CO5140097A1 - Derivados quinolin-2-ona sustituidos con heteroarilo utiles como agnetes anticancerigenos - Google Patents

Derivados quinolin-2-ona sustituidos con heteroarilo utiles como agnetes anticancerigenos

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Publication number
CO5140097A1
CO5140097A1 CO00008430A CO00008430A CO5140097A1 CO 5140097 A1 CO5140097 A1 CO 5140097A1 CO 00008430 A CO00008430 A CO 00008430A CO 00008430 A CO00008430 A CO 00008430A CO 5140097 A1 CO5140097 A1 CO 5140097A1
Authority
CO
Colombia
Prior art keywords
cr13r14
aryl
groups
substituents
cycloalkyl
Prior art date
Application number
CO00008430A
Other languages
English (en)
Inventor
Vera Yang Bingwei
Original Assignee
Pfizer Prod Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of CO5140097A1 publication Critical patent/CO5140097A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Un compuesto de fórmula<EMI FILE="00008430_1" ID="1" IMF=JPEG >o una sal o solvato farmacéuticamente aceptable del mismo, en la que la línea de puntos indica un segundo enlace opcional que une C-3 y C-4 del anillo quinolin-2-ona; R1 se selecciona entre H, alquilo C1-C10, -(CR13R14)qC(O)R12, -(CR13R14)qC(O)OR15, -(CR13C14)qOR12, -(CR13R14)qCSO2R15, -(CR13R14)t(cicloalquilo C3-C10), -(CR13R14)t(arilo C6-C10) y -(CR13R14)t(heterociclo de 4 a 10 miembros), estando dichos grupos R1 cicloalquilo, arilo y heterocíclico opcionalmente condensados con un grupo arilo C6-C10, un grupo cíclico saturado C5-C8, o un grupo heterocíclico de 4 a 10 miembros; y estando los grupos anteriores R1, excepto H, pero incluyendo cualquier anillo condensado de los citados más arriba, sustituidos con 1 a 4 grupos R6; R2 es halógeno, ciano, -C(O)OR15, o un grupo seleccionado de los sustituyentes proporcionados en la definición de R12; cada R3, R4, R5, R6, y R7 se selecciona independientemente de H, alquilo C1-C10, alquenilo C2-C10, alquinilo C2-C10, halógeno, ciano, nitro, trifluorometilo, trifluorometoxi, azido, -OR12, -C(O)R12, -C(O)OR12, -NR13C(O)OR15, -OC(O)R12, -NR13S02R15, -SO2NR12R13, -NR13C(O)R12, -C(O)NR12R13, -NR12R13, -CH=NOR12, -S(O)jR12 siendo j un número entero de 0 a 2, -(CR13R14)t(arilo C6-C10), -(CR13R14)t(heterociclo de 4-10 miembros),(CR13R14)t(cicloalquilo C3-C10), y -(CR13R14)tC=CR16; y estando los restos cicloalquilo, arilo y heterocíclico de los grupos anteriores opcionalmente condensados con un grupo arilo C6-C10, un grupo cíclico saturado C5-C8, o un grupo heterocíclico de 4 a 10 miembros; y estando dichos grupos alquilo, alquenilo, cicloalquilo, arilo y heterocíclico opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados de halógeno, ciano, nitro, trifluorometilo, trifluorometoxi, azido, -NR13SO2R15, -SO2NR12R13, -C(O)R12, -C(O)OR12, -OC(O)R12,- 2 --NR13C(O)OR15, -NR13C(O)R12, -C(0)NR12R13, -NR12R13, -OR12, alquilo C1-C10, alquenilo C2-C10, alquinilo C2-C10, -(CR13R14)t(arilo C6-C10), y -(CR13R14)t(heterociclo de 4-10 miembros); Z es un grupo heterocíclico aromático de 4-10 miembros, sustituido con 1 a 4 sustituyentes R6; R8 es H, -OR12, -OC(0)R12, -NR12R13, -N=CR12R13, -NR12C(O)R13, ciano, -C(O)OR13, -SR12 o -(CR13R14)t(heterociclo de 4 a 10 miembros), estando dichos grupos R8 heterocíclicos sustituidos con 1 a 4 grupos R6; R9 es -(CR13R14)t(imidazolilo) o - (CR13R14)t(piridinilo), estando dicho resto imidazolilo o piridinilo sustituido con 1 ó 2 sustituyentes R6; cada R12 se selecciona independientemente de H, alquilo C1-C10, -(CR13R14)t(cicloalquilo C3-C10), -(CR13R14)t(arilo C6-C10), y -(CR13R14)t(heterociclo de 4-10 miembros); estando dichos grupos cicloalquilo, arilo, heterocíclico R12 opcionalmente condensados con un grupo arilo C6-C10, un grupo cíclico saturado C5-C8, o un grupo heterocíclico de 4 a 10 miembros; y estando los anteriores sustituyentes R12, exceptuando H pero incluyendo cualquier anillo opcionalmente condensado, opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados de halógeno, ciano, nitro, trifluorometilo, trifluorometoxi, azido, -C(O)R13, -C(O)OR13, -OC(O)R13, -NR13C(O)R14, -C(O)NR13R14, -NR13R14, hidroxi, alquilo C1-C6, alcoxi C1-C6; cada t es independientemente un número entero de 0 a 5 y cada q es independientemente un número entero de 1 a 5; cada R13 y R14 es independientemente H o alquilo C1-C6, y estando R13 y R14 en la forma - (CR13R14)q o -(CR13R14)t estando cada uno independientemente definido para cada iteración de q o t superior a 1; R15 se selecciona de los sustituyentes proporcionados en la definición de R12 excepto que R15 no es H; R16 se selecciona de la lista de sustituyentes proporcionados en la definición de R12 y -SiR17R18R19; y, R17, R18 y R19 se seleccionan cada uno independientemente de los sustituyentes proporcionados en la definición de R12 excepto que al menos uno de R17, R18 y R19 no es H.
CO00008430A 1999-02-11 2000-02-09 Derivados quinolin-2-ona sustituidos con heteroarilo utiles como agnetes anticancerigenos CO5140097A1 (es)

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US (3) US6258824B1 (es)
EP (1) EP1150973B1 (es)
JP (3) JP4090200B2 (es)
KR (1) KR20010102073A (es)
CN (1) CN1340051A (es)
AP (1) AP2001002241A0 (es)
AR (1) AR028985A1 (es)
AT (1) ATE297916T1 (es)
AU (1) AU2124800A (es)
BG (1) BG105860A (es)
BR (1) BR0008202A (es)
CA (1) CA2362394C (es)
CO (1) CO5140097A1 (es)
CZ (1) CZ20012910A3 (es)
DE (1) DE60020812T2 (es)
DZ (1) DZ3009A1 (es)
EA (1) EA200100766A1 (es)
EE (1) EE200100425A (es)
ES (1) ES2243228T3 (es)
GT (1) GT200000014A (es)
HK (1) HK1042096A1 (es)
HN (1) HN2000000019A (es)
HR (1) HRP20010574A2 (es)
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ID (1) ID29584A (es)
IL (1) IL144307A0 (es)
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MA (1) MA26718A1 (es)
NO (1) NO20013909L (es)
OA (1) OA11833A (es)
PA (1) PA8490601A1 (es)
PE (1) PE20001464A1 (es)
PL (1) PL349839A1 (es)
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TR (2) TR200201296T2 (es)
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ZA (1) ZA200106520B (es)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL140721A0 (en) * 1998-07-06 2002-02-10 Janssen Pharmaceutica Nv Farnesyl protein transferase inhibitors with in vivo radiosensitizing properties
HUP0105231A3 (en) * 1999-02-11 2003-01-28 Pfizer Prod Inc Heteroaryl-substituted quinolin-2-one derivatives useful as anticancer agents and medicaments containing the compounds
ATE260269T1 (de) 1999-11-05 2004-03-15 Cytovia Inc Substituierte 4h-chromene und ähnliche verbindungen als kaspasis aktivatoren und apoptosis induktoren und deren verwendung
DE60008206T2 (de) * 1999-11-30 2004-12-02 Pfizer Products Inc., Groton Chinolinderivate verwendbar zur Hemmung der Farnesyl-Protein Transferase
HN2000000266A (es) * 2000-01-21 2001-05-21 Pfizer Prod Inc Compuesto anticanceroso y metodo de separacion de enantiomeros util para sintetizar dicho compuesto.
EP1253921A4 (en) * 2000-01-28 2004-10-13 Merck & Co Inc TREATMENT AND PROPHYLAXIS OF PROSTATE CANCER WITH COX-2 SELECTIVE INHIBITORS
JO2361B1 (en) 2000-06-22 2006-12-12 جانسين فارماسيوتيكا ان. في Enaniumer 1,2-anylated quinoline inhibitor for the transporter - farnesyl
EP1170011A1 (en) * 2000-07-06 2002-01-09 Boehringer Ingelheim International GmbH Novel use of inhibitors of the epidermal growth factor receptor
US7173040B2 (en) 2000-09-25 2007-02-06 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting 6-[(substituted phenyl)methyl]-quinoline and quinazoline derinazoline derivatives
EP1322644A1 (en) * 2000-09-25 2003-07-02 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting 6-heterocyclylmethyl quinolinone derivatives
US7053105B2 (en) 2000-09-25 2006-05-30 Janssen Pharmaceutica, N.V. Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors
AU2002220559A1 (en) * 2000-09-25 2002-04-02 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting 6-heterocyclylmethyl quinoline and quinazoline derivatives
AU2001293847B2 (en) * 2000-10-02 2007-05-24 Janssen Pharmaceutica N.V. Metabotropic glutamate receptor antagonists
WO2002042296A1 (en) 2000-11-21 2002-05-30 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting benzoheterocyclic derivatives
ES2260316T3 (es) 2000-12-27 2006-11-01 Janssen Pharmaceutica N.V. Derivados de quinazolina y quinolina 4-sustituidos que inhiben la farnesil transferasa.
US20040067968A1 (en) * 2000-12-27 2004-04-08 Angibaud Patrick Rene Farnesyl transferase inhibiting 4-heterocyclyl quinoline and quinazoline
US6858607B1 (en) 2001-05-16 2005-02-22 Cytovia, Inc. 7,8-fused 4H-chromene and analogs as activators of caspases and inducers of apoptosis and the use thereof
ATE450531T1 (de) * 2001-05-16 2009-12-15 Cytovia Inc Substituierte 4h-chromene und analoga als aktivatoren von caspasen und induktoren von apoptose, und deren verwendung als antikrebsmittel
EP1392283A4 (en) 2001-05-16 2004-10-20 Cytovia Inc COUMARINS AND SUBSTITUTED QUINOLINES USED AS CASPASE ACTIVATORS
US20030139332A1 (en) * 2001-07-09 2003-07-24 The Regents Of The University Of California Use of matrix metalloproteinase inhibitors to mitigate nerve damage
ES2323265T3 (es) 2001-12-19 2009-07-10 Janssen Pharmaceutica Nv Derivados de quinolina condensados en 1,8 sustituidos con triazoles unidos por el carbono como inhibidores de la farnesil-transferasa.
WO2003080058A1 (en) * 2002-03-22 2003-10-02 Janssen Pharmaceutica. N.V. Benzylimidazolyl substituted 2-quinoline and quinazoline derivatives for use as farnesyl transferase inhibitors
CA2479109C (en) * 2002-03-29 2011-08-02 Janssen Pharmaceutica N.V. Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands
ATE336496T1 (de) 2002-04-15 2006-09-15 Janssen Pharmaceutica Nv Farnesyl transferase hemmende tricyclische quinazolinederivate substitutiert mit kohlenstoff-gebundenen imidazolen oder triazolen
US7476741B2 (en) 2002-05-16 2009-01-13 Cytovia, Inc. Substituted 4H-chromens, 2H-chromenes, chromans and analogs as activators of caspases and inducers of apoptosis and the use thereof
EP1509515A4 (en) 2002-05-16 2006-07-05 Cytovia Inc SUBSTITUTED 4-ARYL-4H-PYRROLO 2,3-H | CHROMENES AND ANALOGUES AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THEIR USE
US20040186160A1 (en) * 2002-12-13 2004-09-23 Sugen, Inc. Hexahydro-cyclohepta-pyrrole oxindole as potent kinase inhibitors
EP1585743B1 (en) * 2002-12-19 2007-05-23 Pfizer Inc. 2-(1h-indazol-6-ylamino)- benzamide compounds as protein kinases inhibitors useful for the treatment of ophthalmic diseases
DK2476667T3 (da) 2003-02-26 2014-09-15 Sugen Inc Aminoheteroaryl-forbindelser som proteinkinase-inhibitorer
TW200504057A (en) * 2003-02-27 2005-02-01 Chugai Pharmaceutical Co Ltd Benzothiophene derivative
CA2533626A1 (en) * 2003-07-22 2005-02-03 Janssen Pharmaceutica, N.V. Quinolinone derivatives as inhibitors of c-fms kinase
WO2005051392A1 (en) 2003-11-20 2005-06-09 Children's Hospital Medical Center Gtpase inhibitors and methods of use
WO2005089502A2 (en) * 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
US20070293539A1 (en) * 2004-03-18 2007-12-20 Lansbury Peter T Methods for the treatment of synucleinopathies
EP1732549A4 (en) * 2004-03-18 2009-11-11 Brigham & Womens Hospital METHOD FOR THE TREATMENT OF SYNUCLEINOPATHIES
WO2005089515A2 (en) * 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
WO2005089504A2 (en) * 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
EP1740184A1 (en) * 2004-03-30 2007-01-10 Pfizer Products Incorporated Combinations of signal transduction inhibitors
KR100859891B1 (ko) 2004-08-26 2008-09-23 화이자 인코포레이티드 단백질 키나제 억제제로서 거울상이성질체적으로 순수한아미노헤테로아릴 화합물
NZ552946A (en) * 2004-08-26 2010-09-30 Pfizer Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors
BRPI0514687A (pt) * 2004-08-26 2008-06-17 Pfizer compostos amino heteroarila como inibidores de proteìna tirosina cinase
EP1807426A2 (en) * 2004-10-07 2007-07-18 Cytovia, Inc. SUBSTITUTED N-ARYL-1H-PYRAZOLOÝ3,4-b¨QUINOLIN-4-AMINES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS
CA2617056A1 (en) 2005-07-29 2007-02-08 Children's Hospital Medical Center Gtpase inhibitors and methods of use and crystal structure of rac-1 gtpase
PL2960253T3 (pl) 2005-09-07 2018-11-30 Amgen Fremont Inc. Ludzkie przeciwciała monoklonalne przeciwko kinazie podobnej do receptora aktywiny-1
ES2374450T3 (es) 2005-09-20 2012-02-16 OSI Pharmaceuticals, LLC Marcadores biológicos predictivos de respuesta anticancerígena para inhibidores de cinasa del receptor del factor de crecimiento 1 similar a insulina.
CA2634598A1 (en) * 2005-12-23 2007-07-05 Link Medicine Corporation Treatment of synucleinopathies
TW200812615A (en) 2006-03-22 2008-03-16 Hoffmann La Roche Tumor therapy with an antibody for vascular endothelial growth factor and an antibody for human epithelial growth factor receptor type 2
BRPI0711358A2 (pt) 2006-05-09 2011-09-27 Pfizer Prod Inc derivados do ácido cicloalquilamino e suas composições farmacêuticas
NZ574580A (en) 2006-08-21 2011-12-22 Hoffmann La Roche Her2 tumor therapy with an anti-vegf antibody
RU2472788C9 (ru) * 2007-05-23 2013-04-20 Аллерган, Инк. (бициклогетероарил)имидазолил)метилгетероарильные соединения как агонисты адренергических рецепторов
PL2155733T3 (pl) * 2007-05-23 2013-02-28 Allergan Inc Cykliczne laktamy do leczenia jaskry lub podwyższonego ciśnienia śródgałkowego
US8129356B2 (en) * 2007-10-01 2012-03-06 Vanderbilt University Bmx mediated signal transduction in irradiated vascular endothelium
US8232402B2 (en) * 2008-03-12 2012-07-31 Link Medicine Corporation Quinolinone farnesyl transferase inhibitors for the treatment of synucleinopathies and other indications
DE102008022221A1 (de) * 2008-05-06 2009-11-12 Universität des Saarlandes Inhibitoren der humanen Aldosteronsynthase CYP11B2
EP2370436A1 (en) * 2008-11-13 2011-10-05 Link Medicine Corporation Azaquinolinone derivatives and uses thereof
US20100331363A1 (en) * 2008-11-13 2010-12-30 Link Medicine Corporation Treatment of mitochondrial disorders using a farnesyl transferase inhibitor
US20110060005A1 (en) * 2008-11-13 2011-03-10 Link Medicine Corporation Treatment of mitochondrial disorders using a farnesyl transferase inhibitor
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
US20110171124A1 (en) 2009-02-26 2011-07-14 Osi Pharmaceuticals, Inc. In situ methods for monitoring the EMT status of tumor cells in vivo
US8642834B2 (en) 2009-02-27 2014-02-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
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
EP2401613A2 (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
AU2011223655A1 (en) 2010-03-03 2012-06-28 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
US20110275644A1 (en) 2010-03-03 2011-11-10 Buck Elizabeth A Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
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
WO2012149014A1 (en) 2011-04-25 2012-11-01 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
HUE052198T2 (hu) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology Inc Heterociklusos protein kináz inhibitorok
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
WO2013166043A1 (en) 2012-05-02 2013-11-07 Children's Hospital Medical Center Rejuvenation of precursor cells
WO2014062655A1 (en) 2012-10-16 2014-04-24 Janssen Pharmaceutica Nv HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
AU2013331496B2 (en) 2012-10-16 2017-07-27 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of ROR-gamma-t
KR20150070350A (ko) 2012-10-16 2015-06-24 얀센 파마슈티카 엔.브이. Ror-감마-t의 페닐 결합 퀴놀리닐 조절제
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
AR094403A1 (es) 2013-01-11 2015-07-29 Hoffmann La Roche Terapia de combinación de anticuerpos anti-her3
KR102334260B1 (ko) 2013-03-14 2021-12-02 스미토모 다이니폰 파마 온콜로지, 인크. Jak2 및 alk2 억제제 및 이들의 사용 방법
US9206188B2 (en) 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
BR112016008215A2 (pt) 2013-10-15 2017-09-26 Janssen Pharmaceutica Nv moduladores de quinolinila ligados por alquila de roryt
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of RORγt
WO2015057626A1 (en) 2013-10-15 2015-04-23 Janssen Pharmaceutica Nv QUINOLINYL MODULATORS OF RORyT
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
US10028503B2 (en) 2014-06-18 2018-07-24 Children's Hospital Medical Center Platelet storage methods and compositions for same
CA3006743A1 (en) 2015-12-03 2017-06-08 Agios Pharmaceuticals, Inc. Mat2a inhibitors for treating mtap null cancer
CN108003150A (zh) * 2016-10-31 2018-05-08 河南工业大学 4-杂芳基喹啉酮衍生物的制备方法及其应用
KR20210038906A (ko) 2018-07-26 2021-04-08 스미토모 다이니폰 파마 온콜로지, 인크. 비정상적 acvr1 발현과 연관된 질환을 치료하는 방법 및 그에 사용하기 위한 acvr1 억제제
JP2022520361A (ja) 2019-02-12 2022-03-30 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 複素環式タンパク質キナーゼ阻害剤を含む製剤
WO2021155006A1 (en) 2020-01-31 2021-08-05 Les Laboratoires Servier Sas Inhibitors of cyclin-dependent kinases and uses thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2732531A1 (de) * 1977-07-19 1979-02-01 Hoechst Ag Imidazolcarbonsaeuren und deren derivate
US4835154A (en) * 1987-06-01 1989-05-30 Smithkline Beckman Corporation 1-aralykyl-5-piperazinylmethyl-2-mercaptoimidazoles and 2-alkylthioimidazoles and their use as dopamine-βhydroxylase inhibitors
US5053543A (en) * 1990-11-28 1991-10-01 Glaxo Inc. Synthesis of 2-aminobenzophenones
US5136085A (en) * 1990-11-28 1992-08-04 Glaxo Inc. Synthesis of 2-aminobenzophenones
TW349948B (en) 1995-10-31 1999-01-11 Janssen Pharmaceutica Nv Farnesyl transferase inhibiting 2-quinolone derivatives
AU711142B2 (en) * 1995-12-08 1999-10-07 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibiting (imidazol-5-YL)methyl-2-quinolinone derivatives
EP0988038B1 (en) * 1997-06-02 2002-08-14 Janssen Pharmaceutica N.V. (imidazol-5-yl)methyl-2-quinolinone derivatives as inhibitors of smooth muscle cell proliferation
GEP20033001B (en) 1998-08-27 2003-06-25 Pfizer Prod Inc Alkynyl-Substituted Quinolin-2-One Derivatives Useful As Anticancer Agents
HUP0105231A3 (en) * 1999-02-11 2003-01-28 Pfizer Prod Inc Heteroaryl-substituted quinolin-2-one derivatives useful as anticancer agents and medicaments containing the compounds

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