EA002647B1 - Пролекарства - Google Patents

Пролекарства Download PDF

Info

Publication number
EA002647B1
EA002647B1 EA200000838A EA200000838A EA002647B1 EA 002647 B1 EA002647 B1 EA 002647B1 EA 200000838 A EA200000838 A EA 200000838A EA 200000838 A EA200000838 A EA 200000838A EA 002647 B1 EA002647 B1 EA 002647B1
Authority
EA
Eurasian Patent Office
Prior art keywords
mmol
acid
solution
valyloxy
added
Prior art date
Application number
EA200000838A
Other languages
English (en)
Russian (ru)
Other versions
EA200000838A1 (ru
Inventor
Нильс Гуннар Йоханссон
Ксиао-Ксионг Жоу
Хорст Велинг
Кристиан Сунд
Ханс Валльберг
Лурдес Сальвадор
Стефан Линдстрем
Original Assignee
Медивир Аб
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
Priority claimed from SE9800452A external-priority patent/SE9800452D0/xx
Priority claimed from SE9800469A external-priority patent/SE9800469D0/xx
Priority claimed from SE9801216A external-priority patent/SE9801216D0/xx
Priority claimed from ZA987267A external-priority patent/ZA987267B/xx
Priority claimed from PCT/SE1998/001467 external-priority patent/WO1999009031A1/en
Priority claimed from SE9803438A external-priority patent/SE9803438D0/xx
Application filed by Медивир Аб filed Critical Медивир Аб
Publication of EA200000838A1 publication Critical patent/EA200000838A1/ru
Publication of EA002647B1 publication Critical patent/EA002647B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4025—Esters of poly(thio)phosphonic acids
    • C07F9/404—Esters of poly(thio)phosphonic acids containing hydroxy substituents in the hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4075—Esters with hydroxyalkyl compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
    • 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
    • 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
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrane Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cephalosporin Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)
  • Saccharide Compounds (AREA)
EA200000838A 1998-02-13 1999-02-15 Пролекарства EA002647B1 (ru)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
SE9800452A SE9800452D0 (sv) 1998-02-13 1998-02-13 Antivirals
SE9800469A SE9800469D0 (sv) 1998-02-16 1998-02-16 Pharmaceuticals
SE9801216A SE9801216D0 (sv) 1998-04-03 1998-04-03 Pharmaceuticals
ZA987267A ZA987267B (en) 1997-08-15 1998-08-13 Nucleosides
PCT/SE1998/001467 WO1999009031A1 (en) 1997-08-15 1998-08-14 Nucleosides analogues, such as antivirals including inhibitors of retroviral reverse transcriptase and the dna polymerase of hepatitis b virus (hbv)
SE9803438A SE9803438D0 (sv) 1998-10-07 1998-10-07 Antivirals
PCT/SE1999/000194 WO1999041275A1 (en) 1998-02-13 1999-02-15 Prodrugs

Publications (2)

Publication Number Publication Date
EA200000838A1 EA200000838A1 (ru) 2001-04-23
EA002647B1 true EA002647B1 (ru) 2002-08-29

Family

ID=56289887

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000838A EA002647B1 (ru) 1998-02-13 1999-02-15 Пролекарства

Country Status (7)

Country Link
US (4) US6458772B1 (enExample)
EP (1) EP1054891A1 (enExample)
JP (1) JP2002503673A (enExample)
AU (1) AU754733B2 (enExample)
CA (1) CA2318978A1 (enExample)
EA (1) EA002647B1 (enExample)
WO (1) WO1999041275A1 (enExample)

Families Citing this family (44)

* 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
WO1999051613A1 (en) * 1998-04-03 1999-10-14 Medivir Ab Prodrugs of phosphorous-containing pharmaceuticals
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
CZ301182B6 (cs) * 2000-05-26 2009-12-02 Idenix (Cayman) Limited Použití nukleosidových derivátu pro výrobu farmaceutických prostredku pro lécení infekcí vyvolaných flaviviry a pestiviry
US7527807B2 (en) * 2000-06-21 2009-05-05 Cubist Pharmaceuticals, Inc. Compositions and methods for increasing the oral absorption of antimicrobials
AU2001271259A1 (en) * 2000-06-28 2002-01-08 Intertainer, Inc. Intelligent media targeting system and method
US7144877B2 (en) 2000-10-06 2006-12-05 Xenoport, Inc. Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
IL142535A0 (en) * 2001-04-11 2002-03-10 Yeda Res & Dev Pharmaceutical compositions for the treatment of inflammation
US20050019399A1 (en) * 2001-09-21 2005-01-27 Gina Fischer Controlled release solid dispersions
EP1429739A1 (en) * 2001-09-21 2004-06-23 Egalet A/S Polymer release system
WO2004002422A2 (en) 2002-06-28 2004-01-08 Idenix (Cayman) Limited 2’-c-methyl-3’-o-l-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
CN101172993A (zh) 2002-06-28 2008-05-07 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
US7608600B2 (en) * 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
ZA200502613B (en) * 2002-10-10 2006-10-25 Yeda Res & Dev Basic esters of fatty alcohols and their use as anti-inflammatory or immunomodulatory agents
US20040152769A1 (en) * 2002-11-09 2004-08-05 Ekwuribe Nnochiri Nkem Modified carbamate-containing prodrugs and methods of synthesizing same
ES2624353T3 (es) 2002-11-15 2017-07-13 Idenix Pharmaceuticals Llc 2'-Metil nucleósidos en combinación con interferón y mutación de Flaviviridae
RU2005121904A (ru) 2002-12-12 2006-01-20 Айденикс (Кайман) Лимитед (Ky) Способ получения 2`-разветвленных нуклеозидов
GB0301938D0 (en) * 2003-01-28 2003-02-26 Biochemie Gmbh Organic compounds
DE602004031096D1 (de) 2003-03-26 2011-03-03 Egalet As Morphin-system mit kontrollierter freisetzung
WO2004087169A1 (en) * 2003-03-27 2004-10-14 Boehringer Ingelheim International Gmbh Antiviral combination of nevirapine and a further antiretroviral compound
WO2005075655A2 (en) 2004-02-02 2005-08-18 Pioneer Hi-Bred International, Inc. Ap2 domain transcription factor odp2 (ovule development protein 2) and methods of use
EP2974718A1 (en) * 2005-04-29 2016-01-20 Cubist Pharmaceuticals, Inc. Therapeutic compositions
JP5254033B2 (ja) 2005-12-23 2013-08-07 イデニク プハルマセウティカルス，インコーポレイテッド 分岐型ヌクレオシドを調製するための合成中間体の製造方法
WO2007084548A2 (en) * 2006-01-18 2007-07-26 Fil-Am Tech., Inc. Viral treatment
WO2008106091A1 (en) * 2007-02-26 2008-09-04 Yeda Research And Development Co. Ltd. Use of long-chain alcohol derivatives for the treatment of alopecia areata
US7964751B2 (en) * 2007-02-26 2011-06-21 Yeda Research And Development Co. Ltd. Enantiomers of amino-phenyl-acetic acid octadec-9-(Z) enyl ester, their salts and their uses
CA2687192C (en) 2007-06-04 2015-11-24 Egalet A/S Controlled release pharmaceutical compositions for prolonged effect
BRPI0813237B8 (pt) 2007-06-18 2021-05-25 Sunshine Lake Pharma Co Ltd composto, método para preparar o composto, medicamento, e, uso do composto
NZ594207A (en) 2009-02-06 2013-03-28 Egalet Ltd Immediate release composition resistant to abuse by intake of alcohol
NZ597283A (en) 2009-06-24 2013-07-26 Egalet Ltd Controlled release formulations
AU2010339481B2 (en) 2009-12-30 2016-02-04 Pioneer Hi-Bred International, Inc. Methods and compositions for targeted polynucleotide modification
EP2529018B1 (en) 2009-12-30 2016-06-22 Pioneer Hi-Bred International, Inc. Methods and compositions for the introduction and regulated expression of genes in plants
US8530444B2 (en) * 2010-06-01 2013-09-10 Aposense Ltd. Pharmaceutical compounds
US9192680B2 (en) 2010-06-01 2015-11-24 Aposense Ltd. Pharmaceutical compounds
JP2014506593A (ja) * 2011-02-21 2014-03-17 メディヴィル・アクチエボラーグ Ｆｌｇの合成
CA3207643A1 (en) * 2015-09-23 2017-03-30 XWPharma Ltd. Prodrugs of gamma-hydroxybutyric acid, compositions and uses thereof
KR102378845B1 (ko) 2017-03-30 2022-03-24 엑스더블유파마 리미티드 이환형 헤테로아릴 유도체 및 이의 제조 및 용도
CN112004802B (zh) 2018-09-30 2021-12-28 凯瑞康宁生物工程（武汉）有限公司 作为神经元组胺受体-3拮抗剂的化合物及其用途
CN115244028A (zh) 2019-12-20 2022-10-25 凯瑞康宁生物工程有限公司 4-缬氨酰氧基丁酸的合成方法
AU2021292406B2 (en) 2020-06-18 2024-03-14 XWPharma Ltd. Controlled release granulations of water-soluble active pharmaceutical ingredients
AU2021293941B2 (en) 2020-06-18 2024-03-28 XWPharma Ltd. Pharmaceutical granulations of water-soluble active pharmaceutical ingredients
CN116261451A (zh) 2020-07-24 2023-06-13 凯瑞康宁生物工程有限公司 γ-羟基丁酸衍生物的药物组合物和药物动力学
CN115666527B (zh) 2020-10-05 2025-03-07 凯瑞康宁生物工程有限公司 γ-羟基丁酸衍生物的修饰释放组合物
TW202300139A (zh) 2021-03-19 2023-01-01 凱瑞康寧生技股份有限公司 γ-羟基丁酸衍生物的聯合釋放製劑的藥代動力學

