DE60123283D1 - Pyrazolverbindungen als protein- kinasehemmer - Google Patents

Pyrazolverbindungen als protein- kinasehemmer

Info

Publication number
DE60123283D1
DE60123283D1 DE60123283T DE60123283T DE60123283D1 DE 60123283 D1 DE60123283 D1 DE 60123283D1 DE 60123283 T DE60123283 T DE 60123283T DE 60123283 T DE60123283 T DE 60123283T DE 60123283 D1 DE60123283 D1 DE 60123283D1
Authority
DE
Germany
Prior art keywords
protein kinase
kinase inhibitor
pyrazol compounds
pyrazol
compounds
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
DE60123283T
Other languages
English (en)
Other versions
DE60123283T2 (de
Inventor
David Bebbington
Jean-Damien Charrier
Julian Golec
Andrew Miller
Ronald Knegtel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of DE60123283D1 publication Critical patent/DE60123283D1/de
Application granted granted Critical
Publication of DE60123283T2 publication Critical patent/DE60123283T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20Antivirals for DNA viruses
    • 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
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • 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
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
DE60123283T 2000-12-21 2001-12-19 Pyrazolverbindungen als protein- kinasehemmer Expired - Lifetime DE60123283T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US25788700P 2000-12-21 2000-12-21
US257887P 2000-12-21
US28694901P 2001-04-27 2001-04-27
US286949P 2001-04-27
PCT/US2001/049401 WO2002057259A2 (en) 2000-12-21 2001-12-19 Pyrazole compounds useful as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
DE60123283D1 true DE60123283D1 (de) 2006-11-02
DE60123283T2 DE60123283T2 (de) 2007-04-12

Family

ID=26946273

Family Applications (8)

Application Number Title Priority Date Filing Date
DE60119776T Expired - Lifetime DE60119776T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als protein-kinase-inhibitoren
DE60123283T Expired - Lifetime DE60123283T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als protein- kinasehemmer
DE60126828T Expired - Lifetime DE60126828T2 (de) 2000-12-21 2001-12-19 "pyrazolverbindungen, die sich als proteinkinaseinhibitoren eignen"
DE60120219T Expired - Lifetime DE60120219T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als protein-kinase-inhibitoren
DE60119775T Expired - Lifetime DE60119775T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als proteinkinasehemmer
DE60119774T Expired - Lifetime DE60119774T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als proteinkinasehemmer
DE60119777T Expired - Lifetime DE60119777T2 (de) 2000-12-21 2001-12-20 Pyrazolverbindungen als protein-kinasehemmer
DE60126658T Expired - Lifetime DE60126658T2 (de) 2000-12-21 2001-12-20 Pyrazolverbindungen als proteinkinasehemmer

Family Applications Before (1)

Application Number Title Priority Date Filing Date
DE60119776T Expired - Lifetime DE60119776T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als protein-kinase-inhibitoren

Family Applications After (6)

Application Number Title Priority Date Filing Date
DE60126828T Expired - Lifetime DE60126828T2 (de) 2000-12-21 2001-12-19 "pyrazolverbindungen, die sich als proteinkinaseinhibitoren eignen"
DE60120219T Expired - Lifetime DE60120219T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als protein-kinase-inhibitoren
DE60119775T Expired - Lifetime DE60119775T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als proteinkinasehemmer
DE60119774T Expired - Lifetime DE60119774T2 (de) 2000-12-21 2001-12-19 Pyrazolverbindungen als proteinkinasehemmer
DE60119777T Expired - Lifetime DE60119777T2 (de) 2000-12-21 2001-12-20 Pyrazolverbindungen als protein-kinasehemmer
DE60126658T Expired - Lifetime DE60126658T2 (de) 2000-12-21 2001-12-20 Pyrazolverbindungen als proteinkinasehemmer

Country Status (28)

Country Link
US (16) US6653300B2 (de)
EP (10) EP2264028A1 (de)
JP (19) JP4160389B2 (de)
KR (8) KR100947185B1 (de)
CN (6) CN102250071A (de)
AP (2) AP2003002825A0 (de)
AR (4) AR042169A1 (de)
AT (9) ATE326462T1 (de)
AU (7) AU2001297619B2 (de)
BR (2) BR0116493A (de)
CA (8) CA2432799C (de)
CY (1) CY1106297T1 (de)
DE (8) DE60119776T2 (de)
DK (3) DK1355905T3 (de)
ES (7) ES2272567T3 (de)
HK (8) HK1059776A1 (de)
HU (5) HUP0400639A3 (de)
IL (8) IL156407A0 (de)
MX (8) MXPA03005607A (de)
MY (1) MY140377A (de)
NO (5) NO328537B1 (de)
NZ (8) NZ526472A (de)
PL (2) PL210414B1 (de)
PT (3) PT1345922E (de)
RU (1) RU2355688C2 (de)
SI (2) SI1353916T1 (de)
TW (2) TWI290551B (de)
WO (8) WO2002062789A1 (de)

Families Citing this family (367)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6982260B1 (en) 1999-11-22 2006-01-03 Warner-Lambert Company Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
IL154817A0 (en) * 2000-09-15 2003-10-31 Vertex Pharma Pyrazole derivatives and pharmaceutical compositions containing the same
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP4377583B2 (ja) * 2000-12-05 2009-12-02 バーテックス ファーマシューティカルズ インコーポレイテッド C−junn末端キナーゼ(jnk)および他のタンパク質キナーゼのインヒビター
ES2272567T3 (es) * 2000-12-21 2007-05-01 Vertex Pharmaceuticals Incorporated Compuestos de pirazol utiles como inhibidores de proteina quinasas.
HN2002000067A (es) * 2001-03-23 2003-10-24 Bayer Healthcare Llc Inhibidores de la rho - quinasa.
AU2002252614B2 (en) 2001-04-10 2006-09-14 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US7105667B2 (en) * 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
US7138404B2 (en) * 2001-05-23 2006-11-21 Hoffmann-La Roche Inc. 4-aminopyrimidine derivatives
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
WO2003026665A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
JP4542338B2 (ja) 2001-09-26 2010-09-15 ファイザー イタリア ソシエタ ア レスポンサビリタ リミタータ キナーゼ阻害因子として活性なアミノインダゾール誘導体、それらの製造方法及びそれらを含有する医薬組成物
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
WO2003055866A1 (en) * 2001-12-21 2003-07-10 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
AU2003235798A1 (en) 2002-01-10 2003-07-24 F. Hoffmann-La Roche Ag Use of a gsk-3beta inhibitor in the manufacture of a medicament for increasing bone formation
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
MXPA04007697A (es) * 2002-02-06 2004-11-10 Vertex Pharma Compuestos de heteroarilo utiles como inhibidores de gsk-3.
US7179826B2 (en) 2002-03-15 2007-02-20 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US20040009981A1 (en) * 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
WO2003077921A1 (en) * 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
US7223738B2 (en) 2002-04-08 2007-05-29 Merck & Co., Inc. Inhibitors of Akt activity
EP1552842A1 (de) 2002-06-07 2005-07-13 Kyowa Hakko Kogyo Co., Ltd. Bizyklische pyrimidin-derivate
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
AU2003261204A1 (en) * 2002-07-23 2004-02-09 Smithkline Beecham Corporation Pyrazolopyrimidines as kinase inhibitors
ATE451104T1 (de) 2002-07-29 2009-12-15 Rigel Pharmaceuticals Inc Verfahren zur behandlung oder pruvention von autoimmunkrankheiten mit 2,4-pyrimidindiamin- verbindungen
EP1739087A1 (de) * 2002-08-02 2007-01-03 Vertex Pharmaceuticals Incorporated Pyrazolenthaltende Zusammensetzungen und ihre Verwendung als Gsk-3 Inhibitoren
WO2004013140A1 (en) * 2002-08-02 2004-02-12 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
WO2004022544A1 (fr) * 2002-09-05 2004-03-18 Aventis Pharma S.A. Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
FR2844267B1 (fr) * 2002-09-05 2008-02-15 Aventis Pharma Sa Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
AU2003255482A1 (en) * 2002-10-02 2004-04-23 Merck Patent Gmbh Use of 4 amino-quinazolines as anti cancer agents
EP2210892A3 (de) * 2002-10-04 2010-10-27 Prana Biotechnology Limited Neurologisch aktive Verbindungen
KR100490893B1 (ko) * 2002-10-11 2005-05-23 (주) 비엔씨바이오팜 2-메톡시-1,3,5-트리아진 유도체, 그 제조방법 및 이를 포함하는 항바이러스용 약학적 조성물
GB0226583D0 (en) * 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
FR2847253B1 (fr) * 2002-11-19 2007-05-18 Aventis Pharma Sa Nouveaux derives de pyridazinones a titre de medicaments et compositions pharmaceutiques les renfermant
US7309701B2 (en) 2002-11-19 2007-12-18 Sanofi-Aventis Deutschland Gmbh Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them
US7462613B2 (en) 2002-11-19 2008-12-09 Sanofi-Aventis Deutschland Gmbh Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them
ATE527250T1 (de) 2002-11-21 2011-10-15 Novartis Ag 2,4,6-trisubstituierten pyrimidinen als phosphotidylinositol (pi) 3-kinase inhibitoren und deren verwendung zur behandlung von krebs
WO2004072029A2 (en) * 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
US7157455B2 (en) * 2003-02-10 2007-01-02 Hoffmann-La Roche Inc. 4-Aminopyrimidine-5-one derivatives
EP1644338A1 (de) * 2003-04-01 2006-04-12 Aponetics AG 2,4,6-trisubstituierte pyrimidinderivate, die sich für die behandlung von neoplastischen krankheiten und autoimmunkrankheiten eignen
JP2006526599A (ja) * 2003-06-02 2006-11-24 アストラゼネカ アクチボラグ 癌のような増殖性疾患の治療のためのオーロラキナーゼインヒビターとしての(3−((キナゾリン−4−イル)アミノ)−1h−ピラゾール−1−イル)アセトアミド誘導体及び関連化合物
ATE532781T1 (de) * 2003-06-19 2011-11-15 Glaxosmithkline Llc 5-(acylamino)indazol-derivate als kinase- inhibitoren
US8309562B2 (en) 2003-07-03 2012-11-13 Myrexis, Inc. Compounds and therapeutical use thereof
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
CN1984660B (zh) * 2003-07-03 2010-12-15 美瑞德生物工程公司 作为天冬氨酸特异性半胱氨酸蛋白酶活化剂和细胞程序死亡诱导剂的4-芳基氨基-喹唑啉
WO2006074147A2 (en) 2005-01-03 2006-07-13 Myriad Genetics, Inc. Nitrogen containing bicyclic compounds and therapeutical use thereof
GB0315966D0 (en) * 2003-07-08 2003-08-13 Cyclacel Ltd Compounds
PL1651612T3 (pl) 2003-07-22 2012-09-28 Astex Therapeutics Ltd Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3)
CA2533474A1 (en) * 2003-07-30 2005-02-10 Shudong Wang 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
WO2005016893A2 (en) 2003-07-30 2005-02-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US20060024690A1 (en) * 2003-09-19 2006-02-02 Kao H P Normalization of data using controls
US20050221357A1 (en) * 2003-09-19 2005-10-06 Mark Shannon Normalization of gene expression data
US7417726B2 (en) * 2003-09-19 2008-08-26 Applied Biosystems Inc. Normalization of data using controls
WO2005030131A2 (en) * 2003-09-23 2005-04-07 Replidyne, Inc Bis-quinazoline compounds for the treatment of bacterial infections
ES2328820T3 (es) 2003-10-17 2009-11-18 Astrazeneca Ab Derivados de 4-(pirazol-3-ilamino)pirimidina para uso en el tratamiento de cancer.
EP1694671A2 (de) * 2003-12-04 2006-08-30 Vertex Pharmaceuticals Incorporated Als inhibitoren von proteinkinasen geeignete chinoxaline
EP1709045A1 (de) * 2003-12-09 2006-10-11 Vertex Pharmaceuticals Incorporated Naphthyridinderivate und deren verwendung als modulatoren von muscarinischen rezeptoren
US7572914B2 (en) 2003-12-19 2009-08-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
TW200530235A (en) 2003-12-24 2005-09-16 Renovis Inc Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
WO2005077938A1 (en) * 2004-02-11 2005-08-25 Amgen Inc. Vanilloid receptor ligands and their use in treatments
WO2005083105A2 (en) * 2004-02-26 2005-09-09 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with glycogen synthase kinase 3 beta (gsk3b)
EP1726580A4 (de) * 2004-03-15 2008-02-13 Takeda Pharmaceutical Aminophenylpropansäurederivat
WO2005099688A2 (en) * 2004-04-07 2005-10-27 Takeda Pharmaceutical Company Limited Cyclic compounds
JP2007533717A (ja) * 2004-04-21 2007-11-22 アストラゼネカ アクチボラグ 化合物
WO2005105788A1 (en) * 2004-04-23 2005-11-10 Takeda San Diego, Inc. Indole derivatives and use thereof as kinase inhibitors
US7880000B2 (en) * 2004-05-07 2011-02-01 Amgen Inc. Protein kinase modulators and method of use
US7793137B2 (en) 2004-10-07 2010-09-07 Cisco Technology, Inc. Redundant power and data in a wired data telecommunincations network
ATE381566T1 (de) * 2004-05-14 2008-01-15 Millennium Pharm Inc Verbindungen und verfahren zur inhibierung der mitotischen progression durch hemmung von aurorakinase
CA2566444A1 (en) * 2004-05-14 2005-12-01 Vertex Pharmaceuticals Incorporated Prodrugs of pyrrolylpyrimidine erk protein kinase inhibitors
AU2012200416B2 (en) * 2004-05-14 2014-07-31 Millennium Pharmaceuticals, Inc. "Compounds and methods for inhibiting mitotic progression by inhibition of Aurora kinase"
EP1905773B1 (de) * 2004-05-14 2012-07-18 Millennium Pharmaceuticals, Inc. Verbindungen und Verfahren zum Hemmen der Mitoseprogression durch Hemmung der Aurora-Kinase
US20050255485A1 (en) * 2004-05-14 2005-11-17 Livak Kenneth J Detection of gene duplications
CA2567352A1 (en) * 2004-05-20 2005-12-01 Bayer Pharmaceuticals Corporation 5-anilino-4-heteroarylpyrazole derivatives useful for the treatment of diabetes
WO2005119372A1 (en) * 2004-05-27 2005-12-15 E.I. Dupont De Nemours And Company Developer for a photopolymer protective layer
WO2006007532A2 (en) * 2004-07-01 2006-01-19 Synta Pharmaceuticals Corp. 2-substituted heteroaryl compounds
CA2573103A1 (en) * 2004-07-06 2006-02-09 Angion Biomedica Corporation Quinazoline modulators of hepatocyte growth factor / c-met activity for the treatment of cancer
WO2006023931A2 (en) * 2004-08-18 2006-03-02 Takeda San Diego, Inc. Kinase inhibitors
TW200624431A (en) * 2004-09-24 2006-07-16 Hoffmann La Roche Phthalazinone derivatives, their manufacture and use as pharmaceutical agents
US7285569B2 (en) 2004-09-24 2007-10-23 Hoff Hoffmann-La Roche Inc. Tricycles, their manufacture and use as pharmaceutical agents
MX2007003797A (es) * 2004-09-30 2007-04-23 Tibotec Pharm Ltd 5-heterociclil pirimidinas inhibidoras del virus de inmunodeficiencia humana.
AU2005288865B2 (en) * 2004-09-30 2012-07-19 Janssen Sciences Ireland Uc HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
AU2005288866B2 (en) * 2004-09-30 2012-07-26 Janssen Sciences Ireland Uc HIV inhibiting 5-substituted pyrimidines
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
KR20070072562A (ko) * 2004-10-29 2007-07-04 반유 세이야꾸 가부시끼가이샤 오로라 a 선택적 억제 활성을 갖는 신규한 아미노피리딘유도체
US7491720B2 (en) 2004-10-29 2009-02-17 Banyu Pharmaceutical Co., Ltd. Aminopyridine derivatives having Aurora A selective inhibitory action
WO2006050476A2 (en) 2004-11-03 2006-05-11 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as ion channel modulators and methods of use
WO2006055831A2 (en) * 2004-11-17 2006-05-26 Miikana Therapeutics, Inc. Kinase inhibitors
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
JP2008525422A (ja) * 2004-12-23 2008-07-17 ファイザー・プロダクツ・インク 抗癌剤として有用な複素芳香族誘導体
WO2006074057A2 (en) 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
AU2005321091B2 (en) 2004-12-30 2012-04-12 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of CDK, GSK and Aurora kinases
US8258145B2 (en) 2005-01-03 2012-09-04 Myrexis, Inc. Method of treating brain cancer
RU2416616C2 (ru) 2005-01-19 2011-04-20 Райджел Фармасьютикалз, Инк. Пролекарства соединений 2,4-пиримидиндиамина и их применения
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
ES2336243T3 (es) * 2005-01-26 2010-04-09 Schering Corporation Derivados de 3-(indazol-5-il)-(1,2,4)triazina y composiciones similares como inhibidores de proteina quinasa para el tratamiento del cancer.
CA2595834C (en) 2005-02-04 2013-04-30 Astrazeneca Ab Pyrazolylaminopyridine derivatives useful as kinase inhibitors
ATE473975T1 (de) * 2005-02-16 2010-07-15 Astrazeneca Ab Chemische verbindungen
SI1853588T1 (sl) * 2005-02-16 2008-10-31 Astrazeneca Ab Kemične spojine
BRPI0608513A2 (pt) * 2005-03-15 2010-01-05 Irm Llc compostos e composições como inibidores da proteìna quinase
WO2006100461A1 (en) * 2005-03-23 2006-09-28 Astrazeneca Ab 2-AZETIDINYL-4-(lH-PYRAZOL-3-YLAMINO)PYRIMIDINES AS INHIBITORS OF INSULIN-LIKE GROWTH FACTOR-I RECEPTOR ACTIVITY
US7402596B2 (en) 2005-03-24 2008-07-22 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
DE602006002271D1 (de) * 2005-04-05 2008-09-25 Astrazeneca Ab Pyrimidinderivate zur verwendung als antikrebsmittel
GB0507347D0 (en) * 2005-04-12 2005-05-18 Astrazeneca Ab Chemical compounds
EP1879894A1 (de) 2005-04-14 2008-01-23 F.Hoffmann-La Roche Ag Aminopyrazolderivate, ihre herstellung und verwendung als pharmazeutische mittel
JP2008540335A (ja) * 2005-04-27 2008-11-20 アストラゼネカ・アクチエボラーグ ピラゾリル・ピリミジン誘導体の疼痛治療における使用
ES2545382T3 (es) * 2005-04-28 2015-09-10 Mitsubishi Tanabe Pharma Corporation Derivado de cianopiridina y su uso como medicamento
EP1885454A2 (de) 2005-05-04 2008-02-13 DeveloGen Aktiengesellschaft Verwendung von gsk-3-hemmern zur prävention und behandlung von pankreatischen autoimmunkrankheiten
EP1885369B1 (de) 2005-05-04 2015-09-23 Evotec AG Fusionierte heterozyklische verbindungen und zusammensetzungen sowie anwendungen davon
US20080194606A1 (en) * 2005-05-05 2008-08-14 Astrazeneca Pyrazolyl-Amino-Substituted Pyrimidines and Their Use in the Treatment of Cancer
NZ564317A (en) * 2005-05-16 2011-01-28 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8193206B2 (en) 2005-06-14 2012-06-05 Taigen Biotechnology Co., Ltd. Pyrimidine compounds
US20060281712A1 (en) 2005-06-14 2006-12-14 Chi-Feng Yen Pyrimidine compounds
EP1746096A1 (de) 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazol-Analoge zur Verwendung als Antikrebsmittel
AU2006279376B2 (en) * 2005-08-18 2011-04-14 Vertex Pharmaceuticals Incoporated Pyrazine kinase inhibitors
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
EP1928437A2 (de) 2005-08-26 2008-06-11 Braincells, Inc. Neurogenese mittels muscarinrezeptormodulation
EP2258358A3 (de) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenese mit Acetylcholinesterasehemmer
UA96427C2 (en) * 2005-09-30 2011-11-10 Мийкана Терапьютикс, Инк. Substituted pyrazole compounds
AU2006297120B2 (en) * 2005-09-30 2011-05-19 Miikana Therapeutics, Inc. Substituted pyrazole compounds
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP2377530A3 (de) 2005-10-21 2012-06-20 Braincells, Inc. Modulation von Neurogenese durch PDE-Hemmung
JP2009513615A (ja) 2005-10-28 2009-04-02 アストラゼネカ アクチボラグ 癌の治療においてチロシンキナーゼ阻害剤として使用するための4−(3−アミノピラゾール)ピリミジン誘導体
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
ES2372540T3 (es) * 2005-11-01 2012-01-23 Array Biopharma, Inc. Activadores de glucocinasa.
AR056763A1 (es) * 2005-11-03 2007-10-24 Vertex Pharma Aminopirimidinas sustituidas con tiazol o pirazol,utiles como agentes anticancer y composiciones farmaceuticas que las contienen.
EP1951716B1 (de) * 2005-11-16 2011-05-04 Vertex Pharmaceuticals, Inc. als kinaseinhibitoren geeignete aminopyrimidine
US8546404B2 (en) * 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
US7572809B2 (en) * 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
US20080058312A1 (en) * 2006-01-11 2008-03-06 Angion Biomedica Corporation Modulators of hepatocyte growth factor/c-Met activity
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
ATE485268T1 (de) * 2006-02-16 2010-11-15 Schering Corp Pyrrolidin-derivate als erk-hemmer
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
PE20080145A1 (es) 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
CA2645958C (en) * 2006-03-30 2014-11-04 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5-amido substituted pyrimidines
CA2644910C (en) * 2006-03-31 2014-01-28 Abbott Laboratories Indazole compounds
PT2007391E (pt) 2006-04-07 2013-03-11 Novartis Ag Combinação compreendendo: a) um composto de pirimidil-aminobenzamida e b) um inibidor da cinase thr315ile
BRPI0710737A2 (pt) 2006-04-14 2011-05-10 Prana Biotechnology Ltd uso de compostos pb-10 33 éteis para o tratamento de degeneraÇço macular relacionada À idade (amd), assim como referidos compostos
