WO2017089518A1 - Heterocyclic indoles for use in influenza virus infection - Google Patents

Heterocyclic indoles for use in influenza virus infection Download PDF

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Publication number
WO2017089518A1
WO2017089518A1 PCT/EP2016/078778 EP2016078778W WO2017089518A1 WO 2017089518 A1 WO2017089518 A1 WO 2017089518A1 EP 2016078778 W EP2016078778 W EP 2016078778W WO 2017089518 A1 WO2017089518 A1 WO 2017089518A1
Authority
WO
WIPO (PCT)
Prior art keywords
mmol
influenza
mixture
compound
reduced pressure
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP2016/078778
Other languages
English (en)
French (fr)
Inventor
Tim Hugo Maria Jonckers
David Craig Mc Gowan
Jérôme Émile Georges GUILLEMONT
Ludwig Paul Cooymans
Werner Constant Johan Embrechts
Christophe Francis Robert Nestor Buyck
Wendy Mia Albert Balemans
Pierre Jean-Marie Bernard Raboisson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Sciences Ireland ULC
Original Assignee
Janssen Sciences Ireland ULC
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
Application filed by Janssen Sciences Ireland ULC filed Critical Janssen Sciences Ireland ULC
Priority to DK16801246.6T priority Critical patent/DK3380467T3/da
Priority to AU2016359907A priority patent/AU2016359907B2/en
Priority to HRP20211223TT priority patent/HRP20211223T1/hr
Priority to ES16801246T priority patent/ES2882671T3/es
Priority to EA201891278A priority patent/EA201891278A1/ru
Priority to KR1020187016921A priority patent/KR20180087290A/ko
Priority to CN201680068994.8A priority patent/CN108290869B/zh
Priority to LTEPPCT/EP2016/078778T priority patent/LT3380467T/lt
Priority to SI201631276T priority patent/SI3380467T1/sl
Priority to US15/779,468 priority patent/US10626108B2/en
Priority to EP16801246.6A priority patent/EP3380467B1/en
Priority to JP2018527221A priority patent/JP6903658B2/ja
Priority to CA3005514A priority patent/CA3005514A1/en
Publication of WO2017089518A1 publication Critical patent/WO2017089518A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Definitions

  • X is N and Y is N;
  • the carrier optionally comprises a penetration enhancing agent and/or a suitable wetting agent, optionally combined with suitable additives of any nature in minor proportions, which additives do not introduce a significant deleterious effect on the skin. Said additives may facilitate the administration to the skin and/or may be helpful for preparing the desired compositions.
  • These compositions may be administered in various ways, e.g., as a transdermal patch, as a spot-on, as an ointment.
  • the compounds of the present invention may also be administered via inhalation or insufflation by means of methods and formulations employed in the art for administration via this way.
  • the compounds of the present invention may be administered to the lungs in the form of a solution, a suspension or a dry powder.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
PCT/EP2016/078778 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection Ceased WO2017089518A1 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
DK16801246.6T DK3380467T3 (da) 2015-11-27 2016-11-25 Heterocykliske indoler til anvendelse ved influenzavirusinfektion
AU2016359907A AU2016359907B2 (en) 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection
HRP20211223TT HRP20211223T1 (hr) 2015-11-27 2016-11-25 Heterociklički indoli za upotrebu kod infekcije virusom influence
ES16801246T ES2882671T3 (es) 2015-11-27 2016-11-25 Indoles heterocíclicos para su uso en infecciones por el virus de la gripe
EA201891278A EA201891278A1 (ru) 2015-11-27 2016-11-25 Гетероциклические индолы для применения при инфекции, вызванной вирусом гриппа
KR1020187016921A KR20180087290A (ko) 2015-11-27 2016-11-25 인플루엔자 바이러스 감염에서 사용하기 위한 복소환식 인돌
CN201680068994.8A CN108290869B (zh) 2015-11-27 2016-11-25 用于在流感病毒感染中使用的杂环吲哚
LTEPPCT/EP2016/078778T LT3380467T (lt) 2015-11-27 2016-11-25 Heterocikliniai indolai, skirti naudoti gripo viruso infekcijų atveju
SI201631276T SI3380467T1 (sl) 2015-11-27 2016-11-25 Heterociklični indoli za uporabo v okužbi z virusom gripe
US15/779,468 US10626108B2 (en) 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection
EP16801246.6A EP3380467B1 (en) 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection
JP2018527221A JP6903658B2 (ja) 2015-11-27 2016-11-25 インフルエンザウィルス感染に使用するための複素環インドール
CA3005514A CA3005514A1 (en) 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15196811 2015-11-27
EP15196811.2 2015-11-27

Publications (1)

Publication Number Publication Date
WO2017089518A1 true WO2017089518A1 (en) 2017-06-01

Family

ID=54707665

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2016/078778 Ceased WO2017089518A1 (en) 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection

Country Status (16)

Country Link
US (1) US10626108B2 (cg-RX-API-DMAC10.html)
EP (1) EP3380467B1 (cg-RX-API-DMAC10.html)
JP (1) JP6903658B2 (cg-RX-API-DMAC10.html)
KR (1) KR20180087290A (cg-RX-API-DMAC10.html)
CN (1) CN108290869B (cg-RX-API-DMAC10.html)
AU (1) AU2016359907B2 (cg-RX-API-DMAC10.html)
CA (1) CA3005514A1 (cg-RX-API-DMAC10.html)
DK (1) DK3380467T3 (cg-RX-API-DMAC10.html)
EA (1) EA201891278A1 (cg-RX-API-DMAC10.html)
ES (1) ES2882671T3 (cg-RX-API-DMAC10.html)
HR (1) HRP20211223T1 (cg-RX-API-DMAC10.html)
HU (1) HUE055200T2 (cg-RX-API-DMAC10.html)
LT (1) LT3380467T (cg-RX-API-DMAC10.html)
MA (1) MA43298A (cg-RX-API-DMAC10.html)
SI (1) SI3380467T1 (cg-RX-API-DMAC10.html)
WO (1) WO2017089518A1 (cg-RX-API-DMAC10.html)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018033082A1 (en) * 2016-08-16 2018-02-22 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
US10273233B2 (en) 2015-05-13 2019-04-30 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
US10533004B2 (en) 2015-05-13 2020-01-14 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
US10875855B2 (en) 2011-08-01 2020-12-29 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
US10874673B2 (en) 2009-06-17 2020-12-29 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112018014794A2 (pt) * 2016-01-20 2018-12-11 Janssen Sciences Ireland Uc pirimidinas substituídas com arila para uso em infecção pelo vírus influenza
US10647693B2 (en) 2016-08-30 2020-05-12 North & South Brother Pharmacy Investment Company Limited Inhibitors of influenza virus replication, application methods and uses thereof
CA3045371C (en) 2016-12-15 2024-05-14 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
EP4306166A3 (en) * 2016-12-23 2024-06-26 Aquinnah Pharmaceuticals Inc. Compounds, compositions and methods of use
WO2018127096A1 (en) 2017-01-05 2018-07-12 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
US10927118B2 (en) 2017-03-02 2021-02-23 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof

Citations (1)

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WO2012083122A1 (en) * 2010-12-16 2012-06-21 Vertex Pharmaceutical Incorporated Inhibitors of influenza viruses replication

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CN101801971A (zh) 2005-09-30 2010-08-11 沃泰克斯药物股份有限公司 可用作janus激酶抑制剂的脱氮嘌呤
EP2040546A4 (en) * 2006-06-22 2009-12-23 Merck & Co Inc tyrosine kinase inhibitor
RU2481340C2 (ru) 2007-02-08 2013-05-10 Тиботек Фармасьютикалз Лтд. Пиримидин-замещенные макроциклические ингибиторы hcv
GEP20207129B (en) 2009-06-17 2020-07-10 Vertex Pharma Inhibitors of influenza viruses replication
EP2613781B1 (en) 2010-09-08 2016-08-24 GlaxoSmithKline Intellectual Property Development Limited Indazole derivatives for use in the treatment of influenza virus infection
RU2013132681A (ru) 2010-12-16 2015-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
ES2691745T3 (es) 2011-04-08 2018-11-28 Janssen Sciences Ireland Uc Derivados de pirimidina para el tratamiento de infecciones víricas
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
WO2013184985A1 (en) 2012-06-08 2013-12-12 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
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KR102300861B1 (ko) 2013-02-21 2021-09-10 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염의 치료를 위한 2-아미노피리미딘 유도체
BR112018014794A2 (pt) 2016-01-20 2018-12-11 Janssen Sciences Ireland Uc pirimidinas substituídas com arila para uso em infecção pelo vírus influenza

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WO2012083122A1 (en) * 2010-12-16 2012-06-21 Vertex Pharmaceutical Incorporated Inhibitors of influenza viruses replication

Non-Patent Citations (1)

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MICHAEL P. CLARK ET AL: "Discovery of a Novel, First-in-Class, Orally Bioavailable Azaindole Inhibitor (VX-787) of Influenza PB2", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, no. 15, 14 July 2014 (2014-07-14), US, pages 6668 - 6678, XP055155585, ISSN: 0022-2623, DOI: 10.1021/jm5007275 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10874673B2 (en) 2009-06-17 2020-12-29 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
US10875855B2 (en) 2011-08-01 2020-12-29 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
US10273233B2 (en) 2015-05-13 2019-04-30 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
US10533004B2 (en) 2015-05-13 2020-01-14 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
WO2018033082A1 (en) * 2016-08-16 2018-02-22 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof

Also Published As

Publication number Publication date
ES2882671T3 (es) 2021-12-02
CN108290869A (zh) 2018-07-17
JP2019501879A (ja) 2019-01-24
HRP20211223T1 (hr) 2021-11-12
EP3380467A1 (en) 2018-10-03
US10626108B2 (en) 2020-04-21
CN108290869B (zh) 2021-05-18
CA3005514A1 (en) 2017-06-01
DK3380467T3 (da) 2021-09-27
AU2016359907A1 (en) 2018-05-24
US20180258074A1 (en) 2018-09-13
KR20180087290A (ko) 2018-08-01
LT3380467T (lt) 2021-08-10
EA201891278A1 (ru) 2018-11-30
SI3380467T1 (sl) 2021-08-31
MA43298A (fr) 2021-04-14
EP3380467B1 (en) 2021-07-07
JP6903658B2 (ja) 2021-07-14
AU2016359907B2 (en) 2021-04-01
HUE055200T2 (hu) 2021-11-29

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