AR031251A1 - Derivado de pirimidina, composicion farmaceutica que lo comprende, su uso en la fabricacion de un medicamento y proceso de preparacion - Google Patents

Derivado de pirimidina, composicion farmaceutica que lo comprende, su uso en la fabricacion de un medicamento y proceso de preparacion

Info

Publication number
AR031251A1
AR031251A1 ARP010103279A ARP010103279A AR031251A1 AR 031251 A1 AR031251 A1 AR 031251A1 AR P010103279 A ARP010103279 A AR P010103279A AR P010103279 A ARP010103279 A AR P010103279A AR 031251 A1 AR031251 A1 AR 031251A1
Authority
AR
Argentina
Prior art keywords
6alkyl
optionally substituted
carbamoyl
6alkynyl
6alkenyl
Prior art date
Application number
ARP010103279A
Other languages
English (en)
Inventor
David Heaton
Ab Astrazeneca
Original Assignee
Ab Astrazeneca
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ab Astrazeneca filed Critical Ab Astrazeneca
Publication of AR031251A1 publication Critical patent/AR031251A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links

Abstract

Derivado de pirimidina de formula (1) donde R1 es halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, mercapto, C1-6alquilo, C2-6alquenilo o C2-6alquinilo; p es 0-4; donde los valores de R1 pueden ser iguales o diferentes: R2 es sulfamoilo o un grupo B-E; q es 0-2; donde los valores de R2 pueden ser iguales o diferentes; y donde p + q = 1-5; R3 es hidrogeno, C1-6alquilo, C2-6alquenilo, C2-6alquinilo o C3-8cicloalquilo; donde R3 puede ser opcionalmente sustituido en un carbono por uno o más M; R4 es C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C3-8cicloalquilo o heterociclilo; donde R4 puede ser opcionalmente sustituido por uno o más M; donde si dicho heterociclilo contiene una porcion ûNH- dicho nitrogeno puede ser opcionalmente sustituido por un grupo seleccionado entre Z; o R3 y R4 junto con el nitrogeno al cual están unidos forman un anillo heterocíclico opcionalmente sustituido en un carbono por uno o más M; donde si dicho anillo heterocíclico contiene una porcion ûNH- dicho nitrogeno puede ser opcionalmente sustituido por un grupo seleccionado entre Q; B se selecciona entre C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C3-8cicloalquilo, C3-8cicloalquilC1-6alquilo, fenilo, un grupo heterocíclico, fenilC1-6alquilo o (grupo heterocíclico)C1-6alquilo; donde B puede ser opcionalmente sustituido en un carbono por uno o más D; y donde si dicho grupo heterocíclico contiene una porcion ûNH- dicho nitrogeno puede ser opcionalmente sustituido por un grupo seleccionado entre G; E es ûC(O)-, N(Ra)C(O)-, -C(O)N(Ra)-, -S(O)r-, -SO2N(Ra)- o ûN(Ra)SO2-; donde R3 es hidrogeno o C1-6 alquilo opcionalmente sustituido por uno o más D y r es 1-2; D se selecciona independientemente entre halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C1-6alcoxi, C1-6alcanoilo, C1-6alcanoiloxi, N-(C1-6alquil)amino, N,N-((C1-6alquil)2amino, C1-6alcanoilamino, N-(C1-6alquil)carbamoilo, N,N-(C1-6alquil)2carbamoilo, C1-6alquilS(O)a, donde a es entre 0 y 2, C1-8alcoxicarbonilo, N-(C1-6alquil)sulfamoilo y N,N-(C1-6alquil)2sulfamoilo; donde D puede ser opcionalmente sustituido en un carbono por uno o más V; M se selecciona independientemente entre halo, nitro, ciano, hidroxi, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C1-6alcoxi, C1-6alcanoilo, C1-6alcanoiloxi, N-(C1-6alquil)amino, N,N-(C1-6alquil)2amino, C1-6alcanoilamino, N-(C1-6alquil)carbamoilo, N,N-(C1-6alquil)2carbamoilo, C1-6alquilS(O)a donde a es entre 0 y 2, C1-6alcoxicarbonilo, N-(C1-6alquil)sulfamoilo, N,N-(C1-6alquil)2sulfamoilo, C3-8cicloalquilo, fenilo o un grupo heterocíclico; donde M puede ser opcionalmente sustituido en un carbono por uno o más P; y donde si dicho grupo heterocíclico contiene una porcion û NH - dicho nitrogeno puede ser opcionalmente sustituido por un grupo seleccionado entre T; P, S y V se seleccionan independientemente entre halo, nitro, ciano, hidroxi, trifluorometoxi, trifluorometilo, amino, carboxi, carbamoilo, mercapto, sulfamoilo, metilo, etilo, metoxi, etoxi, acetilo, acetoxi, metilamino, etilamino, dimetilamino, dietilamino, N-metil-N-etilamino, acetilamino, N-metilcarbamoilo, N,N-dimetilcarbamoilo, N,N-dietilcarbamoilo, N-metil-N-etilcarbamoilo, metiltio, etiltio, metilsufinilo, etilsulfinilo, mesilo, etilsulfonilo, metoxicarbonilo, etoxicarbonilo, N-metilsulfamoilo, N-etilsulfamoilo, N,N-dimetilsulfamoilo, N,N-dietilsulfamoilo o N-metil-N-etilsulfamoilo; y G, Q, T y Z se seleccionan independientemente entre C1-4alquilo, C1-4alcanoilo, C1-4alquilsulfonilo, C1-4alcoxicarbonilo, carbamoilo, N-(C1-4alquil)carbamoilo, N,N-(C1-4alquil)carbamoilo, bencilo, benciloxicarbonilo, benzoilo, y fenilsulfonilo donde G, Q y T pueden ser independientemente opcionalmente sustituido en un carbono por uno o más X; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo. También se describen procesos para su elaboracion y su uso como medicamentos para producir un efecto de inhibicion del ciclo celular (anti-proliferacion celular) en un animal de sangre caliente, por ejemplo el ser humano.
ARP010103279A 2000-07-11 2001-07-11 Derivado de pirimidina, composicion farmaceutica que lo comprende, su uso en la fabricacion de un medicamento y proceso de preparacion AR031251A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0016877.3A GB0016877D0 (en) 2000-07-11 2000-07-11 Chemical compounds

Publications (1)

Publication Number Publication Date
AR031251A1 true AR031251A1 (es) 2003-09-17

Family

ID=9895337

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010103279A AR031251A1 (es) 2000-07-11 2001-07-11 Derivado de pirimidina, composicion farmaceutica que lo comprende, su uso en la fabricacion de un medicamento y proceso de preparacion

Country Status (33)

Country Link
US (1) US6908920B2 (es)
EP (1) EP1303496B9 (es)
JP (1) JP2004502763A (es)
KR (1) KR100783447B1 (es)
CN (1) CN1196685C (es)
AR (1) AR031251A1 (es)
AT (1) ATE372988T1 (es)
AU (2) AU2001269317B2 (es)
BG (1) BG107451A (es)
BR (1) BR0112420A (es)
CA (1) CA2415486C (es)
CY (1) CY1107807T1 (es)
CZ (1) CZ200376A3 (es)
DE (1) DE60130463T2 (es)
DK (1) DK1303496T3 (es)
EE (1) EE200300020A (es)
ES (1) ES2292599T3 (es)
GB (1) GB0016877D0 (es)
HK (1) HK1054940A1 (es)
HU (1) HUP0301722A3 (es)
IL (2) IL153754A0 (es)
IS (1) IS2521B (es)
MX (1) MXPA03000254A (es)
NO (1) NO325280B1 (es)
NZ (1) NZ523357A (es)
PL (1) PL360385A1 (es)
PT (1) PT1303496E (es)
RU (1) RU2299201C2 (es)
SK (1) SK282003A3 (es)
TW (1) TWI221470B (es)
UA (1) UA75084C2 (es)
WO (1) WO2002004429A1 (es)
ZA (1) ZA200300079B (es)

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