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HRP20100263T1 - Ciklopropil amini kao modulatori histaminskog h3 receptora - Google Patents

Ciklopropil amini kao modulatori histaminskog h3 receptora Download PDF

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HRP20100263T1
HRP20100263T1 HR20100263T HRP20100263T HRP20100263T1 HR P20100263 T1 HRP20100263 T1 HR P20100263T1 HR 20100263 T HR20100263 T HR 20100263T HR P20100263 T HRP20100263 T HR P20100263T HR P20100263 T1 HRP20100263 T1 HR P20100263T1
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Croatia
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cyclopropyl
piperazin
ylmethyl
phenyl
methanone
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HR20100263T
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D. Allison Brett
I. Carruthers Nicholas
A. Grice Cheryl
A. Letavic Michael
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Janssen Pharmaceutica N.V.
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Publication of HRP20100263T1 publication Critical patent/HRP20100263T1/hr

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Abstract

Spoj, naznačen time, da je izabran iz skupine koju čine: (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon, (4-ciklopropil-piperazin-1-il)-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-metanon, (4-ciklopropil-piperazin-1-il)-(4-tiomorfolin-4-ilmetil-fenil)-metanon, te (4-ciklopropil-piperazin-1-il)-[4-(2-hidroksimetil-morfolin-4-ilmetil)-fenil]-metanon, te njihovi enantiomeri, hidrati, solvati i farmaceutski prihvatljive soli. Patent sadrži još 27 patentnih zahtjeva.

Claims (28)

1. Spoj, naznačen time, da je izabran iz skupine koju čine: (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon, (4-ciklopropil-piperazin-1-il)-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-metanon, (4-ciklopropil-piperazin-1-il)-(4-tiomorfolin-4-ilmetil-fenil)-metanon, te (4-ciklopropil-piperazin-1-il)-[4-(2-hidroksimetil-morfolin-4-ilmetil)-fenil]-metanon, te njihovi enantiomeri, hidrati, solvati i farmaceutski prihvatljive soli.
2. Spoj u skladu sa zahtjevom 1, naznačen time, da je (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon ili njegov enantiomer, hidrat, solvat ili farmaceutski prihvatljiva sol.
3. Spoj u skladu sa zahtjevom 1, naznačen time, da je (4-ciklopropil-piperazin-1-il)-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-metanon ili njegov enantiomer, hidrat, solvat ili farmaceutski prihvatljiva sol.
4. Spoj u skladu sa zahtjevom 1, naznačen time, da je (4-ciklopropil-piperazin-1-il)-(4-tiomorfolin-4-ilmetil-fenil)-metanon ili njegov enantiomer, hidrat, solvat ili farmaceutski prihvatljiva sol.
5. Spoj u skladu sa zahtjevom 1, naznačen time, da je (4-ciklopropil-piperazin-1-il)-[4-(2-hidroksimetil-morfolin-4-ilmetil)-fenil]-metanon ili njegov enantiomer, hidrat, solvat ili farmaceutski prihvatljiva sol.
6. Spoj u skladu sa zahtjevom 2, naznačen time, da je izabran iz skupine koju čine (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon i (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon dihidroklorid.
7. Spoj u skladu sa zahtjevom 6, naznačen time, da je (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon.
8. Spoj u skladu sa zahtjevom 6, naznačen time, da je (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon dihidroklorid.
9. Spoj u skladu sa zahtjevom 2, naznačen time, da je (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon citratna sol.
10. Spoj u skladu sa zahtjevom 1, naznačen time, da je (4-ciklopropil-piperazin-1-il)-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-metanon citratna sol, (4-ciklopropil-piperazin-1-il)-(4-tiomorfolin-4-ilmetil-fenil)-metanon citratna sol ili (4-ciklopropil-piperazin-1-il)-[4-(2-hidroksimetil-morfolin-4-ilmetil)-fenil]-metanon citratna sol.
11. Farmaceutski pripravak, naznačen time, da sadrži farmaceutski prihvatljivu podlogu i učinkovitu količinu najmanje jednog spoja izabranog iz skupine koju čine: (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon, (4-ciklopropil-piperazin-1-il)-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-metanon, (4-ciklopropil-piperazin-1-il)-(4-tiomorfolin-4-ilmetil-fenil)-metanon, te (4-ciklopropil-piperazin-1-il)-[4-(2-hidroksimetil-morfolin-4-ilmetil)-fenil]-metanon, te njihovi enantiomeri, hidrati, solvati i farmaceutski prihvatljive soli.
12. Najmanje jedan spoj izabran iz skupine koju čine: (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon, (4-ciklopropil-piperazin-1-il)-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-metanon, (4-ciklopropil-piperazin-1-il)-(4-tiomorfolin-4-ilmetil-fenil)-metanon, te (4-ciklopropil-piperazin-1-il)-[4-(2-hidroksimetil-morfolin-4-ilmetil)-fenil]-metanon, te njihovi enantiomeri, hidrati, solvati i farmaceutski prihvatljive soli, naznačen time, da se koristi u liječenju ili prevenciji CNS poremećaja izabranog iz skupine koju čine: neurološki poremećaji uključujući i poremećaje spavanje/buđenje i napetost/opreznost (na primjer nesanica i promjena vremenskih zona (jet lag)), hiperaktivni poremećaji s deficitom pozornosti (ADHD), poremećaji učenja i pamćenja, kognitivna disfunkcija, migrena, neurogena upala, demencija, blago kognitivno oštećenje (pre-demencija), Alzheimer-ova bolest, epilepsija, narkolepsija s ili bez pridružene katapleksije, katapleksija, poremećaji homeostaze spavanje/buđenje, idiopatska somnolencija (pospanost), pretjerana dnevna pospanost (EDS), poremećaji cirkadijskog ritma, poremećaji spavanje/umor, umor, iscrpljenost povezana s apnejom u snu, poremećaj sna zbog perimenopauzalnih hormonalnih pomaka, umor povezan s Parkinsonovom bolesti, MS-povezan umor, umor povezan s depresijom, umor izazvan s kemoterapijom, poremećaji hranjenja, debljina, bolest putovanja, vertigo, šizofrenija, zlouporaba supstancija, bipolarni poremećaji, manični poremećaji i depresija kod sisavaca.
13. Najmanje jedan spoj izabran iz skupine koju čine: (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon, (4-ciklopropil-piperazin-1-il)-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-metanon, (4-ciklopropil-piperazin-1-il)-(4-tiomorfolin-4-ilmetil-fenil)-metanon, te (4-ciklopropil-piperazin-1-il)-[4-(2-hidroksimetil-morfolin-4-ilmetil)-fenil]-metanon, te njihovi enantiomeri, hidrati, solvati i farmaceutski prihvatljive soli, naznačen time, da se koristi u liječenju ili prevenciji alergijskih reakcija gornjih dišnih puteva, astme, svrbeža, nazalne kongestije ili alergijskog rinitisa kod sisavaca.
14. Najmanje jedan spoj u skladu sa zahtjevom 1 te b) jedan ili više histaminskih H1 ili H2 antagonista, naznačeni time, da se koriste u liječenju ili prevenciji alergijskog rinitisa, nazalne kongestije i alergijske kongestije.
15. Najmanje jedan spoj u skladu sa zahtjevom 1 te b) jedan ili više blokatora ponovnog vezivanja neurotransmitera, naznačeni time, da se koriste u liječenju ili prevenciji depresije, poremećaja raspoloženja ili šizofrenije.
16. Najmanje jedan spoj u skladu sa zahtjevom 1 te b) modafinil, naznačeni time, da se koriste u liječenju ili prevenciji narkolepsije, pretjerane dnevne pospanosti (EDS), Alzheimer-ove bolesti, depresije, poremećaja deficita pozornosti, MS-povezanog umora, omamljenosti nakon anestezije, kognitivnog oštećenja, šizofrenije, spazma povezanog sa cerebralnom paralizom, slabljenja pamćenja zbog dobi, idiopatske somnolencije ili jet-lag.
17. Spoj u skladu sa zahtjevom 1, naznačen time, da je izotopno označen tako da se može prepoznati pomoću PET ili SPECT.
18. Spoj u skladu sa zahtjevom 1 koji je 18F-označen ili 11C-označen, naznačen time, da se koristi u postupku proučavanja poremećaja posredovanih histaminom, a navedeni postupak obuhvaća korak uporabe navedenog spoja kao molekularne probe pozitron emisijske tomografije (PET).
19. Farmaceutski pripravak u skladu sa zahtjevom 11, naznačen time, da nadalje sadrži topiramat.
20. Spoj izabran iz skupine koju čine: (4-ciklopropil-piperazin-1-il)-(4-morfolin-4-ilmetil-fenil)-metanon, (4-ciklopropil-piperazin-1-il)-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-metanon, (4-ciklopropil-piperazin-1-il)-(4-tiomorfolin-4-ilmetil-fenil)-metanon, te (4-ciklopropil-piperazin-1-il)-[4-(2-hidroksimetil-morfolin-4-ilmetil)-fenil]-metanon, te njihove farmaceutski prihvatljive soli, naznačen time, da se koristi u liječenju pojedinca koji pati od bolesti ili mu je dijagnosticirana bolest izabrana iz skupine koju čine: kognitivni poremećaji, poremećaji spavanja, psihijatrijski poremećaji i ostali poremećaji.
21. Spoj u skladu sa zahtjevom 20, naznačen time, da je bolest izabrana iz skupine koju čine: demencija, Alzheimer-ova bolest, kognitivna disfunkcija, blago kognitivno oštećenje, pre-demencija, hiperaktivni poremećaj s deficitom pozornosti, poremećaji deficita pozornosti te poremećaji učenja i pamćenja.
22. Spoj u skladu sa zahtjevom 21, naznačen time, da je bolest izabrana iz skupine koju čine: smanjena sposobnost učenja, smanjena sposobnost pamćenja i gubitak pamćenja.
23. Spoj u skladu sa zahtjevom 20, naznačen time, da je bolest izabrana iz skupine koju čine: insomnija, poremećeno spavanje, narkolepsija s ili bez pridružene katapleksije, katapleksija, poremećaj homeostaze spavanje/budnost, idiopatska somnolencija, pretjerana dnevna pospanost, poremećaji cirkadijskog ritma, umor, letargija i jet-lag.
24. Spoj u skladu sa zahtjevom 23, naznačen time, da je bolest izabrana iz skupine koju čine: apneja u snu, perimenopauzalni hormonalni pomaci, Parkinsonova bolest, multipla skleroza, depresija, kemoterapija te poremećaj zbog rada u smjenama.
25. Spoj u skladu sa zahtjevom 20, naznačen time, da je bolest izabrana iz skupine koju čine: šizofrenija, bipolarni poremećaji, manični poremećaji, depresija, opsesivno-konvulzivni poremećaj i post-traumatski stresni poremećaj.
26. Spoj u skladu sa zahtjevom 20, naznačen time, da je bolest izabrana iz skupine koju čine: bolest putovanja, vertigo, epilepsija, migrena, neurogena upala, poremećaji hranjenja, debljina i poremećaji zlouporabe supstancija.
27. Spoj u skladu sa zahtjevom 20, naznačen time, da je bolest izabrana iz skupine koju čine: depresija, poremećeno spavanje, umor, letargija, kognitivno oštećenje, smanjena sposobnost pamćenja, gubitak pamćenja, smanjena sposobnost učenja, poremećaji deficita pozornosti i poremećaji hranjenja.
28. Spoj u skladu sa zahtjevom 20, naznačen time, da je bolest izabrana iz skupine koju čine: slabljenje pamćenja zbog dobi, poremećaj REM-ponašanja, benigni posturalni vertigo, tinitus, poremećaji pokreta, sindrom nemirnih nogu, poremećaji povezani s očima, makularna degeneracija i retinitis pigmentosis.
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