[go: up one dir, main page]

NO20053624L - Tetrahydro-4H-pyrido [1,2-A] pyrimidiner og beslektede forbindelser som er anvendbare som HIV-integrase inhibitorer - Google Patents

Tetrahydro-4H-pyrido [1,2-A] pyrimidiner og beslektede forbindelser som er anvendbare som HIV-integrase inhibitorer

Info

Publication number
NO20053624L
NO20053624L NO20053624A NO20053624A NO20053624L NO 20053624 L NO20053624 L NO 20053624L NO 20053624 A NO20053624 A NO 20053624A NO 20053624 A NO20053624 A NO 20053624A NO 20053624 L NO20053624 L NO 20053624L
Authority
NO
Norway
Prior art keywords
compounds
pyrido
pyrimidines
tetrahydro
hiv
Prior art date
Application number
NO20053624A
Other languages
English (en)
Other versions
NO20053624D0 (no
Inventor
Benedetta Crescenzi
Ester Muraglia
Giovanna Pescatore
Michael Rowley
Vincenzo Summa
Olaf Kinzel
Frederica Orvieto
Original Assignee
Angeletti P Ist Richerche Bio
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 Angeletti P Ist Richerche Bio filed Critical Angeletti P Ist Richerche Bio
Publication of NO20053624D0 publication Critical patent/NO20053624D0/no
Publication of NO20053624L publication Critical patent/NO20053624L/no

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Tetrahydro-4H-pyrido[ 1,2-a]pyrimidiner og beslektede forbinder av Formel (I) er beskrevet som inhibitorer av HIV-integrase og inhibitorer av HIV-replikasjon, hvori n er et heltall lik 0, 1 eller 2, og R1, R3, R4, R12 og R14 er som her definert.
NO20053624A 2002-12-27 2005-07-26 Tetrahydro-4H-pyrido [1,2-A] pyrimidiner og beslektede forbindelser som er anvendbare som HIV-integrase inhibitorer NO20053624L (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US43683002P 2002-12-27 2002-12-27
US52877603P 2003-12-12 2003-12-12
PCT/GB2003/005543 WO2004058757A1 (en) 2002-12-27 2003-12-18 Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
NO20053624D0 NO20053624D0 (no) 2005-07-26
NO20053624L true NO20053624L (no) 2005-09-26

Family

ID=32685467

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20053624A NO20053624L (no) 2002-12-27 2005-07-26 Tetrahydro-4H-pyrido [1,2-A] pyrimidiner og beslektede forbindelser som er anvendbare som HIV-integrase inhibitorer

Country Status (20)

