AR040500A1 - Inhibidores de cinasas - Google Patents

Inhibidores de cinasas

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Publication number
AR040500A1
AR040500A1 AR20030102587A ARP030102587A AR040500A1 AR 040500 A1 AR040500 A1 AR 040500A1 AR 20030102587 A AR20030102587 A AR 20030102587A AR P030102587 A ARP030102587 A AR P030102587A AR 040500 A1 AR040500 A1 AR 040500A1
Authority
AR
Argentina
Prior art keywords
substituted
heterocycle
aryl
alkyl
hydrogen
Prior art date
Application number
AR20030102587A
Other languages
English (en)
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR040500A1 publication Critical patent/AR040500A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
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    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/22—Antivirals for DNA viruses for herpes viruses
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Reivindicación 1: Un compuesto de la fórmula en donde: Z es seleccionado del grupo que consiste de O, S, N, OH, y Cl, con la condición que cuando Z es O u S, R41 está ausente, y cuando Z es OH o Cl, ambos R41 y R42 están ausentes, y cuando Z es N, entonces R41 es H; X e Y son independientemente seleccionados del grupo que consiste de O, OCO; S; SO, SO2, CO, CO2, NR10, NR11CO, NR12CONR13, NR14CO2, NR15SO2, NR16SO2NR17, SO2NR18, CONR19, halógeno, nitro y ciano, o X o Y están ausentes; R1 es hidrógeno, CH3, OH, OCH3, SH, SCH3, OCOR21, SOR22, SO2R23, SO2NR24R25, CO2R26, CONR27R28, NH2, NR29SO2NR30R31, NR32SO2R33, NR34COR35, NR36CO2R37, NR38CONR39R40, halógeno, nitro, o ciano; R2 y R3 son independientemente hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, arilo sustituido, heterociclo, heterociclo sustituido, aralquilo, aralquilo sustituido, heteroarilo, heteroarilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido; con la condición que cuando X es halo, nitro o ciano, R2 está ausente, y, cuando Y es halo, nitro o ciano, R3 está ausente; R6 es H, alquilo, alquilo sustituido, arilo, arilo sustituido, heterociclo, heterociclo sustituido, NR7R8, OR9 o halógeno; R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R21, R24, R25, R26, R27, R28, R29, R30, R31, R32, R34, R35, R36, R38, R39 y R40 son independientemente seleccionados del grupo que consiste de hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclo, o heterociclo sustituido; R22, R23, R33 y R37 son independientemente seleccionados del grupo que consiste de alquilo, alquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclo, o heterociclo sustituido; R42 es la fórmula (2) en donde: (R43)n en donde n es igual a 0, 1 ó 2 y cada R43 está independientemente seleccionado del grupo que consiste de hidrógeno, flúor, cloro y metilo; y R44 es metilo, o hidrógeno, con la condición adicional que: a) R2 no puede ser hidrógeno si X es SO, SO2, NR13CO2, o NR14SO2; y b) R3 no puede ser hidrógeno si Y es SO, SO2, NR13CO2, o NR14SO2; o un enantiómero, diaestereómero, o sal, profármaco, o solvato farmacéuticamente aceptable del mismo. Reivindicación 7: Una composición farmacéutica, que comprende al menos uno de los compuestos de la reivindicación 1 y un portador farmacéuticamente aceptable del mismo. Reivindicación 10: Una composición farmacéutica, que comprende al menos uno o más compuestos de la reivindicación 1 en combinación con un portador farmacéuticamente aceptable y al menos un agente anti-cáncer o citotóxico adicional. Reivindicación 14: Un método para producir un efecto antiangiogénico, que comprende administrar a una especie de mamífero que necesita del mismo, una cantidad efectiva que produce un antiangiogénico de al menos uno de los compuestos de conformidad con la reivindicación 1. Reivindicación 26: Un método para el tratamiento de enfermedades asociadas con las trayectorias de transducción de senal que operan a través de los receptores del factor de crecimiento, que comprende administrar a una especie de mamífero que necesita del mismo, una cantidad terapéuticamente efectiva de al menos uno de los compuestos de conformidad con la reivindicación 1.
AR20030102587A 2002-07-19 2003-07-18 Inhibidores de cinasas AR040500A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39725602P 2002-07-19 2002-07-19
US44721303P 2003-02-13 2003-02-13

Publications (1)

Publication Number Publication Date
AR040500A1 true AR040500A1 (es) 2005-04-06

Family

ID=30773005

Family Applications (1)

Application Number Title Priority Date Filing Date
AR20030102587A AR040500A1 (es) 2002-07-19 2003-07-18 Inhibidores de cinasas

Country Status (33)

Country Link
US (6) US6869952B2 (es)
EP (3) EP2280012A3 (es)
JP (2) JP4381978B2 (es)
KR (1) KR100901939B1 (es)
CN (3) CN1315833C (es)
AR (1) AR040500A1 (es)
AT (2) ATE505471T1 (es)
AU (2) AU2003254088B2 (es)
BR (2) BRPI0312940B1 (es)
CA (2) CA2492665A1 (es)
CO (1) CO5680407A2 (es)
CY (1) CY1112628T1 (es)
DE (1) DE60336732D1 (es)
DK (1) DK1534290T3 (es)
ES (1) ES2377963T3 (es)
GE (2) GEP20074124B (es)
HK (1) HK1072545A1 (es)
HR (2) HRP20050059B8 (es)
IL (3) IL166129A0 (es)
IS (2) IS7646A (es)
MX (2) MXPA05000715A (es)
MY (1) MY134848A (es)
NO (2) NO330132B1 (es)
NZ (1) NZ537523A (es)
PE (1) PE20040680A1 (es)
PL (2) PL216663B1 (es)
PT (1) PT1534290E (es)
RS (2) RS52325B (es)
RU (2) RU2005104818A (es)
SI (1) SI1534290T1 (es)
TW (1) TWI329112B (es)
UA (1) UA82846C2 (es)
WO (2) WO2004009601A1 (es)

