AR038922A1 - 2-heteroaril-pirimidinas inhibidoras de cdk, su preparacion y su uso como medicamentos - Google Patents

2-heteroaril-pirimidinas inhibidoras de cdk, su preparacion y su uso como medicamentos

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Publication number
AR038922A1
AR038922A1 ARP030100819A ARP030100819A AR038922A1 AR 038922 A1 AR038922 A1 AR 038922A1 AR P030100819 A ARP030100819 A AR P030100819A AR P030100819 A ARP030100819 A AR P030100819A AR 038922 A1 AR038922 A1 AR 038922A1
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Argentina
Prior art keywords
alkyl
alkoxy
optionally
hydroxy
halogen
Prior art date
Application number
ARP030100819A
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English (en)
Inventor
Ulrich Luecking
Martin Krueger
Rolf Jautelat
Olaf Prien
Gerd Siemeister
Alexander Ernst
Original Assignee
Schering Ag
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 DE2002112100 external-priority patent/DE10212100A1/de
Priority claimed from DE10255984A external-priority patent/DE10255984A1/de
Application filed by Schering Ag filed Critical Schering Ag
Publication of AR038922A1 publication Critical patent/AR038922A1/es

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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • 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
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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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
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  • Psychiatry (AREA)
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  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Inhibidores de las quinasas dependientes de las ciclinas, su preparación y su uso como medicamento para el tratamiento de diversas enfermedades. Reivindicación 1: Compuestos de la fórmula general (1), donde: Q es un resto de fórmula (2) ó (3); D, E, G, L, M y T son cada uno, independientemente entre sí, carbono, oxígeno, nitrógeno o azufre, donde al menos debe estar contenido en el anillo un heteroátomo; R1 es hidrógeno, halógeno, alquilo C1-6, alquinilo C1-6, nitro, ciano, heteroarilo o el grupo -COR5, -OCF3, -S-CF3 o -SO2CF3; R2 es hidrógeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, heteroarilo o cicloalquilo C3-7 o alquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, heteroarilo o cicloalquilo C3-7, opcionalmente mono polisustituido, igual o diferente, por hidroxi, halógeno, alcoxi C1-6, alquiltio C1-6, amino, ciano, alquilo C1-6, alquenilo C2-6, alcoxi(C1-6)-alquilo(C1-6), alcoxi(C1-6)- alcoxi(C1-6)-alquilo(C1-6), cicloalquilo C3-7, -NHalquilo C1-6, -NHcicloalquilo C3-7, -N(alquilo C1-6)2, -SO(alquilo C1-6), -SO2(alquilo C1-6), alcanoilo C1-6, -CONR3R4, -COR5, alquil(C1-6)OAc, fenilo o por el grupo -R6, el anillo del cicloalquilo C3-7 puede estar opcionalmente interrumpido por uno o varios átomos de nitrógeno, oxígeno y/o azufre y/o puede estar interrumpido en el anillo por uno o varios grupos =C=O y/u opcionalmente pueden estar contenidos en el anillo uno o varios enlaces dobles posibles, y el fenilo, arilo o cicloalquilo C3-7 en sí puede estar opcionalmente mono o polisustituido, igual o diferente, por halógeno, hidroxi, alquilo C1-6, alcoxi C1-6, o por el grupo -CF3 u -OCF3, X es halógeno, oxígeno, azufre o el grupo -NH- o -N(alquilo C1-3)-o X y R2 forman juntos un anillo de cicloalquilo C3-10, que opcionalmente puede contener uno o varios heteroátomos y que opcionalmente puede estar mono o polisustituido por hidroxi, alquilo C1-6, hidroxi-alquilo(C1-6) o halógeno; A y B son cada uno, independientemente entre sí, hidrógeno, hidroxi, halógeno o el grupo -SR7, -S(O)R7, -SO2R7, -NHSO2R7, -CH(OH)R7,-CR7(OH)-R7, alquil(C1-6)P(O)OR3OR4 o -COR7; o Ay B forman juntos un anillo cicloalquilo C3-7 que pueden estar opcionalmente interrumpido por uno o varios átomos de nitrógeno, oxígeno y/o azufre y/o puede estar interrumpido en el anillo por uno o varios grupos =C=O, y/u opcionalmente puede estar contenidos en el anillo uno o varios enlaces dobles posibles y el anillo cicloalquilo C3-7 puede estar opcionalmente mono o polisustituido, igual o diferente, por hidroxi, halógeno, alcoxi C1-6, alquiltio C1-6, amino, ciano, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-7, alcoxi(C1-6)alquilo(C1-6), -NHalquilo C1-6, -N(alquilo C1-6)2, -SO(alquilo C1-6), -SO2(alquilo C1-6), alcanoilo C1-6, -CONR3R4, -COR5, alquil(C1-6)OAc, fenilo, o por el grupo R6, donde el fenilo a su vez puede estar opcionalmente mono o polisustituido, igual o diferente, por halógeno, hidroxi, alquilo C1-6, alcoxi C1-6, o por el grupo -CF3 u -OCF3; R3 y R4 son cada uno, independientemente entre sí, hidrógeno, hidroxi, alcoxi C1-6 o alquilo C1-6 opcionalmente mono o polisustituido, igual o diferente, por hidroxi, alcoxi C1-6, alquiltio C1-6, -N(alquilo C1-6)2, el grupo R6 o -N(alquilo C1-6)R6, R3 y R4 forman juntos un anillo cicloalquilo C3-7 que opcionalmente puede estar interrumpido por uno o varios átomos de nitrógeno, oxígeno y/o azufre y/o puede estar interrumpido en el anillo por uno o varios grupos =C=O, y/u opcionalmente pueden estar contenidos opcionalmente en el anillo uno o varios enlaces dobles posibles; R5 es hidroxi, benzoxi, alquilo C1-6, alquiltio C1-6, o alcoxi C1-6; R6 es un benciltio, feniloxi o anillo cicloalquilo C3-7 opcionalmente mono o polisustituido, igual o diferente, por halógeno, hidroxi, alquilo C1-6, alcoxi(C1-6) o -SO2NR3R4, donde el anillo cicloalquilo C3-7 tiene el significado indicado en R2; R7 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, bencilo, cicloalquilo C3-7, donde el anillo cicloalquilo C3-7 tiene el significado indicado en R2, o el grupo -NR3R4, o alquilo C1-10, alquenilo C2-10, alquinilo C2-10 o cicloalquilo C3-7, opcionalmente mono o polisustituido, igual o diferente, por hidroxi, alcoxi C1-6, halógeno, fenilo, -NR3R4 o fenilo que, a su vez, puede estar opcionalmente mono o polisustituido, igual o diferente, por halógeno, hidroxi, alquilo C1-6, alcoxi C1-6, halo-alquilo C1-6, halo-alcoxi C1-6, o fenilo que, a su vez, puede estar opcionalmente mono o polisustituido, igual o diferente, por halógeno, hidroxi, alquilo C1-6 o alcoxi C1-6, halo-alquilo C1-6, halo-alcoxi C1-6; y n es 0 ó 1, en caso de que n = 0, entonces X es halógeno, así como los isómeros, diastereómeros, enantiómeros y sales de los mismos.
ARP030100819A 2002-03-11 2003-03-11 2-heteroaril-pirimidinas inhibidoras de cdk, su preparacion y su uso como medicamentos AR038922A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2002112100 DE10212100A1 (de) 2002-03-11 2002-03-11 CDK inhibitorische 2-Heteroaryl-Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
DE10255984A DE10255984A1 (de) 2002-11-26 2002-11-26 CDK inhibitorische 2-Heteroaryl-Pyrimidine, deren Herstellung und Verwendung als Arnzeimittel

Publications (1)

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AR038922A1 true AR038922A1 (es) 2005-02-02

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EP (1) EP1483260A1 (es)
JP (1) JP2005526765A (es)
AR (1) AR038922A1 (es)
AU (1) AU2003212282A1 (es)
PE (1) PE20040156A1 (es)
TW (1) TW200406406A (es)
UY (1) UY27714A1 (es)
WO (1) WO2003076437A1 (es)

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