DE69836332T2 - Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosin kinasen, insbesondere von raf kinasen - Google Patents

Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosin kinasen, insbesondere von raf kinasen Download PDF

Info

Publication number
DE69836332T2
DE69836332T2 DE69836332T DE69836332T DE69836332T2 DE 69836332 T2 DE69836332 T2 DE 69836332T2 DE 69836332 T DE69836332 T DE 69836332T DE 69836332 T DE69836332 T DE 69836332T DE 69836332 T2 DE69836332 T2 DE 69836332T2
Authority
DE
Germany
Prior art keywords
het
aliphatic
compound
halogen
optionally substituted
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 - Fee Related
Application number
DE69836332T
Other languages
German (de)
English (en)
Other versions
DE69836332D1 (de
Inventor
Walton Robert Research Triangle Park McNUTT
Kendall David Research Triangle Park JUNG
Anthony Philip Research Triangle Park HARRIS
Neil Robert Research Triangle Park HUNTER
Marvin James Research Triangle Park VEAL
Glaxo Wellcome Inc. Scott Research Triangle Park DICKERSON
Elizabeth Karen Research Triangle Park LACKEY
Robert Michael Research Triangle Park PEEL
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.)
Glaxo Group Ltd
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
Publication of DE69836332D1 publication Critical patent/DE69836332D1/de
Application granted granted Critical
Publication of DE69836332T2 publication Critical patent/DE69836332T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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
DE69836332T 1997-08-06 1998-08-04 Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosin kinasen, insbesondere von raf kinasen Expired - Fee Related DE69836332T2 (de)

Applications Claiming Priority (3)

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
GB9716557 1997-08-06
PCT/EP1998/004844 WO1999010325A1 (en) 1997-08-06 1998-08-04 Benzylidene-1,3-dihydro-indol-2-one derivatives as receptor tyrosine kinase inhibitors, particularly of raf kinases

Publications (2)

Publication Number Publication Date
DE69836332D1 DE69836332D1 (de) 2006-12-14
DE69836332T2 true DE69836332T2 (de) 2007-12-13

Family

ID=10817030

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69836332T Expired - Fee Related DE69836332T2 (de) 1997-08-06 1998-08-04 Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosin kinasen, insbesondere von raf kinasen

Country Status (13)

Country Link
US (1) US6268391B1 (US06268391-20010731-C00114.png)
EP (1) EP1003721B1 (US06268391-20010731-C00114.png)
JP (1) JP2002514228A (US06268391-20010731-C00114.png)
AR (1) AR016789A1 (US06268391-20010731-C00114.png)
AT (1) ATE344241T1 (US06268391-20010731-C00114.png)
AU (1) AU9158498A (US06268391-20010731-C00114.png)
DE (1) DE69836332T2 (US06268391-20010731-C00114.png)
ES (1) ES2272008T3 (US06268391-20010731-C00114.png)
GB (1) GB9716557D0 (US06268391-20010731-C00114.png)
MA (1) MA26529A1 (US06268391-20010731-C00114.png)
PE (1) PE112699A1 (US06268391-20010731-C00114.png)
WO (1) WO1999010325A1 (US06268391-20010731-C00114.png)
ZA (1) ZA987037B (US06268391-20010731-C00114.png)

Families Citing this family (232)

* 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
US6316635B1 (en) 1995-06-07 2001-11-13 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
CA2222545A1 (en) * 1995-06-07 1996-12-19 Sugen, Inc. Quinazolines and pharmaceutical compositions
US6906093B2 (en) 1995-06-07 2005-06-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
US6147106A (en) * 1997-08-20 2000-11-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods 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
US6248771B1 (en) 1997-03-05 2001-06-19 Sugen, Inc. Formulations for hydrophobic pharmaceutical agents
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
US6486185B1 (en) 1997-05-07 2002-11-26 Sugen, Inc. 3-heteroarylidene-2-indolinone protein kinase inhibitors
US6316429B1 (en) 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic 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
US6114371A (en) * 1997-06-20 2000-09-05 Sugen, Inc. 3-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
US6130238A (en) * 1997-06-20 2000-10-10 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
CA2314156C (en) 1998-05-29 2010-05-25 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
TR200101860T2 (tr) 1998-12-17 2001-12-21 F.Hoffmann-La Roche Ag Sikline bağlı kinaz inhibitörleri olarak 4-alkenil (ve alkinil) oksidoller
US6153634A (en) 1998-12-17 2000-11-28 Hoffmann-La Roche Inc. 4,5-azolo-oxindoles
TR200101858T2 (tr) 1998-12-17 2001-12-21 F.Hoffmann-La Roche Ag JNK protein kinaz inhibitörleri olarak 4-ariloksindoller
KR20010108024A (ko) * 1998-12-17 2001-12-07 프리돌린 클라우스너, 롤란드 비. 보레르 단백질 키나제 억제제로서의 4,5-피라진옥신돌
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
CA2368041A1 (en) * 1999-03-24 2000-09-28 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
EP1173254A2 (en) * 1999-04-27 2002-01-23 Smithkline Beecham Plc Novel treatment of neurotraumatic conditions with a raf inhibitor
US6444668B1 (en) 1999-05-04 2002-09-03 Wyeth Combination regimens using progesterone receptor modulators
US6498154B1 (en) 1999-05-04 2002-12-24 Wyeth Cyclic regimens using quinazolinone and benzoxazine derivatives
US6358948B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
US6509334B1 (en) 1999-05-04 2003-01-21 American Home Products Corporation Cyclocarbamate derivatives as progesterone receptor modulators
US6329416B1 (en) 1999-05-04 2001-12-11 American Home Products Corporation Combination regimens using 3,3-substituted indoline derivatives
US6355648B1 (en) 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
US6339098B1 (en) 1999-05-04 2002-01-15 American Home Products Corporation 2,1-benzisothiazoline 2,2-dioxides
US6319912B1 (en) 1999-05-04 2001-11-20 American Home Products Corporation Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides
US6417214B1 (en) 1999-05-04 2002-07-09 Wyeth 3,3-substituted indoline derivatives
US6423699B1 (en) 1999-05-04 2002-07-23 American Home Products Corporation Combination therapies using benzimidazolones
US6407101B1 (en) 1999-05-04 2002-06-18 American Home Products Corporation Cyanopyrroles
US6391907B1 (en) * 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
US6369056B1 (en) 1999-05-04 2002-04-09 American Home Products Corporation Cyclic urea and cyclic amide derivatives
US6380178B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Cyclic regimens using cyclocarbamate and cyclic amide derivatives
US6358947B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6462032B1 (en) 1999-05-04 2002-10-08 Wyeth Cyclic regimens utilizing indoline derivatives
US6399593B1 (en) 1999-05-04 2002-06-04 Wyeth Cyclic regimens using cyclic urea and cyclic amide derivatives
US6306851B1 (en) 1999-05-04 2001-10-23 American Home Products Corporation Cyclocarbamate and cyclic amide derivatives
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
DE60029138T2 (de) 1999-12-22 2007-06-06 Sugen, Inc., San Francisco Verwendung von Indolinonverbindungen zur Herstellung von Pharmazeutika für die Modulation der Funktion c-kit Proteintyrosinkinase