Families Citing this family (192)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4579351B2 (ja) * 1996-12-03 2010-11-10 スローン−ケッタリング インスティトュート フォア キャンサー リサーチ エポチロンの合成とその中間体及びその類似物並びにその使用
DE69734871D1 (de) * 1997-05-30 2006-01-19 St Microelectronics Srl Verfahren zur Herstellung eines Germanium-implantierten bipolaren Heteroübergangtransistors
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
US6982265B1 (en) * 1999-05-21 2006-01-03 Bristol Myers Squibb Company Pyrrolotriazine inhibitors of kinases
US6670357B2 (en) * 2000-11-17 2003-12-30 Bristol-Myers Squibb Company Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors
US6867300B2 (en) * 2000-11-17 2005-03-15 Bristol-Myers Squibb Company Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors
TW200300350A (en) * 2001-11-14 2003-06-01 Bristol Myers Squibb Co C-5 modified indazolylpyrrolotriazines
TW200306841A (en) 2002-04-23 2003-12-01 Bristol Myers Squibb Co Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors
AU2003231034B2 (en) * 2002-04-23 2009-03-05 Bristol-Myers Squibb Company Pyrrolo-triazine aniline compounds useful as kinase inhibitors
TW200401638A (en) * 2002-06-20 2004-02-01 Bristol Myers Squibb Co Heterocyclic inhibitors of kinases
TWI329112B (en) * 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
MXPA05002113A (es) * 2002-08-23 2005-06-03 Sloan Kettering Inst Cancer Sintesis de epotilonas, intermediarios para ellas, analogos y usos de los mismos.
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
TW200420565A (en) 2002-12-13 2004-10-16 Bristol Myers Squibb Co C-6 modified indazolylpyrrolotriazines
CA2515218A1 (en) 2003-02-05 2004-08-26 Bristol-Myers Squibb Company Process for preparing pyrrolotriazine kinase inhibitors
JP5105874B2 (ja) 2003-07-18 2012-12-26 アムジエン・インコーポレーテツド 肝細胞増殖因子に対する特異的結合因子
US7102001B2 (en) 2003-12-12 2006-09-05 Bristol-Myers Squibb Company Process for preparing pyrrolotriazine
US20060014741A1 (en) * 2003-12-12 2006-01-19 Dimarco John D Synthetic process, and crystalline forms of a pyrrolotriazine compound
MY145634A (en) 2003-12-29 2012-03-15 Bristol Myers Squibb Co Pyrrolotriazine compounds as kinase inhibitors
US7064203B2 (en) * 2003-12-29 2006-06-20 Bristol Myers Squibb Company Di-substituted pyrrolotriazine compounds
US7459562B2 (en) * 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
TW200538453A (en) * 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
US7102002B2 (en) * 2004-06-16 2006-09-05 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
US7173031B2 (en) * 2004-06-28 2007-02-06 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US7432373B2 (en) * 2004-06-28 2008-10-07 Bristol-Meyers Squibb Company Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors
CN100577663C (zh) * 2004-06-28 2010-01-06 布里斯托尔-迈尔斯·斯奎布公司 稠合杂环型激酶抑制剂
US7439246B2 (en) * 2004-06-28 2008-10-21 Bristol-Myers Squibb Company Fused heterocyclic kinase inhibitors
TW200600513A (en) 2004-06-30 2006-01-01 Bristol Myers Squibb Co A method for preparing pyrrolotriazine compounds
US7253167B2 (en) * 2004-06-30 2007-08-07 Bristol-Myers Squibb Company Tricyclic-heteroaryl compounds useful as kinase inhibitors
US7102003B2 (en) * 2004-07-01 2006-09-05 Bristol-Myers Squibb Company Pyrrolotriazine compounds
SE0401790D0 (sv) * 2004-07-07 2004-07-07 Forskarpatent I Syd Ab Tamoxifen response in pre- and postmenopausal breast cancer patients
US7504521B2 (en) * 2004-08-05 2009-03-17 Bristol-Myers Squibb Co. Methods for the preparation of pyrrolotriazine compounds
PE20060421A1 (es) 2004-08-12 2006-06-01 Bristol Myers Squibb Co Procedimiento para preparar un compuesto de pirrolotriazina anilina como inhibidores de cinasa
US7151176B2 (en) 2004-10-21 2006-12-19 Bristol-Myers Squibb Company Pyrrolotriazine compounds
AU2005312048B2 (en) 2004-11-30 2012-08-02 Amgen Inc. Quinolines and quinazoline analogs and their use as medicaments for treating cancer
DE102004060659A1 (de) 2004-12-15 2006-07-06 Lanxess Deutschland Gmbh Neue substituierte 1H-Pyrrolo[2,3-b]pyridine und deren Herstellung
US7534882B2 (en) 2005-04-06 2009-05-19 Bristol-Myers Squibb Company Method for preparing pyrrolotriazine compounds via in situ amination of pyrroles
US20060257400A1 (en) * 2005-05-13 2006-11-16 Bristol-Myers Squibb Company Combination therapy
JP2008545652A (ja) 2005-05-17 2008-12-18 プレキシコン，インコーポレーテッド ｃ−ｋｉｔおよびｃ−ｆｍｓ活性を調節する化合物およびその用途
WO2006130657A2 (en) * 2005-05-31 2006-12-07 Bristol-Myers Squibb Company Stereoselective reduction process for the preparation of pyrrolotriazine compounds
US20060288309A1 (en) * 2005-06-16 2006-12-21 Cross Charles W Jr Displaying available menu choices in a multimodal browser
