AR078674A1 - Derivados de pirazolo[3, 4-d]pirimidina, un intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la inhibicion de las pi3-quinasas - Google Patents

Derivados de pirazolo[3, 4-d]pirimidina, un intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la inhibicion de las pi3-quinasas

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Publication number
AR078674A1
AR078674A1 ARP100103812A ARP100103812A AR078674A1 AR 078674 A1 AR078674 A1 AR 078674A1 AR P100103812 A ARP100103812 A AR P100103812A AR P100103812 A ARP100103812 A AR P100103812A AR 078674 A1 AR078674 A1 AR 078674A1
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AR
Argentina
Prior art keywords
alkyl
3alkyl
hydrogen
nr6r7
alkoxy
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ARP100103812A
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English (en)
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Respivert Ltd
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Application filed by Respivert Ltd filed Critical Respivert Ltd
Publication of AR078674A1 publication Critical patent/AR078674A1/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
    • C07D487/02—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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • A61P35/04—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
    • A61P37/08—Antiallergic agents
    • 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
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

Composiciones farmacéuticas que los comprenden y al uso de los compuestos y sus composiciones en tratamiento, por ejemplo, en el tratamiento de enfermedades inflamatorias, en particular enfermedad inflamatoria respiratoria. También se provee un intermediario de la preparacion de dichos compuestos. Reivindicacion 1: Un compuesto de la formula (1) en donde R1 es H, una cadena de alquilo C1-15 ramificada o no ramificada, saturada o insaturada, en donde opcionalmente uno o varios carbonos (por ejemplo, 1, 2 o 3 carbonos, apropiadamente 1 o 2, en particular 1) están reemplazados por un heteroátomo seleccionado de O, N, S(O)p (por ejemplo, un grupo CH2 está reemplazado con O o con NH o con S o con SO2 o un grupo -CH3 en el término de la cadena o en una ramificacion está reemplazado con OH o con NH2), en donde dicha cadena está opcionalmente sustituida con uno o varios grupos (por ejemplo, 1 a 3, tales como 2 grupos) seleccionados, de modo independiente, de oxo, halogeno, un grupo arilo, heteroarilo, carbociclilo o un grupo heterociclilo, cada grupo arilo, heteroarilo, carbociclilo o heterociclilo que lleva 0 a 3 sustituyentes seleccionados de halogeno, -hidroxilo, -alquilo C1-6, -alcoxi C1-6, -alcoxi C2-3-Oalquilo C1-3, -alquil C2-3-Oalquilo C1-3, - hidroxialquilo C1-3, -haloalquilo C1-6, amino, -monoalquil C1-4 o dialquil C2-8-amino, -monoacil C1-4 o -diacil C2-8-amino, -alquil C0-6-S(O)palquilo C1-6, -alquil C0-6-S(O)pNR6R7, -alquil C0-6-NR8alquil C0-6-S(O)palquilo C1-6, -alquil C0-6-C(O)Oalquilo C0-6, -NR8alquil C0-6-C(O)NR6R7-NR8alquil C0-6-C(O)alquilo C0-6, -alquil C0-6-C(O)NR6R7 y -alquil C0-6-C(O)alquilo C1-6; y/o un arilo heterociclilo o carbociclilo; X es arilo C6-10 o un heteroarilo C5-9 sustituido cada uno con R2a y bi R2b en donde R2a está seleccionado de hidrogeno, -alquilo C1-3, halo, hidroxilo, ciano, -haloalquilo C1-3, -alcoxi C1-3, -alcoxi C2-3-Oalquilo C1-3, -alquil C2-3-Oalquilo C1-3, -hidroxialquilo C1-3, -alquil C0-6-S(O)qalquilo C1-3, -alquil C0-6-S(O)NR6R7, -alquil C0-6-NR8alquil C0-6-S(O)palquilo C1-6, -alquil C0-6-C(O)OH, -alquil C0-6-C(O)Oalquilo C1-6, -NR8alquil C0-6-C(O)NR6R7, -NR8aIquil C0-6-C(O)alquilo C1-6, -alquil C0-6-C(O)NR6R7 y -alquil C0-6-C(O)aIquilo C1-6; y R2b está seleccionado de hidrogeno, alquilo C1-3, halo, hidroxilo, ciano, -haloalquilo C1-3, -alcoxi C1-3 y -alquil C0-6-S(O)qaIquilo C1-3; R3a es hidroxilo; R3b está seleccionado de hidrogeno, hidroxilo, halo, ciano, -haloalquilo C1-3, -hidroxialquilo C1-3, -alcoxi C1-3 y -S(O)qalquilo C1-3; R4 es hidrogeno o -alquilo C1-3; R5 es hidrogeno o -alquilo C1-3; R6 es hidrogeno o -alquilo C1-6; R7 es hidrogeno o -alquilo C1-6; R8 es hidrogeno o -alquilo C1-6; p es 0 o un numero entero 1 o 2; q es 0 o un numero entero 1 o 2 o una de sus sales farmacéuticamente aceptables, incluyendo todos sus estereoisomeros, tautomeros y derivados isotopicos. Reivindicacion 22: Un intermediario de la formula (6).
ARP100103812A 2009-10-19 2010-10-19 Derivados de pirazolo[3, 4-d]pirimidina, un intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la inhibicion de las pi3-quinasas AR078674A1 (es)

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GBGB0918249.4A GB0918249D0 (en) 2009-10-19 2009-10-19 Compounds

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AR078674A1 true AR078674A1 (es) 2011-11-23

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ARP100103812A AR078674A1 (es) 2009-10-19 2010-10-19 Derivados de pirazolo[3, 4-d]pirimidina, un intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la inhibicion de las pi3-quinasas

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US (4) US8741909B2 (es)
EP (1) EP2491037B1 (es)
JP (1) JP5889792B2 (es)
KR (1) KR101770616B1 (es)
CN (1) CN102712645B (es)
AR (1) AR078674A1 (es)
AU (1) AU2010309832B2 (es)
BR (1) BR112012009214A2 (es)
CA (1) CA2777902C (es)
CL (1) CL2012000981A1 (es)
CR (1) CR20120264A (es)
CY (1) CY1116057T1 (es)
DK (1) DK2491037T3 (es)
EA (1) EA020330B3 (es)
EC (1) ECSP12011805A (es)
ES (1) ES2477270T3 (es)
GB (1) GB0918249D0 (es)
HK (1) HK1173728A1 (es)
HR (1) HRP20140599T1 (es)
IL (1) IL219248A (es)
ME (1) ME02064B (es)
MX (1) MX2012004525A (es)
MY (1) MY164731A (es)
NI (2) NI201200061A (es)
NZ (2) NZ599162A (es)
PE (1) PE20121390A1 (es)
PL (1) PL2491037T3 (es)
PT (1) PT2491037E (es)
RS (1) RS53385B (es)
SI (1) SI2491037T1 (es)
SM (1) SMT201400086B (es)
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UA (1) UA108743C2 (es)
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