JP5161072B2 (ja) * 2006-04-27 2013-03-13 Msd株式会社 オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
US7678808B2 (en) 2006-05-09 2010-03-16 Braincells, Inc. 5 HT receptor mediated neurogenesis
AU2007265966B2 (en) 2006-06-27 2012-05-17 Takeda Pharmaceutical Company Limited Fused cyclic compounds
WO2008001115A2 (en) 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3- [3- (5-m0rphoolin-4-ylmethyl-1h-benzoimidazol-2-yl) -lh-1-pyrazol- 4-yl] -urea
US20110159111A1 (en) * 2006-06-29 2011-06-30 Astex Therapeutics Limited Pharmaceutical combinations
CA2654852A1 (en) * 2006-06-30 2008-01-03 Astrazeneca Ab Pyrimidine derivatives useful in the treatment of cancer
WO2008001886A1 (fr) * 2006-06-30 2008-01-03 Kyowa Hakko Kirin Co., Ltd. Inhibiteur d'aurora
WO2008005538A2 (en) 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
CA2666193A1 (en) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use
US7718648B2 (en) * 2006-08-09 2010-05-18 Millennium Pharmaceuticals, Inc. Pyridobenzazepine compounds and methods for inhibiting mitotic progression
US7744164B2 (en) * 2006-08-11 2010-06-29 Schluimberger Technology Corporation Shield of a degradation assembly
JP2008081492A (ja) * 2006-08-31 2008-04-10 Banyu Pharmaceut Co Ltd オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
US7998971B2 (en) * 2006-09-08 2011-08-16 Braincells Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
EP2223925A1 (de) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase-Inhibitoren
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
JP5528806B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
WO2008044045A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
WO2008053812A1 (fr) * 2006-10-27 2008-05-08 Mitsubishi Tanabe Pharma Corporation Dérivé de cyanopyridine et son utilisation médicale
AU2007317435A1 (en) * 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
CL2007003244A1 (es) 2006-11-16 2008-04-04 Millennium Pharm Inc Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer.
MX2009006690A (es) * 2006-12-19 2009-07-31 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
ES2618057T3 (es) * 2006-12-29 2017-06-20 Janssen Sciences Ireland Uc Pirimidinas 5,6-sustituidas inhibidoras del VIH
CN101573343B (zh) * 2006-12-29 2016-02-24 爱尔兰詹森科学公司 抑制人免疫缺陷病毒的6-取代的嘧啶
ATE551334T1 (de) 2007-02-06 2012-04-15 Novartis Ag Pi3-kinase-hemmer und verfahren zu ihrer verwendung
JPWO2008111441A1 (ja) 2007-03-05 2010-06-24 協和発酵キリン株式会社 医薬組成物
JP5393489B2 (ja) * 2007-03-09 2014-01-22 バーテックス ファーマシューティカルズ インコーポレイテッド 蛋白キナーゼの阻害剤として有用なアミノピリミジン
CN101663295B (zh) * 2007-03-09 2014-11-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的氨基嘧啶类化合物
CA2679701A1 (en) * 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
CA2682195A1 (en) * 2007-03-20 2008-09-25 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
WO2008117050A1 (en) * 2007-03-27 2008-10-02 Astrazeneca Ab Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer
MX2009011059A (es) 2007-04-13 2009-11-26 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasas.
WO2008129255A1 (en) * 2007-04-18 2008-10-30 Astrazeneca Ab 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer
JP4782239B2 (ja) 2007-04-18 2011-09-28 ファイザー・プロダクツ・インク 異常細胞増殖治療のためのスルホニルアミド誘導体
AU2008247594A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
JP5572087B2 (ja) * 2007-05-02 2014-08-13 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害として有用なアミノピリミジン
JP5389785B2 (ja) * 2007-05-02 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用なチアゾールおよびピラゾール
UA99459C2 (en) 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
ES2369596T3 (es) * 2007-05-04 2011-12-02 Astrazeneca Ab Derivados de amino-tiazolil-pirimidina y su uso para el tratamiento del cáncer.
CN101687852A (zh) * 2007-05-24 2010-03-31 沃泰克斯药物股份有限公司 可用作激酶抑制剂的噻唑类和吡唑类化合物
KR101294731B1 (ko) * 2007-06-04 2013-08-16 삼성디스플레이 주식회사 어레이 기판, 이를 갖는 표시패널 및 이의 제조방법
AU2008262291A1 (en) * 2007-06-11 2008-12-18 Miikana Therapeutics, Inc. Substituted pyrazole compounds
EP2178563A2 (de) * 2007-07-06 2010-04-28 OSI Pharmaceuticals, Inc. Kombinationskrebstherapie mit einem hemmer sowohl für mtorc1 als auch für mtorc2
WO2009007753A2 (en) * 2007-07-11 2009-01-15 Astrazeneca Ab 4- (3-aminopyrazole) -pyrimidine derivativee and their use as tyrosine kinase inhibitors for the treatment of cancer
ES2392003T3 (es) * 2007-07-25 2012-12-03 Bristol-Myers Squibb Company Inhibidores de la triazina quinasa
WO2009013545A2 (en) * 2007-07-26 2009-01-29 Astrazeneca Ab Chemical compounds
ES2400104T3 (es) * 2007-07-31 2013-04-05 Vertex Pharmaceuticals Incorporated Proceso para preparación de 5-fluoro-1H-pirazolo[3,4-b]piridin-3-amina y derivados de la misma
TW200906818A (en) * 2007-07-31 2009-02-16 Astrazeneca Ab Chemical compounds
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
WO2009027736A2 (en) * 2007-08-27 2009-03-05 Astrazeneca Ab 2,4 diaminopyrimid'lnes for the treatment of myeloproliferative disorders and cancer
EP2209778B1 (de) 2007-09-21 2012-08-29 Array Biopharma, Inc. Pyridin-2 -yl-amino-i, 2, 4 -thiadiazolderivate als glucokinase-aktivatoren zur behandlung von diabetes mellitus
DK2214487T3 (da) 2007-10-11 2014-02-10 Glaxosmithkline Llc Nye sEH-inhibitorer og deres anvendelse
US8288397B2 (en) 2007-12-17 2012-10-16 Janssen Pharmaceutica Nv Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1
US20090270418A1 (en) * 2008-01-09 2009-10-29 Marianne Sloss Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith
WO2009097995A1 (de) * 2008-02-07 2009-08-13 Sanofi-Aventis Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
NZ587504A (en) 2008-02-21 2012-09-28 Merck Sharp & Dohme Benzopyrazole derivatives as ERK inhibitors
CA2714215A1 (en) * 2008-02-22 2009-08-27 Banyu Pharmaceutical Co., Ltd. Novel aminopyridine derivatives having aurora a selective inhibitory action
PL2268635T3 (pl) 2008-04-21 2015-11-30 Taigen Biotechnology Co Ltd Związki heterocykliczne
WO2010011411A1 (en) 2008-05-27 2010-01-28 The Trustees Of Columbia University In The City Of New York Systems, methods, and media for detecting network anomalies
AR072085A1 (es) * 2008-06-11 2010-08-04 Astrazeneca Ab Compuestos triciclicos, metodos para su preparacion, composicion farma-ceutica que los comprende y su uso en el tratamiento de enfermedades me-diadas por la actividad de las proteinas quinasas
EP2310372B1 (de) 2008-07-09 2012-05-23 Sanofi Heterocyclische Verbindungen, Verfahren zu ihrer Herstellung, Arzneimitteln mit diesen Verbindungen und ihre Verwendung
AR073354A1 (es) * 2008-07-31 2010-11-03 Genentech Inc Compuestos de pirimidina, composiciones farmaceuticas y su uso en el tratamiento del cancer.
WO2010027921A1 (en) * 2008-09-03 2010-03-11 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical formulations comprising the same
CN102405284B (zh) * 2008-09-05 2016-01-20 新基阿维罗米克斯研究公司 设计不可逆抑制剂的算法
CN104230901A (zh) * 2008-09-15 2014-12-24 加利福尼亚大学董事会 用于调节ire1、src和abl活性的方法和组合物
RU2011116928A (ru) * 2008-09-30 2012-11-20 Астразенека Аб (Se) Гетероциклические ингибиторы jак киназы
US8759362B2 (en) * 2008-10-24 2014-06-24 Purdue Pharma L.P. Bicycloheteroaryl compounds and their use as TRPV1 ligands
WO2010056758A1 (en) * 2008-11-12 2010-05-20 Yangbo Feng Quinazoline derivatives as kinase inhibitors
US9023834B2 (en) 2008-11-13 2015-05-05 Taigen Biotechnology Co., Ltd. Lyophilization formulation
WO2010068601A1 (en) 2008-12-08 2010-06-17 Sanofi-Aventis A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof
PA8851101A1 (es) 2008-12-16 2010-07-27 Lilly Co Eli Compuesto amino pirazol
US8524707B2 (en) 2008-12-19 2013-09-03 Nerviano Medical Sciences S.R.L. Bicyclic pyrazoles as protein kinase inhibitors
US20100183601A1 (en) 2008-12-22 2010-07-22 Millennium Pharmaceuticals, Inc. Combination of Aurora Kinase Inhibitors and Anti-CD20 Antibodies
WO2010072155A1 (zh) * 2008-12-26 2010-07-01 复旦大学 一种嘧啶类衍生物及其制备方法和用途
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CA2752885A1 (en) * 2009-02-27 2010-09-02 Ambit Biosciences Corporation Jak kinase modulating quinazoline derivatives and methods of use thereof
CA2660962A1 (en) 2009-03-31 2010-09-30 Astellas Pharma Inc. Novel pharmaceutical composition for treatment of schizophrenia
US8399663B2 (en) 2009-04-03 2013-03-19 Astellas Pharma Inc. Salt of 1,3,5-triazine-2,4,6-triamine derivative
JO3635B1 (ar) 2009-05-18 2020-08-27 Millennium Pharm Inc مركبات صيدلانية صلبة وطرق لانتاجها
BRPI1010881A2 (pt) * 2009-06-08 2016-05-31 California Capital Equity Llc derivados de triazina e suas aplicações terapêuticas.
KR20120034726A (ko) * 2009-06-08 2012-04-12 아브락시스 바이오사이언스, 엘엘씨 트리아진 유도체와 이들의 치료적 용도
KR101457027B1 (ko) * 2009-06-09 2014-10-31 캘리포니아 캐피탈 에쿼티, 엘엘씨 트리아진 유도체와 이들의 치료적 용도
CN102573484B (zh) * 2009-06-09 2015-07-01 加利福尼亚资本权益有限责任公司 苄基取代的三嗪衍生物及其治疗应用
JP2012529519A (ja) * 2009-06-09 2012-11-22 アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー スチリル−トリアジン誘導体類及びそれらの治療応用
BRPI1011527A2 (pt) * 2009-06-09 2016-07-26 California Capital Equity Llc derivados de triazina substituídos com ureidofenil e suas aplicações terapêuticas.
CA2763730A1 (en) * 2009-06-18 2010-12-23 Cellzome Limited Heterocyclylaminopyrimidines as kinase inhibitors
TWI468402B (zh) * 2009-07-31 2015-01-11 必治妥美雅史谷比公司 降低β-類澱粉生成之化合物
US8637525B2 (en) 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
DK2470552T3 (en) 2009-08-26 2014-02-17 Sanofi Sa NOVEL, CRYSTALLINE, heteroaromatic FLUORGLYCOSIDHYDRATER, MEDICINES COVERING THESE COMPOUNDS AND THEIR USE
NZ620174A (en) 2009-09-16 2016-08-26 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
CN102596058B (zh) * 2009-11-13 2015-10-21 直观外科手术操作公司 具有复设的闭合机构的末端执行器
EP2937345B1 (de) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Typ-ii-raf-kinase-hemmer
AU2010339456A1 (en) 2009-12-30 2012-07-05 Celgene Avilomics Research, Inc. Ligand-directed covalent modification of protein
SA111320200B1 (ar) * 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
CN104031049A (zh) 2010-02-19 2014-09-10 米伦纽姆医药公司 极光激酶抑制剂的结晶形式
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2571359A4 (de) * 2010-05-20 2013-10-23 Merck Sharp & Dohme Neuartige prolylcarboxypeptidase-hemmer
CA2798578C (en) 2010-05-21 2015-12-29 Chemilia Ab Novel pyrimidine derivatives
EP3075730B1 (de) 2010-06-04 2018-10-24 Genentech, Inc. Aminopyrimidinderivate als lrrk2-modulatoren
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
MX341732B (es) 2010-07-29 2016-08-30 Oryzon Genomics S A * Inhibidores de la demetilasa lsd1 basados en arilciclopropilamina y sus usos médicos.
CN103270030B (zh) * 2010-09-01 2016-01-20 埃姆比特生物科学公司 吡唑基氨基喹唑啉的氢溴酸盐
EP2611502A1 (de) * 2010-09-01 2013-07-10 Ambit Biosciences Corporation Adenosin-a3-rezeptormodulierende verbindungen und ihre verwendung
US20130296363A1 (en) * 2010-09-01 2013-11-07 Ambit Biosciences Corporation Quinoline and isoquinoline derivatives for use as jak modulators
US8912324B2 (en) * 2010-09-01 2014-12-16 Ambit Biosciences Corporation Optically active pyrazolylaminoquinazoline, and pharmaceutical compositions and methods of use thereof
US20130225615A1 (en) * 2010-09-01 2013-08-29 Ambit Biosciences Corporation 2-cycloquinazoline derivatives and methods of use thereof
US20130225614A1 (en) * 2010-09-01 2013-08-29 Ambit Biosciences Corporation 4-azolylaminoquinazoline derivatives and methods of use thereof
AU2011296024B2 (en) 2010-09-01 2015-05-28 Ambit Biosciences Corporation Quinazoline compounds and methods of use thereof
WO2012059932A1 (en) 2010-11-01 2012-05-10 Aurigene Discovery Technologies Limited 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors
HUE037844T2 (hu) 2010-11-10 2018-09-28 Genentech Inc Pirazol-aminopirimidin-származékok mint LRRK2 modulátorok
EP2683698B1 (de) 2011-03-08 2017-10-04 Sanofi Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8895547B2 (en) 2011-03-08 2014-11-25 Sanofi Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8901114B2 (en) 2011-03-08 2014-12-02 Sanofi Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof
WO2012120055A1 (de) 2011-03-08 2012-09-13 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8846666B2 (en) 2011-03-08 2014-09-30 Sanofi Oxathiazine derivatives which are substituted with benzyl or heteromethylene groups, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
WO2012120050A1 (de) 2011-03-08 2012-09-13 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2683700B1 (de) 2011-03-08 2015-02-18 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120053A1 (de) 2011-03-08 2012-09-13 Sanofi Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2688883B1 (de) 2011-03-24 2016-05-18 Noviga Research AB Pyrimidinderivate
CN104024248A (zh) * 2011-08-25 2014-09-03 霍夫曼-拉罗奇有限公司 丝氨酸/苏氨酸pak1抑制剂
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP5914667B2 (ja) 2011-09-22 2016-05-11 ファイザー・インク ピロロピリミジンおよびプリン誘導体
EP2760862B1 (de) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridin-4-carbonsäureamidderivate als kinaseinhibitoren
CA2849995A1 (en) 2011-09-27 2013-04-04 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
BR112014015549A8 (pt) 2011-12-22 2017-07-04 Hoffmann La Roche composto, método de inibição da atividade pak1, método para o tratamento, processo, composição, utilização de um composto e invenção
AU2013221286B2 (en) * 2012-02-17 2017-06-15 Abbvie Inc. Diaminopyrimidines useful as inhibitors of the human respiratory syncytial virus (RSV)
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
TWI485146B (zh) * 2012-02-29 2015-05-21 Taiho Pharmaceutical Co Ltd Novel piperidine compounds or salts thereof
AR092809A1 (es) 2012-03-16 2015-05-06 Axikin Pharmaceuticals Inc 3,5-diaminopirazol como inhibidor de quinasa
US20130303519A1 (en) 2012-03-20 2013-11-14 Millennium Pharmaceuticals, Inc. Methods of treating cancer using aurora kinase inhibitors
HUE054031T2 (hu) 2012-04-24 2021-08-30 Vertex Pharma DNS-PK inhibitorok
JP6197031B2 (ja) * 2012-05-24 2017-09-13 セルゾーム リミティッド Tyk2阻害剤としてのヘテロシクリルピリミジン類似体
KR102427777B1 (ko) 2012-06-26 2022-08-01 델 마 파마슈티컬스 디안하이드로갈락티톨, 디아세틸디안하이드로갈락티톨, 디브로모둘시톨, 또는 그의 유사체 또는 유도체를 이용하여 유전학적 다형성이 있는 환자에 있어서 티로신-키나아제-억제제 내성 악성종양, ahi1 조절곤란 또는 돌연변이를 치료하는 방법
MX2015000129A (es) * 2012-07-10 2015-04-14 Ares Trading Sa Derivados de pirimidin pirazolilo.
MY183976A (en) * 2012-09-19 2021-03-17 Taiho Pharmaceutical Co Ltd Pharmaceutical composition for oral administration with improved dissolution and/or absorption
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
CN103059002B (zh) * 2012-12-31 2015-04-22 中山大学 具有Aurora激酶抑制活性的嘧啶衍生物及其制备方法以及应用
CN103202843B (zh) * 2012-12-31 2015-04-29 刘强 一种嘧啶衍生物在制备预防和/或治疗和/或辅助治疗癌症的药物中的用途
CN103191120B (zh) * 2012-12-31 2015-11-25 刘强 一种嘧啶衍生物在制备预防和/或治疗和/或辅助治疗肿瘤的药物中的用途
CN103910716A (zh) * 2013-01-07 2014-07-09 华东理工大学 2,4-二取代-环烷基[d]嘧啶类化合物及其用途
HRP20211855T1 (hr) 2013-03-12 2022-03-04 Vertex Pharmaceuticals Incorporated Inhibitori dnk-pk
CN105263929B (zh) 2013-03-14 2018-08-28 诺华股份有限公司 作为突变idh抑制剂的3-嘧啶-4-基-噁唑烷-2-酮化合物
WO2014145485A2 (en) 2013-03-15 2014-09-18 The Trustees Of Columbia University In The City Of New York Map kinase modulators and uses thereof
EP2976086B1 (de) 2013-03-22 2020-10-14 Millennium Pharmaceuticals, Inc. Kombination aus katalytischen mtorc 1/2-inhibitoren und selektiven inhibitoren der aurora-a-kinase
WO2015003355A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015013579A1 (en) 2013-07-26 2015-01-29 Update Pharma Inc. Compositions to improve the therapeutic benefit of bisantrene
WO2015028848A1 (en) * 2013-09-02 2015-03-05 Piramal Enterprises Limited Bicyclic heterocyclic compounds as multi-kinase inhibitors
NZ631142A (en) 2013-09-18 2016-03-31 Axikin Pharmaceuticals Inc Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors
PL3057953T3 (pl) 2013-10-17 2019-01-31 Vertex Pharmaceuticals Incorporated Kokryształy (S)-N-metylo-8-(1-((2'-metylo-[4,5'-bipirymidyn]-6-ylo)amino)propan-2-ylo)chinolino-4-karboksyamidu i ich deuterowane pochodne jako inhibitory DNA-PK
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
CA2935392C (en) 2014-01-01 2022-07-26 Medivation Technologies, Inc. Amino pyridine derivatives for the treatment of conditions associated with excessive tgf.beta activity
DK3116475T3 (da) 2014-03-13 2020-12-07 Neuroderm Ltd Dopa-decarboxylasehæmmersammensætninger
US10258585B2 (en) 2014-03-13 2019-04-16 Neuroderm, Ltd. DOPA decarboxylase inhibitor compositions
MX2016012574A (es) 2014-03-28 2017-09-26 Calitor Sciences Llc Compuestos heteroarilo sustituidos y metodos de uso.
NZ725860A (en) 2014-04-04 2019-08-30 Iomet Pharma Ltd Indole derivatives for use in medicine
CA2945263A1 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
CN105367555B (zh) * 2014-08-07 2019-06-25 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
TWI703133B (zh) 2014-12-23 2020-09-01 美商艾克斯基製藥公司 3,5-二胺基吡唑激酶抑制劑
WO2016105528A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2016123627A1 (en) * 2015-01-30 2016-08-04 Vanderbilt University Isoquiniline and napthalene-substituted compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3283482B1 (de) 2015-04-17 2022-04-06 Ludwig Institute for Cancer Research Ltd Plk4 hemmer
WO2016191524A1 (en) 2015-05-28 2016-12-01 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors
JP2018135268A (ja) * 2015-06-05 2018-08-30 大日本住友製薬株式会社 新規ヘテロアリールアミノ−3−ピラゾール誘導体およびその薬理学上許容される塩
AU2016319125B2 (en) 2015-09-09 2021-04-08 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3347097B1 (de) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituierte aminopyrimidin-derivate als modulatoren der kinasen jak, flt3 und aurora
SI3386511T1 (sl) 2015-12-10 2021-09-30 Ptc Therapeutics, Inc. Postopki za zdravljenje Huntingtonove bolezni
CN105399695B (zh) * 2015-12-11 2019-04-19 浙江大学 三嗪类化合物及其制备方法和用途
CN105503754B (zh) * 2015-12-11 2017-11-17 浙江大学 2‑氨基‑4‑苄基‑6‑吗啉‑1,3,5‑三嗪及其制备和应用
CN105384702B (zh) * 2015-12-11 2018-04-10 浙江大学 三取代均三嗪类化合物及其制备方法
EP3390387B1 (de) 2015-12-18 2021-11-17 Bayer Pharma Aktiengesellschaft Heteroarylbenzimidazolverbindungen
CA3016773A1 (en) 2016-03-14 2017-09-21 Ronald Charles Hawley Pyrimidines and variants thereof, and uses therefor
CN108779119B (zh) * 2016-03-25 2022-02-08 传入制药公司 嘧啶及其变体、及其用途
JP6881879B2 (ja) 2016-04-28 2021-06-02 セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー Jakキナーゼ阻害剤としてのピリミジン化合物
WO2017207534A1 (en) 2016-06-03 2017-12-07 Bayer Pharma Aktiengesellschaft Substituted heteroarylbenzimidazole compounds
EP3518931A4 (de) 2016-09-27 2020-05-13 Vertex Pharmaceuticals Incorporated Verfahren zur behandlung von krebs mit einer kombination aus dna-schädigenden substanzen und dna-pk-inhibitoren
US10858319B2 (en) 2016-10-03 2020-12-08 Iomet Pharma Ltd. Indole derivatives for use in medicine
US10968227B2 (en) * 2016-11-08 2021-04-06 Vanderbilt University Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
CN108239071B (zh) * 2016-12-27 2020-12-04 沈阳药科大学 酰胺及硫代酰胺类衍生物及其制备方法和应用
FR3064275B1 (fr) 2017-03-21 2019-06-07 Arkema France Procede de chauffage et/ou climatisation d'un vehicule
BR112019025295A2 (pt) 2017-05-30 2020-06-23 Basf Se Compostos, composição, uso de um composto da fórmula i, método para combater fungos fitopatogênicos e semente
EA201992878A1 (ru) 2017-06-05 2020-05-08 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Соединения для лечения болезни хантингтона
BR112019027717A2 (pt) 2017-06-28 2020-07-28 Ptc Therapeutics, Inc. métodos para tratar a doença de huntington
US11395822B2 (en) 2017-06-28 2022-07-26 Ptc Therapeutics, Inc. Methods for treating Huntington's disease
US10323023B2 (en) 2017-06-30 2019-06-18 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
EP3421465B1 (de) * 2017-06-30 2022-10-26 Beijing Tide Pharmaceutical Co., Ltd. Rho-assoziierte proteinkinasehemmer, pharmazeutische zusammensetzung damit sowie herstellungsverfahren und verwendung davon
KR102585860B1 (ko) 2017-06-30 2023-10-06 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Rho-관련 단백질 키나아제 억제제, 이를 포함하는 약학 조성물, 및 이의 제조 방법 및 용도
EP3676264A1 (de) * 2017-08-28 2020-07-08 Acurastem Inc. Pikfyve-kinase-inhibitoren
WO2019046163A1 (en) * 2017-08-28 2019-03-07 Zhihong Chen SUBSTITUTED PYRIMIDINES, PHARMACEUTICAL COMPOSITIONS AND ASSOCIATED THERAPEUTIC METHODS
KR102613503B1 (ko) 2017-10-27 2023-12-13 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 키나제 저해제로서 피리미딘 화합물
CN111247139A (zh) * 2017-11-23 2020-06-05 艾克斯生物医药股份有限公司 嘧啶衍生物作为原肌球蛋白受体激酶a(trka)抑制剂
EP3720560A4 (de) * 2017-12-06 2022-01-05 Ludwig Institute for Cancer Research Ltd Verfahren zur behandlung von krebs mit plk4-inhibitoren
CA3094703A1 (en) 2018-03-27 2019-10-03 Ptc Therapeutics, Inc. Compounds for treating huntington's disease
JP2021528470A (ja) * 2018-06-25 2021-10-21 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 Taireファミリーキナーゼインヒビターおよびそれらの使用
WO2020005873A1 (en) 2018-06-27 2020-01-02 Ptc Therapeutics, Inc. Heterocyclic and heteroaryl compounds for treating huntington's disease
US11685746B2 (en) 2018-06-27 2023-06-27 Ptc Therapeutics, Inc. Heteroaryl compounds for treating Huntington's disease
EP3958969B1 (de) 2019-04-24 2024-01-10 Theravance Biopharma R&D IP, LLC Ester- und carbonatpyrimidinverbindungen als jak-kinase-inhibitoren
EP3959213A1 (de) 2019-04-24 2022-03-02 Theravance Biopharma R&D IP, LLC Pyrimidin-jak inhibitoren zur behandlung von hauterkrankungen
CN114728949A (zh) * 2019-08-01 2022-07-08 整体生物科学私人有限公司 作为激酶抑制剂的杂环化合物及其用途
EP4031547A1 (de) 2019-09-18 2022-07-27 Takeda Pharmaceutical Company Limited Plasma-kallikreininhibitoren und verwendungen dafür
CN110483493A (zh) * 2019-09-19 2019-11-22 广东工业大学 一种二唑类衍生物及其制备方法和应用
US11331293B1 (en) 2020-11-17 2022-05-17 Neuroderm, Ltd. Method for treatment of Parkinson's disease
US11213502B1 (en) 2020-11-17 2022-01-04 Neuroderm, Ltd. Method for treatment of parkinson's disease
US11844754B2 (en) 2020-11-17 2023-12-19 Neuroderm, Ltd. Methods for treatment of Parkinson's disease
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Alk﹘5抑制劑和彼之用途
CN117355523A (zh) * 2021-03-17 2024-01-05 武田药品工业株式会社 血浆激肽释放酶的多环抑制剂
AU2022243600A1 (en) * 2021-03-26 2023-10-12 Sumitomo Pharma Oncology, Inc. Alk-5 inhibitors and uses thereof
KR20240035390A (ko) 2021-05-11 2024-03-15 오릭 파마슈티칼스, 인크. 폴로 유사 키나제 4 억제제
UY39832A (es) 2021-06-28 2023-01-31 Blueprint Medicines Corp Inhibidores de cdk2
CN116354938B (zh) * 2021-12-28 2024-02-20 沈阳药科大学 一类喹唑啉衍生物与其类似物的制备方法及应用
CN114276302B (zh) * 2022-01-11 2023-07-25 山东百启生物医药有限公司 一种制备2,4-二氨基喹唑啉衍生物的方法
WO2024003773A1 (en) 2022-07-01 2024-01-04 Pfizer Inc. 2,7-naphthyridine compounds as mastl inhibitors
CN117736198A (zh) * 2022-09-21 2024-03-22 科辉智药生物科技(深圳)有限公司 大环含氮冠醚化合物及其作为蛋白激酶抑制剂的应用
CN115403568B (zh) * 2022-09-21 2023-09-29 中山大学 一种喹唑啉类Aurora A共价抑制剂及其制备方法和应用

Family Cites Families (97)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US18436A (en) * 1857-10-20 And saml
US3133081A (en) * 1964-05-12 J-aminoindazole derivatives
US2585906A (en) 1952-02-12 Quaternary salts of pyrimdjines
US3935183A (en) * 1970-01-26 1976-01-27 Imperial Chemical Industries Limited Indazole-azo phenyl compounds
BE754242A (fr) * 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3755332A (en) * 1971-07-01 1973-08-28 Ciba Geigy Corp Substituted 4 indazolaminoquinolines
US3998951A (en) * 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
DE2458965C3 (de) 1974-12-13 1979-10-11 Bayer Ag, 5090 Leverkusen 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel
MA18829A1 (fr) 1979-05-18 1980-12-31 Ciba Geigy Ag Derives de la pyrimidine,procedes pour leur preparation,compositions pharmaceutiques contenant ces composes et leur utilisation therapeutique
DOP1981004033A (es) * 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102194L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
SE8102193L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
JPS58124773A (ja) 1982-01-20 1983-07-25 Mitsui Toatsu Chem Inc 5−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤
EP0136976A3 (de) 1983-08-23 1985-05-15 Ciba-Geigy Ag Verwendung von Phenylpyrimidinen als Pflanzenregulatoren
DE3725638A1 (de) 1987-08-03 1989-02-16 Bayer Ag Neue aryloxy (bzw. thio)aminopyrimidine
JPH0532662A (ja) 1990-11-09 1993-02-09 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5714493A (en) * 1991-05-10 1998-02-03 Rhone-Poulenc Rorer Pharmaceuticals, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5597920A (en) 1992-04-30 1997-01-28 Neurogen Corporation Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes
JPH0665237A (ja) * 1992-05-07 1994-03-08 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
ES2262137T3 (es) 1993-10-01 2006-11-16 Novartis Ag Derivados de pirimidinamina farmacologicamente activos y procedimientos para su preparacion.
AU700964B2 (en) 1994-11-10 1999-01-14 Cor Therapeutics, Inc. Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
IL117659A (en) * 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
US5935966A (en) 1995-09-01 1999-08-10 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
CA2230896A1 (en) 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US6716575B2 (en) * 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
ATE227283T1 (de) 1996-07-13 2002-11-15 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
JPH10130150A (ja) 1996-09-05 1998-05-19 Dainippon Pharmaceut Co Ltd 酢酸アミド誘導体からなる医薬
GB9619284D0 (en) * 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
EP0929553B1 (de) 1996-10-02 2005-03-16 Novartis AG Pyrimiderivate und verfahren zu ihrer herstellung
EP0932598A1 (de) 1996-10-11 1999-08-04 Warner-Lambert Company Asparat ester als inhibitoren von interleukin-1 beta-konvertierenden enzymen
WO1999018781A1 (en) 1997-10-10 1999-04-22 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
US6267952B1 (en) * 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
JP2000026421A (ja) 1998-01-29 2000-01-25 Kumiai Chem Ind Co Ltd ジアリ―ルスルフィド誘導体及び有害生物防除剤
DE69909756D1 (de) 1998-02-17 2003-08-28 Tularik Inc Antivirale pyrimidinderivate
ATE295177T1 (de) 1998-03-16 2005-05-15 Cytovia Inc Dipeptid kaspase inhibitoren und deren verwendung
AU763658B2 (en) 1998-06-02 2003-07-31 Osi Pharmaceuticals, Inc. Pyrrolo(2,3d)pyrimidine compositions and their use
EP1087963B1 (de) 1998-06-19 2004-08-25 Chiron Corporation Glycogen synthase kinase 3 inhibitoren
WO2000003901A1 (de) * 1998-07-16 2000-01-27 Continental Teves Ag & Co. Ohg Verfahren und vorrichtung zum ermitteln von kritischen fahrzuständen bei im fahrbetrieb befindlichen fahrzeugen
CA2339188A1 (en) * 1998-08-21 2000-03-02 Dupont Pharmaceuticals Company Isoxazolo¬4,5-d|pyrimidines as crf antagonists
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
EP1119567B1 (de) 1998-10-08 2005-05-04 AstraZeneca AB Chinazolin derivate
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
EP1144394B1 (de) 1999-01-13 2005-08-24 Warner-Lambert Company LLC 1-heterozyklus-substituierte diarylaminen
ATE329596T1 (de) 1999-03-30 2006-07-15 Novartis Pharma Gmbh Phthalazinderivate zur behandlung von entzündlicher erkrankungen
EP1185528A4 (de) 1999-06-17 2003-03-26 Shionogi Biores Corp Inhibitoren der il-12 herstellung
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
JP2003531103A (ja) 1999-08-12 2003-10-21 バーテックス ファーマシューティカルズ インコーポレイテッド c−JUNN−末端キナーゼ(JNK)および他のタンパク質キナーゼの阻害剤
EP1218360B1 (de) * 1999-10-07 2008-05-28 Amgen Inc., Triazin-kinase-hemmer
CZ20021703A3 (cs) 1999-11-30 2003-06-18 Pfizer Products Inc. 2,4-Diaminopyrimidinové sloučeniny užitečné jako imunosupresiva
ATE335489T1 (de) 1999-12-02 2006-09-15 Osi Pharm Inc Für adenosin a3, a2a und a3 rezeptoren spezifische verbindungen und deren verwendungen
MY125768A (en) 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6376489B1 (en) 1999-12-23 2002-04-23 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
SK14082001A3 (sk) * 2000-02-05 2002-03-05 Vertex Pharmaceuticals Incorporated Deriváty pyrazolu ako inhibítory ERK a farmaceutická kompozícia, ktorá ich obsahuje
CN1429222A (zh) * 2000-02-17 2003-07-09 安姆根有限公司 激酶抑制剂
GB0004890D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
ES2240446T3 (es) 2000-04-03 2005-10-16 Vertex Pharma Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.
EP1274706A1 (de) 2000-04-18 2003-01-15 Agouron Pharmaceuticals, Inc. Pyrazole zur inhibierung von proteinkinasen
JP3890184B2 (ja) * 2000-05-15 2007-03-07 Necパーソナルプロダクツ株式会社 電源装置及びその電力制御方法、情報処理機器
DE60133897D1 (de) * 2000-06-28 2008-06-19 Astrazeneca Ab Substituierte chinazolin-derivate und deren verwendung als aurora-2-kinase inhibitoren
CN1518543A (zh) 2000-08-31 2004-08-04 �Ʒ� 吡唑衍生物和它们作为蛋白激酶抑制剂的用途
US6610677B2 (en) * 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002022610A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Isoxazoles and their use as inhibitors of erk
US6613776B2 (en) * 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
IL154817A0 (en) 2000-09-15 2003-10-31 Vertex Pharma Pyrazole derivatives and pharmaceutical compositions containing the same
MXPA03002410A (es) 2000-09-20 2003-06-19 Merck Patent Gmbh 4-amino-quinazolinas.
US6641579B1 (en) * 2000-09-29 2003-11-04 Spectrasonics Imaging, Inc. Apparatus and method for ablating cardiac tissue
DE10061863A1 (de) * 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
EP1351691A4 (de) 2000-12-12 2005-06-22 Cytovia Inc Substituierte 2-aryl-4-arylaminopyrimidine und ihre analoge als aktivatoren von caspasen und apoptoseinduktoren, sowie deren verwendung
US6716851B2 (en) * 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
ES2272567T3 (es) * 2000-12-21 2007-05-01 Vertex Pharmaceuticals Incorporated Compuestos de pirazol utiles como inhibidores de proteina quinasas.
MY130778A (en) * 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
US6949544B2 (en) * 2001-03-29 2005-09-27 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
WO2002083667A2 (en) * 2001-04-13 2002-10-24 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
AU2002305205A1 (en) * 2001-04-20 2002-11-05 Jingrong Cao 9-deazaguanine derivatives as inhibitors of gsk-3
EP1404669A2 (de) * 2001-05-16 2004-04-07 Vertex Pharmaceuticals Incorporated Heterocyclisch substituierte pyrazole als inhibitoren von src und anderen protein kinasen
US6825190B2 (en) * 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
ES2271283T3 (es) * 2001-07-03 2007-04-16 Vertex Pharmaceuticals Incorporated Isoxazolil-pirimidinas como inhibidores de las proteinas quinasas src y lck.
WO2003026665A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
US6569499B2 (en) * 2001-10-02 2003-05-27 Xerox Corporation Apparatus and method for coating photoreceptor substrates
WO2003049739A1 (en) * 2001-12-07 2003-06-19 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as gsk-3 inhibitors
DE60314603T2 (de) * 2002-03-15 2008-02-28 Vertex Pharmaceuticals Inc., Cambridge Zusammensetzungen brauchbar als protein-kinase-inhibitoren
WO2003077921A1 (en) * 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
US20040009981A1 (en) * 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
US7179826B2 (en) * 2002-03-15 2007-02-20 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
AU2003237121A1 (en) * 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
WO2004005283A1 (en) * 2002-07-09 2004-01-15 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
WO2004013140A1 (en) 2002-08-02 2004-02-12 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
MX2009006690A (es) 2006-12-19 2009-07-31 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.

Also Published As

Publication number Publication date
US6989385B2 (en) 2006-01-24
EP1702920B1 (de) 2011-10-12
DE60120219T2 (de) 2007-04-12
ES2265452T3 (es) 2007-02-16
HK1060346A1 (en) 2004-08-06
CY1106297T1 (el) 2011-10-12
NO20032704L (no) 2003-08-21
US7087603B2 (en) 2006-08-08
AU2002246754B2 (en) 2006-06-08
ATE326463T1 (de) 2006-06-15
US20080287444A1 (en) 2008-11-20
JP2004517894A (ja) 2004-06-17
WO2002057259A2 (en) 2002-07-25
CA2432131A1 (en) 2002-08-01
HK1062565A1 (en) 2004-11-12
KR20030061466A (ko) 2003-07-18
NZ526469A (en) 2005-10-28
HK1061389A1 (en) 2004-09-17
US6653301B2 (en) 2003-11-25
DK1353916T3 (da) 2007-01-29
DE60126828D1 (de) 2007-04-05
US20040214814A1 (en) 2004-10-28
ES2265450T3 (es) 2007-02-16
NO20032703L (no) 2003-08-19
PT1353916E (pt) 2007-01-31
MY140377A (en) 2009-12-31
ATE326460T1 (de) 2006-06-15
EP1345928A2 (de) 2003-09-24
HK1059776A1 (en) 2004-07-16
ATE528303T1 (de) 2011-10-15
JP2008247920A (ja) 2008-10-16
NO328537B1 (no) 2010-03-15
HUP0400908A3 (en) 2010-03-29
NO20032736D0 (no) 2003-06-16
US20030105090A1 (en) 2003-06-05
KR100843114B1 (ko) 2008-07-02
KR20030061463A (ko) 2003-07-18
WO2002059112A2 (en) 2002-08-01
US6653300B2 (en) 2003-11-25
US7982037B2 (en) 2011-07-19
DE60126658D1 (de) 2007-03-29
NZ526473A (en) 2005-06-24
EP1345929B1 (de) 2006-05-17
SI1355905T1 (sl) 2007-08-31
NZ526468A (en) 2004-03-26
IL156408A0 (en) 2004-01-04
DE60119774T2 (de) 2007-05-16
ES2266095T3 (es) 2007-03-01
JP2008189682A (ja) 2008-08-21
EP1345925A2 (de) 2003-09-24
NZ526471A (en) 2005-08-26
NO20032704D0 (no) 2003-06-13
NO20032670L (no) 2003-08-15
WO2002062789A1 (en) 2002-08-15
MXPA03005605A (es) 2003-10-06
IL156369A0 (en) 2004-01-04
CN100436452C (zh) 2008-11-26
JP2004519479A (ja) 2004-07-02
US20030055068A1 (en) 2003-03-20
MXPA03005608A (es) 2003-10-06
TWI290551B (en) 2007-12-01
HK1060349A1 (en) 2004-08-06
JP2013213068A (ja) 2013-10-17
JP2009155352A (ja) 2009-07-16
JP2004516292A (ja) 2004-06-03
PL363244A1 (en) 2004-11-15
CA2432303C (en) 2010-04-13
AU2002234047A1 (en) 2002-07-01
DK1355905T3 (da) 2007-06-18
ES2265446T3 (es) 2007-02-16
DE60119776D1 (de) 2006-06-22
DE60119776T2 (de) 2007-05-16
US8697698B2 (en) 2014-04-15
JP2004518743A (ja) 2004-06-24
AR042169A1 (es) 2005-06-15
EP2264028A1 (de) 2010-12-22
US20030004161A1 (en) 2003-01-02
JP4234435B2 (ja) 2009-03-04
NO20032670D0 (no) 2003-06-12
DE60119777T2 (de) 2007-05-03
CA2432222A1 (en) 2002-08-15
MXPA03005609A (es) 2003-10-06
EP1345927B1 (de) 2006-05-17
WO2002059111A2 (en) 2002-08-01
NO20032671D0 (no) 2003-06-12
EP1345927A1 (de) 2003-09-24
JP2008222719A (ja) 2008-09-25
CN1487933A (zh) 2004-04-07
US8304414B2 (en) 2012-11-06
CA2432872A1 (en) 2002-06-27
WO2002050065A3 (en) 2002-10-24
ATE327989T1 (de) 2006-06-15
TW200716617A (en) 2007-05-01
EP1355905A1 (de) 2003-10-29
CN1486312A (zh) 2004-03-31
ATE340172T1 (de) 2006-10-15
DK1345922T3 (da) 2006-09-18
IL156389A (en) 2011-01-31
AU3116602A (en) 2002-07-01
US20040132781A1 (en) 2004-07-08
HUP0400641A2 (hu) 2004-06-28
HK1060347A1 (en) 2004-08-06
AR042397A1 (es) 2005-06-22
ES2375491T3 (es) 2012-03-01
US20030036543A1 (en) 2003-02-20
HK1062433A1 (en) 2004-11-05
EP1345926A2 (de) 2003-09-24
EP1345926B1 (de) 2006-05-17
ATE353890T1 (de) 2007-03-15
JP5249842B2 (ja) 2013-07-31
CN100340555C (zh) 2007-10-03
CA2432799A1 (en) 2002-06-27
PL210066B1 (pl) 2011-11-30
DE60119774D1 (de) 2006-06-22
BR0116411A (pt) 2003-11-11
NZ526472A (en) 2004-04-30
CN1486311A (zh) 2004-03-31
KR20030061468A (ko) 2003-07-18
NO328501B1 (no) 2010-03-01
US7427681B2 (en) 2008-09-23
AR042398A1 (es) 2005-06-22
EP1702920A1 (de) 2006-09-20
KR100875091B1 (ko) 2008-12-22
US6727251B2 (en) 2004-04-27
WO2002050065A2 (en) 2002-06-27
US20140187772A1 (en) 2014-07-03
US20030022885A1 (en) 2003-01-30
TWI313269B (en) 2009-08-11
IL156368A0 (en) 2004-01-04
HUP0400641A3 (en) 2010-03-29
MXPA03005610A (es) 2003-10-06
WO2002068415A1 (en) 2002-09-06
WO2002057259A3 (en) 2003-04-24
PT1355905E (pt) 2007-05-31
JP2004516291A (ja) 2004-06-03
KR100947185B1 (ko) 2010-03-15
JP2008260767A (ja) 2008-10-30
JP2005097322A (ja) 2005-04-14
CA2432303A1 (en) 2002-08-29
CN100406454C (zh) 2008-07-30
AU2002255452B2 (en) 2006-06-08
CA2432132C (en) 2008-07-29
EP1345922A1 (de) 2003-09-24
CA2432129A1 (en) 2002-07-25
MXPA03005612A (es) 2003-10-06
CN102250071A (zh) 2011-11-23
NO20032736L (no) 2003-08-18
SI1353916T1 (sl) 2007-02-28
KR20030061857A (ko) 2003-07-22
CA2432799C (en) 2008-08-19
BR0116493A (pt) 2003-09-30
RU2355688C2 (ru) 2009-05-20
WO2002050066A3 (en) 2003-01-23
KR100909665B1 (ko) 2009-07-29
CN100408573C (zh) 2008-08-06
ES2280313T3 (es) 2007-09-16
AP2003002816A0 (en) 2003-06-30
NO20032703D0 (no) 2003-06-13
KR20030061465A (ko) 2003-07-18
EP1353916B1 (de) 2006-09-20
ATE326462T1 (de) 2006-06-15
AU2001297619B2 (en) 2006-06-08
WO2002059111A3 (en) 2003-01-09
HUP0400639A3 (en) 2010-03-29
KR100889246B1 (ko) 2009-03-19
AR040925A1 (es) 2005-04-27
NZ526470A (en) 2006-03-31
DE60126828T2 (de) 2007-11-08
ATE354573T1 (de) 2007-03-15
EP1353916A2 (de) 2003-10-22
CN1549812A (zh) 2004-11-24
HUP0400638A2 (hu) 2004-06-28
CA2432131C (en) 2008-07-08
HK1060557A1 (en) 2004-08-13
WO2002050066A2 (en) 2002-06-27
AP1588A (en) 2006-03-06
PL363246A1 (en) 2004-11-15
US20030078275A1 (en) 2003-04-24
JP4160395B2 (ja) 2008-10-01
NZ526475A (en) 2005-06-24
CN1486310A (zh) 2004-03-31
EP1345929A2 (de) 2003-09-24
JP4160392B2 (ja) 2008-10-01
KR20030061464A (ko) 2003-07-18
HUP0400639A2 (hu) 2004-06-28
CA2432129C (en) 2008-08-26
DE60120219D1 (de) 2006-07-06
IL156369A (en) 2011-02-28
CA2432872C (en) 2008-09-23
CA2432223A1 (en) 2002-09-06
US7625913B2 (en) 2009-12-01
EP1345922B1 (de) 2006-05-31
HUP0400908A2 (hu) 2004-07-28
EP1355905B1 (de) 2007-02-21
CA2432132A1 (en) 2002-08-01
CA2432223C (en) 2008-05-20
KR20030061858A (ko) 2003-07-22
US20030004164A1 (en) 2003-01-02
US20040157893A1 (en) 2004-08-12
HUP0400842A2 (hu) 2004-07-28
IL156407A0 (en) 2004-01-04
US20130096128A1 (en) 2013-04-18
PL210414B1 (pl) 2012-01-31
ATE326461T1 (de) 2006-06-15
JP4210520B2 (ja) 2009-01-21
US20050038023A1 (en) 2005-02-17
JP2004517927A (ja) 2004-06-17
WO2002059112A3 (en) 2003-02-06
PT1345922E (pt) 2006-09-29
MXPA03005606A (es) 2003-10-06
DE60126658T2 (de) 2007-11-22
JP2004518703A (ja) 2004-06-24
JP2008189687A (ja) 2008-08-21
US20090312543A1 (en) 2009-12-17
US6664247B2 (en) 2003-12-16
RU2003122209A (ru) 2005-02-10
MXPA03005607A (es) 2003-10-06
WO2002066461A1 (en) 2002-08-29
NO330527B1 (no) 2011-05-09
DE60119775T2 (de) 2007-05-10
US20040167141A1 (en) 2004-08-26
AU2002231166B2 (en) 2008-02-21
JP2009286805A (ja) 2009-12-10
US7531536B2 (en) 2009-05-12
CA2432222C (en) 2008-07-29
AP2003002825A0 (en) 2003-09-30
JP4160389B2 (ja) 2008-10-01
US6656939B2 (en) 2003-12-02
IL156389A0 (en) 2004-01-04
EP1345928B1 (de) 2007-02-14
ES2272567T3 (es) 2007-05-01
NZ526474A (en) 2005-10-28
JP2008201808A (ja) 2008-09-04
AU2006201267B2 (en) 2010-07-29
AU2006201267A1 (en) 2006-04-27
NO20032671L (no) 2003-08-18
DE60119777D1 (de) 2006-06-22
JP2008247921A (ja) 2008-10-16
IL209827A0 (en) 2011-02-28
KR20030061467A (ko) 2003-07-18
JP2004517926A (ja) 2004-06-17
DE60119775D1 (de) 2006-06-22
MXPA03005611A (es) 2003-10-06
EP1345925B1 (de) 2006-05-17
DE60123283T2 (de) 2007-04-12

Similar Documents

Publication Publication Date Title
DE60119774D1 (de) Pyrazolverbindungen als proteinkinasehemmer
ATE327992T1 (de) Pyrazolverbindungen als protein-kinasehemmer
DE122008000002I1 (de) Pyrrol substituierte indolin-2-on protein kinase inhibitoren
DK1317448T4 (da) Pyrazolforbindelser anvendelige som proteinkinaseinhibitorer

Legal Events

Date Code Title Description
8364 No opposition during term of opposition