HRP20040373B1 - N-supstituirani hidroksipiridinon karboksamid inhibitori hiv integraze - Google Patents

N-supstituirani hidroksipiridinon karboksamid inhibitori hiv integraze

Info

Publication number
HRP20040373B1
HRP20040373B1 HRP20040373AA HRP20040373A HRP20040373B1 HR P20040373 B1 HRP20040373 B1 HR P20040373B1 HR P20040373A A HRP20040373A A HR P20040373AA HR P20040373 A HRP20040373 A HR P20040373A HR P20040373 B1 HRP20040373 B1 HR P20040373B1
Authority
HR
Croatia
Prior art keywords
hiv integrase
alkyl
carboxamide inhibitors
substituted hydroxypyrimidinone
hydroxypyrimidinone carboxamide
Prior art date
Application number
HRP20040373AA
Other languages
English (en)
Inventor
Crescenzi Benedetta
Pescatore Giovanna
Petrocchi Alessia
Poma Marco
Rowley Michael
Scarpelli Rita
Cristina Gardelli
Muraglia Ester
Nizi Emanuela
Orvieto Federica
Pace Paola
Summa Vinzenzo
Original Assignee
Instituto Di Ricerche Di Biologia Molecolare P. Angeletti 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26991691&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20040373(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Instituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. filed Critical Instituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A.
Publication of HRP20040373A2 publication Critical patent/HRP20040373A2/hr
Publication of HRP20040373B1 publication Critical patent/HRP20040373B1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/06—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/02—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
    • C07D403/04—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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/02—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
    • C07D403/06—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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/02—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
    • C07D403/10—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 aromatic rings
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/02—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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—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
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Immunology (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)

Abstract

Spoj Formule (I): naznačen time, da jeR1 (1) -H, (2) -C1-6 alkil, koji je opcionalno supstituiran sa jednim ili vi®e supstituenata, od kojih je svaki neovisno halogen, -OH, -CN, -O- C1-6 alkil, -O- C1-6 haloalkil, -C(=O)Ra -CO2Ra, -SRa, -S(=O)Ra, -N(RaRb), -C(=O)-C0-6 alkil-N(RaRb), N(Ra)-C(=O)-C0-6 alkil-N(RbRc), -SO2Ra, -N(Ra)SO2Rb, -SO2N(RaRb),
HRP20040373AA 2001-10-26 2004-04-26 N-supstituirani hidroksipiridinon karboksamid inhibitori hiv integraze HRP20040373B1 (hr)

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
HRP20040373A2 HRP20040373A2 (en) 2005-08-31
HRP20040373B1 true HRP20040373B1 (hr) 2012-09-30

Family

ID=26991691

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20040373AA HRP20040373B1 (hr) 2001-10-26 2004-04-26 N-supstituirani hidroksipiridinon karboksamid inhibitori hiv integraze

Country Status (35)

Country Link
US (5) US7169780B2 (hr)
EP (1) EP1441735B1 (hr)
JP (1) JP3927175B2 (hr)
KR (1) KR100862879B1 (hr)
CN (3) CN102229605B (hr)
AT (1) ATE318140T1 (hr)
BR (1) BRPI0213522C1 (hr)
CA (1) CA2463976C (hr)
CO (1) CO5580777A2 (hr)
CY (1) CY2008008I1 (hr)
DE (3) DE60209381T2 (hr)
DK (1) DK1441735T3 (hr)
EA (1) EA007060B1 (hr)
ES (1) ES2258668T3 (hr)
FR (1) FR08C0026I2 (hr)
GE (1) GEP20063848B (hr)
HK (1) HK1085665A1 (hr)
HR (1) HRP20040373B1 (hr)
HU (2) HU230248B1 (hr)
IL (2) IL161337A0 (hr)
IS (1) IS2436B (hr)
LT (1) LTC1441735I2 (hr)
LU (1) LU91428I2 (hr)
ME (1) ME00427B (hr)
MX (1) MXPA04003932A (hr)
NL (1) NL300340I2 (hr)
NO (3) NO325206B1 (hr)
NZ (1) NZ533057A (hr)
PL (1) PL212914B1 (hr)
PT (1) PT1441735E (hr)
RS (1) RS51542B (hr)
SI (1) SI1441735T1 (hr)
UA (1) UA77454C2 (hr)
WO (1) WO2003035077A1 (hr)
ZA (1) ZA200402796B (hr)