Family Cites Families (59)

* 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
IE34948B1 (en) 1970-03-12 1975-10-01 Leo Pharm Prod Ltd New penicillin esters
US3705191A (en) 1970-04-13 1972-12-05 Monsanto Co Substituted ethane diphosphonic acids and salts and esters thereof
US4168267A (en) 1978-10-23 1979-09-18 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl prolines
GB2043072B (en) 1979-02-13 1983-11-23 Symphar Sa Diphosphonate compounds
US4486425A (en) 1980-09-30 1984-12-04 Sankyo Company Limited 7-[2-(2-Aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]-3-methoxymethyl-3-cephem-4-carboxylates
US4337201A (en) 1980-12-04 1982-06-29 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl substituted prolines
US4760057A (en) 1983-06-23 1988-07-26 Merck & Co., Inc. (Acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs
US4594199A (en) 1983-09-19 1986-06-10 E. R. Squibb & Sons, Inc. Method for making phosphinic acid intermediates
GB8421112D0 (en) 1984-08-20 1984-09-26 Unilever Plc Pyroglutamic acid esters
US4968788A (en) 1986-04-04 1990-11-06 Board Of Regents, The University Of Texas System Biologically reversible phosphate and phosphonate protective gruops
SE8602981D0 (sv) 1986-07-04 1986-07-04 Astra Laekemedel Ab Novel medicinal use
DE3623397A1 (de) 1986-07-11 1988-01-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
DD279407A1 (de) 1986-07-24 1990-06-06 Akad Wissenschaften Ddr Verfahren zur herstellung eines mittels gegen aids
DK406686D0 (da) 1986-08-26 1986-08-26 Hans Bundgaard Carboxylsyrederivater
GB8719367D0 (en) 1987-08-15 1987-09-23 Wellcome Found Therapeutic compounds
CA1321994C (en) 1987-10-28 1993-09-07 Reid Von Borstel Acylated uridine and cytidine and uses thereof
US5198539A (en) 1988-08-19 1993-03-30 Burroughs Wellcome Co. 5'-esters of 2',3'-dideoxy-3'-fluoro-5-ethynyluridine
ZA898567B (en) 1988-11-15 1990-08-29 Merrell Dow Pharma Novel 2'-halomethylidene,2'-ethenylidene and 2'-ethynyl cytidine,uridine and guanosine derivatives
AU618436B2 (en) 1988-12-19 1991-12-19 Wellcome Foundation Limited, The Antiviral cytosine and guanine derivatives
DK24089D0 (da) 1989-01-20 1989-01-20 Hans Bundgaard Novel prodrug derivatives of biologically active agents containing hydroxyl groups or nh-acidic groups
US5001115A (en) 1989-05-17 1991-03-19 University Of Florida Prodrugs of biologically active hydroxyaromatic compounds
FI83421C (fi) 1989-06-21 1991-07-10 Huhtamaeki Oy Foerfarande foer framstaellning av farmakologiskt anvaendbara metylenbisfosfonsyraderivat.
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
US5227506A (en) 1989-09-06 1993-07-13 Merck & Co., Inc. Acyloxymethyl esters of bisphosphonic acids as bone resorption inhibitors
AU636678B2 (en) * 1989-11-06 1993-05-06 Nycomed Imaging As Nucleoside derivatives
DE69115694T2 (de) 1990-06-13 1996-10-17 Arnold Newton Mass. Glazier Phosphorylierte prodrugs
US5177064A (en) 1990-07-13 1993-01-05 University Of Florida Targeted drug delivery via phosphonate derivatives
WO1992013561A1 (en) 1991-02-08 1992-08-20 Pro-Neuron, Inc. Oxypurine nucleosides and their congeners, and acyl derivatives thereof, for improvement of hematopoiesis
JP3132167B2 (ja) 1991-08-23 2001-02-05 藤沢薬品工業株式会社 デプシペプチド誘導体の製造法
EP0541037A3 (en) 1991-11-06 1997-02-26 Takeda Chemical Industries Ltd Squalene synthetase inhibitory composition and use thereof
