CA2557926A1 - Hiv integrase inhibitors - Google Patents

Hiv integrase inhibitors Download PDF

Info

Publication number
CA2557926A1
CA2557926A1 CA002557926A CA2557926A CA2557926A1 CA 2557926 A1 CA2557926 A1 CA 2557926A1 CA 002557926 A CA002557926 A CA 002557926A CA 2557926 A CA2557926 A CA 2557926A CA 2557926 A1 CA2557926 A1 CA 2557926A1
Authority
CA
Canada
Prior art keywords
alkyl
ring
hydroxy
fluorobenzyl
atom
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
CA002557926A
Other languages
English (en)
French (fr)
Inventor
Monica Donghi
Cristina Gardelli
Philip Jones
Vincenzo Summa
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.)
Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34961192&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2557926(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Individual filed Critical Individual
Publication of CA2557926A1 publication Critical patent/CA2557926A1/en
Abandoned 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed 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
    • 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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/16—Peri-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA002557926A 2004-03-09 2005-03-01 Hiv integrase inhibitors Abandoned CA2557926A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US55160104P 2004-03-09 2004-03-09
US60/551,601 2004-03-09
PCT/GB2005/000746 WO2005087766A1 (en) 2004-03-09 2005-03-01 Hiv integrase inhibitors

Publications (1)

Publication Number Publication Date
CA2557926A1 true CA2557926A1 (en) 2005-09-22

Family

ID=34961192

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002557926A Abandoned CA2557926A1 (en) 2004-03-09 2005-03-01 Hiv integrase inhibitors

Country Status (7)

Country Link
US (2) US20070161639A1 (https=)
EP (1) EP1725554A1 (https=)
JP (1) JP2007528379A (https=)
CN (1) CN1930161A (https=)
AU (1) AU2005221864A1 (https=)
CA (1) CA2557926A1 (https=)
WO (1) WO2005087766A1 (https=)

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* Cited by examiner, † Cited by third party
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TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
JP4625838B2 (ja) * 2004-03-09 2011-02-02 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖインテグラーゼ阻害薬
US7820680B2 (en) * 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
CN101014574A (zh) * 2004-03-09 2007-08-08 默克公司 Hiv整合酶抑制剂
WO2006066414A1 (en) * 2004-12-23 2006-06-29 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase
KR101363875B1 (ko) 2005-04-28 2014-02-21 시오노기세야쿠 가부시키가이샤 Ｈｉｖ 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체
WO2006121831A2 (en) * 2005-05-10 2006-11-16 Merck & Co., Inc. Hiv integrase inhibitors
EP1906971A2 (en) * 2005-07-27 2008-04-09 Gilead Sciences, Inc. Antiviral compounds
US7939537B2 (en) * 2005-10-04 2011-05-10 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. HIV integrase inhibitors
AU2006306355A1 (en) * 2005-10-27 2007-05-03 Merck & Co., Inc. HIV integrase inhibitors
MX2008005137A (es) 2005-10-27 2008-09-29 Shionogi & Co Derivado de carbamoilpiridona policiclica que tiene actividad inhibidora en vih integrasa.
WO2008048538A1 (en) * 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
WO2010011814A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
CN102245572B (zh) 2008-12-11 2015-03-25 盐野义制药株式会社 氨甲酰基吡啶酮hiv整合酶抑制剂的方法和中间体
KR101733625B1 (ko) 2008-12-11 2017-05-10 시오노기세야쿠 가부시키가이샤 카르바모일피리돈 ｈｉｖ 인테그라제 억제제 및 중간체의 합성
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
US8927710B2 (en) 2009-06-15 2015-01-06 Shionogi & Co., Ltd. Substituted polycyclic carbamoylpyridone derivative
ES2446720T3 (es) 2009-10-13 2014-03-10 Elanco Animal Health Ireland Limited Inhibidores de la integrasa macrocíclica
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
CA2789457A1 (en) 2010-02-26 2011-09-01 Susumu Miyazaki 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor
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
WO2011121105A1 (en) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
DK2620436T3 (en) 2010-09-24 2018-07-30 Shionogi & Co Substituted polycyclic carbamoylpyridone derivative prodrug
ES3018133T3 (en) 2011-11-30 2025-05-14 Univ Emory Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
WO2013102142A1 (en) 2011-12-28 2013-07-04 Global Blood Therapeutics, Inc. Substituted benzaldehyde compounds and methods for their use in increasing tissue oxygenation
HK1203412A1 (en) 2011-12-28 2015-10-30 Global Blood Therapeutics, Inc. Substituted heteroaryl aldehyde compounds and methods for their use in increasing tissue oxygenation
CA2894642A1 (en) 2013-01-08 2014-07-17 Savira Pharmaceuticals Gmbh Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
US10266551B2 (en) 2013-03-15 2019-04-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9802900B2 (en) 2013-03-15 2017-10-31 Global Blood Therapeutics, Inc. Bicyclic heteroaryl compounds and uses thereof for the modulation of hemoglobin
US20140274961A1 (en) 2013-03-15 2014-09-18 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9422279B2 (en) 2013-03-15 2016-08-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
WO2014145040A1 (en) 2013-03-15 2014-09-18 Global Blood Therapeutics, Inc. Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation
EP3919056B1 (en) 2013-03-15 2024-08-28 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
AP2015008718A0 (en) 2013-03-15 2015-09-30 Global Blood Therapeutics Inc Compounds and uses thereof for the modulation of hemoglobin
SG10201802911RA (en) 2013-03-15 2018-05-30 Global Blood Therapeutics Inc Compounds and uses thereof for the modulation of hemoglobin
US9604999B2 (en) 2013-03-15 2017-03-28 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US8952171B2 (en) 2013-03-15 2015-02-10 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9458139B2 (en) 2013-03-15 2016-10-04 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9493479B2 (en) 2013-04-16 2016-11-15 Merck Sharp & Dohme Corp. Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
RS56701B1 (sr) * 2013-05-17 2018-03-30 Merck Sharp & Dohme Fuzionisana triciklična heterociklična jedinjenja kao inhibitori hiv integraze
MX377396B (es) 2013-09-12 2025-03-10 Janssen Biopharma Inc Compuestos de azapiridona y usos de los mismos.
UA117499C2 (uk) * 2013-09-27 2018-08-10 Мерк Шарп Енд Доум Корп. Заміщені похідні хінолізину, які можна використовувати як інгібітори інтегрази віл
EA202092627A1 (ru) 2013-11-18 2021-09-30 Глобал Блад Терапьютикс, Инк. Соединения и их применения для модуляции гемоглобина
WO2015089847A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
ES2860648T5 (es) 2014-02-07 2024-11-27 Global Blood Therapeutics Inc Polimorfos cristalinos de la base libre de 2-hidroxi-6-((2-(1-isopropil-1H-pirazol-5-il)piridin-3-il)metoxi)benzaldehído
CN107074880A (zh) * 2014-07-07 2017-08-18 萨维拉制药有限公司 二氢吡啶并吡嗪‑1,8‑二酮和它们在治疗、改善或预防病毒疾病中的用途
EP3166943A1 (en) * 2014-07-07 2017-05-17 Savira Pharmaceuticals GmbH Pyridopyrazine compounds and their use in the treatment, amelioration or prevention of influenza
MA41841A (fr) 2015-03-30 2018-02-06 Global Blood Therapeutics Inc Composés aldéhyde pour le traitement de la fibrose pulmonaire, de l'hypoxie, et de maladies auto-immunes et des tissus conjonctifs
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
US11020382B2 (en) 2015-12-04 2021-06-01 Global Blood Therapeutics, Inc. Dosing regimens for 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
WO2017109088A1 (en) 2015-12-23 2017-06-29 Savira Pharmaceuticals Gmbh Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
WO2017113288A1 (en) * 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
CN105418609B (zh) * 2015-12-31 2017-06-23 山东大学 4‑(1,2,3‑三氮唑取代苯胺基)‑吡啶骈嘧啶酮衍生物及其制备方法与应用
ES2881776T3 (es) 2016-03-08 2021-11-30 Novartis Ag Compuestos tricíclicos útiles para tratar las infecciones por ortomixovirus
WO2017158147A1 (en) 2016-03-18 2017-09-21 Savira Pharmaceuticals Gmbh Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
WO2017158151A1 (en) 2016-03-18 2017-09-21 Savira Pharmaceuticals Gmbh Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
TWI825524B (zh) 2016-05-12 2023-12-11 美商全球血液治療公司 用於合成2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)-吡啶-3-基)甲氧基)苯甲醛之方法
JOP20170169A1 (ar) 2016-08-29 2019-01-30 Novartis Ag مركبات بيريدازين ثلاثية الحلقة مندمجة تفيد في علاج العدوى بفيروس أورثوميكسو
TW202332423A (zh) 2016-10-12 2023-08-16 美商全球血液治療公司 包含2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)吡啶-3-基)甲氧基)-苯甲醛之片劑
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)
CN107382963A (zh) * 2017-07-25 2017-11-24 威海迪素制药有限公司 一种奥美拉唑杂质的制备方法
CN118878544A (zh) 2018-02-28 2024-11-01 诺华股份有限公司 作为正粘病毒复制抑制剂用于治疗流感的化合物
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WO2020221294A1 (zh) * 2019-04-30 2020-11-05 上海拓界生物医药科技有限公司 桥环-3,4-二氢-吡啶并[1,2-a]吡嗪-1,8-二酮化合物及其药物用途
US20200398978A1 (en) 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
CN114426540B (zh) * 2020-10-29 2024-04-26 上海拓界生物医药科技有限公司 吡啶并[1,2-a]吡嗪-1,8-二酮类前药衍生物、其制备方法及其应用

Family Cites Families (18)

* 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
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
AU5880600A (en) 1999-06-25 2001-01-31 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
ATE345129T1 (de) 2000-10-12 2006-12-15 Merck & Co Inc Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
WO2002036734A2 (en) 2000-10-12 2002-05-10 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
PL360944A1 (en) * 2000-10-12 2004-09-20 Merck & Co, Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
EP1326611B1 (en) 2000-10-12 2007-06-13 Merck & Co., Inc. Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
ES2572030T3 (es) 2001-08-10 2017-07-19 Shionogi & Co., Ltd. Agente antiviral
ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
IL161337A0 (en) 2001-10-26 2004-09-27 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone 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
TW200510425A (en) * 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
CN101014574A (zh) * 2004-03-09 2007-08-08 默克公司 Hiv整合酶抑制剂
JP4625838B2 (ja) * 2004-03-09 2011-02-02 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖインテグラーゼ阻害薬
US7820680B2 (en) * 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
WO2006066414A1 (en) * 2004-12-23 2006-06-29 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase

Also Published As

Publication number Publication date
US20070161639A1 (en) 2007-07-12
US20090099168A1 (en) 2009-04-16
AU2005221864A1 (en) 2005-09-22
JP2007528379A (ja) 2007-10-11
WO2005087766A1 (en) 2005-09-22
EP1725554A1 (en) 2006-11-29
CN1930161A (zh) 2007-03-14

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EEER Examination request
FZDE Discontinued