CA2498566A1 - 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors - Google Patents

8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors Download PDF

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Publication number
CA2498566A1
CA2498566A1 CA002498566A CA2498566A CA2498566A1 CA 2498566 A1 CA2498566 A1 CA 2498566A1 CA 002498566 A CA002498566 A CA 002498566A CA 2498566 A CA2498566 A CA 2498566A CA 2498566 A1 CA2498566 A1 CA 2498566A1
Authority
CA
Canada
Prior art keywords
alkyl
haloalkyl
independently
substituents
optionally substituted
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.)
Abandoned
Application number
CA002498566A
Other languages
English (en)
French (fr)
Inventor
John S. Wai
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.)
Merck and Co Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2498566A1 publication Critical patent/CA2498566A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • AIDS & HIV (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)
CA002498566A 2002-09-11 2003-09-10 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors Abandoned CA2498566A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40974502P 2002-09-11 2002-09-11
US60/409,745 2002-09-11
PCT/US2003/028363 WO2004047725A2 (en) 2002-09-11 2003-09-10 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors

Publications (1)

Publication Number Publication Date
CA2498566A1 true CA2498566A1 (en) 2004-06-10

Family

ID=32393259

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002498566A Abandoned CA2498566A1 (en) 2002-09-11 2003-09-10 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors

Country Status (7)

Country Link
US (1) US7399763B2 (https=)
EP (1) EP1539714B1 (https=)
JP (1) JP2005538184A (https=)
AT (1) ATE404563T1 (https=)
CA (1) CA2498566A1 (https=)
DE (1) DE60322919D1 (https=)
WO (1) WO2004047725A2 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2498111A1 (en) * 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
CA2542047A1 (en) * 2003-10-20 2005-05-12 Merck & Co., Inc. Hydroxy pyridopyrrolopyrazine dione compounds useful as hiv integrase inhibitors
ES2529038T3 (es) * 2004-05-07 2015-02-16 Merck Sharp & Dohme Corp. Inhibidores de la integrasa de VIH
US7476666B2 (en) 2004-06-09 2009-01-13 Merck & Co., Inc. HIV integrase inhibitors
US20080280849A1 (en) * 2005-06-01 2008-11-13 Herve Leh Synergic Combinations Comprising a Quinoline Compound and Other Hiv Infection Therapeutic Agents
JP2009513640A (ja) * 2005-10-27 2009-04-02 メルク エンド カムパニー インコーポレーテッド Ｈｉｖインテグラーゼインヒビター
WO2010031816A1 (en) 2008-09-19 2010-03-25 Nerviano Medical Sciences S.R.L. 3,4 DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES
PE20130010A1 (es) 2010-02-26 2013-02-05 Japan Tobacco Inc Derivado de 1,3,4,8-tetrahidro-2h-pirido[1,2-a]pirazina como inhibidor de la integrasa del vih
EP2841417A1 (en) 2012-04-26 2015-03-04 Francis Xavier Tavares Synthesis of lactams
JP7106462B2 (ja) * 2016-07-01 2022-07-26 ジー１ セラピューティクス， インコーポレイテッド Ｎ－（ヘテロアリール）－ピロロ［３，２－ｄ］ピリミジン－２－アミンの合成
RS67557B1 (sr) 2018-08-24 2026-01-30 Pharmacosmos Holding As Unapređena sinteza 1,4-diazaspiro[5.5]undekan-3-ona

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL101860A0 (en) * 1991-05-31 1992-12-30 Ici Plc Heterocyclic derivatives
US5821241A (en) * 1994-02-22 1998-10-13 Merck & Co., Inc. Fibrinogen receptor antagonists
WO2000000478A1 (en) * 1998-06-26 2000-01-06 Bristol-Myers Squibb Pharma Company Substituted quinoxalin-2(1h)-ones useful as hiv reverse transcriptase inhibitors
CA2425440C (en) 2000-10-12 2010-04-13 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
JP2004513134A (ja) * 2000-10-12 2004-04-30 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−ナフタレニルケトン類
US6919351B2 (en) * 2000-10-12 2005-07-19 Merck & Co., Inc. Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors
NZ533057A (en) 2001-10-26 2005-11-25 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
EP1441734B1 (en) 2001-10-26 2007-02-28 Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
CA2498111A1 (en) * 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors

Also Published As

Publication number Publication date
EP1539714A4 (en) 2007-04-25
US20050288293A1 (en) 2005-12-29
EP1539714A2 (en) 2005-06-15
EP1539714B1 (en) 2008-08-13
ATE404563T1 (de) 2008-08-15
US7399763B2 (en) 2008-07-15
WO2004047725A3 (en) 2004-09-30
AU2003302382A1 (en) 2004-06-18
WO2004047725A2 (en) 2004-06-10
JP2005538184A (ja) 2005-12-15
DE60322919D1 (de) 2008-09-25

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued