ATE270670T1 - Bicyclische heteroaromatische verbindungen als protein tyrosine kinase inhibitoren - Google Patents

Bicyclische heteroaromatische verbindungen als protein tyrosine kinase inhibitoren

Info

Publication number
ATE270670T1
ATE270670T1 AT99902522T AT99902522T ATE270670T1 AT E270670 T1 ATE270670 T1 AT E270670T1 AT 99902522 T AT99902522 T AT 99902522T AT 99902522 T AT99902522 T AT 99902522T AT E270670 T1 ATE270670 T1 AT E270670T1
Authority
AT
Austria
Prior art keywords
tyrosine kinase
kinase inhibitors
protein tyrosine
heteroaromatic compounds
bicyclic heteroaromatic
Prior art date
Application number
AT99902522T
Other languages
English (en)
Inventor
Malcolm Clive Carter
George Stuart Cockerill
Stephen Barry Guntrip
Karen Elizabeth Lackey
Kathryn Jane Smith
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10825153&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE270670(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Application granted granted Critical
Publication of ATE270670T1 publication Critical patent/ATE270670T1/de

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/04—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 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
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur 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
    • 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
    • C07D417/14—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 three or more hetero rings
AT99902522T 1998-01-12 1999-01-08 Bicyclische heteroaromatische verbindungen als protein tyrosine kinase inhibitoren ATE270670T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9800569.7A GB9800569D0 (en) 1998-01-12 1998-01-12 Heterocyclic compounds
PCT/EP1999/000048 WO1999035146A1 (en) 1998-01-12 1999-01-08 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors

Publications (1)

Publication Number Publication Date
ATE270670T1 true ATE270670T1 (de) 2004-07-15

Family

ID=10825153

Family Applications (3)

Application Number Title Priority Date Filing Date
AT99902522T ATE270670T1 (de) 1998-01-12 1999-01-08 Bicyclische heteroaromatische verbindungen als protein tyrosine kinase inhibitoren
AT04076762T ATE417847T1 (de) 1998-01-12 1999-01-08 Chinazolin- und pyridopyrimidinderivate
AT04076761T ATE322491T1 (de) 1998-01-12 1999-01-08 Bicyclische heteroaromatische verbindungen als protein tyrosine kinase inhibitoren

Family Applications After (2)

Application Number Title Priority Date Filing Date
AT04076762T ATE417847T1 (de) 1998-01-12 1999-01-08 Chinazolin- und pyridopyrimidinderivate
AT04076761T ATE322491T1 (de) 1998-01-12 1999-01-08 Bicyclische heteroaromatische verbindungen als protein tyrosine kinase inhibitoren

Country Status (48)

Country Link
US (11) US6727256B1 (de)
EP (3) EP1454907B1 (de)
JP (2) JP3390741B2 (de)
KR (1) KR100569776B1 (de)
CN (1) CN1134438C (de)
AP (1) AP1446A (de)
AR (2) AR015507A1 (de)
AT (3) ATE270670T1 (de)
AU (2) AU749549C (de)
BG (1) BG64825B1 (de)
BR (1) BR9906904B1 (de)
CA (1) CA2317589C (de)
CO (1) CO4820390A1 (de)
CY (3) CY1105618T1 (de)
CZ (1) CZ298047B6 (de)
DE (4) DE69930773T2 (de)
DK (3) DK1047694T3 (de)
EA (1) EA002455B1 (de)
EE (1) EE04616B1 (de)
EG (1) EG24743A (de)
ES (3) ES2262087T3 (de)
FR (1) FR08C0038I2 (de)
GB (1) GB9800569D0 (de)
GE (1) GEP20022678B (de)
HK (1) HK1031883A1 (de)
HR (2) HRP20000469B1 (de)
HU (1) HU227593B1 (de)
IL (2) IL137041A0 (de)
IS (1) IS2276B (de)
LU (1) LU91475I2 (de)
MA (1) MA26596A1 (de)
ME (1) ME00757B (de)
MY (1) MY124055A (de)
NL (1) NL300360I2 (de)
NO (2) NO316176B1 (de)
NZ (1) NZ505456A (de)
OA (1) OA11444A (de)
PE (1) PE20000230A1 (de)
PL (1) PL192746B1 (de)
PT (3) PT1460072E (de)
RS (1) RS49779B (de)
SI (3) SI1454907T1 (de)
SK (1) SK285405B6 (de)
TR (1) TR200002015T2 (de)
TW (1) TW477788B (de)
UA (1) UA66827C2 (de)
WO (1) WO1999035146A1 (de)
ZA (1) ZA99172B (de)

Families Citing this family (413)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6294532B1 (en) 1997-08-22 2001-09-25 Zeneca Limited Oxindolylquinazoline derivatives as angiogenesis inhibitors
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
KR100860295B1 (ko) 1998-10-08 2008-09-25 아스트라제네카 아베 퀴나졸린 유도체
GB2345486A (en) * 1999-01-11 2000-07-12 Glaxo Group Ltd Heteroaromatic protein tyrosine kinase inhibitors
CN1167422C (zh) 1999-02-10 2004-09-22 阿斯特拉曾尼卡有限公司 用作血管生成抑制剂的喹唑啉衍生物
GB9910579D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9910580D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
PT1731511E (pt) 1999-06-21 2015-11-13 Boehringer Ingelheim Pharma Heterociclos bicíclicos, medicamentos contendo estes compostos, a sua utilização e processos para a sua preparação
US6933299B1 (en) 1999-07-09 2005-08-23 Smithkline Beecham Corporation Anilinoquinazolines as protein tyrosine kinase inhibitors
ATE377597T1 (de) 1999-07-09 2007-11-15 Glaxo Group Ltd Anilinochinazoline als protein-tyrosin- kinasehemmer
JP4870304B2 (ja) * 1999-09-21 2012-02-08 アストラゼネカ アクチボラグ キナゾリン誘導体およびそれらの医薬品としての使用
UA74803C2 (uk) 1999-11-11 2006-02-15 Осі Фармасьютікалз, Інк. Стійкий поліморф гідрохлориду n-(3-етинілфеніл)-6,7-біс(2-метоксіетокси)-4-хіназолінаміну, спосіб його одержання (варіанти) та фармацевтичне застосування
JP2003520855A (ja) * 2000-01-28 2003-07-08 アストラゼネカ アクチボラグ 化学的化合物
GB0002952D0 (en) * 2000-02-09 2000-03-29 Pharma Mar Sa Process for producing kahalalide F compounds
AR035851A1 (es) * 2000-03-28 2004-07-21 Wyeth Corp 3-cianoquinolinas, 3-ciano-1,6-naftiridinas y 3-ciano-1,7-naftiridinas como inhibidoras de proteina quinasas
US6521618B2 (en) 2000-03-28 2003-02-18 Wyeth 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
CA2409139A1 (en) 2000-05-02 2001-11-08 Array Biopharma, Inc. Process for the reduction of cyano-substituted sulfones to aminoalkylene-substituted sulfones
EA005525B1 (ru) 2000-06-22 2005-04-28 Пфайзер Продактс Инк. Замещенные бициклические производные для лечения аномального роста клеток
PL360439A1 (en) 2000-06-28 2004-09-06 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
HU229624B1 (en) * 2000-06-30 2014-03-28 Glaxo Group Ltd Quinazoline ditosylate salt compounds
EP1792902A1 (de) * 2000-06-30 2007-06-06 Glaxo Group Limited Verfahren zur Herstellung von 5-(6-Chinazolinyl)-furan-2-carbaldehyden
WO2002012226A1 (en) 2000-08-09 2002-02-14 Astrazeneca Ab Quinoline derivatives having vegf inhibiting activity
JP2004509876A (ja) 2000-09-20 2004-04-02 メルク　パテント　ゲゼルシャフト　ミット　ベシュレンクテル　ハフトング ４−アミノ−キナゾリン
EP1777218B1 (de) 2000-10-20 2008-12-31 Eisai R&D Management Co., Ltd. Verfahren zur Herstellung von 4-Phenoxy chinolin Derivaten
US7776315B2 (en) 2000-10-31 2010-08-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and additional active ingredients
US7067532B2 (en) 2000-11-02 2006-06-27 Astrazeneca Substituted quinolines as antitumor agents
WO2002036570A1 (en) 2000-11-02 2002-05-10 Astrazeneca Ab 4-substituted quinolines as antitumor agents
US7019012B2 (en) 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
DK1399483T3 (da) 2001-01-05 2010-08-02 Pfizer Antistoffer til insulinlignende vækstfaktorrecptor I
EP1488809A1 (de) 2001-01-16 2004-12-22 Glaxo Group Limited Pharmazeutische Mischung gegen Krebs, die ein 4-Chinazolinamin in Kombination mit einem anderen antineoplastischen Wirkstoff enthält
ES2236481T3 (es) * 2001-01-16 2005-07-16 Glaxo Group Limited Combinacion farmaceutica que contiene una 4-quinazolinamina y paclitaxel, carboplatino o vinorelbina para el tratamiento de cancer.
AU2002252338B2 (en) * 2001-03-15 2007-09-13 Rhode Island Hospital, A Lifespan Partner Taurine compounds
CA2441501C (en) * 2001-03-23 2010-09-14 Bayer Corporation Rho-kinase inhibitors
UY27224A1 (es) * 2001-03-23 2002-10-31 Bayer Corp Inhibidores de la rho-quinasa
EP1249451B1 (de) 2001-04-13 2006-06-21 Pfizer Products Inc. Bizyklisch substituierte 4-Aminopyridopyrimidinderivate
WO2002092578A1 (en) * 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
US6995171B2 (en) 2001-06-21 2006-02-07 Agouron Pharmaceuticals, Inc. Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents
US20090197852A9 (en) * 2001-08-06 2009-08-06 Johnson Robert G Jr Method of treating breast cancer using 17-AAG or 17-AG or a prodrug of either in combination with a HER2 inhibitor
US7829566B2 (en) 2001-09-17 2010-11-09 Werner Mederski 4-amino-quinazolines
AR039067A1 (es) 2001-11-09 2005-02-09 Pfizer Prod Inc Anticuerpos para cd40
WO2003059913A1 (en) 2002-01-10 2003-07-24 Bayer Healthcare Ag Roh-kinase inhibitors
TW200406390A (en) 2002-01-17 2004-05-01 Neurogen Corp Substituted quinazolin-4-ylamine analogues
MXPA04007191A (es) 2002-01-23 2005-03-31 Bayer Pharmaceuticals Corp Derivados de pirimidina como inhibidores de rho-quinasa.
ATE381557T1 (de) 2002-01-23 2008-01-15 Bayer Pharmaceuticals Corp Rho-kinase inhibitoren
BR0307151A (pt) 2002-02-01 2004-12-07 Astrazeneca Ab Composto ou um sal do mesmo, processo para a preparação do mesmo, composição farmacêutica, uso do composto ou de um seu sal, método para produzir um efeito antiangiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente, como um ser humano, que necessita de um tratamento do tipo referido, e, processos para a preparação de 5-bromo-7- azaindol, e para a produção de 5-metóxi-7-azaindol
WO2003066602A1 (fr) * 2002-02-06 2003-08-14 Ube Industries, Ltd. Procede relatif a l'elaboration d'un compose 4-aminoquinazoline
WO2003086467A1 (en) * 2002-04-08 2003-10-23 Smithkline Beecham Corporation Cancer treatment method comprising administering an erb-family inhibitor and a raf and/or ras inhibitor
DE10221018A1 (de) 2002-05-11 2003-11-27 Boehringer Ingelheim Pharma Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie
JPWO2003101491A1 (ja) * 2002-06-03 2005-09-29 三菱ウェルファーマ株式会社 Ｈｅｒ２又は／及びＥＧＦＲ発現又は活性化対象に用いる予防又は／及び治療剤
UA77303C2 (en) 2002-06-14 2006-11-15 Pfizer Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use
US20040048887A1 (en) * 2002-07-09 2004-03-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and EGFR kinase inhibitors
GB0215823D0 (en) 2002-07-09 2002-08-14 Astrazeneca Ab Quinazoline derivatives
US7504408B2 (en) 2002-07-09 2009-03-17 Astrazeneca Ab Quinzoline derivatives for use in the treatment of cancer
EP2280003B1 (de) 2002-07-15 2014-04-02 Symphony Evolution, Inc. Verfahren zur Herstellung von Rezeptorkinase-Modulatoren
GB0304367D0 (en) * 2003-02-26 2003-04-02 Pharma Mar Sau Methods for treating psoriasis
GB0225579D0 (en) 2002-11-02 2002-12-11 Astrazeneca Ab Chemical compounds
US8505468B2 (en) * 2002-11-19 2013-08-13 Sharp Kabushiki Kaisha Substrate accommodating tray
US7432275B2 (en) * 2002-12-13 2008-10-07 Neurogen Corporation Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators
CA2510850A1 (en) 2002-12-19 2004-07-08 Pfizer Inc. 2-(1h-indazol-6-ylamino)-benzamide compounds as protein kinases inhibitors useful for the treatment of ophthalmic diseases
AU2003292435A1 (en) * 2002-12-23 2004-07-14 Astrazeneca Ab 4- (pyridin-4-ylamino) -quinazoline derivatives as anti-tumor agents
US20060167026A1 (en) * 2003-01-06 2006-07-27 Hiroyuki Nawa Antipsychotic molecular-targeting epithelial growth factor receptor
US7223749B2 (en) 2003-02-20 2007-05-29 Boehringer Ingelheim International Gmbh Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
OA13151A (en) 2003-02-26 2006-12-13 Sugen Inc Aminoheteroaryl compounds as protein kinase inhibitors.
EP1633870B1 (de) 2003-05-30 2013-03-27 OncoTherapy Science, Inc. Prozess zum screening einer medikamentenansprache in krebspatienten
TW200510373A (en) 2003-07-14 2005-03-16 Neurogen Corp Substituted quinolin-4-ylamine analogues
US7329664B2 (en) 2003-07-16 2008-02-12 Neurogen Corporation Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues
PT1648998E (pt) 2003-07-18 2014-11-04 Amgen Inc Agentes de ligação específica ao factor de crescimento do hepatócito
WO2005011607A2 (en) 2003-08-01 2005-02-10 Smithkline Beecham Corporation Treatment of cancers expressing p95 erbb2
WO2005021554A1 (en) 2003-08-29 2005-03-10 Pfizer Inc. Thienopyridine-phenylacet amides and their derivatives useful as new anti-angiogenic agents
GB0321066D0 (en) * 2003-09-09 2003-10-08 Pharma Mar Sau New antitumoral compounds
AR045563A1 (es) 2003-09-10 2005-11-02 Warner Lambert Co Anticuerpos dirigidos a m-csf
DK2210607T3 (da) * 2003-09-26 2011-12-12 Exelixis Inc N-[3-fluor-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorphenyl)cyclopropan-1,1-dicarboxamid til behandling af kræft
DE10349113A1 (de) 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
JP2007510667A (ja) * 2003-11-07 2007-04-26 スミスクライン ビーチャム （コーク） リミテッド 癌の治療法
EP1683785B1 (de) 2003-11-11 2013-10-16 Eisai R&D Management Co., Ltd. Harnstoffderivate und verfahren zu deren herstellung
GB0326459D0 (en) 2003-11-13 2003-12-17 Astrazeneca Ab Quinazoline derivatives
JP4936897B2 (ja) * 2003-12-18 2012-05-23 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 抗増殖剤としてのピリド−およびピリミドピリミジン誘導体
GB0330002D0 (en) 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
EP1755394A4 (de) * 2004-04-16 2009-08-05 Smithkline Beecham Corp Krebsbehandlungsverfahren
NZ550796A (en) 2004-05-06 2010-07-30 Warner Lambert Co 4-phenylamino-quinazolin-6-yl-amides
BRPI0511754A (pt) * 2004-06-03 2008-01-02 Smithkline Beechman Cork Ltd uso de um composto ou sais ou solvatos do mesmo
EP1781293A1 (de) * 2004-06-04 2007-05-09 Amphora Discovery Corporation Verbindungen auf chinolin- und isochinolin-basis mit atp-verwendender enzymhemmender aktivität und zusammensetzungen und verwendungen daraus
CN101564535A (zh) * 2004-06-04 2009-10-28 史密丝克莱恩比彻姆（科克）有限公司 癌症治疗方法
EP1765313A2 (de) 2004-06-24 2007-03-28 Novartis Vaccines and Diagnostics, Inc. Verbindungen als immunstimulatoren
US20100226931A1 (en) * 2004-06-24 2010-09-09 Nicholas Valiante Compounds for immunopotentiation
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
UA87153C2 (ru) 2004-08-26 2009-06-25 Пфайзер Инк. Энантиомерно чистые аминогетероарильные соединения как ингибиторы протеинкиназы
WO2006030826A1 (ja) 2004-09-17 2006-03-23 Eisai R & D Management Co., Ltd. 医薬組成物
TW200621251A (en) 2004-10-12 2006-07-01 Neurogen Corp Substituted biaryl quinolin-4-ylamine analogues
JP2008521900A (ja) 2004-11-30 2008-06-26 アムジエン・インコーポレーテツド キノリン及びキナゾリン類似体並びにがん治療のための医薬としてのその使用
GB0427131D0 (en) * 2004-12-10 2005-01-12 Glaxosmithkline Biolog Sa Novel combination
US7947676B2 (en) 2004-12-14 2011-05-24 Astrazeneca Ab Pyrazolo[3,4-d]pyrimidine compounds as antitumor agents
ES2426007T3 (es) * 2004-12-17 2013-10-18 Smithkline Beecham (Cork) Limited Método para el tratamiento del cáncer
US7812022B2 (en) 2004-12-21 2010-10-12 Glaxosmithkline Llc 2-pyrimidinyl pyrazolopyridine ErbB kinase inhibitors
ATE430747T1 (de) * 2004-12-21 2009-05-15 Smithkline Beecham Corp 2-pyrimidinyl-pyrazolopyridin-erbb- kinaseinhibitoren
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
JP2008526997A (ja) * 2005-01-14 2008-07-24 ニューロジェン・コーポレーション ヘテロアリール置換キノリン−４−イルアミン類縁体
SI2301531T1 (sl) 2005-02-18 2018-11-30 Abraxis Bioscience, Llc Kombinacije in načini dajanja terapevtskih sredstev in kombinacijska terapija
US8735394B2 (en) * 2005-02-18 2014-05-27 Abraxis Bioscience, Llc Combinations and modes of administration of therapeutic agents and combination therapy
US20060216288A1 (en) * 2005-03-22 2006-09-28 Amgen Inc Combinations for the treatment of cancer
EP1863848A4 (de) 2005-03-31 2009-09-23 Agensys Inc An 161p2f10b-proteine bindende antikörper und verwandte moleküle
HUE030982T2 (en) 2005-04-19 2017-06-28 Novartis Ag Pharmaceutical preparation
WO2006114704A2 (en) 2005-04-26 2006-11-02 Pfizer Inc. P-cadherin antibodies
WO2007015578A1 (ja) 2005-08-02 2007-02-08 Eisai R & D Management Co., Ltd. 血管新生阻害物質の効果を検定する方法
PT2447283E (pt) 2005-09-07 2015-10-08 Pfizer Anticorpos monoclonais humanos para cinase-1 tipo recetor de activina (alk-1)
WO2007034144A1 (en) 2005-09-20 2007-03-29 Astrazeneca Ab 4- (ih-indazol-s-yl-amino)-quinazoline compounds as erbb receptor tyrosine kinase inhibitors for the treatment of cancer
US8062838B2 (en) 2005-09-20 2011-11-22 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
UA96139C2 (uk) 2005-11-08 2011-10-10 Дженентек, Інк. Антитіло до нейропіліну-1 (nrp1)
JP5688877B2 (ja) 2005-11-11 2015-03-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 癌疾患の治療用キナゾリン誘導体
JP5103403B2 (ja) * 2005-12-05 2012-12-19 スミスクライン ビーチャム コーポレーション ２−ピリミジニルピラゾロピリジンＥｒｂＢキナーゼ阻害剤
CN101003514A (zh) * 2006-01-20 2007-07-25 上海艾力斯医药科技有限公司 喹唑啉衍生物、其制备方法及用途
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
AR059066A1 (es) * 2006-01-27 2008-03-12 Amgen Inc Combinaciones del inhibidor de la angiopoyetina -2 (ang2) y el inhibidor del factor de crecimiento endotelial vascular (vegf)
CA2636981A1 (en) * 2006-01-31 2007-08-09 F. Hoffmann-La Roche Ag 7h-pyrido[3,4-d]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
TW200808739A (en) * 2006-04-06 2008-02-16 Novartis Vaccines & Diagnostic Quinazolines for PDK1 inhibition
US20090203718A1 (en) * 2006-04-13 2009-08-13 Smithkline Beecham (Cork) Ltd. Cancer treatment method
AU2007240496A1 (en) 2006-04-19 2007-11-01 Novartis Ag Indazole compounds and methods for inhibition of CDC7
AU2007251282A1 (en) 2006-05-09 2007-11-22 Pfizer Products Inc. Cycloalkylamino acid derivatives and pharmaceutical compositions thereof
NL2000613C2 (nl) 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
CA2652442C (en) 2006-05-18 2014-12-09 Eisai R & D Management Co., Ltd. Antitumor agent for thyroid cancer
ATE417274T1 (de) * 2006-06-01 2008-12-15 Cellzome Ag Verfahren zur identifizierung von mit zap-70 wechselwirkenden molekülen und zur zap-70- reinigung
EP2032989B2 (de) 2006-06-30 2015-10-28 Merck Sharp & Dohme Corp. Igfbp2-biomarker
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
US20080051422A1 (en) * 2006-08-22 2008-02-28 Concert Pharmaceuticals Inc. 4-Aminoquinazoline derivatives and methods of use thereof
US20110053964A1 (en) * 2006-08-22 2011-03-03 Roger Tung 4-aminoquinazoline derivatives and methods of use thereof
KR101472600B1 (ko) 2006-08-28 2014-12-15 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암에 대한 항종양제
SI2068880T1 (sl) 2006-09-18 2012-08-31 Boehringer Ingelheim Int Postopek za zdravljenje raka, ki vsebuje mutacije EGFR
KR101129868B1 (ko) * 2006-10-04 2012-04-12 화이자 프로덕츠 인코포레이티드 칼슘 수용체 길항제로서의 피리도［4,3-ｄ］피리미딘-4(3Ｈ)-온 유도체
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
JP5528807B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
WO2008054633A1 (en) * 2006-10-31 2008-05-08 Janssen Pharmaceutica N.V. Hydrazone derivatives as kinase inhibitors
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
CN102123712B (zh) 2006-12-13 2014-03-19 默沙东公司 使用igf1r抑制剂治疗癌症的方法
EP2125781A2 (de) 2006-12-20 2009-12-02 Amgen Inc. Substituierte heterocyclen und anwendungsverfahren
ES2449482T3 (es) 2007-01-09 2014-03-19 Amgen Inc. Derivados de bis-aril-amida útiles para el tratamiento de cáncer
EP2119707B1 (de) 2007-01-29 2015-01-14 Eisai R&D Management Co., Ltd. Zusammensetzung zur behandlung von nicht differenzierten formen von magenkrebsen
CN101245050A (zh) * 2007-02-14 2008-08-20 上海艾力斯医药科技有限公司 4-苯胺喹唑啉衍生物的盐
MX2009008531A (es) 2007-02-16 2009-08-26 Amgen Inc Cetonas de heterociclilo que contienen nitrogeno y su uso como inhibidores de c-met.
AU2008239594B2 (en) 2007-04-13 2013-10-24 Beth Israel Deaconess Medical Center Methods for treating cancer resistant to ErbB therapeutics
AU2008249745B2 (en) * 2007-05-09 2012-01-12 Pfizer Inc. Substituted heterocyclic derivatives and compositions and their pharmaceutical use as antibacterials
EP2166859A4 (de) * 2007-06-11 2011-09-07 Smithkline Beecham Cork Ltd Chinazolinsalzverbindungen
UY31137A1 (es) * 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
TWI595005B (zh) 2007-08-21 2017-08-11 安健股份有限公司 人類ｃ－ｆｍｓ抗原結合蛋白質
WO2009033094A2 (en) 2007-09-07 2009-03-12 Agensys, Inc. Antibodies and related molecules that bind to 24p4c12 proteins
US20090215802A1 (en) * 2007-09-13 2009-08-27 Protia, Llc Deuterium-enriched lapatinib
CN101861159A (zh) * 2007-10-19 2010-10-13 马尔药品公司 改进的抗肿瘤治疗
WO2009055343A2 (en) 2007-10-22 2009-04-30 Schering Corporation Fully human anti-vegf antibodies and methods of using
EP2220054A2 (de) 2007-10-29 2010-08-25 Natco Pharma Limited Neue 4-(tetrazol-5-yl)chinazolinderivate als antikrebsmittel
JP5638244B2 (ja) 2007-11-09 2014-12-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質と抗腫瘍性白金錯体との併用
AR069798A1 (es) 2007-12-20 2010-02-17 Novartis Ag Derivados de 1, 3-tiazol, metodos para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de medicamentos para el tratamiento de enfermedades mediadas por la fosfatidilinositol 3-cinasa.
CN101492445A (zh) * 2008-01-22 2009-07-29 孙飘扬 杂芳族化合物、其制备方法以及其用途
AU2009209541A1 (en) * 2008-01-30 2009-08-06 Pharma Mar, S.A. Improved antitumoral treatments
RU2010140890A (ru) * 2008-03-07 2012-04-20 Фарма Мар, С.А. (Es) Улучшенные способы противоопухолевого лечения
TWI574698B (zh) 2008-03-18 2017-03-21 建南德克公司 抗ｈｅｒ２抗體-藥物結合物及化療劑之組合及使用方法
WO2009137714A2 (en) * 2008-05-07 2009-11-12 Teva Pharmaceutical Industries Ltd. Forms of lapatinib ditosylate and processes for preparation thereof
US20090306106A1 (en) * 2008-05-15 2009-12-10 Leonid Metsger Forms of crystalline lapatinib and processes for preparation thereof
CN101584696A (zh) 2008-05-21 2009-11-25 上海艾力斯医药科技有限公司 包含喹唑啉衍生物的组合物及制备方法、用途
WO2010017387A2 (en) * 2008-08-06 2010-02-11 Teva Pharmaceutical Industries Ltd. Lapatinib intermediates
EP2158912A1 (de) 2008-08-25 2010-03-03 Ratiopharm GmbH Pharmazeutische Zusammensetzung mit N-[3-chlor-4-(3-fluorophenyl)methoxy)phenyl)6-(5(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furyl)-4-chinazolinamin
EP2158913A1 (de) 2008-08-25 2010-03-03 Ratiopharm GmbH Pharmazeutische Zusammensetzung mit N-[3-chlor-4-(3-fluorophenyl)methoxy)phenyl)6-(5(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furyl)-4-chinazolinamin
WO2010027848A2 (en) * 2008-08-26 2010-03-11 Teva Pharmaceutical Industries Ltd. Forms of lapatinib compounds and processes for the preparation thereof
WO2010045495A2 (en) 2008-10-16 2010-04-22 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Fully human antibodies to high molecular weight-melanoma associated antigen and uses thereof
CA2740977A1 (en) 2008-11-03 2010-06-03 Natco Pharma Limited A novel process for the preparation of lapatinib and its pharmaceutically acceptable salts
EP2349235A1 (de) 2008-11-07 2011-08-03 Triact Therapeutics, Inc. Verwendung von catecholbutan-derivaten in der krebstherapie
WO2010083414A1 (en) 2009-01-16 2010-07-22 Exelixis, Inc. Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer
CN101787017A (zh) * 2009-01-23 2010-07-28 岑均达 光学纯喹唑啉类化合物
CN102307875A (zh) 2009-02-09 2012-01-04 苏伯俭股份有限公司 吡咯并嘧啶基axl激酶抑制剂
US20120189641A1 (en) 2009-02-25 2012-07-26 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
WO2010099137A2 (en) 2009-02-26 2010-09-02 Osi Pharmaceuticals, Inc. In situ methods for monitoring the emt status of tumor cells in vivo
EP2401613A2 (de) 2009-02-27 2012-01-04 OSI Pharmaceuticals, LLC Verfahren zur identifizierung von mesenchymähnlichen tumorzellen oder deren bildung hemmenden stoffen
US20100222381A1 (en) 2009-02-27 2010-09-02 Hariprasad Vankayalapati Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
JP2012519281A (ja) 2009-02-27 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー 間葉様腫瘍細胞またはその生成を阻害する薬剤を同定するための方法
US8481503B2 (en) 2009-03-06 2013-07-09 Merck Sharp & Dohme Corp. Combination cancer therapy with an AKT inhibitor and other anticancer agents
EP2408479A1 (de) 2009-03-18 2012-01-25 OSI Pharmaceuticals, LLC Kombinationskrebstherapie mit verabreichung eines egfr-hemmers und eines igf-1r-hemmers
RU2504553C2 (ru) * 2009-03-20 2014-01-20 Дженентек, Инк. Антитела к her
US8816077B2 (en) 2009-04-17 2014-08-26 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
WO2010120386A1 (en) 2009-04-17 2010-10-21 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
US8293753B2 (en) 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
LT2451445T (lt) 2009-07-06 2019-06-25 Boehringer Ingelheim International Gmbh Bibw2992, jo druskų ir kietų farmacinių kompozicijų, apimančių šį aktyvųjį ingredientą, džiovinimo būdas
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
EP2467140B1 (de) 2009-08-21 2016-06-01 Novartis AG Lapatinib zur krebsbehandlung
CA2772194A1 (en) 2009-09-01 2011-03-10 Pfizer Inc. Benzimidazole derivatives
ES2535176T3 (es) 2009-09-28 2015-05-06 Qilu Pharmaceutical Co., Ltd Derivados de 4-(anilino sustituido)quinazolina como inhibidores de la tirosina quinasa
US20120245351A1 (en) * 2009-09-29 2012-09-27 Natco Pharma Limited Process for the preparation of lapatinib and its pharmaceutically acceptable salts
WO2011058164A1 (en) 2009-11-13 2011-05-19 Pangaea Biotech, S.A. Molecular biomarkers for predicting response to tyrosine kinase inhibitors in lung cancer
CN102079759B (zh) * 2009-12-01 2014-09-17 天津药物研究院 6位取代的喹唑啉类衍生物、其制备方法和用途
AR079256A1 (es) 2009-12-04 2012-01-04 Genentech Inc Metodo para el tratamiento del cancer de mama metastasico con trastuzumab-mcc-dm1
AU2010338038B2 (en) 2009-12-31 2015-07-09 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Tricyclic compounds for use as kinase inhibitors
CA2787714C (en) 2010-01-22 2019-04-09 Joaquin Pastor Fernandez Inhibitors of pi3 kinase
WO2011098971A1 (en) 2010-02-12 2011-08-18 Pfizer Inc. Salts and polymorphs of 8-fluoro-2-{4-[(methylamino}methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one
SG183361A1 (en) 2010-02-18 2012-09-27 Ct Nac Investigaciones Oncologicas Cnio Triazolo [4, 5 - b] pyridin derivatives
CA2783665A1 (en) 2010-03-03 2011-09-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
EP2519826A2 (de) 2010-03-03 2012-11-07 OSI Pharmaceuticals, LLC Biologische marker als prädiktoren der antikrebsreaktion auf insulinähnlichen wachstumsfaktor-1-rezeptor-kinaseinhibitoren
US8563719B2 (en) 2010-03-23 2013-10-22 Scinopharm Taiwan, Ltd. Process and intermediates for preparing lapatinib
US8710221B2 (en) 2010-03-23 2014-04-29 Scinopharm Taiwan, Ltd. Process and intermediates for preparing lapatinib
US9393318B2 (en) 2010-03-29 2016-07-19 Abraxis Bioscience, Llc Methods of treating cancer
AU2011232862B2 (en) 2010-03-29 2016-03-03 Abraxis Bioscience, Llc Methods of enhancing drug delivery and effectiveness of therapeutic agents
WO2011121317A1 (en) 2010-04-01 2011-10-06 Centro Nacional De Investigaciones Oncologicas (Cnio) Imidazo [2,1-b] [1,3,4] thiadiazoles as protein or lipid kinase inhibitors
US20130072507A1 (en) 2010-05-21 2013-03-21 Glaxosmithkline Llc Combination
WO2011146712A1 (en) 2010-05-21 2011-11-24 Glaxosmithkline Llc Combination
AU2011261685B2 (en) 2010-06-04 2016-02-11 Abraxis Bioscience, Llc Methods of treatment of pancreatic cancer
CA2802857C (en) 2010-06-16 2018-09-11 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Antibodies to endoplasmin and their use
WO2011161217A2 (en) 2010-06-23 2011-12-29 Palacký University in Olomouc Targeting of vegfr2
KR101677790B1 (ko) 2010-06-25 2016-11-18 에자이 알앤드디 매니지먼트 가부시키가이샤 키나제 저해 작용을 갖는 화합물의 병용에 의한 항종양제
SG186983A1 (en) 2010-07-09 2013-02-28 Genentech Inc Anti-neuropilin antibodies and methods of use
CN102344444B (zh) * 2010-07-23 2015-07-01 岑均达 光学纯喹唑啉类化合物
CN102344445B (zh) * 2010-07-23 2015-11-25 岑均达 光学纯喹唑啉类化合物
AR082418A1 (es) 2010-08-02 2012-12-05 Novartis Ag Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico
EP3264089A1 (de) 2010-08-31 2018-01-03 Genentech, Inc. Biomarker und behandlungsverfahren
ES2543151T3 (es) 2010-10-20 2015-08-17 Pfizer Inc Derivados de 2-piridina como moduladores del receptor Smoothened
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
WO2012069557A1 (en) 2010-11-24 2012-05-31 Glaxo Group Limited Multispecific antigen binding proteins targeting hgf
CN102558160B (zh) * 2010-12-20 2015-09-23 天津药物研究院 4-取代对甲磺酰胺苯胺基-喹唑啉衍生物及其制备方法和用途
CN102558159A (zh) * 2010-12-20 2012-07-11 天津药物研究院 4-取代间甲磺酰胺苯胺基-喹唑啉衍生物及其制备方法和用途
EP2468883A1 (de) 2010-12-22 2012-06-27 Pangaea Biotech S.L. Molekulare Biomarker zur Vorhersage der Reaktion auf Tyrosinkinaseinhibitoren bei Lungenkrebs
US8952154B2 (en) 2010-12-23 2015-02-10 Apotex Pharmachem Inc. Process for the preparation of lapatinib and its ditosylate salt
US9134297B2 (en) 2011-01-11 2015-09-15 Icahn School Of Medicine At Mount Sinai Method and compositions for treating cancer and related methods
WO2012098387A1 (en) 2011-01-18 2012-07-26 Centro Nacional De Investigaciones Oncológicas (Cnio) 6, 7-ring-fused triazolo [4, 3 - b] pyridazine derivatives as pim inhibitors
UY33883A (es) 2011-01-31 2012-08-31 Novartis Ag Novedosos derivados heterocíclicos
US20120214830A1 (en) 2011-02-22 2012-08-23 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors in hepatocellular carcinoma
EP2492688A1 (de) 2011-02-23 2012-08-29 Pangaea Biotech, S.A. Molekulare Biomarker zur Vorhersage der Reaktion auf die Antitumorbehandlung bei Lungenkrebs
EP2680850B1 (de) 2011-03-04 2018-05-23 Newgen Therapeutics, Inc. Alkynsubstituierte chinazolinverbindung und verfahren zu ihrer verwendung
KR101940340B1 (ko) 2011-03-04 2019-01-18 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 키나제 억제제로서의 아미노-퀴놀린
DK2683643T3 (da) 2011-03-09 2019-08-12 Richard G Pestell Prostatacancercellelinjer, gensignaturer og anvendelser deraf
US9295676B2 (en) 2011-03-17 2016-03-29 The Trustees Of The University Of Pennsylvania Mutation mimicking compounds that bind to the kinase domain of EGFR
WO2012125913A1 (en) 2011-03-17 2012-09-20 The Trustees Of The University Of Pennsylvania Methods and use of bifunctional enzyme-building clamp-shaped molecules
WO2012129145A1 (en) 2011-03-18 2012-09-27 OSI Pharmaceuticals, LLC Nscle combination therapy
DK2937349T3 (en) 2011-03-23 2017-02-20 Amgen Inc CONDENSED TRICYCLIC DUAL INHIBITORS OF CDK 4/6 AND FLT3
CA2844699C (en) 2011-04-01 2019-05-07 Genentech, Inc. Combinations of akt inhibitor compounds and abiraterone, and methods of use
WO2012142164A1 (en) 2011-04-12 2012-10-18 The United States Of America, As Represented By The Secretary, Department Of Health & Human Services Human monoclonal antibodies that bind insulin-like growth factor (igf) i and ii
AU2012246490B2 (en) 2011-04-18 2016-08-04 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
ES2724801T3 (es) 2011-04-19 2019-09-16 Pfizer Combinaciones de anticuerpos anti-4-1BB y anticuerpos inductores de ADCC para el tratamiento del cáncer
US9896730B2 (en) 2011-04-25 2018-02-20 OSI Pharmaceuticals, LLC Use of EMT gene signatures in cancer drug discovery, diagnostics, and treatment
CN102918029B (zh) 2011-05-17 2015-06-17 江苏康缘药业股份有限公司 4-苯胺-6-丁烯酰胺-7-烷醚喹唑啉衍生物及其制备方法和用途
HRP20220319T1 (hr) 2011-05-19 2022-05-13 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Makrociklički spojevi kao inhibitori protein kinaze
EP2524918A1 (de) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazinderivate als Kinase Inhibitoren
ITMI20110894A1 (it) 2011-05-20 2012-11-21 Italiana Sint Spa Impurezza del lapatinib e suoi sali
JP5414739B2 (ja) 2011-05-25 2014-02-12 三菱電機株式会社 半導体テスト治具
WO2012166899A2 (en) 2011-06-03 2012-12-06 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
WO2013005041A1 (en) 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) Tricyclic heterocyclic compounds as kinase inhibitors
WO2013005057A1 (en) 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) New compounds
WO2013004984A1 (en) 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncologicas (Cnio) Tricyclic compounds for use as kinase inhibitors
DK3409278T3 (da) 2011-07-21 2020-11-09 Sumitomo Dainippon Pharma Oncology Inc Heterocykliske proteinkinaseinhibitorer
US9499530B2 (en) * 2011-08-01 2016-11-22 Hangzhou Minsheng Institutes For Pharma Research Quinazoline derivative, composition having the derivative, and use of the derivative in preparing medicament
US9745288B2 (en) 2011-08-16 2017-08-29 Indiana University Research And Technology Corporation Compounds and methods for treating cancer by inhibiting the urokinase receptor
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
WO2013033380A1 (en) 2011-08-31 2013-03-07 Genentech, Inc. Diagnostic markers
AU2012311184A1 (en) 2011-09-22 2014-03-06 Pfizer Inc. Pyrrolopyrimidine and purine derivatives
US20130084287A1 (en) 2011-09-30 2013-04-04 Genentech, Inc. Diagnostic markers
ES2654160T3 (es) 2011-10-04 2018-02-12 Igem Therapeutics Limited Anticuerpos de IgE anti-HMW-MAA
JP6059731B2 (ja) 2011-10-28 2017-01-11 ノバルティス アーゲー 新規プリン誘導体および疾患の処置におけるその使用
BR112014011115A2 (pt) 2011-11-08 2017-06-13 Pfizer métodos para tratamento de distúrbios inflamatórios usando anticorpos anti-m-csf
WO2013080218A1 (en) 2011-11-28 2013-06-06 Fresenius Kabi Oncology Ltd. Novel intermediates and process for the preparation of lapatinib and its pharmaceutically acceptable salts
BR112014019034A8 (pt) 2012-01-31 2017-07-11 Smithkline Beecham Cork Ltd Método para tratamento de câncer
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
CN104245701A (zh) 2012-04-03 2014-12-24 诺华有限公司 有酪氨酸激酶抑制剂的组合产品和其应用
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
CN104853806A (zh) 2012-05-14 2015-08-19 理查德·G·佩斯泰尔 使用ccr5调节剂治疗癌症
SG11201406550QA (en) 2012-05-16 2014-11-27 Novartis Ag Dosage regimen for a pi-3 kinase inhibitor
WO2013190089A1 (en) 2012-06-21 2013-12-27 Pangaea Biotech, S.L. Molecular biomarkers for predicting outcome in lung cancer
EP2890696A1 (de) 2012-08-29 2015-07-08 Amgen, Inc. Quinazolinonverbindungen und derivate davon
AR092529A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de aminoquinazolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
ES2644758T3 (es) 2012-10-16 2017-11-30 Tolero Pharmaceuticals, Inc. Moduladores de PKM2 y métodos para su uso
CZ2012712A3 (cs) 2012-10-17 2014-04-30 Zentiva, K.S. Nový způsob výroby klíčového intermediátu výroby lapatinibu
CN102942561A (zh) * 2012-11-06 2013-02-27 深圳海王药业有限公司 4-氨基喹唑啉杂环化合物及其用途
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
MX2015004979A (es) 2012-12-21 2015-07-17 Eisai R&D Man Co Ltd Forma amorfa de derivado de quinolina y metodo para su produccion.
CN103896889B (zh) * 2012-12-27 2016-05-25 上海创诺制药有限公司 拉帕替尼中间体及其制备方法和应用
WO2014127214A1 (en) 2013-02-15 2014-08-21 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
ES2635620T3 (es) 2013-02-19 2017-10-04 Hexal Ag Composición farmacéutica que comprende n-[3-cloro-4-(3-fluorobenciloxi)fenil]-6-[5({[2-(metilsulfonil)etil]amino} metil)-2-furil]quinazolin-4-amina o una sal, solvato o sal solvatada farmacéuticamente aceptables de la misma
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
EP2958895B1 (de) 2013-02-20 2020-08-19 Kala Pharmaceuticals, Inc. Therapeutische verbindungen und verwendungen davon
KR20150118152A (ko) 2013-02-21 2015-10-21 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 키나제 억제제로서의 퀴나졸린
CA2900097A1 (en) 2013-02-22 2014-08-28 F. Hoffmann-La Roche Ag Methods of treating cancer and preventing drug resistance
AU2014223548A1 (en) 2013-02-26 2015-10-15 Triact Therapeutics, Inc. Cancer therapy
CN103159747A (zh) * 2013-02-26 2013-06-19 常州鸿创高分子科技有限公司 一种二对甲苯磺酸拉帕替尼的合成方法
US9468681B2 (en) 2013-03-01 2016-10-18 California Institute Of Technology Targeted nanoparticles
CA2902263A1 (en) 2013-03-06 2014-09-12 Genentech, Inc. Methods of treating and preventing cancer drug resistance
JP6433974B2 (ja) 2013-03-14 2018-12-05 トレロ ファーマシューティカルズ， インコーポレイテッド Ｊａｋ２およびａｌｋ２阻害剤およびその使用方法
EP2968565A2 (de) 2013-03-14 2016-01-20 Genentech, Inc. Verfahren zur behandlung von krebs und prävention einer antikrebsmittelresistenz
CA2905123A1 (en) 2013-03-15 2014-09-18 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
US20160051556A1 (en) 2013-03-21 2016-02-25 INSERM (Institut National de la Santé et de la Recherche Médicale) Method and Pharmaceutical Composition for use in the Treatment of Chronic Liver Diseases Associated with a Low Hepcidin Expression
WO2014170910A1 (en) 2013-04-04 2014-10-23 Natco Pharma Limited Process for the preparation of lapatinib
US9206188B2 (en) 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
RU2658601C2 (ru) 2013-05-14 2018-06-21 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Биомаркер для прогнозирования и оценки чувствительности субъектов с раком эндометрия к соединениям ленватиниба
HU231012B1 (hu) 2013-05-24 2019-11-28 Egis Gyógyszergyár Nyilvánosan Működő Részvénytársaság Lapatinib sók
EP3022186B1 (de) * 2013-07-18 2020-02-26 Shanghai Fochon Pharmaceutical Co. Ltd Chinazolinderivate, zusammensetzungen davon und verwendung als arzneimittel
EP3044593A4 (de) 2013-09-09 2017-05-17 Triact Therapeutics, Inc. Krebstherapie
WO2015051302A1 (en) 2013-10-04 2015-04-09 Aptose Biosciences Inc. Compositions and methods for treating cancers
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
CN106061261B (zh) 2013-11-01 2018-04-24 卡拉制药公司 治疗化合物的结晶形式及其用途
CN103554091B (zh) * 2013-11-05 2016-05-18 沈阳工业大学 喹唑啉衍生物及其制备方法和用途
UA115388C2 (uk) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
EP3076969B1 (de) 2013-12-06 2021-09-01 Novartis AG Dosierungsschema für einen alpha-isoform-selektiven phosphatidylinositol-3-kinase-hemmer
US9242965B2 (en) 2013-12-31 2016-01-26 Boehringer Ingelheim International Gmbh Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors
EP3636648A1 (de) 2014-01-24 2020-04-15 Turning Point Therapeutics, Inc. Diaryl-makrocyclen als modulatoren von proteinkinasen
EP3111222A1 (de) 2014-02-26 2017-01-04 Glaxosmithkline Intellectual Property (No. 2) Limited Verfahren zur behandlung von krebspatienten mit reaktion auf ezh2-inhibitor gsk126
BR112016021383A2 (pt) 2014-03-24 2017-10-03 Genentech Inc Método para identificar um paciente com câncer que é susceptível ou menos susceptível a responder ao tratamento com um antagonista de cmet, método para identificar um paciente apresentando câncer previamente tratado, método para determinar a expressão do biomarcador hgf, antagonista anti-c-met e seu uso, kit de diagnóstico e seu método de preparo
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
WO2015155624A1 (en) 2014-04-10 2015-10-15 Pfizer Inc. Dihydropyrrolopyrimidine derivatives
EP2937346A1 (de) 2014-04-24 2015-10-28 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Co-Kristalle von Lapatinib
US20170050958A1 (en) 2014-04-30 2017-02-23 Pfizer Inc. Cycloalkyl-Linked Diheterocycle Derivatives
US9388239B2 (en) 2014-05-01 2016-07-12 Consejo Nacional De Investigation Cientifica Anti-human VEGF antibodies with unusually strong binding affinity to human VEGF-A and cross reactivity to human VEGF-B
WO2016001789A1 (en) 2014-06-30 2016-01-07 Pfizer Inc. Pyrimidine derivatives as pi3k inhibitors for use in the treatment of cancer
US10934360B2 (en) 2014-07-31 2021-03-02 The Hong Kong University Of Science And Technology Human monoclonal antibodies against EPHA4 and their use
EP4089076A1 (de) 2014-08-28 2022-11-16 Eisai R&D Management Co., Ltd. Hochreines chinolinderivat und verfahren zum herstellen davon
WO2016059600A1 (en) 2014-10-17 2016-04-21 Novartis Ag Combination of ceritinib with an egfr inhibitor
CA2969974C (en) 2014-12-15 2020-08-04 The Regents Of The University Of Michigan Small molecule inhibitors of egfr and pi3k
EP3233829B1 (de) 2014-12-18 2019-08-14 Pfizer Inc Pyrimidin und triazinderivate und deren verwendung als axl-inhibitoren
RU2739942C2 (ru) 2014-12-24 2020-12-30 Дженентек, Инк. Терапевтические, диагностические и прогностические способы для рака мочевого пузыря
CN105801565B (zh) * 2014-12-30 2020-04-03 天津法莫西医药科技有限公司 N-[3-氯-4-[(3-氟苯基)甲氧基]苯基]-6-[(5-甲酰基)呋喃-2-基]-4-喹唑啉胺制备方法
AU2016205311B2 (en) 2015-01-08 2022-02-17 The Board Of Trustees Of The Leland Stanford Junior University Factors and cells that provide for induction of bone, bone marrow, and cartilage
MA41414A (fr) 2015-01-28 2017-12-05 Centre Nat Rech Scient Protéines de liaison agonistes d' icos
CA2974442A1 (en) * 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Novel fluorinated derivatives as egfr inhibitors useful for treating cancers
RS65049B1 (sr) 2015-02-25 2024-02-29 Eisai R&D Man Co Ltd Metoda za suzbijanje gorčine derivata kinolina
CA2978226A1 (en) 2015-03-04 2016-09-09 Merck Sharpe & Dohme Corp. Combination of a pd-1 antagonist and a vegfr/fgfr/ret tyrosine kinase inhibitor for treating cancer
JP6851978B2 (ja) 2015-04-20 2021-03-31 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド ミトコンドリアプロファイリングによるアルボシジブ応答の予測
US10011629B2 (en) 2015-05-01 2018-07-03 Cocrystal Pharma, Inc. Nucleoside analogs for treatment of the flaviviridae family of viruses and cancer
CN111349118B (zh) 2015-05-18 2023-08-22 住友制药肿瘤公司 具有增加的生物利用度的阿伏西地前药
CN106279307B (zh) * 2015-05-19 2019-07-26 正大天晴药业集团股份有限公司 芳氨代葡萄糖衍生物、其制备方法及抗肿瘤用途
ES2886107T3 (es) 2015-06-16 2021-12-16 Prism Biolab Co Ltd Antineoplásico
ES2882255T3 (es) 2015-07-01 2021-12-01 California Inst Of Techn Sistemas de administración basados en polímeros de ácido múcico catiónicos
EP3317285B1 (de) 2015-07-02 2021-01-27 Turning Point Therapeutics, Inc. Chirale diaryl-makrocyclen als modulatoren von proteinkinasen
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
JP6817287B2 (ja) 2015-07-21 2021-01-20 ターニング・ポイント・セラピューティクス・インコーポレイテッドＴｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． キラルジアリール大環状分子及びその使用
AU2016301315C1 (en) 2015-08-03 2022-07-07 Sumitomo Pharma Oncology, Inc. Combination therapies for treatment of cancer
WO2017025871A1 (en) 2015-08-07 2017-02-16 Glaxosmithkline Intellectual Property Development Limited Combination therapy comprising anti ctla-4 antibodies
WO2017040982A1 (en) * 2015-09-02 2017-03-09 The Regents Of The University Of California Her3 ligands and uses thereof
CN106632276B (zh) * 2015-10-28 2021-06-15 上海天慈生物谷生物工程有限公司 一种治疗乳腺癌药物的制备方法
WO2017077445A1 (en) 2015-11-02 2017-05-11 Novartis Ag Dosage regimen for a phosphatidylinositol 3-kinase inhibitor
WO2017093942A1 (en) 2015-12-01 2017-06-08 Glaxosmithkline Intellectual Property Development Limited Combination treatments and uses and methods thereof
CN108601752A (zh) 2015-12-03 2018-09-28 安吉奥斯医药品有限公司 用于治疗mtap缺失型癌症的mat2a抑制剂
WO2017157825A1 (en) 2016-03-15 2017-09-21 F. Hoffmann-La Roche Ag Combinations of lsd1 inhibitors for use in the treatment of solid tumors
KR20190034225A (ko) 2016-07-28 2019-04-01 티피 테라퓨틱스, 인크. 거대환 키나제 억제제
WO2018025221A1 (en) 2016-08-04 2018-02-08 Glaxosmithkline Intellectual Property Development Limited Anti-icos and anti-pd-1 antibody combination therapy
WO2018048747A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3509423A4 (de) 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. Kristalline formen von therapeutischen verbindungen und verwendungen davon
MX2019002629A (es) 2016-09-08 2019-10-07 Kala Pharmaceuticals Inc Formas cristalinas de compuestos terapéuticos y usos de los mismos.
WO2018060833A1 (en) 2016-09-27 2018-04-05 Novartis Ag Dosage regimen for alpha-isoform selective phosphatidylinositol 3-kinase inhibitor alpelisib
WO2018094275A1 (en) 2016-11-18 2018-05-24 Tolero Pharmaceuticals, Inc. Alvocidib prodrugs and their use as protein kinase inhibitors
KR20190099260A (ko) 2016-12-19 2019-08-26 톨레로 파마수티컬스, 인크. 프로파일링 펩티드 및 감도 프로파일링을 위한 방법
CR20190338A (es) 2016-12-22 2019-09-09 Amgen Inc Inhibidores de kras g12c y métodos para su uso
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
PE20200700A1 (es) * 2017-07-28 2020-06-23 Turning Point Therapeutics Inc Compuestos macrociclicos y usos de los mismos
SG11202001499WA (en) 2017-09-08 2020-03-30 Amgen Inc Inhibitors of kras g12c and methods of using the same
JP7196160B2 (ja) 2017-09-12 2022-12-26 スミトモ ファーマ オンコロジー， インコーポレイテッド Ｍｃｌ－１阻害剤アルボシジブを用いた、ｂｃｌ－２阻害剤に対して非感受性である癌の治療レジメン
WO2019075367A1 (en) 2017-10-13 2019-04-18 Tolero Pharmaceuticals, Inc. PKM2 ACTIVATORS IN COMBINATION WITH OXYGEN REACTIVE SPECIES FOR THE TREATMENT OF CANCER
WO2019126136A2 (en) 2017-12-18 2019-06-27 Sterngreene, Inc. Pyrimidine compounds useful as tyrosine kinase inhibitors
PL3728271T3 (pl) 2017-12-19 2023-01-23 Turning Point Therapeutics, Inc. Związki makrocykliczne do leczenia chorób
WO2019213526A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11090304B2 (en) 2018-05-04 2021-08-17 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2020011907A (es) 2018-05-10 2021-01-29 Amgen Inc Inhibidores de kras g12c para el tratamiento de cancer.
WO2019232419A1 (en) 2018-06-01 2019-12-05 Amgen Inc. Kras g12c inhibitors and methods of using the same
EP4268898A3 (de) 2018-06-11 2024-01-17 Amgen Inc. Kras-g12c-inhibitoren zur behandlung von krebs
EP3807276A2 (de) 2018-06-12 2021-04-21 Amgen Inc. Einen piperazinring umfassende kras g12c-inhibitoren und ihre verwendung zur krebsbehandlung
JP7200453B2 (ja) * 2018-06-27 2023-01-10 オスコテック インコーポレイテッド Ａｘｌ阻害剤として使用するためのピリドピリミジノン誘導体
EP3826684A4 (de) 2018-07-26 2022-04-06 Sumitomo Dainippon Pharma Oncology, Inc. Verfahren zur behandlung von mit abnormaler acvr1 -expression verbundenen krankheiten und acvr1 -inhibitoren zur verwendung in demselben
BR112021006407A8 (pt) 2018-10-04 2022-12-06 Inst Nat Sante Rech Med uso de inibidores do egfr para ceratodermas
JP2020090482A (ja) 2018-11-16 2020-06-11 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
EP3883565A1 (de) 2018-11-19 2021-09-29 Amgen Inc. Kras-g12c-inhibitoren und verfahren zu deren verwendung
JP2022511029A (ja) 2018-12-04 2022-01-28 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド がんの処置のための薬剤としての使用のためのｃｄｋ９インヒビターおよびその多形
EP3898626A1 (de) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituierte pyrazolo[1,5-a]pyridin-verbindungen als inhibitoren von fgfr-tyrosinkinasen
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020132649A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
JOP20210154B1 (ar) 2018-12-20 2023-09-17 Amgen Inc مثبطات kif18a
MA54550A (fr) 2018-12-20 2022-03-30 Amgen Inc Inhibiteurs de kif18a
JP2022513971A (ja) 2018-12-20 2022-02-09 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤として有用なヘテロアリールアミド
CN113795512A (zh) 2019-02-01 2021-12-14 葛兰素史克知识产权开发有限公司 包含贝兰他单抗莫福汀和抗ox4抗体的癌症组合治疗及其用途和方法
US11471456B2 (en) 2019-02-12 2022-10-18 Sumitomo Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors
WO2020180770A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
US20230148450A9 (en) 2019-03-01 2023-05-11 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
US11793802B2 (en) 2019-03-20 2023-10-24 Sumitomo Pharma Oncology, Inc. Treatment of acute myeloid leukemia (AML) with venetoclax failure
CA3133460A1 (en) 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
EP3738593A1 (de) 2019-05-14 2020-11-18 Amgen, Inc Dosierung von kras-inhibitor zur behandlung von krebserkrankungen
AU2020280024A1 (en) 2019-05-21 2021-12-09 Amgen Inc. Solid state forms
US20230295313A1 (en) 2019-06-26 2023-09-21 Glaxosmithkline Intellectual Property Development Limited Il1rap binding proteins
AU2020324406A1 (en) 2019-08-02 2022-03-17 Amgen Inc. KIF18A inhibitors
CN114269731A (zh) 2019-08-02 2022-04-01 美国安进公司 Kif18a抑制剂
JP2022542392A (ja) 2019-08-02 2022-10-03 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤としてのピリジン誘導体
EP4007752A1 (de) 2019-08-02 2022-06-08 Amgen Inc. Kif18a-inhibitoren
WO2021046293A1 (en) 2019-09-06 2021-03-11 Glaxosmithkline Intellectual Property Development Limited Dosing regimen for the treatment of cancer with an anti icos agonistic antibody and tremelimumab
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
CA3155857A1 (en) 2019-10-24 2021-04-29 Amgen Inc. PYRIDOPYRIMIDINE DERIVATIVES USEFUL AS KRAS G12C AND KRAS G12D INHIBITORS IN THE TREATMENT OF CANCER
EP4055028A1 (de) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras-inhibitoren
EP4054720A1 (de) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras-inhibitoren
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ｒａｓ抑制劑
PE20230249A1 (es) 2019-11-08 2023-02-07 Revolution Medicines Inc Compuestos de heteroarilo biciclicos y usos de estos
AR120456A1 (es) 2019-11-14 2022-02-16 Amgen Inc Síntesis mejorada del compuesto inhibidor de g12c de kras
WO2021097212A1 (en) 2019-11-14 2021-05-20 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
EP4065231A1 (de) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Kovalente ras-inhibitoren und verwendungen davon
CN114929279A (zh) 2020-01-07 2022-08-19 锐新医药公司 Shp2抑制剂给药和治疗癌症的方法
US20230067202A1 (en) 2020-01-28 2023-03-02 Glaxosmithkline Intellectual Property Development Limited Combination Treatments and Uses and Methods Thereof
WO2021155006A1 (en) 2020-01-31 2021-08-05 Les Laboratoires Servier Sas Inhibitors of cyclin-dependent kinases and uses thereof
BR112022017425A2 (pt) * 2020-03-02 2022-11-29 Turning Point Therapeutics Inc Usos terapêuticos de compostos macrocíclicos
CA3183032A1 (en) 2020-06-18 2021-12-23 Mallika Singh Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
AU2021344830A1 (en) 2020-09-03 2023-04-06 Revolution Medicines, Inc. Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
EP4214209A1 (de) 2020-09-15 2023-07-26 Revolution Medicines, Inc. Indolderivate als ras-inhibitoren bei der behandlung von krebs
CA3203111A1 (en) 2020-12-22 2022-06-30 Kailiang Wang Sos1 inhibitors and uses thereof
EP4267554A1 (de) 2020-12-22 2023-11-01 Mekanistic Therapeutics LLC Substituierte aminobenzylheteroarylverbindungen als egfr- und/oder pi3k-hemmer
IL308193A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors
PE20240089A1 (es) 2021-05-05 2024-01-16 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cancer
EP4334324A1 (de) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Kovalente ras-inhibitoren und verwendungen davon
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4227307A1 (de) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazinverbindungen als shp2-inhibitoren
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024081916A1 (en) 2022-10-14 2024-04-18 Black Diamond Therapeutics, Inc. Methods of treating cancers using isoquinoline or 6-aza-quinoline derivatives

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4074057A (en) 1973-12-12 1978-02-14 Takeda Chemical Co., Ltd. 2-Halopropionic acid and its derivatives
US4166735A (en) 1977-01-21 1979-09-04 Shell Oil Company Cycloalkanecarboxanilide derivative herbicides
WO1986006718A1 (en) 1985-05-17 1986-11-20 The Australian National University Antimalarial compounds
US5141941A (en) 1988-11-21 1992-08-25 Ube Industries, Ltd. Aralkylamine derivatives, and fungicides containing the same
US5034393A (en) 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
CA2039411A1 (en) 1990-03-30 1991-10-01 Ronnie Gerald Edie Thienopyrimidine derivatives
US5480883A (en) 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
DE4131924A1 (de) 1991-09-25 1993-07-08 Hoechst Ag Substituierte 4-alkoxypyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel
GB9127252D0 (en) 1991-12-23 1992-02-19 Boots Co Plc Therapeutic agents
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
WO1993017682A1 (en) 1992-03-04 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
WO1993018035A1 (en) 1992-03-04 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
US5326766A (en) 1992-08-19 1994-07-05 Dreikorn Barry A 4-(2-(4-(2-pyridinyloxy)phenyl)ethoxy)quinazoline and analogues thereof
DE4308014A1 (de) 1993-03-13 1994-09-15 Hoechst Schering Agrevo Gmbh Kondensierte Stickstoffheterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel und Fungizide
GB9312891D0 (en) 1993-06-22 1993-08-04 Boots Co Plc Therapeutic agents
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5679683A (en) 1994-01-25 1997-10-21 Warner-Lambert Company Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
GB9510757D0 (en) 1994-09-19 1995-07-19 Wellcome Found Therapeuticaly active compounds
TW321649B (de) * 1994-11-12 1997-12-01 Zeneca Ltd
GB9424233D0 (en) 1994-11-30 1995-01-18 Zeneca Ltd Quinazoline derivatives
WO1996040142A1 (en) 1995-06-07 1996-12-19 Pfizer Inc. Heterocyclic ring-fused pyrimidine derivatives
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
AU7292096A (en) 1995-11-14 1997-06-05 Pharmacia & Upjohn S.P.A. Aryl and heteroaryl purine compounds
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
WO1998002434A1 (en) 1996-07-13 1998-01-22 Glaxo Group Limited Fused heterocyclic compounds as protein tyrosine kinase inhibitors
HRP970371A2 (en) * 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
CN1230185A (zh) 1996-07-13 1999-09-29 葛兰素集团有限公司 双环芳杂环化合物用作蛋白质酪氨酸激酶的抑制剂
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
EA005525B1 (ru) * 2000-06-22 2005-04-28 Пфайзер Продактс Инк. Замещенные бициклические производные для лечения аномального роста клеток
HU229624B1 (en) * 2000-06-30 2014-03-28 Glaxo Group Ltd Quinazoline ditosylate salt compounds
ES2236481T3 (es) * 2001-01-16 2005-07-16 Glaxo Group Limited Combinacion farmaceutica que contiene una 4-quinazolinamina y paclitaxel, carboplatino o vinorelbina para el tratamiento de cancer.
BR0307151A (pt) * 2002-02-01 2004-12-07 Astrazeneca Ab Composto ou um sal do mesmo, processo para a preparação do mesmo, composição farmacêutica, uso do composto ou de um seu sal, método para produzir um efeito antiangiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente, como um ser humano, que necessita de um tratamento do tipo referido, e, processos para a preparação de 5-bromo-7- azaindol, e para a produção de 5-metóxi-7-azaindol
US7488823B2 (en) * 2003-11-10 2009-02-10 Array Biopharma, Inc. Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors

Also Published As

Publication number Publication date
KR20010015902A (ko) 2001-02-26
US20070238875A1 (en) 2007-10-11
EP1460072B1 (de) 2006-04-05
IS5549A (is) 2000-06-27
EA200000637A1 (ru) 2001-02-26
PL192746B1 (pl) 2006-12-29
BG64825B1 (bg) 2006-05-31
DE69930773D1 (de) 2006-05-18
EP1047694B1 (de) 2004-07-07
NL300360I2 (nl) 2009-02-02
US7109333B2 (en) 2006-09-19
FR08C0038I1 (de) 2008-11-14
AR066982A2 (es) 2009-09-23
ES2319119T3 (es) 2009-05-04
NO20003561L (no) 2000-09-11
OA11444A (en) 2004-04-29
PE20000230A1 (es) 2000-04-03
ATE417847T1 (de) 2009-01-15
HUP0100941A2 (hu) 2001-09-28
CY1108859T1 (el) 2014-07-02
DE69918528D1 (de) 2004-08-12
LU91475I9 (de) 2019-01-02
US20150065527A1 (en) 2015-03-05
SI1047694T1 (en) 2005-02-28
IS2276B (is) 2007-09-15
DE122008000048I1 (de) 2009-01-02
HRP20060387A2 (en) 2008-02-29
AU749549B2 (en) 2002-06-27
TW477788B (en) 2002-03-01
MY124055A (en) 2006-06-30
LU91475I2 (fr) 2008-11-10
SI1460072T1 (sl) 2006-08-31
WO1999035146A1 (en) 1999-07-15
DK1460072T3 (da) 2006-07-31
HUP0100941A3 (en) 2002-09-30
IL137041A (en) 2006-10-05
DK1454907T3 (da) 2009-03-09
HRP20000469A2 (en) 2001-06-30
CY1105618T1 (el) 2010-12-22
NO316176B1 (no) 2003-12-22
NZ505456A (en) 2003-06-30
ZA99172B (en) 2000-07-11
ATE322491T1 (de) 2006-04-15
JP2002326990A (ja) 2002-11-15
IL137041A0 (en) 2001-06-14
ME00757B (me) 2008-06-05
US20070015775A1 (en) 2007-01-18
BG104668A (en) 2001-04-30
EP1454907B1 (de) 2008-12-17
CY2008015I2 (el) 2009-11-04
PT1460072E (pt) 2006-07-31
CN1292788A (zh) 2001-04-25
HRP20000469B1 (en) 2007-05-31
US20020147205A1 (en) 2002-10-10
US20160051551A1 (en) 2016-02-25
EE04616B1 (et) 2006-04-17
US8912205B2 (en) 2014-12-16
SI1454907T1 (sl) 2009-04-30
JP2002500225A (ja) 2002-01-08
PL341595A1 (en) 2001-04-23
US8513262B2 (en) 2013-08-20
UA66827C2 (uk) 2004-06-15
PT1454907E (pt) 2009-02-18
BR9906904A (pt) 2000-10-17
US20130310562A1 (en) 2013-11-21
EG24743A (en) 2010-07-14
DE69940128D1 (de) 2009-01-29
CN1134438C (zh) 2004-01-14
CO4820390A1 (es) 1999-07-28
GEP20022678B (en) 2002-04-25
US20100120804A1 (en) 2010-05-13
AP1446A (en) 2005-07-19
CZ20002587A3 (en) 2001-05-16
US20030176451A1 (en) 2003-09-18
DE69918528T2 (de) 2005-07-28
EE200000411A (et) 2001-12-17
HU227593B1 (en) 2011-09-28
ES2262087T3 (es) 2006-11-16
EP1454907A1 (de) 2004-09-08
MA26596A1 (fr) 2004-12-20
ES2221354T3 (es) 2004-12-16
KR100569776B1 (ko) 2006-04-11
PT1047694E (pt) 2004-11-30
EP1460072A1 (de) 2004-09-22
JP3390741B2 (ja) 2003-03-31
GB9800569D0 (en) 1998-03-11
SK285405B6 (sk) 2007-01-04
FR08C0038I2 (fr) 2012-02-22
AR015507A1 (es) 2001-05-02
US6727256B1 (en) 2004-04-27
US20050130996A1 (en) 2005-06-16
DK1047694T3 (da) 2004-11-08
US20160339027A1 (en) 2016-11-24
NL300360I1 (nl) 2008-11-03
SK10502000A3 (sk) 2001-08-06
NO2008017I1 (no) 2008-12-01
US6713485B2 (en) 2004-03-30
CZ298047B6 (cs) 2007-06-06
EP1047694A1 (de) 2000-11-02
NO2008017I2 (de) 2011-10-17
RS49779B (sr) 2008-06-05
DE69930773T2 (de) 2006-09-28
AU2010276460A1 (en) 2011-02-17
CA2317589A1 (en) 1999-07-15
BR9906904B1 (pt) 2011-05-03
AU749549C (en) 2003-03-20
NO20003561D0 (no) 2000-07-11
AP2000001861A0 (en) 2000-09-30
CA2317589C (en) 2007-08-07
TR200002015T2 (tr) 2001-01-22
AU2278399A (en) 1999-07-26
HK1031883A1 (en) 2001-06-29
US9199973B2 (en) 2015-12-01
CY2008015I1 (el) 2009-11-04
EA002455B1 (ru) 2002-04-25
YU44800A (sh) 2002-11-15

Similar Documents

Publication Publication Date Title
ATE270670T1 (de) Bicyclische heteroaromatische verbindungen als protein tyrosine kinase inhibitoren
ATE231148T1 (de) Bicyclische heteroaromatische verbindungen als protein tyrosine kinase inhibitoren
ATE249458T1 (de) Bicyclische heteroaromatic verbindungen als protein tyrosin kinase inhibitoren
ATE255575T1 (de) Substituierte 3-cyanochinoline als protein tyrosine kinase inhibitoren
ATE227283T1 (de) Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
CY2014034I2 (el) Υποκατεστημενες 3-κυανοκινολινες ως αναστολεις κινασων πρωτεϊνης τυροσινης
ATE349447T1 (de) Alkylamino-substituierte bicyclische heterocyclen als p38 protein kinase inhibitoren
ATE430149T1 (de) Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren
ATE257157T1 (de) Pyrrolo(2,3-d)pyrimidin-verbindungen als protein kinasen hemmer
DE60128709D1 (de) Triazol-verbindungen als protein-kinase-inhibitoren
DE60120219D1 (de) Pyrazolverbindungen als protein-kinase-inhibitoren
CY2013005I1 (el) Κυκλικοι αναστολεις κινασης τυροσινης πρωτεϊνων
ATE205836T1 (de) Bicyclische 4-aralkylaminopyrimidin-derivate als tyrosinkinase-inhibitoren
ATE387448T1 (de) 4,5-pyrazinoxindole als proteinkinasehemmer