ES2083580T3 - Profarmacos de fosforo. - Google Patents

Profarmacos de fosforo.

Info

Publication number
ES2083580T3
ES2083580T3 ES91912398T ES91912398T ES2083580T3 ES 2083580 T3 ES2083580 T3 ES 2083580T3 ES 91912398 T ES91912398 T ES 91912398T ES 91912398 T ES91912398 T ES 91912398T ES 2083580 T3 ES2083580 T3 ES 2083580T3
Authority
ES
Spain
Prior art keywords
prodrugs
drugs
methods
elimination reaction
phosphoric
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES91912398T
Other languages
English (en)
Inventor
Arnold Glazier
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Application granted granted Critical
Publication of ES2083580T3 publication Critical patent/ES2083580T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/555—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/732—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4087—Esters with arylalkanols
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/409—Compounds containing the structure P(=X)-X-acyl, P(=X) -X-heteroatom, P(=X)-X-CN (X = O, S, Se)
    • C07F9/4093—Compounds containing the structure P(=X)-X-C(=X)- (X = O, S, Se)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • 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

Abstract

SE DESCRIBEN LA COMPOSICION Y METODOS PARA LA SINTESIS DE VARIOS PROFARMACOS. ESTOS METODOS SE PUEDEN UTILIZAR PARA CONVERTIR LOS FARMACOS CON FOSFORO CARGADOS NEGATIVAMENTE EN OTROS CARGADOS DE MANERA NEUTRA; LOS PROFARMACOS SOLUBLES EN LIPIDOS CAPACES DE DIFUNDIRSE PASIVAMENTE EN CELULAS Y A TRAVES DE MEMBRANAS BIOLOGICAS. SE DESCRIBEN LOS PROFARMACOS PARA UNA VARIEDAD DE AGENTES ANTIVIRALES Y ANTILEUCEMICOS. SE DESCRIBE UNA CLASE DE PROFARMACOS QUE SON SOMETIDOS A UNA DEGRADACION MEDIANTE UNA REACCION DE ELIMINACION PARA FORMAR UN ENLACE DOBLE CARBONOCARBONO. ESTA REACCION DE ELIMINACION SE PROVOCA CON LA ESTERASA.
ES91912398T 1990-06-13 1991-06-11 Profarmacos de fosforo. Expired - Lifetime ES2083580T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US53733290A 1990-06-13 1990-06-13

Publications (1)

Publication Number Publication Date
ES2083580T3 true ES2083580T3 (es) 1996-04-16

Family

ID=24142202

Family Applications (1)

Application Number Title Priority Date Filing Date
ES91912398T Expired - Lifetime ES2083580T3 (es) 1990-06-13 1991-06-11 Profarmacos de fosforo.

Country Status (10)

Country Link
EP (1) EP0533833B1 (es)
JP (1) JP3347723B2 (es)
AT (1) ATE131825T1 (es)
AU (1) AU651835B2 (es)
CA (1) CA2083386C (es)
DE (1) DE69115694T2 (es)
DK (1) DK0533833T3 (es)
ES (1) ES2083580T3 (es)
GR (1) GR3019284T3 (es)
WO (1) WO1991019721A1 (es)

Families Citing this family (156)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6458772B1 (en) 1909-10-07 2002-10-01 Medivir Ab Prodrugs
US5627165A (en) * 1990-06-13 1997-05-06 Drug Innovation & Design, Inc. Phosphorous prodrugs and therapeutic delivery systems using same
CA2112803A1 (en) * 1991-07-12 1993-01-21 Karl Y. Hostetler Antiviral liponucleosides: treatment of hepatitis b
US5879700A (en) * 1991-10-15 1999-03-09 Hostetler; Karl Y. Nucleoside analogue phosphates for topical use
US5580571A (en) * 1991-10-15 1996-12-03 Hostetler; Karl Y. Nucleoside analogues
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
FR2692265B1 (fr) 1992-05-25 1996-11-08 Centre Nat Rech Scient Composes biologiquement actifs de type phosphotriesters.
US6020482A (en) * 1992-05-25 2000-02-01 Gosselin; Gilles Phosphotriester type biologically active compounds
US5955591A (en) * 1993-05-12 1999-09-21 Imbach; Jean-Louis Phosphotriester oligonucleotides, amidites and method of preparation
US6015573A (en) * 1993-05-12 2000-01-18 Hostetler; Karl Y. Nucleoside phosphate therapy for viral infection
US5654286A (en) * 1993-05-12 1997-08-05 Hostetler; Karl Y. Nucleotides for topical treatment of psoriasis, and methods for using same
US20020120130A1 (en) 1993-09-10 2002-08-29 Gilles Gosselin 2' or 3' -deoxy and 2', 3' -dideoxy-beta-L-pentofuranonucleo-side compounds, method of preparation and application in therapy, especially as anti- viral agents
US5798340A (en) 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
JPH09506333A (ja) * 1993-09-17 1997-06-24 ギリアード サイエンシーズ，インコーポレイテッド 治療化合物の投薬方法
US5656745A (en) * 1993-09-17 1997-08-12 Gilead Sciences, Inc. Nucleotide analogs
US5627185A (en) * 1994-11-23 1997-05-06 Gosselin; Gilles Acyclovir derivatives as antiviral agents
PT831852E (pt) 1995-06-07 2007-02-28 Uab Research Foundation Nucleósidos com actividade anti-vírus da hepatite b
US5717095A (en) * 1995-12-29 1998-02-10 Gilead Sciences, Inc. Nucleotide analogs
US5789589A (en) * 1996-04-22 1998-08-04 Drug Innovation & Design, Inc. Guanine analog phosphates
US5922695A (en) 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
JP2001527561A (ja) * 1997-05-15 2001-12-25 ドラッグ イノベーション アンド デザイン，インコーポレーテッド アシクロビルジエステル誘導体
US6180790B1 (en) 1997-05-15 2001-01-30 Drug Innovation And Design, Inc. Methods of preparing acyclovir prodrugs
EP1058686B1 (en) 1998-02-25 2006-11-02 Emory University 2'-fluoronucleosides
US6312662B1 (en) 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
WO2000009531A2 (en) 1998-08-10 2000-02-24 Novirio Pharmaceuticals Limited β-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B
US6444652B1 (en) 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
DK1382343T3 (da) 1998-11-02 2010-04-26 Gilead Sciences Inc Kombinationsterapi til behandling af hepatitis B-virus
US7205404B1 (en) 1999-03-05 2007-04-17 Metabasis Therapeutics, Inc. Phosphorus-containing prodrugs
KR100875335B1 (ko) 1999-12-22 2008-12-22 메타베이시스 테라퓨틱스, 인크. 신규 비스아미데이트 포스포네이트 프로드러그
CZ20023018A3 (cs) 2000-03-08 2003-01-15 Metabasis Therapeutics, Inc. Nové inhibitory fruktóza-1,6-bisfosfatázy obsahující arylovou skupinu
US6670342B2 (en) 2000-03-29 2003-12-30 Georgetown University Method of treating hepatitis delta virus infection
US6684250B2 (en) 2000-04-03 2004-01-27 Quova, Inc. Method and apparatus for estimating a geographic location of a networked entity
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
EP1294735A2 (en) 2000-05-26 2003-03-26 Novirio Pharmaceuticals Limited Methods and compositions for treating flaviviruses and pestiviruses
US6875751B2 (en) 2000-06-15 2005-04-05 Idenix Pharmaceuticals, Inc. 3′-prodrugs of 2′-deoxy-β-L-nucleosides
US7563774B2 (en) 2000-06-29 2009-07-21 Metabasis Therapeutics, Inc. Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes
DE10035189A1 (de) * 2000-07-20 2002-02-21 Hassan Jomaa Arzneimittel zur oralen Applikation mit einem Gehalt an 3-N-Formylhydroxylaminopropylphosphonsäureestern oder 3-N-Acetylhydroxylaminopropylphosphonsäureestern als Wirkstoff
KR101201552B1 (ko) 2000-10-18 2012-11-15 파마셋 인코포레이티드 바이러스 감염 및 비정상적인 세포 증식의 치료를 위한 변형된 뉴클레오시드
EP1903041B1 (en) 2001-03-01 2015-02-18 AbbVie Inc. Polymorphic and other crystalline forms of cis-FTC
CA2481449A1 (en) 2002-04-26 2003-11-06 Gilead Sciences, Inc. Method and compositions for identifying anti-hiv therapeutic compounds
WO2003095665A2 (en) 2002-05-13 2003-11-20 Metabasis Therapeutics, Inc. Pmea and pmpa cyclic producing synthesis
KR20050035194A (ko) 2002-06-28 2005-04-15 이데닉스 (케이만) 리미티드 플라비비리다에 감염 치료용 2'-ｃ-메틸-3'-ｏ-ｌ-발린에스테르 리보푸라노실 사이티딘
RS114004A (en) 2002-06-28 2007-02-05 Idenix (Cayman) Limited, Modified 2' and 3'-nucleoside produgs for treating flaviridae infections
MXPA04012779A (es) 2002-06-28 2005-08-19 Idenix Cayman Ltd Profarmacos de 2'- y 3'-nucleosido para tratar infecciones por flaviviridae.
US7608600B2 (en) 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
TWI244393B (en) 2002-08-06 2005-12-01 Idenix Pharmaceuticals Inc Crystalline and amorphous forms of beta-L-2'-deoxythymidine
AU2003278816A1 (en) 2002-09-13 2004-04-30 Idenix (Cayman) Limited ss-L-2'-DEOXYNUCLEOSIDES FOR THE TREATMENT OF RESISTANT HBV STRAINS AND COMBINATION THERAPIES
WO2004035577A2 (en) 2002-10-16 2004-04-29 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
ATE442375T1 (de) 2002-10-31 2009-09-15 Metabasis Therapeutics Inc Cytarabin-monophosphate prodrugs
CN1849142A (zh) 2002-11-15 2006-10-18 埃迪尼克斯(开曼)有限公司 2′－支链核苷和黄病毒突变
EP1923063A3 (en) 2003-01-14 2009-04-08 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
WO2004096233A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Nucleoside phosphonate conjugates
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
US7273716B2 (en) 2003-04-25 2007-09-25 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds with GS-7340 ester hydrolase
US7427636B2 (en) 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
EP1620109A2 (en) 2003-04-25 2006-02-01 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
WO2004096285A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
WO2005002626A2 (en) 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
NZ542342A (en) 2003-04-25 2009-05-31 Gilead Sciences Inc Antiviral phosphonate analogs
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
EP2345661A1 (en) 2003-05-30 2011-07-20 Pharmasset, Inc. Modified fluorinated nucleoside analogues
DK1658302T3 (da) 2003-07-25 2010-11-22 Idenix Pharmaceuticals Inc Purinnukleosidanaloge til behandling af sygdomme forårsaget af Flavirividae, herunder hepatitis C
AU2004260789B2 (en) 2003-07-30 2011-06-30 Gilead Sciences, Inc. Nucleobase phosphonate analogs for antiviral treatment
DE602004021611D1 (de) * 2003-09-19 2009-07-30 Gilead Sciences Inc Azachinolinolphosphonatverbindungen als integraseinhibitoren
WO2005044308A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
WO2005044279A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
CA2546601A1 (en) 2003-11-19 2005-06-09 Metabasis Therapeutics, Inc. Novel phosphorus-containing thyromimetics
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
PT1716162E (pt) 2003-12-30 2010-11-24 Gilead Sciences Inc Fosfonatos, monofosfonamidatos, bisfosfonamidatos para o tratamento de doenças virais
WO2005094322A2 (en) 2004-03-29 2005-10-13 University Of South Florida Effective treatment of tumors and cancer with triciribine and related compounds
US7582758B2 (en) 2004-06-08 2009-09-01 Metabasis Therapeutics, Inc. Lewis acid mediated synthesis of cyclic esters
UA93354C2 (ru) 2004-07-09 2011-02-10 Гилиад Сайенсиз, Инк. Местный противовирусный препарат
BRPI0513426A (pt) 2004-07-16 2007-11-27 Gilead Sciences Inc processo de preparação de amino ácidos úteis na preparação de moduladores de receptores de peptìdeos
AU2011218664B2 (en) * 2004-07-27 2014-08-21 Gilead Sciences, Inc. Antiviral compounds
AU2005330489B2 (en) 2004-07-27 2011-08-25 Gilead Sciences, Inc. Nucleoside phosphonate conjugates as anti HIV agents
AU2005285045B2 (en) 2004-09-14 2011-10-13 Gilead Pharmasset Llc Preparation of 2'fluoro-2'- alkyl- substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
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
EP1906971A2 (en) * 2005-07-27 2008-04-09 Gilead Sciences, Inc. Antiviral compounds
EA200800932A1 (ru) 2005-09-26 2008-10-30 Фармассет, Инк. Модифицированные 4`-нуклеозиды в качестве противовирусных агентов
US8895531B2 (en) 2006-03-23 2014-11-25 Rfs Pharma Llc 2′-fluoronucleoside phosphonates as antiviral agents
JP2009537546A (ja) 2006-05-16 2009-10-29 ギリアード サイエンシーズ， インコーポレイテッド インテグラーゼ阻害剤
AR061840A1 (es) 2006-07-07 2008-09-24 Gilead Sciences Inc Compuestos fosfinatos antivirales
JP5322951B2 (ja) 2007-02-09 2013-10-23 リガンド・ファーマシューティカルズ・インコーポレイテッド グルカゴン受容体の新規アンタゴニスト
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
CA2681267C (en) 2007-04-13 2013-11-19 Southern Research Institute Anti-angiogenic agents and methods of use
JP5572549B2 (ja) 2007-08-13 2014-08-13 リガンド・ファーマシューティカルズ・インコーポレイテッド グルコキナーゼの新規な活性化剤
CA2722308C (en) 2008-04-15 2024-02-27 Rfs Pharma, Llc. Nucleoside derivatives for treatment of caliciviridae infections, including norovirus infections
BRPI0911410A2 (pt) 2008-04-23 2015-10-06 Gilead Sciences Inc análogos de carba-nucleosídeo para tratamento antiviral
WO2010005986A1 (en) 2008-07-08 2010-01-14 Gilead Sciences, Inc. Salts of hiv inhibitor compounds
KR101599089B1 (ko) 2008-08-13 2016-03-02 메타베이시스 테라퓨틱스, 인크. 글루카곤 길항제
AR074897A1 (es) 2008-12-23 2011-02-23 Pharmasset Inc Fosforamidatos de nucleosidos
SG172361A1 (en) 2008-12-23 2011-07-28 Pharmasset Inc Nucleoside analogs
