AR102722A2 - 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 - Google Patents

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

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Publication number
AR102722A2
AR102722A2 ARP150103780A ARP150103780A AR102722A2 AR 102722 A2 AR102722 A2 AR 102722A2 AR P150103780 A ARP150103780 A AR P150103780A AR P150103780 A ARP150103780 A AR P150103780A AR 102722 A2 AR102722 A2 AR 102722A2
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AR
Argentina
Prior art keywords
heterocyclyl
cycloalkyl
alkyl
group selected
heterocyclylalkyl
Prior art date
Application number
ARP150103780A
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English (en)
Inventor
Fancelli Daniele
Vianello Paola
Ferguson Ron
Quartieri Francesca
Panzeri Achille
Pevarello Paolo
Vulpetti Anna
Roletto Fulvia
Polucci Paolo
Dalessio Roberto
Gabriella Brasca Maria
Traquandi Gabriella
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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=33476970&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR102722(A2) "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 AR102722A2 publication Critical patent/AR102722A2/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • 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
    • A61K31/495—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
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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

Abstract

Se revelan derivados de pirazolo-quinazolina de fórmula (1) ó (2) como se definen en la memoria y sales farmacéuticamente aceptables de los mismos, un procedimiento para su preparación y composiciones farmacéuticas que los comprenden; estos 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) ó (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 ó S; R¹ ligado a uno cualquiera de los átomos de nitrógeno del anillo pirazol según la fórmula (1) ó (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 -NRR, -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 ó 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. Reivindicación 26: Un compuesto de fórmula (3) ó (4), como se definió en el paso (p.3) de la reivindicación 24 en donde R¹ es 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.
ARP150103780A 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 AR102722A2 (es)

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US47266103P 2003-05-22 2003-05-22

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AR102722A2 true AR102722A2 (es) 2017-03-22

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ID=33476970

Family Applications (2)

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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

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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

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US (8) US7482354B2 (es)
EP (1) EP1636236B1 (es)
JP (1) JP5043432B2 (es)
KR (1) KR101084871B1 (es)
CN (2) CN102079746A (es)
AP (1) AP2064A (es)
AR (2) AR044543A1 (es)
AU (1) AU2004240772B2 (es)
BR (2) BR122019010200B8 (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)
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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) RS20050944A (es)
SI (1) SI1636236T1 (es)
TN (1) TNSN05298A1 (es)
TW (1) TWI349672B (es)
UA (1) UA80763C2 (es)
WO (1) WO2004104007A1 (es)
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