PE107699A1 - Derivados de oxindol sustituidos - Google Patents

Derivados de oxindol sustituidos

Info

Publication number
PE107699A1
PE107699A1 PE1998000818A PE00081898A PE107699A1 PE 107699 A1 PE107699 A1 PE 107699A1 PE 1998000818 A PE1998000818 A PE 1998000818A PE 00081898 A PE00081898 A PE 00081898A PE 107699 A1 PE107699 A1 PE 107699A1
Authority
PE
Peru
Prior art keywords
aliphatic group
compound
kinasa
inhibitor
formula
Prior art date
Application number
PE1998000818A
Other languages
English (en)
Inventor
Stephen Thomas Davis
Scott Howard Dickerson
Stephen Vernon Frye
Philip Anthony Harris
Iii Robert Neil Hunter
Lee Frederick Kuyper
Karen Elizabeth Lackey
Michael Joseph Luzzio
James Marvin Veal
Duncan Herrick Walker
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 PE107699A1 publication Critical patent/PE107699A1/es

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    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
    • 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
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Cosmetics (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE X ES N, CH, CCF3 o UN C(GRUPO ALIFATICO C1-C12); R1 ES H, UN GRUPO ALIFATICO C1-C12, TIOL, OH, ENTRE OTROS; R2 ES H, UN GRUPO ALIFATICO C1-C12, ALCOXI C1-C12, ENTRE OTROS; R3 ES H, UN GRUPO ALIFATICO C1-C12, HIDROXI, ENTRE OTROS; O R2 Y R3 FORMAN UN ANILLO FUSIONADO OPCIONALMENTE SUSTITUIDO; CON LA CONDICION QUE R1, R2 Y R3 NO SON H A LA VEZ; R4 ES ACIDO SULFONICO, UN GRUPO ALIFATICO C1-C12-(SULFONILO), UN GRUPO ALIFATICO C1-C6(AMINO), ENTRE OTROS; R5 ES H; O R4 Y R5 FORMAN UN ANILLO FUSIONADO OPCIONALMENTE SUSTITUIDO. CUANDO R2 ES TIADIAZINA, ENTONCES R4 NO ES METILSULFONA. UN COMPUESTO PREFERIDO DE FORMULA A, ENTRE OTROS. EL COMPUESTO SE PRESENTA EN UNA FORMA FARMACEUTICA DE USO TOPICO. EL COMPUESTO I ES UN INHIBIDOR DE CINASA E INHIBIDOR SELECTIVO DE LA CINASA DEPENDIENTE DE CICLINA, POR LO QUE PUEDE SER UTIL PARA EL TRATAMIENTO DE RECHAZO DE TRASPLANTE DE ORGANOS, INHIBICION DEL CRECIMIENTO DE TUMORES, ALOPECIA, TROMBOCITOPENIA, LEUCOPENIA INDUCIDA POR QUIMIOTERAPIA
PE1998000818A 1997-09-05 1998-09-02 Derivados de oxindol sustituidos PE107699A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9718913.8A GB9718913D0 (en) 1997-09-05 1997-09-05 Substituted oxindole derivatives

Publications (1)

Publication Number Publication Date
PE107699A1 true PE107699A1 (es) 1999-11-24

Family

ID=10818643

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1998000818A PE107699A1 (es) 1997-09-05 1998-09-02 Derivados de oxindol sustituidos

Country Status (23)

Country Link
US (4) US6387919B1 (es)
EP (1) EP1009738B1 (es)
JP (1) JP2001517652A (es)
KR (1) KR20010023695A (es)
CN (1) CN1278794A (es)
AR (1) AR015432A1 (es)
AT (1) ATE267170T1 (es)
AU (1) AU747506B2 (es)
BR (1) BR9812048A (es)
CA (1) CA2302572A1 (es)
CO (1) CO4960633A1 (es)
DE (1) DE69824014T2 (es)
EE (1) EE200000117A (es)
ES (1) ES2221211T3 (es)
GB (1) GB9718913D0 (es)
HU (1) HUP0004490A3 (es)
MA (1) MA26542A1 (es)
PE (1) PE107699A1 (es)
PL (1) PL338991A1 (es)
TR (1) TR200001174T2 (es)
TW (1) TW520358B (es)
WO (1) WO1999015500A1 (es)
ZA (1) ZA988078B (es)

Families Citing this family (255)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6407132B1 (en) * 1997-07-25 2002-06-18 James Black Foundation Limited Substituted imidazole derivatives and their use as histamine H3 receptor ligands
GB9718913D0 (en) * 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
DE19816624A1 (de) * 1998-04-15 1999-10-21 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
DE19824922A1 (de) * 1998-06-04 1999-12-09 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
US6319918B1 (en) 1998-06-04 2001-11-20 Boehringer Ingelheim Pharma Kg Substituted indolinones with kinase inhibitory activity
US6153634A (en) 1998-12-17 2000-11-28 Hoffmann-La Roche Inc. 4,5-azolo-oxindoles
KR20010108024A (ko) 1998-12-17 2001-12-07 프리돌린 클라우스너, 롤란드 비. 보레르 단백질 키나제 억제제로서의 4,5-피라진옥신돌
BR9916216A (pt) * 1998-12-17 2001-09-11 Hoffmann La Roche 4.5-azolo-oxindóis
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
CA2354591A1 (en) 1998-12-17 2000-06-22 F. Hoffmann-La Roche Ag 4-aryloxindoles as inhibitors of jnk protein kinases
EP1147214B1 (en) 1999-01-13 2011-01-05 The Research Foundation Of State University Of New York A novel method for designing protein kinase inhibitors
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
US6492398B1 (en) * 1999-03-04 2002-12-10 Smithkline Beechman Corporation Thiazoloindolinone compounds
GB9904933D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Compounds
