CA2871471C - Dna-pk inhibitors - Google Patents

Dna-pk inhibitors Download PDF

Info

Publication number
CA2871471C
CA2871471C CA2871471A CA2871471A CA2871471C CA 2871471 C CA2871471 C CA 2871471C CA 2871471 A CA2871471 A CA 2871471A CA 2871471 A CA2871471 A CA 2871471A CA 2871471 C CA2871471 C CA 2871471C
Authority
CA
Canada
Prior art keywords
inhibitors
dna
compounds
compositions
disorders
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.)
Active
Application number
CA2871471A
Other languages
English (en)
French (fr)
Other versions
CA2871471A1 (en
Inventor
Huai Gao
Paul S. Charifson
Kevin Michael Cottrell
Hongbo Deng
John P. Duffy
Simon Giroux
Jeremy Green
Katrina Lee Jackson
John Patrick Maxwell
Mark A. Morris
Albert Charles Pierce
Nathan D. Waal
David J. Lauffer
Joseph M. Kennedy
Mark Willem Ledeboer
Pan Li
Jinwang Xu
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of CA2871471A1 publication Critical patent/CA2871471A1/en
Application granted granted Critical
Publication of CA2871471C publication Critical patent/CA2871471C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K41/00—Medicinal preparations obtained by treating materials with wave energy or particle radiation ; Therapies using these preparations
    • A61K41/0038—Radiosensitizing, i.e. administration of pharmaceutical agents that enhance the effect of radiotherapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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 C07D415/00
    • C07D417/02—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 C07D415/00 containing two hetero rings
    • C07D417/04—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 C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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 C07D415/00
    • C07D417/02—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 C07D415/00 containing two hetero rings
    • C07D417/10—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 C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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 C07D415/00
    • C07D417/14—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 C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D521/00—Heterocyclic compounds containing unspecified hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/09—Geometrical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CA2871471A 2012-04-24 2013-04-23 Dna-pk inhibitors Active CA2871471C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261637512P 2012-04-24 2012-04-24
US61/637,512 2012-04-24
US201261725652P 2012-11-13 2012-11-13
US61/725,652 2012-11-13
US201361777806P 2013-03-12 2013-03-12
US61/777,806 2013-03-12
PCT/US2013/037811 WO2013163190A1 (en) 2012-04-24 2013-04-23 Dna-pk inhibitors

Publications (2)

Publication Number Publication Date
CA2871471A1 CA2871471A1 (en) 2013-10-31
CA2871471C true CA2871471C (en) 2021-06-01

Family

ID=48225150

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2871471A Active CA2871471C (en) 2012-04-24 2013-04-23 Dna-pk inhibitors

Country Status (30)

