ATE520403T1 - N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs - Google Patents

N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs

Info

Publication number
ATE520403T1
ATE520403T1 AT10160517T AT10160517T ATE520403T1 AT E520403 T1 ATE520403 T1 AT E520403T1 AT 10160517 T AT10160517 T AT 10160517T AT 10160517 T AT10160517 T AT 10160517T AT E520403 T1 ATE520403 T1 AT E520403T1
Authority
AT
Austria
Prior art keywords
compounds
ylüoxy
phenylü
oxyüquinolin
ylpropyl
Prior art date
Application number
AT10160517T
Other languages
English (en)
Inventor
Lynne Canne Bannen
Diva Sze-Ming Chan
Jeff Chen
Lisa Esther Dalrymple
Timothy Patrick Forsyth
Tai Phat Huynh
Vasu Jammalamadaka
Richard George Khoury
James William Leahy
Morrison B Mac
Grace Mann
Larry W Mann
John M Nuss
Jason Jevious Parks
Craig Stacy Takeuchi
Yong Wang
Wei Xu
Original Assignee
Exelixis 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34397024&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE520403(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Exelixis Inc filed Critical Exelixis Inc
Application granted granted Critical
Publication of ATE520403T1 publication Critical patent/ATE520403T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/233Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • 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
    • 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
    • A61K31/4709Non-condensed quinolines and 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
    • A61K31/435Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and 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
    • A61K31/505Pyrimidines; 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/505Pyrimidines; 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
    • A61K31/535Heterocyclic 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/36Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • C07D215/46Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00Screening for compounds of potential therapeutic value
    • G01N2500/04Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • General Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Microbiology (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
AT10160517T 2003-09-26 2004-09-24 N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs ATE520403T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US50618103P 2003-09-26 2003-09-26
US53537704P 2004-01-09 2004-01-09
US57738404P 2004-06-04 2004-06-04

Publications (1)

Publication Number Publication Date
ATE520403T1 true ATE520403T1 (de) 2011-09-15

Family

ID=34397024

Family Applications (3)

Application Number Title Priority Date Filing Date
AT04789057T ATE532782T1 (de) 2003-09-26 2004-09-24 C-met-modulatoren und anwendungsverfahren
AT10160518T ATE517091T1 (de) 2003-09-26 2004-09-24 C-met-modulatoren und verwendungsverfahren
AT10160517T ATE520403T1 (de) 2003-09-26 2004-09-24 N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs

Family Applications Before (2)

Application Number Title Priority Date Filing Date
AT04789057T ATE532782T1 (de) 2003-09-26 2004-09-24 C-met-modulatoren und anwendungsverfahren
AT10160518T ATE517091T1 (de) 2003-09-26 2004-09-24 C-met-modulatoren und verwendungsverfahren

Country Status (19)

Country Link
US (14) US9174947B2 (de)
EP (9) EP2392564B1 (de)
JP (14) JP4638436B2 (de)
AT (3) ATE532782T1 (de)
AU (3) AU2004275842B2 (de)
BE (1) BE2014C055I2 (de)
CA (2) CA2744997A1 (de)
CY (3) CY1111956T1 (de)
DK (4) DK2213661T3 (de)
ES (6) ES2651730T3 (de)
FR (1) FR14C0067I2 (de)
HR (4) HRP20110707T1 (de)
HU (1) HUS1400052I1 (de)
LU (1) LU92508I2 (de)
NL (1) NL300678I2 (de)
PL (3) PL2213661T3 (de)
PT (2) PT2210607E (de)
SI (4) SI2392564T1 (de)
WO (1) WO2005030140A2 (de)

