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

Info

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
Family has litigation
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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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; 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
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • 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
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (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)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR046959A1 (es) * 2003-12-18 2006-01-04 Tibotec Pharm Ltd Morfolinilo que contiene bencimidazoles como inhibidores de la replicacion del virus sincitial respiratorio
TWI370820B (en) 2005-04-27 2012-08-21 Takeda Pharmaceutical Fused heterocyclic compounds
MX2007016537A (es) * 2005-06-20 2008-03-06 Tibotec Pharm Ltd 1,3-dihidro-benzoimidazol-onas 1-(2-amino-3-(alquilo sustituido)-3h-bencimidazolilmetil)-3-sustituidas con actividad sobre virus respiratorios sinciciales.
WO2006136562A1 (en) * 2005-06-20 2006-12-28 Tibotec Pharmaceuticals Ltd Heterocyclylaminoalkyl substituted benzimidazoles
US20120148678A1 (en) 2010-12-08 2012-06-14 Advanced Technologies And Regenerative Medicine, Llc. Sustained release of poorly water soluble active compounds
MY167575A (en) 2011-10-14 2018-09-20 Ambit Biosciences Corp Heterocyclic compounds and use thereof as modulators of type iii receptor tyrosine kinases
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
WO2017196982A1 (en) * 2016-05-10 2017-11-16 Georgia State University Research Foundation, Inc. Bicyclic fused pyrazole derivatives for the treatment of rsv
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
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
EP3680241A1 (en) 2017-03-20 2020-07-15 Forma Therapeutics, Inc. Pyrrolopyrrole compositions as pyruvate kinase (pkr) activators
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
CA3095277A1 (en) 2018-04-23 2019-10-31 Janssen Sciences Ireland Unlimited Company Heteroaromatic compounds having activity against rsv
WO2020061255A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
US10675274B2 (en) 2018-09-19 2020-06-09 Forma Therapeutics, Inc. Activating pyruvate kinase R
GB201820751D0 (en) * 2018-12-19 2019-01-30 Bp Oil Int Methods for preparing intermediates
PE20220937A1 (es) 2019-07-22 2022-05-31 Lupin Ltd Compuestos macrociclicos como agonistas de sting y metodos y usos de los mismos
HUE072832T2 (hu) 2019-09-19 2025-12-28 Novo Nordisk Healthcare Ag Piruvát kináz R-t (PKR) aktiváló készítmények
US12544371B2 (en) 2020-03-20 2026-02-10 Calcimedica, Inc. Methods and compositions for treating acute lung injury and acute respiratory distress syndrome
US12522589B2 (en) 2020-11-13 2026-01-13 Calcimedica, Inc. Synthesis of CRAC channel inhibitors
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
US20240352013A1 (en) * 2021-08-13 2024-10-24 Georgia State University Research Foundation, Inc. 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

Family Cites Families (5)

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Publication number Priority date Publication date Assignee Title
ATE258928T1 (de) * 1999-06-28 2004-02-15 Janssen Pharmaceutica Nv Respiratorisches syncytialvirus replikation inhibitoren
EP1418175A1 (en) * 1999-06-28 2004-05-12 Janssen Pharmaceutica N.V. Respiratory syncytial virus replication inhibitors
EP1400519B1 (en) * 1999-06-28 2007-03-07 Janssen Pharmaceutica N.V. Respiratory syncytial virus replication inhibitors
AR046959A1 (es) * 2003-12-18 2006-01-04 Tibotec Pharm Ltd Morfolinilo que contiene bencimidazoles como inhibidores de la replicacion del virus sincitial respiratorio
TWI356055B (en) * 2003-12-18 2012-01-11 Tibotec Pharm Ltd Aminobenzimidazoles and benzimidazoles as inhibito

Also Published As

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

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Legal Events

Date Code Title Description
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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