AR036042A1 - Derivados aralquilsufonil-3-(pirrol-2-ilmetiliden)-2-indolinona, sus composiciones farmaceuticas y metodo para la modulacion de la actividad catalitica de una proteina quinasa - Google Patents
Derivados aralquilsufonil-3-(pirrol-2-ilmetiliden)-2-indolinona, sus composiciones farmaceuticas y metodo para la modulacion de la actividad catalitica de una proteina quinasaInfo
- Publication number
- AR036042A1 AR036042A1 ARP020102024A ARP020102024A AR036042A1 AR 036042 A1 AR036042 A1 AR 036042A1 AR P020102024 A ARP020102024 A AR P020102024A AR P020102024 A ARP020102024 A AR P020102024A AR 036042 A1 AR036042 A1 AR 036042A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- heterocyclylalkyl
- alkylaminoalkyl
- dialkylaminoalkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Abstract
Se describen determinados derivados 5-aralquilsulfonil-3-(pirrol-2-il-metiliden)-2-indolinona que inhiben quinasas, en particular, la met quinasa, de fórmula (1)donde: n es 0, 1 o 2; m es 1, 2 o 3; R1 y R2 son independientemente hidrógeno o alquilo; R3, R4 y R5 son independientemente hidrógeno, halo, alquilo, cicloalquilo, haloalquilo, hidroxilo, alcoxilo, alcoxicarbonilo, haloalcoxilo, ciano, carboxilo, carboxialquilo, nitro, arilo, ariloxilo, heteroarilo, heteroariloxilo, -(alquilen)-CONR10R11, -CONR10R11, o NR10R11, (donde R10 es hidrógeno o alquilo; y R11 es arilo, heteroarilo, heterociclo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, hidroxialquilo, acetilalquilo, cianoalquilo, carboxialquilo, alcoxicarbonilalquilo, heteroaralquilo, aralquilo, o heterociclilalquilo, donde la cadena de alquilo en aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, aralquilo, heteroaralquilo,o heterociclilalquilo está opcionalmente sustituida con uno o dos hidroxilos, o R10 y R11, junto con el átomo de nitrógeno al que están unidos, se combinan para formar un heterocicloamino saturado o insaturado); R6 es hidrógeno, alquilo, cicloalquilo, hidroxialquilo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, carboxialquilo, heterociclilalquilo, arilo, heteroarilo, carboxilo, alcoxicarbonilo, heterociclilcarbonilo, aminoalquilcarbonilo, alquilaminoalquilcarbonilo, dialquilaminoalquilcarbonilo, -CONR10R11 o -(alquilen)-CONR10R11 (donde R10 es hidrógeno o alquilo, y R11 es arilo, heteroarilo, heterociclo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, hidroxialquilo, acetilalquilo, cianoalquilo, carboxialquilo, alcoxicarbonilalquilo, heteroaralquilo, aralquilo, o heterociclilalquilo, donde la cadena de alquilo en aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, aralquilo, heteroaralquilo,o heterociclilalquilo está opcionalmente sustituida con uno o dos hidroxilos, o R10 y R11, junto con el átomo de nitrógeno al que están unidos, se combinan para formar un heterocicloamino saturado o insaturado); R7 y R8 son independientemente hidrógeno, alquilo, cicloalquilo, heterociclilalquilo, -COR12, -(alquilen)-COR12 (donde R12 es alcoxilo, hidroxilo, o heterociclilo, alquilamino, dialquilamino), -SO2R14, -CONR13R14, o -(alquilen)-CONR13R14 (donde R13 es hidrógeno o alquilo, y R14 es aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, hidroxialquilo, acetilalquilo, cianoalquilo, carboxialquilo, alcoxicarbonilalquilo, heteroaralquilo, o heterociclilalquilo, donde la cadena de alquilo en aminoalquilo, heteroaralquilo, o heterociclilalquilo está opcionalmente sustituida con uno o dos grupos hidroxilo, o cuando R13 y R14 están unidos a un átomo de nitrógeno; R13 y R14, junto con el átomo de nitrógeno al que están unidos, forman un heterocicloamino saturado o insaturado); R6 y R7 o R7 y R8 pueden combinarse para formar un anillo saturado o insaturado de 5 a 8 miembros; y R9 es: (a) hidrógeno o alquilo; (b) -PO(OR15)2 donde cada R15 es independientemente hidrógeno o alquilo; (c) -COR16 donde R16 es hidrógeno o alquilo; o (d) -CHR17NR18R19 donde R17 es hidrógeno o alquilo; y R18 y R19 son independientemente hidrógeno o alquilo o R18 y R19, junto con el átomo de nitrógeno al que están unidos forman heterocicloamino; o una sal de los mismos aceptable para el uso farmacéutico. También, se describen composiciones farmacéuticas que comprenden estos compuestos, métodos para tratar enfermedades mediadas por quinasas utilizando estos compuestos, y métodos para prepararlas.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US29454401P | 2001-05-30 | 2001-05-30 | |
US32840801P | 2001-10-10 | 2001-10-10 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR036042A1 true AR036042A1 (es) | 2004-08-04 |
Family
ID=26968598
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP020102024A AR036042A1 (es) | 2001-05-30 | 2002-05-30 | Derivados aralquilsufonil-3-(pirrol-2-ilmetiliden)-2-indolinona, sus composiciones farmaceuticas y metodo para la modulacion de la actividad catalitica de una proteina quinasa |
Country Status (5)
Country | Link |
---|---|
US (1) | US6599902B2 (es) |
AR (1) | AR036042A1 (es) |
AU (1) | AU2002303892A1 (es) |
PE (1) | PE20030062A1 (es) |
WO (1) | WO2002096361A2 (es) |
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BR9916223A (pt) | 1998-12-17 | 2001-09-04 | Hoffmann La Roche | 4-ariloxindóis como inibidores de cinases de proteìna jnk |
AU760964B2 (en) | 1998-12-31 | 2003-05-22 | Sugen, Inc. | 3-heteroarylidenyl-2-indolinone compounds for modulating protein kinase activityand for use in cancer chemotherapy |
CA2368041A1 (en) | 1999-03-24 | 2000-09-28 | Sugen, Inc. | Indolinone compounds as kinase inhibitors |
AR034118A1 (es) | 2000-02-15 | 2004-02-04 | Sugen Inc | Compuestos de 2-indolinonas sustituidas con pirroles inhibidoras de proteinquinasas; sus composiciones farmaceuticas e intermediarios de sintesis |
TWI270545B (en) | 2000-05-24 | 2007-01-11 | Sugen Inc | Mannich base prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives |
-
2002
- 2002-05-30 US US10/157,007 patent/US6599902B2/en not_active Expired - Fee Related
- 2002-05-30 PE PE2002000458A patent/PE20030062A1/es not_active Application Discontinuation
- 2002-05-30 WO PCT/US2002/016841 patent/WO2002096361A2/en not_active Application Discontinuation
- 2002-05-30 AR ARP020102024A patent/AR036042A1/es unknown
- 2002-05-30 AU AU2002303892A patent/AU2002303892A1/en not_active Abandoned
Also Published As
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US6599902B2 (en) | 2003-07-29 |
PE20030062A1 (es) | 2003-02-08 |
AU2002303892A1 (en) | 2002-12-09 |
WO2002096361A2 (en) | 2002-12-05 |
US20030125370A1 (en) | 2003-07-03 |
WO2002096361A3 (en) | 2003-03-13 |
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