AR040286A1 - Proceso para la preparacion de pirimidinas sustituidas - Google Patents

Proceso para la preparacion de pirimidinas sustituidas

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Publication number
AR040286A1
AR040286A1 ARP030102187A ARP030102187A AR040286A1 AR 040286 A1 AR040286 A1 AR 040286A1 AR P030102187 A ARP030102187 A AR P030102187A AR P030102187 A ARP030102187 A AR P030102187A AR 040286 A1 AR040286 A1 AR 040286A1
Authority
AR
Argentina
Prior art keywords
independently selected
monocyclic
saturated
substituted
optionally
Prior art date
Application number
ARP030102187A
Other languages
English (en)
Inventor
Jean-Damien Charrier
Francesca Mazzei
David Kay
William Miller
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of AR040286A1 publication Critical patent/AR040286A1/es

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    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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
    • 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
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • 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
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un proceso sencillo para la preparación de pirimidinas tri y tetra-sustituidas. El proceso es útil para preparar inhibidores de cinasas de proteínas, especialmente, cinasa Aurora. Estos inhibidores son de utilidad para el tratamiento o disminución de la gravedad de condiciones o enfermedades reguladas por Aurora. Compuestos seleccionados a partir de los que poseen la fórmula (1), composición farmacéutica que contiene dichos compuestos y un método de inhibición de Aurora-1. Reivindicación 1: Un método de preparación de un compuesto de fórmula (1) en donde: Q y T son, cada uno en forma independiente, seleccionados entre O, S, o N (R); cada R se selecciona en forma independiente entre H o un grupo alifático C1-6 opcionalmente sustituido, en donde; dos R ligados al mismo átomo de N en forma opcional se toman junto con el N para formar un anillo opcionalmente sustituido, de 3 a 7 miembros, monocíclico, o de 8 a 10 miembros bicíclico, saturado, parcialmente insaturado o completamente insaturado, que tiene 0-3 heteroátomos, además del N ligado al mismo, seleccionados de manera independiente entre N, O, o S; Rx es U-R5; R5 se selecciona entre halógeno, NO2, CN, R, o Ar; cada U se selecciona de manera independiente entre un enlace de valencia o una cadena alquilideno C1-4, en donde; hasta dos unidades metileno de U son en forma opcional e independiente reemplazados con -O-, -S-, -SO-, -SO2-, -N(R)SO2-, -SO2N(R)-, -N(R)-, -C(O)-, -CO2-, -N(R)C(O)-, -N(R)C(O)O-, -N(R)CON(R)-, -N(R)SO2N(R)-, -N(R)N(R)-, -C(O)N(R)-, -OC(O)N(R)-, C(R)=NN(R)-, o -C(R)=N-O-; cada Ar se selecciona en forma independiente entre un anillo opcionalmente sustituido seleccionado entre un anillo de 3 a 7 miembros monocíclico, o uno de 8 a 10 miembros bicíclico, saturado, parcialmente insaturado, o completamente insaturado, que tiene 0 a 4 heteroátomos seleccionados en forma independiente entre N, O, o S; Ry es -N(R1)2, -OR1, o -SR1; cada R1 se selecciona de manera independiente entre R o un anillo 3 a 8 miembros monocíclico, uno de 8 a 10 miembros bicíclico, o uno de 10 a 12 miembros tricíclico, saturado, parcialmente insaturado, o completamente insaturado, que tiene 0 a 4 heteroátomos seleccionados en forma independiente entre N, O ó S; y en donde: cada R1 está opcional o independientemente sustituido con hasta 4 sustituyentes que se seleccionan en forma independiente entre R2; cada R2 se selecciona en forma independiente entre -R3, -OR3, -SR3, -CN, -NO2, oxo, halógeno, -N(R3)2, -C(O)R3, -OC(O)R3, -CO2R3, -SO2R3, -SO2N(R3)2, -N(R3)SO2R3, -C(O)NR(R3), -C(O)N(R3)2, -OC(O)NR(R3), -OC(O)N(R3)2, -NR3C(O)R3, -NR3C(O)N(R3)2, o -NR3CO2(R3); cada R3 se selecciona de manera independiente entre R o Ar; Rz1 se selecciona entre un grupo alifático C1-6, o un anillo 3 a 8 miembros monocíclico, uno de 8 a 10 miembros bicíclico, o uno de 10 a 12 miembros tricíclico, saturado, parcialmente insaturado, o completamente insaturado, que tiene 0 a 4 heteroátomos seleccionados en forma independiente entre N, O ó S; en donde; Rz1 está sustituido con 0 a 4 grupos R2 seleccionados en forma independiente; Rz2 es un grupo alifático C1-6, o un anillo 3 a 8 miembros monocíclico, o uno de 8 a 10 miembros bicíclico, saturado, parcialmente insaturado, o completamente insaturado, que tiene 0 a 4 heteroátomos seleccionados en forma independiente entre N, O ó S; en donde; Rz2 está sustituido con 0 a 4 sustituyentes seleccionados en forma independiente entre oxo o U-R5; dicho proceso comprende la etapa de combinar un compuesto de fórmula (2) y un compuesto de fórmula Ry-H en un medio adecuado; en donde dicho medio adecuado comprende; i) un solvente apropiado y ii) en forma opcional, una base apropiada; y L3 es un grupo de salida adecuado.
ARP030102187A 2002-06-20 2003-06-19 Proceso para la preparacion de pirimidinas sustituidas AR040286A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39065802P 2002-06-20 2002-06-20
US41160902P 2002-09-18 2002-09-18

Publications (1)

Publication Number Publication Date
AR040286A1 true AR040286A1 (es) 2005-03-23

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ID=30003168

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030102187A AR040286A1 (es) 2002-06-20 2003-06-19 Proceso para la preparacion de pirimidinas sustituidas

Country Status (27)

Country Link
US (4) US20040049032A1 (es)
EP (4) EP1746093B1 (es)
JP (5) JP4237701B2 (es)
KR (2) KR101141959B1 (es)
CN (1) CN100484934C (es)
AR (1) AR040286A1 (es)
AT (2) ATE498621T1 (es)
AU (1) AU2003245568B2 (es)
BR (1) BR0312443A (es)
CA (1) CA2489824C (es)
CO (1) CO5680433A2 (es)
DE (1) DE60336092D1 (es)
EA (2) EA015990B1 (es)
EC (1) ECSP055561A (es)
ES (1) ES2386781T3 (es)
HK (3) HK1077057A1 (es)
HR (1) HRP20050064A2 (es)
IL (1) IL165849A0 (es)
IS (2) IS7606A (es)
MX (1) MXPA05000068A (es)
MY (1) MY141867A (es)
NO (2) NO331925B1 (es)
NZ (4) NZ562953A (es)
PL (1) PL374953A1 (es)
SG (1) SG170614A1 (es)
TW (2) TWI354554B (es)
WO (1) WO2004000833A1 (es)

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