DE69330114T2 (de) 1992-07-10 2001-08-02 Toray Industries, Inc. Methandiphosphonat-derivat, dessen produktion und dessen verwendung als arzneimittel
US5484911A (en) 1993-04-01 1996-01-16 Health Research, Inc. Nucleoside 5'-diphosphate conjugates of ether lipids
GB9515279D0 (en) 1995-07-25 1995-09-20 Norsk Hydro As Improved therapeutic agents
DE4311801A1 (de) 1993-04-09 1994-10-13 Hoechst Ag Neue Carbonsäureester von 2-Amino-7-(1,3-dihydroxy-2-propoxymethyl)purin, deren Herstellung sowie deren Verwendung
DE4321946A1 (de) 1993-07-01 1995-01-12 Hoechst Ag Methylphosphonsäureester, Verfahren zu deren Herstellung und deren Verwendung
AU5722694A (en) 1993-11-05 1995-05-23 Astra Aktiebolag Novel amino acid derivatives
IL111584A0 (en) 1993-11-18 1995-01-24 Merck & Co Inc Prodrugs of an inhibitor of hiv protease and pharmaceutical compositions containing them
DE4342907A1 (de) 1993-12-16 1995-06-22 Bayer Ag Neue cyclische Depsipeptide mit 18 Ringatomen und ihre Verwendung zur Bekämpfung von Endoparasiten
DE4418690A1 (de) 1994-05-28 1996-01-11 Boehringer Mannheim Gmbh Neue Lipidester von Nucleosid-Monophosphaten und deren Verwendung als immunsuppressive Arzneimittel
US5441942A (en) * 1994-05-27 1995-08-15 The Scripps Research Institute 2'3'-dideoxy-2',3'-didehydro-7,8-disubstituted guanosines and their immunostimulative effect
US5466811A (en) 1994-07-18 1995-11-14 Merck & Co., Inc. Dioxolenylmethyl carbamates pro moieties for amine drugs
US5543414A (en) 1994-07-28 1996-08-06 Syntex (Usa) Inc. Achiral amino acid acyl esters of ganciclovir and its derivatives
PE32296A1 (es) 1994-07-28 1996-08-07 Hoffmann La Roche Ester de l-monovalina derivado de 2-(2-amino-1,6-dihidro-6-oxo-purin-9-il) metoxi-1,3-propandiol y sus sales farmaceuticamente aceptables
US5696277A (en) 1994-11-15 1997-12-09 Karl Y. Hostetler Antiviral prodrugs
WO1996021440A1 (en) 1995-01-09 1996-07-18 Alpha-Therapeutics, Inc. Methods for increasing the bioavailability of biological active agents
BR9607492A (pt) 1995-01-16 1999-06-29 Commw Scient Ind Res Org Conjugados de ácidos graxos de composto terapêutico
IL113246A (en) 1995-04-04 2004-08-31 Yissum Res Dev Co Bisphosphonates and pharmaceutical compositions containing them
WO1996033201A1 (en) 1995-04-21 1996-10-24 Centre National De La Recherche Scientifique (Cnrs) Acyclovir derivatives as antiviral agents
DE19529604A1 (de) 1995-08-11 1997-02-13 Bayer Ag Endoparasitizide Mittel auf Basis von Didepsipeptiden, neue Didepsipeptide und ein Verfahren zu ihrer Herstellung
US5717095A (en) 1995-12-29 1998-02-10 Gilead Sciences, Inc. Nucleotide analogs
AU1592897A (en) 1996-01-26 1997-08-20 F. Hoffmann-La Roche Ag Process for preparing purine derivatives
US5869493A (en) 1996-02-16 1999-02-09 Medivir Ab Acyclic nucleoside derivatives
JP2001503767A (ja) 1996-11-12 2001-03-21 メディヴィル・アクチボラグ ヌクレオシド
ATE297904T1 (de) 1997-04-15 2005-07-15 Genentech Inc Halo-alkoxycarbonylverbindungen
WO1998051692A1 (en) 1997-05-15 1998-11-19 Drug Innovation & Design, Inc. Acyclovir diester derivatives
DE69800753D1 (de) * 1997-08-15 2001-06-07 Medivir Ab Huddinge Analoge nukleoside, wie antivirale einschliesslich inhibitoren der retroviralen reverstranskriptase und der dna polymerase des hepatitis b virus
WO1999051613A1 (en) * 1998-04-03 1999-10-14 Medivir Ab Prodrugs of phosphorous-containing pharmaceuticals
US6974803B2 (en) * 2001-12-06 2005-12-13 Pfizer Inc Pharmaceutical combination

Also Published As

Publication number Publication date
EP1054891A1 (en) 2000-11-29
CA2318978A1 (en) 1999-08-19
JP2002503673A (ja) 2002-02-05
WO1999041275A1 (en) 1999-08-19
US20060058259A1 (en) 2006-03-16
US6974802B2 (en) 2005-12-13
EA200000838A1 (ru) 2001-04-23
US20030186924A1 (en) 2003-10-02
US6458772B1 (en) 2002-10-01
US7071173B2 (en) 2006-07-04
AU3282099A (en) 1999-08-30
AU754733B2 (en) 2002-11-21
US7825238B2 (en) 2010-11-02
US20060122383A1 (en) 2006-06-08

Similar Documents

Publication Publication Date Title
EA002647B1 (ru) Пролекарства
KR100296543B1 (ko) 시토킨생산을유도하는우레탄및우레아,이의제조방법
US5684018A (en) Acyloxyisopropyl carbamates as prodrugs for amine drugs
US4916230A (en) Process for preparing novel N-(acyloxy-alkoxy)carbonyl derivatives useful as bioreversible prodrug moieties for primary and secondary amine functions in drugs
US5466811A (en) Dioxolenylmethyl carbamates pro moieties for amine drugs
DE69620727T2 (de) Paclitaxel Prodrogen, Verfahren zur Herstellung und ihre Verwendung zur selektiven Chemotherapie
WO2003077902A1 (en) Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
RU2124509C1 (ru) Производные нейраминовой кислоты, или их фармацевтически приемлемые соли, или их сложные эфиры, а также фармацевтическая композиция, обладающая сиалидазу-ингибирующей активностью
Barrett et al. Applications of crotyldiisopinocampheylboranes in synthesis: the total synthesis of nikkomycin B
JP2002536435A (ja) 非ヌクレオシド逆転写酵素インヒビター
JP3416142B2 (ja) ヒト白血球エラスターゼの阻害剤としてのジアステレオマー純粋なトリフルオロメチルケトンペプチド誘導体
JP2001513767A (ja) メタロプロテアーゼ阻害剤としての逆ヒドロキサメート誘導体
EP0096296A2 (de) 1-Sulfo-2-oxoazetidinderivate
JP3844654B2 (ja) レトロウイルス逆転写酵素およびｂ型肝炎ウイルス（ｈｂｖ）のｄｎａポリメラーゼのインヒビターを含む抗ウイルス剤などのヌクレオシドアナログ
AU723994B2 (en) Neuraminic acid compound
JP2002521312A (ja) ノイラミニダーゼの阻害剤
JP4233262B2 (ja) カルバ糖アミン誘導体及びそれを用いるグリコシダーゼ阻害剤
EP0271443B1 (de) N,N'-Disubstituierte Harnstoffe und Verfahren zu ihrer Herstellung
EP0240338B1 (en) Butenoic acid derivatives
KR950005775B1 (ko) 4-하이드록시-4-(치환된 알케닐)사이클로헥산 카복실산
ES2219711T3 (es) 6-(hidroximetil-etil)piridina como inhibidores de la hmg-coa-reductasa.
RU2444516C2 (ru) Способ синтеза производных имидазоламинокислот и родственных соединений
JP2011241170A (ja) ビタミンｄ誘導体およびその製造方法
MXPA99001527A (en) Neuraminic acid compounds
JPH0586020A (ja) α，β−ジヒドロキシ−γ，δ−不飽和カルボン酸チオールエステル誘導体およびその製造方法

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU