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AR067599A1 - Derivados de indazol sustituido activos como inhibidores de quinasa - Google Patents

Derivados de indazol sustituido activos como inhibidores de quinasa

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Publication number
AR067599A1
AR067599A1 ARP080103104A ARP080103104A AR067599A1 AR 067599 A1 AR067599 A1 AR 067599A1 AR P080103104 A ARP080103104 A AR P080103104A AR P080103104 A ARP080103104 A AR P080103104A AR 067599 A1 AR067599 A1 AR 067599A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
aryl
substituted
heteroaryl
Prior art date
Application number
ARP080103104A
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English (en)
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Nerviano Medical Sciences Srl
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39764856&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR067599(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Nerviano Medical Sciences Srl filed Critical Nerviano Medical Sciences Srl
Publication of AR067599A1 publication Critical patent/AR067599A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/06Free radical scavengers or antioxidants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D403/14Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
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  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Se describen derivados de indazol sustituido de la formula (1) y sales farmacéuticamente aceptables de estos, como se define en la especificacion, procesos para su preparacion y composiciones farmacéuticas que los comprenden. Los compuestos de la presente pueden ser utiles en terapia, en el tratamiento de enfermedades asociadas con una actividad desregulada de la proteína quinasa, como el cáncer. Reivindicacion 1: Un compuesto de la formula (1), caracterizado porque X es -CH2-, -CH(OH)-, -CH(OR')- o -C(R'Rö)-, en donde: R' es alquilo C1-6 y Rö es H o alquilo C1-6; Ar es arilo o heteroarilo opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halogeno, alquenilo C2-6, alquinilo C2-6, ciano, nitro, NHCOR4, COR4, NR5R6, NR5COR4, OR7, SR7, SOR10, SO2R10, NHSOR10, NHSO2R10, R8R9N-alquilo C1-6, R8O-alquilo C1-6, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo y heteroarilo de cadena recta o ramificada opcionalmente más sustituido en donde: R4 es hidrogeno, alquenilo C2-6, alquinilo C2-6, NR5R6, OR7, SR7, R8R9N-alquilo C1-6, R8O-alquilo C1-6, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada opcionalmente más sustituido; R5 y R6 son independientemente hidrogeno, alquenilo C2-6, alquinilo C2-6, R8R9N-alquilo C2-6, R8O-alquilo C2-6, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada, opcionalmente más sustituido, o R5 y R6, tomados juntos con el átomo de nitrogeno al cual están unidos pueden forman un grupo heterociclilo opcionalmente sustituido; R7 es hidrogeno, alquenilo C2-6, alquinilo C2-6, COR4, SOR10, SO2R10, R8R9N-alquilo C2-6, R8O-alquilo C2-6, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada, opcionalmente más sustituido, en donde R4 es como se definiera anteriormente; R8 y R9 son independientemente hidrogeno, alquenilo C2-6, alquinilo C2-6, COR4, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada opcionalmente más sustituido, o R8 y R9, tomados juntos con el átomo de nitrogeno al cual están unidos, pueden formar un grupo heterociclilo opcionalmente sustituido, en donde R4 es como se definiera anteriormente; R10 es hidrogeno, alquenilo C2-6, alquinilo C2-6, NR5R6, OR7, R8R9N-alquilo C1-6, R8O-alquilo C1-6, alquilo C1-6de cadena recta o ramificado, opcionalmente más sustituido, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo, en donde R5, R6, R7, R8 y R9 son como se definiera anteriormente; Res un alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada, opcionalmente sustituido, R1, R2 y R3 son independientemente hidrogeno, halogeno, nitro, alquilo C1-6 de cadena recta o ramificada, opcionalmente sustituido, NR5R6, u OR7, en donde R5, R6 y R7 son como se definiera anteriormente; o isomeros, tautomeros, prodrogas o sales de estos farmacéuticamente aceptables.
ARP080103104A 2007-07-20 2008-07-18 Derivados de indazol sustituido activos como inhibidores de quinasa AR067599A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07112881 2007-07-20

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AR067599A1 true AR067599A1 (es) 2009-10-14

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ARP080103104A AR067599A1 (es) 2007-07-20 2008-07-18 Derivados de indazol sustituido activos como inhibidores de quinasa

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US (11) US8299057B2 (es)
EP (1) EP2176231B1 (es)
JP (1) JP5506674B2 (es)
KR (2) KR101567763B1 (es)
CN (2) CN103923072B (es)
AR (1) AR067599A1 (es)
AU (1) AU2008280283B2 (es)
BR (1) BRPI0814628B1 (es)
CA (1) CA2693901C (es)
CL (1) CL2008002129A1 (es)
DK (1) DK2176231T3 (es)
EA (1) EA018503B1 (es)
ES (1) ES2605230T3 (es)
FI (1) FIC20200051I1 (es)
FR (1) FR20C1064I2 (es)
HU (2) HUE030929T2 (es)
IL (1) IL203292A (es)
NL (1) NL301090I2 (es)
NO (2) NO2020042I1 (es)
NZ (1) NZ583450A (es)
PH (1) PH12013501594A1 (es)
PL (1) PL2176231T3 (es)
PT (1) PT2176231T (es)
SG (1) SG183049A1 (es)
SI (1) SI2176231T1 (es)
TW (1) TWI421073B (es)
UA (1) UA99141C2 (es)
WO (1) WO2009013126A1 (es)
ZA (1) ZA201001086B (es)

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