AR061847A1 - Derivados de pirimidina 2- amino -5- sustituida. como inhibidores de quinasas. composiciones farmaceuticas. - Google Patents

Derivados de pirimidina 2- amino -5- sustituida. como inhibidores de quinasas. composiciones farmaceuticas.

Info

Publication number
AR061847A1
AR061847A1 ARP070103039A ARP070103039A AR061847A1 AR 061847 A1 AR061847 A1 AR 061847A1 AR P070103039 A ARP070103039 A AR P070103039A AR P070103039 A ARP070103039 A AR P070103039A AR 061847 A1 AR061847 A1 AR 061847A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
optionally substituted
heteroaryl
nra
Prior art date
Application number
ARP070103039A
Other languages
English (en)
Inventor
Colleen Gritzen
Richard M Soll
Glenn Noronha
Ved P Pathak
Jianguo Cao
Joel Renick
Binqi Zeng
Pherson Andrew Mc
Original Assignee
Targe Gen Inc
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 Targe Gen Inc filed Critical Targe Gen Inc
Publication of AR061847A1 publication Critical patent/AR061847A1/es

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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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D413/02—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

Landscapes

  • 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)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Composiciones farmacéuticas que los comprenden y uso como inhibidores de quinasas. Reivindicacion 1: Un compuesto caracterizado porque responde a la estructura en donde: G1 se selecciona entre un grupo que consiste de un enlace, H, un arilo opcionalmente sustituido, o un heteroarilo opcionalmente sustituido; L1 se selecciona entre el grupo que consiste de O, SO, SO2, SO2-alquilo, SO2NH, CO, C(O)NH, SO2NH-alquilo, CO-alquilo, C(O)NH-alquilo, OC(O); C(O)O, alquilo opcionalmente sustituido, alquilo ramificado, aminoalquilo, alcoxi, o hidroxialquilo; L2 se selecciona entre el grupo que consiste de H, alquilo opcionalmente sustituido, alquilo ramificado, aminoalquilo, hidroxialquilo, cicloalquilo, o heterociclo; o cuando G1 es heteroarilo o H, L1 o L2 o ambos L y L2 pueden estar ausentes; A1 se selecciona entre un grupo que consiste de un enlace, NRa, C(O), S(O), S(O)2, P(O)2, O, S, y C(Ra)2, en donde si A1 es un enlace, entonces el anillo fenilo está conectado directamente al grupo A2, A2 se selecciona entre un grupo que consiste de NRa, C(O), S(O), S(O)2, P(O)2, O, y S; y la conectividad entre el anillo fenilo, A1, A2 y el anillo pirimidina son químicamente correctos; Ra se selecciona entre un grupo que consiste de H, alquilo inferior, alquilo ramificado, hidroxialquilo, aminoalquilo, tioalquilo, alquilhidroxilo, alquiltiol, y alquilamino; R3 se selecciona en forma independiente en cada caso de un grupo que consiste de hidrogeno, alquilo, alquilo ramificado, alcoxi, halogeno, CF3, ciano, alquilo sustituido, hidroxilo, alquililhidroxilo, tiol, alquiltiol, tioalquilo, amino, y aminoalquilo; n es un entero que tiene un valor entre 0 y 4 inclusive; L3 y L4 son cada uno en forma independiente seleccionados entre un grupo que consiste de NH, NRa, NHCH2, NHCHRa, NHC(Ra)2, N(O), C(O), S(O), S(O)2, OS(O)2, O, CH2, CHRa, (CRa)2, P(O), OP, OP(O), OP(O)2, P(O)NH, P(O)NRa, P(O)2NH, C(O)NH, C(O) NRa, NHC(O), CNRaC(O), NHS(O), NRaS(O), NHS(O)2, NRaS(O)2, NHP(O), y NRaP(O)2; cada uno de s y t es un entero en forma independiente con un valor de 0 o 1, la salvedad de que si s = 0, entonces t = 1, y si t = 0, entonces s = 1: y L5 se selecciona entre un grupo que consiste de alquilo inferior, alquilo ramificado, CF3, cicloalquilo, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, arilo bicíclico, heteroarilo bicíclico, bicíclico donde uno de los anillos es arilo o heteroarilo y el otro anillo es nonarilo, y bicíclico donde ambos anillos son nonarilo; en donde un arilo opcionalmente sustituido o heteroarilo, en forma independiente en cada caso, puede estar sustituido en 1, 2, 3, o 4 carbonos con alquilo, alquilo ramificado, alcoxi, halogeno, CF3, ciano, alquilo sustituido, hidroxilo, tiol, alquiltiol, tioalquilo, amino, y aminoalquilo; y sales aceptables para uso farmacéutico, hidratos, solvatos, prodrogas, estereoisomeros, N-oxidos o sus formas cristalinas.
ARP070103039A 2006-07-07 2007-07-06 Derivados de pirimidina 2- amino -5- sustituida. como inhibidores de quinasas. composiciones farmaceuticas. AR061847A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US81917006P 2006-07-07 2006-07-07
US11/772,572 US8030487B2 (en) 2006-07-07 2007-07-02 2-amino—5-substituted pyrimidine inhibitors

Publications (1)

Publication Number Publication Date
AR061847A1 true AR061847A1 (es) 2008-09-24

Family

ID=38923534

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070103039A AR061847A1 (es) 2006-07-07 2007-07-06 Derivados de pirimidina 2- amino -5- sustituida. como inhibidores de quinasas. composiciones farmaceuticas.

Country Status (4)

Country Link
US (1) US8030487B2 (es)
AR (1) AR061847A1 (es)
TW (1) TW200819439A (es)
WO (1) WO2008008234A1 (es)

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WO2008008234A1 (en) 2008-01-17
US8030487B2 (en) 2011-10-04
US20080027070A1 (en) 2008-01-31
TW200819439A (en) 2008-05-01

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