AU2005250356C1 - Bicyclic heterocycles as HIV integrase inhibitors - Google Patents

Bicyclic heterocycles as HIV integrase inhibitors Download PDF

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Publication number
AU2005250356C1
AU2005250356C1 AU2005250356A AU2005250356A AU2005250356C1 AU 2005250356 C1 AU2005250356 C1 AU 2005250356C1 AU 2005250356 A AU2005250356 A AU 2005250356A AU 2005250356 A AU2005250356 A AU 2005250356A AU 2005250356 C1 AU2005250356 C1 AU 2005250356C1
Authority
AU
Australia
Prior art keywords
oxo
methyl
oxazine
fluoro
hydroxy
Prior art date
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.)
Ceased
Application number
AU2005250356A
Other languages
English (en)
Other versions
AU2005250356A1 (en
AU2005250356B2 (en
Inventor
Jacques Banville
Francis Beaulieu
Timothy P. Connolly
Mark R. Krystal
John D. Matiskella
B. Narasimhulu Naidu
Carl Ouellet
Serge Plamondon
Roger Remillard
Margaret E. Sorenson
Yasutsugu Ueda
Michael A. Walker
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
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.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AU2005250356A1 publication Critical patent/AU2005250356A1/en
Application granted granted Critical
Publication of AU2005250356B2 publication Critical patent/AU2005250356B2/en
Publication of AU2005250356C1 publication Critical patent/AU2005250356C1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (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)
AU2005250356A 2004-05-28 2005-05-12 Bicyclic heterocycles as HIV integrase inhibitors Ceased AU2005250356C1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US57551304P 2004-05-28 2004-05-28
US60/575,513 2004-05-28
US60337104P 2004-08-20 2004-08-20
US60/603,371 2004-08-20
US11/126,891 US7176196B2 (en) 2004-05-28 2005-05-11 Bicyclic heterocycles as HIV integrase inhibitors
US11/126,891 2005-05-11
PCT/US2005/016473 WO2005118593A1 (en) 2004-05-28 2005-05-12 Bicyclic heterocycles as hiv integrase inhibitors

Publications (3)

Publication Number Publication Date
AU2005250356A1 AU2005250356A1 (en) 2005-12-15
AU2005250356B2 AU2005250356B2 (en) 2011-03-17
AU2005250356C1 true AU2005250356C1 (en) 2011-10-06

Family

ID=35456854

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005250356A Ceased AU2005250356C1 (en) 2004-05-28 2005-05-12 Bicyclic heterocycles as HIV integrase inhibitors

Country Status (26)

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

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2006103399A1 (en) * 2005-03-31 2006-10-05 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa 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
JP5094725B2 (ja) * 2005-10-04 2012-12-12 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・エルレ・エルレ Ｈｉｖインテグラーゼ阻害剤
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
CA2657034A1 (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
WO2009120841A1 (en) * 2008-03-27 2009-10-01 Bristol-Myers Squibb Company Crystalline form of n-[[4-fluoro-2-(5-methyl-1h-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate
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
WO2011045330A1 (en) 2009-10-13 2011-04-21 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
SG181524A1 (en) 2009-12-07 2012-07-30 Univ Georgia Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications
EP3351249A1 (en) 2010-01-27 2018-07-25 VIIV Healthcare Company Antiviral therapy
WO2011121105A1 (en) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals 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
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
EP2807149A2 (en) * 2012-01-26 2014-12-03 CRO Consulting Limited Agents for treating neurodegenerative disorders
EP2931730B1 (en) 2012-12-17 2019-08-07 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
US9951079B2 (en) 2013-06-13 2018-04-24 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
CA2924829C (en) 2013-09-27 2019-10-29 Merck Sharp & Dohme Corp. 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
EP3389380B1 (en) 2015-12-15 2021-07-21 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
WO2018102634A1 (en) 2016-12-02 2018-06-07 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)
WO2018140368A1 (en) 2017-01-26 2018-08-02 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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5693641A (en) * 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
DE122009000048I1 (de) 2001-10-26 2010-04-08 Angeletti P Ist Richerche Bio N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase
CA2463975A1 (en) 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
US7094783B2 (en) * 2002-06-26 2006-08-22 Bristol-Myers Squibb Company Bicyclic pyrimidinones as coagulation cascade inhibitors
WO2004058756A1 (en) 2002-12-27 2004-07-15 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
BRPI0518741A2 (pt) 2004-12-03 2008-12-02 Merck & Co Inc uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero
WO2006103399A1 (en) 2005-03-31 2006-10-05 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors

Also Published As

Publication number Publication date
US20050267105A1 (en) 2005-12-01
KR20070039502A (ko) 2007-04-12
ATE412656T1 (de) 2008-11-15
TW200600503A (en) 2006-01-01
WO2005118593A1 (en) 2005-12-15
HRP20090005T3 (hr) 2009-02-28
NO20065879L (no) 2007-02-20
HK1107343A1 (en) 2008-04-03
RU2381228C2 (ru) 2010-02-10
TWI366567B (en) 2012-06-21
US7511037B2 (en) 2009-03-31
IL179455A0 (en) 2007-05-15
AR049124A1 (es) 2006-06-28
AU2005250356A1 (en) 2005-12-15
EP1749011B1 (en) 2008-10-29
CA2568356A1 (en) 2005-12-15
ES2315875T3 (es) 2009-04-01
NZ551282A (en) 2009-05-31
CY1110266T1 (el) 2015-01-14
PE20060242A1 (es) 2006-03-31
DE602005010690D1 (de) 2008-12-11
US7176196B2 (en) 2007-02-13
MXPA06013835A (es) 2007-02-02
IL179455A (en) 2011-10-31
DK1749011T3 (da) 2009-02-16
PT1749011E (pt) 2008-11-27
JP4874959B2 (ja) 2012-02-15
US20060276466A1 (en) 2006-12-07
JP2008501018A (ja) 2008-01-17
RS50700B (sr) 2010-06-30
RU2006146970A (ru) 2008-07-10
PL1749011T3 (pl) 2009-04-30
BRPI0511623A (pt) 2008-03-11
CA2568356C (en) 2012-07-03
AU2005250356B2 (en) 2011-03-17
EP1749011A1 (en) 2007-02-07
SI1749011T1 (sl) 2009-08-31
KR101097623B1 (ko) 2011-12-22

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Legal Events

Date Code Title Description
DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 17 MAY 2011.

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 17 MAY 2011

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired