[go: up one dir, main page]

AR084044A1 - Compuestos 2’-espiro-nucleosidos - Google Patents

Compuestos 2’-espiro-nucleosidos

Info

Publication number
AR084044A1
AR084044A1 ARP110104450A ARP110104450A AR084044A1 AR 084044 A1 AR084044 A1 AR 084044A1 AR P110104450 A ARP110104450 A AR P110104450A AR P110104450 A ARP110104450 A AR P110104450A AR 084044 A1 AR084044 A1 AR 084044A1
Authority
AR
Argentina
Prior art keywords
alkyl
iii
hydrogen
acyl
formula
Prior art date
Application number
ARP110104450A
Other languages
English (en)
Inventor
Jinfa Du
Michael Joseph Sofia
Original Assignee
Pharmasset 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 Pharmasset Inc filed Critical Pharmasset Inc
Publication of AR084044A1 publication Critical patent/AR084044A1/es

Links

Classifications

    • 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
    • C07H19/207—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine adenine dinucleotide or nicotinamide-adenine dinucleotide
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61K31/708—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 having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • C07H19/06—Pyrimidine radicals
    • 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
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Management, Administration, Business Operations System, And Electronic Commerce (AREA)
  • User Interface Of Digital Computer (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Se revelan en la presente 2’-espiro-nucleósidos y sus derivados de utilidad para tratar a un sujeto infectado por el virus de hepatitis C o el virus del dengue. Se revela también un procedimiento para preparar el compuesto.Reivindicación 1: Un compuesto o su estereoisómero o su sal o metabolito o su deuteruro representado por la fórmula (1), en donde: I) R1 está seleccionado de entre a) hidrógeno, b) -P(O)(OH)2, c) -P(O)(O(CH2)1-3OC(O)O(alquilo))2, d) -P(O)(O(CH2)1-3OC(O)(alquilo))2, e) -P(O)(O(CH2)1-3SC(O)(alquilo))2, f) -P(O)(O(CH2)1-3OCH2(arilo))2, g) -P(O)(O(CH2)1-3SCH2(arilo))2, h) -P*(O)(OR1a)(NHCHR1bC(O)OR1c), donde R1a es i) hidrógeno, ii) alquilo, iii) cicloalquilo o iv) arilo, R1b es i) hidrógeno, ii) alquilo C1-6, iii) cicloalquilo, iv) alcarilo o v) alk(heteroarilo) y R1c es i) hidrógeno, ii) alquilo, iii) cicloalquilo o iv) alcarilo, i) -P*(O)(NH(alcaril)(O(CH2)1-3SC(O)(alquilo)), j) un 1,3,2-dioxafosfinan-2-óxido, k) un 4H-benzo[d][1,3,2]dioxafosfinin-2-óxido, l) -P*(O)(OR1c) ~, cuando Y es -O~, donde R1c se define con anterioridad, m) -P(O)(OH)-O-P(O)(OH)2, n) -P(O)(OH)-O-P(O)(OH)-O-P(O)(OH)2, o) un acilo, p) un alquilen C1-6-oxi-acilo, y q) un -C(O)-O-alquilo; II) R2 está seleccionado de entre a) hidrógeno, b) fluoro, c) azido, d) ciano, e) un alquilo C1-6, f) un vinilo y g) un etinilo; III) R3 está seleccionado de entre a) hidrógeno, b) metilo, y c) ciano; IV) Y está seleccionado de entre a) hidrógeno, b) fluoro, c) -OH, d) -O~, cuando R1 es -P(O)(OR1c) ~, donde R1c se define con anterioridad, e) -O(acilo), f) -O(alquilen C1-6-oxi-acilo), g) -O-C(O)-O-alquilo, h) -NH2, i) -NH(acilo), j) -NH-C(O)-O-alquilo, y k) azido; V) X está seleccionado de entre a) -O-, b) -S-, c) -NH-, d) -CH2-, e) >C=CH2, y f) -NH-C(O)-O-alquilo; VI) el anillo Z es un anillo de cuatro o cinco miembros seleccionado de entre radicales representado por las estructuras de fórmulas (a) - (o), donde * representa el punto de unión con el carbono 2’ y donde a) A está seleccionado de entre i) -O-, ii) -S-, iii) -S(O)-, iv) -S(O)2-, y v) -NH-, b) D está seleccionado de entre i) -O-, ii) -S- excepto por los anillos de fórmula (i) y (j), iii) -S(O)- excepto por los anillos de fórmula (i) y (j), iv) -S(O)2- excepto por los anillos de fórmula (i) y (j), y v) -NH- excepto por los anillos de fórmula (i) y (j), vi) -N-, vii) un metileno excepto por los anillos de fórmula (i) y (j), viii) un metino, y ix) un vinilideno excepto por los anillos de fórmula (i) y (j), c) R4, R4’, R5, R5’, R6, R7, R8, R8’, R9 y R9’ están seleccionados, de modo independiente, de entre i) hidrógeno, ii) halo, iii) alquilo C1-6, iv) hidroxi, v) alcoxi, vi) cicloalcoxi, vii) -O(acilo), viii) -O(alquilen C1-6-oxiacilo), ix) -O-C(O)-O-alquilo, x) alquilen C1-6-oxi(alquilo), xi) alquenilo, xii) etinilo, xiii) -NH2, xiv) -NH(alquilo), xv) -NH(cicloalquilo), xvi) heterociclilo, xvii) arilo, y xviii) heteroarilo; y VII) B está seleccionado de entre las estructuras de fórmula (B1), (B2) y (B3), donde para la estructura de fórmula (B1), n es 0 ó 1, a) cuando n es 0, - - - - - es un enlace doble y R10 está seleccionado de entre i) -NH2, ii) -NH(alquilo), iii) -NH(acilo), iv) -NH-C(O)-O-alquilo, v) -cicloheteroalquilo, vi) -heteroarilo, vii) -O(alquilo), viii) -O(acilo), ix) -O(alquilen C1-6-oxiacilo) y x) -O-C(O)-O-alquilo, o b) cuando n es 1, - - - - - es un enlace simple y R10 está seleccionado de entre i) =O, ii) =NH, y iii) =N(alquilo), y c) independientemente del valor de n, R11 y R12 están seleccionados, de modo independiente, de entre i) hidrógeno, ii) halo, iii) ciano, iv) alquilo C1-6, v) alquenilo C2-5 y vi) alquinilo C2-5; donde para la estructura de fórmula (B2), a) R13 está seleccionado de entre i) hidrógeno, ii) halo, iii) ciano, iv) -C(O)NH2, v) alquilo C1-6, vi) vinilo, y vii) etinilo; donde para la estructura de fórmula (B3), m es 0 ó 1 y - - - - - es un enlace simple o doble a) cuando m es 0, - - - - - es un enlace doble y R16 y R17 están seleccionados, de modo independiente, de entre i) hidrógeno, ii) -NH2, iii) -NH(alquilo), iv) -NH(acilo), iv) -NH-C(O)-O-alquilo, v) -cicloheteroalquilo, vi) -O(alquilo), vii) -O(acilo), viii) -O(alquilen C1-6-oxiacilo), ix) -O-C(O)-O-alquilo, y x) -S(alquilo), o b) cuando m es 1, - - - - - es un enlace simple, b1) R16 está seleccionado de entre i) =O, ii) =NH y iii) =N(alquilo) y b2) R17 está seleccionado de entre i) -NH2, ii) -NH(alquilo), iii) -NH(acilo), iv) -NH-C(O)-O-alquilo, y v) -cicloheteroalquilo, c) independientemente del valor de m, cada par de enlace, W1- - - - -W2, W2- - - - -C, C- - - - -W4, W4- - - - -W3 y W3- - - - -W1, contenido en el anillo de cinco miembros comprende un enlace simple o doble y i) W1 es O, S, N o CR14, ii) W2 es N o CR15, iii) W3 es C o N, y iv) W4 es C o N y donde R14 y R15, de estar presentes, están seleccionados, de modo independiente, de entre i) hidrógeno, ii) halo, iii) ciano, iv) -C(O)NH2, iv) alquilo C1-6, vii) vinilo, y viii) etinilo.
ARP110104450A 2010-11-30 2011-11-30 Compuestos 2’-espiro-nucleosidos AR084044A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US41794610P 2010-11-30 2010-11-30

Publications (1)

Publication Number Publication Date
AR084044A1 true AR084044A1 (es) 2013-04-17

Family

ID=45316116

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104450A AR084044A1 (es) 2010-11-30 2011-11-30 Compuestos 2’-espiro-nucleosidos

Country Status (10)

