AR046996A1 - Derivados de amino-pirimidinas - Google Patents

Derivados de amino-pirimidinas

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Publication number
AR046996A1
AR046996A1 ARP040104907A ARP040104907A AR046996A1 AR 046996 A1 AR046996 A1 AR 046996A1 AR P040104907 A ARP040104907 A AR P040104907A AR P040104907 A ARP040104907 A AR P040104907A AR 046996 A1 AR046996 A1 AR 046996A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
amino
saturated
groups
Prior art date
Application number
ARP040104907A
Other languages
English (en)
Inventor
Clifford Jones
Richard Luke
William Mccoull
Original Assignee
Astrazeneca Ab
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
Priority claimed from GB0330001A external-priority patent/GB0330001D0/en
Priority claimed from GB0416850A external-priority patent/GB0416850D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR046996A1 publication Critical patent/AR046996A1/es

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    • 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • 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
    • C07D403/12—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
    • 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
    • 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
    • C07D413/02—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composiciones farmacéuticas de dichos compuestos, el uso de dichos compuestos como médicamente y en la produccion de un efecto anti-angiogénico. Procesos para la preparacion de dichos compuestos. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1), donde: R1 y R2 se seleccionan independientemente entre hidrogeno, (C1-6) alquilsulfonilo, fenil(CH2)u- donde u es 0, 1, 2, 3, 4, 5 o 6, (C1-6) alcanoilo, (C1-6) alquilo, (C1-6) alcoxicarbonilo, (C3-6)cicloalquil(CH2)x- en donde x es 0, 1, 2, 3, 4, 5 o 6, o un anillo heteroarilo de 5 o 6 miembros, o R1 y R2 junto con el átomo de nitrogeno al cual se encuentran unidos representan un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado que contiene opcionalmente otro heteroátomo seleccionado entre N o O; donde los grupos (C1-6) alquilo, (C1-6) alcanoilo y (C3-6) cicloalquilo se sustituyen opcionalmente con uno o más grupos seleccionados independientemente entre fluoro, hidroxi, (C1-6) alquilo, (C1-6) alcoxi, (C1-6)alcoxi(C1-6)alcoxi, (C1-6)alcoxi(C1-6)alcoxi(C1-6)alcoxi, amino, mono(C1-6)alquilamino, di-[(C1-6)alquil]amino, carbamoilo, mono(C1-6)alquilcarbamoilo, di-[(C1-6)alquil]carbamoilo o -N(Rd)C(O)(C1-6)alquilo en donde Rd es hidrogeno o (C1-6) alquilo, o un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado, o un anillo heteroarilo de 5 o 6 miembros, donde los grupos (C1-6) alcoxi, (C1-6)alcoxi(C1-6)alcoxi y (C1-6)alcoxi(C1-6)alcoxi(C1-6)alcoxi y los grupos (C1-6) alquilo de los grupos mono(C1-6)alquilamino, di-[(C1-6)alquil]amino, mono(C1-6)alquilcarbamoilo, di-[(C1-6)alquil]carbamoilo y/o N(Rd)C(O)(C1-6)alquilo se sustituyen opcionalmente con uno o más grupos hidroxi; donde el fenilo se sustituye opcionalmente con uno o más grupos seleccionados independientemente entre halo, (C1-6) alquilo, (C1-6) alcoxi, amino, mono(C1-6)alquilamino o di-[(C1-6)alquil]amino, donde los grupos (C1-6) alquilo y (C1-6) alcoxi se sustituyen opcionalmente con uno o más grupos seleccionados independientemente entre hidroxi, amino, mono(C1-6)alquilamino o di-[(C1-6)alquil]amino; y donde cualquier anillo heterocíclico y heteroarilo en R1 y/o R2 se sustituye opcionalmente independientemente con uno o más de los siguientes: (C1-4) alquilo, (C1-4) alcoxi, (C1-4)alcoxi(C1-4)alquilo, hidroxi, amino, mono(C1-6)alquilamino o di-[(C1-6)alquil]amino, o un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado, o -C(O)(CH2)z y donde z es 0, 1, 2 o 3 e Y se selecciona entre hidrogeno, hidroxi, (C1-4) alcoxi, amino, mono(C1-6)alquilamino, di-[(C1-6)alquil]amino o un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado; y con la condicion de que cuando R1 y/o R2 es un grupo (C1)alcanoilo, luego el (C1)alcanoilo no se sustituye con fluoro o hidroxi; R3 se selecciona entre hidrogeno, (C1-6) alquilo o (C1-6) alcoxi, donde los grupos alquilo y alcoxi se sustituyen opcionalmente con uno o más grupos seleccionados entre: fluoro, hidroxi, (C1-6) alquilo, (C1-6) alcoxi, carbamoilo, mono(C1-6)alquilcarbamoilo o