RU2014111055A - 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение - Google Patents
2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение Download PDFInfo
- Publication number
- RU2014111055A RU2014111055A RU2014111055/04A RU2014111055A RU2014111055A RU 2014111055 A RU2014111055 A RU 2014111055A RU 2014111055/04 A RU2014111055/04 A RU 2014111055/04A RU 2014111055 A RU2014111055 A RU 2014111055A RU 2014111055 A RU2014111055 A RU 2014111055A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- group
- heteroalkyl
- cycloalkyl
- compound
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title claims 10
- 239000000203 mixture Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 44
- 125000000217 alkyl group Chemical group 0.000 claims abstract 39
- 125000001188 haloalkyl group Chemical group 0.000 claims abstract 32
- 125000004404 heteroalkyl group Chemical group 0.000 claims abstract 30
- -1 alkyl-OH Chemical group 0.000 claims abstract 27
- 229910052736 halogen Inorganic materials 0.000 claims abstract 21
- 150000002367 halogens Chemical class 0.000 claims abstract 21
- 125000003118 aryl group Chemical group 0.000 claims abstract 18
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 15
- 150000003839 salts Chemical class 0.000 claims abstract 14
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 11
- 125000004438 haloalkoxy group Chemical group 0.000 claims abstract 11
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 4
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims abstract 4
- 125000003367 polycyclic group Chemical group 0.000 claims abstract 4
- 238000006467 substitution reaction Methods 0.000 claims abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 33
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 15
- 125000000304 alkynyl group Chemical group 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 125000002877 alkyl aryl group Chemical group 0.000 claims 13
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 13
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 208000024827 Alzheimer disease Diseases 0.000 claims 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 6
- 208000018737 Parkinson disease Diseases 0.000 claims 5
- 239000000556 agonist Substances 0.000 claims 5
- 125000002541 furyl group Chemical group 0.000 claims 5
- 125000002971 oxazolyl group Chemical group 0.000 claims 5
- 125000003373 pyrazinyl group Chemical group 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 229940044551 receptor antagonist Drugs 0.000 claims 5
- 239000002464 receptor antagonist Substances 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 201000010374 Down Syndrome Diseases 0.000 claims 4
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 4
- 230000001906 cholesterol absorption Effects 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000007170 pathology Effects 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims 4
- 208000000044 Amnesia Diseases 0.000 claims 3
- 208000026139 Memory disease Diseases 0.000 claims 3
- 239000005557 antagonist Substances 0.000 claims 3
- 239000003529 anticholesteremic agent Substances 0.000 claims 3
- 229940127226 anticholesterol agent Drugs 0.000 claims 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 230000006984 memory degeneration Effects 0.000 claims 3
- 208000023060 memory loss Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 2
- 101800001718 Amyloid-beta protein Proteins 0.000 claims 2
- 102000009132 CB1 Cannabinoid Receptor Human genes 0.000 claims 2
- 108010073366 CB1 Cannabinoid Receptor Proteins 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 claims 2
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 claims 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 2
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 claims 2
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 claims 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 2
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 229940125753 fibrate Drugs 0.000 claims 2
- ASUTZQLVASHGKV-JDFRZJQESA-N galanthamine Chemical compound O1C(=C23)C(OC)=CC=C2CN(C)CC[C@]23[C@@H]1C[C@@H](O)C=C2 ASUTZQLVASHGKV-JDFRZJQESA-N 0.000 claims 2
- 238000001631 haemodialysis Methods 0.000 claims 2
- 230000000322 hemodialysis Effects 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 229960003512 nicotinic acid Drugs 0.000 claims 2
- 235000001968 nicotinic acid Nutrition 0.000 claims 2
- 239000011664 nicotinic acid Substances 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 2
- 239000000018 receptor agonist Substances 0.000 claims 2
- 229940044601 receptor agonist Drugs 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000004588 thienopyridyl group Chemical group S1C(=CC2=C1C=CC=N2)* 0.000 claims 2
- 230000009529 traumatic brain injury Effects 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- VHNYOQKVZQVBLC-RTCGXNAVSA-N (4r,7e,9as)-7-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]-4-(3,4,5-trifluorophenyl)-1,3,4,8,9,9a-hexahydropyrido[2,1-c][1,4]oxazin-6-one Chemical compound C1([C@@H]2COC[C@@H]3CC\C(C(N32)=O)=C/C=2C=C(C(=CC=2)N2C=C(C)N=C2)OC)=CC(F)=C(F)C(F)=C1 VHNYOQKVZQVBLC-RTCGXNAVSA-N 0.000 claims 1
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 claims 1
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims 1
- 108091005435 5-HT6 receptors Proteins 0.000 claims 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- 206010059245 Angiopathy Diseases 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims 1
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 108010001483 Glycogen Synthase Proteins 0.000 claims 1
- 102000018997 Growth Hormone Human genes 0.000 claims 1
- 108010051696 Growth Hormone Proteins 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 102000004384 Histamine H3 receptors Human genes 0.000 claims 1
- 108090000981 Histamine H3 receptors Proteins 0.000 claims 1
- 101000870945 Homo sapiens Ras guanyl-releasing protein 3 Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 102100023915 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 claims 1
- 102100036834 Metabotropic glutamate receptor 1 Human genes 0.000 claims 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 claims 1
- 102000010750 Metalloproteins Human genes 0.000 claims 1
- 108010063312 Metalloproteins Proteins 0.000 claims 1
- 102100040243 Microtubule-associated protein tau Human genes 0.000 claims 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- 108010022233 Plasminogen Activator Inhibitor 1 Proteins 0.000 claims 1
- 102100039418 Plasminogen activator inhibitor 1 Human genes 0.000 claims 1
- 206010036631 Presenile dementia Diseases 0.000 claims 1
- 229940122144 Prostaglandin receptor antagonist Drugs 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 102100033450 Ras guanyl-releasing protein 3 Human genes 0.000 claims 1
- 206010039966 Senile dementia Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 229940122777 Tau aggregation inhibitor Drugs 0.000 claims 1
- 229930003427 Vitamin E Natural products 0.000 claims 1
- 150000005215 alkyl ethers Chemical class 0.000 claims 1
- 230000006933 amyloid-beta aggregation Effects 0.000 claims 1
- 230000003941 amyloidogenesis Effects 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 208000005881 bovine spongiform encephalopathy Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229960003980 galantamine Drugs 0.000 claims 1
- ASUTZQLVASHGKV-UHFFFAOYSA-N galanthamine hydrochloride Natural products O1C(=C23)C(OC)=CC=C2CN(C)CCC23C1CC(O)C=C2 ASUTZQLVASHGKV-UHFFFAOYSA-N 0.000 claims 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims 1
