AR072791A1 - DERIVADOS DE TIAZOLIDIN-2, 4-DIONA, MÉTODOS PARA SU PREPARACIoN, COMPOSICIoN FARMACÉUTICA QUE LOS COMPRENDE Y SU USO EN LA ELABORACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DEL CÁNCER. - Google Patents

DERIVADOS DE TIAZOLIDIN-2, 4-DIONA, MÉTODOS PARA SU PREPARACIoN, COMPOSICIoN FARMACÉUTICA QUE LOS COMPRENDE Y SU USO EN LA ELABORACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DEL CÁNCER.

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Publication number
AR072791A1
AR072791A1 ARP090102486A ARP090102486A AR072791A1 AR 072791 A1 AR072791 A1 AR 072791A1 AR P090102486 A ARP090102486 A AR P090102486A AR P090102486 A ARP090102486 A AR P090102486A AR 072791 A1 AR072791 A1 AR 072791A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
pim
carbocyclyl
aryl
Prior art date
Application number
ARP090102486A
Other languages
English (en)
Inventor
Michelle Lamb
Leslie Dakin
Qibin Su
Xiaolan Zheng
Jon Read
James Edward Dowling
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41050276&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR072791(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR072791A1 publication Critical patent/AR072791A1/es

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    • 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
    • C07D417/10—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 carbon chain containing aromatic 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/34—Oxygen atoms
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Estos compuestos actuan como inhibidores o moduladores de la actividad o funcion enzimática de las proteína quinasas Pim-1 y/o Pim-2 y/o Pim-3. Se proveen además métodos para su preparacion composiciones farmacéuticas que comprenden a los compuestos divulgados en la presente y su uso en la prevencion y el tratamiento de condiciones y enfermedades relacionadas con Pim quinasas, preferentemente cáncer. Reivindicacion 1: Un método de tratar o prevenir el cáncer, caracterizado porque comprende. a) proveer una composicion farmacéutica que comprende un compuesto de la formula 1, o sus sales, cuya funcionalidad es inhibir una quinasa Pim, donde R1 se selecciona entre un carbociclilo, arilo, y heterociclilo, donde R1 se sustituye opcionalmente con uno o más R2 iguales o diferentes: R2 se selecciona entre halogeno, alquilo C1-6, alquilo C1-6 halogenado, amino, aIquilamino C1-6, (alquil C1-6)2amino, y heterociclilo, donde R2 se sustituye opcionalmente con uno o más R3 iguales o diferentes; R3 se selecciona entre alquilo C1-6, halogeno, nitro, ciano, hidroxi, amino, mercapto, formilo, carboxi, carbamoilo, alcoxi C1-6, alquiltio C1-6, alquilamino C1-6, (alquil C1-6)2amino, alquilsulfinilo C1-6, alquilsulfonilo C1-6, arilsulfonilo, carbociclilo, arilo, y heterociclilo, donde R3 se sustituye opcionalmente con uno o más R4 iguales o diferentes; R4 se selecciona entre alquilo C1-6, halogeno, nitro, ciano, hidroxi, amino, mercapto, formilo, carboxi, carbamoilo, alcoxi C1-6, alquiltio C1-6, alquilamino C1-6, (alquil C1-6)2amino, alquilsulfinilo C1-6, alquilsulfonilo C1-6, arilsulfonilo, carbociclilo, arilo, y heterociclilo, donde R4 se sustituye opcionalmente con uno o más R5 iguales o diferentes; y R5 se selecciona entre halogeno, nitro, ciano, hidroxi, trifluorometoxi, trifluorometilo, amino, formilo, carboxi, carbamoilo, mercapto, sulfamoilo, metilo, etilo, metoxi, etoxi, acetilo, acetoxi, metilamino, etilamino, dimetilamino, dietilamino, N-metil-N-etilamino, acetilamino, N-metilcarbamoilo, N-etilcarbamoilo, N,N-dimetilcarbamoilo. N,N-dietilcarbamoilo, N-metil-N-etilcarbamoilo, metiltio, etiltio, metilsulfinilo, etilsulfinilo, mesilo, etilsulfonilo, metoxicarbonilo, etoxicarbonilo, N-metilsulfamoilo, N-etilsulfamoilo, N,N-dimetilsulfamoilo, N,N-dietilsulfamoilo, N-metil-N-etilsulfamoilo, carbociclilo, arilo, y heterociclilo; y b) administrar dicha composicion farmacéutica a un sujeto con diagnostico, síntomas , o en riesgo de contraer cáncer.
ARP090102486A 2008-07-02 2009-07-02 DERIVADOS DE TIAZOLIDIN-2, 4-DIONA, MÉTODOS PARA SU PREPARACIoN, COMPOSICIoN FARMACÉUTICA QUE LOS COMPRENDE Y SU USO EN LA ELABORACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DEL CÁNCER. AR072791A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US7763908P 2008-07-02 2008-07-02
US18327809P 2009-06-02 2009-06-02

Publications (1)

Publication Number Publication Date
AR072791A1 true AR072791A1 (es) 2010-09-22

Family

ID=41050276

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102486A AR072791A1 (es) 2008-07-02 2009-07-02 DERIVADOS DE TIAZOLIDIN-2, 4-DIONA, MÉTODOS PARA SU PREPARACIoN, COMPOSICIoN FARMACÉUTICA QUE LOS COMPRENDE Y SU USO EN LA ELABORACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DEL CÁNCER.

Country Status (27)

Country Link
US (2) US8901307B2 (es)
EP (1) EP2310010A2 (es)
JP (2) JP5261575B2 (es)
KR (1) KR20110031367A (es)
CN (2) CN102137666B (es)
AR (1) AR072791A1 (es)
AU (1) AU2009265362B2 (es)
BR (1) BRPI0914599A2 (es)
CA (1) CA2729557A1 (es)
CL (1) CL2010001636A1 (es)
CO (1) CO6341555A2 (es)
CR (1) CR20110016A (es)
DO (1) DOP2010000408A (es)
EA (1) EA018989B1 (es)
EC (1) ECSP10010735A (es)
HN (1) HN2010002786A (es)
IL (1) IL210127A0 (es)
MX (1) MX2010014233A (es)
MY (1) MY155961A (es)
NI (1) NI201100007A (es)
NZ (1) NZ590859A (es)
PE (1) PE20120304A1 (es)
SV (1) SV2011003786A (es)
TW (1) TWI461423B (es)
UY (1) UY31952A (es)
WO (1) WO2010001169A2 (es)
ZA (1) ZA201100844B (es)

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EA018989B1 (ru) 2013-12-30
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