US6339100B1 (en) * 1999-12-29 2002-01-15 The Trustees Of Columbia University In The City Of New York Methods for inhibiting mastocytosis
WO2001056557A2 (en) * 2000-02-05 2001-08-09 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of erk
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
JP2003535847A (ja) 2000-06-02 2003-12-02 スージェン・インコーポレーテッド 蛋白質キナーゼ／ホスファターゼ阻害剤としてのインドリノン誘導体
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
JP2004508372A (ja) * 2000-09-01 2004-03-18 グラクソ　グループ　リミテッド オキシインドール誘導体
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
EP1488809A1 (en) 2001-01-16 2004-12-22 Glaxo Group Limited Pharmaceutical combination containing a 4-quinazolineamine and another anti-neoplastic agent for the treatment of cancer
US7186745B2 (en) 2001-03-06 2007-03-06 Astrazeneca Ab Indolone derivatives having vascular damaging activity
US6599902B2 (en) 2001-05-30 2003-07-29 Sugen, Inc. 5-aralkysufonyl-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
EP1430053B1 (en) * 2001-09-27 2006-10-25 SmithKline Beecham Corporation AZAOXOINDOLE DERIVATIVES AS Trk PROTEIN KINASE INHIBITORS FOR THE TREATMENT OF CANCER AND CHRONIC PAIN
US20030119839A1 (en) * 2001-12-13 2003-06-26 Nan-Horng Lin Protein kinase inhibitors
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li 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
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
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
AU2003221684A1 (en) * 2002-04-08 2003-10-27 Smithkline Beecham Corporation Cancer treatment method comprising administering an erb-family inhibitor and a raf and/or ras inhibitor
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
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
ITMI20021620A1 (it) * 2002-07-23 2004-01-23 Novuspharma Spa Composto ad ativita' antitumorale
CA2494061C (en) * 2002-07-31 2011-06-14 Wayne R. Danter Protein tyrosine kinase inhibitors
EP2573079A3 (en) * 2002-08-23 2015-03-11 Novartis AG Benzimidazole quinolinones and uses thereof
US7825132B2 (en) * 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
PT1537116E (pt) 2002-09-04 2010-09-03 Schering Corp Pirazolopirimidinas adequadas para o tratamento de doenças cancerosas
US8673924B2 (en) 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
EP1551824B1 (en) * 2002-10-09 2007-12-12 Critical Outcome Technologies, Inc. Protein tyrosine kinase inhibitors
WO2004043389A2 (en) * 2002-11-13 2004-05-27 Chiron Corporation Methods of treating cancer and related methods
WO2004050681A2 (en) * 2002-11-15 2004-06-17 Exelixis, 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
PL1631291T3 (pl) 2003-05-27 2010-04-30 Haegerkvist Robert P Zastosowanie inhibitorów kinazy tyrozynowej do leczenia cukrzycy
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.
JP4755991B2 (ja) * 2003-10-16 2011-08-24 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド Ｒａｆキナーゼインヒビターとしての置換ベンゾアゾールおよびその使用
WO2005046590A2 (en) * 2003-11-07 2005-05-26 Chiron Corporation Methods for synthesizing quinolinone compounds
WO2005068424A1 (en) * 2004-01-20 2005-07-28 Cell Therapeutics Europe S.R.L. Indolinone derivatives as receptor tyrosine kinase ihibitors
EP1719771A1 (en) * 2004-02-19 2006-11-08 Takeda Pharmaceutical Company Limited Pyrazoloquinolone derivative and use thereof
JP5019884B2 (ja) * 2004-02-20 2012-09-05 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド 炎症プロセスおよび転移プロセスの調節
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
US7759383B2 (en) 2005-02-22 2010-07-20 The Regents Of The University Of Michigan Small molecule inhibitors of MDM2 and the uses thereof
MX2007014206A (es) * 2005-05-13 2008-02-07 Novartis Ag Metodos para tratar cancer resistente a los farmacos.
EP2270000B1 (en) 2005-05-23 2015-07-29 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
TWI387592B (zh) * 2005-08-30 2013-03-01 Novartis Ag 經取代之苯并咪唑及其作為與腫瘤形成相關激酶之抑制劑之方法
CN102670530A (zh) * 2005-11-29 2012-09-19 诺瓦提斯公司 喹啉酮类的制剂
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
DE602007009932D1 (de) 2006-02-16 2010-12-02 Schering Corp Pyrrolidin-derivate als erk-hemmer
ATE459338T1 (de) * 2006-07-21 2010-03-15 Novartis Ag Formulierungen für benzimidazolylpyridylether
BRPI0716944A2 (pt) * 2006-09-19 2013-09-17 Novartis Ag biomarcadores de modulaÇço alvo, eficÁcia, diagnàstico, e/ou prognàstico para inibidores de raf
US8034815B2 (en) 2007-01-11 2011-10-11 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
US8138191B2 (en) 2007-01-11 2012-03-20 Critical Outcome Technologies Inc. Inhibitor compounds and cancer treatment methods
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
US20110160130A1 (en) * 2007-02-16 2011-06-30 Connie Erickson-Miller Cancer treatment method
US20110129550A1 (en) * 2007-02-16 2011-06-02 Connie Erickson-Miller Cancer treatment method
UY30915A1 (es) 2007-02-16 2008-09-02 Smithkline Beecham Corp Método de tratamiento de canceres
WO2008134124A1 (en) * 2007-04-30 2008-11-06 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
EP2162445B1 (en) 2007-06-05 2013-11-27 Takeda Pharmaceutical Company Limited Heterobicyclic compounds as kinase inhibitors
WO2009025358A1 (ja) 2007-08-23 2009-02-26 Takeda Pharmaceutical Company Limited 複素環化合物およびその用途
US8344135B2 (en) 2007-08-29 2013-01-01 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
WO2009033033A2 (en) 2007-09-06 2009-03-12 Boston Biomedical, Inc. Compositions of kinase inhibitors and their use for treatment of cancer and other diseases related to kinases
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 (en) * 2007-12-26 2016-08-17 Critical Outcome Technologies, Inc. Compounds and their use in a method for treatment of cancer
US8716483B2 (en) 2008-02-21 2014-05-06 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
WO2010059658A1 (en) 2008-11-20 2010-05-27 Glaxosmithkline Llc Chemical compounds
EP2399921B1 (en) 2008-12-01 2015-08-12 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
JO3101B1 (ar) 2008-12-02 2017-09-20 Takeda Pharmaceuticals Co مشتقات بنزوثيازول كعوامل مضادة للسرطان
AR074506A1 (es) 2008-12-09 2011-01-19 Gilead Sciences Inc Moduladores de los receptores tipo toll
BRPI1006896B1 (pt) 2009-01-30 2022-05-24 Novartis Ag Cloridrato de n-{(1s)-2-amino-1-[(3-fluorfenil)metil]etil}-5-cloro-4-(4-cloro-1-metil-1h- pirazol-5-il)-2-tiofenocarboxamida cristalino, composição farmacêutica compreendendo o mesmo e uso do dito composto para tratar ou diminuir a gravidade de câncer e artrite
WO2010100127A1 (en) 2009-03-04 2010-09-10 Novartis Ag Disubstituted imidazole derivatives as modulators of raf kinase
EP2417127B1 (en) 2009-04-06 2014-02-26 University Health Network Kinase inhibitors and method of treating cancer with same
JP5554833B2 (ja) 2009-05-20 2014-07-23 グラクソスミスクライン エルエルシー Ｐｉ３キナーゼ阻害剤としてのチアゾロピリミジノン誘導体
WO2011022439A1 (en) 2009-08-17 2011-02-24 Intellikine, Inc. Heterocyclic compounds and uses thereof
BR112012003653A2 (pt) 2009-08-21 2016-03-22 Smithkline Beecham Cork Ltd "método de tratar o câncer."
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
AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
NO2477987T3 (US06268391-20010731-C00114.png) 2009-09-14 2018-06-09
MX2012004413A (es) 2009-10-16 2012-05-08 Glaxosmithkline Llc Combinacion.
PT2491035T (pt) 2009-10-22 2017-10-30 Gilead Sciences Inc Derivados de purina ou deazapurina úteis para o tratamento de (entre outros) infeções virais
US20150018301A1 (en) * 2009-11-06 2015-01-15 The Johns Hopkins University LRRK-2-Mediated Neuronal Toxicity
JP5728499B2 (ja) 2010-02-05 2015-06-03 アイアールエム・リミテッド・ライアビリティ・カンパニーＩｒｍ，Ｌｌｃ タンパク質キナーゼ阻害剤としての化合物および組成物
US8598156B2 (en) 2010-03-25 2013-12-03 Glaxosmithkline Llc Chemical compounds
CA2999435A1 (en) 2010-04-01 2011-10-06 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv
BR112012025496B1 (pt) 2010-04-06 2021-02-23 University Health Network composto inibidor quinase e composição farmacêutica que o compreende
KR20140117684A (ko) 2010-06-25 2014-10-07 노파르티스 아게 단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물
WO2012036919A2 (en) 2010-09-14 2012-03-22 Glaxosmithkline Llc Combination of braf and vegf inhibitors
EP2624696B1 (en) 2010-10-06 2016-12-21 Glaxosmithkline LLC Benzimidazole derivatives as pi3 kinase inhibitors
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
EA029000B1 (ru) 2011-01-11 2018-01-31 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи КОМБИНАЦИЯ БОРТЕЗОМИДА И Akt-ИНГИБИТОРА ДЛЯ ЛЕЧЕНИЯ МНОЖЕСТВЕННОЙ МИЕЛОМЫ
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
CN108542906A (zh) 2011-11-11 2018-09-18 诺华股份有限公司 治疗增生性疾病的方法
BR112014011981B8 (pt) 2011-11-23 2022-07-19 Novartis Ag Formulações farmacêuticas sólidas orais, seus processos de preparação e usos
EP3045543A3 (en) 2012-01-31 2016-10-12 Novartis AG Method of treating cancer
WO2013143597A1 (en) 2012-03-29 2013-10-03 Glaxo Group Limited Demethylase enzymes inhibitors
RU2015118647A (ru) 2012-11-20 2017-01-10 Дженентек, Инк. Аминопиримидиновые соединения в качестве ингибиторов содержащих т790м мутантных egfr
MY170427A (en) 2012-11-30 2019-07-31 Glaxosmithkline Llc Novel pharmaceutical composition
BR112015016559A2 (pt) 2013-01-09 2017-07-11 Glaxosmithkline Ip No 2 Ltd combinação
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
SG11201507346PA (en) * 2013-03-13 2015-10-29 Boston Biomedical Inc 3-(aryl or heteroaryl) methyleneindolin-2-one derivatives as inhibitors of cancer stem cell pathway kinases for the treatment of cancer
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
BR112015028326A8 (pt) 2013-06-03 2018-01-23 Novartis Ag combinações de anticorpo anti-pd-l1, inibidor de mek e/ou inibidor de braf, seus kits e seus usos, e composição farmacêutica
EP3052494B1 (en) 2013-06-28 2018-12-26 H. Hoffnabb-La Roche Ag Azaindazole compounds as inhibitors of t790m containing egfr mutants
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
KR20160065910A (ko) 2013-10-01 2016-06-09 노파르티스 아게 조합물
KR101797415B1 (ko) 2013-10-01 2017-11-13 노파르티스 아게 암의 치료를 위한 아푸레세르팁과 조합된 엔잘루타미드
WO2015056180A1 (en) 2013-10-15 2015-04-23 Glaxosmithkline Intellectual Property (No.2) Limited Indoline derivatives as inhibitors of perk
MX357763B (es) 2013-10-18 2018-07-23 Univ Health Network Tratamiento para cancer pancreatico.
JP2017500307A (ja) 2013-12-12 2017-01-05 ノバルティス アーゲー がんの処置のためのトラメチニブ、パニツムマブおよびダブラフェニブの組合せ
EP3111222A1 (en) 2014-02-26 2017-01-04 Glaxosmithkline Intellectual Property (No. 2) Limited Methods of treating cancer patients responding to ezh2 inhibitor gsk126
CA2942204A1 (en) 2014-03-12 2015-09-17 Novartis Ag Combination comprising a btk inhibitor and an akt inhibitor
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.
ES2930667T3 (es) 2014-07-11 2022-12-21 Gilead Sciences Inc Moduladores de receptores de tipo Toll para el tratamiento de VIH
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
MX2017003284A (es) 2014-09-16 2017-06-28 Gilead Sciences Inc Formas solidas de modulador de receptor tipo toll.
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
AU2016303550B2 (en) 2015-08-04 2019-06-13 Glaxosmithkline Intellectual Property Development Limited Combination treatments and uses and methods thereof
WO2017021913A1 (en) 2015-08-04 2017-02-09 Glaxosmithkline Intellectual Property Development Limited Combination treatments and uses and methods thereof
EP3331918A1 (en) 2015-08-04 2018-06-13 GlaxoSmithKline Intellectual Property Development Limited Combination treatments and uses and methods thereof
JP2018522053A (ja) 2015-08-06 2018-08-09 グラクソスミスクライン、インテレクチュアル、プロパテ Ｔｌｒ４アゴニストおよびその組成物ならびに癌の処置におけるそれらの使用
WO2017021912A1 (en) 2015-08-06 2017-02-09 Glaxosmithkline Intellectual Property Development Limited Combined tlrs modulators with anti ox40 antibodies
