NL300340I2 - N-gesubstitueerde hydroxypyrimidon-carboxamideremmers van hiv-integrase - Google Patents

N-gesubstitueerde hydroxypyrimidon-carboxamideremmers van hiv-integrase

Info

Publication number
NL300340I2
NL300340I2 NL300340C NL300340C NL300340I2 NL 300340 I2 NL300340 I2 NL 300340I2 NL 300340 C NL300340 C NL 300340C NL 300340 C NL300340 C NL 300340C NL 300340 I2 NL300340 I2 NL 300340I2
Authority
NL
Netherlands
Prior art keywords
hiv
substituted
compounds
inhibitors
hydroxypyrimidone
Prior art date
Application number
NL300340C
Other languages
English (en)
Other versions
NL300340I1 (nl
Original Assignee
Angeletti S P A Inst Di Richerche
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=26991691&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NL300340(I2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Angeletti S P A Inst Di Richerche filed Critical Angeletti S P A Inst Di Richerche
Publication of NL300340I1 publication Critical patent/NL300340I1/nl
Publication of NL300340I2 publication Critical patent/NL300340I2/nl

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545Two 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
    • C07D239/557Two 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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 aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • 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)
NL300340C 2001-10-26 2008-03-31 N-gesubstitueerde hydroxypyrimidon-carboxamideremmers van hiv-integrase NL300340I2 (nl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US33956801P 2001-10-26 2001-10-26
US36219102P 2002-03-06 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
NL300340I1 NL300340I1 (nl) 2008-06-02
NL300340I2 true NL300340I2 (nl) 2008-08-01

Family

ID=26991691

Family Applications (1)

Application Number Title Priority Date Filing Date
NL300340C NL300340I2 (nl) 2001-10-26 2008-03-31 N-gesubstitueerde hydroxypyrimidon-carboxamideremmers van hiv-integrase

Country Status (35)

Country Link
US (5) US7169780B2 (nl)
EP (1) EP1441735B1 (nl)
JP (1) JP3927175B2 (nl)
KR (1) KR100862879B1 (nl)
CN (3) CN1700918B (nl)
AT (1) ATE318140T1 (nl)
BR (1) BRPI0213522C1 (nl)
CA (1) CA2463976C (nl)
CO (1) CO5580777A2 (nl)
CY (1) CY2008008I1 (nl)
DE (3) DE122008000016I1 (nl)
DK (1) DK1441735T3 (nl)
EA (1) EA007060B1 (nl)
ES (1) ES2258668T3 (nl)
FR (1) FR08C0026I2 (nl)
GE (1) GEP20063848B (nl)
HK (1) HK1085665A1 (nl)
HR (1) HRP20040373B1 (nl)
HU (2) HU230248B1 (nl)
IL (2) IL161337A0 (nl)
IS (1) IS2436B (nl)
LT (1) LTC1441735I2 (nl)
LU (1) LU91428I2 (nl)
ME (1) ME00427B (nl)
MX (1) MXPA04003932A (nl)
NL (1) NL300340I2 (nl)
NO (3) NO325206B1 (nl)
NZ (1) NZ533057A (nl)
PL (1) PL212914B1 (nl)
PT (1) PT1441735E (nl)
RS (1) RS51542B (nl)
SI (1) SI1441735T1 (nl)
UA (1) UA77454C2 (nl)
WO (1) WO2003035077A1 (nl)
ZA (1) ZA200402796B (nl)

