PE20040802A1 - Derivados de 3-(3,5-dioxo-4,5-dihidro-3h-[1,2,4]-triazin-2-il)-benzamidas como inhibidores del receptor p2x7 - Google Patents
Derivados de 3-(3,5-dioxo-4,5-dihidro-3h-[1,2,4]-triazin-2-il)-benzamidas como inhibidores del receptor p2x7Info
- Publication number
- PE20040802A1 PE20040802A1 PE2003001267A PE2003001267A PE20040802A1 PE 20040802 A1 PE20040802 A1 PE 20040802A1 PE 2003001267 A PE2003001267 A PE 2003001267A PE 2003001267 A PE2003001267 A PE 2003001267A PE 20040802 A1 PE20040802 A1 PE 20040802A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- triazin
- dioxo
- benzamide
- dihydro
- Prior art date
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- C07D253/06—1,2,4-Triazines
- C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
- C07D253/07—1,2,4-Triazines having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D253/075—Two hetero atoms, in positions 3 and 5
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- C07D253/06—1,2,4-Triazines
- C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
- C07D253/07—1,2,4-Triazines having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract
SE REFIERE A COMPUESTOS DE FORMULA I, EN LA QUE R1 ES ALQUILO(C1-C6), OPCIONALMENTE SUSTITUIDO CON CICLOALQUILO(C3-C10), ARILO(C6-C10), HETEROCICLILO(C1-C10) O HETEROARILO(C1-C10), OPCIONALMENTE SUSTITUIDOS; R2 ES H, HALOGENO, -CN O UN ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON 1 A 3 GRUPOS HALO, HIDROXI, AMINO, CN, ALQUILO(C1-C6), ALCOXI(C1-C6), CF3, ENTRE OTROS; R3 ES UN HETEROCICLILO(C1-C10), UNIDO POR NITROGENO, DE FORMULA III O IV; DONDE R4 ES H, HALO, HIDROXI, -CN, OH-ALQUILO(C1-C6), ALQUILO(C1-C6), ALCOXI(C1-C6), -HO2C-, ALQUIL(C1-C6)-O-S-[(ALQUIL (C1-C6)-N], ENTRE OTROS; R7 ES H O ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDOS. SON COMPUESTOS PREFERIDOS: 2-CLORO-N-(1-HIDROXICICLOHEXILMETIL)-5-[4-(2-HIDROXI-3-METOXIPROPIL)-3,5-DIOXO-4,5-DIHIDRO-3H-[1,2,4]TRIAZIN-2-IL]BENZAMIDA, 2-CLORO-5-[4-(2,3-DIHIDROXIPROPIL)-3,5-DIOXO-4,5-DIHIDRO-3H-[1,2,4]-TRIAZIN-2-IL]-N-(1-HIDROXICICLOHEXILMETIL)BENZAMIDA, 2-CLORO-5-(4-CIANOMETIL-3,5-DIOXO-4,5-DIHIDRO-3H-[1,2,4]TRIAZIN-2-IL)-N-(1-HIDROXICICLOHEPTILMETIL)BENZAMIDA, ENTRE OTROS.ESTOS COMPUESTOS SON INHIBIDORES DEL RECEPTOR P2X7 Y SON UTILES PARA EL TRATAMIENTO DE TRANSTORNOS MEDIADOS POR IL-1 COMO ENFERMEDADES INFLAMATORIAS, OSTEOARTRITIS Y ARTRITIS REUMATOIDEA, ALERGIAS, ASMA, COPD Y OTROS TRANSTORNOS
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BRPI0512781A (pt) | 2004-06-29 | 2008-04-08 | Pfizer Prod Inc | método para preparação de derivados de 5-{4-(2-hidroxi-propil)-3,5-dioxo-4,5-diidro-3h-[1,2,4]tria zin-2-il}-benzamida através da desproteção dos precursores de protetores de hidroxila |
EP1768965A1 (en) | 2004-06-29 | 2007-04-04 | Pfizer Products Incorporated | Method for preparing 5-¬4-(2-hydroxy-ethyl)-3,5-dioxo-4,5-dihydro-3h-¬1,2,4|-triazin-2-yl|benzamide derivatives with p2x7 inhibiting activity by reaction of the derivative unsubstituted in 4-position of the triazine with an oxiran in the presence of a lewis acid |
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2003
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