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AR044543A1 - Derivados de pirazolo-quinazolina, un procedimiento para su preparacion y su uso como inhibidor de quinasa - Google Patents

Derivados de pirazolo-quinazolina, un procedimiento para su preparacion y su uso como inhibidor de quinasa

Info

Publication number
AR044543A1
AR044543A1 ARP040101748A ARP040101748A AR044543A1 AR 044543 A1 AR044543 A1 AR 044543A1 AR P040101748 A ARP040101748 A AR P040101748A AR P040101748 A ARP040101748 A AR P040101748A AR 044543 A1 AR044543 A1 AR 044543A1
Authority
AR
Argentina
Prior art keywords
heterocyclyl
cycloalkyl
alkyl
group
heterocyclylalkyl
Prior art date
Application number
ARP040101748A
Other languages
English (en)
Inventor
Gabriella Traquandi
Maria Gabriella Brasca
Paolo Polucci
Fulvia Roletto
Anna Vulpetti
Achille Panzeri
Francesca Quartieri
Ron Ferguson
Paola Vianello
Daniele Fancelli
Alessio Roberto D
Paolo Pevarello
Original Assignee
Pharmacia Italia Spa
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33476970&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR044543(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pharmacia Italia Spa filed Critical Pharmacia Italia Spa
Publication of AR044543A1 publication Critical patent/AR044543A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D403/14Heterocyclic 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Oncology (AREA)
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  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
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  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
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  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Los compuestos pueden ser útiles, en terapéutica, en el tratamiento de enfermedades asociadas con una actividad desregulada de la proteína quinasa, como cáncer. Reivindicación 1: Un derivado de pirazolo-quinazolina representado por la fórmula (1) o (2), caracterizado porque: R es hidrógeno o un grupo opcionalmente sustituido seleccionado entre amino, alquilo C1-6 lineal o ramificado, cicloalquilo C3-10, arilo, arilalquilo, heterociclilo o heterociclilalquilo; X es un enlace simple o un radical divalente seleccionado entre -NR'-, -CONR'-, -NH-CO-NH-, -O-, -S- o -SO2-, en donde R' es hidrógeno o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 lineal o ramificado, cicloalquilo C3-6, arilo, arilalquilo, heterociclilo, heterociclilalquilo o, junto con el átomo de nitrógeno al cual están unidos, R y R' pueden formar un grupo heteroarilo o heterociclilo de 5 a 6 miembros, que contiene opcionalmente un heteroátomo adicional seleccionado entre N, O o S; R1 ligado a uno cualquiera de los átomos de nitrógeno del anillo pirazol según la fórmula (1) o (2), representa un átomo de hidrógeno o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 lineal o ramificado, cicloalquilo C3-6, arilo, arilalquilo, heterociclilo o heterociclilalquilo o, en la fórmula (2), R1 es un grupo -(CH2)n-NH- divalente que está ligado a R2, en donde n es 2 ó 3; R2 es un grupo seleccionado entre -NR''R''', -N(OH)R'', -OR'' o -R'', en donde R'' y R''' son, cada uno independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 lineal o ramificado, cicloalquilo C3-6, o cicloalquilo-alquilo, arilo, arilalquilo, heterociclilo o heterociclilalquilo o, junto con el átomo de nitrógeno al cual están unidos, R'' y R''' pueden formar un grupo heteroarilo o heterociclilo de 5 a 6 miembros, que contiene opcionalmente un heteroátomo adicional seleccionado entre N, O o S; A es un grupo divalente seleccionado entre -CH2-, - (CH2)2-, -CH2-C(CH3)2-, -C(CH3)2-CH2- o -CH=CH-; o una sal farmacéuticamente aceptable de los mismos.
ARP040101748A 2003-05-22 2004-05-20 Derivados de pirazolo-quinazolina, un procedimiento para su preparacion y su uso como inhibidor de quinasa AR044543A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US47266103P 2003-05-22 2003-05-22

Publications (1)

Publication Number Publication Date
AR044543A1 true AR044543A1 (es) 2005-09-21

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ID=33476970

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP040101748A AR044543A1 (es) 2003-05-22 2004-05-20 Derivados de pirazolo-quinazolina, un procedimiento para su preparacion y su uso como inhibidor de quinasa
ARP150103780A AR102722A2 (es) 2003-05-22 2015-11-20 Un derivado de pirazolo-quinazolina, su uso, un procedimiento para prepararlos, composiciones farmacéuticas que los comprenden, compuestos utilizables en su preparación, una biblioteca de dos o más compuestos, y un producto o kit

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP150103780A AR102722A2 (es) 2003-05-22 2015-11-20 Un derivado de pirazolo-quinazolina, su uso, un procedimiento para prepararlos, composiciones farmacéuticas que los comprenden, compuestos utilizables en su preparación, una biblioteca de dos o más compuestos, y un producto o kit

Country Status (36)

Country Link
US (9) US7482354B2 (es)
EP (1) EP1636236B1 (es)
JP (1) JP5043432B2 (es)
KR (1) KR101084871B1 (es)
CN (2) CN1826343A (es)
AP (1) AP2064A (es)
AR (2) AR044543A1 (es)
AU (1) AU2004240772B2 (es)
BR (2) BRPI0410563B8 (es)
CA (1) CA2526578C (es)
CO (1) CO5721006A2 (es)
CR (1) CR8102A (es)
CY (1) CY1114708T1 (es)
DK (1) DK1636236T3 (es)
EA (1) EA010904B1 (es)
EC (1) ECSP056194A (es)
ES (1) ES2436524T3 (es)
GE (1) GEP20094664B (es)
HR (1) HRP20050967B8 (es)
IL (1) IL172046A (es)
IS (1) IS2939B (es)
ME (1) ME00142B (es)
MX (1) MXPA05012573A (es)
MY (1) MY142019A (es)
NO (1) NO334992B1 (es)
NZ (1) NZ543661A (es)
OA (1) OA13170A (es)
PL (1) PL1636236T3 (es)
PT (1) PT1636236E (es)
RS (2) RS52899B (es)
SI (1) SI1636236T1 (es)
TN (1) TNSN05298A1 (es)
TW (1) TWI349672B (es)
UA (1) UA80763C2 (es)
WO (1) WO2004104007A1 (es)
ZA (1) ZA200509486B (es)

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