JP5620376B2 - Ｈｉｖ阻害剤化合物の塩 - Google Patents

Ｈｉｖ阻害剤化合物の塩 Download PDF

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JP5620376B2
JP5620376B2 JP2011517525A JP2011517525A JP5620376B2 JP 5620376 B2 JP5620376 B2 JP 5620376B2 JP 2011517525 A JP2011517525 A JP 2011517525A JP 2011517525 A JP2011517525 A JP 2011517525A JP 5620376 B2 JP5620376 B2 JP 5620376B2
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salt
pharmaceutical composition
hydrate
fluoro
ethyl
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JP2011527687A (ja
JP2011527687A5 (https=
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ベンジャミン アール． グレーツ，
ベンジャミン アール． グレーツ，
リチャード ピー． ポルニアスゼク，
リチャード ピー． ポルニアスゼク，
Original Assignee
ギリアード サイエンシーズ， インコーポレイテッド
ギリアード サイエンシーズ， インコーポレイテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Biophysics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • AIDS & HIV (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2011517525A 2008-07-08 2009-07-07 Ｈｉｖ阻害剤化合物の塩 Active JP5620376B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US7898908P 2008-07-08 2008-07-08
US61/078,989 2008-07-08
PCT/US2009/049838 WO2010005986A1 (en) 2008-07-08 2009-07-07 Salts of hiv inhibitor compounds

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2014054797A Division JP2014122235A (ja) 2008-07-08 2014-03-18 Ｈｉｖ阻害剤化合物の塩

Publications (3)

Publication Number Publication Date
JP2011527687A JP2011527687A (ja) 2011-11-04
JP2011527687A5 JP2011527687A5 (https=) 2012-08-23
JP5620376B2 true JP5620376B2 (ja) 2014-11-05

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Family Applications (2)

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JP2011517525A Active JP5620376B2 (ja) 2008-07-08 2009-07-07 Ｈｉｖ阻害剤化合物の塩
JP2014054797A Withdrawn JP2014122235A (ja) 2008-07-08 2014-03-18 Ｈｉｖ阻害剤化合物の塩

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Country Status (26)

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US (6) US20100093667A1 (https=)
EP (1) EP2307435B1 (https=)
JP (2) JP5620376B2 (https=)
KR (1) KR101642527B1 (https=)
CN (1) CN102089318B (https=)
AP (1) AP3347A (https=)
AU (1) AU2009268681B2 (https=)
BR (1) BRPI0915878A2 (https=)
CA (1) CA2729769C (https=)
CL (1) CL2011000014A1 (https=)
CO (1) CO6321288A2 (https=)
CY (1) CY1113240T1 (https=)
DK (1) DK2307435T3 (https=)
EA (1) EA018308B1 (https=)
EC (1) ECSP11010807A (https=)
ES (1) ES2393962T3 (https=)
HR (1) HRP20120700T1 (https=)
IL (1) IL210006A (https=)
MX (1) MX2011000306A (https=)
NZ (1) NZ590075A (https=)
PE (1) PE20110219A1 (https=)
PL (1) PL2307435T3 (https=)
PT (1) PT2307435E (https=)
UA (1) UA103329C2 (https=)
WO (1) WO2010005986A1 (https=)
ZA (1) ZA201100694B (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2359833A1 (en) 2003-04-25 2011-08-24 Gilead Sciences, Inc. Antiviral phosphonate analogs
ME03423B (me) * 2004-07-27 2020-01-20 Gilead Sciences Inc Fosfonatni analozi jedinjenja hiv inhibitora
UA103329C2 (ru) 2008-07-08 2013-10-10 Гилиад Сайенсиз, Инк. Соли соединений-ингибиторов вич
US9447050B2 (en) 2011-04-05 2016-09-20 The Translational Genomics Research Institute Solid forms of curcumin
CA2835932C (en) 2011-05-19 2020-03-24 Gilead Sciences, Inc. Processes and intermediates for preparing anti-hiv agents
DK3236972T3 (en) 2014-12-26 2021-10-04 Univ Emory Antivirale N4-hydroxycytidin-derivativer
WO2018064071A1 (en) * 2016-09-27 2018-04-05 Gilead Sciences, Inc. Therapeutic compositions for treatment of human immunodeficiency virus
SI3661937T1 (sl) 2017-08-01 2021-11-30 Gilead Sciences, Inc. Kristalinične oblike etil((S)-((((2R,5R)-5-(6-amino-9H-purin-9-IL)-4- fluoro-2,5-dihidrofuran-2-IL)oksi)metil)(fenoksi)fosforil)-L-alaninata (GS-9131) za zdravljenje virusnih okužb
JP6804790B1 (ja) 2017-12-07 2020-12-23 エモリー ユニバーシティー Ｎ４−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途

Family Cites Families (164)

* 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
US4649041A (en) * 1983-07-20 1987-03-10 Warner-Lambert Company Magnesium trisilicate suitable for preparation of medicament adsorbates of antinauseants
DK159431C (da) * 1984-05-10 1991-03-18 Byk Gulden Lomberg Chem Fab 6-phenyl-3(2h)-pyridazinoner, fremgangsmaade til fremstilling deraf, laegemidler indeholdende disse samt anvendelse af forbindelserne til fremstilling af laegemidler
US4968788A (en) 1986-04-04 1990-11-06 Board Of Regents, The University Of Texas System Biologically reversible phosphate and phosphonate protective gruops
US5455339A (en) * 1986-05-01 1995-10-03 University Of Georgia Research Foundation, Inc. Method for the preparation of 2',3'-dideoxy and 2',3'-dideoxydide-hydro nucleosides
IE63869B1 (en) 1986-11-06 1995-06-14 Res Dev Foundation Aerosols containing liposomes and method for their preparation
FR2611203B1 (fr) 1987-02-20 1989-06-09 Sturtz Georges Analogues gem-diphosphoniques d'amethopterine (methotrexate) et de derives deaza-n-10 amethopterine. leur preparation et les compositions pharmaceutiques qui les contiennent
JP2737191B2 (ja) * 1987-12-28 1998-04-08 東ソー株式会社 均質な石英ガラス塊の製造方法
US5631370A (en) * 1988-01-20 1997-05-20 Regents Of The University Of Minnesota Optically-active isomers of dideoxycarbocyclic nucleosides
US5466793A (en) * 1988-03-01 1995-11-14 Ajinomoto Co., Inc. Process for preparing 2', 3'- dideoxyinosine
ZA894534B (en) 1988-06-20 1990-03-28 Merrell Dow Pharma Novel neplanocin derivatives
US5744600A (en) * 1988-11-14 1998-04-28 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Phosphonomethoxy carbocyclic nucleosides and nucleotides
CA2001715C (en) 1988-11-14 1999-12-28 Muzammil M. Mansuri Carbocyclic nucleosides and nucleotides
US5202128A (en) * 1989-01-06 1993-04-13 F. H. Faulding & Co. Limited Sustained release pharmaceutical composition
JP2722673B2 (ja) 1989-05-31 1998-03-04 住友化学工業株式会社 光学活性なアシルビフェニル誘導体の製造法
DE4003574A1 (de) 1990-02-07 1991-08-08 Bayer Ag Neue dipeptide, verfahren zu ihrer herstellung und ihre verwendung als renininhibitoren in arzneimitteln
ATE131825T1 (de) 1990-06-13 1996-01-15 Arnold Glazier Phosphorylierte prodrugs
EP0465297B1 (en) 1990-07-04 1996-01-31 Merrell Dow Pharmaceuticals Inc. 9-Purinyl phosphonic acid derivatives
US5177064A (en) 1990-07-13 1993-01-05 University Of Florida Targeted drug delivery via phosphonate derivatives
EP0468119A1 (en) 1990-07-24 1992-01-29 Merrell Dow Pharmaceuticals Inc. Novel carbocyclic analogs of certain nucleosides
US5223618A (en) 1990-08-13 1993-06-29 Isis Pharmaceuticals, Inc. 4'-desmethyl nucleoside analog compounds
EP0481214B1 (en) * 1990-09-14 1998-06-24 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
US5672697A (en) 1991-02-08 1997-09-30 Gilead Sciences, Inc. Nucleoside 5'-methylene phosphonates
DE4111730A1 (de) 1991-04-10 1992-10-15 Knoll Ag Neue cytarabin-derivate, ihre herstellung und verwendung
JP2648897B2 (ja) * 1991-07-01 1997-09-03 塩野義製薬株式会社 ピリミジン誘導体
EP0531597A1 (en) 1991-09-12 1993-03-17 Merrell Dow Pharmaceuticals Inc. Novel unsaturated acyclic phosphonate derivatives of purine and pyrimidine
US5610294A (en) * 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
DE4138584A1 (de) 1991-11-23 1993-05-27 Hoechst Ag Carbocyclische phosphonat-nucleotidanaloge, deren herstellung und verwendung
GB9126144D0 (en) 1991-12-10 1992-02-12 British Bio Technology Compounds
FR2692265B1 (fr) 1992-05-25 1996-11-08 Centre Nat Rech Scient Composes biologiquement actifs de type phosphotriesters.
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
DE4308096A1 (de) 1993-03-13 1994-09-15 Hoechst Ag Prodrug-Derivate von Enzyminhibitoren mit Hydroxylgruppen, Verfahren zu deren Herstellung und ihre Verwendung
US5654286A (en) * 1993-05-12 1997-08-05 Hostetler; Karl Y. Nucleotides for topical treatment of psoriasis, and methods for using same
ATE199906T1 (de) 1993-06-29 2001-04-15 Mitsubishi Chem Corp Phosphonat-nukleotid ester-derivate
WO1995002582A1 (en) * 1993-07-14 1995-01-26 Ciba-Geigy Ag Cyclic hydrazine compounds
US5656745A (en) 1993-09-17 1997-08-12 Gilead Sciences, Inc. Nucleotide analogs
AU691527B2 (en) 1993-09-17 1998-05-21 Gilead Sciences, Inc. Nucleotide analogs
US5446137B1 (en) * 1993-12-09 1998-10-06 Behringwerke Ag Oligonucleotides containing 4'-substituted nucleotides
US5493030A (en) * 1994-02-18 1996-02-20 Syntex (U.S.A.) Inc. 5-substituted derivatives of mycophenolic acid
US5854227A (en) 1994-03-04 1998-12-29 Hartmann; John F. Therapeutic derivatives of diphosphonates
RU2157368C2 (ru) 1994-09-26 2000-10-10 Сионоги Энд Ко., Лтд. Производные имидазола и фармацевтическая композиция на их основе
WO1996014314A2 (en) 1994-11-04 1996-05-17 Gilead Sciences, Inc. Thiepane compounds inhibiting and detecting hiv protease
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
ES2097703B1 (es) * 1995-04-12 1997-12-01 Decox S L Una nueva composicion estimulante de la actividad cerebral basada en alcaloides de nucleo de eburnamenina, y sus metodos de preparacion.