Families Citing this family (126)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU1532802A (en) 2000-10-12 2002-04-22 Merck & Co Inc Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
US6841558B2 (en) 2000-10-12 2005-01-11 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as HIV intergrase inhibitors
ATE430745T1 (de) 2000-10-12 2009-05-15 Merck & Co Inc Aza- und polyaza naphthalenyl karboxamide als inhibitoren der hiv-integrase
ES2587564T1 (es) 2001-08-10 2016-10-25 Shionogi & Co., Ltd. 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
IL161337A0 (en) * 2001-10-26 2004-09-27 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
DK1441734T3 (da) * 2001-10-26 2007-06-11 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
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
CN100491358C (zh) * 2002-05-09 2009-05-27 赛特凯恩蒂克公司 嘧啶酮类化合物、组合物及方法
WO2003099211A2 (en) * 2002-05-23 2003-12-04 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2004004657A2 (en) 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
WO2004047725A2 (en) * 2002-09-11 2004-06-10 Merck & Co. Inc. 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors
JP2006506352A (ja) 2002-09-11 2006-02-23 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ジヒドロキシピリドピラジン−1,6−ジオン化合物
KR20050087865A (ko) 2002-12-27 2005-08-31 이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티에스.피.에이. HIV 인테그라제 억제제로서 유용한테트라하이드로-4H-피리도[1,2-a]피리미딘 및 관련화합물
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
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
US7435735B2 (en) * 2003-10-20 2008-10-14 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
AR046938A1 (es) * 2003-12-12 2006-01-04 Merck & Co Inc Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
CA2547209A1 (en) 2003-12-19 2005-07-07 Merck & Co., Inc. Mitotic kinesin inhibitors
TW200526635A (en) * 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
EP1711476A2 (en) * 2004-01-12 2006-10-18 Gilead Sciences, Inc. Pyrimidyl phosphonate antiviral compounds and methods of use
EA200601654A1 (ru) 2004-03-09 2007-02-27 Мерк Энд Ко., Инк. Ингибиторы интегразы вич
CN1930161A (zh) 2004-03-09 2007-03-14 P·安杰莱蒂分子生物学研究所 Hiv整合酶抑制剂
US7619086B2 (en) 2004-03-09 2009-11-17 Merck & Co., Inc. HIV integrase inhibitors
US7820680B2 (en) * 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
US7538112B2 (en) * 2004-05-07 2009-05-26 Merck & Co., Inc. HIV integrase inhibitors
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
US7173022B2 (en) * 2004-05-28 2007-02-06 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
US7176196B2 (en) 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
JP2008502741A (ja) 2004-06-09 2008-01-31 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
KR101351059B1 (ko) 2004-12-03 2014-02-17 머크 샤프 앤드 돔 코포레이션 방출 속도 조절용 조성물을 포함하는 카복스아미드 hiv 인테그라제 억제제의 약제학적 제형
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
EP1819323B2 (en) 2004-12-03 2023-03-22 Merck Sharp & Dohme Corp. Pharmaceutical composition containing an anti-nucleating agent
KR20070085702A (ko) * 2004-12-03 2007-08-27 머크 앤드 캄파니 인코포레이티드 Ugt1a1에 의해 대사된 약물의 약력학을 개선시키기위한 아타자나비르의 용도
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
LT3284520T (lt) 2005-04-28 2019-09-25 Viiv Healthcare Company Policiklinis karbamoilpiridono darinys, turintis živ integrazę slopinantį poveikį
US7741315B2 (en) * 2005-05-10 2010-06-22 Merck Sharp & Dohme Corp. HIV integrase inhibitors
AU2006272521A1 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of HIV
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
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
JP2009543865A (ja) 2006-07-19 2009-12-10 ユニバーシティ オブ ジョージア リサーチ ファウンデーション, インコーポレーテッド ピリジノンジケト酸:併用療法におけるhiv複製の阻害剤
AU2007313293A1 (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
AU2008268627A1 (en) * 2007-06-22 2008-12-31 Bristol-Myers Squibb Company Tableted compositions containing atazanavir
US7687509B2 (en) * 2007-07-09 2010-03-30 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives
EP2234608A2 (en) 2007-12-11 2010-10-06 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitors using metal binding moieties in combination with targeting moieties
BRPI0821349A2 (pt) 2007-12-21 2019-09-24 Hoffmann La Roche compostos antivirais heterocíclicos
EP2231621B1 (en) * 2008-01-08 2016-11-02 Merck Sharp & Dohme Corp. Process for preparing n-substituted hydroxypyrimidinone carboxamides
WO2010000030A1 (en) * 2008-07-02 2010-01-07 Avexa Limited Thiazopyrimidinones and uses thereof
BRPI0920605A8 (pt) * 2008-10-06 2016-04-26 Merck Sharp & Dohme Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, método para o tratamento ou profilaxia de infecção pelo hiv ou para o tratamento, profilaxia, ou retardo no início ou progressão da aids em um paciente em necessidade deste.
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
WO2010140156A2 (en) 2009-06-02 2010-12-09 Hetero Research Foundation Novel polymorphs of raltegravir potassium
ES2514318T3 (es) * 2009-07-06 2014-10-28 Syngenta Participations Ag Compuestos insecticidas
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
HRP20211826T1 (hr) 2009-10-26 2022-03-04 Merck Sharp & Dohme Corp. Čvrste farmaceutske kompozicije koje sadrže inhibitor integraze
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
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
MX2012010188A (es) * 2010-03-04 2012-10-03 Merck Sharp & Dohme Inhibidores de catecol o-metil transferasa y su uso en el tratamiento de transtornos psicoticos.
BR112012021656A2 (pt) * 2010-03-04 2017-02-07 Merck Sharp & Dohme composto, uso do mesmo, e, composição farmacêutica
EP2542076B1 (en) 2010-03-04 2021-01-13 Merck Sharp & Dohme Corp. Inhibitors of catechol o-methyl transferase and their use in the treatment of psychotic disorders
SI2796458T1 (en) 2010-04-01 2018-04-30 Teva Pharmaceutical Industries Ltd. CRYSTALINIC SODIUM RALTEGRAVIR SOLUTIONS
WO2011120153A1 (en) * 2010-04-01 2011-10-06 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv
US20130203759A1 (en) 2010-04-09 2013-08-08 Faranak Nikfar ATAZANAVIR SULFATE FORMULATIONS WITH IMPROVED pH EFFECT
US8962833B2 (en) 2010-05-25 2015-02-24 Hetero Research Foundation Salts of raltegravir
US9107922B2 (en) 2010-07-16 2015-08-18 Concert Pharmaceuticals, Inc. 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
EP2694497A1 (en) 2011-04-06 2014-02-12 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
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
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
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
WO2013098854A2 (en) * 2011-12-26 2013-07-04 Emcure Pharmaceuticals Limited Synthesis of raltegravir
RU2014134257A (ru) 2012-01-25 2016-03-20 Люпин Лимитед Устойчивый аморфный премикс на основе ралтегравира калия и способ его получения
US20150166520A1 (en) * 2012-07-20 2015-06-18 Merck Sharp & Dohme Corp. Amido-substituted pyrimidinone derivatives useful for the treatment of hiv infection
US8921388B2 (en) 2012-08-06 2014-12-30 European Molecular Biology Laboratory Dihydroxypyrimidine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
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
EP2912047B1 (en) 2012-10-29 2016-08-24 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
US9714243B2 (en) 2012-12-17 2017-07-25 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as HIV integrase inhibitors
PT3608325T (pt) 2012-12-21 2022-10-17 Gilead Sciences Inc Compostos carbamoílpiridona policíclicos e sua utilização farmacêutica
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
ME02977B (me) 2013-05-17 2018-10-20 Merck Sharp & Dohme Fuzionisana triciklicna heterociklicna jedinjenja као inhibiтori hiv integraze
US9951079B2 (en) 2013-06-13 2018-04-24 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
NO2865735T3 (nl) 2013-07-12 2018-07-21
PT3019503T (pt) 2013-07-12 2017-11-27 Gilead Sciences Inc Compostos carbamoílpiridona- policíclicos e seu uso para o tratamento de infecções por hiv
WO2015048363A1 (en) 2013-09-27 2015-04-02 Merck Sharp & Dohme Corp. Substituted quinolizine derivatives useful as hiv integrase inhibitors
US9815796B2 (en) 2013-12-23 2017-11-14 Merck Sharp & Dohme Corp. Pyrimidone carboxamide compounds as PDE2 inhibitors
EP3102565B1 (en) * 2014-02-03 2019-01-02 Mylan Laboratories Ltd. Processes for the preparation of intermediates of raltegravir
WO2015140765A1 (en) 2014-03-21 2015-09-24 Mylan Laboratories Ltd. A premix of crystalline raltegravir potassium salt and a process for the preparation thereof
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
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
NO2717902T3 (nl) 2014-06-20 2018-06-23
US9353093B2 (en) 2014-10-07 2016-05-31 Allergan, Inc. Indole-1-carboxamides as kinase inhibitors
US10259778B2 (en) 2014-11-10 2019-04-16 Aurobindo Pharma Ltd 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
PL3277691T3 (pl) 2015-04-02 2019-07-31 Gilead Sciences, Inc. Policykliczne związki karbamoilopirydonowe i ich zastosowanie farmaceutyczne
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
WO2016209749A1 (en) 2015-06-25 2016-12-29 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
WO2017087257A1 (en) 2015-11-17 2017-05-26 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
EP3472134B1 (en) 2016-06-21 2021-10-20 Pharmathen S.A. Process for preparing compounds useful as intermediates for the preparation of raltegravir
WO2018051239A1 (en) 2016-09-15 2018-03-22 Lupin Limited Process for the preparation of pure and stable crystalline raltegravir potassium form 3
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)
RU2749043C2 (ru) 2016-12-02 2021-06-03 Мерк Шарп И Доум Корп. Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич
EP3573984A4 (en) 2017-01-26 2020-07-29 Merck Sharp & Dohme Corp. USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
PL3710445T3 (pl) 2017-11-14 2022-06-20 Cambrex Profarmaco Milano S.R.L. Sposób wytwarzania raltegrawiru
CN114174290A (zh) * 2019-07-23 2022-03-11 星座制药公司 Trex1的调节剂
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

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU572019B2 (en) 1985-03-16 1988-04-28 Wellcome Foundation Limited, The 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
US6642245B1 (en) * 1990-02-01 2003-11-04 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
US5519021A (en) * 1992-08-07 1996-05-21 Merck & Co., Inc. Benzoxazinones as inhibitors of HIV reverse transcriptase
TW287160B (nl) 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
CA2326166A1 (en) 1998-03-26 1999-10-07 Shionogi & Co., Ltd. Indole derivatives with antiviral activity
US6306891B1 (en) 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
JP2002517390A (ja) 1998-06-03 2002-06-18 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
EP1082121A4 (en) 1998-06-03 2003-02-05 Merck & Co Inc INTEGRASE HIV INHIBITORS
RU2224520C2 (ru) 1998-08-20 2004-02-27 Тояма Кемикал Ко., Лтд. Азотсодержащие гетероциклические производные карбоксамида или их соли и противовирусные средства, включающие их
ATE411286T1 (de) 1998-12-25 2008-10-15 Shionogi & Co Aromatische heterocyclen mit hiv integrase inhibierenden eigenschaften
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
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
WO2001085700A2 (en) 2000-05-08 2001-11-15 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines and triazines
GB0017676D0 (en) 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
ATE430745T1 (de) 2000-10-12 2009-05-15 Merck & Co Inc Aza- und polyaza naphthalenyl karboxamide als inhibitoren der hiv-integrase
US6841558B2 (en) 2000-10-12 2005-01-11 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as HIV intergrase inhibitors
AU1532802A (en) 2000-10-12 2002-04-22 Merck & Co Inc Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
WO2002036734A2 (en) 2000-10-12 2002-05-10 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
KR20030078958A (ko) 2001-03-01 2003-10-08 시오노기세이야쿠가부시키가이샤 Hiv 인테그라제 저해 활성을 갖는 질소 함유의헤테로아릴 화합물
ES2587564T1 (es) 2001-08-10 2016-10-25 Shionogi & Co., Ltd. Agente antiviral
DK1441734T3 (da) 2001-10-26 2007-06-11 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
IL161337A0 (en) * 2001-10-26 2004-09-27 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
WO2004004657A2 (en) 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
CZ2004764A3 (cs) 2002-11-20 2005-02-16 Japan Tobacco Inc 4-Oxochinolinová sloučenina a její použití jako inhibitoru HIV-integrázy
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

Also Published As

Publication number Publication date
HUS1600016I1 (hu) 2018-05-02
IL161337A0 (en) 2004-09-27
NO325206B1 (no) 2008-02-25
US20110034449A1 (en) 2011-02-10
HRP20040373A2 (en) 2005-08-31
US7820660B2 (en) 2010-10-26
CA2463976A1 (en) 2003-05-01
IS2436B (is) 2008-10-15
SI1441735T1 (sl) 2006-06-30
CY2008008I1 (el) 2009-11-04
ME00427B (me) 2011-10-10
BR0213522A (pt) 2004-09-08
GEP20063848B (en) 2006-06-12
US20080275004A1 (en) 2008-11-06
CN1700918B (zh) 2011-06-08
US20070123524A1 (en) 2007-05-31
BR0213522B8 (pt) 2017-07-04
JP3927175B2 (ja) 2007-06-06
DE122009000048I1 (de) 2010-04-08
HU230248B1 (hu) 2015-11-30
JP2005511543A (ja) 2005-04-28
LTPA2008007I1 (lt) 2020-05-11
US7435734B2 (en) 2008-10-14
DE122008000016I1 (de) 2011-12-01
CO5580777A2 (es) 2005-11-30
HRP20040373B1 (en) 2012-09-30
BRPI0213522C1 (pt) 2021-05-25
US7169780B2 (en) 2007-01-30
DE60209381D1 (de) 2006-04-27
KR100862879B1 (ko) 2008-10-15
PL212914B1 (pl) 2012-12-31
NO2008007I2 (nl) 2010-09-27
MXPA04003932A (es) 2004-06-18
FR08C0026I2 (fr) 2010-01-22
ATE318140T1 (de) 2006-03-15
NL300340I1 (nl) 2008-06-02
FR08C0026I1 (nl) 2008-07-18
PL369223A1 (en) 2005-04-18
HUP0401740A2 (hu) 2004-12-28
IS7213A (is) 2004-04-07
ES2258668T3 (es) 2006-09-01
NO2020026I1 (no) 2020-08-10
NZ533057A (en) 2005-11-25
DE60209381T2 (de) 2006-10-05
LTC1441735I2 (lt) 2020-06-25
CN102229605B (zh) 2015-01-14
NO20042165L (no) 2004-05-25
CN102219750B (zh) 2013-05-29
CN1700918A (zh) 2005-11-23
IL161337A (en) 2010-02-17
US20050025774A1 (en) 2005-02-03
CN102229605A (zh) 2011-11-02
CN102219750A (zh) 2011-10-19
EA200400585A1 (ru) 2004-10-28
NO2008007I1 (no) 2008-06-23
AU2002334207A2 (en) 2003-05-06
LU91428I2 (fr) 2008-06-09
KR20040047981A (ko) 2004-06-05
RS51542B (sr) 2011-06-30
YU35604A (sh) 2006-08-17
HK1085665A1 (en) 2006-09-01
EP1441735A1 (en) 2004-08-04
UA77454C2 (en) 2006-12-15
PT1441735E (pt) 2006-06-30
DK1441735T3 (da) 2006-06-12
CA2463976C (en) 2007-02-13
BR0213522B1 (pt) 2017-06-13
US20060258860A1 (en) 2006-11-16
HUP0401740A3 (en) 2009-06-29
AU2002334207B2 (en) 2006-02-23
EP1441735B1 (en) 2006-02-22
WO2003035077A1 (en) 2003-05-01
EA007060B1 (ru) 2006-06-30
ZA200402796B (en) 2005-03-30
US7217713B2 (en) 2007-05-15

Similar Documents

Publication Publication Date Title
NO2020026I1 (no) Raltegravir eller et farmasøytisk akseptabelt salt derav, spesielt kaliumsaltet
DK1441734T3 (da) Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
DE60315796D1 (de) Hydroxynaphthyridinoncarbonsäureamide, die sich als inhibitoren der hiv-integrase eignen
WO2004024078A3 (en) Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
ATE364385T1 (de) Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
ATE345129T1 (de) Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
WO2005110414A3 (en) Hiv integrase inhibitors
DE60323743D1 (en) N-(substituierte benzyl)-8-hydroxy-1,6-naphthyridin-7- carbonsäureamide als hiv-integrase-hemmer
WO2004047725A3 (en) 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors
TW200640460A (en) HIV integrase inhibitors