JP6740354B2 - オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 - Google Patents
オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 Download PDFInfo
- Publication number
- JP6740354B2 JP6740354B2 JP2018536715A JP2018536715A JP6740354B2 JP 6740354 B2 JP6740354 B2 JP 6740354B2 JP 2018536715 A JP2018536715 A JP 2018536715A JP 2018536715 A JP2018536715 A JP 2018536715A JP 6740354 B2 JP6740354 B2 JP 6740354B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- group
- optionally substituted
- formula
- racemates
- 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 - Fee Related
Links
- 230000004900 autophagic degradation Effects 0.000 title claims description 13
- 108090000623 proteins and genes Proteins 0.000 title claims description 6
- 102000004169 proteins and genes Human genes 0.000 title claims description 6
- 102000011420 Phospholipase D Human genes 0.000 title description 13
- 108090000553 Phospholipase D Proteins 0.000 title description 13
- 238000000034 method Methods 0.000 title description 11
- 239000012190 activator Substances 0.000 title description 7
- 150000001875 compounds Chemical class 0.000 claims description 73
- 150000003839 salts Chemical class 0.000 claims description 37
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 208000024827 Alzheimer disease Diseases 0.000 claims description 13
- 230000004770 neurodegeneration Effects 0.000 claims description 9
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 9
- 208000034799 Tauopathies Diseases 0.000 claims description 4
- 230000002708 enhancing effect Effects 0.000 claims description 4
- 239000000203 mixture Substances 0.000 description 29
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 16
- 125000005843 halogen group Chemical group 0.000 description 16
- 125000003118 aryl group Chemical group 0.000 description 14
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 description 13
- 125000004432 carbon atom Chemical group C* 0.000 description 12
- 125000000753 cycloalkyl group Chemical group 0.000 description 12
- 125000005842 heteroatom Chemical group 0.000 description 12
- 229910052757 nitrogen Inorganic materials 0.000 description 12
- 229910052760 oxygen Inorganic materials 0.000 description 12
- 229910052717 sulfur Inorganic materials 0.000 description 12
- 125000005000 thioaryl group Chemical group 0.000 description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- 229910052799 carbon Inorganic materials 0.000 description 6
- 101001040875 Homo sapiens Glucosidase 2 subunit beta Proteins 0.000 description 5
- 101000730665 Homo sapiens Phospholipase D1 Proteins 0.000 description 5
- 101000964266 Loxosceles laeta Dermonecrotic toxin Proteins 0.000 description 5
- 102100032967 Phospholipase D1 Human genes 0.000 description 5
- 230000015572 biosynthetic process Effects 0.000 description 5
- 238000003786 synthesis reaction Methods 0.000 description 5
- 102000013498 tau Proteins Human genes 0.000 description 5
- 108010026424 tau Proteins Proteins 0.000 description 5
- 208000004051 Chronic Traumatic Encephalopathy Diseases 0.000 description 4
- 201000011240 Frontotemporal dementia Diseases 0.000 description 4
- 210000004957 autophagosome Anatomy 0.000 description 4
- 210000004556 brain Anatomy 0.000 description 4
- 208000017004 dementia pugilistica Diseases 0.000 description 4
- 206010012289 Dementia Diseases 0.000 description 3
- JCABVIFDXFFRMT-DIPNUNPCSA-N [(2r)-1-[ethoxy(hydroxy)phosphoryl]oxy-3-hexadecanoyloxypropan-2-yl] octadec-9-enoate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OCC)OC(=O)CCCCCCCC=CCCCCCCCC JCABVIFDXFFRMT-DIPNUNPCSA-N 0.000 description 3
- 230000004913 activation Effects 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 235000003642 hunger Nutrition 0.000 description 3
- 150000003904 phospholipids Chemical class 0.000 description 3
- 230000037351 starvation Effects 0.000 description 3
- 102000013455 Amyloid beta-Peptides Human genes 0.000 description 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 description 2
- 208000023105 Huntington disease Diseases 0.000 description 2
- 208000010191 Osteitis Deformans Diseases 0.000 description 2
- 208000027067 Paget disease of bone Diseases 0.000 description 2
- 208000018737 Parkinson disease Diseases 0.000 description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 2
- XDHNQDDQEHDUTM-UHFFFAOYSA-N bafliomycin A1 Natural products COC1C=CC=C(C)CC(C)C(O)C(C)C=C(C)C=C(OC)C(=O)OC1C(C)C(O)C(C)C1(O)OC(C(C)C)C(C)C(O)C1 XDHNQDDQEHDUTM-UHFFFAOYSA-N 0.000 description 2
- 208000016738 bone Paget disease Diseases 0.000 description 2
- 210000003618 cortical neuron Anatomy 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 210000003712 lysosome Anatomy 0.000 description 2
- 230000001868 lysosomic effect Effects 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 230000036963 noncompetitive effect Effects 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 238000001262 western blot Methods 0.000 description 2
- WZJWWTFRSPUCDG-UHFFFAOYSA-N 1-chloro-7-fluoroisoquinoline Chemical compound C1=CN=C(Cl)C2=CC(F)=CC=C21 WZJWWTFRSPUCDG-UHFFFAOYSA-N 0.000 description 1
- 208000011403 Alexander disease Diseases 0.000 description 1
- 206010001881 Alveolar proteinosis Diseases 0.000 description 1
- 206010059245 Angiopathy Diseases 0.000 description 1
- 208000010482 CADASIL Diseases 0.000 description 1
- 208000002177 Cataract Diseases 0.000 description 1
- 208000033221 Cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy Diseases 0.000 description 1
- 208000033935 Cerebral autosomal dominant arteriopathy-subcortical infarcts-leukoencephalopathy Diseases 0.000 description 1
- 101100163433 Drosophila melanogaster armi gene Proteins 0.000 description 1
- LHABRXRGDLASIH-UHFFFAOYSA-N FIPI Chemical compound C12=CC=CC=C2NC(=O)N1C(CC1)CCN1CCNC(=O)C1=CC2=CC(F)=CC=C2N1 LHABRXRGDLASIH-UHFFFAOYSA-N 0.000 description 1
- 101000605630 Homo sapiens Phosphatidylinositol 3-kinase catalytic subunit type 3 Proteins 0.000 description 1
- 208000021642 Muscular disease Diseases 0.000 description 1
- 201000009623 Myopathy Diseases 0.000 description 1
- 101150012367 PLD1 gene Proteins 0.000 description 1
- 206010057249 Phagocytosis Diseases 0.000 description 1
- 102100038329 Phosphatidylinositol 3-kinase catalytic subunit type 3 Human genes 0.000 description 1
- 208000024777 Prion disease Diseases 0.000 description 1
- 208000037065 Subacute sclerosing leukoencephalitis Diseases 0.000 description 1
- 206010042297 Subacute sclerosing panencephalitis Diseases 0.000 description 1
- 206010048327 Supranuclear palsy Diseases 0.000 description 1
- 206010002022 amyloidosis Diseases 0.000 description 1
- 230000004908 autophagic flux Effects 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 208000016886 cerebral arteriopathy with subcortical infarcts and leukoencephalopathy Diseases 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000001086 cytosolic effect Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 125000001072 heteroaryl group Chemical group 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 238000009169 immunotherapy Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 210000003000 inclusion body Anatomy 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 150000002611 lead compounds Chemical class 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 230000004807 localization Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 230000004142 macroautophagy Effects 0.000 description 1
- 239000013642 negative control Substances 0.000 description 1
- 230000002981 neuropathic effect Effects 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 238000005192 partition Methods 0.000 description 1
- 230000007310 pathophysiology Effects 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 230000008782 phagocytosis Effects 0.000 description 1
- 230000009038 pharmacological inhibition Effects 0.000 description 1
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 description 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 208000007056 sickle cell anemia Diseases 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- QDLHCMPXEPAAMD-QAIWCSMKSA-N wortmannin Chemical compound C1([C@]2(C)C3=C(C4=O)OC=C3C(=O)O[C@@H]2COC)=C4[C@@H]2CCC(=O)[C@@]2(C)C[C@H]1OC(C)=O QDLHCMPXEPAAMD-QAIWCSMKSA-N 0.000 description 1
- QDLHCMPXEPAAMD-UHFFFAOYSA-N wortmannin Natural products COCC1OC(=O)C2=COC(C3=O)=C2C1(C)C1=C3C2CCC(=O)C2(C)CC1OC(C)=O QDLHCMPXEPAAMD-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic 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
- C07D513/02—Heterocyclic 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
- C07D513/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/93—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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 two hetero rings
- C07D405/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/02—Heterocyclic 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
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/02—Heterocyclic 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
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic 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
- C07D495/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562237342P | 2015-10-05 | 2015-10-05 | |
| US62/237,342 | 2015-10-05 | ||
| PCT/US2016/055561 WO2017062500A2 (en) | 2015-10-05 | 2016-10-05 | Activators of autophagic flux and phospholipase d and clearance of protein aggregates including tau and treatment of proteinopathies |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020102147A Division JP2020147597A (ja) | 2015-10-05 | 2020-06-12 | オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018530608A JP2018530608A (ja) | 2018-10-18 |
| JP2018530608A5 JP2018530608A5 (OSRAM) | 2019-11-14 |
| JP6740354B2 true JP6740354B2 (ja) | 2020-08-12 |
Family
ID=58488491
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018536715A Expired - Fee Related JP6740354B2 (ja) | 2015-10-05 | 2016-10-05 | オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 |
| JP2019518267A Pending JP2019529514A (ja) | 2015-10-05 | 2017-10-03 | オートファジーフラックス及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 |
| JP2020102147A Withdrawn JP2020147597A (ja) | 2015-10-05 | 2020-06-12 | オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019518267A Pending JP2019529514A (ja) | 2015-10-05 | 2017-10-03 | オートファジーフラックス及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 |
| JP2020102147A Withdrawn JP2020147597A (ja) | 2015-10-05 | 2020-06-12 | オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (6) | US20190112317A1 (OSRAM) |
| EP (2) | EP3359526A4 (OSRAM) |
| JP (3) | JP6740354B2 (OSRAM) |
| KR (2) | KR20180086187A (OSRAM) |
| CN (2) | CN108473435A (OSRAM) |
| AU (2) | AU2016333987A1 (OSRAM) |
| BR (2) | BR112018006873A2 (OSRAM) |
| CA (2) | CA3000988A1 (OSRAM) |
| IL (2) | IL258498A (OSRAM) |
| MX (2) | MX2018004109A (OSRAM) |
| WO (2) | WO2017062500A2 (OSRAM) |
| ZA (2) | ZA201802294B (OSRAM) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3359526A4 (en) * | 2015-10-05 | 2019-04-03 | The Trustees of Columbia University in the City of New York | ACTIVATORS OF AUTOPHAGIC RIVER AND PHOSPHOLIPASE D AND PURIFICATION OF PROTEIN AGGREGATES INCLUDING TAU AND TREATMENT OF PROTEINOPATHIES |
| EP3887357A1 (en) | 2018-11-28 | 2021-10-06 | Basf Se | Pesticidal compounds |
| AU2019387489A1 (en) * | 2018-11-30 | 2021-06-03 | Celularity Inc. | Aromatic compounds for use in activating hematopoietic stem and progenitor cells |
| EP4215199A4 (en) | 2020-09-17 | 2024-10-09 | Resonac Corporation | AUTOPHAGY ACTIVATOR |
| WO2022059767A1 (ja) | 2020-09-17 | 2022-03-24 | 昭和電工株式会社 | オートファジー活性化剤 |
| EP4215200A4 (en) | 2020-09-17 | 2024-10-09 | Resonac Corporation | Autophagy activator |
| CN116437912A (zh) * | 2020-09-17 | 2023-07-14 | 株式会社力森诺科 | 自噬激活剂 |
| CN112209888B (zh) * | 2020-10-14 | 2024-02-02 | 河南中医药大学 | 一种4-芳巯基喹唑啉类化合物、制备方法和医药用途 |
| WO2023081857A1 (en) * | 2021-11-04 | 2023-05-11 | Skyhawk Therapeutics, Inc. | Condensed pyridazine amine derivatives treating sca3 |
Family Cites Families (157)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3272824A (en) | 1962-12-06 | 1966-09-13 | Norwich Pharma Co | 4-amino-6, 7-di(lower) alkoxyquinolines |
| US3266990A (en) | 1963-09-24 | 1966-08-16 | Warner Lambert Pharmaceutical | Derivatives of quinazoline |
| US3936461A (en) | 1973-09-24 | 1976-02-03 | Warner-Lambert Company | Substituted 4-benzylquinolines |
| US4114939A (en) | 1976-09-13 | 1978-09-19 | Conco Inc. | Vacuum pickup head |
| IL89027A (en) | 1988-01-29 | 1993-01-31 | Lilly Co Eli | Quinazoline derivatives, process for their preparation and fungicidal, insecticidal and miticidal compositions containing them |
| GT198900008A (es) | 1988-01-29 | 1990-07-17 | Derivados de quinolina, quinazolina y cinolina. | |
| IL89029A (en) | 1988-01-29 | 1993-01-31 | Lilly Co Eli | Fungicidal quinoline and cinnoline derivatives, compositions containing them, and fungicidal methods of using them |
| WO1990005523A2 (en) | 1988-11-15 | 1990-05-31 | The Upjohn Company | Phenanthrolinedicarboxylate esters, 4-aminoquinoline and isoquinoline derivatives as inhibitors of hiv reverse transcriptase |
| US5034393A (en) * | 1989-07-27 | 1991-07-23 | Dowelanco | Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives |
| WO1992017452A1 (en) | 1991-04-03 | 1992-10-15 | Korea Research Institute Of Chemical Technology | 2-quinolinone derivatives |
| US5721237A (en) | 1991-05-10 | 1998-02-24 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties |
| JPH05213884A (ja) | 1991-06-14 | 1993-08-24 | Upjohn Co:The | 新規な4−アミノキノリン類およびこれを有効成分とする高血圧・鬱血性心不全の予防・治療剤 |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| PT100905A (pt) | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem |
| GB9300059D0 (en) | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
| DE4208254A1 (de) | 1992-03-14 | 1993-09-16 | Hoechst Ag | Substituierte pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel und fungizid |
| US5326766A (en) * | 1992-08-19 | 1994-07-05 | Dreikorn Barry A | 4-(2-(4-(2-pyridinyloxy)phenyl)ethoxy)quinazoline and analogues thereof |
| AU4790893A (en) | 1992-08-19 | 1994-03-15 | Dowelanco | Pyridylethoxy-, pyridylethylamino-, and pyridylpropyl-derivatives of quinoline and quinazoline as insecticides and fungicides |
| GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
| GB9314884D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Tricyclic derivatives |
| IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| GB9510757D0 (en) | 1994-09-19 | 1995-07-19 | Wellcome Found | Therapeuticaly active compounds |
| US5650415A (en) | 1995-06-07 | 1997-07-22 | Sugen, Inc. | Quinoline compounds |
| EP0832073B1 (en) | 1995-06-07 | 2002-01-16 | Sugen, Inc. | Quinazolines and pharmaceutical compositions |
| GB9514265D0 (en) | 1995-07-13 | 1995-09-13 | Wellcome Found | Hetrocyclic compounds |
| EP0860433B1 (en) | 1995-11-07 | 2002-07-03 | Kirin Beer Kabushiki Kaisha | Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of growth factor receptor originating in platelet and pharmaceutical compositions containing the same |
| WO1997030035A1 (en) | 1996-02-13 | 1997-08-21 | Zeneca Limited | Quinazoline derivatives as vegf inhibitors |
| EP0912559B1 (en) | 1996-07-13 | 2002-11-06 | Glaxo Group Limited | Fused heterocyclic compounds as protein tyrosine kinase inhibitors |
| US6809097B1 (en) | 1996-09-25 | 2004-10-26 | Zeneca Limited | Quinoline derivatives inhibiting the effect of growth factors such as VEGF |
| UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| US6251912B1 (en) | 1997-08-01 | 2001-06-26 | American Cyanamid Company | Substituted quinazoline derivatives |
| WO1999031072A1 (en) | 1997-12-18 | 1999-06-24 | E.I. Du Pont De Nemours And Company | Cyclohexylamine arthropodicides and fungicides |
| ES2219033T3 (es) * | 1998-07-22 | 2004-11-16 | Daiichi Suntory Pharma Co., Ltd. | Inhibidores de nf-kappa b que contienen derivados de indano como ingrediente activo. |
| US6297258B1 (en) | 1998-09-29 | 2001-10-02 | American Cyanamid Company | Substituted 3-cyanoquinolines |
| HK1039126B (en) | 1998-10-08 | 2005-09-30 | 阿斯特拉曾尼卡有限公司 | Quinazoline derivatives |
| ATE253051T1 (de) | 1999-01-22 | 2003-11-15 | Kirin Brewery | Chinolinderivate und chinazolinderivate |
| BRPI0017548B8 (pt) | 1999-02-10 | 2023-05-02 | Astrazeneca Ab | Composto |
| GB9904103D0 (en) | 1999-02-24 | 1999-04-14 | Zeneca Ltd | Quinoline derivatives |
| GB9910580D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
| GB9910579D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
| GB9910577D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
| HK1046688A1 (zh) | 1999-09-21 | 2003-01-24 | Astrazeneca Ab | 喹唑啉化合物和含有喹唑啉化合物的藥物組合物 |
| CZ20021009A3 (cs) | 1999-09-21 | 2002-06-12 | Astrazeneca Ab | Deriváty chinazolinu, způsob jejich přípravy a jejich pouľití jako léčiv |
| GB9930061D0 (en) | 1999-12-20 | 2000-02-09 | Glaxo Group Ltd | Quinolone compounds for use in treating viral infections |
| AU2223201A (en) | 1999-12-24 | 2001-07-09 | Kirin Beer Kabushiki Kaisha | Quinoline and quinazoline derivatives and drugs containing the same |
| US6906063B2 (en) | 2000-02-04 | 2005-06-14 | Portola Pharmaceuticals, Inc. | Platelet ADP receptor inhibitors |
| CN1240688C (zh) | 2000-04-07 | 2006-02-08 | 阿斯特拉曾尼卡有限公司 | 喹唑啉化合物 |
| IL153246A0 (en) | 2000-06-28 | 2003-07-06 | Astrazeneca Ab | Substituted quinazoline derivatives and their use as inhibitors |
| DE10042064A1 (de) | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Chinazoline, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US6576644B2 (en) | 2000-09-06 | 2003-06-10 | Bristol-Myers Squibb Co. | Quinoline inhibitors of cGMP phosphodiesterase |
| AU2002210714A1 (en) | 2000-11-02 | 2002-06-11 | Astrazeneca Ab | Substituted quinolines as antitumor agents |
| ES2312557T3 (es) | 2001-04-19 | 2009-03-01 | Astrazeneca Ab | Derivados de quinazolina. |
| PL209822B1 (pl) | 2001-04-27 | 2011-10-31 | Kirin Pharma Kk | Pochodna chinoliny lub chinazoliny, zawierająca ją kompozycja farmaceutyczna i zastosowanie |
| PE20030008A1 (es) | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | Inhibidores duales de pde 7 y pde 4 |
| KR100883731B1 (ko) | 2001-06-22 | 2009-02-12 | 기린 파마 가부시끼가이샤 | 간세포 증식 인자 수용체 자기 인산화를 저해하는 퀴놀린유도체 및 퀴나졸린 유도체 및 이들을 함유하는 의약 조성물 |
| JP4326328B2 (ja) | 2001-07-16 | 2009-09-02 | アストラゼネカ アクチボラグ | キノリン誘導体及びそれらのチロシンキナーゼ阻害薬としての使用 |
| EP1447405A4 (en) | 2001-10-17 | 2005-01-12 | Kirin Brewery | CHINOLIN OR CHINAZOLINE DERIVATIVES THAT PREVENT THE AUTOPHOSPHORYLATION OF RECEPTORS FOR THE FIBROBLAST GROWTH FACTOR |
| EP1451156A4 (en) | 2001-11-27 | 2005-05-25 | Merck & Co Inc | 4-AMINOCHINOLINVERBINDUNGEN |
| WO2003047585A1 (en) | 2001-12-05 | 2003-06-12 | Astrazeneca Ab | Pharmaceutical compositions comprising benzofuranyl substituted 3-cyanoquinoline derivatives and their use for the treatment of solid tumours |
| AU2002365665A1 (en) | 2001-12-05 | 2003-06-17 | Astrazeneca Ab | Pharmaceutical compositions comprising benzofuranyl substituted 3-cyanoquinoline derivatives and their use for the treatment of solid tumours |
| AU2002347359A1 (en) | 2001-12-05 | 2003-06-17 | Astrazeneca Ab | Quinoline derivatives |
| WO2003047582A1 (en) | 2001-12-05 | 2003-06-12 | Astrazeneca Ab | Quinoline derivatives as antitumour agents |
| GB0129099D0 (en) | 2001-12-05 | 2002-01-23 | Astrazeneca Ab | Chemical compounds |
| WO2003048159A1 (en) | 2001-12-05 | 2003-06-12 | Astrazeneca Ab | Quinoline derivatives |
| AU2002361846A1 (en) | 2001-12-21 | 2003-07-15 | Bayer Pharmaceuticals Corporation | Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents |
| CN1625555A (zh) | 2002-02-01 | 2005-06-08 | 阿斯特拉曾尼卡有限公司 | 喹唑啉化合物 |
| US7598258B2 (en) | 2002-05-01 | 2009-10-06 | Kirin Beer Kabushiki Kaisha | Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor |
| DE10221018A1 (de) | 2002-05-11 | 2003-11-27 | Boehringer Ingelheim Pharma | Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie |
| MY140680A (en) | 2002-05-20 | 2010-01-15 | Bristol Myers Squibb Co | Hepatitis c virus inhibitors |
| GB0215823D0 (en) | 2002-07-09 | 2002-08-14 | Astrazeneca Ab | Quinazoline derivatives |
| DE60327323D1 (de) | 2002-07-09 | 2009-06-04 | Astrazeneca Ab | Chinazoline derivative und ihre anwendung in der krebsbehandlung |
| US7576074B2 (en) | 2002-07-15 | 2009-08-18 | Rice Kenneth D | Receptor-type kinase modulators and methods of use |
| AU2003257666A1 (en) | 2002-08-23 | 2004-03-11 | Kirin Beer Kabushiki Kaisha | COMPOUND HAVING TGFss INHIBITORY ACTIVITY AND MEDICINAL COMPOSITION CONTAINING THE SAME |
| AU2003280599A1 (en) | 2002-10-29 | 2004-05-25 | Kirin Beer Kabushiki Kaisha | QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF Flt3 AND MEDICINAL COMPOSITIONS CONTAINING THE SAME |
| GB0225579D0 (en) | 2002-11-02 | 2002-12-11 | Astrazeneca Ab | Chemical compounds |
| US7462623B2 (en) | 2002-11-04 | 2008-12-09 | Astrazeneca Ab | Quinazoline derivatives as Src tyrosine kinase inhibitors |
| JO2785B1 (en) | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| ATE440825T1 (de) * | 2003-06-06 | 2009-09-15 | Vertex Pharma | Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern |
| CN1838950A (zh) * | 2003-06-23 | 2006-09-27 | 神经化学(国际)有限公司 | 治疗蛋白质聚集疾病的方法 |
| US20050026805A1 (en) | 2003-07-14 | 2005-02-03 | Ici Americas, Inc. | Solvated nonionic surfactants and fatty acids |
| GB0318422D0 (en) | 2003-08-06 | 2003-09-10 | Astrazeneca Ab | Chemical compounds |
| GB0322722D0 (en) | 2003-09-27 | 2003-10-29 | Glaxo Group Ltd | Compounds |
| CA2549869C (en) | 2003-12-18 | 2015-05-05 | Janssen Pharmaceutica N.V. | Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents |
| CA2549728C (en) | 2003-12-18 | 2015-07-21 | Janssen Pharmaceutica N.V. | 3-cyano-quinoline derivatives with antiproliferative activity |
| AP2006003619A0 (en) | 2003-12-23 | 2006-06-30 | Pfizer | Novel quinoline derivatives |
| CN1930128A (zh) | 2004-01-16 | 2007-03-14 | 惠氏公司 | 受体酪氨酸激酶抑制剂的喹啉中间体及其合成 |
| CN101163684B (zh) | 2005-02-23 | 2012-08-29 | 盐野义制药株式会社 | 具有酪氨酸激酶抑制作用的喹唑啉衍生物 |
| JP4966958B2 (ja) * | 2005-03-14 | 2012-07-04 | ノイロサーチ アクティーゼルスカブ | カリウムチャネル調節剤及び医療における使用 |
| CN101115736A (zh) * | 2005-03-14 | 2008-01-30 | 神经研究公司 | 钾通道调节剂和它们的医药用途 |
| CA2603748A1 (en) | 2005-04-06 | 2006-10-12 | Exelixis, Inc. | C-met modulators and methods of use |
| GB0509227D0 (en) | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Intracellular enzyme inhibitors |
| US20090221624A1 (en) | 2005-05-06 | 2009-09-03 | Olivo Paul D | 4-aminoquinoline compounds for treating virus-related conditions |
| WO2007052849A1 (ja) | 2005-11-07 | 2007-05-10 | Eisai R & D Management Co., Ltd. | 血管新生阻害物質とc-kitキナーゼ阻害物質との併用 |
| WO2007055513A1 (en) | 2005-11-08 | 2007-05-18 | Hanmi Pharm. Co., Ltd. | Quinazoline derivatives as a signal transduction inhibitor and method for the preparation thereof |
| JP5688877B2 (ja) | 2005-11-11 | 2015-03-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌疾患の治療用キナゾリン誘導体 |
| EP1979349B1 (en) | 2005-12-21 | 2010-07-28 | Abbott Laboratories | Anti-viral compounds |
| DK1981863T3 (da) | 2006-01-26 | 2013-01-02 | Boehringer Ingelheim Int | Fremgangsmåde til fremstilling af aminocrotonylaminosubtituerede quinazolinderivater |
| US7601716B2 (en) | 2006-05-01 | 2009-10-13 | Cephalon, Inc. | Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors |
| MX2009000148A (es) | 2006-07-07 | 2009-10-26 | Kalypsys Inc | Inhibidores heteroaril biciclicos de fosfodiesterasa 4. |
| WO2008009077A2 (en) | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections |
| CA2677001A1 (en) | 2006-08-23 | 2008-02-28 | Xtl Biopharmaceuticals Ltd. | 4-thio substituted quinoline and naphthyridine compounds |
| CN101558070A (zh) * | 2006-10-23 | 2009-10-14 | Sgx药品公司 | 三唑并哒嗪蛋白激酶调节剂 |
| AU2008219166B2 (en) | 2007-02-16 | 2013-05-16 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors |
| US8148532B2 (en) | 2007-03-14 | 2012-04-03 | Guoqing Paul Chen | Spiro substituted compounds as angiogenesis inhibitors |
| US8163923B2 (en) | 2007-03-14 | 2012-04-24 | Advenchen Laboratories, Llc | Spiro substituted compounds as angiogenesis inhibitors |
| DE102007032739A1 (de) | 2007-07-13 | 2009-01-15 | Merck Patent Gmbh | Chinazolinamidderivate |
| CN101784533B (zh) | 2007-08-22 | 2013-08-21 | 艾博特股份有限两合公司 | 4-苄基氨基喹啉、含有它们的药物组合物和它们在治疗中的用途 |
| US8143276B2 (en) | 2007-08-22 | 2012-03-27 | Xtl Biopharmaceuticals Ltd. | 4-thio substituted quinoline and naphthyridine compounds |
| PL2229369T3 (pl) | 2008-01-18 | 2017-01-31 | Natco Pharma Limited | Pochodne 6,7-dialkoksychinazoliny użyteczne do leczenia zaburzeń związanych z rakiem |
| US20110045100A1 (en) | 2008-03-05 | 2011-02-24 | Georgetown University | Antimalarial Quinolines and Methods of Use Thereof |
| KR101713501B1 (ko) | 2008-03-17 | 2017-03-07 | 암비트 바이오사이언시즈 코포레이션 | Raf 키나아제 조절제로서의 퀴나졸린 유도체 및 그의 사용방법 |
| US7829574B2 (en) | 2008-05-09 | 2010-11-09 | Hutchison Medipharma Enterprises Limited | Substituted quinazoline compounds and their use in treating angiogenesis-related diseases |
| CA2727103A1 (en) | 2008-07-03 | 2010-01-07 | Merck Patent Gmbh | Naphthyridinones as aurora kinase inhibitors |
| AP2848A (en) | 2008-08-14 | 2014-02-28 | Univ Cape Town | Quinoline compounds containing a dibemethin group |
| WO2010025451A2 (en) | 2008-08-29 | 2010-03-04 | Dow Agrosciences Llc | 5,8-difluoro-4-(2-(4-(heteroaryloxy)-phenyl)ethylamino)quinazolines and their use as agrochemicals |
| IT1393351B1 (it) | 2009-03-16 | 2012-04-20 | Eos Ethical Oncology Science Spa In Forma Abbreviata Eos Spa | Procedimento per la preparazione della 6-(7-((1-amminociclopropil)metossi)-6-metossichinolin-4-ilossi)-n-metil-1-naftammide e suoi intermedi di sintesi |
| WO2010107965A1 (en) | 2009-03-19 | 2010-09-23 | Boehringer Ingelheim International Gmbh | Process for preparing sulfonyl quinolines |
| RU2011142597A (ru) | 2009-03-21 | 2013-04-27 | Саншайн Лейк Фарма Ко., Лтд. | Производные сложных эфиров аминокислот, их соли и способы применения |
| ES2353093B1 (es) * | 2009-05-20 | 2012-01-03 | Consejo Superior De Investigaciones Científicas (Csic) | Uso de derivados de quinazolinas y sus composiciones farmacéuticas en enfermedades neurodegenerativas. |
| WO2010151791A1 (en) | 2009-06-25 | 2010-12-29 | Amgen Inc. | Heterocyclic compounds and their uses |
| PH12012500097A1 (en) * | 2009-07-21 | 2011-01-27 | Shanghai Inst Organic Chem | Potent small molecule inhibitors of autophagy, and methods of use thereof |
| WO2011014039A1 (en) * | 2009-07-31 | 2011-02-03 | Rohm And Haas Electronic Materials Korea Ltd. | Novel organic electroluminescent compounds and organic electroluminescent device using the same |
| CN102844304B (zh) | 2010-01-04 | 2014-12-31 | 日本曹达株式会社 | 含氮杂环化合物以及农园艺用杀菌剂 |
| US8575203B2 (en) | 2010-04-21 | 2013-11-05 | Boehringer Ingelheim International Gmbh | Chemical compounds |
| WO2011143444A2 (en) | 2010-05-14 | 2011-11-17 | President And Fellows Of Harvard College | Diphenylbutypiperidine autophagy inducers |
| MX2012015143A (es) | 2010-06-30 | 2013-07-03 | Amgen Inc | Compuestos heterociclicos que contienen nitrogeno como inhibidores de pi3k delta. |
| WO2012012320A1 (en) * | 2010-07-19 | 2012-01-26 | Millenium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| UY33549A (es) | 2010-08-10 | 2012-01-31 | Glaxo Group Ltd | Quinolil aminas como agentes inhibidores de las quinasas |
| WO2012044993A1 (en) * | 2010-09-30 | 2012-04-05 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Compounds, pharmaceutical compositions, and methods of treating or preventing neurodegenerative diseases or disorders |
| WO2012080729A2 (en) * | 2010-12-14 | 2012-06-21 | Electrophoretics Limited | CASEIN KINASE 1δ (CK1δ) INHIBITORS |
| WO2012090179A2 (en) * | 2010-12-30 | 2012-07-05 | Lupin Limited | Isoquinoline derivatives as cannabinoid receptor modulators |
| CN103857288B (zh) | 2011-03-04 | 2016-09-21 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为激酶抑制剂的氨基-喹啉 |
| US8664230B2 (en) | 2011-03-17 | 2014-03-04 | The Asan Foundation | Pyridopyrimidine derivatives and use thereof |
| ITMI20110480A1 (it) | 2011-03-25 | 2012-09-26 | F I S Fabbrica Italiana Sint P A | Procedimento per la preparazione di lapatinib e suoi sali |
| AU2012284088B2 (en) * | 2011-07-19 | 2015-10-08 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
| UY34451A (es) | 2011-11-14 | 2013-05-31 | Cephalon Inc | Derivados de uracilo como inhibidores de la quinasa axl y c-met |
| CN102643268B (zh) | 2011-12-30 | 2014-05-21 | 沈阳药科大学 | 喹啉类及噌啉类化合物及其应用 |
| EP2828250B1 (en) | 2012-03-19 | 2021-03-10 | Imperial College Innovations Limited | Quinazoline compounds and their use in therapy |
| US9193718B2 (en) | 2012-03-26 | 2015-11-24 | Fujian Institute Of Research On The Structure Of Matter, Chinese Academy Of Sciences | Quinazoline derivative and application thereof |
| AR092530A1 (es) | 2012-09-13 | 2015-04-22 | Glaxosmithkline Llc | Compuesto de amino-quinolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento |
| US9024023B2 (en) | 2013-01-14 | 2015-05-05 | F.I.S.—Fabbrica Italiana Sintetici S.p.A. | Efficient process for the preparation of lapatinib and salts thereof by means of new intermediates |
| AU2014216178B2 (en) | 2013-02-15 | 2018-06-28 | KALA BIO, Inc. | Therapeutic compounds and uses thereof |
| CA2905417A1 (en) | 2013-03-15 | 2014-09-18 | Rexahn Pharmaceuticals, Inc. | Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl) methanone compounds as cancer cell growth inhibitors |
| CN103232401B (zh) * | 2013-04-12 | 2015-11-04 | 浙江工业大学 | 一种4-芳硫基喹唑啉类化合物的合成方法 |
| EP2994140A4 (en) | 2013-05-07 | 2017-05-03 | Inhibikase Therapeutics, Inc. | Methods for treating hcv infection |
| PL2998296T3 (pl) | 2013-05-13 | 2018-12-31 | Shanghai Hengrui Pharmaceutical Co. Ltd. | Pochodna kwasu cykloalkilowego, sposób jej otrzymywania i jej zastosowanie farmaceutyczne |
| CN105916506B (zh) | 2013-11-20 | 2020-01-07 | 圣诺康生命科学公司 | 作为tam家族激酶抑制剂的喹唑啉衍生物 |
| GB201321146D0 (en) | 2013-11-29 | 2014-01-15 | Cancer Rec Tech Ltd | Quinazoline compounds |
| GB201321126D0 (en) | 2013-11-29 | 2014-01-15 | Velgene Biotechnology | Autophagy stimulants |
| CA2935944A1 (en) * | 2014-01-09 | 2015-07-16 | The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone | Substituted benzoxazine and related compounds |
| NZ724691A (en) | 2014-03-24 | 2018-02-23 | Guangdong Zhongsheng Pharmaceutical Co Ltd | Quinoline derivatives as smo inhibitors |
| FR3019819B1 (fr) | 2014-04-09 | 2018-03-23 | Centre National De La Recherche Scientifique (Cnrs) | Composes cytotoxiques inhibiteurs de la polymerisation de la tubuline |
| WO2015164374A1 (en) | 2014-04-22 | 2015-10-29 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN104193728A (zh) * | 2014-08-26 | 2014-12-10 | 北京大学深圳研究生院 | 流感病毒抑制剂及其应用 |
| EP3359526A4 (en) * | 2015-10-05 | 2019-04-03 | The Trustees of Columbia University in the City of New York | ACTIVATORS OF AUTOPHAGIC RIVER AND PHOSPHOLIPASE D AND PURIFICATION OF PROTEIN AGGREGATES INCLUDING TAU AND TREATMENT OF PROTEINOPATHIES |
| US9853396B1 (en) | 2016-12-05 | 2017-12-26 | Delphi Technologies, Inc. | Electrical plug having a flexible terminal retention feature |
-
2016
- 2016-10-05 EP EP16854245.4A patent/EP3359526A4/en not_active Withdrawn
- 2016-10-05 US US15/765,801 patent/US20190112317A1/en not_active Abandoned
- 2016-10-05 CA CA3000988A patent/CA3000988A1/en not_active Abandoned
- 2016-10-05 BR BR112018006873-0A patent/BR112018006873A2/pt not_active IP Right Cessation
- 2016-10-05 MX MX2018004109A patent/MX2018004109A/es unknown
- 2016-10-05 JP JP2018536715A patent/JP6740354B2/ja not_active Expired - Fee Related
- 2016-10-05 KR KR1020187012344A patent/KR20180086187A/ko not_active Abandoned
- 2016-10-05 WO PCT/US2016/055561 patent/WO2017062500A2/en not_active Ceased
- 2016-10-05 AU AU2016333987A patent/AU2016333987A1/en not_active Abandoned
- 2016-10-05 CN CN201680062131.XA patent/CN108473435A/zh active Pending
-
2017
- 2017-04-05 US US15/480,220 patent/US10487091B2/en active Active
- 2017-10-03 MX MX2019003805A patent/MX2019003805A/es unknown
- 2017-10-03 JP JP2019518267A patent/JP2019529514A/ja active Pending
- 2017-10-03 AU AU2017338769A patent/AU2017338769A1/en not_active Abandoned
- 2017-10-03 KR KR1020197012934A patent/KR20190058620A/ko not_active Abandoned
- 2017-10-03 CA CA3037260A patent/CA3037260A1/en not_active Abandoned
- 2017-10-03 BR BR112019006887A patent/BR112019006887A2/pt not_active Application Discontinuation
- 2017-10-03 CN CN201780064731.4A patent/CN110023289A/zh active Pending
- 2017-10-03 WO PCT/US2017/054969 patent/WO2018067589A1/en not_active Ceased
- 2017-10-03 EP EP17859036.0A patent/EP3523281A4/en not_active Withdrawn
-
2018
- 2018-04-04 IL IL258498A patent/IL258498A/en unknown
- 2018-04-09 ZA ZA2018/02294A patent/ZA201802294B/en unknown
- 2018-07-05 US US16/027,990 patent/US10865214B2/en not_active Expired - Fee Related
- 2018-07-05 US US16/027,951 patent/US11230558B2/en active Active
- 2018-07-05 US US16/027,930 patent/US11008341B2/en not_active Expired - Fee Related
-
2019
- 2019-03-19 ZA ZA2019/01694A patent/ZA201901694B/en unknown
- 2019-04-01 IL IL265750A patent/IL265750B/en unknown
-
2020
- 2020-03-13 US US16/818,388 patent/US11261199B2/en active Active
- 2020-06-12 JP JP2020102147A patent/JP2020147597A/ja not_active Withdrawn
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6740354B2 (ja) | オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 | |
| Hung et al. | Drug candidates in clinical trials for Alzheimer’s disease | |
| US11091444B2 (en) | Hydantoins that modulate BACE-mediated app processing | |
| US20140364451A1 (en) | Tropinol esters and related compounds to promote normal processing of app | |
| Tran et al. | Long-term everolimus treatment in individuals with tuberous sclerosis complex: a review of the current literature | |
| JP2018507886A5 (OSRAM) | ||
| JP2015510941A (ja) | App特異性のbace(asbi)およびその使用 | |
| JP2014515408A (ja) | 行動及び精神障害の治療のためのシロ−イノシトール | |
| US10844071B2 (en) | Substituted [1,2,3]triazolo[4,5-d]pyrimidines that lower stress-induced p-tau | |
| US10287227B2 (en) | Myricanol derivatives and uses thereof for treatment of neurodegenerative diseases | |
| WO2010110440A1 (ja) | 新規認知機能障害治療剤 | |
| JP2009155223A (ja) | DAPKs阻害剤 | |
| JP2016210737A (ja) | 中枢神経細胞保護剤、及び中枢神経変性疾患の予防又は治療剤 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20191003 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20191003 |
|
| A871 | Explanation of circumstances concerning accelerated examination |
Free format text: JAPANESE INTERMEDIATE CODE: A871 Effective date: 20191003 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20191219 |
|
| A975 | Report on accelerated examination |
Free format text: JAPANESE INTERMEDIATE CODE: A971005 Effective date: 20191225 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20200106 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20200406 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200612 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20200623 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A821 Effective date: 20200612 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20200722 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6740354 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |