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)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
Virology (AREA)
Tropical Medicine & Parasitology (AREA)
Molecular Biology (AREA)
AIDS & HIV (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (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
US7939537B2 (en)	2005-10-04	2011-05-10	Istituto Di Ricerche 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
EP2046328A4 (en) *	2006-07-19	2009-10-28	Univ Georgia Res Found	PYRIDINONE DIKETOIC 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
CN102046637B (zh) *	2008-03-27	2013-10-02	百时美施贵宝公司	N-[[4-氟-2-(5-甲基-1H-1,2,4-三唑-1-基)苯基]甲基]-4,6,7,9-四氢-3-羟基-9,9-二甲基-4-氧代-嘧啶并[2,1-c][1,4]噁嗪-2-甲酰胺钠盐一水合物的晶体形式
EP2349276B1 (en) *	2008-10-06	2019-11-27	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
BR112012008586A2 (pt)	2009-10-13	2016-11-29	Elanco Animal Health Ireland	inibidores da integrase macrocíclicos
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
SI2932970T1 (en)	2010-01-27	2018-07-31	Viiv Healthcare Company	Antiviral therapy
BR112012024796A2 (pt)	2010-04-02	2016-06-07	Janssen R&D Ireland	inibidores de integrase macrocíclicos
WO2012007500A2 (de)	2010-07-15	2012-01-19	Bayer Cropscience Ag	Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel
US8791108B2 (en)	2011-08-18	2014-07-29	Bristol-Myers Squibb Company	Inhibitors of human immunodeficiency virus replication
EP3750544B1 (en)	2011-11-30	2025-03-05	Emory University	Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
EP2807149A2 (en) *	2012-01-26	2014-12-03	CRO Consulting Limited	Agents for treating neurodegenerative disorders
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
SI2997033T1 (en)	2013-05-17	2018-04-30	Merck Sharp & Dohme Corp.	FUZYCLE TRICYCLE HETEROCYCLIC COMPOUNDS AS HIV INTEGRATED INHIBITORS
WO2014200880A1 (en)	2013-06-13	2014-12-18	Merck Sharp & Dohme Corp.	Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
KR101809392B1 (ko)	2013-09-27	2017-12-14	머크 샤프 앤드 돔 코포레이션	Hiv 인테그라제 억제제로서 유용한 치환된 퀴놀리진 유도체
WO2016187788A1 (en)	2015-05-25	2016-12-01	Merck Sharp & Dohme Corp.	Fused tricyclic heterocyclic compounds useful for treating hiv infection
WO2017087257A1 (en)	2015-11-17	2017-05-26	Merck Sharp & Dohme Corp.	Amido-substituted pyridotriazine derivatives useful as hiv integrase inhibitors
WO2017106071A1 (en)	2015-12-15	2017-06-22	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
US10934312B2 (en)	2016-12-02	2021-03-02	Merck Sharp & Dohme Corp.	Tricyclic heterocycle compounds useful 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)
US10786488B2 (en)	2017-01-26	2020-09-29	Merck Sharp & Dohme Corp.	Substituted quinolizine derivatives useful 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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US5693641A (en) *	1996-08-16	1997-12-02	Berlex Laboratories Inc.	Bicyclic pyrimidine derivatives and their use as anti-coagulants
ATE355064T1 (de)	2001-10-26	2006-03-15	Angeletti P Ist Richerche Bio	Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
WO2003035077A1 (en)	2001-10-26	2003-05-01	Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa	N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
EP1539762A2 (en) *	2002-06-26	2005-06-15	Bristol-Myers Squibb Company	Bicyclic pyrimidinones as coagulation cascade inhibitors
AU2003292437A1 (en)	2002-12-27	2004-07-22	Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa	Tetrahydro-4h-pyrido(1,2-a)pyrimidines and related compounds useful as hiv integrase inhibitors
AR046938A1 (es)	2003-12-12	2006-01-04	Merck & Co Inc	Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
TW200526635A (en)	2003-12-22	2005-08-16	Shionogi & Co	Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
NZ555215A (en)	2004-12-03	2010-08-27	Merck Sharp & Dohme	Use of atazanavir for improving the pharmacokinetics of raltegravir
US7981879B2 (en)	2005-03-31	2011-07-19	Instituto di Ricerchi di Biologia Molecolare P. Angeletti S.p.A.	HIV integrase inhibitors

2005
- 2005-05-11 US US11/126,891 patent/US7176196B2/en not_active Expired - Lifetime
- 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 BR BRPI0511623-6A patent/BRPI0511623A/pt not_active IP Right Cessation
- 2005-05-12 PT PT05750075T patent/PT1749011E/pt unknown
- 2005-05-12 AU AU2005250356A patent/AU2005250356C1/en not_active Ceased
- 2005-05-12 ES ES05750075T patent/ES2315875T3/es not_active Expired - Lifetime
- 2005-05-12 SI SI200530481T patent/SI1749011T1/sl unknown
- 2005-05-12 RU RU2006146970/04A patent/RU2381228C2/ru not_active IP Right Cessation
- 2005-05-12 PL PL05750075T patent/PL1749011T3/pl unknown
- 2005-05-12 AT AT05750075T patent/ATE412656T1/de active
- 2005-05-12 NZ NZ551282A patent/NZ551282A/en not_active IP Right Cessation
- 2005-05-12 CA CA2568356A patent/CA2568356C/en not_active Expired - Fee Related
- 2005-05-12 EP EP05750075A patent/EP1749011B1/en not_active Expired - Lifetime
- 2005-05-12 JP JP2007515142A patent/JP4874959B2/ja not_active Expired - Fee Related
- 2005-05-12 DK DK05750075T patent/DK1749011T3/da active
- 2005-05-12 DE DE602005010690T patent/DE602005010690D1/de not_active Expired - Lifetime
- 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
EP1749011A1 (en)	2007-02-07
TW200600503A (en)	2006-01-01
HRP20090005T3 (en)	2009-02-28
EP1749011B1 (en)	2008-10-29
ES2315875T3 (es)	2009-04-01
US7176196B2 (en)	2007-02-13
DK1749011T3 (da)	2009-02-16
SI1749011T1 (sl)	2009-08-31
IL179455A (en)	2011-10-31
RU2381228C2 (ru)	2010-02-10
KR101097623B1 (ko)	2011-12-22
AU2005250356C1 (en)	2011-10-06
AU2005250356B2 (en)	2011-03-17
PE20060242A1 (es)	2006-03-31
AU2005250356A1 (en)	2005-12-15
IL179455A0 (en)	2007-05-15
JP4874959B2 (ja)	2012-02-15
CA2568356C (en)	2012-07-03
US20050267105A1 (en)	2005-12-01
PT1749011E (pt)	2008-11-27
CA2568356A1 (en)	2005-12-15
ATE412656T1 (de)	2008-11-15
KR20070039502A (ko)	2007-04-12
US20060276466A1 (en)	2006-12-07
NZ551282A (en)	2009-05-31
BRPI0511623A (pt)	2008-03-11
RS50700B (sr)	2010-06-30
DE602005010690D1 (de)	2008-12-11
WO2005118593A1 (en)	2005-12-15
JP2008501018A (ja)	2008-01-17
HK1107343A1 (en)	2008-04-03
PL1749011T3 (pl)	2009-04-30
NO20065879L (no)	2007-02-20
RU2006146970A (ru)	2008-07-10
AR049124A1 (es)	2006-06-28
CY1110266T1 (el)	2015-01-14
US7511037B2 (en)	2009-03-31
MXPA06013835A (es)	2007-02-02

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
PL1948666T3 (pl)	2010-08-31	Inhibitory integrazy HIV
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
ZA200703444B (en)	2008-11-26	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