HRP20220595T1 - Prstenasti eterski derivati pirazolo[1,5-a]pirimidin-3-karboksamida - Google Patents

Prstenasti eterski derivati pirazolo[1,5-a]pirimidin-3-karboksamida Download PDF

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HRP20220595T1
HRP20220595T1 HRP20220595TT HRP20220595T HRP20220595T1 HR P20220595 T1 HRP20220595 T1 HR P20220595T1 HR P20220595T T HRP20220595T T HR P20220595TT HR P20220595 T HRP20220595 T HR P20220595T HR P20220595 T1 HRP20220595 T1 HR P20220595T1
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Christoph Hoenke
Barbara Bertani
Marco Ferrara
Giacomo FOSSATI
Sara Frattini
Riccardo Giovannini
Scott Hobson
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Boehringer Ingelheim International Gmbh
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Claims (47)

1. Spoj, naznačen time, da je predstavljen formulom (I) [image] pri čemu A se bira iz skupine Aa koju čine [image] pri čemu su gore navedene skupine supstituirane s jednim R5 i s jednim R6; R1 se bira iz skupine R1a koju čine halogen, C1-3-alkil- i C3-6-cikloalkil-, pri čemu gore navedene skupine C1-3-alkil-, i C3-6-cikloalkil- mogu biti opcionalno supstituirane s 1 do 5 supstituenata koje se neovisno bira iz skupine koju čine halogen, NC- i HO-; R2 se bira iz skupine R2a koju čine aril i heteroaril, pri čemu gore navedene skupine aril- i heteroaril- mogu biti opcionalno supstituirane s 1 do 5 supstituenata R4; R3 se bira iz skupine R3a koju čine H- i C1-3-alkil-, pri čemu gore navedena skupina C1-3-alkil- može biti opcionalno supstituirana s 1 do 7 supstituenata koje se međusobno neovisno bira iz skupine koju čini halogen; R4 se međusobno neovisno bira iz skupine R4a koju čine halogen, NC-, HO-, C1-4-alkil- i C1-3-alkil-O-, pri čemu gore navedene skupine C1-4-alkil- i C1-3-alkil-O- mogu biti opcionalno supstituirane s 1 do 5 supstituenata koje se neovisno bira iz skupine koju čine HO- i F-; R5 se bira iz skupine R5a koju čine H-, halogen, NC-, HO- i C1-3-alkil-, pri čemu gore navedena skupina C1-3-alkil- može biti opcionalno supstituirana s 1 do 5 supstituenata koje se neovisno bira iz skupine koju čine HO- i F- ili R5 i R6 zajedno tvore skupinu O=; R6 se bira iz skupine R6a koju čine H-, halogen, NC-, HO- i C1-3-alkil-, pri čemu gore navedena skupina C1-3-alkil- može biti opcionalno supstituirana s 1 do 5 supstituenata koje se neovisno bira iz skupine koju čine HO- i F- ili R5 i R6 zajedno tvore skupinu O=; ili njegova sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da A se bira iz skupine Ab koju čine [image] pri čemu su gore navedene skupine supstituirane s jednim R5 i s jednim R6. ili njegova sol.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da A se bira iz skupine Ac koju čine [image] ili njegova sol.
4. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 3, naznačen time, da R1 se bira iz skupine R1b koju čine F-, Cl-, C1-3-alkil- i C3-6-cikloalkil-, pri čemu gore navedene skupine C1-3-alkil- i C3-6-cikloalkil- mogu biti opcionalno supstituirane s 1 do 3 supstituenta koje se neovisno bira iz skupine koju čini F-, ili njegova sol.
5. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 3, naznačen time, da R1 se bira iz skupine R1c koju čine F-, H3C- i ciklopropil-, ili njegova sol.
6. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 5, naznačen time, da R2 se bira iz skupine R2b koju čine kinolinil, fenil i piridinil, pri čemu gore navedeni kinolin i skupine fenil- i piridil- mogu biti opcionalno supstituirani s 1 do 5 supstituenata R4, ili njegova sol.
7. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 5, naznačen time, da R2 se bira iz skupine R2c koju čine fenil i piridil, pri čemu gore navedene skupine fenil- i piridil- mogu biti opcionalno supstituirane s 1 do 2 supstituenata R4, ili njegova sol.
8. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 7, naznačen time, da R3 se bira iz skupine R3b koju čine H-, H3C-, F3C-, F2HC-, FH2C- i F3C-, ili njegova sol.
9. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 8, naznačen time, da R4 se međusobno neovisno bira iz skupine R4b koju čine halogen, C1-4-alkil- i C1-3-alkil-O-, pri čemu gore navedene skupine C1-4-alkil- i C1-3-alkil-O- mogu biti opcionalno supstituirane s 1 do 5 supstituenata koje se neovisno bira iz skupine koju čine HO-, i F-, ili njegova sol.
10. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 9, naznačen time, da R5 se bira iz skupine R5b koju čine H-, HO- i C1-2-alkil-, pri čemu gore navedena skupina C1-2-alkil- može biti opcionalno supstituirana s 1 do 5 F-, ili R5 i R6 zajedno tvore skupinu O=, ili njegova sol.
11. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 10, naznačen time, da R6 se bira iz skupine R6b koju čine H- i C1-2-alkil-, pri čemu gore navedena skupina C1-2-alkil- može biti opcionalno supstituirana s 1 do 5 F-, ili R5/R6 zajedno tvore skupinu O=, ili njegova sol.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da se bira iz skupine koju čine [image] [image] [image] [image] [image] [image] [image]
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
15. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
16. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
17. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
18. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
19. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
20. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
21. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
22. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
23. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
24. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
25. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
26. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
27. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
28. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
29. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
30. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
31. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
32. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
33. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
34. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
35. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
36. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
37. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
38. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
39. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
40. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
41. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
42. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom: [image]
43. Farmaceutski prihvatljiva sol, naznačena time, da je od bilo kojeg od spojeva u skladu s patentnim zahtjevima 1 do 42.
44. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 42, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je namijenjen uporabi kao medikament.
45. Farmaceutski pripravci, naznačeni time, da sadrže najmanje jedan spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 42, ili njegovu farmaceutski prihvatljivu sol, zajedno s jednim ili više farmaceutski prihvatljivih nosača.
46. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 42, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 45, naznačen time, da je namijenjen uporabi u sprečavanju ili liječenju (1) poremećaja koji sadrže simptom kognitivne deficijencije; (2) organskih, uključujući simptomatskih, mentalnih poremećaja, demencije; (3) mentalne zaostalosti; (4) poremećaja raspoloženja (afektivnih poremećaja); (5) neurotskih, poremećaja povezanih sa stresom i somatoformnih poremećaja, uključujući anksiozne poremećaje; (6) poremećaja ponašanja i emocija, koji obično počinju u djetinjstvu i adolescenciji, sindroma hiperaktivnosti uz nedostatak pažnje (ADHD) i poremećaja autističnog spektra; (7) poremećaja psihološkog razvoja, razvojnih poremećaja vještina učenja; (8) shizofrenije i drugih psihotičnih poremećaja; (9) poremećaja osobnosti i ponašanja kod odraslih osoba; (10) mentalnih i poremećaja ponašanja uzrokovanih uporabom psihoaktivnih tvari; (11) ekstrapiramidalnih i poremećaja kretanja; (12) epizodnih i paroksizmalnih poremećaja, epilepsije; (13) sistemnih atrofija koje primarno utječu na središnji živčani sustav, ataksiju; (14) bihevioralnih sindroma povezanih s fiziološkim poremećajima i fizičkim čimbenicima; (15) spolne disfunkcije koju čini prekomjerni spolni nagon; (16) činjeničnih poremećaja; (17) liječenju, ublažavanju i/ili sprečavanju kognitivnog poremećaja povezanog s percepcijom, koncentracijom, spoznajom, učenjem ili pamćenjem; (18) liječenju, ublažavanju i/ili sprečavanju kognitivnog poremećaja povezanog s poremećajima učenja i pamćenja uzrokovanim starenjem; (19) gubitka pamćenja uzrokovanog starenjem; (20) vaskularne demencije; (21) kraniocerebralne traume; (22) inzulta; (23) demencije do koje dolazi nakon inzulta (postinzultne demencije); (24) posttraumatske demencije; (25) općih poremećaja koncentracije; (26) poremećaja koncentracije kod djece koja imaju probleme s učenjem i pamćenjem; (27) Alzheimerove bolesti; (28) demencije s Lewyjevim tjelešcima; (29) demencije s degeneracijom čeonih režnjeva; uključujući Pickov sindrom; (30) Parkinsonove bolesti; (31) progresivne nuklearne paralize; (32) demencije s kortikobazalnom degeneracijom; (33) amiotrofne lateralne skleroze (ALS); (34) Huntingtonove bolesti; (35) multiple skleroze; (36) degeneracije talamusa; (37) Creutzfeld-Jacobove demencije; (38) demencije uzrokovane HIV-om; (38) shizofrenije s demencijom ili Korsakovljeve psihoze; (39) poremećaja spavanja; (40) bipolarnog poremećaja; (41) metaboličkog sindroma; (42) pretilosti; (43) dijabetesa melitusa; (44) hiperglikemije; (45) dislipidemije; (46) poremećenog podnošenja glukoze; (47) bolesti testisa, mozga, tankog crijeva, skeletnih mišića, srca, pluća, prsne žlijezde ili slezene; (48) bolnih poremećaja; (49) neuropsihijatrijskih simptoma (primjerice depresivnih simptoma kod Alzheimerove bolesti); (50) mješovite demencije; (51) kognitivnog poremećaja kod shizoafektivnog poremećaja; (52) kognitivnog poremećaja kod bipolarnog poremećaja; (53) kognitivnog poremećaja kod velikog depresivnog poremećaja i (54) kognitivnog poremećaja povezanog s shizofrenijom; (55) simptomatskom liječenju Alzheimerove bolesti; (56) simptomatskom liječenju prodromalne i blage do umjerene Alzheimerove bolesti; (57) kognitivnog poremećaja kod Huntingtonove bolesti; (58) kognitivnog poremećaja kod poremećaja autističnog spektra; (59) kognitivnog poremećaja kod Parkinsonove bolesti; (60) kognitivnog poremećaja nakon inzulta (postinzultne demencije); (61) kognitivnog poremećaja kod vaskularne demencije.
47. Spoj u skladu s bilo kojim od jednog ili više patentnih zahtjeva 1 do 42, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 45, koji je namijenjen uporabi u skladu s patentnim zahtjevom 46, naznačen time, da se spoj primjenjuje uz druge aktivne tvari namijenjene liječenju ili sprečavanju bolesti i stanja u skladu s patentnim zahtjevom 46.
HRP20220595TT 2015-10-13 2016-10-12 Prstenasti eterski derivati pirazolo[1,5-a]pirimidin-3-karboksamida HRP20220595T1 (hr)

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