ATE433974T1 - Azachinolinolphosphonatverbindungen als integraseinhibitoren - Google Patents

Azachinolinolphosphonatverbindungen als integraseinhibitoren

Info

Publication number
ATE433974T1
ATE433974T1 AT04784571T AT04784571T ATE433974T1 AT E433974 T1 ATE433974 T1 AT E433974T1 AT 04784571 T AT04784571 T AT 04784571T AT 04784571 T AT04784571 T AT 04784571T AT E433974 T1 ATE433974 T1 AT E433974T1
Authority
AT
Austria
Prior art keywords
azachinolinol
integras
inhibitors
phosphonate compounds
phosphonate
Prior art date
Application number
AT04784571T
Other languages
English (en)
Inventor
Haolun Jin
Choung Kim
Peter Nelson
Original Assignee
Gilead Sciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Application granted granted Critical
Publication of ATE433974T1 publication Critical patent/ATE433974T1/de

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65744—Esters of oxyacids of phosphorus condensed with carbocyclic or heterocyclic rings or ring systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thyristors (AREA)
  • Metal-Oxide And Bipolar Metal-Oxide Semiconductor Integrated Circuits (AREA)
AT04784571T 2003-09-19 2004-09-17 Azachinolinolphosphonatverbindungen als integraseinhibitoren ATE433974T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US50405003P 2003-09-19 2003-09-19
PCT/US2004/030743 WO2005028478A1 (en) 2003-09-19 2004-09-17 Aza-quinolinol phosphonate integrase inhibitor compounds

Publications (1)

Publication Number Publication Date
ATE433974T1 true ATE433974T1 (de) 2009-07-15

Family

ID=34375443

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04784571T ATE433974T1 (de) 2003-09-19 2004-09-17 Azachinolinolphosphonatverbindungen als integraseinhibitoren

Country Status (7)

Country Link
US (2) US7462721B2 (de)
EP (1) EP1664046B1 (de)
AT (1) ATE433974T1 (de)
AU (1) AU2004274493A1 (de)
CA (1) CA2537325A1 (de)
DE (1) DE602004021611D1 (de)
WO (1) WO2005028478A1 (de)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8539401A1 (es) * 2001-02-14 2002-10-28 Warner Lambert Co Quinazolinas como inhibidores de mmp-13
US7572914B2 (en) * 2003-12-19 2009-08-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
KR20070002006A (ko) 2004-02-11 2007-01-04 스미스클라인 비참 코포레이션 Ｈｉｖ 인테그라제 억제제
EP1763524A1 (de) * 2004-04-23 2007-03-21 Takeda San Diego, Inc. Indolderivate und deren verwendung als kinaseinhibitoren
WO2006023931A2 (en) * 2004-08-18 2006-03-02 Takeda San Diego, Inc. Kinase inhibitors
US7713973B2 (en) * 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
US20080234231A1 (en) * 2005-08-04 2008-09-25 Johns Brian A Hiv Integrase Inhibitors
EP1910356A4 (de) * 2005-08-04 2009-10-21 Smithkline Beecham Corp Hiv-integrasehemmer
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
US20070287707A1 (en) * 2006-02-28 2007-12-13 Arrington Mark P Phosphodiesterase 10 inhibitors
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
US8071766B2 (en) 2008-02-01 2011-12-06 Takeda Pharmaceutical Company Limited HSP90 inhibitors
NZ598766A (en) 2009-10-13 2013-09-27 Elanco Animal Health Ireland Macrocyclic integrase inhibitors
EP2552923B1 (de) 2010-04-02 2014-03-26 Janssen R&D Ireland Makrocyclische integraseinhibitoren
JP5605029B2 (ja) * 2010-07-06 2014-10-15 住友化学株式会社 化合物、樹脂及びレジスト組成物
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
CN102885846B (zh) * 2011-07-18 2014-02-19 中国医学科学院医药生物技术研究所 2-硫代-6-氮杂尿苷在制备抗hiv-1病毒的药物中的应用
US8954475B2 (en) 2011-11-10 2015-02-10 Microsoft Technology Licensing, Llc Deep cloning of objects using binary format
CN104185420B (zh) 2011-11-30 2017-06-09 埃默里大学 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂
WO2013095684A1 (en) 2011-12-22 2013-06-27 Geron Corporation Guanine analogs as telomerase substrates and telomere length affectors
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
SG10202105371YA (en) 2014-12-26 2021-07-29 Univ Emory N4-hydroxycytidine and derivatives and anti-viral uses related thereto
TW201636329A (zh) 2015-02-02 2016-10-16 佛瑪治療公司 作為ｈｄａｃ抑制劑之雙環［４，６，０］異羥肟酸
ES2770123T3 (es) 2015-02-02 2020-06-30 Forma Therapeutics Inc Acidos 3-alquil-4-amido-bicíclicos [4,5,0]hidroxámicos como inhibidores de HDAC
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
EP3472131B1 (de) 2016-06-17 2020-02-19 Forma Therapeutics, Inc. 2-spiro-5- und 6-hydroxamsäureindane als hdac-inhibitoren
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN107325099A (zh) * 2017-06-05 2017-11-07 李芷琪 具有杀虫活性的哌啶并吡啶并4,5‑二氢‑1,2,3‑三氮唑类衍生物的制备方法
FI3706762T3 (fi) 2017-12-07 2024-12-13 Univ Emory N4-hydroksisytidiini ja johdannaisia sekä niihin liittyviä virusten vastaisia käyttötapoja
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
KR20230057341A (ko) 2020-07-02 2023-04-28 인사이트 코포레이션 Jak2 v617f 억제제로서 삼환계 우레아 화합물
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
EP4323405A1 (de) 2021-04-12 2024-02-21 Incyte Corporation Kombinationstherapie mit einem fgfr-inhibitor und einem auf nectin-4 abzielenden mittel
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
PT4426434T (pt) 2021-11-02 2025-11-24 Flare Therapeutics Inc Agonistas inversos de pparg e suas utilizações
PE20251706A1 (es) 2022-03-17 2025-07-02 Incyte Corp Compuestos de urea triciclica como inhibidores de v617f de jak2

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4816570A (en) * 1982-11-30 1989-03-28 The Board Of Regents Of The University Of Texas System Biologically reversible phosphate and phosphonate protective groups
US4968788A (en) * 1986-04-04 1990-11-06 Board Of Regents, The University Of Texas System Biologically reversible phosphate and phosphonate protective gruops
EP0533833B1 (de) * 1990-06-13 1995-12-20 GLAZIER, Arnold Phosphorylierte prodrugs
DE69129650T2 (de) * 1990-09-14 1999-03-25 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic, Prag/Praha Wirkstoffvorläufer von Phosphonaten
US5883255A (en) * 1990-10-31 1999-03-16 Smithkline Beecham Corporation Substituted indolizino 1,2-b!quinolinones
US5639881A (en) * 1991-11-08 1997-06-17 Arizona Board Of Regents Acting On Behalf Of Arizona State University Synthesis and elucidation of pyrimido (4,5-Q) quinazoline derivatives
WO1993017681A1 (en) 1992-03-02 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
US5798340A (en) * 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
DE19613591A1 (de) * 1996-04-04 1997-10-09 Hoechst Ag Substituierte-Chinolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung
AU4172197A (en) * 1996-09-10 1998-04-02 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
WO1999062520A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
CA2329134A1 (en) 1998-06-03 1999-12-09 David L. Clark Hiv integrase inhibitors
WO2000000475A1 (en) * 1998-06-30 2000-01-06 Du Pont Pharmaceuticals Company Substituted quinolin-2(1h)-ones useful as hiv reverse transcriptase inhibitors
US6187907B1 (en) * 1998-08-31 2001-02-13 James Chen Triple helix coil template having a biologically active ligand
AU3118200A (en) 1998-12-14 2000-07-03 Merck & Co., Inc. Hiv integrase inhibitors
TR200103801T2 (tr) 1999-06-02 2002-04-22 Shonogi & Co., Ltd. Yeni ikameli propenon türevlerinin hazırlanması için prosesler
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
US6245806B1 (en) 1999-08-03 2001-06-12 Merck & Co., Inc. HIV integrase inhibitors
AU8009900A (en) * 1999-10-13 2001-04-23 Merck & Co., Inc. Hiv integrase inhibitors
US6245402B1 (en) * 1999-12-14 2001-06-12 Xerox Corporation Imageable seam intermediate transfer belt having an overcoat
PE20011349A1 (es) 2000-06-16 2002-01-19 Upjohn Co 1-aril-4-oxo-1,4-dihidro-3-quinolincarboxamidas como agentes antivirales
US6525049B2 (en) 2000-07-05 2003-02-25 Pharmacia & Upjohn Company Pyrroloquinolones as antiviral agents
WO2002030931A2 (en) * 2000-10-12 2002-04-18 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
CA2425625A1 (en) 2000-10-12 2002-07-18 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
CA2425067A1 (en) 2000-10-12 2002-05-10 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
DE60128936T2 (de) 2000-10-12 2008-04-10 Merck & Co, Inc. Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
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
CA2456155A1 (en) 2001-08-17 2003-02-27 Merck & Co., Inc. Process for preparing 5-sulfonamido-8-hydroxy-1, 6-naphthyridine-7-carboxamides
FR2830863B1 (fr) 2001-10-12 2004-01-30 Bioalliance Pharma Derives de quinoleine, procede de synthese, et medicaments renfermant ces derives
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
AU2003301439A1 (en) 2002-10-16 2004-05-04 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds

Also Published As

Publication number Publication date
EP1664046B1 (de) 2009-06-17
US20070185007A1 (en) 2007-08-09
EP1664046A1 (de) 2006-06-07
US7462721B2 (en) 2008-12-09
WO2005028478A1 (en) 2005-03-31
AU2004274493A1 (en) 2005-03-31
US20050137199A1 (en) 2005-06-23
CA2537325A1 (en) 2005-03-31
DE602004021611D1 (de) 2009-07-30

Similar Documents

Publication Publication Date Title
ATE433974T1 (de) Azachinolinolphosphonatverbindungen als integraseinhibitoren
WO2004035577A3 (en) Pre-organized tricyclic integrase inhibitor compounds
WO2007056281A3 (en) Multivalent indole compounds and use thereof as phospholipase-a2 inhibitors
DE60322224D1 (de) Kondensierte heterozyklische verbindungen als petidase inhibitoren
ATE478044T1 (de) Biphenylderivate und ihre verwendung bei der behandlung von hepatitis c
ATE425983T1 (de) Siloxy substituierte metallocenkatalysatoren
HUP0303849A2 (hu) Benzimidazol- és piridolimidazol-származékok GABA receptor ligandumokként, előállításuk és ezeket tartalmazó gyógyszerkészítmények
EP1731523A4 (de) Thiazolopyrimidinderivat
MEP8409A (en) Fused heterocyclic compound
TW200602319A (en) Indole derivative and use thereof
ATE423113T1 (de) Substituierte oxoazaheterozyclische verbindungen
UA83243C2 (ru) Соединения, которые ингибируют натриезависимый переносчик глюкозы
TW200716632A (en) Integrase inhibitor compounds
WO2006109075A3 (en) Hydroxybenzamide derivatives and their use as inhibitors of hsp90
EA200870117A1 (ru) Азаиндоловые ингибиторы аурора-киназ
TW200740752A (en) 4-Biarylyl-1-phenylazetidin-2-ones
DE602005010413D1 (de) Phosphonatanaloga von hiv-integrasehemmerverbindungen
UA96568C2 (en) Polycyclic carbamoyl pyridone derivative as hiv-integrase inhibitor
HUP0004227A2 (hu) Eljárás orto-helyzetben közvetlen fémbevitelre 5-(2-szubsztituált-fenil)-tetrazol-származékok előállításánál
ATE447575T1 (de) Selektive spirocyclische glucocorticoid-rezeptor- modulatoren
EA200970642A1 (ru) Трициклическое соединение и его фармацевтическое применение
TW200420559A (en) Amine compounds and method for producing the same
ATE427310T1 (de) Kondensierte bicyclische pyrimidinderivate
MY139258A (en) Carbamoyl-type benzofuran derivatives
EA201300599A1 (ru) Замещенные гидрированные тиено-пирроло[3,2-с]пиридины, лиганды, фармацевтическая композиция и способ их применения

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties