[go: up one dir, main page]

MX353257B - Compuestos heterociclicos utiles como inhibidores de proteina cinasa-1 dependiente de 3-fosfoinositido (pdk1). - Google Patents

Compuestos heterociclicos utiles como inhibidores de proteina cinasa-1 dependiente de 3-fosfoinositido (pdk1).

Info

Publication number
MX353257B
MX353257B MX2012004114A MX2012004114A MX353257B MX 353257 B MX353257 B MX 353257B MX 2012004114 A MX2012004114 A MX 2012004114A MX 2012004114 A MX2012004114 A MX 2012004114A MX 353257 B MX353257 B MX 353257B
Authority
MX
Mexico
Prior art keywords
compounds useful
heterocyclic compounds
pdk1 inhibitors
pdk1
inhibitors
Prior art date
Application number
MX2012004114A
Other languages
English (en)
Other versions
MX2012004114A (es
Inventor
Lee Wen-Cherng
Sun Lihong
Guckian Kevin
Scott Daniel
Yin-Shiang-Lin Edward
Chan Timothy
Thomas Jermaine
Kumaravel Gnanasambandam
Arndt Joseph
Van Vloten Kurt
Wang Deping
Zhang Lei
Erlanson Daniel
Original Assignee
Millennium Pharmaceuticals Inc Star
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 Pharmaceuticals Inc Star filed Critical Millennium Pharmaceuticals Inc Star
Publication of MX2012004114A publication Critical patent/MX2012004114A/es
Publication of MX353257B publication Critical patent/MX353257B/es

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/452—Piperidinium derivatives
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—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
    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon 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
    • C07D241/28—Carbon 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
    • 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
    • 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
    • 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
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • 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
    • A61K31/53—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
    • 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
    • C07D403/14—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Treating Waste Gases (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La presente invención proporciona compuestos útiles como inhibidores de PDK1. La presente invención también proporciona composiciones de los mismos, y métodos para tratar enfermedades mediadas por PDK1.
MX2012004114A 2009-10-06 2010-10-05 Compuestos heterociclicos utiles como inhibidores de proteina cinasa-1 dependiente de 3-fosfoinositido (pdk1). MX353257B (es)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
MX2012004114A MX2012004114A (es) 2012-08-23
MX353257B true MX353257B (es) 2018-01-05

Family

ID=43857093

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012004114A MX353257B (es) 2009-10-06 2010-10-05 Compuestos heterociclicos utiles como inhibidores de proteina cinasa-1 dependiente de 3-fosfoinositido (pdk1).

Country Status (28)

Country Link
US (6) US9546165B2 (es)
EP (3) EP2485731B1 (es)
JP (5) JP6016635B2 (es)
KR (3) KR20120087936A (es)
CN (1) CN102665718B (es)
AR (2) AR078540A1 (es)
AU (3) AU2010303567B2 (es)
BR (1) BR112012007747B8 (es)
CA (1) CA2776690C (es)
CY (1) CY1118143T1 (es)
DK (2) DK2485731T3 (es)
ES (2) ES2586856T3 (es)
HK (1) HK1168044A1 (es)
HR (1) HRP20160967T1 (es)
HU (2) HUE028082T2 (es)
IL (4) IL266563B (es)
IN (1) IN2012DN03883A (es)
LT (1) LT2485731T (es)
MX (1) MX353257B (es)
PH (1) PH12012500674A1 (es)
PL (1) PL2485731T4 (es)
PT (1) PT2485731T (es)
RS (1) RS55101B1 (es)
RU (2) RU2615130C2 (es)
SI (1) SI2485731T1 (es)
SM (1) SMT201600275B (es)
TW (1) TWI525093B (es)
WO (1) WO2011044157A1 (es)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2376485T (pt) 2008-12-19 2018-03-12 Vertex Pharma Derivados de pirazina úteis como inibidores da cinase atr
MX353257B (es) 2009-10-06 2018-01-05 Millennium Pharmaceuticals Inc Star Compuestos heterociclicos utiles como inhibidores de proteina cinasa-1 dependiente de 3-fosfoinositido (pdk1).
EP2569287B1 (en) 2010-05-12 2014-07-09 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
WO2011143423A2 (en) * 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2595965B1 (en) 2010-07-20 2016-06-22 Vestaron Corporation Insecticidal triazines and pyrimidines
JP5634609B2 (ja) * 2010-09-16 2014-12-03 ハチソン メディファーマ リミテッド 縮合ヘテロアリールおよびその使用
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
WO2012149106A1 (en) 2011-04-29 2012-11-01 The Board Of Trustees Of The Leland Stanford Junior University Compositions and methods for increasing proliferation of adult salivary stem cells
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
EP2751097A2 (en) 2011-09-30 2014-07-09 Vertex Pharmaceuticals Incorporated Processes for making compounds useful as inhibitors of atr kinase
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
CA2869730A1 (en) 2012-04-25 2013-10-31 Takeda Pharmaceutical Company Limited Nitrogenated heterocyclic compound
EP2846803B1 (en) * 2012-05-08 2017-06-21 Alpharmagen, LLC Alpha 7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
JP6205356B2 (ja) 2012-07-13 2017-09-27 武田薬品工業株式会社 複素環化合物
EP2900673A4 (en) 2012-09-26 2016-10-19 Univ California IRE1 MODULATION
EP2904406B1 (en) 2012-10-04 2018-03-21 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
WO2014160185A2 (en) * 2013-03-14 2014-10-02 The Board Of Trustees Of The Leland Stanford Junior University Mitochondrial aldehyde dehydrogenase-2 modulators and methods of use thereof
JP6280912B2 (ja) 2013-03-14 2018-02-14 武田薬品工業株式会社 複素環化合物
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
EP3018126A4 (en) 2013-07-03 2016-12-07 Takeda Pharmaceuticals Co HETEROCYCLIC CONNECTION
ES2950424T3 (es) 2013-07-03 2023-10-09 Takeda Pharmaceuticals Co Compuesto de amida
JPWO2015012328A1 (ja) 2013-07-24 2017-03-02 武田薬品工業株式会社 複素環化合物
CA2927567C (en) 2013-10-18 2022-04-26 Celgene Quanticel Research, Inc. Bromodomain inhibitors
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
JP6502939B2 (ja) 2013-11-22 2019-04-17 シーエル バイオサイエンシズ リミティド ライアビリティ カンパニー 骨粗鬆症の処置及び予防のためのガストリン拮抗薬
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
MX2017006366A (es) 2014-11-14 2018-02-01 Nerviano Medical Sciences Srl Derivados de 6-amino-7-biciclo-7-deaza-purina como inhibidores de la proteina quinasa.
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 COMBINATION THERAPY WITH 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
EP3350178B1 (en) * 2015-09-14 2021-10-20 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
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
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
RU2018118786A (ru) * 2015-10-23 2019-11-26 Санесис Фармасьютикалз, Инк. Гетероциклические ингибиторы pdk1 для применения для лечения рака
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
HRP20231614T1 (hr) 2016-03-28 2024-03-15 Incyte Corporation Spojevi pirolotriazina kao tam inhibitori
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
AU2017315343A1 (en) 2016-08-24 2019-02-28 Arqule, Inc. Amino-pyrrolopyrimidinone compounds and methods of use thereof
ES2981507T3 (es) 2016-12-22 2024-10-09 Global Blood Therapeutics Inc Inhibidores de histonas metiltransferasa
EP3594249A4 (en) * 2017-03-10 2020-11-11 Otsuka Chemical Co., Ltd. REACTION PRODUCT AND RUBBER COMPOSITION
MX2019014759A (es) * 2017-06-09 2020-02-12 Global Blood Therapeutics Inc Compuestos de azaindol como inhibidores de metiltransferasa de histona.
US20190175589A1 (en) * 2017-11-09 2019-06-13 Sunesis Pharmaceuticals, Inc. Pharmaceutical formulations, processes for preparation, and methods of use
SG11202007035YA (en) 2018-01-26 2020-08-28 Bristol Myers Squibb Co Aminopyrrolotriazines as kinase inhibitors
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
US11780857B2 (en) * 2019-04-17 2023-10-10 EWHA University—Industry Collaboration Foundation Probe compounds for amino alcohols, and simultaneous fluorescence and circular dichroism analysis method
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
KR20210064093A (ko) * 2019-11-25 2021-06-02 주식회사 대웅제약 신규한 트리아졸로피리딘 유도체 및 이를 포함하는 약학 조성물
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
JP2594486B2 (ja) 1991-01-15 1997-03-26 アルコン ラボラトリーズ インコーポレイテッド 局所的眼薬組成物
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
CA2358095A1 (en) * 1998-12-23 2000-07-06 Eli Lilly And Company Heteroroaromatic amides as inhibitor of factor xa
WO2000039111A1 (en) 1998-12-23 2000-07-06 Eli Lilly And Company Antithrombotic amides
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
AU2004255342C1 (en) 2003-07-08 2009-05-14 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
EP1891047A4 (en) 2005-06-03 2008-07-09 Bayer Healthcare Ag A 1-METHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID SUITABLE FOR THE CHEMOTHERAPY OF CANCER
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
ES2401099T3 (es) 2005-11-02 2013-04-16 Bayer Intellectual Property Gmbh Pirrolo[2,1-F] [1,2,4]-triazin-4-ilaminas como inhibidores de la quinasa IGF-1R para el tratamiento del cáncer y de otras enfermedades hiperproliferativas
EP1979353A2 (en) 2006-01-19 2008-10-15 OSI Pharmaceuticals, Inc. Fused heterobicyclic kinase inhibitors
JP5523829B2 (ja) 2006-06-29 2014-06-18 アステックス、セラピューティックス、リミテッド 複合薬剤
US8778977B2 (en) 2006-06-30 2014-07-15 Sunesis Pharmaceuticals, Inc. Pyridinonyl PDK1 inhibitors
WO2008016643A2 (en) 2006-08-01 2008-02-07 Cytokinetics, Incorporated Certain chemical entities, compositions, and methods
CA2672440A1 (en) * 2006-12-20 2008-07-03 Amgen Inc. Substituted heterocycles and methods of use
WO2008118455A1 (en) * 2007-03-23 2008-10-02 Amgen Inc. δ3- SUBSTITUTED QUINOLINE OR QUINOXALINE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE ( PI3K) INHIBITORS
ES2395581T3 (es) * 2007-06-20 2013-02-13 Merck Sharp & Dohme Corp. Inhibidores de quinasas janus
US7868001B2 (en) 2007-11-02 2011-01-11 Hutchison Medipharma Enterprises Limited Cytokine inhibitors
WO2010144345A1 (en) * 2009-06-08 2010-12-16 Abraxis Bioscience, Llc Triazine derivatives and their therapeutical applications
MX353257B (es) 2009-10-06 2018-01-05 Millennium Pharmaceuticals Inc Star Compuestos heterociclicos utiles como inhibidores de proteina cinasa-1 dependiente de 3-fosfoinositido (pdk1).

Also Published As

Publication number Publication date
US20120208819A1 (en) 2012-08-16
EP2485731A1 (en) 2012-08-15
HK1168044A1 (zh) 2013-02-08
US10030016B2 (en) 2018-07-24
IL218915B (en) 2019-05-30
KR20120087936A (ko) 2012-08-07
SI2485731T1 (sl) 2016-09-30
MX2012004114A (es) 2012-08-23
CN102665718A (zh) 2012-09-12
IL218915A0 (en) 2012-06-28
US20190119268A1 (en) 2019-04-25
US20240294524A1 (en) 2024-09-05
BR112012007747B8 (pt) 2021-05-25
TW201124416A (en) 2011-07-16
EP3466929B1 (en) 2023-09-06
AU2016225896B2 (en) 2018-06-07
HUE028082T2 (en) 2016-11-28
EP3466929A1 (en) 2019-04-10
RS55101B1 (sr) 2016-12-30
EP2485731A4 (en) 2013-05-22
PL2485731T4 (pl) 2017-07-31
IL295518B2 (en) 2023-11-01
EP3070077B1 (en) 2018-11-28
KR101947307B1 (ko) 2019-02-12
LT2485731T (lt) 2016-09-12
IN2012DN03883A (es) 2015-09-25
CN102665718B (zh) 2016-03-09
US9546165B2 (en) 2017-01-17
ES2712875T3 (es) 2019-05-16
ES2586856T3 (es) 2016-10-19
IL302896A (en) 2023-07-01
EP3070077A1 (en) 2016-09-21
AU2016225896A1 (en) 2016-09-29
RU2615130C2 (ru) 2017-04-04
JP2016188253A (ja) 2016-11-04
JP2023002840A (ja) 2023-01-10
JP6016635B2 (ja) 2016-10-26
IL266563A (en) 2019-07-31
AR124483A2 (es) 2023-03-29
RU2012118667A (ru) 2013-11-20
BR112012007747A2 (pt) 2017-09-05
DK3070077T3 (en) 2019-04-01
US20230113598A1 (en) 2023-04-13
AU2010303567B2 (en) 2016-06-09
BR112012007747B1 (pt) 2020-11-10
HUE043536T2 (hu) 2019-08-28
IL295518A (en) 2022-10-01
KR20190025680A (ko) 2019-03-11
AU2016225896C1 (en) 2018-09-13
TWI525093B (zh) 2016-03-11
JP2020203925A (ja) 2020-12-24
PH12012500674A1 (en) 2016-06-15
JP2013506715A (ja) 2013-02-28
KR102097664B1 (ko) 2020-04-06
AU2018222943A1 (en) 2018-09-20
US20210070752A1 (en) 2021-03-11
CY1118143T1 (el) 2017-06-28
RU2017109664A (ru) 2019-01-23
JP2018145196A (ja) 2018-09-20
AU2018222943B2 (en) 2019-09-26
SMT201600275B (it) 2016-11-10
CA2776690C (en) 2020-05-12
HRP20160967T1 (hr) 2016-10-07
KR20170142992A (ko) 2017-12-28
US20160331756A1 (en) 2016-11-17
IL266563B (en) 2022-09-01
AU2010303567A1 (en) 2012-05-03
PT2485731T (pt) 2016-08-17
WO2011044157A1 (en) 2011-04-14
RU2017109664A3 (es) 2020-07-15
AR078540A1 (es) 2011-11-16
CA2776690A1 (en) 2011-04-14
PL2485731T3 (pl) 2017-04-28
IL295518B1 (en) 2023-07-01
EP2485731B1 (en) 2016-05-11
DK2485731T3 (en) 2016-08-22

Similar Documents

Publication Publication Date Title
PH12012500674A1 (en) Heterocyclic compounds useful as pdk1 inhibitors
SG179085A1 (en) Pi3 kinase inhibitors and uses thereof
MY181898A (en) Heterocyclic compounds and uses thereof
TW201713640A (en) Bruton's tyrosine kinase inhibitors
MX2012004780A (es) Inhibidores de akt.
UA101478C2 (ru) Соединения, полезные как ингибиторы raf-киназы
TN2011000673A1 (en) Bace inhibitors
EA201200323A1 (ru) Соединения и композиции, как ингибиторы протеинкиназы
CA2871471C (en) Dna-pk inhibitors
MY153915A (en) Organic compounds
PT2470546E (pt) Compostos de hexa-hidrooxazinopteridina para serem utilizados como inibidores de mtor
MX2012000709A (es) Inhibidores de pirrolopiridina de cinasas.
PH12012501346A1 (en) Heteroaryl compounds and uses thereof
MY150542A (en) Cmet inhibitors
MX2009006627A (es) Quinazolinas para la inhibicion de pdk1.
JO2788B1 (en) Amido phenoxyendazole compounds beneficial as C-MET inhibitors
MX2011014019A (es) Derivados de diazahomoadamantano y sus metodos de uso.
IN2012DN00971A (es)
MX2009010960A (es) Compuestos heterociclicos y sus metodos de uso.
MX341456B (es) Amino-quinolinas como inhibidores de cinasa.
MX2013002851A (es) Inhibidores de tonum pectinacetilesterasa y metodos de su uso.
MY150600A (en) Use of opioid antagonists for treating urinary retention
EA201170447A1 (ru) Производные изохинолинона в качестве антагонистов nk3
MX2011010046A (es) Derivados de diaminopteridina.
MX2009012079A (es) Compuestos heterociclicos condensados como inhibidores de proteina cinasas.

Legal Events

Date Code Title Description
FG Grant or registration