1. WO2012018065 - PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY

Publication Number WO/2012/018065

Publication Date 09.02.2012

International Application No. PCT/JP2011/067832

International Filing Date 04.08.2011

IPC

C07D 498/14 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
498	Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12	in which the condensed system contains three hetero rings
14	Ortho-condensed systems

A61K 31/5365 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535	having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365	ortho- or peri-condensed with heterocyclic ring systems

A61P 31/18 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31	Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12	Antivirals
14	for RNA viruses
18	for HIV

A61P 43/00 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43	Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108

C07D 211/94 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
211	Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92	with a hetero atom directly attached to the ring nitrogen atom
94	Oxygen atom, e.g. piperidine N-oxide

C07D 498/14 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
498	Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12	in which the condensed system contains three hetero rings
14	Ortho-condensed systems

A61K 31/5365 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535	having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365	ortho- or peri-condensed with heterocyclic ring systems

A61P 31/18 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31	Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12	Antivirals
14	for RNA viruses
18	for HIV

A61P 43/00 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43	Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108

C07D 211/94 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
211	Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92	with a hetero atom directly attached to the ring nitrogen atom
94	Oxygen atom, e.g. piperidine N-oxide

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CPC

A61K 31/5365

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535	having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365	ortho- or peri-condensed with heterocyclic ring systems

A61P 31/18

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31	Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12	Antivirals
14	for RNA viruses
18	for HIV

A61P 43/00

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43	Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

C07B 2200/13

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
B	GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200	Indexing scheme relating to specific properties of organic compounds
13	Crystalline forms, e.g. polymorphs

C07D 211/94

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
211	Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92	with a hetero atom directly attached to the ring nitrogen atom
94	Oxygen atom, e.g. piperidine N-oxide

C07D 213/79

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic 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
02	having three double bonds between ring members or between ring members and non-ring members
04	having 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
60	with 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
78	Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79	Acids; Esters

View more classifications

A61K 31/5365

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535	having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365	ortho- or peri-condensed with heterocyclic ring systems

A61P 31/18

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31	Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12	Antivirals
14	for RNA viruses
18	for HIV

A61P 43/00

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43	Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

C07B 2200/13

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
B	GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200	Indexing scheme relating to specific properties of organic compounds
13	Crystalline forms, e.g. polymorphs

C07D 211/94

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
211	Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92	with a hetero atom directly attached to the ring nitrogen atom
94	Oxygen atom, e.g. piperidine N-oxide

C07D 213/79

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic 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
02	having three double bonds between ring members or between ring members and non-ring members
04	having 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
60	with 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
78	Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79	Acids; Esters

C07D 213/80

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic 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
02	having three double bonds between ring members or between ring members and non-ring members
04	having 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
60	with 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
78	Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79	Acids; Esters
80	in position 3

C07D 498/14

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
498	Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12	in which the condensed system contains three hetero rings
14	Ortho-condensed systems

View less classifications

Applicants

• 塩野義製薬株式会社 Shionogi & Co., Ltd. [JP]/[JP](AllExceptUS)
• 隅野　幸仁 SUMINO, Yukihito [JP]/[JP](UsOnly)
• 岡本　和也 OKAMOTO, Kazuya [JP]/[JP](UsOnly)
• 桝井　盛泰 MASUI, Moriyasu [JP]/[JP](UsOnly)
• 山田　大輔 YAMADA, Daisuke [JP]/[JP](UsOnly)
• 五十嵐　史也 IKARASHI, Fumiya [JP]/[JP](UsOnly)

Inventors

• 隅野　幸仁 SUMINO, Yukihito
• 岡本　和也 OKAMOTO, Kazuya
• 桝井　盛泰 MASUI, Moriyasu
• 山田　大輔 YAMADA, Daisuke
• 五十嵐　史也 IKARASHI, Fumiya

Agents

• 高山　裕貢 TAKAYAMA, Hirotsugu

Priority Data

2010-175899		05.08.2010		JP
2010-277713		14.12.2010		JP

Publication Language Japanese (ja)

Filing Language Japanese (ja)

Designated States

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AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)

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Title

(EN) PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY

(FR) PROCÉDÉ POUR PRÉPARER UN COMPOSÉ AYANT UNE ACTIVITÉ INHIBITRICE D'INTÉGRASE DE VIH

(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

(EN) A process for preparing a compound represented by formula (Y1) or (Y2) [wherein R^x is an optionally substituted carbocyclyl -lower-alkyl group, or the like], using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R^1d is hydrogen, halogen, or the like; R^2d is hydrogen, a lower alkyl group, or the like, said lower alkyl group being optionally substituted with one or more selected from substituent group E; R^4d is a lower alkyl group or the like, said lower alkyl group being optionally substituted with one or more selected from substituent group E; and R^6d is a lower alkyl group or the like, said lower alkyl group being optionally substituted with one or more selected from substituent group E].

(FR) La présente invention concerne un procédé pour préparer un composé représenté par la formule (Y1) ou (Y2) [dans lesquelles R^x est un groupe carbocyclyl-(alkyle inférieur) facultativement substitué, ou similaire], utilisant un nouveau processus pour préparer un dérivé de pyridone représenté par la formule (X4) [dans laquelle R^1d est un hydrogène, un halogène, ou similaire; R^2d est un hydrogène, un groupe alkyle inférieur, ou similaire, ledit groupe alkyle inférieur étant facultativement substitué par un ou plusieurs choisis parmi le groupe de substituant E; R^4d est un groupe alkyle inférieur ou similaire, ledit groupe alkyle inférieur étant facultativement substitué par un ou plusieurs choisis parmi le groupe de substituant E; et R^6d est un groupe alkyle inférieur ou similaire, ledit groupe alkyle inférieur étant facultativement substitué par un ou plusieurs choisis parmi un groupe substituant E].

(JA) 式（Ｘ４）： （式中、Ｒ^１ｄは、水素、ハロゲン等であり、 Ｒ^２ｄ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、 Ｒ^４ｄ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 Ｒ^６ｄ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、Ｒ^ｘ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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