ATE344241T1 - Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosine kinasesn, insbesondere von raf kinasen - Google Patents

Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosine kinasesn, insbesondere von raf kinasen

Info

Publication number
ATE344241T1
ATE344241T1 AT98943832T AT98943832T ATE344241T1 AT E344241 T1 ATE344241 T1 AT E344241T1 AT 98943832 T AT98943832 T AT 98943832T AT 98943832 T AT98943832 T AT 98943832T AT E344241 T1 ATE344241 T1 AT E344241T1
Authority
AT
Austria
Prior art keywords
kinasesn
kinasen
benzylidene
indol
dihydro
Prior art date
Application number
AT98943832T
Other languages
English (en)
Inventor
Robert Walton Mcnutt Jr
David Kendall Jung
Philip Anthony Harris
Robert Neil Hunter Iii
James Marvin Veal
Scott Dickerson
Karen Elizabeth Lackey
Michael Robert Peel
Original Assignee
Glaxo Group Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Application granted granted Critical
Publication of ATE344241T1 publication Critical patent/ATE344241T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AT98943832T 1997-08-06 1998-08-04 Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosine kinasesn, insbesondere von raf kinasen ATE344241T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9716557.5A GB9716557D0 (en) 1997-08-06 1997-08-06 Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity

Publications (1)

Publication Number Publication Date
ATE344241T1 true ATE344241T1 (de) 2006-11-15

Family

ID=10817030

Family Applications (1)

Application Number Title Priority Date Filing Date
AT98943832T ATE344241T1 (de) 1997-08-06 1998-08-04 Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosine kinasesn, insbesondere von raf kinasen

Country Status (13)

Country Link
US (1) US6268391B1 (de)
EP (1) EP1003721B1 (de)
JP (1) JP2002514228A (de)
AR (1) AR016789A1 (de)
AT (1) ATE344241T1 (de)
AU (1) AU9158498A (de)
DE (1) DE69836332T2 (de)
ES (1) ES2272008T3 (de)
GB (1) GB9716557D0 (de)
MA (1) MA26529A1 (de)
PE (1) PE112699A1 (de)
WO (1) WO1999010325A1 (de)
ZA (1) ZA987037B (de)

Families Citing this family (242)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6147106A (en) 1997-08-20 2000-11-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
EP0832073B1 (de) * 1995-06-07 2002-01-16 Sugen, Inc. Chinazoline und pharmazeutische zusammensetzungen
US6316635B1 (en) 1995-06-07 2001-11-13 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
US6906093B2 (en) 1995-06-07 2005-06-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US6696448B2 (en) 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
JP4713698B2 (ja) 1997-03-05 2011-06-29 スージェン， インク． 疎水性薬剤の処方
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
US6316429B1 (en) 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
US6486185B1 (en) 1997-05-07 2002-11-26 Sugen, Inc. 3-heteroarylidene-2-indolinone protein kinase inhibitors
US6316479B1 (en) 1997-05-19 2001-11-13 Sugen, Inc. Isoxazole-4-carboxamide compounds active against protein tryosine kinase related disorders
US6987113B2 (en) 1997-06-11 2006-01-17 Sugen, Inc. Tyrosine kinase inhibitors
US6130238A (en) * 1997-06-20 2000-10-10 Sugen, Inc. 3-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
US6114371A (en) * 1997-06-20 2000-09-05 Sugen, Inc. 3-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
US6313158B1 (en) 1997-06-20 2001-11-06 Sugen, Inc. Bioavailability of 3-heteroarylidenyl-2-indolinones active as protein tyrosine kinase inhibitors
US6051593A (en) 1997-06-20 2000-04-18 Sugen, Inc. 3-(cycloalkanoheteroarylidenyl)-2- indolinone protein tyrosine kinase inhibitors
US6235769B1 (en) 1997-07-03 2001-05-22 Sugen, Inc. Methods of preventing and treating neurological disorders with compounds that modulate the function of the C-RET receptor protein tyrosine kinase
US6133305A (en) 1997-09-26 2000-10-17 Sugen, Inc. 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity
US6531502B1 (en) 1998-01-21 2003-03-11 Sugen, Inc. 3-Methylidenyl-2-indolinone modulators of protein kinase
US6514981B1 (en) 1998-04-02 2003-02-04 Sugen, Inc. Methods of modulating tyrosine protein kinase function with indolinone compounds
US6569868B2 (en) 1998-04-16 2003-05-27 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
IL139934A (en) 1998-05-29 2007-10-31 Sugen Inc History 2 - Indulinone converted to pyrrole and pharmaceutical preparations containing them
JP2002532492A (ja) * 1998-12-17 2002-10-02 エフ．ホフマン−ラ ロシュ アーゲー サイクリン−依存性キナーゼ、特にｃｄｋ２のインヒビターとしての４−アルケニル（及びアルキニル）オキシドール
BR9916223A (pt) 1998-12-17 2001-09-04 Hoffmann La Roche 4-ariloxindóis como inibidores de cinases de proteìna jnk
CA2354402A1 (en) 1998-12-17 2000-06-22 F. Hoffmann-La Roche Ag 4,5-pyrazinoxindoles as protein kinase inhibitors
US6153634A (en) * 1998-12-17 2000-11-28 Hoffmann-La Roche Inc. 4,5-azolo-oxindoles
GB9904932D0 (en) * 1999-03-04 1999-04-28 Glaxo Group Ltd Composition and method for preventing/reducing the severity of side effects of chemotherapy and/or radiation therapy
US7064114B2 (en) 1999-03-19 2006-06-20 Parker Hughes Institute Gel-microemulsion formulations
US6689806B1 (en) 1999-03-24 2004-02-10 Sugen, Inc. Indolinone compounds as kinase inhibitors
AU3770000A (en) * 1999-03-24 2000-10-09 Sugen, Inc. Indolinone compounds as kinase inhibitors
JP2000281588A (ja) * 1999-03-30 2000-10-10 Sankyo Co Ltd ガンの予防又は治療薬及びそのスクリーニング方法
JP2002542280A (ja) * 1999-04-27 2002-12-10 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 新規な治療
US6423699B1 (en) 1999-05-04 2002-07-23 American Home Products Corporation Combination therapies using benzimidazolones
US6417214B1 (en) 1999-05-04 2002-07-09 Wyeth 3,3-substituted indoline derivatives
US6339098B1 (en) 1999-05-04 2002-01-15 American Home Products Corporation 2,1-benzisothiazoline 2,2-dioxides
US6369056B1 (en) 1999-05-04 2002-04-09 American Home Products Corporation Cyclic urea and cyclic amide derivatives
US6306851B1 (en) 1999-05-04 2001-10-23 American Home Products Corporation Cyclocarbamate and cyclic amide derivatives
US6407101B1 (en) 1999-05-04 2002-06-18 American Home Products Corporation Cyanopyrroles
US6355648B1 (en) 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
US6391907B1 (en) 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
US6358947B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods
US6509334B1 (en) 1999-05-04 2003-01-21 American Home Products Corporation Cyclocarbamate derivatives as progesterone receptor modulators
US6498154B1 (en) 1999-05-04 2002-12-24 Wyeth Cyclic regimens using quinazolinone and benzoxazine derivatives
US6462032B1 (en) 1999-05-04 2002-10-08 Wyeth Cyclic regimens utilizing indoline derivatives
US6444668B1 (en) 1999-05-04 2002-09-03 Wyeth Combination regimens using progesterone receptor modulators
US6358948B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
US6319912B1 (en) 1999-05-04 2001-11-20 American Home Products Corporation Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides
US6380178B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Cyclic regimens using cyclocarbamate and cyclic amide derivatives
US6329416B1 (en) 1999-05-04 2001-12-11 American Home Products Corporation Combination regimens using 3,3-substituted indoline derivatives
US6399593B1 (en) 1999-05-04 2002-06-04 Wyeth Cyclic regimens using cyclic urea and cyclic amide derivatives
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6432979B1 (en) 1999-08-12 2002-08-13 American Cyanamid Company Method of treating or inhibiting colonic polyps and colorectal cancer
US6878733B1 (en) 1999-11-24 2005-04-12 Sugen, Inc. Formulations for pharmaceutical agents ionizable as free acids or free bases
US6313310B1 (en) 1999-12-15 2001-11-06 Hoffmann-La Roche Inc. 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles
PT1255536E (pt) 1999-12-22 2006-09-29 Sugen Inc Derivados de indolinona para a modulacao da tirosina proteina cinase de tipo c-kit
US6339100B1 (en) 1999-12-29 2002-01-15 The Trustees Of Columbia University In The City Of New York Methods for inhibiting mastocytosis
AU2001236720A1 (en) * 2000-02-05 2001-08-14 Bemis, Guy Compositions useful as inhibitors of erk
DE122008000002I1 (de) 2000-02-15 2008-04-17 Sugen Inc Pyrrol substituierte indolin-2-on protein kinase inhibitoren
US6620818B1 (en) 2000-03-01 2003-09-16 Smithkline Beecham Corporation Method for reducing the severity of side effects of chemotherapy and/or radiation therapy
UA73119C2 (en) 2000-04-19 2005-06-15 American Home Products Corpoir Derivatives of cyclic thiocarbamates, pharmaceutical composition including noted derivatives of cyclic thiocarbamates and active ingredients of medicines as modulators of progesterone receptors
TWI270545B (en) 2000-05-24 2007-01-11 Sugen Inc Mannich base prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
CA2410509A1 (en) 2000-06-02 2001-12-13 Sugen, Inc. Indolinone derivatives as protein kinase/phosphatase inhibitors
GB0016454D0 (en) 2000-07-04 2000-08-23 Hoffmann La Roche Thienopyrrolidinones
CA2417500C (en) * 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
ES2230337T3 (es) * 2000-09-01 2005-05-01 Glaxo Group Limited Derivados de oxindol.
US6638965B2 (en) 2000-11-01 2003-10-28 Boehringer Ingelheim Pharma Kg Substituted indolinones, preparation thereof and their use as pharmaceutical compositions
DE10054019A1 (de) * 2000-11-01 2002-05-23 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
EP1512413A3 (de) 2001-01-16 2009-09-23 Glaxo Group Limited Pharmazeutische Mischung gegen Krebs, die ein 4-Chinazolinamin in Kombination mit einem anderen antineoplastischen Wirkstoff enthält
AR042586A1 (es) 2001-02-15 2005-06-29 Sugen Inc 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa
JP2004529110A (ja) 2001-03-06 2004-09-24 アストラゼネカ アクチボラグ 脈管損傷活性を有するインドール誘導体
AU2002303892A1 (en) 2001-05-30 2002-12-09 Jingrong Cui 5-aralkylsulfonyl-3- (pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors
DE10134196B4 (de) * 2001-07-13 2005-08-18 Forschungszentrum Karlsruhe Gmbh Technik Und Umwelt Pharmazeutische Zusammensetzung zur Hemmung der unkontrollierten Vermehrung und/oder Induzierung der Apoptose von Zellen
ES2275021T3 (es) * 2001-09-27 2007-06-01 Smithkline Beecham Corporation Derivados de azoxoindol como inhibidores de trk proteina quinasa para el tratamiento de cancer y dolor cronico.
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
US20030119839A1 (en) * 2001-12-13 2003-06-26 Nan-Horng Lin Protein kinase inhibitors
US6797825B2 (en) 2001-12-13 2004-09-28 Abbott Laboratories Protein kinase inhibitors
GB0206861D0 (en) * 2002-03-22 2002-05-01 Glaxo Group Ltd Medicaments
CN100564375C (zh) * 2002-04-03 2009-12-02 阿勒根公司 作为激酶抑制剂的(3z)-3-(2,3-二氢-1h-茚-1-叉)-1,3-二氢-2h-吲哚-2-酮
US6541504B1 (en) 2002-04-03 2003-04-01 Allergan Sales, Llc (3Z)-3-(2,3-dihydro-1H-inden-1-ylidene)-1,3-dihydro-2H-indol-2-ones as kinase inhibitors
US20050176740A1 (en) * 2002-04-08 2005-08-11 Spector Neil L. Cancer treatment method comprising administering an erb-family inhibitor and a raf and/or ras inhibitor
ITMI20021620A1 (it) * 2002-07-23 2004-01-23 Novuspharma Spa Composto ad ativita' antitumorale
US7169936B2 (en) 2002-07-23 2007-01-30 Boehringer Ingelheim Pharma Gmbh & Co. Kg Indolinone derivatives substituted in the 6-position, their preparation and their use as medicaments
US7514468B2 (en) 2002-07-23 2009-04-07 Boehringer Ingelheim Pharma Gmbh & Co. Kg Indolinone derivatives substituted in the 6 position, the preparation thereof and their use as pharmaceutical compositions
EP1542989B1 (de) * 2002-07-31 2007-04-18 Critical Outcome Technologies, Inc. Protein tyrosin kinase inhibitoren
US7825132B2 (en) * 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
BR0313743A (pt) * 2002-08-23 2005-07-05 Chiron Corp Benzimidazol quinolinonas e usos destas
US8673924B2 (en) 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
RU2380369C9 (ru) 2002-09-04 2011-07-10 Шеринг Корпорейшн Новые пиразолопиримидины как ингибиторы циклин-зависимой киназы
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
AU2003273675A1 (en) * 2002-10-09 2004-05-04 Wayne R. Danter Protein tyrosine kinase inhibitors
MXPA05004754A (es) * 2002-11-13 2005-08-02 Chiron Corp Metodos para tratar cancer y metodos relacionados.
AU2003302665B2 (en) * 2002-11-15 2009-12-24 Symphony Evolution, Inc. Kinase modulators
US20050019366A1 (en) * 2002-12-31 2005-01-27 Zeldis Jerome B. Drug-coated stents and methods of use therefor
WO2004064733A2 (en) * 2003-01-15 2004-08-05 Board Of Regents, University Of Texas System The use of c-raf inhibitors for the treatment of neurodegenerative diseases
US7875616B2 (en) * 2003-05-27 2011-01-25 Haegerkvist Robert Per Use of tyrosine kinase inhibitor to treat diabetes
AR045037A1 (es) 2003-07-10 2005-10-12 Aventis Pharma Sa Tetrahidro-1h-pirazolo [3,4-c] piridinas sustituidas, composiciones que las contienen y su utilizacion.
DE602004021838D1 (de) * 2003-10-16 2009-08-13 Novartis Vaccines & Diagnostic Substituierte benzazole und ihre verwendung als raf-kinase-hemmer
WO2005047244A2 (en) * 2003-11-07 2005-05-26 Chiron Corporation Inhibition of fgfr3 and treatment of multiple myeloma
WO2005068424A1 (en) * 2004-01-20 2005-07-28 Cell Therapeutics Europe S.R.L. Indolinone derivatives as receptor tyrosine kinase ihibitors
US7842701B2 (en) * 2004-02-19 2010-11-30 Takeda Pharmaceutical Company Limited Pyrazoloquinolone derivative and use thereof
US7875624B2 (en) * 2004-02-20 2011-01-25 Novartis Vaccines And Diagnostics, Inc. Modulating and measuring cellular adhesion
DE102004012070A1 (de) * 2004-03-12 2005-09-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue cycloalkyl-haltige 5-Acylindolinone, deren Herstellung und deren Verwendung als Arzneimittel
SG176463A1 (en) 2005-02-22 2011-12-29 Univ Michigan Small molecule inhibitors of mdm2 and uses thereof
CN101222850B (zh) * 2005-05-13 2012-10-03 诺瓦提斯公司 治疗对药物有抗性的癌症的方法
NZ563692A (en) * 2005-05-23 2011-04-29 Novartis Ag Crystalline and other forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts
PE20070427A1 (es) 2005-08-30 2007-04-21 Novartis Ag Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas
PL1957074T3 (pl) * 2005-11-29 2014-08-29 Novartis Ag Preparaty chinolinonów
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
CN101415674A (zh) 2006-02-16 2009-04-22 先灵公司 作为erk抑制剂的吡咯烷衍生物
DE602007005139D1 (de) * 2006-07-21 2010-04-15 Novartis Ag Formulierungen für benzimidazolylpyridylether
CN101541977A (zh) * 2006-09-19 2009-09-23 诺瓦提斯公司 用于raf抑制剂的靶向调节、效力、诊断和/或预后的生物标志物
EP2121681B1 (de) 2007-01-11 2015-04-15 Critical Outcome Technologies, Inc. Verbindungen und verfahren zur behandlung von krebs
KR100799821B1 (ko) * 2007-02-05 2008-01-31 동화약품공업주식회사 신규한 이마티닙 캠실레이트 및 그의 제조방법
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
US20110129550A1 (en) 2007-02-16 2011-06-02 Connie Erickson-Miller Cancer treatment method
US20110160130A1 (en) * 2007-02-16 2011-06-30 Connie Erickson-Miller Cancer treatment method
UY30915A1 (es) 2007-02-16 2008-09-02 Smithkline Beecham Corp Método de tratamiento de canceres
US20100143440A1 (en) * 2007-04-30 2010-06-10 The Uab Research Foundation Ul97 inhibitors for treatment of proliferative disorders
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
CA2689514C (en) 2007-06-05 2015-09-29 Takeda Pharmaceutical Company Limited Heterobicyclic compounds as kinase inhibitors
JP5270553B2 (ja) 2007-08-23 2013-08-21 武田薬品工業株式会社 複素環化合物およびその用途
JP5350247B2 (ja) 2007-08-29 2013-11-27 武田薬品工業株式会社 複素環化合物およびその用途
CN101848908B (zh) * 2007-09-06 2014-07-02 北京强新生物科技有限公司 激酶抑制剂的组合物及其在治疗癌症和其它与激酶相关的疾病中的用途
CN101888841B (zh) * 2007-10-09 2012-09-26 宾夕法尼亚大学理事会 血小板生成素受体激动剂(TpoRA)杀死急性人骨髓样白血病细胞
JP2011506494A (ja) 2007-12-21 2011-03-03 ユニバーシティ・ヘルス・ネットワーク 癌の治療に有用なキナーゼ阻害剤としてのインダゾリル、ベンズイミダゾリル、ベンゾトリアゾリル置換インドルモン誘導体
EP2225226B1 (de) 2007-12-26 2016-08-17 Critical Outcome Technologies, Inc. Verbindungen und ihre verwending in einem verfahren zur behandlung von krebs
NZ587504A (en) 2008-02-21 2012-09-28 Merck Sharp & Dohme Benzopyrazole derivatives as ERK inhibitors
EP3023426A1 (de) 2008-07-17 2016-05-25 Critical Outcome Technologies, Inc. Thiosemicarbazonhemmerverbindungen und krebsbehandlungsverfahren
US8697685B2 (en) 2008-11-20 2014-04-15 Glaxosmithkline Llc Chemical compounds
EP2399921B1 (de) 2008-12-01 2015-08-12 Takeda Pharmaceutical Company Limited Heterocyclische verbindung und deren verwendung
JO3101B1 (ar) 2008-12-02 2017-09-20 Takeda Pharmaceuticals Co مشتقات بنزوثيازول كعوامل مضادة للسرطان
WO2010077613A1 (en) 2008-12-09 2010-07-08 Gilead Sciences, Inc. Modulators of toll-like receptors
MY161598A (en) 2009-01-30 2017-04-28 Glaxosmithkline Llc Crystalline n-{ (1s)-2-amino-1-[(3-fluorophenyl)methyl]ethyl} -5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride
WO2010100127A1 (en) 2009-03-04 2010-09-10 Novartis Ag Disubstituted imidazole derivatives as modulators of raf kinase
US8481525B2 (en) 2009-04-06 2013-07-09 University Of Health Network Kinase inhibitors and method of treating cancer with same
US8410095B2 (en) 2009-05-20 2013-04-02 Glaxosmithkline Llc Thiazolopyrimidinone derivatives as PI3 kinase inhibitors
GEP201706639B (en) 2009-08-17 2017-03-27 Intellikine Llc Heterocyclic compounds and uses thereof
SI2467140T1 (sl) 2009-08-21 2016-10-28 Novartis Ag Lapatinib za zdravljenje raka
JP2013503178A (ja) 2009-08-26 2013-01-31 サイリーン ファーマシューティカルズ インコーポレーティッド タンパク質キナーゼ調節物質としての縮合キノリン
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
JO3002B1 (ar) 2009-08-28 2016-09-05 Irm Llc مركبات و تركيبات كمثبطات كيناز بروتين
EP2477987B1 (de) 2009-09-14 2018-01-10 Gilead Sciences, Inc. Modulatoren des toll-like-rezeptors
DK3560498T3 (da) 2009-10-16 2022-11-14 Novartis Ag Kombination, der omfatter en mek-hæmmer og en b-raf-hæmmer
CN102666541B (zh) 2009-10-22 2015-11-25 吉里德科学公司 用于治疗特别是病毒感染的嘌呤或脱氮嘌呤的衍生物
US20150018301A1 (en) * 2009-11-06 2015-01-15 The Johns Hopkins University LRRK-2-Mediated Neuronal Toxicity
EP2531498B1 (de) 2010-02-05 2016-07-13 Novartis AG Verbindungen und zusammensetzungen als proteinkinase-hemmer
BR112012024380A2 (pt) 2010-03-25 2015-09-15 Glaxosmithkline Llc compostos químicos
US8987272B2 (en) 2010-04-01 2015-03-24 Critical Outcome Technologies Inc. Compounds and method for treatment of HIV
EA023173B1 (ru) 2010-04-06 2016-04-29 Юниверсити Хелс Нетворк Ингибиторы киназы и способ лечения злокачественной опухоли с их помощью
US20130096149A1 (en) 2010-06-25 2013-04-18 Novartis Ag Heteroaryl compounds and compositions as protein kinase inhibitors
US20130172378A1 (en) 2010-09-14 2013-07-04 Glaxosmithkline Llc Combination of BRAF and VEGF Inhibitors
EP3170813B1 (de) 2010-10-06 2018-12-12 GlaxoSmithKline LLC Benzimidazol-derivate als pi3-kinase-hemmer
GB201112607D0 (en) 2011-07-22 2011-09-07 Glaxo Group Ltd Novel compounds
TWI505828B (zh) 2010-12-20 2015-11-01 葛蘭素史克智慧財產（第二）有限公司 新穎醫藥組成物
AU2012205601B2 (en) 2011-01-11 2016-03-24 Novartis Ag Combination
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン， エルエルシー 複素環化合物およびその使用
CN103917236A (zh) 2011-11-11 2014-07-09 诺华股份有限公司 治疗增生性疾病的方法
DK2782557T3 (en) 2011-11-23 2018-12-10 Array Biopharma Inc PHARMACEUTICAL FORMULATIONS
KR20140117644A (ko) 2012-01-31 2014-10-07 스미스클라인 비이참 (코르크) 리미티드 암을 치료하는 방법
WO2013143597A1 (en) 2012-03-29 2013-10-03 Glaxo Group Limited Demethylase enzymes inhibitors
WO2014081718A1 (en) 2012-11-20 2014-05-30 Genentech, Inc. Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
US20150328320A1 (en) 2012-11-30 2015-11-19 Glaxosmithkline Llc Novel Pharmaceutical Composition
KR20150103735A (ko) 2013-01-09 2015-09-11 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 조합물
US20150329524A1 (en) 2013-01-10 2015-11-19 Glaxosmithkline Intellectual Property (No.2) Limited Fatty acid synthase inhibitors
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
EP2970206A1 (de) * 2013-03-13 2016-01-20 Boston Biomedical, Inc. 3-(aryl- oder heteroaryl)-methylenindolin-2-on-derivate als hemmer von krebsstammzellenbahnpfadkinasen zur krebsbehandlung
