[go: up one dir, main page]

WO1999010365A3 - 5',5'-linked oligomers having anti-thrombin activity - Google Patents

5',5'-linked oligomers having anti-thrombin activity Download PDF

Info

Publication number
WO1999010365A3
WO1999010365A3 PCT/US1998/017913 US9817913W WO9910365A3 WO 1999010365 A3 WO1999010365 A3 WO 1999010365A3 US 9817913 W US9817913 W US 9817913W WO 9910365 A3 WO9910365 A3 WO 9910365A3
Authority
WO
WIPO (PCT)
Prior art keywords
thrombin activity
thrombin
compounds
linked oligomers
oligomers
Prior art date
Application number
PCT/US1998/017913
Other languages
French (fr)
Other versions
WO1999010365A2 (en
Inventor
Norbert W Bischofberger
Chris A Buhr
Joseph P Dougherty
Brian C Froehler
Arnold J Gutierrez
Gong-Xin He
Regan G Shea
Sundaramoorthi Swaminathan
Matthew A Williams
Original Assignee
Gilead Sciences Inc
Norbert W Bischofberger
Chris A Buhr
Joseph P Dougherty
Brian C Froehler
Arnold J Gutierrez
He Gong Xin
Regan G Shea
Sundaramoorthi Swaminathan
Matthew A Williams
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 Gilead Sciences Inc, Norbert W Bischofberger, Chris A Buhr, Joseph P Dougherty, Brian C Froehler, Arnold J Gutierrez, He Gong Xin, Regan G Shea, Sundaramoorthi Swaminathan, Matthew A Williams filed Critical Gilead Sciences Inc
Priority to AU92104/98A priority Critical patent/AU9210498A/en
Publication of WO1999010365A2 publication Critical patent/WO1999010365A2/en
Publication of WO1999010365A3 publication Critical patent/WO1999010365A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • 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
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/56—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving blood clotting factors, e.g. involving thrombin, thromboplastin, fibrinogen

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Microbiology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Novel compounds are described. The compounds generally comprise two oligomers (5'-GGTTGG-3') are linked in a 5',5' manner via a synthetic linking moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting thrombin in samples suspected of containing thrombin are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting thrombin activity are also described.
PCT/US1998/017913 1997-08-29 1998-08-28 5',5'-linked oligomers having anti-thrombin activity WO1999010365A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU92104/98A AU9210498A (en) 1997-08-29 1998-08-28 5',5'-linked oligomers having anti-thrombin activity

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5736497P 1997-08-29 1997-08-29
US60/057,364 1997-08-29

Publications (2)

Publication Number Publication Date
WO1999010365A2 WO1999010365A2 (en) 1999-03-04
WO1999010365A3 true WO1999010365A3 (en) 1999-05-14

Family

ID=22010124

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1998/017913 WO1999010365A2 (en) 1997-08-29 1998-08-28 5',5'-linked oligomers having anti-thrombin activity

Country Status (2)

Country Link
AU (1) AU9210498A (en)
WO (1) WO1999010365A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9394330B2 (en) 2012-03-21 2016-07-19 Alios Biopharma, Inc. Solid forms of a thiophosphoramidate nucleotide prodrug

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2013003153A (en) 2010-09-22 2013-05-01 Alios Biopharma Inc Substituted nucleotide analogs.
WO2013096680A1 (en) 2011-12-22 2013-06-27 Alios Biopharma, Inc. Substituted phosphorothioate nucleotide analogs
EP2827876A4 (en) 2012-03-22 2015-10-28 Alios Biopharma Inc Pharmaceutical combinations comprising a thionucleotide analog

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992014843A1 (en) * 1991-02-21 1992-09-03 Gilead Sciences, Inc. Aptamer specific for biomolecules and method of making

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992014843A1 (en) * 1991-02-21 1992-09-03 Gilead Sciences, Inc. Aptamer specific for biomolecules and method of making

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CUSHLEY, ROBERT J. ET AL: "Nucleosides. LIII. Transformation of pyrimidine nucleosides in alkaline media. 2. Reactions of 5-fluorouracil derivatives with sodium deuteroxide", TETRAHEDRON LETT. (1968), (52), 5393-6, XP002095456 *
GROMOVA, M. ET AL: "The direct effect of heavy ions and electrons on thymidine in the solid state", INT. J. RADIAT. BIOL. (1998), 74(1), 81-97, XP002095454 *
GUPTA, V. S. ET AL: "Synthesis and cell culture studies on the antiviral activity of 5-mercaptomethyl-2'-deoxyuridine", J. MED. CHEM. (1975), 18(10), 973-6, XP002095455 *
SHAW, ANTHONY A. ET AL: "Radical combination processes under the direct effects of gamma radiation on thymidine", J. CHEM. SOC., PERKIN TRANS. 2 (1990), (12), 2063-70, XP002095453 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9394330B2 (en) 2012-03-21 2016-07-19 Alios Biopharma, Inc. Solid forms of a thiophosphoramidate nucleotide prodrug

Also Published As

Publication number Publication date
WO1999010365A2 (en) 1999-03-04
AU9210498A (en) 1999-03-16

Similar Documents

Publication Publication Date Title
PL322000A1 (en) Novel selective inhibitors of viral or bacterial neuramidazes
EP0980524A4 (en) DETECTION OF MOLECULAR INTERACTIONS BY COMPLEMENTATION OF MARKING SUB-UNITS
CA2256545A1 (en) Probe for analysis of nucleic acids
WO1999041273A3 (en) Pna and dna conjugates and methods for preparation thereof
BR9910207A (en) Monomeric, oligomeric and polymeric knoevenagel condensation products
NO990518D0 (en) Long-acting drugs and pharmaceutical compositions comprising them
BR9812649A (en) Compounds containing six-membered rings, process for their preparation, and their use as medicines
CA2309556A1 (en) Detection systems for registering protein interactions and functional relationships
AU8347391A (en) Simultaneous assay for detecting one or more analytes
PL351917A1 (en) Pharmaceutical preparation containing low molecular mass thrombin inhibitor and its agonist
WO1999010365A3 (en) 5',5'-linked oligomers having anti-thrombin activity
IL98769A (en) Synthetic peptides, mixtures thereof, methods utilizing the same for detecting hiv antibodies and pharmaceutical compositions containing the same
EP1118622A4 (en) NOVEL ANTIBODIES, MEDICAMENTS CONTAINING THEM, AND METHODS FOR SCREENING FOR COMPOUNDS USING THE SAME
EP1182458A4 (en) METHOD OF DETECTING PROTEINS WITH MUTUAL INTERACTION
EP0749320A4 (en) SPECIFIC FIBRIN ANTIBODIES AS AN ANTITHROMBOSIS AGENT
EP0976734A3 (en) Selective inhibitors of viral or bacterial neuraminidase
BR9910454A (en) Effervescent preparations
WO2002050715A3 (en) Default address matching system
AU5971598A (en) Novel antibody, renin-active substance containing the same and prorenin assay reagent using the same
WO2000077518A3 (en) Methods and compositions for opsonophagocytic assays
FR2720611B1 (en) Device for presenting articles.
AU652474C (en) Assay methods and compositions for detecting serum proteases, particularly activated protein C
FR2754799B1 (en) DEVICE FOR CONVEYING OBJECTS SUCH AS, IN PARTICULAR, BOTTLES, VIALS OR THE LIKE
AU6856798A (en) Device for inspecting, sorting and/or dosing of chaotically arranged objects
CA2559998A1 (en) Rapamycin conjugates and antibodies

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GE GH GM HR HU ID IL IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW SD SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

AK Designated states

Kind code of ref document: A3

Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GE GH GM HR HU ID IL IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW SD SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
NENP Non-entry into the national phase

Ref country code: KR

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: CA