HRP20170458T1 - Modulatori atp - vezujućih kasetnih transportera - Google Patents
Modulatori atp - vezujućih kasetnih transportera Download PDFInfo
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- HRP20170458T1 HRP20170458T1 HRP20170458TT HRP20170458T HRP20170458T1 HR P20170458 T1 HRP20170458 T1 HR P20170458T1 HR P20170458T T HRP20170458T T HR P20170458TT HR P20170458 T HRP20170458 T HR P20170458T HR P20170458 T1 HRP20170458 T1 HR P20170458T1
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- abc transporter
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- 108010006533 ATP-Binding Cassette Transporters Proteins 0.000 title claims 14
- 102000005416 ATP-Binding Cassette Transporters Human genes 0.000 title claims 14
- 150000001875 compounds Chemical class 0.000 claims 32
- 230000000694 effects Effects 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 239000012634 fragment Substances 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 239000012472 biological sample Substances 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 2
- 206010014561 Emphysema Diseases 0.000 claims 2
- PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 230000007812 deficiency Effects 0.000 claims 2
- 150000003839 salts Chemical class 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
- 102000004321 Atrophin-1 Human genes 0.000 claims 1
- 108090000806 Atrophin-1 Proteins 0.000 claims 1
- 206010008025 Cerebellar ataxia Diseases 0.000 claims 1
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims 1
- 206010053567 Coagulopathies 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
- 201000008163 Dentatorubral pallidoluysian atrophy Diseases 0.000 claims 1
- 206010013883 Dwarfism Diseases 0.000 claims 1
- 208000024720 Fabry Disease Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000005139 Hereditary Angioedema Types I and II 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
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims 1
- 206010020850 Hyperthyroidism Diseases 0.000 claims 1
- 206010051125 Hypofibrinogenaemia Diseases 0.000 claims 1
- 208000000038 Hypoparathyroidism Diseases 0.000 claims 1
- 208000006302 Laron syndrome 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
- 208000008955 Mucolipidoses Diseases 0.000 claims 1
- 206010072928 Mucolipidosis type II Diseases 0.000 claims 1
- 208000002678 Mucopolysaccharidoses Diseases 0.000 claims 1
- 102100026784 Myelin proteolipid protein Human genes 0.000 claims 1
- 206010068871 Myotonic dystrophy Diseases 0.000 claims 1
- 201000005118 Nephrogenic diabetes insipidus Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000003450 Neurogenic Diabetes Insipidus Diseases 0.000 claims 1
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000017493 Pelizaeus-Merzbacher disease Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 208000025237 Polyendocrinopathy Diseases 0.000 claims 1
- 208000024777 Prion disease Diseases 0.000 claims 1
- 208000033063 Progressive myoclonic epilepsy Diseases 0.000 claims 1
- 201000005660 Protein C Deficiency Diseases 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims 1
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 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
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 210000000988 bone and bone Anatomy 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
- 230000009852 coagulant 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
- 230000020764 fibrinolysis Effects 0.000 claims 1
- 208000012770 hereditary angioedema type 1 Diseases 0.000 claims 1
- 208000013746 hereditary thrombophilia due to congenital protein C deficiency Diseases 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000037356 lipid metabolism Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 208000020460 mucolipidosis II alpha/beta 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
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000005119 neurohypophyseal diabetes insipidus Diseases 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 230000001590 oxidative effect Effects 0.000 claims 1
- 239000000825 pharmaceutical preparation 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
- 239000000523 sample Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
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- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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Claims (19)
1. Spoj formule II:
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time da neovisno u svakom slučaju:
R je H, OH, OCH3 ili dva R zajedno tvore -OCH2O- ili -OCF2O-;
R1 je H ili do dva C1-C6 alkila;
R2 je H ili halo;
R3 je H ili C1-C6 alkil;
Y je O ili NR4; i
R4 je H ili C1-C6alkil.
2. Spoj prema zahtjevu 1 formule II, naznačen time da dva R zajedno tvore - OCF2O-, R1 je H, i R2 je F.
3. Spoj prema zahtjevu 1 formule II, naznačen time da dva R zajedno tvore - OCF2O-, R1 je H, R2 je F, i R3 je CH3.
4. Spoj prema zahtjevu 1, naznačen time da ima formulu IIa:
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu:
R2 je H ili halo.
5. Spoj prema zahtjevu 4, naznačen time da R2 je F.
6. Spoj prema zahtjevu 1, naznačen time da je spoj
[image]
ili
[image]
7. Spoj prema zahtjevu 1, naznačen time da je spoj
[image]
8. Farmaceutski pripravak naznačen time da sadrži
(i) spoj prema bilo kojem od zahtjeva 1-7; i
(ii) farmaceutski prihvatljiv nosač.
9. Pripravak prema zahtjevu 8, naznačen time da još sadrži dodatno sredstvo odabrano iz skupine koju čine mukolitičko sredstvo, bronhodilatator, antibiotik, protuinfektivno sredstvo, protuupalno sredstvo, CFTR korektor, CFTR potencijator, ili hranjivo sredstvo.
10. Ex vivo postupak za povećavanje broja funkcionalnih ABC transportera u staničnoj membrani, naznačen time da sadrži korak dovođenja stanice u kontakt sa spojem prema bilo kojem od zahtjeva 1-7.
11. Postupak prema zahtjevu 10, naznačen time da je ABC transporter CFTR.
12. Spoj prema bilo kojem od zahtjeva 1 do 7 ili pripravak prema bilo kojem od zahtjeva 8 do 9 za upotrebu u postupku liječenja stanja, bolesti ili poremećaja kod subjekta koji uključuju aktivnost ABC transportera, naznačen time da navedeni postupak sadrži korak davanja subjektu spoja prema bilo kojem od zahtjeva 1 do 7 ili pripravka prema bilo kojem od zahtjeva 8 do 9, pri čemu je stanje, bolest ili poremećaj odabran od cistične fibroze, emfizema, nasljedne hemokromatoze, nedostataka koagulacije - fibrinolize, nedostatka proteina C, nasljednog angioedema tipa 1, nedostatka u metabolizmu lipida, obiteljske hiperkolesterolemije, kilomikronemije tipa 1, abetalipoproteinemije, bolesti lizosomskog nakupljanja, bolesti I-stanica/pseudo-Hurler, mukopolisaharidoze, Sandhof/Tay-Sachs, Crigler-Najjar tipa II, poliendokrinopatije/hiperinzulemije, dijabetes melitusa, Laronovog sindroma patuljastog rasta, nedostatka mijeloperoksidaze, primarnog hipoparatiroidizma, melanoma, glikanoza CDG tipa 1, kongenitalne hipertireoze, lako lomljivih kosti (osteogenesis imperfecta), nasljedne hipofibrinogenemije, nedostatka ACT, insipidnog dijabetesa (di), neurohipofizarnog insipidnog dijabetesa, nefrogenog insipidnog dijabetesa, Charcot-Marie Tooth sindroma, Pelizaeus-Merzbacherove bolesti, neurodegenerativne bolesti, Alzheimerove bolesti, Parkinsonove bolesti, amiotrofne lateralne skleroze, progresivne supranuklearne paralize, Pickove bolesti, poliglutaminskog neurološkog poremećaja, Huntingtonove bolesti, spinocerebelarne ataksije tipa I, spinalne i bulbarne mišićne atrofije, dentatorubralna palidolujzianska atrofija, miotonične distrofije, spongiformne encefalopatije, nasljedne Creutzfeldt-Jakobove bolesti, Fabrijeve bolesti, sindroma Straussler-Scheinker, COPD, bolesti suhog oka, ili Sjögrenove bolesti.
13. Spoj prema bilo kojem od zahtjeva 1 do 7 ili pripravak prema bilo kojem od zahtjeva 8 do 9 za upotrebu prema zahtjevu 12, naznačen time da se stanje, bolest ili poremećaj bira između cistične fibroze, emfizema, COPD ili bolesti suhog oka.
14. Komplet za upotrebu u mjerenju aktivnosti ABC – transportera ili njegovog fragmenta u biološkom uzorku in vitro, naznačen time da sadrži
(i) spoj prema bilo kojem od zahtjeva 1-7; i
(ii) upute za:
a) dovođenje u kontakt spoja s biološkim uzorkom; i
b) mjerenje aktivnosti navedenog ABC transportera ili njegovog fragmenta.
15. Komplet prema zahtjevu 14, naznačen time da nadalje sadrži upute za
a) dovođenje u kontakt dodatnog spoja s biološkim uzorkom;
b) mjerenje aktivnosti navedenog ABC transportera ili njegovog fragmenta u prisutnosti navedenog dodatnog spoja i
c) usporedbu aktivnosti ABC transportera u prisutnosti dodatnog spoja s gustoćom ABC transportera u prisutnosti prvog spoja.
16. Komplet za upotrebu za mjerenje aktivnosti ABC transportera ili njegovog fragmenta u uzorku in vivo naznačen time da sadrži:
(i) spoj prema bilo kojem od zahtjeva 1-7; i
(ii) upute za:
a) dovođenje u kontakt spoja s biološkim uzorkom; i
b) mjerenje aktivnosti navedenog ABC transportera ili njegovog fragmenta.
17. Komplet prema zahtjevu 16, naznačen time da nadalje sadrži upute za
a) dovođenje u kontakt dodatnog spoja s biološkim uzorkom;
b) mjerenje aktivnosti navedenog ABC transportera ili njegovog fragmenta u prisutnosti navedenog dodatnog spoja i
c) usporedbu aktivnosti ABC transportera u prisutnosti dodatnog spoja s gustoćom ABC transportera u prisutnosti prvog spoja.
18. Postupak za dobivanje spoja formule IIa
[image]
pri čemu R2 je H ili halo, naznačen time da sadrži
(a) dovođenje u kontakt spoja formule I-5 s karbonil diimidazolom (CDI) u prisutnosti otapala da se dobije spoj formule I-4;
[image]
(b) dovođenje u kontakt spoja formule I-4 sa oksidansom u prisutnosti otapala da se dobije spoj formule I-3;
[image]
i
(c) dovođenje u kontakt spoja formule I-3 s bazom u prisutnosti otapala da se dobije spoj formule IIa:
[image]
19. Postupak prema zahtjevu 18, naznačen time da R2 je H ili F.
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2012
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- 2012-11-08 AU AU2012335714A patent/AU2012335714B2/en active Active
- 2012-11-08 IN IN885KON2014 patent/IN2014KN00885A/en unknown
- 2012-11-08 CN CN201280054919.8A patent/CN104039775B/zh active Active
- 2012-11-08 WO PCT/US2012/064217 patent/WO2013070961A1/en active Application Filing
- 2012-11-08 SI SI201230931A patent/SI2776427T1/sl unknown
- 2012-11-08 LT LTEP12794811.5T patent/LT2776427T/lt unknown
- 2012-11-08 US US13/672,538 patent/US9254291B2/en active Active
- 2012-11-08 ES ES12794811.5T patent/ES2622154T3/es active Active
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- 2012-11-08 MX MX2014005462A patent/MX357328B/es active IP Right Grant
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- 2012-11-08 ME MEP-2017-72A patent/ME02650B/me unknown
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- 2014-05-06 ZA ZA2014/03262A patent/ZA201403262B/en unknown
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Also Published As
| Publication number | Publication date |
|---|---|
| ME02650B (me) | 2017-06-20 |
| JP6072056B2 (ja) | 2017-02-01 |
| IL232308A (en) | 2016-11-30 |
| JP2014534236A (ja) | 2014-12-18 |
| EP2776427A1 (en) | 2014-09-17 |
| CN104039775B (zh) | 2017-03-01 |
| RU2640420C2 (ru) | 2018-01-09 |
| SI2776427T1 (sl) | 2017-05-31 |
| AU2012335714A1 (en) | 2014-05-22 |
| WO2013070961A1 (en) | 2013-05-16 |
| ES2622154T3 (es) | 2017-07-05 |
| MX2014005462A (es) | 2015-03-23 |
| US9254291B2 (en) | 2016-02-09 |
| CN104039775A (zh) | 2014-09-10 |
| KR20140090231A (ko) | 2014-07-16 |
| CA2852991C (en) | 2019-12-31 |
| MX357328B (es) | 2018-07-05 |
| CA2852991A1 (en) | 2013-05-16 |
| ZA201403262B (en) | 2017-09-27 |
| NZ624440A (en) | 2016-09-30 |
| LT2776427T (lt) | 2017-04-10 |
| US20130116238A1 (en) | 2013-05-09 |
| KR101985044B1 (ko) | 2019-05-31 |
| EP2776427B1 (en) | 2017-02-01 |
| IN2014KN00885A (hr) | 2015-10-02 |
| RU2014123381A (ru) | 2015-12-20 |
| IL232308A0 (en) | 2014-06-30 |
| AU2012335714B2 (en) | 2017-04-13 |
| HK1201827A1 (en) | 2015-09-11 |
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