Country Link
US (11) US9296701B2 (show.php)
EP (2) EP2841428B1 (show.php)
JP (3) JP6378171B2 (show.php)
KR (1) KR102089239B1 (show.php)
CN (3) CN106977495B (show.php)
AU (2) AU2013251804B2 (show.php)
BR (1) BR112014026703B1 (show.php)
CA (1) CA2871471C (show.php)
CL (1) CL2014002873A1 (show.php)
CY (2) CY1120866T1 (show.php)
DK (2) DK3459942T3 (show.php)
ES (2) ES2860299T3 (show.php)
HR (2) HRP20181862T1 (show.php)
HU (1) HUE054031T2 (show.php)
IL (2) IL235297A (show.php)
IN (1) IN2014KN02601A (show.php)
LT (2) LT3459942T (show.php)
MX (2) MX357261B (show.php)
NZ (2) NZ731797A (show.php)
PL (2) PL3459942T3 (show.php)
PT (2) PT3459942T (show.php)
RS (2) RS58043B1 (show.php)
RU (1) RU2638540C1 (show.php)
SG (2) SG11201406584TA (show.php)
SI (2) SI3459942T1 (show.php)
SM (2) SMT201800608T1 (show.php)
TR (1) TR201816379T4 (show.php)
UA (1) UA115983C2 (show.php)
WO (1) WO2013163190A1 (show.php)
ZA (1) ZA201407554B (show.php)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3330257T3 (pl) 2011-04-08 2020-06-15 Janssen Sciences Ireland Unlimited Company Pochodne pirymidyny do leczenia zakażeń wirusowych
MX347596B (es) 2011-11-09 2017-05-03 Janssen Sciences Ireland Uc Derivados de purina para el tratamiento de infecciones viricas.
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
HUE054031T2 (hu) 2012-04-24 2021-08-30 Vertex Pharma DNS-PK inhibitorok
JP6250046B2 (ja) 2012-07-13 2017-12-20 ヤンセン・サイエンシズ・アイルランド・ユーシー ウイルス感染症の処置のための大環状プリン
HUE037064T2 (hu) 2012-10-10 2018-08-28 Janssen Sciences Ireland Uc Pirrolo[3,2-d]-pirimidin származékok vírusos fertõzések és egyéb betegségek kezelésére
US9663474B2 (en) 2012-11-16 2017-05-30 Janssen Sciences Ireland Uc Heterocyclic substituted 2-amino quinazoline derivatives for the treatment of viral infections
CN105189468B (zh) 2013-02-21 2018-10-30 爱尔兰詹森科学公司 用于治疗病毒性感染的2-氨基嘧啶衍生物
RU2676259C2 (ru) 2013-03-12 2018-12-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы днк-пк
KR102280554B1 (ko) 2013-03-29 2021-07-22 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염증의 치료를 위한 거대환식 데아자-퓨리논
JP6377139B2 (ja) 2013-05-24 2018-08-22 ヤンセン・サイエンシズ・アイルランド・ユーシー ウイルス感染症およびさらなる疾患の処置のためのピリドン誘導体
NO3030563T3 (show.php) 2013-06-27 2018-01-06
WO2015014815A1 (en) 2013-07-30 2015-02-05 Janssen R&D Ireland THIENO[3,2-d]PYRIMIDINES DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS
DK3424920T3 (da) * 2013-10-17 2020-06-08 Vertex Pharma Co-krystaller af (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinolin-4-carboxamid og deuterede derivater deraf som dna-pk-inhibitorer
PL3057959T3 (pl) * 2013-10-17 2018-08-31 Vertex Pharmaceuticals Incorporated Inhibitory DNA-PK
AU2015292818B2 (en) 2014-07-21 2020-01-16 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
CN104352488B (zh) * 2014-10-31 2016-08-31 厦门大学 一类取代杂环衍生物在制备治疗疼痛药物中的应用
WO2016066115A1 (zh) * 2014-10-31 2016-05-06 厦门大学 取代杂环衍生物、其制备方法和用途
CN104356082B (zh) * 2014-10-31 2016-07-13 厦门大学 一类取代杂环衍生物及其制备方法
WO2017059702A1 (en) * 2015-10-09 2017-04-13 Acea Biosciences, Inc Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
WO2017068412A1 (en) * 2015-10-21 2017-04-27 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
MX391850B (es) 2015-12-10 2025-03-19 Ptc Therapeutics Inc Compuestos para usarse en el tratamiento o mejoramiento de la enfermedad de huntington
CN109476675B (zh) 2016-07-01 2022-12-09 爱尔兰詹森科学公司 用于治疗病毒性感染的二氢吡喃并嘧啶衍生物
WO2018009544A1 (en) 2016-07-05 2018-01-11 The Broad Institute, Inc. Bicyclic urea kinase inhibitors and uses thereof
EP4219462A1 (en) * 2016-07-13 2023-08-02 Vertex Pharmaceuticals Incorporated Methods, compositions and kits for increasing genome editing efficiency
US11241435B2 (en) 2016-09-16 2022-02-08 The General Hospital Corporation Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
AU2017335648B2 (en) 2016-09-27 2022-02-17 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors
KR102450287B1 (ko) 2016-09-29 2022-09-30 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염 및 추가적인 질환의 치료를 위한 피리미딘 프로드러그
JP7113826B2 (ja) * 2016-12-19 2022-08-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング プロテインキナーゼ阻害剤および追加的化学療法剤の組み合わせ
CN111163771B (zh) 2017-02-28 2023-07-14 通用医疗公司 嘧啶并嘧啶酮类作为sik抑制剂的用途
US20200101080A1 (en) * 2017-03-31 2020-04-02 Bioventures, Llc Inhibitors of dna pk and uses thereof
CA3059072A1 (en) 2017-04-07 2018-10-11 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
AR111806A1 (es) 2017-05-18 2019-08-21 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituidos
US11325899B2 (en) 2017-05-18 2022-05-10 Idorsia Pharmaceuticals Ltd Benzofurane and benzothiophene derivatives as PGE2 receptor modulators
AU2018269666B2 (en) * 2017-05-18 2022-02-03 Idorsia Pharmaceuticals Ltd Phenyl derivatives as PGE2 receptor modulators
HUE056382T2 (hu) * 2017-05-18 2022-02-28 Idorsia Pharmaceuticals Ltd Pirimidin-származékok mint PGE2 receptor modulátorok
JP7253500B2 (ja) * 2017-05-18 2023-04-06 イドーシア ファーマシューティカルズ リミテッド ピリミジン誘導体
CA3066224A1 (en) 2017-06-05 2018-12-13 Ptc Therapeutics Inc. Compounds for treating huntington's disease
US11382918B2 (en) 2017-06-28 2022-07-12 Ptc Therapeutics, Inc. Methods for treating Huntington's Disease
MX2019015580A (es) 2017-06-28 2020-07-28 Ptc Therapeutics Inc Metodos para tratar la enfermedad de huntington.
IL276081B2 (en) 2018-01-17 2023-10-01 Vertex Pharma Quinoxalinone compounds, compositions, methods, and kits for increasing genome editing efficiency
CA3088792A1 (en) 2018-01-17 2019-07-25 Vertex Pharmaceuticals Incorporated Dna-pk inhibitors
EA202091709A1 (ru) 2018-01-17 2020-11-10 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы днк-пк
TW202415645A (zh) 2018-03-01 2024-04-16 愛爾蘭商健生科學愛爾蘭無限公司 ２，４－二胺基喹唑啉衍生物及其醫學用途
AU2019240065A1 (en) 2018-03-20 2020-09-24 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
JP7399870B2 (ja) 2018-03-27 2023-12-18 ピーティーシー セラピューティクス， インコーポレイテッド ハンチントン病を処置するための化合物
US11685746B2 (en) 2018-06-27 2023-06-27 Ptc Therapeutics, Inc. Heteroaryl compounds for treating Huntington's disease
KR20210038845A (ko) 2018-06-27 2021-04-08 피티씨 테라퓨틱스, 인크. 헌팅턴병 치료를 위한 헤테로아릴 화합물
HUE068060T2 (hu) * 2018-06-27 2024-12-28 Ptc Therapeutics Inc Heterociklikus és heteroaril vegyületek Huntington-kór kezelésére
CA3124353A1 (en) * 2018-12-31 2020-07-09 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
CN111909144A (zh) * 2019-05-10 2020-11-10 山东轩竹医药科技有限公司 喹唑啉类dna-pk抑制剂
TWI899080B (zh) * 2019-05-27 2025-10-01 大陸商迪哲（江蘇）醫藥股份有限公司 Ｄｎａ依賴性蛋白激酶抑制劑
EP3983545A1 (en) 2019-06-17 2022-04-20 Vertex Pharmaceuticals Incorporated Compositions and methods for editing beta-globin for treatment of hemaglobinopathies
CN112300126A (zh) * 2019-07-31 2021-02-02 山东轩竹医药科技有限公司 杂环类dna-pk抑制剂
KR20220070443A (ko) 2019-08-27 2022-05-31 버텍스 파마슈티칼스 인코포레이티드 반복성 dna와 연관된 장애의 치료용 조성물 및 방법
WO2021050059A1 (en) 2019-09-11 2021-03-18 Provincial Health Services Authority Dna-pk inhibiting compounds
CN112574211B (zh) * 2019-09-29 2022-06-14 山东轩竹医药科技有限公司 杂环类激酶抑制剂
CN112574179B (zh) * 2019-09-29 2022-05-10 山东轩竹医药科技有限公司 Dna-pk抑制剂
JP7428806B2 (ja) * 2019-12-31 2024-02-06 成都百裕制薬股▲ふん▼有限公司 プリン誘導体および医薬におけるその使用
CN113372345B (zh) * 2020-02-25 2022-08-16 山东轩竹医药科技有限公司 氘代杂环类激酶抑制剂
AU2021256235B2 (en) * 2020-04-17 2024-05-09 Kangbaida (Sichuan) Biotechnology Co., Ltd. Imidazolidinone derivatives and medical use thereof
EP4263829A1 (en) 2020-12-17 2023-10-25 Vertex Pharmaceuticals Incorporated Compositions and methods for editing beta-globin for treatment of hemaglobinopathies
EP4298221A1 (en) 2021-02-26 2024-01-03 Vertex Pharmaceuticals Incorporated Compositions and methods for treatment of myotonic dystrophy type 1 with crispr/slucas9
TW202302848A (zh) 2021-02-26 2023-01-16 美商維泰克斯製藥公司 以crispr/sacas9治療第1型肌強直性營養不良之組合物及方法
WO2023018637A1 (en) 2021-08-09 2023-02-16 Vertex Pharmaceuticals Incorporated Gene editing of regulatory elements
CA3262455A1 (en) * 2022-12-12 2024-06-20 Avelos Therapeutics Inc. DERIVATIVES OF SUBSTITUTED HETEROCYCLIC COMPOUNDS AND THEIR PHARMACEUTICAL USE
WO2025181336A1 (en) 2024-03-01 2025-09-04 Cellectis Sa Compositions and methods for hbb-editing in hspc
WO2025229177A1 (en) 2024-05-02 2025-11-06 Idorsia Pharmaceuticals Ltd Crystalline forms of an n-substituted indole derivative

Family Cites Families (179)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5571506A (en) 1989-08-14 1996-11-05 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aromatic oligomeric compounds useful as mimics of bioactive macromolecules
EP0507863A4 (en) 1989-12-28 1993-07-07 Virginia Commonwealth University Sigma receptor ligands and the use thereof
ATE156120T1 (de) 1991-02-07 1997-08-15 Roussel Uclaf Bizyklische stickstoffverbindungen, ihre herstellung, erhaltene zwischenprodukte, ihre verwendung als arzneimittel und diese enthaltende pharmazeutische zusammensetzungen
US6004979A (en) 1991-02-07 1999-12-21 Hoechst Marion Roussel Nitrogenous bicycles
EP0519211A1 (de) 1991-05-17 1992-12-23 Hoechst Schering AgrEvo GmbH Substituierte 4-Aminopyrimidine, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel
DE4208254A1 (de) 1992-03-14 1993-09-16 Hoechst Ag Substituierte pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel und fungizid
AU3933493A (en) 1992-04-24 1993-11-29 E.I. Du Pont De Nemours And Company Arthropodicidal and fungicidal aminopyrimidines
US5595756A (en) 1993-12-22 1997-01-21 Inex Pharmaceuticals Corporation Liposomal compositions for enhanced retention of bioactive agents
DE4437406A1 (de) 1994-10-19 1996-04-25 Hoechst Ag Chinoxaline, Verfahren zu ihrer Herstellung und ihre Verwendung
US5977117A (en) 1996-01-05 1999-11-02 Texas Biotechnology Corporation Substituted phenyl compounds and derivatives thereof that modulate the activity of endothelin
ATE345339T1 (de) 1997-02-19 2006-12-15 Berlex Lab N-heterocyclische derivate als nos inhibitoren
JPH10251255A (ja) 1997-03-14 1998-09-22 Nissan Chem Ind Ltd アジン誘導体
ATE493389T1 (de) 1997-05-28 2011-01-15 Aventis Pharma Inc Chinoxalin-derivate die den von blutplättchen abstammenden wachstumsfaktor und/oder p56lck- tyrosinkinase hemmen
DE19801598C2 (de) 1998-01-17 2000-05-11 Aventis Res & Tech Gmbh & Co Katalytische Synthese von N-alkylierten Anilinen aus Olefinen und Anilinen
DE19836697A1 (de) 1998-08-13 2000-02-17 Hoechst Marion Roussel De Gmbh Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
EP1147094A1 (en) 1999-01-15 2001-10-24 Novo Nordisk A/S Non-peptide glp-1 agonists
AU770600B2 (en) * 1999-10-07 2004-02-26 Amgen, Inc. Triazine kinase inhibitors
GB9924092D0 (en) 1999-10-13 1999-12-15 Zeneca Ltd Pyrimidine derivatives
US6552016B1 (en) 1999-10-14 2003-04-22 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
WO2001057021A2 (en) 2000-02-01 2001-08-09 Cor Therapeutics, Inc. 2-[1H]-QUINOLONE AND 2-[1H]-QUINOXALONE INHIBITORS OF FACTOR Xa
EP1259485B1 (en) 2000-02-29 2005-11-30 Millennium Pharmaceuticals, Inc. BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa
US6605615B2 (en) 2000-03-01 2003-08-12 Tularik Inc. Hydrazones and analogs as cholesterol lowering agents
DE10013318A1 (de) 2000-03-17 2001-09-20 Merck Patent Gmbh Formulierung enthaltend Chinoxalinderivate
US7498304B2 (en) 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
EP1351946A2 (en) * 2000-09-01 2003-10-15 Icos Corporation Materials and methods to potentiate cancer treatment
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
DE60128709T2 (de) 2000-09-15 2007-12-27 Vertex Pharmaceuticals Inc., Cambridge Triazol-verbindungen als protein-kinase-inhibitoren
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
MXPA03005001A (es) 2000-12-05 2003-09-05 Vertex Pharma Inhibidores de n- terminal c-jun cinasas (jnk) y otras proteinas cinasas.
NZ526468A (en) 2000-12-21 2004-03-26 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
WO2002062787A1 (en) 2001-02-02 2002-08-15 Glaxo Group Limited Pyrazoles as tgf inhibitors
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
CA2441733A1 (en) 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
ES2271322T3 (es) 2001-04-13 2007-04-16 Vertex Pharmaceuticals Incorporated Inhibidores de quinasas n-terminales c-jun y otras proteinas quinasa.
EP1383771A1 (en) 2001-04-20 2004-01-28 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives as inhibitors of gsk-3
US6884804B2 (en) 2001-05-16 2005-04-26 Vertex Pharmaceuticals Incorporated Inhibitors of Src and other protein kinases
US6762179B2 (en) 2001-05-31 2004-07-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
ES2274035T3 (es) 2001-06-01 2007-05-16 Vertex Pharmaceuticals Incorporated Compuestos de tiazol utiles como inhibidores de proteina quinasas.
US6825190B2 (en) 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
ES2271283T3 (es) 2001-07-03 2007-04-16 Vertex Pharmaceuticals Incorporated Isoxazolil-pirimidinas como inhibidores de las proteinas quinasas src y lck.
AU2002364536B2 (en) 2001-12-07 2008-10-23 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as GSK-3 inhibitors
CA2475633C (en) 2002-02-06 2013-04-02 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
US20030207873A1 (en) 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
EP1506189A1 (en) 2002-04-26 2005-02-16 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
AU2003299472A1 (en) 2002-05-06 2004-07-22 Vertex Pharmaceuticals Incorporated Thiadiazoles or oxadiazoles and their use as inhibitors of JAK kinase
MXPA04011956A (es) 2002-05-30 2005-03-31 Vertex Pharma Inhibidores de proteinas cinasas jak y cdk2.
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
US20040208608A1 (en) 2002-06-24 2004-10-21 Alex Tager Dispersion compensation architecture for switch-ready optical networks
CA2491895C (en) 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
RU2005106871A (ru) 2002-08-14 2005-10-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы протеинкиназ и их применение
US7419984B2 (en) 2002-10-17 2008-09-02 Cell Therapeutics, Inc. Pyrimidines and uses thereof
JP2006512314A (ja) 2002-11-01 2006-04-13 バーテックス ファーマシューティカルズ インコーポレイテッド Ｊａｋインヒビターおよび他のプロテインキナーゼインヒビターとしての組成物の使用
WO2004041814A1 (en) 2002-11-04 2004-05-21 Vertex Pharmaceuticals Incorporated Heteroaryl-pyramidine derivatives as jak inhibitors
EP1581526B1 (en) 2002-12-18 2009-03-11 Vertex Pharmaceuticals Incorporated Benzisoxazole derivatives useful as inhibitors of protein kinases
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
JP5069905B2 (ja) 2003-01-21 2012-11-07 アプテュイト （ウエスト ラファイエット）、エルエルシー 新規な共結晶化
CA2515132C (en) 2003-02-07 2012-01-03 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrroles useful as inhibitors of protein kinases
EP1606284B1 (en) 2003-03-13 2009-12-02 Vertex Pharmaceuticals Incorporated Compositions useful as protein kinase inhibitors
WO2004085418A2 (en) 2003-03-24 2004-10-07 Luitpold Pharmaceuticals, Inc. Xanthones, thioxanthones and acridinones as dna-pk inhibitors
AU2004225965A1 (en) 2003-03-25 2004-10-14 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
US6875781B2 (en) 2003-04-04 2005-04-05 Cell Therapeutics, Inc. Pyridines and uses thereof
US7189724B2 (en) 2003-04-15 2007-03-13 Valeant Research And Development Quinoxaline derivatives having antiviral activity
WO2005026129A1 (en) * 2003-09-15 2005-03-24 Gpc Biotech Ag Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
EP1697375A2 (en) 2003-12-02 2006-09-06 Vertex Pharmaceuticals Incorporated Heterocyclic protein kinase inhibitors and uses thereof
EP1694671A2 (en) 2003-12-04 2006-08-30 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
TW200533357A (en) 2004-01-08 2005-10-16 Millennium Pharm Inc 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
ES2358267T3 (es) 2004-03-15 2011-05-09 Sunesis Pharmaceuticals, Inc. Composición farmacéutica que comprende sns-595 y sus usos.
GB0405985D0 (en) 2004-03-17 2004-04-21 Novartis Forschungsstiftung Kinase
MXPA06013208A (es) 2004-05-14 2007-01-16 Vertex Pharma Profarmacos de pirrolipirimidina como inhibidotes de la proteina cinasa erk.
JP4449580B2 (ja) 2004-05-31 2010-04-14 宇部興産株式会社 ４−アラルキルアミノピリミジン誘導体及び抗菌剤
DE602005011279D1 (de) 2004-06-04 2009-01-08 Arena Pharm Inc Substituierte aryl- und heteroarylderivate als modulatoren des stoffwechsels und für die prophylaxe und behandlung von damit in zusammenhang stehenden erkrankungen
CN101039933B (zh) 2004-09-17 2012-06-06 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的二氨基三唑化合物
US9315467B2 (en) 2004-10-13 2016-04-19 Ptc Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
CA2583096A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
GT200500284A (es) 2004-10-15 2006-03-27 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
US20060166936A1 (en) 2004-10-29 2006-07-27 Hayley Binch Diaminotriazole compounds useful as inhibitors of protein kinases
US7517870B2 (en) 2004-12-03 2009-04-14 Fondazione Telethon Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization
EP1831181A2 (en) 2004-12-14 2007-09-12 Vertex Pharmaceuticals Incorporated Pyrimidine inhibitors of erk protein kinase and uses thereof
JP2008525461A (ja) 2004-12-23 2008-07-17 バーテックス ファーマシューティカルズ インコーポレイテッド Ｅｒｋプロテインキナーゼの選択的阻害剤およびその使用
EP1850681B1 (en) 2005-02-04 2019-12-18 Firmenich Incorporated Compounds comprising linked hetero aryl moieties and their use as novel umami flavor modifiers, tastants and taste enhancers for comestible compositions
CN101184395A (zh) 2005-04-06 2008-05-21 Irm责任有限公司 包含二芳基胺的化合物和组合物及其作为类固醇激素核受体调节剂的用途
AR054438A1 (es) 2005-04-15 2007-06-27 Kudos Pharm Ltd Inhibidores de adn -pk
US20090221581A1 (en) * 2005-05-25 2009-09-03 Philipp Wabnitz Methods of treating pain
WO2006138418A2 (en) 2005-06-14 2006-12-28 President And Fellows Of Harvard College Improvement of cognitive performance with sirtuin activators
JP2007008045A (ja) 2005-06-30 2007-01-18 Mitsui Chemicals Inc 光記録媒体および１ｈ−キノキサリン−２−オン誘導体
US7874452B2 (en) 2005-07-22 2011-01-25 Berkeley Law & Technology Group, Llp Cup cover
CA2616517A1 (en) 2005-07-26 2007-02-01 Vertex Pharmaceuticals Incorporated Abl kinase inhibition
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
JP2009514875A (ja) 2005-11-02 2009-04-09 サイトキネティクス・インコーポレーテッド 化学物質、組成物、および方法
RU2008122070A (ru) 2005-11-03 2009-12-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Аминопиридины, используемые в качестве ингибиторов киназ
DE602006021776D1 (de) 2005-11-16 2011-06-16 Vertex Pharma Als kinaseinhibitoren geeignete aminopyrimidine
WO2007082899A1 (en) 2006-01-17 2007-07-26 Vib Vzw Inhibitors of prolyl-hydroxylase 1 for the treatment of skeletal muscle degeneration
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
UY30118A1 (es) 2006-01-31 2007-06-29 Tanabe Seiyaku Co Compueto amina trisustituido
US8013153B2 (en) 2006-03-23 2011-09-06 Janssen Pharmaceutica, N.V. Substituted pyrimidine kinase inhibitors
US20080280891A1 (en) 2006-06-27 2008-11-13 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
WO2008008852A2 (en) 2006-07-11 2008-01-17 Emory University Cxcr4 antagonists including heteroatoms for the treatment of medical disorders
TW200811134A (en) 2006-07-12 2008-03-01 Irm Llc Compounds and compositions as protein kinase inhibitors
AU2007271964B2 (en) 2006-07-14 2012-01-19 Novartis Ag Pyrimidine derivatives as ALK-5 inhibitors
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US7635683B2 (en) 2006-08-04 2009-12-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl tripeptide hepatitis C virus inhibitors
CA2661307C (en) 2006-08-22 2016-07-19 Technion Research And Development Foundation Ltd. Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (pbr)
EP1903038A1 (de) 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren
US7875603B2 (en) 2006-09-21 2011-01-25 Nova Southeastern University Specific inhibitors for vascular endothelial growth factor receptors
AU2007305016B2 (en) * 2006-10-02 2011-11-03 Novartis Ag Compounds and compositions as protein kinase inhibitors
DE102006050512A1 (de) 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte heterocyclische Verbindungen und ihre Verwendung
AU2007317435A1 (en) 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
US20100234341A1 (en) 2006-12-04 2010-09-16 Marion Lanier Substituted pyrimidines as adenosine receptor antagonists
WO2008077086A1 (en) 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
CA2671851A1 (en) 2006-12-28 2008-07-10 Ambrx, Inc. Phenazine and quinoxaline substituted amino acids and polypeptides
CA2702647C (en) 2007-01-31 2016-03-22 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
WO2008106202A1 (en) 2007-02-27 2008-09-04 Housey Gerard M Theramutein modulators
NZ579485A (en) 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
ES2435997T3 (es) 2007-03-09 2013-12-26 Vertex Pharmaceuticals, Inc. Aminopirimidinas útiles como inhibidores de las proteínas cinasas
MX2009009592A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopiridinas utiles como inhibidores de proteinas cinasas.
CN101675041A (zh) 2007-03-20 2010-03-17 沃泰克斯药物股份有限公司 用作激酶抑制剂的氨基嘧啶类化合物
DE102007015169A1 (de) 2007-03-27 2008-10-02 Universität des Saarlandes Campus Saarbrücken 17Beta-Hydroxysteroid-Dehydrogenase-Typ1-Inhibitoren zur Behandlung hormonabhängiger Erkrankungen
JP2010523700A (ja) 2007-04-13 2010-07-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼインヒビターとして有用なアミノピリミジン
US7910587B2 (en) 2007-04-26 2011-03-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl dipeptide hepatitis C virus inhibitors
EP2155730A2 (en) 2007-05-02 2010-02-24 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247594A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
NZ580884A (en) 2007-05-02 2012-02-24 Vertex Pharma Thiazoles and pyrazoles useful as kinase inhibitors
TW200902008A (en) 2007-05-10 2009-01-16 Smithkline Beecham Corp Quinoxaline derivatives as PI3 kinase inhibitors
WO2008144253A1 (en) 2007-05-14 2008-11-27 Irm Llc Protein kinase inhibitors and methods for using thereof
CN101687852A (zh) 2007-05-24 2010-03-31 沃泰克斯药物股份有限公司 可用作激酶抑制剂的噻唑类和吡唑类化合物
EP2167464B1 (en) 2007-05-25 2014-12-03 AbbVie Deutschland GmbH & Co KG Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (mglu2 receptor)
US8685962B2 (en) 2007-07-02 2014-04-01 Technion Research & Development Foundation Limited Compositions, articles and methods comprising TSPO ligands for preventing or reducing tobacco-associated damage
WO2009008991A2 (en) 2007-07-06 2009-01-15 Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services National Institutes Of Health Dna-pkcs modulates energy regulation and brain function
UY31232A1 (es) 2007-07-19 2009-03-02 Compuestos derivados de dibenzotifenilamino-cromen-4-onas activas sustituidas y sus isomeros y aplicaciones
KR101546819B1 (ko) 2007-08-01 2015-08-24 구미아이 가가쿠 고교 가부시키가이샤 옥소피라진 유도체 및 제초제
WO2009042294A2 (en) 2007-08-10 2009-04-02 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
DE102007044032A1 (de) 2007-09-14 2009-03-19 Bayer Healthcare Ag Substituierte heterocyclische Verbindungen und ihre Verwendung
JP5681855B2 (ja) 2007-10-12 2015-03-11 アストラゼネカ エービー プロテインキナーゼの阻害剤
EP2205086B1 (en) 2007-11-06 2013-08-14 E. I. du Pont de Nemours and Company Fungicidal heterocyclic amines
WO2009091388A2 (en) 2007-12-21 2009-07-23 Progenics Pharmaceuticals, Inc. Triazines and related compounds having antiviral activity, compositions and methods thereof
WO2009105220A1 (en) 2008-02-19 2009-08-27 Janssen Pharmaceutica N.V. Aryl-hydroxyethylamino-pyrimidines and triazines as modulators of fatty acid amide hydrolase
US20110009421A1 (en) 2008-02-27 2011-01-13 Takeda Pharmaceutical Company Limited Compound having 6-membered aromatic ring
EP2247580B1 (en) 2008-03-05 2015-07-08 Merck Patent GmbH Quinoxalinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
CA2725316A1 (en) 2008-06-02 2009-12-10 Banyu Pharmaceutical Co., Ltd. Novel isoxazole derivative
HRP20131069T1 (hr) 2008-06-16 2013-12-20 Merck Patent Gmbh Derivati kinoksalindiona
EP2138488A1 (en) 2008-06-26 2009-12-30 sanofi-aventis 4-(pyridin-4-yl)-1H-[1,3,5]triazin-2-one derivatives as GSK3-beta inhibitors for the treatment of neurodegenerative diseases
MX2011000839A (es) 2008-07-23 2011-04-05 Vertex Pharma Inhibidores de pirazolpiridina cinasa.
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
AR074199A1 (es) 2008-11-20 2010-12-29 Glaxosmithkline Llc Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer.
EP2706057B1 (en) 2008-12-05 2016-04-20 Molecular Insight Pharmaceuticals, Inc. Bis(imidazolyl)compounds and radionuclide complexes
SG172248A1 (en) 2008-12-19 2011-07-28 Vertex Pharma Pyrazine derivatives useful as inhibitors of atr kinase
US8592415B2 (en) 2009-02-11 2013-11-26 Reaction Biology Corp. Selective kinase inhibitors
JP2010111702A (ja) 2009-02-16 2010-05-20 Tetsuya Nishio 複素環化合物、その製造法および用途
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US8906914B2 (en) 2009-08-18 2014-12-09 Janssen Pharmaceutica Nv Ethylene diamine modulators of fatty acid hydrolase
AR077999A1 (es) 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
CN105153188B (zh) 2009-10-22 2018-06-01 法博太科制药有限公司 抗纤维化剂的稠环类似物
ES2360333B1 (es) 2009-10-29 2012-05-04 Consejo Superior De Investigaciones Cientificas (Csic) (70%) Derivados de bis (aralquil) amino y sistemas (hetero) aromaticos de seis miembros y su uso en el tratamiento de patologias neurodegenerativas, incluida la enfermedad de alzheimer
CA2779398A1 (en) 2009-10-30 2011-05-05 Mochida Phamaceutical Co., Ltd. Novel 3-hydroxy-5-arylisoxazole derivative
EA201290574A1 (ru) 2009-12-25 2012-12-28 Мотида Фармасьютикал Ко., Лтд. Новое производное 3-гидрокси-5-арилизотиазола
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
WO2011113512A1 (de) 2010-03-16 2011-09-22 Merck Patent Gmbh Morpholinylchinazoline
TWI516264B (zh) 2010-05-06 2016-01-11 臺北醫學大學 芳香醯喹啉化合物
JP2011246389A (ja) 2010-05-26 2011-12-08 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有する縮環ピラゾール誘導体
DE102010025786A1 (de) 2010-07-01 2012-01-05 Merck Patent Gmbh Pyrazolochinoline
DE102010035744A1 (de) 2010-08-28 2012-03-01 Merck Patent Gmbh Imidazolonylchinoline
WO2012129562A2 (en) 2011-03-24 2012-09-27 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
GB201114051D0 (en) 2011-08-15 2011-09-28 Domainex Ltd Compounds and their uses
EP2747767B8 (en) 2011-08-26 2019-07-17 Neupharma, Inc. Certain chemical entities, compositions, and methods
CN108794411B (zh) 2011-09-14 2022-06-07 润新生物公司 某些化学实体、组合物及方法
EP2757885B1 (en) 2011-09-21 2017-03-15 Neupharma, Inc. Certain chemical entites, compositions, and methods
US9249111B2 (en) 2011-09-30 2016-02-02 Neupharma, Inc. Substituted quinoxalines as B-RAF kinase inhibitors
DE102011118830A1 (de) 2011-11-18 2013-05-23 Merck Patent Gmbh Morpholinylbenzotriazine
GB201120993D0 (en) 2011-12-06 2012-01-18 Imp Innovations Ltd Novel compounds and their use in therapy
US9670180B2 (en) 2012-01-25 2017-06-06 Neupharma, Inc. Certain chemical entities, compositions, and methods
HUE054031T2 (hu) * 2012-04-24 2021-08-30 Vertex Pharma DNS-PK inhibitorok
EP2916838B1 (en) 2012-11-12 2019-03-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
RU2676259C2 (ru) 2013-03-12 2018-12-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы днк-пк
DK3424920T3 (da) 2013-10-17 2020-06-08 Vertex Pharma Co-krystaller af (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinolin-4-carboxamid og deuterede derivater deraf som dna-pk-inhibitorer

Also Published As

Publication number Publication date
AU2013251804A1 (en) 2014-10-30
SG11201406584TA (en) 2014-11-27
NZ700928A (en) 2017-06-30
UA115983C2 (uk) 2018-01-25
CY1124311T1 (el) 2022-07-22
NZ731797A (en) 2018-08-31
RS61664B1 (sr) 2021-04-29
US9296701B2 (en) 2016-03-29
WO2013163190A8 (en) 2014-11-27
US20180193341A1 (en) 2018-07-12
US20160368899A1 (en) 2016-12-22
US20200062732A1 (en) 2020-02-27
US10501439B2 (en) 2019-12-10
US10391095B2 (en) 2019-08-27
AU2013251804B2 (en) 2017-10-12
DK2841428T3 (da) 2018-12-10
WO2013163190A1 (en) 2013-10-31
HUE054031T2 (hu) 2021-08-30
US20150111871A1 (en) 2015-04-23
ES2702707T3 (es) 2019-03-05
EP2841428A1 (en) 2015-03-04
IL252063A0 (en) 2017-07-31
US20140045869A1 (en) 2014-02-13
LT2841428T (lt) 2018-12-10
AU2017239481A1 (en) 2017-10-26
US10076521B2 (en) 2018-09-18
IL252063B (en) 2019-03-31
IL235297A (en) 2017-05-29
BR112014026703A2 (pt) 2017-06-27
US20160250212A1 (en) 2016-09-01
KR102089239B1 (ko) 2020-03-16
ZA201407554B (en) 2016-01-27
US11008305B2 (en) 2021-05-18
US20130281431A1 (en) 2013-10-24
RU2638540C1 (ru) 2017-12-14
US20180325898A1 (en) 2018-11-15
MX2014012960A (es) 2015-02-05
US10442791B2 (en) 2019-10-15
PL2841428T3 (pl) 2019-07-31
US9925188B2 (en) 2018-03-27
DK3459942T3 (da) 2021-03-08
JP2015514804A (ja) 2015-05-21
RS58043B1 (sr) 2019-02-28
CY1120866T1 (el) 2019-12-11
US9878993B2 (en) 2018-01-30
ES2860299T3 (es) 2021-10-04
EP3459942B1 (en) 2020-12-30
CL2014002873A1 (es) 2015-04-24
JP6741825B2 (ja) 2020-08-19
SI3459942T1 (sl) 2021-05-31
SI2841428T1 (sl) 2018-12-31
PT3459942T (pt) 2021-03-26
BR112014026703B1 (pt) 2022-10-25
KR20150005645A (ko) 2015-01-14
SMT202100158T1 (it) 2021-05-07
US11021465B2 (en) 2021-06-01
MX357261B (es) 2018-07-03
SG10201704095UA (en) 2017-06-29
IN2014KN02601A (show.php) 2015-05-08
CN106977495A (zh) 2017-07-25
CA2871471A1 (en) 2013-10-31
TR201816379T4 (tr) 2018-11-21
PL3459942T3 (pl) 2021-10-11
PT2841428T (pt) 2018-11-29
US20180208579A1 (en) 2018-07-26
CN106977495B (zh) 2020-08-04
MX371331B (es) 2020-01-27
HK1207859A1 (en) 2016-02-12
HK1208022A1 (en) 2016-02-19
JP2017165788A (ja) 2017-09-21
CN104640852B (zh) 2017-04-26
EP2841428B1 (en) 2018-08-22
JP2019147833A (ja) 2019-09-05
US9376448B2 (en) 2016-06-28
HRP20210365T1 (hr) 2021-04-16
AU2017239481B2 (en) 2019-05-16
EP3459942A1 (en) 2019-03-27
US20170258789A1 (en) 2017-09-14
CN104640852A (zh) 2015-05-20
US20200109130A1 (en) 2020-04-09
HRP20181862T1 (hr) 2019-01-11
CN106986863B (zh) 2019-12-31
US9592232B2 (en) 2017-03-14
CN106986863A (zh) 2017-07-28
SMT201800608T1 (it) 2019-01-11
LT3459942T (lt) 2021-05-10
JP6378171B2 (ja) 2018-08-22

Similar Documents

Publication Publication Date Title
CA2871471C (en) Dna-pk inhibitors
MX365294B (es) Inhibidores de proteína cinasa dependiente de adn.
PH12014502772A1 (en) Substituted tricyclic compounds as fgfr inhibitors
EP4620528A3 (en) Bipyrazole derivatives as jak inhibitors
MX2015006152A (es) Compuestos de aminopirimidina como inhibidores de mutantes de egfr que contienen t7 9 0m.
TN2014000016A1 (en) 4 - piperidinyl compounds for use as tankyrase inhibitors
IN2015DN01156A (show.php)
PH12013500299B1 (en) Pyrrolopyrimidine compounds and uses thereof
MX2014005928A (es) Inhibidores ciclicos de glutaminasa.
EA024842B9 (ru) Соединения в качестве модуляторов протеинкиназы pi3k
CA2818187C (en) Bromodomain inhibitors and uses thereof
TN2013000348A1 (en) Compounds and compositions as trk inhibitors
EA201101650A1 (ru) Новые производные пиримидина и их применение в лечении злокачественных новообразований и последующих заболеваний
EA201200473A1 (ru) Замещенные (гетероарилметил)тиогидантоины
SG195319A1 (en) Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors
MX2011013032A (es) Inhibidores de fosfatidilinositol 3-cinasa.
CA2878796C (en) Derivatives of pyridinone as inhibitors for tissue transglutaminase
CA2929436C (en) Compounds, pharmaceutical composition and methods for use in treating inflammatory diseases
MX2011008645A (es) Inhibidores de tetrahidrotiazolopiridina de fosfatidilinositol 3 cinasa.
AU2012312301A8 (en) Compounds useful as inhibitors of choline kinase
PH12016502133A1 (en) Substituted tricycle compounds as fgfr inhibitors
MY198316A (en) Piperidin-4-YL Azetidine Derivatives as JAK1 Inhibitors
UA110793C2 (uk) Піразолілхіноксалінові інгібітори кінази

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20180423