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
JPH11508541A (ja) 1995-06-29 1999-07-27 ノボ ノルディスク アクティーゼルスカブ 新規な置換アザ二環式化合物
US5750493A (en) * 1995-08-30 1998-05-12 Raymond F. Schinazi Method to improve the biological and antiviral activity of protease inhibitors
EP0852233A4 (en) 1995-09-21 1999-09-15 Nippon Shinyaku Co Ltd CYCLOSPORIN PHOSPHATE DERIVATIVES AND MEDICINAL COMPOSITION
US5914332A (en) * 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
RU2106353C1 (ru) 1996-03-19 1998-03-10 Корпорация "С энд Ти Сайенс энд Текнолоджи Инк." Соли 5'-н-фосфоната 3'- азидо-3'-дезокситимидина, являющиеся специфическими ингибиторами продукции вируса иммунодефицита человека вич-1 и вич-2
US5656746A (en) * 1996-03-28 1997-08-12 The Proctor & Gamble Company Temporary wet strength polymers from oxidized reaction product of polyhydroxy polymer and 1,2-disubstituted carboxylic alkene
US5874577A (en) * 1996-04-03 1999-02-23 Medichem Research, Inc. Method for the preparing 9-12-(Diethoxyphosphonomethoxy)ethyl!adenine and analogues thereof
US5795909A (en) * 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
CA2261619C (en) 1996-07-26 2006-05-23 Gilead Sciences, Inc. Nucleotide analogs
US6194398B1 (en) 1996-08-13 2001-02-27 Mitsubishi Chemical Corporation Phosphonate nucleotide compound
EP0948341A4 (en) 1996-09-17 2003-05-21 Supergen Inc DERIVATIVES OF PHOSPHOLIPIDE MEDICINES
JP4118958B2 (ja) 1996-10-09 2008-07-16 ファーマセット，リミティド テトラホスホネート二環式トリス無水物
JP3378016B2 (ja) * 1996-12-26 2003-02-17 塩野義製薬株式会社 カルバモイル基を有するイミダゾール誘導体の製造法
WO1999029702A2 (en) 1997-12-10 1999-06-17 The Government Of The United States Of America Reppresented By The Secretary, Department Of Health And Human Services METHOD FOR SYNTHESIZING 9-(2,3-DIDEOXY-2-FLUORO-β-D-THREO-PENTOFURANOSYL)ADENINE (β-FddA)
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
US6174888B1 (en) * 1998-05-28 2001-01-16 Novartis Ag 2-amino-7-(1-substituted-2-hydroxyethyl)-3,5-dihydropyrrolo[3,2-D]pyrimidin-4-ones
AU4125099A (en) 1998-06-01 1999-12-20 S & T Science And Technology Inc. Antiviral phosphorus derivatives of 4'-thio-5-ethyl-2'-deoxyuridine
GB9815567D0 (en) 1998-07-18 1998-09-16 Glaxo Group Ltd Antiviral compound
TWI260322B (en) * 1999-02-12 2006-08-21 Vertex Pharma Inhibitors of aspartyl protease
US6761903B2 (en) * 1999-06-30 2004-07-13 Lipocine, Inc. Clear oil-containing pharmaceutical compositions containing a therapeutic agent
HUP0200260A3 (en) 1999-03-05 2002-11-28 Metabasis Therapeutics Inc San Novel phosphorus-containing prodrugs, their preparation and their use
DE19912636A1 (de) 1999-03-20 2000-09-21 Aventis Cropscience Gmbh Bicyclische Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Herbizide und pharmazeutische Mittel
US6258831B1 (en) * 1999-03-31 2001-07-10 The Procter & Gamble Company Viral treatment
US6608027B1 (en) * 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
DE19927689A1 (de) * 1999-06-17 2000-12-21 Gruenenthal Gmbh Orale Darreichungsformen zur Verabreichung einer fixen Kombination von Tramadol und Diclofenac
CA2377278C (en) * 1999-06-25 2010-03-23 Vertex Pharmaceuticals Incorporated Prodrugs of carbamate inhibitors of impdh
US6581606B2 (en) * 1999-07-06 2003-06-24 The Rx Files Corporation Method, apparatus and system for use in treating patient with a drug having an antineoplastic effect to optimize therapy and prevent an adverse drug response
CA2381425A1 (en) 1999-08-24 2001-03-01 Cellgate, Inc. Enhancing drug delivery across and into epithelial tissues using oligo arginine moieties
GB9920872D0 (en) 1999-09-04 1999-11-10 Glaxo Group Ltd Benzophenones as inhibitors of reverse transcriptase
IL131887A0 (en) 1999-09-14 2001-03-19 Dpharm Ltd Phospholipid prodrugs of anti-proliferative drugs
DE60038038T2 (de) 1999-12-03 2009-02-12 The Regents of The University of California at San Diego, La Jolla Phosphonatverbindungen
WO2001046204A1 (en) 1999-12-22 2001-06-28 Merck Frosst Canada & Co. Aromatic phosphonates as protein tyrosine phosphatase 1b (ptp-1b) inhibitors
WO2001064693A1 (fr) 2000-02-29 2001-09-07 Mitsubishi Pharma Corporation Compose de nucleotide de phosphonate
MY164523A (en) * 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
IL153363A0 (en) 2000-06-13 2003-07-06 Shionogi & Co Pharmaceutical compositions containing propenone derivatives
FR2810322B1 (fr) 2000-06-14 2006-11-10 Pasteur Institut PRODUCTION COMBINATOIRE D'ANALOGUES DE NUCLEOTIDES ET NUCLEOTIDES (XiTP)
UA72612C2 (en) 2000-07-06 2005-03-15 Pyrido[2.3-d]pyrimidine and pyrimido[4.5-d]pyrimidine nucleoside analogues, prodrugs and method for inhibiting growth of neoplastic cells
US6617310B2 (en) 2000-07-19 2003-09-09 Bristol-Myers Squibb Pharma Company Phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines
CZ304734B6 (cs) 2000-07-21 2014-09-10 Gilead Sciences, Inc. Způsob přípravy 9-[2-(fosfonomethoxy)propyl]adeninu a 9-[2-(fosfonomethoxy)ethyl]adeninu
US6420586B1 (en) 2000-08-15 2002-07-16 University Of Kansas Amino acid-derived cyclic phosphonamides and methods of synthesizing the same
WO2002020010A1 (en) * 2000-09-08 2002-03-14 Zeria Pharmaceutical Co., Ltd. Pharmaceutical compositions containing aminothiazole derivatives for the treatment of colonic motor dysfunctions
RU2188203C2 (ru) 2000-10-05 2002-08-27 Государственный научный центр вирусологии и биотехнологии "Вектор" 2',3'-дидегидро-2',3'-дидезокситимидин-5'[(этоксикарбонил)(этил)фосфонат]- ингибитор репродукции вируса иммунодефицита человека
GB0028429D0 (en) * 2000-11-22 2001-01-10 Astrazeneca Ab Therapy
WO2002048165A2 (en) 2000-12-15 2002-06-20 Pharmasset Ltd. Antiviral agents for treatment of flaviviridae infections
PL209375B1 (pl) * 2000-12-28 2011-08-31 Kissei Pharmaceutical Pochodne glukopiranozyloksypirazolu, kompozycja farmaceutyczna zawierająca takie pochodne i zastosowanie tych pochodnych do wytwarzania kompozycji farmaceutycznej
WO2002057425A2 (en) 2001-01-22 2002-07-25 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
MXPA03005403A (es) * 2001-01-31 2003-09-25 Warner Lambert Co Metodo para carbamoilar alcoholes.
EP1864967A1 (en) * 2001-02-12 2007-12-12 Wyeth Method for preparing O-desmethyl-venlafaxine
US6962684B2 (en) * 2001-05-31 2005-11-08 Sumitomo Chemical Company, Limited Activated alumina formed body and method for producing the same
GB0114286D0 (en) 2001-06-12 2001-08-01 Hoffmann La Roche Nucleoside Derivatives
ATE371026T1 (de) 2001-06-20 2007-09-15 Nuevolution As Eine methode zur synthese von matrizenabhängigen molekülen
KR20020097384A (ko) * 2001-06-20 2002-12-31 미쯔비시 도꾜 세이야꾸 가부시끼가이샤 기존의 약제에 내성변이를 가지는 바이러스에 유효한 약제
ATE411805T1 (de) * 2001-07-20 2008-11-15 Bioagency Ag Organo-phosphorverbindungen zur aktivierung von gamma/delta-t-zellen
KR100879693B1 (ko) * 2001-08-17 2009-01-21 상꾜 아그로 가부시키가이샤 2-시클로프로필-6-메틸페놀
WO2003028737A1 (en) 2001-08-30 2003-04-10 Mitsubishi Pharma Corporation Anti-viral agents and in-vitro method for the identification of candidates able to inhibit binding of polymerase to epsilon
EP1461040B1 (en) * 2001-11-29 2006-03-15 Pfizer Products Inc. Succinic acid salts of 5,8,14-triazatetracyclo[10.3.1.0 2,11 .0 4,9 ]-hexadeca-2(11),3,5,7,9,-pentaene and pharmaceutical compositions thereof
AU2002343556A1 (en) 2001-12-07 2003-06-23 Eli Lilly And Company Use of phosphonate nucleotide analogue for treating hepatitis b virus infections
GEP20063872B (en) * 2001-12-12 2006-07-10 Pfizer Prod Inc Salt forms of e-2-methoxy-n-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quina-zolin-6-yl}-allyl)-acetamide and method of production
KR101016969B1 (ko) 2001-12-21 2011-02-25 에이자이 아이엔씨. 알콜 및 페놀의 수용성 포스포노옥시메틸 유도체를제조하는 방법
US20030198666A1 (en) * 2002-01-07 2003-10-23 Richat Abbas Oral insulin therapy
JP4547911B2 (ja) 2002-02-01 2010-09-22 アリアド・ファーマシューティカルズ・インコーポレイテッド リン含有化合物およびその用途
EP1472230B1 (en) 2002-02-08 2009-06-17 Conforma Therapeutic Corporation Ansamycins having improved pharmacological and biological properties
US7927613B2 (en) * 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
WO2003080078A1 (en) 2002-03-18 2003-10-02 Mitsubishi Pharma Corporation Treatment of pre-core hepatitis b virus mutant infections
WO2003087090A2 (en) * 2002-04-10 2003-10-23 Ortho-Mcneil Pharmaceutical,Inc. Novel heteroaryl alkylamide derivatives useful as bradykinin receptor modulators
AU2003231765B9 (en) 2002-04-26 2010-01-28 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such
US20050239054A1 (en) 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
US6872827B2 (en) * 2002-04-26 2005-03-29 Chembridge Research Laboratories, Inc. Somatostatin analogue compounds
US6808572B2 (en) * 2002-05-15 2004-10-26 Aerojet-General Corporation Solid propellant formulations and methods and devices employing the same for the destruction of airborne biological and/or chemical agents
EP1546138B1 (en) 2002-09-30 2012-01-18 A/S GEA Farmaceutisk Fabrik Raloxifene l-lactate or a hemihydrate thereof, their uses, pharmaceutical compositions and preparation processes
US20040157793A1 (en) * 2002-11-12 2004-08-12 Stuyver Lieven J. Modified nucleosides as antiviral agents
EA012844B1 (ru) * 2003-02-19 2009-12-30 Йельский Университет Аналоги противовирусных нуклеозидов и способы лечения вирусных инфекций, в частности вич-инфекций
WO2004100960A2 (en) 2003-04-25 2004-11-25 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
US7273716B2 (en) 2003-04-25 2007-09-25 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds with GS-7340 ester hydrolase
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
CN101410120A (zh) 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
WO2004096233A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Nucleoside phosphonate conjugates
WO2004096287A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
EP2359833A1 (en) 2003-04-25 2011-08-24 Gilead Sciences, Inc. Antiviral phosphonate analogs
US7470724B2 (en) 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7452901B2 (en) * 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
WO2004096235A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
WO2005002626A2 (en) 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
NZ542343A (en) 2003-04-25 2009-03-31 Gilead Sciences Inc Immunomodulator phosphonate conjugates
US7300924B2 (en) 2003-04-25 2007-11-27 Gilead Sciences, Inc. Anti-infective phosphonate analogs
MXPA05011296A (es) 2003-04-25 2006-01-24 Gilead Sciences Inc Conjugados de fosfonato inhibidores de la cinasa.
WO2004096237A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
WO2005000786A1 (en) 2003-05-23 2005-01-06 Transform Pharmaceuticals, Inc. Sertraline compositions
EP1634882A4 (en) * 2003-06-16 2008-01-09 Ajinomoto Kk INOSIN DERIVATIVE AND METHOD FOR THE PRODUCTION THEREOF
AU2004260789B2 (en) 2003-07-30 2011-06-30 Gilead Sciences, Inc. Nucleobase phosphonate analogs for antiviral treatment
BRPI0413595B8 (pt) * 2003-08-18 2021-05-25 H Lundbeck As sal de malonato, composição farmacêutica, uso de um sal de malonato, e, método de fabricação de um composto
US7427624B2 (en) 2003-10-24 2008-09-23 Gilead Sciences, Inc. Purine nucleoside phosphorylase inhibitory phosphonate compounds
WO2005044308A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
WO2005063751A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. 4’-substituted carbovir-and abacavir-derivatives as well as related compounds with hiv and hcv antiviral activity
CA2548951A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
US20050171126A1 (en) * 2003-12-26 2005-08-04 Ajinomoto Co., Inc. Process for the production of purine nucleoside compounds
US7404949B2 (en) * 2004-03-15 2008-07-29 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Methods and compositions useful to prevent in-grown hair arising from shaving
US20090035315A1 (en) * 2004-06-17 2009-02-05 Stephan Christgau Method of Improving Treatments in Rheumatic and Arthritic Diseases
ME03423B (me) * 2004-07-27 2020-01-20 Gilead Sciences Inc Fosfonatni analozi jedinjenja hiv inhibitora
WO2006015262A2 (en) 2004-07-29 2006-02-09 Coherix, Inc. Method for processing multiwavelength interferometric imaging data
US20060069060A1 (en) * 2004-09-27 2006-03-30 Sanjeev Redkar Salts of decitabine
US7154505B2 (en) 2004-11-11 2006-12-26 Stonecube Limited Method of and apparatus for generating a representation of an object
KR20060080817A (ko) * 2005-01-06 2006-07-11 씨제이 주식회사 시부트라민의 디카복실산염
MY148074A (en) * 2005-05-10 2013-02-28 Novartis Ag Pharmaceutical compositions comprising imatinib and a release retardant
AU2006278596A1 (en) * 2005-08-04 2007-02-15 Novartis Ag Salts of vildagliptin
DE102005041860A1 (de) * 2005-09-02 2007-03-08 Schering Ag Nanopartikulärer Einschluss- und Ladungskomplex für pharmazeutische Formulierungen
JP2009519952A (ja) * 2005-12-16 2009-05-21 ワイス トリアゾロピリミジン化合物の凍結乾燥組成物
US20060223820A1 (en) * 2006-03-21 2006-10-05 Chemagis Ltd. Crystalline aripiprazole salts and processes for preparation and purification thereof
US8895531B2 (en) * 2006-03-23 2014-11-25 Rfs Pharma Llc 2′-fluoronucleoside phosphonates as antiviral agents
JP5243413B2 (ja) * 2006-05-26 2013-07-24 スリーディー システムズ インコーポレーテッド ３次元プリンターで材料を処理する装置と方法
PL3150586T3 (pl) * 2007-02-23 2020-06-01 Gilead Sciences, Inc. Modulatory farmakokinetycznych właściwości środków terapeutycznych
US20090163449A1 (en) * 2007-12-20 2009-06-25 Eastman Chemical Company Sulfo-polymer powder and sulfo-polymer powder blends with carriers and/or additives
UA103329C2 (ru) * 2008-07-08 2013-10-10 Гилиад Сайенсиз, Инк. Соли соединений-ингибиторов вич
JP4330086B1 (ja) 2009-02-09 2009-09-09 株式会社テクネス 非酸化物セラミックス製品の製造方法
EP2305680A3 (en) 2009-09-30 2011-05-18 Aurobindo Pharma Limited Novel salts of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol
WO2014055618A1 (en) 2012-10-03 2014-04-10 Gilead Sciences, Inc. Solid state forms of hiv inhibitor: hemi-succinate of (2s)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid)
US20140094609A1 (en) 2012-10-03 2014-04-03 Gilead Sciences, Inc. Process for the preparation of an hiv integrase inhibitor

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