di-[(C1-6)alquil]carbamoilo, amino, mono(C1-6)alquilamino o di(C1-6)alquilamino, un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado o un anillo heteroarilo de 5 o 6 miembros donde dichos anillo heterocíclicos y heteroarilo se sustituyen opcionalmente independientemente con uno o más de los siguientes: (C1-4) alquilo, (C1-4)alcoxi, hidroxi, amino, mono(C1- 6)alquilamino o di-(C1-6)alquilamino o un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado; o R3 representa un grupo NR1R2 como se define precedentemente; R4 se selecciona entre hidrogeno, (C1-6) alquilo o (C1-6) alcoxi; A representa un grupo arilo o un anillo heteroarilo de 5 o 6 miembros seleccionado entre furilo, pirrolilo, tienilo, oxazolilo, isoxazolilo, imidazolilo, pirazolilo, tiazolilo, isotiozolilo, oxadiazolilo, tiadiazolilo, triazolilo, tetrazolilo, piridilo, piridazinilo, pirimidinilo, pirazinilo o 1,3,5-triazonilo; R5 se selecciona entre ciclopropilo, ciano, halo, (C1-6) alcoxi o (C1-6) alquilo, donde los grupos (C1-6) alquilo y (C1-6) alcoxi se sustituyen opcionalmente con ciano o con uno o más fluoro; n es 0, 1, 2 o 3; L se encuentra unido meta o para en el anillo A respecto del punto de union del grupo etinilo y representa -C(RaRb)C(O)N(R9)-, N(R8)C(O)C(RaRb)-, -N(R8)C(O)N(R9)-, N(R8)C(O)O-, o OC(O)N(R9)-, donde R8 y R9 representan independientemente hidrogeno o (C1-6) alquilo y donde Ra y Rb representan independientemente hidrogeno o (C1-6) alquilo o Ra y Rb junto con el átomo de carbono al cual se encuentran unidos representan (C3-6) cicloalquilo; B representa un anillo (C3- 7) cicloalquilo, un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado, un grupo arilo, un anillo heteroarilo de 5 o 6 miembros seleccionado entre furilo, pirrolilo, tienilo, oxazolilo, isoxazolilo, imidazolilo, pirazolilo, tiazolilo, isotiazolilo, oxadiazolilo, tiadiazolilo, triazolilo, tetrazolilo, piridilo, piridazinilo, pirimidinilo, pirazinilo o 1,3,5-triazonilo, o un grupo bicíclico de 8, 9 o 10 miembros el cual contiene opcionalmente 1, 2, 3 o 4 heteroátomos seleccionados independientemente entre N, O y S y el cual es saturado, parcialmente saturados o aromático; R6 se selecciona entre halo, ciano, oxo, un anillo (C3-7) cicloalquilo, un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado -S(O)p-(C1-6)alquilo donde p es 0, 1 o 2, -N(Ra)C(O)(C1-6)alquilo en donde Ra es hidrogeno o (C1-6) alquilo; o R6 se selecciona entre (C1-6) alquilo o (C1-6) alcoxi, donde los grupos (C1-6) alquilo, -S(O)p-(C1-6)alquilo y (C1-6) alcoxi se sustituyen opcionalmente con uno o más grupos seleccionados independientemente entre ciano, fluoro, hidroxi, (C1-6) alcoxi, amino, mono(C1-6)alquilamino, di-[(C1-6)alquil]amino, un anillo(C3-7) cicloalquilo o un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado; donde el anillo (C3-7) cicloalquilo y anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado se sustituyen opcionalmente independientemente con uno o más grupos seleccionados entre (C1-6) alquilo; y m es 0, 1, 2 o 3; y cuando B es un anillo (C3-7) cicloalquilo o un anillo heterocíclico de 3 a 7 miembros saturado o parcialmente saturado o un grupo bicíclico de 8, 9 o 10 miembros saturado o parcialmente saturado, los anillo y el grupo bicíclico llevan opcionalmente 1 o 2 sustituyentes oxo o tioxo; y sales, prodrogas o solvatos del mismo.
ARP040104907A 2003-12-24 2004-12-27 Derivados de amino-pirimidinas AR046996A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0330001A GB0330001D0 (en) 2003-12-24 2003-12-24 Compounds
GB0416850A GB0416850D0 (en) 2004-07-29 2004-07-29 Compounds

Publications (1)

Publication Number Publication Date
AR046996A1 true AR046996A1 (es) 2006-01-04

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Country Status (11)

Country Link
US (1) US20080027076A1 (es)
EP (1) EP1737462B1 (es)
JP (1) JP2007517006A (es)
AR (1) AR046996A1 (es)
AT (1) ATE402705T1 (es)
DE (1) DE602004015509D1 (es)
ES (1) ES2309591T3 (es)
HK (1) HK1102045A1 (es)
TW (1) TW200524607A (es)
UY (1) UY28700A1 (es)
WO (1) WO2005060969A1 (es)

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ATE402705T1 (de) 2008-08-15
DE602004015509D1 (de) 2008-09-11
UY28700A1 (es) 2005-07-29
EP1737462A1 (en) 2007-01-03
ES2309591T3 (es) 2008-12-16
EP1737462B1 (en) 2008-07-30
US20080027076A1 (en) 2008-01-31

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