ME02105B - Modulatori atp-vezujucih kasetnih transportera - Google Patents
Modulatori atp-vezujucih kasetnih transporteraInfo
- Publication number
- ME02105B ME02105B MEP-2015-37A MEP3715A ME02105B ME 02105 B ME02105 B ME 02105B ME P3715 A MEP3715 A ME P3715A ME 02105 B ME02105 B ME 02105B
- Authority
- ME
- Montenegro
- Prior art keywords
- disease
- compound
- abc transporter
- activity
- composition
- Prior art date
Links
- 108010006533 ATP-Binding Cassette Transporters Proteins 0.000 title claims 9
- 102000005416 ATP-Binding Cassette Transporters Human genes 0.000 title claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 238000000338 in vitro Methods 0.000 claims 4
- 239000012472 biological sample Substances 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 239000003623 enhancer Substances 0.000 claims 3
- 239000012634 fragment Substances 0.000 claims 3
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 206010014561 Emphysema Diseases 0.000 claims 2
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 0.000 claims 2
- 230000007812 deficiency Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102100032187 Androgen receptor Human genes 0.000 claims 1
- 102000014461 Ataxins Human genes 0.000 claims 1
- 108010078286 Ataxins Proteins 0.000 claims 1
- 206010003694 Atrophy Diseases 0.000 claims 1
- 208000014644 Brain disease Diseases 0.000 claims 1
- 206010008025 Cerebellar ataxia Diseases 0.000 claims 1
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010062264 Congenital hyperthyroidism 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
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013883 Dwarfism Diseases 0.000 claims 1
- 208000032274 Encephalopathy Diseases 0.000 claims 1
- 208000024720 Fabry Disease Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- 208000033981 Hereditary haemochromatosis Diseases 0.000 claims 1
- 101000775732 Homo sapiens Androgen receptor Proteins 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims 1
- 206010051125 Hypofibrinogenaemia Diseases 0.000 claims 1
- 208000000038 Hypoparathyroidism Diseases 0.000 claims 1
- 102100024640 Low-density lipoprotein receptor Human genes 0.000 claims 1
- 208000015439 Lysosomal storage disease Diseases 0.000 claims 1
- 208000002678 Mucopolysaccharidoses Diseases 0.000 claims 1
- 206010068871 Myotonic dystrophy Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 208000025237 Polyendocrinopathy Diseases 0.000 claims 1
- 201000005660 Protein C Deficiency Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims 1
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 claims 1
- 208000004622 abetalipoproteinemia Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 229960005475 antiinfective agent Drugs 0.000 claims 1
- 239000004599 antimicrobial Substances 0.000 claims 1
- 230000037444 atrophy Effects 0.000 claims 1
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 229940124630 bronchodilator Drugs 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 210000000170 cell membrane Anatomy 0.000 claims 1
- 238000005345 coagulation Methods 0.000 claims 1
- 230000007547 defect Effects 0.000 claims 1
- 201000010064 diabetes insipidus Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003172 expectorant agent Substances 0.000 claims 1
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims 1
- 208000013746 hereditary thrombophilia due to congenital protein C deficiency Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- PURKAOJPTOLRMP-UHFFFAOYSA-N ivacaftor Chemical group C1=C(O)C(C(C)(C)C)=CC(C(C)(C)C)=C1NC(=O)C1=CNC2=CC=CC=C2C1=O PURKAOJPTOLRMP-UHFFFAOYSA-N 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 229940066491 mucolytics Drugs 0.000 claims 1
- 206010028093 mucopolysaccharidosis Diseases 0.000 claims 1
- 208000000638 myeloperoxidase deficiency Diseases 0.000 claims 1
- 230000002988 nephrogenic effect Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 108010040003 polyglutamine Proteins 0.000 claims 1
- 229920000155 polyglutamine Polymers 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Classifications
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- 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
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- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/12—Radicals substituted by oxygen atoms
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Claims (12)
1. Spoj koji je:
2. Farmaceutski sastav koji sadrži (i) spoj prema patentnom zahtjevu 1; i (ii) farmaceutski prihvatljivnosač.
3. Sastav prema patentnom zahtjevu 2, naznačen time da nadalje sadrži dodatno sredstvo izabrano od mukolitičkog sredstva, bronhodilatatora, antibiotika, anti-infektivnog sredstva, protu-upalnog sredstva, CFTR korektora, CFTR pojačivača, ili nutritivnog sredstva.
4. Sastav prema patentom zahtjevu 3, naznačen time da je dodatno sredstvo CFTR pojačivač.
5. Sastav prema patentom zahtjevu 4, naznačen time da je pojačivač N-(5-hidroksi-2,4-diterc-butil-fenil)-4-okso-1H-kinolin-3-karboksamid.
6. In vitro metoda povećanja broja funkcionalnih ABC transportera u membrani satnice in vitro, koji sadrži korak uspostavljanja kontakta navedene stanice sa spojem koji je:
7. In vitro metoda prema patentnom zahtjevu 6, naznačen time da je ABC transporter CFTR.
8. Spoj koji je: za upotrebu u liječenju stanja, bolesti ili poremećaja kod pacijenta a koji su implicirani aktivnošću ABC transportera, pri čemu je navedeno stanje, bolest ili poremećaj izabrano od cistične fibroze, nasljednog emfizema, nasljedne hemokromatoze, fibrinolize-nedostataka koagulacije, kao što su nedostatak proteina C, Tip 1 nasljedni angioedem, nedostaci prerade lipida, kao što su familijarna hiperkolesterolemija, Tip 1 hilomikronemija, abetalipoproteinemija, bolesti lizosomalnog nakupljanja, kao što je 1-stanična bolest/Pseudo-Hurler, mukopolisaharidoze, Sandhof/Tay-Sachs, Crigler-Najjar tip II, poliendokrinopatija/hiperinsulinemija, dijabetes melitus, Laronov patuljasti rast, nedostatak mijeloperoksidaze, primarni hipoparatireoidizam, melanom, Glikanozis CDG tip 1, nesljedni emfizem, kongenitalni hipertireoidizam, osteogenezis imperfekta, nasljedna hipofibrinogenemia, ACT nedostatak, dijabetes insipidus (DI), neurohipofizealni DI, nefrogeni DI, tzv. "Charcot-Marie Tooth sindrom", tzv. "Perlizaeus-Merzbacher bolest", neurodegenerativne bolesti kao što su Alzheimerova bolest, Parkinsonova bolest, amiotrofična lateralna skleroza, progresivna supranuklearna paraliza, Pikova bolest, nekoliko poliglutamin neuroloških poremećaja kao što su, Hantingtonova bolest, spinocerebelarna ataksija tip I, spinalna i bulbarna mišična atrofija, dentatorubralna-palidolizinska atrofija i miotonična distrofija, kao i spongioformne encefalopatije, kao što su nasljedna Creutzfeldt-Jakobova bolest, Fabrijeva bolest, Gerstmann-Sträussler-Scheinkerov sindrom, COPD, bolest suhog oka, Sjögrenov sindrom.
9. Spoj za upotrebu prema patentnom zahtjevu 8, naznačen time da je stanje, bolest ili poremećaj cistična fibroza.
10. Oprema za upotrebu u mjerenju aktivnosti ABC transportera ili njegovog fragmenta u biološkom uzorku in vitro ili in vivo, koji sadrži: (i) prvi sastav koji sadrži spoj prema patentnom zahtjevu 1; i (ii) instrukcije za: a) kontaktiranje sastava s biološkim uzorkom; b) mjerenje aktivnosti navedenog ABC transportera ili njegovog fragmenta.
11. Oprema za upotrebu prema patentnom zahtjevu 10, naznačena time da nadalje sadrži instrukcije za a) kontaktiranje dodatnog sastava s biološkim uzorkom; b) mjerenje aktivnosti navedenog ABC transportera ili njegovog fragmenta u prisutnosti navedenog dodatnog spoja, i c) usporedba aktivnosti ABC transportera u prisutnosti dodatnog spoja s gustoćom ABC transportera u prisutnosti navedene prvog sastava.
12. Oprema za upotrebu prema patentnom zahtjevu 10, naznačena time da se oprema koristi za mjerenje gustoće CPTR.
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