SV2003000861A - Derivados de eteres utiles como agentes inhibidores de las isozimas pde4 ref. pc11896arms/bb - Google Patents

Derivados de eteres utiles como agentes inhibidores de las isozimas pde4 ref. pc11896arms/bb

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Publication number
SV2003000861A
SV2003000861A SV2002000861A SV2002000861A SV2003000861A SV 2003000861 A SV2003000861 A SV 2003000861A SV 2002000861 A SV2002000861 A SV 2002000861A SV 2002000861 A SV2002000861 A SV 2002000861A SV 2003000861 A SV2003000861 A SV 2003000861A
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SV
El Salvador
Prior art keywords
rent
nr16r17
ilo
replaced
nr22ac
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SV2002000861A
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English (en)
Inventor
Robert James Chambers
Thomas Victor Magee
Anthony Marfat
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Pfizer Prod Inc
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Publication of SV2003000861A publication Critical patent/SV2003000861A/es

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    • C—CHEMISTRY; METALLURGY
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
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    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/04—Antibacterial agents
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    • A61P31/10—Antimycotics
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    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
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    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
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    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D—HETEROCYCLIC COMPOUNDS
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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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Abstract

COMPUESTOS UTILES COMO INHIBIDORES DE LA PDE4 EN EL TRATAMIENTO DE ENFERMEDADES REGULADAS POR LA ACTIVACION DE EOSINOFILOS ESPECIALMENTE ASMA, BRONQUITIS CRONICA Y ENFERMEDAD PULMONAR OBSTRUCTIVA CRONICA, DE LA FORMULA, VER FORMULA EN LA QUE J ES 0 O 1, CON LA CONDICION DE QUE CUANDO J ES 0, N DE BE SER 2; K ES 0 O 1; M ES 1,2 O 3; N ES 1 O 2; W1 Y W2 SON -O-; -S(=O)T-, EN QUE T ES 0,1 O 2, O -N(R3)-; Y ES =C(R1A)- O -[N-(O)K-EN QUE K ES 0 O 1; R1A ES -H, -F, -CL, -CN, -NO2, ALQUILO(C1-C4) ALQUINILO(C2-C4), ALQUILO(C1-C3)FLUORADO, ALCOXI(C1-C3)FLUORADO, -OR16, O -C(=O)NR22AR22B; RA Y RB SON -H, -F, CF3, ALQULO(C1-C4)CICLOALQUILO(C3-C7), FENILO O BENCILO SUSTITUIDO CON 0-3 R10; O RA Y RB SE TOMAN JUNTOS PARA FORMAR UN RESTO ESPIRO EN QUE R Y S SON 0-4 CON LA CONDICION DE QUE R+S HA DE SER 1 PERO NO5; Y XA ES -CH2-, -CHF, -CF2; -NR15-, -O-, O -S(=O)T-, EN QUE T ES 0,1; RC Y RD SON LOS MISMOS QUE RA Y RB EXCEPTO QUE UNO DE ELLOS DEBE SER -H; R1 Y R2 SON -H, R1 Y R2 SON -H, -F, -CL, CN, -NOP2, ALQUILO(C1-C4), ALQUINILO(C2-C4), ALQUILO(C1-C3)FLUORADO, -OR16 O -C(=O)NR22AR22B; R3 ES -H, ALQUILO(C1-C4), FENILO, BENCILO O -OR16; R4, R5 Y R6 SON(A)-H, -F, -CL, ALQUILO(C2-C4), -R16, -OR16, -S(=O)PR6, -S(=O)R16, -C(=O)OR16, -OC(=O)R16CN, -NO2, C(=O)NR16R17, -OC(=O)NR16R17, -NR22AC(=O)NR16R17, -NR22AC(=NR12)NR16R17, -NR22AC(=NCN)NR16R17, -NR22AC(=N-NO2)NR16R17, -C=NR22A)NR16R17, -CH2C(=NR22A)NR16R17, -OC(=NR22A)NR16R17, -OC(=N-NO2)NR16R17 -NR16R17, -CH2NR16R17, -NR22AC(=O)R16, -NR22AC(=O)OR16, =NOR16, -NR22AS(=O)R17, -S(=O)PNR16R17; O -CH2C(=NR22)NR16R17; EN QUE P ES 0,1 O 2; (B)ALQUILO(C1-C4)O ALCOXI(C1-C4)SUSTITUIDO CON 0-3 DE -F O -CL; O 0 O 1 DE ALCOXI(C1-C2)-CARBONILO, ALQUIL(C1-C2)-CARBONILO O ALQUIL(C1-C2)-CARBONILOXI; O (C)FENILO, BENCILO, FURANILO, TETRAHIDROFURANILO, OXETANILO, TIENILO, TETRAHIDROTIENILO, PIRROLILO, PIRROLIDINILO, OXAZOLILO, OXAZOLIDINILO, ISOXAZOLILO, ISOXAZOLIDINILO, TIAZOLILO, TIAZOLIDINILO, ISOTIAZOZLILO, ISOTIAZOLIDINILO, PIRAZOLILO, PIRAZOLIDINILO, OXAZIAZOLILO, TIADIAZOLILO, IMIDAZOLIDINILO,, PIRIDINILO, PIRAZINILO, PIRIMIDINILO, PIRIDAZINILO, PIPERIDINILO, PIPERAZINILO, TRIAZOLILO, TRIAZINILO, TETRAZOLILO, PIRANILO, AZETIDINILO, MORFOLINILO, PARATIAZINILO, INDOLILO, BENZO[B]FURANILO, 2,3-DIHIDRO-BENZOFURANILO, 2-H-CROMENILO, CROMANILO, BENZOTIENILO, 1H-INDALILO, BENCIMIDAZOLILO, BENZOXAZOLILO, BENZOISOXAZOLILO, BENZOTIAZOLILO, QUINOLINILO, ISOQUINOLINILO, FTALAZINILO, QUINAZOLINILO, QUINOXALINILO O PURINILO, TODOS ELLOS SUSTITUIDOS CON 0-2 DE R14 O (D)R5 Y R6 SSE TOMAN CONJUNTAMENTE PARA FORMAR UN RESTO DE FORMULAS PARCIALES(1.3.1)HASTA(1.3.15); D ES UN GRUPO DE FORMULAS PARCIALES(1.1.1)HASTA(1.1.9):VER FORMULAS EN QUE Q ES 2 O 3, R9 HA DE SER -H; V ES 0-1 W3 ES -O-, N(R9)- O -OC(=O)-; R7 ES (A) -H; (B)ALQUILO(C1-C6), ALQUENILO(C2-C6) O ALQUINILO(C2-C6), TODOS ELLOS SUSTITUIDOS CON 0-3 DE R10; (C)-(CH2)U-CICLOALQUILO(C3-C7)EN QUE U ES 0-2 SUSTITUIDO CON 0-3 DE R10; O (D)FENILO O BENCILO SUSTITUIDO CON 0-3 DE R10; R8 ES (A)TETRAZOL-5-ILO, 1,2,4-TRIAZOL-3-ILO, 1,2,4-TRIAZOL-3-ON-5-ILO, 1,2,3-TRIAZOL-5-ILO, IMIDAZOL-2-ILO, IMIDAZOL-4-ILO, IMIDAZOLIDIN-2-ON-4-ILO, 1,2,4-OXADIAZOL-3-ILO, 1,2,4-OXADIAZOL-5-ON-3-ILO, 1,2,4-OXADIAZOL-5-ILO, 1,2,4-OXADIAZOL--ON-5-ILO, 1,3,4-OXADIAZOLILO, 1,3,4-OXADIAZOL-2-ON-5-ILO, OXAZOLILO, ISOXAZOLILO, PIRROLILO, PIRAZOLILO, SUCCIMIDILO, GLUTARIMIDILO, PIRROLIDONILO, 2-PIPERIDONILO, 2-PIRIDONILO, PIRIDAZIN-3-ONILO, TIADIAZOLILO, PARATIAZINILO; (B)INDOLILO, INDOLINILO, ISOINDOLINILO, BENZO[B]FURANILO, 2,3-DIHIDROBENZOFURANILO, 2-H-CROMENILO, CROMANILO, BENZOTIENILO, 1H-INDAZOLILO, BENCIMIDAZOLILO, BENZOPXAZOLILO, BENZOISOXAZOLILO, BENZOTIAZOLILO, BENZOTRIAZOLILO, BENZOTRIAZINILO, QUINAZOLINILO, QUINOXALINILO, PIRAZOLO[3,4-D]PIRIMIDINILO, PIRIMIDO[4,5-D]PIRIDIMIDINILO, IMIDAZO[1,2-A]PIRIDINILO, PIRIDO-PIRIDINILO, PTERIDINILO O PURINILO, TODOS ELLOS OPCIONALMENTE SUSTITUIDOS EN UN ATOMO DE CABRONO CON R14, EN UN ATOMO DE NITROGENO CON R15 Y TODAS SUS FORMAS TAUTOMERAS EN UN ATOMO DE AZUFGRE CON 0-2 ATOMOS DE OXIGENO; R9 ES -H, ALQUIL(C1-C4)CICLOALQUILO(C3-C7)FENILO, BENCILO; -C(=O)OR16, -C(=O)R16, -OR16, ALQUIL(C1-C2)-OR16 O ALQUIL(C1-C2)-C(=O)OR16; O(C)-O-P)=O)(OH)2(FOSFORICO), -PG¿H(=O)OH(FOSFINICO), -P(=O)(OH)2(FOSFONICO)(OH)-O-ALQUILO(C1-C4)(ALQUIL FOSFONO)VER FORMULA, -S(=O)2NHS(=O)2R25, EN QUE R25 ES -H, -ALQUIL(C1-C4), FENILO O -OR16, J1 Y J2 SON UN RESTO QUE COMPRENDE UN SISTEMA ANULAR DE CARBONOS SATURADO O INSATURADO QUE ES MONOCICLICO DE 3 A 7 MIEMBROS, O QUE ES POLICICLICO CONDENSADO O DISCONTINUO DE 7 A 12 MIEMBROS; EN QUE OPCIONALMENTE UN ATOMO DE CARBONO DE DICHO SISTEMA ANULAR DE CARBONOS PUEDE SER REEMPLAZADO POR UN HETEROATOMO SELECCIONADO ENTRE N, O Y S; Y CUANDO SE SELECCIONA N, OPCIONALMENTE UN SEGUNDO ATOMO DE CARBONO DE ESTE PUEDE SER REEMPLAZADO POR UN HETEROATOMO SELECCIONADO ENTRE N, O Y S; O UNA SAL FARMACEUTICAMENTE ACEPTABLE DE ESTE.
SV2002000861A 2001-01-31 2002-01-30 Derivados de eteres utiles como agentes inhibidores de las isozimas pde4 ref. pc11896arms/bb SV2003000861A (es)

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US (3) US6828333B2 (es)
EP (1) EP1373258B1 (es)
JP (1) JP2004518689A (es)
KR (1) KR20030070150A (es)
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