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1. JPWO2012018065 - ＨＩＶインテグラーゼ阻害活性を有する化合物の製造方法

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Japan
Application Number 2012527760
Application Date 04.08.2011
Publication Number WO2012018065
Publication Date 09.02.2012
Grant Number 5636054
Grant Date 24.10.2014
Publication Kind B2
IPC
C07D 498/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
A61K 31/4985
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5365
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365ortho- or peri-condensed with heterocyclic ring systems
A61P 31/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
18for HIV
C07B 53/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
53Asymmetric syntheses
C07B 61/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
61Other general methods
CPC
C07D 498/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 213/79
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79Acids; Esters
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
A61K 31/5365
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365ortho- or peri-condensed with heterocyclic ring systems
C07D 213/80
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79Acids; Esters
80in position 3
C07D 211/94
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92with a hetero atom directly attached to the ring nitrogen atom
94Oxygen atom, e.g. piperidine N-oxide
FI
A61K 31/4985
A61K 31/5365
A61P 31/18
A61P 43/00,111
C07B 53/00C
C07B 61/00,300
F-term
4C055AA10
4C055BA02
4C055BA57
4C055BB02
4C055CA03
4C055CA42
Applicants 塩野義製薬株式会社
Inventors 隅野　幸仁
岡本　和也
桝井　盛泰
山田　大輔
五十嵐　史也
Agents 平木　祐輔
藤田　節
新井　栄一
田中　夏夫
藤井　愛
Priority Data 2010175899 05.08.2010 JP
2010277713 14.12.2010 JP
Title
(JA) ＨＩＶインテグラーゼ阻害活性を有する化合物の製造方法
Abstract
(JA)

式（Ｘ４）：

（式中、Ｒ１ｄは、水素、ハロゲン等であり、
Ｒ２ｄは、水素、置換基群Ｅで置換されていてもよい低級アルキル等であり、
Ｒ４ｄは、置換基群Ｅで置換されていてもよい低級アルキル等であり、ならびに
Ｒ６ｄは、置換基群Ｅで置換されていてもよい低級アルキル等である）
で表わされるピリドン誘導体の新規な製造方法を用いた、式（Ｙ１）または式（Ｙ２）：

（式中、Ｒｘは、置換されていてもよい炭素環低級アルキル等である）
で表わされる化合物またはその塩の製造方法。
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