RS49779B - Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze - Google Patents

Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze

Info

Publication number
RS49779B
RS49779B YUP-448/00A YU44800A RS49779B RS 49779 B RS49779 B RS 49779B YU 44800 A YU44800 A YU 44800A RS 49779 B RS49779 B RS 49779B
Authority
RS
Serbia
Prior art keywords
halo
byciclic
tyrosine kinase
kinase inhibitors
protein tyrosine
Prior art date
Application number
YUP-448/00A
Other languages
English (en)
Inventor
Malcolm Cl ive Carter
George Stuart Cockerill
Stephen Barry Guntrip
Karen Elizabeth Lackey
Kathryn Jane Smith
Original Assignee
Glaxo Group Limited,
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=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RS49779(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glaxo Group Limited, filed Critical Glaxo Group Limited,
Publication of YU44800A publication Critical patent/YU44800A/sh
Publication of RS49779B publication Critical patent/RS49779B/sr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D411/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02Heterocyclic 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
    • C07D411/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Abstract

Jedinjenje formule (I) ili njegova so ili solvat; gde Y je CR1 i V je N; ili Y je CR1 i V je CR2; R1 predstavlja grupu CH3S02CH2CH2NHCH2-Ar-, gde Ar se bira između furana i tiazola, od kojih svaki može biti opciono supstituisan sa jednim ili dva halo, C1-4 alkil ili C1-4aloksi grupama; R2 je vodonik ili C1-4 alkoksi; ili R2 je halo; R3 se bira iz grupe koju čine benzil-, halo-, dihalo- i trihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi, halo-, dihalo- i trihalobenziloksi i benzensulfonil ; R4 je halo ili C1-4 alkoksi ili nije prisutan; gde ili (a)R3predstavlja 3-florobenziloksi; i/ili (b) R4 se bira od halo i supstituent je u položaju 3 fenil prstena; i halo predstavlja fluoro, hloro ili bromo. Prijava sadrži još 27 zahteva.
YUP-448/00A 1998-01-12 1998-01-12 Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze RS49779B (sr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9800569.7A GB9800569D0 (en) 1998-01-12 1998-01-12 Heterocyclic compounds

Publications (2)

Publication Number Publication Date
YU44800A YU44800A (sh) 2002-11-15
RS49779B true RS49779B (sr) 2008-06-05

Family

ID=10825153

Family Applications (1)

Application Number Title Priority Date Filing Date
YUP-448/00A RS49779B (sr) 1998-01-12 1998-01-12 Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze

Country Status (48)

Country Link
US (11) US6727256B1 (sr)
EP (3) EP1454907B1 (sr)
JP (2) JP3390741B2 (sr)
KR (1) KR100569776B1 (sr)
CN (1) CN1134438C (sr)
AP (1) AP1446A (sr)
AR (2) AR015507A1 (sr)
AT (3) ATE270670T1 (sr)
AU (2) AU749549C (sr)
BG (1) BG64825B1 (sr)
BR (1) BR9906904B1 (sr)
CA (1) CA2317589C (sr)
CO (1) CO4820390A1 (sr)
CY (3) CY1105618T1 (sr)
CZ (1) CZ298047B6 (sr)
DE (4) DE69918528T2 (sr)
DK (3) DK1454907T3 (sr)
EA (1) EA002455B1 (sr)
EE (1) EE04616B1 (sr)
EG (1) EG24743A (sr)
ES (3) ES2319119T3 (sr)
FR (1) FR08C0038I2 (sr)
GB (1) GB9800569D0 (sr)
GE (1) GEP20022678B (sr)
HK (1) HK1031883A1 (sr)
HR (2) HRP20000469B1 (sr)
HU (1) HU227593B1 (sr)
IL (2) IL137041A0 (sr)
IS (1) IS2276B (sr)
LU (1) LU91475I2 (sr)
MA (1) MA26596A1 (sr)
ME (1) ME00757B (sr)
MY (1) MY124055A (sr)
NL (1) NL300360I2 (sr)
NO (2) NO316176B1 (sr)
NZ (1) NZ505456A (sr)
OA (1) OA11444A (sr)
PE (1) PE20000230A1 (sr)
PL (1) PL192746B1 (sr)
PT (3) PT1454907E (sr)
RS (1) RS49779B (sr)
SI (3) SI1047694T1 (sr)
SK (1) SK285405B6 (sr)
TR (1) TR200002015T2 (sr)
TW (1) TW477788B (sr)
UA (1) UA66827C2 (sr)
WO (1) WO1999035146A1 (sr)
ZA (1) ZA99172B (sr)

Families Citing this family (412)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU8816298A (en) 1997-08-22 1999-03-16 Zeneca Limited Oxindolylquinazoline derivatives as angiogenesis inhibitors
GB9800569D0 (en) * 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
CA2344290C (en) 1998-10-08 2009-06-02 Astrazeneca Ab Quinazoline derivatives
GB2345486A (en) * 1999-01-11 2000-07-12 Glaxo Group Ltd Heteroaromatic protein tyrosine kinase inhibitors
KR100838617B1 (ko) 1999-02-10 2008-06-16 아스트라제네카 아베 혈관형성 억제제로서의 퀴나졸린 유도체
GB9910579D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9910580D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
UA71976C2 (en) 1999-06-21 2005-01-17 Boehringer Ingelheim Pharma Bicyclic heterocycles and a medicament based thereon
ES2295035T3 (es) 1999-07-09 2008-04-16 Glaxo Group Limited Anilinoquinazolinas como inhibidores de proteina tirosina quinasa.
US6933299B1 (en) 1999-07-09 2005-08-23 Smithkline Beecham Corporation Anilinoquinazolines as protein tyrosine kinase inhibitors
RU2002110461A (ru) 1999-09-21 2004-03-10 Астразенека Аб (Se) Производные хиназолина и их применение в качестве фармацевтических веществ
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
AU2001228638A1 (en) * 2000-01-28 2001-08-07 Astrazeneca Ab Chemical compounds
GB0002952D0 (en) * 2000-02-09 2000-03-29 Pharma Mar Sa Process for producing kahalalide F compounds
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
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
AU2001257353A1 (en) 2000-05-02 2001-11-12 Array Biopharma, Inc. Process for the reduction of cyano-substituted sulfones to aminoalkylene-substituted sulfones
HUP0301120A2 (hu) 2000-06-22 2003-08-28 Pfizer Products Inc. Szubsztituált fenilamino-kinazolin-származékok, alkalmazásuk rendellenes sejtnövekedés kezelésére és azokat tartalmazó gyógyszerkészítmények
US6919338B2 (en) 2000-06-28 2005-07-19 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors of aurora-2 kinase
TWI307339B (en) * 2000-06-30 2009-03-11 Glaxo Group Ltd Quinazoline ditosylate salt comprounds
EP1792902A1 (en) * 2000-06-30 2007-06-06 Glaxo Group Limited Processes for preparation of 5-(6-quinazolinyl)-furan-2-carbaldehydes
IL153947A0 (en) 2000-08-09 2003-07-31 Astrazeneca Ab Quinoline derivatives having vegf inhibiting activity
AU2001293817A1 (en) 2000-09-20 2002-04-02 Merck Patent Gmbh 4-amino-quinazolines
NZ525324A (en) 2000-10-20 2005-03-24 Eisai Co Ltd Nitrogenous aromatic ring compounds
US7776315B2 (en) 2000-10-31 2010-08-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and additional active ingredients
US7253184B2 (en) 2000-11-02 2007-08-07 Astrazeneca Ab 4-Substituted quinolines as antitumor agents
EP1337524A1 (en) 2000-11-02 2003-08-27 AstraZeneca AB 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
CA2433800C (en) 2001-01-05 2016-09-13 Pfizer Inc. Antibodies to insulin-like growth factor i receptor
EP1353693B1 (en) * 2001-01-16 2005-03-16 Glaxo Group Limited Pharmaceutical combination containing a 4-quinazolineamine and paclitaxel, carboplatin or vinorelbine for the treatment of cancer
EP1488809A1 (en) 2001-01-16 2004-12-22 Glaxo Group Limited Pharmaceutical combination containing a 4-quinazolineamine and another anti-neoplastic agent for the treatment of cancer
EP1377281A4 (en) * 2001-03-15 2009-06-17 Rhode Island Hospital TAURIN CONNECTIONS
ATE325795T1 (de) * 2001-03-23 2006-06-15 Bayer Corp Rho-kinase inhibitoren
DK1370552T3 (da) * 2001-03-23 2007-05-07 Bayer Pharmaceuticals Corp Rho-kinase-inhibitorer
DE60212487T2 (de) 2001-04-13 2006-12-21 Pfizer Products Inc., Groton Bizyklisch substituierte 4-Aminopyridopyrimidinderivate
WO2002092578A1 (en) * 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2003000194A2 (en) 2001-06-21 2003-01-03 Pfizer Inc. Thienopyridine and thienopyrimidine 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
US20040014755A1 (en) 2002-01-10 2004-01-22 Dhanapalan Nagarathnam Rho-kinase inhibitors
PL371587A1 (en) 2002-01-17 2005-06-27 Neurogen Corporation Substituted quinazolin-4-ylamine analogues as modulators of capsaicin receptors
WO2003062225A1 (en) 2002-01-23 2003-07-31 Bayer Pharmaceuticals Corporation Pyrimidine derivatives as rho-kinase inhibitors
ES2298497T3 (es) 2002-01-23 2008-05-16 Bayer Pharmaceuticals Corporation Inhibidores de quinasa rho.
ES2381781T3 (es) 2002-02-01 2012-05-31 Astrazeneca Ab Compuestos de quinazolina
EP1481971B1 (en) * 2002-02-06 2011-11-16 Ube Industries, Ltd. Process for producing 4-aminoquinazoline compound
US20050176740A1 (en) * 2002-04-08 2005-08-11 Spector Neil L. Cancer treatment method comprising administering an erb-family inhibitor and a raf and/or ras inhibitor
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
EP1510221A4 (en) * 2002-06-03 2009-04-29 Mitsubishi Tanabe Pharma Corp MEANS FOR THE PREVENTION AND / OR TREATMENT OF PERSONS EXPRESSING OR ACTIVATING HER2 AND / OR EGFR
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
GB0215823D0 (en) 2002-07-09 2002-08-14 Astrazeneca Ab Quinazoline derivatives
WO2004004732A1 (en) 2002-07-09 2004-01-15 Astrazeneca Ab Quinazoline derivatives for use in the treatment of cancer
US20040048887A1 (en) * 2002-07-09 2004-03-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and EGFR kinase inhibitors
US7576074B2 (en) 2002-07-15 2009-08-18 Rice Kenneth D Receptor-type kinase modulators and methods of use
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
TWI229650B (en) * 2002-11-19 2005-03-21 Sharp Kk Substrate accommodating tray
AU2003300898A1 (en) * 2002-12-13 2004-07-09 Neurogen Corporation Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators
PL377713A1 (pl) 2002-12-19 2006-02-06 Pfizer Inc. Związki 2-(1H-indazol-6-iloamino)benzamidowe jako inhibitory kinaz białkowych użyteczne w leczeniu chorób oczu
AU2003292435A1 (en) * 2002-12-23 2004-07-14 Astrazeneca Ab 4- (pyridin-4-ylamino) -quinazoline derivatives as anti-tumor agents
WO2004060400A1 (ja) * 2003-01-06 2004-07-22 Mitsubishi Pharma Corp 上皮成長因子受容体を分子標的とする抗精神病薬
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
AP2114A (en) 2003-02-26 2010-03-04 Sugen Inc Aminoheteroaryl compounds as protein kinase inhibitors
KR101126560B1 (ko) 2003-05-30 2012-04-05 도꾜 다이가꾸 약제 반응 예측 방법
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
MEP31408A (en) 2003-07-18 2010-10-10 Abgenix Inc Specific binding agents to hepatocyte growth factor
US20060204966A1 (en) 2003-08-01 2006-09-14 Spector Neil L Treatment of cancers expressing p95 erbb2
ATE412655T1 (de) 2003-08-29 2008-11-15 Pfizer Als neue antiangiogene mittel geeignete thienopyridinphenylacetamide und derivate davon
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
CA2537812C (en) 2003-09-26 2013-01-22 Exelixis, Inc. C-met modulators and method of use
DE10349113A1 (de) 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
WO2005046678A1 (en) * 2003-11-07 2005-05-26 Smithkline Beecham (Cork) Limited Cancer treatment method
CN101337930B (zh) 2003-11-11 2010-09-08 卫材R&D管理有限公司 脲衍生物的制备方法
GB0326459D0 (en) 2003-11-13 2003-12-17 Astrazeneca Ab Quinazoline derivatives