Country Link
US (2) US7414045B2 (no)
EP (1) EP1578748B1 (no)
JP (1) JP4733986B2 (no)
KR (1) KR20050087865A (no)
CN (1) CN100343253C (no)
AT (1) ATE481401T1 (no)
AU (2) AU2003292436B2 (no)
BR (1) BR0317749A (no)
CA (1) CA2509554C (no)
DE (1) DE60334248D1 (no)
EC (1) ECSP055890A (no)
HR (1) HRP20050593A2 (no)
IS (1) IS7892A (no)
MA (1) MA27583A1 (no)
MX (1) MXPA05007010A (no)
NO (1) NO20053624L (no)
NZ (1) NZ540729A (no)
PL (1) PL377354A1 (no)
RU (1) RU2329265C2 (no)
WO (2) WO2004058757A1 (no)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7135467B2 (en) * 2003-01-13 2006-11-14 Bristol-Myers Squibb Company HIV integrase inhibitors
EP1677599A4 (en) * 2003-10-20 2008-10-22 Merck & Co Inc HYDROXYPYRIDOPYRROLOPYRAZINDION COMPOUNDS 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
US7273859B2 (en) 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
US7192948B2 (en) 2004-05-28 2007-03-20 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7157447B2 (en) 2004-05-28 2007-01-02 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7173022B2 (en) 2004-05-28 2007-02-06 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7176196B2 (en) 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
WO2006060225A2 (en) * 2004-11-23 2006-06-08 Merck & Co., Inc. Process for asymmetric synthesis of hexahydropyrimido[1,2-a] azepine-2-carboxamides and related compounds
CA2588466A1 (en) * 2004-12-03 2006-06-08 Merck & Co., Inc. Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1
CN101068550B (zh) 2004-12-03 2011-03-30 默沙东公司 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
EP3165220B2 (en) * 2004-12-03 2024-11-13 Merck Sharp & Dohme LLC Pharmaceutical composition containing an anti-nucleating agent
JP5317257B2 (ja) * 2005-02-21 2013-10-16 塩野義製薬株式会社 Hivインテグラーゼ阻害活性を有する2環性カルバモイルピリドン誘導体
CN101146811B (zh) * 2005-03-31 2012-01-11 P.安杰莱蒂分子生物学研究所 Hiv整合酶抑制剂
ES2567197T3 (es) * 2005-04-28 2016-04-20 Viiv Healthcare Company Derivado de carbamoilpiridona policíclico que tiene actividad inhibidora de la integrasa del VIH
JP2009500329A (ja) 2005-06-30 2009-01-08 ワイス アミノ−5−(6員)ヘテロアリールイミダゾロン化合物およびβ−セレクターゼ調節のためのその使用
US7494984B2 (en) * 2005-08-31 2009-02-24 Bristol-Myers Squibb Company Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
WO2007039218A1 (en) * 2005-10-04 2007-04-12 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
JP5131689B2 (ja) * 2005-10-27 2013-01-30 塩野義製薬株式会社 Hivインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体
US20090312335A1 (en) * 2005-10-27 2009-12-17 John S Wai Hiv Integrase Inhibitors
WO2007058646A1 (en) * 2005-11-15 2007-05-24 Bristol-Myers Squibb Company Hiv integrase inhibitors: cyclic pyrimidinone compounds
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
WO2007064316A1 (en) * 2005-11-30 2007-06-07 Bristol-Myers Squibb Company Bicyclic heterocycles as hiv integrase inhibitors
US20070129379A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Hiv integrase inhibitors
WO2007087188A2 (en) * 2006-01-20 2007-08-02 Merck & Co., Inc. Taste-masked tablets and granules
US7897593B2 (en) 2006-05-30 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
US7893055B2 (en) * 2006-06-28 2011-02-22 Bristol-Myers Squibb Company 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
US8513234B2 (en) * 2008-10-06 2013-08-20 Merck Sharp & Dohme Corp. HIV integrase inhibitors
US8624023B2 (en) * 2008-12-11 2014-01-07 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
HRP20140786T1 (hr) * 2009-07-02 2014-11-07 Sanofi DERIVATI 6,7,8,9-TETRAHIDROPIRIMIDO[1,2-a]PIRIMIDIN-4-ONA, NJIHOVO DOBIVANJE I NJIHOVA FARMACEUTSKA UPOTREBA
MX2012004426A (es) 2009-10-13 2012-07-30 Elanco Animal Health Ireland Inhibidores macrociclicos de integrasa.
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
JP6122639B2 (ja) 2009-10-26 2017-04-26 メルク・シャープ・エンド・ドーム・コーポレイション インテグラーゼ阻害剤を含有する固形医薬組成物
JP5739517B2 (ja) 2010-04-02 2015-06-24 ヤンセン・アールアンドデイ・アイルランド 大環状インテグラーゼ阻害剤
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
DK2790705T3 (en) 2011-12-15 2018-03-12 Novartis Ag Use of inhibitors of the activity or function of PI3K
WO2014099586A1 (en) 2012-12-17 2014-06-26 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
WO2014183532A1 (en) 2013-05-17 2014-11-20 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
US9951079B2 (en) 2013-06-13 2018-04-24 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
EA030695B1 (ru) 2013-09-27 2018-09-28 Мерк Шарп И Доум Корп. Замещенные производные хинолизина, которые можно использовать как ингибиторы интегразы вич
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
CN110062627A (zh) 2016-12-02 2019-07-26 默沙东公司 可用作hiv整合酶抑制剂的三环杂环化合物
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)
EP3573984A4 (en) 2017-01-26 2020-07-29 Merck Sharp & Dohme Corp. USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
KR20250002769A (ko) 2018-05-31 2025-01-07 시오노기 앤드 컴파니, 리미티드 다환성 카바모일피리돈 유도체
AU2019277547B2 (en) 2018-05-31 2024-10-10 Shionogi & Co., Ltd. Polycyclic pyridone derivative

Family Cites Families (19)

* 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
US6380249B1 (en) * 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
US6306891B1 (en) * 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
EP1196384A4 (en) 1999-06-25 2002-10-23 Merck & Co Inc 1- (AROMATIC OR HETEROAROMATICALLY SUBSTITUTED) -3- (HETEROAROMATICALLY SUBSTITUTED) -1,3-PROPANDIONS AND THEIR APPLICATIONS
IL152845A0 (en) * 2000-06-07 2003-06-24 Vertex Pharma Fused heterocyclic compounds and pharmaceutical compositions containing the same
GB0017676D0 (en) * 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
CA2321348A1 (en) * 2000-09-27 2002-03-27 Blaise Magloire N'zemba Aromatic derivatives with hiv integrase inhibitory properties
US6841558B2 (en) 2000-10-12 2005-01-11 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as HIV intergrase inhibitors
HUP0302367A2 (hu) * 2000-10-12 2003-11-28 Merck & Co., Inc. HIV Integráz inhibitorokként hasznos aza- és poliazanaftalenil-karboxamidok, ezeket tartalmazó gyógyszerkészítmények
WO2002036734A2 (en) 2000-10-12 2002-05-10 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
WO2002030426A1 (en) 2000-10-12 2002-04-18 Merck & Co., Inc. Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
EP2181985B1 (en) 2001-08-10 2011-10-26 Shionogi & Co., Ltd. Antiviral Agent
HRP20040373B1 (en) 2001-10-26 2012-09-30 Instituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
CA2463975A1 (en) * 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
CA2472372C (en) * 2002-01-17 2010-08-17 Melissa Egbertson Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
AU2003248872A1 (en) * 2002-07-09 2004-01-23 Bristol-Myers Squibb Company Hiv integrase inhibitors
US7135467B2 (en) * 2003-01-13 2006-11-14 Bristol-Myers Squibb Company HIV integrase inhibitors
US7037908B2 (en) * 2003-04-24 2006-05-02 Bristol-Myers Squibb Company 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

Also Published As

Publication number Publication date
WO2004058756A1 (en) 2004-07-15
IS7892A (is) 2005-06-13
MXPA05007010A (es) 2005-08-18
MA27583A1 (fr) 2005-10-03
CN100343253C (zh) 2007-10-17
CN1753892A (zh) 2006-03-29
BR0317749A (pt) 2005-11-22
ATE481401T1 (de) 2010-10-15
RU2005123807A (ru) 2006-01-20
JP2006513200A (ja) 2006-04-20
KR20050087865A (ko) 2005-08-31
EP1578748A1 (en) 2005-09-28
AU2003292437A1 (en) 2004-07-22
ECSP055890A (es) 2005-09-20
CA2509554C (en) 2011-02-01
HRP20050593A2 (en) 2006-03-31
RU2329265C2 (ru) 2008-07-20
US20080176869A1 (en) 2008-07-24
US7968553B2 (en) 2011-06-28
WO2004058757A1 (en) 2004-07-15
NO20053624D0 (no) 2005-07-26
JP4733986B2 (ja) 2011-07-27
CA2509554A1 (en) 2004-07-15
DE60334248D1 (de) 2010-10-28
NZ540729A (en) 2008-03-28
AU2003292436B2 (en) 2009-07-30
US20060046985A1 (en) 2006-03-02
PL377354A1 (pl) 2006-01-23
US7414045B2 (en) 2008-08-19
AU2003292436A1 (en) 2004-07-22
EP1578748B1 (en) 2010-09-15

Similar Documents

Publication Publication Date Title
NO20053624L (no) Tetrahydro-4H-pyrido [1,2-A] pyrimidiner og beslektede forbindelser som er anvendbare som HIV-integrase inhibitorer
NO2020026I1 (no) Raltegravir eller et farmasøytisk akseptabelt salt derav, spesielt kaliumsaltet
DK1441734T3 (da) Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
WO2005086700A3 (en) Hiv integrase inhibitors
WO2006103399A8 (en) Hiv integrase inhibitors
WO2007146230A3 (en) Non-nucleoside reverse transcriptase inhibitors
WO2004024078A3 (en) Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
WO2005120516A3 (en) Hiv integrase inhibitors
WO2007050510A3 (en) Hiv integrase inhibitors
ATE517899T1 (de) Hiv-integrasehemmer
WO2004047725A3 (en) 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors
WO2007002458A3 (en) Non-nucleoside reverse transcriptase inhibitors
WO2007002368A3 (en) Non-nucleoside reverse transcriptase inhibitors

Legal Events

Date Code Title Description
FC2A Withdrawal, rejection or dismissal of laid open patent application