CA2537812C - C-met modulators and method of use - Google Patents

C-met modulators and method of use Download PDF

Info

Publication number
CA2537812C
CA2537812C CA2537812A CA2537812A CA2537812C CA 2537812 C CA2537812 C CA 2537812C CA 2537812 A CA2537812 A CA 2537812A CA 2537812 A CA2537812 A CA 2537812A CA 2537812 C CA2537812 C CA 2537812C
Authority
CA
Canada
Prior art keywords
optionally substituted
quinolin
phenyl
fluoro
oxy
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
CA2537812A
Other languages
English (en)
French (fr)
Other versions
CA2537812A1 (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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Exelixis Inc
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=CA2537812(C) "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
Priority to CA2744997A priority Critical patent/CA2744997A1/en
Publication of CA2537812A1 publication Critical patent/CA2537812A1/en
Application granted granted Critical
Publication of CA2537812C publication Critical patent/CA2537812C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
CA2537812A 2003-09-26 2004-09-24 C-met modulators and method of use Expired - Lifetime CA2537812C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2744997A CA2744997A1 (en) 2003-09-26 2004-09-24 C-met modulators and method of use

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US50618103P 2003-09-26 2003-09-26
US60/506,181 2003-09-26
US53537704P 2004-01-09 2004-01-09
US60/535,377 2004-01-09
US57738404P 2004-06-04 2004-06-04
US60/577,384 2004-06-04
PCT/US2004/031523 WO2005030140A2 (en) 2003-09-26 2004-09-24 C-met modulators and methods of use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2744997A Division CA2744997A1 (en) 2003-09-26 2004-09-24 C-met modulators and method of use

Publications (2)

Publication Number Publication Date
CA2537812A1 CA2537812A1 (en) 2005-04-07
CA2537812C true CA2537812C (en) 2013-01-22

Family

ID=34397024

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2537812A Expired - Lifetime CA2537812C (en) 2003-09-26 2004-09-24 C-met modulators and method of use
CA2744997A Abandoned CA2744997A1 (en) 2003-09-26 2004-09-24 C-met modulators and method of use

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2744997A Abandoned CA2744997A1 (en) 2003-09-26 2004-09-24 C-met modulators and method of use

Country Status (19)

Country Link
US (14) US9174947B2 (en:Method)
EP (9) EP1673085B1 (en:Method)
JP (14) JP4638436B2 (en:Method)
AT (3) ATE517091T1 (en:Method)
AU (3) AU2004275842B2 (en:Method)
BE (1) BE2014C055I2 (en:Method)
CA (2) CA2537812C (en:Method)
CY (3) CY1111956T1 (en:Method)
DK (4) DK2213661T3 (en:Method)
ES (6) ES2369652T3 (en:Method)
FR (1) FR14C0067I2 (en:Method)
HR (4) HRP20110707T1 (en:Method)
HU (1) HUS1400052I1 (en:Method)
LU (1) LU92508I2 (en:Method)
NL (1) NL300678I2 (en:Method)
PL (3) PL2213661T3 (en:Method)
PT (2) PT2213661E (en:Method)
SI (4) SI2210607T1 (en:Method)
WO (1) WO2005030140A2 (en:Method)

Families Citing this family (280)

* 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
WO2002032872A1 (fr) 2000-10-20 2002-04-25 Eisai Co., Ltd. Composes a noyau aromatique azote
US7994159B2 (en) 2003-03-10 2011-08-09 Eisai R&D Management Co., Ltd. c-Kit kinase inhibitor
SI1667992T1 (sl) 2003-09-19 2007-06-30 Astrazeneca Ab Kinazolinski derivati
PT2213661E (pt) * 2003-09-26 2011-12-15 Exelixis Inc Moduladores de c-met e métodos de uso
CN100450998C (zh) 2003-11-11 2009-01-14 卫材R&D管理有限公司 脲衍生物的制备方法
US7750160B2 (en) * 2003-11-13 2010-07-06 Ambit Biosciences Corporation Isoxazolyl urea derivatives as kinase modulators
CA2553433A1 (en) * 2004-01-23 2005-08-11 Amgen Inc. Quinoline quinazoline pyridine and pyrimidine compounds and their use in the treatment of inflammation angiogenesis and cancer
AU2005217325B2 (en) * 2004-02-27 2007-11-29 Eisai R & D Management Co., Ltd. Novel pyridine derivative and pyrimidine derivative (1)
NZ588139A (en) 2004-04-08 2012-02-24 Targegen Inc 7-Aryl-3-arylamino-benzo[1,2,4]triazine derivatives
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
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
US7173031B2 (en) 2004-06-28 2007-02-06 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
EP1799656A4 (en) * 2004-08-25 2009-09-02 Targegen Inc HETEROCYCLIC COMPOUNDS AND METHODS OF USE
ATE428421T1 (de) 2004-09-17 2009-05-15 Eisai R&D Man Co Ltd Medizinische zusammensetzung mit verbesserter stabilität und reduzierten gelierungseigenschaften
AR051026A1 (es) 2004-09-20 2006-12-13 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
CA2580857A1 (en) 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
AU2005286648A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
WO2006034341A2 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
BRPI0515505A (pt) 2004-09-20 2008-07-29 Xenon Pharmaceuticals Inc derivados heterocìclicos e sua utilização como inibidores da estearoil-coa desaturase
MX2007003321A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
AU2005286728A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
MX2007004403A (es) 2004-10-12 2007-04-27 Astrazeneca Ab Derivados de quinazolina.
CA2587642C (en) 2004-11-30 2013-04-09 Amgen Inc. Substituted heterocycles and methods of use
US7576090B2 (en) * 2004-12-27 2009-08-18 4Sc Ag Benzazole analogues and uses thereof
EP1674466A1 (en) * 2004-12-27 2006-06-28 4Sc Ag 2,5- and 2,6-disubstituted benzazole analogues useful as protein kinase inhibitors
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
KR101378716B1 (ko) * 2005-05-20 2014-04-10 메틸진 인코포레이티드 Ｖｅｇｆ 수용체 및 ｈｇｆ 수용체 신호전달의 억제제
CA2607699A1 (en) * 2005-06-02 2006-12-07 Galaxy Biotech, Llc Methods of treating brain tumors with antibodies
MX2007015216A (es) 2005-06-03 2008-02-22 Xenon Pharmaceuticals Inc Derivados de aminotiazol y sus usos como agentes terapeuticos.
EP2281901B1 (en) 2005-08-02 2013-11-27 Eisai R&D Management Co., Ltd. Anti-tumour pharmaceutical composition with angiogenesis inhibitors
ES2424651T3 (es) 2005-08-24 2013-10-07 Eisai R&D Management Co., Ltd. Nuevo derivado de piridina y derivado de pirimidina (3)
PE20070335A1 (es) 2005-08-30 2007-04-21 Novartis Ag Benzimidazoles sustituidos y metodos para su preparacion
WO2007033196A1 (en) 2005-09-14 2007-03-22 Bristol-Myers Squibb Company Met kinase inhibitors
EP1964837A4 (en) * 2005-11-22 2010-12-22 Eisai R&D Man Co Ltd Antitumor agent against multiple myeloma
EP1989211A2 (en) * 2006-01-30 2008-11-12 Array Biopharma, Inc. Heterobicyclic thiophene compounds for the treatment of cancer
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
KR101464385B1 (ko) * 2006-04-19 2014-11-21 노파르티스 아게 ６-ｏ-치환된 벤즈옥사졸 및 벤조티아졸 화합물, 및 ｃｓｆ-１ｒ 신호전달의 억제 방법
ES2556173T3 (es) 2006-05-18 2016-01-13 Eisai R&D Management Co., Ltd. Agente antitumoral para un cáncer de tiroides
CA2647830C (en) 2006-05-19 2016-02-09 Abbott Laboratories Central nervous system active fused bicycloheterocycle substituted azabicyclic alkane derivatives
WO2008035209A2 (en) * 2006-05-30 2008-03-27 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
WO2007146824A2 (en) * 2006-06-08 2007-12-21 Array Biopharma Inc. Quinoline compounds and methods of use
CA2660836A1 (en) 2006-08-07 2008-02-21 Incyte Corporation Triazolotriazines as kinase inhibitors
EP2062886B1 (en) 2006-08-23 2011-11-30 Eisai R&D Management Co., Ltd. Salt of phenoxypyridine derivative or crystal thereof and process for producing the same
CN101511793B (zh) 2006-08-28 2011-08-03 卫材R&D管理有限公司 针对未分化型胃癌的抗肿瘤剂
US7790885B2 (en) 2006-08-31 2010-09-07 Eisai R&D Management Co., Ltd. Process for preparing phenoxypyridine derivatives
ES2555803T3 (es) 2006-10-23 2016-01-08 Cephalon, Inc. Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met
WO2008049855A2 (en) * 2006-10-27 2008-05-02 Glaxo Group Limited 7-azaindole derivatives as c-met kinase inhibitors
DK2497470T3 (en) 2006-11-22 2015-12-07 Incyte Holdings Corp Imidazotriaziner and imidazopyrimidines as kinase inhibitors
CA2672440A1 (en) * 2006-12-20 2008-07-03 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
US8551995B2 (en) * 2007-01-19 2013-10-08 Xcovery Holding Company, Llc Kinase inhibitor compounds
CN101600694A (zh) 2007-01-29 2009-12-09 卫材R&D管理有限公司 未分化型胃癌治疗用组合物
EA200901548A1 (ru) * 2007-05-21 2010-06-30 Новартис Аг Ингибиторы csf-1r, композиции и способы применения
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
CL2008002384A1 (es) 2007-08-15 2009-07-17 Glaxo Group Ltd Compuestos derivados de quinoliniloxipiperidina y pirrolidina, composicion farmaceutica, combinacion farmaceutica, util para el tratamiento de enfermedades inflamatorias y/o alergicas del tracto respiratorio.
WO2009026717A1 (en) 2007-08-29 2009-03-05 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
EP2218712B1 (en) 2007-11-09 2015-07-01 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
KR101608096B1 (ko) 2008-01-23 2016-03-31 브리스톨-마이어스 스큅 컴퍼니 ４-피리디논 화합물 및 암을 위한 그의 용도
MX2010010172A (es) 2008-03-17 2010-11-25 Ambit Biosciences Corp Derivados de quinazolina como moduladores de quinasa raf y metodos de uso de los mismos.
CA2720552C (en) 2008-04-10 2016-06-14 Taiho Pharmaceutical Co., Ltd. Acylthiourea compound or salt thereof, and use thereof
MX2010011224A (es) * 2008-04-16 2011-02-25 Max Planck Ges Zur Fa Rderung Der Wissenschaften E V Derivados de quinoleina como inhibidores de la cinasa axl.
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
CN103936743B (zh) 2008-05-21 2018-04-24 因西特控股公司 2-氟-N-甲基-4-[7-(喹啉-6-基甲基)咪唑并[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺的盐及与其相关的制备方法
US8344018B2 (en) 2008-07-14 2013-01-01 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
WO2010009155A2 (en) 2008-07-14 2010-01-21 Gilead Colorado, Inc. Fused heterocyclyc inhibitor compounds
AU2009271003A1 (en) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Imidazolylpyrimidine compounds as HDAC and/or CDK inhibitors
EP2149565A1 (de) * 2008-07-24 2010-02-03 Bayer Schering Pharma AG Sulfonsubstituierte Chinazolinderivate als Immunmodulatoren zur Behandlung von enzündlichen und allergischen Erkrankungen
US8088771B2 (en) 2008-07-28 2012-01-03 Gilead Sciences, Inc. Cycloalkylidene and heterocycloalkylidene inhibitor compounds
TW201035017A (en) * 2008-09-26 2010-10-01 Smithkline Beecham Corp Preparation of a quinolinyloxydiphenylcyclopropanedicarboxamide
JP5734193B2 (ja) * 2008-10-14 2015-06-17 クイ ニング 化合物及び使用方法
JP5444365B2 (ja) * 2008-10-29 2014-03-19 デシフェラ ファーマシューティカルズ，エルエルシー 抗癌活性および抗増殖活性を示すシクロプロパンアミドおよび類似物質
EA019247B1 (ru) * 2008-11-13 2014-02-28 Экселиксис, Инк. Способы получения хинолиновых производных
WO2010065838A1 (en) 2008-12-04 2010-06-10 Exelixis, Inc. Methods of preparing quinoline derivatives
DE102009003975A1 (de) 2009-01-07 2010-07-08 Merck Patent Gmbh Benzothiazolonderivate
PL2387563T5 (pl) 2009-01-16 2023-03-13 Exelixis, Inc. Sól jabłczanowa N-(4-{[6,7-bis(metyloksy)chinolin-4-ylo]oksy}fenylo-N′-(4-fluorofenylo)cykloproano-1,1-dikarboksyamidu oraz jej krystaliczne postaci do leczenia raka
EP2210891A1 (en) * 2009-01-26 2010-07-28 Domain Therapeutics New adenosine receptor ligands and uses thereof
JP5583751B2 (ja) * 2009-03-21 2014-09-03 クイ ニング アミノエステル誘導体、その塩、及び使用方法
PE20120399A1 (es) 2009-06-05 2012-04-24 Pfizer Derivados del l-(piperidin-4-il)-pirazol como moduladores de gpr 119
US8283357B2 (en) 2009-06-08 2012-10-09 Gilead Sciences, Inc. Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds
CA2763786C (en) 2009-06-08 2014-09-30 Gilead Sciences, Inc. Alkanoylamino benzamide aniline hdac inihibitor compounds
CA2768370A1 (en) * 2009-07-17 2011-01-20 Exelixis, Inc. Crystalline forms 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
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 (en) * 2009-10-16 2011-04-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Quinolinyloxyphenylsulfonamides
EA021439B1 (ru) * 2009-11-03 2015-06-30 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Хиназолиновые соединения
JP2013518810A (ja) * 2009-11-27 2013-05-23 プロテオロジクス リミテッド キナゾリン−４（３ａ）−オン誘導体とその使用方法
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
AU2011269788B2 (en) 2010-02-03 2015-12-10 Incyte Holdings Corporation Imidazo[1,2-b][1,2,4]triazines as c-Met inhibitors
CA2792852A1 (en) * 2010-03-12 2011-09-15 Exelixis, Inc. Hydrated crystalline forms 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
WO2011117741A2 (en) * 2010-03-26 2011-09-29 EastNets Mobile remittance computer 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
US9133123B2 (en) 2010-04-23 2015-09-15 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
WO2011139891A1 (en) 2010-04-29 2011-11-10 Deciphera Pharmaceuticals, Llc Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activites
EA201690998A1 (ru) 2010-05-17 2017-01-30 Инкозен Терапьютикс Пвт. Лтд. НОВЫЕ СОЕДИНЕНИЯ 3,5-ДИЗАМЕЩЕННОГО-3H-ИМИДАЗО[4,5-b]ПИРИДИНА И 3,5-ДИЗАМЕЩЕННОГО-3H-[1,2,3]ТРИАЗОЛО[4,5-b]ПИРИДИНА КАК МОДУЛЯТОРЫ ПРОТЕИНКИНАЗ
AU2011270165B2 (en) 2010-06-25 2015-12-24 Eisai R&D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
US20130315895A1 (en) 2010-07-01 2013-11-28 Takeda Pharmaceutical Company Limited COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET
US9724342B2 (en) * 2010-07-16 2017-08-08 Exelixis, Inc. C-met modulator pharmaceutical compositions
WO2012009723A1 (en) 2010-07-16 2012-01-19 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
EP2621483A1 (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
SI2621481T2 (sl) * 2010-09-27 2023-02-28 Exelixis, Inc., Dvojni inhibitorji MET in VEGF za zdravljenje proti kastraciji odpornega raka prostate in osteoblastnih kostnih metastaz
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
WO2012042421A1 (en) 2010-09-29 2012-04-05 Pfizer Inc. Method of treating abnormal cell growth
JP2013543011A (ja) * 2010-11-22 2013-11-28 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、ナンバー２、リミテッド 癌の治療法
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
EP2673262B1 (en) 2011-02-10 2021-11-03 Exelixis, Inc. Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
CA2829131C (en) 2011-03-04 2018-11-20 Glaxosmithkline Intellectual Property (No.2) Limited Amino-quinolines as kinase inhibitors
US20120252840A1 (en) * 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
KR101762999B1 (ko) 2011-04-18 2017-07-28 에자이 알앤드디 매니지먼트 가부시키가이샤 종양 치료제
US8759380B2 (en) 2011-04-22 2014-06-24 Cytokinetics, Inc. Certain heterocycles, compositions thereof, and methods for their use
UA115527C2 (uk) * 2011-05-02 2017-11-27 Екселіксіс, Інк. Застосування n-(4-{[6,7-бic(мeтилoкcи)xiнoлiн-4-iл]oкcи}фeнiл)-n'-(4-фтopфeнiл)циклoпpoпaн-1,1-дикapбoкcaмiду для лікування нирково-клітинної карциноми (варіанти)
US9945862B2 (en) 2011-06-03 2018-04-17 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
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
CA2848512A1 (en) 2011-09-22 2013-03-28 Exelixis, Inc. Method for treating osteoporosis
BR112014009302B1 (pt) * 2011-10-20 2020-04-28 Exelis Inc Us/Us processo para preparar derivados de quinolina
US8843421B2 (en) 2011-11-01 2014-09-23 Accenture Global Services Limited Identification of entities likely to engage in a behavior
AR088813A1 (es) 2011-11-08 2014-07-10 Exelixis Inc Metodo para cuantificar el tratamiento de cancer
TW201818937A (zh) 2011-11-08 2018-06-01 美商艾克塞里克斯公司 治療癌症之方法
AR092289A1 (es) 2011-11-14 2015-04-15 Sunshine Lake Pharma Co Ltd Derivados de aminoquinazolina y sus sales y metodos de uso
WO2013091507A1 (zh) * 2011-12-20 2013-06-27 Qian Wei 杂环胺基烷氧基取代的喹唑啉衍生物及其用途
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
EA026412B1 (ru) 2012-03-30 2017-04-28 Ризен Фармасьютикалз Са НОВЫЕ СОЕДИНЕНИЯ 3,5-ДИЗАМЕЩЕННОГО-3H-ИМИДАЗО[4,5-b]ПИРИДИНА И 3,5-ДИЗАМЕЩЕННОГО-3H-[1,2,3]ТРИАЗОЛО[4,5-b]ПИРИДИНА КАК МОДУЛЯТОРЫ c-MET ПРОТЕИНКИНАЗ
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
US9861624B2 (en) 2012-05-02 2018-01-09 Exelixis, Inc. Method of treating cancer
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
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
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
TW201425307A (zh) 2012-09-13 2014-07-01 Glaxosmithkline Llc 作為激酶抑制劑之胺基－喹啉類
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
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
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
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
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
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
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
WO2014098176A1 (ja) 2012-12-21 2014-06-26 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
RU2662810C2 (ru) 2013-02-21 2018-07-31 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Хиназолины в качестве ингибиторов киназы
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
WO2014145715A1 (en) * 2013-03-15 2014-09-18 Exelixis, Inc. Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
CA2902252A1 (en) * 2013-03-15 2014-09-18 Monique Bodil Van Niel Aryl sulfamide and sulfamate derivatives as rorc modulators
CN108472242A (zh) 2013-04-04 2018-08-31 埃克塞里艾克西斯公司 治疗癌症的药物组合
WO2014165786A1 (en) 2013-04-04 2014-10-09 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
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
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
SG11201509278XA (en) 2013-05-14 2015-12-30 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
EP3039424B1 (en) 2013-08-28 2020-07-29 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
CA3181899A1 (en) 2014-02-14 2015-08-20 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
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
KR102408123B1 (ko) * 2014-02-28 2022-06-10 고쿠리츠다이가쿠호진 도호쿠다이가쿠 아마이드 유도체
WO2015142928A1 (en) 2014-03-17 2015-09-24 Exelixis, Inc. Dosing of cabozantinib formulations
CA2943329A1 (en) 2014-03-24 2015-10-01 Genentech, Inc. Cancer treatment with c-met antagonists and correlation of the latter with hgf expression
SG11201608657QA (en) 2014-04-25 2016-11-29 Exelixis Inc Method of treating lung adenocarcinoma
EP3145913A1 (en) 2014-05-23 2017-03-29 Mylan Laboratories Ltd. Novel 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
EP3174854B1 (en) * 2014-07-31 2022-08-24 Exelixis, Inc. Method of preparing fluorine-18 labeled cabozantinib and its analogs
EP3177311B1 (en) 2014-08-05 2024-10-30 Exelixis, Inc. Drug combinations of cabozantinib with proteasome inhibitor to treat multiple myeloma
PL3524595T3 (pl) 2014-08-28 2022-10-31 Eisai R&D Management Co., Ltd. Pochodna chinoliny o wysokiej czystości i sposób jej wytwarzania
ES2764440T3 (es) 2014-09-19 2020-06-03 New York Blood Center Inc Fenilpirrolcarboxamidas sustituidas con actividad terapéutica en VIH
WO2016089760A1 (en) 2014-12-02 2016-06-09 Ignyta, Inc. Combinations for the treatment of neuroblastoma
ES2764299T3 (es) 2014-12-09 2020-06-02 Inst Nat Sante Rech Med Anticuerpos monoclonales humanos contra AXL
HUE064614T2 (hu) 2015-02-25 2024-04-28 Eisai R&D Man Co Ltd Eljárás egy kinolin-származék keserû ízének elnyomására
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
WO2016140717A1 (en) 2015-03-04 2016-09-09 Merck Sharp & Dohme Corp. Combination of a pd-1 antagonist and a vegfr/fgfr/ret tyrosine kinase inhibitor for treating cancer
EP3274332B1 (en) 2015-03-25 2018-12-19 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
ES2886107T3 (es) 2015-06-16 2021-12-16 Prism Biolab Co Ltd Antineoplásico
US20170020856A1 (en) * 2015-06-29 2017-01-26 Ontogenesis, Llc N-Acylalkyl Prodrugs of Multi-Tyrosine Kinase Inhibitors and Methods of Use
WO2017029362A1 (en) 2015-08-19 2017-02-23 Sandoz Ag Asymmetric bisamidation of malonic ester derivatives
US12220398B2 (en) 2015-08-20 2025-02-11 Eisai R&D Management Co., Ltd. Tumor therapeutic agent
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 (en) 2015-12-18 2019-12-18 Ignyta, Inc. COMBINATIONS FOR TREATING CANCER
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
WO2017181187A1 (en) 2016-04-15 2017-10-19 Exelixis, Inc. Method of treating renal cell carcinoma using n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluoropheny)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
CN109922790B (zh) * 2016-09-12 2022-06-14 珠海贝海生物技术有限公司 卡博替尼制剂
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
JP2019529476A (ja) 2016-09-27 2019-10-17 ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ Ｎ−（４−（６，７−ジメトキシキノリン−４−イルオキシ）フェニル）−ｎ’−（４−フルオロフェニル）シクロプロパン−１，１−ジカルボキサミドを用いた尿路上皮癌及び他の尿生殖器悪性腫瘍の治療方法
EP3530654B1 (en) * 2016-10-18 2022-12-14 Beijing Konruns Pharmaceutical Co., Ltd. Quinolinyl-substituted carboxylic acid compound or pharmaceutically acceptable salt thereof, pharmaceutical composition thereof, and use thereof
JP7105774B2 (ja) 2016-12-01 2022-07-25 イグナイタ インコーポレイテッド がん治療のための方法
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
KR102610764B1 (ko) 2017-01-20 2023-12-07 엑셀리시스, 인코포레이티드 암을 치료하기 위한 카보잔티닙 및 아테졸리주맙의 조합
KR102539920B1 (ko) 2017-02-08 2023-06-05 에자이 알앤드디 매니지먼트 가부시키가이샤 종양-치료용 약제학적 조성물
EP3583943B1 (en) 2017-02-15 2024-09-18 Taiho Pharmaceutical Co., Ltd. Pharmaceutical composition
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
JP7117323B2 (ja) * 2017-04-27 2022-08-12 アストラゼネカ・アクチエボラーグ フェノキシキナゾリン化合物及び癌の処置におけるそれらの使用
CA3061888A1 (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.
JP7249962B2 (ja) 2017-06-09 2023-03-31 エグゼリクシス， インコーポレイテッド がんを治療するための液体剤形
NZ761519A (en) 2017-07-14 2023-07-28 Innate Tumor Immunity Inc Nlrp3 modulators
KR102718538B1 (ko) 2017-07-19 2024-10-21 이그니타, 인코포레이티드 엔트렉티닙을 포함하는 약학적 조성물
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.
MA50251A (fr) 2017-09-08 2021-06-02 Taiho Pharmaceutical Co Ltd Agent antitumoral et potentialisateur d'effet antitumoral
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
IL273924B2 (en) 2017-10-20 2024-07-01 Univ Vanderbilt Muscarinic acetylcholine M4 receptor antagonists
EP3703680B1 (en) 2017-10-31 2024-05-15 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor 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
EP3727364A4 (en) * 2017-12-20 2021-08-11 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
WO2019148036A1 (en) * 2018-01-26 2019-08-01 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders
EP3743070B1 (en) * 2018-01-26 2025-07-23 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders
IL276411B2 (en) 2018-02-02 2024-04-01 Univ Vanderbilt M4 muscarinic acetylcholine receptor antagonists
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
CA3090876C (en) 2018-02-11 2022-12-06 Beijing Scitech-Mq Pharmaceuticals Limited Dioxinoquinoline compounds, preparation method and uses thereof
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
CN115192540A (zh) 2018-06-15 2022-10-18 汉达癌症医药责任有限公司 激酶抑制剂的盐类及其组合物
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
SI3894012T1 (sl) * 2018-12-13 2025-10-30 Exelixis, Inc. Kristalinične oblike in oblike soli kinaznega inhibitorja
JPWO2020130125A1 (ja) 2018-12-21 2021-11-04 第一三共株式会社 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
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
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
JP7579281B2 (ja) * 2019-06-03 2024-11-07 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塩形態
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
IL303655A (en) * 2020-12-17 2023-08-01 Astrazeneca Ab N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)- quinoline-4-carboxamides
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
CA3237696A1 (en) 2021-11-08 2023-05-11 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
JP2025506934A (ja) 2022-03-01 2025-03-13 シントン・ビー．ブイ． カボザンチニブのｌ－（＋）－酒石酸塩とその固体
WO2023222946A1 (en) 2022-05-18 2023-11-23 Fermion Oy Process for the preparation of cabozantinib
JP2025517908A (ja) 2022-05-24 2025-06-12 第一三共株式会社 抗ｃｄｈ６抗体－薬物コンジュゲートの投薬量レジメン
IL318241A (en) 2022-07-08 2025-03-01 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors in combination with HGF receptor inhibitors for cancer treatment
WO2024110606A1 (en) 2022-11-25 2024-05-30 Synthon B.V. A process for preparation of cabozantinib or tivozanib
CN120239695A (zh) * 2022-12-01 2025-07-01 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
WO2024163400A1 (en) * 2023-01-31 2024-08-08 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

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 (en:Method) 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
EP0832073B1 (en) * 1995-06-07 2002-01-16 Sugen, Inc. Quinazolines and pharmaceutical compositions
HUP9802199A3 (en) 1995-06-07 1999-07-28 Smithkline Beecham Biolog Vaccine comprising a polysaccharide antigen-carrier protein conjugate and free carrier protein and use of
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
PT880508E (pt) * 1996-02-13 2003-07-31 Astrazeneca Ab Derivados de quinazolina como inibidores de vegf
GB9603095D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
IL125954A (en) 1996-03-05 2003-06-24 Zeneca Ltd Quinazoline derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the manufacture of medicaments having an antiangiogenic and/or vascular permeability reducing effect
DE69734149T2 (de) * 1996-03-15 2006-07-06 Astrazeneca Ab Cinoline derivate und verwendung als heilmittel
US6107300A (en) * 1996-03-27 2000-08-22 Dupont Pharmaceuticals Arylamino fused pyrimidines
PL190489B1 (pl) * 1996-04-12 2005-12-30 Warner Lambert Co Nieodwracalne inhibitory kinaz tyrozyny, kompozycja farmaceutyczna je zawierająca i ich zastosowanie
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
ATE227283T1 (de) * 1996-07-13 2002-11-15 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
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
JP4073961B2 (ja) * 1996-10-01 2008-04-09 協和醗酵工業株式会社 含窒素複素環化合物
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 (en) 1997-04-18 2003-07-02 Kirin Beer Kabushiki Kaisha Process for producing quinolone derivatives
ATE250035T1 (de) 1997-04-22 2003-10-15 Janssen Pharmaceutica Nv 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
US6294532B1 (en) * 1997-08-22 2001-09-25 Zeneca Limited Oxindolylquinazoline derivatives as angiogenesis inhibitors
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
KR20010052450A (ko) * 1998-05-28 2001-06-25 파커 휴우즈 인스티튜트 뇌종양 치료를 위한 퀴나졸린
EP1107964B8 (en) * 1998-08-11 2010-04-07 Novartis AG Isoquinoline derivatives with angiogenesis inhibiting activity
HUP0103386A3 (en) * 1998-08-21 2002-07-29 Parker Hughes Inst St Paul Use of quinazoline derivatives for producing pharmaceutical compositions having jak 3-inhibitor effect
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
BR9914167B1 (pt) 1998-09-29 2011-03-09 compostos e composições farmacêuticas compreendendo 3-ciano quinolinas substituìdas.
US6288082B1 (en) * 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
DK1117653T3 (da) 1998-10-01 2003-05-26 Astrazeneca Ab Quinolin- og quinazolinderivater og deres anvendelse som inhibitorer af cykokin-merierede sygdomme
WO2000021955A1 (en) 1998-10-08 2000-04-20 Astrazeneca Ab Quinazoline derivatives
US6344455B1 (en) * 1998-11-19 2002-02-05 Warner-Lambert Company N-[4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, and irreversible inhibitor of tyrosine kinases
ATE253051T1 (de) * 1999-01-22 2003-11-15 Kirin Brewery Chinolinderivate und chinazolinderivate
CZ305827B6 (cs) 1999-02-10 2016-03-30 Astrazeneca Ab Indolové deriváty
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
WO2000056338A1 (en) 1999-03-19 2000-09-28 Parker Hughes Institute Quinazoline formulations and therapeutic use thereof
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
SK287010B6 (sk) * 1999-06-21 2009-09-07 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyklické heterocyklické zlúčeniny, spôsob ich prípravy, farmaceutický prostriedok s ich obsahom a ich použitie
GB9922171D0 (en) 1999-09-21 1999-11-17 Zeneca Ltd Chemical compounds
US7709479B1 (en) * 1999-09-21 2010-05-04 Astrazeneca Quinazoline derivatives and their use as pharmaceuticals
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
TWI281915B (en) * 1999-12-24 2007-06-01 Kirin Brewery 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
JP2003520855A (ja) * 2000-01-28 2003-07-08 アストラゼネカ アクチボラグ 化学的化合物
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
IL151249A0 (en) 2000-03-13 2003-04-10 American Cyanamid Co Use of cyanoquinolines for treating or inhibiting colonic polyps
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
CN1330640C (zh) * 2000-06-22 2007-08-08 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
DE60133897D1 (de) 2000-06-28 2008-06-19 Astrazeneca Ab Substituierte chinazolin-derivate und deren verwendung als aurora-2-kinase inhibitoren
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
EE05387B1 (et) 2000-08-21 2011-02-15 Astrazenecaab KinasoliiniÁderivaadid,ÁnendeÁvalmistamismeetodÁjaÁkasutamine
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
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
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
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
US6849625B2 (en) 2000-10-13 2005-02-01 Astrazeneca Ab Quinazoline derivatives with anti-tumour activity
WO2002030926A1 (en) 2000-10-13 2002-04-18 Astrazeneca Ab Quinazoline derivatives
WO2002032872A1 (fr) * 2000-10-20 2002-04-25 Eisai Co., Ltd. Composes a noyau aromatique azote
EP1332141A1 (en) 2000-10-25 2003-08-06 AstraZeneca AB Quinazoline derivatives
DE60132484T2 (de) 2000-11-02 2009-01-15 Nippon Shinyaku Co., Ltd. Chinazolinderivate und -arzneimittel
JP2004517059A (ja) 2000-11-02 2004-06-10 アストラゼネカ アクチボラグ 抗腫瘍剤用の４−置換キノリン類
US7067532B2 (en) 2000-11-02 2006-06-27 Astrazeneca 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
US7141577B2 (en) 2001-04-19 2006-11-28 Astrazeneca Ab Quinazoline derivatives
PL209822B1 (pl) 2001-04-27 2011-10-31 Kirin Pharma Kk Pochodna chinoliny lub chinazoliny, zawierająca ją kompozycja farmaceutyczna i zastosowanie
SE0101675D0 (sv) 2001-05-11 2001-05-11 Astrazeneca Ab Novel composition
WO2002092577A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2002092579A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab 4-anilinoquinazoline 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
AU2002313249B2 (en) * 2001-06-22 2008-08-21 Kirin Pharma Kabushiki Kaisha Quinoline derivative and quinazoline derivate inhibiting self-phosphorylation of hepatocytus proliferator receptor, and medicinal composition containing 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
WO2003033472A1 (en) * 2001-10-17 2003-04-24 Kirin Beer Kabushiki Kaisha Quinoline or quinazoline derivatives inhibiting auto- phosphorylation of fibroblast growth factor receptors
AU2002361577A1 (en) 2001-10-30 2003-05-12 Merck And 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
CA2467573A1 (en) * 2001-11-27 2003-06-19 Wyeth Holdings Corporation 3-cyanoquinolines as inhibitors of egf-r and her2 kinases
GB0129099D0 (en) 2001-12-05 2002-01-23 Astrazeneca Ab Chemical compounds
AU2002347336A1 (en) 2001-12-05 2003-06-17 Astrazeneca Ab Quinoline derivatives
AU2002347359A1 (en) 2001-12-05 2003-06-17 Astrazeneca Ab Quinoline derivatives
WO2003049740A1 (en) * 2001-12-12 2003-06-19 Pfizer Products Inc. Quinazoline derivatives for the treatment of abnormal cell growth
BR0214876A (pt) 2001-12-12 2004-12-28 Pfizer Prod Inc Formas de sal de e-2-metóxi-n-(3-(4-(3-metil-piridin-3-ilóxi)-fenilamino)qui nazolin-6-il)-alil)-acetamida, suas preparações e uso dos mesmos contra o câncer
TW200301123A (en) 2001-12-21 2003-07-01 Astrazeneca Uk Ltd New use
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
RU2323215C2 (ru) 2001-12-24 2008-04-27 Астразенека Аб Замещенные производные хиназолина как ингибиторы ауроракиназы
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
RU2365588C2 (ru) 2002-02-01 2009-08-27 Астразенека Аб Хиназолиновые соединения
DE10204462A1 (de) 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
WO2003074497A1 (en) * 2002-03-01 2003-09-12 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
EP2280003B1 (en) 2002-07-15 2014-04-02 Symphony Evolution, Inc. Process for preparing receptor-type kinase modulators
GB0219746D0 (en) 2002-08-23 2002-10-02 Inst Of Ex Botany Ascr Azapurine derivatives
CN1688549A (zh) * 2002-08-23 2005-10-26 麒麟麦酒株式会社 具有TGFβ抑制活性的化合物和含所述化合物的药用组合物
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
US20080207617A1 (en) * 2002-10-29 2008-08-28 Kirin Beer Kabushiki Kaisha Quinoline Derivatives and Quinazoline Derivatives Inhibiting Autophosphrylation of Flt3 and Medicinal Compositions Containing the Same
JP4593464B2 (ja) 2002-11-04 2010-12-08 アストラゼネカ アクチボラグ Ｓｒｃチロシンキナーゼ阻害剤としてのキナゾリン誘導体
US20040156869A1 (en) 2002-12-13 2004-08-12 Neurogen Corporation 2-substituted quinazolin-4-ylamine analogues
CN1729001A (zh) 2002-12-18 2006-02-01 辉瑞产品公司 用于治疗异常细胞生长的4－苯胺基喹唑啉衍生物
US7238679B2 (en) 2002-12-23 2007-07-03 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
US20070213374A1 (en) 2003-07-07 2007-09-13 Merck Patent Gmbh Malonamide Derivatives
PT2213661E (pt) * 2003-09-26 2011-12-15 Exelixis Inc Moduladores de c-met e métodos de uso
CA2553433A1 (en) 2004-01-23 2005-08-11 Amgen Inc. Quinoline quinazoline pyridine and pyrimidine compounds and their use in the treatment of inflammation angiogenesis and cancer
US7173031B2 (en) * 2004-06-28 2007-02-06 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
CA2572331A1 (en) * 2004-07-02 2006-02-09 Exelixis, Inc. C-met modulators and method of use
US20080161305A1 (en) * 2005-04-06 2008-07-03 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
CA2738583A1 (en) 2008-10-01 2010-04-08 Ludwig Institute For Cancer Research Methods for the treatment of cancer
WO2010065838A1 (en) * 2008-12-04 2010-06-10 Exelixis, Inc. Methods of preparing quinoline derivatives
PL2387563T5 (pl) * 2009-01-16 2023-03-13 Exelixis, Inc. Sól jabłczanowa N-(4-{[6,7-bis(metyloksy)chinolin-4-ylo]oksy}fenylo-N′-(4-fluorofenylo)cykloproano-1,1-dikarboksyamidu oraz jej krystaliczne postaci do leczenia raka
CA2768370A1 (en) * 2009-07-17 2011-01-20 Exelixis, Inc. Crystalline forms 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
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
PL2392565T3 (pl) 2014-08-29
EP2392564A1 (en) 2011-12-07
EP2612853A1 (en) 2013-07-10
DK2392564T3 (da) 2014-01-13
JP2010235632A (ja) 2010-10-21
PT2210607E (pt) 2012-01-31
HK1164313A1 (en) 2012-09-21
JP2021050233A (ja) 2021-04-01
ES2371383T3 (es) 2011-12-30
EP3329918B1 (en) 2022-05-25
EP2392565A1 (en) 2011-12-07
JP2007506777A (ja) 2007-03-22
JP4638436B2 (ja) 2011-02-23
JP2014055190A (ja) 2014-03-27
JP2015131859A (ja) 2015-07-23
ES2436888T3 (es) 2014-01-07
JP2019070015A (ja) 2019-05-09
AU2010204459B2 (en) 2013-06-20
ES2925655T3 (es) 2022-10-19
CY1112056T1 (el) 2015-11-04
US20070225307A1 (en) 2007-09-27
EP2409704A2 (en) 2012-01-25
JP2010235631A (ja) 2010-10-21
EP2392565B1 (en) 2014-03-19
HK1143068A1 (en) 2010-12-24
US20130252940A1 (en) 2013-09-26
US8497284B2 (en) 2013-07-30
JP5325173B2 (ja) 2013-10-23
CA2744997A1 (en) 2005-04-07
HK1141799A1 (en) 2010-11-19
JP2014055191A (ja) 2014-03-27
HUS1400052I1 (hu) 2022-02-28
AU2010204461B2 (en) 2013-06-20
DK2213661T3 (da) 2011-09-19
EP1673085A4 (en) 2008-12-10
EP1673085A2 (en) 2006-06-28
AU2010204459A1 (en) 2010-08-19
JP2014074059A (ja) 2014-04-24
US20110077233A1 (en) 2011-03-31
FR14C0067I2 (fr) 2015-11-20
JP5185331B2 (ja) 2013-04-17
LU92508I2 (fr) 2015-11-02
JP2010280674A (ja) 2010-12-16
SI2392565T1 (sl) 2014-05-30
HK1256476A1 (en) 2019-09-27
JP5694501B2 (ja) 2015-04-01
US20070244116A1 (en) 2007-10-18
ATE517091T1 (de) 2011-08-15
AU2010204461A1 (en) 2010-08-19
ATE520403T1 (de) 2011-09-15
CA2537812A1 (en) 2005-04-07
SI2392564T1 (sl) 2014-02-28
US20120022065A1 (en) 2012-01-26
EP2409704B1 (en) 2017-09-20
WO2005030140A3 (en) 2005-05-19
EP2609919A3 (en) 2014-02-26
ES2651730T3 (es) 2018-01-29
CY2014037I1 (el) 2015-11-04
HRP20140012T1 (hr) 2014-02-14
US8178532B2 (en) 2012-05-15
US20120184523A1 (en) 2012-07-19
US9174947B2 (en) 2015-11-03
ES2466818T3 (es) 2014-06-11
US20200331860A1 (en) 2020-10-22
DK2392565T3 (da) 2014-05-05
HK1164312A1 (en) 2012-09-21
HRP20110707T1 (hr) 2011-10-31
AU2004275842B2 (en) 2010-09-02
HRP20110810T1 (hr) 2011-12-31
US8476298B2 (en) 2013-07-02
EP2213661A1 (en) 2010-08-04
US20160185725A1 (en) 2016-06-30
US11124482B2 (en) 2021-09-21
EP2409704A3 (en) 2013-02-13
JP2010265302A (ja) 2010-11-25
JP5185332B2 (ja) 2013-04-17
US20150376133A1 (en) 2015-12-31
ATE532782T1 (de) 2011-11-15
SI2210607T1 (sl) 2011-11-30
CY1111956T1 (el) 2015-11-04
FR14C0067I1 (en:Method) 2014-10-17
JP2024023447A (ja) 2024-02-21
US20090170896A1 (en) 2009-07-02
EP1673085B1 (en) 2011-11-09
SI2213661T1 (sl) 2011-11-30
PL2210607T3 (pl) 2012-01-31
US20070054928A1 (en) 2007-03-08
DK2210607T3 (da) 2011-12-12
ES2369652T3 (es) 2011-12-02
WO2005030140A2 (en) 2005-04-07
US7579473B2 (en) 2009-08-25
CY2014037I2 (el) 2019-07-10
JP2017160270A (ja) 2017-09-14
AU2004275842A1 (en) 2005-04-07
EP2609919A2 (en) 2013-07-03
EP3329918A3 (en) 2018-08-15
EP3329918A2 (en) 2018-06-06
EP2213661B1 (en) 2011-07-20
NL300678I2 (en:Method) 2017-01-31
PT2213661E (pt) 2011-12-15
HRP20140563T1 (hr) 2014-07-18
US20140155396A1 (en) 2014-06-05
EP2210607A1 (en) 2010-07-28
BE2014C055I2 (en:Method) 2023-12-14
US20140155378A9 (en) 2014-06-05
EP2392564B1 (en) 2013-10-23
US20090105299A1 (en) 2009-04-23
PL2213661T3 (pl) 2011-12-30
JP2011042686A (ja) 2011-03-03
US20170355678A1 (en) 2017-12-14
JP5325172B2 (ja) 2013-10-23
US20210253530A9 (en) 2021-08-19
EP2210607B1 (en) 2011-08-17
US8067436B2 (en) 2011-11-29

Similar Documents

Publication Publication Date Title
CA2537812C (en) C-met modulators and method of use
HK1256476B (en) C-met modulators and methods of use
HK1187896A (en) C-met modulators and methods of use
HK1164312B (en) C-met modulators and methods of use
HK1186975A (en) C-met modulators and methods of use
HK1165313B (en) C-met modulators and methods of use
HK1143068B (en) 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
HK1141799B (en) C-met modulators and methods of use

Legal Events

Date Code Title Description
EEER Examination request