TWI366567B - Bicyclic heterocycles as hiv integrase inhibitors - Google Patents

Bicyclic heterocycles as hiv integrase inhibitors

Info

Publication number: TWI366567B
Authority: TW; Taiwan
Prior art keywords: hiv integrase; integrase inhibitors; bicyclic heterocycles; heterocycles; bicyclic
Prior art date: 2004-05-28

Application number

TW094117105A

Other languages

English (en)

Other versions

TW200600503A (en

Inventor

B Narasimhulu Naidu

Carl Ouellet

Jacques Banville

Serge Plamondon

Francis Beaulieu

Roger Remillard

Timothy Paul Connolly

Margaret E Sorenson

Mark R Krystal

Yasutsugu Ueda

John D Matiskella

Michael A Walker

Original Assignee

Bristol Myers Squibb Co

Priority date (The priority date 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 date listed.)

2004-05-28

Filing date

2005-05-25

Publication date

2012-06-21

2005-05-25 Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co

2006-01-01 Publication of TW200600503A publication Critical patent/TW200600503A/zh

2012-06-21 Application granted granted Critical

2012-06-21 Publication of TWI366567B publication Critical patent/TWI366567B/zh

Links

229940099797 HIV integrase inhibitor Drugs 0.000 title 1
125000002618 bicyclic heterocycle group Chemical group 0.000 title 1
239000003084 hiv integrase inhibitor Substances 0.000 title 1

Classifications

- 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
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Veterinary Medicine (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Virology (AREA)
Communicable Diseases (AREA)
Oncology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
AIDS & HIV (AREA)
Tropical Medicine & Parasitology (AREA)
Molecular Biology (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

TW094117105A 2004-05-28 2005-05-25 Bicyclic heterocycles as hiv integrase inhibitors TWI366567B (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US57551304P	2004-05-28	2004-05-28
US60337104P	2004-08-20	2004-08-20
US11/126,891 US7176196B2 (en)	2004-05-28	2005-05-11	Bicyclic heterocycles as HIV integrase inhibitors

Publications (2)

Publication Number	Publication Date
TW200600503A TW200600503A (en)	2006-01-01
TWI366567B true TWI366567B (en)	2012-06-21

Family

ID=35456854

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
TW094117105A TWI366567B (en)	2004-05-28	2005-05-25	Bicyclic heterocycles as hiv integrase inhibitors

Country Status (27)

Country	Link
US (2)	US7176196B2 (zh)
EP (1)	EP1749011B1 (zh)
JP (1)	JP4874959B2 (zh)
KR (1)	KR101097623B1 (zh)
AR (1)	AR049124A1 (zh)
AT (1)	ATE412656T1 (zh)
AU (1)	AU2005250356C1 (zh)
BR (1)	BRPI0511623A (zh)
CA (1)	CA2568356C (zh)
CY (1)	CY1110266T1 (zh)
DE (1)	DE602005010690D1 (zh)
DK (1)	DK1749011T3 (zh)
ES (1)	ES2315875T3 (zh)
HK (1)	HK1107343A1 (zh)
HR (1)	HRP20090005T3 (zh)
IL (1)	IL179455A (zh)
MX (1)	MXPA06013835A (zh)
NO (1)	NO20065879L (zh)
NZ (1)	NZ551282A (zh)
PE (1)	PE20060242A1 (zh)
PL (1)	PL1749011T3 (zh)
PT (1)	PT1749011E (zh)
RS (1)	RS50700B (zh)
RU (1)	RU2381228C2 (zh)
SI (1)	SI1749011T1 (zh)
TW (1)	TWI366567B (zh)
WO (1)	WO2005118593A1 (zh)

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US7115601B2 (en)	2004-05-18	2006-10-03	Bristol-Myers Squibb Company	HIV integrase inhibitors
US7981879B2 (en) *	2005-03-31	2011-07-19	Instituto di Ricerchi di Biologia Molecolare P. Angeletti S.p.A.	HIV integrase inhibitors
US7494984B2 (en) *	2005-08-31	2009-02-24	Bristol-Myers Squibb Company	Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
CA2622639C (en) *	2005-10-04	2012-01-03	Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A.	Hiv integrase inhibitors
US7902182B2 (en) *	2005-11-16	2011-03-08	Bristol-Myers Squibb Company	HIV integrase inhibitors
WO2007064316A1 (en) *	2005-11-30	2007-06-07	Bristol-Myers Squibb Company	Bicyclic heterocycles as hiv integrase inhibitors
WO2007064502A1 (en) *	2005-12-01	2007-06-07	Bristol-Myers Squibb Company	Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide
US20070129379A1 (en) *	2005-12-01	2007-06-07	Bristol-Myers Squibb Company	Hiv integrase inhibitors
WO2007143446A1 (en) *	2006-05-30	2007-12-13	Bristol-Myers Squibb Company	Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors
US7893055B2 (en) *	2006-06-28	2011-02-22	Bristol-Myers Squibb Company	HIV integrase inhibitors
AU2007275805A1 (en) *	2006-07-19	2008-01-24	University Of Georgia Research Foundation, Inc.	Pyridinone diketo acids: Inhibitors of HIV replication in combination therapy
US7763630B2 (en) *	2007-06-06	2010-07-27	Bristol-Myers Squibb Company	HIV integrase inhibitors
US8129398B2 (en) *	2008-03-19	2012-03-06	Bristol-Myers Squibb Company	HIV integrase inhibitors
KR20100138959A (ko) *	2008-03-27	2010-12-31	브리스톨-마이어스 스큅 컴퍼니	Ｎ-[[４-플루오로-２-(５-메틸-1Ｈ-１,２,４-트리아졸-1-일)페닐]메틸]-４,６,７,９-테트라히드로-３-히드록시-９,９-디메틸-４-옥소-피리미도[２,１-ｃ][１,４]옥사진-２-카르복스아미드, 나트륨 염 일수화물의 결정질 형태
CA2738814C (en) *	2008-10-06	2014-01-28	Merck Sharp & Dohme Corp.	Hiv integrase inhibitors
US8143244B2 (en) *	2009-02-26	2012-03-27	Bristol-Myers Squibb Company	Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
CN102574854B (zh)	2009-10-13	2014-04-16	伊兰科动物健康爱尔兰有限公司	大环整合酶抑制剂
US8383639B2 (en)	2009-10-15	2013-02-26	Bristol-Myers Squibb Company	HIV integrase inhibitors
PH12012501095A1 (en)	2009-12-07	2015-04-22	Univ Georgia	Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications
ES2688925T3 (es)	2010-01-27	2018-11-07	Viiv Healthcare Company	Tratamiento antiviral
US8716293B2 (en)	2010-04-02	2014-05-06	Janssen R&D Ireland	Macrocyclic integrase inhibitors
EP2593447B1 (de)	2010-07-15	2016-08-17	Bayer Intellectual Property GmbH	3-pyridyl-heteroarylcarboxamidverbindungen als schädlingsbekämpfungsmittel
US8791108B2 (en)	2011-08-18	2014-07-29	Bristol-Myers Squibb Company	Inhibitors of human immunodeficiency virus replication
WO2013082476A1 (en)	2011-11-30	2013-06-06	Emory University	Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
JP2015508417A (ja) *	2012-01-26	2015-03-19	クロコンサルティングリミテッド	神経変性障害を治療するためのジアジリジン
US9714243B2 (en)	2012-12-17	2017-07-25	Merck Sharp & Dohme Corp.	4-pyridinonetriazine derivatives as HIV integrase inhibitors
US9493479B2 (en)	2013-04-16	2016-11-15	Merck Sharp & Dohme Corp.	Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
AU2014267951A1 (en)	2013-05-17	2015-11-19	Merck Sharp & Dohme Corp.	Fused Tricyclic Heterocyclic compounds as HIV integrase inhibitors
WO2014200880A1 (en)	2013-06-13	2014-12-18	Merck Sharp & Dohme Corp.	Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
TN2016000090A1 (en)	2013-09-27	2017-07-05	Merck Sharp & Dohme	Substituted quinolizine derivatives useful as hiv integrase inhibitors.
WO2016187788A1 (en)	2015-05-25	2016-12-01	Merck Sharp & Dohme Corp.	Fused tricyclic heterocyclic compounds useful for treating hiv infection
US10548910B2 (en)	2015-11-17	2020-02-04	Merck Sharp & Dohme Corp.	Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
US10544155B2 (en)	2015-12-15	2020-01-28	Merck Sharp & Dohme Corp.	Spirocyclic quinolizine derivatives useful as HIV integrase inhibitors
WO2017113288A1 (en)	2015-12-31	2017-07-06	Merck Sharp & Dohme Corp.	Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
JOP20190130A1 (ar)	2016-12-02	2019-06-02	Merck Sharp & Dohme	مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
EP3548031B1 (en)	2016-12-02	2023-07-19	Merck Sharp & Dohme LLC	Tricyclic heterocycle compounds useful as hiv integrase inhibitors
EP3573984A4 (en)	2017-01-26	2020-07-29	Merck Sharp & Dohme Corp.	USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
WO2021050555A1 (en) *	2019-09-10	2021-03-18	X-Chem, Inc.	Compositions and uses thereof
CN113912622B (zh) *	2020-07-10	2023-12-01	上海纽思克生物科技有限公司	三环嘧啶酮类化合物、其制备方法、其组合物和用途

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HU230248B1 (hu)	2001-10-26	2015-11-30	Msd Italia S.R.L.	N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok
DE60218511T2 (de)	2001-10-26	2007-10-25	Istituto Di Richerche Di Biologia Molecolare P. Angeletti S.P.A.	Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
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AR046938A1 (es)	2003-12-12	2006-01-04	Merck & Co Inc	Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
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2005
- 2005-05-11 US US11/126,891 patent/US7176196B2/en not_active Expired - Lifetime
- 2005-05-12 CA CA2568356A patent/CA2568356C/en not_active Expired - Fee Related
- 2005-05-12 PT PT05750075T patent/PT1749011E/pt unknown
- 2005-05-12 DE DE602005010690T patent/DE602005010690D1/de not_active Expired - Lifetime
- 2005-05-12 RU RU2006146970/04A patent/RU2381228C2/ru not_active IP Right Cessation
- 2005-05-12 EP EP05750075A patent/EP1749011B1/en not_active Expired - Lifetime
- 2005-05-12 AT AT05750075T patent/ATE412656T1/de active
- 2005-05-12 BR BRPI0511623-6A patent/BRPI0511623A/pt not_active IP Right Cessation
- 2005-05-12 SI SI200530481T patent/SI1749011T1/sl unknown
- 2005-05-12 AU AU2005250356A patent/AU2005250356C1/en not_active Ceased
- 2005-05-12 PL PL05750075T patent/PL1749011T3/pl unknown
- 2005-05-12 ES ES05750075T patent/ES2315875T3/es not_active Expired - Lifetime
- 2005-05-12 DK DK05750075T patent/DK1749011T3/da active
- 2005-05-12 NZ NZ551282A patent/NZ551282A/en not_active IP Right Cessation
- 2005-05-12 MX MXPA06013835A patent/MXPA06013835A/es active IP Right Grant
- 2005-05-12 WO PCT/US2005/016473 patent/WO2005118593A1/en active Application Filing
- 2005-05-12 JP JP2007515142A patent/JP4874959B2/ja not_active Expired - Fee Related
- 2005-05-12 RS RSP-2008/0569A patent/RS50700B/sr unknown
- 2005-05-25 TW TW094117105A patent/TWI366567B/zh not_active IP Right Cessation
- 2005-05-27 AR ARP050102187A patent/AR049124A1/es not_active Application Discontinuation
- 2005-05-30 PE PE2005000602A patent/PE20060242A1/es not_active Application Discontinuation
2006
- 2006-08-16 US US11/505,149 patent/US7511037B2/en active Active
- 2006-11-21 IL IL179455A patent/IL179455A/en not_active IP Right Cessation
- 2006-12-19 NO NO20065879A patent/NO20065879L/no not_active Application Discontinuation
- 2006-12-27 KR KR1020067027455A patent/KR101097623B1/ko not_active Expired - Fee Related
2007
- 2007-11-26 HK HK07112893.6A patent/HK1107343A1/xx not_active IP Right Cessation
2009
- 2009-01-07 HR HR20090005T patent/HRP20090005T3/xx unknown
- 2009-01-19 CY CY20091100068T patent/CY1110266T1/el unknown

Also Published As

Publication number	Publication date
IL179455A (en)	2011-10-31
MXPA06013835A (es)	2007-02-02
PT1749011E (pt)	2008-11-27
PE20060242A1 (es)	2006-03-31
JP2008501018A (ja)	2008-01-17
HRP20090005T3 (en)	2009-02-28
IL179455A0 (en)	2007-05-15
US7511037B2 (en)	2009-03-31
JP4874959B2 (ja)	2012-02-15
US7176196B2 (en)	2007-02-13
CA2568356C (en)	2012-07-03
NO20065879L (no)	2007-02-20
DK1749011T3 (da)	2009-02-16
AR049124A1 (es)	2006-06-28
BRPI0511623A (pt)	2008-03-11
KR101097623B1 (ko)	2011-12-22
NZ551282A (en)	2009-05-31
HK1107343A1 (en)	2008-04-03
KR20070039502A (ko)	2007-04-12
CY1110266T1 (el)	2015-01-14
EP1749011A1 (en)	2007-02-07
WO2005118593A1 (en)	2005-12-15
US20060276466A1 (en)	2006-12-07
ES2315875T3 (es)	2009-04-01
RU2006146970A (ru)	2008-07-10
AU2005250356C1 (en)	2011-10-06
PL1749011T3 (pl)	2009-04-30
US20050267105A1 (en)	2005-12-01
EP1749011B1 (en)	2008-10-29
TW200600503A (en)	2006-01-01
DE602005010690D1 (de)	2008-12-11
RS50700B (sr)	2010-06-30
SI1749011T1 (sl)	2009-08-31
AU2005250356A1 (en)	2005-12-15
AU2005250356B2 (en)	2011-03-17
RU2381228C2 (ru)	2010-02-10
ATE412656T1 (de)	2008-11-15
CA2568356A1 (en)	2005-12-15

Legal Events

Date	Code	Title	Description
2018-03-21	MM4A	Annulment or lapse of patent due to non-payment of fees

Publication	Publication Date	Title
TWI366567B (en)	2012-06-21	Bicyclic heterocycles as hiv integrase inhibitors
EP1753767A4 (en)	2010-06-30	BICYCLIC HETEROCYCLES AS HIV INTEGRASE INHIBITORS
EP1749008A4 (en)	2010-07-07	BICYCLIC HETEROCYCLES AS HIV INTEGRASE INHIBITORS
IL177189A0 (en)	2006-12-10	Hiv integrase inhibitors
IL177858A0 (en)	2006-12-31	Hiv integrase inhibitors
EP1725535A4 (en)	2009-11-25	HIV integrase
EP1756069A4 (en)	2007-11-28	HIV INTEGRASE INHIBITORS
SI1948666T1 (sl)	2010-06-30	Hiv integrazni inhibitorji
IL179161A0 (en)	2007-03-08	Hiv integrase inhibitors: cyclic pyrimidinone compounds
EP1725102A4 (en)	2009-04-29	HIV integrase
ZA200704130B (en)	2008-08-27	Protassium salt of an HIV integrase inhibitor
EP2132211A4 (en)	2011-12-07	4-CYANPHENYLAMINO-SUBSTITUTED BICYCLIC AND HETEROCYCLIC COMPOUNDS AS AN HIV HEMMER
EP2280981B8 (en)	2014-09-17	Bridged heterocycles as hiv integrase inhibitors
IL180963A0 (en)	2007-07-04	Hiv inhibiting bicyclic pyrimidine derivatives
AP2702A (en)	2013-07-23	Methods for improving the pharmacokinetics of HIV integrase inhibitors
AU2005310968A1 (en)	2006-06-08	Bicyclic amides as kinase inhibitors
EP1910363A4 (en)	2010-05-26	INHIBITORS OF HIV INTEGRASE
AP2321A (en)	2011-11-16	Quinoline derivatives for use as mycobactrial inhibitor.
IL187694A0 (en)	2008-11-03	Bicyclic 6-alkylidene-penems as class-d beta-lactamases inhibitors
EP1758585A4 (en)	2009-07-22	HIV integrase
EP1622615A4 (en)	2009-02-18	INHIBITORS OF THE INTEGRASE OF NAPHTHYRIDINE
EP1799653A4 (en)	2010-07-28	NEW HETEROCYCLES
EP1910356A4 (en)	2009-10-21	HIV integrase
ZA200609935B (en)	2008-06-25	Bicyclic heterocycles as HIV integrase inhibitors
IL189939A0 (en)	2008-08-07	Inhibitors of the hiv integrase enzyme