Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are of Formula AI or 1001 or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof.
Provided herein are hepatitis C virus inhibitor compounds, for example, of any of Formulae I to XIV, Ilia to XlVa, Illb to XlVb, IIIc to XIVc, Hid to XlVd, Ille to XlVe, IA to IAe, IIA to IIAe, IB, IIB to IIBd, IIIB to IIIBd, IC to ICc, ID to IDd, and IE to lEc.pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for treating an HCV infection.
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
UNIVERSITE DE MONTPELLIER (France)
Inventor
Dukhan, David
Gosselin, Gilles
Dousson, Cyril B.
Abstract
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 1',4'-thio nucleoside compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula 3001: (3001); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof; wherein Base, RA, RB, W, X, Y, and Z are as described herein.
C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
Provided herein are compounds, methods and pharmaceutical compositions for use in treatment of viral infections, including hepatitis C virus (HCV) infections, in hosts in need thereof. In certain embodiments, the compounds are 2',4'-fluoro nucleosides according to Formula 1001: (1001); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, RA, and PD are as described herein. In certain embodiments, 2',4'-fluoro nucleosides are provided which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human.
A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
UNIVERSITE DE MONTPELLIER (France)
Inventor
Dukhan, David
Parsy, Christophe Claude
Gosselin, Gilles
Griffon, Jean-François
Brandt, Guillaume
Dousson, Cyril B.
Moussa, Adel M.
Mayes, Benjamin Alexander
Stewart, Alistair James
Abstract
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2'-cyano, azido or amino nucleosides according to or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, W, R1, R2, R10, and R11 are as described herein.
Provided herein are compounds, compositions, and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, the compounds are according to Formula 2001; where PD, Base, RA and RB are as provided herein. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
UNIVERSITE DE MONTPELLIER (France)
Inventor
Stewart, Alistair James
Moussa, Adel M.
Mayes, Benjamin Alexander
Alexandre, Francois-Rene
Surleraux, Dominique
Parsy, Christophe Claude
Pierra, Claire
Dukhan, David
Gosselin, Gilles
Abstract
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3'- deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Base1 and Base2 are as provided herein.
C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
UNIVERSITE DE MONTPELLIER (France)
Inventor
Mayes, Benjamin Alexander
Moussa, Adel M.
Stewart, Alistair James
Gosselin, Gilles
Abstract
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are according to Formula (1501): or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, PD, RA, RB, RC, L, M and Z are as described herein.
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, provided herein is an isolated compound according to Formula 1a: or a pharmaceutically acceptable salt or solvate thereof.
A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, provided herein is an isolated compound according to Formula Ib: or a pharmaceutically acceptable salt or solvate thereof.
A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2',4'-bridged nucleosides which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the 2',4'-bridged nucleosides are of Formula 3001:(I) (3001); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, where PD, B, W, X, RA, RB, RC and RD are as described herein.
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds comprise two 2 '-methyl nucleotides linked according to Formula (I): N1 - L - N2 or a pharmaceutically acceptable salt, ester, solvate, stereoisomer, isomeric form, tautomeric form or polymorphic form thereof; wherein N1, L and N2 are as described herein.
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
UNIVERSITÉ MONTPELLIER 2 SCIENCES ET TECHNIQUES (France)
Inventor
Gosselin, Gilles
Parsy, Christophe Claude
Alexandre, Francois-Rene
Rahali, Houcine
Griffon, Jean-François
Surleraux, Dominique
Dousson, Cyril B.
Pierra, Claire
Moussa, Adel M.
Mayes, Benjamin Alexander
Stewart, Alistair James
Dukhan, David
Abstract
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2'-chloro nucleosides according to Formula 2001: (2001); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.
C07H 19/00 - Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radicalNucleosidesMononucleotidesAnhydro derivatives thereof
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, provided herein are compounds according to Formula 1001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein Base, Y, Z, A, RC and RD are as described herein.
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
Provided herein are methods of administering a 5,5-fused heteroarylene hepatitis C virus inhibitor compound or an isotopic variant thereof, or a pharmaceutically acceptable salt or solvate thereof; for treating or preventing hepatitis C virus infection in a subject.
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
16.
3',5'-CYCLIC PHOSPHORAMIDATE PRODRUGS FOR HCV INFECTION
Provided herein are compounds of formula (I) compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. Formula (I) or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein: each X is independently alkoxyl, hydrogen, or hydroxyl; each Y is independently hydroxyl, acetoxyl, or fluoro; each Z is independently substituted alkyl; and each R is independently hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, or heteroaryl.
C07H 19/11 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
UNIVERSITÉ MONTPELLIER 2 SCIENCES ET TECHNIQUES (France)
Inventor
Parsy, Christophe Claude
Alexandre, Francois-Rene
Dousson, Cyril B.
Dukhan, David
Gosselin, Gilles
Rahali, Houcine
Surleraux, Dominique
Abstract
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
Provided herein are compounds comprising a D-amino acid, compositions and methods for the treatment of liver disease and conditions, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
Provided herein are stable pharmaceutical compositions comprising 2'-C-methyl-guanosine, 5'-[2-[(3-hydroxy-2,2-dimethyl-l-oxopropyl) thio]ethyl N-(phenylmethyl)phosphoramidate (also known s IDX-184), and in particular, oral pharmaceutical compositions such as tablets. The compositions are designed to avoid the formation of diethylene sulfide upon storage. Discosed are also methods of using these pharmaceutical compositions in the treatment of viral infections, including hepatitis C virus infections in hosts in need thereof.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
22.
SUBSTITUTED CARBONYLOXYMETHYLPHOSPHORAMIDATE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
UNIVERSITÉ MONTPELLIER 2 SCIENCES ET TECHNIQUES ()
Inventor
Surleraux, Dominique
Dousson, Cyril B.
Gosselin, Gilles
Dukhan, David
Pierra, Claire
Peyronnet, Jerome
Abstract
Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
Inventor
Surleraux, Dominique
Gosselin, Gilles
Abstract
Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti- viral agents.
C07H 19/167 - Purine radicals with ribosyl as the saccharide radical
C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
Provided herein are methods for treating or preventing drug-resistant hepatitis C virus infection in a subject, which comprises administering to the subject a 5,5-fused heteroarylene hepatitis C virus inhibitor compound, for example, of Formula I, IA, or IB.
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
A61K 31/424 - Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
A61K 31/4706 - 4-Aminoquinolines8-Aminoquinolines, e.g. chloroquine, primaquine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
Inventor
Surleraux, Dominique
Gosselin, Gilles
Abstract
Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
Centre National de la Recherche Scientifique (France)
Inventor
Surleraux, Dominique
Gosselin, Gilles
Abstract
Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof. Formula (I), (IA), (IB).
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula (Ia) or (Ib), pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, HA, IIIA, IVA, VA, VIA, VIIA, IB, HB, IIIB, IVB, VB, VIB and VIIB disclosed herein, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host infected with HCV.
C07F 9/6553 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
Provided herein are ruthenium complexes of Formula (I), and processes of preparation thereof. Also provided are methods of their use as a metathesis catalyst.
Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti- viral agents.
C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
Provided herein are pharmaceutical compositions of a phosphoindole compound that can have advantageous release properties. The pharmaceutical compositions can comprise a phosphoindole compound and one or more polyglycolyzed glycerides. The pharmaceutical compositions can be useful for inhibiting viral replication. The pharmaceutical compositions provided herein can also be useful, for example, for the treatment of viral infection such as human immunodeficiency virus infection.
Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, provided herein are solid forms comprising (2-carbamoyl-5-chloro-1H-indol-3-yl)-[3-((E)-2-cyano-vinyl)-5-methyl-phenyl]-(R)-phosphinic acid methyl ester, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, human immunodeficiency virus infection.
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula (I), pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formulas V, V', I', II', or Va, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
C07F 9/6584 - 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
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formula I, II, III, I', II', I', II', Ia, IIa, or IIIa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
C07F 9/6584 - 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
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Provided herein are phosphadiazine polymerase inhibitor, for example, of Formula (III), pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
C07F 9/6584 - 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
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formulas (IV), (IV), (I'), (II'), or (IVa), pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
C07F 9/6584 - 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
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
C07D 255/04 - Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups condensed with carbocyclic rings or ring systems
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
L'UNIVERSITE MONTPELLIER II (France)
Inventor
Sommadossi, Jean-Pierre
Gosselin, Gilles
Pierra, Claire
Perigaud, Christian
Peyrottes, Suzanne
Abstract
Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
L'UNIVERSITE MONTPELLIER II (France)
Inventor
Sommadossi, Jean-Pierre
Gosselin, Gilles
Pierra, Claire
Perigaud, Christian
Peyrottes, Suzanne
Abstract
Provided herein are compounds, compositions and methods for the treatment of liver disorders, including liver cancer and metabolic diseases, such as diabetes, hyperlipidemia, atherosclerosis, and obesity. Specifically, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-cancer agents.
3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HLV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other antiviral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds. The 3-phosphoindole compounds are of the formula (A) or (B) and the pharmaceutically acceptable salts, solvates, hydrates, or esters thereof. In the formulae X is hydrogen; aryl or heterocyclyl; C2-6 alkenyl, C2-6 alkynyl or alkyl; Y is hydrogen, -R, -O-R, -NH-R, or -NRR; Z is -OR, -NHR, -NRR, carboxamido, arnido, carboxyl, carbonyl, or an amino acid residue; R1 is hydrogen, acyl, -S(O)n-R, carboxyl, carbonyl, or an amino acid residue; each R4', R5', R6' and R7' is independently hydrogen, C2-6 alkenyl, C2-6 alkynyl, aryl, heterocyclyl, halogen, -CN, -CF3, -OR, -NHR, -NRR, or -NO2; n is 0, 1, or 2; and each R is independently hydrogen, alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, or heterocyclyl.
A process is provided for the preparation of a key intermediate in the preparation of 2'-branched nucleoside compounds. The process includes contacting a protected precursor 3,4-O-isopropylidene-2-C-substituted-D-arabinono-l,5-lactone with a fluorinating agent under anhydrous conditions and converting the precursor into a protected 2-deoxy-2-halo-2-C-disubstituted ribono-l,5-lactone and optionally into a 2- deoxy-2-halo-2-C-disubstituted ribono- 1 ,4-lactone.
A01N 43/08 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom five-membered rings with oxygen as the ring hetero atom
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A01N 43/00 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (France)
Inventor
Storer, Richard
Gosselin, Gilles
Dukhan, David
Leroy, Frederic
Meillon, Jean-Christophe
Converd, Thierry
Abstract
The present invention provides nucleoside analogue Compounds that treat a host infected with a Flaviviridae virus infection, or other viruses that exhibit RNA- dependent RNA viral replication, compositions comprising' these Compounds and methods of using the Compounds for the treatment and/or Prophylaxis of viral infection, especially hepatitis C, in an infected host.
C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 473/40 - Heterocyclic compounds containing purine ring systems with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
THE CHANCELLORS, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD (United Kingdom)
IDENIX PHARMACEUTICALS, INC. (USA)
NOVARTIS AG (Switzerland)
Inventor
Hotchkiss, David
Fleet, George
Heinz, Thomas
Storer, Richard
Abstract
An improved process for preparing a saccharinic acid or lactone is disclosed that utilizes the well-known Amadori rearrangement reaction. The synthesis utilizes protected or unprotected sugars or their analogues as starting materials, and reagents not previously utilized to afford increased product yields in decreased reaction time.
patents