UA83881C2 (en) * 2003-12-18 2008-08-26 Янссен Фармацевтика Н.В. Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents
GB0330002D0 (en) 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
US20070208023A1 (en) * 2004-04-16 2007-09-06 Smithkline Beecham Corporation Cancer Treatment Method
GEP20084551B (en) 2004-05-06 2008-11-25 Warner Lambert Co 4-phenylamino-quinazolin-6-yl-amides
JP2008501690A (ja) * 2004-06-03 2008-01-24 スミスクライン ビーチャム (コーク) リミテッド がんの治療方法
AU2005251735A1 (en) * 2004-06-04 2005-12-22 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
CN1984656B (zh) * 2004-06-04 2010-05-26 史密丝克莱恩比彻姆(科克)有限公司 癌症治疗药物
JP2008504292A (ja) * 2004-06-24 2008-02-14 ノバルティス ヴァクシンズ アンド ダイアグノスティクス, インコーポレイテッド 免疫増強用の化合物
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
DK1786785T3 (da) 2004-08-26 2010-05-31 Pfizer Enantiomerisk rene aminoheteroaryl-forbindelser som proteinkinasehæmmere
AU2005283422C1 (en) 2004-09-17 2017-02-02 Eisai R & D Management Co., Ltd. Medicinal composition
TW200621251A (en) 2004-10-12 2006-07-01 Neurogen Corp Substituted biaryl quinolin-4-ylamine analogues
EP1827434B1 (en) 2004-11-30 2014-01-15 Amgen Inc. Quinolines and quinazoline analogs and their use as medicaments for treating cancer
GB0427131D0 (en) * 2004-12-10 2005-01-12 Glaxosmithkline Biolog Sa Novel combination
ATE501148T1 (de) 2004-12-14 2011-03-15 Astrazeneca Ab Pyrazolopyrimidinverbindungen als antitumormittel
NZ555462A (en) * 2004-12-17 2009-03-31 Smithkline Beecham Cork Ltd Cancer treatment method
EP1828185B1 (en) * 2004-12-21 2009-05-06 SmithKline Beecham Corporation 2-pyrimidinyl pyrazolopyridine erbb kinase inhibitors
US7812022B2 (en) * 2004-12-21 2010-10-12 Glaxosmithkline Llc 2-pyrimidinyl pyrazolopyridine ErbB kinase inhibitors
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
WO2006076646A2 (en) * 2005-01-14 2006-07-20 Neurogen Corporation Heteroaryl substituted quinolin-4-ylamine analogues
KR101976003B1 (ko) 2005-02-18 2019-05-09 아브락시스 바이오사이언스, 엘엘씨 치료제의 조합 및 투여 방식, 및 조합 요법
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
BRPI0609655A2 (pt) 2005-03-31 2010-03-16 Agensys Inc anticorpos e moléculas relacionadas que ligam-se às proteìnas 161p2f10b
SI1871347T1 (sl) 2005-04-19 2016-11-30 Novartis Ag Farmacevtski sestavek
CA2604357C (en) 2005-04-26 2012-01-17 Pfizer Inc. P-cadherin antibodies
EP2281901B1 (en) 2005-08-02 2013-11-27 Eisai R&D Management Co., Ltd. Anti-tumour pharmaceutical composition with angiogenesis inhibitors
UY29783A1 (es) 2005-09-07 2007-04-30 Pfizer Anticuerpos monoclonales humanos para la quinasa-1 tipo receptor de activina
EP1928861B1 (en) 2005-09-20 2010-11-17 AstraZeneca AB 4- (ih-indazol-5-yl-amino)-quinazoline compounds as erbb receptor tyrosine kinase inhibitors for the treatment of cancer
AU2006292278B2 (en) 2005-09-20 2012-03-08 Osi Pharmaceuticals, Inc. 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)
US8404697B2 (en) 2005-11-11 2013-03-26 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
CN101326182B (zh) * 2005-12-05 2011-09-28 史密丝克莱恩比彻姆公司 2-嘧啶基吡唑并吡啶ErbB激酶抑制剂
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)
WO2007088014A1 (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)
AR060358A1 (es) * 2006-04-06 2008-06-11 Novartis Vaccines & Diagnostic Quinazolinas para la inhibicion de pdk 1
US20090203718A1 (en) * 2006-04-13 2009-08-13 Smithkline Beecham (Cork) Ltd. Cancer treatment method
MX2008013430A (es) 2006-04-19 2009-01-26 Novartis Vaccines & Diagnostic Compuestos de indazol y metodos para la inhibición de cdc7.
RS20080525A (en) 2006-05-09 2009-09-08 Pfizer Products Inc., Cycloalkylamino acid derivatives and pharmaceutical compositions thereof
NL2000613C2 (nl) 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
US20090209580A1 (en) 2006-05-18 2009-08-20 Eisai R & D Management Co., Ltd. Antitumor agent for thyroid cancer
EP1862802B1 (en) * 2006-06-01 2008-12-10 Cellzome Ag Methods for the identification of ZAP-70 interacting molecules and for the purification of ZAP-70
JP5399900B2 (ja) 2006-06-30 2014-01-29 メルク・シャープ・アンド・ドーム・コーポレーション Igfbp2インヒビター
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
US20110053964A1 (en) * 2006-08-22 2011-03-03 Roger Tung 4-aminoquinazoline derivatives and methods of use thereof
KR20090042994A (ko) * 2006-08-22 2009-05-04 콘서트 파마슈티컬즈, 인크. 4-아미노퀴나졸린 유도체 및 이의 사용방법
EP2065372B1 (en) 2006-08-28 2012-11-28 Eisai R&D Management Co., Ltd. Antitumor agent for undifferentiated gastric cancer
CA2663599A1 (en) 2006-09-18 2008-03-27 Boehringer Ingelheim International Gmbh Method for treating cancer harboring egfr mutations
EP2079739A2 (en) * 2006-10-04 2009-07-22 Pfizer Products Inc. Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists
EP2073803B1 (en) 2006-10-12 2018-09-19 Astex Therapeutics Limited Pharmaceutical combinations
US8883790B2 (en) 2006-10-12 2014-11-11 Astex Therapeutics Limited Pharmaceutical combinations
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
WO2008079291A2 (en) 2006-12-20 2008-07-03 Amgen Inc. Substituted heterocycles and methods of use
AU2008205252B2 (en) 2007-01-09 2013-02-21 Amgen Inc. Bis-aryl amide derivatives useful for the treatment of cancer
KR101445892B1 (ko) 2007-01-29 2014-09-29 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암 치료용 조성물
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
CA2676173A1 (en) 2007-02-16 2008-08-28 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors
WO2008127710A2 (en) 2007-04-13 2008-10-23 Dana Farber Cancer Institute Methods for treating cancer resistant to erbb therapeutics
KR20090130347A (ko) * 2007-05-09 2009-12-22 화이자 인코포레이티드 치환된 헤테로사이클릭 유도체 및 조성물 및 항균제로서의 이의 약학적 용도
US20110245496A1 (en) * 2007-06-11 2011-10-06 Andrew Simon Craig Quinazoline Salt Compounds
UY31137A1 (es) * 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
WO2009026303A1 (en) 2007-08-21 2009-02-26 Amgen Inc. Human c-fms antigen binding proteins
JP5518711B2 (ja) 2007-09-07 2014-06-11 アジェンシス,インコーポレイテッド 24p4c12タンパク質に結合する抗体および関連分子
US20090215802A1 (en) * 2007-09-13 2009-08-27 Protia, Llc Deuterium-enriched lapatinib
AU2008312400A1 (en) * 2007-10-19 2009-04-23 Albert Einstein College Of Medicine Of Yeshiva University Improved antitumoral treatments
EP2212432A4 (en) 2007-10-22 2011-10-19 Schering Corp COMPLETELY HUMAN ANTI-VEGF ANTIBODIES AND USE PROCEDURES
US8080558B2 (en) 2007-10-29 2011-12-20 Natco Pharma Limited 4-(tetrazol-5-yl)-quinazoline derivatives as anti-cancer agent
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
CA2710122A1 (en) 2007-12-20 2009-07-02 Novartis Ag Thiazole derivatives used as pi 3 kinase inhibitors
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
WO2009095480A1 (en) * 2008-01-30 2009-08-06 Pharma Mar, S.A. Improved antitumoral treatments
JP2011513370A (ja) * 2008-03-07 2011-04-28 ファルマ・マール・ソシエダード・アノニマ 改善された抗腫瘍治療法
KR20210131473A (ko) 2008-03-18 2021-11-02 제넨테크, 인크. 항-her2 항체-약물 접합체와 화학요법제의 병용물, 및 사용 방법
US8252805B2 (en) 2008-05-07 2012-08-28 Teva Pharmaceutical Industries Ltd. Forms of lapatinib ditosylate and processes for preparation thereof
WO2009140144A1 (en) * 2008-05-15 2009-11-19 Teva Pharmaceutical Industries Ltd. 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 (en) 2008-08-25 2010-03-03 Ratiopharm GmbH Pharmaceutical composition comprising N-[3-chhloro-4-[3-fluorophenyl)methoxy)phenyl]6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine
EP2158913A1 (en) 2008-08-25 2010-03-03 Ratiopharm GmbH Pharmaceutical composition comprising N-[3-chhloro-4-[(3-fluorophenyl)methoxy]phenyl]6-(5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine
WO2010027848A2 (en) * 2008-08-26 2010-03-11 Teva Pharmaceutical Industries Ltd. Forms of lapatinib compounds and processes for the preparation thereof
US8476410B2 (en) 2008-10-16 2013-07-02 University of Pittsburgh—of the Commonwealth System of Higher Education Fully human antibodies to high molecular weight-melanoma associated antigen and uses thereof
WO2010061400A1 (en) 2008-11-03 2010-06-03 Natco Pharma Limited A novel process for the preparation of lapatinib and its pharmaceutically acceptable salts
EP2349235A1 (en) 2008-11-07 2011-08-03 Triact Therapeutics, Inc. Use of catecholic butane derivatives in cancer therapy
EA019959B1 (ru) 2009-01-16 2014-07-30 Экселиксис, Инк. Малатная соль n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида и ее кристаллические формы для лечения рака
CN101787017A (zh) * 2009-01-23 2010-07-28 岑均达 光学纯喹唑啉类化合物
AU2010210986A1 (en) 2009-02-09 2011-08-25 Supergen, Inc. Pyrrolopyrimidinyl Axl kinase inhibitors
EP2400985A2 (en) 2009-02-25 2012-01-04 OSI Pharmaceuticals, LLC Combination of an either an anti-igf-1r antibody or an igf binding protein and a small molecule igf-1r kinase inhibitor
EP2400990A2 (en) 2009-02-26 2012-01-04 OSI Pharmaceuticals, LLC In situ methods for monitoring the emt status of tumor cells in vivo
US8465912B2 (en) 2009-02-27 2013-06-18 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
EP2401614A1 (en) 2009-02-27 2012-01-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
TW201035088A (en) 2009-02-27 2010-10-01 Supergen Inc 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
US8481503B2 (en) 2009-03-06 2013-07-09 Merck Sharp & Dohme Corp. Combination cancer therapy with an AKT inhibitor and other anticancer agents
EP2408479A1 (en) 2009-03-18 2012-01-25 OSI Pharmaceuticals, LLC Combination cancer therapy comprising administration of an egfr inhibitor and an igf-1r inhibitor
US8597652B2 (en) 2009-03-20 2013-12-03 Genentech, Inc. Multispecific anti-HER antibodies
US8530492B2 (en) 2009-04-17 2013-09-10 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
WO2010120388A1 (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
DK2451445T3 (da) 2009-07-06 2019-06-24 Boehringer Ingelheim Int Fremgangsmåde til at tørre bibw2992, dets salte og faste farmaceutiske formuleringer omfattende denne aktive ingrediens
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
BR112012003653A2 (pt) 2009-08-21 2016-03-22 Smithkline Beecham Cork Ltd "método de tratar o câncer."
WO2011027249A2 (en) 2009-09-01 2011-03-10 Pfizer Inc. Benzimidazole derivatives
US8916574B2 (en) 2009-09-28 2014-12-23 Qilu Pharmaceutical Co., Ltd. 4-(substituted anilino)-quinazoline derivatives useful as tyrosine kinase inhibitors
US20120245351A1 (en) * 2009-09-29 2012-09-27 Natco Pharma Limited Process for the preparation of lapatinib and its pharmaceutically acceptable salts
EP2510110A1 (en) 2009-11-13 2012-10-17 Pangaea Biotech S.L. 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
US20110165155A1 (en) 2009-12-04 2011-07-07 Genentech, Inc. Methods of treating metastatic breast cancer with trastuzumab-mcc-dm1
JP5913126B2 (ja) 2009-12-31 2016-04-27 フンダシオン セントロ ナシオナル デ インベスティガシオネス オンコロヒカス カルロス ザ サードFundacion Centro Nacional de Investigaciones Oncologicas Carlos III キナーゼ阻害剤としての使用のための三環式化合物
ES2627703T3 (es) 2010-01-22 2017-07-31 Fundación Centro Nacional De Investigaciones Oncológicas Carlos Iii Inhibidores de PI3·quinasa
ES2753748T3 (es) 2010-02-12 2020-04-14 Pfizer Sales y polimorfos de 8-fluoro-2-{4-[(metilamino}metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona
WO2011101644A1 (en) 2010-02-18 2011-08-25 Centro Nacional De Investigaciones Oncologicas (Cnio) Triazolo [4, 5 - b] pyridin derivatives
CA2783656A1 (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
EP2542893A2 (en) 2010-03-03 2013-01-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
CA2793742C (en) 2010-03-23 2015-06-23 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
LT2552415T (lt) 2010-03-29 2016-12-27 Abraxis Bioscience, Llc Vėžio gydymo būdai
CN107158389A (zh) 2010-03-29 2017-09-15 阿布拉科斯生物科学有限公司 增强药物递送和治疗剂有效性的方法
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
ES2530755T3 (es) 2010-05-21 2015-03-05 Glaxosmithkline Llc Terapia de combinación para el tratamiento del cáncer
KR20190038684A (ko) 2010-06-04 2019-04-08 아브락시스 바이오사이언스, 엘엘씨 췌장암의 치료 방법
CN103068851B (zh) 2010-06-16 2015-03-11 高等教育联邦***-匹兹堡大学 内质蛋白的抗体及其用途
WO2011161217A2 (en) 2010-06-23 2011-12-29 Palacký University in Olomouc Targeting of vegfr2
US9012458B2 (en) 2010-06-25 2015-04-21 Eisai R&D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
AU2011274528B2 (en) 2010-07-09 2015-04-23 Genentech, Inc. Anti-neuropilin antibodies and methods of use
CN102344445B (zh) * 2010-07-23 2015-11-25 岑均达 光学纯喹唑啉类化合物
CN102344444B (zh) * 2010-07-23 2015-07-01 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
CA2808236A1 (en) 2010-08-31 2012-03-08 Genentech, Inc. Biomarkers and methods of treatment
WO2012052948A1 (en) 2010-10-20 2012-04-26 Pfizer Inc. Pyridine- 2- derivatives as smoothened receptor modulators
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
US20130236467A1 (en) 2010-11-24 2013-09-12 Jeremy Griggs 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 (en) 2010-12-22 2012-06-27 Pangaea Biotech S.L. Molecular biomarkers for predicting response to tyrosine kinase inhibitors in lung cancer
WO2012083440A1 (en) 2010-12-23 2012-06-28 Apotex Pharmachem Inc A 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
PL2670753T3 (pl) 2011-01-31 2017-05-31 Novartis Ag Nowe pochodne heterocykliczne
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 (en) 2011-02-23 2012-08-29 Pangaea Biotech, S.A. Molecular biomarkers for predicting response to antitumor treatment in lung cancer
BR112013022307A2 (pt) 2011-03-04 2020-09-24 Glaxosmithkline Intellectual Property (No. 2) Limited aminoquinolinas como inibidores de quinase
KR20210043016A (ko) 2011-03-04 2021-04-20 뉴젠 세러퓨틱스 인코포레이티드 알킨 치환된 퀴나졸린 화합물 및 그것의 사용 방법
JP2014518610A (ja) 2011-03-09 2014-08-07 リチャード ジー. ペステル 前立腺癌細胞系、遺伝子シグネチャー及びその使用
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
EP2688887B1 (en) 2011-03-23 2015-05-13 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
CN107233343A (zh) 2011-04-01 2017-10-10 基因泰克公司 Akt抑制剂化合物和化疗剂的组合以及使用方法
US9150644B2 (en) 2011-04-12 2015-10-06 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Human monoclonal antibodies that bind insulin-like growth factor (IGF) I and II
US8962650B2 (en) 2011-04-18 2015-02-24 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
DK2699598T3 (en) 2011-04-19 2019-04-23 Pfizer COMBINATIONS OF ANTI-4-1BB ANTIBODIES AND ADCC-INducing ANTIBODIES FOR TREATMENT OF CANCER
WO2012149014A1 (en) 2011-04-25 2012-11-01 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
