Claims (18)
1. Spoj formule:
[image]
,
ili njegova farmaceutski prihvatljiva sol,
namijenjen upotrebi u liječenju ili sprječavanju raka, naznačen time što spoj treba upotrijebiti u kombinaciji s imunoterapijom.1. Compound formula:
[image]
,
or a pharmaceutically acceptable salt thereof,
intended for use in the treatment or prevention of cancer, characterized in that the compound is to be used in combination with immunotherapy.
2. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule:
[image]
.2. A compound intended for use in accordance with claim 1, characterized in that it is a compound of the formula:
[image]
.
3. Polimorfni oblik spoja formule:
[image]
,
namijenjen upotrebi u liječenju ili sprječavanju raka, naznačen time što polimorfni oblik treba upotrijebiti u kombinaciji s imunoterapijom; i
gdje polimorfni oblik ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži halo maksimum kod otprilike 14 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 5,6, 7,0, 10,6, 12,7, te 14,6 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 7,0, 7,8, 8,6, 11,9, 13,9 (dvostruki maksimum), 14,2, te 16,0 °2θ, ili
polimorfni oblik je hemisolvat s acetonitrilom koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 7,5, 11,4, 15,6, te 16,6 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 6,8, 9,3, 9,5, 10,5, 13,6, te 15,6 °2θ.3. Polymorphic form of the compound of the formula:
[image]
,
intended for use in the treatment or prevention of cancer, characterized in that the polymorphic form is to be used in combination with immunotherapy; and
wherein the polymorphic form has an X-ray powder diffraction pattern (CuKα) containing a halo maximum at approximately 14 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 5.6, 7.0, 10.6, 12.7, and 14.6 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 7.0, 7.8, 8.6, 11.9, 13.9 (double maximum), 14.2, and 16 ,0 °2θ, or
the polymorphic form is a hemisolvate with acetonitrile that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 7.5, 11.4, 15.6, and 16.6 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 6.8, 9.3, 9.5, 10.5, 13.6, and 15.6 °2θ.
4. Farmaceutski pripravak namijenjen upotrebi u liječenju ili sprječavanju raka, naznačen time što farmaceutski pripravak sadrži:
aktivni sastojak, kojeg čini spoj u skladu s patentnim zahtjevom 1 ili 2 ili polimorfni oblik u skladu s patentnim zahtjevom 3; i
farmaceutski prihvatljivi nosač;
gdje farmaceutski pripravak treba upotrijebiti u kombinaciji s imunoterapijom.4. Pharmaceutical preparation intended for use in the treatment or prevention of cancer, characterized in that the pharmaceutical preparation contains:
the active ingredient, which consists of a compound according to claim 1 or 2 or a polymorphic form according to claim 3; and
a pharmaceutically acceptable carrier;
where the pharmaceutical preparation is to be used in combination with immunotherapy.
5. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 1 ili 2 ili polimorfni oblik namijenjen upotrebi u skladu s patentnim zahtjevom 3 ili farmaceutski pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 4, naznačeni time što je imunoterapija imunoterapija koja cilja na rak, imunoterapija na bazi dendritičkih stanica ili adoptivna imunoterapija T-stanicama.5. A compound intended for use in accordance with claim 1 or 2 or a polymorphic form intended for use in accordance with claim 3 or a pharmaceutical preparation intended for use in accordance with claim 4, characterized in that the immunotherapy is cancer-targeting immunotherapy, based immunotherapy dendritic cells or adoptive T-cell immunotherapy.
6. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 1 ili 2 ili polimorfni oblik namijenjen upotrebi u skladu s patentnim zahtjevom 3 ili farmaceutski pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 4, naznačeni time što imunoterapija je protutijelo koje cilja na rak, kojeg se bira između trastuzumaba, alemtuzumaba, bevacizumaba, cetuksimaba, panitumumaba, ibritumomab tiuksetana, tositumomaba, brentuksimab vedotina, ado-trastuzumab emtansina, te denileukin dititoksa.6. A compound intended for use in accordance with claim 1 or 2 or a polymorphic form intended for use in accordance with claim 3 or a pharmaceutical preparation intended for use in accordance with claim 4, characterized in that the immunotherapy is an antibody that targets cancer, which is selected between trastuzumab, alemtuzumab, bevacizumab, cetuximab, panitumumab, ibritumomab tiuxetan, tositumomab, brentuximab vedotin, ado-trastuzumab emtansine, and denileukin dititox.
7. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 6 ili polimorfni oblik namijenjen upotrebi u skladu s patentnim zahtjevom 6 ili farmaceutski pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 6, naznačeni time što je rak karcinom, sarkom, limfom, leukemia, melanom, mezoteliom, multipli mijelom ili seminom.7. A compound intended for use in accordance with patent claim 6 or a polymorphic form intended for use in accordance with patent claim 6 or a pharmaceutical preparation intended for use in accordance with patent claim 6, characterized in that the cancer is carcinoma, sarcoma, lymphoma, leukemia, melanoma, mesothelioma , multiple myeloma or seminoma.
8. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 7 ili polimorfni oblik namijenjen upotrebi u skladu s patentnim zahtjevom 7 ili farmaceutski pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 7, naznačeni time što je rak melanom.8. A compound intended for use in accordance with patent claim 7 or a polymorphic form intended for use in accordance with patent claim 7 or a pharmaceutical preparation intended for use in accordance with patent claim 7, characterized in that the cancer is melanoma.
9. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 6 ili polimorfni oblik namijenjen upotrebi u skladu s patentnim zahtjevom 6 ili farmaceutski pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 6, naznačeni time što je rak rak mokraćnog mjehura, krvi, kostiju, na mozgu, dojke, središnjeg živčanog sustava, vrata maternice, kolona, endometrija, jajnika, žučnog mjehura, genitalija, genitourinarnog sustava, glave, bubrega, grkljana, jetre, pluća, mišićnog tkiva, vrata, sluznice usta ili nosa, jajnika, gušterače, prostate, kože, slezene, tankog crijeva, debelog crijeva, želuca, testisa ili štitnjače.9. A compound intended for use in accordance with patent claim 6 or a polymorphic form intended for use in accordance with patent claim 6 or a pharmaceutical preparation intended for use in accordance with patent claim 6, characterized in that the cancer is bladder, blood, bone, brain cancer, breast, central nervous system, cervix, colon, endometrium, ovary, gall bladder, genitalia, genitourinary system, head, kidney, larynx, liver, lung, muscle tissue, neck, mucous membrane of the mouth or nose, ovary, pancreas, prostate, skin , spleen, small intestine, large intestine, stomach, testes or thyroid gland.
10. Spoj formule:
[image]
,
ili njegova farmaceutski prihvatljiva sol,
naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju stanja povezanog s oksidativnim stresom uzrokovanim mitohondrijskom disfunkcijom.10. Compound formula:
[image]
,
or a pharmaceutically acceptable salt thereof,
characterized in that it is intended for use in the treatment or prevention of a condition associated with oxidative stress caused by mitochondrial dysfunction.
11. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 10, naznačen time što je spoj formule:
[image]
.11. A compound intended for use in accordance with claim 10, characterized in that it is a compound of the formula:
[image]
.
12. Polimorfni oblik spoja formule:
[image]
,
namijenjen upotrebi u liječenju ili sprječavanju stanja povezanog s oksidativnim stresom uzrokovanim mitohondrijskom disfunkcijom;
gdje polimorfni oblik ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži halo maksimum kod otprilike 14 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 5,6, 7,0, 10,6, 12,7, te 14,6 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 7,0, 7,8, 8,6, 11,9, 13,9 (dvostruki maksimum), 14,2, te 16,0 °2θ, ili
polimorfni oblik je hemisolvat s acetonitrilom koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 7,5, 11,4, 15,6, te 16,6 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 6,8, 9,3, 9,5, 10,5, 13,6, te 15,6 °2θ.12. Polymorphic form of the compound of the formula:
[image]
,
intended for use in the treatment or prevention of a condition associated with oxidative stress caused by mitochondrial dysfunction;
wherein the polymorphic form has an X-ray powder diffraction pattern (CuKα) containing a halo maximum at approximately 14 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 5.6, 7.0, 10.6, 12.7, and 14.6 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 7.0, 7.8, 8.6, 11.9, 13.9 (double maximum), 14.2, and 16 ,0 °2θ, or
the polymorphic form is a hemisolvate with acetonitrile that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 7.5, 11.4, 15.6, and 16.6 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 6.8, 9.3, 9.5, 10.5, 13.6, and 15.6 °2θ.
13. Farmaceutski pripravak namijenjen upotrebi u liječenju ili sprječavanju stanja povezanog s oksidativnim stresom uzrokovanim mitohondrijskom disfunkcijom, naznačen time što farmaceutski pripravak sadrži:
aktivni sastojak, kojeg čini spoj u skladu s patentnim zahtjevom 10 ili 11 ili polimorfni oblik u skladu s patentnim zahtjevom 12; i
farmaceutski prihvatljivi nosač.13. A pharmaceutical preparation intended for use in the treatment or prevention of a condition associated with oxidative stress caused by mitochondrial dysfunction, characterized in that the pharmaceutical preparation contains:
the active ingredient, which consists of a compound according to patent claim 10 or 11 or a polymorphic form according to patent claim 12; and
a pharmaceutically acceptable carrier.
14. Spoj formule:
[image]
,
ili njegova farmaceutski prihvatljiva sol,
naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju konvulzivnog poremećaja.14. Compound formula:
[image]
,
or a pharmaceutically acceptable salt thereof,
indicated that it is intended for use in the treatment or prevention of a convulsive disorder.
15. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 14, naznačen time što je spoj formule:
[image]
.15. A compound intended for use in accordance with claim 14, characterized in that it is a compound of the formula:
[image]
.
16. Polimorfni oblik spoja formule:
[image]
,
naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju konvulzivnog poremećaja;
gdje polimorfni oblik ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži halo maksimum kod otprilike 14 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 5,6, 7,0, 10,6, 12,7, te 14,6 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 7,0, 7,8, 8,6, 11,9, 13,9 (dvostruki maksimum), 14,2, te 16,0 °2θ, ili
polimorfni oblik je hemisolvat s acetonitrilom koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 7,5, 11,4, 15,6, te 16,6 °2θ, ili
polimorfni oblik je solvat koji ima uzorak difrakcije rendgenskih zraka na prahu (CuKα) koji sadrži maksimume kod otprilike 6,8, 9,3, 9,5, 10,5, 13,6, te 15,6 °2θ.16. Polymorphic form of the compound of the formula:
[image]
,
indicated that it is intended for use in the treatment or prevention of a convulsive disorder;
wherein the polymorphic form has an X-ray powder diffraction pattern (CuKα) containing a halo maximum at approximately 14 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 5.6, 7.0, 10.6, 12.7, and 14.6 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 7.0, 7.8, 8.6, 11.9, 13.9 (double maximum), 14.2, and 16 ,0 °2θ, or
the polymorphic form is a hemisolvate with acetonitrile that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 7.5, 11.4, 15.6, and 16.6 °2θ, or
the polymorphic form is a solvate that has an X-ray powder diffraction pattern (CuKα) containing maxima at approximately 6.8, 9.3, 9.5, 10.5, 13.6, and 15.6 °2θ.
17. Farmaceutski pripravak namijenjen upotrebi u liječenju ili sprječavanju konvulzivnog poremećaja, naznačen time što farmaceutski pripravak sadrži:
aktivni sastojak, kojeg čini spoj u skladu s patentnim zahtjevom 14 ili 15 ili polimorfni oblik u skladu s patentnim zahtjevom 16; i
farmaceutski prihvatljivi nosač.17. A pharmaceutical preparation intended for use in the treatment or prevention of a convulsive disorder, characterized in that the pharmaceutical preparation contains:
the active ingredient, which consists of a compound according to patent claim 14 or 15 or a polymorphic form according to patent claim 16; and
a pharmaceutically acceptable carrier.
18. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 14 ili 15 ili polimorfni oblik namijenjen upotrebi u skladu s patentnim zahtjevom 16 ili farmaceutski pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 17, naznačen time što je konvulzivni poremećaj epilepsija.18. A compound intended for use in accordance with claim 14 or 15 or a polymorphic form intended for use in accordance with claim 16 or a pharmaceutical preparation intended for use in accordance with claim 17, characterized in that the convulsive disorder is epilepsy.