Country Link
US (2) US8841275B2 (es)
EP (2) EP2646453A1 (es)
JP (2) JP6069215B2 (es)
AR (1) AR084044A1 (es)
AU (1) AU2011336632B2 (es)
CA (1) CA2818853A1 (es)
ES (1) ES2716158T3 (es)
PT (1) PT3042910T (es)
TW (1) TW201242974A (es)
WO (1) WO2012075140A1 (es)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
DK1576138T3 (en) 2002-11-15 2017-05-01 Idenix Pharmaceuticals Llc 2'-METHYL NUCLEOSIDES IN COMBINATION WITH INTERFERON AND FLAVIVIRIDAE MUTATION
PT1633766T (pt) 2003-05-30 2019-06-04 Gilead Pharmasset Llc Análogos de nucleósido fluorado modificado
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
AU2009329872B2 (en) 2008-12-23 2016-07-07 Gilead Pharmasset Llc Synthesis of purine nucleosides
US9676797B2 (en) 2015-09-02 2017-06-13 Abbvie Inc. Anti-viral compounds
US8563530B2 (en) 2010-03-31 2013-10-22 Gilead Pharmassel LLC Purine nucleoside phosphoramidate
EP2646453A1 (en) 2010-11-30 2013-10-09 Gilead Pharmasset LLC Compounds
CN102863428B (zh) * 2011-07-09 2014-12-24 广东东阳光药业有限公司 作为丙型肝炎病毒抑制剂的螺环化合物
US9403863B2 (en) 2011-09-12 2016-08-02 Idenix Pharmaceuticals Llc Substituted carbonyloxymethylphosphoramidate compounds and pharmaceutical compositions for the treatment of viral infections
KR20190075142A (ko) 2011-09-16 2019-06-28 길리애드 파마셋 엘엘씨 Hcv 치료 방법
WO2013056046A1 (en) 2011-10-14 2013-04-18 Idenix Pharmaceuticals, Inc. Substituted 3',5'-cyclic phosphates of purine nucleotide compounds and pharmaceutical compositions for the treatment of viral infections
KR20140129019A (ko) 2012-02-14 2014-11-06 유니버시티 오브 조지아 리서치 파운데이션, 인코포레이티드 플라비비리다에 감염의 치료를 위한 스피로[2.4]헵탄
WO2013177188A1 (en) 2012-05-22 2013-11-28 Idenix Pharmaceuticals, Inc. 3',5'-cyclic phosphoramidate prodrugs for hcv infection
MX355708B (es) 2012-05-22 2018-04-27 Idenix Pharmaceuticals Llc Compuestos de d-aminoacidos para enfermedades del higado.
WO2013177195A1 (en) 2012-05-22 2013-11-28 Idenix Pharmaceuticals, Inc. 3',5'-cyclic phosphate prodrugs for hcv infection
TW201408688A (zh) 2012-05-25 2014-03-01 Janssen R & D Ireland 尿嘧啶基螺氧環丁烷（ｓｐｉｒｏｏｘｅｔａｎｅ）核苷類
EP2900682A1 (en) 2012-09-27 2015-08-05 IDENIX Pharmaceuticals, Inc. Esters and malonates of sate prodrugs
AP2015008384A0 (en) 2012-10-08 2015-04-30 Univ Montpellier Ct Nat De La Rech Scient 2'-Chloro nucleoside analogs for hcv infection
CN103804417B (zh) * 2012-11-13 2017-09-19 北京美倍他药物研究有限公司 抗乙肝病毒药物
US9211300B2 (en) 2012-12-19 2015-12-15 Idenix Pharmaceuticals Llc 4′-fluoro nucleosides for the treatment of HCV
HUE047777T2 (hu) 2013-01-31 2020-05-28 Gilead Pharmasset Llc Két vírusellenes vegyület kombinációs készítménye
WO2014137926A1 (en) 2013-03-04 2014-09-12 Idenix Pharmaceuticals, Inc. 3'-deoxy nucleosides for the treatment of hcv
US9339541B2 (en) 2013-03-04 2016-05-17 Merck Sharp & Dohme Corp. Thiophosphate nucleosides for the treatment of HCV
US20140271547A1 (en) 2013-03-13 2014-09-18 Idenix Pharmaceuticals, Inc. Amino acid phosphoramidate pronucleotides of 2'-cyano, azido and amino nucleosides for the treatment of hcv
WO2014165542A1 (en) 2013-04-01 2014-10-09 Idenix Pharmaceuticals, Inc. 2',4'-fluoro nucleosides for the treatment of hcv
AU2014250764A1 (en) 2013-04-12 2015-10-29 Achillion Pharmaceuticals, Inc. Deuterated nucleoside prodrugs useful for treating HCV
WO2014197578A1 (en) 2013-06-05 2014-12-11 Idenix Pharmaceuticals, Inc. 1',4'-thio nucleosides for the treatment of hcv
US20150037282A1 (en) 2013-08-01 2015-02-05 Idenix Pharmaceuticals, Inc. D-amino acid phosphoramidate pronucleotides of halogeno pyrimidine compounds for liver disease
EP3074412A4 (en) * 2013-11-28 2017-05-31 Janssen Sciences Ireland UC Crystal form of nucleoside inhibitor of hcv
WO2015095305A1 (en) 2013-12-17 2015-06-25 Idenix Pharmaceuticals, Inc. Production of cyclic phosphate, phosphoramidate, thiophosphate, and phosphonate nucleoside compounds
WO2015161137A1 (en) 2014-04-16 2015-10-22 Idenix Pharmaceuticals, Inc. 3'-substituted methyl or alkynyl nucleosides for the treatment of hcv
TWI713455B (zh) 2014-06-25 2020-12-21 美商伊凡克特治療公司 ＭｎＫ抑制劑及其相關方法
CN104151384B (zh) * 2014-08-20 2016-09-28 济南尚博生物科技有限公司 一种制备n6-苯甲酰基-d-腺苷的改进方法
WO2016044243A1 (en) * 2014-09-16 2016-03-24 Achillion Pharmaceuticals, Inc. Pyrimidine nucleoside phosphoramidate
TWI767201B (zh) 2014-10-29 2022-06-11 美商基利科學股份有限公司 絲狀病毒科病毒感染之治療
WO2016134053A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Anti-viral compounds
WO2016134057A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Anti-viral compounds
WO2016134056A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Anti-viral compounds
WO2016134051A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Anti-viral compounds
WO2016134054A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Anti-viral compounds
WO2016134050A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Anti-viral compounds
RU2764767C2 (ru) 2015-03-06 2022-01-21 Атеа Фармасьютикалс, Инк. β-D-2'-ДЕЗОКСИ-2'-α-ФТОР-2'-β-С-ЗАМЕЩЕННЫЕ-2-МОДИФИЦИРОВАННЫЕ-N6-ЗАМЕЩЕННЫЕ ПУРИНОВЫЕ НУКЛЕОТИДЫ ДЛЯ ЛЕЧЕНИЯ ВЫЗВАННЫХ HCV ЗАБОЛЕВАНИЙ
WO2016182938A1 (en) * 2015-05-08 2016-11-17 Abbvie Inc. Anti-viral compounds
WO2016182937A1 (en) * 2015-05-08 2016-11-17 Abbvie Inc. Anti-viral compounds
EP4088718A1 (en) 2015-09-16 2022-11-16 Gilead Sciences, Inc. Methods for treating coronaviridae virus infections
CN106543220A (zh) * 2015-09-16 2017-03-29 博瑞生物医药（苏州）股份有限公司 氨基磷酸酯化合物及其制备方法和晶体
CN106543252A (zh) * 2015-09-16 2017-03-29 博瑞生物医药（苏州）股份有限公司 核苷氨基磷酸酯类前药的制备方法及其中间体
CN106478753A (zh) * 2015-09-16 2017-03-08 博瑞生物医药（苏州）股份有限公司 一种nuc‑1031单一异构体的制备方法和用途
AU2016343980A1 (en) 2015-10-29 2018-06-07 Effector Therapeutics, Inc. Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit Mnk1 and Mnk2
AU2016343687A1 (en) 2015-10-29 2018-06-07 Effector Therapeutics, Inc. Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of Mnk1 and Mnk2
WO2017087808A1 (en) 2015-11-20 2017-05-26 Effector Therapeutics, Inc. Heterocyclic compounds that inhibit the kinase activity of mnk useful for treating various cancers
MY196772A (en) * 2015-12-11 2023-05-03 NuCana plc Diastereoselective synthesis of phosphate derivatives and of the gemcitabine prodrug nuc-1031
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
ES2990061T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros espirocíclicos para la degradación de proteínas diana
ES2989988T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros heterorocíclicos para la degradación de proteínas diana
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
KR102202984B1 (ko) 2016-05-27 2021-01-13 길리애드 사이언시즈, 인코포레이티드 Ns5a, ns5b 또는 ns3 억제제를 사용하여 b형 간염 바이러스 감염을 치료하는 방법
LU100724B1 (en) 2016-07-14 2018-07-31 Atea Pharmaceuticals Inc Beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-c-substituted-4'-fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection
CN116036114A (zh) 2016-09-07 2023-05-02 阿堤亚制药公司 用于rna病毒治疗的2’-取代的-n6-取代的嘌呤核苷酸
CA3048033C (en) 2017-02-01 2023-06-20 Atea Pharmaceuticals, Inc. Nucleotide hemi-sulfate salt for the treatment of hepatitis c virus
ES2969988T3 (es) 2017-02-14 2024-05-23 Effector Therapeutics Inc Inhibidores de Mnk sustituidos con piperidina y métodos relacionados con los mismos
GB201709471D0 (en) 2017-06-14 2017-07-26 Nucana Biomed Ltd Diastereoselective synthesis of hosphate derivatives
WO2018237026A1 (en) 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
MA50025A (fr) * 2017-09-01 2021-04-14 Janssen Pharmaceutica Nv Nucléosides de spirothiétane
EP3773753A4 (en) 2018-04-10 2021-12-22 ATEA Pharmaceuticals, Inc. TREATMENT OF PATIENTS INFECTED WITH THE HEPATITIS C VIRUS WITH CIRRHOSIS
JP2022505846A (ja) 2018-10-24 2022-01-14 イーフェクター セラピューティクス， インコーポレイテッド Ｍｎｋ阻害剤の結晶形態
SI4106876T1 (sl) 2020-02-18 2025-11-28 Gilead Sciences, Inc. Protivirusne spojine
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
CN112274516B (zh) * 2020-10-26 2022-08-05 中山大学附属第三医院 一种新型含碘抗病毒药物
US12274700B1 (en) 2020-10-30 2025-04-15 Accencio LLC Methods of treating symptoms of coronavirus infection with RNA polymerase inhibitors
IL308921A (en) 2021-06-17 2024-01-01 Atea Pharmaceuticals Inc Combination anti-HCV therapy is beneficial

Family Cites Families (371)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3798209A (en) 1971-06-01 1974-03-19 Icn Pharmaceuticals 1,2,4-triazole nucleosides
USRE29835E (en) 1971-06-01 1978-11-14 Icn Pharmaceuticals 1,2,4-Triazole nucleosides
US3994974A (en) 1972-02-05 1976-11-30 Yamanouchi Pharmaceutical Co., Ltd. α-Aminomethylbenzyl alcohol derivatives
US3852267A (en) 1972-08-04 1974-12-03 Icn Pharmaceuticals Phosphoramidates of 3{40 ,5{40 -cyclic purine nucleotides
US4138547A (en) 1977-12-22 1979-02-06 Icn Pharmaceuticals, Inc. Process for preparing 1,2,4-triazole nucleosides
JPS57146593A (en) 1981-03-09 1982-09-10 Ajinomoto Co Inc Preparation of ribofuranosyltriazole derivative
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
US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
US5736155A (en) 1984-08-08 1998-04-07 The Liposome Company, Inc. Encapsulation of antineoplastic agents in liposomes
US5077056A (en) 1984-08-08 1991-12-31 The Liposome Company, Inc. Encapsulation of antineoplastic agents in liposomes
NL8403224A (nl) 1984-10-24 1986-05-16 Oce Andeno Bv Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen.
US5223263A (en) 1988-07-07 1993-06-29 Vical, Inc. Liponucleotide-containing liposomes
US5246937A (en) 1985-09-18 1993-09-21 Beecham Group P.L.C. Purine derivatives
US4797285A (en) 1985-12-06 1989-01-10 Yissum Research And Development Company Of The Hebrew University Of Jerusalem Lipsome/anthraquinone drug composition and method
US5154930A (en) 1987-03-05 1992-10-13 The Liposome Company, Inc. Pharmacological agent-lipid solution preparation
GB8719367D0 (en) 1987-08-15 1987-09-23 Wellcome Found Therapeutic compounds
WO1989002733A1 (en) 1987-09-22 1989-04-06 The Regents Of The University Of California Liposomal nucleoside analogues for treating aids
IL91664A (en) 1988-09-28 1993-05-13 Yissum Res Dev Co Ammonium transmembrane gradient system for efficient loading of liposomes with amphipathic drugs and their controlled release
US6132763A (en) 1988-10-20 2000-10-17 Polymasc Pharmaceuticals Plc Liposomes
US5705363A (en) 1989-03-02 1998-01-06 The Women's Research Institute Recombinant production of human interferon τ polypeptides and nucleic acids
US5077057A (en) 1989-04-05 1991-12-31 The Regents Of The University Of California Preparation of liposome and lipid complex compositions
US5549910A (en) 1989-03-31 1996-08-27 The Regents Of The University Of California Preparation of liposome and lipid complex compositions
US5277914A (en) 1989-03-31 1994-01-11 The Regents Of The University Of California Preparation of liposome and lipid complex compositions
US5411947A (en) 1989-06-28 1995-05-02 Vestar, Inc. Method of converting a drug to an orally available form by covalently bonding a lipid to the drug
US5194654A (en) 1989-11-22 1993-03-16 Vical, Inc. Lipid derivatives of phosphonoacids for liposomal incorporation and method of use
US5225212A (en) 1989-10-20 1993-07-06 Liposome Technology, Inc. Microreservoir liposome composition and method
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
US5463092A (en) 1989-11-22 1995-10-31 Vestar, Inc. Lipid derivatives of phosphonacids for liposomal incorporation and method of use
US5026687A (en) 1990-01-03 1991-06-25 The United States Of America As Represented By The Department Of Health And Human Services Treatment of human retroviral infections with 2',3'-dideoxyinosine alone and in combination with other antiviral compounds
US5443965A (en) 1990-04-06 1995-08-22 Genelabs Incorporated Hepatitis C virus epitopes
US5091188A (en) 1990-04-26 1992-02-25 Haynes Duncan H Phospholipid-coated microcrystals: injectable formulations of water-insoluble drugs
WO1991016920A1 (en) 1990-05-07 1991-11-14 Vical, Inc. Lipid prodrugs of salicylate and nonsteroidal anti-inflammatory drugs
JPH05507279A (ja) 1990-05-29 1993-10-21 ネクススター・ファーマシューティカルズ・インコーポレイテッド グリセロールジ―およびトリホスフェート誘導体の合成
DE69115694T2 (de) 1990-06-13 1996-10-17 Arnold Newton Mass. Glazier Phosphorylierte prodrugs
US6060080A (en) 1990-07-16 2000-05-09 Daiichi Pharmaceutical Co., Ltd. Liposomal products
JP2599492B2 (ja) 1990-08-21 1997-04-09 第一製薬株式会社 リポソーム製剤の製造法
ES2118069T3 (es) 1990-09-14 1998-09-16 Acad Of Science Czech Republic Profarmacos de fosfonatos.
US5372808A (en) 1990-10-17 1994-12-13 Amgen Inc. Methods and compositions for the treatment of diseases with consensus interferon while reducing side effect
US5543390A (en) 1990-11-01 1996-08-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University Covalent microparticle-drug conjugates for biological targeting
US5543389A (en) 1990-11-01 1996-08-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education On Behalf Of The Oregon Health Sciences University, A Non Profit Organization Covalent polar lipid-peptide conjugates for use in salves
US5149794A (en) 1990-11-01 1992-09-22 State Of Oregon Covalent lipid-drug conjugates for drug targeting
US5256641A (en) 1990-11-01 1993-10-26 State Of Oregon Covalent polar lipid-peptide conjugates for immunological targeting
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
US5595732A (en) 1991-03-25 1997-01-21 Hoffmann-La Roche Inc. Polyethylene-protein conjugates
US5157027A (en) 1991-05-13 1992-10-20 E. R. Squibb & Sons, Inc. Bisphosphonate squalene synthetase inhibitors and method
WO1993000910A1 (en) 1991-07-12 1993-01-21 Vical, Inc. Antiviral liponucleosides: treatment of hepatitis b
HU9202318D0 (en) 1991-07-22 1992-10-28 Bristol Myers Squibb Co Method for preparing medical preparatives containing didesoxi-purine nucleoside
US5554728A (en) 1991-07-23 1996-09-10 Nexstar Pharmaceuticals, Inc. Lipid conjugates of therapeutic peptides and protease inhibitors
TW224053B (es) 1991-09-13 1994-05-21 Paul B Chretien
DE4200821A1 (de) 1992-01-15 1993-07-22 Bayer Ag Geschmacksmaskierte pharmazeutische mittel
US5676942A (en) 1992-02-10 1997-10-14 Interferon Sciences, Inc. Composition containing human alpha interferon species proteins and method for use thereof
US5405598A (en) 1992-02-24 1995-04-11 Schinazi; Raymond F. Sensitizing agents for use in boron neutron capture therapy
US5610054A (en) 1992-05-14 1997-03-11 Ribozyme Pharmaceuticals, Inc. Enzymatic RNA molecule targeted against Hepatitis C virus
US5770725A (en) 1992-05-25 1998-06-23 Gosselin; Gilles Phosphotriester type biologically active compounds
US5849905A (en) 1994-11-23 1998-12-15 Centre National De La Recherche Scientifique Biologically active phosphotriester-type nucleosides and methods for preparing same
US6020482A (en) 1992-05-25 2000-02-01 Gosselin; Gilles Phosphotriester type biologically active compounds
IL106075A (en) 1992-06-22 2000-12-06 Lilly Co Eli Process for preparing alpha-anomer enriched 1-halo-2-deoxy-2,2-difluoro-alpha-D-erythropentofuranose derivatives
US5426183A (en) 1992-06-22 1995-06-20 Eli Lilly And Company Catalytic stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US5256798A (en) 1992-06-22 1993-10-26 Eli Lilly And Company Process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates
HU214980B (hu) 1992-09-01 1998-08-28 Eli Lilly And Co. Eljárás nukleozidok anomerizálására
GB9226729D0 (en) 1992-12-22 1993-02-17 Wellcome Found Therapeutic combination
US6749868B1 (en) 1993-02-22 2004-06-15 American Bioscience, Inc. Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof
US6537579B1 (en) 1993-02-22 2003-03-25 American Bioscience, Inc. Compositions and methods for administration of pharmacologically active compounds
US6753006B1 (en) 1993-02-22 2004-06-22 American Bioscience, Inc. Paclitaxel-containing formulations
US5439686A (en) 1993-02-22 1995-08-08 Vivorx Pharmaceuticals, Inc. Methods for in vivo delivery of substantially water insoluble pharmacologically active agents and compositions useful therefor
DK0693924T4 (da) 1993-02-22 2008-08-04 Abraxis Bioscience Inc Fremgangsmåde til (in vivo) levering af biologiske materialer og sammensætninger, der er egnede dertil
US6096331A (en) 1993-02-22 2000-08-01 Vivorx Pharmaceuticals, Inc. Methods and compositions useful for administration of chemotherapeutic agents
AU6247594A (en) 1993-02-24 1994-09-14 Jui H. Wang Compositions and methods of application of reactive antiviral polymers
US6180134B1 (en) 1993-03-23 2001-01-30 Sequus Pharmaceuticals, Inc. Enhanced ciruclation effector composition and method
JPH08510236A (ja) 1993-05-12 1996-10-29 カール ワイ． ホステトラー 局所使用のためのアシクロビル誘導体
