AR082727A1 - Derivados de furopiridina, procesos de preparacion y composiciones farmaceuticas que los contienen - Google Patents

Derivados de furopiridina, procesos de preparacion y composiciones farmaceuticas que los contienen

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Publication number
AR082727A1
AR082727A1 ARP110103112A AR082727A1 AR 082727 A1 AR082727 A1 AR 082727A1 AR P110103112 A ARP110103112 A AR P110103112A AR 082727 A1 AR082727 A1 AR 082727A1
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Argentina
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mono
nhet3
conh
hal
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Burgdorf Lars Dr
Schultz Melanie Dra
Hofmann Tatjana Dra
Brian Hodous
Justin Potnick
Amanda E Sutton
Bayard R Huck
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Merck Patent Gmbh
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Publication of AR082727A1 publication Critical patent/AR082727A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4355Heterocyclic 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 five-membered ring having oxygen as a ring hetero atom
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/535Heterocyclic 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
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/02Nasal agents, e.g. decongestants
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
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    • A61P37/02Immunomodulators
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Immunology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Son inhibidores de Syk y se pueden emplear, entre otros, para el tratamiento de artritis reumatoidea y/o lupus sistémico.Reivindicación 1: Compuestos de la fórmula (1) en donde R1 denota Ar1 o Het1; R2 denota Ar2, Het2, NH(CH2)nAr2, O(CH2)nAr2 o NH(CH2)nHet2; Ar1 denota fenilo, naftilo o bifenilo, cada uno de los cuales no está sustituido o está mono-, di- o trisustituido con Hal, A, O(CH2)pCyc, Alk, (CH2)nOH, (CH2)nOA, (CH2)nCOOH, (CH2)nCOOA, S(O)mA, fenoxi, benciloxi, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, [C(R3)2]nCN, NO2, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, SO2NH2, SO2NHA, SO2NA2, NHCONH2, (CH2)nNHCOA, (CH2)nNHCOAlk, NHCOCH=CH(CH2)pNA2, CHO, COA, SO3H, O(CH2)pNH2, O(CH2)pNHCOOA, O(CH2)pNHA, O(CH2)pNA2, NH(CH2)pNH2, NH(CH2)pNHCOOA, NH(CH2)pNHA, NH(CH2)pNA2, NHCOHet3, COHet3, (CH2)nHet3, O(CH2)nHet3 y/u O(CH2)nCH(OH)(CH2); Ar2 denota fenilo, naftilo o bifenilo, cada uno de los cuales no está sustituido o está mono-, di- o trisustituido con Hal, A, (CH2)nOH, (CH2)nOA, O(CH2)pCyc, OAr3, benciloxi, (CH2)nCOOH, (CH2)nCOOA, S(O)mA, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, [C(R3)2]nCN, NO2, CONH(CH2)pNH2, CONH(CH2)pNHA, CONH(CH2)pNA2, CONH(CH2)pOA, CONH(CH2)pOH, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, SO2NH2, SO2NHA, SO2NA2, NHCONH2, (CH2)nNHCOA, (CH2)nNHCOAlk, CHO, COA, SO3H, O(CH2)pNH2, O(CH2)pNHA, O(CH2)pNA2, CONHAr3, NHCOAr3, CONH(CH2)nHet3, NHCOHet3, COHet3, (CH2)nHet3, S(CH2)nHet3 y/u O(CH2)nHet3; Het1 denota un heterociclo aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono- o disustituido con A, bencilo, Het4, OH y/u OA; Het2 denota un heterociclo saturado, insaturado o aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di-, tri- o tetrasustituido con Hal, A, (CH2)nHet4, OHet4, NH(CH2)nHet4, (CH2)nCOOH, (CH2)nCOOA, fenilo, bencilo, CHO, COA, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, CN, (CH2)nOH, (CH2)nOA, (CH2)pCH(OH)(CH2)pOH, (CH2)pCH(OH)(CH2)pOA, NH(CH2)pNH2, NHSO2A, NASO2A, SO2A y/u =O; Het3 denota un heterociclo saturado, insaturado o aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di-, tri- o tetrasustituido con A, Hal, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, (CH2)nOH, (CH2)nOA, COOA, Ar3 y/u =O; Het4 denota un heterociclo saturado, insaturado o aromático monocíclico que tiene 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con A; R3 denota H o alquilo C1-4; A denota alquilo C1-10 no ramificado o ramificado, en donde 1 - 7 átomos de H pueden estar reemplazados por F y/o Cl y/o en donde uno o dos grupos no adyacentes CH2 pueden estar reemplazados por O, NH, S, SO, SO2 y/o por grupos CH=CH, o alquilo cíclico C3-7, que puede no estar sustituido o que puede estar sustituido con OH, NHCOOA o NH2; Cyc denota alquilo cíclico C3-7; Alk denota alquenilo o alquinilo C2-6; Ar3 denota fenilo, que no está sustituido o está mono-, di- o trisustituido con Hal y/o A; Hal denota F, Cl, Br o I; m denota 0, 1 ó 2; n denota 0, 1, 2, 3 ó 4; p denota 1, 2, 3 ó 4; y sus solvatos, sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP110103112 2010-08-27 2011-08-26 Derivados de furopiridina, procesos de preparacion y composiciones farmaceuticas que los contienen AR082727A1 (es)

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US (1) US9006440B2 (es)
EP (1) EP2609100B1 (es)
JP (1) JP5789300B2 (es)
KR (1) KR20130108318A (es)
CN (1) CN103052640B (es)
AR (1) AR082727A1 (es)
AU (1) AU2011295441B2 (es)
BR (1) BR112013004624A2 (es)
CA (1) CA2809333C (es)
EA (1) EA201300283A1 (es)
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CA2985859A1 (en) * 2015-06-29 2017-01-05 Merck Patent Gmbh Tbk/ikk.epsilon. inhibitor compounds and uses thereof
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JP5789300B2 (ja) 2015-10-07
US20130225569A1 (en) 2013-08-29
SG187956A1 (en) 2013-03-28
MX2013002199A (es) 2013-03-18
EP2609100A2 (en) 2013-07-03
EA201300283A1 (ru) 2013-08-30
WO2012025187A2 (en) 2012-03-01
KR20130108318A (ko) 2013-10-02
IL224870A (en) 2016-05-31
BR112013004624A2 (pt) 2016-07-05
US9006440B2 (en) 2015-04-14
EP2609100B1 (en) 2015-06-24
CN103052640A (zh) 2013-04-17
JP2013536208A (ja) 2013-09-19
WO2012025187A3 (en) 2012-06-21
AU2011295441A1 (en) 2013-04-11
CA2809333C (en) 2018-09-25
AU2011295441B2 (en) 2015-04-09
CA2809333A1 (en) 2012-03-01
CN103052640B (zh) 2017-06-30

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