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
WO2014151147A1 (en) 2013-03-15 2014-09-25 Intellikine, Llc Combination of kinase inhibitors and uses thereof
HK1216231A1 (zh) 2013-06-03 2016-10-28 Novartis Ag Anti-pd-l1抗体及mek抑制剂及/或braf抑制剂的混合物
WO2014210354A1 (en) 2013-06-28 2014-12-31 Genentech, Inc. Azaindazole compounds as inhibitors of t790m containing egfr mutants
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
MX2016004267A (es) 2013-10-01 2016-07-08 Novartis Ag Combinacion.
US20160235714A1 (en) 2013-10-01 2016-08-18 Novartis Ag Enzalutamide in combination with afuresertib for the treatment of cancer
WO2015056180A1 (en) 2013-10-15 2015-04-23 Glaxosmithkline Intellectual Property (No.2) Limited Indoline derivatives as inhibitors of perk
EP3057593B1 (de) 2013-10-18 2021-12-08 University Health Network Behandlung von bauchspeicheldrüsenkrebs
BR112016011222A2 (pt) 2013-12-12 2017-09-19 Novartis Ag Combinações de trametinib, panitumumab e dabrafenib para o tratamento de câncer
EP3111222A1 (de) 2014-02-26 2017-01-04 Glaxosmithkline Intellectual Property (No. 2) Limited Verfahren zur behandlung von krebspatienten mit reaktion auf ezh2-inhibitor gsk126
KR20160127754A (ko) 2014-03-12 2016-11-04 노파르티스 아게 Btk 억제제 및 akt 억제제를 포함하는 조합물
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2016001907A1 (en) 2014-07-02 2016-01-07 Prendergast Patrick T Mogroside iv and mogroside v as agonist/stimulator/un-blocking agent for toll-like receptor 4 and adjuvant for use in human/animal vaccine and to stimulate immunity against disease agents.
EP4140485A1 (de) 2014-07-11 2023-03-01 Gilead Sciences, Inc. Modulatoren von toll-like-rezeptoren zur behandlung von hiv
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
EA201790369A1 (ru) 2014-09-16 2017-10-31 Джилид Сайэнс, Инк. Твердые формы модулятора толл-подобного рецептора
WO2016055935A1 (en) 2014-10-06 2016-04-14 Glaxosmithkline Intellectual Property (No.2) Limited Combination of lysine-specific demethylase 1 inhibitor and thrombopoietin agonist
WO2016059602A2 (en) 2014-10-16 2016-04-21 Glaxo Group Limited Methods of treating cancer and related compositions
MA41414A (fr) 2015-01-28 2017-12-05 Centre Nat Rech Scient Protéines de liaison agonistes d' icos
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
EP3331917A1 (de) 2015-08-04 2018-06-13 GlaxoSmithKline Intellectual Property Development Limited Kombinationsbehandlungen sowie verwendungen und verfahren davon
BR112018002436A2 (pt) 2015-08-04 2018-09-18 Glaxosmithkline Ip Dev Ltd tratamento de combinação de usos de métodos destes
EP3331918A1 (de) 2015-08-04 2018-06-13 GlaxoSmithKline Intellectual Property Development Limited Kombinationsbehandlungen und verwendungen und verfahren dafür
TW201716084A (zh) 2015-08-06 2017-05-16 葛蘭素史克智慧財產發展有限公司 組合物及其用途與治療
BR112018002520A2 (pt) 2015-08-06 2018-09-18 Glaxosmithkline Ip Dev Ltd Agonistas de tlr4 e composições dos mesmos e seuuso no tratamento de câncer
WO2017021912A1 (en) 2015-08-06 2017-02-09 Glaxosmithkline Intellectual Property Development Limited Combined tlrs modulators with anti ox40 antibodies
US20180230431A1 (en) 2015-08-07 2018-08-16 Glaxosmithkline Intellectual Property Development Limited Combination Therapy
EP4015537A1 (de) 2015-12-01 2022-06-22 GlaxoSmithKline Intellectual Property Development Limited Kombinationsbehandlungen und verwendungen und verfahren dafür
CA3006930A1 (en) 2015-12-03 2017-06-08 Glaxosmithkline Intellectual Property Development Limited Cyclic purine dinucleotides as modulators of sting
WO2017098421A1 (en) 2015-12-08 2017-06-15 Glaxosmithkline Intellectual Property Development Limited Benzothiadiazine compounds
WO2017153952A1 (en) 2016-03-10 2017-09-14 Glaxosmithkline Intellectual Property Development Limited 5-sulfamoyl-2-hydroxybenzamide derivatives
EP3429596B1 (de) 2016-03-18 2022-08-31 Immune Sensor, LLC Cyclische di-nukleotid-verbindungen und verfahren zur verwendung
PE20181884A1 (es) 2016-04-07 2018-12-07 Glaxosmithkline Ip Dev Ltd Amidas heterociclicas utiles como moduladores de proteinas
ES2781474T3 (es) 2016-04-07 2020-09-02 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas útiles como moduladores de proteínas
WO2018015879A1 (en) 2016-07-20 2018-01-25 Glaxosmithkline Intellectual Property Development Limited Isoquinoline derivatives as perk inhibitors
US11649289B2 (en) 2016-08-04 2023-05-16 Glaxosmithkline Intellectual Property Development Limited Anti-ICOS and anti-PD-1 antibody combination therapy
US20180072711A1 (en) 2016-09-15 2018-03-15 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
WO2018051306A1 (en) 2016-09-19 2018-03-22 Novartis Ag Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
KR102839545B1 (ko) 2016-12-23 2025-07-29 아비나스 오퍼레이션스, 인코포레이티드 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법
KR20190101406A (ko) 2016-12-23 2019-08-30 아비나스 오퍼레이션스, 인코포레이티드 Egfr 단백질분해 표적화 키메라 분자 및 관련 사용 방법
EP3582855A1 (de) 2017-02-15 2019-12-25 GlaxoSmithKline Intellectual Property Development Limited Kombinationstherapie zur behandlung von krebs
KR20240032157A (ko) 2017-05-02 2024-03-08 노파르티스 아게 병용 요법
CN110831582B (zh) 2017-07-05 2023-08-11 诺华股份有限公司 药物组合物
WO2019021208A1 (en) 2017-07-27 2019-01-31 Glaxosmithkline Intellectual Property Development Limited USEFUL INDAZOLE DERIVATIVES AS PERK INHIBITORS
TW201922721A (zh) 2017-09-07 2019-06-16 英商葛蘭素史克智慧財產發展有限公司 化學化合物
WO2019053617A1 (en) 2017-09-12 2019-03-21 Glaxosmithkline Intellectual Property Development Limited CHEMICAL COMPOUNDS
EP3692033A1 (de) 2017-10-05 2020-08-12 GlaxoSmithKline Intellectual Property Development Limited Modulatoren des stimulators von interferongenen (sting) zur verwendung bei der behandlung von hiv
CN111417630B (zh) 2017-10-05 2023-06-06 葛兰素史克知识产权开发有限公司 干扰素基因刺激因子(sting)的调节剂
WO2019106605A1 (en) 2017-12-01 2019-06-06 Board Of Regents, The University Of Texas System Combination treatment for cancer
GB201807924D0 (en) 2018-05-16 2018-06-27 Ctxt Pty Ltd Compounds
US12324807B2 (en) 2018-06-01 2025-06-10 Cornell University Combination therapy for PI3K-associated disease or disorder
WO2020030571A1 (en) 2018-08-06 2020-02-13 Glaxosmithkline Intellectual Property Development Limited Combinations of a pd-1 antibody and a tlr4 modulator and uses thereof
WO2020030570A1 (en) 2018-08-06 2020-02-13 Glaxosmithkline Intellectual Property Development Limited Combinations of an ox40 antibody and a tlr4 modulator and uses thereof
KR20210022695A (ko) * 2018-08-07 2021-03-03 메타곤 바이오테크 인코퍼레이티드 3-(3,5-디브로모-4-하이드록시벤질리덴)-5-요오도-1,3-디하이드로인돌-2-온의 암모늄 염 및 그의 용도
JP7589949B2 (ja) * 2018-09-18 2024-11-26 １グローブ バイオメディカル カンパニー， リミテッド 肥満に対する処置
EP4342473A3 (de) 2018-11-30 2024-05-15 GlaxoSmithKline Intellectual Property Development Limited Verbindungen zur verwendung in der hiv-therapie
WO2020160375A1 (en) 2019-02-01 2020-08-06 Glaxosmithkline Intellectual Property Development Limited Combination treatments for cancer comprising belantamab mafodotin and an anti ox40 antibody and uses and methods thereof
MX2021013817A (es) 2019-05-13 2021-12-14 Novartis Ag Nuevas formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinop iridin-4-il)-4-metilfenil)-2-(trifluorometil)isonicotinamida como inhibidores de raf para el tratamiento del cancer.
CN114302875A (zh) 2019-05-16 2022-04-08 斯汀塞拉股份有限公司 氧代吖啶基乙酸衍生物及使用方法
CN114391015A (zh) 2019-05-16 2022-04-22 斯汀塞拉股份有限公司 苯并[b][1,8]萘啶乙酸衍生物和使用方法
MA56397A (fr) 2019-06-26 2022-05-04 Glaxosmithkline Ip Dev Ltd Protéines de liaison à l'il1rap
GB201910305D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
GB201910304D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
WO2021043961A1 (en) 2019-09-06 2021-03-11 Glaxosmithkline Intellectual Property Development Limited Dosing regimen for the treatment of cancer with an anti icos agonistic antibody and chemotherapy
WO2021046293A1 (en) 2019-09-06 2021-03-11 Glaxosmithkline Intellectual Property Development Limited Dosing regimen for the treatment of cancer with an anti icos agonistic antibody and tremelimumab
CN114981265B (zh) 2019-12-18 2025-01-03 Ctxt私人有限公司 化合物
US20230067202A1 (en) 2020-01-28 2023-03-02 Glaxosmithkline Intellectual Property Development Limited Combination Treatments and Uses and Methods Thereof
US12180193B2 (en) 2020-08-28 2024-12-31 Arvinas Operations, Inc. Accelerating fibrosarcoma protein degrading compounds and associated methods of use
CN114573453B (zh) * 2020-12-02 2024-12-03 荆楚理工学院 一种选择性的羧酸酯裂解方法
CA3227706A1 (en) 2021-07-27 2023-02-02 Toray Industries, Inc. Medicament for treatment and/or prevention of cancer
KR102566028B1 (ko) * 2021-08-10 2023-08-10 계명대학교 산학협력단 신규한 다중 단백질 키나아제 억제제
CN114671887A (zh) * 2021-10-29 2022-06-28 四川大学华西医院 一种二氢吲哚酮类化合物的制备及其抗肿瘤应用
AR129423A1 (es) 2022-05-27 2024-08-21 Viiv Healthcare Co Compuestos útiles en la terapia contra el hiv
EP4584258A1 (de) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Schnell beschleunigte fibrosarkom (raf)-abbauende verbindungen und zugehörige verfahren zur verwendung

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5880141A (en) * 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
GB2306108A (en) 1995-10-13 1997-04-30 Merck & Co Inc Treatment of Raf-mediated cancers with imidazole derivatives
WO1997025986A1 (en) 1996-01-17 1997-07-24 Taiho Pharmaceutical Co., Ltd. Intimal thickening inhibitors
AU4155697A (en) * 1996-08-23 1998-03-06 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease

Also Published As

Publication number Publication date
GB9716557D0 (en) 1997-10-08
ES2272008T3 (es) 2007-04-16
MA26529A1 (fr) 2004-12-20
AU9158498A (en) 1999-03-16
ZA987037B (en) 2000-02-07
JP2002514228A (ja) 2002-05-14
PE112699A1 (es) 1999-11-16
WO1999010325A1 (en) 1999-03-04
DE69836332T2 (de) 2007-12-13
DE69836332D1 (de) 2006-12-14
US6268391B1 (en) 2001-07-31
EP1003721B1 (de) 2006-11-02
AR016789A1 (es) 2001-08-01
EP1003721A1 (de) 2000-05-31

Similar Documents

Publication Publication Date Title
ATE344241T1 (de) Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosine kinasesn, insbesondere von raf kinasen
ATE255575T1 (de) Substituierte 3-cyanochinoline als protein tyrosine kinase inhibitoren
CY2014034I2 (el) Υποκατεστημενες 3-κυανοκινολινες ως αναστολεις κινασων πρωτεϊνης τυροσινης
NO20000487D0 (no) Substituerte quinazolinderivater og anvendelse derav som tyrosin kinase inhibitorer
ATE430149T1 (de) Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren
DE60017179D1 (de) Tyrosin kinaseinhibitoren
NO20014970D0 (no) Cyklisk protein-tyrosin-kinase-inhibitor
DK0912559T3 (da) Kondenserede heterocykliske forbindelser som proteintyrosinkinaseinhibitorer
ATE316527T1 (de) Substituierte indolinone als tyrosinkinase inhibitoren
DE60021423D1 (de) 4-substituierte 7-aza-indolin-2-one und ihre anwendung als protein kinase inhibitoren
FI950859A7 (fi) Arylideeni- ja heteroarylideeni-oksindolijohdannaiset tyrosiinikinaasi-inhibiittoreina
ATE315394T1 (de) Benzothiazole als protein tyrosin-kinase inhibitoren
DE69627179D1 (de) Substituierte 2-anilino-pyrimidines verwendbar als protein kinase inhibitoren
ATE267170T1 (de) Substituierte oxindolderivate als protein tyrosin kinase und als protein serin/threonin kinase inhibitoren
DE69511253D1 (de) Wasserlösliche 3-arylidene-2-oxindole derivate als tyrosine kinase inhibitoren
DE60044004D1 (de) Verwendung von Omega-Carboxyaryl-substituierten Diphenylharnstoffen als raf-Kinase-Inhibitoren
FI972492A0 (fi) Imidatsolijohdoksia proteiinikinaasien, erityisesti EGF-R-tyrosiinikinaasin, inhibiittoreina
EP1161433A4 (de) Tyrosin-kinase-inhibitoren
DE69935600D1 (de) Dihydrobenzodioxincarbonsäureamid- und ketonderivate als 5-ht4-rezeptorantagonisten
ATE205836T1 (de) Bicyclische 4-aralkylaminopyrimidin-derivate als tyrosinkinase-inhibitoren
ATE264328T1 (de) Substituierte 3-cyano-(1.7), (1.5) und (1.8)naphthyridininhibitoren von tyrosin kinasen
ATE387448T1 (de) 4,5-pyrazinoxindole als proteinkinasehemmer
FI955661A7 (fi) Substituoidut beta-aryyli- ja beta-heteroaryyli-alfa-syanoakryyliamidi johdannaiset tyrosiinikinaasi-inhibiittoreina
DE59900869D1 (de) Mahltrocknung von zellulose-derivaten, insbesondere methyl-zellulose
FI971352A0 (fi) Sytoplasminen tyrosiinikinaasi

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties