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
Application number
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 CN201510893692.1A priority Critical patent/CN105481853A/zh
Priority to CN201510893703.6A priority patent/CN105503862B/zh
Publication of CN103764654A publication Critical patent/CN103764654A/zh
Application granted granted Critical
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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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
CN201510893692.1A CN105481853A (zh) 2011-08-01 2012-08-01 流感病毒复制抑制剂
CN201510893703.6A CN105503862B (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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ID=46650922

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 (https=)
EP (2) EP3147284B1 (https=)
JP (3) JP5917692B2 (https=)
KR (1) KR101967172B1 (https=)
CN (3) CN103764654B (https=)
AP (1) AP3867A (https=)
AR (1) AR087418A1 (https=)
AU (2) AU2012290127B2 (https=)
CA (1) CA2844054C (https=)
CL (1) CL2014000245A1 (https=)
CO (1) CO6940412A2 (https=)
CY (1) CY1118726T1 (https=)
DK (1) DK2739623T3 (https=)
EA (3) EA023423B1 (https=)
EC (1) ECSP14013189A (https=)
ES (2) ES2763535T3 (https=)
GE (2) GEP201706698B (https=)
HK (1) HK1223915A1 (https=)
HR (1) HRP20170421T1 (https=)
HU (1) HUE033752T2 (https=)
IL (2) IL230618A (https=)
IN (1) IN2014CN00562A (https=)
LT (1) LT2739623T (https=)
ME (1) ME02638B (https=)
MX (1) MX339149B (https=)
PE (1) PE20141209A1 (https=)
PH (1) PH12014500257A1 (https=)
PL (1) PL2739623T3 (https=)
PT (1) PT2739623T (https=)
RS (1) RS55858B1 (https=)
SG (2) SG10201503835TA (https=)
SI (1) SI2739623T1 (https=)
TW (3) TWI594997B (https=)
UA (2) UA118010C2 (https=)
UY (1) UY34234A (https=)
WO (1) WO2013019828A1 (https=)
ZA (2) ZA201400604B (https=)

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JP6618901B2 (ja) * 2013-11-13 2019-12-11 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤を調製する方法
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WO2018041091A1 (en) * 2016-08-30 2018-03-08 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
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
CN108276401B (zh) * 2017-01-05 2020-12-22 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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WO2013019828A1 (en) 2013-02-07
HK1194736A1 (zh) 2014-10-24
JP2016121196A (ja) 2016-07-07
HK1223914A1 (zh) 2017-08-11
IL230618A (en) 2016-04-21
ZA201400604B (en) 2015-10-28
AU2016228190A1 (en) 2016-10-27
TWI537268B (zh) 2016-06-11
PT2739623T (pt) 2017-04-03
TW201313713A (zh) 2013-04-01
RS55858B1 (sr) 2017-08-31
DK2739623T3 (en) 2017-04-24
EA201490396A1 (ru) 2014-06-30
EA027210B1 (ru) 2017-06-30
EA201692506A2 (ru) 2017-06-30
IL244597A0 (en) 2016-04-21
SG10201503835TA (en) 2015-06-29
US10875855B2 (en) 2020-12-29
PL2739623T3 (pl) 2017-07-31
CN105481853A (zh) 2016-04-13
EA023423B1 (ru) 2016-06-30
HUE033752T2 (en) 2017-12-28
EA037372B1 (ru) 2021-03-22
EP2739623A1 (en) 2014-06-11
US20210040092A1 (en) 2021-02-11

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