HRP20160185T1 - Spojevi iminotiadiazin dioksida kao inhibitori bace, smjese i njihova uporaba - Google Patents
Spojevi iminotiadiazin dioksida kao inhibitori bace, smjese i njihova uporaba Download PDFInfo
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- HRP20160185T1 HRP20160185T1 HRP20160185T HRP20160185T HRP20160185T1 HR P20160185 T1 HRP20160185 T1 HR P20160185T1 HR P20160185 T HRP20160185 T HR P20160185T HR P20160185 T HRP20160185 T HR P20160185T HR P20160185 T1 HRP20160185 T1 HR P20160185T1
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- 150000001875 compounds Chemical class 0.000 title claims 38
- 239000000203 mixture Substances 0.000 title claims 2
- IBIDQDPPONSSPQ-UHFFFAOYSA-N 1-imino-2H-thiadiazine Chemical compound N=S1NN=CC=C1 IBIDQDPPONSSPQ-UHFFFAOYSA-N 0.000 title 1
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 14
- 208000024827 Alzheimer disease Diseases 0.000 claims 5
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 230000007170 pathology Effects 0.000 claims 2
- 206010063409 Acarodermatitis Diseases 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
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010036631 Presenile dementia Diseases 0.000 claims 1
- 241000447727 Scabies Species 0.000 claims 1
- 206010039966 Senile dementia Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000003941 amyloidogenesis Effects 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 208000005881 bovine spongiform encephalopathy Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000001054 cortical effect Effects 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
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010014599 encephalitis Diseases 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 230000007388 microgliosis Effects 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 208000005687 scabies Diseases 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
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Claims (15)
1. Spoj, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu koja se bira između:
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i
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2. Spoj iz zahtjeva 1, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu:
[image]
3. Spoj iz zahtjeva 1, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu:
[image]
4. Spoj iz zahtjeva 1, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu:
[image]
5. Spoj iz zahtjeva 1, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu:
[image]
6. Spoj iz zahtjeva 1, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu:
[image]
7. Spoj iz zahtjeva 1, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu:
[image]
8. Spoj iz zahtjeva 1, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu:
[image]
9. Spoj iz zahtjeva 1, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera, naznačeni time, što spomenuti spoj ima strukturu:
[image]
10. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, što je u obliku slobodne baze.
11. Spoj prema bilo kojem od zahtjeva 1-9, naznačen time, što je u obliku kisele adicijske soli.
12. Spoj, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera prema bilo kojem od prethodnih zahtjeva, naznačeni time, što se koriste u medicini.
13. Farmaceutska smjesa, naznačena time, što sadrži najmanje jedan spoj iz bilo kojeg od zahtjeva 1-11, ili njegov tautomer, ili farmaceutski prihvatljivu sol spomenutog spoja ili spomenutog tautomera i farmaceutski prihvatljivi nosač ili razblaživač.
14. Spoj, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera prema bilo kojem od zahtjeva 1-11, naznačeni time, što se koriste za liječenje, prevenciju i/ili odgađanje pojave patologije koja se bira između: Alzheimer-ove bolesti, Down-ovog sindroma, Parkinson-ove bolesti, moždanog udara, mikroglioze, upale mozga, presenilne demencije, senilne demencije, progresivne supranukleusne paralize, kortikalne bazalne degeneracije, poremećaja čula mirisa udruženog sa Alzheimer-ovom bolešću, Parkinson-ovom bolešću, i/ili Down-ovim sindromom, β-amiloidne angiopatije, cerebralne amiloidne angiopatije, hereditarne cerebralne hemoragije, blagog kognitivnog poremećaja, glaukoma, amiloidoze, dijabetesa tipa II, amiloidogeneze udružene sa dijabetesom, šuge, goveđeg spongiformnog encefalitisa, Creutzfeld-Jakob-ove bolesti i traumatske povrede mozga.
15. Spoj, ili njegov tautomer, ili farmaceutski prihvatljiva sol spomenutog spoja ili spomenutog tautomera za uporabu prema zahtjevu 14, naznačeni time, što je spomenuta patologija Alzheimer-ova bolest.
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