JP4295353B2 - Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体 - Google Patents

Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体 Download PDF

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JP4295353B2
JP4295353B2 JP2008509227A JP2008509227A JP4295353B2 JP 4295353 B2 JP4295353 B2 JP 4295353B2 JP 2008509227 A JP2008509227 A JP 2008509227A JP 2008509227 A JP2008509227 A JP 2008509227A JP 4295353 B2 JP4295353 B2 JP 4295353B2
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optionally substituted
substituted
hydroxy
methyl
alkyl
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JP2008540343A (ja
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ジョンズ，ブライアン，アルヴィン
孝 川筋
照彦 大司
善之 垰田
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Shionogi and Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495—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
    • A61K31/535—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
    • A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2008509227A 2005-04-28 2006-04-28 Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体 Active JP4295353B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2005131161 2005-04-28
JP2005312076 2005-10-27
PCT/US2006/016604 WO2006116764A1 (en) 2005-04-28 2006-04-28 Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity

Related Child Applications (1)

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JP2008261344A Division JP2009079058A (ja) 2005-04-28 2008-10-08 Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体

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JP2008540343A JP2008540343A (ja) 2008-11-20
JP4295353B2 true JP4295353B2 (ja) 2009-07-15

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JP2008261344A Pending JP2009079058A (ja) 2005-04-28 2008-10-08 Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体

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US (22) US8129385B2 (enExample)
EP (9) EP3045206B2 (enExample)
JP (2) JP4295353B2 (enExample)
KR (4) KR101363875B1 (enExample)
AU (1) AU2006239177B8 (enExample)
BE (1) BE2021C519I2 (enExample)
BR (1) BRPI0610030B8 (enExample)
CA (1) CA2606282C (enExample)
CY (7) CY1115151T1 (enExample)
DK (6) DK3045206T3 (enExample)
EA (1) EA014162B1 (enExample)
ES (7) ES2906792T3 (enExample)
FI (1) FIC20210017I1 (enExample)
FR (1) FR14C0041I2 (enExample)
HK (2) HK1249742A1 (enExample)
HU (6) HUE037795T2 (enExample)
IL (4) IL186555A (enExample)
LT (5) LT3045206T (enExample)
LU (2) LU92446I2 (enExample)
MA (1) MA29460B1 (enExample)
MX (2) MX302718B (enExample)
NL (2) NL300676I2 (enExample)
NO (5) NO339525B1 (enExample)
NZ (1) NZ562339A (enExample)
PL (5) PL3372281T3 (enExample)
PT (5) PT1874117E (enExample)
SI (6) SI3372281T1 (enExample)
TW (1) TWI378931B (enExample)
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Cited By (3)

* Cited by examiner, † Cited by third party
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JP2009079058A (ja) * 2005-04-28 2009-04-16 Smithkline Beecham Corp Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体
US9216995B2 (en) 2010-04-12 2015-12-22 Shionogi & Co., Ltd. Pyridone derivative having integrase inhibitory activity
US10426780B2 (en) 2010-01-27 2019-10-01 Viiv Healthcare Company Antiviral therapy

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CA2744019C (en) 2008-12-11 2017-03-14 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
AU2014277831C1 (en) * 2008-12-11 2022-10-06 Shionogi & Co. Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
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TWI518084B (zh) 2009-03-26 2016-01-21 鹽野義製藥股份有限公司 哌喃酮與吡啶酮衍生物之製造方法
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TWI508968B (zh) 2010-02-08 2015-11-21 Biota Scient Management 用於治療呼吸道融合性病毒感染的化合物
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TWI577377B (zh) * 2010-09-16 2017-04-11 Ｖｉｉｖ醫療保健公司 醫藥組合物
HUE039859T2 (hu) * 2010-09-24 2019-02-28 Shionogi & Co Helyettesített policiklusos karbamoil-piridon-származék prodrug
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NZ562339A (en) 2011-01-28
ES2667868T3 (es) 2018-05-14
EP3372281B1 (en) 2021-07-07
LU92446I2 (fr) 2015-10-29
EA200702080A1 (ru) 2008-04-28
DK2465580T3 (en) 2014-03-10
EP3372281A1 (en) 2018-09-12
NO20161315A1 (no) 2007-11-22
VN34404A1 (en) 2013-07-25
US20170224694A1 (en) 2017-08-10
LTPA2021512I1 (enExample) 2021-07-12
HUS2100023I1 (hu) 2021-07-28
US20170260203A1 (en) 2017-09-14
KR101504998B1 (ko) 2015-03-23
HK1251191A1 (en) 2019-01-25
HK1172282A1 (en) 2013-04-19
PT1874117E (pt) 2013-10-17
US20170029438A1 (en) 2017-02-02
EP2465580A1 (en) 2012-06-20
US11267823B2 (en) 2022-03-08
EP3284520B1 (en) 2019-06-05
KR101363875B1 (ko) 2014-02-21
CY2021016I2 (el) 2021-12-31
EP3284520A1 (en) 2018-02-21
CY2021016I1 (el) 2021-10-15
SI3284520T1 (sl) 2019-10-30
US20170224695A1 (en) 2017-08-10
EP3284519A8 (en) 2018-04-18
KR20130133061A (ko) 2013-12-05
PT2465580E (pt) 2014-02-25
NO20075165L (no) 2007-11-22
CY1115151T1 (el) 2015-12-09
US10927129B2 (en) 2021-02-23
US20170369509A1 (en) 2017-12-28
SI1874117T1 (sl) 2014-01-31
ES2667868T5 (es) 2023-06-01
EP1874117B8 (en) 2014-03-12
LT3284520T (lt) 2019-09-25
EP3187226A1 (en) 2017-07-05
US20160207939A1 (en) 2016-07-21
KR20160003889A (ko) 2016-01-11
US20160137666A1 (en) 2016-05-19
US20150232479A1 (en) 2015-08-20
LTC1874117I2 (lt) 2025-03-25
NO2017010I1 (no) 2017-03-27
JP2009079058A (ja) 2009-04-16
US20170267693A1 (en) 2017-09-21
ES2892304T3 (es) 2022-02-03
ES2446324T3 (es) 2014-03-07
DK3045206T3 (en) 2018-05-22
FR14C0041I1 (enExample) 2014-06-27
DK3187225T3 (da) 2022-02-28
SI3045206T1 (en) 2018-07-31
BRPI0610030B1 (pt) 2020-09-15
HUS1400039I1 (hu) 2016-08-29
HUE037795T2 (hu) 2018-09-28
PL3284520T3 (pl) 2020-01-31
HK1249742A1 (en) 2018-11-09
NO340111B1 (no) 2017-03-13
US20170145033A1 (en) 2017-05-25
PL3045206T3 (pl) 2018-08-31
LUC00210I2 (enExample) 2022-10-07
US20120115875A1 (en) 2012-05-10
PL2465580T3 (pl) 2014-05-30
EP2527007A1 (en) 2012-11-28
CY1122052T1 (el) 2020-10-14
US20130172559A1 (en) 2013-07-04
US20200339598A1 (en) 2020-10-29
PT3372281T (pt) 2021-10-14
SI3372281T1 (sl) 2021-11-30
LTC2465580I2 (enExample) 2022-10-10
MA29460B1 (fr) 2008-05-02
TW200716635A (en) 2007-05-01
US9273065B2 (en) 2016-03-01
CA2606282C (en) 2016-04-26
ES2906792T3 (es) 2022-04-20
EP3187225B1 (en) 2022-01-05
CY1116331T1 (el) 2017-02-08
KR101848819B1 (ko) 2018-04-16
NL301109I2 (nl) 2021-09-15
US20220213121A1 (en) 2022-07-07
US8410103B2 (en) 2013-04-02
MX302718B (es) 2012-08-27

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