Families Citing this family (281)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3366959B2 (ja) 1998-06-19 2003-01-14 三洋昭和パネルシステム株式会社 高さ調整自在な幅木
EP1506962B1 (de) 2000-10-20 2008-07-02 Eisai R&D Management Co., Ltd. Stickstoff enthaltende aromatische Heterozyklen
JPWO2004080462A1 (ja) 2003-03-10 2006-06-08 エーザイ株式会社 c−Kitキナーゼ阻害剤
PL1667992T3 (pl) 2003-09-19 2007-05-31 Astrazeneca Ab Pochodne chinazoliny
ES2651730T3 (es) * 2003-09-26 2018-01-29 Exelixis, Inc. Moduladores c-Met y métodos de uso
JP4303726B2 (ja) 2003-11-11 2009-07-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 ウレア誘導体およびその製造方法
EP1684762A4 (de) * 2003-11-13 2009-06-17 Ambit Biosciences Corp Harnstoff-derivate als kinase-modulatoren
EP1711495A2 (de) * 2004-01-23 2006-10-18 Amgen Inc. Chinolin-, chinazolin-, pyridin- und pyrimidinverbindungen und deren verwendung bei der behandlung von entzündungen, angiogenese und krebs
JPWO2005082855A1 (ja) 2004-02-27 2007-10-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規ピリジン誘導体およびピリミジン誘導体(2)
NZ551027A (en) 2004-04-08 2011-01-28 Targegen Inc Benzotriazine inhibitors of kinases
US7459562B2 (en) 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
TW200538453A (en) 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
US7432373B2 (en) 2004-06-28 2008-10-07 Bristol-Meyers Squibb Company Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors
US20050288290A1 (en) 2004-06-28 2005-12-29 Borzilleri Robert M Fused heterocyclic kinase inhibitors
US7439246B2 (en) 2004-06-28 2008-10-21 Bristol-Myers Squibb Company Fused heterocyclic kinase inhibitors
MX2007002208A (es) 2004-08-25 2007-05-08 Targegen Inc Compuestos hetrociclicos y metodos de uso.
US8969379B2 (en) 2004-09-17 2015-03-03 Eisai R&D Management Co., Ltd. Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7=methoxy-6-quinolinecarboxide
AU2005286728A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
BRPI0515483A (pt) 2004-09-20 2008-07-22 Xenon Pharmaceuticals Inc derivados heterocìclicos para o tratamento de doenças mediadas por enzimas estearoil-coa desaturase
CN101084211A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为治疗剂的用途
CA2580855A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
WO2006034441A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
JP4958785B2 (ja) 2004-09-20 2012-06-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド 複素環誘導体およびステアロイル−CoAデサチュラーゼインヒビターとしてのそれらの使用
TW200626155A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
WO2006040520A1 (en) 2004-10-12 2006-04-20 Astrazeneca Ab Quinazoline derivatives
MX2007006230A (es) * 2004-11-30 2007-07-25 Amgen Inc Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer.
EP1674466A1 (de) * 2004-12-27 2006-06-28 4Sc Ag 2,5- und 2-6-disubstituierte Benzazol-Derivate zur Verwendung als Protein Kinase Inhibitoren
US7576090B2 (en) * 2004-12-27 2009-08-18 4Sc Ag Benzazole analogues and uses thereof
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
EP1957498B1 (de) * 2005-05-20 2017-02-15 MethylGene Inc. Vegf- und hgf-rezeptorensignalisierungshemmer
MX2007015056A (es) * 2005-06-02 2008-03-11 Galaxy Biotech Llc Metodos para el tratamiento de tumores de cerebro con anticuerpos.
WO2007130075A1 (en) 2005-06-03 2007-11-15 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
WO2007015578A1 (ja) 2005-08-02 2007-02-08 Eisai R & D Management Co., Ltd. 血管新生阻害物質の効果を検定する方法
ES2424651T3 (es) 2005-08-24 2013-10-07 Eisai R&D Management Co., Ltd. Nuevo derivado de piridina y derivado de pirimidina (3)
TWI387592B (zh) 2005-08-30 2013-03-01 Novartis Ag 經取代之苯并咪唑及其作為與腫瘤形成相關激酶之抑制劑之方法
WO2007033196A1 (en) 2005-09-14 2007-03-22 Bristol-Myers Squibb Company Met kinase inhibitors
WO2007061127A1 (ja) * 2005-11-22 2007-05-31 Eisai R & D Management Co., Ltd. 多発性骨髄腫に対する抗腫瘍剤
US8003662B2 (en) * 2006-01-30 2011-08-23 Array Biopharma, Inc. Heterobicyclic thiophene compounds and methods of use
UY30183A1 (es) 2006-03-02 2007-10-31 Astrazeneca Ab Derivados de quinolina
JP2009529047A (ja) 2006-03-07 2009-08-13 アレイ バイオファーマ、インコーポレイテッド ヘテロ二環系ピラゾール化合物およびその使用
AR059922A1 (es) * 2006-04-01 2008-05-07 Galaxy Biotech Llc Anticuerpos monoclonales humanizados para el factor de crecimiento de hepatocitos
MX2008013427A (es) 2006-04-19 2008-11-04 Novartis Ag Compuestos de benzoxazole y benzotiazole sustituidos-6-0 y metodos para inhibir la señalizacion csf-1r.
CA2652442C (en) 2006-05-18 2014-12-09 Eisai R & D Management Co., Ltd. Antitumor agent for thyroid cancer
MX2008014672A (es) 2006-05-19 2009-03-09 Abbott Lab Derivados de alcano azabiciclico sustituidos con bicicloheterociclo fusionado activos en el sistema nervioso central.
US20080004273A1 (en) * 2006-05-30 2008-01-03 Stephane Raeppel Inhibitors of protein tyrosine kinase activity
EP2032538A2 (de) * 2006-06-08 2009-03-11 Array Biopharma, Inc. Chinolinverbindungen und anwendungsverfahren dafür
JP2010500365A (ja) 2006-08-07 2010-01-07 インサイト・コーポレイション キナーゼ阻害剤としてのトリアゾロトリアジン
AU2007288793B2 (en) 2006-08-23 2012-04-19 Eisai R & D Management Co., Ltd. Salt of phenoxypyridine derivative or crystal thereof and process for producing the same
EP2065372B1 (de) 2006-08-28 2012-11-28 Eisai R&D Management Co., Ltd. Antitumormittel gegen undifferenzierten magenkrebs
US7790885B2 (en) 2006-08-31 2010-09-07 Eisai R&D Management Co., Ltd. Process for preparing phenoxypyridine derivatives
ES2633318T3 (es) 2006-10-23 2017-09-20 Cephalon, Inc. Derivados bicíclicos fusionados de 2,4-diaminopirimidina como inhibidores de ALK y c-Met
WO2008049855A2 (en) * 2006-10-27 2008-05-02 Glaxo Group Limited 7-azaindole derivatives as c-met kinase inhibitors
BRPI0719333A2 (pt) 2006-11-22 2014-02-04 Incyte Corp Midazotriazinas e imidazopirimidinas como inbidores de cinase
US7915287B2 (en) * 2006-12-20 2011-03-29 Amgen Inc. Substituted heterocycles and methods of use
US7687522B2 (en) 2006-12-20 2010-03-30 Amgen Inc. Substituted pyridines and pyrimidines and their use in treatment of cancer
ES2531002T3 (es) * 2007-01-19 2015-03-09 Xcovery Inc Compuestos inhibidores de quinasa
US8962655B2 (en) 2007-01-29 2015-02-24 Eisai R&D Management Co., Ltd. Composition for treatment of undifferentiated gastric cancer
US8293769B2 (en) * 2007-05-21 2012-10-23 Novartis Ag CSF-1R inhibitors, compositions, and methods of use
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
WO2009021965A2 (en) 2007-08-15 2009-02-19 Glaxo Group Limited Substituted quinoline derivatives as h1 receptor antagonists
AU2008293038B2 (en) 2007-08-29 2013-08-29 Mirati Therapeutics, Inc. Inhibitors of protein tyrosine kinase activity
CN101848895B (zh) 2007-11-09 2013-10-23 卫材R&D管理有限公司 血管新生抑制物质和抗肿瘤性铂络合物的组合使用
JP2009132660A (ja) 2007-11-30 2009-06-18 Eisai R & D Management Co Ltd 食道癌治療用組成物
CN101977905B (zh) 2008-01-23 2014-07-02 百时美施贵宝公司 4-吡啶酮化合物及其对于癌症的用途
PT2947072T (pt) 2008-03-17 2016-12-06 Ambit Biosciences Corp 1-(3-(6,7-dimetoxiquinazolin-4-iloxi)fenil)-3-(5-(1,1,1-trifluoro-2-metilpropan-2-il)isoxazol-3-il)ureia como modulador da cinase raf no tratamento de doenças oncológicas
PT2287155E (pt) 2008-04-10 2013-07-26 Taiho Pharmaceutical Co Ltd Composto de aciltioureia ou um seu sal, e sua utilização
EP2262772B8 (de) 2008-04-16 2013-03-13 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Chinolinderivate als axl-kinase-inhibitoren
UY31800A (es) * 2008-05-05 2009-11-10 Smithkline Beckman Corp Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb
BRPI0912882A2 (pt) 2008-05-21 2017-05-16 Incyte Corp sais de 2-flúor-n-metil-4-[7-(quinolin-6-il-metil)-imidazo[1,2-b][1,2,4]triazin-2-il]benzamida e processos relacionados à preparação dos mesmos
CA2728228A1 (en) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
NZ590320A (en) 2008-07-14 2012-12-21 Gilead Sciences Inc Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
JP5640005B2 (ja) 2008-07-14 2014-12-10 ギリアード サイエンシーズ, インコーポレイテッド Hdacおよび/またはcdk阻害剤としてのイミダゾシルピリジン化合物
EP2149565A1 (de) * 2008-07-24 2010-02-03 Bayer Schering Pharma AG Sulfonsubstituierte Chinazolinderivate als Immunmodulatoren zur Behandlung von enzündlichen und allergischen Erkrankungen
MX2011001090A (es) 2008-07-28 2011-03-15 Gilead Sciences Inc Compuestos de inhibidor de desacetilasa de histona de cicloalquilideno y heterocicloalquilideno.
AR075084A1 (es) * 2008-09-26 2011-03-09 Smithkline Beecham Corp Metodo de preparacion de quinolinil -oxidifenil - ciclopropanodicarboxamidas e intermediarios correspondientes
US8293897B2 (en) * 2008-10-14 2012-10-23 Ning Xi Compounds comprising a spiro-ring and methods of use
KR20110099687A (ko) * 2008-10-29 2011-09-08 데시페라 파마슈티칼스, 엘엘씨. 항-암과 항-증식성 활성을 나타내는 시클로프로판 아미드와 유사체
EP2350011A1 (de) * 2008-11-13 2011-08-03 Exelixis, Inc. Verfahren zur herstellung von chinolinderivaten
EP2367795A1 (de) * 2008-12-04 2011-09-28 Exelixis, Inc. Verfahren zur herstellung von chinolinderivaten
DE102009003975A1 (de) 2009-01-07 2010-07-08 Merck Patent Gmbh Benzothiazolonderivate
CA2758030C (en) * 2009-01-16 2019-01-08 Exelixis, Inc. Malate salt of n-(4-{[6,7-bis(methyloxy)quin0lin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer
EP2210891A1 (de) * 2009-01-26 2010-07-28 Domain Therapeutics Neue Adenosin-Rezeptorliganden und Verwendungen davon
CA2752421C (en) * 2009-03-21 2013-08-06 Ning Xi Amino ester derivatives, salts thereof and methods of use
KR20120061063A (ko) 2009-06-05 2012-06-12 화이자 인코포레이티드 Gpr 119 조절제로서의 l-(피페리딘-4-일)-피라졸 유도체
MX2011013166A (es) 2009-06-08 2012-01-30 Gilead Sciences Inc Compuestos inhibidores de hdac de cicloalquilcarbamatobenzamida-an ilina.
WO2010144371A1 (en) 2009-06-08 2010-12-16 Gilead Colorado, Inc. Alkanoylamino benzamide aniline hdac inihibitor compounds
WO2011009095A1 (en) * 2009-07-17 2011-01-20 Exelixis, Inc. Crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quin0lin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide
UA108618C2 (uk) * 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
CN102030705B (zh) * 2009-09-30 2012-12-19 上海睿智化学研究有限公司 7-苄氧基-6-甲氧基-4-羟基喹啉的合成方法
EP2311809A1 (de) * 2009-10-16 2011-04-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Chinolinyloxyphenylsulfonamide
MX2012005155A (es) * 2009-11-03 2012-08-31 Glaxosmithkline Llc Compuestos de quinazolina.
EP2521548A2 (de) * 2009-11-27 2012-11-14 Proteologics, Ltd Chinazolin-4(3a)-on-derivate und verwendungsverfahren dafür
DE102009056886A1 (de) 2009-12-03 2011-06-09 Bayer Schering Pharma Aktiengesellschaft cMet-Inhibitoren zur Behandlung der Endometriose
CN102086211B (zh) * 2009-12-08 2013-09-11 广东东阳光药业有限公司 作为蛋白激酶抑制剂的芳杂环化合物
MX2012008898A (es) 2010-02-03 2012-11-06 Incyte Corp Imidazo - [1, 2 - b] [1, 2, 4] triazinas como inhibidores de c - met.
MX2012010506A (es) * 2010-03-12 2012-10-15 Exelixis Inc Formas cristalinas hidratadas del n-[3-fluoro-4-({6-(metiloxi)-7-[ (3-morfolin-4-ilpropil)oxi]-quinolin-4-il}oxi)fenil]-n'-(4-fluoro fenil)ciclopropano-1,1-dicarboxamida.
EP2553641A4 (de) * 2010-03-26 2015-01-07 EastNets Mobiles computerüberweisungssystem und -verfahren
CN102212062B (zh) * 2010-04-02 2015-04-29 广东东阳光药业有限公司 氨基酯类衍生物及其盐和使用方法
US20120070368A1 (en) * 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
EP2560488B1 (de) 2010-04-23 2015-10-28 Cytokinetics, Inc. Bestimmte aminopyrimidine und aminotriazine, zusammensetzungen daraus und verfahren zu ihrer verwendung
WO2011139891A1 (en) 2010-04-29 2011-11-10 Deciphera Pharmaceuticals, Llc Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activites
EP2571878B1 (de) 2010-05-17 2018-10-17 Incozen Therapeutics Pvt. Ltd. Neuartige 3,5-disubstituierte-3h-imidazo[4,5-b]pyridin- und 3,5- disubstituierte -3h-[1,2,3]triazol[4,5-b]pyridin- verbindungen als proteinkinasemodulatoren
ES2573515T3 (es) 2010-06-25 2016-06-08 Eisai R&D Management Co., Ltd. Agente antitumoral que emplea compuestos con efecto inhibitorio de cinasas combinados
WO2012003338A1 (en) 2010-07-01 2012-01-05 Takeda Pharmaceutical Company Limited COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET
TWI619495B (zh) 2010-07-16 2018-04-01 艾克塞里克斯公司 C-met調節劑醫藥組合物
WO2012009723A1 (en) 2010-07-16 2012-01-19 Exelixis, Inc. C-met modulator pharmaceutical compositions
EP2423208A1 (de) 2010-08-28 2012-02-29 Lead Discovery Center GmbH Pharmazeutisch aktive Zusammensetzungen als Axl-Hemmer
US8664244B2 (en) * 2010-09-12 2014-03-04 Advenchen Pharmaceuticals, LLC Compounds as c-Met kinase inhibitors
WO2012044574A1 (en) 2010-09-27 2012-04-05 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
US20140057908A1 (en) * 2010-09-27 2014-02-27 Exelixis, Inc. Method of Treating Cancer
EP2621481B2 (de) * 2010-09-27 2022-10-19 Exelixis, Inc. Met- und vegf-doppelinhibitoren zur behandlung von kastrationsresistentem prostatakrebs und osteoblastischen knochenmetastasen
WO2012042421A1 (en) 2010-09-29 2012-04-05 Pfizer Inc. Method of treating abnormal cell growth
WO2012071321A1 (en) * 2010-11-22 2012-05-31 Glaxosmithkline Llc Method of treating cancer
CN102093421B (zh) 2011-01-28 2014-07-02 北京康辰药业有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
CA2826751C (en) 2011-02-10 2021-05-18 Exelixis, Inc. Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
ES2609578T3 (es) 2011-03-04 2017-04-21 Glaxosmithkline Intellectual Property Development Limited Amino-quinolinas como inhibidores de quinasa
US20120252840A1 (en) * 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
MX2013009931A (es) 2011-04-18 2013-10-01 Eisai R&D Man Co Ltd Agentes terapeuticos contra tumores.
US8759380B2 (en) 2011-04-22 2014-06-24 Cytokinetics, Inc. Certain heterocycles, compositions thereof, and methods for their use
MX2013012695A (es) 2011-05-02 2014-03-27 Exelixis Inc Metodo para el tratamiento del cancer y el dolor por cancer de hueso.
EP2714937B1 (de) 2011-06-03 2018-11-14 Eisai R&D Management Co., Ltd. Biomarker zur vorhersage und beurteilung des ansprechens von schilddrüsen- und nierenkrebspatienten auf lenvatinibverbindungen
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
US9309237B2 (en) 2011-09-06 2016-04-12 New York Blood Center, Inc. HIV inhibitors
CN102408411B (zh) * 2011-09-19 2014-10-22 北京康辰药业股份有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
KR20140069133A (ko) 2011-09-22 2014-06-09 엑셀리시스, 인코포레이티드 골다공증의 치료방법
EP2768796B1 (de) * 2011-10-20 2019-11-20 Exelixis, Inc. Verfahren zur herstellung von chinolinderivaten
US8843421B2 (en) 2011-11-01 2014-09-23 Accenture Global Services Limited Identification of entities likely to engage in a behavior
MX2014005458A (es) 2011-11-08 2015-04-16 Exelixis Inc Inhibidor doble de met y del factor de crecimiento endotelial vascular (vegf) para el tratamiento del cáncer.
JP2015505360A (ja) 2011-11-08 2015-02-19 エクセリクシス, インク. 癌治療を定量化する方法
TWI577671B (zh) 2011-11-14 2017-04-11 Sunshine Lake Pharma Co Ltd Aminoquinazoline derivatives and salts thereof and methods of use thereof
US9546179B2 (en) * 2011-12-20 2017-01-17 Wei Qian Heterocycle amido alkyloxy substituted quinazoline derivative and use thereof
CN102643268B (zh) * 2011-12-30 2014-05-21 沈阳药科大学 喹啉类及噌啉类化合物及其应用
EP2620869B1 (de) 2012-01-27 2017-11-01 Optim Corporation Tragbares Endgerät, Verfahren und Programm zum Ändern einer Benutzeroberfläche
US9358235B2 (en) * 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
KR20140144726A (ko) 2012-03-30 2014-12-19 리젠 파마슈티컬스 소시에떼 아노님 C-met 단백질 키나제의 조절제로서의 신규한 3,5-디치환-3h-이미다조[4,5-b]피리딘 및 3,5- 디치환 -3h-[1,2,3]트리아졸로[4,5-b] 피리딘 화합물
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
WO2013166296A1 (en) 2012-05-02 2013-11-07 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
WO2013180128A1 (ja) * 2012-05-28 2013-12-05 協和発酵キリン株式会社 4-[4-(5員環芳香族複素環カルボニルウレイド)フェニルオキシ]キノリン誘導体
CN103509024B (zh) * 2012-06-28 2015-10-28 上海医药工业研究院 嘧啶并苯并氮杂卓类化合物及其作为抗肿瘤药物的应用
CN103626761B (zh) * 2012-08-24 2015-07-29 上海医药工业研究院 苯并吡啶氮杂卓类化合物及其作为抗肿瘤药物的应用
CN103626762B (zh) * 2012-08-24 2015-07-29 上海医药工业研究院 苯并吡啶氮杂卓类化合物及其应用
TWI592417B (zh) 2012-09-13 2017-07-21 葛蘭素史克智慧財產發展有限公司 胺基喹唑啉激酶抑制劑之前藥
TW201425307A (zh) 2012-09-13 2014-07-01 Glaxosmithkline Llc 作為激酶抑制劑之胺基-喹啉類
CN103664776B (zh) * 2012-09-26 2016-05-04 正大天晴药业集团股份有限公司 一种酪氨酸激酶抑制剂及其中间体的制备方法
CN103705521A (zh) * 2012-09-28 2014-04-09 韩冰 一类治疗脑梗塞的化合物及其用途
CN103804382A (zh) * 2012-11-05 2014-05-21 韩文毅 一类治疗湿疹的化合物及其用途
CN102977014B (zh) 2012-11-05 2015-01-07 沈阳药科大学 新的喹啉类化合物及其用途
CN103804305A (zh) * 2012-11-05 2014-05-21 韩文毅 一类治疗湿疹的化合物及其用途
CN103804381A (zh) * 2012-11-06 2014-05-21 韩冰 一类治疗缺血性脑损伤的化合物及其用途
CN103804290A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103800328A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804361A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804291A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804298A (zh) * 2012-11-09 2014-05-21 韩冰 一类治疗青光眼的化合物及其用途
CN103800340A (zh) * 2012-11-09 2014-05-21 韩冰 一类治疗青光眼的化合物及其用途
CN103804362A (zh) * 2012-11-12 2014-05-21 韩文毅 一类治疗糖尿病的化合物及其用途
CN103804306A (zh) * 2012-11-12 2014-05-21 韩文毅 一类治疗糖尿病的化合物及其用途
CN103804363A (zh) * 2012-11-14 2014-05-21 韩冰 一类具有神经保护作用的化合物及其用途
CN102964308B (zh) * 2012-11-30 2015-03-18 中国药科大学 新型嘧啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途
MX2015004979A (es) 2012-12-21 2015-07-17 Eisai R&D Man Co Ltd Forma amorfa de derivado de quinolina y metodo para su produccion.
CN103965104B (zh) * 2013-01-29 2017-09-29 正大天晴药业集团股份有限公司 一种酪氨酸激酶抑制剂及其中间体的制备方法
BR112015019624A2 (pt) 2013-02-21 2017-07-18 Glaxosmithkline Ip Dev Ltd quinazolinas como inibidores de quinase
JP2016510781A (ja) * 2013-03-15 2016-04-11 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft RORcモジュレーターとしてのアリールスルファミド及びスルファミン酸誘導体
BR112015023109A2 (pt) * 2013-03-15 2018-05-15 Exelixis Inc Metabolitos de n-(4-{[6,7-bis(metiloxi)quinoloin-4-il] oxi}fenil)-n -(4-fluorofenil)ciclopropano-1, 1- dicarboxamida
WO2014145693A1 (en) * 2013-03-15 2014-09-18 Exelixis, Inc. Metabolites of n-[3-fluoro-4-({ 6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
JP2016515628A (ja) 2013-04-04 2016-05-30 エグゼリクシス, インコーポレイテッド 癌を治療するための複合薬
WO2014165786A1 (en) 2013-04-04 2014-10-09 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
CN104109128B (zh) * 2013-04-19 2016-10-05 连云港润众制药有限公司 卡博替尼苹果酸盐及其制备方法
CN104109124B (zh) * 2013-04-19 2016-08-31 正大天晴药业集团股份有限公司 卡博替尼·0.5苹果酸盐的晶体
NZ714049A (en) 2013-05-14 2020-05-29 Eisai R&D Man Co Ltd Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
CN104370811B (zh) * 2013-08-15 2019-02-12 广东东阳光药业有限公司 一种喹啉化合物的新晶型及其制备方法
DK3039424T3 (da) 2013-08-28 2020-08-31 Crown Bioscience Inc Taicang Genekspressionssignaturer, der er prædiktive for et individs respons på en multikinaseinhibitor, og fremgangsmåder til anvendelse af disse
CN104628657A (zh) * 2013-11-06 2015-05-20 韩冰 一类治疗缺血性脑损伤的化合物及其用途
CA2939546C (en) 2014-02-14 2023-01-17 Exelixis, Inc. Crystalline solid forms of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
TWI672141B (zh) 2014-02-20 2019-09-21 美商醫科泰生技 投予ros1突變癌細胞之分子
AU2015223835B2 (en) * 2014-02-28 2019-07-11 Fuso Pharmaceutical Industries, Ltd. Amide derivatives
EA201691850A1 (ru) 2014-03-17 2016-12-30 Экселиксис, Инк. Дозирование составов, содержащих кабозантиниб
CN107002119A (zh) 2014-03-24 2017-08-01 豪夫迈·罗氏有限公司 使用c‑met拮抗剂的癌症治疗及前者与hgf表达的关联
BR112016024672A2 (pt) 2014-04-25 2021-02-02 Exelixis, Inc método para o tratamento de adenocarcinoma de pulmão
EP3145913A1 (de) 2014-05-23 2017-03-29 Mylan Laboratories Ltd. Neuartige polymorphe aus cabozantinib-(s)-malat und cabozantinibfreier base
CN104788372B (zh) * 2014-07-25 2018-01-30 上海圣考医药科技有限公司 一种氘代卡博替尼衍生物、其制备方法、应用及其中间体
MA40386A (fr) * 2014-07-31 2016-02-04 Exelixis Inc Procédé de préparation de cabozantinib marqué au fluor-18 et d'analogues de celui-ci
BR112017002318A2 (pt) * 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
CN113683564A (zh) 2014-08-28 2021-11-23 卫材R&D管理有限公司 高纯度喹啉衍生物及其生产方法
EP3194030B1 (de) 2014-09-19 2019-11-06 New York Blood Center, Inc. Substituierte phenylpyrrolecarboxamide mit therapeutischer aktivität bei hiv
KR102595599B1 (ko) 2014-12-02 2023-11-02 이그니타, 인코포레이티드 신경모세포종의 치료를 위한 병용
US10398774B2 (en) 2014-12-09 2019-09-03 INSERM (Institut National de la Santé et de la Recherche Médicale) Human monoclonal antibodies against AXL
LT3263106T (lt) 2015-02-25 2024-01-10 Eisai R&D Management Co., Ltd. Chinolino darinių kartumo sumažinimo būdas
WO2016135041A1 (en) 2015-02-26 2016-09-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Fusion proteins and antibodies comprising thereof for promoting apoptosis
CA2978226C (en) 2015-03-04 2025-02-18 Eisai R&D Management Co., Ltd. COMBINATION OF A PD-1 ANTAGONIST AND A VEGFR/FGFR/RET TYROSINE KINASE INHIBITOR TO TREAT CANCER
ES2716633T3 (es) 2015-03-25 2019-06-13 Sandoz Ag Formas cristalinas de fosfato de cabozantinib e hidrocloruro de cabozantinib
CN106279147A (zh) * 2015-05-21 2017-01-04 中国科学院上海药物研究所 一种吡啶并氮杂环化合物及其制备方法和用途
CN107801379B (zh) 2015-06-16 2021-05-25 卫材R&D管理有限公司 抗癌剂
US20170020856A1 (en) * 2015-06-29 2017-01-26 Ontogenesis, Llc N-Acylalkyl Prodrugs of Multi-Tyrosine Kinase Inhibitors and Methods of Use
EP3337786B1 (de) * 2015-08-19 2019-12-11 Sandoz AG Asymmetrische bisamidierung von malonesterderivaten
RU2718048C2 (ru) 2015-08-20 2020-03-30 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое терапевтическое средство
CN105218445B (zh) * 2015-08-25 2018-05-22 江苏中邦制药有限公司 一种酪氨酸激酶抑制剂Foretinib的制备方法
CN106543143B (zh) * 2015-09-22 2019-03-22 合肥中科普瑞昇生物医药科技有限公司 一类新型的flt3激酶抑制剂及其用途
EP3389645A4 (de) 2015-12-18 2019-12-18 Ignyta, Inc. Kombinationen zur behandlung von krebs
CN105541798B (zh) * 2016-02-03 2018-01-23 中国人民解放军第二军医大学 具有抗肿瘤活性的喹啉类多靶点激酶抑制剂及其制备方法
CN107129465B (zh) * 2016-02-26 2020-06-19 中国科学院上海药物研究所 芳基胍类化合物及其制备方法和用途
US20170283426A1 (en) * 2016-03-31 2017-10-05 Merck Patent Gmbh Compounds for the inhibition of cyclophilins and uses thereof
CN109069499A (zh) 2016-04-15 2018-12-21 埃克塞里艾克西斯公司 使用 n-(4-(6,7-二甲氧基喹啉-4-基氧基)苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺,(2s)-羟基丁二酸盐治疗肾细胞癌的方法
CN105906568A (zh) * 2016-04-28 2016-08-31 西安交通大学 一种具有抗肿瘤活性的环丙二酰胺化合物及其制备方法和应用
CN106083715A (zh) * 2016-06-01 2016-11-09 谢阳 一种喹啉、喹唑啉类化合物及其药物组合物和应用
CN106008371A (zh) * 2016-06-24 2016-10-12 谢阳 1-芳基脲基环烷基-1-甲酰胺类化合物及其药物组合物和应用
CN107556238A (zh) * 2016-06-30 2018-01-09 深圳万乐药业有限公司 一种卡博替尼的合成方法
US9957233B1 (en) 2016-08-05 2018-05-01 Calitor Sciences, Llc Process for preparing substituted quinolin-4-ol compounds
US10980792B2 (en) * 2016-09-12 2021-04-20 Zhuhai Beihai Biotech Co., Ltd. Formulations of Cabozantinib
