AR059308A1 - Compuestos inhibidores de enzimas activadoras e1, composiciones farmaceuticas que los contienen y usos en trastornos proliferativos celulares, que incluyen canceres y trastornos inflamatorios. - Google Patents

Compuestos inhibidores de enzimas activadoras e1, composiciones farmaceuticas que los contienen y usos en trastornos proliferativos celulares, que incluyen canceres y trastornos inflamatorios.

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AR059308A1
AR059308A1 ARP070100458A ARP070100458A AR059308A1 AR 059308 A1 AR059308 A1 AR 059308A1 AR P070100458 A ARP070100458 A AR P070100458A AR P070100458 A ARP070100458 A AR P070100458A AR 059308 A1 AR059308 A1 AR 059308A1
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Argentina
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aliphatic
optionally substituted
fluorine
independently
hydrogen
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ARP070100458A
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Millennium Pharm Inc
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Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of AR059308A1 publication Critical patent/AR059308A1/es

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
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    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
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    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/14—Pyrrolo-pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
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    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/173—Purine radicals with 2-deoxyribosyl as the saccharide radical

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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Biochemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Biotechnology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Epoxy Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1): o una de sus sales farmacéuticamente aceptables, caracterizado porque: configuraciones estereoquímicas representadas en las posiciones con asterisco indican una estereoquímica relativa; Anillo A está seleccionado del grupo que consiste en: formulas (A-1) a (A-7), en donde un átomo de nitrogeno anular en el Anillo A opcionalmente está oxidado; X es -C(R11)2, -N(R12)- u -O-;Y es -O-, -S- o -C(Rm)(Rn)-; Ra está seleccionado del grupo que consiste en hidrogeno, fluor, -CN, -N3, -OR5, - N(R4)2, -NR4CO2R6, -NR4C(O)R5, -C(O)N(R4)2, -C(O)R5, -OC(O)N(R4)2, - OC(O)R5, -OCO2R6 o un alifático C1-4 o fluoroalifático C1-4 opcionalmente sustituidos con uno o dos sustituyentes seleccionados, de modo independiente, del grupo que consiste en -OR5x, -N(R4x)(R4y), -CO2R5x o -C(O)N(R4x)(R4y); o Ra y Rb forman juntos =O; o Ra y Rc forman juntos un enlace; Rb está seleccionado del grupo que consiste en hidrogeno, fluor, alifático C1-4 y fluoroalifático C1-4; o Rb y Ra forman juntos =O; o Rb, tomado junto con Rd y los átomos de carbono intervinientes, forma un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4; o Rb, tomado junto con Ra y los átomos de carbono intervinientes, forma un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4, Rc está seleccionado del grupo que consiste en hidrogeno, fluor, -CN, -N3, -OR5, - N(R4)2, -NR4CO2R6, -NR4C(O)R5, -C(O)N(R4)2, -C(O)R5, -OC(O)N(R4)2, - OC(O)R5, -OCO2R6 o un alifático C1-4 o fluoroalifático C1-4 opcionalmente sustituidos con uno o dos sustituyentes seleccionados, de modo independiente, del grupo que consiste en -OR5x, -N(R4x)(R4y), -CO2R5x o -C(O)N(R4x)(R4y); o Ra y Rc forman juntos un enlace; o Rc y Rd forman juntos =O; Rd está seleccionado del grupo que consiste en hidrogeno, fluor, alifático C1-4 y fluoroalifático C1-4; o Rd y Rc forman juntos =O; o Rd, tomado junto con Rb y los átomos de carbono intervinientes, forma un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4, o Rd, tomado junto con Re' y los átomos de carbono intervinientes, forma un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4, Re es hidrogeno o alifático C1-4; o Re, tomado junto con un Rf y los átomos de carbono intervinientes, forma un anillo espirocíclico de 3 a 6 miembros, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4, o Re, tomado junto con Rm y los átomos de carbono intervinientes, forma un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4; o Re, tomado junto con Rb y los átomos de carbono intervinientes, forma un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4; Re' es hidrogeno o alifático C1-4; o Re', tomado junto con Rm y los átomos de carbono intervinientes, forma un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4; o Re', tomado junto con Rd y los átomos de carbono intervinientes, forma un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4; cada Rf es, de modo independiente, hidrogeno, fluor, alifático C1-4 o fluoroalifático C1-4, con la condicion de que, si X es - O- o -NH-, Rf no sea fluor; o dos Rf tomados juntos forman =O; o dos Rf, tomados junto con el átomo de carbono al que están unidos, forman un anillo carbocíclico de 3 a 6 miembros; o un Rf, tomado junto con Re y los átomos de carbono intervinientes, forma un anillo espirocíclico de 3 a 6 miembros, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4 o un Rf, tomado junto con un Rf1 adyacente y los átomos de carbono intervinientes, forma un anillo ciclopropilo, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4 o un Rf y un Rf1 forman juntos un enlace doble; cada Rf1 es, de modo independiente, hidrogeno o fluor; o un Rf1, tomado junto con un Rf adyacente y los átomos de carbono intervinientes forma un anillo ciclopropilo, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4, o un Rf1 y un Rf forman juntos un enlace doble; Rf2 es hidrogeno, alifático C1-4 o fluoroalifático C1-4; Rg es hidrogeno, halo, -NO2, -CN, -C(R5)=C(R5)2, -C:::C-R5, -OR5, -SR6, -S(O)R6, - SO2R6, -SO2N(R4)2, -N(R4)2, - NR4C(O)R5, -NR4C(O)N(R4)2, -N(R4)C(=NR4)-N(R4)2, -N(R4)C(=NR4)-R6, -NR4CO2R6, -N(R4)SO2R6, -N(R4)SO2N(R4)2, -O-C(O)R 5, -OCO2R6, -OC(O)N(R4)2, -C(O)R5, -CO2R5, -C(O)N(R4)2, -C(O)N(R4)-OR5, -C(O)N(R4)C(=NR4)-N(R4)2, -N(R4)C(=NR4)-N(R4)-C(O)R5, - C(=NR4)-N(R4)2, -C(=NR4)-OR5, -N(R4)-N(R4)2, -N(R4)-OR5, -C(=NR4)-N(R4)-OR5, -C(R6)=N-OR5 o un alifático opcionalmente sustituido, arilo, heteroarilo o heterociclilo; cada Rh es, de modo independiente, hidrogeno, halo, -CN-, -OR5, -N(R4)2, -SR6 o un grupo alifático C1-4 opcionalmente sustituido; Rj es hidrogeno, -OR5, -SR6, -N(R4)2 o un alifático opcionalmente sustituido, arilo o grupo heteroarilo; Rk es hidrogeno, halo, -OR5, -SR6, -N(R4)2 o un grupo alifático C1-4 opcionalmente sustituido; Rm es hidrogeno, fluor, -N(R4)2 o un grupo alifático C1-4 opcionalmente sustituido; o Rm y Rn forman juntos =O o =C(R5)2 o Rm' y Re, tomados junto con los átomos de carbono intervinientes, forman un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4, Rm y Re', tomados junto con los átomos de carbono intervinientes, forman un anillo ciclopropano fusionado, que está opcionalmente sustituido con uno o dos sustituyentes seleccionados, de modo independiente, de fluor o alifático C1-4, Rn es hidrogeno, fluor o un grupo alifático C1-4 opcionalmente sustituido; o Rm y R forman juntos =O o =C(R5)2; cada R4 es, de modo independiente, hidrogeno o un alifático opcionalmente sustituido, arilo, heteroarilo o grupo heterociclilo; o dos R4 en el mismo átomo de nitrogeno, tomados junto con el átomo de nitrogeno, forman un anillo heterociclilo de 4 a 8 miembros opcionalmente sustituido que tiene, además del átomo de nitrogeno, 0-2 heteroátomos del anillo seleccionados, de modo independiente, de N, O y S; R4x es hidrogeno, alquilo C1-4, fluoroalquilo C1-4 o ar C6-10-alquilo C1-4, cuya porcion arilo puede estar opcionalmente sustituida; R4yes hidrogeno, alquilo C1-4, fluoroalquilo C1-4, ar C6-10-alquilo C1-4, cuya porcion arilo puede estar opcionalmente sustituida o un anillo arilo, heteroarilo o heterociclilo de 5 o 6 miembros opcionalmente sustituido; o R4x y R4y, tomados junto con el átomo de nitrogeno al que están unidos, forman un anillo heterociclilo de 4 a 8 miembros opcionalmente sustituido que tiene, además del átomo de nitrogeno, 0-2 heteroátomos del anillo seleccionados, de modo independiente, de N, O y S; y cada R5 es, de modo independiente, hidrogeno o un alifático opcionalmente sustituido, arilo, heteroarilo o grupo heterociclilo; cada R5x es, de modo independiente, hidrogeno, alquilo C1-4, fluoroalquilo C1-4 o un arilo C6-10 o ar C6-10-alquilo C1-4 opcionalmente sustituido; cada R6 es, de modo independiente, un alifático, arilo o grupo heteroarilo opcionalmente sustituido; y m 0, 1, 2 o 3, con la condicion de que Y sea -C(Rm)(R)- cuando mes 0.
ARP070100458A 2006-02-02 2007-02-02 Compuestos inhibidores de enzimas activadoras e1, composiciones farmaceuticas que los contienen y usos en trastornos proliferativos celulares, que incluyen canceres y trastornos inflamatorios. AR059308A1 (es)

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US (6) US8207177B2 (es)
EP (2) EP2402334B1 (es)
JP (6) JP5231251B2 (es)
KR (2) KR101450535B1 (es)
CN (4) CN103288835A (es)
AR (1) AR059308A1 (es)
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DK (1) DK1989206T3 (es)
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GT200500281A (es) * 2004-10-22 2006-04-24 Novartis Ag Compuestos organicos.
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