KR101580310B1 - Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체 - Google Patents

Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체 Download PDF

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KR101580310B1
KR101580310B1 KR1020147017235A KR20147017235A KR101580310B1 KR 101580310 B1 KR101580310 B1 KR 101580310B1 KR 1020147017235 A KR1020147017235 A KR 1020147017235A KR 20147017235 A KR20147017235 A KR 20147017235A KR 101580310 B1 KR101580310 B1 KR 101580310B1
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substituted
unsubstituted
methyl
hydroxy
dioxo
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KR20140097438A (ko
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브라이언 알빈 존스
타카시 카와스지
테루히코 타이시
요시유키 타오다
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비이브 헬쓰케어 컴퍼니
시오노기세야쿠 가부시키가이샤
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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
    • C07D471/12—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
    • 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
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    • 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
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    • 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
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    • 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
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    • 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
    • C07D471/22—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)
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  • Organic Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Nutrition Science (AREA)
  • Physiology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (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)
KR1020147017235A 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체 Expired - Lifetime KR101580310B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JPJP-P-2005-131161 2005-04-28
JP2005131161 2005-04-28
JPJP-P-2005-312076 2005-10-27
JP2005312076 2005-10-27
PCT/US2006/016604 WO2006116764A1 (en) 2005-04-28 2006-04-28 Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020137028203A Division KR101504998B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020157036007A Division KR101848819B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체

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KR20140097438A KR20140097438A (ko) 2014-08-06
KR101580310B1 true KR101580310B1 (ko) 2016-01-04

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Application Number Title Priority Date Filing Date
KR1020147017235A Expired - Lifetime KR101580310B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체
KR1020077027734A Expired - Lifetime KR101363875B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체
KR1020157036007A Expired - Lifetime KR101848819B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체
KR1020137028203A Expired - Lifetime KR101504998B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체

Family Applications After (3)

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KR1020077027734A Expired - Lifetime KR101363875B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체
KR1020157036007A Expired - Lifetime KR101848819B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체
KR1020137028203A Expired - Lifetime KR101504998B1 (ko) 2005-04-28 2006-04-28 Hiv 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체

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EP (9) EP2527007B1 (enExample)
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KR (4) KR101580310B1 (enExample)
AU (1) AU2006239177B8 (enExample)
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CY (7) CY1115151T1 (enExample)
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FI (1) FIC20210017I1 (enExample)
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PL (5) PL2465580T3 (enExample)
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KR20130133061A (ko) 2013-12-05
PT2465580E (pt) 2014-02-25
EP3187225B1 (en) 2022-01-05
ES2437268T3 (es) 2014-01-09
LT3045206T (lt) 2018-06-11
BE2014C038I2 (fr) 2026-01-07
EP3045206B2 (en) 2023-02-15
US8410103B2 (en) 2013-04-02
IL225206A (en) 2017-11-30
MA29460B1 (fr) 2008-05-02
HUE056603T2 (hu) 2022-02-28
AU2006239177A1 (en) 2006-11-02
LT3284520T (lt) 2019-09-25
BE2021C519I2 (enExample) 2025-12-10
US20170224694A1 (en) 2017-08-10
IL186555A0 (en) 2008-01-20
EP3187226A1 (en) 2017-07-05
CY1115151T1 (el) 2015-12-09
FR21C1023I2 (fr) 2022-07-08
IL186555A (en) 2016-10-31
EP3045206A1 (en) 2016-07-20
SI3187225T1 (sl) 2022-04-29
PL3284520T3 (pl) 2020-01-31
US20170224695A1 (en) 2017-08-10
HUS2100023I1 (hu) 2021-07-28
AU2006239177B8 (en) 2012-02-16
JP2009079058A (ja) 2009-04-16
ES2906792T3 (es) 2022-04-20
CY2014024I2 (el) 2025-05-09
PL2465580T3 (pl) 2014-05-30
EP1874117B8 (en) 2014-03-12
EP2465580A1 (en) 2012-06-20
NO339525B1 (no) 2016-12-27
CY2021016I1 (el) 2021-10-15
WO2006116764A1 (en) 2006-11-02
JP2008540343A (ja) 2008-11-20
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EP1874117B1 (en) 2013-08-28
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NL301109I1 (nl) 2021-09-15
US20170267693A1 (en) 2017-09-21
US20170253616A1 (en) 2017-09-07
DK2465580T3 (en) 2014-03-10
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KR20080009733A (ko) 2008-01-29
SI1874117T1 (sl) 2014-01-31
US20220213121A1 (en) 2022-07-07
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MX302718B (es) 2012-08-27
ES2446324T3 (es) 2014-03-07
LTC2465580I2 (enExample) 2022-10-10
BRPI0610030A2 (pt) 2011-10-11
HUS2100022I1 (hu) 2021-07-28
US20150232479A1 (en) 2015-08-20
CY1122052T1 (el) 2020-10-14
US20130172559A1 (en) 2013-07-04
KR20140097438A (ko) 2014-08-06
EP2527007B1 (en) 2016-03-30
EP1874117A1 (en) 2008-01-09
NL301109I2 (nl) 2021-09-15
US20170029438A1 (en) 2017-02-02
EP1874117A4 (en) 2009-12-30
FR14C0041I2 (fr) 2015-11-13
ES2667868T5 (es) 2023-06-01
EP3284520B1 (en) 2019-06-05
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DK1874117T3 (da) 2013-09-23
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US11267823B2 (en) 2022-03-08
EP3284519A8 (en) 2018-04-18
HK1107227A1 (en) 2008-04-03
LTPA2021512I1 (enExample) 2021-07-12
IL225207A (en) 2017-11-30
MX2007013351A (es) 2008-01-21
CY1124601T1 (el) 2022-07-22
NO20075165L (no) 2007-11-22
DK3187225T3 (da) 2022-02-28
NO340111B1 (no) 2017-03-13
EP3372281A1 (en) 2018-09-12
ES2892304T3 (es) 2022-02-03
NO20161315A1 (no) 2007-11-22
VN34404A1 (en) 2013-07-25
US20170209454A1 (en) 2017-07-27
SI3372281T1 (sl) 2021-11-30
US20120115875A1 (en) 2012-05-10
LU92446I2 (fr) 2015-10-29
CY1116331T1 (el) 2017-02-08
EP3045206B1 (en) 2018-03-28
PT3372281T (pt) 2021-10-14
US10927129B2 (en) 2021-02-23
US20170369509A1 (en) 2017-12-28
CY2014024I1 (el) 2015-12-09
LTPA2014021I1 (lt) 2014-07-25
US9051337B2 (en) 2015-06-09
FR21C1023I1 (fr) 2021-07-23
PT3284520T (pt) 2019-09-10
EA200702080A1 (ru) 2008-04-28
CY2021016I2 (el) 2021-12-31
EP3284520A1 (en) 2018-02-21
FIC20210017I1 (fi) 2021-06-10
NO2017010I1 (no) 2017-03-27
TW200716635A (en) 2007-05-01
US9273065B2 (en) 2016-03-01
HUE037795T2 (hu) 2018-09-28
HK1172282A1 (en) 2013-04-19
PL3372281T3 (pl) 2021-12-27
US20160137666A1 (en) 2016-05-19
US8778943B2 (en) 2014-07-15
ES2743531T3 (es) 2020-02-19
EA014162B1 (ru) 2010-10-29
US20200339598A1 (en) 2020-10-29
LUC00210I2 (enExample) 2022-10-07
KR101848819B1 (ko) 2018-04-16

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