CA2167537A1 (en) 1993-07-19 1995-02-02 Tsuneo Ozeki Hepatitis c virus proliferation inhibitor
US6156501A (en) 1993-10-26 2000-12-05 Affymetrix, Inc. Arrays of modified nucleic acid probes and methods of use
US7375198B2 (en) 1993-10-26 2008-05-20 Affymetrix, Inc. Modified nucleic acid probes
AU691225B2 (en) 1993-11-10 1998-05-14 Schering Corporation Improved interferon polymer conjugates
US5951974A (en) 1993-11-10 1999-09-14 Enzon, Inc. Interferon polymer conjugates
WO1995024185A1 (en) 1994-03-11 1995-09-14 Isis Pharmaceuticals, Inc. Novel pyrimidine nucleosides
DE4447588C2 (de) 1994-05-03 1997-11-20 Omer Osama Dr Dr Med Pflanzliches Arzneimittel zur Behandlung von chronischen und allergischen Rhino-Sino-Bronchitiden
WO1995035102A1 (en) 1994-06-22 1995-12-28 Nexstar Pharmaceuticals, Inc. Novel method of preparation of known and novel 2'-modified nucleosides by intramolecular nucleophilic displacement
US5840891A (en) 1994-07-28 1998-11-24 Syntex (U.S.A.) Inc. 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol derivative
DE4432623A1 (de) 1994-09-14 1996-03-21 Huels Chemische Werke Ag Verfahren zur Bleichung von wäßrigen Tensidlösungen
US5738846A (en) 1994-11-10 1998-04-14 Enzon, Inc. Interferon polymer conjugates and process for preparing the same
US5696277A (en) 1994-11-15 1997-12-09 Karl Y. Hostetler Antiviral prodrugs
US5703058A (en) 1995-01-27 1997-12-30 Emory University Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent
US6391859B1 (en) 1995-01-27 2002-05-21 Emory University [5-Carboxamido or 5-fluoro]-[2′,3′-unsaturated or 3′-modified]-pyrimidine nucleosides
GB9505025D0 (en) 1995-03-13 1995-05-03 Medical Res Council Chemical compounds
DE19514523A1 (de) 1995-04-12 1996-10-17 Schering Ag Neue Cytosin- und Cytidinderivate
AU719122B2 (en) 1995-09-27 2000-05-04 Emory University Recombinant hepatitis C virus RNA replicase
US5908621A (en) 1995-11-02 1999-06-01 Schering Corporation Polyethylene glycol modified interferon therapy
US5767097A (en) 1996-01-23 1998-06-16 Icn Pharmaceuticals, Inc. Specific modulation of Th1/Th2 cytokine expression by ribavirin in activated T-lymphocytes
GB9602028D0 (en) 1996-02-01 1996-04-03 Amersham Int Plc Nucleoside analogues
US5980884A (en) 1996-02-05 1999-11-09 Amgen, Inc. Methods for retreatment of patients afflicted with Hepatitis C using consensus interferon
WO1997032018A2 (en) 1996-02-29 1997-09-04 Immusol, Inc. Hepatitis c virus ribozymes
US5830905A (en) 1996-03-29 1998-11-03 Viropharma Incorporated Compounds, compositions and methods for treatment of hepatitis C
US5633388A (en) 1996-03-29 1997-05-27 Viropharma Incorporated Compounds, compositions and methods for treatment of hepatitis C
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
GB9609932D0 (en) 1996-05-13 1996-07-17 Hoffmann La Roche Use of IL-12 and IFN alpha for the treatment of infectious diseases
US5891874A (en) 1996-06-05 1999-04-06 Eli Lilly And Company Anti-viral compound
US5837257A (en) 1996-07-09 1998-11-17 Sage R&D Use of plant extracts for treatment of HIV, HCV and HBV infections
US6214375B1 (en) 1996-07-16 2001-04-10 Generex Pharmaceuticals, Inc. Phospholipid formulations
US5922695A (en) 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
US5922757A (en) 1996-09-30 1999-07-13 The Regents Of The University Of California Treatment and prevention of hepatic disorders
US6224903B1 (en) 1996-10-11 2001-05-01 Sequus Pharmaceuticals, Inc. Polymer-lipid conjugate for fusion of target membranes
TW520297B (en) 1996-10-11 2003-02-11 Sequus Pharm Inc Fusogenic liposome composition and method
US6455690B1 (en) 1996-10-16 2002-09-24 Robert Tam L-8-oxo-7-propyl-7,8-dihydro-(9H)-guanosine
US6509320B1 (en) 1996-10-16 2003-01-21 Icn Pharmaceuticals, Inc. Purine L-nucleosides, analogs and uses thereof
HUP0001186A3 (en) 1996-10-16 2002-04-29 Icn Pharmaceuticals Inc Costa Purine l-nucleosides,analogs and pharmaceutical compositions thereof
KR100398923B1 (ko) 1996-10-16 2003-09-19 아이씨엔 파마슈티컬스, 인코포레이티드 모노시클릭 ｌ-누클레오시드, 이의 유사체 및 이들의 용도
EP0932617B1 (en) 1996-10-18 2002-01-16 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
IL119833A (en) 1996-12-15 2001-01-11 Lavie David Hypericum perforatum extracts for the preparation of pharmaceutical compositions for the treatment of hepatitis
US5827533A (en) 1997-02-06 1998-10-27 Duke University Liposomes containing active agents aggregated with lipid surfactants
US6004933A (en) 1997-04-25 1999-12-21 Cortech Inc. Cysteine protease inhibitors
KR100630506B1 (ko) 1997-06-30 2006-09-29 메르츠 파마 게엠베하 운트 코. 카가아 Ｎｍｄａ 수용체 길항물질로서의 1-아미노-알킬시클로헥산 화합물, 이를 함유하는 제약학적 조성물 및 이것으로 치료하는 방법
PT1012180E (pt) 1997-08-11 2005-04-29 Boehringer Ingelheim Ca Ltd Analogos de peptidos inibidores da hepatite c
EP1317929A3 (en) 1997-09-21 2003-07-02 Schering Corporation Combination therapy for eradicating detectable HCV-RNA in patients having chronic hepatitis c infection
US6703374B1 (en) 1997-10-30 2004-03-09 The United States Of America As Represented By The Department Of Health And Human Services Nucleosides for imaging and treatment applications
US5981709A (en) 1997-12-19 1999-11-09 Enzon, Inc. α-interferon-polymer-conjugates having enhanced biological activity and methods of preparing the same
US6339151B1 (en) 1998-01-23 2002-01-15 Newbiotics, Inc. Enzyme catalyzed therapeutic agents
AU2787199A (en) 1998-02-25 1999-09-15 Emory University 2'-fluoronucleosides
US6312662B1 (en) 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
US6787305B1 (en) 1998-03-13 2004-09-07 Invitrogen Corporation Compositions and methods for enhanced synthesis of nucleic acid molecules
WO1999049873A1 (en) 1998-03-27 1999-10-07 Regents Of The University Of Minnesota Nucleosides with antiviral and anticancer activity
GB9806815D0 (en) 1998-03-30 1998-05-27 Hoffmann La Roche Amino acid derivatives
ATE216591T1 (de) 1998-05-15 2002-05-15 Schering Corp Kombinationstherapie enthaltend ribavirin und interferon alpha bei patienten mit chronischer hepatitis c infektion, die nicht antiviral vorbehandelt sind
US20010014352A1 (en) 1998-05-27 2001-08-16 Udit Batra Compressed tablet formulation
IL139786A0 (en) 1998-06-08 2002-02-10 Hoffmann La Roche Use of peg-ifn-alpha and ribavirin for the treatment of chronic hepatitis c
US6726925B1 (en) 1998-06-18 2004-04-27 Duke University Temperature-sensitive liposomal formulation
US6200598B1 (en) 1998-06-18 2001-03-13 Duke University Temperature-sensitive liposomal formulation
GB9816358D0 (en) 1998-07-27 1998-09-23 Angeletti P Ist Richerche Bio Enzyme inhibitors
AU756627B2 (en) 1998-07-27 2003-01-16 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Diketoacid-derivatives as inhibitors of polymerases
CN1257912C (zh) 1998-08-10 2006-05-31 艾丹尼克斯(开曼)有限公司 用于治疗乙型肝炎的β－L－2′－脱氧－核苷
US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
NZ511093A (en) 1998-10-16 2003-04-29 Mercian Corp Crystallization of doxorubicin hydrochloride
US6635278B1 (en) 1998-12-15 2003-10-21 Gilead Sciences, Inc. Pharmaceutical formulations
CA2354536A1 (en) 1998-12-18 2000-06-29 Schering Corporation Ribavirin-pegylated interferon alfa induction hcv combination therapy
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6294192B1 (en) 1999-02-26 2001-09-25 Lipocine, Inc. Triglyceride-free compositions and methods for improved delivery of hydrophobic therapeutic agents
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
US6383471B1 (en) 1999-04-06 2002-05-07 Lipocine, Inc. Compositions and methods for improved delivery of ionizable hydrophobic therapeutic agents
US6395300B1 (en) 1999-05-27 2002-05-28 Acusphere, Inc. Porous drug matrices and methods of manufacture thereof
US7919119B2 (en) 1999-05-27 2011-04-05 Acusphere, Inc. Porous drug matrices and methods of manufacture thereof
CN1079473C (zh) 1999-05-31 2002-02-20 李岭群 预制梁连接筋
AU5905400A (en) 1999-07-14 2001-02-05 Board Of Regents, The University Of Texas System Methods and compositions for delivery and retention of active agents to lymph nodes
JP2003506368A (ja) 1999-07-30 2003-02-18 バスフ アクチエンゲゼルシヤフト ２−ピラゾリン−５−オン
WO2001018013A1 (en) 1999-09-08 2001-03-15 Metabasis Therapeutics, Inc. Prodrugs for liver specific drug delivery
AU1262001A (en) 1999-11-04 2001-05-14 Biochem Pharma Inc. Method for the treatment or prevention of flaviviridae viral infection using nucleoside analogues
