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 LTEPPCT/EP2016/078778T priority Critical patent/LT3380467T/lt
Priority to ES16801246T priority patent/ES2882671T3/es
Priority to AU2016359907A priority patent/AU2016359907B2/en
Priority to SI201631276T priority patent/SI3380467T1/sl
Priority to CN201680068994.8A priority patent/CN108290869B/zh
Priority to CA3005514A priority patent/CA3005514A1/en
Priority to HRP20211223TT priority patent/HRP20211223T1/hr
Priority to KR1020187016921A priority patent/KR20180087290A/ko
Priority to US15/779,468 priority patent/US10626108B2/en
Priority to EA201891278A priority patent/EA201891278A1/ru
Priority to JP2018527221A priority patent/JP6903658B2/ja
Priority to EP16801246.6A priority patent/EP3380467B1/en
Priority to DK16801246.6T priority patent/DK3380467T3/da
Publication of WO2017089518A1 publication Critical patent/WO2017089518A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/53Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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
LTEPPCT/EP2016/078778T LT3380467T (lt) 2015-11-27 2016-11-25 Heterocikliniai indolai, skirti naudoti gripo viruso infekcijų atveju
ES16801246T ES2882671T3 (es) 2015-11-27 2016-11-25 Indoles heterocíclicos para su uso en infecciones por el virus de la gripe
AU2016359907A AU2016359907B2 (en) 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection
SI201631276T SI3380467T1 (sl) 2015-11-27 2016-11-25 Heterociklični indoli za uporabo v okužbi z virusom gripe
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
CA3005514A CA3005514A1 (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
KR1020187016921A KR20180087290A (ko) 2015-11-27 2016-11-25 인플루엔자 바이러스 감염에서 사용하기 위한 복소환식 인돌
US15/779,468 US10626108B2 (en) 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection
EA201891278A EA201891278A1 (ru) 2015-11-27 2016-11-25 Гетероциклические индолы для применения при инфекции, вызванной вирусом гриппа
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
EP16801246.6A EP3380467B1 (en) 2015-11-27 2016-11-25 Heterocyclic indoles for use in influenza virus infection
DK16801246.6T DK3380467T3 (da) 2015-11-27 2016-11-25 Heterocykliske indoler til anvendelse ved influenzavirusinfektion

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15196811.2 2015-11-27
EP15196811 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 (enExample)
EP (1) EP3380467B1 (enExample)
JP (1) JP6903658B2 (enExample)
KR (1) KR20180087290A (enExample)
CN (1) CN108290869B (enExample)
AU (1) AU2016359907B2 (enExample)
CA (1) CA3005514A1 (enExample)
DK (1) DK3380467T3 (enExample)
EA (1) EA201891278A1 (enExample)
ES (1) ES2882671T3 (enExample)
HR (1) HRP20211223T1 (enExample)
HU (1) HUE055200T2 (enExample)
LT (1) LT3380467T (enExample)
MA (1) MA43298A (enExample)
SI (1) SI3380467T1 (enExample)
WO (1) WO2017089518A1 (enExample)

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
DK3405466T3 (da) 2016-01-20 2021-02-01 Janssen Sciences Ireland Unlimited Co Arylsubstituerede pyrimidiner til anvendelse ved influenzavirusinfektion
WO2018041091A1 (en) 2016-08-30 2018-03-08 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
EP3555095B1 (en) 2016-12-15 2023-04-12 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
CA3047404A1 (en) * 2016-12-23 2018-06-28 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012083122A1 (en) * 2010-12-16 2012-06-21 Vertex Pharmaceutical Incorporated Inhibitors of influenza viruses replication

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EP2532667A1 (en) 2005-09-30 2012-12-12 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
EP2040546A4 (en) * 2006-06-22 2009-12-23 Merck & Co Inc tyrosine kinase inhibitor
BRPI0807087A2 (pt) 2007-02-08 2014-06-10 Tibotec Pharm Ltd Inibidores de hcv macrocíclicos substituídos de pirimidina
GEAP202213376A (en) 2009-06-17 2022-02-25 Vertex Pharmaceuticals Incorporated Us Inhibitors of influenza viruses replication
WO2012032065A1 (en) 2010-09-08 2012-03-15 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
CN103492381A (zh) 2010-12-16 2014-01-01 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
KR101946499B1 (ko) 2011-04-08 2019-02-11 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염 치료를 위한 피리미딘 유도체
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
EP2858984A1 (en) 2012-06-08 2015-04-15 Vertex Pharmaceuticals Inc. Inhibitors of influenza viruses replication
LT2909195T (lt) 2012-10-16 2017-09-25 Janssen Sciences Ireland Uc Antivirusiniai rsv junginiai
KR102225233B1 (ko) 2013-02-21 2021-03-09 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염의 치료를 위한 2-아미노피리미딘 유도체
DK3405466T3 (da) 2016-01-20 2021-02-01 Janssen Sciences Ireland Unlimited Co Arylsubstituerede pyrimidiner til anvendelse ved influenzavirusinfektion

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

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