- 239000003540 gamma secretase inhibitor Substances 0.000 claims 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims 1
- 239000000122 growth hormone Substances 0.000 claims 1
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims 1
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 1
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 1
- 239000003395 histamine H3 receptor antagonist Substances 0.000 claims 1
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 1
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 208000020658 intracerebral hemorrhage Diseases 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 229940127592 mGluR2/3 antagonist Drugs 0.000 claims 1
- 108010014719 metabotropic glutamate receptor type 1 Proteins 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000007388 microgliosis Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000003959 neuroinflammation Effects 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 239000000387 serotonin 5-HT4 receptor agonist Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 229960005486 vaccine Drugs 0.000 claims 1
- 229940046009 vitamin E Drugs 0.000 claims 1
- 235000019165 vitamin E Nutrition 0.000 claims 1
- 239000011709 vitamin E Substances 0.000 claims 1
- 229940124648 γ-Secretase Modulator Drugs 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/14—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
- C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
- C07D279/18—[b, e]-condensed with two six-membered rings
- C07D279/34—[b, e]-condensed with two six-membered rings with hetero atoms directly attached to the ring sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/04—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/10—Heterocyclic 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 linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D513/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Otolaryngology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161526049P | 2011-08-22 | 2011-08-22 | |
| US61/526,049 | 2011-08-22 | ||
| PCT/US2012/051687 WO2013028670A1 (en) | 2011-08-22 | 2012-08-21 | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2014111055A true RU2014111055A (ru) | 2015-09-27 |
Family
ID=47746812
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2014111055/04A RU2014111055A (ru) | 2011-08-22 | 2012-08-21 | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9181236B2 (OSRAM) |
| EP (1) | EP2747769B1 (OSRAM) |
| JP (1) | JP2014524472A (OSRAM) |
| KR (1) | KR20140054295A (OSRAM) |
| CN (1) | CN103874496A (OSRAM) |
| AU (1) | AU2012298983A1 (OSRAM) |
| BR (1) | BR112014004181A2 (OSRAM) |
| CA (1) | CA2844988A1 (OSRAM) |
| MX (1) | MX2014002113A (OSRAM) |
| RU (1) | RU2014111055A (OSRAM) |
| WO (1) | WO2013028670A1 (OSRAM) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| UA108363C2 (uk) * | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| KR20140054295A (ko) | 2011-08-22 | 2014-05-08 | 머크 샤프 앤드 돔 코포레이션 | Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도 |
| SG11201406759YA (en) | 2012-04-26 | 2014-11-27 | Bristol Myers Squibb Co | Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
| MX2014012741A (es) | 2012-04-26 | 2015-04-13 | Bristol Myers Squibb Co | Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activado de proteasa (par4) para tratamiento de agregacion plaquetaria. |
| BR112014026643B1 (pt) | 2012-04-26 | 2023-03-07 | Universite De Montreal | Derivados de imidazotiadiazol e imidazopirazina como inibidores de receptor 4 ativado por protease (par4) para o tratamento de agregação de plaqueta, seus usos e composição farmacêutica |
| EA026004B1 (ru) * | 2012-05-24 | 2017-02-28 | Ф. Хоффманн-Ля Рош Аг | 5-АМИНО[1,4]ТИАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ β-СЕКРЕТАЗЫ 1 |
| US9556135B2 (en) * | 2012-10-12 | 2017-01-31 | Amgen, Inc. | Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
| CN104870000A (zh) | 2012-12-20 | 2015-08-26 | 默沙东公司 | 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途 |
| MX366855B (es) | 2013-03-01 | 2019-07-26 | Amgen Inc | Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso. |
| JP6374889B2 (ja) | 2013-03-08 | 2018-08-15 | アムジエン・インコーポレーテツド | β−セクレターゼ阻害剤としての過フッ素化シクロプロピル縮合1,3−オキサジン−2−アミン化合物、及び使用方法 |
| WO2014150344A1 (en) * | 2013-03-15 | 2014-09-25 | Merck Sharp & Dohme Corp. | C2-azaspiro iminothiazine dioxides as bace inhibitors |
| WO2015017407A1 (en) * | 2013-07-30 | 2015-02-05 | Amgen Inc. | Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta- secretase |
| EP3043802B1 (en) | 2013-09-13 | 2018-04-18 | Merck Sharp & Dohme Corp. | C5-spiro iminothiazine dioxides as bace inhibitors, compositions, and their use |
| US9745324B2 (en) | 2013-12-18 | 2017-08-29 | Merck Sharp & Dohme Corp. | Iminothiadiazepane dioxide compounds as BACE inhibitors, compositions, and their use |
| EP3083575B1 (en) * | 2013-12-18 | 2021-11-03 | Merck Sharp & Dohme Corp. | C-6 spirocarbocyclic iminothiadiazine dioxides as bace inhibitors, compositions, and their use |
| KR102285306B1 (ko) * | 2013-12-20 | 2021-08-04 | 에프. 호프만-라 로슈 아게 | 5-아릴-1-이미노-1-옥소-[1,2,4]티아다이아진 |
| EP3148996B1 (en) | 2014-06-02 | 2021-05-05 | Merck Sharp & Dohme Corp. | C2-carbocyclic iminothiazine dioxides as bace inhibitors, compositions, and their use |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| US10047098B2 (en) | 2014-11-25 | 2018-08-14 | Merck Sharp & Dohme Corp. | C5-C6-oxacyclic fused iminopyrimidinone compounds as bace inhibitors, compositions, and their use |
| EP3271355B1 (en) * | 2015-03-20 | 2020-07-29 | H. Hoffnabb-La Roche Ag | Bace1 inhibitors |
| AU2016250519A1 (en) | 2015-04-21 | 2017-11-30 | Allgenesis Biotherapeutics, Inc. | Compounds and their use as BACE1 inhibitors |
| WO2017024180A1 (en) | 2015-08-06 | 2017-02-09 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| WO2017025491A1 (en) * | 2015-08-12 | 2017-02-16 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
| WO2017095759A1 (en) | 2015-12-04 | 2017-06-08 | Merck Sharp & Dohme Corp. | C5-c6-carbocyclic fused iminothiadiazine dioxides as bace inhibitors, compositions, and their use |
| MX387729B (es) | 2016-12-15 | 2025-03-18 | Amgen Inc | Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso. |
| US10889579B2 (en) | 2016-12-15 | 2021-01-12 | Amgen Inc. | Thiazine derivatives as β-secretase inhibitors and methods of use |
| ES2910367T3 (es) | 2016-12-15 | 2022-05-12 | Amgen Inc | Derivados de tiazina y oxazina bicíclicos como inhibidores de beta-secretasa y métodos de uso |
| AU2017378316B2 (en) | 2016-12-15 | 2021-04-01 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| AU2017376441B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| MX2020011382A (es) | 2018-04-27 | 2020-11-24 | Shionogi & Co | Derivados de tetrahidropiranoxazina que tienen actividad inhibidora de beta-secretasa 1 (bace1) selectiva. |
| CN109180671A (zh) * | 2018-09-21 | 2019-01-11 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
| CA3183551A1 (en) * | 2020-06-30 | 2022-01-06 | Theodore J. Price | Pyridine-1,5-diones exhibiting mnk inhibition and their method of use |
| CN113105318B (zh) * | 2021-02-23 | 2022-05-20 | 中山大学 | 一种2,2-二氟环丁烷-1-羧酸的制备方法及应用 |
Family Cites Families (131)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL92011A0 (en) | 1988-10-19 | 1990-07-12 | Abbott Lab | Heterocyclic peptide renin inhibitors |
| US5534520A (en) | 1990-04-10 | 1996-07-09 | Fisher; Abraham | Spiro compounds containing five-membered rings |
| AU2436792A (en) | 1991-08-16 | 1993-03-16 | Merck & Co., Inc. | Quinazoline derivatives as inhibitors of hiv reverse transcriptase |
| US5629322A (en) | 1994-11-15 | 1997-05-13 | Merck & Co., Inc. | Cyclic amidine analogs as inhibitors of nitric oxide synthase |
| US6191127B1 (en) | 1997-05-02 | 2001-02-20 | Schering Aktiengesellschaft | Substituted heterocycles and their use in medicaments |
| WO2000051992A1 (en) | 1999-03-04 | 2000-09-08 | E.I. Du Pont De Nemours And Company | Fused bicyclic oxazinone and thiazinone fungicides |
| US7161962B1 (en) | 1999-05-27 | 2007-01-09 | Nuera Communications, Inc. | Method and apparatus for coding modem signals for transmission over voice networks |
| ATE515495T1 (de) | 2001-08-03 | 2011-07-15 | Schering Corp | Gamma sekretase inhibitoren |
| US7244764B2 (en) | 2003-06-23 | 2007-07-17 | Neurochem (International) Limited | Methods and compositions for treating amyloid-related diseases |
| TW200519084A (en) | 2003-08-08 | 2005-06-16 | Schering Corp | Cyclic amine bace-1 inhibitors having a benzamide substituent |
| TW200524910A (en) | 2003-08-08 | 2005-08-01 | Schering Corp | Cyclic amine BACE-1 inhibitors having a heterocyclic substituent |
| GB0319463D0 (en) | 2003-08-20 | 2003-09-17 | Givaudan Sa | Compounds |
| US20060034848A1 (en) | 2003-11-07 | 2006-02-16 | Ayae Kinoshita | Methods and compositions for treating Alzheimer's disease |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP2153832B1 (en) * | 2003-12-15 | 2016-03-09 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors |
| DE602005017033D1 (de) | 2004-06-16 | 2009-11-19 | Wyeth Corp | Amino-5,5-diphenylimidazolon-derivate zur beta-sekretase-hemmung |
| MXPA06014792A (es) | 2004-06-16 | 2007-02-16 | Wyeth Corp | Difenilimidazopirimidina y aminas imidazol como inhibidores de ??-secretasa. |
| AR049726A1 (es) | 2004-07-22 | 2006-08-30 | Schering Corp | Amidas sustituidas inhibidoras de beta secretasa |
| US7652003B2 (en) | 2004-07-28 | 2010-01-26 | Schering-Plough Corporation | Macrocyclic β-secretase inhibitors |
| CN101068545A (zh) | 2004-10-13 | 2007-11-07 | 默克公司 | 作为β-分泌酶抑制剂用于治疗阿尔茨海默病的螺哌啶化合物 |
| US20090221579A1 (en) | 2004-10-15 | 2009-09-03 | Jeffrey Scott Albert | Substituted Amino-Compounds and Uses Thereof |
| WO2006041405A1 (en) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Substituted amino-pyrimidones and uses thereof |
| CN101052618A (zh) | 2004-10-29 | 2007-10-10 | 默克公司 | 用作治疗阿尔茨海默氏病的β-分泌酶抑制剂的2-氨基吡啶化合物 |
| CA2593515A1 (en) | 2005-01-14 | 2006-07-20 | Wyeth | Amino-imidazolones for the inhibition of beta-secretase |
| DE102005023943A1 (de) | 2005-05-20 | 2006-11-23 | Grünenthal GmbH | Pentafluorsulfanyl-substituierte Verbindung und deren Verwendung zur Herstellung von Arzneimitteln |
| AR054617A1 (es) | 2005-06-14 | 2007-07-04 | Schering Corp | Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden |
| MX2007016183A (es) | 2005-06-14 | 2008-03-10 | Schering Corp | Preparacion y uso de compuestos como inhibidores de proteasas. |
| CA2609562A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Macrocyclic heterocyclic aspartyl protease inhibitors |
| US7759353B2 (en) | 2005-06-14 | 2010-07-20 | Schering Corporation | Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment |
| JP2008543846A (ja) | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | プロテアーゼ阻害剤として化合物の調製およびその使用 |
| CN101198609A (zh) | 2005-06-14 | 2008-06-11 | 先灵公司 | 天冬氨酰基蛋白酶抑制剂 |
| EP2194047A1 (en) | 2005-06-14 | 2010-06-09 | Schering Corporation | Preparation and use of aspartyl protease inhibitors |
| TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| MX2008000212A (es) | 2005-06-30 | 2008-03-24 | Wyeth Corp | Compuestos amino-5-(6 miembros)heteroarilimidazolona y el uso de estos para la modulacion de la (-secretasa. |
| AU2006270084B2 (en) | 2005-07-18 | 2011-08-25 | Merck Sharp & Dohme Corp. | Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease |
| TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| KR20080050430A (ko) | 2005-09-26 | 2008-06-05 | 와이어쓰 | 베타-세크레타제 (bace) 억제제로서아미노-5-[4-(디플루오로메톡시)페닐]-5-페닐이미다졸론화합물 |
| CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| ES2349433T3 (es) | 2005-10-27 | 2011-01-03 | Schering Corporation | Inhibidores heterocíclicos de aspartil proteasa. |
| AR056211A1 (es) | 2005-10-31 | 2007-09-26 | Schering Corp | Derivados de [1,4,6]oxadiazepinas, composiciones farmaceuticas que los contienen en combinacion con otros agentes terapeuticos y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de aspartil-proteasas |
| EP1951680A4 (en) | 2005-11-15 | 2011-08-10 | Astrazeneca Ab | NOVEL 2-AMINOPYRIMIDINONE DERIVATIVES AND THEIR USE |
| WO2007058581A1 (en) | 2005-11-15 | 2007-05-24 | Astrazeneca Ab | Novel 2-aminopyrimidine derivatives and their use |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| WO2007059125A2 (en) * | 2005-11-15 | 2007-05-24 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| TW200734311A (en) | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
| US20090176850A1 (en) | 2005-11-21 | 2009-07-09 | Astrazeneca Ab | Novel 2-Amino-Imidazole-4-One Compounds And Their Use In The Manufacture Of A Medicament To Be Used In The Treatment Of Cognitive Impairment, Alzheimer's Disease, Neurodegeneration And Dementia |
| AR058381A1 (es) | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
| CN101360737A (zh) | 2005-12-19 | 2009-02-04 | 惠氏公司 | 2-氨基-5-哌啶咪唑酮化合物和其用于β分泌酶调节的用途 |
| WO2007100536A1 (en) | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
| US20090099217A1 (en) | 2006-04-05 | 2009-04-16 | Astex Therapeutics Ltd. | 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies |
| CA2653650A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| TW200815443A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
| TW200808796A (en) | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
| TW200815449A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| TW200817406A (en) | 2006-08-17 | 2008-04-16 | Wyeth Corp | Imidazole amines as inhibitors of β-secretase |
| WO2008063114A1 (en) | 2006-11-20 | 2008-05-29 | Astrazeneca Ab | Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia |
| MX2009006228A (es) | 2006-12-12 | 2009-06-22 | Schering Corp | Inhibidores de aspartil proteasa. |
| JP2010512390A (ja) | 2006-12-12 | 2010-04-22 | シェーリング コーポレイション | 三環式系を含むアスパルチルプロテアーゼ阻害剤 |
| WO2008076043A1 (en) | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Novel 2-amino-5,5-diaryl-imidazol-4-ones |
| TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| CL2008000784A1 (es) | 2007-03-20 | 2008-05-30 | Wyeth Corp | Compuestos amino-5-[-4-(diflourometoxi) fenil sustituido]-5-fenilmidazolona, inhibidores de b-secretasa; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar alzheimer, deterioro cognitivo, sindrome de down, disminucion co |
| AR065814A1 (es) | 2007-03-23 | 2009-07-01 | Wyeth Corp | Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. |
| RU2476430C2 (ru) | 2007-04-24 | 2013-02-27 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина, замещенные циклической группой |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| JP2010535762A (ja) | 2007-08-06 | 2010-11-25 | シェーリング コーポレイション | ガンマセクレターゼモジュレーター |
| US20090041201A1 (en) | 2007-08-06 | 2009-02-12 | Carestream Health, Inc. | Alignment apparatus for imaging system |
| BRPI0906962B8 (pt) | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| EP2257167B1 (en) | 2008-02-28 | 2015-07-22 | Merck Sharp & Dohme Corp. | 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease |
| AR072952A1 (es) | 2008-04-22 | 2010-10-06 | Schering Corp | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| KR20110000749A (ko) | 2008-05-05 | 2011-01-05 | 화이자 인코포레이티드 | 신경변성 질환의 치료용 스피로 피페리딘류 |
| ES2738123T3 (es) | 2008-06-13 | 2020-01-20 | Shionogi & Co | Derivado heterocíclico que contiene azufre que tiene actividad inhibitoria de ß-secretasa |
| WO2010013302A1 (ja) | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| CN102105475B (zh) | 2008-07-28 | 2014-04-09 | 卫材R&D管理有限公司 | 螺氨基二氢噻嗪衍生物 |
| WO2010021680A2 (en) | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| KR20110073511A (ko) | 2008-09-11 | 2011-06-29 | 암젠 인크 | 베타세크레타제 조절제로서의 스피로-테트라사이클릭 고리 화합물 및 사용 방법 |
| US20110207723A1 (en) | 2008-09-30 | 2011-08-25 | Eisai R&D Management Co., Ltd. | Novel fused aminodihydrothiazine derivative |
| WO2010047372A1 (ja) | 2008-10-22 | 2010-04-29 | 塩野義製薬株式会社 | Bace1阻害活性を有する2-アミノピリミジン-4-オンおよび2-アミノピリジン誘導体 |
| WO2010063718A1 (en) | 2008-12-02 | 2010-06-10 | ETH Zürich | Screening assay for metabolic disease therapeuticals |
| US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| US20110065695A1 (en) | 2009-09-11 | 2011-03-17 | Jeremy Beauchamp | Use of aminodihydrothiazines for the treatment or prevention of diabetes |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2500344A4 (en) | 2009-11-13 | 2013-05-01 | Shionogi & Co | AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION |
| WO2011072064A1 (en) | 2009-12-08 | 2011-06-16 | Array Biopharma Inc. | S piro [chroman - 4, 4 ' - imidazol] ones as beta - secretase inhibitors |
| WO2011071057A1 (ja) | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物 |
| JPWO2011070781A1 (ja) | 2009-12-09 | 2013-04-22 | 塩野義製薬株式会社 | 置換アミノチアジン誘導体 |
| US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
| UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
| WO2011071135A1 (ja) | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
| JPWO2011071109A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
| JPWO2011077726A1 (ja) | 2009-12-24 | 2013-05-02 | 塩野義製薬株式会社 | 4−アミノ−1,3−チアジンまたはオキサジン誘導体 |
| AU2010338365B2 (en) | 2009-12-31 | 2014-01-30 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| EP2539322B1 (en) | 2010-02-24 | 2014-01-01 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| CA2791281A1 (en) | 2010-03-15 | 2011-09-22 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators |
| JP5584352B2 (ja) | 2010-03-15 | 2014-09-03 | アムジエン・インコーポレーテツド | β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途 |
| WO2011123674A1 (en) | 2010-03-31 | 2011-10-06 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
| US20130108645A1 (en) | 2010-04-13 | 2013-05-02 | The Johns Hopkins University | Methods for enhancing axonal regeneration |
| WO2011130741A1 (en) | 2010-04-16 | 2011-10-20 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
| US8673894B2 (en) | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
| PH12012502377A1 (en) * | 2010-06-09 | 2014-10-14 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| CN102918036A (zh) | 2010-06-09 | 2013-02-06 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5-氨基-3,6-二氢-1H-吡嗪-2-酮衍生物 |
| CA2771928C (en) | 2010-07-13 | 2013-08-06 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| US8815881B2 (en) | 2010-08-09 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds |
| AR083169A1 (es) | 2010-09-24 | 2013-02-06 | Array Biopharma Inc | Compuestos para tratar enfermedades neurodegenerativas |
| US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| TW201307357A (zh) | 2010-11-22 | 2013-02-16 | Array Biopharma Inc | 治療神經退化性疾病之化合物 |
| US8957083B2 (en) | 2010-11-23 | 2015-02-17 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| US8399459B2 (en) | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| CN103596939A (zh) * | 2011-04-13 | 2014-02-19 | 默沙东公司 | 作为bace抑制剂的5-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其应用 |
| RU2013150349A (ru) | 2011-04-13 | 2015-05-20 | Мерк Шарп И Доум Корп. | 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение |
| US9079919B2 (en) | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
| JP2012250933A (ja) | 2011-06-03 | 2012-12-20 | Shionogi & Co Ltd | オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物 |
| KR20140054295A (ko) | 2011-08-22 | 2014-05-08 | 머크 샤프 앤드 돔 코포레이션 | Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도 |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| EA026004B1 (ru) * | 2012-05-24 | 2017-02-28 | Ф. Хоффманн-Ля Рош Аг | 5-АМИНО[1,4]ТИАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ β-СЕКРЕТАЗЫ 1 |
-
2012
- 2012-08-21 KR KR1020147007258A patent/KR20140054295A/ko not_active Withdrawn
- 2012-08-21 BR BR112014004181A patent/BR112014004181A2/pt unknown
- 2012-08-21 JP JP2014527238A patent/JP2014524472A/ja active Pending
- 2012-08-21 RU RU2014111055/04A patent/RU2014111055A/ru not_active Application Discontinuation
- 2012-08-21 WO PCT/US2012/051687 patent/WO2013028670A1/en not_active Ceased
- 2012-08-21 CN CN201280051313.9A patent/CN103874496A/zh active Pending
- 2012-08-21 MX MX2014002113A patent/MX2014002113A/es unknown
- 2012-08-21 AU AU2012298983A patent/AU2012298983A1/en not_active Abandoned
- 2012-08-21 EP EP12825781.3A patent/EP2747769B1/en active Active
- 2012-08-21 CA CA2844988A patent/CA2844988A1/en not_active Abandoned
- 2012-08-21 US US14/240,215 patent/US9181236B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP2747769A4 (en) | 2015-02-11 |
| KR20140054295A (ko) | 2014-05-08 |
| MX2014002113A (es) | 2014-04-25 |
| EP2747769A1 (en) | 2014-07-02 |
| CN103874496A (zh) | 2014-06-18 |
| BR112014004181A2 (pt) | 2017-06-13 |
| EP2747769B1 (en) | 2017-08-02 |
| JP2014524472A (ja) | 2014-09-22 |
| AU2012298983A1 (en) | 2014-02-27 |
| WO2013028670A1 (en) | 2013-02-28 |
| US20140200213A1 (en) | 2014-07-17 |
| US9181236B2 (en) | 2015-11-10 |
| CA2844988A1 (en) | 2013-02-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2014111055A (ru) | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение | |
| RU2013150349A (ru) | 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение | |
| JP2014524472A5 (OSRAM) | ||
| JP2014514302A5 (OSRAM) | ||
| JP6760249B2 (ja) | 三環性スピロ化合物 | |
| KR101640263B1 (ko) | 세라마이드 유도체로 다낭성 신장질환을 치료하는 방법 | |
| JP2018502891A5 (OSRAM) | ||
| RU2011147232A (ru) | Производное карбоновой кислоты | |
| JP2017531688A5 (OSRAM) | ||
| RU2014122335A (ru) | ХИНОЛИНКАРБОКСАМИДНЫЕ И ХИНОЛИНКАРБОНИТРИЛЬНЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ mGluR2-НЕГАТИВНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ, КОМПОЗИЦИИ И ИХ ПРИМЕНЕНИЕ | |
| JP2011523412A5 (OSRAM) | ||
| PE20081228A1 (es) | Compuesto heteromonociclico | |
| JP2009544618A5 (OSRAM) | ||
| RU2017116196A (ru) | 2-амино-6-(дифторметил)-5,5-дифтор-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы васе1 | |
| JP7647552B2 (ja) | Ep2アンタゴニスト | |
| JP2020500866A5 (OSRAM) | ||
| KR20100099172A (ko) | 관절염의 치료 방법 | |
| JP6569661B2 (ja) | 選択的ep2アゴニスト活性を有する化合物 | |
| RU2011123862A (ru) | Модуляторы гамма-секретазы | |
| RU2014109747A (ru) | Морфолино-замещенные производные мочевины или карбамата в качестве ингибиторов mtor | |
| RU2012150501A (ru) | Противораковые стероидные лактоны, ненасыщенные в положении 7(8) | |
| JPWO2021026009A5 (OSRAM) | ||
| JP2017538711A5 (OSRAM) | ||
| KR20210039417A (ko) | 치환된 테트라하이드로사이클로펜타[c]피롤, 치환된 디하이드로피롤리진, 이의 유사체, 및 이의 사용 방법 | |
| RU2016102080A (ru) | Ppar-поддерживающие соединения для лечения метаболических заболеваний |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20161128 |