LU92508I2 - Cabozantinib et toutes les formes thérapeutiquement équivalentes qui en dérivent telles que protégées par le brevet de base, y compris les sels pharmacetuiquement acceptables - Google Patents

Cabozantinib et toutes les formes thérapeutiquement équivalentes qui en dérivent telles que protégées par le brevet de base, y compris les sels pharmacetuiquement acceptables Download PDF

Info

Publication number
LU92508I2
LU92508I2 LU92508C LU92508C LU92508I2 LU 92508 I2 LU92508 I2 LU 92508I2 LU 92508 C LU92508 C LU 92508C LU 92508 C LU92508 C LU 92508C LU 92508 I2 LU92508 I2 LU 92508I2
Authority
LU
Luxembourg
Prior art keywords
compounds
pharmacetually
cabozantinib
protected
acceptable salts
Prior art date
Application number
LU92508C
Other languages
English (en)
French (fr)
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=LU92508(I2) "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
Publication of LU92508I2 publication Critical patent/LU92508I2/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • 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
    • 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
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C07D215/46—Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/14—Heterocyclic 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
    • C07D295/145—Heterocyclic 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
    • C07D295/15—Heterocyclic 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
    • 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
    • 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
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING 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
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening 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)
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against 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)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Physics & Mathematics (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
LU92508C 2003-09-26 2014-07-25 Cabozantinib et toutes les formes thérapeutiquement équivalentes qui en dérivent telles que protégées par le brevet de base, y compris les sels pharmacetuiquement acceptables LU92508I2 (fr)

Applications Claiming Priority (4)

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
EP04789057A EP1673085B1 (en) 2003-09-26 2004-09-24 C-met modulators and methods of use

Publications (1)

Publication Number Publication Date
LU92508I2 true LU92508I2 (fr) 2015-11-02

Family

ID=34397024

Family Applications (1)

Application Number Title Priority Date Filing Date
LU92508C LU92508I2 (fr) 2003-09-26 2014-07-25 Cabozantinib et toutes les formes thérapeutiquement équivalentes qui en dérivent telles que protégées par le brevet de base, y compris les sels pharmacetuiquement acceptables

Country Status (19)

Country Link
US (14) US9174947B2 (enExample)
EP (9) EP2210607B1 (enExample)
JP (14) JP4638436B2 (enExample)
AT (3) ATE517091T1 (enExample)
AU (3) AU2004275842B2 (enExample)
BE (1) BE2014C055I2 (enExample)
CA (2) CA2744997A1 (enExample)
CY (3) CY1111956T1 (enExample)
DK (4) DK2213661T3 (enExample)
ES (6) ES2466818T3 (enExample)
FR (1) FR14C0067I2 (enExample)
HR (4) HRP20110707T1 (enExample)
HU (1) HUS1400052I1 (enExample)
LU (1) LU92508I2 (enExample)
NL (1) NL300678I2 (enExample)
PL (3) PL2392565T3 (enExample)
PT (2) PT2213661E (enExample)
SI (4) SI2392564T1 (enExample)
WO (1) WO2005030140A2 (enExample)

Families Citing this family (286)

* 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
KR100600550B1 (ko) 2000-10-20 2006-07-13 에자이 가부시키가이샤 질소 함유 방향환 유도체
EP1604665B1 (en) 2003-03-10 2011-05-11 Eisai R&D Management Co., Ltd. C-kit kinase inhibitor
BRPI0414532B1 (pt) 2003-09-19 2018-06-05 Astrazeneca Ab Composto derivado de quinazolina, processo para preparar 0 mesmo, composição farmaceutica, e, uso de um composto derivado de quinazolina
EP2210607B1 (en) * 2003-09-26 2011-08-17 Exelixis Inc. N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer
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
WO2005048953A2 (en) 2003-11-13 2005-06-02 Ambit Biosciences Corporation Amide derivatives as kinase modulators
US7626030B2 (en) * 2004-01-23 2009-12-01 Amgen Inc. Compounds and methods of use
KR100799534B1 (ko) * 2004-02-27 2008-01-31 에자이 알앤드디 매니지먼트 가부시키가이샤 신규 피리딘 유도체 및 피리미딘 유도체(1)
AU2005231507B2 (en) 2004-04-08 2012-03-01 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
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
US7432373B2 (en) 2004-06-28 2008-10-07 Bristol-Meyers Squibb Company Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors
NZ588896A (en) * 2004-08-25 2012-05-25 Targegen Inc Heterocyclic compounds and methods of use
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
US7767677B2 (en) 2004-09-20 2010-08-03 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
EP1804799B1 (en) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
EP2289510A1 (en) 2004-09-20 2011-03-02 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes
US7951805B2 (en) 2004-09-20 2011-05-31 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
EP2316458A1 (en) 2004-09-20 2011-05-04 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
CA2580856A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
EP1799667B1 (en) 2004-09-20 2013-03-20 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
MX2007004403A (es) 2004-10-12 2007-04-27 Astrazeneca Ab Derivados de quinazolina.
MX2007006230A (es) 2004-11-30 2007-07-25 Amgen Inc Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer.
EP1674466A1 (en) * 2004-12-27 2006-06-28 4Sc Ag 2,5- and 2,6-disubstituted benzazole analogues useful as protein kinase inhibitors
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
WO2008041053A2 (en) * 2005-05-20 2008-04-10 Methylgene, Inc. Inhibitors of vegf receptor and hgf receptor signaling
RU2007146986A (ru) * 2005-06-02 2009-06-27 ГЭЛЭКСИ БАЙОТЕК, ЭлЭлСи (US) Способы лечения опухолей головного мозга с использованием антител
EP2029138A1 (en) 2005-06-03 2009-03-04 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
JP4989476B2 (ja) 2005-08-02 2012-08-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質の効果を検定する方法
TWI377198B (en) 2005-08-24 2012-11-21 Eisai R&D Man Co Ltd Novel pyridine derivatives and pyrimidine derivatives (3)
PE20070335A1 (es) 2005-08-30 2007-04-21 Novartis Ag Benzimidazoles sustituidos y metodos para su preparacion
US7732613B2 (en) 2005-09-14 2010-06-08 Bristol-Myers Squibb Company Met kinase inhibitors
US20090247576A1 (en) * 2005-11-22 2009-10-01 Eisai R & D Management Co., Ltd. Anti-tumor agent for multiple myeloma
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
US7723330B2 (en) 2006-03-07 2010-05-25 Array Biopharma Inc. Heterobicyclic pyrazole compounds and methods of use
AR059922A1 (es) * 2006-04-01 2008-05-07 Galaxy Biotech Llc Anticuerpos monoclonales humanizados para el factor de crecimiento de hepatocitos
KR101464385B1 (ko) 2006-04-19 2014-11-21 노파르티스 아게 ６-ｏ-치환된 벤즈옥사졸 및 벤조티아졸 화합물, 및 ｃｓｆ-１ｒ 신호전달의 억제 방법
CN104706637A (zh) 2006-05-18 2015-06-17 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
NZ573735A (en) 2006-05-19 2011-10-28 Abbott Lab Cns active fused bicycloheterocycle substituted azabicyclic alkane derivatives
WO2008035209A2 (en) * 2006-05-30 2008-03-27 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
US20110053931A1 (en) * 2006-06-08 2011-03-03 John Gaudino Quinoline compounds and methods of use
US7683060B2 (en) 2006-08-07 2010-03-23 Incyte Corporation Triazolotriazines as kinase inhibitors
ATE535520T1 (de) * 2006-08-23 2011-12-15 Eisai R&D Man Co Ltd Salz eines phenoxypyridinderivats oder kristall davon und verfahren zu dessen herstellung
JP5368096B2 (ja) 2006-08-28 2013-12-18 エーザイ・アール・アンド・ディー・マネジメント株式会社 未分化型胃癌に対する抗腫瘍剤
US7790885B2 (en) 2006-08-31 2010-09-07 Eisai R&D Management Co., Ltd. Process for preparing phenoxypyridine derivatives
MX2009004426A (es) 2006-10-23 2009-08-12 Cephalon Inc Derivados biciclicos fusionados de 2,4-diaminopirimidina como inhibidores alk y c-met.
US20100016307A1 (en) * 2006-10-27 2010-01-21 Toshihiro Hamajima Novel compounds
GEP20125658B (en) 2006-11-22 2012-10-10 Incyte Corp Imidazotriazines and imidazo pyrimidines as kinase inhibitors
AU2007338792B2 (en) * 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
WO2008079294A1 (en) * 2006-12-20 2008-07-03 Amgen Inc. Substituted heterocycles and methods of use
CA2675755C (en) * 2007-01-19 2015-10-06 Xcovery, Inc. Pyridine and pyridazine derivatives as kinase inhibitors
WO2008093855A1 (ja) 2007-01-29 2008-08-07 Eisai R & D Management Co., Ltd. 未分化型胃癌治療用組成物
AU2008254425A1 (en) * 2007-05-21 2008-11-27 Novartis Ag CSF-1R inhibitors, compositions, and methods of use
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
PE20090595A1 (es) 2007-08-15 2009-06-06 Glaxo Group Ltd Derivados de quinoliniloxipiperidina y pirrolidina como antagonistas del receptor h1
EP2183254B1 (en) 2007-08-29 2017-06-21 MethylGene Inc. Inhibitors of protein tyrosine kinase activity
CA2704000C (en) 2007-11-09 2016-12-13 Eisai R&D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
JP2009132660A (ja) 2007-11-30 2009-06-18 Eisai R & D Management Co Ltd 食道癌治療用組成物
ES2531396T3 (es) 2008-01-23 2015-03-13 Bristol Myers Squibb Co Proceso para preparar compuestos de piridinona
AU2009226136B2 (en) 2008-03-17 2013-08-15 Ambit Biosciences Corporation Quinazoline derivatives as RAF kinase modulators and methods of use thereof
JP4667537B2 (ja) 2008-04-10 2011-04-13 大鵬薬品工業株式会社 アシルチオウレア化合物又はその塩、及びその用途
JP5746015B2 (ja) * 2008-04-16 2015-07-08 マックス プランク ゲゼルシャフト ツゥアー フェデルゥン デル ヴィッセンシャフテン エー フォー Ａｘｌキナーゼ阻害剤としてのキノリン誘導体
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
SI2300455T1 (sl) 2008-05-21 2017-12-29 Incyte Holdings Corporation Soli 2-fluoro-n-metil-4-(7-(kinolin-6-il-metil)-imidazo(1,2-b)1,2,4) triazin-2-il)benzamid in postopki v zvezi z njihovo pripravo
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
EP2303881A2 (en) 2008-07-14 2011-04-06 Gilead Sciences, Inc. Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
EP2303841A1 (en) 2008-07-14 2011-04-06 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
EP2149565A1 (de) * 2008-07-24 2010-02-03 Bayer Schering Pharma AG Sulfonsubstituierte Chinazolinderivate als Immunmodulatoren zur Behandlung von enzündlichen und allergischen Erkrankungen
KR20110038159A (ko) 2008-07-28 2011-04-13 길리애드 사이언시즈, 인코포레이티드 사이클로알킬리덴 및 헤테로사이클로알킬리덴 히스톤 데아세틸라아제 억제제 화합물
AR075084A1 (es) * 2008-09-26 2011-03-09 Smithkline Beecham Corp Metodo de preparacion de quinolinil -oxidifenil - ciclopropanodicarboxamidas e intermediarios correspondientes
AU2009303602B2 (en) * 2008-10-14 2012-06-14 Sunshine Lake Pharma Co., Ltd. Compounds and methods of use
CA2742007C (en) * 2008-10-29 2014-07-08 Deciphera Pharmaceuticals, Llc Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities
CA2743416A1 (en) * 2008-11-13 2010-05-20 Exelixis Inc. Methods of preparing quinoline derivatives
US20130030172A1 (en) * 2008-12-04 2013-01-31 Exelixis, Inc. Methods of Preparing Quinoline Derivatives
DE102009003975A1 (de) 2009-01-07 2010-07-08 Merck Patent Gmbh Benzothiazolonderivate
TW201920110A (zh) * 2009-01-16 2019-06-01 美商艾克塞里克斯公司 包含n-(4-{[6,7-雙(甲氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲醯胺之蘋果酸鹽之醫藥組合物及其用途
EP2210891A1 (en) * 2009-01-26 2010-07-28 Domain Therapeutics New adenosine receptor ligands and uses thereof
EP2408300B1 (en) * 2009-03-21 2016-05-11 Sunshine Lake Pharma Co., Ltd. Amino ester derivatives, salts thereof and methods of use
GEP20135907B (en) 2009-06-05 2013-08-12 Pfizer L-(piperidin-4-yl)-pyrazole derivatives as gpr 119 modulators
ES2463826T3 (es) 2009-06-08 2014-05-29 Gilead Sciences, Inc. Compuestos inhibidores de HDAC de cicloalquilcarbamato benzamida anilina
CA2763786C (en) 2009-06-08 2014-09-30 Gilead Sciences, Inc. Alkanoylamino benzamide aniline hdac inihibitor compounds
BR112012001118A2 (pt) 2009-07-17 2016-02-23 Exelixis Inc formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer
UA108618C2 (uk) * 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
CA2771403C (en) 2009-08-19 2015-02-24 Eisai R&D Management Co. Ltd. Quinoline derivative-containing pharmaceutical composition
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 (en) * 2009-10-16 2011-04-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Quinolinyloxyphenylsulfonamides
MX2012005155A (es) 2009-11-03 2012-08-31 Glaxosmithkline Llc Compuestos de quinazolina.
AU2010322796A1 (en) * 2009-11-27 2012-07-12 Proteologics, Ltd. Quinazolin-4(3A)-one derivatives and methods of use thereof
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.
EA201290906A1 (ru) * 2010-03-12 2013-03-29 Экселиксис, Инк. Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида
EP2553641A4 (en) * 2010-03-26 2015-01-07 EastNets MOBILE PAYMENT COMPUTING SYSTEM AND METHOD
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
EP2560488B1 (en) 2010-04-23 2015-10-28 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
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
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
EP2563773A1 (en) 2010-04-29 2013-03-06 Deciphera Pharmaceuticals, LLC Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activites
JP5960688B2 (ja) 2010-05-17 2016-08-02 インコゼン セラピューティクス プライベート リミテッド プロテインキナーゼ調節物質としての新規３，５−二置換−３ｈ−［１，２，３］トリアゾロ［４，５−ｂ］ピリジン化合物
CN102958523B (zh) 2010-06-25 2014-11-19 卫材R&D管理有限公司 使用具有激酶抑制作用的组合的抗肿瘤剂
EP2588107A1 (en) 2010-07-01 2013-05-08 Takeda Pharmaceutical Company Limited COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET
WO2012009722A1 (en) 2010-07-16 2012-01-19 Exelixis, Inc. C-met modulator pharmaceutical compositions
EP2593091A1 (en) 2010-07-16 2013-05-22 Exelixis, Inc. C-met modulator pharmaceutical compositions
EP2423208A1 (en) * 2010-08-28 2012-02-29 Lead Discovery Center GmbH Pharmaceutically active compounds as Axl inhibitors
US8664244B2 (en) * 2010-09-12 2014-03-04 Advenchen Pharmaceuticals, LLC Compounds as c-Met kinase inhibitors
EP2621482A1 (en) 2010-09-27 2013-08-07 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
HUE045810T2 (hu) * 2010-09-27 2020-01-28 Exelixis Inc MET és VEGF kettõs inhibitorai kasztrációrezisztens prosztatarák és oszteoblasztos csontáttétek kezelésére
WO2012044577A1 (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
WO2012042421A1 (en) 2010-09-29 2012-04-05 Pfizer Inc. Method of treating abnormal cell growth
US20130252956A1 (en) * 2010-11-22 2013-09-26 Howard Kallender Methods 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
TW201309650A (zh) 2011-02-10 2013-03-01 艾克塞里克斯公司 製造喹啉化合物之方法及包含該化合物之醫藥組合物
JP6026441B2 (ja) 2011-03-04 2016-11-16 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ キナーゼ阻害剤としてのアミノキノリン
US20120252840A1 (en) * 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
AU2012246490B2 (en) 2011-04-18 2016-08-04 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
US8759380B2 (en) 2011-04-22 2014-06-24 Cytokinetics, Inc. Certain heterocycles, compositions thereof, and methods for their use
EP2704717A1 (en) * 2011-05-02 2014-03-12 Exelixis, Inc. Method of treating cancer and bone cancer pain
JP6038128B2 (ja) 2011-06-03 2016-12-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー
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
WO2013036676A1 (en) 2011-09-06 2013-03-14 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
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
PL2768796T3 (pl) * 2011-10-20 2020-05-18 Exelixis, Inc. Sposób wytwarzania pochodnych chinoliny
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.
WO2013070903A1 (en) 2011-11-08 2013-05-16 Exelixis, Inc. Method of quantifying cancer treatment
AR092289A1 (es) 2011-11-14 2015-04-15 Sunshine Lake Pharma Co Ltd Derivados de aminoquinazolina y sus sales y metodos de uso
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 (en) 2012-01-27 2017-11-01 Optim Corporation Portable terminal, method, and program of changing user interface
US9358235B2 (en) * 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
CN104321322A (zh) 2012-03-30 2015-01-28 理森制药股份公司 作为c-met蛋白激酶调节剂的新型3,5-二取代-3h-咪唑并[4,5-b]吡啶和3,5-二取代-3h-[1,2,3]三唑并[4,5-b]吡啶化合物
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
HK1207587A1 (en) 2012-05-02 2016-02-05 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
AR092529A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de aminoquinazolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
AR092530A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de amino-quinolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
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
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
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
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
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
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
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
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
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
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
JPWO2014098176A1 (ja) 2012-12-21 2017-01-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体のアモルファス及びその製造方法
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
CN105143208B (zh) 2013-02-21 2017-09-26 葛兰素史密斯克莱知识产权发展有限公司 作为激酶抑制剂的喹唑啉
CN105121404A (zh) * 2013-03-15 2015-12-02 豪夫迈·罗氏有限公司 作为RORc调节剂的芳基磺酰胺和氨基磺酸衍生物
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
GEP20196995B (en) * 2013-03-15 2019-07-25 Inc Exelixis Metabolites of n-(4-{[6,7-bis (methyloxy)quinolin-4-yl] oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
ES2927651T3 (es) 2013-04-04 2022-11-10 Exelixis Inc Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer
EP2983639A1 (en) * 2013-04-04 2016-02-17 Exelixis, Inc. Drug combinations to treat 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
CA2912219C (en) 2013-05-14 2021-11-16 Eisai R&D Management 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
US11136625B2 (en) 2013-08-28 2021-10-05 Crown Bioscience, Inc. (Taicang) Gene expression signatures predictive of subject response to a multi-kinase inhibitor and methods of using the same
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
EA032757B1 (ru) 2014-02-14 2019-07-31 Экселиксис, Инк. Кристаллические твердые формы n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и способы применения
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
CN106029632B (zh) * 2014-02-28 2019-06-21 国立大学法人东北大学 酰胺衍生物
CN106255499A (zh) 2014-03-17 2016-12-21 埃克塞里艾克西斯公司 卡博替尼制剂的给药
EP3122900A1 (en) 2014-03-24 2017-02-01 F. Hoffmann-La Roche AG Cancer treatment with c-met antagonists and correlation of the latter with hgf expression
JP6696908B2 (ja) 2014-04-25 2020-05-20 エグゼリクシス， インコーポレイテッド 肺腺癌の治療方法
US9815789B2 (en) 2014-05-23 2017-11-14 Mylan Laboratories, Ltd. Polymorphs of cabozantinib (S)-malate and cabozantinib free 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
EA033834B1 (ru) * 2014-07-31 2019-11-29 Exelixis Inc Способ получения кабозантиниба, меченного фтором-18, и его аналогов
MA40457A (fr) * 2014-08-05 2017-06-14 Exelixis Inc Combinaison de médicaments pour traiter le myélome multiple
EP3187491A4 (en) 2014-08-28 2018-08-01 Eisai R&D Management Co., Ltd. High-purity quinoline derivative and method for manufacturing same
EP3194030B1 (en) 2014-09-19 2019-11-06 New York Blood Center, Inc. Substituted phenylpyrrolecarboxamides with therapeutic activity in hiv
CN107207471B (zh) 2014-12-02 2020-06-26 伊尼塔公司 用于治疗神经母细胞瘤的组合
EP3229836B1 (en) 2014-12-09 2019-11-13 Institut National de la Sante et de la Recherche Medicale (INSERM) Human monoclonal antibodies against axl
US20180028662A1 (en) 2015-02-25 2018-02-01 Eisai R&D Management Co., Ltd. Method for Suppressing Bitterness of Quinoline Derivative
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
KR20240064733A (ko) 2015-03-04 2024-05-13 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
US10053427B2 (en) 2015-03-25 2018-08-21 Sandoz Ag Crystalline forms of cabozantinib phosphate and cabozantinib hydrochloride
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
CA2988707C (en) 2015-06-16 2023-10-10 Eisai R&D Management Co., Ltd. Combination of cbp/catenin inhibitor and immune checkpoint inhibitor for treating cancer
US20170020856A1 (en) * 2015-06-29 2017-01-26 Ontogenesis, Llc N-Acylalkyl Prodrugs of Multi-Tyrosine Kinase Inhibitors and Methods of Use
CN107646030A (zh) * 2015-08-19 2018-01-30 桑多斯股份公司 丙二酸酯衍生物的不对称双酰胺化
CN108135894B (zh) 2015-08-20 2021-02-19 卫材R&D管理有限公司 肿瘤治疗剂
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
BR112018012255A2 (pt) 2015-12-18 2018-12-04 Ignyta Inc método para tratar câncer
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
WO2017173049A1 (en) * 2016-03-31 2017-10-05 Merck Patent Gmbh Compounds for the inhibition of cyclophilins and uses thereof
US11141413B2 (en) 2016-04-15 2021-10-12 Exelixis, Inc. Method of treating renal cell carcinoma using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2S)-hydroxybutanedioate
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
AU2017336547A1 (en) 2016-09-27 2019-05-02 The United States Of America, As Represented By The Secretary, Department Of Health & Human Services Method of treating urothelial carcinoma and other genitourinary malignancies using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
US10723701B2 (en) 2016-10-18 2020-07-28 Beijing Konruns Pharmaceutical Co., Ltd. Quinolyl-substituted carboxylic acid compound or pharmaceutically acceptable salt thereof, pharmaceutical composition of the same, and use of the same
WO2018102455A1 (en) 2016-12-01 2018-06-07 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
UA126970C2 (uk) 2017-01-20 2023-03-01 Екселіксіс, Інк. Комбінації кабозантинібу і атезолізумабу для лікування раку
CN110072528B (zh) 2017-02-08 2022-04-26 卫材R&D管理有限公司 治疗肿瘤的药物组合物
DK3583943T3 (da) 2017-02-15 2024-10-14 Taiho Pharmaceutical Co Ltd Farmaceutisk sammensætning
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
US11053223B2 (en) * 2017-04-27 2021-07-06 Astrazeneca Ab Phenoxyquinazoline compounds and their use in treating cancer
WO2018212202A1 (en) 2017-05-16 2018-11-22 Eisai R&D Management Co., Ltd. Treatment of hepatocellular carcinoma
MX2019012505A (es) 2017-05-26 2019-12-19 Exelixis Inc Formas solidas cristalinas de sales de ciclopropano-1,1-dicarboxam ida de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofen il), procesos para realizarlas y metodos de uso.
US11504362B2 (en) 2017-06-09 2022-11-22 Exelixis, Inc. Liquid dosage forms to treat cancer
EP3651762B1 (en) 2017-07-12 2024-07-03 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
ES3002968T3 (en) 2017-07-14 2025-03-10 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
AU2018325445A1 (en) * 2017-08-31 2020-03-19 Abbvie Inc. Ectonucleotide pyrophosphatase-phosphodiesterase 1 (ENPP-1) inhibitors and uses thereof
EP3682882A4 (en) 2017-09-08 2021-06-02 Taiho Pharmaceutical Co., Ltd. ANTI-TUMOR AGENT AND ANTI-TUMOR POTENTIALIZER
WO2019077506A1 (en) 2017-10-17 2019-04-25 Ignyta, Inc. PHARMACEUTICAL COMPOSITIONS AND SOLID GALENIC FORMS
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
ES2982890T3 (es) 2017-10-31 2024-10-18 Univ Vanderbilt Antagonistas del receptor muscarínico de acetilcolina M4
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
SG11202005719UA (en) * 2017-12-20 2020-07-29 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
AU2019212800B2 (en) * 2018-01-26 2024-05-23 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders
HRP20251184T1 (hr) * 2018-01-26 2025-12-05 Exelixis, Inc. Spojevi za liječenje poremećaja ovisnih o kinazi
SG11202006945PA (en) * 2018-01-26 2020-08-28 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
CA3090130A1 (en) 2018-02-02 2019-08-08 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
KR102433023B1 (ko) 2018-02-11 2022-08-16 베이징 사이텍-엠큐 파마슈티컬즈 리미티드 디옥시노퀴놀린 화합물, 이의 제조방법 및 용도
WO2019180141A1 (en) 2018-03-23 2019-09-26 Bayer Aktiengesellschaft Combinations of rogaratinib
WO2019234761A1 (en) 2018-06-05 2019-12-12 Natco Pharma Limited An improved process for the preparation of cabozantinib and its pharmaceutically acceptable salts thereof
TWI787523B (zh) 2018-06-15 2022-12-21 漢達生技醫藥股份有限公司 達沙替尼十二烷基硫酸鹽之結晶
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
PL3894012T4 (pl) * 2018-12-13 2026-01-05 Exelixis, Inc. Postacie krystaliczne i postacie soli inhibitora kinazy
BR112021011894A2 (pt) 2018-12-21 2021-09-08 Daiichi Sankyo Company, Limited Composição farmacêutica
EP3914356A1 (en) * 2019-01-25 2021-12-01 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
AU2020271855B2 (en) * 2019-04-12 2025-11-27 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
KR102826380B1 (ko) * 2019-06-03 2025-06-26 엑셀리시스, 인코포레이티드 카이네이스 저해제의 결정질 염 형태
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
US20240190825A1 (en) * 2021-03-24 2024-06-13 Biocon Limited Process for preparation of cabozantinib
KR20240026985A (ko) * 2021-06-25 2024-02-29 아카데미아 시니카 상피 세포 부착 분자(epcam) 억제제 및 간세포 성장 인자 수용체(hgfr) 억제제와의 조합된 암 요법
KR20230064560A (ko) * 2021-10-29 2023-05-10 보로노이바이오 주식회사 퀴나졸린 유도체 화합물 및 이의 용도
US20250129067A1 (en) 2021-11-08 2025-04-24 Progentos Therapeutics, Inc. Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
CN118339144A (zh) * 2021-12-03 2024-07-12 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
US20250171403A1 (en) 2022-03-01 2025-05-29 Synthon B.V. Cabozantinib salt with l-(+)-tartaric acid and solid forms thereof
WO2023222946A1 (en) 2022-05-18 2023-11-23 Fermion Oy Process for the preparation of cabozantinib
CN119255825A (zh) 2022-05-24 2025-01-03 第一三共株式会社 抗-cdh6抗体-药物缀合物的剂量方案
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
KR20250136810A (ko) 2023-01-31 2025-09-16 한다 온콜로지, 엘엘씨 개선된 카보잔티닙 조성물 및 사용 방법
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
WO2026074526A1 (en) 2024-10-04 2026-04-09 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
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
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
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 (enExample) 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
US5650415A (en) * 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
NZ311000A (en) 1995-06-07 1999-04-29 Smithkline Beecham Biolog Vaccine comprising a polysaccharide antigen-carrier protein conjugate and a free carrier protein
JPH11507052A (ja) * 1995-06-07 1999-06-22 スージェン・インコーポレーテッド キナゾリンおよび医薬組成物
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
DE69622183D1 (de) * 1995-11-07 2002-08-08 Kirin Brewery Chinolinderivate und chinazolinderivate welche die autophosphorylierung des von blutplättchen abstammenden wachstumsfaktorrezeptors inhibiren und sie enthaltende pharmazeutische zusammensetzungen
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
CA2242425C (en) 1996-02-13 2006-07-18 Zeneca Limited Quinazoline derivatives as vegf inhibitors
GB9603095D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
NZ331191A (en) 1996-03-05 2000-03-27 Zeneca Ltd 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof
EP0888310B1 (en) * 1996-03-15 2005-09-07 AstraZeneca AB Cinnoline derivatives and use as medicine
US6107300A (en) * 1996-03-27 2000-08-22 Dupont Pharmaceuticals Arylamino fused pyrimidines
CN100503580C (zh) * 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
US6391874B1 (en) * 1996-07-13 2002-05-21 Smithkline Beecham Corporation Fused heterocyclic compounds as protein tyrosine kinase inhibitors
CN1252054C (zh) 1996-09-25 2006-04-19 曾尼卡有限公司 抑制生长因子的作用的喹啉衍生物
GB9718972D0 (en) * 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
AU719392B2 (en) * 1996-10-01 2000-05-11 Kyowa Hakko Kirin Co., Ltd. Nitrogen-containing heterocyclic compounds
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
JP4303792B2 (ja) 1997-04-18 2009-07-29 協和発酵キリン株式会社 キノロン誘導体の製造方法
DK0977737T3 (da) 1997-04-22 2004-01-26 Janssen Pharmaceutica Nv CRF-antagonistisk quino- og quinazoline
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
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
HUP0102793A3 (en) * 1998-05-28 2002-07-29 Parker Hughes Inst St Paul Quinazolines for treating brain tumor and medicaments containing them
ES2342240T3 (es) * 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
AU5682799A (en) * 1998-08-21 2000-03-14 Parker Hughes Institute Quinazoline derivatives
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
AU5404399A (en) 1998-09-10 2000-04-03 Ipr-Institute For Pharmaceutical Research Ag Topical application products
US6288082B1 (en) * 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
CZ303899B6 (cs) 1998-09-29 2013-06-19 Wyeth Holdings Corporation Substituovaný 3-kyanochinolin, zpusob jeho prípravy a farmaceutická kompozice s jeho obsahem
CN1158266C (zh) 1998-10-01 2004-07-21 阿斯特拉曾尼卡有限公司 化合物
ES2241324T3 (es) 1998-10-08 2005-10-16 Astrazeneca Ab Derivados de quinazolina.
CN1160338C (zh) * 1998-11-19 2004-08-04 沃尼尔·朗伯公司 N-[4-(3-氯-4-氟-苯基氨基)-7-(3-吗啉-4-基-丙氧基)-喹唑啉-6-基]-丙烯酰胺,不可逆的酪氨酸激酶抑制剂
IL144461A0 (en) * 1999-01-22 2002-05-23 Kirin Brewery Quinoline and quinazoline derivatives and pharmaceutical compositions containing them
EE05345B1 (et) 1999-02-10 2010-10-15 Astrazeneca Ab Kinasoliini derivaadid angiogeneesi inhibiitoritena
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
JP2002539262A (ja) 1999-03-19 2002-11-19 パーカー ヒューズ インスティテュート キナゾリン化合物製剤および治療におけるその使用
YU13200A (sh) * 1999-03-31 2002-10-18 Pfizer Products Inc. Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja
GB9910580D0 (en) * 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9910577D0 (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
NZ516633A (en) * 1999-06-21 2004-09-24 Boehringer Ingelheim Pharma Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof
EE200200119A (et) * 1999-09-21 2003-04-15 Astrazeneca Ab Kinasoliini derivaadid ja nende kasutamine ravimitena
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
AU4903201A (en) * 1999-11-30 2001-07-03 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20020002169A1 (en) * 1999-12-08 2002-01-03 Griffin John H. Protein kinase inhibitors
EP1243582A4 (en) * 1999-12-24 2003-06-04 Kirin Brewery CHINOLINE AND CHINAZOLINE DERIVATIVES AND MEDICATIONS CONTAINING THEM
US6525046B1 (en) * 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
EP1294709A2 (en) * 2000-01-28 2003-03-26 AstraZeneca AB Quinoline derivatives and their use as aurora 2 kinase inhibitors
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
PL357099A1 (en) * 2000-02-07 2004-07-12 Abbott Gmbh & Co.Kg 2-benzothiazolyl urea derivatives and their use as protein kinase inhibitors
AU4545201A (en) 2000-03-13 2001-09-24 American Cyanamid Co Method of treating or inhibiting colonic polyps
US6608048B2 (en) * 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
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
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
CN1437594A (zh) * 2000-06-22 2003-08-20 辉瑞产品公司 用于治疗异常细胞生长的取代的双环衍生物
BR0111754A (pt) 2000-06-28 2003-04-29 Astrazeneca Ab Uso de um composto, método para inibir aurora 2 quinase em um animal de sangue quente, composto, e, composição farmacêutica
EP1174118A1 (de) 2000-06-28 2002-01-23 Cognis France S.A. Verwendung von Inulinen und Inulinderivaten
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
CA2417500C (en) * 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
AU2001278609B2 (en) 2000-08-21 2005-04-14 Astrazeneca Ab Quinazoline derivatives
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
DE10042058A1 (de) 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
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
US6740651B2 (en) * 2000-08-26 2004-05-25 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
WO2002030926A1 (en) 2000-10-13 2002-04-18 Astrazeneca Ab Quinazoline derivatives
WO2002030924A1 (en) 2000-10-13 2002-04-18 Astrazeneca Ab Quinazoline derivatives with anti-tumour activity
KR100600550B1 (ko) * 2000-10-20 2006-07-13 에자이 가부시키가이샤 질소 함유 방향환 유도체
US20040063733A1 (en) 2000-10-25 2004-04-01 Lambert Christine Marie Paul Quinazoline derivatives
US7220751B2 (en) 2000-11-02 2007-05-22 Nippon Shinyaku Co., Ltd. Quinazoline derivatives and drugs
US7067532B2 (en) 2000-11-02 2006-06-27 Astrazeneca Substituted quinolines as antitumor agents
WO2002036570A1 (en) 2000-11-02 2002-05-10 Astrazeneca Ab 4-substituted quinolines as antitumor agents
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
ATE409185T1 (de) 2001-04-19 2008-10-15 Astrazeneca Ab Chinazolin derivate
EP1382604B1 (en) 2001-04-27 2005-12-28 Kirin Beer Kabushiki Kaisha Quinoline derivative having azolyl group and quinazoline derivative
SE0101675D0 (sv) 2001-05-11 2001-05-11 Astrazeneca Ab Novel composition
WO2002092579A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab 4-anilinoquinazoline derivatives
WO2002092577A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2002092578A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline 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
US7132427B2 (en) 2001-06-21 2006-11-07 Ariad Pharmaceuticals, Inc. Quinazolines and uses thereof
CA2454538A1 (en) * 2001-06-22 2003-01-03 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives capable of inhibiting autophosphorylation of hepatocyte growth factor receptors, and pharmaceutical composition comprising the same
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
JP4383870B2 (ja) * 2001-10-17 2009-12-16 協和発酵キリン株式会社 線維芽細胞増殖因子受容体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
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
US6821988B2 (en) * 2001-11-27 2004-11-23 Wyeth Holdings Corporation 3-cyanoquinolines as inhibitors of EGF-R and HER2 kinases
AU2002347336A1 (en) 2001-12-05 2003-06-17 Astrazeneca Ab Quinoline derivatives
AU2002347359A1 (en) 2001-12-05 2003-06-17 Astrazeneca Ab Quinoline derivatives
GB0129099D0 (en) 2001-12-05 2002-01-23 Astrazeneca Ab Chemical compounds
IL161908A0 (en) * 2001-12-12 2005-11-20 Pfizer Prod Inc Quinazoline derivatives for the treatment of abnormal cell growth
CN1608062A (zh) 2001-12-12 2005-04-20 辉瑞产品公司 E－2－甲氧基－n－(3－{4－[3－甲基－4－(6－甲基－吡啶－3－基氧基) －苯氨基]－喹唑啉－6基}－烯丙基)－乙酰胺的盐，其制备和抗癌用途
WO2003055866A1 (en) 2001-12-21 2003-07-10 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
ATE446093T1 (de) 2001-12-24 2009-11-15 Astrazeneca Ab Substituierte chinazolin-derivate als aurora- kinase inhibitoren
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
US7109213B2 (en) 2002-01-29 2006-09-19 Glaxo Group Limited Aminopiperidine compounds, process for their preparation, and pharmaceutical compositions containing them
EP2292615A1 (en) 2002-02-01 2011-03-09 AstraZeneca AB Quinazoline compounds
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
JPWO2003093238A1 (ja) * 2002-05-01 2005-09-08 麒麟麦酒株式会社 マクロファージコロニー刺激因子受容体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
EP1521747B1 (en) 2002-07-15 2018-09-05 Symphony Evolution, Inc. Receptor-type kinase modulators and methods of use
AU2003257666A1 (en) * 2002-08-23 2004-03-11 Kirin Beer Kabushiki Kaisha COMPOUND HAVING TGFss INHIBITORY ACTIVITY AND MEDICINAL COMPOSITION CONTAINING THE SAME
GB0219746D0 (en) 2002-08-23 2002-10-02 Inst Of Ex Botany Ascr Azapurine derivatives
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
WO2004039782A1 (ja) * 2002-10-29 2004-05-13 Kirin Beer Kabushiki Kaisha 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
RU2350618C2 (ru) 2002-11-04 2009-03-27 Астразенека Аб ПРОИЗВОДНЫЕ ХИНАЗОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ Src ТИРОЗИНКИНАЗЫ
AU2003296984A1 (en) 2002-12-13 2004-07-09 Neurogen Corporation 2-substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators
KR20050085749A (ko) 2002-12-18 2005-08-29 화이자 프로덕츠 인크. 비정상적 세포 성장의 치료를 위한 4-아닐리노 퀴나졸린유도체
WO2004058267A1 (en) 2002-12-23 2004-07-15 Ariad Pharmaceuticals, Inc. Heterocycles and uses thereof
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
WO2005005389A2 (en) 2003-07-07 2005-01-20 Merck Patent Gmbh Malonamide derivatives
EP2210607B1 (en) * 2003-09-26 2011-08-17 Exelixis Inc. N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer
US7626030B2 (en) 2004-01-23 2009-12-01 Amgen Inc. Compounds and methods of use
US20050288290A1 (en) * 2004-06-28 2005-12-29 Borzilleri Robert M Fused heterocyclic kinase inhibitors
CA2572331A1 (en) * 2004-07-02 2006-02-09 Exelixis, Inc. C-met modulators and method of use
WO2006108059A1 (en) * 2005-04-06 2006-10-12 Exelixis, Inc. C-met modulators and methods of use
US7594258B2 (en) * 2005-06-27 2009-09-22 Yahoo! Inc. Access control systems and methods using visibility tokens with automatic propagation
WO2008035209A2 (en) * 2006-05-30 2008-03-27 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
AU2009300328A1 (en) 2008-10-01 2010-04-08 Ludwig Institute For Cancer Research Methods for the treatment of cancer
US20130030172A1 (en) * 2008-12-04 2013-01-31 Exelixis, Inc. Methods of Preparing Quinoline Derivatives
TW201920110A (zh) * 2009-01-16 2019-06-01 美商艾克塞里克斯公司 包含n-(4-{[6,7-雙(甲氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲醯胺之蘋果酸鹽之醫藥組合物及其用途
BR112012001118A2 (pt) * 2009-07-17 2016-02-23 Exelixis Inc formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer
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
SI2392564T1 (sl) 2014-02-28
BE2014C055I2 (enExample) 2023-12-14
AU2010204461A1 (en) 2010-08-19
US20170355678A1 (en) 2017-12-14
EP2409704A2 (en) 2012-01-25
HUS1400052I1 (hu) 2022-02-28
EP2213661A1 (en) 2010-08-04
ES2371383T3 (es) 2011-12-30
EP2392564A1 (en) 2011-12-07
JP2014055190A (ja) 2014-03-27
CA2744997A1 (en) 2005-04-07
HK1141799A1 (en) 2010-11-19
US20200331860A1 (en) 2020-10-22
FR14C0067I2 (fr) 2015-11-20
PT2213661E (pt) 2011-12-15
US20140155378A9 (en) 2014-06-05
HK1164312A1 (en) 2012-09-21
WO2005030140A2 (en) 2005-04-07
EP2392564B1 (en) 2013-10-23
SI2213661T1 (sl) 2011-11-30
EP2210607B1 (en) 2011-08-17
HRP20140012T1 (hr) 2014-02-14
US20070225307A1 (en) 2007-09-27
JP2015131859A (ja) 2015-07-23
WO2005030140A3 (en) 2005-05-19
PL2210607T3 (pl) 2012-01-31
HK1256476A1 (en) 2019-09-27
JP2017160270A (ja) 2017-09-14
JP2011042686A (ja) 2011-03-03
PL2213661T3 (pl) 2011-12-30
US20150376133A1 (en) 2015-12-31
ATE520403T1 (de) 2011-09-15
CA2537812A1 (en) 2005-04-07
JP5325172B2 (ja) 2013-10-23
EP2392565B1 (en) 2014-03-19
HK1143068A1 (en) 2010-12-24
EP2609919A3 (en) 2014-02-26
ES2651730T3 (es) 2018-01-29
CY2014037I1 (el) 2015-11-04
FR14C0067I1 (enExample) 2014-10-17
EP2409704B1 (en) 2017-09-20
JP5185331B2 (ja) 2013-04-17
US20110077233A1 (en) 2011-03-31
JP2010235631A (ja) 2010-10-21
JP4638436B2 (ja) 2011-02-23
ES2925655T3 (es) 2022-10-19
JP2014055191A (ja) 2014-03-27
AU2004275842A1 (en) 2005-04-07
US20160185725A1 (en) 2016-06-30
PL2392565T3 (pl) 2014-08-29
AU2004275842B2 (en) 2010-09-02
JP2010265302A (ja) 2010-11-25
JP5325173B2 (ja) 2013-10-23
US20090170896A1 (en) 2009-07-02
US7579473B2 (en) 2009-08-25
DK2210607T3 (da) 2011-12-12
ES2369652T3 (es) 2011-12-02
JP2007506777A (ja) 2007-03-22
PT2210607E (pt) 2012-01-31
US11124482B2 (en) 2021-09-21
US20210253530A9 (en) 2021-08-19
US20120184523A1 (en) 2012-07-19
ATE517091T1 (de) 2011-08-15
EP1673085A4 (en) 2008-12-10
SI2210607T1 (sl) 2011-11-30
US8476298B2 (en) 2013-07-02
US9174947B2 (en) 2015-11-03
EP2213661B1 (en) 2011-07-20
DK2213661T3 (da) 2011-09-19
JP5185332B2 (ja) 2013-04-17
AU2010204461B2 (en) 2013-06-20
JP2014074059A (ja) 2014-04-24
CY1112056T1 (el) 2015-11-04
DK2392565T3 (da) 2014-05-05
ES2466818T3 (es) 2014-06-11
JP2019070015A (ja) 2019-05-09
US8178532B2 (en) 2012-05-15
CY2014037I2 (el) 2019-07-10
US8067436B2 (en) 2011-11-29
US20120022065A1 (en) 2012-01-26
EP1673085A2 (en) 2006-06-28
EP2210607A1 (en) 2010-07-28
EP2392565A1 (en) 2011-12-07
US20070244116A1 (en) 2007-10-18
AU2010204459A1 (en) 2010-08-19
EP3329918A3 (en) 2018-08-15
JP2024023447A (ja) 2024-02-21
NL300678I2 (enExample) 2017-01-31
US20130252940A1 (en) 2013-09-26
ATE532782T1 (de) 2011-11-15
HRP20110810T1 (hr) 2011-12-31
US20070054928A1 (en) 2007-03-08
EP3329918A2 (en) 2018-06-06
HRP20140563T1 (hr) 2014-07-18
AU2010204459B2 (en) 2013-06-20
HK1164313A1 (en) 2012-09-21
EP2609919A2 (en) 2013-07-03
JP2010280674A (ja) 2010-12-16
JP5694501B2 (ja) 2015-04-01
EP2409704A3 (en) 2013-02-13
EP1673085B1 (en) 2011-11-09
CA2537812C (en) 2013-01-22
SI2392565T1 (sl) 2014-05-30
EP3329918B1 (en) 2022-05-25
US20140155396A1 (en) 2014-06-05
EP2612853A1 (en) 2013-07-10
JP2021050233A (ja) 2021-04-01
CY1111956T1 (el) 2015-11-04
US20090105299A1 (en) 2009-04-23
DK2392564T3 (da) 2014-01-13
ES2436888T3 (es) 2014-01-07
JP2010235632A (ja) 2010-10-21
HRP20110707T1 (hr) 2011-10-31
US8497284B2 (en) 2013-07-30

Similar Documents

Publication Publication Date Title
NL300678I2 (enExample)
WO2006014325A3 (en) C-met modulators and method of use
ATE543821T1 (de) Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungen
EP1503757A4 (en) Tyrosine kinase inhibitor
WO2004092196A3 (en) Tie-2 modulators and methods of use
WO2004006846A3 (en) Receptor-type kinase modulators and methods of use
UA98449C2 (xx) ГЕТЕРОАРИЛЗАМІЩЕНІ ПІРОЛО$2,3-b]ПІРИДИНИ Й ПІРОЛО$2,3-b]ПІРИМІДИНИ ЯК ІНГІБІТОРИ ЯНУС-КІНАЗИ$ГЕТЕРОАРИЛЗАМЕЩЕННЫЕ ПИРРОЛО$2,3-b]ПИРИДИНЫ И ПИРРОЛО$2,3-b]ПИРИМИДИНЫ КАК ИНГИБИТОРЫ ЯНУС-КИНАЗЫ
BR0306988A (pt) Piridazinonas substituìdas como inibidores de p38
ATE331514T1 (de) Indolinonderivate zur abänderung der c-kit tyrosinproteinkinase
WO2004091480A3 (en) Tie-2 modulators and methods of use
DE60023926D1 (de) Tyrosin kinase inhibitoren
DE60018782D1 (de) Tyrosin kinase inhibitoren
ATE450530T1 (de) Zusammensetzungen zur verwendung als protein- kinase-inhibitoren
ATE303998T1 (de) Oral aktive salze mit tyrosinkinaseaktivität
ATE548363T1 (de) 3,5-disubstituierte pyrid-2-one, die sich als inhibitoren der tec-familie von nicht-rezeptor- tyrosinkinasen eignen
WO2005039506A3 (en) P70s6 kinase modulators and method of use
WO2004083235A3 (en) Tie-2 modulators and methods of use
WO2004050681A3 (en) Kinase modulators
ATE540951T1 (de) Substituierte 7,8-dihydro-1h-pyrimidoä4,5- büdiazepin-4-amine als kinase inhibitoren