WO2000052015A3 - Novel phosphorus-containing prodrugs - Google Patents

Novel phosphorus-containing prodrugs Download PDF

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Publication number
WO2000052015A3
WO2000052015A3 PCT/US2000/005672 US0005672W WO0052015A3 WO 2000052015 A3 WO2000052015 A3 WO 2000052015A3 US 0005672 W US0005672 W US 0005672W WO 0052015 A3 WO0052015 A3 WO 0052015A3
Authority
WO
WIPO (PCT)
Prior art keywords
containing prodrugs
novel phosphorus
drugs
novel
phosphorus
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.)
Ceased
Application number
PCT/US2000/005672
Other languages
French (fr)
Other versions
WO2000052015A2 (en
Inventor
Mark D Erion
K Raja Reddy
Serge H Boyer
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.)
Metabasis Therapeutics Inc
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
Priority to EP00917729A priority Critical patent/EP1165570B9/en
Priority to AU38658/00A priority patent/AU775332B2/en
Priority to SK1244-2001A priority patent/SK12442001A3/en
Priority to HK02104972.2A priority patent/HK1043796B/en
Priority to CA002362805A priority patent/CA2362805A1/en
Priority to MXPA01008937A priority patent/MXPA01008937A/en
Priority to JP2000602240A priority patent/JP5063837B2/en
Priority to IL14505200A priority patent/IL145052A0/en
Application filed by Metabasis Therapeutics Inc filed Critical Metabasis Therapeutics Inc
Priority to DE60030263T priority patent/DE60030263T2/en
Publication of WO2000052015A2 publication Critical patent/WO2000052015A2/en
Publication of WO2000052015A3 publication Critical patent/WO2000052015A3/en
Priority to IL145052A priority patent/IL145052A/en
Anticipated expiration legal-status Critical
Priority to CY20061101686T priority patent/CY1105799T1/en
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • C07F9/6564—Heterocyclic 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
    • C07F9/6581—Heterocyclic 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 nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic 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 nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65842—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
    • C07F9/65846—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a six-membered ring which may be condensed with another ring system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07F9/6564—Heterocyclic 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
    • C07F9/6581—Heterocyclic 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 nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic 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 nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65848—Cyclic amide derivatives of acids of phosphorus, in which two nitrogen atoms belong to the ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)

Abstract

Novel cyclic phosphoramidate prodrugs of drugs of formula (I) of parent drugs MH their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.
PCT/US2000/005672 1999-03-05 2000-03-03 Novel phosphorus-containing prodrugs Ceased WO2000052015A2 (en)

Priority Applications (11)

Application Number Priority Date Filing Date Title
JP2000602240A JP5063837B2 (en) 1999-03-05 2000-03-03 New phosphorus-containing prodrug
SK1244-2001A SK12442001A3 (en) 1999-03-05 2000-03-03 Cyclic phosphoramidates, method for preparing thereof and pharmaceutical compositions containing the same
HK02104972.2A HK1043796B (en) 1999-03-05 2000-03-03 Novel phosphorus-containing prodrugs
CA002362805A CA2362805A1 (en) 1999-03-05 2000-03-03 Novel phosphorus-containing prodrugs
MXPA01008937A MXPA01008937A (en) 1999-03-05 2000-03-03 Novel phosphorus-containing prodrugs.
IL14505200A IL145052A0 (en) 1999-03-05 2000-03-03 Novel phosphorus-containing prodrugs
DE60030263T DE60030263T2 (en) 1999-03-05 2000-03-03 NEW PHOSPHORE-CONTAINING MEDICATION PROCESSING COMPOUNDS
EP00917729A EP1165570B9 (en) 1999-03-05 2000-03-03 Novel phosphorus-containing prodrugs
AU38658/00A AU775332B2 (en) 1999-03-05 2000-03-03 Novel phosphorus-containing prodrugs
IL145052A IL145052A (en) 1999-03-05 2001-08-22 Phosphorus-containing prodrugs
CY20061101686T CY1105799T1 (en) 1999-03-05 2006-11-20 NEW PHOSPHORUS FIXING PRODRUGS

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US12301399P 1999-03-05 1999-03-05
US60/123,013 1999-03-05
US15312799P 1999-09-08 1999-09-08
US60/153,127 1999-09-08

Publications (2)

Publication Number Publication Date
WO2000052015A2 WO2000052015A2 (en) 2000-09-08
WO2000052015A3 true WO2000052015A3 (en) 2001-02-15

Family

ID=26821130

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/005672 Ceased WO2000052015A2 (en) 1999-03-05 2000-03-03 Novel phosphorus-containing prodrugs

Country Status (19)

Country Link
EP (2) EP1724276A1 (en)
JP (1) JP5063837B2 (en)
CN (1) CN1321999C (en)
AT (1) ATE337324T1 (en)
AU (1) AU775332B2 (en)
CA (1) CA2362805A1 (en)
CY (1) CY1105799T1 (en)
CZ (1) CZ20013180A3 (en)
DE (1) DE60030263T2 (en)
DK (1) DK1165570T3 (en)
ES (1) ES2272268T3 (en)
HK (1) HK1043796B (en)
HU (1) HUP0200260A3 (en)
IL (2) IL145052A0 (en)
MX (1) MXPA01008937A (en)
NZ (1) NZ513728A (en)
PT (1) PT1165570E (en)
SK (1) SK12442001A3 (en)
WO (1) WO2000052015A2 (en)

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US7138376B2 (en) 2001-09-28 2006-11-21 Idenix Pharmaceuticals, Inc. Methods and compositions for treating hepatitis C virus using 4'-modified nucleosides
US7192936B2 (en) 2002-06-28 2007-03-20 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
US7300924B2 (en) 2003-04-25 2007-11-27 Gilead Sciences, Inc. Anti-infective phosphonate analogs
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
US7417055B2 (en) 2003-04-25 2008-08-26 Gilead Sciences, Inc. Kinase inhibitory phosphonate analogs
US7427624B2 (en) 2003-10-24 2008-09-23 Gilead Sciences, Inc. Purine nucleoside phosphorylase inhibitory phosphonate compounds
US7427636B2 (en) 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
US7429565B2 (en) 2003-04-25 2008-09-30 Gilead Sciences, Inc. Antiviral phosphonate analogs
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
US7432272B2 (en) 2003-12-22 2008-10-07 Gilead Sciences, Inc. Antiviral analogs
US7432273B2 (en) 2003-10-24 2008-10-07 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US7456155B2 (en) 2002-06-28 2008-11-25 Idenix Pharmaceuticals, Inc. 2′-C-methyl-3′-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
US7470724B2 (en) 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7582618B2 (en) 2002-06-28 2009-09-01 Idenix Pharmaceuticals, Inc. 2′-C-methyl-3′-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
US7598373B2 (en) 2002-12-12 2009-10-06 Idenix Pharmaceuticals, Inc. Process for the production of 2-C-methyl-D-ribonolactone
US7608597B2 (en) 2000-05-23 2009-10-27 Idenix Pharmaceuticals, Inc. Methods and compositions for treating hepatitis C virus
US7645747B2 (en) 2003-04-25 2010-01-12 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US8329914B2 (en) 2008-10-31 2012-12-11 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8410284B2 (en) 2008-10-22 2013-04-02 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8563746B2 (en) 2008-10-29 2013-10-22 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8951986B2 (en) 2008-07-08 2015-02-10 Gilead Sciences, Inc. Salts of HIV inhibitor compounds
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US7456155B2 (en) 2002-06-28 2008-11-25 Idenix Pharmaceuticals, Inc. 2′-C-methyl-3′-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
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