CA2557785A1 - Hiv integrase inhibitors - Google Patents

Hiv integrase inhibitors Download PDF

Info

Publication number
CA2557785A1
CA2557785A1 CA002557785A CA2557785A CA2557785A1 CA 2557785 A1 CA2557785 A1 CA 2557785A1 CA 002557785 A CA002557785 A CA 002557785A CA 2557785 A CA2557785 A CA 2557785A CA 2557785 A1 CA2557785 A1 CA 2557785A1
Authority
CA
Canada
Prior art keywords
alkyl
optionally substituted
pyrazino
fluorobenzyl
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.)
Abandoned
Application number
CA002557785A
Other languages
English (en)
French (fr)
Inventor
Peter D. Williams
John S. Wai
Mark W. Embrey
Donnette D. Staas
Linghang Zhuang
H. Marie Langford
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 CA2557785A1 publication Critical patent/CA2557785A1/en
Abandoned legal-status Critical Current

Links

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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • 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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA002557785A 2004-03-09 2005-03-04 Hiv integrase inhibitors Abandoned CA2557785A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US55160204P 2004-03-09 2004-03-09
US60/551,602 2004-03-09
PCT/US2005/006916 WO2005092099A1 (en) 2004-03-09 2005-03-04 Hiv integrase inhibitors

Publications (1)

Publication Number Publication Date
CA2557785A1 true CA2557785A1 (en) 2005-10-06

Family

ID=35055916

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002557785A Abandoned CA2557785A1 (en) 2004-03-09 2005-03-04 Hiv integrase inhibitors

Country Status (7)

Country Link
US (1) US7820680B2 (https=)
EP (1) EP1725102A4 (https=)
JP (1) JP2007528394A (https=)
CN (1) CN1929737A (https=)
AU (1) AU2005227258A1 (https=)
CA (1) CA2557785A1 (https=)
WO (1) WO2005092099A1 (https=)

Families Citing this family (25)

* 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
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
EP1725556A1 (en) * 2004-03-09 2006-11-29 Merck & Co., Inc. Hiv integrase inhibitors
WO2005087766A1 (en) * 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
JP2007528396A (ja) * 2004-03-09 2007-10-11 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
US8129385B2 (en) 2005-04-28 2012-03-06 Shionogi & Co., Ltd. Substituted 5-hydroxy-3,4,6,9,9a, 10-hexanhydro-2h-1-oxa04a,8a-diaza-anthracene-6,10-dioness
KR20110022620A (ko) 2008-05-30 2011-03-07 다케다 야쿠힌 고교 가부시키가이샤 복소환 화합물
EP2320909B8 (en) 2008-07-25 2016-03-30 VIIV Healthcare Company Chemical compounds
WO2010011819A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
CA2744019C (en) 2008-12-11 2017-03-14 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
KR101682058B1 (ko) 2008-12-11 2016-12-02 비이브 헬쓰케어 컴퍼니 카르바모일피리돈 ｈｉｖ 인테그라제 억제제를 위한 제조방법 및 중간체
TWI518084B (zh) 2009-03-26 2016-01-21 鹽野義製藥股份有限公司 哌喃酮與吡啶酮衍生物之製造方法
LT2444400T (lt) 2009-06-15 2018-06-11 Shionogi & Co., Ltd. Pakeistasis policiklinis karbamoilpiridono darinys
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
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
TWI582097B (zh) 2010-03-23 2017-05-11 Ｖｉｉｖ醫療保健公司 製備胺甲醯吡啶酮衍生物及中間體之方法
JP5903718B2 (ja) * 2010-08-09 2016-04-13 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル Ｈｉｖ−１感染の処置のための方法及び医薬的組成物
MX2013003139A (es) 2010-09-24 2013-06-18 Shionogi & Co Profarmaco de derivado de carbamoilpiridona policiclica substituida.
EP2691393B1 (en) 2011-03-31 2016-09-14 Pfizer Inc Novel bicyclic pyridinones
EP4556010A3 (en) 2011-11-30 2025-07-23 Emory University Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
CN102775371B (zh) * 2012-07-26 2015-01-21 山东大学 一种取代噻二嗪类衍生物及其制备方法与应用
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
AU2014267951A1 (en) 2013-05-17 2015-11-19 Merck Sharp & Dohme Corp. Fused Tricyclic Heterocyclic compounds as HIV integrase inhibitors
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
TW201726678A (zh) 2015-10-30 2017-08-01 赫孚孟拉羅股份公司 嘧啶酮衍生物及其於治療、改善或預防病毒性疾病之用途

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6306891B1 (en) * 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
US6262055B1 (en) * 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
US6380249B1 (en) * 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
US6187000B1 (en) * 1998-08-20 2001-02-13 Endius Incorporated Cannula for receiving surgical instruments
JP2003503386A (ja) * 1999-06-25 2003-01-28 メルク エンド カムパニー インコーポレーテッド １−（芳香族またはヘテロ芳香族置換）−３−（ヘテロ芳香族置換）−１，３−プロパンジオン類およびそれの使用
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
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
US6919351B2 (en) * 2000-10-12 2005-07-19 Merck & Co., Inc. Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors
BR0211750A (pt) 2001-08-10 2004-10-13 Shionogi & Co Agente antiviral
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
EP1467970B1 (en) * 2002-01-17 2007-08-22 Merck & Co., Inc. Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
US7109186B2 (en) * 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
US7169497B2 (en) * 2003-05-15 2007-01-30 The Gillette Company Electrochemical cells
TW200510425A (en) * 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
JP2007528396A (ja) * 2004-03-09 2007-10-11 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
WO2005087766A1 (en) * 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
EP1725556A1 (en) * 2004-03-09 2006-11-29 Merck & Co., Inc. Hiv integrase inhibitors
PT1729810T (pt) * 2004-04-02 2018-11-22 Swedish Orphan Biovitrum Ab Publ Métodos de redução da agregação de il-ira
CA2607151C (en) * 2005-05-10 2012-06-19 Merck & Co., Inc. Hiv integrase inhibitors

Also Published As

Publication number Publication date
US7820680B2 (en) 2010-10-26
AU2005227258A1 (en) 2005-10-06
US20080009490A1 (en) 2008-01-10
EP1725102A4 (en) 2009-04-29
CN1929737A (zh) 2007-03-14
EP1725102A1 (en) 2006-11-29
JP2007528394A (ja) 2007-10-11
WO2005092099A1 (en) 2005-10-06

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued