KR100862879B1 - Ｈｉｖ 인테그라제의 ｎ-치환된 하이드록시피리미디논 카복스아미드 억제제 - Google Patents

Ｈｉｖ 인테그라제의 ｎ-치환된 하이드록시피리미디논 카복스아미드 억제제 Download PDF

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KR100862879B1
KR100862879B1 KR1020047006234A KR20047006234A KR100862879B1 KR 100862879 B1 KR100862879 B1 KR 100862879B1 KR 1020047006234 A KR1020047006234 A KR 1020047006234A KR 20047006234 A KR20047006234 A KR 20047006234A KR 100862879 B1 KR100862879 B1 KR 100862879B1
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alkyl
methyl
oxo
hydroxy
fluorobenzyl
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Expired - Lifetime
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KR20040047981A (ko
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크레센치베네데타
가르델리크리스티나
무라글리아에스터
니치엠마누엘라
오르비에토페데리카
파체파올라
페스카토레지오반나
페트로치알레씨아
포마마르코
로울리마이클
스카르펠리리타
숨마빈켄초
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이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티에스.피.에이.
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Application filed by 이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티에스.피.에이. filed Critical 이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티에스.피.에이.
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Assigned to 엠에스디 이탈리아 에스.알.엘. reassignment 엠에스디 이탈리아 에스.알.엘. 권리의 전부이전등록 Assignors: 이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티 에스.알.엘.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
    • 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
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020047006234A 2001-10-26 2002-10-21 Ｈｉｖ 인테그라제의 ｎ-치환된 하이드록시피리미디논 카복스아미드 억제제 Expired - Lifetime KR100862879B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US33956801P 2001-10-26 2001-10-26
US60/339,568 2001-10-26
US36219102P 2002-03-06 2002-03-06
US60/362,191 2002-03-06
PCT/GB2002/004753 WO2003035077A1 (en) 2001-10-26 2002-10-21 N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase

Publications (2)

Publication Number Publication Date
KR20040047981A KR20040047981A (ko) 2004-06-05
KR100862879B1 true KR100862879B1 (ko) 2008-10-15

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US (5) US7169780B2 (https=)
EP (1) EP1441735B1 (https=)
JP (1) JP3927175B2 (https=)
KR (1) KR100862879B1 (https=)
CN (3) CN1700918B (https=)
AT (1) ATE318140T1 (https=)
BR (1) BRPI0213522C1 (https=)
CA (1) CA2463976C (https=)
CO (1) CO5580777A2 (https=)
CY (1) CY2008008I1 (https=)
DE (3) DE122009000048I1 (https=)
DK (1) DK1441735T3 (https=)
EA (1) EA007060B1 (https=)
ES (1) ES2258668T3 (https=)
FR (1) FR08C0026I2 (https=)
GE (1) GEP20063848B (https=)
HR (1) HRP20040373B1 (https=)
HU (2) HU230248B1 (https=)
IL (2) IL161337A0 (https=)
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LT (1) LTC1441735I2 (https=)
LU (1) LU91428I2 (https=)
ME (1) ME00427B (https=)
MX (1) MXPA04003932A (https=)
NL (1) NL300340I2 (https=)
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NZ (1) NZ533057A (https=)
PL (1) PL212914B1 (https=)
PT (1) PT1441735E (https=)
RS (1) RS51542B (https=)
SI (1) SI1441735T1 (https=)
UA (1) UA77454C2 (https=)
WO (1) WO2003035077A1 (https=)
ZA (1) ZA200402796B (https=)

Families Citing this family (135)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US7230000B1 (en) 1999-10-27 2007-06-12 Cytokinetics, Incorporated Methods and compositions utilizing quinazolinones
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
AR036256A1 (es) 2001-08-17 2004-08-25 Merck & Co Inc Sal sodica de un inhibidor de integrasa del vih, procesos para su preparacion, composiciones farmaceuticas que lo contienen y su uso para la manufactura de un medicamento
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
NZ533057A (en) * 2001-10-26 2005-11-25 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
WO2003070701A2 (en) 2002-02-15 2003-08-28 Cytokinetics, Inc. Syntheses of quinazolinones
WO2003077857A2 (en) 2002-03-15 2003-09-25 Merck & Co., Inc. N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors
US7214800B2 (en) 2002-05-09 2007-05-08 Cytokinetics, Inc. Compounds, compositions, and methods
CA2485148A1 (en) * 2002-05-09 2003-11-20 Cytokinetics, Inc. Pyrimidinone compounds, compositions and methods
EP1513820A4 (en) 2002-05-23 2006-09-13 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
JP2005530806A (ja) * 2002-05-23 2005-10-13 メルク　エンド　カムパニー　インコーポレーテッド 有糸分裂キネシン阻害薬
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
AU2003256805A1 (en) 2002-07-23 2004-02-09 Cytokinetics, Inc. Compounds compositions and methods
JP2005538184A (ja) 2002-09-11 2005-12-15 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剤として有用な８−ヒドロキシ−１−オキソ−テトラヒドロピロロピラジン化合物
CA2498111A1 (en) 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
WO2004034972A2 (en) 2002-09-30 2004-04-29 Cytokinetics, Inc. Compounds, compositions, and methods
EP1578748B1 (en) * 2002-12-27 2010-09-15 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors
WO2004062613A2 (en) * 2003-01-13 2004-07-29 Bristol-Myers Squibb Company Hiv integrase inhibitors
US7037908B2 (en) 2003-04-24 2006-05-02 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
CA2542047A1 (en) 2003-10-20 2005-05-12 Merck & Co., Inc. Hydroxy pyridopyrrolopyrazine dione compounds useful as hiv integrase inhibitors
US20050090668A1 (en) * 2003-10-28 2005-04-28 Dreher Spencer D. Preparation of 5-hydroxy-6-oxo-1,6-dihydropyrimidine compounds
EP1692112A4 (en) 2003-12-08 2008-09-24 Cytokinetics Inc COMPOUNDS, COMPOSITIONS, AND METHODS
AR046938A1 (es) * 2003-12-12 2006-01-04 Merck & Co Inc Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
JP2007518711A (ja) 2003-12-19 2007-07-12 メルク　エンド　カムパニー　インコーポレーテッド 有糸分裂キネシン阻害剤
TW200526635A (en) 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
MXPA06007906A (es) * 2004-01-12 2007-02-14 Gilead Sciences Inc Compuestos antivirales de fosfonato de pirimidilo y metodos de uso.
JP2007528394A (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
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
ES2529038T3 (es) * 2004-05-07 2015-02-16 Merck Sharp & Dohme Corp. Inhibidores de la integrasa de VIH
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
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
US7476666B2 (en) 2004-06-09 2009-01-13 Merck & Co., Inc. HIV integrase inhibitors
RU2403066C2 (ru) * 2004-12-03 2010-11-10 Мерк Шарп Энд Домэ Корп Применение атазанавира для улучшения фармакокинетики лекарственных средств, метаболизируемых ugt1a1
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
MX2007006635A (es) * 2004-12-03 2007-06-19 Merck & Co Inc Formulacion farmaceutica de inhibidores dela carboxamida vih integrasa que contienen una composicion que controla la velocidad de liberacion.
EP1819323B2 (en) 2004-12-03 2023-03-22 Merck Sharp & Dohme Corp. Pharmaceutical composition containing an anti-nucleating agent
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
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
CA2607151C (en) * 2005-05-10 2012-06-19 Merck & Co., Inc. Hiv integrase inhibitors
CA2616314A1 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
CA2622639C (en) * 2005-10-04 2012-01-03 Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
JP2009513640A (ja) * 2005-10-27 2009-04-02 メルク エンド カムパニー インコーポレーテッド Ｈｉｖインテグラーゼインヒビター
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
US20100056516A1 (en) * 2006-07-17 2010-03-04 Williams Peter D 1-hydroxy naphthyridine compounds as anti-hiv agents
EP2046328A4 (en) 2006-07-19 2009-10-28 Univ Georgia Res Found PYRIDINONE DIKETOIC ACIDS: INHIBITORS OF HIV REPLICATION IN COMBINATION THERAPY
WO2008048538A1 (en) * 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
CN101206209B (zh) * 2006-12-19 2011-08-10 北京德众万全药物技术开发有限公司 一种用hplc法分析西多福韦原料及其制剂的方法
US7763630B2 (en) * 2007-06-06 2010-07-27 Bristol-Myers Squibb Company HIV integrase inhibitors
ES2360336T3 (es) * 2007-06-22 2011-06-03 Bristol-Myers Squibb Company Composiciones en comprimidos que contienen atazanavir.
WO2009009531A2 (en) * 2007-07-09 2009-01-15 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives for the treatment of hiv infections
JP2011517313A (ja) 2007-12-11 2011-06-02 ビアメト ファーマシューティカルズ，インク． 金属結合部分を標的化部分と組み合わせて使用する金属酵素阻害剤
RU2495878C2 (ru) 2007-12-21 2013-10-20 Ф.Хоффманн-Ля Рош Аг Гетероциклические антивирусные соединения
CN101918372B (zh) * 2008-01-08 2014-03-26 默沙东公司 用于制备n-取代的羟基嘧啶酮羧酰胺类化合物的方法
JP5539978B2 (ja) * 2008-07-02 2014-07-02 アベキサ・リミテッド チアゾピリミジノンおよびその使用
WO2010042392A2 (en) * 2008-10-06 2010-04-15 Merck & Co., Inc. Hiv integrase inhibitors
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
US8742105B2 (en) 2009-06-02 2014-06-03 Hetero Research Foundation Polymorphs of raltegravir potassium
AU2010270464B2 (en) * 2009-07-06 2015-01-22 Syngenta Participations Ag Insecticidal compounds
WO2011024192A2 (en) 2009-07-27 2011-03-03 Matrix Laboratories Ltd Novel polymorphs of raltegravir
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
IN2012DN03377A (https=) 2009-10-26 2015-10-23 Merck Sharp & Dohme
DE102009056636A1 (de) 2009-12-02 2011-06-09 Ratiopharm Gmbh Raltegravir-Polymorphe
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
AU2011223976B2 (en) * 2010-03-04 2015-05-21 Merck Sharp & Dohme Corp. Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders
AU2011223969B2 (en) * 2010-03-04 2015-06-11 Merck Sharp & Dohme Llc Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders
US9260413B2 (en) 2010-03-04 2016-02-16 Merck Sharp & Dohme Corp. Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders
ES2662332T3 (es) 2010-03-04 2018-04-06 Merck Sharp & Dohme Corp. Inhibidores de la catecol-O-metil-transferasa y su uso en el tratamiento de trastornos psicóticos
CA2999435A1 (en) * 2010-04-01 2011-10-06 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv
CA2795157C (en) 2010-04-01 2015-11-24 Teva Pharmaceutical Industries Ltd. Raltegravir salts and crystalline forms thereof
EP2555757B1 (en) 2010-04-09 2016-05-25 Bristol-Myers Squibb Holdings Ireland Atazanavir sulfate formulations with improved ph effect
US8962833B2 (en) 2010-05-25 2015-02-24 Hetero Research Foundation Salts of raltegravir
WO2012009446A1 (en) 2010-07-16 2012-01-19 Concert Pharmaceuticals Inc. Novel pyrimidinecarboxamide derivatives
CN101914067B (zh) * 2010-08-26 2012-07-11 陈岱岭 N-甲基嘧啶酮的合成方法
WO2012103105A1 (en) * 2011-01-24 2012-08-02 Assia Chemical Industries Ltd. Processes for preparing raltegravir and intermediates in the processes
WO2012137142A1 (en) 2011-04-06 2012-10-11 Lupin Limited Novel salts of raltegravir
US9968607B2 (en) 2011-04-25 2018-05-15 Hetero Research Foundation Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof
EP2522665A1 (en) * 2011-05-03 2012-11-14 Sandoz Ag Crystalline sodium salt of an HIV integrase inhibitor
ES2450944T3 (es) 2011-06-01 2014-03-25 Ratiopharm Gmbh Composición y comprimido que comprenden raltegravir
CN103130787B (zh) * 2011-11-24 2015-06-10 南开大学 嘧啶酮酰胺类化合物及其制备方法、抗hiv活性和抗tmv活性
CN103130788B (zh) * 2011-11-24 2015-09-02 南开大学 嘧啶酰胺类化合物及其制备方法、抗hiv活性和抗tmv活性
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
ES2825029T3 (es) * 2011-12-26 2021-05-14 Emcure Pharmaceuticals Ltd Síntesis de raltegravir
WO2013111100A1 (en) 2012-01-25 2013-08-01 Lupin Limited Stable amorphous raltegravir potassium premix and process for the preparation thereof
US20150166520A1 (en) * 2012-07-20 2015-06-18 Merck Sharp & Dohme Corp. Amido-substituted pyrimidinone derivatives useful for the treatment of hiv infection
KR20150039832A (ko) 2012-08-06 2015-04-13 사피라 파르마슈티칼즈 게엠베하 디하이드록시피리미딘 탄산 유도체 및 바이러스성 질환의 치료, 개선 또는 예방에서의 이의 용도
CN102911124B (zh) * 2012-10-25 2015-11-25 山东大学 羟基嘧啶酮类化合物及其制备方法与应用
CA2889903C (en) 2012-10-29 2021-03-09 Manjinder Singh Phull Antiviral phosphonate analogues and process for preparation thereof
EP2931730B1 (en) 2012-12-17 2019-08-07 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
EA030003B1 (ru) 2012-12-21 2018-06-29 Джилид Сайэнс, Инк. Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
AU2014267951A1 (en) 2013-05-17 2015-11-19 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
NO2865735T3 (https=) 2013-07-12 2018-07-21
SI3019503T1 (sl) 2013-07-12 2017-11-30 Gilead Sciences, Inc. Policiklične karbamoilpiridonske spojine in njihova uporaba za zdravljenje HIV infekcij
MD4794B1 (ro) 2013-09-27 2022-02-28 Merck Sharp & Dohme Corp Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază HIV
WO2015096651A1 (en) 2013-12-23 2015-07-02 Merck Sharp & Dohme Corp. Pyrimidone carboxamide compounds as pde2 inhibitors
WO2015114608A1 (en) 2014-02-03 2015-08-06 Mylan Laboratories Ltd Processes for the preparation of intermediates of raltegravir
US10391178B2 (en) 2014-03-21 2019-08-27 Mylan Laboratories Limited Premix of crystalline raltegravir potassium salt and a process for the preparation thereof
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
TWI677489B (zh) 2014-06-20 2019-11-21 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
NO2717902T3 (https=) 2014-06-20 2018-06-23
US9353093B2 (en) 2014-10-07 2016-05-31 Allergan, Inc. Indole-1-carboxamides as kinase inhibitors
WO2016075605A1 (en) 2014-11-10 2016-05-19 Aurobindo Pharma Ltd An improved process for the preparation of raltegravir
TWI695003B (zh) 2014-12-23 2020-06-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
WO2016145614A1 (en) 2015-03-17 2016-09-22 Merck Sharp & Dohme Corp. Triazolyl pyrimidinone compounds as pde2 inhibitors
WO2016154081A1 (en) 2015-03-26 2016-09-29 Merck Sharp & Dohme Corp. Pyrazolyl pyrimidinone compounds as pde2 inhibitors
JP6402259B2 (ja) 2015-04-02 2018-10-10 ギリアード サイエンシーズ， インコーポレイテッド 多環式カルバモイルピリドン化合物およびそれらの薬学的使用
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
US10647727B2 (en) 2015-06-25 2020-05-12 Merck Sharp & Dohme Corp. Substituted pyrazolo/imidazolo bicyclic compounds as PDE2 inhibitors
WO2017000277A1 (en) 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Substituted triazolo bicycliccompounds as pde2 inhibitors
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
WO2017106071A1 (en) 2015-12-15 2017-06-22 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
EP3472134B1 (en) 2016-06-21 2021-10-20 Pharmathen S.A. Process for preparing compounds useful as intermediates for the preparation of raltegravir
JP2019529410A (ja) 2016-09-15 2019-10-17 ルピン・リミテッド 純粋で安定な結晶のラルテグラビルカリウム３型の製造方法
US10934312B2 (en) 2016-12-02 2021-03-02 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as HIV integrase inhibitors
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 (en) 2017-01-26 2018-08-02 Merck Sharp & Dohme Corp. Substituted quinolizine derivatives useful as hiv integrase inhibitors
HRP20220613T1 (hr) 2017-11-14 2022-06-24 Cambrex Profarmaco Milano S.R.L. Postupak priprave raltegavira
PT3891145T (pt) 2018-12-06 2023-07-18 Constellation Pharmaceuticals Inc Moduladores de trex1
EP4003985A1 (en) * 2019-07-23 2022-06-01 Constellation Pharmaceuticals, Inc. Modulators of trex1
EP4093380A1 (en) 2020-01-23 2022-11-30 Lupin Limited Pharmaceutical compositions of raltegravir
WO2021165927A1 (en) * 2020-02-21 2021-08-26 Wockhardt Bio Ag 2-cyanopyrroldines, -piperidines or -dazepines as hyperglycemic agents

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001085700A2 (en) * 2000-05-08 2001-11-15 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines and triazines
WO2002006246A1 (en) * 2000-07-19 2002-01-24 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Dihydroxypyrimidine carboxylic acids as viral polymerase inhibitors

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL78158A (en) 1985-03-16 1988-04-29 Wellcome Found Pharmaceutical compositions containing 3'-azido-3'-deoxythymidine
US5047407A (en) 1989-02-08 1991-09-10 Iaf Biochem International, Inc. 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties
US5914331A (en) 1990-02-01 1999-06-22 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
US5637618A (en) * 1990-06-01 1997-06-10 Bioresearch, Inc. Specific eatable taste modifiers
DE4029654A1 (de) 1990-09-19 1992-04-02 Hoechst Ag 2-phenyl-pyrimidine, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung als fungizide
US5665720A (en) 1992-08-07 1997-09-09 Merck & Co., Inc. Benzoxazinones as inhibitors of HIV reverse transcriptase
TW287160B (https=) 1992-12-10 1996-10-01 Hoffmann La Roche
US5919776A (en) * 1996-12-20 1999-07-06 Merck & Co., Inc. Substituted aminoquinolines as modulators of chemokine receptor activity
US5935946A (en) 1997-07-25 1999-08-10 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
US6632823B1 (en) 1997-12-22 2003-10-14 Merck & Co., Inc. Substituted pyridine compounds useful as modulators of acetylcholine receptors
PL343249A1 (en) * 1998-03-26 2001-07-30 Shionogi & Co Indole derivatives with antiviral activity
US6306891B1 (en) * 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
WO1999062520A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
EP1086091A4 (en) 1998-06-03 2001-10-10 Merck & Co Inc INTEGRASE HIV INHIBITORS
MXPA01001843A (es) 1998-08-20 2002-04-08 Toyama Chemical Co Ltd Derivados de carboxamida heterociclica con nitrogeno o sales derivados de los mismos y agentes antivirales que comprenden los mismos.
JP3929244B2 (ja) * 1998-12-25 2007-06-13 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芳香族ヘテロ環誘導体
WO2000051990A1 (en) * 1999-03-04 2000-09-08 Korea Research Institute Of Chemical Technology Antiviral 2,4-pyrimidinedione derivatives and process for the preparation thereof
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
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
CA2425440C (en) * 2000-10-12 2010-04-13 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
US6919351B2 (en) 2000-10-12 2005-07-19 Merck & Co., Inc. Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors
JP3616628B2 (ja) * 2001-03-01 2005-02-02 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含窒素芳香族複素環化合物
BR0211750A (pt) * 2001-08-10 2004-10-13 Shionogi & Co Agente antiviral
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
NZ533057A (en) * 2001-10-26 2005-11-25 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
JP4497347B2 (ja) 2001-12-05 2010-07-07 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誘導体
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
EP2161258A3 (en) 2002-11-20 2010-04-07 Japan Tabacco Inc. 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
WO2004062613A2 (en) 2003-01-13 2004-07-29 Bristol-Myers Squibb Company Hiv integrase inhibitors
US7037908B2 (en) 2003-04-24 2006-05-02 Bristol-Myers Squibb Company HIV integrase inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001085700A2 (en) * 2000-05-08 2001-11-15 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines and triazines
WO2002006246A1 (en) * 2000-07-19 2002-01-24 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Dihydroxypyrimidine carboxylic acids as viral polymerase inhibitors

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