CN109748915B - 流感病毒复制抑制剂及其使用方法和用途 - Google Patents

流感病毒复制抑制剂及其使用方法和用途 Download PDF

Info

Publication number
CN109748915B
CN109748915B CN201910228694.7A CN201910228694A CN109748915B CN 109748915 B CN109748915 B CN 109748915B CN 201910228694 A CN201910228694 A CN 201910228694A CN 109748915 B CN109748915 B CN 109748915B
Authority
CN
China
Prior art keywords
atoms
compound
ring
amino
octane
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.)
Active
Application number
CN201910228694.7A
Other languages
English (en)
Chinese (zh)
Other versions
CN109748915A (zh
Inventor
张英俊
任青云
唐昌华
林小红
殷俊俊
易凯
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.)
Guangdong HEC Pharmaceutical Co Ltd
Original Assignee
Sunshine Lake Pharma Co 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
Application filed by Sunshine Lake Pharma Co Ltd filed Critical Sunshine Lake Pharma Co Ltd
Publication of CN109748915A publication Critical patent/CN109748915A/zh
Application granted granted Critical
Publication of CN109748915B publication Critical patent/CN109748915B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Virology (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201910228694.7A 2015-12-09 2016-12-08 流感病毒复制抑制剂及其使用方法和用途 Active CN109748915B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510908329 2015-12-09
CN2015109083292 2015-12-09
CN201611123253.3A CN106854205B (zh) 2015-12-09 2016-12-08 流感病毒复制抑制剂及其使用方法和用途

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201611123253.3A Division CN106854205B (zh) 2015-12-09 2016-12-08 流感病毒复制抑制剂及其使用方法和用途

Publications (2)

Publication Number Publication Date
CN109748915A CN109748915A (zh) 2019-05-14
CN109748915B true CN109748915B (zh) 2021-03-26

Family

ID=59012608

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201910228694.7A Active CN109748915B (zh) 2015-12-09 2016-12-08 流感病毒复制抑制剂及其使用方法和用途
CN201611123253.3A Active CN106854205B (zh) 2015-12-09 2016-12-08 流感病毒复制抑制剂及其使用方法和用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201611123253.3A Active CN106854205B (zh) 2015-12-09 2016-12-08 流感病毒复制抑制剂及其使用方法和用途

Country Status (9)

Country Link
US (2) US10717732B2 (https=)
EP (1) EP3362451B1 (https=)
JP (1) JP6952695B2 (https=)
KR (1) KR102671350B1 (https=)
CN (2) CN109748915B (https=)
AU (1) AU2016368317B2 (https=)
RU (1) RU2737190C2 (https=)
SG (1) SG11201804225PA (https=)
WO (1) WO2017097234A1 (https=)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109748915B (zh) * 2015-12-09 2021-03-26 广东东阳光药业有限公司 流感病毒复制抑制剂及其使用方法和用途
CN109071567B (zh) * 2016-05-19 2021-03-23 四川大学 抗流感小分子化合物及其制备方法和用途
CN107759571B (zh) 2016-08-16 2021-03-02 广东东阳光药业有限公司 流感病毒复制抑制剂及其使用方法和用途
CN109641868B (zh) 2016-08-30 2021-12-03 广东东阳光药业有限公司 流感病毒复制抑制剂及其使用方法和用途
SG11201901894TA (en) 2016-09-05 2019-04-29 Guangdong Raynovent Biotech Co Ltd Anti-influenza virus pyrimidine derivatives
US10987354B2 (en) 2016-12-15 2021-04-27 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
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
WO2018200425A1 (en) * 2017-04-24 2018-11-01 Cocrystal Pharma, Inc. Pyrrolopyrimidine derivatives useful as inhibitors of influenza virus replication
CN109384783A (zh) * 2017-08-09 2019-02-26 银杏树药业(苏州)有限公司 新型杂环化合物及其作为抗流感病毒抑制剂的医药用途
WO2019155468A1 (en) * 2018-02-08 2019-08-15 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use
JP7031002B2 (ja) * 2018-03-05 2022-03-07 広東衆生睿創生物科技有限公司 ピリジノイミダゾール系化合物の結晶型、塩型及びその製造方法
CN110590768B (zh) * 2018-06-13 2021-02-26 银杏树药业(苏州)有限公司 杂环化合物、其组合物及其作为抗流感病毒药物的应用
CN114340614B (zh) * 2019-09-27 2024-01-16 广东东阳光药业股份有限公司 一种奥司他韦制剂
CN110967239B (zh) * 2020-01-02 2022-05-10 国家地质实验测试中心 一种金属铬溶解氧化方法
CN117362318A (zh) * 2020-07-10 2024-01-09 西藏海思科制药有限公司 Pb2抑制剂及其制备方法和用途
US12274700B1 (en) 2020-10-30 2025-04-15 Accencio LLC Methods of treating symptoms of coronavirus infection with RNA polymerase inhibitors
US20250289826A1 (en) * 2022-04-29 2025-09-18 Tsinghua University Plpro protein inhibitor, and preparation method and application thereof
WO2026016541A1 (zh) * 2024-07-16 2026-01-22 武汉武药科技有限公司 一种新型抗病毒化合物及其用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010148197A1 (en) * 2009-06-17 2010-12-23 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
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
CN103562205A (zh) * 2010-12-16 2014-02-05 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
CN103702998A (zh) * 2011-07-05 2014-04-02 沃泰克斯药物股份有限公司 生产氮杂吲哚类的方法和中间体
WO2015073481A1 (en) * 2013-11-13 2015-05-21 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
CN106854205B (zh) * 2015-12-09 2019-07-09 广东东阳光药业有限公司 流感病毒复制抑制剂及其使用方法和用途

