CA2607151C - Hiv integrase inhibitors - Google Patents

Hiv integrase inhibitors Download PDF

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Publication number
CA2607151C
CA2607151C CA2607151A CA2607151A CA2607151C CA 2607151 C CA2607151 C CA 2607151C CA 2607151 A CA2607151 A CA 2607151A CA 2607151 A CA2607151 A CA 2607151A CA 2607151 C CA2607151 C CA 2607151C
Authority
CA
Canada
Prior art keywords
alkyl
fluorobenzyl
chloro
naphthyridine
alkylene
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.)
Expired - Fee Related
Application number
CA2607151A
Other languages
English (en)
French (fr)
Other versions
CA2607151A1 (en
Inventor
Joseph P. Vacca
John S. Wai
Linda S. Payne
Richard C. A. Isaacs
Wei Han
Melissa Egbertson
Richard Pracitto
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.)
Individual
Original Assignee
Merck Sharp & Dohme LLC
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 Merck Sharp & Dohme LLC filed Critical Merck Sharp & Dohme LLC
Publication of CA2607151A1 publication Critical patent/CA2607151A1/en
Application granted granted Critical
Publication of CA2607151C publication Critical patent/CA2607151C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/14—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2607151A 2005-05-10 2006-05-05 Hiv integrase inhibitors Expired - Fee Related CA2607151C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US67943105P 2005-05-10 2005-05-10
US60/679,431 2005-05-10
PCT/US2006/017369 WO2006121831A2 (en) 2005-05-10 2006-05-05 Hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
CA2607151A1 CA2607151A1 (en) 2006-11-16
CA2607151C true CA2607151C (en) 2012-06-19

Family

ID=37397115

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2607151A Expired - Fee Related CA2607151C (en) 2005-05-10 2006-05-05 Hiv integrase inhibitors

Country Status (7)

Country Link
US (4) US7741315B2 (cg-RX-API-DMAC10.html)
EP (1) EP1881825B1 (cg-RX-API-DMAC10.html)
JP (1) JP4982482B2 (cg-RX-API-DMAC10.html)
AU (1) AU2006244424B2 (cg-RX-API-DMAC10.html)
CA (1) CA2607151C (cg-RX-API-DMAC10.html)
TW (1) TW200819126A (cg-RX-API-DMAC10.html)
WO (1) WO2006121831A2 (cg-RX-API-DMAC10.html)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005087768A1 (en) 2004-03-09 2005-09-22 Merck & Co., Inc. Hiv integrase inhibitors
EP1725535A4 (en) 2004-03-09 2009-11-25 Merck & Co Inc HIV integrase
US7820680B2 (en) * 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
WO2007059125A2 (en) 2005-11-15 2007-05-24 Bristol-Myers Squibb Company Hiv integrase inhibitors
US7902182B2 (en) 2005-11-16 2011-03-08 Bristol-Myers Squibb Company HIV integrase inhibitors
US8039458B2 (en) 2005-11-17 2011-10-18 Bristol-Myers Squibb Company HIV integrase inhibitors
ES2596532T3 (es) 2006-03-16 2017-01-10 Second Genome, Inc. Compuestos de bicicloheteroarilo como moduladores de P2X7 y usos de los mismos
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
CA2665538A1 (en) * 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
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
US8143244B2 (en) 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
AU2011320651A1 (en) * 2010-10-29 2013-05-02 Merck Canada Inc. HIV integrase inhibitors
WO2012131539A1 (en) 2011-03-31 2012-10-04 Pfizer Inc. Novel bicyclic pyridinones
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
US9493479B2 (en) 2013-04-16 2016-11-15 Merck Sharp & Dohme Corp. Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
KR102000382B1 (ko) 2015-02-03 2019-07-15 화이자 인코포레이티드 신규 시클로프로파벤조푸라닐 피리도피라진디온

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6262055B1 (en) * 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
WO1999062513A1 (en) * 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
US6306891B1 (en) * 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
US6380249B1 (en) * 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
WO2001000578A1 (en) * 1999-06-25 2001-01-04 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
AU1532802A (en) * 2000-10-12 2002-04-22 Merck & Co Inc Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
JP2004517860A (ja) * 2000-10-12 2004-06-17 メルク　エンド　カムパニー　インコーポレーテッド Ｈｉｖインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類
EP1326865B1 (en) * 2000-10-12 2009-05-06 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
AU2002230392A1 (en) * 2000-10-12 2002-05-15 Merck & Co., Inc. AZA-and polyaza-naphthalenyl ketones useful as HIV integrase inhibitors
ATE530520T1 (de) * 2001-08-10 2011-11-15 Shionogi & Co Antivirales mittel
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
EP1467970B1 (en) * 2002-01-17 2007-08-22 Merck & Co., Inc. Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
WO2004004657A2 (en) * 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
PA8586801A1 (es) * 2002-10-31 2005-02-04 Pfizer Inhibidores de hiv-integrasa, composiciones farmaceuticas y metodos para su uso
TW200510425A (en) * 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
AU2005221864A1 (en) * 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa HIV integrase inhibitors
WO2005087768A1 (en) * 2004-03-09 2005-09-22 Merck & Co., Inc. Hiv integrase inhibitors
EP1725535A4 (en) * 2004-03-09 2009-11-25 Merck & Co Inc HIV integrase
DK3187225T3 (da) 2005-04-28 2022-02-28 Viiv Healthcare Co Polycyklisk carbamoylpyridonderivat med hiv-integrasehæmmende aktivitet

Also Published As

Publication number Publication date
US7741315B2 (en) 2010-06-22
US20130178468A1 (en) 2013-07-11
US8293731B2 (en) 2012-10-23
TW200819126A (en) 2008-05-01
WO2006121831A2 (en) 2006-11-16
WO2006121831A3 (en) 2007-10-25
EP1881825A2 (en) 2008-01-30
EP1881825A4 (en) 2011-11-30
US7968564B2 (en) 2011-06-28
US20110275621A1 (en) 2011-11-10
JP2008540529A (ja) 2008-11-20
JP4982482B2 (ja) 2012-07-25
US20090054399A1 (en) 2009-02-26
AU2006244424A1 (en) 2006-11-16
EP1881825B1 (en) 2013-07-24
CA2607151A1 (en) 2006-11-16
AU2006244424B2 (en) 2011-09-22
US20100204201A1 (en) 2010-08-12

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Effective date: 20150505