WO2004009784A3 - Novel inhibitors of kinases - Google Patents

Novel inhibitors of kinases Download PDF

Info

Publication number
WO2004009784A3
WO2004009784A3 PCT/US2003/022826 US0322826W WO2004009784A3 WO 2004009784 A3 WO2004009784 A3 WO 2004009784A3 US 0322826 W US0322826 W US 0322826W WO 2004009784 A3 WO2004009784 A3 WO 2004009784A3
Authority
WO
WIPO (PCT)
Prior art keywords
formula
kinases
compounds
useful
growth factor
Prior art date
Application number
PCT/US2003/022826
Other languages
French (fr)
Other versions
WO2004009784A2 (en
Inventor
Rajeev Bhide
Zhen-Wei Cai
Ligang Qian
Stephanie Barbosa
Original Assignee
Bristol Myers Squibb Co
Rajeev Bhide
Zhen-Wei Cai
Ligang Qian
Stephanie Barbosa
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
Priority to CA002492804A priority Critical patent/CA2492804C/en
Priority to NZ537523A priority patent/NZ537523A/en
Application filed by Bristol Myers Squibb Co, Rajeev Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa filed Critical Bristol Myers Squibb Co
Priority to DK03765881.2T priority patent/DK1534290T3/en
Priority to UAA200501515A priority patent/UA82846C2/en
Priority to CN038219158A priority patent/CN1681508B/en
Priority to MXPA05000715A priority patent/MXPA05000715A/en
Priority to EP03765881A priority patent/EP1534290B1/en
Priority to IL16612903A priority patent/IL166129A0/en
Priority to SI200332120T priority patent/SI1534290T1/en
Priority to YU20050042A priority patent/RS52325B/en
Priority to ES03765881T priority patent/ES2377963T3/en
Priority to JP2004523256A priority patent/JP4361485B2/en
Priority to AU2003254088A priority patent/AU2003254088B2/en
Priority to AT03765881T priority patent/ATE537843T1/en
Priority to BRPI0312940-3A priority patent/BRPI0312940B1/en
Publication of WO2004009784A2 publication Critical patent/WO2004009784A2/en
Publication of WO2004009784A3 publication Critical patent/WO2004009784A3/en
Priority to IL166129A priority patent/IL166129A/en
Priority to NO20050072A priority patent/NO330132B1/en
Priority to IS7647A priority patent/IS2880B/en
Priority to HRP20050059A priority patent/HRP20050059B8/en
Priority to HK05105257.2A priority patent/HK1072545A1/en

Links

Classifications

    • 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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
PCT/US2003/022826 2002-07-19 2003-07-18 Novel inhibitors of kinases WO2004009784A2 (en)

Priority Applications (20)

Application Number Priority Date Filing Date Title
ES03765881T ES2377963T3 (en) 2002-07-19 2003-07-18 New kinase inhibitors
YU20050042A RS52325B (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases
DK03765881.2T DK1534290T3 (en) 2002-07-19 2003-07-18 New kinase inhibitors
UAA200501515A UA82846C2 (en) 2002-07-19 2003-07-18 Inhibitors of kinases, pharmaceutical composition based thereon (variants) and method for treatment of diseases (variants)
CN038219158A CN1681508B (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases
MXPA05000715A MXPA05000715A (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases.
EP03765881A EP1534290B1 (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases
IL16612903A IL166129A0 (en) 2002-07-19 2003-07-18 Pyrrolotriazine derivatives and pharmaceutical compositions containing the same
JP2004523256A JP4361485B2 (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases
CA002492804A CA2492804C (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases
SI200332120T SI1534290T1 (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases
NZ537523A NZ537523A (en) 2002-07-19 2003-07-18 Pyrrolo-triazine compounds that inhibit the tyrosine kinase activity of growth factor receptors
AU2003254088A AU2003254088B2 (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases
AT03765881T ATE537843T1 (en) 2002-07-19 2003-07-18 NEW KINASE INHIBITORS
BRPI0312940-3A BRPI0312940B1 (en) 2002-07-19 2003-07-18 KINASE INHIBITORS, COMPOSITION AND USE OF THE SAME.
IL166129A IL166129A (en) 2002-07-19 2005-01-03 5-(1h-indolyloxy)-pyrrolo[2,1-f][1,2,4]triazine derivatives and pharmaceutical compositions containing the same
NO20050072A NO330132B1 (en) 2002-07-19 2005-01-06 Triazine compounds, pharmaceutical compositions comprising such, such compounds for use as a medicament and the use thereof for the manufacture of pharmaceutical preparations for the treatment of disease
IS7647A IS2880B (en) 2002-07-19 2005-01-12 New Chinese cinemas
HRP20050059A HRP20050059B8 (en) 2002-07-19 2005-01-19 Novel inhibitors of kinases
HK05105257.2A HK1072545A1 (en) 2002-07-19 2005-06-23 Novel inhibitors of kinases

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US39725602P 2002-07-19 2002-07-19
US60/397,256 2002-07-19
US44721303P 2003-02-13 2003-02-13
US60/447,213 2003-02-13

Publications (2)

Publication Number Publication Date
WO2004009784A2 WO2004009784A2 (en) 2004-01-29
WO2004009784A3 true WO2004009784A3 (en) 2004-04-22

Family

ID=30773005

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2003/022554 WO2004009601A1 (en) 2002-07-19 2003-07-18 Azaindole kinase inhibitors
PCT/US2003/022826 WO2004009784A2 (en) 2002-07-19 2003-07-18 Novel inhibitors of kinases

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PCT/US2003/022554 WO2004009601A1 (en) 2002-07-19 2003-07-18 Azaindole kinase inhibitors

Country Status (33)

Country Link
US (6) US6969717B2 (en)
EP (3) EP1539763B1 (en)
JP (2) JP4361485B2 (en)
KR (1) KR100901939B1 (en)
CN (3) CN1681508B (en)
AR (1) AR040500A1 (en)
AT (2) ATE505471T1 (en)
AU (2) AU2003254088B2 (en)
BR (2) BR0312801A (en)
CA (2) CA2492804C (en)
CO (1) CO5680407A2 (en)
CY (1) CY1112628T1 (en)
DE (1) DE60336732D1 (en)
DK (1) DK1534290T3 (en)
ES (1) ES2377963T3 (en)
GE (2) GEP20074213B (en)
HK (1) HK1072545A1 (en)
HR (2) HRP20050059B8 (en)
IL (3) IL166129A0 (en)
IS (2) IS2880B (en)
MX (2) MXPA05000716A (en)
MY (1) MY134848A (en)
NO (2) NO330132B1 (en)
NZ (1) NZ537523A (en)
PE (1) PE20040680A1 (en)
PL (2) PL375352A1 (en)
PT (1) PT1534290E (en)
RS (2) RS20050041A (en)
RU (2) RU2005104818A (en)
SI (1) SI1534290T1 (en)
TW (1) TWI329112B (en)
UA (1) UA82846C2 (en)
WO (2) WO2004009601A1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102431405B1 (en) 2016-04-28 2022-08-10 다케다 야쿠힌 고교 가부시키가이샤 Condensed Heterocyclic Compounds

Families Citing this family (189)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0977563B1 (en) * 1996-12-03 2005-10-12 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
DE69734871D1 (en) * 1997-05-30 2006-01-19 St Microelectronics Srl A method of making a germanium-implanted bipolar heterojunction transistor
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
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
WO2003091229A1 (en) 2002-04-23 2003-11-06 Bristol-Myers Squibb Company Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors
PT1497019E (en) * 2002-04-23 2015-09-10 Bristol Myers Squibb Co 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
EP1767535B1 (en) * 2002-08-23 2009-12-02 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
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
MXPA05008183A (en) 2003-02-05 2005-10-05 Bristol Myers Squibb Co Process for preparing pyrrolotriazine kinase inhibitors.
TW201319088A (en) 2003-07-18 2013-05-16 Amgen Inc Specific binding agents to hepatocyte growth factor
US20060014741A1 (en) * 2003-12-12 2006-01-19 Dimarco John D Synthetic process, and crystalline forms of a pyrrolotriazine compound
US7102001B2 (en) 2003-12-12 2006-09-05 Bristol-Myers Squibb Company Process for preparing pyrrolotriazine
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 (en) * 2004-06-28 2010-01-06 布里斯托尔-迈尔斯·斯奎布公司 Fused heterocyclic kinase inhibitors
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 (en) * 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
TW200618803A (en) 2004-08-12 2006-06-16 Bristol Myers Squibb Co Process for preparing pyrrolotriazine aniline compounds useful as kinase inhibitors
US7151176B2 (en) * 2004-10-21 2006-12-19 Bristol-Myers Squibb Company Pyrrolotriazine compounds
CA2587642C (en) 2004-11-30 2013-04-09 Amgen Inc. Substituted heterocycles and methods of use
DE102004060659A1 (en) 2004-12-15 2006-07-06 Lanxess Deutschland Gmbh Novel substituted 1H-pyrrolo [2,3-b] pyridines and their preparation
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
AU2006272951A1 (en) 2005-05-17 2007-02-01 Plexxikon, Inc. Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors
US7393667B2 (en) 2005-05-31 2008-07-01 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
DK1893612T3 (en) 2005-06-22 2011-11-21 Plexxikon Inc Pyrrole [2,3-B] pyridine derivatives as protein kinase inhibitors
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
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
ES2380651T3 (en) 2005-09-01 2012-05-17 Bristol-Myers Squibb Company Biomarkers and procedures to determine the sensitivity to modulators of reciprocator 2 of vascular endothelial growth factor
EP1928880A1 (en) * 2005-09-27 2008-06-11 Brystol-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
CN101466710B (en) 2005-12-02 2013-05-29 拜尔健康护理有限责任公司 Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
PE20070855A1 (en) 2005-12-02 2007-10-14 Bayer Pharmaceuticals Corp DERIVATIVES OF 4-AMINO-PYRROLOTRIAZINE SUBSTITUTE AS KINASE INHIBITORS
US20080108664A1 (en) 2005-12-23 2008-05-08 Liu Belle B Solid-state form of AMG 706 and pharmaceutical compositions thereof
AR059066A1 (en) 2006-01-27 2008-03-12 Amgen Inc COMBINATIONS OF THE ANGIOPOYETINE INHIBITOR -2 (ANG2) AND THE VASCULAR ENDOTELIAL GROWTH FACTOR INHIBITOR (VEGF)
AU2007212696B2 (en) 2006-02-10 2011-05-19 Amgen Inc. Hydrate forms of 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
CA2645031A1 (en) 2006-03-07 2007-09-13 Bristol-Myers Squibb Company Pyrrolotriazine aniline prodrug compounds useful as kinase inhibitors
AU2007240453B2 (en) * 2006-04-21 2012-04-12 Bristol-Myers Squibb Company Process for the preparation 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
ES2427924T3 (en) 2006-06-30 2013-11-04 Merck Sharp & Dohme Corp. IGFBP2 biomarker
EP2041138B1 (en) * 2006-07-07 2014-06-25 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
PE20121506A1 (en) 2006-07-14 2012-11-26 Amgen Inc TRIAZOLOPYRIDINE COMPOUNDS AS C-MET INHIBITORS
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
WO2008021859A1 (en) * 2006-08-09 2008-02-21 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US7531539B2 (en) * 2006-08-09 2009-05-12 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US7851623B2 (en) * 2006-11-02 2010-12-14 Astrazeneca Ab Chemical process
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
PE20081581A1 (en) 2006-12-21 2008-11-12 Plexxikon Inc PIRROLO [2,3-b] PYRIDINES COMPOUNDS AS KINASE MODULATORS
EP2094701A2 (en) 2006-12-21 2009-09-02 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
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
US7759344B2 (en) 2007-01-09 2010-07-20 Amgen Inc. Bis-aryl amide derivatives and methods of use
ATE518946T1 (en) 2007-02-08 2011-08-15 Codexis Inc KETOR REDUCTASES AND USES THEREOF
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
JP2010524003A (en) 2007-04-13 2010-07-15 ブリストル−マイヤーズ スクイブ カンパニー 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
MX2010000617A (en) 2007-07-17 2010-05-17 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor.
CL2008002444A1 (en) 2007-08-21 2009-09-04 Amgen Inc Antibody or fragment thereof that binds to human c-fms protein; nucleic acid molecule that encodes it; vector and host cell; production method; pharmaceutical composition comprising it; and its use to treat or prevent a condition associated with c-fms in a patient.
CN101918579A (en) 2007-10-22 2010-12-15 先灵公司 Fully human anti-VEGF antibodies and using method
US20110086850A1 (en) * 2008-04-11 2011-04-14 Board Of Regents, The University Of Texas System Radiosensitization of tumors with indazolpyrrolotriazines for radiotherapy
CL2009001152A1 (en) 2008-05-13 2009-10-16 Array Biopharma Inc Compounds derived from n- (4- (nitrogen cycloalkyl-1-yl) -1h-pyrrolo [2,3-b] pyridin-3-yl) amide, kinase inhibitors; Preparation process; pharmaceutical composition; and its use for the treatment of a proliferative disease.
ES2539620T3 (en) 2008-12-19 2015-07-02 Cephalon, Inc. Pyrrolotriazine as an inhibitor of ALK and JAK2
JP2012518657A (en) 2009-02-25 2012-08-16 オーエスアイ・ファーマシューティカルズ，エルエルシー Combined anticancer treatment
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
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
WO2010114928A2 (en) 2009-04-03 2010-10-07 F.Hoffmann-La Roche Ag Compositions and uses thereof
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
CN102639700A (en) 2009-09-30 2012-08-15 哈佛大学校长及研究员协会 Methods for modulation of autophagy through the modulation of autophagy-enhancing gene products
US8778893B2 (en) * 2009-10-05 2014-07-15 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
NZ629615A (en) 2009-11-06 2016-01-29 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
JP2013514986A (en) * 2009-12-18 2013-05-02 ノバルティス アーゲー How to treat blood cancer
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 (en) * 2010-02-10 2012-12-12 日本電気株式会社 Composite optical waveguide, wavelength tunable filter, wavelength tunable laser, and optical integrated circuit
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
JP5941069B2 (en) 2011-02-07 2016-06-29 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． Compounds and methods for kinase regulation and indications therefor
AR085279A1 (en) 2011-02-21 2013-09-18 Plexxikon Inc SOLID FORMS OF {3- [5- (4-CHLORINE-PHENYL) -1H-PIRROLO [2,3-B] PIRIDINA-3-CARBONIL] -2,4-DIFLUOR-PHENIL} -AMIDE OF PROPANE ACID-1- SULFONIC
US8623885B2 (en) 2011-03-23 2014-01-07 Amgen Inc. Fused tricyclic dual inhibitors of CDK 4/6 and FLT3
WO2012149014A1 (en) 2011-04-25 2012-11-01 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
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
JP6106685B2 (en) 2011-11-17 2017-04-05 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Inhibitors of C-JUN-N-terminal kinase (JNK)
AR090263A1 (en) 2012-03-08 2014-10-29 Hoffmann La Roche COMBINED ANTIBODY THERAPY AGAINST HUMAN CSF-1R AND USES OF THE SAME
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
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
CN103450204B (en) 2012-05-31 2016-08-17 中国科学院上海药物研究所 Pyrroles [2,1-f] [1,2,4] triazin compound, Preparation Method And The Use
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
CN102675323B (en) * 2012-06-01 2014-04-09 南京药石药物研发有限公司 Pyrrole-[2, 1-f] [1, 2 and 4] triazine derivative and antitumor effect thereof
EP2890696A1 (en) 2012-08-29 2015-07-08 Amgen, Inc. Quinazolinone compounds and derivatives thereof
CN103664957A (en) * 2012-09-25 2014-03-26 杨子娇 Compounds for treating narrow chamber angle and application thereof
WO2014063068A1 (en) 2012-10-18 2014-04-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
FR3000494B1 (en) * 2012-12-28 2015-08-21 Oribase Pharma NOVEL AZAINDOLE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES
US9050345B2 (en) 2013-03-11 2015-06-09 Bristol-Myers Squibb Company Pyrrolotriazines as potassium ion channel inhibitors
MX367772B (en) 2013-04-04 2019-09-05 Janssen Pharmaceutica Nv Novel n-(2,3-dihydro-1h-pyrrolo[2,3-b]jpyrid in-5-yl)-4- quinazolinamine and n-(2,3-dihydro-1h-i ndol-5-yl)-4- quinazolinamine derivatives as perk inhibitors.
EP3059225A4 (en) * 2013-10-17 2017-09-06 Shionogi & Co., Ltd. Novel alkylene derivative
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
CN104725381B (en) * 2013-12-19 2018-04-10 南京圣和药业股份有限公司 Growth factor receptor inhibitor and its application
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 (en) 2015-01-08 2017-12-26 小利兰·斯坦福大学托管委员会 The factor and cell of the induction of bone, marrow and cartilage are provided
WO2016160617A2 (en) 2015-03-27 2016-10-06 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP7028766B2 (en) 2015-09-09 2022-03-02 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド Inhibitor of cyclin-dependent kinase
EP3356345B1 (en) 2015-09-30 2023-11-08 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Heteroaryl derivatives as sepiapterin reductase inhibitors
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
SG10201911076QA (en) * 2016-12-16 2020-01-30 Cystic Fibrosis Found Bycyclic heteroaryl derivatives as cftr potentiators
DK3558955T3 (en) 2016-12-22 2021-10-25 Amgen Inc BENZISOTHIAZOLE, ISOTHIAZOLO [3,4-B] PYRIDINE-, QUINAZOLINE-, PHTHALAZINE-, PYRIDO [2,3-D] PYRIDAZINE- AND PYRIDO [2,3-D] PYRIMIDINE DERIVATIVES LIKE KRAS-GANDERHINH -, PANCREAS OR COLOR RECTAL CANCER
WO2018121650A1 (en) * 2016-12-29 2018-07-05 南京明德新药研发股份有限公司 Fgfr inhibitor
JOP20190272A1 (en) 2017-05-22 2019-11-21 Amgen Inc Kras g12c inhibitors and methods of using the same
CN116003405A (en) 2017-09-08 2023-04-25 美国安进公司 Inhibitors of KRAS G12C and methods of use thereof
AU2019239404B2 (en) 2018-03-19 2021-12-23 Taiho Pharmaceutical Co., Ltd. Pharmaceutical composition including sodium alkyl sulfate
AU2019262589B2 (en) 2018-05-04 2022-07-07 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MA52496A (en) 2018-05-04 2021-03-10 Amgen Inc KRAS G12C INHIBITORS AND THEIR PROCEDURES FOR USE
WO2019217691A1 (en) 2018-05-10 2019-11-14 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
AU2019278998B2 (en) 2018-06-01 2023-11-09 Amgen Inc. KRAS G12C inhibitors and methods of using the same
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3100390A1 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer
JP2020090482A (en) 2018-11-16 2020-06-11 アムジエン・インコーポレーテツド Improved synthesis of key intermediate of kras g12c inhibitor compound
EP3883565A1 (en) 2018-11-19 2021-09-29 Amgen Inc. Kras g12c inhibitors and methods of using the same
JP7377679B2 (en) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド Combination therapy comprising a KRASG12C inhibitor and one or more additional pharmaceutically active agents for the treatment of cancer
IL283639B1 (en) 2018-12-20 2024-02-01 Amgen Inc Kif18a inhibitors
JP2022513967A (en) 2018-12-20 2022-02-09 アムジエン・インコーポレーテツド Heteroarylamide useful as a KIF18A inhibitor
ES2953821T3 (en) 2018-12-20 2023-11-16 Amgen Inc KIF18A inhibitors
JP2022513971A (en) 2018-12-20 2022-02-09 アムジエン・インコーポレーテツド Heteroarylamide useful as a KIF18A inhibitor
CN113195000A (en) 2018-12-21 2021-07-30 第一三共株式会社 Combination of antibody-drug conjugates and kinase inhibitors
KR20210146287A (en) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. Bicyclic heteroaryl compounds and uses thereof
WO2020180770A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
MX2021014126A (en) 2019-05-21 2022-01-04 Amgen Inc Solid state forms.
CA3147451A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
EP4007638A1 (en) 2019-08-02 2022-06-08 Amgen Inc. Pyridine derivatives as kif18a inhibitors
CN114401953A (en) 2019-08-02 2022-04-26 美国安进公司 KIF18A inhibitors
CN114302880A (en) 2019-08-02 2022-04-08 美国安进公司 KIF18A inhibitors
AU2020369569A1 (en) 2019-10-24 2022-04-14 Amgen Inc. Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer
TW202132314A (en) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras inhibitors
BR112022008565A2 (en) 2019-11-04 2022-08-09 Revolution Medicines Inc COMPOUND, PHARMACEUTICAL COMPOSITION, CONJUGATE, METHODS TO TREAT CANCER AND A RAS PROTEIN-RELATED DISORDER
WO2021091967A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021092115A1 (en) 2019-11-08 2021-05-14 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
EP4058432A1 (en) 2019-11-14 2022-09-21 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
US20230192681A1 (en) 2019-11-14 2023-06-22 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
AU2020387982B2 (en) 2019-11-18 2023-08-03 Jumbo Drug Bank Co., Ltd. Pyrrolotriazine compounds acting as MNK inhibitor
JP2023505100A (en) 2019-11-27 2023-02-08 レボリューション メディシンズ インコーポレイテッド Covalent RAS inhibitors and uses thereof
KR20220124768A (en) 2020-01-07 2022-09-14 레볼루션 메디슨즈, 인크. SHP2 inhibitor administration and cancer treatment method
AU2021293228A1 (en) 2020-06-18 2023-02-09 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to RAS inhibitors
KR20230081726A (en) 2020-09-03 2023-06-07 레볼루션 메디슨즈, 인크. Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
MX2023003060A (en) 2020-09-15 2023-04-05 Revolution Medicines Inc Indole derivatives as ras inhibitors in the treatment of cancer.
AR124449A1 (en) 2020-12-22 2023-03-29 Qilu Regor Therapeutics Inc SOS1 INHIBITORS AND USES THEREOF
EP4334324A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
AR125782A1 (en) 2021-05-05 2023-08-16 Revolution Medicines Inc RAS INHIBITORS
US20220396589A1 (en) 2021-05-05 2022-12-15 Revolution Medicines, Inc. Ras inhibitors
AR127308A1 (en) 2021-10-08 2024-01-10 Revolution Medicines Inc RAS INHIBITORS
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000071129A1 (en) * 1999-05-21 2000-11-30 Bristol-Myers Squibb Company Pyrrolotriazine inhibitors of kinases

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6982265B1 (en) 1999-05-21 2006-01-03 Bristol Myers Squibb Company Pyrrolotriazine inhibitors of kinases
WO2001014378A1 (en) * 1999-08-23 2001-03-01 Shionogi & 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
WO2002040486A2 (en) * 2000-11-17 2002-05-23 Bristol-Myers Squibb Company METHODS OF TREATING p38 KINASE-ASSOCIATED CONDITIONS AND 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
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
WO2003091229A1 (en) * 2002-04-23 2003-11-06 Bristol-Myers Squibb Company Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors
PT1497019E (en) * 2002-04-23 2015-09-10 Bristol Myers Squibb Co 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
TWI329112B (en) * 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
TWI272271B (en) * 2002-07-19 2007-02-01 Bristol Myers Squibb Co Process for preparing certain pyrrolotriazine compounds
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
MXPA05008183A (en) * 2003-02-05 2005-10-05 Bristol Myers Squibb Co Process for preparing pyrrolotriazine kinase inhibitors.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000071129A1 (en) * 1999-05-21 2000-11-30 Bristol-Myers Squibb Company Pyrrolotriazine inhibitors of kinases

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102431405B1 (en) 2016-04-28 2022-08-10 다케다 야쿠힌 고교 가부시키가이샤 Condensed Heterocyclic Compounds

Also Published As

Publication number Publication date
RU2005104818A (en) 2005-07-20
AU2003254088B2 (en) 2008-07-17
WO2004009601A1 (en) 2004-01-29
HRP20050059A2 (en) 2005-04-30
HRP20050058A2 (en) 2005-08-31
IS7646A (en) 2005-01-12
SI1534290T1 (en) 2012-05-31
ATE505471T1 (en) 2011-04-15
US6969717B2 (en) 2005-11-29
KR100901939B1 (en) 2009-06-10
CN101880283A (en) 2010-11-10
RU2331642C2 (en) 2008-08-20
KR20080095906A (en) 2008-10-29
US20040063707A1 (en) 2004-04-01
CA2492804C (en) 2009-06-23
TWI329112B (en) 2010-08-21
CN1681508A (en) 2005-10-12
NZ537523A (en) 2007-08-31
IS2880B (en) 2014-05-15
CA2492804A1 (en) 2004-01-29
EP1534290B1 (en) 2011-12-21
CN1681508B (en) 2010-10-06
PL375389A1 (en) 2005-11-28
CO5680407A2 (en) 2006-09-29
JP4381978B2 (en) 2009-12-09
US20070299075A1 (en) 2007-12-27
EP1539763A1 (en) 2005-06-15
GEP20074124B (en) 2007-06-11
EP1539763B1 (en) 2011-04-13
EP2280012A3 (en) 2011-05-18
US7265113B2 (en) 2007-09-04
US20050124621A1 (en) 2005-06-09
JP2005538990A (en) 2005-12-22
PT1534290E (en) 2012-03-05
JP2005538989A (en) 2005-12-22
US7521450B2 (en) 2009-04-21
CN101880283B (en) 2012-07-18
NO330132B1 (en) 2011-02-21
EP1534290A4 (en) 2006-11-29
CN1315833C (en) 2007-05-16
ATE537843T1 (en) 2012-01-15
RS52325B (en) 2012-12-31
DK1534290T3 (en) 2012-04-10
HK1072545A1 (en) 2005-09-02
CN1681818A (en) 2005-10-12
TW200412973A (en) 2004-08-01
EP2280012A2 (en) 2011-02-02
AU2003254017A1 (en) 2004-02-09
BR0312940A (en) 2005-06-21
BR0312801A (en) 2007-06-26
PL375352A1 (en) 2005-11-28
MXPA05000716A (en) 2005-04-08
AR040500A1 (en) 2005-04-06
IL166129A0 (en) 2006-01-15
US7820814B2 (en) 2010-10-26
EP1539763A4 (en) 2007-08-01
JP4361485B2 (en) 2009-11-11
PL216663B1 (en) 2014-04-30
MY134848A (en) 2007-12-31
IL166232A0 (en) 2006-01-15
US20040072832A1 (en) 2004-04-15
GEP20074213B (en) 2007-10-10
HRP20050059B1 (en) 2015-02-27
IS7647A (en) 2005-01-12
US20060058304A1 (en) 2006-03-16
CA2492665A1 (en) 2004-01-29
DE60336732D1 (en) 2011-05-26
EP1534290A2 (en) 2005-06-01
WO2004009784A2 (en) 2004-01-29
US20090170853A1 (en) 2009-07-02
HRP20050059B8 (en) 2016-03-25
ES2377963T3 (en) 2012-04-03
RS20050041A (en) 2007-06-04
PE20040680A1 (en) 2004-10-08
BRPI0312940B1 (en) 2019-07-23
MXPA05000715A (en) 2006-02-22
AU2003254088A1 (en) 2004-02-09
UA82846C2 (en) 2008-05-26
NO20050072L (en) 2005-02-03
US6869952B2 (en) 2005-03-22
NO20050417L (en) 2005-02-17
IL166129A (en) 2015-04-30
BRPI0312940B8 (en) 2021-05-25
RU2005104422A (en) 2005-08-10
CY1112628T1 (en) 2016-02-10
RS20050042A (en) 2007-06-04

Similar Documents

Publication Publication Date Title
WO2004009784A3 (en) Novel inhibitors of kinases
WO2004001059A3 (en) Heterocyclic inhibitors of kinases
WO2006007378A3 (en) Pyrrolotriazine kinase inhibitors
WO2008060907A3 (en) Pyrrolo-pyridine kinase inhibitors
CA2373990A1 (en) Pyrrolotriazine inhibitors of kinases
WO2004009542A3 (en) Process for preparing certain pyrrolotriazine compounds
WO2004054514A3 (en) C-6 modified indazolylpyrrolotriazines
UA89038C2 (en) Pyrrolotriazine compounds as kinase inhibitors
WO2003042172A3 (en) C-5 modified indazolylpyrrolotriazines
TW200613306A (en) Imidazotriazines as protein kinase inhibitors
WO2004031401A3 (en) Novel tyrosine kinases inhibitors
EP1773791A4 (en) Pyrrolotriazine compounds
YU84603A (en) Novel tyrosine kinase inhibitors
WO2008005956A3 (en) Pyrrolotriazine kinase inhibitors
MY141220A (en) Pyrazole derivatives as inhibitors of receptor tyrosine kinases
NO20090581L (en) Hydroxylated and methoxylated cyclopenta [D] pyrimidines as AKT protein kinase inhibitors
SG132683A1 (en) Imidazopyrazine tyrosine kinase inhibitors
NO20090580L (en) Cyclopenta [D] pyrimidines as AKT protein kinase inhibitors
WO2004063151A3 (en) Novel tyrosine kinase inhibitors
TW200621788A (en) Substituted thienopyrrole carboxylic acid amides, pyrrolothiazole carboxylic acid amides, and related analogs as inhibitors of casein kinase Iε
RS20060072A (en) Aminoquinoline derivatives and their use as adenosine a3 ligands
TW200621711A (en) 3-substituted-5- and 6-aminoalkyl indole-2-carboxylic acid amides and related analogs as inhibitors of casein kinase I ε
ATE421510T1 (en) COMPETITIVE ATP KINASE INHIBITORS

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 1200500195

Country of ref document: VN

Ref document number: P-2005/0042

Country of ref document: YU

AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NI NO NZ OM PG PH PL PT RO RU SC SD SE SG SK SL SY TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
WWE Wipo information: entry into national phase

Ref document number: 166129

Country of ref document: IL

WWE Wipo information: entry into national phase

Ref document number: 537523

Country of ref document: NZ

WWE Wipo information: entry into national phase

Ref document number: 78/DELNP/2005

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: PA/a/2005/000715

Country of ref document: MX

Ref document number: 2003765881

Country of ref document: EP

Ref document number: 2492804

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 2005/00492

Country of ref document: ZA

Ref document number: 375389

Country of ref document: PL

Ref document number: 2003254088

Country of ref document: AU

Ref document number: 1020057000977

Country of ref document: KR

Ref document number: 200500492

Country of ref document: ZA

WWE Wipo information: entry into national phase

Ref document number: P20050059A

Country of ref document: HR

Ref document number: 2004523256

Country of ref document: JP

Ref document number: 05003967

Country of ref document: CO

Ref document number: 05003967A

Country of ref document: CO

WWE Wipo information: entry into national phase

Ref document number: 8643

Country of ref document: GE

ENP Entry into the national phase

Ref document number: 2005104422

Country of ref document: RU

Kind code of ref document: A

WWP Wipo information: published in national office

Ref document number: 1020057000977

Country of ref document: KR

WWE Wipo information: entry into national phase

Ref document number: 20038219158

Country of ref document: CN

WWP Wipo information: published in national office

Ref document number: 2003765881

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 1-2005-500069

Country of ref document: PH

ENP Entry into the national phase

Ref document number: 2003254088

Country of ref document: AU

Date of ref document: 20030718

Kind code of ref document: B