AU2009329872B2 (en) 2008-12-23 2016-07-07 Gilead Pharmasset Llc Synthesis of purine nucleosides
PE20160858A1 (es) 2009-02-10 2016-09-03 Gilead Sciences Inc Analogos carba-nucleosidicos para tratamiento antiviral
NZ619205A (en) 2009-05-13 2015-04-24 Gilead Pharmasset Llc Antiviral compounds
TWI583692B (zh) 2009-05-20 2017-05-21 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
EP2270021A1 (en) * 2009-06-18 2011-01-05 Centre National de la Recherche Scientifique Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability
US7973013B2 (en) 2009-09-21 2011-07-05 Gilead Sciences, Inc. 2'-fluoro substituted carba-nucleoside analogs for antiviral treatment
SI2480559T1 (sl) 2009-09-21 2013-10-30 Gilead Sciences, Inc. Postopki in intermediati za pripravo 1'-ciano-karbanukleozidnih analogov
PE20210668A1 (es) 2009-09-21 2021-04-05 Gilead Sciences Inc Analogos de carba-nucleosidos sustituidos con 2'-fluoro antivirales
US20110223131A1 (en) 2010-02-24 2011-09-15 Gilead Sciences, Inc. Antiviral compounds
EP2752422B1 (en) 2010-03-31 2017-08-16 Gilead Pharmasset LLC Stereoselective synthesis of phosphorus containing actives
CA2797872A1 (en) 2010-05-21 2011-11-24 Gilead Sciences, Inc. Heterocyclic flaviviridae virus inhibitors
AU2011274323B2 (en) 2010-07-02 2015-08-06 Gilead Sciences, Inc. 2 -quinolinyl- acetic acid derivatives as HIV antiviral compounds
US9102614B2 (en) 2010-07-02 2015-08-11 Gilead Sciences, Inc. Naphth-2-ylacetic acid derivatives to treat AIDS
KR20200052384A (ko) 2010-07-19 2020-05-14 길리애드 사이언시즈, 인코포레이티드 부분입체 이성질성으로 순수한 포스포라미데이트 전구약물의 제조 방법
PT2595980E (pt) 2010-07-22 2014-11-27 Gilead Sciences Inc Métodos e compostos para tratar infeções pelo vírus da família paramyxoviridae
TW201305185A (zh) 2010-09-13 2013-02-01 Gilead Sciences Inc 用於抗病毒治療之２’－氟取代之碳－核苷類似物
BR112013008017A2 (pt) 2010-09-20 2016-06-14 Gilead Sciences Inc análogos de carba-nucleosídeo 2-flúor substituídos para tratamento antiviral
AU2011328980B2 (en) 2010-11-17 2015-07-30 Gilead Pharmasset Llc Antiviral compounds
ES2716158T3 (es) 2010-11-30 2019-06-10 Gilead Pharmasset Llc 2'-spiro-nucleótidos para el tratamiento de hepatitis C
EA201391264A1 (ru) 2011-04-13 2014-03-31 Джилид Сайэнс, Инк. 1'-замещенные пиримидиновые n-нуклеозидные аналоги для противовирусного лечения
AP2015008931A0 (en) 2011-04-21 2015-12-31 Gilead Sciences Inc Benzothiazole compounds and their pharmaceutical use
US9540343B2 (en) 2011-07-06 2017-01-10 Gilead Sciences, Inc. Compounds for the treatment of HIV
PL2635588T3 (pl) 2011-11-16 2015-10-30 Gilead Pharmasset Llc Skondensowane imidazoliloimidazole jako związki antywirusowe
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
EP2794624B1 (en) 2011-12-22 2019-05-15 Geron Corporation Guanine analogs as telomerase substrates and telomere length affectors
WO2013103724A1 (en) 2012-01-04 2013-07-11 Gilead Sciences, Inc. 2- (tert - butoxy) -2- (7 -methylquinolin- 6 - yl) acetic acid derivatives for treating aids
WO2013103738A1 (en) 2012-01-04 2013-07-11 Gilead Sciences, Inc. Napthalene acetic acid derivatives against hiv infection
CA2850881C (en) 2012-04-20 2021-02-16 Gilead Sciences, Inc. Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection
CN103665043B (zh) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 一种替诺福韦前药及其在医药上的应用
ES2900570T3 (es) 2013-08-27 2022-03-17 Gilead Pharmasset Llc Formulación de combinación de dos compuestos antivirales
CN104016865B (zh) * 2014-01-14 2015-10-07 杭州福斯特药业有限公司 酚羟基取代的苯甲酰乙酸乙酯的合成方法
US10202353B2 (en) 2014-02-28 2019-02-12 Gilead Sciences, Inc. Therapeutic compounds
JP2017519000A (ja) 2014-06-12 2017-07-13 リガンド・ファーマシューティカルズ・インコーポレイテッド グルカゴンアンタゴニスト
TWI698444B (zh) 2014-10-29 2020-07-11 美商基利科學股份有限公司 製備核糖苷的方法
CA2998189C (en) 2015-09-16 2021-08-03 Gilead Sciences, Inc. Methods for treating arenaviridae and coronaviridae virus infections
HUE063811T2 (hu) 2016-08-19 2024-02-28 Gilead Sciences Inc HIV-vírus-fertõzés megelõzõ vagy terápiás kezelésére alkalmas terápiás vegyületek
US10449208B2 (en) * 2016-08-25 2019-10-22 Merck Sharp & Dohme Corp. Antiviral prodrugs of tenofovir
CN110869028B (zh) 2017-03-14 2023-01-20 吉利德科学公司 治疗猫冠状病毒感染的方法
CN115403626A (zh) 2017-05-01 2022-11-29 吉利德科学公司 新结晶形式
US10675296B2 (en) 2017-07-11 2020-06-09 Gilead Sciences, Inc. Compositions comprising an RNA polymerase inhibitor and cyclodextrin for treating viral infections
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
TW202024061A (zh) 2017-08-17 2020-07-01 美商基利科學股份有限公司 Hiv蛋白質膜抑制劑之固體形式
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
KR102587510B1 (ko) 2018-02-15 2023-10-11 길리애드 사이언시즈, 인코포레이티드 피리딘 유도체 및 hiv 감염을 치료하기 위한 그의 용도
WO2019161280A1 (en) 2018-02-16 2019-08-22 Gilead Sciences, Inc. Methods and intermediates for preparing a therapeutic compound useful in the treatment of retroviridae viral infection
CA3216031A1 (en) 2018-07-16 2020-01-23 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
KR20220106165A (ko) 2019-11-26 2022-07-28 길리애드 사이언시즈, 인코포레이티드 Hiv의 예방을 위한 캡시드 억제제
WO2021154687A1 (en) 2020-01-27 2021-08-05 Gilead Sciences, Inc. Methods for treating sars cov-2 infections
CN115298181A (zh) 2020-03-12 2022-11-04 吉利德科学公司 制备1’-氰基核苷的方法
EP4132651A1 (en) 2020-04-06 2023-02-15 Gilead Sciences, Inc. Inhalation formulations of 1'-cyano substituted carbanucleoside analogs
CA3179226A1 (en) 2020-05-29 2021-12-02 Tomas Cihlar Remdesivir treatment methods
CN115996928A (zh) 2020-06-24 2023-04-21 吉利德科学公司 1’-氰基核苷类似物及其用途
EP4172157A1 (en) 2020-06-25 2023-05-03 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
PE20231983A1 (es) 2020-08-27 2023-12-12 Gilead Sciences Inc Compuestos y metodos para el tratamiento de infecciones virales
WO2022246109A1 (en) 2021-05-21 2022-11-24 Gilead Sciences, Inc. Pentacyclic derivatives as zika virus inhibitors
TW202337439A (zh) 2021-12-03 2023-10-01 美商基利科學股份有限公司 用於ｈｉｖ病毒感染之治療性化合物
WO2023167944A1 (en) 2022-03-02 2023-09-07 Gilead Sciences, Inc. Compounds and methods for treatment of viral infections

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU610344B2 (en) * 1988-02-29 1991-05-16 Taiho Pharmaceutical Co., Ltd. 2'-deoxy-5-fluorouridine derivatives
EP0338372A3 (en) * 1988-04-22 1991-10-09 American Cyanamid Company Solubilized pro-drugs
US5194599A (en) * 1988-09-23 1993-03-16 Gilead Sciences, Inc. Hydrogen phosphonodithioate compositions

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