MA27583A1 - Tetrahydro-4h-pyrido [1,2-a] pyrimidines et les composes apparentes utiles comme inhibiteurs de l'integrase du vih. - Google Patents

Tetrahydro-4h-pyrido [1,2-a] pyrimidines et les composes apparentes utiles comme inhibiteurs de l'integrase du vih.

Info

Publication number
MA27583A1
MA27583A1 MA28407A MA28407A MA27583A1 MA 27583 A1 MA27583 A1 MA 27583A1 MA 28407 A MA28407 A MA 28407A MA 28407 A MA28407 A MA 28407A MA 27583 A1 MA27583 A1 MA 27583A1
Authority
MA
Morocco
Prior art keywords
inhibitors
compounds
pyrido
pyrimidines
tetrahydro
Prior art date
Application number
MA28407A
Other languages
English (en)
Inventor
Benedetta Crescenzi
Olaf Kinzel
Ester Muraglia
Federica Orvieto
Giovanna Pescatore
Michael Rowley
Vincenzo Summa
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 MA27583A1 publication Critical patent/MA27583A1/fr

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
    • 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

Landscapes

  • 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)

Abstract

EXTRAIT DE LA DESCRIPTION Tétrahydro-4H-pyrido[l,2-a]pyrimidines et les composés apparentés de la Formule I: sont décrits comme inhibiteurs de l'intégrase du VIH et comme inhibiteurs de la réplication du VTH, oé n est un nombre entier égal à zéro, 1 ou 2, et R1, R3, R4, Rl2 et Rl4 sont définis dans ces présentes. Ces composés sont utiles dans la prévention et le traitement d'infection par le VIH et dans la prévention, le retardement du déclenchement, et le traitement du SIDA. Les composés sont utilisés contre l'infection par le VTH et le SIDA comme composés per se ou sous la forme de sels pharmaceutiquement acceptables. Les composés et leurs sels peuvent être utilisés comme ingrédients dans des compositions pharmaceutiques, facultativement en combinaison avec d'autres antiviraux, immunomodulateurs, antibiotiques ou vaccins.
MA28407A 2002-12-27 2005-07-21 Tetrahydro-4h-pyrido [1,2-a] pyrimidines et les composes apparentes utiles comme inhibiteurs de l'integrase du vih. MA27583A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US43683002P 2002-12-27 2002-12-27
US52877603P 2003-12-12 2003-12-12

Publications (1)

Publication Number Publication Date
MA27583A1 true MA27583A1 (fr) 2005-10-03

Family

ID=32685467

Family Applications (1)

Application Number Title Priority Date Filing Date
MA28407A MA27583A1 (fr) 2002-12-27 2005-07-21 Tetrahydro-4h-pyrido [1,2-a] pyrimidines et les composes apparentes utiles comme inhibiteurs de l'integrase du vih.

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
HRP20050593A2 (en) 2006-03-31
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
ATE481401T1 (de) 2010-10-15
JP4733986B2 (ja) 2011-07-27
US20060046985A1 (en) 2006-03-02
CA2509554C (fr) 2011-02-01

Similar Documents

Publication Publication Date Title
PL377354A1 (pl) Tetrahydro-4H-pirydo[1,2-a]pirymidyny i związki pokrewne użyteczne jako inhibitory integrazy HIV
NO2020026I1 (no) Raltegravir eller et farmasøytisk akseptabelt salt derav, spesielt kaliumsaltet
DK1441734T3 (da) Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
EP1467970A4 (fr) Carboxamides hydroxynaphthyridinone utiles comme inhibiteurs de l'integrase du vih
WO2005086700A3 (fr) Inhibiteurs de l'integrase du vih
WO2007146230A3 (fr) Inhibiteurs de transcriptase inverse non nucléosidiques
WO2004024078A3 (fr) Composes de dihydroxypyridopyrazine-1,6-diones utiles en tant qu'inhibiteurs de l'integrase du vih
WO2005120516A3 (fr) Inhibiteurs intégrase vih
EP1539714A4 (fr) Composes de 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine utilises comme inhibiteurs de l'integrase du vih
WO2007050510A3 (fr) Inhibiteurs de l'integrase du vih
ATE517899T1 (de) Hiv-integrasehemmer
WO2005115147A3 (fr) Inhibiteurs de la transcriptase inverse du vih