TWI347325B - Novel phosphonic acid based prodrugs of pmea and its analogues - Google Patents

Novel phosphonic acid based prodrugs of pmea and its analogues

Info

Publication number
TWI347325B
TWI347325B TW092132408A TW92132408A TWI347325B TW I347325 B TWI347325 B TW I347325B TW 092132408 A TW092132408 A TW 092132408A TW 92132408 A TW92132408 A TW 92132408A TW I347325 B TWI347325 B TW I347325B
Authority
TW
Taiwan
Prior art keywords
pmea
analogues
phosphonic acid
acid based
based prodrugs
Prior art date
Application number
TW092132408A
Other languages
English (en)
Chinese (zh)
Other versions
TW200426152A (en
Inventor
K Raja Reddy
Mark D Erion
Michael C Matelich
Joseph J Kopcho
Original Assignee
Metabasis Therapeutics 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 Metabasis Therapeutics Inc filed Critical Metabasis Therapeutics Inc
Publication of TW200426152A publication Critical patent/TW200426152A/zh
Application granted granted Critical
Publication of TWI347325B publication Critical patent/TWI347325B/zh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574Esters of oxyacids of phosphorus
    • C07F9/65742Esters of oxyacids of phosphorus non-condensed with carbocyclic rings or heterocyclic rings or ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • C07F9/65616Heterocyclic 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

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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW092132408A 2002-05-13 2003-11-18 Novel phosphonic acid based prodrugs of pmea and its analogues TWI347325B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38054502P 2002-05-13 2002-05-13
PCT/US2003/014821 WO2004037161A2 (en) 2002-05-13 2003-05-12 Cyclic prodrugs of pmea one of its analogues

Publications (2)

Publication Number Publication Date
TW200426152A TW200426152A (en) 2004-12-01
TWI347325B true TWI347325B (en) 2011-08-21

Family

ID=32176361

Family Applications (1)

Application Number Title Priority Date Filing Date
TW092132408A TWI347325B (en) 2002-05-13 2003-11-18 Novel phosphonic acid based prodrugs of pmea and its analogues

Country Status (9)

Country Link
US (1) US7214668B2 (https=)
EP (2) EP2223927B1 (https=)
JP (1) JP4476811B2 (https=)
AU (1) AU2003299492B2 (https=)
CA (1) CA2485702C (https=)
IL (2) IL164809A0 (https=)
NZ (1) NZ536328A (https=)
TW (1) TWI347325B (https=)
WO (1) WO2004037161A2 (https=)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6312662B1 (en) 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
EP2223927B1 (en) 2002-05-13 2014-10-15 Metabasis Therapeutics, Inc. Salts of a phosphonic acid based prodrug of PMEA
WO2003095665A2 (en) * 2002-05-13 2003-11-20 Metabasis Therapeutics, Inc. Pmea and pmpa cyclic producing synthesis
BR0315795A (pt) 2002-10-31 2005-09-13 Metabasis Therapeutics Inc Pró-medicamentos de monofosfato de citarabina
US20070281911A1 (en) * 2004-01-21 2007-12-06 Gilead Sciences Inc. Use of Adefovir or Tenofovir for Inhibiting Mmtv-Like Viruses Involved in Breast Cancer and Primary Biliary Cirrhosis
US20050182252A1 (en) * 2004-02-13 2005-08-18 Reddy K. R. Novel 2'-C-methyl nucleoside derivatives
CA2565966A1 (en) * 2004-06-08 2005-12-29 Metabasis Therapeutics, Inc. Lewis acid mediated synthesis of cyclic esters
AU2005306612B2 (en) * 2004-11-15 2010-12-16 Ceptyr, Inc. Protein tyrosine phosphatase inhibitors and methods of use thereof
EP1907391A1 (en) * 2005-07-26 2008-04-09 Hetero Drugs Limited Novel process for acyclic phosphonate nucleotide analogs
US20070042501A1 (en) * 2005-08-20 2007-02-22 Institute Of Nuclear Energy Research A novel technology for the purity assay of TRODAT-1 raw material
SI2020996T1 (sl) * 2006-05-16 2012-03-30 Gilead Sciences Inc Postopek in sestavki za zdravljenje hematološkihmalignosti
CN101371841A (zh) * 2007-08-23 2009-02-25 浙江医药股份有限公司新昌制药厂 结晶型恩替卡韦制剂及其制备方法和应用
JP2009196959A (ja) * 2008-02-25 2009-09-03 Yamaguchi Univ がん治療用医薬組成物
CN101475594B (zh) * 2009-02-06 2012-05-30 廖国超 肝靶向抗病毒前体药物环状磷酸酯及其应用
CN101659676B (zh) * 2009-09-07 2012-06-20 徐奎 一种硫代阿德福韦、替诺福韦肝靶向酯前体药物
US8940313B2 (en) 2010-04-23 2015-01-27 University Of Southern California Tyrosine-based prodrugs of antiviral agents
US8884027B2 (en) 2010-10-22 2014-11-11 University Of Rochester Melampomagnolide B derivatives as antileukemic and cytotoxic agents
CN103221037A (zh) * 2010-11-12 2013-07-24 葛兰素惠尔康制造业私人有限公司 新药物组合物
WO2012079035A1 (en) 2010-12-10 2012-06-14 Sigmapharm Laboratories, Llc Highly stable compositions of orally active nucleotide analogues or orally active nucleotide analogue prodrugs
US9550803B2 (en) 2011-05-06 2017-01-24 University Of Southern California Method to improve antiviral activity of nucleotide analogue drugs
EP3578563B1 (en) 2011-12-22 2021-04-14 Geron Corporation Guanine analogs as telomerase substrates and telomere length affectors
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
CN103333209B (zh) * 2013-07-05 2015-09-30 西安新通药物研究有限公司 替诺福韦前药(hts)新晶体
CN104710477A (zh) * 2013-12-16 2015-06-17 安徽贝克联合制药有限公司 替诺福韦环膦酸酯化合物及其药学上可接受的盐和其制备方法及应用
AU2015217221A1 (en) 2014-02-13 2016-08-11 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
DK3116511T3 (da) 2014-03-14 2020-11-23 Alltech Inc Sammensætninger af selenoorganiske forbindelser og fremgangsmåder til anvendelse deraf
CN106687118A (zh) 2014-07-02 2017-05-17 配体药物公司 前药化合物及其用途
WO2017048252A1 (en) 2015-09-15 2017-03-23 Alltech, Inc. Compositions of selenoorganic compounds and methods of use thereof
WO2017220028A1 (zh) 2016-06-24 2017-12-28 浙江柏拉阿图医药科技有限公司 肝递送抗病毒前体药物核苷环磷酸酯化合物及应用
CN107540710B (zh) * 2016-06-24 2020-10-16 浙江柏拉阿图医药科技有限公司 肝递送抗病毒前体药物核苷环磷酸酯化合物及应用
CA3087932A1 (en) 2018-01-09 2019-07-18 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof
CN108863797B (zh) * 2018-07-02 2021-01-15 吉首大学 一类3-(取代/非取代苯基)-3-羟基丙酰氧肟酸的制备方法
CN116178440B (zh) * 2022-12-23 2025-12-30 杏林中医药科技(广州)有限公司 一种肝脏靶向烷化剂及其应用

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL222157A (https=) 1956-12-20
CS233665B1 (en) 1983-01-06 1985-03-14 Antonin Holy Processing of isomere o-phosphonylmethylderivative of anantiomere racemic vicinal diene
US4579849A (en) 1984-04-06 1986-04-01 Merck & Co., Inc. N-alkylguanine acyclonucleosides as antiviral agents
FR2562543B1 (fr) 1984-04-10 1987-09-25 Elf Aquitaine Nouveaux phosphonites cycliques, leur preparation et applications
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.
CS263952B1 (en) 1985-04-25 1989-05-12 Holy Antonin Remedy with antiviral effect
CS263951B1 (en) 1985-04-25 1989-05-12 Antonin Holy 9-(phosponylmethoxyalkyl)adenines and method of their preparation
CS264222B1 (en) 1986-07-18 1989-06-13 Holy Antonin N-phosphonylmethoxyalkylderivatives of bases of pytimidine and purine and method of use them
EP0338372A3 (en) 1988-04-22 1991-10-09 American Cyanamid Company Solubilized pro-drugs
CA1334752C (en) 1988-08-02 1995-03-14 Ryozo Sakoda Drug effect-enhancing agent for antitumor drug
US5658889A (en) 1989-01-24 1997-08-19 Gensia Pharmaceuticals, Inc. Method and compounds for aica riboside delivery and for lowering blood glucose
CS387190A3 (en) 1990-08-06 1992-03-18 Ustav Organicke Chemie A Bioch (2r)-2-/di(2-propyl)phosphonylmethoxy/-3-p-toluenesulfonyloxy -1- trimethylacetoxypropane and process for preparing thereof
EP0481214B1 (en) 1990-09-14 1998-06-24 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
US5157027A (en) 1991-05-13 1992-10-20 E. R. Squibb & Sons, Inc. Bisphosphonate squalene synthetase inhibitors and method
GB9205917D0 (en) 1992-03-18 1992-04-29 Smithkline Beecham Plc Pharmaceuticals
US5514798A (en) 1993-06-02 1996-05-07 Gilead Sciences, Inc. Method and cyclic carbonates for nucleotide analogues
ATE199906T1 (de) 1993-06-29 2001-04-15 Mitsubishi Chem Corp Phosphonat-nukleotid ester-derivate
EP0719273B1 (en) 1993-09-17 2010-11-03 Gilead Sciences, Inc. Nucleotide analogs
US5567592A (en) 1994-02-02 1996-10-22 Regents Of The University Of California Screening method for the identification of bioenhancers through the inhibition of P-glycoprotein transport in the gut of a mammal
DE69520360T2 (de) 1994-07-04 2001-08-09 Takeda Chemical Industries, Ltd. Phosphonsäure verbindungen imre herstellung und verwendung
DE4445829A1 (de) 1994-12-22 1996-06-27 Leybold Ag Gegenstrom-Schnüffellecksucher
US5665386A (en) 1995-06-07 1997-09-09 Avmax, Inc. Use of essential oils to increase bioavailability of oral pharmaceutical compounds
US5716928A (en) 1995-06-07 1998-02-10 Avmax, Inc. Use of essential oils to increase bioavailability of oral pharmaceutical compounds
ATE253920T1 (de) 1995-07-17 2003-11-15 Cephalon Inc Phosphor enthaltende hemmer von cystein- und serin-proteasen
US5962440A (en) 1996-05-09 1999-10-05 Bristol-Myers Squibb Company Cyclic phosphonate ester inhibitors of microsomal triglyceride transfer protein and method
US6054587A (en) 1997-03-07 2000-04-25 Metabasis Therapeutics, Inc. Indole and azaindole inhibitors of fructose-1,6-bisphosphatase
US6284748B1 (en) 1997-03-07 2001-09-04 Metabasis Therapeutics, Inc. Purine inhibitors of fructose 1,6-bisphosphatase
DE69819311T2 (de) 1997-03-07 2004-07-29 Metabasis Therapeutics Inc., San Diego Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase
TR200000224T2 (tr) 1997-07-25 2000-07-21 Gilead Sciences, Inc. Nükleotid analog kompozisyonlar.
US5962522A (en) 1997-09-05 1999-10-05 Avmax, Inc. Propyl gallate to increase bioavailability of orally administered pharmaceutical compounds
US6180666B1 (en) 1997-09-05 2001-01-30 Anmax, Inc. Use of gallic acid esters to increase bioavailability of orally administered pharmaceutical compounds
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
KR100818845B1 (ko) 1998-09-09 2008-04-01 메타베이시스 테라퓨틱스, 인크. 신규한 프럭토스 1,6-비스포스파타제의 헤테로방향족 억제제
PL352756A1 (en) 1998-12-24 2003-09-08 Metabasis Therapeutics, Inc. A combination of fbpase inhibitors and insulin sensitizers for the treatment of diabetes
MXPA01008937A (es) 1999-03-05 2004-04-05 Metabasis Therapeutics Inc Nuevos profarmacos que contienen fosforo.
AU7361400A (en) * 1999-09-08 2001-04-10 Metabasis Therapeutics, Inc. Prodrugs for liver specific drug delivery
US20020119443A1 (en) 2000-07-21 2002-08-29 Gilead Sciences, Inc. Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
WO2003095665A2 (en) * 2002-05-13 2003-11-20 Metabasis Therapeutics, Inc. Pmea and pmpa cyclic producing synthesis
EP2223927B1 (en) 2002-05-13 2014-10-15 Metabasis Therapeutics, Inc. Salts of a phosphonic acid based prodrug of PMEA
BR0315795A (pt) 2002-10-31 2005-09-13 Metabasis Therapeutics Inc Pró-medicamentos de monofosfato de citarabina
ATE478082T1 (de) * 2003-12-30 2010-09-15 Gilead Sciences Inc Phosphonate, monophosphonamidate, bisphosphonamidate zur behandlung von virenerkrankungen
CA2565966A1 (en) * 2004-06-08 2005-12-29 Metabasis Therapeutics, Inc. Lewis acid mediated synthesis of cyclic esters

Also Published As

Publication number Publication date
WO2004037161A2 (en) 2004-05-06
IL164809A0 (en) 2005-12-18
JP4476811B2 (ja) 2010-06-09
TW200426152A (en) 2004-12-01
EP2223927A2 (en) 2010-09-01
EP2223927A3 (en) 2010-09-15
EP1532157A4 (en) 2009-02-25
WO2004037161A3 (en) 2005-03-31
AU2003299492A1 (en) 2004-05-13
CA2485702C (en) 2011-07-19
AU2003299492B2 (en) 2010-06-10
EP1532157A2 (en) 2005-05-25
JP2006511490A (ja) 2006-04-06
IL164809A (en) 2012-08-30
NZ536328A (en) 2007-11-30
US7214668B2 (en) 2007-05-08
EP2223927B1 (en) 2014-10-15
US20030229225A1 (en) 2003-12-11
CA2485702A1 (en) 2004-05-06

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