BR112013029201A2 - compostos de pirrolidinil ureia e pirrolidinil tioureia como inibidores de trka quinase - Google Patents

compostos de pirrolidinil ureia e pirrolidinil tioureia como inibidores de trka quinase

Info

Publication number
BR112013029201A2
BR112013029201A2 BR112013029201A BR112013029201A BR112013029201A2 BR 112013029201 A2 BR112013029201 A2 BR 112013029201A2 BR 112013029201 A BR112013029201 A BR 112013029201A BR 112013029201 A BR112013029201 A BR 112013029201A BR 112013029201 A2 BR112013029201 A2 BR 112013029201A2
Authority
BR
Brazil
Prior art keywords
pyrrolidinyl
trka kinase
kinase inhibitors
diseases
urea
Prior art date
Application number
BR112013029201A
Other languages
English (en)
Other versions
BR112013029201B1 (pt
Inventor
R Kolakowski Gabrielle
F Blake James
Seo Jeongbeob
Haas Julia
R Condroski Kevin
Huang Lily
Allen Shelley
W Andrews Steven
Kercher Timothy
Jiang Yutong
Original Assignee
Array Biopharma 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 Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of BR112013029201A2 publication Critical patent/BR112013029201A2/pt
Publication of BR112013029201B1 publication Critical patent/BR112013029201B1/pt

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
    • C07D403/02Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41921,2,3-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433Thidiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/14Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • 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
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

abstract compounds of formula i: i or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where r1, r2, ra, rb, rc, rd, x, y, b, and ring c are as defined herein, and wherein the y-b moiety and the nh-c(=x)-nh moiety are in the trans configuration, are inhibitors of trka kinase and are useful in the treatment of diseases which can be treated with a trka kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases. tradução do resumo resumo patente de invenção: "compostos de pirrolidinil ureia e pirrolidinil tioureia como inibidores de trka quinase". compostos de fórmula i: i ou estereoisômeros, tautômeros ou sais farmaceuticamente aceitáveis, ou solvatos ou pró-drogas dos mesmos, onde r1, r2, ra, rb, rc, rd, x, y, b, e anel c são como definidos aqui e em que a fração y-b e a fração nh-c(=x)-nh estão na configuração trans, são inibidores de trka quinase e são úteis no tratamento de doenças as quais podem ser tratadas com um inibidor de trka quinase, tal como dor, câncer, inflamação, doenças neurodegenerativas e certas doenças infecciosas.
BR112013029201-6A 2011-05-13 2012-05-09 Compostos de pirrolidinil ureia e pirrolidinil tioureia, seu processo de preparação, seu uso e composições farmacêuticas BR112013029201B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161485858P 2011-05-13 2011-05-13
US61/485,858 2011-05-13
PCT/US2012/037003 WO2012158413A2 (en) 2011-05-13 2012-05-09 Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors

Publications (2)

Publication Number Publication Date
BR112013029201A2 true BR112013029201A2 (pt) 2017-02-14
BR112013029201B1 BR112013029201B1 (pt) 2022-08-09

Family

ID=46614580

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013029201-6A BR112013029201B1 (pt) 2011-05-13 2012-05-09 Compostos de pirrolidinil ureia e pirrolidinil tioureia, seu processo de preparação, seu uso e composições farmacêuticas

Country Status (34)

Country Link
US (4) US9562055B2 (pt)
EP (1) EP2712358B1 (pt)
JP (4) JP5933902B2 (pt)
KR (2) KR102001364B1 (pt)
CN (3) CN103649076B (pt)
AR (1) AR086367A1 (pt)
AU (2) AU2012256237B2 (pt)
BR (1) BR112013029201B1 (pt)
CA (1) CA2835835C (pt)
CL (1) CL2013003257A1 (pt)
CO (1) CO6821961A2 (pt)
CR (1) CR20130646A (pt)
CY (1) CY1119014T1 (pt)
DK (1) DK2712358T3 (pt)
ES (1) ES2615738T3 (pt)
HR (1) HRP20161786T1 (pt)
HU (1) HUE030791T2 (pt)
IL (2) IL229377A (pt)
LT (1) LT2712358T (pt)
ME (1) ME02583B (pt)
MX (2) MX369142B (pt)
MY (1) MY173181A (pt)
NZ (1) NZ618795A (pt)
PL (1) PL2712358T3 (pt)
PT (1) PT2712358T (pt)
RS (1) RS55582B1 (pt)
RU (1) RU2606131C2 (pt)
SG (2) SG10201913053QA (pt)
SI (1) SI2712358T1 (pt)
SM (1) SMT201700035B (pt)
TW (2) TWI649315B (pt)
UA (1) UA114711C2 (pt)
UY (1) UY34067A (pt)
WO (1) WO2012158413A2 (pt)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
CN103965200B (zh) 2008-09-22 2016-06-08 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物
RS57221B2 (sr) 2008-10-22 2020-08-31 Array Biopharma Inc Jedinjenja supstituisanog pirazolo[1,5-]pirimidina kao inhibitori trk kinaze
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
EP2353598A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for use in the prevention and/or treatment of postoperative pain
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
RU2735545C2 (ru) 2010-05-20 2020-11-03 Эррэй Биофарма Инк. Макроциклические соединения в качестве ингибиторов киназы trk
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
RU2606131C2 (ru) * 2011-05-13 2017-01-10 Эррэй Биофарма Инк. СОЕДИНЕНИЯ ПИРРОЛИДИНИЛМОЧЕВИНЫ И ПИРРОЛИДИНИЛТИОМОЧЕВИНЫ КАК ИНГИБИТОРЫ КИНАЗЫ TrkA
EP2524694A1 (en) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
WO2014078328A1 (en) * 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078408A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
RS57001B1 (sr) * 2012-11-13 2018-05-31 Array Biopharma Inc Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kao inhibitori trka kinaze
WO2014078325A1 (en) * 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
UA117573C2 (uk) 2012-11-13 2018-08-27 Ерей Біофарма Інк. Біциклічні сполуки сечовини, тіосечовини, гуанідину й ціаногуанідину, придатні для лікування болю
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
US9969694B2 (en) 2012-11-13 2018-05-15 Array Biopharma Inc. N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078372A1 (en) * 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
CA2896187A1 (en) 2013-01-18 2014-07-24 F. Hoffmann-La Roche Ag 3-substituted pyrazoles and use as dlk inhibitors
EP2818166A1 (en) * 2013-06-26 2014-12-31 Laboratorios del Dr. Esteve S.A. Use of sigma receptor ligands for the prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS)
WO2015039334A1 (en) * 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
WO2015039333A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
TN2016000210A1 (en) 2013-11-28 2017-10-06 Kyorin Seiyaku Kk Urea derivative or pharmacologically acceptable salt thereof.
AU2014364647A1 (en) 2013-12-17 2016-06-23 Laboratorios Del Dr. Esteve, S.A. Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) and Sigma receptor ligands combinations
WO2015091645A1 (en) 2013-12-18 2015-06-25 Basf Se Azole compounds carrying an imine-derived substituent
JP2016540811A (ja) 2013-12-20 2016-12-28 ファイザー・リミテッドPfizer Limited N−アシルピペリジンエーテルトロポミオシン関連キナーゼ阻害剤
WO2015143652A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143654A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143653A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015159175A1 (en) 2014-04-15 2015-10-22 Pfizer Inc. Tropomyosin-related kinase inhibitors containing both a 1h-pyrazole and a pyrimidine moiety
EP3140298A1 (en) 2014-05-07 2017-03-15 Pfizer Inc. Tropomyosin-related kinase inhibitors
HUE045340T2 (hu) * 2014-05-15 2019-12-30 Array Biopharma Inc 1-((3S,4R)-4-(3-fluorfenil)-1-(2-metoxietil)pirrolidin-3-il)-3-(4-metil-3-(2- metilpirimidin-5-il)-1-fenil-1H-pirazol-5-il)karbamid mint TrkA kináz inhibitor
WO2016009296A1 (en) 2014-07-16 2016-01-21 Pfizer Inc. N-acylpiperidine ether tropomyosin-related kinase inhibitors
WO2016020784A1 (en) 2014-08-05 2016-02-11 Pfizer Inc. N-acylpyrrolidine ether tropomyosin-related kinase inhibitors
US10160727B2 (en) * 2014-08-06 2018-12-25 Shionogi & Co., Ltd. Heterocycle and carbocycle derivatives having TrkA inhibitory activity
SG11201703962XA (en) 2014-11-16 2017-06-29 Array Biopharma Inc Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
BR112017009701B1 (pt) 2014-12-08 2021-09-08 Fmc Corporation Composto e métodos de preparação de compostos
WO2016161572A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
PE20180234A1 (es) * 2015-05-27 2018-01-31 Kyorin Seiyaku Kk Derivado de urea o sal farmacologicamente aceptable del mismo
MA44936A1 (fr) 2015-06-01 2021-09-30 Loxo Oncology Inc Méthodes de diagnostic et de traitement du cancer
EP3330256B1 (en) * 2015-07-07 2021-06-16 Shionogi & Co., Ltd. HETEROCYCLIC DERIVATIVE HAVING TrkA-INHIBITING ACTIVITY
AU2016291676B2 (en) 2015-07-16 2020-04-30 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors
RU2744852C2 (ru) 2015-10-26 2021-03-16 Локсо Онколоджи, Инк. Точечные мутации в устойчивых к ингибитору trk злокачественных опухолях и связанные с ними способы
CA3006911A1 (en) 2015-12-22 2017-06-29 Syngenta Participations Ag Pesticidally active pyrazole derivatives
EP3412663B1 (en) 2016-02-04 2022-09-07 Shionogi & Co., Ltd. Nitrogen-containing heterocycle and carbocycle derivatives having trka inhibitory activity
KR102400423B1 (ko) 2016-04-04 2022-05-19 록쏘 온콜로지, 인코포레이티드 (s)-n-(5-((r)-2-(2,5-디플루오로페닐)-피롤리딘-1-일)-피라졸로[1,5-a]피리미딘-3-일)-3-하이드록시피롤리딘-1-카복사미드의 액체 제형
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CN109310694A (zh) 2016-04-04 2019-02-05 洛克索肿瘤学股份有限公司 治疗儿科癌症的方法
LT3800189T (lt) 2016-05-18 2023-10-10 Loxo Oncology, Inc. (s)-n-(5-((r)-2-(2,5-difluorfenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3- il)-3-hidroksipirolidin-1-karboksamido gavimas
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JP6888101B2 (ja) 2017-01-18 2021-06-16 アレイ バイオファーマ インコーポレイテッド RETキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピラジン化合物
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
WO2018185187A1 (en) 2017-04-05 2018-10-11 Syngenta Participations Ag Pesticidally active pyrazole derivatives
CA3070497A1 (en) 2017-06-19 2018-12-27 Syngenta Participations Ag Pesticidally active pyrazole derivatives
JP2019026646A (ja) * 2017-08-03 2019-02-21 塩野義製薬株式会社 含窒素複素環および炭素環誘導体を含有する、疼痛の治療および/または予防用医薬組成物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
EP3700576A1 (en) 2017-10-26 2020-09-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
WO2019099307A1 (en) * 2017-11-17 2019-05-23 Hepagene Therapeutics, Inc. Urea derivatives as inhibitors of ask1
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
TW201938169A (zh) 2018-01-18 2019-10-01 美商亞雷生物製藥股份有限公司 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物
IL277044B2 (en) 2018-03-05 2023-10-01 Bristol Myers Squibb Co Phenylpyrrolidinone formyl peptide 2 receptor agonists
MA52218A (fr) 2018-03-29 2021-02-17 Loxo Oncology Inc Traitement de cancers associés à trk
TW202014408A (zh) * 2018-07-03 2020-04-16 美商Ifm Due有限公司 用於治療與sting活性相關之病症的化合物及組合物
WO2020011227A1 (zh) * 2018-07-12 2020-01-16 南京明德新药研发有限公司 吡咯烷基脲衍生物及其在TrkA相关疾病的应用
GB201811825D0 (en) 2018-07-19 2018-09-05 Benevolentai Bio Ltd Organic compounds
US20210330643A1 (en) 2018-07-31 2021-10-28 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
GB201813791D0 (en) 2018-08-23 2018-10-10 Benevolental Bio Ltd Organic compounds
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのfgfr阻害剤としての7-((3,5-ジメトキシフェニル)アミノ)キノキサリン誘導体
WO2020127345A1 (en) 2018-12-21 2020-06-25 Syngenta Participations Ag Pesticidally active pyrazole derivatives
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
JP7439124B2 (ja) * 2019-11-14 2024-02-27 ユニマテック株式会社 含フッ素ピラゾール化合物およびその製造方法
JP7337279B2 (ja) * 2020-01-10 2023-09-01 ▲ザン▼州片仔▲ファン▼薬業股▲フン▼有限公司 ピロリジニル尿素誘導体の調製方法
WO2021139794A1 (zh) * 2020-01-10 2021-07-15 漳州片仔癀药业股份有限公司 一种吡咯烷基脲衍生物的晶型及其应用
JP2023511170A (ja) 2020-01-22 2023-03-16 ベネボレントエーアイ バイオ リミティド 医薬組成物及びその使用
EP4093376A1 (en) 2020-01-22 2022-11-30 BenevolentAI Bio Limited Pharmaceutical compositions and their uses
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2022003377A1 (en) 2020-07-02 2022-01-06 Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A. Thieno[3,4-c]pyrazol-3-yl acetamides as autotaxin inhibitors
EP4274660A1 (en) * 2021-01-08 2023-11-15 IFM Due, Inc. Compounds and compositions for treating conditions associated with sting activity
EP4323353A1 (en) * 2021-04-12 2024-02-21 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (trk) degradation compounds and methods of use
WO2022234287A1 (en) 2021-05-06 2022-11-10 Benevolentai Bio Limited Imidazopyridazine derivatives useful as trk inhibitors
CN114031556B (zh) * 2021-11-08 2023-03-31 温州大学 一种绿色的一锅法制备5-氨基-n-芳基-3-芳基吡唑类化合物的合成方法
US11970499B1 (en) * 2023-12-22 2024-04-30 King Faisal University Pyrazolo[1,5-c]pyrimidine compounds as CK2 inhibitors

Family Cites Families (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63198664A (ja) * 1986-03-31 1988-08-17 Sankyo Co Ltd キノロンカルボン酸誘導体
DE3906365A1 (de) * 1988-07-15 1990-01-18 Bayer Ag 7-(1-pyrrolidinyl)-3-chinolon- und -naphthyridoncarbonsaeure-derivate, verfahren sowie substituierte (oxa)diazabicyclooctane und -nonane als zwischenprodukte zu ihrer herstellung, und sie enthaltende antibakterielle mittel und futterzusatzstoffe
WO1992010492A1 (en) * 1990-12-05 1992-06-25 Synphar Laboratories, Inc. 7-substituted-6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid compounds useful as antibacterial agents
JP3086837B2 (ja) * 1991-06-06 2000-09-11 三協化学株式会社 3−アミノピロリジン類の製造方法
ES2163512T3 (es) * 1994-06-14 2002-02-01 Dainippon Pharmaceutical Co Nuevo compuesto, procedimiento para producirlo, y agente antitumoral.
AU679887B2 (en) 1995-09-11 1997-07-10 Nihon Nohyaku Co., Ltd. Azole derivatives, their use, production and usage
CA2206201A1 (en) 1996-05-29 1997-11-29 Yoshiaki Isobe Pyrazole derivatives and their pharmaceutical use
US6083986A (en) 1996-07-26 2000-07-04 Icagen, Inc. Potassium channel inhibitors
US5998424A (en) 1997-06-19 1999-12-07 Dupont Pharmaceuticals Company Inhibitors of factor Xa with a neutral P1 specificity group
AU1367599A (en) 1997-11-03 1999-05-24 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
ES2155817T3 (es) 1997-12-22 2007-06-16 Bayer Pharmaceuticals Corp. Inhibicion de la actividad de la quinasa p38 utilizando ureas heterociclicas sustituidas con arilo y heteroarilo.
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
US6197798B1 (en) 1998-07-21 2001-03-06 Novartis Ag Amino-benzocycloalkane derivatives
WO2000039116A1 (fr) 1998-12-25 2000-07-06 Teikoku Hormone Mfg. Co., Ltd. Derives d'aminopyrazole
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
US6387900B1 (en) 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
EP1220836A2 (en) * 1999-10-15 2002-07-10 Bristol-Myers Squibb Pharma Company Benzylcycloalkyl amines as modulators of chemokine receptor activity
US6410533B1 (en) 2000-02-10 2002-06-25 Genzyme Corporation Antibacterial compounds
AU2001273129A1 (en) 2000-06-30 2002-01-14 Bristol-Myers Squibb Pharma Company N-ureidoheterocycloaklyl-piperidines as modulators of chemokine receptor activity
JP2004534017A (ja) 2001-04-27 2004-11-11 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 Baceのインヒビター
GB0110901D0 (en) 2001-05-02 2001-06-27 Smithkline Beecham Plc Novel Compounds
WO2003037274A2 (en) 2001-11-01 2003-05-08 Icagen, Inc. Pyrazole-amides and-sulfonamides
EP1451156A4 (en) 2001-11-27 2005-05-25 Merck & Co Inc 4-AMINOQUINOLINE COMPOUNDS
SE0104248D0 (sv) 2001-12-14 2001-12-14 Astrazeneca Ab Method of treatment
EP1506172B1 (en) 2002-05-20 2011-03-30 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
JP4498133B2 (ja) 2002-07-02 2010-07-07 シェーリング コーポレイション 新規神経ペプチドyy5レセプターアンタゴニスト
DE60335957D1 (de) 2002-10-08 2011-03-17 Rinat Neuroscience Corp Verfahren zur behandlung von postoperativen schmerzen durch verabreichung eines antikörpers gegen nervenwachstumsfaktor und diesen enthaltende zusammensetzungen
JP4448821B2 (ja) * 2002-10-30 2010-04-14 アステラス製薬株式会社 セフェム化合物
US20040171075A1 (en) 2002-12-31 2004-09-02 Flynn Daniel L Modulation of protein functionalities
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
WO2005024755A2 (en) 2002-12-31 2005-03-17 Deciphera Pharmaceuticals, Llc. Medicaments for the treatment of neurodegenerative disorders or diabetes
AU2004247721C1 (en) 2003-06-12 2011-12-22 Abbvie Inc. Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
WO2005048953A2 (en) 2003-11-13 2005-06-02 Ambit Biosciences Corporation Amide derivatives as kinase modulators
MY141220A (en) * 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
US20080220497A1 (en) 2003-12-24 2008-09-11 Flynn Daniel L Modulation of protein functionalities
JP4573223B2 (ja) * 2004-01-23 2010-11-04 東レ・ファインケミカル株式会社 光学活性trans−4−アミノ−1−ベンジル−3−ピロリジノールの製造方法
ATE517885T1 (de) * 2004-04-30 2011-08-15 Bayer Healthcare Llc Substituierte pyrazolyl-harnstoff-derivate zur behandlung von krebs
JP2008509179A (ja) * 2004-08-09 2008-03-27 グラクソ グループ リミテッド グルタミン酸受容体を強化する化合物および医学におけるその使用
US20080081833A1 (en) 2004-12-20 2008-04-03 Astrazeneca Ab Novel Pyrazole Derivatives And Their Use As Modulators Of Nicotinic Acetylcholine Receptors
EP2942349A1 (en) 2004-12-23 2015-11-11 Deciphera Pharmaceuticals, LLC Enzyme modulators and treatments
US20090312349A1 (en) 2004-12-23 2009-12-17 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
AU2005317928B2 (en) 2004-12-24 2010-06-10 Astrazeneca Ab Heterocyclic compounds as CCR2b antagonists
EP1836188A1 (en) 2004-12-30 2007-09-26 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
WO2010104488A1 (en) 2009-02-19 2010-09-16 University Of Connecticut Novel hetero pyrrole analogs acting on cannapinoid receptors
GB0510141D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
US20060281768A1 (en) 2005-06-10 2006-12-14 Gaul Michael D Thienopyrimidine and thienopyridine kinase modulators
WO2007059202A2 (en) 2005-11-15 2007-05-24 Bayer Healthcare Ag Pyrazolyl urea derivatives useful in the treatment of cancer
US7514435B2 (en) * 2005-11-18 2009-04-07 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
JP2009518298A (ja) 2005-12-01 2009-05-07 バイエル ヘルスケア リミティド ライアビリティ カンパニー 癌治療に有用な尿素化合物
UA94733C2 (ru) 2006-01-31 2011-06-10 Эррей Биофарма Инк. Ингибиторы киназы и способы их использования
GB0607953D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
WO2008016811A2 (en) 2006-07-31 2008-02-07 Neurogen Corporation Aminopiperidines and realted compounds
EP2049542B1 (en) 2006-08-09 2012-09-19 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US7897762B2 (en) 2006-09-14 2011-03-01 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of proliferative diseases
US8188113B2 (en) 2006-09-14 2012-05-29 Deciphera Pharmaceuticals, Inc. Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US7790756B2 (en) 2006-10-11 2010-09-07 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
CL2007003627A1 (es) 2006-12-15 2008-07-25 Bayer Schering Pharma Ag Compuestos derivados de 3-h-pirazolopiridinas; metodo de preparacion; composicion farmaceutica; y uso para el tratamiento de enfermedades de crecimiento vascular desregulado tal como leucemia mielogena aguda, retinopatia, artritis reumatoide, psorias
AU2008242720A1 (en) 2007-04-20 2008-10-30 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
JP5203449B2 (ja) * 2007-04-20 2013-06-05 エフ.ホフマン−ラ ロシュ アーゲー 二重nk1/nk3受容体アンタゴニストとしてのピロリジン誘導体
WO2008150899A1 (en) 2007-05-29 2008-12-11 Emory University Combination therapies for treatment of cancer and inflammatory diseases
AR067630A1 (es) 2007-07-12 2009-10-21 Novartis Ag Soluciones farmaceuticas de telbivudina y metodo de tratamiento
ITMI20071731A1 (it) 2007-09-06 2009-03-07 Univ Degli Studi Genova Nuovi derivati ureici dell'acido 1h-pirazol-4-carbossilico con attivita inibente nei confronti della chemiotassi di neutrofili
EP2227460B1 (en) * 2007-10-24 2012-06-20 Cancer Research Technology Limited Therapeutic oxy-phenyl-aryl compounds and their use
EP2070929A1 (en) * 2007-12-11 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
DK2268623T3 (en) 2008-03-17 2015-06-29 Ambit Biosciences Corp QUINAZOLINE DERIVATIVES AS RAF CHINESE MODULATORS AND PROCEDURES FOR USE THEREOF
KR101324804B1 (ko) 2008-05-13 2013-11-01 아이알엠 엘엘씨 키나제 억제제로서의 질소 함유 융합 헤테로사이클 및 그의 조성물
CA2728054A1 (en) * 2008-06-16 2009-12-23 F. Hoffmann-La Roche Ag Pyrrolidine derivatives as nk2 receptor antagonists
JP5816087B2 (ja) 2008-08-29 2015-11-18 エンメエッセディ・イタリア・エッセ・エッレ・エッレ Smoアンタゴニストとしての飽和二環式複素環誘導体
USRE49686E1 (en) 2008-09-19 2023-10-10 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use of same
CN103965200B (zh) 2008-09-22 2016-06-08 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物
MX2011003312A (es) 2008-10-09 2011-04-26 Hoffmann La Roche Derivados de pirrolidina n-bencilo.
RS57221B2 (sr) * 2008-10-22 2020-08-31 Array Biopharma Inc Jedinjenja supstituisanog pirazolo[1,5-]pirimidina kao inhibitori trk kinaze
US8022099B2 (en) * 2008-11-03 2011-09-20 Hoffmann-La Roche Inc. N-benzyl pyrrolidine derivatives
ES2605811T3 (es) 2008-11-19 2017-03-16 Merial, Inc. Derivados de 1-arilpirazol diméricos
KR101805754B1 (ko) 2008-12-08 2017-12-07 먼디파머 인터내셔널 코포레이션 리미티드 단백질 수용체 티로신 키나아제 억제제의 조성물
EP2367824B1 (en) 2008-12-23 2016-03-23 AbbVie Inc. Anti-viral derivatives of pyrimidine
GB0904285D0 (en) * 2009-03-12 2009-04-22 Prosidion Ltd Compounds for the treatment of metabolic disorders
US8680139B2 (en) * 2009-04-01 2014-03-25 Progenra Anti-neoplastic compounds, compositions and methods
EP2426135A4 (en) 2009-04-27 2013-02-20 Shionogi & Co UREA DERIVATIVE WITH PI3K-INHIBITING EFFECT
US20120083476A1 (en) 2009-06-05 2012-04-05 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
EP2467137A1 (en) 2009-08-19 2012-06-27 Ambit Biosciences Corporation Biaryl compounds and methods of use thereof
US20120220564A1 (en) 2009-09-18 2012-08-30 Zalicus Pharmaceuticals Ltd. Selective calcium channel modulators
US20110144081A1 (en) * 2009-12-15 2011-06-16 Henner Knust Pyrrolidine derivatives
US20110152233A1 (en) * 2009-12-18 2011-06-23 Henner Knust Pyrrolidine compounds
RU2735545C2 (ru) 2010-05-20 2020-11-03 Эррэй Биофарма Инк. Макроциклические соединения в качестве ингибиторов киназы trk
WO2011150198A1 (en) 2010-05-27 2011-12-01 Ambit Biosciences Corporation Azolyl urea compounds and methods of use thereof
BR112013002212A2 (pt) * 2010-07-29 2017-09-26 Merck Patent Gmbh carboxamidas aza-heterocíclicas de aminas cíclicas
US9242981B2 (en) * 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
AR083904A1 (es) * 2010-11-18 2013-04-10 Prosidion Ltd Derivados de 1,4-pirrolidinas disustituidos y 3-il-aminas y sus usos en el tratamiento de desordenes metabolicos
RU2606131C2 (ru) 2011-05-13 2017-01-10 Эррэй Биофарма Инк. СОЕДИНЕНИЯ ПИРРОЛИДИНИЛМОЧЕВИНЫ И ПИРРОЛИДИНИЛТИОМОЧЕВИНЫ КАК ИНГИБИТОРЫ КИНАЗЫ TrkA
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2013096226A1 (en) 2011-12-19 2013-06-27 Abbvie Inc. Trpv1 antagonists
US9181261B2 (en) 2012-05-22 2015-11-10 Merck Sharp & Dohme Corp. TrkA kinase inhibitors, compositions and methods thereof
RU2660429C2 (ru) 2012-09-28 2018-07-06 Мерк Шарп И Доум Корп. Новые соединения, которые являются ингибиторами erk
WO2014052566A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
UA117573C2 (uk) 2012-11-13 2018-08-27 Ерей Біофарма Інк. Біциклічні сполуки сечовини, тіосечовини, гуанідину й ціаногуанідину, придатні для лікування болю
US9969694B2 (en) 2012-11-13 2018-05-15 Array Biopharma Inc. N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
RS57001B1 (sr) * 2012-11-13 2018-05-31 Array Biopharma Inc Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kao inhibitori trka kinaze
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078408A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2015039333A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF

Also Published As

Publication number Publication date
DK2712358T3 (en) 2017-02-06
SMT201700035B (it) 2017-03-08
EP2712358A2 (en) 2014-04-02
CN108329246A (zh) 2018-07-27
CO6821961A2 (es) 2013-12-31
KR20140037872A (ko) 2014-03-27
TW201249831A (en) 2012-12-16
JP2014514360A (ja) 2014-06-19
RS55582B1 (sr) 2017-06-30
TWI649315B (zh) 2019-02-01
IL252841A0 (en) 2017-08-31
PL2712358T3 (pl) 2017-05-31
SG194902A1 (en) 2013-12-30
JP2017171672A (ja) 2017-09-28
HRP20161786T1 (hr) 2017-03-10
ES2615738T3 (es) 2017-06-08
NZ618795A (en) 2015-07-31
ME02583B (me) 2017-06-20
SG10201913053QA (en) 2020-03-30
WO2012158413A3 (en) 2013-05-10
CN105130967B (zh) 2018-04-17
PT2712358T (pt) 2017-02-20
JP6382867B2 (ja) 2018-08-29
AU2017201418A1 (en) 2017-03-23
SI2712358T1 (sl) 2017-03-31
KR20190031585A (ko) 2019-03-26
AU2017201418B2 (en) 2018-11-22
MX347952B (es) 2017-05-19
AU2012256237B2 (en) 2017-01-05
CN108329246B (zh) 2021-02-26
BR112013029201B1 (pt) 2022-08-09
CN105130967A (zh) 2015-12-09
CY1119014T1 (el) 2018-01-10
KR102001364B1 (ko) 2019-07-22
RU2606131C2 (ru) 2017-01-10
US10323022B2 (en) 2019-06-18
US9878997B2 (en) 2018-01-30
CA2835835A1 (en) 2012-11-22
CR20130646A (es) 2014-03-11
JP5933902B2 (ja) 2016-06-15
WO2012158413A2 (en) 2012-11-22
IL252841B (en) 2018-03-29
US9562055B2 (en) 2017-02-07
MY173181A (en) 2020-01-02
MX369142B (es) 2019-10-30
IL229377A0 (en) 2014-01-30
US20150166564A1 (en) 2015-06-18
RU2013155456A (ru) 2015-06-20
US20170217936A1 (en) 2017-08-03
KR101960555B1 (ko) 2019-03-20
EP2712358B1 (en) 2016-12-21
TW201736363A (zh) 2017-10-16
CN103649076B (zh) 2015-09-09
US20180334450A1 (en) 2018-11-22
JP2019001819A (ja) 2019-01-10
HUE030791T2 (en) 2017-06-28
CA2835835C (en) 2019-04-02
JP2016128500A (ja) 2016-07-14
AU2012256237A1 (en) 2014-01-09
TWI589573B (zh) 2017-07-01
AR086367A1 (es) 2013-12-11
LT2712358T (lt) 2017-01-25
CL2013003257A1 (es) 2014-05-23
UY34067A (es) 2013-11-29
UA114711C2 (uk) 2017-07-25
MX2013013342A (es) 2014-06-11
CN103649076A (zh) 2014-03-19
US20190359597A1 (en) 2019-11-28
IL229377A (en) 2017-06-29

Similar Documents

Publication Publication Date Title
BR112013029201A2 (pt) compostos de pirrolidinil ureia e pirrolidinil tioureia como inibidores de trka quinase
BR112015010875A2 (pt) compostos de n-pirrolidinil, n'-pirazolil-ureia, tioureia, guanidina e cianoguanidina como inibidores de trka quinase
PH12015500938A1 (en) Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
BR112017010882B8 (pt) Compostos de n-((het)-arilmetil)-heteroaril-carboxamidas como inibidores de calicreína plasmática e seus usos
MX2015008957A (es) Fluoro-[1,3]oxazinas como inhibidores de beta-secretasa 1 (bace1).
MX2012003644A (es) Compuestos de 2-piridona empleados como inhibidores de la elastasa neutrofila.
BR112015016293A2 (pt) derivados de benzilamina
HK1137028A1 (en) Phosphadiazine hcv polymerase inhibitors iv
PH12015502365B1 (en) Bace1 inhibitors
UY31860A (es) Piridinas de tiazolo como inhibidoras de la adn girasa
CO7151509A2 (es) Difluoro-hexahidro-ciclopentaoxacinilos y difluoro-hexahidro-benzooxacinilos como inhibidores de bace1
CO7131369A2 (es) 5-amino[1,4]tiazinas como inhibidores de bace1
PH12015500185B1 (en) Azaheterocycles as bir2 and/or bir3 inhibitors
MY151198A (en) A medicament for treating dengue

Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07G Grant request does not fulfill article 229-c lpi (prior consent of anvisa) [chapter 7.7 patent gazette]

Free format text: NOTIFICACAO DE DEVOLUCAO DO PEDIDO EM FUNCAO DA REVOGACAO DO ART. 229-C DA LEI NO 9.279, DE 1996, POR FORCA DA LEI NO 14.195, DE 2021

B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B09X Republication of the decision to grant [chapter 9.1.3 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 09/05/2012, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF, QUE DETERMINA A ALTERACAO DO PRAZO DE CONCESSAO.