BR112012007747B8 - compostos heterocíclicos úteis como inibidores de pdk1, sua composição farmacêutica e seus usos - Google Patents

compostos heterocíclicos úteis como inibidores de pdk1, sua composição farmacêutica e seus usos

Info

Publication number
BR112012007747B8
BR112012007747B8 BR112012007747A BR112012007747A BR112012007747B8 BR 112012007747 B8 BR112012007747 B8 BR 112012007747B8 BR 112012007747 A BR112012007747 A BR 112012007747A BR 112012007747 A BR112012007747 A BR 112012007747A BR 112012007747 B8 BR112012007747 B8 BR 112012007747B8
Authority
BR
Brazil
Prior art keywords
compounds useful
pharmaceutical composition
heterocyclic compounds
pdk1 inhibitors
pdk1
Prior art date
Application number
BR112012007747A
Other languages
English (en)
Other versions
BR112012007747A2 (pt
BR112012007747B1 (pt
Inventor
Erlanson Daniel
Scott Daniel
Wang Deping
Yin-Shiang Lin Edward
Kumaravel Gnanasambandam
Thomas Jermaine
Arndt Joseph
Guckian Kevin
Van Vloten Kurt
Zhang Lei
Sun Lihong
Chan Timothy
Lee Wen-Cherng
Original Assignee
Millennium Pharm Inc
Sunesis 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 Millennium Pharm Inc, Sunesis Pharmaceuticals Inc filed Critical Millennium Pharm Inc
Publication of BR112012007747A2 publication Critical patent/BR112012007747A2/pt
Publication of BR112012007747B1 publication Critical patent/BR112012007747B1/pt
Publication of BR112012007747B8 publication Critical patent/BR112012007747B8/pt

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/452Piperidinium derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
    • C07D213/85Nitriles in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

Abstract

compostos heterocíclicos úteis como inibidores de pdk1, sua composição farmacêutica e seus usos. a presente invenção fornece compostos úteis como inibidores de pdk1. a presente invenção também fornece composições dos mesmos, e métodos de tratamento de doenças mediadas por pdk1.
BR112012007747A 2009-10-06 2010-10-05 compostos heterocíclicos úteis como inibidores de pdk1, sua composição farmacêutica e seus usos BR112012007747B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24909509P 2009-10-06 2009-10-06
US61/249,095 2009-10-06
PCT/US2010/051517 WO2011044157A1 (en) 2009-10-06 2010-10-05 Heterocyclic compounds useful as pdk1 inhibitors

Publications (3)

Publication Number Publication Date
BR112012007747A2 BR112012007747A2 (pt) 2017-09-05
BR112012007747B1 BR112012007747B1 (pt) 2020-11-10
BR112012007747B8 true BR112012007747B8 (pt) 2021-05-25

Family

ID=43857093

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012007747A BR112012007747B8 (pt) 2009-10-06 2010-10-05 compostos heterocíclicos úteis como inibidores de pdk1, sua composição farmacêutica e seus usos

Country Status (27)