CN110437145A (zh) * 2016-09-13 2019-11-12 上海翔锦生物科技有限公司 酪氨酸激酶抑制剂及其应用
EP3518928A1 (de) 2016-09-27 2019-08-07 The United States of America, as Represented by The Secretary, Department of Health and Human Services Office of Technology Transfer Verfahren zur behandlung von urothelialem karzinom und anderen urogenitalen malignomen mithilfe von n-(4-(6,7-dimethoxychinolin-4-yloxy)-phenyl)-n'-(4-fluorphenyl)cyclopropan-1,1-dicarboxamid
CN109496212B (zh) * 2016-10-18 2020-08-14 北京康辰药业股份有限公司 一种喹啉基取代的羧酸化合物或其药学上可接受的盐、其药物组合物及应用
US10799503B2 (en) 2016-12-01 2020-10-13 Ignyta, Inc. Methods for the treatment of cancer
CN106632028B (zh) * 2016-12-22 2019-01-22 上海再启生物技术有限公司 一种卡博替尼的制备方法
CN108329298A (zh) * 2017-01-17 2018-07-27 南昌弘益药业有限公司 一类喹啉类新化合物制备方法
CN117205313A (zh) 2017-01-20 2023-12-12 埃克塞里艾克西斯公司 治疗癌症的卡博替尼与阿特珠单抗组合
WO2018147275A1 (ja) 2017-02-08 2018-08-16 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療用医薬組成物
ES2991062T3 (es) 2017-02-15 2024-12-02 Taiho Pharmaceutical Co Ltd Composición farmacéutica
CN108503650B (zh) * 2017-02-27 2021-02-12 北京赛特明强医药科技有限公司 二噁烷并喹唑啉类化合物或其药用盐或其水合物及其作为酪氨酸激酶抑制剂的应用
ES2887261T3 (es) * 2017-04-27 2021-12-22 Astrazeneca Ab Compuestos de fenoxiquinazolina y su uso para tratar el cáncer
RU2019134940A (ru) 2017-05-16 2021-06-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Лечение гепатоцеллюлярной карциномы
EA039654B1 (ru) * 2017-05-26 2022-02-22 Экселиксис, Инк. Кристаллические твердые формы солей n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и методы использования
KR102647794B1 (ko) 2017-06-09 2024-03-15 엑셀리시스, 인코포레이티드 암을 치료하기 위한 액체 투여형
CA3069524A1 (en) * 2017-07-14 2019-01-17 Innate Tumor Immunity, Inc. Nlrp3 modulators
WO2019018570A1 (en) 2017-07-19 2019-01-24 Ignyta, Inc. PHARMACEUTICAL COMPOSITIONS CONTAINING ENTRECTINIB
US10180422B1 (en) 2017-08-22 2019-01-15 Scripps Health Methods of treating a neuroendocrine tumor
MX2020002183A (es) * 2017-08-31 2020-10-05 Abbvie Inc Inhibidores de la ectonucleótido pirofosfatasa-fosfodiesterasa 1 (enpp-1) y usos de los mismos.
US12280045B2 (en) 2017-09-08 2025-04-22 Taiho Pharmaceutical Co., Ltd. Antitumor agent and antitumor effect potentiator
JP7311498B2 (ja) 2017-10-17 2023-07-19 イグナイタ インコーポレイテッド 薬学的組成物および剤形
JP7270989B2 (ja) 2017-10-20 2023-05-11 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体m4のアンタゴニスト
JP2021503443A (ja) 2017-10-31 2021-02-12 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体m4のアンタゴニスト
CN109824587A (zh) * 2017-11-23 2019-05-31 上海翔锦生物科技有限公司 酪氨酸激酶抑制剂xjf007及其中间体的制备方法
CN109896997A (zh) * 2017-12-08 2019-06-18 中国药科大学 N-酰基苯胺类c-Met激酶抑制剂的制备方法及其用途
AU2018388439B2 (en) * 2017-12-20 2021-05-20 Angex Pharmaceutical, Inc. Carbamate and urea compounds as multikinase inhibitors
US20190262330A1 (en) * 2017-12-21 2019-08-29 Exelixis, Inc. Method of Treating Hepatocellular Carcinoma Using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2S)-hydroxybutanedioate
CN112312909B (zh) 2018-01-26 2024-07-02 埃克塞里艾克西斯公司 用于治疗激酶依赖性病症的化合物
AU2019212800B2 (en) * 2018-01-26 2024-05-23 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders
CA3088200A1 (en) * 2018-01-26 2019-08-01 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders
AU2019216492A1 (en) 2018-02-02 2020-08-20 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
CN108264482A (zh) * 2018-02-05 2018-07-10 南京法恩化学有限公司 一种卡博替尼的制备方法
JP7022454B2 (ja) 2018-02-11 2022-02-18 北京賽特明強医薬科技有限公司 ジオキシノキノリン系化合物、その調製方法および使用
WO2019180141A1 (en) 2018-03-23 2019-09-26 Bayer Aktiengesellschaft Combinations of rogaratinib
US11498902B2 (en) 2018-06-05 2022-11-15 Natco Pharma Limited Process for the preparation of Cabozantinib and its pharmaceutically acceptable salts thereof
TWI770624B (zh) 2018-06-15 2022-07-11 漢達生技醫藥股份有限公司 尼洛替尼十二烷基硫酸鹽在製備用於治療慢性骨髓性白血病之劑型的用途
WO2020027723A1 (en) 2018-08-01 2020-02-06 Agency For Science, Technology And Research Bicyclic compounds as kinase modulators, methods and uses thereof
WO2020042972A1 (zh) * 2018-08-27 2020-03-05 北京赛特明强医药科技有限公司 脲取代的芳环连二噁烷并喹唑啉或喹啉类化合物、组合物及其应用
WO2020075196A1 (en) 2018-10-11 2020-04-16 Cipla Limited Polymorphs of n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide, (s)- malate, methods of production and pharmaceutical uses thereof
CN111303024B (zh) * 2018-12-12 2023-03-28 安徽中科拓苒药物科学研究有限公司 一种喹啉结构的pan-KIT激酶抑制剂及其用途
JP7509779B2 (ja) * 2018-12-13 2024-07-02 エグゼリクシス, インコーポレイテッド キナーゼ阻害剤の結晶性形態及び塩形態
CN113195000A (zh) 2018-12-21 2021-07-30 第一三共株式会社 抗体-药物缀合物和激酶抑制剂的组合
CA3126721A1 (en) * 2019-01-25 2020-07-30 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders
CN109776432B (zh) * 2019-03-21 2020-07-24 广州六顺生物科技股份有限公司 一种多靶点激酶抑制剂、药物组合物及多靶点激酶抑制剂的制备方法和应用
US20220213064A1 (en) * 2019-04-12 2022-07-07 National Health Research Institutes Heterocyclic compounds as kinase inhibitors for therapeutic uses
CN111825609A (zh) 2019-04-22 2020-10-27 北京康辰药业股份有限公司 化合物晶型、其制备方法、药物组合物以及应用
CA3139148A1 (en) * 2019-06-03 2020-12-10 Exelixis, Inc. Crystalline salt forms of a kinase inhibitor
AR119069A1 (es) * 2019-06-04 2021-11-24 Exelixis Inc Compuestos para el tratamiento de trastornos dependientes de quinasas
CN110117254B (zh) * 2019-06-20 2022-05-13 江苏君若药业有限公司 卡博替尼的制备方法
CN112390749B (zh) * 2019-08-19 2024-12-03 鲁南制药集团股份有限公司 一种卡博替尼及其中间体的合成方法
CN112778217B (zh) * 2019-11-08 2024-01-26 沈阳化工研究院有限公司 一种喹唑啉类化合物及其应用
CN111393363B (zh) * 2020-04-27 2022-12-20 威海海洋生物医药产业技术研究院有限公司 4-苯氧基喹啉并n-磺酰脒类化合物及其制备方法和用途
CN113577066B (zh) * 2020-04-30 2022-12-16 中国科学院上海药物研究所 芳基胍化合物或其药学上可接受的盐的用途
IT202000027678A1 (it) 2020-11-18 2022-05-18 Indena Spa Dispersioni solide amorfe di cabozantinib-(s)-malato e processi per la loro preparazione
CA3202761A1 (en) 2020-11-25 2022-06-02 Nanocopoeia, Llc Amorphous cabozantinib particles and uses thereof
UY39569A (es) * 2020-12-17 2022-07-29 Astrazeneca Ab N-(2-(4-cianotiazolidin-3-il)-2-oxoetil)- quinolin-4-carboxamidas
JP2024513179A (ja) * 2021-03-24 2024-03-22 バイオコン・リミテッド カボザンチニブの調製のためのプロセス
IL312506A (en) 2021-11-08 2024-07-01 Progentos Therapeutics Inc Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
WO2023098853A1 (zh) * 2021-12-03 2023-06-08 湖南湘源美东医药科技有限公司 卡博替尼共晶及制备方法以及作为药物或在药物制剂中的应用
CN114605391B (zh) * 2022-02-21 2024-01-26 广州六顺生物科技股份有限公司 喹喔啉类衍生物及其制备方法和应用
CA3245315A1 (en) 2022-03-01 2023-09-07 Synthon B.V. L(+) TARTARIC ACID CABOZANTINIB SALT AND ITS SOLID FORMS
WO2023222946A1 (en) 2022-05-18 2023-11-23 Fermion Oy Process for the preparation of cabozantinib
EP4531927A1 (de) 2022-05-24 2025-04-09 Daiichi Sankyo Company, Limited Dosierungsplan eines anti-cdh6-antikörper-wirkstoff-konjugats
CA3261476A1 (en) 2022-07-08 2024-01-11 Astrazeneca Ab Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Combination with HGF Receptor Inhibitors for the Treatment of Cancer
WO2024110606A1 (en) 2022-11-25 2024-05-30 Synthon B.V. A process for preparation of cabozantinib or tivozanib
WO2024114710A1 (zh) * 2022-12-01 2024-06-06 江苏奥赛康药业有限公司 一种制备卡博替尼及其中间体的方法
AU2024215796A1 (en) * 2023-01-31 2025-05-15 Handa Oncology, Llc Improved cabozantinib compositions and methods of use
CN116751161A (zh) * 2023-06-28 2023-09-15 中国人民解放军军事科学院军事医学研究院 喹啉类化合物及其制备方法、药物组合物及医药用途
IL316197A (en) * 2023-10-17 2025-05-01 Great Novel Therapeutics Biotech & Medicals Corp Tyrosine kinase inhibitors and their uses
CN117843713A (zh) * 2023-12-18 2024-04-09 上海亲合力生物医药科技股份有限公司 基于肿瘤微环境激活的激酶抑制剂、组合物及应用
WO2025253311A1 (en) 2024-06-04 2025-12-11 Hetero Labs Limited 1,2-dicarboxamide compounds as kinase inhibitors

Family Cites Families (170)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US506181A (en) 1893-10-03 Folding crate
GB2160201B (en) * 1984-06-14 1988-05-11 Wyeth John & Brother Ltd Quinazoline and cinnoline derivatives
US5123951A (en) * 1986-03-31 1992-06-23 Rhone-Poulenc Nederland B.V. Synergistic plant growth regulator compositions
JPS646261A (en) * 1987-03-31 1989-01-10 Nisshin Flour Milling Co 4-thioquinazoline derivative, its production and antiulcer agent containing said derivative as active component
US5143854A (en) * 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5034393A (en) * 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
US5238951A (en) * 1991-02-01 1993-08-24 E. R. Squibb & Sons, Inc. Heterocyclic amido prostaglandin analogs
DE4114733A1 (de) * 1991-05-06 1992-11-12 Huels Chemische Werke Ag Verfahren zur herstellung von substituierten malonesteraniliden und malonsaeure-monoaniliden
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5358941A (en) 1992-12-02 1994-10-25 Merck & Co., Inc. Dry mix formulation for bisphosphonic acids with lactose
US6498144B1 (en) * 1993-10-18 2002-12-24 North Shore - Long Island Jewish Research Institute Use of scatter factor to enhance angiogenesis
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
GB9510757D0 (en) 1994-09-19 1995-07-19 Wellcome Found Therapeuticaly active compounds
TW321649B (de) 1994-11-12 1997-12-01 Zeneca Ltd
GB9508538D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
WO1996040648A1 (en) * 1995-06-07 1996-12-19 Sugen, Inc. Quinazolines and pharmaceutical compositions
ATE400295T1 (de) 1995-06-07 2008-07-15 Glaxosmithkline Biolog Sa Vakzine mit einem polysaccharide antigen- trägerprotein konjugat und freiem trägerprotein
US5650415A (en) * 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
AU7340096A (en) * 1995-11-07 1997-05-29 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of growth factor receptor originating in platelet and pharmaceutical compositions containing the same
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9624482D0 (en) * 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
GB9526546D0 (en) * 1995-12-23 1996-02-28 Pfizer Ltd Compounds useful in therapy
KR19990082463A (ko) * 1996-02-13 1999-11-25 돈 리사 로얄 혈관 내피 성장 인자 억제제로서의 퀴나졸린유도체
GB9603095D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
AU719327B2 (en) 1996-03-05 2000-05-04 Astrazeneca Ab 4-anilinoquinazoline derivatives
WO1997034876A1 (en) * 1996-03-15 1997-09-25 Zeneca Limited Cinnoline derivatives and use as medicine
US6107300A (en) * 1996-03-27 2000-08-22 Dupont Pharmaceuticals Arylamino fused pyrimidines
EA001595B1 (ru) * 1996-04-12 2001-06-25 Варнер-Ламберт Компани Необратимые ингибиторы тирозинкиназ
HRP970371A2 (en) * 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
AR007857A1 (es) * 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
CA2263479A1 (en) 1996-09-25 1998-04-02 Zeneca Limited Quinoline derivatives inhibiting the effect of growth factors such as vegf
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
DE69739986D1 (de) * 1996-10-01 2010-10-21 Kyowa Hakko Kogyo Kk Stickstoff enthaltende heterocyclische verbindungen
GB9700504D0 (en) * 1997-01-11 1997-02-26 Pfizer Ltd Pharmaceutical compounds
GB9705361D0 (en) * 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
EP0990647B1 (de) 1997-04-18 2003-07-02 Kirin Beer Kabushiki Kaisha Verfahren zur herstellung von chinolinderivaten
DE69818248T2 (de) 1997-04-22 2004-06-17 Janssen Pharmaceutica N.V. Chinolin- und chinazolin-derivate als crf antagonisten
GB9708917D0 (en) 1997-05-01 1997-06-25 Pfizer Ltd Compounds useful in therapy
AR012634A1 (es) * 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
ZA986732B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
DE69838172T2 (de) * 1997-08-22 2008-04-10 Astrazeneca Ab Oxindolylchinazolinderivate als angiogenesehemmer
JP4194678B2 (ja) * 1997-11-28 2008-12-10 キリンファーマ株式会社 キノリン誘導体およびそれを含む医薬組成物
GB9800569D0 (en) * 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
AU4317399A (en) * 1998-05-28 1999-12-13 Parker Hughes Institute Quinazolines for treating brain tumor
JP4516690B2 (ja) * 1998-08-11 2010-08-04 ノバルティス アーゲー 血管形成阻害活性を有するイソキノリン誘導体
KR20010089171A (ko) 1998-08-21 2001-09-29 추후제출 퀴나졸린 유도체
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
JP5170486B2 (ja) 1998-09-10 2013-03-27 バイオイコール ア−ゲー 局所適用性産物
CN1165532C (zh) 1998-09-29 2004-09-08 惠氏控股有限公司 作为蛋白质酪氨酸激酶抑制剂的取代的3-氰基喹啉
US6288082B1 (en) * 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
WO2000020402A1 (en) 1998-10-01 2000-04-13 Astrazeneca Ab Chemical compounds
BR9914326A (pt) 1998-10-08 2001-06-26 Astrazeneca Ab Uso de um composto, composto, processo para a preparação do mesmo, composição farmacêutica, e, método para produzir um efeito antiangiogênico e/ou de redução da permeabilidade vascular em animais de sangue quente em necessidade de um tal tratamento
PT1131304E (pt) * 1998-11-19 2003-04-30 Warner Lambert Co N-¬4-(3-cloro-4-fluoro-fenilamino)-7-(3-morfolin-4-il-propoxi)-quinazolin-6-il|-acrilamida um inibidor irreversivel de tirosino quinases
EP1384712B1 (de) * 1999-01-22 2007-03-07 Kirin Beer Kabushiki Kaisha Derivate des N-((Chinolinyl)oxy)-phenyl)-Harnstoffs und des N-((Chinazolinyl)oxy)-phenyl)-Harnstoffs mit Antitumor Aktivität
SK288365B6 (sk) 1999-02-10 2016-07-01 Astrazeneca Ab Medziprodukty pre chinazolínové deriváty ako inhibítory angiogenézy
GB9904103D0 (en) * 1999-02-24 1999-04-14 Zeneca Ltd Quinoline derivatives
US6080747A (en) * 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
DE19911509A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US6258820B1 (en) * 1999-03-19 2001-07-10 Parker Hughes Institute Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
EP1162974A1 (de) 1999-03-19 2001-12-19 Parker Hughes Institute Quinazoline formulierungen und therapeutische verwendung
RS49836B (sr) 1999-03-31 2008-08-07 Pfizer Products Inc., Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9910580D0 (en) * 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
US6126917A (en) * 1999-06-01 2000-10-03 Hadasit Medical Research Services And Development Ltd. Epidermal growth factor receptor binding compounds for positron emission tomography
MEP45508A (en) * 1999-06-21 2011-02-10 Boehringer Ingelheim Pharma Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof
CZ20021009A3 (cs) * 1999-09-21 2002-06-12 Astrazeneca Ab Deriváty chinazolinu, způsob jejich přípravy a jejich pouľití jako léčiv
GB9922171D0 (en) 1999-09-21 1999-11-17 Zeneca Ltd Chemical compounds
US6759410B1 (en) * 1999-11-23 2004-07-06 Smithline Beecham Corporation 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors
JP2003518023A (ja) * 1999-11-30 2003-06-03 パーカー ヒューズ インスティテュート トロンビン誘導血小板凝集の阻害剤
US20020002169A1 (en) * 1999-12-08 2002-01-03 Griffin John H. Protein kinase inhibitors
HK1049839A1 (en) * 1999-12-24 2003-05-30 Kirin Pharma Kabushiki Kaisha Quinoline and quinazoline derivatives and drugs containing the same
US6525046B1 (en) * 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
EP1294709A2 (de) * 2000-01-28 2003-03-26 AstraZeneca AB Chinolinderivate und deren verwendung als aurora 2 kinase inhibitoren
US6664390B2 (en) 2000-02-02 2003-12-16 Warner-Lambert Company Llc Method for the simplified production of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitro-quinazoline-4-yl]-amine or (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-amino-quinazoline-4-yl]-amine
SK12712002A3 (sk) * 2000-02-07 2003-02-04 Abbott Gmbh & Co. Kg Deriváty 2-benzotiazolylmočoviny a ich použitie ako inhibítorov proteínkináz
KR100817423B1 (ko) 2000-03-13 2008-03-27 와이어쓰 홀딩스 코포레이션 시아노퀴놀린을 포함하는 결장 폴립의 치료 또는 억제를 위한 약제학적 조성물
US6521618B2 (en) * 2000-03-28 2003-02-18 Wyeth 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
US6608048B2 (en) * 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
US6627634B2 (en) * 2000-04-08 2003-09-30 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
UA73993C2 (uk) 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
JP4044839B2 (ja) * 2000-06-22 2008-02-06 ファイザー・プロダクツ・インク 異常細胞増殖を治療するための置換2環式誘導体
EP1174118A1 (de) 2000-06-28 2002-01-23 Cognis France S.A. Verwendung von Inulinen und Inulinderivaten
WO2002000649A1 (en) 2000-06-28 2002-01-03 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
FR2811658B1 (fr) 2000-07-17 2004-07-02 Cfpi Nufarm Reacteur biologique a lit fixe immerge et procede de traitement d'effluents liquides
JP2002030083A (ja) * 2000-07-18 2002-01-29 Kirin Brewery Co Ltd N−(2−クロロ−4−{[6−メトキシ−7−(3−ピリジルメトキシ)−4−キノリル]オキシ}フェニル)−n’−プロピルウレアの二塩酸塩
US7427689B2 (en) * 2000-07-28 2008-09-23 Georgetown University ErbB-2 selective small molecule kinase inhibitors
KR100821446B1 (ko) 2000-08-21 2008-04-10 아스트라제네카 아베 퀴나졸린 유도체
US6403580B1 (en) * 2000-08-26 2002-06-11 Boehringer Ingelheim Pharma Kg Quinazolines, pharmaceutical compositions containing these compounds, their use and processes for preparing them
US6656946B2 (en) 2000-08-26 2003-12-02 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US6617329B2 (en) * 2000-08-26 2003-09-09 Boehringer Ingelheim Pharma Kg Aminoquinazolines and their use as medicaments
US6653305B2 (en) * 2000-08-26 2003-11-25 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
US6740651B2 (en) * 2000-08-26 2004-05-25 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
DE10042058A1 (de) 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
AU2001292137A1 (en) 2000-10-13 2002-04-22 Astrazeneca Ab Quinazoline derivatives
EP1326859A1 (de) 2000-10-13 2003-07-16 AstraZeneca AB Chinazoline derivate mit aktivität gegen tumore
EP1506962B1 (de) * 2000-10-20 2008-07-02 Eisai R&D Management Co., Ltd. Stickstoff enthaltende aromatische Heterozyklen
EP1332141A1 (de) 2000-10-25 2003-08-06 AstraZeneca AB Chinazolin derivate
US7253184B2 (en) 2000-11-02 2007-08-07 Astrazeneca Ab 4-Substituted quinolines as antitumor agents
JP2004514718A (ja) 2000-11-02 2004-05-20 アストラゼネカ アクチボラグ 抗癌剤としての置換キノリン類
US7220751B2 (en) 2000-11-02 2007-05-22 Nippon Shinyaku Co., Ltd. Quinazoline derivatives and drugs
US7019012B2 (en) * 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
US6900220B2 (en) * 2001-01-02 2005-05-31 Syntex (U.S.A.) Llc Quinazolone derivatives as alpha 1A/B adrenergic receptor antagonists
DE60229046D1 (de) 2001-04-19 2008-11-06 Astrazeneca Ab Chinazolin derivate
EP1382604B1 (de) * 2001-04-27 2005-12-28 Kirin Beer Kabushiki Kaisha Chinolinderivate mit einer azolylgruppe und chinazolinderivate
SE0101675D0 (sv) 2001-05-11 2001-05-11 Astrazeneca Ab Novel composition
WO2002092577A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2002092578A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2002092579A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab 4-anilinoquinazoline derivatives
US6734303B2 (en) * 2001-05-18 2004-05-11 Pfizer Inc. Process for the production of quinazolines
DE10125432A1 (de) * 2001-05-25 2002-11-28 Bayer Ag Substituierte Benzoylketone
EP1408980A4 (de) 2001-06-21 2004-10-20 Ariad Pharma Inc Neue chinazoline und ihre verwendungszwecke
WO2003000660A1 (fr) 2001-06-22 2003-01-03 Kirin Beer Kabushiki Kaisha Derive de quinoleine et derive de quinoleine permettant d'inhiber l'auto-phosphorylation du recepteur des proliferateurs des hepatocytes, ainsi que des compositions medicinales contenant ce derive
KR100397792B1 (ko) * 2001-06-28 2003-09-13 한국과학기술연구원 4-(페닐아미노)-[1,4]디옥사노[2,3-g]퀴나졸린 유도체 및그의 제조방법
GB0118752D0 (en) * 2001-08-01 2001-09-26 Pfizer Ltd Process for the production of quinazolines
US7229774B2 (en) 2001-08-02 2007-06-12 Regents Of The University Of Michigan Expression profile of prostate cancer
US20030066060A1 (en) 2001-09-28 2003-04-03 Ford Richard L. Cross profile guided optimization of program execution
WO2003033472A1 (en) * 2001-10-17 2003-04-24 Kirin Beer Kabushiki Kaisha Quinoline or quinazoline derivatives inhibiting auto- phosphorylation of fibroblast growth factor receptors
WO2003037252A2 (en) 2001-10-30 2003-05-08 Merck & Co., Inc. Tyrosine kinase inhibitors
GB0126433D0 (en) 2001-11-03 2002-01-02 Astrazeneca Ab Compounds
GB0128108D0 (en) 2001-11-23 2002-01-16 Astrazeneca Ab Therapeutic use
AU2002359489B2 (en) * 2001-11-27 2008-10-30 Wyeth Holdings Corporation 3-cyanoquinolines as inhibitors of EGF-R and Her2 kinases
WO2003047584A1 (en) 2001-12-05 2003-06-12 Astrazeneca Ab Quinoline derivatives
WO2003048159A1 (en) 2001-12-05 2003-06-12 Astrazeneca Ab Quinoline derivatives
GB0129099D0 (en) 2001-12-05 2002-01-23 Astrazeneca Ab Chemical compounds
AU2002339687A1 (en) * 2001-12-12 2003-06-23 Pfizer Products Inc. Quinazoline derivatives for the treatement of abnormal cell growth
HRP20040530A2 (en) 2001-12-12 2004-10-31 Pfizer Prod Inc Salt forms of e-2-methoxy-n-(3-(4-(3-methyl-pyridin-3-yloxy)-phenylamino)-quinazolin-6-yl)-allyl)-acetamide, its preparation and its use against cancer
AU2002361846A1 (en) 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
TW200301123A (en) 2001-12-21 2003-07-01 Astrazeneca Uk Ltd New use
UA82058C2 (uk) 2001-12-24 2008-03-11 Астразенека Аб Заміщені похідні хіназоліну як інгібітори ауроракінази, спосіб їх одержання, фармацевтична композиція на їх основі
WO2003064431A2 (en) 2002-01-29 2003-08-07 Glaxo Group Limited Aminopiperidine compounds, process for their preparation, and pharmaceutical compositions containing them
JP4445753B2 (ja) 2002-01-29 2010-04-07 グラクソ グループ リミテッド アミノピペリジン誘導体
CN1625555A (zh) 2002-02-01 2005-06-08 阿斯特拉曾尼卡有限公司 喹唑啉化合物
DE10204462A1 (de) * 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
AU2003225668A1 (en) * 2002-03-01 2003-09-16 Pintex Pharmaceutical, Inc. Pin1-modulating compounds and methods of use thereof
DE10217689A1 (de) 2002-04-19 2003-11-13 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung
WO2003093238A1 (en) * 2002-05-01 2003-11-13 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor
JP4703183B2 (ja) 2002-07-15 2011-06-15 シンフォニー エボルーション, インク. 受容体型キナーゼモジュレーターおよびその使用方法
GB0219746D0 (en) 2002-08-23 2002-10-02 Inst Of Ex Botany Ascr Azapurine derivatives
WO2004018430A1 (ja) * 2002-08-23 2004-03-04 Kirin Beer Kabushiki Kaisha TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
DE60316590T2 (de) 2002-10-21 2008-06-19 Kirin Beer K.K. N-(2-CHLOR-4-((6,7-DIMETHOXY-4-CHINOLYL)OXYÜPHENYLü-N'-(5-METHYL-3-ISOXAZOLYL)HARNSTOFFSALZIN KRISTALLINER FORM
JPWO2004039782A1 (ja) * 2002-10-29 2006-03-02 麒麟麦酒株式会社 Flt3自己リン酸化を阻害するキノリン誘導体およびキナゾリン誘導体並びにそれらを含有する医薬組成物
NZ539408A (en) 2002-11-04 2007-09-28 Astrazeneca Ab Quinazoline derivatives as SRC tyrosine kinase inhibitors for treating solid tumours
JP2006515847A (ja) 2002-12-13 2006-06-08 ニューロジェン・コーポレーション カプサイシン受容体調節剤としてのカルボン酸、ホスフェート又はホスホネート置換キナゾリン−4−イルアミン類縁体
RU2005119172A (ru) 2002-12-18 2006-01-20 Пфайзер Продактс Инк. (Us) Производные 4-анилинхиназолина для лечения патологического роста клеток
EP1575591A4 (de) 2002-12-23 2007-09-12 Ariad Pharma Inc Heterocyclen und ihre verwendung
WO2004060373A1 (ja) * 2002-12-27 2004-07-22 Santen Pharmaceutical Co., Ltd. 滲出型加齢黄斑変性治療剤
US8176532B1 (en) * 2003-03-17 2012-05-08 Sprint Communications Company L.P. Secure access point for scada devices
KR100559180B1 (ko) * 2003-05-20 2006-03-14 김민서 조건부 거래에 따른 전자결제 방법 및 전자결제 서버
WO2005003140A1 (en) 2003-07-02 2005-01-13 Pharmacia & Upjohn Company Llc 4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxamides as antiviral agents
US20070213374A1 (en) 2003-07-07 2007-09-13 Merck Patent Gmbh Malonamide Derivatives
ES2651730T3 (es) * 2003-09-26 2018-01-29 Exelixis, Inc. Moduladores c-Met y métodos de uso
EP1711495A2 (de) 2004-01-23 2006-10-18 Amgen Inc. Chinolin-, chinazolin-, pyridin- und pyrimidinverbindungen und deren verwendung bei der behandlung von entzündungen, angiogenese und krebs
US20050288290A1 (en) * 2004-06-28 2005-12-29 Borzilleri Robert M Fused heterocyclic kinase inhibitors
EP1773826A4 (de) * 2004-07-02 2009-06-03 Exelixis Inc C-met-modulatoren und anwendungsverfahren
EP1874759A4 (de) * 2005-04-06 2009-07-15 Exelixis Inc C-met-modulatoren und anwendungsverfahren
US7594258B2 (en) * 2005-06-27 2009-09-22 Yahoo! Inc. Access control systems and methods using visibility tokens with automatic propagation
US20080004273A1 (en) * 2006-05-30 2008-01-03 Stephane Raeppel Inhibitors of protein tyrosine kinase activity
CA2738583A1 (en) 2008-10-01 2010-04-08 Ludwig Institute For Cancer Research Methods for the treatment of cancer
EP2367795A1 (de) * 2008-12-04 2011-09-28 Exelixis, Inc. Verfahren zur herstellung von chinolinderivaten
CA2758030C (en) * 2009-01-16 2019-01-08 Exelixis, Inc. Malate salt of n-(4-{[6,7-bis(methyloxy)quin0lin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer
WO2011009095A1 (en) * 2009-07-17 2011-01-20 Exelixis, Inc. Crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quin0lin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
WO2011031840A1 (en) 2009-09-09 2011-03-17 Quintiles Transnational Corp. Methods and compositions for the treatment of receptor tyrosine kinase mediated diseases or disorders
JP5461213B2 (ja) 2010-01-29 2014-04-02 三洋電機株式会社 空気調和装置の室外ユニット
US20120070368A1 (en) * 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
US20120252840A1 (en) * 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer

Also Published As

Publication number Publication date
AU2010204461A1 (en) 2010-08-19
AU2010204459A1 (en) 2010-08-19
EP2392565B1 (de) 2014-03-19
HK1143068A1 (en) 2010-12-24
SI2392564T1 (sl) 2014-02-28
US20070244116A1 (en) 2007-10-18
CY2014037I1 (el) 2015-11-04
JP5694501B2 (ja) 2015-04-01
US9174947B2 (en) 2015-11-03
CY2014037I2 (el) 2019-07-10
EP2213661B1 (de) 2011-07-20
JP2011042686A (ja) 2011-03-03
US20090170896A1 (en) 2009-07-02
EP2409704B1 (de) 2017-09-20
JP2021050233A (ja) 2021-04-01
US8476298B2 (en) 2013-07-02
CY1111956T1 (el) 2015-11-04
EP1673085A4 (de) 2008-12-10
JP2017160270A (ja) 2017-09-14
JP4638436B2 (ja) 2011-02-23
JP2010265302A (ja) 2010-11-25
CA2744997A1 (en) 2005-04-07
HK1141799A1 (en) 2010-11-19
US20170355678A1 (en) 2017-12-14
EP2409704A3 (de) 2013-02-13
JP2015131859A (ja) 2015-07-23
HRP20110707T1 (hr) 2011-10-31
WO2005030140A2 (en) 2005-04-07
DK2392564T3 (da) 2014-01-13
FR14C0067I1 (de) 2014-10-17
JP2010280674A (ja) 2010-12-16
JP2014055191A (ja) 2014-03-27
PL2213661T3 (pl) 2011-12-30
CA2537812A1 (en) 2005-04-07
JP5185332B2 (ja) 2013-04-17
HRP20140563T1 (hr) 2014-07-18
HK1256476A1 (en) 2019-09-27
HUS1400052I1 (hu) 2022-02-28
US8497284B2 (en) 2013-07-30
US20130252940A1 (en) 2013-09-26
US20150376133A1 (en) 2015-12-31
US20120022065A1 (en) 2012-01-26
HK1164312A1 (en) 2012-09-21
PT2213661E (pt) 2011-12-15
EP2210607B1 (de) 2011-08-17
US20160185725A1 (en) 2016-06-30
AU2004275842B2 (en) 2010-09-02
ES2371383T3 (es) 2011-12-30
EP2392564B1 (de) 2013-10-23
US11124482B2 (en) 2021-09-21
JP5185331B2 (ja) 2013-04-17
JP2014055190A (ja) 2014-03-27
SI2213661T1 (sl) 2011-11-30
EP2609919A2 (de) 2013-07-03
LU92508I2 (fr) 2015-11-02
ES2925655T3 (es) 2022-10-19
US20070225307A1 (en) 2007-09-27
US20140155378A9 (en) 2014-06-05
EP3329918A2 (de) 2018-06-06
ES2436888T3 (es) 2014-01-07
US7579473B2 (en) 2009-08-25
US20090105299A1 (en) 2009-04-23
ES2466818T3 (es) 2014-06-11
US8067436B2 (en) 2011-11-29
ATE517091T1 (de) 2011-08-15
JP2010235631A (ja) 2010-10-21
JP5325172B2 (ja) 2013-10-23
EP2392564A1 (de) 2011-12-07
EP3329918A3 (de) 2018-08-15
EP2210607A1 (de) 2010-07-28
AU2010204461B2 (en) 2013-06-20
US20140155396A1 (en) 2014-06-05
US20120184523A1 (en) 2012-07-19
JP2024023447A (ja) 2024-02-21
HK1164313A1 (en) 2012-09-21
NL300678I2 (de) 2017-01-31
DK2213661T3 (da) 2011-09-19
HRP20140012T1 (hr) 2014-02-14
ATE532782T1 (de) 2011-11-15
EP2409704A2 (de) 2012-01-25
FR14C0067I2 (fr) 2015-11-20
WO2005030140A3 (en) 2005-05-19
CY1112056T1 (el) 2015-11-04
CA2537812C (en) 2013-01-22
JP2014074059A (ja) 2014-04-24
SI2392565T1 (sl) 2014-05-30
PL2210607T3 (pl) 2012-01-31
PT2210607E (pt) 2012-01-31
EP3329918B1 (de) 2022-05-25
PL2392565T3 (pl) 2014-08-29
US8178532B2 (en) 2012-05-15
JP2010235632A (ja) 2010-10-21
JP5325173B2 (ja) 2013-10-23
EP2609919A3 (de) 2014-02-26
ES2651730T3 (es) 2018-01-29
JP2019070015A (ja) 2019-05-09
US20070054928A1 (en) 2007-03-08
US20110077233A1 (en) 2011-03-31
EP2213661A1 (de) 2010-08-04
JP2007506777A (ja) 2007-03-22
EP1673085A2 (de) 2006-06-28
US20200331860A1 (en) 2020-10-22
HRP20110810T1 (hr) 2011-12-31
AU2004275842A1 (en) 2005-04-07
US20210253530A9 (en) 2021-08-19
DK2392565T3 (da) 2014-05-05
EP1673085B1 (de) 2011-11-09
DK2210607T3 (da) 2011-12-12
ES2369652T3 (es) 2011-12-02
BE2014C055I2 (de) 2023-12-14
SI2210607T1 (sl) 2011-11-30
EP2392565A1 (de) 2011-12-07
AU2010204459B2 (en) 2013-06-20
EP2612853A1 (de) 2013-07-10

Similar Documents

Publication Publication Date Title
ATE520403T1 (de) N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs
WO2004006846A3 (en) Receptor-type kinase modulators and methods of use
WO2006014325A3 (en) C-met modulators and method of use
WO2005020921A3 (en) C-kit modulators and methods of use
WO2004092196A3 (en) Tie-2 modulators and methods of use
EA200200473A1 (ru) Ингибиторы тирозинкиназы
WO2004091480A3 (en) Tie-2 modulators and methods of use
DE69520499D1 (de) Histidine und homohistidine derivate zur verwendung als protein farnesyltransferase hemmstoffe
EA200200351A1 (ru) Ингибиторы тирозинкиназы
EA201300713A1 (ru) Варианты, происходящие из actriib, и их применение
ATE290865T1 (de) Tyrosin kinase inhibitoren
EP1503757A4 (de) Tyrosinkinase-hemmer
WO2004083235A3 (en) Tie-2 modulators and methods of use
ATE313561T1 (de) Vgf polypeptide und verfahren zur behandlung von vgf-erkrankungen
ATE428712T1 (de) 4-amino-5-oxo-8-phenyl-5h-pyrido-ä2,3-dü- pyrimidin-derivate als inhibitoren der tyrosinkinasen und der raf-kinasen zur behandlung von tumoren
WO2004050681A3 (en) Kinase modulators
ATE482217T1 (de) Dithiolopyrrolon-derivate zur behandlung von proliferativen störungen
ATE386748T1 (de) Verwendung von liganden von cd52 antigen zur behandlung von soliden tumoren und von knochenkrebserkrankungen
DE60228056D1 (de) Verfahren und zusammensetzungen zur modulierung der gluconeogenese mit pgc-1
EA201990964A1 (ru) Варианты, происходящие из actriib, и их применение

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 2210607

Country of ref document: EP