TR200601784T2 (tr) 1999-11-12 2007-01-22 Pharmasset Ltd. 2'-deoksi-L-nükleositlerin sentezi
US20060034937A1 (en) 1999-11-23 2006-02-16 Mahesh Patel Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6495677B1 (en) 2000-02-15 2002-12-17 Kanda S. Ramasamy Nucleoside compounds
JP2003523978A (ja) 2000-02-18 2003-08-12 シャイアー・バイオケム・インコーポレイテッド ヌクレオシドアナログを用いるｆｌａｖｉｖｉｒｕｓ感染の処置もしくは予防するための方法
ATE414520T1 (de) 2000-04-13 2008-12-15 Pharmasset Inc 3 oder 2 hydroxymethyl substituierte nucleoside derivate und ihre verwendung zur behandlung von virusinfektionen
WO2001081359A1 (en) 2000-04-20 2001-11-01 Schering Corporation Ribavirin-interferon alfa combination therapy for eradicating detectable hcv-rna in patients having chronic hepatitis c infection
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
US6787526B1 (en) 2000-05-26 2004-09-07 Idenix Pharmaceuticals, Inc. Methods of treating hepatitis delta virus infection with β-L-2′-deoxy-nucleosides
EA007867B1 (ru) 2000-05-26 2007-02-27 Айденикс (Кайман) Лимитед Композиции для лечения флавивирусных и пестивирусных инфекций и способы их применения
ES2227203T3 (es) 2000-05-26 2005-04-01 Idenix (Cayman) Limited Metodos para tratar la infeccion por el virus de la hepatitis delta con beta-1-2'-desoxinucleosidos.
FR2810322B1 (fr) 2000-06-14 2006-11-10 Pasteur Institut PRODUCTION COMBINATOIRE D'ANALOGUES DE NUCLEOTIDES ET NUCLEOTIDES (XiTP)
MY141594A (en) 2000-06-15 2010-05-14 Novirio Pharmaceuticals Ltd 3'-PRODRUGS OF 2'-DEOXY-ß-L-NUCLEOSIDES
US6815542B2 (en) 2000-06-16 2004-11-09 Ribapharm, Inc. Nucleoside compounds and uses thereof
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
US6680068B2 (en) 2000-07-06 2004-01-20 The General Hospital Corporation Drug delivery formulations and targeting
AR034127A1 (es) 2000-07-21 2004-02-04 Schering Corp Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
EE05366B1 (et) 2000-07-21 2010-12-15 Gilead Sciences, Inc Fosfonaatnukleotiidanaloogide eelravimid ja skriinimise meetodid nende identifitseerimiseks
CZ2003195A3 (cs) 2000-07-21 2003-04-16 Schering Corporation Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostředek
WO2002008251A2 (en) 2000-07-21 2002-01-31 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
US7018985B1 (en) 2000-08-21 2006-03-28 Inspire Pharmaceuticals, Inc. Composition and method for inhibiting platelet aggregation
US6897201B2 (en) 2000-08-21 2005-05-24 Inspire Pharmaceuticals, Inc. Compositions and methods for the treatment of glaucoma or ocular hypertension
AR039558A1 (es) 2000-08-21 2005-02-23 Inspire Pharmaceuticals Inc Composiciones y metodo para el tratamiento de glaucoma o hipertension ocular
US20030008841A1 (en) 2000-08-30 2003-01-09 Rene Devos Anti-HCV nucleoside derivatives
CN1516599A (zh) 2000-10-18 2004-07-28 ���鹫˾ 病毒唑-聚乙二醇化干扰素α联合治疗慢性传染性丙型肝炎的方法
KR100905221B1 (ko) 2000-10-18 2009-07-01 파마셋 인코포레이티드 바이러스 감염 및 비정상적인 세포 증식의 치료를 위한변형된 뉴클레오시드
US6555677B2 (en) 2000-10-31 2003-04-29 Merck & Co., Inc. Phase transfer catalyzed glycosidation of an indolocarbazole
MXPA03004299A (es) 2000-11-20 2004-02-12 Bristol Myers Squibb Co Inhibidores de tripeptido de hepatitis c.
AU3659102A (en) 2000-12-12 2002-06-24 Schering Corp Diaryl peptides as ns3-serine protease inhibitors of hepatits c virus
WO2002048157A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
AU2002230763A1 (en) 2000-12-13 2008-01-03 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
BR0116221A (pt) 2000-12-15 2005-09-13 Pharmasset Ltd Agentes antivirais para tratamento de infecções por flaviviridae
SI1355916T1 (sl) 2001-01-22 2007-04-30 Merck & Co Inc Nukleozidni derivati kot inhibitorji RNA-odvisne RNA virusne polimeraze
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
MY129350A (en) 2001-04-25 2007-03-30 Bristol Myers Squibb Co Aripiprazole oral solution
GB0112617D0 (en) 2001-05-23 2001-07-18 Hoffmann La Roche Antiviral nucleoside derivatives
GB0114286D0 (en) 2001-06-12 2001-08-01 Hoffmann La Roche Nucleoside Derivatives
WO2003000713A1 (en) 2001-06-21 2003-01-03 Glaxo Group Limited Nucleoside compounds in hcv
WO2003006490A1 (en) 2001-07-11 2003-01-23 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
EP2335700A1 (en) 2001-07-25 2011-06-22 Boehringer Ingelheim (Canada) Ltd. Hepatitis C virus polymerase inhibitors with a heterobicylic structure
DE60101056T2 (de) 2001-07-30 2004-05-19 Clariant Life Science Molecules (Italia) S.P.A., Origgio Verfahren zur Herstellung von Ribavirin
EP1412369B1 (en) 2001-08-02 2008-05-07 Ilex Oncology, Inc. Process for preparing purine nucleosides
US6962991B2 (en) 2001-09-12 2005-11-08 Epoch Biosciences, Inc. Process for the synthesis of pyrazolopyrimidines
US7227019B2 (en) 2001-09-13 2007-06-05 Bristol-Myers Squibb Company Process for the preparation of rebeccamycin and analogs thereof
WO2003024461A1 (en) 2001-09-20 2003-03-27 Schering Corporation Hcv combination therapy
AU2002330154A1 (en) 2001-09-28 2003-04-07 Centre National De La Recherche Scientifique Methods and compositions for treating hepatitis c virus using 4'-modified nucleosides
JP2005515172A (ja) 2001-11-02 2005-05-26 グラクソ　グループ　リミテッド Ｈｃｖ阻害剤としての４−（６−員）−ヘテロアリールアシルピロリジン誘導体
AU2002359518A1 (en) 2001-11-27 2003-06-10 Bristol-Myers Squibb Company Efavirenz tablet formulation having unique biopharmaceutical characteristics
GB0129945D0 (en) 2001-12-13 2002-02-06 Mrc Technology Ltd Chemical compounds
EP1569652A4 (en) 2001-12-14 2008-07-02 Pharmasset Inc NUCLEOSIDES N SP 4 / SP-ACYLCYTOSINES FOR THE TREATMENT OF VIRAL INFECTIONS
AU2002353165A1 (en) 2001-12-17 2003-06-30 Ribapharm Inc. Deazapurine nucleoside libraries and compounds
WO2003055896A2 (en) 2001-12-21 2003-07-10 Micrologix Biotech Inc. Anti-viral 7-deaza l-nucleosides
WO2003062256A1 (en) 2002-01-17 2003-07-31 Ribapharm Inc. 2'-beta-modified-6-substituted adenosine analogs and their use as antiviral agents
US7070801B2 (en) 2002-01-30 2006-07-04 National Institute Of Advanced Industrial Science And Technology Sugar-modified liposome and products comprising the liposome
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
CA2370396A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
JP2005527499A (ja) 2002-02-13 2005-09-15 メルク　エンド　カムパニー　インコーポレーテッド ヌクレオシド化合物を用いてオルトポックスウイルスの複製を阻害する方法
EP1485395A4 (en) 2002-02-28 2011-04-13 Biota Scient Management NUCLEOTIDE MIMETICS AND PRODRUGS THEREOF
JP2005524662A (ja) 2002-02-28 2005-08-18 ビオタ インコーポレーティッド ヌクレオシド５’−一リン酸模倣物およびこれらのプロドラッグ
CN101074242A (zh) 2002-04-26 2007-11-21 吉里德科学公司 Hiv蛋白酶抑制剂化合物的膦酸酯类似物的细胞蓄积及这类化合物
AU2003241621A1 (en) 2002-05-24 2003-12-12 Isis Pharmaceuticals, Inc. Oligonucleotides having modified nucleoside units
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
WO2003101993A1 (en) 2002-06-04 2003-12-11 Neogenesis Pharmaceuticals, Inc. Pyrazolo` 1,5a! pyrimidine compounds as antiviral agents
CA2488611C (en) 2002-06-07 2011-11-15 Kylix, B.V. Compounds for modulating the activity of exchange proteins directly activated by camp (epacs)
AU2003248708A1 (en) 2002-06-17 2003-12-31 Isis Pharmaceuticals, Inc. Oligomeric compounds that include carbocyclic nucleosides and their use in gene modulation
CA2488842A1 (en) 2002-06-17 2003-12-24 Merck & Co., Inc. Carbocyclic nucleoside analogs as rna-antivirals
CA2488534A1 (en) 2002-06-21 2003-12-31 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
WO2004003138A2 (en) 2002-06-27 2004-01-08 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
US7608600B2 (en) 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
CN1678326A (zh) 2002-06-28 2005-10-05 埃迪尼克斯(开曼)有限公司 用于治疗黄病毒感染的2'－c－甲基－3'－o－l－缬氨酸酯核糖呋喃基胞苷
AU2003263412A1 (en) 2002-06-28 2004-01-19 Centre National De La Recherche Scientifique (Cnrs) 1'-, 2'- and 3'- modified nucleoside derivatives for treating flaviviridae infections
CN104193791A (zh) 2002-06-28 2014-12-10 埃迪尼克斯医药公司 用于治疗黄病毒感染的修饰的2’和3’-核苷前药
US6973905B2 (en) 2002-07-01 2005-12-13 Cinetic Automation Corporation Valve lash adjustment apparatus and method
BR0305426A (pt) 2002-07-01 2004-08-24 Upjohn Co Compostos inibidores de ns5b polimerase de hcv, bem como composição farmacêutica compreendendo os mesmos
US20040142993A1 (en) 2002-07-01 2004-07-22 Carlo Battistini Inhibitors of HCV NS5B polymerase
JP2005533108A (ja) 2002-07-16 2005-11-04 メルク　エンド　カムパニー　インコーポレーテッド Ｒｎａ依存性ｒｎａウイルスポリメラーゼの阻害剤としてのヌクレオシド誘導体
US7323449B2 (en) 2002-07-24 2008-01-29 Merck & Co., Inc. Thionucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