Country Link
US (5) US9546165B2 (pt)
EP (3) EP3070077B1 (pt)
JP (5) JP6016635B2 (pt)
KR (3) KR20120087936A (pt)
CN (1) CN102665718B (pt)
AR (2) AR078540A1 (pt)
AU (3) AU2010303567B2 (pt)
BR (1) BR112012007747B8 (pt)
CA (1) CA2776690C (pt)
CY (1) CY1118143T1 (pt)
DK (2) DK2485731T3 (pt)
ES (2) ES2586856T3 (pt)
HK (1) HK1168044A1 (pt)
HR (1) HRP20160967T1 (pt)
HU (2) HUE028082T2 (pt)
IL (4) IL266563B (pt)
IN (1) IN2012DN03883A (pt)
LT (1) LT2485731T (pt)
MX (1) MX353257B (pt)
PL (1) PL2485731T4 (pt)
PT (1) PT2485731T (pt)
RS (1) RS55101B1 (pt)
RU (2) RU2615130C2 (pt)
SI (1) SI2485731T1 (pt)
SM (1) SMT201600275B (pt)
TW (1) TWI525093B (pt)
WO (1) WO2011044157A1 (pt)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3354650T1 (sl) 2008-12-19 2022-06-30 Vertex Pharmaceuticals Incorporated Spojine, uporabne kot zaviralci ATR kinaze
WO2011044157A1 (en) 2009-10-06 2011-04-14 Biogen Idec Ma Inc. Heterocyclic compounds useful as pdk1 inhibitors
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
EP2569286B1 (en) * 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
RU2012153675A (ru) 2010-05-12 2014-06-20 Вертекс Фармасьютикалз Инкорпорейтед Соединения, пригодные в качестве ингибиторов atr киназы
WO2012012528A1 (en) 2010-07-20 2012-01-26 Vestaron Corporation Insecticidal triazines and pyrimidines
KR20130087020A (ko) 2010-09-16 2013-08-05 허치슨 메디파르마 리미티드 축합 헤테로아릴 및 그 용도
US8791112B2 (en) * 2011-03-30 2014-07-29 Arrien Pharmaceuticals Llc Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-B] pyridine and pyrazolo [3, 4-B] pyridine derivatives as protein kinase inhibitors
US10457659B2 (en) 2011-04-29 2019-10-29 The Board Of Trustees Of The Leland Stanford Junior University Compositions and methods for increasing proliferation of adult salivary stem cells
IN2014KN00929A (pt) 2011-09-30 2015-08-21 Vertex Pharma
CN108685922A (zh) 2011-09-30 2018-10-23 沃泰克斯药物股份有限公司 用atr抑制剂治疗胰腺癌和非小细胞肺癌
CN103159741B (zh) * 2011-12-19 2016-08-24 天津市国际生物医药联合研究院 一类酪氨酸激酶抑制剂的制备和用途
PL2833973T3 (pl) 2012-04-05 2018-02-28 Vertex Pharmaceuticals Incorporated Związki użyteczne jako inhibitory kinazy ATR i ich terapie skojarzone
CN102627632B (zh) * 2012-04-16 2014-06-18 中国科学院广州生物医药与健康研究院 一种胺基喹唑啉衍生物及其制备方法和用途
PE20142258A1 (es) 2012-04-25 2015-01-15 Takeda Pharmaceutical Compuesto heterociclico nitrogenado
SG11201406914XA (en) * 2012-05-08 2014-11-27 Anvyl Llc Alpha 7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
US9527841B2 (en) 2012-07-13 2016-12-27 Takeda Pharmaceutical Company Limited Substituted pyrido[2,3-b]pyrazines as phosphodiesterase 2A inhibitors
BR112015006828A8 (pt) 2012-09-26 2019-09-17 Univ California composto, ou um sal farmaceuticamente aceitável do mesmo; composição farmacêutica; uso do composto; e método para modular a atividade de uma proteína ire1
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
JP6410790B2 (ja) 2013-03-14 2018-10-24 ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー ミトコンドリアアルデヒドデヒドロゲナーゼ−2調節因子およびその使用方法
EP2975031A4 (en) 2013-03-14 2017-04-19 Takeda Pharmaceutical Company Limited Heterocyclic compound
BR112015029899B1 (pt) * 2013-05-31 2020-07-21 Nissan Chemical Corporation composto de amida heterocíclica e sal do mesmo da formula (1), produto quimico agrícola e herbicida obtido
WO2015002230A1 (ja) 2013-07-03 2015-01-08 武田薬品工業株式会社 アミド化合物
US10053468B2 (en) 2013-07-03 2018-08-21 Takeda Pharmaceutical Company Limited Heterocyclic compound
JPWO2015012328A1 (ja) 2013-07-24 2017-03-02 武田薬品工業株式会社 複素環化合物
FI3640241T3 (fi) 2013-10-18 2023-01-13 Bromodomeeni-inhibiittorit
WO2015073804A2 (en) * 2013-11-15 2015-05-21 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Method of blocking transmission of malarial parasite
PL3071206T3 (pl) 2013-11-22 2022-01-17 CL BioSciences LLC Antagoniści gastryny (eg yf476, netazepid) do leczenia i zapobiegania osteoporozie
CN104130256B (zh) * 2014-08-01 2016-08-24 上海毕得医药科技有限公司 一种吡啶并[3,4-d]嘧啶-4(3H)-酮衍生物的制备方法
EP3209664B1 (en) * 2014-10-22 2020-06-03 Bristol-Myers Squibb Company Bicyclic heteroaryl amine compounds as pi3k inhibitors
PL3218378T3 (pl) 2014-11-14 2020-10-19 Nerviano Medical Sciences S.R.L. Pochodne 6-amino-7-bicyklo-7-deazapuryny jako inhibitory kinaz białkowych
AR104259A1 (es) 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
EP3325100A4 (en) 2015-07-17 2019-02-20 Memorial Sloan-Kettering Cancer Center COMBINED THERAPY USING PDK1 AND PI3K INHIBITORS
CN105130980B (zh) * 2015-09-09 2018-05-22 沈阳药科大学 N-3-苯并咪唑噻唑胺类衍生物及其制备方法与应用
AU2016322813B2 (en) * 2015-09-14 2021-04-01 Pfizer Inc. Novel imidazo (4,5-c) quinoline and imidazo (4,5-c)(1,5) naphthyridine derivatives as LRRK2 inhibitors
EP3355926A4 (en) 2015-09-30 2019-08-21 Vertex Pharmaceuticals Inc. METHOD FOR THE TREATMENT OF CANCER WITH A COMBINATION OF DNA DAMAGING AGENTS AND ATR INHIBITORS
KR101753652B1 (ko) * 2015-10-21 2017-07-05 한국화학연구원 N-아릴-1h-피라졸로피리딘-3-아민 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 melk 관련 질환의 예방 또는 치료용 약학적 조성물
KR101753654B1 (ko) 2015-10-21 2017-07-05 한국화학연구원 3-(4-(피페라진-1-일)벤즈아미도)-1h-피라졸로피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 melk 관련 질환의 예방 또는 치료용 약학적 조성물
AU2016342352B2 (en) 2015-10-23 2022-06-02 Sunesis Pharmaceuticals, Inc. Heterocyclic PDK1 inhibitors for use to treat cancer
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
CA3019145A1 (en) 2016-03-28 2017-10-05 Incyte Corporation Pyrrolotriazine compounds as tam inhibitors
WO2017184462A1 (en) 2016-04-18 2017-10-26 Celgene Quanticel Research, Inc. Therapeutic compounds
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
JP2019530650A (ja) 2016-08-24 2019-10-24 アークル インコーポレイテッド アミノ−ピロロピリミジノン化合物およびその使用方法
EP3558971B1 (en) 2016-12-22 2022-02-23 Global Blood Therapeutics, Inc. Histone methyltransferase inhibitors
WO2018164248A1 (ja) * 2017-03-10 2018-09-13 大塚化学株式会社 反応生成物及びゴム組成物
WO2018226998A1 (en) * 2017-06-09 2018-12-13 Global Blood Therapeutics, Inc. Azaindole compounds as histone methyltransferase inhibitors
WO2019094779A1 (en) * 2017-11-09 2019-05-16 Sunesis Pharmaceuticals, Inc. Pharmaceutical formulations, processes for preparation, and methods of use
EA202091777A1 (ru) 2018-01-26 2020-10-14 Бристол-Маерс Сквибб Компани Аминопирролотриазины в качестве ингибиторов киназы
CN109087534A (zh) * 2018-10-09 2018-12-25 王业宝 一种基于车辆行驶轨迹的交通冲突检测方法
KR102293339B1 (ko) * 2019-04-17 2021-08-25 이화여자대학교 산학협력단 아미노알코올을 포함하는 아민 화합물에 대한 형광 및/또는 원편광 이색성 센서용 신규 프로브 화합물, 및 이를 이용한 형광 및 원편광 이색성 동시 분석 방법
CN110066221B (zh) * 2019-05-16 2022-03-08 海门瑞一医药科技有限公司 一种环丙基甲胺的制备方法
WO2021064141A1 (en) * 2019-10-02 2021-04-08 Tolremo Therapeutics Ag Inhibitors of dual specificity tyrosine phosphorylation regulated kinase 1b
US20220389010A1 (en) * 2019-11-25 2022-12-08 Daewoong Pharmaceutical Co., Ltd. Novel Triazolopyridine Derivatives and Pharmaceutical Composition Comprising Same
AR127972A1 (es) * 2021-12-17 2024-03-13 Pi Industries Ltd Novedosos compuestos de piridina carboxamida bicíclica sustituida fusionada para combatir hongos fitopatogénicos
WO2024040242A1 (en) 2022-08-19 2024-02-22 Viracta Therapeutics, Inc. Combinations of pdk1 inhibitors and kinase inhibitors
WO2024040241A1 (en) 2022-08-19 2024-02-22 Viracta Therapeutics, Inc. Pharmaceutical formulations, processes for preparation, and methods of use

