CN102470137A - 用于治疗神经元蜡样脂褐质沉积症的1h-喹唑啉-2,4-二酮 - Google Patents
用于治疗神经元蜡样脂褐质沉积症的1h-喹唑啉-2,4-二酮 Download PDFInfo
- Publication number
- CN102470137A CN102470137A CN2010800334750A CN201080033475A CN102470137A CN 102470137 A CN102470137 A CN 102470137A CN 2010800334750 A CN2010800334750 A CN 2010800334750A CN 201080033475 A CN201080033475 A CN 201080033475A CN 102470137 A CN102470137 A CN 102470137A
- Authority
- CN
- China
- Prior art keywords
- quinazoline
- methanesulfomide
- dioxo
- dihydro
- trifluoromethyl
- 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.)
- Pending
Links
- 201000008051 neuronal ceroid lipofuscinosis Diseases 0.000 title claims abstract description 80
- 238000011282 treatment Methods 0.000 title claims abstract description 24
- 208000002537 Neuronal Ceroid-Lipofuscinoses Diseases 0.000 title abstract description 3
- SDQJTWBNWQABLE-UHFFFAOYSA-N 1h-quinazoline-2,4-dione Chemical class C1=CC=C2C(=O)NC(=O)NC2=C1 SDQJTWBNWQABLE-UHFFFAOYSA-N 0.000 title 1
- 230000002265 prevention Effects 0.000 claims abstract description 8
- 150000001875 compounds Chemical class 0.000 claims description 84
- 229940002612 prodrug Drugs 0.000 claims description 50
- 239000000651 prodrug Substances 0.000 claims description 50
- 150000003839 salts Chemical class 0.000 claims description 41
- 206010027336 Menstruation delayed Diseases 0.000 claims description 19
- 239000003814 drug Substances 0.000 claims description 19
- 238000000034 method Methods 0.000 claims description 19
- 206010015037 epilepsy Diseases 0.000 claims description 18
- 125000001424 substituent group Chemical group 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 238000002360 preparation method Methods 0.000 claims description 8
- 208000017478 adult neuronal ceroid lipofuscinosis Diseases 0.000 claims description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 208000036626 Mental retardation Diseases 0.000 claims description 5
- 229910052739 hydrogen Inorganic materials 0.000 claims description 5
- 239000001257 hydrogen Substances 0.000 claims description 5
- 208000017476 juvenile neuronal ceroid lipofuscinosis Diseases 0.000 claims description 5
- 230000001225 therapeutic effect Effects 0.000 claims description 5
- 208000025014 late infantile neuronal ceroid lipofuscinosis Diseases 0.000 claims description 4
- 230000002860 competitive effect Effects 0.000 abstract description 6
- 229940098747 AMPA receptor antagonist Drugs 0.000 abstract description 2
- 239000000775 AMPA receptor antagonist Substances 0.000 abstract description 2
- 238000012360 testing method Methods 0.000 description 23
- 230000000694 effects Effects 0.000 description 17
- 230000008859 change Effects 0.000 description 14
- 241000699670 Mus sp. Species 0.000 description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 12
- 238000002474 experimental method Methods 0.000 description 11
- 201000010099 disease Diseases 0.000 description 9
- 239000000203 mixture Substances 0.000 description 9
- 239000002904 solvent Substances 0.000 description 8
- 208000024891 symptom Diseases 0.000 description 8
- -1 Alcohol ester Chemical class 0.000 description 7
- 230000006870 function Effects 0.000 description 7
- 239000005557 antagonist Substances 0.000 description 6
- 238000013461 design Methods 0.000 description 6
- 238000001727 in vivo Methods 0.000 description 6
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 description 5
- 230000008499 blood brain barrier function Effects 0.000 description 5
- 210000001218 blood-brain barrier Anatomy 0.000 description 5
- 238000003745 diagnosis Methods 0.000 description 5
- 230000006872 improvement Effects 0.000 description 5
- 238000006722 reduction reaction Methods 0.000 description 5
- 238000011160 research Methods 0.000 description 5
- 102000003678 AMPA Receptors Human genes 0.000 description 4
- 108090000078 AMPA Receptors Proteins 0.000 description 4
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- 241001597008 Nomeidae Species 0.000 description 4
- 230000002950 deficient Effects 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 238000009510 drug design Methods 0.000 description 4
- 230000009467 reduction Effects 0.000 description 4
- 208000029257 vision disease Diseases 0.000 description 4
- 0 **1C(N)=CC=*1 Chemical compound **1C(N)=CC=*1 0.000 description 3
- 206010003591 Ataxia Diseases 0.000 description 3
- 102100022440 Battenin Human genes 0.000 description 3
- 101150038645 CLN3 gene Proteins 0.000 description 3
- 208000012661 Dyskinesia Diseases 0.000 description 3
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 3
- 101000901683 Homo sapiens Battenin Proteins 0.000 description 3
- 101000574223 Homo sapiens Palmitoyl-protein thioesterase 1 Proteins 0.000 description 3
- 102000016979 Other receptors Human genes 0.000 description 3
- 102100025824 Palmitoyl-protein thioesterase 1 Human genes 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 230000004071 biological effect Effects 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 230000001149 cognitive effect Effects 0.000 description 3
- 230000002354 daily effect Effects 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 230000005584 early death Effects 0.000 description 3
- 230000007062 hydrolysis Effects 0.000 description 3
- 238000006460 hydrolysis reaction Methods 0.000 description 3
- 208000017482 infantile neuronal ceroid lipofuscinosis Diseases 0.000 description 3
- 201000007635 neuronal ceroid lipofuscinosis 8 northern epilepsy variant Diseases 0.000 description 3
- 238000007254 oxidation reaction Methods 0.000 description 3
- 230000002441 reversible effect Effects 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 239000000829 suppository Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 208000024255 Audiogenic seizures Diseases 0.000 description 2
- 206010012289 Dementia Diseases 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 102000000079 Kainic Acid Receptors Human genes 0.000 description 2
- 108010069902 Kainic Acid Receptors Proteins 0.000 description 2
- 208000015439 Lysosomal storage disease Diseases 0.000 description 2
- 208000019695 Migraine disease Diseases 0.000 description 2
- 241000699666 Mus <mouse, genus> Species 0.000 description 2
- 208000037006 Progressive epilepsy-intellectual disability syndrome, Finnish type Diseases 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 230000003213 activating effect Effects 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 239000003513 alkali Substances 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- 150000007942 carboxylates Chemical class 0.000 description 2
- 238000004891 communication Methods 0.000 description 2
- 230000007850 degeneration Effects 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 230000002349 favourable effect Effects 0.000 description 2
- 125000000524 functional group Chemical group 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 229930195712 glutamate Natural products 0.000 description 2
- 150000002466 imines Chemical class 0.000 description 2
- 230000001771 impaired effect Effects 0.000 description 2
- 230000001939 inductive effect Effects 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 2
- 230000002503 metabolic effect Effects 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 206010027599 migraine Diseases 0.000 description 2
- 230000007659 motor function Effects 0.000 description 2
- 230000002151 myoclonic effect Effects 0.000 description 2
- 210000000653 nervous system Anatomy 0.000 description 2
- 230000001537 neural effect Effects 0.000 description 2
- 230000003287 optical effect Effects 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 210000000664 rectum Anatomy 0.000 description 2
- 210000000225 synapse Anatomy 0.000 description 2
- 230000008685 targeting Effects 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- 230000000007 visual effect Effects 0.000 description 2
- 230000004393 visual impairment Effects 0.000 description 2
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 description 1
- ZRNSSRODJSSVEJ-UHFFFAOYSA-N 2-methylpentacosane Chemical compound CCCCCCCCCCCCCCCCCCCCCCCC(C)C ZRNSSRODJSSVEJ-UHFFFAOYSA-N 0.000 description 1
- 208000031277 Amaurotic familial idiocy Diseases 0.000 description 1
- 201000004569 Blindness Diseases 0.000 description 1
- 101150043138 CLN1 gene Proteins 0.000 description 1
- 101150100050 CLN2 gene Proteins 0.000 description 1
- 101150104491 CLN6 gene Proteins 0.000 description 1
- 101150113700 CLN8 gene Proteins 0.000 description 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 1
- 208000018152 Cerebral disease Diseases 0.000 description 1
- 101150047836 Cln5 gene Proteins 0.000 description 1
- 208000033001 Complex partial seizures Diseases 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 241000557626 Corvus corax Species 0.000 description 1
- 101000845893 Homo sapiens DnaJ homolog subfamily C member 5 Proteins 0.000 description 1
- 101000575454 Homo sapiens Major facilitator superfamily domain-containing protein 8 Proteins 0.000 description 1
- 101000710213 Homo sapiens Protein CLN8 Proteins 0.000 description 1
- 208000006083 Hypokinesia Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- 208000025966 Neurological disease Diseases 0.000 description 1
- 238000011795 OF1 mouse Methods 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 208000033063 Progressive myoclonic epilepsy Diseases 0.000 description 1
- 102100034479 Protein CLN8 Human genes 0.000 description 1
- 208000010340 Sleep Deprivation Diseases 0.000 description 1
- 206010043376 Tetanus Diseases 0.000 description 1
- 241000053227 Themus Species 0.000 description 1
- HJAXHGKQQWJCLH-LSBLOZSASA-N [(3s,6r,8s,9s,13r,14s,17r)-3-hydroxy-13-methyl-17-[(2r)-6-methylheptan-2-yl]-1,2,3,4,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-6-yl]methylastatine-211 Chemical compound C1([C@H](C[211At])C[C@H]2[C@@H]3CC[C@@H]([C@]3(CC[C@@H]22)C)[C@H](C)CCCC(C)C)=C2CC[C@H](O)C1 HJAXHGKQQWJCLH-LSBLOZSASA-N 0.000 description 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 description 1
- 125000002777 acetyl group Chemical class [H]C([H])([H])C(*)=O 0.000 description 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 description 1
- 230000029936 alkylation Effects 0.000 description 1
- 238000005804 alkylation reaction Methods 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 230000002052 anaphylactic effect Effects 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 210000001130 astrocyte Anatomy 0.000 description 1
- 208000021024 autosomal recessive inheritance Diseases 0.000 description 1
- 230000006399 behavior Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 230000003925 brain function Effects 0.000 description 1
- 244000309464 bull Species 0.000 description 1
- 229960000623 carbamazepine Drugs 0.000 description 1
- FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 238000007385 chemical modification Methods 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000002566 clonic effect Effects 0.000 description 1
- 230000019771 cognition Effects 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 125000000000 cycloalkoxy group Chemical group 0.000 description 1
- 125000000753 cycloalkyl group Chemical group 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 238000011157 data evaluation Methods 0.000 description 1
- 238000006900 dealkylation reaction Methods 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 230000001066 destructive effect Effects 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 1
- 230000008034 disappearance Effects 0.000 description 1
- 150000002081 enamines Chemical class 0.000 description 1
- 230000001037 epileptic effect Effects 0.000 description 1
- 238000006735 epoxidation reaction Methods 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 238000013401 experimental design Methods 0.000 description 1
- 125000003709 fluoroalkyl group Chemical group 0.000 description 1
- YLRFCQOZQXIBAB-RBZZARIASA-N fluoxymesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1CC[C@](C)(O)[C@@]1(C)C[C@@H]2O YLRFCQOZQXIBAB-RBZZARIASA-N 0.000 description 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 125000000291 glutamic acid group Chemical group N[C@@H](CCC(O)=O)C(=O)* 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 230000009599 head growth Effects 0.000 description 1
- 230000003483 hypokinetic effect Effects 0.000 description 1
- 238000003384 imaging method Methods 0.000 description 1
- 230000003116 impacting effect Effects 0.000 description 1
- 238000005462 in vivo assay Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 230000033001 locomotion Effects 0.000 description 1
- 210000003141 lower extremity Anatomy 0.000 description 1
- 210000003712 lysosome Anatomy 0.000 description 1
- 230000001868 lysosomic effect Effects 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 238000007431 microscopic evaluation Methods 0.000 description 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 1
- NBVXSUQYWXRMNV-UHFFFAOYSA-N monofluoromethane Natural products FC NBVXSUQYWXRMNV-UHFFFAOYSA-N 0.000 description 1
- 230000004973 motor coordination Effects 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 230000000626 neurodegenerative effect Effects 0.000 description 1
- 201000007607 neuronal ceroid lipofuscinosis 3 Diseases 0.000 description 1
- 201000007638 neuronal ceroid lipofuscinosis 8 Diseases 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007833 oxidative deamination reaction Methods 0.000 description 1
- 150000002923 oximes Chemical class 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 210000001428 peripheral nervous system Anatomy 0.000 description 1
- 239000008024 pharmaceutical diluent Substances 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 230000001242 postsynaptic effect Effects 0.000 description 1
- 201000001204 progressive myoclonus epilepsy Diseases 0.000 description 1
- 108091006082 receptor inhibitors Proteins 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 150000003462 sulfoxides Chemical class 0.000 description 1
- 230000005062 synaptic transmission Effects 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
Classifications
-
- 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
-
- 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
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
- C07D239/96—Two oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22794009P | 2009-07-23 | 2009-07-23 | |
| US61/227,940 | 2009-07-23 | ||
| PCT/EP2010/060733 WO2011009951A1 (en) | 2009-07-23 | 2010-07-23 | 1h-quinazoline-2, 4 -diones for use in the treatment of neuronal ceroid lipofuscinosis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102470137A true CN102470137A (zh) | 2012-05-23 |
Family
ID=42671655
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010800334750A Pending CN102470137A (zh) | 2009-07-23 | 2010-07-23 | 用于治疗神经元蜡样脂褐质沉积症的1h-喹唑啉-2,4-二酮 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20120122903A1 (enExample) |
| EP (1) | EP2456442A1 (enExample) |
| JP (1) | JP2012533605A (enExample) |
| KR (1) | KR20120052341A (enExample) |
| CN (1) | CN102470137A (enExample) |
| AU (1) | AU2010274921B2 (enExample) |
| BR (1) | BR112012001258A2 (enExample) |
| CA (1) | CA2768333A1 (enExample) |
| IN (1) | IN2012DN00235A (enExample) |
| MX (1) | MX2012000956A (enExample) |
| RU (1) | RU2012106426A (enExample) |
| WO (1) | WO2011009951A1 (enExample) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5976011B2 (ja) * | 2011-04-05 | 2016-08-23 | 武田薬品工業株式会社 | スルホンアミド誘導体およびその用途 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101155789A (zh) * | 2005-04-11 | 2008-04-02 | 诺瓦提斯公司 | 1h-喹唑啉-2,4-二酮及其作为ampa-受体配体的用途 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9400680D0 (en) * | 1994-01-14 | 1994-03-09 | Sandoz Ltd | Improvements in or relating to organic compounds |
| GB0416730D0 (en) * | 2004-07-27 | 2004-09-01 | Novartis Ag | Organic compounds |
-
2010
- 2010-07-23 CN CN2010800334750A patent/CN102470137A/zh active Pending
- 2010-07-23 RU RU2012106426/04A patent/RU2012106426A/ru not_active Application Discontinuation
- 2010-07-23 MX MX2012000956A patent/MX2012000956A/es not_active Application Discontinuation
- 2010-07-23 IN IN235DEN2012 patent/IN2012DN00235A/en unknown
- 2010-07-23 BR BR112012001258A patent/BR112012001258A2/pt not_active IP Right Cessation
- 2010-07-23 US US13/384,280 patent/US20120122903A1/en not_active Abandoned
- 2010-07-23 AU AU2010274921A patent/AU2010274921B2/en not_active Expired - Fee Related
- 2010-07-23 WO PCT/EP2010/060733 patent/WO2011009951A1/en not_active Ceased
- 2010-07-23 KR KR1020127004575A patent/KR20120052341A/ko not_active Withdrawn
- 2010-07-23 EP EP10734746A patent/EP2456442A1/en not_active Withdrawn
- 2010-07-23 JP JP2012521055A patent/JP2012533605A/ja active Pending
- 2010-07-23 CA CA2768333A patent/CA2768333A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101155789A (zh) * | 2005-04-11 | 2008-04-02 | 诺瓦提斯公司 | 1h-喹唑啉-2,4-二酮及其作为ampa-受体配体的用途 |
Non-Patent Citations (1)
| Title |
|---|
| BERND ELGER ET AL: "Optimized Synthesis of AMPA Receptor Antagonist ZK 187638 and Neurobehavioral Activity in a Mouse Model of Neuronal Ceroid Lipofuscinosis", 《CHEMMEDCHEM》, vol. 1, no. 10, 31 December 2006 (2006-12-31), pages 1142 - 1148, XP002599854, DOI: doi:10.1002/cmdc.200600144 * |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20120052341A (ko) | 2012-05-23 |
| AU2010274921A1 (en) | 2012-02-02 |
| BR112012001258A2 (pt) | 2016-02-10 |
| JP2012533605A (ja) | 2012-12-27 |
| CA2768333A1 (en) | 2011-01-27 |
| EP2456442A1 (en) | 2012-05-30 |
| MX2012000956A (es) | 2012-02-28 |
| AU2010274921B2 (en) | 2014-08-14 |
| IN2012DN00235A (enExample) | 2015-05-01 |
| RU2012106426A (ru) | 2013-08-27 |
| US20120122903A1 (en) | 2012-05-17 |
| WO2011009951A1 (en) | 2011-01-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US8993552B2 (en) | Compositions and methods for treatment of leukemia | |
| JP2018138555A (ja) | ブレクスピプラゾール又はその塩を含有する神経変性疾患に伴う周辺症状又は精神疾患に伴う衝動性症状の予防及び/又は治療剤 | |
| US12208079B2 (en) | Enantiomers of A2-73, analogues, and sigma agonist activity | |
| CN106983747A (zh) | 治疗依赖性的方法 | |
| US20140163050A1 (en) | Use of 1H-quinazoline-2,4-diones | |
| US20200215089A1 (en) | Ambroxol to improve and/or extend healthspan, lifespan and/or mental acuity | |
| EP4337316A1 (en) | Therapeutic aminoindane compounds and compositions | |
| CN101676287B (zh) | 用作抗癫痫药的6-(取代苯氧基)-四唑并[5,1-a]酞嗪衍生物及其可药用盐 | |
| CN102470137A (zh) | 用于治疗神经元蜡样脂褐质沉积症的1h-喹唑啉-2,4-二酮 | |
| CN101429191B (zh) | 取代的四氢异喹啉衍生物的用途 | |
| US20250205191A1 (en) | R(-)-mdma compositions and methods of treatment | |
| ES2662570T3 (es) | Composición para tratar el trastorno de deseo sexual hipoactivo | |
| WO2015157451A1 (en) | Methods for treating attention deficit hyperactivity disorder | |
| CN112822997A (zh) | 用于治疗孤独症的组合物和方法 | |
| CN112789045A (zh) | 用于治疗孤独症的组合物和方法 | |
| EP2753331A1 (en) | Use of 1h-quinazoline- 2, 4 -diones for use in the prevention or treatment photosensitive epilepsy | |
| US11970439B1 (en) | 8-(4-chlorobenzylideneamino)naphthalene-1,3-disulfonic acid as an antioxidant compound | |
| EP3646886A1 (en) | Treatment of pain with serotonin-3 receptor agonist | |
| US20250332138A1 (en) | Pharmaceutical composition for preventing or treating mental disorder | |
| Wrzosek | electroencephalography: Methodology and findings in California sea lions (Zalophus californianus) | |
| CN103896949A (zh) | 哌嗪酮醇类磷酸二酯酶-5抑制剂 | |
| Sajja et al. | Practice questions in Psychopharmacology | |
| DATE | Investigator’s Brochure |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C53 | Correction of patent of invention or patent application | ||
| CB02 | Change of applicant information |
Address after: Basel Applicant after: Novartis Ag Address before: Basel Applicant before: Novartis AG |
|
| COR | Change of bibliographic data |
Free format text: CORRECT: APPLICANT; FROM: NOVARTIS AG TO: NOVARTIS CO., LTD. |
|
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20120523 |