CN103764654B - 流感病毒复制抑制剂 - Google Patents

流感病毒复制抑制剂 Download PDF

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Publication number
CN103764654B
CN103764654B CN201280043260.6A CN201280043260A CN103764654B CN 103764654 B CN103764654 B CN 103764654B CN 201280043260 A CN201280043260 A CN 201280043260A CN 103764654 B CN103764654 B CN 103764654B
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CN
China
Prior art keywords
fluoro
compound
mmol
pyrrolo
pyridin
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.)
Expired - Fee Related
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CN201280043260.6A
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English (en)
Chinese (zh)
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CN103764654A (zh
Inventor
P·S·查理弗森
M·P·克拉克
U·K·班达拉格
R·S·贝希尔
M·J·博伊德
I·戴维斯
邓红波
J·P·杜菲
L·J·弗雷姆尔
高淮
顾文鑫
J·M·肯尼迪
B·莱德弗德
M·W·里德博尔
F·玛尔泰斯
E·佩罗拉
王天生
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46650922&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN103764654(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Priority to CN201510893703.6A priority Critical patent/CN105503862B/zh
Priority to CN201510893692.1A priority patent/CN105481853A/zh
Publication of CN103764654A publication Critical patent/CN103764654A/zh
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Publication of CN103764654B publication Critical patent/CN103764654B/zh
Expired - Fee Related legal-status Critical Current
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    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/506—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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
CN201280043260.6A 2011-08-01 2012-08-01 流感病毒复制抑制剂 Expired - Fee Related CN103764654B (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN201510893703.6A CN105503862B (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂
CN201510893692.1A CN105481853A (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161513793P 2011-08-01 2011-08-01
US61/513,793 2011-08-01
PCT/US2012/049097 WO2013019828A1 (en) 2011-08-01 2012-08-01 Inhibitors of influenza viruses replication

Related Child Applications (2)

Application Number Title Priority Date Filing Date
CN201510893692.1A Division CN105481853A (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂
CN201510893703.6A Division CN105503862B (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂

Publications (2)

Publication Number Publication Date
CN103764654A CN103764654A (zh) 2014-04-30
CN103764654B true CN103764654B (zh) 2016-01-20

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Family Applications (3)

Application Number Title Priority Date Filing Date
CN201280043260.6A Expired - Fee Related CN103764654B (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂
CN201510893703.6A Expired - Fee Related CN105503862B (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂
CN201510893692.1A Pending CN105481853A (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂

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Application Number Title Priority Date Filing Date
CN201510893703.6A Expired - Fee Related CN105503862B (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂
CN201510893692.1A Pending CN105481853A (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂

Country Status (37)

Country Link
US (5) US9051319B2 (enExample)
EP (2) EP3147284B1 (enExample)
JP (3) JP5917692B2 (enExample)
KR (1) KR101967172B1 (enExample)
CN (3) CN103764654B (enExample)
AP (1) AP3867A (enExample)
AR (1) AR087418A1 (enExample)
AU (2) AU2012290127B2 (enExample)
CA (1) CA2844054C (enExample)
CL (1) CL2014000245A1 (enExample)
CO (1) CO6940412A2 (enExample)
CY (1) CY1118726T1 (enExample)
DK (1) DK2739623T3 (enExample)
EA (3) EA027210B1 (enExample)
EC (1) ECSP14013189A (enExample)
ES (2) ES2618919T3 (enExample)
GE (2) GEP201706698B (enExample)
HK (1) HK1223915A1 (enExample)
HR (1) HRP20170421T1 (enExample)
HU (1) HUE033752T2 (enExample)
IL (2) IL230618A (enExample)
IN (1) IN2014CN00562A (enExample)
LT (1) LT2739623T (enExample)
ME (1) ME02638B (enExample)
MX (1) MX339149B (enExample)
PE (1) PE20141209A1 (enExample)
PH (1) PH12014500257A1 (enExample)
PL (1) PL2739623T3 (enExample)
PT (1) PT2739623T (enExample)
RS (1) RS55858B1 (enExample)
SG (2) SG10201503835TA (enExample)
SI (1) SI2739623T1 (enExample)
TW (3) TWI619715B (enExample)
UA (2) UA118010C2 (enExample)
UY (1) UY34234A (enExample)
WO (1) WO2013019828A1 (enExample)
ZA (2) ZA201400604B (enExample)

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CN103922966B (zh) * 2014-04-14 2015-10-21 武汉大学 作为甲型流感病毒抑制剂的甲酰胺和异腈类化合物及其制备与应用
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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
CN106478460B (zh) * 2016-09-28 2018-06-12 衢州学院 一种手性N-Boc-3-氨基-4-芳基-丁酸的合成方法
JP7034162B2 (ja) 2016-12-15 2022-03-11 サンシャイン・レイク・ファーマ・カンパニー・リミテッド インフルエンザウイルス複製の阻害剤及びその使用
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CN110446711B (zh) 2017-03-02 2022-02-15 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
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