HRP20201011T1 - Sukristali (s)-n-metil-8-(1-((2′-metil-[4,5′-biptrimidin]-6-tl)amino)propan-2-tl)kinolin-4-karboksamida i njegovih deuteriranih derivata kao inhibitora dna-pk - Google Patents
Sukristali (s)-n-metil-8-(1-((2′-metil-[4,5′-biptrimidin]-6-tl)amino)propan-2-tl)kinolin-4-karboksamida i njegovih deuteriranih derivata kao inhibitora dna-pk Download PDFInfo
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- HRP20201011T1 HRP20201011T1 HRP20201011TT HRP20201011T HRP20201011T1 HR P20201011 T1 HRP20201011 T1 HR P20201011T1 HR P20201011T T HRP20201011T T HR P20201011TT HR P20201011 T HRP20201011 T HR P20201011T HR P20201011 T1 HRP20201011 T1 HR P20201011T1
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- 239000013078 crystal Substances 0.000 title claims 22
- PEACIOGDEQRHFA-CQSZACIVSA-N n-methyl-8-[(2s)-1-[[6-(2-methylpyrimidin-5-yl)pyrimidin-4-yl]amino]propan-2-yl]quinoline-4-carboxamide Chemical compound C([C@@H](C)C1=C2N=CC=C(C2=CC=C1)C(=O)NC)NC(N=CN=1)=CC=1C1=CN=C(C)N=C1 PEACIOGDEQRHFA-CQSZACIVSA-N 0.000 title claims 3
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 18
- 206010028980 Neoplasm Diseases 0.000 claims 14
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid group Chemical group C(CCCCC(=O)O)(=O)O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 6
- 238000001959 radiotherapy Methods 0.000 claims 5
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 4
- 235000011037 adipic acid Nutrition 0.000 claims 4
- 239000001361 adipic acid Substances 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 4
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- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
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- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 3
- AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-VTZDEGQISA-N 0.000 claims 2
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims 2
- PEACIOGDEQRHFA-KIYKJNLWSA-N 8-[(2s)-1-[[6-(4,6-dideuterio-2-methylpyrimidin-5-yl)pyrimidin-4-yl]amino]propan-2-yl]-n-methylquinoline-4-carboxamide Chemical compound [2H]C1=NC(C)=NC([2H])=C1C1=CC(NC[C@@H](C)C=2C3=NC=CC(=C3C=CC=2)C(=O)NC)=NC=N1 PEACIOGDEQRHFA-KIYKJNLWSA-N 0.000 claims 2
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- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 2
- HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 claims 2
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- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims 2
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- IDLFZVILOHSSID-OVLDLUHVSA-N corticotropin Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@@H](N)CO)C1=CC=C(O)C=C1 IDLFZVILOHSSID-OVLDLUHVSA-N 0.000 claims 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
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Claims (12)
1. Sukristal koji što sadrži spoj formule
[image]
i
sredstvo za stvaranje sukristala,
gdje je sredstvo za stvaranje sukristala adipiska kiselina, gdje je svaki od R1 i R2 neovisno vodik ili deuterij,
naznačen time što je namijenjen upotrebi u potencijaciji terapijskog režima u liječenju raka,
gdje se upotreba sastoji u primjeni na osobi kojoj je to potrebno djelotvorne količine navedenog sukristala, i
gdje je terapijski režim terapija zračenjem.
2. Sukristal namijenjen upotrebi u skladu s patentnim zahtjevom 1, naznačen time što je terapija zračenjem adjuvantna terapija zračenjem.
3. Sukristal namijenjen upotrebi u skladu s patentnim zahtjevom 2, naznačen time što se rak bira između raka dojke, kolorektalnog raka, gastroezofagealnog raka, fibrosarkoma, glioblastoma, hepatocelularnog karcinoma, karcinoma pločastih stanica glave i vrata, melanoma, raka pluća, raka gušterače ili raka prostate.
4. Sukristal namijenjen upotrebi u skladu s patentnih zahtjeva 1 do 3, naznačen time što je molarni omjer između adipiske kiseline i spoja formule I otprilike 1 do 2.
5. Sukristal namijenjen upotrebi u skladu s patentnim zahtjevom 4, naznačen time što je spoj formule I (S)-N-metil-8-(1-((2′-metil-[4,5′-bipirimidin]-6-il)amino)propan-2-il)kinolin-4-karboksamid;
izborno gdje:
(I) spoj ima maksimume difrakcije rendgenskih zraka na prahu kod otprilike 6,46, 7,91, 11,92, 12,26, 12,99, 14,19, 18,68, te 19,07 °2θ; ili
(II) spoj ima maksimum DSC u svom DSC termogramu kod otprilike 195 °C i otprilike 245 °C.
6. Sukristal namijenjen upotrebi u skladu s patentnim zahtjevom 4, naznačen time što je spoj formule I (S)-N-metil-8-(1-((2′-metil-4′,6′-dideutero-[4,5′-bipirimidin]-6-il)amino)propan-2-il)kinolin-4-karboksamid;
izborno gdje:
(I) spoj ima maksimum DSC u svom DSC termogramu kod otprilike 195 °C i otprilike 245 °C; ili
(II) spoj ima maksimume difrakcije rendgenskih zraka na prahu kod otprilike 6,46, 7,91, 11,92, 12,26, 12,99, 14,19, 18,68, te 19,07 °2θ.
7. Sukristal namijenjen upotrebi u skladu s patentnih zahtjeva 1 do 3, naznačen time što
(I) spoj se primijenjuje u farmaceutskom pripravku; ili
(II) sukristal se primijenjuje uz etopozid, doksorubicin, daunorubicin, epirubicin ili bleomicin.
8. Sukristal koji što sadrži spoj formule
[image]
i
sredstvo za stvaranje sukristala,
gdje je sredstvo za stvaranje sukristala adipiska kiselina, gdje je svaki od R1 i R2 neovisno vodik ili deuterij,
naznačen time što je namijenjen upotrebi u liječenju raka,
gdje se upotreba sastoji u primjeni na osobi kojoj je to potrebno terapijski djelotvorne količine navedenog sukristala, i
naznačen time što se rak bira između rasta čvrstih tumora/zloćudnih novotvorina, karcinoma miksoidnih i okruglih stanica, lokalno napredujućih tumora, metastazirajućeg raka, sarkoma ljudskih mekih tkiva, uključujući Ewingov sarkom, metastaza raka, uključujući limfatičke metastaze, karcinoma pločastih stanica, osobito glave i vrata, karcinoma pločastih stanica jednjaka, oralnog karcinoma, zloćudnih novotvorina krvnih stanica, uključujući multipli mijelom, leukemija, uključujući akutnu limfocitnu leukemiju, akutnu nelimfocitnu leukemiju, kroničnu limfocitnu leukemiju, kroničnu mijelocitnu leukemiju, te leukemiju vlasastih stanica, efuzijskih limfoma (limfoma na bazi tjelesnih šupljina), limfoma timusa, raka pluća, uključujući karcinom malih stanica, kutanog limfoma T-stanica, Hodgkinovog limfoma, nehodgkinovskog limfoma, raka kore nadbubrežne žlijezde, tumori koji proizvode ACTH, raka velikih stanica, raka dojke, uključujući karcinom malih stanica i duktalni karcinom, gastrointestinalnog raka, uključujući rak želuca, raka debelog crijeva, kolorektalni rak, polipe povezane s kolorektalnim novotvorinama, rak gušterače, rak jetre, urološkog raka, uključujući rak mokraćnog mjehura, uključujući primarne superficijalne tumore mokraćnog mjehura, invazivni karcinom prijelaznih stanica mokraćnog mjehura, te rak amokraćnog mjehura koji invadira u mišić, rak prostate, zloćudnih novotvorina ženskog genitalnog sustava, uključujući karcinom jajnika, primarne novotvorine peritonejskog epitela, karcinom vrata maternice, rak endometrija maternice, rak vagine, rak vulve, rak maternice i čvrste tumore u folikulu jajnika, zloćudnih novotvorina muškog genitalnog sustava, uključujući rak testisa i rak penisa, raka bubrega, uključujući karcinom bubrežnih stanica, raka na mozgu, uključujući intrinzične tumore mozga, neuroblastom, astrocitne tumore mozga, gliome, invaziju metastatskih tumorskih stanica u središnjem živčanom sustavu, raka kostiju, uključujući osteome i osteosarkom, raka kože, uključujući zloćudni melanom, tumorsku progresiju keratinocita ljudske kože, rak pločastih stanica, raka štitnjače, retinoblastoma, neuroblastoma, peritonealne efuzije, zloćudne pleuralne efuzije, mezotelioma, Wilmsovih tumora, raka žučnog mjehura, trofoblastne novotvorine, hemangiopericitoma, te Kaposijevog sarkoma.
9. Sukristal namijenjen upotrebi u skladu s patentnim zahtjevom 8, naznačen time što je molarni omjer između adipiske kiseline i spoja formule I otprilike 1 do 2.
10. Sukristal namijenjen upotrebi u skladu s patentnim zahtjevom 9, naznačen time što je spoj formule I (S)-N-metil-8-(1-((2′-metil-[4,5′-bipirimidin]-6-il)amino)propan-2-il)kinolin-4-karboksamid;
izborno gdje:
(I) spoj ima maksimume difrakcije rendgenskih zraka na prahu kod otprilike 6,46, 7,91, 11,92, 12,26, 12,99, 14,19, 18,68, te 19,07 °2θ; ili
(II) spoj ima maksimum DSC u svom DSC termogramu kod otprilike 195 °C i otprilike 245 °C.
11. Sukristal namijenjen upotrebi u skladu s patentnim zahtjevom 9, naznačen time što je spoj formule I (S)-N-metil-8-(1-((2′-metil-4′,6′-dideutero-[4,5′-bipirimidin]-6-il)amino)propan-2-il)kinolin-4-karboksamid;
izborno gdje:
(I) spoj ima maksimum DSC u svom DSC termogramu kod otprilike 195 °C i otprilike 245 °C; ili
(II) spoj ima maksimume difrakcije rendgenskih zraka na prahu kod otprilike 6,46, 7,91, 11,92, 12,26, 12,99, 14,19, 18,68, te 19,07 °2θ.
12. Sukristal namijenjen upotrebi u skladu s patentnim zahtjevom 8, naznačen time što
(I) spoj se primijenjuje u farmaceutskom pripravku; ili
(II) sukristal se primijenjuje uz dodatno terapijsko sredstvo, gdje dodatno terapijsko sredstvo uključuje terapija zračenjem ili kemoterapiju, ili i terapiju zračenjem i kemoterapiju; ili
(III) sukristal se primijenjuje uz etopozid, doksorubicin, daunorubicin, epirubicin ili bleomicin.
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HRP20201011TT HRP20201011T1 (hr) | 2013-10-17 | 2020-06-26 | Sukristali (s)-n-metil-8-(1-((2′-metil-[4,5′-biptrimidin]-6-tl)amino)propan-2-tl)kinolin-4-karboksamida i njegovih deuteriranih derivata kao inhibitora dna-pk |
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EP2806874B1 (en) | 2012-01-25 | 2017-11-15 | Neupharma, Inc. | Quinoxaline-oxy-phenyl derivatives as kinase inhibitors |
PT2841428T (pt) | 2012-04-24 | 2018-11-29 | Vertex Pharma | Inibidores de adn-pk |
WO2014075077A1 (en) | 2012-11-12 | 2014-05-15 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
DK3527563T3 (da) | 2013-03-12 | 2021-12-06 | Vertex Pharma | Dna-pk-inhibitorer |
SG11201602962PA (en) * | 2013-10-17 | 2016-05-30 | Vertex Pharma | Co-crystals of (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as dna-pk inhibitors |
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