GB9904930D0 (en) * 1999-03-04 1999-04-28 Glaxo Group Ltd Thiazoloindolinone compounds
US6624171B1 (en) 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
US6358947B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods
US6399593B1 (en) 1999-05-04 2002-06-04 Wyeth Cyclic regimens using cyclic urea and cyclic amide derivatives
US6391907B1 (en) 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
US6358948B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
US6306851B1 (en) 1999-05-04 2001-10-23 American Home Products Corporation Cyclocarbamate and cyclic amide derivatives
US6339098B1 (en) 1999-05-04 2002-01-15 American Home Products Corporation 2,1-benzisothiazoline 2,2-dioxides
US6417214B1 (en) 1999-05-04 2002-07-09 Wyeth 3,3-substituted indoline derivatives
US6319912B1 (en) 1999-05-04 2001-11-20 American Home Products Corporation Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides
US6369056B1 (en) 1999-05-04 2002-04-09 American Home Products Corporation Cyclic urea and cyclic amide derivatives
US6355648B1 (en) 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6444668B1 (en) 1999-05-04 2002-09-03 Wyeth Combination regimens using progesterone receptor modulators
US6423699B1 (en) 1999-05-04 2002-07-23 American Home Products Corporation Combination therapies using benzimidazolones
US6380178B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Cyclic regimens using cyclocarbamate and cyclic amide derivatives
US6498154B1 (en) 1999-05-04 2002-12-24 Wyeth Cyclic regimens using quinazolinone and benzoxazine derivatives
US6509334B1 (en) 1999-05-04 2003-01-21 American Home Products Corporation Cyclocarbamate derivatives as progesterone receptor modulators
US6462032B1 (en) 1999-05-04 2002-10-08 Wyeth Cyclic regimens utilizing indoline derivatives
US6407101B1 (en) 1999-05-04 2002-06-18 American Home Products Corporation Cyanopyrroles
US6329416B1 (en) 1999-05-04 2001-12-11 American Home Products Corporation Combination regimens using 3,3-substituted indoline derivatives
GB9911053D0 (en) * 1999-05-12 1999-07-14 Pharmacia & Upjohn Spa 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents
DE19924401A1 (de) * 1999-05-27 2000-11-30 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
AU6998000A (en) 1999-08-27 2001-03-26 Boehringer Ingelheim Pharma Kg Substituted indolinones as tyrosine kinase inhibitors
ATE350044T1 (de) * 1999-09-24 2007-01-15 Smithkline Beecham Corp Thrombopoietinmimetika
DE19949209A1 (de) * 1999-10-13 2001-04-19 Boehringer Ingelheim Pharma In 5-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
UA75054C2 (uk) * 1999-10-13 2006-03-15 Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу
US6762180B1 (en) 1999-10-13 2004-07-13 Boehringer Ingelheim Pharma Kg Substituted indolines which inhibit receptor tyrosine kinases
US6313310B1 (en) 1999-12-15 2001-11-06 Hoffmann-La Roche Inc. 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
HN2001000008A (es) 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
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
WO2001079198A1 (en) 2000-04-18 2001-10-25 Agouron Pharmaceuticals, Inc. Pyrazoles for inhibiting protein kinase
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
US6534531B2 (en) * 2000-04-27 2003-03-18 Bristol-Myers Squibb Company Methods for preventing and treating alopecia induced by chemotherapy or radiotherapy
JP4216503B2 (ja) * 2000-04-28 2009-01-28 アステラス製薬株式会社 βアミロイド産生抑制用医薬組成物
CY2010012I2 (el) 2000-05-25 2020-05-29 Novartis Ag Μιμητικα θρομβοποιητινης
GB0016454D0 (en) 2000-07-04 2000-08-23 Hoffmann La Roche Thienopyrrolidinones
WO2002012250A2 (en) 2000-08-09 2002-02-14 Agouron Pharmaceuticals, Inc. Pyrazole-thiazole compounds, pharmaceutical compositions containing them, and methods of their use for inhibiting cyclin-dependent kinases
ATE295354T1 (de) 2000-08-18 2005-05-15 Agouron Pharma Heterozyklische-hydroximino-fluorene und ihre verwendung zur inhibierung von proteinkinasen
EP1317446A1 (en) * 2000-09-01 2003-06-11 Glaxo Group Limited Oxindole derivatives
DE60106947T2 (de) * 2000-09-01 2005-11-10 Glaxo Group Ltd., Greenford Oxindolderivate
WO2002020479A1 (en) 2000-09-01 2002-03-14 Glaxo Group Limited Substituted oxindole derivatives as tyrosine kinase inhibitors
EP1201765A3 (en) * 2000-10-16 2003-08-27 Axxima Pharmaceuticals Aktiengesellschaft Cellular kinases involved in cytomegalovirus infection and their inhibition
DE10054019A1 (de) * 2000-11-01 2002-05-23 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
US6638965B2 (en) 2000-11-01 2003-10-28 Boehringer Ingelheim Pharma Kg Substituted indolinones, preparation thereof and their use as pharmaceutical compositions
DE10117204A1 (de) 2001-04-06 2002-10-10 Boehringer Ingelheim Pharma In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
SE0101230L (sv) * 2001-04-06 2002-10-07 Innoventus Project Ab Ny användning av en tyrosinkinasinhibitor
WO2002094809A1 (en) * 2001-05-24 2002-11-28 Yamanouchi Pharmaceutical Co., Ltd. 3-quinoline-2-(1h)-ylideneindolin-2-one derivatives
ATE330608T1 (de) 2001-06-29 2006-07-15 Ab Science Die verwendung von n-phenyl-2-pyrimidine-amine derivaten zur behandlung von entzündlichen erkrankungen
US7678805B2 (en) 2001-06-29 2010-03-16 Ab Science Use of tyrosine kinase inhibitors for treating inflammatory bowel diseases (IBD)
JP2005500041A (ja) 2001-06-29 2005-01-06 アブ サイエンス 強力で選択的かつ非毒性のｃ−ｋｉｔ阻害剤
US20040242612A1 (en) * 2001-09-20 2004-12-02 Alain Moussy Use of tyrosine kinase inhibitors for promoting hair growth
CA2461181A1 (en) * 2001-09-20 2003-05-01 Ab Science Use of potent, selective and non-toxic c-kit inhibitors for treating bacterial infections
WO2003027109A1 (en) * 2001-09-27 2003-04-03 Allergan, Inc. 3-(heteroarylamino)methylene-1, 3-dihydro-2h-indol-2-ones as kinase inhibitors
US6765012B2 (en) * 2001-09-27 2004-07-20 Allergan, Inc. 3-(Arylamino)methylene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors
WO2003033491A1 (fr) * 2001-10-16 2003-04-24 Nippon Kayaku Kabushiki Kaisha Composition medicinale de prevention ou de soulagement d'effets secondaires chez les patients souffrant de cancer et composition anticancereuse medicinale
EP1444204A4 (en) * 2001-10-22 2009-11-04 Univ New York State Res Found INHIBITORS OF PROTEIN KINASES AND PROTEINS PHOSPHATASES, METHODS OF IDENTIFICATION AND METHODS OF USE THEREOF
US7005445B2 (en) 2001-10-22 2006-02-28 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors and methods for designing them
US6797825B2 (en) 2001-12-13 2004-09-28 Abbott Laboratories Protein kinase inhibitors
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
EP1464645A1 (en) * 2001-12-18 2004-10-06 Kyowa Hakko Kogyo Co., Ltd. Indole derivative
US7482366B2 (en) * 2001-12-21 2009-01-27 X-Ceptor Therapeutics, Inc. Modulators of LXR
AU2002351412B2 (en) 2001-12-21 2010-05-20 Exelixis Patent Company Llc Modulators of LXR
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
FR2836914B1 (fr) 2002-03-11 2008-03-14 Aventis Pharma Sa Indazoles substitues, compositions les contenant, procede de fabrication et utilisation
KR20040104566A (ko) * 2002-04-30 2004-12-10 알콘, 인코퍼레이티드 안압 저하 및 녹내장성 망막병증/시신경병증 치료를 위한특유의 수단으로서의 결합 조직 성장 인자 (ｃｔｇｆ)의활성 및/또는 발현 조절, 저해, 또는 변조제
MY142390A (en) 2002-05-22 2010-11-30 Glaxosmithkline Llc 3' - [(2z)-[1-(3,4-dimethylphenyl)-1,5- dihydro-3- methyl-5-0xo-4h-pyrazol-4- ylidene]hydrazino]-2' -hydroxy -[1,1' -biphenyl]-3-carboxylic acid bis-(monoethanolamine)
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
DE10233500A1 (de) * 2002-07-24 2004-02-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg 3-Z-[1-(4-(N-((4-Methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylen]-6-methoxycarbonyl-2-indolinon-Monoethansulfonat und dessen Verwendung als Arzneimittel
US20040082615A1 (en) * 2002-08-07 2004-04-29 Michael Konkel 3-Imino-2-indolones for the treatement of depression and/or anxiety
AU2003259689A1 (en) * 2002-08-07 2004-02-25 Synaptic Pharmaceutical Corporation 3-imino-2-indolones for the treatment of depression and/or anxiety
GB0225873D0 (en) * 2002-11-06 2002-12-11 Cyclacel Ltd Combination
AU2003284572A1 (en) * 2002-11-22 2004-06-18 Yamanouchi Pharmaceutical Co., Ltd. 2-oxoindoline derivatives
ATE354096T1 (de) 2002-12-23 2007-03-15 Astex Therapeutics Ltd Synthese und screening von liganden mit hilfe von röntgenkristallographie
DK1656372T3 (da) 2003-07-30 2013-07-01 Rigel Pharmaceuticals Inc 2,4-pyrimidindiaminforbindelser til anvendelse til behandling eller forebyggelse af autoimmunsygdomme
TW200526638A (en) 2003-10-22 2005-08-16 Smithkline Beecham Corp 2-(3,4-dimethylphenyl)-4-{[2-hydroxy-3'-(1H-tetrazol-5-yl)biphenyl-3-yl]-hydrazono}-5-methyl-2,4-dihydropyrazol-3-one choline
GB0328180D0 (en) * 2003-12-04 2004-01-07 Cyclacel Ltd Combination
DE102004012069A1 (de) * 2004-03-12 2005-09-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue aryl-haltige 5-Acylindolinone, deren Herstellung und deren Verwendung als Arzneimittel
WO2005118551A2 (en) * 2004-05-28 2005-12-15 Ligand Pharmaceuticals Inc. Thrombopoietin activity modulating compounds and methods
CA2583764C (en) * 2004-10-25 2009-06-09 Ligand Pharmaceuticals, Inc. Thrombopoietin activity modulating compounds and methods
GT200500321A (es) * 2004-11-09 2006-09-04 Compuestos y composiciones como inhibidores de proteina kinase.
US20080125432A1 (en) 2004-12-01 2008-05-29 Devgen Nv 5-Carboxamido Substituted Thiazole Derivatives that Interact With Ion Channels, In Particular With Ion Channels From the Kv Family
EP2460408A1 (en) * 2004-12-17 2012-06-06 deVGen N.V. Nematicidal compositions
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
US7662824B2 (en) 2005-03-18 2010-02-16 Janssen Pharmaceutica Nv Acylhydrazones as kinase modulators
WO2006119660A1 (en) * 2005-05-11 2006-11-16 Givaudan Sa Encapsulation method
JP5225079B2 (ja) 2005-06-08 2013-07-03 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋ経路の阻害のための組成物および方法
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7749530B2 (en) 2005-07-13 2010-07-06 Allergan, Inc. Kinase inhibitors
WO2007008895A1 (en) * 2005-07-13 2007-01-18 Allergan, Inc. Kinase inhibitors
CA2602453A1 (en) 2005-07-13 2007-01-18 Allergan, Inc. Kinase inhibitors
GB0523041D0 (en) * 2005-11-11 2005-12-21 Cyclacel Ltd Combination
EP1991532B1 (en) 2006-02-24 2017-01-11 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8987474B2 (en) * 2006-04-07 2015-03-24 University Of South Florida Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
US7838542B2 (en) 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade
US8217177B2 (en) * 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8036664B2 (en) * 2006-09-22 2011-10-11 Kineto Wireless, Inc. Method and apparatus for determining rove-out
KR20090063240A (ko) * 2006-10-06 2009-06-17 아이알엠 엘엘씨 단백질 키나제 억제제 및 그의 사용 방법
GB0625283D0 (en) * 2006-12-19 2007-01-24 Cyclacel Ltd Combination
JP5568312B2 (ja) * 2007-02-13 2014-08-06 アーべー・シオンス キナーゼ阻害剤としての２−アミノチアゾール化合物の合成方法
WO2008134124A1 (en) * 2007-04-30 2008-11-06 The Uab Research Foundation Ul97 inhibitors for treatment of proliferative disorders
ECSP077628A (es) 2007-05-03 2008-12-30 Smithkline Beechman Corp Nueva composición farmacéutica
US7863315B2 (en) * 2008-01-15 2011-01-04 Shenzhen Chipscreen Biosciences, Ltd. 2-indolinone derivatives as selective histone deacetylase inhibitors
EP2265607B1 (en) 2008-02-15 2016-12-14 Rigel Pharmaceuticals, Inc. Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
US20110092452A1 (en) * 2008-03-05 2011-04-21 The Regents Of The University Of Michigan Compositions and methods for diagnosing and treating pancreatic cancer
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
PT2323993E (pt) 2008-04-16 2015-10-12 Portola Pharm Inc 2,6-diamino-pirimidina-5-il-carboxamidas como inibidores de quinasses syk ou jak
EP2116236A1 (en) 2008-04-21 2009-11-11 Université de Mons-Hainaut Bisbenzamidine derivatives for use as antioxidant
WO2009131687A2 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
WO2009135000A2 (en) * 2008-04-30 2009-11-05 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-117199 and analogs
WO2009139834A1 (en) * 2008-05-13 2009-11-19 Poniard Pharmaceuticals, Inc. Bioactive compounds for treatment of cancer and neurodegenerative diseases
JP6006938B2 (ja) 2008-06-09 2016-10-12 サイクラセル リミテッド スパシタビン（ｃｎｄａｃ）と、デシタビン及びプロカイン等のｄｎａメチルトランスフェラーゼ阻害剤との組合せ
WO2010039997A2 (en) * 2008-10-01 2010-04-08 The University Of North Carolina At Chapel Hill Hematopoietic protection against chemotherapeutic compounds using selective cyclin-dependent kinase 4/6 inhibitors
JP2012504645A (ja) * 2008-10-01 2012-02-23 ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル 健康な細胞に対する電離放射線の影響を低下させる又は防止するための医薬組成物
WO2010121212A2 (en) 2009-04-17 2010-10-21 H. Lee Moffit Cancer Center And Research Institute, Inc. Indoline scaffold shp-2 inhibitors and method of treating cancer
CA2761896A1 (en) 2009-05-13 2010-11-18 The University Of North Carolina At Chapel Hill Cyclin dependent kinase inhibitors and methods of use
CN102458120A (zh) 2009-05-29 2012-05-16 葛兰素史密斯克莱有限责任公司 给药血小板生成素激动剂化合物的方法
EP2459195A1 (en) * 2009-07-28 2012-06-06 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
AU2010300531A1 (en) 2009-09-30 2012-05-24 President And Fellows Of Harvard College Methods for modulation of autophagy through the modulation of autophagy-inhibiting gene products
US8652534B2 (en) * 2009-10-14 2014-02-18 Berry Pharmaceuticals, LLC Compositions and methods for treatment of mammalian skin
EP2493895B1 (en) * 2009-10-29 2017-04-26 Vectura Limited N-containing heteroaryl derivatives as jak3 kinase inhibitors
WO2011100528A2 (en) 2010-02-12 2011-08-18 Emory University Compositions and uses of lectins
EP2542528B1 (en) 2010-03-02 2013-06-19 Amakem NV Heterocyclic amides as rock inhibitors
