O-alquilo, alquilo, halo, o NR5R6; R7 y R8 son cada uno independientemente hidrogeno, alquilo, heterociclilo, arilo, heteroarilo o cicloalquilo; R5 está seleccionado del grupo integrado por hidrogeno, alquilo, alquenilo, alcoxialquilo, -alquil-S-alquilo, aminoalquilo, arilo, heteroarilo, heterociclenilo, heterocicloalquilo, cicloalquilo, ciclenilo, heterociclilalcoxilo, -S-alquilheterociclilo, heterociclilo, heterociclenilo, alquilN(alquilo)2, alquilNH(alquilo), alquilN(alquenilo)2, -alquilN(alcoxilo)2, -alquil-SH, hidroxialquilo, trihaloalquilo, dihaloalquilo, monohaloalquio, en donde cada uno de dichos alquilo, alquenilo, alcoxialquilo, -alquil-S-alquilo aminoalquilo, arilo, heteroarilo, heterociclenilo, heterocicloalquilo, cicloalquilo, ciclenilo, heterociclilalcoxilo, -S-alquilheterociclilo, heterociclilo, heterociclenilo, alquilN(alquilo)2, alquilNH(alquilo), alquilN(alquenilo)2, -alquilN(alcoxilo)2, -alquil-SH, hidroxialquilo, trihaloalquilo, dihaloalquilo, monohaloalquilo pueden estar no sustituidos o sustituidos con uno o más restos independientemente seleccionados del grupo integrado por alquilo, alquenilo, arilo, ciclenilo, cicloalquilo, arilalquilo, ciclenilalquilo, cicloalquilalquilo, heteroarilo, heterociclenilo, heterociclilo, heteroarilalquilo, heterociclenilalquilo, heterocicloalquilalquilo, alcoxialquilo, -alquil-S-alquilo, -alquilSH, alcoxilo, -Salquilo, hidroxialquilo, y aminoalquilo; R6 está seleccionado del grupo integrado por hidrogeno, alquilo, alquenilo, arilo, ciclenilo, cicloalquilo, arilalquilo, ciclenilalquilo, cicloalquilalquilo, heteroarilo, heterociclenilo, heterociclilo, heteroarilalquilo, heterociclenilalquilo, heterocicloalquilalquilo, alcoxialquilo, -alquil-S-alquilo, -alquilSH, alcoxilo, -S-alquilo, hidroxialquilo, aminoalquilo, -alquil-OC(O)alquilo, -alquilOC(O)cicloalquilo, -alquilOC(O)arilo, -alquilOC(O)aralquilo, -alquilOC(O)NR5arilo, -alquilOC(O)NR5alquilo, -alquilOC(O)NR5heterociclilo, -alquilOC(O)NR5heteroaril-alquilOC(O)NR5cicloalquilo, -alquilOC(O)heterociclilo, alquilOC(O)OH, alquilC(O)Oalquilo, -alquiIC(O)Ocicloalquilo, -alquiIC(O)Oarilo, -alquilC(O)Oaralquilo, -alquilC(O)ONR5arilo, -alquilC(O)ONR5alquilo, -alquilC(O)ONR5heterociclilo, -alquilC(O)ONR5heteroaril-alquilC(O)ONR5cicloalquilo, -alquilC(O)Oheterociclilo, alquilC(O)OH, y alquilC(O)Oalquilo en donde cada uno de dichos arilo, ciclenilo, cicloalquilo, arilalquilo, ciclenilalquilo, cicloalquilalquilo, heteroarilo, heterociclenilo, heterociclilo, heteroarilalquilo, heterociclenilalquilo, heterocicloalquilalquilo, -alquilOC(O)alquilo, -alquilOC(O)cicloalquilo, -alquilOC(O)arilo, -alquilOC(O)aralquilo, -alquilOC(O)NR5arilo, -alquilOC(O)NR5alquilo, -alquilOC(O)NR5heterociclilo, -alquilOC(O)NR5heteroaril-alquilOC(O)NR5cicloalquilo, -alquilOC(O)heterociclilo, alquilC(O)OH, alquilC(O)Oalquilo, -alquilC(O)Ocicloalquilo, -alquilC(O)Oarilo, -alquilC(O)Oaralquilo, -alquilC(O)ONR5arilo, -alquilC(O)ONR5alquilo, -alquilC(O)ONR5heterociclilo, -alquilC(O)ONR5heteroaril-alquilC(O)ONR5cicloalquilo, -alquilC(O)Oheterociclilo, alquilC(O)OH, y alquilC(O)Oalquilo, pueden estar no sustituidos o sustituidos con uno o más restos independientemente seleccionados del grupo integrado por alquilo, alquenilo, arilo, ciclenilo, cicloalquilo, arilalquilo, ciclenilalquilo, cicloalquilalquilo, heteroarilo, heterociclenilo, heterociclilo, heteroarilalquilo, heterociclenilalquilo, heterocicloalquilalquilo, alcoxialquilo, -alquil-S-alquilo, -alquilSH, alcoxilo, -Salquilo, hidroxialquilo, aminoalquilo, amino, aminodialquilo, aminocicloalquilo, halo, trihaloalquilo, dihaloalquilo, y monohaloalquilo; además en donde en cualquier -NR5R6 en la Formula 1, dichos R5 y R6 pueden opcionalmente estar unidos conjuntamente con el N de dicho -NR5R6 para formar un anillo cíclico o un anillo cíclico en puente, en donde cada uno de dichos anillo cíclico o anillo cíclico en puente, puede estar no sustituido o sustituido con uno o más restos, los cuales pueden ser los mismos o diferentes, independientemente seleccionados del grupo integrado por hidroxilo, -SH, alquilo, alquenilo, hidroxialquilo, -alquil-SH, alcoxilo, -S-alquilo, -CO2-alquilo, -CO2-alquenilo, arilalquilo, ciclenilalquilo, cicloalquilalquilo, heteroarilalquilo, heterociclenilalquilo, heterocicloalquilalquilo, heteroarilo, arilo, ciclenilo, cicloalquilo, espiroheterociclilo, espiroheterociclenilo, espiroheteroarilo, espirociclilo, espirociclenilo, espiroarilo, alcoxialquilo, -alquil-S-alquilo, heterociclilo, heterociclenilo, halo, trihaloalquilo, dihaloalquilo, CN y monohaloalquilo.Methods of preparing said compounds, pharmaceutical compositions that include one or more of said compounds, methods of preparing pharmaceutical formulations that include one or more of said compounds, and methods of treatment, prevention, inhibition, or improvement of one or more associated diseases with the proteins or Aurora kinases that use said compounds or pharmaceutical compositions. Claim 1: A compound of the formula 1: or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, wherein: R is H, CN, -NR5R6, cycloalkyl, cycloalkenyl, heterocyclynyl, heteroaryl, -C (O) NR5R6 , -N (R5) C (O) R6, heterocyclyl, heteroaryl substituted with (CH2) 1-3NR5R6, unsubstituted alkyl, or alkyl substituted with one or more moieties which may be the same or different, each moiety being independently selected from the group consisting of -OR5, heterocyclyl, -N (R5) C (O) N (R5R6), -N (R5) -C (O) OR6, - (CH2) 13-N (R5R6) and -NR5R6; R1 is H, halo, aryl or heteroaryl, wherein each of said aryl and heteroaryl may be unsubstituted or substituted with one or more moieties which may be the same or different, each moiety being independently selected from the group consisting of halo, alkyl , alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, -CH2OR5, -C (O) NR5R6, -C (O) OH, -C (O) NH2, -NR5R6 (where R5 and R6, together with N of said -NR5R6, form a heterocyclyl ring), -S (O) R5, -S (O2) R5, -CN, -CHO, -SR5, -C (O) OR5, -C (O) R5 and - OR5; R2 is H, halo, aryl, arylalkyl or heteroaryl, wherein each of said aryl, arylalkyl and heteroaryl may be unsubstituted or optionally independently substituted with one or more moieties which may be the same or different with each moiety independently selected from group consisting of halo, amide, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, -C (O) OH, -C (O) NH2, -NR5R6 (wherein R5 and R6, together with the N of said -NR5R6, form a heterocyclyl ring), -CN, arylalkyl, -CH2OR5, -S (O) R5, -S (O2) R5, -CN, -CHO, -SR5, -C (O) OR5, -C (O) R5 , heteroaryl and heterocyclyl; R3 is heterocyclyl- (CR7R8) nX, heterocyclynyl- (CR7R8) nX, heteroaryl- (CR7R8) nX or aryl- (CR7R8) nX wherein each of the heterocyclyl-, heterocyclyl-, heteroaryl- or aryl- moieties of said R3 they may be unsubstituted or substituted with one or more moieties, independently selected from the group consisting of -CONR5R6, -OR5 and alkyl, n is 1-6, X is selected from the group consisting of -NR5R6, -OR5, -SO-R5, -SR5, SO2R5, heteroaryl, heterocyclyl and aryl, wherein said heteroaryl or aryl may be unsubstituted or substituted with one or more moieties, independently selected from the group consisting of -O-alkyl, alkyl, halo, or NR5R6; R7 and R8 are each independently hydrogen, alkyl, heterocyclyl, aryl, heteroaryl or cycloalkyl; R5 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkoxyalkyl, -alkyl-S-alkyl, aminoalkyl, aryl, heteroaryl, heterocyclynyl, heterocycloalkyl, cycloalkyl, ciclenyl, heterocyclylalkoxy, -S-alkylheterocyclyl, heterocyclyl, heterocyclyl, heterocyclyl, heterocyclyl, heterocyclyl, heterocyclyl, heterocyclyl, heterocyclyl, heterocyclyl, heterocyclyl ) 2, alkyl NH (alkyl), alkyl N (alkenyl) 2, -alkylN (alkoxy) 2, -alkyl-SH, hydroxyalkyl, trihaloalkyl, dihaloalkyl, monohaloalkyl, wherein each of said alkyl, alkenyl, alkoxyalkyl, -alkyl-S -alkyl aminoalkyl, aryl, heteroaryl, heterocyclynyl, heterocycloalkyl, cycloalkyl, ciclenyl, heterocyclylalkoxy, -S-alkylheterocyclyl, heterocyclyl, heterocyclynyl, alkylN (alkyl) 2, alkylNH (alkyl), alkylN (alkenyl) 2-alkynyl , -alkyl-SH, hydroxyalkyl, trihaloalkyl, dihaloalkyl, monohaloalkyl may be unsubstituted or substituted with one or more moieties independently selected from the group consisting of alkyl, alkenyl, aryl, ci Chenyl, cycloalkyl, arylalkyl, cyclylalkyl, cycloalkylalkyl, heteroaryl, heterocyclynyl, heterocyclyl, heteroarylalkyl, heterocyclylalkyl, heterocycloalkylalkyl, alkoxyalkyl, -alkyl-S-alkyl, -alkyl-H-alkyl, alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl; R6 is selected from the group consisting of hydrogen, alkyl, alkenyl, aryl, ciclenyl, cycloalkyl, arylalkyl, ciclenylalkyl, cycloalkylalkyl, heteroaryl, heterocyclynyl, heterocyclyl, heteroarylalkyl, heterocyclylalkyl, heterocycloalkylalkyl, alkylalkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl-alkyl , -S-alkyl, hydroxyalkyl, aminoalkyl, -alkyl-OC (O) alkyl, -alkylOC (O) cycloalkyl, -alkylOC (O) aryl, -alkylOC (O) aralkyl, -alkylOC (O) NR5aryl, -alkylOC ( O) NR5alkyl, -alkylOC (O) NR5heterocyclyl, -alkylOC (O) NR5heteroaryl -alkylOC (O) NR5cycloalkyl, -alkylOC (O) heterocyclyl, alkylOC (O) OH, alkylC (O) Oalkyl, -alkyl (O) Occycloalkyl -alkyl (O) Oaryl, -alkylC (O) Oaralkyl, -alkylC (O) ONR5aryl, -alkylC (O) ONR5alkyl, -alkylC (O) ONR5heterocyclyl, -alkyl C (O) ONR5heteroaryl-alkylC (O) ONR5alkyl-alkyl, (O) Oheterocyclyl, alkylC (O) OH, and alkylC (O) Oalkyl wherein each of said aryl, cyclynyl, cycloalkyl, arylalkyl, cyclylalkyl, cycloalkylalkyl, heteroaryl, heterocyclynyl, heterocyclyl, heteroarylalkyl, heterocyclylalkyl, heterocycloalkylalkyl, -alkylOC (O) alkyl, -alkylOC (O) cycloalkyl, -alkylOC (O) aryl, -alkylOC (O) aralkyl, -5-alkyl-NR5-O -alkyl -C5 -alkyl-NR5-O -alkyl -C5 -alkyl-NR5-O -alkyl-NR5 alkylOC (O) NR5alkyl, -alkylOC (O) NR5heterocyclyl, -alkylOC (O) NR5heteroaryl -alkylOC (O) NR5cycloalkyl, -alkylOC (O) heterocyclyl, alkylC (O) OH, alkylC (O) Oalkyl, -alkylC (O) Occycloalkyl, -alkylC (O) Oaryl, -alkylC (O) Oaralkyl, -alkylC (O) ONR5aryl, -alkylC (O) ONR5alkyl, -alkylC (O) ONR5heterocyclyl, -alkylC (O) ONR5heteroaryl-alkylC (O) ONR5, -C (O) alkylheterocyclyl, alkylC (O) OH, and alkylC (O) Oalkyl, may be unsubstituted or substituted with one or more moieties independently selected from the group consisting of alkyl, alkenyl, aryl, ciclenyl, cycloalkyl, arylalkyl, cyclylalkyl , cycloalkylalkyl, heteroaryl, heterocyclynyl, heterocyclyl, heteroarylalkyl, heterocyclylalkyl, heterocycloalkyl ilalkyl, alkoxyalkyl, -alkyl-S-alkyl, -alkylSH, alkoxy, -Salkyl, hydroxyalkyl, aminoalkyl, amino, aminodialkyl, aminocycloalkyl, halo, trihaloalkyl, dihaloalkyl, and monohaloalkyl; further where in any -NR5R6 in Formula 1, said R5 and R6 may optionally be joined together with the N of said -NR5R6 to form a cyclic ring or a cyclic bridge ring, wherein each of said cyclic ring or ring bridge cyclic, may be unsubstituted or substituted with one or more moieties, which may be the same or different, independently selected from the group consisting of hydroxyl, -SH, alkyl, alkenyl, hydroxyalkyl, -alkyl-SH, alkoxy, - S-alkyl, -CO2-alkyl, -CO2-alkenyl, arylalkyl, ciclenilalquilo, cycloalkylalkyl, heteroarylalkyl, heterociclenilalquilo, heterocycloalkylalkyl, heteroaryl, aryl, ciclenilo, cycloalkyl, espiroheterociclilo, espiroheterociclenilo, espiroheteroarilo, spirocyclyl, espirociclenilo, espiroarilo, alkoxyalkyl, -C -S-alkyl, heterocyclyl, heterocyclynyl, halo, trihaloalkyl, dihaloalkyl, CN and monohaloalkyl.

ARP080102481A 2007-06-14 2008-06-11 IMIDAZOPIRAZINS AS INHIBITORS OF PROTEIN QUINASA AR066958A1 (en)

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US98793207P 2007-11-14 2007-11-14

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EP (1) EP2170892A2 (en)
JP (1) JP2010529195A (en)
CN (1) CN101772500A (en)
AR (1) AR066958A1 (en)
CA (1) CA2690557A1 (en)
CL (1) CL2008001745A1 (en)
MX (1) MX2009013729A (en)
PE (1) PE20090365A1 (en)
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