ES2528441T3 - Hetarilaminonaftiridinas - Google Patents

Hetarilaminonaftiridinas Download PDF

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ES2528441T3
ES2528441T3 ES11700994.4T ES11700994T ES2528441T3 ES 2528441 T3 ES2528441 T3 ES 2528441T3 ES 11700994 T ES11700994 T ES 11700994T ES 2528441 T3 ES2528441 T3 ES 2528441T3
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alq
nyy
indicates
atoms
het3
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Alfred Jonczyk
Dieter Dorsch
Frank Zenke
Christiane Amendt
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Merck Patent GmbH
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P9/10—Drugs 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • AIDS & HIV (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (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

Compuesto de fórmula (I)**Fórmula** donde W1, W5, W6 indican independientemente entre sí N o CH; W2 indica N o CR6; W3 indica N o CR5; con la condición de que al menos uno de W1, W2, W3, W5 o W6 indique N; X indica NR1, Alq, O o S R1 indica H, A o Cic; R5 indica H, A, Hal, OY, CN, -Alq-OY, COOY, -CO-NYY, SA, SO2A, NYY, -OAlq-OY, -OAlq-NYY, -OAlq-NYCOOY, -OAlq-Het3, NO2, -NH-Alq-COOY, -NH-CO-Alq-OY, -NH-CO-Alq-OCOY, -NH-CO-Alq-NYY, -NH-CO-NYY, - NH-CO-Het3, -NY-COOY, -NY-SO2Y, -NH-SO2-NYY, -NH-Het2, -NH-R2, -NY-CO-R2, -NY-CO-NY-R2, -NY-COO-R2, -NY-SO2-R2, -NY-SO2-NY-R2, -OAr, -NY-Ar, -OHet1, NY-Het1, -CO-NYY-NYY, -CO-Het3 o -CO-NH-Alq-Het3; R1, R5 juntos también indican -CH>=CH-, -C(Y)>=N-, -N>=C(Y)-, -C(COY)>=N-, -C(CO-R2)>=N-, -CO-NH-, -NH-CO-, -SO2- NH-, -NH-SO2-, >=CH-NH-CO-, -CH-N(Alq-Het3)-CO-, -CH>=C(NO2)- o -CH>=C(Hal)-; R6 indica H, A, Hal, OY, CN, -Alq-OY, COOY, -CO-NYY, NYY, -NY-COOY, -NH-Alq-NYY, -NH-COA, -NH-COAlq- NYY, -NH-Het2, Het3, -OAr, -NY-Ar, -OHet1, NY-Het1, Het1, -NH-SO2Y, -NH-Cic, -NH-Het3, -NH-Alq-Het3, -NHAlq- OY, -NH-CO-NYY, -NH-CO-Het3, -CO-NH-Het3, -NH-CO-Alq-OY, -NH-CO-Alq-Het3, -CO-NH-Alq-Het3, -NH-CO20 Alq-NH-COOY o -CO-NH-Alq-NYY; R2 indica un carboarilo monocíclico con 5-8 átomos de C o un heteroarilo monocíclico con 2-7 átomos de C y 1- 4 átomos de N, O y/o S, cada uno de los cuales puede estar sustituido por al menos un sustituyente seleccionado a partir del grupo de A, Hal, CN, NYY, OY, >=O; R3, R4 indican independientemente entre sí H, A, Hal, CN, NYY, OY, -OAlq-NYY, -OAlq-OY; Y indica H o A; A indica alquilo ramificado o no ramificado con 1-10 átomos de C, en el que 1-7 átomos de H pueden estar sustituidos por Hal; Cic indica cicloalquilo con 3-7 átomos de C; en el que 1-4 átomos de H pueden estar sustituidos por otro distinto de A, Hal y/u OY; Alq indica alquileno con 1-6 átomos de C, en el que 1-4 átomos de H pueden estar sustituidos independientemente entre sí por Hal y/o CN; Ar indica un carbociclo saturado, insaturado o aromático, monocíclico o bicíclico con 6-10 átomos de C, que puede estar sustituido por al menos un sustituyente seleccionado a partir del grupo de Het3, A, Hal, OY, COOY, -Alq-OY, -Alq-SO2, -Alq-Het1, -OAlq-Het1, NYY, -CO-NYY, -SO2NYY, CN; Het1 indica un heteroarilo monocíclico con 2-7 átomos de C y 1-4 átomos de N, O y/o S, que puede estar sustituido por al menos un sustituyente seleccionado a partir del grupo de A, Hal, OY, COOY, -Alq- OY, -Alq-SO2, NYY, -CO-NYY, -SO2NYY, CN; Het2 indica un heteroarilo bicíclico con 2-9 átomos de C y 1-4 átomos de N, que puede estar sustituido por al menos un sustituyente seleccionado a partir del grupo de R2, A, Hal, OY, COOY, - Alq-OY, -Alq-SO2, NYY, -CO-NYY, -SO2NYY, CN; Het3 indica un heterociclo monocíclico saturado con 2-7 átomos de C y 1-4 átomos de N, O y/o S, que puede estar sustituido por al menos un sustituyente seleccionado a partir del grupo de A, Hal, OY, COOY, -Alq- OY, -Alq-SO2, NYY, -CO-NYY, -SO2NYY, CN; y Hal indica F, Cl, Br o I; y/o las sales fisiológicamente aceptables del mismo.
ES11700994.4T 2010-02-22 2011-01-10 Hetarilaminonaftiridinas Active ES2528441T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10001758 2010-02-22
EP10001758 2010-02-22
PCT/EP2011/000054 WO2011101069A2 (en) 2010-02-22 2011-01-10 Hetarylaminonaphthyridines

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ES2528441T3 true ES2528441T3 (es) 2015-02-10

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US (1) US8815893B2 (es)
EP (1) EP2539336B1 (es)
JP (1) JP6151919B2 (es)
KR (1) KR20130036201A (es)
CN (1) CN103097381B (es)
AU (1) AU2011217561B2 (es)
BR (1) BR112012019561A2 (es)
CA (1) CA2790613C (es)
EA (1) EA022064B1 (es)
ES (1) ES2528441T3 (es)
IL (1) IL221221A0 (es)
MX (1) MX2012009475A (es)
SG (1) SG183233A1 (es)
WO (1) WO2011101069A2 (es)
ZA (1) ZA201207133B (es)

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EA201201081A1 (ru) * 2010-02-05 2013-03-29 Мерк Патент Гмбх Производные гетарил[1,8]нафтиридина
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Publication number Publication date
EP2539336A2 (en) 2013-01-02
WO2011101069A2 (en) 2011-08-25
US20120316166A1 (en) 2012-12-13
CN103097381B (zh) 2015-10-07
EA022064B1 (ru) 2015-10-30
IL221221A0 (en) 2012-10-31
CA2790613C (en) 2018-01-02
ZA201207133B (en) 2013-05-29
KR20130036201A (ko) 2013-04-11
MX2012009475A (es) 2012-09-12
EP2539336B1 (en) 2014-10-22
SG183233A1 (en) 2012-09-27
CN103097381A (zh) 2013-05-08
AU2011217561A1 (en) 2012-10-11
BR112012019561A2 (pt) 2019-09-24
EA201201170A1 (ru) 2013-04-30
CA2790613A1 (en) 2011-08-25
US8815893B2 (en) 2014-08-26
AU2011217561B2 (en) 2016-04-21
JP2013520453A (ja) 2013-06-06
WO2011101069A3 (en) 2013-02-21
JP6151919B2 (ja) 2017-06-21

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