WO2011161256A1 (en) 2010-06-25 2011-12-29 Facultes Universitaires Notre Dame De La Paix Beta carboline derivatives useful in the treatment of proliferative disorders
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
CN103153352B (zh) 2010-08-18 2015-07-15 爱默蕾大学 用于骨化的化合物和组合物以及其相关的方法
WO2012022780A1 (en) 2010-08-19 2012-02-23 Université Libre de Bruxelles 18-beta-glycyrrhetinic acid derivatives with anti-tumor activity
CA2961937C (en) 2010-10-25 2018-09-25 G1 Therapeutics, Inc. Cdk inhibitors
US8691830B2 (en) 2010-10-25 2014-04-08 G1 Therapeutics, Inc. CDK inhibitors
CA2816022C (en) 2010-10-29 2019-09-10 Emory University Quinazoline derivatives, compositions, and uses related thereto
US9102625B2 (en) 2010-11-01 2015-08-11 Portola Pharmaceuticals, Inc. Nicotinamides as JAK kinase modulators
GB201019043D0 (en) 2010-11-10 2010-12-22 Protea Biopharma N V Use of 2',5'-oligoadenylate derivative compounds
EP2640394A4 (en) 2010-11-17 2015-02-25 Univ North Carolina PROTECTION OF RENAL TISSUES AGAINST ISCHEMIA THROUGH INHIBITION OF CDK4 AND CDK6 PROLIFERATIVE KINASES
EP3153510B1 (en) 2010-12-03 2020-05-06 Emory University Fused azines as chemokine cxcr4 receptor modulators and uses related thereto
US8691777B2 (en) 2011-01-27 2014-04-08 Emory University Combination therapy
WO2012116137A2 (en) 2011-02-24 2012-08-30 Emory University Jab1 blocking compositions for ossification and methods related thereto
WO2012116135A2 (en) 2011-02-24 2012-08-30 Emory University Noggin blocking compositions for ossification and methods related thereto
WO2012135296A2 (en) 2011-03-31 2012-10-04 Emory University Imidazolyl amide compounds and uses related thereto
US10226478B2 (en) 2011-04-14 2019-03-12 Cyclacel Limited Dosage regimen for sapacitabine and decitabine in combination for treating acute myeloid leukemia
EP2699539B1 (en) 2011-04-21 2019-03-06 Emory University Cyclopropyl derivatives and methods of use
GB201107223D0 (en) 2011-04-29 2011-06-15 Amakem Nv Novel rock inhibitors
WO2012152807A1 (en) 2011-05-09 2012-11-15 Universiteit Antwerpen Activity-based probes for the urokinase plasminogen activator
GB201108225D0 (en) 2011-05-17 2011-06-29 Amakem Nv Novel KBC inhibitors
CA2839956A1 (en) 2011-06-20 2012-12-27 Emory University Prostaglandin receptor ep2 antagonists, derivatives, compositions, and uses related thereto
GB201113689D0 (en) 2011-08-09 2011-09-21 Amakem Nv Novel PDE4 inhibitors
EP2744775B1 (en) 2011-08-19 2018-03-07 Emory University Bax agonist, compositions, and methods related thereto
GB201114854D0 (en) 2011-08-29 2011-10-12 Amakem Nv Novel rock inhibitors
JP2014525426A (ja) 2011-08-31 2014-09-29 アマケン エンヴェー 新規のソフトｒｏｃｋ阻害剤
KR20140078710A (ko) 2011-09-30 2014-06-25 온코디자인 에스.에이. 거대고리 flt3 키나제 억제제
US9096609B2 (en) 2011-09-30 2015-08-04 Ipsen Pharma S.A.S. Macrocyclic LRRK2 kinase inhibitors
GB201119358D0 (en) 2011-11-10 2011-12-21 Lewi Paulus J Disubstituted triazine dimers for treatment and/or prevention of infectious diseases
DE102011119127A1 (de) * 2011-11-22 2013-05-23 Merck Patent Gmbh 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate
MX363551B (es) 2011-11-23 2019-03-27 Portola Pharmaceuticals Inc Star Compuestos derivados de pirazina como inhibidores de cinasa.
PL2810198T3 (pl) 2012-01-30 2024-01-22 Universiteit Gent Związki przeciwinwazyjne
GB201204756D0 (en) 2012-03-19 2012-05-02 Lewi Paulus J Triazines with suitable spacers for treatment and/or prevention of HIV infections
CA2868966C (en) 2012-03-29 2021-01-26 Francis Xavier Tavares Lactam kinase inhibitors
WO2013181135A1 (en) 2012-05-31 2013-12-05 Emory University Quinazoline derivatives, compositions, and uses related thereto
US9593125B2 (en) 2012-07-27 2017-03-14 Emory University Heterocyclic flavone derivatives, compositions, and methods related thereto
WO2014058921A2 (en) 2012-10-08 2014-04-17 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
US9877981B2 (en) 2012-10-09 2018-01-30 President And Fellows Of Harvard College NAD biosynthesis and precursors for the treatment and prevention of cancer and proliferation
EP2914585B1 (en) 2012-11-05 2018-03-07 Emory University 7,8-dihydroxyflavone and 7,8-substituted flavone derivatives, compositions, and methods related thereto
WO2014072419A1 (en) 2012-11-08 2014-05-15 Universiteit Antwerpen Novel anti-hiv compounds
BR112015018168B1 (pt) 2013-01-29 2023-04-11 Redx Pharma Plc Derivados de piridina e composição que os compreende derivados de piridina e composição que os compreende
EP2967050A4 (en) 2013-03-15 2016-09-28 G1 Therapeutics Inc HIGH-ACTIVE ANTINEOPLASTIC AND ANTIPROLIFERATIVE AGENTS
EP2968291A4 (en) 2013-03-15 2016-09-28 G1 Therapeutics Inc HSPC-PROOF TREATMENTS FOR RB-POSITIVE ABNORMAL CELLULAR PROLIFERATION
WO2014140313A1 (en) 2013-03-15 2014-09-18 Oncodesign S.A. Macrocyclic salt-inducible kinase inhibitors
US9572815B2 (en) 2013-03-15 2017-02-21 St. Jude Children's Research Hospital Methods and compositions of p27KIP1 transcriptional modulators
KR101548803B1 (ko) * 2013-09-09 2015-09-01 경북대학교병원 ３­（６­（４­（트리플루오로메톡시）페닐아미노）피리미딘­４­일）벤자미드 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 함유하는 당뇨병의 예방 또는 치료용 약학적 조성물
PL3043803T3 (pl) 2013-09-11 2022-11-07 Emory University Kompozycje nukleotydowe i nukleozydowe oraz ich zastosowanie
JP6595463B2 (ja) 2013-10-16 2019-10-23 ユニベルシテ リブレ デ ブリュッセル 気道に影響する増殖性疾患の処置に有用な製剤
CN103588758A (zh) * 2013-11-04 2014-02-19 南京大学 一类含1,4-苯并二噁烷骨架的硝基咪唑衍生物的合成、制备及其在抗癌药物中的应用
NO3068888T3 (es) 2013-11-12 2018-06-30
AU2014354643B2 (en) 2013-11-27 2020-03-05 Redwood Bioscience, Inc. Hydrazinyl-pyrrolo compounds and methods for producing a conjugate
KR101602203B1 (ko) * 2014-03-11 2016-03-11 경북대학교병원 N­（2­하이드록시에틸）­3­（6­（4­（트리플루오로메톡시）페닐아미노）피리미딘-4-일）벤자미드 또는 이의 약학적으로 허용 가능한 염을 유효성분으로 함유하는 당뇨병의 예방 또는 치료용 약학적 조성물
WO2015150337A1 (en) 2014-04-01 2015-10-08 Amakem Nv Lim kinase inhibitors
EP3125940A2 (en) 2014-04-01 2017-02-08 Université Libre de Bruxelles New strategies for treating melanoma
WO2015161288A1 (en) 2014-04-17 2015-10-22 G1 Therapeutics, Inc. Tricyclic lactams for use as anti-neoplastic and anti-proliferative agents
US9980936B2 (en) 2014-05-05 2018-05-29 Emory University BH4 antagonists and methods related thereto
US10450293B2 (en) 2014-05-16 2019-10-22 Emory University Chemokine CXCR4 and CCR5 receptor modulators and uses related thereto
EP3180003B1 (en) 2014-07-01 2022-01-12 The Regents of the University of California Pkc-epsilon inhibitors
WO2016005340A1 (en) 2014-07-08 2016-01-14 Universiteit Gent Hamamelitannin analogues and uses thereof
WO2016040858A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
WO2016040848A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors
MY186523A (en) 2014-09-17 2021-07-24 Oncodesign Sa Macrocyclic rip2 kinase inhibitors
DK3194405T3 (en) 2014-09-17 2019-04-15 Oncodesign Sa MACROCYCLIC LRRK2 KINase INHIBITORS
WO2016083490A1 (en) 2014-11-27 2016-06-02 Remynd Nv Compounds for the treatment of amyloid-associated diseases
SG10202013032YA (en) 2014-12-15 2021-02-25 Univ Emory Phosphoramidates for the treatment of hepatitis b virus
BR112017013858A2 (pt) 2014-12-26 2018-02-27 Univ Emory n4-hidroxicitidina e derivados e usos antivirais relacionados aos mesmos
WO2016146651A1 (en) 2015-03-16 2016-09-22 Oncodesign Sa Macrocyclic activin-like receptor kinase inhibitors
WO2016176437A1 (en) 2015-04-28 2016-11-03 Newsouth Innovations Pty Limited Targeting nad+ to treat chemotherapy and radiotherapy induced cognitive impairment, neuropathies and inactivity
EP3804706B1 (en) 2015-05-29 2023-08-23 Emory University 2-amino-n'-benzylideneacetohydrazides and derivatives for the management of cftr protein mediated diseases
EP3786164A1 (en) * 2015-06-18 2021-03-03 Ting Therapeutics LLC Methods and compositions for the prevention and treatment of hearing loss
DK3423113T3 (da) 2016-02-29 2020-11-30 Oncodesign Sa Radiomærket makrocyklisk egfr-hæmmer
WO2017157882A1 (en) 2016-03-14 2017-09-21 Université Catholique de Louvain Serine biosynthetic pathway inhibitors
WO2017161253A1 (en) * 2016-03-18 2017-09-21 Tufts Medical Center Compositions and methods for treating and preventing metabolic disorders
WO2017189978A1 (en) 2016-04-28 2017-11-02 Emory University Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto
US11166967B2 (en) 2016-05-19 2021-11-09 Universiteit Antwerpen Bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of PAR-related diseases
BE1023757B1 (nl) 2016-06-30 2017-07-12 Yun NV Bewaring van micro-organismen
WO2018065387A1 (en) 2016-10-04 2018-04-12 Universiteit Gent Novel hamamelitannin analogues and uses thereof
CN109923123B (zh) 2016-10-14 2024-01-23 爱默蕾大学 具有结合或阻断pd-l1的分子的纳米颗粒及其在治疗癌症中的用途
EP3532289B1 (en) 2016-10-26 2024-03-06 Emory University Polyoxometalate complexes and uses in managing cancer
WO2018096088A1 (en) 2016-11-24 2018-05-31 Universiteit Antwerpen Halogenated benzotropolones as atg4b inhibitors
EP3909598A1 (en) 2016-12-13 2021-11-17 Emory University Polypeptides for managing viral infections
BR112019013814A2 (pt) 2017-01-06 2020-01-21 G1 Therapeutics Inc método para tratamento de câncer ou de um tumor em um indivíduo, composição farmacêutica, combinação, e, kit.
WO2018138358A1 (en) 2017-01-30 2018-08-02 Université de Liège Perk and ire-1a inhibitors against neurodevelopmental disorders
IL292923B2 (en) 2017-02-21 2024-05-01 Univ Emory CXCR4 cytokine receptor modulators and related uses
WO2018160967A1 (en) * 2017-03-02 2018-09-07 Board Of Regents, The University Of Texas System Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase
CN106977508A (zh) * 2017-05-05 2017-07-25 遵义医学院 具有靛红结构的吡唑衍生物用于防治肿瘤的药物及其制法
EP3621963B1 (en) 2017-05-11 2024-01-24 Remynd N.V. Compounds for the treatment of epilepsy, neurodegenerative disorders and other cns disorders
US11661581B2 (en) * 2017-05-25 2023-05-30 University Of Massachusetts Use of CDK inhibitors to enhance growth and self-renewal of progenitor cells
WO2019006393A1 (en) 2017-06-29 2019-01-03 G1 Therapeutics, Inc. MORPHIC FORMS OF GIT38 AND METHODS OF MAKING SAME
KR102626210B1 (ko) 2017-12-07 2024-01-18 에모리 유니버시티 N4-하이드록시사이티딘 및 유도체 및 이와 관련된 항-바이러스 용도
EP3773562A1 (en) 2018-04-05 2021-02-17 Universiteit Hasselt Selective pde4d inhibitors against demyelinating diseases
IL309939A (en) 2018-06-29 2024-03-01 Rejuvenate Biomed Medicinal combination for use in age-related and/or degenerative diseases
EP4344743A3 (en) 2018-08-07 2024-06-19 Emory University Heterocyclic flavone derivatives, compositions, and methods related thereto
EP3840756A4 (en) 2018-08-24 2022-04-27 G1 Therapeutics, Inc. IMPROVED SYNTHESIS OF 1,4-DIAZASPIRO[5.5]UNDECAN-3-ONE
WO2020047229A1 (en) 2018-08-29 2020-03-05 University Of Massachusetts Inhibition of protein kinases to treat friedreich ataxia
JP7101311B2 (ja) * 2018-10-05 2022-07-14 イクノス サイエンシズ エスエー Ｍａｐ４ｋ１阻害剤として使用するためのインドリノン化合物
US20220227757A1 (en) 2019-05-14 2022-07-21 Suzhou Four Health Pharmaceuticals Co., Ltd. Quinazoline-2,4-dione derivatives as parp inhibitors
JP2023514443A (ja) 2020-02-24 2023-04-05 カトリーケ、ユニベルシテート、ルーベン ピロロピリジンおよびイミダゾピリジン抗ウイルス化合物
GB202003240D0 (en) 2020-03-05 2020-04-22 Ecosynth Nv Antiviral treatment
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
US11857551B1 (en) 2020-07-10 2024-01-02 Ting Therapeutics Llc Methods for the prevention and treatment of hearing loss
WO2022157381A1 (en) 2021-01-25 2022-07-28 Universiteit Hasselt Phloretin for use in the treatment of neurodegenerative and demyelinating diseases
WO2022191501A1 (ko) * 2021-03-12 2022-09-15 주식회사 온코크로스 항암제 내성 암의 치료를 위한 조성물
IL310243A (en) 2021-07-26 2024-03-01 Celcuity Inc 1-(4-{[4-(DIMETHYLAMINO)PIPERIDIN-1-YL]CARBONYL}PHENYL)-3-[4-(4,6-DIMORHOLIN-4-YL-1,3,5-TRIAZIN-2-YL )PHENYL]urea (GEDATOLISIB) and its combinations for use in cancer treatment
EP4377307A1 (en) 2021-07-30 2024-06-05 Confo Therapeutics N.V. Compounds for the treatment of pain, in particular neuropathic pain, and/or other diseases or disorders that are associated with at2r and/or at2r mediated signaling
WO2023021132A1 (en) 2021-08-18 2023-02-23 Katholieke Universiteit Leuven 6-substituted- and 6,7-disubstituted-7-deazapurine ribonucleoside analogues
WO2023046900A1 (en) 2021-09-23 2023-03-30 Katholieke Universiteit Leuven Ribonucleoside analogues against -sars-cov-2
WO2023105283A1 (en) 2021-12-08 2023-06-15 Fundacio Privada Institut De Recerca De La Sida - Caixa Nucleoside reverse transcriptase inhibitors for use in down syndrome and alzheimer`s disease therapy
US11541071B1 (en) 2021-12-16 2023-01-03 Ascletis BioScience Co., Ltd Nucleoside derivatives and methods of use thereof
WO2023111683A1 (en) 2021-12-16 2023-06-22 Ascletis Bioscience Co., Ltd. N4-hydroxycytidine derivatives and use thereof as antiviral agent
US11760722B2 (en) 2022-01-18 2023-09-19 Ascletis Bioscience Co., Ltd. Inhibitors of cysteine proteases and methods of use thereof
WO2023139402A1 (en) 2022-01-18 2023-07-27 Ascletis Bioscience Co., Ltd. Inhibitors of cysteine proteases and methods of use thereof
WO2023180567A1 (en) 2022-03-24 2023-09-28 Fundacion Privada Institut De Recerca De La Sida-Caixa Cyclodextrins for use in coronavirus infection therapy
WO2023241799A1 (en) 2022-06-15 2023-12-21 Université Libre de Bruxelles Flavanols for use in the treatment of retroviral infections
WO2024009120A1 (en) 2022-07-08 2024-01-11 Ascletis Bioscience Co., Ltd. Triazine derivatives and methods of use thereof
CN116514783A (zh) 2022-11-21 2023-08-01 歌礼生物科技（杭州）有限公司 三嗪衍生物

