AR063545A1 - Derivados de tiazoles -1,3 aminosustituidos, composiciones farmaceuticas que las contienen y usos como agentes anticancer - Google Patents

Derivados de tiazoles -1,3 aminosustituidos, composiciones farmaceuticas que las contienen y usos como agentes anticancer

Info

Publication number
AR063545A1
AR063545A1 ARP070104808A ARP070104808A AR063545A1 AR 063545 A1 AR063545 A1 AR 063545A1 AR P070104808 A ARP070104808 A AR P070104808A AR P070104808 A ARP070104808 A AR P070104808A AR 063545 A1 AR063545 A1 AR 063545A1
Authority
AR
Argentina
Prior art keywords
alkylene
alkyl
aryl
heteroaryl
heterocyclyl
Prior art date
Application number
ARP070104808A
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English (en)
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of AR063545A1 publication Critical patent/AR063545A1/es

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Classifications

    • 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • 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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto que tiene la formula (1) o una sal, solvato, éster, profármaco o estereoisomero farmacéuticamente aceptable del mismo, donde la línea entre cortada indica un enlace opcional y adicional y donde: R1 es H, alquilo, alquenilo, alquinilo, -(alquileno)m-arilo, -(alquileno)m-cicloalquilo, -(alquileno)m-heteroarilo, -(alquileno)m-heterociclilo o -(alquileno)m-heterocilenilo, donde cualquier grupo arilo, cicloalquilo, heteroarilo, heterociclilo o heterociclenilo puede estar opcional e independientemente sustituido en un átomo de carbono anular o de nitrogeno anular con hasta 3 sustituyentes seleccionados entre halo, alquilo, -O-alquilo, -(alquenileno)m-NR(9)2, -C(O)OR7, -CN, -OH, -(alquileno)m-heteroarilo y -(alquileno)m-arilo; y donde cualquier grupo sustituyente arilo o heteroarilo puede estar sustituido con hasta 5 sustituyentes, que pueden ser iguales o diferentes, y se seleccionan entre -halo, -OH, alquilo, -C(O)OH, -C(O)O-alquilo, -N(R9)2, y -O- alquilo; y donde cualquier grupo arilo, cicloalquilo, heteroarilo, heterociclilo o heterociclenilo puede estar opcionalmente fusionado a un grupo arilo, cicloalquilo, heteroarilo, heterociclilo o heterociclenilo; R2 es H, alquilo, arilo, heteroarilo, -C(O)-alquilo o -C(O)-arilo, donde el arilo, heteroarilo o porcion arilo o un grupo -C(O)-arilo puede estar sustituido con hasta 3 sustituyentes, que pueden ser iguales o diferentes, y se seleccionan independientemente entre halo, alquilo, -C(O)OH, y -O-alquilo; cada caso de R3 es independientemente H, alquilo, haloalquilo, hidroxialquilo, -(alquileno)m-C(O)N(R8)2, -(alquileno)m-NHC(O)-R9 o -(alquileno)m-N(R9)2, o R3 y el átomo de carbono anular al cual esta unido se combinan para formar un grupo carbonilo; R4 es H, -alquilo, haloalquilo, hidroxialquilo, -(alquileno)m-C(O)N(R8)2, -(alquileno)m-NHC(O)-R9 o -(alquileno)m-N(R9)2, o R3 y R3a, junto con el átomo de carbono comun al cual cada uno esta unido, se une para formar un grupo carbonilo, cicloalquilo o heterociclilo; R4a es H, -alquilo, haloalquilo, hidroxialquilo, -(alquileno)m-C(O)N(R8)2, -(alquileno)m-NHC(O)-R9 o -(alquileno)m-N(R9)2; cada caso de R5 es independientemente H, -alquilo, -(alquileno)m-arilo, - (alquileno)m-heteroarilo, -(alquileno)m-heterociclilo, -(alquileno)m-N(R9)2, -(alquileno)m-OH, -(alquileno)m-NHC(O)R9, hidroxialquilo, haloalquilo, -C(O)R6, -C(O)OR9, -C(O)-(alquileno)m-N(R9)2, -(alquileno)m-NHC(O)R7, -NHC(O)OR9 o -NHS(O)2R7; R6 es H, alquilo, arilo, heteroarilo o -NHOH; R7 es H, alquilo o haloalquilo; R8 es H, -OH, alquilo, -O-alquilo, o haloalquilo; R9 es H, alquilo, arilo, heterociclilo, heteroarilo o cicloalquilo; R10 es H, -alquilo, haloalquilo, hidroxialquilo, - (alquileno)m-C(O)N(R8)2, -(alquileno)m-NHC(O)R9 o -(alquileno)m-N(R9)2, o R10 y R10a, junto con el átomo de carbono comun al cual cada uno esta unido, se unen para formar un grupo carbonilo, cicloalquilo o heterociclilo; R10a es H, alquilo, haloalquilo, hidroxialquilo, -(alquileno)m-C(O)N(R8)2, -(alquileno)m-NHC(O)-R9 o -(alquileno)m-N(R9)2; cada caso de R11 es independientemente H, alquilo, haloalquilo, hidroxialquilo, -(alquileno)m-C(O)N(R8)2, -(alquileno)m-NHC(O)-R9 o -(alquileno)m- N(R9)2, o R11 y el átomo de carbono anular al cual esta unido se combinan para formar un grupo carbonilo; cada caso de R12 es independientemente H, -(alquileno)m-arilo, -(alquileno)m-heteroarilo, -(alquileno)m-heterociclilo, -S(O)2-alquilo, -S(O)2- arilo, -S(O)2-heteroarilo, hidroxialquilo, -C(O)R9 o -C(O)OR9; Ar es arileno o heteroarileno, donde el arileno o heteroarileno se une mediante 2 cualquiera de sus átomos de carbono anulares adyacentes, y donde el grupo arileno o heteroarileno puede estar opcionalmente sustituido con hasta 4 sustituyentes, que pueden ser iguales o diferentes, y se seleccionan independientemente entre halo, alquilo, alcoxi, ariloxi, -NH2, -NH-alquilo, -N(alquilo)2, -SR8, -S(O)R8, -C(O)R8, -C(O)OR8, -C(O)N(R8)2, - NHC(O)R8, haloalquilo, -CN y NO2, de modo que cuando Ar es tetrahidronaftileno, R3 y r4 son cada uno distinto de hidrogeno; W es -N(R12)2-, -S-, -O- o -C(R5)2-, donde ambos grupos R5 y el átomo de carbono comun al cual están unidos se pueden combinar para formar un grupo cicloalquilo o heterociclilo, cada uno de los cuales puede estar sustituido adicionalmente; Y es H, halo, alquilo o -CN; Z es -C(R8)- o -N-, de modo que cuando está presenta el enlace opcional adicional, Z es -C(R8)-; cada caso de m es independientemente 0 o 1; n es un numero entero que va de 0 a 2; y p es 0 o 1.
ARP070104808A 2006-10-31 2007-10-30 Derivados de tiazoles -1,3 aminosustituidos, composiciones farmaceuticas que las contienen y usos como agentes anticancer AR063545A1 (es)

Applications Claiming Priority (1)

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US85542006P 2006-10-31 2006-10-31

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US (1) US8227605B2 (es)
EP (1) EP2078002B1 (es)
JP (1) JP5103604B2 (es)
KR (1) KR20090075869A (es)
CN (1) CN101573345A (es)
AR (1) AR063545A1 (es)
AU (1) AU2007314341B2 (es)
CA (1) CA2668209A1 (es)
IL (1) IL198398A0 (es)
MX (1) MX2009004785A (es)
TW (1) TW200829582A (es)
WO (1) WO2008054701A1 (es)

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Also Published As

Publication number Publication date
AU2007314341B2 (en) 2013-04-11
CN101573345A (zh) 2009-11-04
MX2009004785A (es) 2009-06-05
JP2010508273A (ja) 2010-03-18
CA2668209A1 (en) 2008-05-08
TW200829582A (en) 2008-07-16
AU2007314341A1 (en) 2008-05-08
US20100055090A1 (en) 2010-03-04
KR20090075869A (ko) 2009-07-09
JP5103604B2 (ja) 2012-12-19
WO2008054701A1 (en) 2008-05-08
US8227605B2 (en) 2012-07-24
EP2078002B1 (en) 2013-08-28
EP2078002A1 (en) 2009-07-15
IL198398A0 (en) 2010-02-17

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