Families Citing this family (126)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60138635D1 (de) 2000-10-12 2009-06-18 Merck & Co Inc Aza- und polyaza naphthalenyl karboxamide als inhibitoren der hiv-integrase
AU2002246499B2 (en) 2000-10-12 2005-12-22 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
DE60128936T2 (de) 2000-10-12 2008-04-10 Merck & Co, Inc. Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
ATE530520T1 (de) * 2001-08-10 2011-11-15 Shionogi & Co Antivirales mittel
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
CA2463976C (en) * 2001-10-26 2007-02-13 Benedetta Crescenzi N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
CA2463975A1 (en) * 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
CA2478310A1 (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
CA2485148A1 (en) * 2002-05-09 2003-11-20 Cytokinetics, Inc. Pyrimidinone 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***キネシン阻害薬
WO2004004657A2 (en) 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
ATE404563T1 (de) 2002-09-11 2008-08-15 Merck & Co Inc 8-hydroxy-1- oxotetrahydropyrrolopyrazinverbindungen, die sich als inhibitoren von hiv-integrase eignen
WO2004024078A2 (en) * 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
AU2003292436B2 (en) * 2002-12-27 2009-07-30 Msd Italia S.R.L. 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
AR046938A1 (es) * 2003-12-12 2006-01-04 Merck & Co Inc Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
WO2005060654A2 (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
CN1934093A (zh) * 2004-01-12 2007-03-21 吉里德科学公司 嘧啶基膦酸酯抗病毒化合物和使用方法
CA2557785A1 (en) * 2004-03-09 2005-10-06 Merck & Co. Inc. Hiv integrase inhibitors
US7619086B2 (en) 2004-03-09 2009-11-17 Merck & Co., Inc. HIV integrase inhibitors
US20070161639A1 (en) 2004-03-09 2007-07-12 Philip Jones Hiv integrase inhibitors
JP4625838B2 (ja) 2004-03-09 2011-02-02 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖインテグラーゼ阻害薬
CN1964975B (zh) * 2004-05-07 2011-11-30 默沙东公司 Hiv整合酶抑制剂
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
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
US7173022B2 (en) * 2004-05-28 2007-02-06 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
CA2568389A1 (en) 2004-06-09 2005-12-22 Merck & Co., Inc. Hiv integrase inhibitors
WO2006060711A2 (en) * 2004-12-03 2006-06-08 Merck & Co., Inc. Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition
CA2588465C (en) * 2004-12-03 2013-10-01 Merck & Co., Inc. 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
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
US7981879B2 (en) * 2005-03-31 2011-07-19 Instituto di Ricerchi di Biologia Molecolare P. Angeletti S.p.A. HIV integrase inhibitors
PL1874117T3 (pl) 2005-04-28 2014-01-31 Viiv Healthcare Co Wielopierścieniowe pochodne karbamoilopirydonu wykazujące aktywność inhibitorową wobec integrazy HIV
AU2006244424B2 (en) 2005-05-10 2011-09-22 Merck Sharp & Dohme Corp. HIV integrase inhibitors
JP2009502964A (ja) * 2005-07-27 2009-01-29 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖを阻害するための抗ウイルス性ホスホン酸結合体
CA2622639C (en) * 2005-10-04 2012-01-03 Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
EP1942736A2 (en) * 2005-10-27 2008-07-16 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
CA2657287A1 (en) * 2006-07-17 2008-01-24 Merck & Co., Inc. 1-hydroxy naphthyridine compounds as anti-hiv agents
MX2009000661A (es) 2006-07-19 2009-03-27 Univ Georgia Res Found Piridinon-diceto-acidos: inhibidores de replicacion de vih en terapia de combinacion.
JP2010506913A (ja) * 2006-10-18 2010-03-04 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
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
CN101801348A (zh) * 2007-06-22 2010-08-11 百时美施贵宝公司 含有阿扎那韦的压片组合物
CA2702317A1 (en) * 2007-07-09 2009-01-15 Concert Pharmaceuticals, Inc. Novel pyrimidinecarboxamide derivatives
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
ES2526649T3 (es) 2007-12-21 2015-01-14 F. Hoffmann-La Roche Ag Compuestos heterocíclicos antivíricos
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
CA2729649A1 (en) * 2008-07-02 2010-01-07 Avexa Limited Thiazopyrimidinones and uses thereof
AU2009302663B2 (en) * 2008-10-06 2012-11-08 Merck Sharp & Dohme Corp. HIV integrase inhibitors
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
ES2549387T3 (es) 2009-06-02 2015-10-27 Hetero Research Foundation Procedimiento de preparación de raltegravir potásico amorfo
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
RU2602865C2 (ru) 2009-10-26 2016-11-20 Мерк Шарп И Доум Корп. Твердые фармацевтические композиции, содержащие ингибитор интегразы
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
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
CA2789475C (en) 2010-03-04 2018-05-29 Merck Sharp & Dohme Corp. Inhibitors of catechol o-methyl transferase and their use in the treatment of psychotic disorders
BR112012021652A2 (pt) 2010-03-04 2016-06-21 Merck Sharp & Dohme composto, uso do mesmo, e, composição farmacêutica
SI2796458T1 (en) 2010-04-01 2018-04-30 Teva Pharmaceutical Industries Ltd. CRYSTALINIC SODIUM RALTEGRAVIR SOLUTIONS
EP2552915B1 (en) * 2010-04-01 2017-07-19 Critical Outcome Technologies Inc. Compounds for the treatment of hiv
CN102917695A (zh) 2010-04-09 2013-02-06 百时美施贵宝公司 具有改进的pH效应的阿扎那韦硫酸盐制剂
EP2575465A4 (en) 2010-05-25 2013-11-20 Hetero Research Foundation Raltegravir SALTS
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
US9163009B2 (en) * 2011-04-06 2015-10-20 Lupin Limited 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
EP2785184B1 (en) 2011-11-30 2020-06-10 Emory University Compositions comprising jak inhibitors and haart drugs for use in the prevention or treatment of hiv
EP2804607B1 (en) * 2011-12-26 2020-09-16 Emcure Pharmaceuticals Limited Synthesis of raltegravir
AU2013213255A1 (en) 2012-01-25 2014-08-07 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
RU2015107803A (ru) * 2012-08-06 2016-09-27 Савира Фармасьютикалз Гмбх Производные дигидроксипиримидинкарбоновой кислоты и их применение в лечении, облегчении или предотвращении вирусного заболевания
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
KR102186030B1 (ko) 2012-10-29 2020-12-03 시플라 리미티드 항 바이러스성 포스포네이트 유사체 및 이의 제조를 위한 방법
US9714243B2 (en) 2012-12-17 2017-07-25 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as HIV integrase inhibitors
CN111303152B (zh) 2012-12-21 2023-04-11 吉利德科学公司 多环-氨基甲酰基吡啶酮化合物及其药物用途
WO2014172188A2 (en) 2013-04-16 2014-10-23 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
HUE036384T2 (hu) 2013-05-17 2018-07-30 Merck Sharp & Dohme Fúzionált triciklusos heterociklikus vegyületek mint HIV integráz inhibitorok
EP3008044B1 (en) 2013-06-13 2018-11-21 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
NO2865735T3 (hr) 2013-07-12 2018-07-21
DK3019503T3 (da) 2013-07-12 2017-11-20 Gilead Sciences Inc Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner
AP2016009157A0 (en) 2013-09-27 2016-04-30 Merck Sharp & Dohme Substituted quinolizine derivatives useful as hiv integrase inhibitors
EP3087060B1 (en) 2013-12-23 2020-05-13 Merck Sharp & Dohme Corp. Pyrimidone carboxamide compounds as pde2 inhibitors
US20170253585A1 (en) * 2014-02-03 2017-09-07 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
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
TWI744723B (zh) 2014-06-20 2021-11-01 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 (hr) 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
EP3285581B1 (en) 2015-03-26 2021-08-11 Merck Sharp & Dohme Corp. Pyrazolyl pyrimidinone compounds as pde2 inhibitors
EP3466490B1 (en) 2015-04-02 2020-10-21 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
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
WO2017220208A1 (en) 2016-06-21 2017-12-28 Pharmathen S.A. Process for preparing compounds useful as intermediates for the preparation of raltegravir
AU2017329049A1 (en) 2016-09-15 2019-04-04 Lupin Limited Process for the preparation of pure and stable crystalline Raltegravir potassium Form 3
RU2749043C2 (ru) 2016-12-02 2021-06-03 Мерк Шарп И Доум Корп. Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич
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
US11246869B2 (en) 2017-11-14 2022-02-15 Cambrex Profarmaco Milano S.R.L. Process for the preparation of Raltegravir
AU2020316056A1 (en) * 2019-07-23 2022-02-03 Constellation Pharmaceuticals, Inc. Modulators of TREX1
US20230073216A1 (en) 2020-01-23 2023-03-09 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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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 (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3608606A1 (de) 1985-03-16 1986-09-18 The Wellcome Foundation Ltd., London 3'-azido-3'-deoxythymidin oder eine, ein pharmazeutisch vertraegliches derivat davon enthaltende pharmazeutische formulierung, verfahren zu ihrer herstellung und ihre verwendung
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 (hr) 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
CA2333771A1 (en) 1998-06-03 1999-12-09 Mark W. Embrey Hiv integrase inhibitors
CN1154493C (zh) 1998-08-20 2004-06-23 富山化学工业株式会社 含氮杂环羧酰胺衍生物或其盐以及含有二者的抗病毒药
ID29027A (id) 1998-12-25 2001-07-26 Shionogi & Co Turunan-turunan heteroaromatik yang mempunyai aktivitas penghambatan terhadap integrase hiv
WO2001000578A1 (en) 1999-06-25 2001-01-04 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
DE60138635D1 (de) 2000-10-12 2009-06-18 Merck & Co Inc Aza- und polyaza naphthalenyl karboxamide als inhibitoren der hiv-integrase
DE60128936T2 (de) 2000-10-12 2008-04-10 Merck & Co, Inc. Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
AU2002246499B2 (en) 2000-10-12 2005-12-22 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
EP1333831A2 (en) 2000-10-12 2003-08-13 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
EP1375486B1 (en) 2001-03-01 2008-10-15 Shionogi & Co., Ltd. Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
ATE530520T1 (de) 2001-08-10 2011-11-15 Shionogi & Co Antivirales mittel
CA2463975A1 (en) 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
CA2463976C (en) * 2001-10-26 2007-02-13 Benedetta Crescenzi 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
TR200401663T1 (tr) 2002-11-20 2005-04-21 Japan Tobacco Inc. 4-oksokuinolin bileşiği ve bunun HIV integraz inhibitörü olarak kullanımı.
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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

Also Published As

Publication number Publication date
EA200400585A1 (ru) 2004-10-28
HRP20040373A2 (en) 2005-08-31
CA2463976C (en) 2007-02-13
HK1085665A1 (en) 2006-09-01
HUP0401740A2 (hu) 2004-12-28
LU91428I2 (fr) 2008-06-09
BR0213522B8 (pt) 2017-07-04
LTC1441735I2 (lt) 2020-06-25
WO2003035077A1 (en) 2003-05-01
US20110034449A1 (en) 2011-02-10
US7435734B2 (en) 2008-10-14
MXPA04003932A (es) 2004-06-18
EP1441735A1 (en) 2004-08-04
NO2008007I2 (hr) 2010-09-27
CA2463976A1 (en) 2003-05-01
DK1441735T3 (da) 2006-06-12
NL300340I1 (nl) 2008-06-02
BRPI0213522C1 (pt) 2021-05-25
YU35604A (sh) 2006-08-17
DE60209381T2 (de) 2006-10-05
CN1700918B (zh) 2011-06-08
JP3927175B2 (ja) 2007-06-06
NO2020026I1 (no) 2020-08-10
DE122009000048I1 (de) 2010-04-08
CN102219750B (zh) 2013-05-29
IS7213A (is) 2004-04-07
SI1441735T1 (sl) 2006-06-30
NO2008007I1 (no) 2008-06-23
US20050025774A1 (en) 2005-02-03
HU230248B1 (hu) 2015-11-30
KR20040047981A (ko) 2004-06-05
KR100862879B1 (ko) 2008-10-15
CY2008008I1 (el) 2009-11-04
BR0213522A (pt) 2004-09-08
US20070123524A1 (en) 2007-05-31
DE122008000016I1 (de) 2011-12-01
IS2436B (is) 2008-10-15
CN102219750A (zh) 2011-10-19
US20060258860A1 (en) 2006-11-16
PL212914B1 (pl) 2012-12-31
LTPA2008007I1 (lt) 2020-05-11
NL300340I2 (nl) 2008-08-01
CO5580777A2 (es) 2005-11-30
HUP0401740A3 (en) 2009-06-29
UA77454C2 (en) 2006-12-15
ES2258668T3 (es) 2006-09-01
EA007060B1 (ru) 2006-06-30
US7820660B2 (en) 2010-10-26
NZ533057A (en) 2005-11-25
RS51542B (sr) 2011-06-30
US7169780B2 (en) 2007-01-30
NO325206B1 (no) 2008-02-25
BR0213522B1 (pt) 2017-06-13
JP2005511543A (ja) 2005-04-28
DE60209381D1 (de) 2006-04-27
IL161337A (en) 2010-02-17
ME00427B (me) 2011-10-10
US20080275004A1 (en) 2008-11-06
FR08C0026I2 (fr) 2010-01-22
CN1700918A (zh) 2005-11-23
GEP20063848B (en) 2006-06-12
IL161337A0 (en) 2004-09-27
FR08C0026I1 (hr) 2008-07-18
PL369223A1 (en) 2005-04-18
HUS1600016I1 (hu) 2018-05-02
CN102229605B (zh) 2015-01-14
AU2002334207A2 (en) 2003-05-06
AU2002334207B2 (en) 2006-02-23
ZA200402796B (en) 2005-03-30
EP1441735B1 (en) 2006-02-22
US7217713B2 (en) 2007-05-15
ATE318140T1 (de) 2006-03-15
PT1441735E (pt) 2006-06-30
CN102229605A (zh) 2011-11-02
NO20042165L (no) 2004-05-25

Similar Documents

Publication Publication Date Title
HRP20040373B1 (hr) N-supstituirani hidroksipiridinon karboksamid inhibitori hiv integraze
RS52883B (en) HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
HRP20100614T1 (hr) Soli 3,7-diamino-10h-fenotiazina i njihova uporaba
HRP20060100T3 (hr) Derivati diaril i arilheteroaril uree kao modulatori 5-ht2a serotonin receptora korisni za profilaksu i liječenje poremećaja povezanih s njima
RS52099B (en) SUBSTITUTED BENZIMIDAZOLES AS KINASE INHIBITORS
EA200602060A1 (ru) Производные пирролидин-2-она и пиперидин-2-она, используемые в качестве ингибиторов 11-бета-гидроксистероид-дегидрогеназы
CO5580832A2 (es) Compuestos isoquinolina terapeuticos
RS53019B (en) DERIVATIVES OF ADAMANTYL DIAMIDE AND THEIR USE
RS52247B (en) SUBSTITUTED PHENOXES N-ALKYLED THIAZOLDINDION AS MODULATORS OF ESTROGEN RELATED ALFA-RECEPTORS
EA200602058A1 (ru) Производные адамантилпирролидин-2-она в качестве ингибиторов 11-бета-гидроксистероид-дегидрогеназы
SE0000540D0 (sv) New compounds
ATE297910T1 (de) Retinoid x rezeptormodulatoren
DK1257553T3 (da) Pyrrolopyrimidinonderivater, fremgangsmåder til fremstilling og anvendelse
HRP20040112B1 (hr) Kristali koji sadrže n-[2-(dietilamino)etil]-5-[(5-fluoro-2-okso-3h-indol-3-iliden)metil]-2,4-dimetil-1h-pirol-3-karboksamidnu sol jabučne kiseline, postupak za njihovu pripravu i njihovi pripravci
HRP20000854B1 (en) Therapeutic biaryl derivatives
CY1107886T1 (el) Αναστολεις κινασης ως θεραπευτικοι παραγοντες
EP1371650A4 (en) ACTIVATED RECEPTOR ACTIVATOR BY PEROXYSOME PROLIFIERS
BG104248A (en) Benzamidoxim derivatives, intermediate products and methods for preparing and using them as fungicides
AR041816A1 (es) Compuesto de acil-pirrolidina, su uso para preparar una composicion farmaceutica, composicion farmaceutica que lo comprende y procedimiento para prepararlo
DE602004024093D1 (de) 2,4-dioxo-3-chinazolinylarylsulfonylharnstoffe
DK0769010T3 (da) 2-[1',2',4'-triazol-3'-yloxymethylen]-anilider og deres anvendelse som pesticider
BR9911048A (pt) Inibidor de spla2 de pirrolo[1,2-b]piridazina
RS51047B (sr) Derivati 4-tetrazolil-4-fenilpiperidina za lečenje bola
RS52661B (en) THERAPEUTIC MEANS
RS50574B (sr) (4-metoksi-7-morfolin-4-il-benzotiazol-2-il)-amid 4-hidroksi-4-metil-piperidin-1-karboksilne kiseline

Legal Events

Date Code Title Description
A1OB Publication of a patent application
ARAI Request for the grant of a patent on the basis of the submitted results of a substantive examination of a patent application
B1PR Patent granted
PNAN Change of the applicant name, address/residence

Owner name: MSD ITALIA S.R.L., IT

Owner name: INSTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. AN

ODRP Renewal fee for the maintenance of a patent

Payment date: 20191009

Year of fee payment: 18

ODRP Renewal fee for the maintenance of a patent

Payment date: 20201001

Year of fee payment: 19

ODRP Renewal fee for the maintenance of a patent

Payment date: 20211005

Year of fee payment: 20

PB20 Patent expired after termination of 20 years

Effective date: 20221021