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2447940A1 (fr) 1979-02-05 1980-08-29 Ato Chimie Nouveaux (co)polycarbonates resistant au feu contenant des fonctions diesters ou hemiesters alcalins d'acides phosphoniques
EP0304493B1 (en) 1987-03-11 1992-09-02 Kanegafuchi Kagaku Kogyo Kabushiki Kaisha Hydroxystyrene derivatives
US5202341A (en) 1987-03-11 1993-04-13 Kanegafuchi Kagaku Kogyo Kabushiki Kaisha Hydroxystyrene compounds having tyrosine kinase inhibiting activity
US5089516A (en) 1987-03-11 1992-02-18 Kanegafuchi Kagaku Kogyo Kabushiki Kaisha 1-phenyl-3,5-pyrazolidinedione hydroxystyrene compounds which have tyrosine kinase inhibiting activity
GB8816944D0 (en) * 1988-07-15 1988-08-17 Sobio Lab Compounds
IE900394L (en) 1989-02-08 1990-08-08 Abbott Lab Thiazole derivatives
WO1991009598A1 (en) 1990-01-05 1991-07-11 Pfizer Inc. Azaoxindole derivatives
GB9004483D0 (en) 1990-02-28 1990-04-25 Erba Carlo Spa New aryl-and heteroarylethenylene derivatives and process for their preparation
US5164404A (en) 1991-03-15 1992-11-17 Neurosearch A/S Hydrazone derivatives and their use
EP0584264A1 (en) 1991-05-16 1994-03-02 Cold Spring Harbor Laboratory D-type cyclin and uses related thereto
GB9115160D0 (en) 1991-07-12 1991-08-28 Erba Carlo Spa Methylen-oxindole derivatives and process for their preparation
DE69233399T2 (de) 1991-09-20 2005-08-04 Fred Hutchinson Cancer Research Center, Seattle Menschliches cyclin e
US5441880A (en) 1991-11-18 1995-08-15 Cold Spring Harbor Laboratory Human cdc25 genes, encoded products and uses thereof
US5294538A (en) 1991-11-18 1994-03-15 Cold Spring Harbor Labs. Method of screening for antimitotic compounds using the CDC25 tyrosine phosphatase
US5770423A (en) 1991-11-18 1998-06-23 Cold Spring Harbor Laboratory Nucleic acids encoding cdc25 A and cdc25 B proteins and method of making cdc25 A and cdc25 B proteins
WO1993024514A1 (en) 1992-05-26 1993-12-09 Mitotix D-type cyclin and uses related thereto
WO1994023029A1 (en) 1993-03-31 1994-10-13 Monash University A nucleotide sequence encoding a chromosomal protein, associated chromosomal proteins and their uses
US5443962A (en) 1993-06-04 1995-08-22 Mitotix, Inc. Methods of identifying inhibitors of cdc25 phosphatase
GB9313638D0 (en) 1993-07-01 1993-08-18 Erba Carlo Spa Arylidene and heteroarylidene oxindole derivatives and process for their preparation
GB9412719D0 (en) 1994-06-24 1994-08-17 Erba Carlo Spa Substituted azaindolylidene compounds and process for their preparation
US5496828A (en) * 1994-08-22 1996-03-05 Eli Lilly And Company Methods of inhibiting ulcerative mucositis
AU729545B2 (en) 1994-10-24 2001-02-01 Baylor College Of Medicine Senescent cell-derived inhibitors of DNA synthesis
GB9423997D0 (en) 1994-11-28 1995-01-11 Erba Carlo Spa Substituted 3-arylidene-7-azaoxindole compounds and process for their preparation
GB9501567D0 (en) 1995-01-26 1995-03-15 Pharmacia Spa Hydrosoluble 3-arylidene-2-oxindole derivatives as tyrosine kinase inhibitors
GB9507298D0 (en) 1995-04-07 1995-05-31 Pharmacia Spa Substituted indolylmethylene-oxindale analogues as tyrosine kinase inhibitors
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
ATE243034T1 (de) 1996-01-17 2003-07-15 Taiho Pharmaceutical Co Ltd Intimale verdickungsinhibitoren
US5672508A (en) 1996-01-23 1997-09-30 Mitotix, Inc. Inhibitors of cell-cycle progression, and uses related thereto
EP0788890A1 (en) 1996-02-06 1997-08-13 Agfa-Gevaert N.V. Dyes and dye-donor elements for thermal dye transfer recording
KR100305071B1 (ko) 1996-03-29 2001-12-12 디. 제이. 우드, 스피겔 알렌 제이 벤질-락탐유도체및/또는벤질리덴-락탐유도체,이들의제조방법및이들의세로토닌1에이및/또는세로토닌1디수용체의선택적인길항제및/또는작용제로서의용도
WO1998007835A2 (en) 1996-08-21 1998-02-26 Sugen, Inc. Crystal structures of a protein tyrosine kinase
AU4155697A (en) 1996-08-23 1998-03-06 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
WO1998050356A1 (en) * 1997-05-07 1998-11-12 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6319918B1 (en) 1998-06-04 2001-11-20 Boehringer Ingelheim Pharma Kg Substituted indolinones with kinase inhibitory activity
GB9904933D0 (en) * 1999-03-04 1999-04-28 Glaxo Group Ltd Compounds
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
GB9904930D0 (en) * 1999-03-04 1999-04-28 Glaxo Group Ltd Thiazoloindolinone compounds
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

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