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3175980A (en) * 1958-05-23 1965-03-30 Geigy Ag J R Compositions of matter of improved appearance in daylight, containing a 3.5-diaminopyrazine-2.6-dicarboxylic acid derivative
PL114780B1 (en) * 1978-03-10 1981-02-28 Inst Przemyslu Farmaceutic Process for preparing novel alkylamides of 2-anilinonicotinic acids
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
DE69212850T2 (de) 1991-01-15 1997-03-06 Alcon Lab Inc Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
EP1140881B1 (en) * 1998-12-23 2006-05-17 Eli Lilly And Company Antithrombotic amides
JP2002533453A (ja) * 1998-12-23 2002-10-08 イーライ・リリー・アンド・カンパニー Xa因子のインヒビターとしてのヘテロ芳香族アミド
GB0001930D0 (en) * 2000-01-27 2000-03-22 Novartis Ag Organic compounds
US6878714B2 (en) * 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
CA2484209C (en) 2002-05-03 2013-06-11 Exelixis, Inc. Protein kinase modulators and methods of use
CL2004000234A1 (es) 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
WO2005005421A1 (en) 2003-07-08 2005-01-20 Novartis Ag Benzenesulfonylamino compounds and pharmaceutical compositions containing these compounds
US7320992B2 (en) 2003-08-25 2008-01-22 Amgen Inc. Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use
US20050182061A1 (en) * 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
MXPA06004438A (es) 2003-10-24 2006-06-20 Schering Ag Derivados de indolinona y su uso en el tratamiento de enfermedades como el cancer.
AR049418A1 (es) * 2004-02-27 2006-08-02 Bayer Pharmaceuticals Corp Derivados de heteroarilaminopirazol y composiciones farmaceuticas para el tratamiento de la diabetes.
SE0401345D0 (sv) * 2004-05-25 2004-05-25 Astrazeneca Ab Therapeutic compounds: Pyridine as scaffold
EP1655297A1 (en) 2004-11-03 2006-05-10 Schering Aktiengesellschaft Nicotinamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors
JP2008545756A (ja) * 2005-06-03 2008-12-18 バイエル・ヘルスケア・アクチェンゲゼルシャフト 癌化学療法剤として有用な1−メチル−1h−ピラゾール−4−カルボキサミド類
US7572808B2 (en) 2005-06-17 2009-08-11 Bristol-Myers Squibb Company Triazolopyridine cannabinoid receptor 1 antagonists
US7547782B2 (en) 2005-09-30 2009-06-16 Bristol-Myers Squibb Company Met kinase inhibitors
WO2007056170A2 (en) 2005-11-02 2007-05-18 Bayer Healthcare Ag Pyrrolo[2,1-f] [1,2,4] triazin-4-ylamines igf-1r kinase inhibitors for the treatment of cancer and other hyperproliferative diseases
EP1979353A2 (en) 2006-01-19 2008-10-15 OSI Pharmaceuticals, Inc. Fused heterobicyclic kinase inhibitors
EP2049119A2 (en) * 2006-06-29 2009-04-22 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea
WO2008005457A2 (en) * 2006-06-30 2008-01-10 Sunesis Pharmaceuticals Pyridinonyl pdk1 inhibitors
WO2008016643A2 (en) * 2006-08-01 2008-02-07 Cytokinetics, Incorporated Certain chemical entities, compositions, and methods
ES2392156T3 (es) 2006-12-20 2012-12-05 Amgen Inc. Heterociclos sustituidos y métodos de uso
EP2139882B1 (en) * 2007-03-23 2013-12-25 Amgen Inc. 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
CA2690141A1 (en) * 2007-06-20 2008-12-24 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
US7868001B2 (en) * 2007-11-02 2011-01-11 Hutchison Medipharma Enterprises Limited Cytokine inhibitors
US20130023497A1 (en) * 2009-06-08 2013-01-24 Chunlin Tao Triazine Derivatives and their Therapeutical Applications
WO2011044157A1 (en) 2009-10-06 2011-04-14 Biogen Idec Ma Inc. Heterocyclic compounds useful as pdk1 inhibitors

Also Published As

Publication number Publication date
RU2017109664A3 (pt) 2020-07-15
SMT201600275B (it) 2016-11-10
HUE028082T2 (en) 2016-11-28
RU2017109664A (ru) 2019-01-23
AR078540A1 (es) 2011-11-16
KR102097664B1 (ko) 2020-04-06
CN102665718B (zh) 2016-03-09
IL266563A (en) 2019-07-31
LT2485731T (lt) 2016-09-12
BR112012007747A2 (pt) 2017-09-05
AU2010303567B2 (en) 2016-06-09
AR124483A2 (es) 2023-03-29
AU2010303567A1 (en) 2012-05-03
US20190119268A1 (en) 2019-04-25
US20120208819A1 (en) 2012-08-16
BR112012007747B1 (pt) 2020-11-10
TW201124416A (en) 2011-07-16
AU2018222943B2 (en) 2019-09-26
EP3070077A1 (en) 2016-09-21
JP2016188253A (ja) 2016-11-04
US9546165B2 (en) 2017-01-17
US10030016B2 (en) 2018-07-24
RS55101B1 (sr) 2016-12-30
JP2020203925A (ja) 2020-12-24
EP3466929A1 (en) 2019-04-10
MX2012004114A (es) 2012-08-23
EP3466929B1 (en) 2023-09-06
IN2012DN03883A (pt) 2015-09-25
WO2011044157A1 (en) 2011-04-14
RU2615130C2 (ru) 2017-04-04
IL295518B1 (en) 2023-07-01
CY1118143T1 (el) 2017-06-28
JP2013506715A (ja) 2013-02-28
KR20190025680A (ko) 2019-03-11
IL302896A (en) 2023-07-01
US20160331756A1 (en) 2016-11-17
CA2776690C (en) 2020-05-12
DK3070077T3 (en) 2019-04-01
KR20120087936A (ko) 2012-08-07
PL2485731T3 (pl) 2017-04-28
EP3070077B1 (en) 2018-11-28
JP2023002840A (ja) 2023-01-10
JP6016635B2 (ja) 2016-10-26
HK1168044A1 (zh) 2013-02-08
AU2016225896C1 (en) 2018-09-13
EP2485731B1 (en) 2016-05-11
DK2485731T3 (en) 2016-08-22
EP2485731A4 (en) 2013-05-22
HUE043536T2 (hu) 2019-08-28
IL295518A (en) 2022-10-01
EP2485731A1 (en) 2012-08-15
AU2016225896A1 (en) 2016-09-29
MX353257B (es) 2018-01-05
SI2485731T1 (sl) 2016-09-30
KR20170142992A (ko) 2017-12-28
KR101947307B1 (ko) 2019-02-12
IL218915A0 (en) 2012-06-28
JP2018145196A (ja) 2018-09-20
IL218915B (en) 2019-05-30
US20210070752A1 (en) 2021-03-11
RU2012118667A (ru) 2013-11-20
TWI525093B (zh) 2016-03-11
HRP20160967T1 (hr) 2016-10-07
CN102665718A (zh) 2012-09-12
IL295518B2 (en) 2023-11-01
ES2586856T3 (es) 2016-10-19
PL2485731T4 (pl) 2017-07-31
CA2776690A1 (en) 2011-04-14
IL266563B (en) 2022-09-01
AU2018222943A1 (en) 2018-09-20
US20230113598A1 (en) 2023-04-13
ES2712875T3 (es) 2019-05-16
AU2016225896B2 (en) 2018-06-07
PT2485731T (pt) 2016-08-17

Similar Documents

Publication Publication Date Title
BR112012007747B8 (pt) compostos heterocíclicos úteis como inibidores de pdk1, sua composição farmacêutica e seus usos
CY1121144T1 (el) Ετεροκυκλικες ενωσεις και χρησεις αυτων
PH12017501306A1 (en) Inhibitors of histone demethylases
CR20130487A (es) 1,3-oxazinas como inhibidores de BACE1 y/o BACE2
IN2012DN00971A (pt)
BRPI0917017B8 (pt) inibidores de pirrol de s-nitrosoglutationa redutase como agentes terapêuticos
PA8842101A1 (es) Heteroarilos sustituidos
BRPI0808775A2 (pt) compostos e composições como moduladores de atividade de gpr119
UA118177C2 (uk) Композиція для лікування гіперліпідемії, яка містить похідну оксинтомодуліну
EA201170963A1 (ru) Ингибиторы поли(адф-рибозо)полимеразы (parp)
TN2013000348A1 (en) Compounds and compositions as trk inhibitors
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201200551A1 (ru) Фармацевтическая композиция, фармацевтическая дозированная форма, способы их получения и применения для лечения
BRPI0916286B8 (pt) amidofenóxi-indazóis úteis como inibidores de c-met, seus usos, e composição farmacêutica
ECSP11011306A (es) Derivados de benzofuranilo
BR112014021531A2 (pt) composto, composição farmacêutica e usos dos mesmos
GEP20156347B (en) Benzodioxane inhibitors of leukotriene production
EA201170531A1 (ru) Соединения на основе пиридина и пиримидина в качестве ингибиторов сигнального пути wnt для лечения рака
EA201200323A1 (ru) Соединения и композиции, как ингибиторы протеинкиназы
EA201170832A1 (ru) Пуриновые соединения
DK2243772T3 (da) Hidtil ukendte P2X7R-antagonister og deres anvendelse
TN2011000647A1 (en) Fused imidazoles and compositions comprising them for the treatment of parasitic diseases such as e.g. malaria
EA201200570A1 (ru) Соединения и композиции в качестве модуляторов активности gpr119
IN2014CN03597A (pt)
IN2015DN01151A (pt)

Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 10/11/2020, OBSERVADAS AS CONDICOES LEGAIS.

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 05/10/2010 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF