BRPI0417268B8 - 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 - Google Patents

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

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Publication number
BRPI0417268B8
BRPI0417268B8 BRPI0417268A BRPI0417268A BRPI0417268B8 BR PI0417268 B8 BRPI0417268 B8 BR PI0417268B8 BR PI0417268 A BRPI0417268 A BR PI0417268A BR PI0417268 A BRPI0417268 A BR PI0417268A BR PI0417268 B8 BRPI0417268 B8 BR PI0417268B8
Authority
BR
Brazil
Prior art keywords
hydrogen
compounds
morpholinyl
substituted
respiratory syncytial
Prior art date
Application number
BRPI0417268A
Other languages
English (en)
Inventor
Meyer Christophe
Marc Maurice Doublet Frédéric
Bonfanti Jean-François
Michel Claude Fortin Jérôme
Jozef Lodewijk Andries Koenraad
Maria Martha Bern Timmerman Philip
Muller Philippe
Edmond Willebrords Rudy
Valerius Josepha Gevers Tom
Original Assignee
Janssen Sciences Ireland Uc
Janssen R&D Ireland
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(B8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Sciences Ireland Uc, Janssen R&D Ireland, Tibotec Pharm Ltd filed Critical Janssen Sciences Ireland Uc
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
    • 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
    • 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
    • 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

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

compostos de benzimidazóis que contêm morfolinila, como inibidores da replicação de vírus sinciciais respiratórios, suas composições farmacêuticas, usos e processo para preparação dos mesmos. 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 pró-droga, n-óxido, sal de adição, amina quaternária, complexo metálico e forma estereoquimicamente isomérica do mesmo, no qual g é uma ligação direta ou c1-10alcanodiila, opcionalmente substituída; r1 é ar1 ou um heterociclo monocíclico ou bicíclico q é r7, pirrolidinila, substituída com r7, piperidinila, substituída com r7 ou homopiperidinila, substituída com r7; um de r2a e r3a é escolhido de halo, c1-6alquila, opcionalmente mono- ou polissubstituída, c2-6alquenila, opcionalmente mono- ou polissubstituída, nitro, hidróxi, ar2, n(r4ar 4b), n(r4ar4b)sulfonila, n(r4ar4b)carbonila, c1-6alquilóxi, ar2óxi, ar2c1-6alquilóxi, carboxila, c1-6alquiloxicaronila, ou -c(=z)ar2; e o outros de r2a e r3a é hidrogênio no caso de r2a ser diferente de hidrogênio, então r2b é hidrogênio, c1-6alquila ou halogênio e r3b é hidrogênio; no caso de r3a ser diferente de hidrogênio, então r3b é hidrogênio, c1-6alquila ou halogênio e r2b é hidrogênio. a invenção refere-se, ainda, a preparação dos mesmo 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 BRPI0417268A (pt) 2007-03-13
BRPI0417268B1 BRPI0417268B1 (pt) 2018-10-23
BRPI0417268B8 true 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 (33)

Country Link
US (2) US7449463B2 (pt)
EP (1) EP1697345B1 (pt)
JP (1) JP4951348B2 (pt)
KR (1) KR100967406B1 (pt)
CN (2) CN1894237A (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)
HK (1) HK1130799A1 (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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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
AU2006260969B2 (en) * 2005-06-20 2011-11-17 Janssen Sciences Ireland Uc 1- ( 2-amino-3- (substituted alkyl)-3H-benzimidazolylmethyl) -3-substituted-1,3-dihydro-benzoimidazol-2-ones with activity on respiratory syncytial virus
CA2612264C (en) * 2005-06-20 2014-09-23 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
PT2766359T (pt) 2011-10-14 2016-07-14 Ambit Biosciences Corp Compostos heterocíclicos e utilização dos mesmos como moduladores de recetores tirosina-cinase de tipo iii
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
CN109562160B (zh) * 2016-05-10 2022-07-29 乔治亚州立大学研究基金会股份有限公司 用于治疗rsv的双环稠合的吡唑衍生物
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
RS60209B1 (sr) 2017-03-20 2020-06-30 Forma Therapeutics Inc Kompozicije pirolopirola kao aktivatori piruvat kinaze (pkr)
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
JP7305658B2 (ja) 2018-01-31 2023-07-10 ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー 抗rsv活性を有するシクロアルキル置換ピラゾロピリミジン
WO2019206828A1 (en) 2018-04-23 2019-10-31 Janssen Sciences Ireland Unlimited Company Heteroaromatic compounds having activity against rsv
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GB201820751D0 (en) * 2018-12-19 2019-01-30 Bp Oil Int Methods for preparing intermediates
BR112022001125A2 (pt) 2019-07-22 2022-03-15 Lupin Ltd Compostos macrocíclicos como agonistas de sting, seus métodos e seus usos
JP7329239B2 (ja) 2019-09-20 2023-08-18 株式会社タマディック フライトシミュレーター
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CZ20014574A3 (cs) * 1999-06-28 2002-05-15 Janssen Pharmaceutica N. V. Inhibitory replikace respiračně syncyciálního viru
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AR046971A1 (es) * 2003-12-18 2006-01-04 Tibotec Pharm Ltd Aminobenzoimidazoles y benzoimidazoles como inhibidores de la replicacion del virus sincitial respiratorio
AR046959A1 (es) * 2003-12-18 2006-01-04 Tibotec Pharm Ltd Morfolinilo que contiene bencimidazoles como inhibidores de la replicacion del virus sincitial respiratorio

Also Published As

Publication number Publication date
ATE388950T1 (de) 2008-03-15
US20080280881A1 (en) 2008-11-13
CN101412709A (zh) 2009-04-22
CA2548668C (en) 2011-09-20
KR100967406B1 (ko) 2010-07-01
IL175910A (en) 2013-08-29
BRPI0417268A (pt) 2007-03-13
EA200601178A1 (ru) 2006-10-27
JP2007514720A (ja) 2007-06-07
NO20063322L (no) 2006-09-18
AP2006003640A0 (en) 2006-06-30
RS50584B (sr) 2010-05-07
ME01042B (me) 2012-10-20
MXPA06007112A (es) 2006-08-23
MY143573A (en) 2011-05-31
US7449463B2 (en) 2008-11-11
NZ547479A (en) 2009-03-31
PT1697345E (pt) 2008-06-12
IL175910A0 (en) 2006-10-05
CA2548668A1 (en) 2005-06-30
EP1697345B1 (en) 2008-03-12
DK1697345T3 (da) 2008-06-23
EG25799A (en) 2012-08-06
HK1130799A1 (en) 2010-01-08
KR20070015507A (ko) 2007-02-05
TW200531972A (en) 2005-10-01
US8883837B2 (en) 2014-11-11
WO2005058871A1 (en) 2005-06-30
DE602004012448D1 (de) 2008-04-24
AR046959A1 (es) 2006-01-04
BRPI0417268B1 (pt) 2018-10-23
NO339314B1 (no) 2016-11-28
AU2004298460A1 (en) 2005-06-30
ES2303653T3 (es) 2008-08-16
US20070043022A1 (en) 2007-02-22
ZA200605894B (en) 2008-01-08
DE602004012448T2 (de) 2009-03-26
JP4951348B2 (ja) 2012-06-13
CY1108142T1 (el) 2014-02-12
AP2150A (en) 2010-09-04
AU2004298460B2 (en) 2009-03-19
EP1697345A1 (en) 2006-09-06
PL1697345T3 (pl) 2008-08-29
CN101412709B (zh) 2015-03-25
HRP20080245T3 (en) 2008-07-31
SI1697345T1 (sl) 2008-08-31
TWI351401B (en) 2011-11-01
EA009876B1 (ru) 2008-04-28
CN1894237A (zh) 2007-01-10
UA84718C2 (ru) 2008-11-25

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B25D Requested change of name of applicant approved

Owner name: TIBOTEC PHARMACEUTICALS (IE)

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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]
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