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
CN103748099B (zh) 2011-05-19 2016-08-17 卡洛斯三世国家癌症研究中心基金会 作为蛋白激酶抑制剂的大环化合物
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
US9945862B2 (en) 2011-06-03 2018-04-17 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
WO2013004984A1 (en) 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncologicas (Cnio) Tricyclic compounds for use as kinase inhibitors
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
EP3812387A1 (en) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
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
WO2013025939A2 (en) 2011-08-16 2013-02-21 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
CA2845179A1 (en) 2011-08-31 2013-03-07 Genentech, Inc. Diagnostic markers
CA2847540C (en) 2011-09-22 2016-05-17 Pfizer Inc. Pyrrolopyrimidine and purine derivatives
CN104066851A (zh) 2011-09-30 2014-09-24 基因泰克公司 肿瘤或肿瘤细胞中上皮或间充质表型的诊断性甲基化标志物和对egfr激酶抑制剂的响应
EP3275902A1 (en) 2011-10-04 2018-01-31 IGEM Therapeutics Limited Ige anti-hmw-maa antibody
AP2014007601A0 (en) 2011-10-28 2014-04-30 Novartis Ag Novel purine derivatives and their use in the treatment of disease
AU2012335247A1 (en) 2011-11-08 2014-05-29 Pfizer Inc. Methods of treating inflammatory disorders using anti-M-CSF antibodies
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
EP2861302A4 (en) 2012-05-14 2016-08-24 Prostagene Llc USE OF CCR5 MODULATORS IN THE TREATMENT OF CANCER
CA2872526A1 (en) 2012-05-16 2013-11-21 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
US9505749B2 (en) 2012-08-29 2016-11-29 Amgen Inc. Quinazolinone compounds and derivatives thereof
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
EP2909181B1 (en) 2012-10-16 2017-08-09 Tolero Pharmaceuticals, Inc. Pkm2 modulators and methods for their use
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
JPWO2014098176A1 (ja) 2012-12-21 2017-01-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体のアモルファス及びその製造方法
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
JP6669499B2 (ja) 2013-02-15 2020-03-18 カラ ファーマシューティカルズ インコーポレイテッド 治療用化合物
CN104981235A (zh) 2013-02-19 2015-10-14 赫克萨尔股份公司 包括n-[3-氯-4-(3-氟苄氧基)苯基]-6-[5({[2-(甲基磺酰基)乙基]氨基}甲基)-2-呋喃基]喹唑啉-4-胺或其药学可接受的盐、溶剂化物或溶剂化盐的药物组合物
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
ES2831625T3 (es) 2013-02-20 2021-06-09 Kala Pharmaceuticals Inc Compuestos terapéuticos y sus usos
KR20150118152A (ko) 2013-02-21 2015-10-21 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 키나제 억제제로서의 퀴나졸린
CN104994879A (zh) 2013-02-22 2015-10-21 霍夫曼-拉罗奇有限公司 治疗癌症和预防药物抗性的方法
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
US9834575B2 (en) 2013-02-26 2017-12-05 Triact Therapeutics, Inc. Cancer therapy
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
EP2970205B1 (en) 2013-03-14 2019-05-08 Tolero Pharmaceuticals, Inc. Jak2 and alk2 inhibitors and methods for their use
RU2015139054A (ru) 2013-03-14 2017-04-19 Дженентек, Инк. Способы лечения рака и профилактики лекарственной резистентности рака
EP2968537A1 (en) 2013-03-15 2016-01-20 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
US10517861B2 (en) 2013-05-14 2019-12-31 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
HU231012B1 (hu) 2013-05-24 2019-11-28 Egis Gyógyszergyár Nyilvánosan Működő Részvénytársaság Lapatinib sók
ES2784664T3 (es) * 2013-07-18 2020-09-29 Shanghai Fochon Pharmaceutical Co Ltd Derivados de quinazolina, composiciones de los mismos y uso como productos farmacéuticos.
WO2015035410A1 (en) 2013-09-09 2015-03-12 Triact Therapeutic, Inc. Cancer therapy
WO2015051302A1 (en) 2013-10-04 2015-04-09 Aptose Biosciences Inc. Compositions and methods for treating cancers
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
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
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
US20170000778A1 (en) 2013-12-06 2017-01-05 Emmanuelle di Tomaso Dosage regimen for an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor
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
HRP20221518T1 (hr) 2014-01-24 2023-02-17 Turning Point Therapeutics, Inc. Diaril makrociklični spojevi kao modulatori protein kinaza
US20160361309A1 (en) 2014-02-26 2016-12-15 Glaxosmithkline Intellectual Property (No.2) Limited Methods of treating cancer patients responding to 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
WO2015155624A1 (en) 2014-04-10 2015-10-15 Pfizer Inc. Dihydropyrrolopyrimidine derivatives
WO2015156674A2 (en) 2014-04-10 2015-10-15 Stichting Het Nederlands Kanker Instituut Method for treating cancer
EP2937346A1 (en) 2014-04-24 2015-10-28 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Co-crystals of lapatinib
MX2016014143A (es) 2014-04-30 2017-02-15 Pfizer Derivados de diheterociclo enlazado a cicloalquilo.
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
CN106999578B (zh) 2014-07-31 2022-03-04 美国政府(由卫生和人类服务部的部长所代表) 针对epha4的人类单克隆抗体和其用途
KR102329681B1 (ko) 2014-08-28 2021-11-23 에자이 알앤드디 매니지먼트 가부시키가이샤 고순도의 퀴놀린 유도체 및 이를 제조하는 방법
JP2017536347A (ja) 2014-10-17 2017-12-07 ノバルティス アーゲー セリチニブとegfr阻害剤の組合せ
US10206924B2 (en) * 2014-12-15 2019-02-19 The Regents Of The University Of Michigan Small molecule inhibitors of EGFR and PI3K
JP6621477B2 (ja) 2014-12-18 2019-12-18 ファイザー・インク ピリミジンおよびトリアジン誘導体ならびにaxl阻害薬としてのそれらの使用
EP3699290A1 (en) 2014-12-24 2020-08-26 F. Hoffmann-La Roche AG Therapeutic, diagnostic, and prognostic methods for cancer
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
EP3242934B1 (en) 2015-01-08 2021-08-18 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
AU2016214923A1 (en) * 2015-02-03 2017-08-24 Trillium Therapeutics Inc. Novel fluorinated derivatives as EGFR inhibitors useful for treating cancers
DK3263106T3 (da) 2015-02-25 2024-01-08 Eisai R&D Man Co Ltd Fremgangsmåde til undertrykkelse af bitterhed af quinolinderivat
WO2016140717A1 (en) 2015-03-04 2016-09-09 Merck Sharp & Dohme Corp. Combination of a pd-1 antagonist and a vegfr/fgfr/ret tyrosine kinase inhibitor for treating cancer
KR20180018507A (ko) 2015-04-20 2018-02-21 톨레로 파마수티컬스, 인크. 미토콘드리아 프로파일링에 의한 알보시딥에 대한 반응 예측
WO2016178876A2 (en) 2015-05-01 2016-11-10 Cocrystal Pharma, Inc. Nucleoside analogs for treatment of the flaviviridae family of viruses and cancer
MX2017014645A (es) 2015-05-18 2018-01-23 Tolero Pharmaceuticals Inc Profarmacos de alvocidib que tienen una biodisponibilidad aumentada.
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
JP6757959B2 (ja) 2015-06-16 2020-09-23 株式会社 PRISM BioLab 抗がん剤
US10287401B2 (en) 2015-07-01 2019-05-14 California Institute Of Technology Cationic mucic acid polymer-based delivery systems
JP6871903B2 (ja) 2015-07-02 2021-05-19 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. プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
MX2018000718A (es) 2015-07-21 2020-01-20 Turning Point Therapeutics Inc Macrociclos de diarilo quirales y usos de los mismos.
WO2017024073A1 (en) 2015-08-03 2017-02-09 Tolero Pharmaceuticals, 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
US11124483B2 (en) 2015-09-02 2021-09-21 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
MX2018005298A (es) 2015-11-02 2018-06-22 Novartis Ag Regimen de dosificacion para un inhibidor de fosfatidilinositol 3-quinasa.
WO2017093942A1 (en) 2015-12-01 2017-06-08 Glaxosmithkline Intellectual Property Development Limited Combination treatments and uses and methods thereof
KR20180100125A (ko) 2015-12-03 2018-09-07 아지오스 파마슈티컬스 아이엔씨. Mtap 널 암을 치료하기 위한 mat2a 억제제
KR102511024B1 (ko) 2016-03-15 2023-03-16 오리존 지노믹스 에스.에이. 고형 종양의 치료에 사용하기 위한 lsd1 억제제의 조합물
CA3031100A1 (en) 2016-07-28 2018-02-01 Tp Therapeutics, Inc. Macrocycle kinase inhibitors
US11649289B2 (en) 2016-08-04 2023-05-16 Glaxosmithkline Intellectual Property Development Limited Anti-ICOS and anti-PD-1 antibody combination therapy
KR20190051010A (ko) 2016-09-08 2019-05-14 칼라 파마슈티컬스, 인크. 치료 화합물의 결정형 및 그의 용도
AU2017324713B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
AU2017324716B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
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
CN110234659A (zh) 2016-12-19 2019-09-13 特雷罗药物股份有限公司 用于敏感性分析的分析肽和方法
MA47107B1 (fr) 2016-12-22 2021-11-30 Amgen Inc Dérivés de benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine et pyrido[2,3-d]pyrimidine en tant qu'inhibiteurs de kras g12c pour le traitement de cancer du poumon, du pancréas ou de l'intestin
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
EP3658148A4 (en) 2017-07-28 2021-04-28 Turning Point Therapeutics, Inc. MACROCYCLIC COMPOUNDS AND USES OF THESE COMPOUNDS
IL272512B (en) 2017-09-08 2022-07-01 Amgen Inc kras g12c inhibitors and methods of using them
US11497756B2 (en) 2017-09-12 2022-11-15 Sumitomo Pharma Oncology, Inc. Treatment regimen for cancers that are insensitive to BCL-2 inhibitors using the MCL-1 inhibitor alvocidib
US20200237766A1 (en) 2017-10-13 2020-07-30 Tolero Pharmaceuticals, Inc. Pkm2 activators in combination with reactive oxygen species for treatment of cancer
CA3085593A1 (en) 2017-12-18 2019-06-27 Sterngreene, Inc. Pyrimidine compounds useful as tyrosine kinase inhibitors
PT3728271T (pt) 2017-12-19 2022-10-06 Turning Point Therapeutics Inc Compostos macrocíclicos para tratar doenças
MX2020011582A (es) 2018-05-04 2020-11-24 Amgen Inc Inhibidores de kras g12c y metodos para su uso.
CA3098574A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
US10988485B2 (en) 2018-05-10 2021-04-27 Amgen Inc. KRAS G12C inhibitors and methods of using the same
ES2938987T3 (es) 2018-06-01 2023-04-18 Amgen Inc Inhibidores de KRAS G12c y métodos de uso de los mismos
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11285156B2 (en) 2018-06-12 2022-03-29 Amgen Inc. Substituted piperazines as KRAS G12C inhibitors
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
CN112512597A (zh) 2018-07-26 2021-03-16 大日本住友制药肿瘤公司 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂
WO2020070239A1 (en) 2018-10-04 2020-04-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Egfr inhibitors for treating keratodermas
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
WO2020106640A1 (en) 2018-11-19 2020-05-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3119807A1 (en) 2018-12-04 2020-06-11 Sumitomo Dainippon Pharma Oncology, Inc. Cdk9 inhibitors and polymorphs thereof for use as agents for treatment of cancer
US20220081438A1 (en) 2018-12-19 2022-03-17 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
US20220041579A1 (en) 2018-12-19 2022-02-10 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of fgfr tyrosine kinases
WO2020132651A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
MX2021007158A (es) 2018-12-20 2021-08-16 Amgen Inc Heteroarilamidas utiles como inhibidores de kif18a.
EP3898592A1 (en) 2018-12-20 2021-10-27 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
CA3123871A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
EP3917963A1 (en) 2019-02-01 2021-12-08 GlaxoSmithKline Intellectual Property Development Limited Belantamab mafodotin in combination with pembrolizumab for treating cancer
CA3127502A1 (en) 2019-02-12 2020-08-20 Sumitomo Dainippon Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
KR20210146288A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로사이클릴 화합물 및 이의 용도
JP2022525149A (ja) 2019-03-20 2022-05-11 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 ベネトクラクスが失敗した急性骨髄性白血病(aml)の処置
KR20210141621A (ko) 2019-03-22 2021-11-23 스미토모 다이니폰 파마 온콜로지, 인크. Pkm2 조정제를 포함하는 조성물 및 그를 사용한 치료 방법
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
BR112021023277A2 (pt) 2019-05-21 2022-01-04 Amgen Inc Formas em estado sólido
JP2022539178A (ja) 2019-06-26 2022-09-07 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド Il1rap結合タンパク質
JP2022542394A (ja) 2019-08-02 2022-10-03 アムジエン・インコーポレーテツド Kif18a阻害剤として有用なヘテロアリールアミド
AU2020324406A1 (en) 2019-08-02 2022-03-17 Amgen Inc. KIF18A inhibitors
AU2020325115A1 (en) 2019-08-02 2022-03-17 Amgen Inc. Pyridine derivatives as KIF18A inhibitors
CA3146693A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
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
WO2021046289A1 (en) 2019-09-06 2021-03-11 Glaxosmithkline Intellectual Property Development Limited Dosing regimen for the treatment of cancer with an anti icos agonistic antibody and ipilimumab
MX2022004656A (es) 2019-10-24 2022-05-25 Amgen Inc Derivados de piridopirimidina utiles como inhibidores de kras g12c y kras g12d en el tratamiento del cancer.
CN114867735A (zh) 2019-11-04 2022-08-05 锐新医药公司 Ras抑制剂
AU2020379734A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
TW202132315A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras 抑制劑
CN114901662A (zh) 2019-11-08 2022-08-12 锐新医药公司 双环杂芳基化合物及其用途
AR120456A1 (es) 2019-11-14 2022-02-16 Amgen Inc Síntesis mejorada del compuesto inhibidor de g12c de kras
US20230192681A1 (en) 2019-11-14 2023-06-22 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
CN114980976A (zh) 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
CA3163703A1 (en) 2020-01-07 2021-07-15 Steve Kelsey Shp2 inhibitor dosing and methods of treating cancer
BR112022014562A2 (pt) 2020-01-28 2022-09-13 Glaxosmithkline Ip Dev Ltd Tratamentos de combinação, usos e métodos dos mesmos
WO2021155006A1 (en) 2020-01-31 2021-08-05 Les Laboratoires Servier Sas Inhibitors of cyclin-dependent kinases and uses thereof
AU2021229457A1 (en) * 2020-03-02 2022-10-20 Turning Point Therapeutics, Inc. Therapeutic uses of macrocyclic compounds
CN115916194A (zh) 2020-06-18 2023-04-04 锐新医药公司 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法
CN116209438A (zh) 2020-09-03 2023-06-02 锐新医药公司 使用sos1抑制剂治疗具有shp2突变的恶性疾病
CN116457358A (zh) 2020-09-15 2023-07-18 锐新医药公司 作为ras抑制剂以治疗癌症的吲哚衍生物
WO2022140456A1 (en) 2020-12-22 2022-06-30 Mekanistic Therapeutics Llc Substituted aminobenzyl heteroaryl compounds as egfr and/or pi3k inhibitors
TW202241885A (zh) 2020-12-22 2022-11-01 大陸商上海齊魯銳格醫藥研發有限公司 Sos1抑制劑及其用途
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
IL308195A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors for cancer treatment
TW202309052A (zh) 2021-05-05 2023-03-01 美商銳新醫藥公司 Ras抑制劑
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 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
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

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
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5480883A (en) 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
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
WO1993018035A1 (en) 1992-03-04 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
WO1993017682A1 (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
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
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
WO1995024190A2 (en) 1994-03-07 1995-09-14 Sugen, Inc. 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 (sr) 1994-11-12 1997-12-01 Zeneca Ltd
GB9424233D0 (en) 1994-11-30 1995-01-18 Zeneca Ltd Quinazoline derivatives
JP3290666B2 (ja) 1995-06-07 2002-06-10 ファイザー・インコーポレーテッド 複素環式の縮合環ピリミジン誘導体
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
US5965563A (en) 1995-11-14 1999-10-12 Pharmacia & Upjohn S.P.A. Aryl and heteroaryl purine compounds
GB9603095D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
HRP970371A2 (en) * 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
ID19430A (id) 1996-07-13 1998-07-09 Glaxo Group Ltd Senyawa senyawa heterosiklik
AR007857A1 (es) * 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
HUP0301120A2 (hu) * 2000-06-22 2003-08-28 Pfizer Products Inc. Szubsztituált fenilamino-kinazolin-származékok, alkalmazásuk rendellenes sejtnövekedés kezelésére és azokat tartalmazó gyógyszerkészítmények
TWI307339B (en) * 2000-06-30 2009-03-11 Glaxo Group Ltd Quinazoline ditosylate salt comprounds
EP1353693B1 (en) * 2001-01-16 2005-03-16 Glaxo Group Limited Pharmaceutical combination containing a 4-quinazolineamine and paclitaxel, carboplatin or vinorelbine for the treatment of cancer
ES2381781T3 (es) * 2002-02-01 2012-05-31 Astrazeneca Ab Compuestos de quinazolina
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
FR08C0038I2 (fr) 2012-02-22
WO1999035146A1 (en) 1999-07-15
SI1454907T1 (sl) 2009-04-30
EP1460072A1 (en) 2004-09-22
US20030176451A1 (en) 2003-09-18
CA2317589C (en) 2007-08-07
HRP20000469B1 (en) 2007-05-31
US20100120804A1 (en) 2010-05-13
AP2000001861A0 (en) 2000-09-30
ATE270670T1 (de) 2004-07-15
ES2262087T3 (es) 2006-11-16
EG24743A (en) 2010-07-14
EE04616B1 (et) 2006-04-17
NO2008017I1 (no) 2008-12-01
CY1108859T1 (el) 2014-07-02
AU749549C (en) 2003-03-20
CY2008015I2 (el) 2009-11-04
BG104668A (en) 2001-04-30
US6713485B2 (en) 2004-03-30
PT1460072E (pt) 2006-07-31
US20130310562A1 (en) 2013-11-21
IS2276B (is) 2007-09-15
ME00757B (me) 2008-06-05
HUP0100941A2 (hu) 2001-09-28
AU2278399A (en) 1999-07-26
EP1454907B1 (en) 2008-12-17
DE69930773T2 (de) 2006-09-28
NZ505456A (en) 2003-06-30
NO316176B1 (no) 2003-12-22
EP1460072B1 (en) 2006-04-05
ES2319119T3 (es) 2009-05-04
US20070015775A1 (en) 2007-01-18
ZA99172B (en) 2000-07-11
IS5549A (is) 2000-06-27
JP2002500225A (ja) 2002-01-08
YU44800A (sh) 2002-11-15
DK1460072T3 (da) 2006-07-31
PT1047694E (pt) 2004-11-30
PT1454907E (pt) 2009-02-18
LU91475I9 (sr) 2019-01-02
MY124055A (en) 2006-06-30
PL341595A1 (en) 2001-04-23
US8513262B2 (en) 2013-08-20
US20160339027A1 (en) 2016-11-24
EA002455B1 (ru) 2002-04-25
AR066982A2 (es) 2009-09-23
ES2221354T3 (es) 2004-12-16
HU227593B1 (en) 2011-09-28
CZ298047B6 (cs) 2007-06-06
EP1047694A1 (en) 2000-11-02
US9199973B2 (en) 2015-12-01
CA2317589A1 (en) 1999-07-15
AU749549B2 (en) 2002-06-27
SK285405B6 (sk) 2007-01-04
ATE417847T1 (de) 2009-01-15
TW477788B (en) 2002-03-01
ATE322491T1 (de) 2006-04-15
BR9906904B1 (pt) 2011-05-03
BR9906904A (pt) 2000-10-17
CN1134438C (zh) 2004-01-14
US20160051551A1 (en) 2016-02-25
EE200000411A (et) 2001-12-17
OA11444A (en) 2004-04-29
DE69940128D1 (de) 2009-01-29
KR20010015902A (ko) 2001-02-26
US20070238875A1 (en) 2007-10-11
IL137041A (en) 2006-10-05
DE69930773D1 (de) 2006-05-18
PE20000230A1 (es) 2000-04-03
GB9800569D0 (en) 1998-03-11
NO20003561L (no) 2000-09-11
EA200000637A1 (ru) 2001-02-26
US7109333B2 (en) 2006-09-19
IL137041A0 (en) 2001-06-14
DE69918528D1 (de) 2004-08-12
BG64825B1 (bg) 2006-05-31
HUP0100941A3 (en) 2002-09-30
CY2008015I1 (el) 2009-11-04
UA66827C2 (uk) 2004-06-15
TR200002015T2 (tr) 2001-01-22
JP3390741B2 (ja) 2003-03-31
EP1047694B1 (en) 2004-07-07
NO20003561D0 (no) 2000-07-11
DK1454907T3 (da) 2009-03-09
HK1031883A1 (en) 2001-06-29
FR08C0038I1 (sr) 2008-11-14
CZ20002587A3 (en) 2001-05-16
CN1292788A (zh) 2001-04-25
AP1446A (en) 2005-07-19
AR015507A1 (es) 2001-05-02
US20020147205A1 (en) 2002-10-10
CO4820390A1 (es) 1999-07-28
US6727256B1 (en) 2004-04-27
NO2008017I2 (sr) 2011-10-17
US8912205B2 (en) 2014-12-16
US20050130996A1 (en) 2005-06-16
AU2010276460A1 (en) 2011-02-17
GEP20022678B (en) 2002-04-25
KR100569776B1 (ko) 2006-04-11
MA26596A1 (fr) 2004-12-20
HRP20060387A2 (en) 2008-02-29
DE69918528T2 (de) 2005-07-28
LU91475I2 (fr) 2008-11-10
US20150065527A1 (en) 2015-03-05
DK1047694T3 (da) 2004-11-08
SI1047694T1 (en) 2005-02-28
NL300360I1 (nl) 2008-11-03
SK10502000A3 (sk) 2001-08-06
JP2002326990A (ja) 2002-11-15
NL300360I2 (nl) 2009-02-02
HRP20000469A2 (en) 2001-06-30
CY1105618T1 (el) 2010-12-22
DE122008000048I1 (de) 2009-01-02
EP1454907A1 (en) 2004-09-08
PL192746B1 (pl) 2006-12-29
SI1460072T1 (sl) 2006-08-31

Similar Documents

Publication Publication Date Title
RS49779B (sr) Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
MEP22008A (en) Derivatives of n-[heteroaryl(piperidine-2-yl)methyl]benzamide, preparation method thereof and application of same in therapeutics
RS50519B (sr) Supstituisani derivati 8'-piri(mi)dinil-dihidrospiro- /cikloalkilamin/-pirimido/1,2-a/pirimidin-6-ona
DE60026514D1 (de) Neue prolinverbindungen als mikrobizide mittel
HUP0300909A2 (hu) NHE-3 inhibitor hatású 2-guanidino-4-aril-kinazolin-származékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
RS50918B (sr) Novi estri fluorenkarbonske kiseline, postupak za njihovo pripremanje, kao i njihova upotreba kao lekova
WO2002094794A8 (en) 4 (phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain anxiety or gastrointestinal disorders
SE0001207D0 (sv) Novel compounds
ME00108B (me) DE RIVATI DIOKSAN-2-ALKILKARBAMATA, POSTUPAK ZA NJIHOVO DOBIJANJ E l PRIMENA ISTIH U TERAPEUTICIMA
RS51193B (sr) Hidantoinski derivati korisni kao inhibitori metaloproteinaza
YU48949B (sh) Benzopiran i srodni ltb-antagonisti
HUP0004725A2 (hu) 2-[3,5-Bisz-(trifluor-metil)-fenil]-N-metil-N-(6-morfolin-4-il-4-o-tolil-piridin-3-il)-izobutiramid
BG106805A (en) Novel compounds
RS50677B (sr) Karbamatna jedinjenja za upotrebu u sprečavanju ili lečenju bipolarnog poremaćaja
IL150126A0 (en) Novel 4(piperazinyl(8-quinolinyl)methyl) benzamides
SE8503415L (sv) Nya isoindolinylalkylpiperaziner och farmaceutiska kompositioner innehallande desamma
SE0101766D0 (sv) Novel compounds
SE0001208D0 (sv) Novel compounds
YU48079B (sh) Heterociklična jedinjenja
SE0101768D0 (sv) Novel compounds
NZ309499A (en) Styryl benzimidazole derivatives useful as inhibitors of smooth muscle cell proliferation
ME00213B (me) Derivati 5-(piridin-3-il)-1-azabiciklo (3.2.1.) oktana, njihova priprema i terapeutska primjena
WO2000008020A3 (en) Tricyclic carboxamides
YU30392A (sh) Piridazinon sirćetne kiseline
ATE266026T1 (de) Benzofurancarboxamide und deren therapeutische verwendung