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
WO2017025871A1 (en) 2015-08-07 2017-02-16 Glaxosmithkline Intellectual Property Development Limited Combination therapy comprising anti ctla-4 antibodies
CN108884161A (zh) 2015-12-01 2018-11-23 葛兰素史密斯克莱知识产权发展有限公司 联合治疗及其用途和方法
MX363780B (es) 2015-12-03 2019-04-03 Glaxosmithkline Ip Dev Ltd Dinucleótidos de purina cíclica como moduladores del estimulador de los genes de interferón.
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
HRP20221263T1 (hr) 2016-03-18 2023-03-03 Immune Sensor, Llc Ciklički di-nukleotidni spojevi i postupci uporabe
WO2017175156A1 (en) 2016-04-07 2017-10-12 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides useful as protein modulators
HRP20220936T1 (hr) 2016-04-07 2022-10-28 Glaxosmithkline Intellectual Property Development Limited Heterociklički amidi korisni kao modulatori proteina
JP2019521166A (ja) 2016-07-20 2019-07-25 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｐｅｒｋ阻害剤としてのイソキノリン誘導体
US11649289B2 (en) 2016-08-04 2023-05-16 Glaxosmithkline Intellectual Property Development Limited Anti-ICOS and anti-PD-1 antibody combination therapy
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
KR20190101406A (ko) 2016-12-23 2019-08-30 아비나스 오퍼레이션스, 인코포레이티드 Egfr 단백질분해 표적화 키메라 분자 및 관련 사용 방법
JP2020504741A (ja) 2016-12-23 2020-02-13 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． Ｒａｆ（急速進行性線維肉腫）ポリペプチドの標的分解のための化合物および方法
WO2018150326A1 (en) 2017-02-15 2018-08-23 Glaxosmithkline Intellectual Property Development Limited Combination treatment for cancer
US11504333B2 (en) 2017-07-05 2022-11-22 Novartis Ag Pharmaceutical composition
WO2019021208A1 (en) 2017-07-27 2019-01-31 Glaxosmithkline Intellectual Property Development Limited USEFUL INDAZOLE DERIVATIVES AS PERK INHIBITORS
UY37866A (es) 2017-09-07 2019-03-29 Glaxosmithkline Ip Dev Ltd Nuevos compuestos derivados de benzoimidazol sustituidos que reducen la proteína myc (c-myc) en las células e inhiben la histona acetiltransferasa de p300/cbp.
WO2019053617A1 (en) 2017-09-12 2019-03-21 Glaxosmithkline Intellectual Property Development Limited CHEMICAL COMPOUNDS
EP3692033A1 (en) 2017-10-05 2020-08-12 GlaxoSmithKline Intellectual Property Development Limited Modulators of stimulator of interferon genes (sting) useful in treating 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
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
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
US11304930B2 (en) 2018-08-07 2022-04-19 Metagone Biotech Inc. Ammonium salts of 3-(3,5-dibromo-4-hydroxybenzyliden)-5-indo-1,3-dihydroindol-2-one and uses thereof
CN112996507B (zh) * 2018-09-18 2023-09-05 北京强新生物科技有限公司 肥胖症的治疗
JP7406556B2 (ja) 2018-11-30 2023-12-27 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド Ｈｉｖ療法に有用な化合物
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
EP3969438A1 (en) 2019-05-16 2022-03-23 Stingthera, Inc. Oxoacridinyl acetic acid derivatives and methods of use
US20220251079A1 (en) 2019-05-16 2022-08-11 Stingthera, Inc. Benzo[b][1,8]naphthyridine acetic acid derivatives and methods of use
EP3990494A1 (en) 2019-06-26 2022-05-04 GlaxoSmithKline Intellectual Property Development Limited Il1rap binding proteins
GB201910305D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
GB201910304D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
WO2021046289A1 (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 ipilimumab
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
JP2023512023A (ja) 2020-01-28 2023-03-23 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド 併用療法及びその使用及び方法
CN114573453A (zh) * 2020-12-02 2022-06-03 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
WO2023230541A1 (en) 2022-05-27 2023-11-30 Viiv Healthcare Company Piperazine derivatives useful in hiv therapy
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use

