HRP20050593A2 - Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors - Google Patents

Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors Download PDF

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Publication number
HRP20050593A2
HRP20050593A2 HR20050593A HRP20050593A HRP20050593A2 HR P20050593 A2 HRP20050593 A2 HR P20050593A2 HR 20050593 A HR20050593 A HR 20050593A HR P20050593 A HRP20050593 A HR P20050593A HR P20050593 A2 HRP20050593 A2 HR P20050593A2
Authority
HR
Croatia
Prior art keywords
oxo
hydroxy
amino
fluorobenzyl
tetrahydro
Prior art date
Application number
HR20050593A
Other languages
English (en)
Croatian (hr)
Inventor
Crescenzi Benedetta
Kinzel Olaf
Muraglia Ester
Orvieto Federica
Pescatore Giovanna
Rowley Michael
Summa Vincenzo
Original Assignee
Instituto di Ricerche di Biologia Molecolare P. An
Geletti S.P.A.
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 Instituto di Ricerche di Biologia Molecolare P. An, Geletti S.P.A. filed Critical Instituto di Ricerche di Biologia Molecolare P. An
Publication of HRP20050593A2 publication Critical patent/HRP20050593A2/hr

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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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
HR20050593A 2002-12-27 2003-12-18 Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors HRP20050593A2 (en)

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 (fr) 2002-12-27 2003-12-18 Tetrahydro-4h-pyrido[1,2-a]pyrimidines et composes associes utilises en tant qu'inhibiteurs de l'integrase du vih

Publications (1)

Publication Number Publication Date
HRP20050593A2 true HRP20050593A2 (en) 2006-03-31

Family

ID=32685467

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20050593A HRP20050593A2 (en) 2002-12-27 2003-12-18 Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors

Country Status (20)

Country Link
US (2) US7414045B2 (fr)
EP (1) EP1578748B1 (fr)
JP (1) JP4733986B2 (fr)
KR (1) KR20050087865A (fr)
CN (1) CN100343253C (fr)
AT (1) ATE481401T1 (fr)
AU (2) AU2003292436B2 (fr)
BR (1) BR0317749A (fr)
CA (1) CA2509554C (fr)
DE (1) DE60334248D1 (fr)
EC (1) ECSP055890A (fr)
HR (1) HRP20050593A2 (fr)
IS (1) IS7892A (fr)
MA (1) MA27583A1 (fr)
MX (1) MXPA05007010A (fr)
NO (1) NO20053624L (fr)
NZ (1) NZ540729A (fr)
PL (1) PL377354A1 (fr)
RU (1) RU2329265C2 (fr)
WO (2) WO2004058756A1 (fr)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004062613A2 (fr) * 2003-01-13 2004-07-29 Bristol-Myers Squibb Company Inhibiteurs d'integrase hiv
CN1870896A (zh) * 2003-10-20 2006-11-29 默克公司 用作hiv整合酶抑制剂的羟基吡啶并吡咯并吡嗪二酮化合物
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
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
US7157447B2 (en) 2004-05-28 2007-01-02 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7192948B2 (en) * 2004-05-28 2007-03-20 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
WO2006060225A2 (fr) * 2004-11-23 2006-06-08 Merck & Co., Inc. Processus destine a la synthese asymetrique d'hexahydropyrimido[1,2-a] azepine-2-carboxamides et de composes correspondants
BRPI0518741A2 (pt) * 2004-12-03 2008-12-02 Merck & Co Inc uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
RU2382648C2 (ru) * 2004-12-03 2010-02-27 Мерк Энд Ко., Инк. Фармацевтический состав карбоксамидных ингибиторов интегразы вич, содержащий композицию с контролируемой скоростью высвобождения
EP3165220B2 (fr) * 2004-12-03 2024-11-13 Merck Sharp & Dohme LLC Composition pharmaceutique contenant un agent d'anti-nucléation
WO2006088173A1 (fr) * 2005-02-21 2006-08-24 Shionogi & Co., Ltd. Dérivé de carbamoylpyridone bicyclique ayant une activité d'inhibition de la vih intégrase
WO2006103399A1 (fr) * 2005-03-31 2006-10-05 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Inhibiteurs de l’integrase du vih
DK3187225T3 (da) * 2005-04-28 2022-02-28 Viiv Healthcare Co Polycyklisk carbamoylpyridonderivat med hiv-integrasehæmmende aktivitet
BRPI0613578A2 (pt) 2005-06-30 2012-01-17 Wyeth Corp composito da fórmula i; uso de um composto de fórmula i; e composição farmacêutica
US7494984B2 (en) * 2005-08-31 2009-02-24 Bristol-Myers Squibb Company Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
JP5094725B2 (ja) * 2005-10-04 2012-12-12 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・エルレ・エルレ Hivインテグラーゼ阻害剤
AU2006306355A1 (en) * 2005-10-27 2007-05-03 Merck & Co., Inc. HIV integrase inhibitors
TW200800988A (en) 2005-10-27 2008-01-01 Shionogi & Amp Co Ltd Polycyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
WO2007058646A1 (fr) * 2005-11-15 2007-05-24 Bristol-Myers Squibb Company Inhibiteurs d’integrase du vih : composes cycliques de la pyrimidinone
WO2007059125A2 (fr) * 2005-11-15 2007-05-24 Bristol-Myers Squibb Company Inhibiteurs de l'integrase du vih
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 (fr) * 2005-11-30 2007-06-07 Bristol-Myers Squibb Company Heterocycles bicycliques en tant qu'inhibiteurs de l'integrase du vih
US20070129379A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Hiv integrase inhibitors
WO2007087188A2 (fr) * 2006-01-20 2007-08-02 Merck & Co., Inc. Comprimes et granules au gout masque
WO2007143446A1 (fr) * 2006-05-30 2007-12-13 Bristol-Myers Squibb Company Composés hétérotricycliques spiro-condensés utilisés en tant qu'inhibiteurs de la vih intégrase
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
EP2349276B1 (fr) * 2008-10-06 2019-11-27 Merck Sharp & Dohme Corp. Inhibiteurs de l'intégrase du vih
SG171308A1 (en) * 2008-12-11 2011-07-28 Shionogi & Co 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
PL2448940T3 (pl) * 2009-07-02 2014-10-31 Sanofi Sa Pochodne 6,7,8,9-tetrahydro-pirymido{1,2-a} pirymidyn-4-onu, ich wytwarzanie i zastosowanie farmaceutyczne
WO2011045330A1 (fr) 2009-10-13 2011-04-21 Tibotec Pharmaceuticals Inhibiteurs macrocycliques d'intégrase
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
AU2010313571B2 (en) 2009-10-26 2014-07-31 Merck Sharp & Dohme Llc Solid pharmaceutical compositions containing an integrase inhibitor
WO2011121105A1 (fr) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals Inhibiteurs de l'intégrase macrocyclique
UA112517C2 (uk) * 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
ES2661510T3 (es) 2011-12-15 2018-04-02 Novartis Ag Uso de inhibidores de la actividad o función de PI3K
EP2931730B1 (fr) 2012-12-17 2019-08-07 Merck Sharp & Dohme Corp. Dérivés 4-pyridinonetriazines en tant qu'inhibiteurs de l'intégrase du vih
US9493479B2 (en) 2013-04-16 2016-11-15 Merck Sharp & Dohme Corp. Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
SI2997033T1 (en) 2013-05-17 2018-04-30 Merck Sharp & Dohme Corp. FUZYCLE TRICYCLE HETEROCYCLIC COMPOUNDS AS HIV INTEGRATED INHIBITORS
US9951079B2 (en) 2013-06-13 2018-04-24 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
CA2924829C (fr) 2013-09-27 2019-10-29 Merck Sharp & Dohme Corp. Derives de quinolizine substitues utiles en tant qu'inhibiteurs de l'integrase du vih
WO2016187788A1 (fr) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Composés hétérocycliques tricycliques fusionnés utiles pour traiter l'infection au vih
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
EP3389380B1 (fr) 2015-12-15 2021-07-21 Merck Sharp & Dohme Corp. Dérivés de quinolizine spirocycliques utiles en tant qu'inhibiteurs de l'intégrase du vih
WO2017113288A1 (fr) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Composés hétérocycliques tricycliques condensés utiles en tant qu'inhibiteurs de l'intégrase du vih
WO2018102634A1 (fr) 2016-12-02 2018-06-07 Merck Sharp & Dohme Corp. Composés hétérocycliques tricycliques utiles en tant qu'inhibiteurs de l'intégrase du vih
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)
WO2018140368A1 (fr) 2017-01-26 2018-08-02 Merck Sharp & Dohme Corp. Dérivés de quinolizine substitués utiles en tant qu'inhibiteurs de l'intégrase du vih
EP3805221A4 (fr) 2018-05-31 2022-01-05 Shionogi & Co., Ltd Dérivé de pyridone polycyclique
CR20230571A (es) 2018-05-31 2024-01-22 Shionogi & Co DERIVADO POLICÍCLICO DE CARBAMOILPIRIDONA (divisional 2020-0644)
WO2021107065A1 (fr) 2019-11-28 2021-06-03 塩野義製薬株式会社 Dérivé de pyridopyrazine polycyclique

Family Cites Families (19)

* 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
US6380249B1 (en) * 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
US6262055B1 (en) * 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
WO2001000578A1 (fr) 1999-06-25 2001-01-04 Merck & Co., Inc. 1,3-propanediones-1-(aromatiques ou heteroaromatiques substitutees)-3-(heteroaromatiques substituees) et leur utilisation
DE60131160T2 (de) * 2000-06-07 2008-08-07 Vertex Pharmaceuticals Inc., Cambridge Caspase-inhibitoren und ihre verwendungen
GB0017676D0 (en) * 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
CA2321348A1 (fr) * 2000-09-27 2002-03-27 Blaise Magloire N'zemba Derives aromatiques ayant des proprietes inhibant l'integrase de l'hiv
EP1326865B1 (fr) * 2000-10-12 2009-05-06 Merck & Co., Inc. Aza- et polyaza-naphthalenyl carboxamides utiles comme inhibiteurs de l'integrase du vih
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
AU1532802A (en) 2000-10-12 2002-04-22 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 (fr) * 2001-10-26 2003-05-01 Maria Emilia Di Francesco Inhibiteurs de l'integrase du vih a base de dihydroxypyrimidine carboxamide
EP1467970B1 (fr) 2002-01-17 2007-08-22 Merck & Co., Inc. Carboxamides hydroxynaphthyridinone utiles comme inhibiteurs de l'integrase du vih
WO2004004657A2 (fr) * 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Inhibiteurs de l'integrase du vih
WO2004062613A2 (fr) * 2003-01-13 2004-07-29 Bristol-Myers Squibb Company Inhibiteurs d'integrase hiv
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
KR20050087865A (ko) 2005-08-31
JP2006513200A (ja) 2006-04-20
CN100343253C (zh) 2007-10-17
NZ540729A (en) 2008-03-28
NO20053624D0 (no) 2005-07-26
PL377354A1 (pl) 2006-01-23
NO20053624L (no) 2005-09-26
MXPA05007010A (es) 2005-08-18
US7968553B2 (en) 2011-06-28
CN1753892A (zh) 2006-03-29
EP1578748A1 (fr) 2005-09-28
US20080176869A1 (en) 2008-07-24
US7414045B2 (en) 2008-08-19
BR0317749A (pt) 2005-11-22
AU2003292437A1 (en) 2004-07-22
DE60334248D1 (de) 2010-10-28
AU2003292436A1 (en) 2004-07-22
WO2004058756A1 (fr) 2004-07-15
WO2004058757A1 (fr) 2004-07-15
RU2329265C2 (ru) 2008-07-20
RU2005123807A (ru) 2006-01-20
CA2509554A1 (fr) 2004-07-15
EP1578748B1 (fr) 2010-09-15
ECSP055890A (es) 2005-09-20
IS7892A (is) 2005-06-13
AU2003292436B2 (en) 2009-07-30
MA27583A1 (fr) 2005-10-03
ATE481401T1 (de) 2010-10-15
JP4733986B2 (ja) 2011-07-27
US20060046985A1 (en) 2006-03-02
CA2509554C (fr) 2011-02-01

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