BRPI0417268A - benzimidazóis que contêm morfolinila, como inibidores da replicação de vìrus sinciciais respiratórios - Google Patents

benzimidazóis que contêm morfolinila, como inibidores da replicação de vìrus sinciciais respiratórios

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Publication number
BRPI0417268A
BRPI0417268A BRPI0417268-0A BRPI0417268A BRPI0417268A BR PI0417268 A BRPI0417268 A BR PI0417268A BR PI0417268 A BRPI0417268 A BR PI0417268A BR PI0417268 A BRPI0417268 A BR PI0417268A
Authority
BR
Brazil
Prior art keywords
hydrogen
respiratory syncytial
substituted
alkyloxy
morpholinyl
Prior art date
Application number
BRPI0417268-0A
Other languages
English (en)
Inventor
Jean-Francois Bonfanti
Koenraad Jozef Lodewij Andries
Jerome Michel Claude Fortin
Philippe Muller
Frederic Marc Maurice Doublet
Christophe Meyer
Rudy Edmond Willebrords
Tom Valerius Josepha Gevers
Philip Maria Martha Timmerman
Original Assignee
Tibotec Pharm Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34704695&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0417268(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of BRPI0417268A publication Critical patent/BRPI0417268A/pt
Publication of BRPI0417268B1 publication Critical patent/BRPI0417268B1/pt
Publication of BRPI0417268B8 publication Critical patent/BRPI0417268B8/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"BENZIMIDAZóIS QUE CONTêM MORFOLINILA, COMO INIBIDORES DA REPLICAçãO DE VìRUS SINCICIAIS RESPIRATóRIOS". A presente invenção refere-se a benzimidazóis contendo morfolinila, com atividade inibidora sobre a replicação do vírus sincicial respiratório e com a fórmula (1), uma prodroga, N-óxido, sal de adição, amina quatemária, complexo metálico e forma estereoquimicamente isomérica do mesmo, no qual G é uma ligação direta ou C~ 1-10~alcanodiila, opcionalmente substituída; R¬ 1¬ é Ar¬ 1¬ ou um heterociclo monocíclico ou bicíclico Q é R¬ 7¬, pirrolidinila, substituída com R¬ 7¬, piperidinila, substituída com R¬ 7¬ ou homopiperidinila, substituída com R¬ 7¬; um de R¬ 2a¬ e R¬ 3a¬ é escolhido de halo, C~ 1-6~ alquila, opcionalmente mono- ou polissubstituída, C~ 2-6~ alquenila, opcionalmente mono- ou polissubstituída, nitro, hidróxi, Ar¬ 2¬, N(R¬ 4a¬R¬ 4b¬), N(R¬ 4a¬R¬ 4b¬)sulfonila, N(R¬ 4a¬ R¬ 4b¬) arbonila, C~ 1-6~alquilóxi, Ar¬ 2¬C~ 1-6~alquilóxi, carboxila, C~ 1-6~alquióxi, caronila, ou -C(=Z)Ar¬ 2¬; no caso de R¬ 2a¬ ser diferente de hidrogênio, então R¬ 2b¬ é hidrogênio, C~ 1-6~alquila ou halogênio e R¬ 3b¬ é hidrogênio; o caso de R¬ 3a¬ diferente de hidrogênio, então R¬ 3b¬ é hidrogênio, C~ 1-6~alquila ou halogênio e R¬ 2b¬ é hidrogênio. A invenção refere-se, ainda, à preparação dos mesmos e a composições que compreendem esses compostos, bem como ao uso dos mesmos como medicamento.
BRPI0417268A 2003-12-18 2004-12-20 compostos benzimidazóis que contêm morfolinila, seu uso como inibidores da replicação de vírus sinciciais respiratórios, composição que os compreende e processo para preparar os referidos compostos BRPI0417268B8 (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP03104810 2003-12-18
US56718204P 2004-04-30 2004-04-30
EP04105312 2004-10-26
PCT/EP2004/053620 WO2005058871A1 (en) 2003-12-18 2004-12-20 Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication

Publications (3)

Publication Number Publication Date
BRPI0417268A true BRPI0417268A (pt) 2007-03-13
BRPI0417268B1 BRPI0417268B1 (pt) 2018-10-23
BRPI0417268B8 BRPI0417268B8 (pt) 2021-05-25

Family

ID=34704695

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0417268A BRPI0417268B8 (pt) 2003-12-18 2004-12-20 compostos benzimidazóis que contêm morfolinila, seu uso como inibidores da replicação de vírus sinciciais respiratórios, composição que os compreende e processo para preparar os referidos compostos

Country Status (32)

Country Link
US (2) US7449463B2 (pt)
EP (1) EP1697345B1 (pt)
JP (1) JP4951348B2 (pt)
KR (1) KR100967406B1 (pt)
CN (2) CN101412709B (pt)
AP (1) AP2150A (pt)
AR (1) AR046959A1 (pt)
AT (1) ATE388950T1 (pt)
AU (1) AU2004298460B2 (pt)
BR (1) BRPI0417268B8 (pt)
CA (1) CA2548668C (pt)
CY (1) CY1108142T1 (pt)
DE (1) DE602004012448T2 (pt)
DK (1) DK1697345T3 (pt)
EA (1) EA009876B1 (pt)
EG (1) EG25799A (pt)
ES (1) ES2303653T3 (pt)
HR (1) HRP20080245T3 (pt)
IL (1) IL175910A (pt)
ME (1) ME01042B (pt)
MX (1) MXPA06007112A (pt)
MY (1) MY143573A (pt)
NO (1) NO339314B1 (pt)
NZ (1) NZ547479A (pt)
PL (1) PL1697345T3 (pt)
PT (1) PT1697345E (pt)
RS (1) RS50584B (pt)
SI (1) SI1697345T1 (pt)
TW (1) TWI351401B (pt)
UA (1) UA84718C2 (pt)
WO (1) WO2005058871A1 (pt)
ZA (1) ZA200605894B (pt)

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TWI370820B (en) 2005-04-27 2012-08-21 Takeda Pharmaceutical Fused heterocyclic compounds
CA2612263C (en) * 2005-06-20 2015-04-14 Tibotec Pharmaceuticals Ltd. 1-(2-amino-3-(substituted alkyl)-3h-benzimidazolylmethyl)-3-subtituted-1,3-dihydro-benzoimidazol-2-ones with activity on respiratory syncytial virus
JP5094716B2 (ja) * 2005-06-20 2012-12-12 テイボテク・フアーマシユーチカルズ ヘテロシクリルアミノアルキル置換ベンズイミダゾール
US20120148678A1 (en) 2010-12-08 2012-06-14 Advanced Technologies And Regenerative Medicine, Llc. Sustained release of poorly water soluble active compounds
CA2851155C (en) 2011-10-14 2021-02-23 Ambit Biosciences Corporation Heterocyclic compounds and methods of use thereof
UA119050C2 (uk) * 2013-11-11 2019-04-25 Ґілеад Саєнсиз, Інк. ПІРОЛО[1.2-f][1.2.4]ТРИАЗИНИ, ЯКІ ВИКОРИСТОВУЮТЬСЯ ДЛЯ ЛІКУВАННЯ РЕСПІРАТОРНО-СИНЦИТІАЛЬНИХ ВІРУСНИХ ІНФЕКЦІЙ
JO3637B1 (ar) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc مركبات بيرازولو- وترايازولو- بيريميدين مضادة للفيروسات rsv
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TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
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TW201932470A (zh) 2017-11-29 2019-08-16 愛爾蘭商健生科學愛爾蘭無限公司 具有抗rsv活性之吡唑并嘧啶
AU2019216260B2 (en) 2018-01-31 2023-03-02 Janssen Sciences Ireland Unlimited Company Cycloalkyl substituted pyrazolopyrimidines having activity against RSV
ES2957316T3 (es) 2018-04-23 2024-01-17 Janssen Sciences Ireland Unlimited Co Compuestos heteroaromáticos que tienen actividad contra VSR
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
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GB201820751D0 (en) * 2018-12-19 2019-01-30 Bp Oil Int Methods for preparing intermediates
GEP20247627B (en) 2019-07-22 2024-05-27 Lupin Ltd Macrocyclic compounds as sting agonists and methods and uses thereof
CN114615977B (zh) 2019-09-19 2025-01-14 诺沃挪第克健康护理股份公司 丙酮酸激酶r(pkr)活化组合物
EP4121089A4 (en) 2020-03-20 2024-04-10 Calcimedica, Inc. METHODS AND COMPOSITIONS FOR THE TREATMENT OF ACUTE LUNG LESION AND ACUTE RESPIRATORY DISTRESS SYNDROME
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US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
EP4384168A4 (en) * 2021-08-13 2025-07-09 Univ Georgia State Res Found BICYCLIC FUSED PYRAZOLE DERIVATIVES FOR THE TREATMENT OF RESPIRATORY INFECTIONS INCLUDING RSV
CN119118850B (zh) * 2023-06-13 2025-12-12 中国科学院兰州化学物理研究所 一种吲哚类化合物结构重整制备胺基苯乙醇类化合物的方法