AU2003261237A1 (en) 2002-07-24 2004-02-09 Ptc Therapeutics, Inc. Use of nucleoside compounds for nonsense suppression and the treatment of genetic diseases
EP1527082A2 (en) 2002-07-25 2005-05-04 Micrologix Biotech, Inc. Anti-viral 7-deaza d-nucleosides and uses thereof
AU2003261434A1 (en) 2002-08-12 2004-02-25 Bristol-Myers Squibb Company Iminothiazolidinones as inhibitors of hcv replication
KR20080053419A (ko) 2002-09-13 2008-06-12 이데닉스 (케이만) 리미티드 내성 ＨＢＶ 균주 치료용 β-Ｌ-2'-데옥시뉴클레오시드 및병용 요법
US20050215614A1 (en) 2002-10-15 2005-09-29 Rigel Pharmaceuticals, Inc. Substituted indoles and their use as hcv inhibitors
US20040229840A1 (en) 2002-10-29 2004-11-18 Balkrishen Bhat Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
AU2003290584B2 (en) 2002-11-01 2009-07-16 Viropharma Incorporated Benzofuran compounds, compositions and methods for treatment and prophylaxis of hepatitis C viral infections and associated diseases
WO2004044139A2 (en) 2002-11-05 2004-05-27 Isis Parmaceuticals, Inc. Modified oligonucleotides for use in rna interference
WO2004041889A2 (en) 2002-11-05 2004-05-21 Isis Pharmaceuticals, Inc. Polycyclic sugar surrogate-containing oligomeric compounds and compositions for use in gene modulation
DK1576138T3 (en) 2002-11-15 2017-05-01 Idenix Pharmaceuticals Llc 2'-METHYL NUCLEOSIDES IN COMBINATION WITH INTERFERON AND FLAVIVIRIDAE MUTATION
TWI332507B (en) 2002-11-19 2010-11-01 Hoffmann La Roche Antiviral nucleoside derivatives
KR20200083657A (ko) 2002-12-09 2020-07-08 아브락시스 바이오사이언스, 엘엘씨 약리학적 물질의 조성물 및 그 전달방법
PL377287A1 (pl) 2002-12-12 2006-01-23 Idenix (Cayman) Limited Sposób wytwarzania 2'-rozgałęzionych nukleozydów
KR20080032014A (ko) 2003-01-14 2008-04-11 길리애드 사이언시즈, 인코포레이티드 복합 항바이러스 치료를 위한 조성물 및 방법
US7223785B2 (en) 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
WO2004080466A1 (en) 2003-03-07 2004-09-23 Ribapharm Inc. Cytidine analogs and methods of use
BRPI0408561A (pt) 2003-03-20 2006-03-21 Microbiol Quimica Farmaceutica métodos para manufatura de 2'-desoxi-59-l-nucleosìeos
ATE422895T1 (de) 2003-04-16 2009-03-15 Bristol Myers Squibb Co Makrocyclische isochinolinpeptidinhibitoren des hepatitis-c-virus
EP1617848A2 (en) 2003-04-25 2006-01-25 Gilead Sciences, Inc. Anti-cancer phosphonate conjugates
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
US7470724B2 (en) 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US20050261237A1 (en) 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
CA2523083C (en) 2003-04-25 2014-07-08 Gilead Sciences, Inc. Antiviral phosphonate analogs
KR20060022647A (ko) 2003-04-25 2006-03-10 길리애드 사이언시즈, 인코포레이티드 키나아제 억제 포스포네이트 유사체
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
WO2004096210A1 (en) 2003-05-01 2004-11-11 Glaxo Group Limited Acylated indoline and tetrahydroquinoline derivatives as hcv inhibitors
US20040259934A1 (en) 2003-05-01 2004-12-23 Olsen David B. Inhibiting Coronaviridae viral replication and treating Coronaviridae viral infection with nucleoside compounds
EP1656093A2 (en) 2003-05-14 2006-05-17 Idenix (Cayman) Limited Nucleosides for treatment of infection by corona viruses, toga viruses and picorna viruses
US20040229839A1 (en) 2003-05-14 2004-11-18 Biocryst Pharmaceuticals, Inc. Substituted nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
WO2004106356A1 (en) 2003-05-27 2004-12-09 Syddansk Universitet Functionalized nucleotide derivatives
PT1633766T (pt) 2003-05-30 2019-06-04 Gilead Pharmasset Llc Análogos de nucleósido fluorado modificado
US7507859B2 (en) 2003-06-16 2009-03-24 Fifth Base Llc Functional synthetic molecules and macromolecules for gene delivery
GB0317009D0 (en) 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
US20050075309A1 (en) 2003-07-25 2005-04-07 Richard Storer Purine nucleoside analogues for treating Flaviviridae including hepatitis C
ES2355565T3 (es) 2003-08-27 2011-03-29 Biota Scientific Management Pty. Ltd. Nuevos nucleósidos o nucleótidos tricíclos como agentes terapéuticos.
CA2538252C (en) 2003-09-18 2014-02-25 Isis Pharmaceuticals, Inc. 4'-thionucleosides and oligomeric compounds
AU2004274468B2 (en) 2003-09-18 2009-07-23 Vertex Pharmaceuticals, Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US20050148534A1 (en) 2003-09-22 2005-07-07 Castellino Angelo J. Small molecule compositions and methods for increasing drug efficiency using compositions thereof
US7491794B2 (en) 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
ES2398912T3 (es) 2003-10-14 2013-03-22 F. Hoffmann-La Roche Ltd. Ácido carboxílico macrocíclico y compuesto de acilsulfonamida como inhibidor de la replicación del virus de la hepatitis C
US20060003942A1 (en) 2003-10-27 2006-01-05 Roger Tung Combinations for HCV treatment
US7026339B2 (en) 2003-11-07 2006-04-11 Fan Yang Inhibitors of HCV NS5B polymerase
TW200528459A (en) 2004-01-06 2005-09-01 Achillion Pharmaceuticals Inc Azabenzofuran substituted thioureas; inhibitors of viral replication
JP2007519734A (ja) 2004-01-28 2007-07-19 メルク　エンド　カムパニー　インコーポレーテッド アミノシクロペンチルピリドピラジノン系ケモカイン受容体活性調節剤
EP1718150A1 (en) 2004-02-25 2006-11-08 The Government of the United States of America, represented by the Secretary, Department of Health and Human Services Methylation inhibitor compounds
WO2005087788A2 (en) 2004-03-04 2005-09-22 The Regents Of The University Of California Methods for preparation of nucleoside phosphonate esters
CA2560897C (en) 2004-03-30 2012-06-12 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
GB0408995D0 (en) 2004-04-22 2004-05-26 Glaxo Group Ltd Compounds
CA2568735A1 (en) 2004-06-03 2005-12-22 Isis Pharmaceuticals, Inc. Double strand compositions comprising differentially modified strands for use in gene modulation
US8394947B2 (en) 2004-06-03 2013-03-12 Isis Pharmaceuticals, Inc. Positionally modified siRNA constructs
WO2005123087A2 (en) 2004-06-15 2005-12-29 Merck & Co., Inc. C-purine nucleoside analogs as inhibitors of rna-dependent rna viral polymerase
WO2006000922A2 (en) 2004-06-23 2006-01-05 Idenix (Cayman) Limited 5-aza-7-deazapurine derivatives for treating infections with flaviviridae
JP5080973B2 (ja) 2004-06-24 2012-11-21 メルク・シャープ・エンド・ドーム・コーポレイション Ｒｎａ依存性ｒｎａウイルスの感染を処置するためのヌクレオシドアリールホスホルアミダート
US7217523B2 (en) 2004-07-02 2007-05-15 Regents Of The University Of Minnesota Nucleoside phosphoramidates and nucleoside phosphoramidases
CN101023094B (zh) 2004-07-21 2011-05-18 法莫赛特股份有限公司 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备
CN102199181B (zh) 2004-07-21 2014-09-17 吉利德制药有限责任公司 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备
AP2412A (en) 2004-07-27 2012-06-01 Gilead Sciences Inc Phosphonate analogs of HIV inhibitor compounds.
US7153848B2 (en) 2004-08-09 2006-12-26 Bristol-Myers Squibb Company Inhibitors of HCV replication
US7348425B2 (en) 2004-08-09 2008-03-25 Bristol-Myers Squibb Company Inhibitors of HCV replication
JP2008510748A (ja) 2004-08-23 2008-04-10 エフ．ホフマン−ラ ロシュ アーゲー 抗ウイルス４’−アジド−ヌクレオシド
JP4624419B2 (ja) 2004-08-23 2011-02-02 エフ．ホフマン−ラ ロシュ アーゲー 抗ウイルス性へテロ環化合物
WO2006029081A2 (en) 2004-09-02 2006-03-16 Neopharm, Inc. Nucleoside-lipid conjugates, their method of preparation and uses thereof
AU2005285045B2 (en) 2004-09-14 2011-10-13 Gilead Sciences, Inc. Preparation of 2'fluoro-2'- alkyl- substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
CA2581523A1 (en) 2004-09-24 2006-04-06 Idenix (Cayman) Limited Methods and compositions for treating flaviviruses, pestiviruses and hepacivirus
AU2005288858B2 (en) 2004-09-30 2011-04-21 Janssen R&D Ireland HCV inhibiting bi-cyclic pyrimidines
WO2006065335A2 (en) 2004-10-21 2006-06-22 Merck & Co., Inc. Fluorinated pyrrolo[2,3-d]pyrimidine nucleosides for the treatment of rna-dependent rna viral infection
EP1827460A4 (en) 2004-12-09 2012-03-14 Univ Minnesota NUCLEOSIDE WITH ANTIVIRAL AND ANTI-CANCER EFFECT
WO2006065590A2 (en) 2004-12-16 2006-06-22 Xtl Biopharmaceuticals Inc. Pyridine and pyrimidine antiviral compositions
EP1828217A2 (en) 2004-12-16 2007-09-05 Febit Biotech GmbH Polymerase-independent analysis of the sequence of polynucleotides
WO2006093801A1 (en) 2005-02-25 2006-09-08 Abbott Laboratories Thiadiazine derivatives useful as anti-infective agents
EA200701849A1 (ru) 2005-02-28 2008-02-28 Дженелабс Текнолоджис, Инк. Пролекарственные соединения трициклических нуклеозидов, фармацевтическая композиция на их основе и способ лечения и/или ингибирования вирусной инфекции у млекопитающего
EP1858889A1 (en) 2005-03-08 2007-11-28 Biota Scientific Management Pty. Ltd. Bicyclic nucleosides and nucleotides as therapeutic agents
JP2008534479A (ja) 2005-03-25 2008-08-28 テイボテク・フアーマシユーチカルズ・リミテツド Ｈｃｖの複素二環式阻害剤
WO2006116557A1 (en) 2005-04-25 2006-11-02 Genelabs Technologies, Inc. Nucleoside compounds for treating viral infections
US7485716B2 (en) 2005-05-02 2009-02-03 Pharmaessentia Corp. Stereoselective synthesis of β-nucleosides
WO2006121820A1 (en) 2005-05-05 2006-11-16 Valeant Research & Development Phosphoramidate prodrugs for treatment of viral infection
AR054122A1 (es) 2005-05-12 2007-06-06 Tibotec Pharm Ltd Pirido[2,3-d]pirimidas utiles como inhibidores de hcv, y metodos para la preparacion de las mismas
AR056347A1 (es) 2005-05-12 2007-10-03 Tibotec Pharm Ltd Uso de compuestos de pteridina para fabricar medicamentos y composiciones farmaceuticas
WO2007027248A2 (en) 2005-05-16 2007-03-08 Valeant Research & Development 3', 5' - cyclic nucleoside analogues for treatment of hcv
US20060276405A1 (en) 2005-06-02 2006-12-07 Schering Corporation Methods for treating hepatitis C
US8143288B2 (en) 2005-06-06 2012-03-27 Bristol-Myers Squibb Company Inhibitors of HCV replication
TWI375560B (en) 2005-06-13 2012-11-01 Gilead Sciences Inc Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same
TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
US20060293752A1 (en) 2005-06-27 2006-12-28 Missoum Moumene Intervertebral disc prosthesis and associated methods
EP2305695A3 (en) 2005-07-25 2011-07-27 Intermune, Inc. Macrocyclic inhibitors of Hepatitis C virus replication
CN101277682B (zh) 2005-07-28 2015-07-29 Isp投资有限公司 无定形依发韦仑及其生产
JP5230417B2 (ja) 2005-07-29 2013-07-10 テイボテク・フアーマシユーチカルズ Ｃ型肝炎ウイルスの大員環インヒビター
BRPI0614242A2 (pt) 2005-07-29 2011-03-15 Medivir Ab inibidores macrocìclicos do vìrus da hepatite c, combinação e composição farmacêutica compreendendo os mesmos, bem como uso e processo para a preparação dos referidos inibidores
US20070059360A1 (en) 2005-07-29 2007-03-15 Ashish Jaiswal Water-dispersible anti-retroviral pharmaceutical compositions
DK1912996T3 (da) 2005-07-29 2012-09-17 Janssen R & D Ireland Makrocykliske inhibitorer af hepatitis C-virus
EP1915585A2 (en) 2005-07-29 2008-04-30 Automotive Systems Laboratory Inc. Magnetic crash sensor
ES2456617T3 (es) 2005-07-29 2014-04-23 Janssen R&D Ireland Inhibidores macrocíclicos del virus de la hepatitis C
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
JP2009504704A (ja) 2005-08-15 2009-02-05 エフ．ホフマン−ラ ロシュ アーゲー 抗ウイルス４′−置換プロヌクレオチドホスホルアミダート
GB0519478D0 (en) 2005-09-23 2005-11-02 Glaxo Group Ltd Compounds
GB0519488D0 (en) 2005-09-23 2005-11-02 Glaxo Group Ltd Compounds
EP1957510A1 (en) 2005-12-09 2008-08-20 F.Hoffmann-La Roche Ag Antiviral nucleosides
CA2633541A1 (en) 2005-12-12 2007-06-21 Genelabs Technologies, Inc. N-(6-membered aromatic ring)-amido anti-viral compounds
US7910595B2 (en) 2005-12-21 2011-03-22 Abbott Laboratories Anti-viral compounds
DE602006015861D1 (de) 2005-12-21 2010-09-09 Abbott Lab Antivirale verbindungen
GB0602046D0 (en) 2006-02-01 2006-03-15 Smithkline Beecham Corp Compounds
WO2007092000A1 (en) 2006-02-06 2007-08-16 Bristol-Myers Squibb Company Inhibitors of hcv replication
EP1987050A2 (en) 2006-02-14 2008-11-05 Merck & Co., Inc. Nucleoside aryl phosphoramidates for the treatment of rna-dependent rna viral infection
ES2374455T3 (es) 2006-02-17 2012-02-16 Pfizer Limited Derivados de 3-deazapurinza como moduladores de tlr7.
US8895531B2 (en) 2006-03-23 2014-11-25 Rfs Pharma Llc 2′-fluoronucleoside phosphonates as antiviral agents
WO2007140200A2 (en) 2006-05-25 2007-12-06 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine hcv ns5b inhibitors
WO2007140254A2 (en) 2006-05-25 2007-12-06 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine hcv ns5b inhibitors
AP2985A (en) 2006-07-07 2014-09-30 Gilead Sciences Inc Modulators of pharmacokinetic properties of therapeutics
EP2043613A1 (en) 2006-07-14 2009-04-08 Fmc Corporation Solid form
EP1881001A1 (en) 2006-07-20 2008-01-23 Tibotec Pharmaceuticals Ltd. HCV NS-3 serine protease inhibitors
US8329159B2 (en) 2006-08-11 2012-12-11 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2008045419A1 (en) 2006-10-10 2008-04-17 Pharmasset, Inc. Preparation of nucleosides ribofuranosyl pyrimidines
PL216525B1 (pl) 2006-10-17 2014-04-30 Ct Badań Molekularnych I Makromolekularnych Polskiej Akademii Nauk 5'-O-[(N-acylo)amidoditiofosforano] nukleozydy oraz sposób wytwarzania 5'-O-[(N-acylo)amidofosforano]-,5'-O-[(N-acylo)amidotiofosforano]-, 5'-O-[(N-acylo)amidoditiofosforano]nukleozydów
GB0623493D0 (en) 2006-11-24 2007-01-03 Univ Cardiff Chemical compounds
US8148349B2 (en) 2006-12-20 2012-04-03 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Nucleoside cyclic phosphoramidates for the treatment of RNA-dependent RNA viral infection
US20080261913A1 (en) 2006-12-28 2008-10-23 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of liver disorders
US8071568B2 (en) 2007-01-05 2011-12-06 Merck Sharp & Dohme Corp. Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
GB0709791D0 (en) 2007-05-22 2007-06-27 Angeletti P Ist Richerche Bio Antiviral agents
CN101108870A (zh) 2007-08-03 2008-01-23 冷一欣 核苷磷酸酯类化合物及制备方法和应用
US8629171B2 (en) 2007-08-08 2014-01-14 Bristol-Myers Squibb Company Crystalline form of methyl ((1S)-1-((25)-2-(5-(4'-(2-((25)-1((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt
ES2369321T3 (es) 2007-09-14 2011-11-29 Schering Corporation Procedimiento para el tratamiento de pacientes con hepatitis c.
JO2778B1 (en) 2007-10-16 2014-03-15 ايساي انك Certain Compounds, Compositions and Methods
JP5238939B2 (ja) 2007-11-07 2013-07-17 三菱化学株式会社 長繊維強化複合樹脂組成物および成形品
US20090318380A1 (en) 2007-11-20 2009-12-24 Pharmasset, Inc. 2',4'-substituted nucleosides as antiviral agents
CL2008003511A1 (es) 2007-11-29 2010-02-19 Metabasis Therapeutics Inc Compuestos derivados nucleotidicos, inhibidores de polimerasa ns5b del virus de la hepatitis c; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la hepatitis c.
WO2009086192A1 (en) 2007-12-21 2009-07-09 Alios Biopharma, Inc. Biodegradable phosphate protected nucleotide derivatives and their use as cancer, anti viral and anti parasitic agents
US8227431B2 (en) 2008-03-17 2012-07-24 Hetero Drugs Limited Nucleoside derivatives
US20110130440A1 (en) 2008-03-26 2011-06-02 Alnylam Pharmaceuticals, Inc. Non-natural ribonucleotides, and methods of use thereof
CA2720729A1 (en) 2008-04-15 2009-11-26 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
EP3042660A3 (en) 2008-04-15 2016-10-26 RFS Pharma, LLC. Nucleoside derivatives for treatment of caliciviridae infections, including norovirus infections
US8012941B2 (en) 2008-04-23 2011-09-06 Gilead Sciences, Inc. Carba-nucleoside analogs for antiviral treatment
WO2010036407A2 (en) 2008-05-15 2010-04-01 Biocryst Pharmaceuticals, Inc. Antiviral nucleoside analogs
US8173621B2 (en) * 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
EP2313102A2 (en) 2008-07-03 2011-04-27 Biota Scientific Management Bycyclic nucleosides and nucleotides as therapeutic agents
EP2346329B1 (en) 2008-10-09 2013-08-21 Anadys Pharmaceuticals, Inc. A method of inhibiting hepatitis c virus by combination of a 5,6-dihydro-1h-pyridin-2-one and one or more additional antiviral compounds
AU2009329872B2 (en) 2008-12-23 2016-07-07 Gilead Pharmasset Llc Synthesis of purine nucleosides
BRPI0922508A8 (pt) 2008-12-23 2016-01-19 Pharmasset Inc Análogos de nucleosídeo
PA8855601A1 (es) 2008-12-23 2010-07-27 Forformidatos de nucleósidos
MX2011007194A (es) 2009-01-07 2013-07-12 Scynexis Inc Combinacion de un derivado ciclosporina y nucleosidos para tratar virus de hepatitis c (vhc).
SG173186A1 (en) 2009-02-10 2011-09-29 Gilead Sciences Inc Carba-nucleoside analogs for antiviral treatment
JO3027B1 (ar) * 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان
TWI598358B (zh) * 2009-05-20 2017-09-11 基利法瑪席特有限責任公司 核苷磷醯胺
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
CA2794671C (en) 2010-03-31 2018-05-01 Gilead Pharmasset Llc Stereoselective synthesis of phosphorus containing actives
US8563530B2 (en) 2010-03-31 2013-10-22 Gilead Pharmassel LLC Purine nucleoside phosphoramidate
EP2646453A1 (en) 2010-11-30 2013-10-09 Gilead Pharmasset LLC Compounds