NZ565255A (en) 2005-06-22 2010-04-30 Plexxikon Inc Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors
US7402582B2 (en) * 2005-07-01 2008-07-22 Bristol-Myers Squibb Company Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith
US7405213B2 (en) * 2005-07-01 2008-07-29 Bristol-Myers Squibb Company Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith
US7442700B2 (en) * 2005-07-01 2008-10-28 Bristol-Myers Squibb Company Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith
EP2182078B1 (en) 2005-09-01 2012-02-01 Bristol-Myers Squibb Company Biomarkers and methods for determining sensitivity to vascular endothelial growth factor receptor-2 modulators
WO2007038648A1 (en) * 2005-09-27 2007-04-05 Bristol-Myers Squibb Company Crystalline forms of [(1r), 2s]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1h-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester
US7547782B2 (en) * 2005-09-30 2009-06-16 Bristol-Myers Squibb Company Met kinase inhibitors
US7514435B2 (en) * 2005-11-18 2009-04-07 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
PE20070855A1 (es) 2005-12-02 2007-10-14 Bayer Pharmaceuticals Corp Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas
CA2631741C (en) 2005-12-02 2014-01-28 Bayer Healthcare Llc Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
US20080108664A1 (en) 2005-12-23 2008-05-08 Liu Belle B Solid-state form of AMG 706 and pharmaceutical compositions thereof
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)
ES2353482T3 (es) 2006-02-10 2011-03-02 Amgen, Inc Formas hidrato de amg706.
US8063208B2 (en) 2006-02-16 2011-11-22 Bristol-Myers Squibb Company Crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol
MX2008011136A (es) 2006-03-07 2008-09-08 Squibb Bristol Myers Co Compuestos de profamarco de pirrolotriazina anilina utiles como inhibidores de cinasa.
PT2010538E (pt) * 2006-04-21 2013-02-22 Bristol Myers Squibb Co Processo para a preparação de éster 2-[4-(4-fluoro-2- metil-1h-indol-5-iloxi)-5-metilpirrolo[2,1-f][1,2,4]- triazin-6-iloxi]-1 -metiletílico do ácido [(1r), 2s]-2- aminopropiónico
ES2427924T3 (es) 2006-06-30 2013-11-04 Merck Sharp & Dohme Corp. Biomarcador IGFBP2
EA018322B1 (ru) * 2006-07-07 2013-07-30 Бристол-Маерс Сквибб Компани ПРОИЗВОДНЫЕ ПИРРОЛО[1,2-f][1,2,4]ТРИАЗИНА
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
US7605160B2 (en) * 2006-08-09 2009-10-20 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US7531539B2 (en) * 2006-08-09 2009-05-12 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
CL2007003158A1 (es) * 2006-11-02 2008-05-16 Astrazeneca Ab Procedimiento de preparacion de compuestos derivados de quinazolina o sus sales farmaceuticamente aceptables; compuestos intermediarios; procedimiento de preparacion.
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
WO2008079291A2 (en) 2006-12-20 2008-07-03 Amgen Inc. Substituted heterocycles and methods of use
US7872018B2 (en) 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
US7851500B2 (en) 2007-01-05 2010-12-14 Bristol-Myers Squibb Company Aminopyrazole kinase inhibitors
CA2673652A1 (en) 2007-01-09 2008-07-17 Amgen Inc. Bis-aryl amide derivatives and methods of use
CN101627116B (zh) 2007-02-08 2013-07-10 科德克希思公司 酮还原酶及其用途
EP2114898A2 (en) 2007-02-16 2009-11-11 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors
WO2008127526A2 (en) * 2007-03-12 2008-10-23 Bristol-Myers Squibb Company Biomarkers and methods for determining sensitivity to vascular endothelial growth factor receptor-2 modulators
WO2008128008A2 (en) 2007-04-13 2008-10-23 Bristol-Myers Squibb Company Biomarkers and methods for determining sensitivity to vascular endothelial growth factor receptor-2 modulators
US8198438B2 (en) * 2007-04-18 2012-06-12 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
TW200902019A (en) * 2007-04-26 2009-01-16 Ono Pharmaceutical Co Dicyclic heterocyclic compound
US20100190777A1 (en) 2007-07-17 2010-07-29 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
RS56743B1 (sr) 2007-08-21 2018-03-30 Amgen Inc Humani c-fms antigen vezujući proteini
EP2212432A4 (en) 2007-10-22 2011-10-19 Schering Corp COMPLETELY HUMAN ANTI-VEGF ANTIBODIES AND USE PROCEDURES
US20110086850A1 (en) * 2008-04-11 2011-04-14 Board Of Regents, The University Of Texas System Radiosensitization of tumors with indazolpyrrolotriazines for radiotherapy
AR071717A1 (es) * 2008-05-13 2010-07-07 Array Biopharma Inc Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer.
AR074830A1 (es) 2008-12-19 2011-02-16 Cephalon Inc Pirrolotriazinas como inhibidores de alk y jak2
WO2010099139A2 (en) 2009-02-25 2010-09-02 Osi Pharmaceuticals, Inc. Combination anti-cancer therapy
WO2010099364A2 (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
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
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
EP2414356B1 (en) 2009-04-03 2015-09-02 F.Hoffmann-La Roche Ag Propane-i-sulfonic acid {3-[5-(4-chloro-phenyl)-1h-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide compositions and uses thereof
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
JP2013506687A (ja) 2009-09-30 2013-02-28 プレジデント アンド フェロウズ オブ ハーバード カレッジ オートファジー促進遺伝子産物の変調によりオートファジーを変調する方法
WO2011044019A1 (en) * 2009-10-05 2011-04-14 Bristol-Myers Squibb Company (R)-1-(4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TRIAZIN-6-YLOXY)PROPAN-2-OL METABOLITES
MX2012005284A (es) 2009-11-06 2012-06-28 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas. e indicaciones para ello.
US20120258940A1 (en) 2009-12-18 2012-10-11 Giordano Caponigro Method for treating haematological cancers
CA2784807C (en) * 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
US8691981B2 (en) * 2010-02-03 2014-04-08 Bristol-Myers Squibb Company Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide
JP5093527B2 (ja) * 2010-02-10 2012-12-12 日本電気株式会社 複合光導波路、波長可変フィルタ、波長可変レーザ、および光集積回路
WO2011161217A2 (en) 2010-06-23 2011-12-29 Palacký University in Olomouc Targeting of vegfr2
US20130178517A1 (en) * 2010-07-09 2013-07-11 Richard L. Atkinson Methods And Compositions For Treatment Of Lipogenic Virus Related Conditions
US8338771B2 (en) * 2010-11-05 2012-12-25 Green Plus Co., Ltd. Apparatus for tracking and condensing sunlight of sliding type
AU2012214762B2 (en) 2011-02-07 2015-08-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
TWI558702B (zh) 2011-02-21 2016-11-21 普雷辛肯公司 醫藥活性物質的固態形式
AU2012230896B9 (en) 2011-03-23 2015-06-18 Amgen Inc. Fused tricyclic dual inhibitors of CDK 4/6 and FLT3
JP2014519813A (ja) 2011-04-25 2014-08-21 オーエスアイ・ファーマシューティカルズ，エルエルシー 癌薬剤発見、診断、および治療におけるｅｍｔ遺伝子シグネチャーの使用
US8921533B2 (en) 2011-07-25 2014-12-30 Chromatin Technologies Glycosylated valproic acid analogs and uses thereof
US9745288B2 (en) 2011-08-16 2017-08-29 Indiana University Research And Technology Corporation Compounds and methods for treating cancer by inhibiting the urokinase receptor
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
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
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
CN103450204B (zh) 2012-05-31 2016-08-17 中国科学院上海药物研究所 吡咯[2，1-f][1，2，4]并三嗪类化合物，其制备方法及用途
US9724352B2 (en) 2012-05-31 2017-08-08 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Pyrrolo[2,1-F[1,2,4]triazine compounds, preparation methods and applications thereof
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
CN102675323B (zh) * 2012-06-01 2014-04-09 南京药石药物研发有限公司 吡咯并[2,1-f][1,2,4]三嗪衍生物及其抗肿瘤用途
EP2890696A1 (en) 2012-08-29 2015-07-08 Amgen, Inc. Quinazolinone compounds and derivatives thereof
CN103664957A (zh) * 2012-09-25 2014-03-26 杨子娇 一类治疗房角狭窄的化合物及其用途
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
FR3000494B1 (fr) * 2012-12-28 2015-08-21 Oribase Pharma Nouveaux derives d'azaindoles en tant qu'inhibiteurs de proteines kinases
US9050345B2 (en) 2013-03-11 2015-06-09 Bristol-Myers Squibb Company Pyrrolotriazines as potassium ion channel inhibitors
ES2638317T3 (es) 2013-04-04 2017-10-19 Janssen Pharmaceutica Nv Nuevos derivados de N-(2,3-dihidro-1H-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina y N-(2,3-dihidro-1H-indol-5-il)-4-quinazolinamina como inhibidores de PERK
US10150728B2 (en) 2013-10-17 2018-12-11 Shionogi & Co., Ltd. Alkylene derivatives
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
CN104725381B (zh) * 2013-12-19 2018-04-10 南京圣和药业股份有限公司 生长因子受体抑制剂及其应用
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
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
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107517589A (zh) 2015-01-08 2017-12-26 小利兰·斯坦福大学托管委员会 提供骨、骨髓及软骨的诱导的因子和细胞
WO2016160617A2 (en) 2015-03-27 2016-10-06 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. ASSOCIATION THERAPY USING TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS
US11142507B2 (en) 2015-09-09 2021-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
JP6896715B2 (ja) 2015-09-30 2021-06-30 マックス−プランク−ゲゼルシャフト ツール フェルデルング デル ヴィッセンシャフテン エーファウ −ジェネラルフェルヴァルトゥング セピアプテリン還元酵素としてのヘテロアリール誘導体
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
KR20220110859A (ko) 2016-03-04 2022-08-09 다이호야쿠힌고교 가부시키가이샤 악성 종양 치료용 제제 및 조성물
EA039529B1 (ru) 2016-04-28 2022-02-07 Такеда Фармасьютикал Компани Лимитед Конденсированные гетероциклические соединения
BR112019012335A2 (pt) * 2016-12-16 2020-03-03 Cystic Fibrosis Foundation Therapeutics, Inc. Derivados de heteroarila bicíclica como potenciadores de cftr
MX2019007643A (es) 2016-12-22 2019-09-09 Amgen Inc Benzoisotiazol, isotiazolo[3,4-b]piridina, quinazolina, ftalazina, pirido[2,3-d]piridazina y derivados de pirido[2,3-d]pirimidina como inhibirores de kras g12c para tratar el cancer de pulmon, pancreatico o colorrectal.
WO2018121650A1 (zh) * 2016-12-29 2018-07-05 南京明德新药研发股份有限公司 Fgfr抑制剂
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
SG11202001499WA (en) 2017-09-08 2020-03-30 Amgen Inc Inhibitors of kras g12c and methods of using the same
JP6918204B2 (ja) 2018-03-19 2021-08-11 大鵬薬品工業株式会社 アルキル硫酸ナトリウムを含む医薬組成物
US11090304B2 (en) 2018-05-04 2021-08-17 Amgen Inc. KRAS G12C inhibitors and methods of using the same
US11045484B2 (en) 2018-05-04 2021-06-29 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7361720B2 (ja) 2018-05-10 2023-10-16 アムジエン・インコーポレーテツド がんの治療のためのｋｒａｓ ｇ１２ｃ阻害剤
MX2020012731A (es) 2018-06-01 2021-02-22 Amgen Inc Inhibidores de kras g12c y metodos para su uso.
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
MX2020012261A (es) 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
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
JP7454572B2 (ja) 2018-11-19 2024-03-22 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤及びその使用方法
CA3123227A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
MA54550A (fr) 2018-12-20 2022-03-30 Amgen Inc Inhibiteurs de kif18a
JP7407196B2 (ja) 2018-12-20 2023-12-28 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤
MA54547A (fr) 2018-12-20 2022-03-30 Amgen Inc Amides d'hétéroaryle utiles en tant qu'inhibiteurs de kif18a
JPWO2020130125A1 (ja) 2018-12-21 2021-11-04 第一三共株式会社 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
US20230096028A1 (en) 2019-03-01 2023-03-30 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
KR20210146287A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로아릴 화합물 및 이의 용도
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
WO2020236947A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
JP2022542392A (ja) 2019-08-02 2022-10-03 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤としてのピリジン誘導体
MX2022001296A (es) 2019-08-02 2022-02-22 Amgen Inc Inhibidores de kif18a.
EP4007756A1 (en) 2019-08-02 2022-06-08 Amgen Inc. Kif18a inhibitors
CN114302880A (zh) 2019-08-02 2022-04-08 美国安进公司 Kif18a抑制剂
JP2022552873A (ja) 2019-10-24 2022-12-20 アムジエン・インコーポレーテツド がんの治療におけるｋｒａｓ ｇ１２ｃ及びｋｒａｓ ｇ１２ｄ阻害剤として有用なピリドピリミジン誘導体
KR20220109407A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
JP2022553858A (ja) 2019-11-04 2022-12-26 レボリューション メディシンズ インコーポレイテッド Ｒａｓ阻害剤
KR20220109406A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
EP4055017A1 (en) 2019-11-08 2022-09-14 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
WO2021094209A1 (en) 2019-11-12 2021-05-20 Bayer Aktiengesellschaft Substituted pyrrolo triazine carboxamide derivatives as prostaglandin ep3 receptor antagonists
AR120457A1 (es) 2019-11-14 2022-02-16 Amgen Inc Síntesis mejorada del compuesto inhibidor de g12c de kras
TW202132271A (zh) 2019-11-14 2021-09-01 美商安進公司 Ｋｒａｓ ｇ１２ｃ抑制劑化合物之改善的合成
AU2020387982B2 (en) 2019-11-18 2023-08-03 Jumbo Drug Bank Co., Ltd. Pyrrolotriazine compounds acting as MNK inhibitor
CN114980976A (zh) 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
TW202140011A (zh) 2020-01-07 2021-11-01 美商銳新醫藥公司 Shp2抑制劑給藥和治療癌症的方法
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
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
TW202227460A (zh) 2020-09-15 2022-07-16 美商銳新醫藥公司 Ｒａｓ抑制劑
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
US20220396589A1 (en) 2021-05-05 2022-12-15 Revolution Medicines, Inc. Ras inhibitors
AR125782A1 (es) 2021-05-05 2023-08-16 Revolution Medicines Inc Inhibidores de ras
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023081923A1 (en) 2021-11-08 2023-05-11 Frequency Therapeutics, Inc. Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
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
WO2023196975A1 (en) * 2022-04-08 2023-10-12 Shy Therapeutics, Llc Compounds that interact with ras superfamily proteins for treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
WO2023228095A1 (en) 2022-05-24 2023-11-30 Daiichi Sankyo Company, Limited Dosage regimen of an anti-cdh6 antibody-drug conjugate
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024081916A1 (en) 2022-10-14 2024-04-18 Black Diamond Therapeutics, Inc. Methods of treating cancers using isoquinoline or 6-aza-quinoline derivatives

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL204437B1 (pl) * 1999-05-21 2010-01-29 Bristol Myers Squibb Co Pochodna pirolotriazyny i jej zastosowanie oraz kompozycja farmaceutyczna i jej zastosowanie
US6982265B1 (en) * 1999-05-21 2006-01-03 Bristol Myers Squibb Company Pyrrolotriazine inhibitors of kinases
US6787545B1 (en) * 1999-08-23 2004-09-07 Shiongi & Co., Ltd. Pyrrolotriazine derivatives having spla2-inhibitory activities
GB0017256D0 (en) * 2000-07-13 2000-08-30 Merck Sharp & Dohme Therapeutic agents
EP1311500A2 (en) * 2000-08-09 2003-05-21 AstraZeneca AB Indole, azaindole and indazole derivatives having vegf inhibiting activity
ES2259051T3 (es) * 2000-11-17 2006-09-16 Bristol-Myers Squibb Company Procedimientos para el tratamiento de dolencias asociadas a la quinasa p38 y compuestos de pirrolotriacina utiles como inhibidores de quinasa.
US6867300B2 (en) * 2000-11-17 2005-03-15 Bristol-Myers Squibb Company Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors
US6670357B2 (en) 2000-11-17 2003-12-30 Bristol-Myers Squibb Company Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors
TW200300350A (en) * 2001-11-14 2003-06-01 Bristol Myers Squibb Co C-5 modified indazolylpyrrolotriazines
TW200306841A (en) * 2002-04-23 2003-12-01 Bristol Myers Squibb Co Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors
AU2003231034B2 (en) * 2002-04-23 2009-03-05 Bristol-Myers Squibb Company Pyrrolo-triazine aniline compounds useful as kinase inhibitors
TW200400034A (en) * 2002-05-20 2004-01-01 Bristol Myers Squibb Co Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
TW200407143A (en) * 2002-05-21 2004-05-16 Bristol Myers Squibb Co Pyrrolotriazinone compounds and their use to treat diseases
TWI272271B (en) * 2002-07-19 2007-02-01 Bristol Myers Squibb Co Process for preparing certain pyrrolotriazine compounds
TWI329112B (en) * 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
EP1543009A4 (en) * 2002-08-02 2007-08-08 Bristol Myers Squibb Co Pyrrolotriazine KINASE INHIBITORS
TW200420565A (en) * 2002-12-13 2004-10-16 Bristol Myers Squibb Co C-6 modified indazolylpyrrolotriazines
CA2515218A1 (en) * 2003-02-05 2004-08-26 Bristol-Myers Squibb Company Process for preparing pyrrolotriazine kinase inhibitors

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