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AR080074A1 - Naftiridinas sustituidas y su uso como medicamentos - Google Patents

Naftiridinas sustituidas y su uso como medicamentos

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Publication number
AR080074A1
AR080074A1 ARP110100305A AR080074A1 AR 080074 A1 AR080074 A1 AR 080074A1 AR P110100305 A ARP110100305 A AR P110100305A AR 080074 A1 AR080074 A1 AR 080074A1
Authority
AR
Argentina
Prior art keywords
alkyl
nr9r10
alkylene
hydrogen
individually selected
Prior art date
Application number
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English (en)
Inventor
Matthias Hoffmann
Guenter Linz
Gerhard Schaenzle
Andreas Schnapp
Georg Dahmann
Michael Philip Mazanetz
John Scott
Jasna Klicic
Edward Walker
Sandra Handschuh
Dennis Fiegen
Stephen P East
Original Assignee
Boehringer Ingelheim Int
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42272624&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR080074(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR080074A1 publication Critical patent/AR080074A1/es

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    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • 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
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00—Drugs for disorders of the metabolism
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    • A61P35/00—Antineoplastic agents
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Composiciones farmacéuticas que contienen estos compuestos, y usos de los mismos. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1) en la que R1 se selecciona entre -O-R3 o -NR3R4 donde R3 es alquilo C1-6 sustituido con R5 y R6 donde R5 se selecciona entre hidrogeno, alquilo C1-6 lineal o ramificado, alquenilo C2-6, -alquilen C1-6-O-alquilo C1-3, haloalquilo C1-3, donde R6 es un anillo X de formula (2); donde n es 0 o 1, donde es o bien un enlace sencillo o un doble enlace y donde A, B, D y E se seleccionan cada uno independientemente entre CH2, CH, C, N, NH, O o S y donde el anillo X se adjunta a la molécula mediante la posicion A, B, D o E, donde dicho anillo X puede estar opcionalmente sustituido con uno, dos o tres residuos seleccionados cada uno individualmente entre el grupo que consiste en -oxo, hidroxi, -alquilo C1-3, -haloalquilo C1-3, -O-alquilo C1-3, -alcanol C1-3 y halogeno, R4 se selecciona entre el grupo que consiste en hidrogeno y alquilo C1-6, R2 se selecciona entre el grupo que consiste en hidrogeno; arilo de 5 a 10 miembros; heteroarilo de 5 a 10 miembros que comprende 1, 2 o 3 heteroátomos cada uno individualmente seleccionado entre N, O y S; heterociclo saturado o parcialmente insaturado de 5 a 10 miembros que comprende 1, 2 o 3 heteroátomos cada uno individualmente seleccionado entre N, O y S; cicloalquilo saturado o parcialmente insaturado de 3 a 10 miembros, donde - en caso de que R2 no sea hidrogeno - dicho R2 puede estar opcionalmente sustituido con 1, 2, 3 o 4 residuos, cada uno individualmente seleccionado entre el grupo que consiste en hidrogeno, -oxo, halogeno, -alquilo C1-6, -alquenilo C2-6, -alquilen C1-6-COOH, -COOH, -CO-NR9R10, -alquilen C1-6-CO-NR9R10, -alquilen C1-6-NR9R10, -alquilen C1-6-CO-Q, -CO-Q, -alquilen C1-6-CO-NR9Q, -CO-NR9Q, -alquilen C1-6-NR11-CO-NR9R10, -alquilen C1-6-NR11-CO-Q, -alquilen C1-6-NR11-SO2R9, -alquilen C1-6-O-CO-R9, -alquilen C1-6-O-CO-NR9R10, -alquilen C1-6-O-R9, -alquilen C1-6-SO-NR9R10, -alquilen C1-6-SO2R9, -alquilen C1-6-SOR9, -alquinilen C1-6-O-R9, -alquinilen C1-6-Q, -alquinilen C1-6-NR9R10, arilo C5-10, -Q, -cicloalquilo C3-8, -O-R7, -O-alquilen C1-6-R7, -O-alquilen C1-6-O-R7, -haloalquilo C1-3, cianuro, -NR11R7, -NR11(alquilen C1-6-R7), -S(O)-alquilo C1-6, -SO2-alquilo C1-6, -S-alquilo C1-6, -SO2-NR9R10, -SO2-NR11Q, heteroarilo de 5 a 10 miembros que comprende 1, 2 o 3 heteroátomos cada uno individualmente seleccionado entre N, O y S, -NR11-CO-R7 y -O-CO-R7, donde R7 se selecciona del grupo que consiste en hidrogeno; alquilo C1-6 lineal o ramificado; -haloalquilo C1-6; -alquilen C1-6-COOH; -alquilen C1-6-CO-NR9R10; -alquilen C1-6-CO-Q; -alquilen C2-6-NR11-CO-NR9R10; -alquilen C2-6-NR11-CO-Q; -alquilen C2-6-NR11-SO2R9; -alquilen C2-6-NR9R10; -alquilen C2-6-Q; -alquilen C2-6-O-CO-R9, -alquilen C2-6-O-CO-NR9R10, -alquilen C2-6-SO-NR9R10, -alquilen C2-6-SO2-R9, -alquilen C2-6-SO-R9, -SO2-R9, -SO-R9, -SO2-NR9R10, -SO2-NR11Q, -SO2-Q, -alquilen C1-6-O-R9 -CO-NR9R10, -CONR9Q, -CO-R9, -CO-Q, -alquilen C1-6-Q, -arilo C5-10, -Q, cicloalquilo saturado o parcialmente insaturado de 3 a 8 miembros; heteroarilo de 5 a 10 miembros que comprende 1, 2 o 3 heteroátomos cada uno individualmente seleccionado entre N, O y S; -alquilen C1-6-heteroarilo, donde este heteroarilo tiene 5 a 10 miembros y comprende 1, 2 o 3 heteroátomos cada uno individualmente seleccionado entre N, O y S; donde - en caso de que R7 no sea hidrogeno - R7 puede estar opcionalmente sustituido con 1, 2 o 3 residuos R8 que se seleccionan individualmente entre el grupo que consiste en hidrogeno; -oxo; hidroxi; -alquilo C1-6; -haloalquilo C1-6; -NR9R10 , -Q, -NR9Q, cicloalquilo saturado o parcialmente insaturado de 3 a 6 miembros; donde - en caso de que R8 no sea hidrogeno - R8 puede estar opcionalmente sustituido con 1, 2 o 3 residuos seleccionados entre hidrogeno, -oxo, -hidroxi, -alquilo C1-6, halogeno, -haloalquilo C1-6, -O-alquilo C1-6, -alquilen C1-3-O-alquilo C1-3, donde cada uno de R9, R1° y R11 se selecciona individualmente uno de otro del grupo que consiste en hidrogeno, -alquilo C1-6, -cicloalquilo C3-8, -alquil C1-6-cicloalquilo C3-8 y fenilo, y donde cada Q se selecciona individualmente o bien de un heterociclo saturado o parcialmente insaturado de 5 a 10 miembros o de un heterociclo parcialmente insaturado que comprende 1, 2 o 3 heteroátomos cada uno individualmente seleccionado entre N, O o S, o entre un heteroarilo de 5 a 10 miembros que comprende 1, 2 o 3 heteroátomos cada uno individualmente seleccionado entre N, O y S; donde Q está unido al resto de la molécula o bien mediante un átomo de carbono o mediante un átomo de nitrogeno, los N-oxidos de los compuestos anteriormente mencionados, particularmente los 1-naftiridinil-oxidos de los compuestos previamente mencionados, y las sales farmacéuticamente aceptables de los compuestos anteriormente mencionados.
ARP110100305 2010-01-29 2011-01-28 Naftiridinas sustituidas y su uso como medicamentos AR080074A1 (es)

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EP (1) EP2528915B1 (es)
JP (1) JP5629331B2 (es)
KR (1) KR20120125267A (es)
CN (1) CN102822172A (es)
AR (1) AR080074A1 (es)
AU (1) AU2011209274B8 (es)
BR (1) BR112012018865A2 (es)
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BR112012018865A2 (pt) 2010-01-29 2016-04-12 Boehringer Ingelheim Int naftiridinas substituídas e seu uso como inibidores de quinase syk
WO2012167423A1 (en) 2011-06-08 2012-12-13 Hutchison Medipharma Limited Substituted pyridopyrazines as novel syk inhibitors
EA024845B1 (ru) 2011-07-26 2016-10-31 Бёрингер Ингельхайм Интернациональ Гмбх Замещенные хинолины и их применение в качестве лекарственных средств
WO2014086032A1 (en) * 2012-12-07 2014-06-12 Hutchison Medipharma Limited Substituted pyridopyrazines as syk inhibitors
CN104812753A (zh) * 2012-12-07 2015-07-29 和记黄埔医药（上海）有限公司 作为Syk抑制剂的取代吡啶并吡嗪类化合物
NZ718576A (en) 2013-10-21 2019-11-29 Genosco Substituted pyrimidine compounds and their use as syk inhibitors
HRP20191364T1 (hr) 2014-03-19 2019-11-01 Boehringer Ingelheim Int Sik-inhibitori tipa heteroarila
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