JP2013209405A5 - - Google Patents

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Publication number: JP2013209405A5
Authority: JP; Japan
Prior art keywords: alkyl; haloalkyl; independently; pharmaceutically acceptable; acceptable salt
Prior art date: 2013-05-23
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.): Granted

Application number

JP2013108533A

Other languages

English (en)

Japanese (ja)

Other versions

JP5886790B2 (ja

JP2013209405A (ja

Filing date

2013-05-23

Publication date

2015-09-17

2013-05-23 Application filed filed Critical

2013-10-10 Publication of JP2013209405A publication Critical patent/JP2013209405A/ja

2015-09-17 Publication of JP2013209405A5 publication Critical patent/JP2013209405A5/ja

2016-03-16 Application granted granted Critical

2016-03-16 Publication of JP5886790B2 publication Critical patent/JP5886790B2/ja

Status Expired - Fee Related legal-status Critical Current

2031-03-28 Anticipated expiration legal-status Critical

Links

125000000217 alkyl group Chemical group 0.000 claims 75
150000001875 compounds Chemical class 0.000 claims 27
125000001424 substituent group Chemical group 0.000 claims 27
150000003839 salts Chemical class 0.000 claims 26
229910052736 halogen Inorganic materials 0.000 claims 20
150000002367 halogens Chemical class 0.000 claims 20
229910052799 carbon Inorganic materials 0.000 claims 14
229910052739 hydrogen Inorganic materials 0.000 claims 14
125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 10
125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 10
125000003709 fluoroalkyl group Chemical group 0.000 claims 9
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 8
125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 7
125000003118 aryl group Chemical group 0.000 claims 6
125000000753 cycloalkyl group Chemical group 0.000 claims 6
125000005842 heteroatom Chemical group 0.000 claims 6
125000001624 naphthyl group Chemical group 0.000 claims 4
229910052760 oxygen Inorganic materials 0.000 claims 4
229910052717 sulfur Inorganic materials 0.000 claims 4
125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
-1 3,5-di-substituted phenyl Chemical group 0.000 claims 3
125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
125000003342 alkenyl group Chemical group 0.000 claims 3
229910052794 bromium Inorganic materials 0.000 claims 3
229910052801 chlorine Inorganic materials 0.000 claims 3
239000008194 pharmaceutical composition Substances 0.000 claims 3
229920006395 saturated elastomer Polymers 0.000 claims 3
125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 2
101100273648 Mus musculus Ccna2 gene Proteins 0.000 claims 2
125000002619 bicyclic group Chemical group 0.000 claims 2
125000001188 haloalkyl group Chemical group 0.000 claims 2
125000001072 heteroaryl group Chemical group 0.000 claims 2
125000000623 heterocyclic group Chemical group 0.000 claims 2
239000002835 hiv fusion inhibitor Substances 0.000 claims 2
229910052757 nitrogen Inorganic materials 0.000 claims 2
125000006574 non-aromatic ring group Chemical group 0.000 claims 2
239000002777 nucleoside Substances 0.000 claims 2
150000003833 nucleoside derivatives Chemical class 0.000 claims 2
230000002265 prevention Effects 0.000 claims 2
239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 2
125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 1
125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 1
125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 claims 1
208000030507 AIDS Diseases 0.000 claims 1
208000031886 HIV Infections Diseases 0.000 claims 1
208000037357 HIV infectious disease Diseases 0.000 claims 1
229940099797 HIV integrase inhibitor Drugs 0.000 claims 1
125000004432 carbon atom Chemical group C* 0.000 claims 1
239000003795 chemical substances by application Substances 0.000 claims 1
125000000392 cycloalkenyl group Chemical group 0.000 claims 1
239000003814 drug Substances 0.000 claims 1
239000003937 drug carrier Substances 0.000 claims 1
229910052731 fluorine Inorganic materials 0.000 claims 1
239000003084 hiv integrase inhibitor Substances 0.000 claims 1
239000004030 hiv protease inhibitor Substances 0.000 claims 1
208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
208000015181 infectious disease Diseases 0.000 claims 1
IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
230000003612 virological effect Effects 0.000 claims 1
0 *C(*1CCCCC1)=O Chemical compound *C(*1CCCCC1)=O 0.000 description 2

JP2013108533A 2010-03-30 2013-05-23 非ヌクレオシド逆転写酵素阻害剤 Expired - Fee Related JP5886790B2 (ja)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date
US31882410P	2010-03-30	2010-03-30
US61/318,824		2010-03-30
US32157310P	2010-04-07	2010-04-07
US61/321,573		2010-04-07

Related Parent Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2012538161A Division JP5281718B2 (ja)	2010-03-30	2011-03-28	非ヌクレオシド逆転写酵素阻害剤

Publications (3)

Publication Number	Publication Date
JP2013209405A JP2013209405A (ja)	2013-10-10
JP2013209405A5 true JP2013209405A5 (2)	2015-09-17
JP5886790B2 JP5886790B2 (ja)	2016-03-16

Family

ID=44710363

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
JP2012538161A Active JP5281718B2 (ja)	2010-03-30	2011-03-28	非ヌクレオシド逆転写酵素阻害剤
JP2013108533A Expired - Fee Related JP5886790B2 (ja)	2010-03-30	2013-05-23	非ヌクレオシド逆転写酵素阻害剤

Family Applications Before (1)

Application Number	Title	Priority Date	Filing Date
JP2012538161A Active JP5281718B2 (ja)	2010-03-30	2011-03-28	非ヌクレオシド逆転写酵素阻害剤

Country Status (44)

Country	Link
US (2)	US8486975B2 (2)
EP (2)	EP2552902B1 (2)
JP (2)	JP5281718B2 (2)
KR (1)	KR101421861B1 (2)
CN (1)	CN102971308B (2)
AR (1)	AR080859A1 (2)
AU (1)	AU2011235568B2 (2)
BR (1)	BR112012024691B1 (2)
CA (1)	CA2794377C (2)
CL (1)	CL2012002744A1 (2)
CO (1)	CO6630126A2 (2)
CR (1)	CR20120503A (2)
CY (3)	CY1118774T1 (2)
DK (2)	DK2552902T3 (2)
DO (1)	DOP2012000256A (2)
EA (1)	EA024804B1 (2)
EC (1)	ECSP12012201A (2)
ES (2)	ES2609636T3 (2)
FI (1)	FIC20190021I1 (2)
GE (1)	GEP20156368B (2)
HN (1)	HN2012002039A (2)
HR (2)	HRP20150427T1 (2)
HU (4)	HUE025336T2 (2)
IL (2)	IL222030A (2)
LT (3)	LT2924034T (2)
LU (2)	LUC00113I9 (2)
MA (1)	MA34170B1 (2)
ME (2)	ME02181B (2)
MX (1)	MX2012011379A (2)
MY (1)	MY163979A (2)
NI (1)	NI201200146A (2)
NL (1)	NL300980I2 (2)
NO (2)	NO2019019I1 (2)
NZ (1)	NZ602670A (2)
PE (1)	PE20130158A1 (2)
PH (1)	PH12012501923A1 (2)
PL (2)	PL2552902T3 (2)
PT (2)	PT2552902E (2)
RS (2)	RS54017B1 (2)
SG (1)	SG184347A1 (2)
SI (2)	SI2924034T1 (2)
TN (1)	TN2012000455A1 (2)
TW (1)	TWI458719B (2)
WO (1)	WO2011120133A1 (2)

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SI2924034T1 (sl) *	2010-03-30	2017-05-31	Merck Canada Inc.	Farmacevtski sestavek, ki obsega nenukleozidni inhibitor reverzne transkriptaze
US20140031250A1 (en)	2010-10-07	2014-01-30	David Tsai Ting	Biomarkers of Cancer
CA2882947A1 (en)	2012-09-26	2014-04-03	Merck Sharp & Dohme Corp.	Crystalline form of a reverse transcriptase inhibitor
JO3470B1 (ar)	2012-10-08	2020-07-05	Merck Sharp & Dohme	مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
BR112015012843B8 (pt)	2012-12-05	2023-04-25	Merck Sharp & Dohme	Método para sintetizar o composto
US20160287568A1 (en) *	2013-11-22	2016-10-06	Merck Sharp & Dohme Corp.	Composition of a non-nucleoside reverse transcriptase inhibitor
CA2930585A1 (en) *	2013-12-04	2015-06-11	Merck Sharp & Dohme Corp.	Process for making reverse transcriptase inhibitors
WO2015153304A1 (en)	2014-04-01	2015-10-08	Merck Sharp & Dohme Corp.	Prodrugs of hiv reverse transcriptase inhibitors
US10301624B2 (en)	2014-06-25	2019-05-28	The General Hospital Corporation	Targeting human satellite II (HSATII)
WO2017095761A1 (en)	2015-12-02	2017-06-08	Merck Sharp & Dohme Corp.	Pharmaceutical compositions containing doravirine, tenofovir disoproxil fumarate and lamivudine
US11077050B2 (en)	2017-03-24	2021-08-03	Merck Sharp & Dohme Corp.	Formulation for parenteral administration
RU2019136678A (ru)	2017-04-18	2021-05-18	Сипла Лимитед	Комбинированная терапия для применения в лечении ретровирусных инфекций
JP2021512956A (ja)	2018-02-06	2021-05-20	ザジェネラルホスピタルコーポレイション	腫瘍免疫応答のバイオマーカーとしてのリピートｒｎａ
EP3823632B1 (en) *	2018-07-17	2025-10-29	Merck Sharp & Dohme LLC	Efda in combination with doravirine for use in treating f227c mutated hiv infections
CA3122571C (en)	2018-12-18	2023-08-01	Merck Sharp & Dohme Corp.	Pyrimidone derivatives as selective cytotoxic agents against hiv infected cells
CN110801455B (zh) *	2019-11-12	2020-06-02	河北医科大学第二医院	用于治疗mrsa的药物组合物及其应用
CN114163309B (zh) *	2021-12-27	2023-04-25	甘肃皓天医药科技有限责任公司	一种多拉韦林中间体的制备方法
CN114349690B (zh) *	2022-02-15	2023-04-25	甘肃皓天医药科技有限责任公司	一种多拉韦林中间体合成方法
CN116903590A (zh) *	2023-06-06	2023-10-20	延边大学	一种含杂环结构的吡啶酮类化合物及其制备方法和用途
CN120157613A (zh) *	2023-12-15	2025-06-17	山东诚创蓝海医药科技有限公司	多拉韦林中间体及其应用和合成方法

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SE9904045D0 (sv)	1999-11-09	1999-11-09	Astra Ab	Compounds
TW200423930A (en) *	2003-02-18	2004-11-16	Hoffmann La Roche	Non-nucleoside reverse transcriptase inhibitors
BRPI0408704A (pt)	2003-03-24	2006-03-07	Hoffmann La Roche	benzil-piridazinonas como inibidores de transcriptase reversa
TW200505441A (en)	2003-03-24	2005-02-16	Hoffmann La Roche	Non-nucleoside reverse transcriptase inhibitorsⅠ
US7166738B2 (en)	2004-04-23	2007-01-23	Roche Palo Alto Llc	Non-nucleoside reverse transcriptase inhibitors
DE602005017604D1 (de)	2004-04-23	2009-12-24	Hoffmann La Roche	Inhibitoren der nicht-nukleosid-inhibitoren der reversen transkriptase
CA2592092A1 (en)	2004-12-22	2006-06-29	Pfizer Limited	Nonnucleoside inhibitors of hiv-1 reverse transcriptase
AR057455A1 (es)	2005-07-22	2007-12-05	Merck & Co Inc	Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica
WO2007045573A1 (en)	2005-10-19	2007-04-26	F. Hoffmann-La Roche Ag	Phenyl-acetamide nnrt inhibitors
AU2006303367A1 (en)	2005-10-19	2007-04-26	F. Hoffmann-La Roche Ag	N-phenyl phenylacetamide non-nucleoside reverse transcriptase inihibitors
TW200831085A (en)	2006-12-13	2008-08-01	Merck & Co Inc	Non-nucleoside reverse transcriptase inhibitors
CN101952274A (zh)	2007-11-20	2011-01-19	默沙东公司	非核苷逆转录酶抑制剂
SI2924034T1 (sl) *	2010-03-30	2017-05-31	Merck Canada Inc.	Farmacevtski sestavek, ki obsega nenukleozidni inhibitor reverzne transkriptaze

2011
- 2011-03-28 SI SI201131054A patent/SI2924034T1/sl unknown
- 2011-03-28 MX MX2012011379A patent/MX2012011379A/es active IP Right Grant
- 2011-03-28 BR BR112012024691-7A patent/BR112012024691B1/pt active IP Right Grant
- 2011-03-28 PH PH1/2012/501923A patent/PH12012501923A1/en unknown
- 2011-03-28 LT LTEP15157348.2T patent/LT2924034T/lt unknown
- 2011-03-28 EP EP11761856.1A patent/EP2552902B1/en active Active
- 2011-03-28 PT PT117618561T patent/PT2552902E/pt unknown
- 2011-03-28 CN CN201180018074.2A patent/CN102971308B/zh active Active
- 2011-03-28 WO PCT/CA2011/000320 patent/WO2011120133A1/en not_active Ceased
- 2011-03-28 HU HUE11761856A patent/HUE025336T2/en unknown
- 2011-03-28 PL PL11761856T patent/PL2552902T3/pl unknown
- 2011-03-28 PL PL15157348T patent/PL2924034T3/pl unknown
- 2011-03-28 DK DK11761856.1T patent/DK2552902T3/en active
- 2011-03-28 PE PE2012001823A patent/PE20130158A1/es active IP Right Grant
- 2011-03-28 ME MEP-2015-76A patent/ME02181B/me unknown
- 2011-03-28 RS RS20150340A patent/RS54017B1/sr unknown
- 2011-03-28 SI SI201130491T patent/SI2552902T1/sl unknown
- 2011-03-28 EA EA201290976A patent/EA024804B1/ru active Protection Beyond IP Right Term
- 2011-03-28 ES ES15157348.2T patent/ES2609636T3/es active Active
- 2011-03-28 MY MYPI2012004342A patent/MY163979A/en unknown
- 2011-03-28 GE GEAP201112882A patent/GEP20156368B/en unknown
- 2011-03-28 DK DK15157348.2T patent/DK2924034T3/en active
- 2011-03-28 ME MEP-2016-282A patent/ME02570B/me unknown
- 2011-03-28 KR KR1020127025733A patent/KR101421861B1/ko active Active
- 2011-03-28 NZ NZ602670A patent/NZ602670A/en unknown
- 2011-03-28 EP EP15157348.2A patent/EP2924034B1/en active Active
- 2011-03-28 HU HUE15157348A patent/HUE031785T2/en unknown
- 2011-03-28 SG SG2012072401A patent/SG184347A1/en unknown
- 2011-03-28 CA CA2794377A patent/CA2794377C/en active Active
- 2011-03-28 PT PT151573482T patent/PT2924034T/pt unknown
- 2011-03-28 ES ES11761856.1T patent/ES2536295T3/es active Active
- 2011-03-28 RS RS20161093A patent/RS55505B1/sr unknown
- 2011-03-28 MA MA35324A patent/MA34170B1/fr unknown
- 2011-03-28 AU AU2011235568A patent/AU2011235568B2/en active Active
- 2011-03-28 US US13/073,631 patent/US8486975B2/en active Active
- 2011-03-28 JP JP2012538161A patent/JP5281718B2/ja active Active
- 2011-03-28 HR HRP20150427TT patent/HRP20150427T1/hr unknown
- 2011-03-29 AR ARP110101028A patent/AR080859A1/es active IP Right Grant
- 2011-03-29 TW TW100110833A patent/TWI458719B/zh active
2012
- 2012-09-20 IL IL222030A patent/IL222030A/en active Protection Beyond IP Right Term
- 2012-09-20 TN TNP2012000455A patent/TN2012000455A1/en unknown
- 2012-09-27 HN HN2012002039A patent/HN2012002039A/es unknown
- 2012-09-28 DO DO2012000256A patent/DOP2012000256A/es unknown
- 2012-09-28 NI NI201200146A patent/NI201200146A/es unknown
- 2012-09-28 CL CL2012002744A patent/CL2012002744A1/es unknown
- 2012-10-01 CO CO12171897A patent/CO6630126A2/es active IP Right Grant
- 2012-10-01 EC ECSP12012201 patent/ECSP12012201A/es unknown
- 2012-10-01 CR CR20120503A patent/CR20120503A/es unknown
2013
- 2013-05-23 JP JP2013108533A patent/JP5886790B2/ja not_active Expired - Fee Related
- 2013-07-03 US US13/934,633 patent/US20130296382A1/en not_active Abandoned
2014
- 2014-06-23 IL IL233334A patent/IL233334A/en active IP Right Grant
2016
- 2016-12-09 HR HRP20161680TT patent/HRP20161680T1/hr unknown
2017
- 2017-01-25 CY CY20171100114T patent/CY1118774T1/el unknown
2019
- 2019-04-09 HU HUS1900022C patent/HUS1900022I1/hu unknown
- 2019-04-09 HU HUS1900021C patent/HUS1900021I1/hu unknown
- 2019-04-11 LT LTPA2019507C patent/LTC2924034I2/lt unknown
- 2019-04-11 LT LTPA2019506 patent/LTC2552902I2/lt unknown
- 2019-04-16 NL NL300980C patent/NL300980I2/nl unknown
- 2019-04-17 FI FIC20190021C patent/FIC20190021I1/fi unknown
- 2019-04-17 LU LU00113C patent/LUC00113I9/fr unknown
- 2019-04-17 LU LU00114C patent/LUC00114I2/fr unknown
- 2019-04-24 NO NO2019019C patent/NO2019019I1/no unknown
- 2019-04-24 NO NO2019018C patent/NO2019018I1/no unknown
- 2019-05-16 CY CY2019026C patent/CY2019026I1/el unknown
- 2019-05-16 CY CY2019025C patent/CY2019025I1/el unknown

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