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI372624B (en) * 2004-03-30 2012-09-21 Vertex Pharma Azaindoles useful as inhibitors of jak and other protein kinases
CN103492382A (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
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
KR20160084465A (ko) 2013-11-13 2016-07-13 버텍스 파마슈티칼스 인코포레이티드 아자인돌 화합물의 제형
RS59144B1 (sr) * 2013-11-13 2019-09-30 Vertex Pharma Inhibitori replikacije virusa influence
UA124609C2 (uk) 2014-08-08 2021-10-20 Янссен Саєнсиз Айрленд Юсі Індоли для застосування при інфекції, спричиненій вірусом грипу
HUE053595T2 (hu) 2014-09-08 2021-07-28 Janssen Sciences Ireland Unlimited Co Pirrolopirimidinek influenzavírus-fertõzésnél történõ alkalmazásra
WO2017133664A1 (en) * 2016-02-05 2017-08-10 Savira Pharmaceuticals Gmbh Bicyclic pyridine and pyrimidine derivatives and their use in the treatment， amelioration or prevention of influenza

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010148197A1 (en) * 2009-06-17 2010-12-23 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
CN102458408A (zh) * 2009-06-17 2012-05-16 沃泰克斯药物股份有限公司 流感病毒复制抑制剂
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
CN103562205A (zh) * 2010-12-16 2014-02-05 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
CN103702998A (zh) * 2011-07-05 2014-04-02 沃泰克斯药物股份有限公司 生产氮杂吲哚类的方法和中间体
WO2015073481A1 (en) * 2013-11-13 2015-05-21 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
CN106854205B (zh) * 2015-12-09 2019-07-09 广东东阳光药业有限公司 流感病毒复制抑制剂及其使用方法和用途

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Discovery of a Novel, First-in-Class, Orally Bioavailable Azaindole Inhibitor (VX-787) of Influenza PB2;Michael P. Clark et al;《Journal of Medicinal Chemistry》;20140714;第57卷(第15期);第6668-6678页 *
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency;Michael J. Boyd et al;《Bioorganic & Medicinal Chemistry Letters》;20150314;第25卷(第9期);第1990-1994页 *

Also Published As

Publication number Publication date
JP2018536681A (ja) 2018-12-13
KR102671350B1 (ko) 2024-05-30
JP6952695B2 (ja) 2021-10-20
RU2737190C2 (ru) 2020-11-25
US11225477B2 (en) 2022-01-18
US10717732B2 (en) 2020-07-21
RU2018124993A3 (https=) 2020-02-05
KR20180088466A (ko) 2018-08-03
US20180346463A1 (en) 2018-12-06
AU2016368317A1 (en) 2018-06-07
CA3005921A1 (en) 2017-06-15
CN109748915A (zh) 2019-05-14
CN106854205A (zh) 2017-06-16
EP3362451A1 (en) 2018-08-22
AU2016368317B2 (en) 2019-05-23
WO2017097234A1 (en) 2017-06-15
SG11201804225PA (en) 2018-06-28
RU2018124993A (ru) 2020-01-14
EP3362451A4 (en) 2019-07-03
HK1254668A1 (en) 2019-07-26
EP3362451B1 (en) 2023-04-12
CN106854205B (zh) 2019-07-09
US20200299294A1 (en) 2020-09-24

Similar Documents

Publication Publication Date Title
CN109748915B (zh) 流感病毒复制抑制剂及其使用方法和用途
CN109641868B (zh) 流感病毒复制抑制剂及其使用方法和用途
CN107759571B (zh) 流感病毒复制抑制剂及其使用方法和用途
TWI785116B (zh) 流感病毒複製抑制劑及其用途
CN108218873B (zh) 流感病毒复制抑制剂及其用途
CN108276401B (zh) 流感病毒复制抑制剂及其用途
CN110446711B (zh) 流感病毒复制抑制剂及其用途
CN110117285B (zh) 流感病毒复制抑制剂及其用途
HK40011746A (en) Inhibitors of influenza virus replication and uses thereof
HK40011746B (en) Inhibitors of influenza virus replication and uses thereof
HK40002434A (en) Inhibitors of influenza virus replication, application methods and uses thereof
HK1245776B (zh) 流感病毒复制抑制剂及其使用方法和用途
HK1252416B (zh) 流感病毒复制抑制剂及其用途
HK40002434B (zh) 流感病毒复制抑制剂及其使用方法和用途

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CP03 Change of name, title or address
CP03 Change of name, title or address

Address after: 523808 No.1, Gongye North Road, Songshanhu Park, Dongguan City, Guangdong Province

Patentee after: Guangdong Dongyangguang Pharmaceutical Co.,Ltd.

Address before: 523808 Songshan Lake Science and Technology Industrial Park, Dongguan City, Guangdong Province

Patentee before: SUNSHINE LAKE PHARMA Co.,Ltd.