HRP20170447T1 - Spiro-prstenasti spoj koji sadrži dušik i njegova upotreba u medicini - Google Patents
Spiro-prstenasti spoj koji sadrži dušik i njegova upotreba u medicini Download PDFInfo
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- HRP20170447T1 HRP20170447T1 HRP20170447TT HRP20170447T HRP20170447T1 HR P20170447 T1 HRP20170447 T1 HR P20170447T1 HR P20170447T T HRP20170447T T HR P20170447TT HR P20170447 T HRP20170447 T HR P20170447T HR P20170447 T1 HRP20170447 T1 HR P20170447T1
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- solvate
- pharmaceutically acceptable
- acceptable salt
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- 150000001875 compounds Chemical class 0.000 title claims 58
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 46
- 239000012453 solvate Substances 0.000 claims 46
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 11
- 230000002265 prevention Effects 0.000 claims 10
- 102000015617 Janus Kinases Human genes 0.000 claims 7
- 108010024121 Janus Kinases Proteins 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 230000003449 preventive effect Effects 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 230000001225 therapeutic effect Effects 0.000 claims 5
- 229940122245 Janus kinase inhibitor Drugs 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 206010012438 Dermatitis atopic Diseases 0.000 claims 3
- 102000006503 Janus Kinase 2 Human genes 0.000 claims 3
- 108010019437 Janus Kinase 2 Proteins 0.000 claims 3
- 102000006500 Janus Kinase 3 Human genes 0.000 claims 3
- 108010019421 Janus Kinase 3 Proteins 0.000 claims 3
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 208000026935 allergic disease Diseases 0.000 claims 3
- 201000008937 atopic dermatitis Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000024908 graft versus host disease Diseases 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 206010023332 keratitis Diseases 0.000 claims 3
- 201000010666 keratoconjunctivitis Diseases 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 210000000056 organ Anatomy 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 238000002054 transplantation Methods 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 claims 2
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
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- C07D487/10—Spiro-condensed systems
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- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Claims (52)
1. Spoj sljedeće opće formula [I]:
[image]
,
naznačen time što je Ra isti ili različiti i svaki od njih je:
(1) C1-6 alkil, ili
(2) atom halogena, n1 je cijeli broj, kojeg se bira između 0 do 4,
Rb je isti ili različiti i svaki od njih je:
(1) C1-6 alkil, ili
(2) atom halogena,
n2 je cijeli broj, kojeg se bira između 0 do 4,
m1 je cijeli broj, kojeg se bira između 0 do 3,
m2 je cijeli broj, kojeg se bira između 1 do 4,
Xa = Xb je:
(1) CH=CH,
(2) N=CH, ili
(3) CH=N,
X je:
(1) atom dušika, ili
(2) C-Rd, gdje je Rd atom vodika ili atom halogena,
Rc je skupina koju se bira između sljedećih (1) do (6):
(1) atom vodika,
(2) C1-6 alkil, koji može biti supstituiran s istim ili različitim 1 do 5 supstituenata, koje se bira između sljedećih skupina A,
(3) -C(=O)-Rc1,
(4) -C(=O)-O-Rc2,
(5) -C(=O)-NRc3Rc4
gdje su Rc1, Rc2, Rc3 i Rc4 isti ili različiti i svaki od njih je:
(i) atom vodika, ili
(ii) C1-6 alkil, koji može biti supstituiran s istim ili različitim 1 do 5 supstituenata, koje se bira između sljedećih skupina A, ili
(6) skupina formule:
[image]
,
gdje je Ya skupina koju se bira između sljedećih (i) do (iii):
(i) C1-6 alkilen,
(ii) -C(=O)-, ili
(iii) -C(=O)-O-,
prsten T je:
(i) C6-10 aril,
(ii) C3-10 cikloalkil, ili
(iii) zasićeni monoheterociklil, gdje zasićeni monoheterociklil ima 1 do 4 heteroatoma, koje se bira između atoma dušika, atoma kisika ili atoma sumpora, kao i atome ugljika, a broj atoma koji čine prsten je 3 do 7,
Rc5 je isti ili različiti i svaki od njih je:
(i) cijano, ili
(ii) nitro,
p je cijeli broj, kojeg se bira između 0 do 4,
skupina A je skupina koju čine:
(a) hidroksil,
(b) C1-6 alkoksi,
(c) cijano,
(d) C1-6 alkoksikarbonil,
(e) C1-6 alkilkarboniloksi, i
(f) C2-6 alkeniloksi, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što, u općoj formuli [I],
n1 je cijeli broj, kojeg se bira između 0 do 2,
n2 je cijeli broj, kojeg se bira između 0 do 2,
m1 je cijeli broj, kojeg se bira između 0 do 3,
m2 je cijeli broj, kojeg se bira između 1 do 3,
X je:
(1) atom dušika, ili
(2) C-Rd, gdje je Rd atom halogena,
Rc je skupina koju se bira između sljedećih (1) do (6):
(1) atom vodika,
(2) C1-6 alkil, supstituiran s jednim supstituentom, kojeg se bira između sljedećih skupina A,
(3) -C(=O)-Rc1,
(4) -C(=O)-O-Rc2,
(5) -C(=O)-NRc3Rc4
gdje je Rc1 C1-6 alkil, koji može biti supstituiran s jednim supstituentom, kojeg se bira između sljedećih skupina A,
Rc2 je C1-6 alkil,
Rc3 je C1-6 alkil, koji može biti supstituiran s jednim supstituentom, kojeg se bira između sljedećih skupina A,
Rc4 je
(i) atom vodika, ili
(ii) C1-6 alkil, ili
(6) skupina formule:
[image]
,
gdje je Ya skupina koju se bira između sljedećih (i) do (iii):
(i) C1-6 alkilen,
(ii) -C(=O)-, ili
(iii) -C(=O)-O-,
prsten T je:
(i) fenil,
(ii) C3-6 cikloalkil, ili
(iii) pirolidinil,
Rc5 je
(i) cijano, ili
(ii) nitro,
p je cijeli broj, kojeg se bira između 0 ili 1,
skupina A je skupina koju čine:
(a) hidroksil,
(b) C1-6 alkoksi,
(c) cijano,
(d) C1-6 alkoksikarbonil,
(e) C1-6 alkilkarboniloksi, i
(f) C2-6 alkeniloksi, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
3. Spoj u skladu s bilo kojim od patentnog zahtjeva 1 ili 2, naznačen time što je m1 cijeli broj 0 ili 1, a m2 je cijeli broj 1 ili 2, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
4. Spoj u skladu s patentnim zahtjevom 3, gdje je kombinacija (m1,m2) (1,2), naznačen time što je spoj opće formule [II]:
[image]
,
gdje svaki simbol ima isto značenje kao što je definirano u patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
5. Spoj u skladu s patentnim zahtjevom 3, gdje je kombinacija (m1,m2) (0,2), naznačen time što je spoj opće formule [III]:
[image]
,
gdje svaki simbol ima isto značenje kao što je definirano u patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
6. Spoj u skladu s patentnim zahtjevom 3, gdje je kombinacija (m1,m2) (0,1), naznačen time što je spoj opće formule [IV]:
[image]
,
gdje svaki simbol ima isto značenje kao što je definirano u patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
7. Spoj u skladu s bilo kojim od patentnog zahtjeva 1 ili 2, naznačen time što se kombinaciju (m1,m2) bira između (0,3), (2,1), (2,2) ili (3,2), ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što je Xa = Xb CH=CH, a X je atom dušika, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
9. Spoj u skladu s bilo kojim od patentnog zahtjeva 1 ili 2, naznačen time što je kombinacija (n1,n2) (0,0), ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
10. Spoj u skladu s bilo kojim od patentnog zahtjeva 1 ili 2, naznačen time što je kombinacija (n1,n2) (1,0), ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
11. Spoj u skladu s bilo kojim od patentnog zahtjeva 1 ili 2, naznačen time što je kombinacija (n1,n2) (0,1), ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
12. Spoj u skladu s bilo kojim od patentnog zahtjeva 1 ili 2, naznačen time što je kombinacija (n1,n2) (2,0), ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
13. Spoj u skladu s bilo kojim od patentnog zahtjeva 1 ili 2, naznačen time što je kombinacija (n1,n2) (0,2), ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
14. Spoj u skladu s bilo kojim od patentnog zahtjeva 10 ili 12, naznačen time što je Ra metil ili atom fluora, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 14, naznačen time što je Rc -C(=O)-Rc1, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
16. Spoj u skladu s patentnim zahtjevom 15, naznačen time što je Rc1 C1-6 alkil, supstituiran s jednom hidroksilnom ili skupinom cijano, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
17. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 14, naznačen time što je Rc -C(=O)-NRc3Rc4, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
18. Spoj u skladu s patentnim zahtjevom 17, naznačen time što je Rc3 C1-6 alkil, supstituiran s jednom skupinom cijano, a Rc4 je vodik, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
19. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između sljedećih kemijskih strukturnih formula:
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
20. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između sljedećih kemijskih strukturnih formula:
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
21. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
,
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
22. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
,
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
23. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
,
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
24. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
,
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
25. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
,
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
26. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
,
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
27. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
,
ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
28. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegovu farmaceutski prihvatljivu sol, ili njegov solvat, kao i farmaceutski prihvatljivu podlogu.
29. Inhibitor Janus kinaze, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegovu farmaceutski prihvatljivu sol, ili njegov solvat.
30. Inhibitor Janus kinaze u skladu s patentnim zahtjevom 29, naznačen time što je Janus kinaza Janus kinaza 3.
31. Inhibitor Janus kinaze u skladu s patentnim zahtjevom 29, naznačen time što je Janus kinaza Janus kinaza 2.
32. Terapijsko ili preventivno sredstvo namijenjeno upotrebi u liječenju bolesti koju se bira iz skupine koju čine odbacivanje presađenog organa, reakcija presatka prema domaćinu nakon presađivanja, autoimuna bolest, alergijska bolest i kronična mijeloproliferativna bolest, naznačeno time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegovu farmaceutski prihvatljivu sol, ili njegov solvat.
33. Terapijsko ili preventivno sredstvo namijenjeno upotrebi u liječenju reumatoidnog artritisa, naznačeno time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegova farmaceutski prihvatljiva sol, ili njegov solvat.
34. Terapijsko ili preventivno sredstvo namijenjeno upotrebi u liječenju psorijaze, naznačeno time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegovu farmaceutski prihvatljivu sol, ili njegov solvat.
35. Terapijsko ili preventivno sredstvo namijenjeno upotrebi u liječenju suhog keratokonjunktivitisa, naznačeno time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegovu farmaceutski prihvatljivu sol, ili njegov solvat.
36. Terapijsko ili preventivno sredstvo namijenjeno upotrebi u liječenju atopičnog dermatitisa, naznačeno time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegovu farmaceutski prihvatljivu sol, ili njegov solvat.
37. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegova farmaceutski prihvatljiva sol ili njegov solvat, naznačen time što je namijenjen upotrebi u inhibiranju Janus kinaza.
38. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 37, naznačen time što je Janus kinaza Janus kinaza 3.
39. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 37, naznačen time što je Janus kinaza Janus kinaza 2.
40. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegova farmaceutski prihvatljiva sol ili njegov solvat, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju bolesti koju se bira iz skupine koju čine odbacivanje presađenog organa, reakcija presatka prema domaćinu nakon presađivanja, autoimuna bolest, alergijske bolesti i kronična mijeloproliferativna bolest.
41. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegova farmaceutski prihvatljiva sol ili njegov solvat, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju reumatoidnog artritisa.
42. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegova farmaceutski prihvatljiva sol ili njegov solvat, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju psorijaze.
43. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegova farmaceutski prihvatljiva sol ili njegov solvat, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju suhog keratokonjunktivitisa.
44. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegova farmaceutski prihvatljiva sol ili njegov solvat, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju atopičnog dermatitisa.
45. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegove farmaceutski prihvatljive soli ili njegovog solvata, naznačena time što je spoj namijenjen proizvodnji inhibitora Janus kinaze.
46. Upotreba u skladu s patentnim zahtjevom 45, naznačena time što je Janus kinaza Janus kinaza 3.
47. Upotreba u skladu s patentnim zahtjevom 45, naznačena time što je Janus kinaza Janus kinaza 2.
48. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegove farmaceutski prihvatljive soli ili njegovog solvata, naznačena time što je spoj namijenjen proizvodnji medikamenta za liječenje ili sprječavanje bolesti koju se bira iz skupine koju čine odbacivanje presađenog organa, reakcija presatka prema domaćinu nakon presađivanja, autoimuna bolest, alergijske bolesti i kronična mijeloproliferativna bolest.
49. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegove farmaceutski prihvatljive soli ili njegovog solvata, naznačena time što je spoj namijenjen proizvodnji medikamenta za liječenje ili sprječavanje reumatoidnog artritisa.
50. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegove farmaceutski prihvatljive soli ili njegovog solvata, naznačena time što je spoj namijenjen proizvodnji medikamenta za liječenje ili sprječavanje psorijaze.
51. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegove farmaceutski prihvatljive soli ili njegovog solvata, naznačena time što je spoj namijenjen proizvodnji medikamenta za liječenje ili sprječavanje suhog keratokonjunktivitisa.
52. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 27, ili njegove farmaceutski prihvatljive soli ili njegovog solvata, naznačena time što je spoj namijenjen proizvodnji medikamenta za liječenje ili sprječavanje atopičnog dermatitisa.
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