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
ES2201266T3 (es) * 1996-01-17 2004-03-16 Taiho Pharmaceutical Company Limited Inhibidores del espesamiento de la capa intima.
EP0929520B1 (en) * 1996-08-23 2005-11-02 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease

Also Published As

Publication number Publication date
MA26529A1 (fr) 2004-12-20
ATE344241T1 (de) 2006-11-15
GB9716557D0 (en) 1997-10-08
DE69836332D1 (de) 2006-12-14
ZA987037B (en) 2000-02-07
EP1003721B1 (en) 2006-11-02
WO1999010325A1 (en) 1999-03-04
PE112699A1 (es) 1999-11-16
AR016789A1 (es) 2001-08-01
AU9158498A (en) 1999-03-16
ES2272008T3 (es) 2007-04-16
EP1003721A1 (en) 2000-05-31
JP2002514228A (ja) 2002-05-14
US6268391B1 (en) 2001-07-31

Similar Documents

Publication Publication Date Title
DE69836332T2 (de) Benzyliden-1,3-dihydro-indol-2-on-derivate als inhibitoren von rezeptor tyrosin kinasen, insbesondere von raf kinasen
DE69824014T2 (de) Substituierte oxindolderivate als proteintyrosinkinase- und als protein-serin/threoninkinaseinhibitoren
US7338966B2 (en) Substituted oxindole derivatives as tyrosine kinase inhibitors
DE60002714T2 (de) Substituierte azaoxindolederivate
DE60215682T2 (de) AZAOXOINDOL DERIVATE ALS Trk PROTEIN KINASE HEMMSTOFFE ZUR BEHANDLUNG VON KREBS UND CHRONISCHEM SCHMERZ
US20050282810A1 (en) Oxindole derivatives
KR20110075010A (ko) 키나제 억제제로서 유용한 이미다조피리다진카르보니트릴
US6624171B1 (en) Substituted aza-oxindole derivatives
DD289529A5 (de) Verfahren zur herstellung heterozyklischer verbindungen
ES2230337T3 (es) Derivados de oxindol.
DE102008062825A1 (de) 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo [4,3-b]pyridazin-derivate
CZ2000798A3 (cs) Substituované oxindolové deriváty

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee