DK2691384T3 - (alpha-substitueret aralkylamino og heteroarylalkylamino) pyrimidinyl og 1,3,5-triazinyl benzimidazoler, farmaceutiske sammensætninger indeholdende dem, og disse forbindelser til anvendelse i behandling af proliferative sygdomme - Google Patents
(alpha-substitueret aralkylamino og heteroarylalkylamino) pyrimidinyl og 1,3,5-triazinyl benzimidazoler, farmaceutiske sammensætninger indeholdende dem, og disse forbindelser til anvendelse i behandling af proliferative sygdomme Download PDFInfo
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- DK2691384T3 DK2691384T3 DK12711551.7T DK12711551T DK2691384T3 DK 2691384 T3 DK2691384 T3 DK 2691384T3 DK 12711551 T DK12711551 T DK 12711551T DK 2691384 T3 DK2691384 T3 DK 2691384T3
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- certain embodiments
- substituents
- optionally substituted
- nr1br1c
- heterocyclyl
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Claims (12)
- (ALPHA-SUBSTITUERET ARALKYLAMINO OG HETEROARYLALKYLAMINO) PYRIMIDINYL OG 1,3,5-TRIAZINYL BENZIMIDAZOLER, FARMACEUTISKE SAMMENSÆTNINGER INDEHOLDENDE DEM, OG DISSE FORBINDELSER TIL ANVENDELSE I BEHANDLING AF PROLIFERATIVE SYGDOMME1. Forbindelse med formel II:(Π) eller en enantiomer, en blanding af enantiomerer, en blanding af to eller flere diastereomerer, eller en isotopisk variant deraf; eller et farmaceutisk acceptabelt salt, solvat, eller hydrat deraf; hvor: X, Y, og Z hver uafhængigt er N eller CRX, med det forbehold at mindst to af X, Y, og Z er nitrogenatomer; hvor Rx er hydrogen eller Ci-6 alkyl; R1 og R2 hver uafhængigt er (a) hydrogen, cyano, halo, eller nitro; (b) Ci-e alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, eller heterocyklyl; eller (c) -C(0)Rla, -C(0)0Rla, -C(0)NRlbRlc, -C(NRla)NRlbRlc, -ORla, - 0C(0)Rla, -0C(0)0Rla, -0C(0)NRlbRlc, -OC( = NRla)NRlbRlc, -0S(0)Rla, -0S(0)2Rla, - 0S(0)NRlbRlc, -0S(0)2NRlbRlc, -NRlbRlc, -NRlaC(0)Rld, -NRlaC(0)0Rld, - NRlaC(0)NRlbRlc, -NRlaC( = NRld)NRlbRlc, -NRlaS(0)Rld, -NRlaS(0)2Rld, - NRlaS(0)NRlbRlc, -NRlaS(0)2NRlbRlc, -SRla, -S(0)Rla, -S(0)2Rla, -S(0)NRlbRlc, eller -S(0)2NRlbRlc; hvor hver Rla, Rlb, Rlc, og Rld uafhængigt er (i) hydrogen; (ii) Ci-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, Ce-14 aryl, C7-15 aralkyl, heteroaryl, eller heterocyklyl; eller (iii) Rlb og Rlc sammen med det N atom til hvilket de er forbundet danner heterocyklyl; R3 og R4 hver uafhængigt er hydrogen eller Ci-6 alkyl; eller R3 og R4 er koblet til hinanden for at danne en binding, Ci-6 alkylen, Ci-6 heteroalkylen, C2-6 alkenylen, eller C2-6 heteroalkenylen; R5a er hydrogen eller Ci-6 alkyl; R5b er Ci-6 alkyl eller -C(0)0Rla; R5c er -(CR5fR59)n-(C6-i4 aryl) eller -(CR5fR58)n-heteroaryl; R5f og R5g hver uafhængigt er (a) hydrogen eller halo; (b) Ci-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, eller heterocyklyl; eller (c) -C(0)Rla, -C(0)0Rla, -C(0)NRlbRlc, -C(NRla)NRlbRlc, -ORla, -0C(0)Rla, - 0C(0)0Rla, -0C(0)NRlbRlc, -OC( = NRla)NRlbRlc, -0S(0)Rla, -OS(0)2R,a,-OS(O)NRlbRlc, -0S(0)2NRlbRlc, -NRlbRlc, -NRlaC(0)Rld, -NRlaC(0)0Rld, - NRlaC(0)NRlbRlc, -NRlaC( = NRld)NRlbRlc, NRlaS(0)Rld, -NRlaS(0)2Rld,-NRlaS(O)NRlbRlc, -NRlaS(0)2NRlbRlc, -SRla, -S(0)Rla, -S(0)2Rla, -S(0)NRlbRlc; eller -S(0)2NRlbRlc; eller (d) når en forekomst af R5f og en forekomst af R5g er forbundet til det samme carbon atom, da danner R5f og R5g sammen med det carbon atom til hvilket de er forbundet en C3-10 cykloalkyl eller heterocyklyl; R6 er hydrogen, Ci-e alkyl, -S-Ci-e alkyl, -S(0)-Ci-6 alkyl, eller -SO2-C1-6 alkyl; og n er 0, 1, 2, 3, eller 4; hvor hver alkyl, alkylen, heteroalkylen, alkenyl, alkenylen, heteroalkenylen, alkynyl, cykloalkyl, aryl, aralkyl, heteroaryl, og heterocyklyl i R1, R2, R3, R4, R6, Rx, Rla, Rlb, Rlc, Rld, R5a, R5b, R5c, R5f, og R5g eventuelt er substitueret med en eller flere, i en udførselsform, en, to, tre, eller fire, substituenter Q, hvor hver substituent Q uafhængigt er valgt fra (a) oxo, cyano, halo, og nitro; (b) Ci-e alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, og heterocyklyl, hver af hvilke er eventuelt yderligere substitueret med en eller flere, i en udførselsform, en, to, tre eller fire, substituenter Qa; og (c) -C(0)Ra, -C(0)0Ra, -C(0)NRbRc, -C(NRa)NRbRc, -0Ra,-0C(0)Ra, -0C(0)0Ra, -0C(0)NRbRc, - OC( = NRa)NRbRc, -0S(0)Ra, -0S(0)2Ra, - 0S(0)NRbRc, -0S(0)2NRbRc, -NRbRc, -NRaC(0)Rd, NRaC(0)0Rd, -NRaC(0)NRbRc, - NRaC(=NRd)l\IRbRc, -NRaS(0)Rd, NRaS(0)2Rd, -NRaS(0)NRbRc, -NRaS(0)2NRbRc, -SRa, -S(0)Ra, -S(0)2Ra, -S(0)NRbRc, og -S(0)2NRbRc, hvor hver Ra, Rb, Rc, og Rd uafhængigt er (i) hydrogen; (ii) Ci-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, Ce-14 aryl, C7-15 aralkyl, heteroaryl, eller heterocyklyl, hver af hvilke er eventuelt yderligere substitueret med en eller flere, i en udførselsform, en, to, tre, eller fire, substituenter Qa; eller (iii) Rb og Rc sammen med det N atom til hvilket de er forbundet danner heterocyklyl, hvilken er eventuelt yderligere substitueret med en eller flere, i en udførselsform, en, to, tre, eller fire, substituenter Qa; hvor hver Qa uafhængigt er valgt fra gruppen bestående af (a) oxo, cyano, halo, og nitro; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, og heterocyklyl; og (c) -C(0)Re, -C(0)0Re, -C(0)NRfRg, -C(NRe)NRfRVORe, -OC(0)Re, -0C(0)0Re, -0C(0)NRfRg, -OC( = NRe)NRfR9, -0S(0)Re, -0S(0)2Re,-0S(0)NRfR9, -0S(0)2NRfR9, -NRfR9, -NReC(0)Rh, NReC(0)0Rh, -NReC(0)NRfR9,-NReC(=NRh)NRfR9, -NReS(0)Rh, -NReS(0)2Rh, NReS(0)NRfR9, -NReS(0)2NRfR9, -SRe, -S(0)Re, -S(0)2Re, -S(0)NRfR9, og -S(0)2NRfRg; hvor hver Re, Rf, R9, og Rb uafhængigt er (i) hydrogen; (ii) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, Ce-i4 aryl, C7-15 aralkyl, heteroaryl, eller heterocyklyl; eller (iii) Rf og R9 sammen med det N atom til hvilket de er forbundet danner heterocyklyl; og hvor forbindelsen ikke er 6-(2-(difluoromethyl)-lW-benzo[c/]imidazol-l-yl)-/V-(l- (4-((R)-3-(methoxymethyl)morpholino)phenyl)ethyl)-2-morpholinopyrimidin-4- amine.
- 2. Forbindelsen ifølge krav 1, hvor R5b er C1-6 alkyl eller -C(0)0Rla; fortrinsvis hvor R5a og R5b hver er methyl, eventuelt substitueret med en eller flere halo; og/eller hvor n er 1; eller hvor n er 0; og/eller hvor R5f og R5g hver er hydrogen.
- 3. Forbindelsen ifølge krav 1 eller 2, med strukturen med formel Ila: (Ha);eller med strukturen med formel Ilb:eller en isotopisk variant deraf; eller et farmaceutisk acceptabelt salt, solvat, eller hydrat deraf.
- 4. Forbindelsen ifølge et hvilket som helst af kravene 1 til 3, med strukturen med formel VII:eller en enantiomer, en blanding af enantiomerer, en blanding af to eller flere diastereomerer, eller en isotopisk variant deraf; eller et farmaceutisk acceptabelt salt, solvat, eller hydrat deraf; hvor: R7a, R7b, R7c, R7d, og R7e hver uafhængigt er (a) hydrogen, cyano, halo, eller nitro; (b) Ci-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, eller heterocyklyl, hver af hvilke er eventuelt substitueret med en eller flere substituenter Q; eller (c) -C(0)Rla, -C(0)0Rla, -C(0)NRlbRlc, -C(NRla)NRlbRlc, -0Rla, - 0C(0)Rla, -0C(0)0Rla, -0C(0)NRlbRlc, -OC( = NRla)NRlbRlc, -0S(0)Rla, -0S(0)2Rla, - 0S(0)NRlbRlc, -0S(0)2NRlbRlc, -NRlbRlc, -NRlaC(0)Rld, -NRlaC(0)0Rld,--NRlaC(0)NRlbRlc, -NRlaC( = l\IRld)l\IRlbRlc, -NRlaS(0)Rld, NRlaS(0)2Rld, - NRlaS(0)NRlbRlc, -NRlaS(0)2NRlbRlc, -SRla, -S(0)Rla, -S(0)2Rla, -S(0)NRlbRlc, eller -S(0)2NRlbRlc; eller to af R7a, R7b, R7c, R7d, og R7e der er tilstødende til hinanden danner C3-10 cykloalkenyl, C6-14 aryl, heteroaryl, eller heterocyklyl, hver eventuelt substitueret med en eller flere substituenter Q; hvor forbindelsen fortrinsvis har strukturen med formel Vila eller Vllb:
- 5. Forbindelsen ifølge et hvilket som helst af kravene 1 til 3, med strukturen med formel XI:(xi) eller en enantiomer, en blanding af enantiomerer, en blanding af to eller flere diastereomerer, eller en isotopisk variant deraf; eller et farmaceutisk acceptabelt salt, solvat, eller hydrat deraf; hvor: R7a, R7b, R7c, R7d, og R7e hver uafhængigt er (a) hydrogen, cyano, halo, eller nitro; (b) Ci-e alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cykloalkyl, Ce-i4 aryl, C7-15 aralkyl, heteroaryl, eller heterocyklyl, hver af hvilke er eventuelt substitueret med en eller flere substituenter Q; eller (c) -C(0)Rla, -C(0)0Rla, -C(0)NRlbRlc, -C(NRla)NRlbRlc, -ORla, - 0C(0)Rla, -0C(0)0Rla, -0C(0)NRlbRlc, -OC( = NRla)NRlbRlc, -0S(0)Rla, -0S(0)2Rla, - 0S(0)NRlbRlc, -0S(0)2NRlbRlc, -NRlbRlc, -NRlaC(0)Rld, -NRlaC(0)0Rld,--NRlaC(0)NRlbRlc, -NRlaC( = NRld)NRlbRlc, -NRlaS(0)Rld, NRlaS(0)2Rld, - NRlaS(0)NRlbRlc, -NRlaS(0)2NRlbRlc, -SRla, -S(0)Rla, -S(0)2Rla, -S(0)NRlbRlc, eller -S(0)2NRlbRlc; eller to af R7a, R7b, R7c, R7d, og R7e der er tilstødende til hinanden danner C3-10 cykloalkenyl, C6-14 aryl, heteroaryl, eller heterocyklyl, hver eventuelt substitueret med en eller flere substituenter Q; hvor forbindelsen fortrinsvis har strukturen med formel XIa, Xlb, XV, XVa eller XVb:(Xla)
- 6. Forbindelsen ifølge et hvilket som helst af kravene 1 til 5, Hvor R1 er hydrogen; eller hvor R1 er -ORla, fortrinsvis -O-Ci-6 alkyl, mere fortrinsvis methoxy; og/eller hvor R2 er hydrogen; eller hvor R2er -NRlbRlc, fortrinsvis amino; og/eller hvor R3 er hydrogen; og/eller hvor R4 er hydrogen; og/eller hvor R6 er Ci-6 alkyl, eventuelt substitueret med en eller flere substituenter Q, fortrinsvis hvor R6 er methyl, fluoromethyl, difluoromethyl, eller trifluoromethyl, mere fortrinsvis hvor R6 er difluoromethyl.
- 7. Forbindelsen ifølge et hvilket som helst af kravene 1 til 6, hvor X er N; eller hvor X er CRX, fortrinsvis hvor X er CH; og/eller hvor Y er N; eller hvor Y er CRX, fortrinsvis hvorY er CH; og/eller hvor Z er N; eller hvor Z er CRX, fortrinsvis hvor Z er CH; eller hvor X, Y, og Z er N.
- 8. Forbindelsen ifølge krav 1 valgt fra gruppen bestående afA7S Α7β og enantiomerer, blandinger af enantiomerer, blandinger af to eller flere diastereomerer, og isotopiske varianter deraf; og farmaceutisk acceptable salte, solvater, og hydrater deraf.
- 9. Farmaceutisk sammensætning omfattende forbindelsen ifølge et hvilket som helst af kravene 1 til 8, eller en enantiomer, en blanding af enantiomerer, eller en blanding af to eller flere diastereomerer deraf; eller et farmaceutisk acceptabelt salt, solvat, eller hydrat deraf; og en eller flere farmaceutisk acceptable excipienser.
- 10. Den farmaceutiske sammensætning ifølge krav 9, hvor sammensætningen er formuleret til enkeltdosis indgivelse; og/eller hvor sammensætningen er formuleret som en oral, parenteral, eller intravenøs dosisform, fortrinsvis hvor sammensætningen er formuleret som en oral dosisform, eventuelt hvor den orale dosisform er en tablet eller kapsel; og/eller hvor sammensætningen yderligere omfatter et andet terapeutisk middel.
- 11. Forbindelsen ifølge et hvilket som helst af kravene 1 til 8 eller den farmaceutiske sammensætning ifølge krav 9 eller 10 til anvendelse i en fremgangsmåde til behandlingen, forebyggelsen, eller lindringen af et eller flere symptomer af en PI3K-medieret lidelse, sygdom, eller tilstand i en patient, hvor den PI3K-medierede lidelse, sygdom, eller tilstand er en inflammatorisk sygdom eller en proliferativ sygdom.
- 12. Forbindelsen eller sammensætningen til anvendelse ifølge krav 11, hvor PI3K er en vildtype, eller hvor PI3K er en PI3K variant; og/eller hvor PI3K er en klasse I PI3K, såsom pllOy.
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2013
- 2013-09-26 ZA ZA2013/07224A patent/ZA201307224B/en unknown
- 2013-09-29 IL IL228600A patent/IL228600B/en active IP Right Grant
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2015
- 2015-06-03 US US14/729,700 patent/US10064868B2/en active Active
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2016
- 2016-03-10 AU AU2016201558A patent/AU2016201558B2/en active Active
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2018
- 2018-07-19 US US16/040,461 patent/US10335415B2/en active Active
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2019
- 2019-04-19 US US16/389,371 patent/US10603324B2/en active Active
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2020
- 2020-02-13 US US16/789,954 patent/US11400097B2/en active Active
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2022
- 2022-06-21 US US17/845,228 patent/US20220323449A1/en active Pending
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