Also Published As

Publication number Publication date
US20120142626A1 (en) 2012-06-07
US8841275B2 (en) 2014-09-23
US20150018300A1 (en) 2015-01-15
EP3042910A2 (en) 2016-07-13
EP2646453A1 (en) 2013-10-09
EP3042910B1 (en) 2019-01-09
CA2818853A1 (en) 2012-06-07
JP2013544286A (ja) 2013-12-12
AU2011336632A1 (en) 2013-05-02
US9394331B2 (en) 2016-07-19
AU2011336632B2 (en) 2015-09-03
JP6286462B2 (ja) 2018-02-28
PT3042910T (pt) 2019-04-16
TW201242974A (en) 2012-11-01
EP3042910A3 (en) 2016-09-07
JP6069215B2 (ja) 2017-02-01
JP2016138120A (ja) 2016-08-04
WO2012075140A1 (en) 2012-06-07
ES2716158T3 (es) 2019-06-10

Similar Documents

Publication Publication Date Title
AR084044A1 (es) Compuestos 2’-espiro-nucleosidos
ES2523565T3 (es) Derivados de hidroxibenzamida y sus usos como inhibidores de la hsp90
AR077505A1 (es) Compuestos de piridina y sus usos
CO6160232A2 (es) Derivados de bencimidazol
ES2637167T3 (es) Compuestos de tetrahidro-pirido-piridina y tetrahidro-pirido-pirimidina y su uso como moduladores de los receptores de C5a
ECSP034475A (es) Derivados de 4-fenil-piridin como antagonistas del receptor de neuroquinina-1
ES2322602T3 (es) Compuestos heterotetraciclicos condensados y su uso como inhibidor de polimerasa del vhc.
NO953447L (no) Nye 4-aminopyridiner, fremgangsmåte for deres fremstilling samt legemidler inneholdende disse
CO6190521A2 (es) Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta -9 desaturasa
ATE293101T1 (de) Piperidine zur verwendung als orexin rezeptor antagonisten
AR063331A1 (es) Derivados de biaril eter urea y composiciones farmaceuticas
AR054809A1 (es) Compuestos de amino -5-heteroarilo (5 miembros) imidazolona y su uso para la modulacion de la b- secretasa
AR076900A1 (es) Derivados heterociclicos nitrogenados utiles como agentes antivirales, composiciones farmaceuticas que los contienen y uso de los mismos como inhibidores del vhc
AR061374A1 (es) Derivados de diamidas de acido antranilico con sus sustituyentes heteroaromaticos y heterociclicos
PE20091376A1 (es) Derivados de fenilamino como moduladores de beta-amiloide
MX2009012885A (es) Nuevo derivado de 1,2,3,4-tetrahidroquinoxalina que tiene, como sustituyente, grupo fenilo que tiene estructura de ester de acido sulfonico o estructura de amida de acido sulfonico introducida en este, y tiene actividad de enlace al receptor de gluco
CO6400139A2 (es) Derivados de ciclopenta[c]pirool-2-carboxilatos, su preparación y su aplicación en terapéutica
AR076579A1 (es) Espironucleosidos uracilicos oxetanicos, composiciones farmaceuticas que los contienen y uso de los mismos como inhibidores del virus de la hepatitis c (vhc).
AR065927A1 (es) Derivados de 5,6-dihidro-1h-piridin-2-ona
AR065863A1 (es) Derivados de imidazolidinona
AR062798A1 (es) Derivados de hexahidropirrolo[3,4-c]pirrol antiviricos
NO20072198L (no) Korrosjons- og gasshydratinhibitorer med foroket biologisk nedbrytbarhet og redusert toksisitet
AR039988A1 (es) Derivados de benzoxazina como moduladores de 5-ht6 y usos de los mismos
SE0201937D0 (sv) Therapeutic agents
NO20073787L (no) Nye pyrimidin-nukleosidforbindelser eller dets salt

Legal Events

Date Code Title Description
FA Abandonment or withdrawal