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CZ20014573A3 (cs) * 1999-06-28 2002-05-15 Janssen Pharmaceutica N. V. Inhibitory replikace respiračně syncyciálního viru
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AR046959A1 (es) * 2003-12-18 2006-01-04 Tibotec Pharm Ltd Morfolinilo que contiene bencimidazoles como inhibidores de la replicacion del virus sincitial respiratorio
ATE435222T1 (de) * 2003-12-18 2009-07-15 Tibotec Pharm Ltd Aminobenzimidazole und benzimidazole als inhibitoren der replikation von respiratory syncytial virus

Also Published As

Publication number Publication date
NZ547479A (en) 2009-03-31
US8883837B2 (en) 2014-11-11
PT1697345E (pt) 2008-06-12
ME01042B (me) 2012-10-20
JP4951348B2 (ja) 2012-06-13
NO339314B1 (no) 2016-11-28
MY143573A (en) 2011-05-31
US7449463B2 (en) 2008-11-11
ES2303653T3 (es) 2008-08-16
ATE388950T1 (de) 2008-03-15
NO20063322L (no) 2006-09-18
EP1697345B1 (en) 2008-03-12
AR046959A1 (es) 2006-01-04
KR20070015507A (ko) 2007-02-05
CY1108142T1 (el) 2014-02-12
SI1697345T1 (sl) 2008-08-31
CN101412709B (zh) 2015-03-25
IL175910A (en) 2013-08-29
AP2150A (en) 2010-09-04
AU2004298460B2 (en) 2009-03-19
CA2548668A1 (en) 2005-06-30
EA200601178A1 (ru) 2006-10-27
PL1697345T3 (pl) 2008-08-29
HK1130799A1 (en) 2010-01-08
IL175910A0 (en) 2006-10-05
RS50584B (sr) 2010-05-07
KR100967406B1 (ko) 2010-07-01
AU2004298460A1 (en) 2005-06-30
CA2548668C (en) 2011-09-20
WO2005058871A1 (en) 2005-06-30
DE602004012448T2 (de) 2009-03-26
ZA200605894B (en) 2008-01-08
HRP20080245T3 (hr) 2008-07-31
DE602004012448D1 (de) 2008-04-24
UA84718C2 (ru) 2008-11-25
BRPI0417268B8 (pt) 2021-05-25
MXPA06007112A (es) 2006-08-23
CN1894237A (zh) 2007-01-10
AP2006003640A0 (en) 2006-06-30
DK1697345T3 (da) 2008-06-23
EG25799A (en) 2012-08-06
TWI351401B (en) 2011-11-01
EA009876B1 (ru) 2008-04-28
CN101412709A (zh) 2009-04-22
TW200531972A (en) 2005-10-01
JP2007514720A (ja) 2007-06-07
US20070043022A1 (en) 2007-02-22
EP1697345A1 (en) 2006-09-06
BRPI0417268B1 (pt) 2018-10-23
US20080280881A1 (en) 2008-11-13

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B25D Requested change of name of applicant approved

Owner name: TIBOTEC PHARMACEUTICALS (IE)

B25D Requested change of name of applicant approved

Owner name: JANSSEN R AND D IRELAND (IE)

B25A Requested transfer of rights approved

Owner name: JANSSEN SCIENCES IRELAND UC (IE)

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

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