BR112014032581A2 - inibidores de bifluorodioxalano-amino-benzimidazol qui-nase para o tratamento de câncer, distúrbios do snc e inflamação autoimune - Google Patents

inibidores de bifluorodioxalano-amino-benzimidazol qui-nase para o tratamento de câncer, distúrbios do snc e inflamação autoimune

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Publication number
BR112014032581A2
BR112014032581A2 BR112014032581A BR112014032581A BR112014032581A2 BR 112014032581 A2 BR112014032581 A2 BR 112014032581A2 BR 112014032581 A BR112014032581 A BR 112014032581A BR 112014032581 A BR112014032581 A BR 112014032581A BR 112014032581 A2 BR112014032581 A2 BR 112014032581A2
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Brazil
Prior art keywords
alkyl
con
heterocyclyl
further described
treatment
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BR112014032581A
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English (en)
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BR112014032581A8 (pt
Inventor
Leban Johann
Zaja Mirko
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4Sc Discovery Gmbh
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Publication date
Application filed by 4Sc Discovery Gmbh filed Critical 4Sc Discovery Gmbh
Publication of BR112014032581A2 publication Critical patent/BR112014032581A2/pt
Publication of BR112014032581A8 publication Critical patent/BR112014032581A8/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

abstract the invention relates to a compound of the general formula (i) or a physiologically functional derivative, solvate or salt thereof, wherein a is a bond, alkyl or alkoxy optionally substituted with one or more r'' as defined herein, *-n(r''')co-, *-con(r''')-, *-n(r''')con(r''')-, -s-, -so-, *-n(r''')-, *-n(r''')co-, *-con(r''')-, -co-, *-coo-, *-ooc-, *-so2n(r''')-, -so2, or *-n(r''')-so2-, wherein r''' is as defined herein and * specifies the point of attachment to x; x is aryl, cycloalkyl, aralkyl, heterocyclyl or heteroaryl, which may be substituted with one or more rx further described herein; l is a bond or *-n(rn)co-, *-con(rn)-, *-n(rn)-, *-c=n(rn)-, *-n(rn)-alkyl-, *-alkyl-n(rn)-, *-n(rn)con(rn)-, *-co-, *-so2-, alkyl, *-alkyl-o-alkyl-, *-nco-ch=ch-, *-ch=ch-conh-, * -so2n(rn)-, *-n(rn)so2-, or heterocyclyl, wherein * specifies the point of attachment to x; y is h, alkyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heteroaryl, which may be substituted with one or more ry further described herein; and r and rn are further described herein; as well as their use as a medicament, a pharmaceutical composition comprising them, a method of treatment or prevention of a medical condition entailing the administration thereof, and the use thereof in the manufacture of a medicament for the treatment or prevention of a medical condition, particularly autoimmune inflammatory disorders, cns disorders, sleeping disorders, or proliferative diseases including cancer. the invention further relates to a specific process for the preparation of said compounds. ______________________________ tradução do resumo "inibidores de bifluorodioxalano-amino-benzimidazol qui-nase para o tratamento de câncer, distúrbios do snc e inflamação autoimune". a presente invenção refere-se a um composto da fórmula geral (i) ou um sal, solvato ou derivado fisiologicamente funcional do mesmo, (i) em que a é uma ligação, alquila ou alcóxi opcionalmente substituída com um ou mais r’’ conforme definido no presente documento, *-n(r’’’)co-, * con(r’’’)-, *-n(r’’’)con(r’’’)-, -s-, -so-, *-n(r’’’)-, *-n(r’’’)co-, * con(r’’’)-, -co-, *-coo-, *-ooc-, *-so2n(r’’’)-, -so2 ou *-n(r’’’)-so2-, em que r’’’ é conforme definido no presente documento e * especifica o ponto de ligação a x; x é arila, cicloalquila, aralquila, heterociclila ou heteroarila, que pode ser substituída com um ou mais rx adicionalmente descrito no presente documento; l é uma ligação ou *-n(rn)co-, *-con(rn)-, *-n(rn)-, *-c=n(rn)-, *-n(rn)-alquila-, *-alquila-n(rn)-, *-n(rn)con(rn)-, *-co-, * so2-, alquila, * alquila-o-alquila-, *-nco-ch=ch-, *-ch=ch-conh-, * so2n(rn)-, *-n(rn)so2- ou heterociclila, em que * especifica o ponto de ligação a x; y é h, alquila, arila, aralquila, cicloalquila, heterociclila ou heteroarila, que pode ser substituída com um ou mais ry adicionalmente descrito no presente documento; e r e rn são adicionalmente descritos no presente documento; bem como o uso dos mesmos como um medicamento, uma composição farmacêutica que compreende os mesmos, um método de tratamento ou prevenção de uma afecção médica que emprega a administração dos mesmos e o uso dos mesmos na fabricação de um medicamento para o tratamento ou prevenção de uma afecção médica, particularmente distúrbios inflamatórios autoimunes, distúrbios do snc, distúrbios do sono ou doenças proliferativas incluindo câncer. a invenção se refere, ainda, a um processo específico para a preparação dos ditos compostos.
BR112014032581A 2012-06-27 2013-06-27 inibidores de bifluorodioxalano-amino-benzimidazol quinase para o tratamento de câncer, distúrbios do snc e inflamação autoimune BR112014032581A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261664936P 2012-06-27 2012-06-27
EP12174669 2012-07-02
PCT/EP2013/063537 WO2014001464A1 (en) 2012-06-27 2013-06-27 Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and cns disorders

Publications (2)

Publication Number Publication Date
BR112014032581A2 true BR112014032581A2 (pt) 2017-06-27
BR112014032581A8 BR112014032581A8 (pt) 2018-08-14

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BR112014032581A BR112014032581A8 (pt) 2012-06-27 2013-06-27 inibidores de bifluorodioxalano-amino-benzimidazol quinase para o tratamento de câncer, distúrbios do snc e inflamação autoimune

Country Status (19)

Country Link
US (2) US9580438B2 (pt)
EP (1) EP2867237A1 (pt)
JP (2) JP6272846B2 (pt)
KR (1) KR102155559B1 (pt)
CN (1) CN104540831B (pt)
AU (2) AU2013283318B2 (pt)
BR (1) BR112014032581A8 (pt)
CA (1) CA2877589C (pt)
EA (1) EA029718B1 (pt)
HK (1) HK1204474A1 (pt)
IL (1) IL236463A0 (pt)
IN (1) IN2014MN02562A (pt)
MX (1) MX350418B (pt)
MY (1) MY167785A (pt)
NZ (1) NZ702618A (pt)
SG (1) SG11201408617PA (pt)
UA (1) UA116541C2 (pt)
WO (1) WO2014001464A1 (pt)
ZA (1) ZA201409194B (pt)

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Publication number Publication date
JP2015525742A (ja) 2015-09-07
SG11201408617PA (en) 2015-01-29
MX350418B (es) 2017-09-06
MY167785A (en) 2018-09-25
US9580438B2 (en) 2017-02-28
AU2018201275A1 (en) 2018-03-15
CA2877589C (en) 2019-11-26
EA201500050A1 (ru) 2015-09-30
HK1204474A1 (en) 2015-11-20
IL236463A0 (en) 2015-02-26
CA2877589A1 (en) 2014-01-03
EP2867237A1 (en) 2015-05-06
KR20150037877A (ko) 2015-04-08
AU2013283318A1 (en) 2015-01-22
MX2014015938A (es) 2015-07-21
NZ702618A (en) 2016-12-23
CN104540831A (zh) 2015-04-22
UA116541C2 (uk) 2018-04-10
CN104540831B (zh) 2017-11-07
WO2014001464A1 (en) 2014-01-03
AU2013283318B2 (en) 2017-11-23
ZA201409194B (en) 2017-08-30
US20150158878A1 (en) 2015-06-11
IN2014MN02562A (pt) 2015-07-24
BR112014032581A8 (pt) 2018-08-14
US20170240556A1 (en) 2017-08-24
KR102155559B1 (ko) 2020-09-15
JP2018076360A (ja) 2018-05-17
EA029718B1 (ru) 2018-05-31
JP6272846B2 (ja) 2018-01-31

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