SI2911699T1 - Modificirano protitelo, protitelo-konjugat in proces za njihovo pripravo - Google Patents
Modificirano protitelo, protitelo-konjugat in proces za njihovo pripravo Download PDFInfo
- Publication number
- SI2911699T1 SI2911699T1 SI201330948T SI201330948T SI2911699T1 SI 2911699 T1 SI2911699 T1 SI 2911699T1 SI 201330948 T SI201330948 T SI 201330948T SI 201330948 T SI201330948 T SI 201330948T SI 2911699 T1 SI2911699 T1 SI 2911699T1
- Authority
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- Slovenia
- Prior art keywords
- antibody
- group
- glcnac
- hetero
- conjugate
- Prior art date
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- 238000000034 method Methods 0.000 title claims abstract 14
- 229940127121 immunoconjugate Drugs 0.000 title claims abstract 13
- OVRNDRQMDRJTHS-UHFFFAOYSA-N N-acelyl-D-glucosamine Natural products CC(=O)NC1C(O)OC(CO)C(O)C1O OVRNDRQMDRJTHS-UHFFFAOYSA-N 0.000 claims abstract 22
- MBLBDJOUHNCFQT-LXGUWJNJSA-N N-acetylglucosamine Natural products CC(=O)N[C@@H](C=O)[C@@H](O)[C@H](O)[C@H](O)CO MBLBDJOUHNCFQT-LXGUWJNJSA-N 0.000 claims abstract 22
- OVRNDRQMDRJTHS-FMDGEEDCSA-N N-acetyl-beta-D-glucosamine Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-FMDGEEDCSA-N 0.000 claims abstract 19
- 229950006780 n-acetylglucosamine Drugs 0.000 claims abstract 15
- 125000001424 substituent group Chemical group 0.000 claims abstract 15
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims abstract 6
- 125000000524 functional group Chemical group 0.000 claims abstract 5
- 125000000304 alkynyl group Chemical group 0.000 claims abstract 4
- 125000000468 ketone group Chemical group 0.000 claims abstract 3
- 239000003814 drug Substances 0.000 claims abstract 2
- 125000005842 heteroatom Chemical group 0.000 claims 19
- 239000000562 conjugate Substances 0.000 claims 13
- OVRNDRQMDRJTHS-RTRLPJTCSA-N N-acetyl-D-glucosamine Chemical compound CC(=O)N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-RTRLPJTCSA-N 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- 239000003054 catalyst Substances 0.000 claims 8
- ZWIADYZPOWUWEW-XVFCMESISA-N CDP Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](COP(O)(=O)OP(O)(O)=O)O1 ZWIADYZPOWUWEW-XVFCMESISA-N 0.000 claims 6
- QGWNDRXFNXRZMB-UUOKFMHZSA-N GDP Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O QGWNDRXFNXRZMB-UUOKFMHZSA-N 0.000 claims 6
- XCCTYIAWTASOJW-XVFCMESISA-N Uridine-5'-Diphosphate Chemical compound O[C@@H]1[C@H](O)[C@@H](COP(O)(=O)OP(O)(O)=O)O[C@H]1N1C(=O)NC(=O)C=C1 XCCTYIAWTASOJW-XVFCMESISA-N 0.000 claims 6
- QGWNDRXFNXRZMB-UHFFFAOYSA-N guanidine diphosphate Natural products C1=2NC(N)=NC(=O)C=2N=CN1C1OC(COP(O)(=O)OP(O)(O)=O)C(O)C1O QGWNDRXFNXRZMB-UHFFFAOYSA-N 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000006686 (C1-C24) alkyl group Chemical group 0.000 claims 4
- SHZGCJCMOBCMKK-UHFFFAOYSA-N D-mannomethylose Natural products CC1OC(O)C(O)C(O)C1O SHZGCJCMOBCMKK-UHFFFAOYSA-N 0.000 claims 4
- SHZGCJCMOBCMKK-DHVFOXMCSA-N L-fucopyranose Chemical compound C[C@@H]1OC(O)[C@@H](O)[C@H](O)[C@@H]1O SHZGCJCMOBCMKK-DHVFOXMCSA-N 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 230000003197 catalytic effect Effects 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 102000030902 Galactosyltransferase Human genes 0.000 claims 3
- 108060003306 Galactosyltransferase Proteins 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- -1 -OR5 Chemical group 0.000 claims 2
- PNNNRSAQSRJVSB-SLPGGIOYSA-N Fucose Natural products C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C=O PNNNRSAQSRJVSB-SLPGGIOYSA-N 0.000 claims 2
- 102000005744 Glycoside Hydrolases Human genes 0.000 claims 2
- 108010031186 Glycoside Hydrolases Proteins 0.000 claims 2
- 150000001540 azides Chemical class 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000017891 HER2 positive breast carcinoma Diseases 0.000 claims 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 1
- PNNNRSAQSRJVSB-UHFFFAOYSA-N L-rhamnose Natural products CC(O)C(O)C(O)C(O)C=O PNNNRSAQSRJVSB-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 229940125644 antibody drug Drugs 0.000 claims 1
- 239000000611 antibody drug conjugate Substances 0.000 claims 1
- 229940049595 antibody-drug conjugate Drugs 0.000 claims 1
- 229960001230 asparagine Drugs 0.000 claims 1
- 235000009582 asparagine Nutrition 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 150000004676 glycans Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 claims 1
- 150000003141 primary amines Chemical group 0.000 claims 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 1
Classifications
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- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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Claims (14)
- MODIFICIRANO PROTITELO, PROTITELO-KONJUGAT IN PROCES ZA NJIHOVO PRIPRAVO PATENTNI ZAHTEVKI1. Proces za pripravo protitelesa-konjugata, ki obsega reagiranje modificiranega protitelesa z linker-konjugatom, kjer omenjeni linker-konjugat obsega (hetero) cikloalkinilno skupino in eno ali več molekul, ki nas zanimajo pri čemer je omenjeno modificirano protitelo je protitelo, ki vsebuje GlcNAc-S(A)x substituent, kjer je GlcNAc N-acetilglukozamin, kjer je S(A)X sladkorni derivat, ki obsega x funkcionalne skupine A, kjer je A azido skupina in x je 1, 2, 3 ali 4, kjer je omenjeni GlcNAc-S(A)x substituent vezan na protitelo preko C1 N-acetilglukozamina omenjenega GlcNAc-S(A)x substituenta in kjer je navedeni GlcNAc po izbiri fukoziliran.
- 2. Proces po zahtevku 1, ki obsega stopnje: (i) kontaktiranje protitelesa, ki vsebuje jedro N-acetilglukozamin (GlcNAc) substituent s spojino s formulo S(A)x-P v prisotnosti katalizatorja, kjer je omenjeni jedrni N-acetilglukozaminski substituent po izbiri fukoziliran, kjer navedeni katalizator obsega mutantno katalitsko domeno iz galaktoziltransferaze, pri čemer je S(A)X derivat sladkorja, ki vsebuje x funkcionalne skupine A, kjer je A azido skupina in je x 1, 2, 3 ali 4, kjer je P izbran iz skupine, ki jo sestavljajo uridin difosfat (UDP), gvanozin difosfat (GDP) in citidin difosfat (CDP), da dobimo modificirano protitelo, kjer je modificirano protitelo definirano kot protitelo, ki obsega GlcNAc-S(A)x substituent, vezan na protitelo preko C1 N-acetilglukozamina omenjenega GlcNAc-S(A)xsubstituenta, in kjer je navedeno modificirano protitelo po formuli (4):pri čemer S(A)X in x sta, kot je definirano zgoraj; AB predstavlja protitelo; GlcNAc je N-acetilglukozamin; Fucjefukoza; b je 0 ali 1; in y je 1 do 20; in (ii) reagiranje omenjenega modificiranega protitelesa z linker-konjugatom, kjer omenjeni linker-konjugat obsega (hetero)cikloalkinil skupino in eno ali več molekul, ki nas zanimajo.
- 3. Proces po zahtevku 1 ali 2, kjer je katalizator katalizator, ki obsega mutantno katalitično domeno iz /3(1,4)-galaktoziltransferaze, prednostno izbrano iz skupine, ki jo sestavljajo GalT Y289L, GalT Υ289Ν, GalT Υ289Ι, GalT Y289F, GalT Υ289Μ, GalT Y289V, GalT Y289G, GalT Υ289Ι in GalT Υ289Α.
- 4. Proces po katerem koli od zahtevkov 1-3, kjer ima omenjeni linker-konjugat formulo (11) ali (11b):pri čemer L je linker; D je molekula, ki nas zanima; rje 1 - 20; R1 je neodvisno izbran iz skupine, ki jo sestavljajo vodik, halogen, -OR5, -N02, -CN, -S(0)2R5, Ci - C24 alkilne skupine, C6-C24 (hetero) aril skupine, C7-C24 alkil(hetero)aril skupine in C7-C24 (hetero)arilalkil skupine in pri čemer so alkilne skupine, (hetero)aril skupine, alkil (hetero)aril skupine in (hetero)arilalkil skupine po izbiri substituirane, pri čemer sta lahko dva substituenta R1 povezana skupaj, da tvorita aneliran cikloalkil ali aneliran (hetero)aren substituent in kjer je R5 neodvisno izbran iz skupine, katero sestavljajo vodik, halogen, CrC24 alkilne skupine, C6-C24 (hetero)arilne skupine, C7-C24 alkil(hetero) arilne skupine in C7-C24 (hetero)arilalkilne skupine; X je C (R1)2, O, S ali NR2, kjer je R2 R1 ali L(D)r, in kjer so L, D in r, kot je definirano zgoraj; q je 0 ali 1, s pridržkom, da če je q 0, potem je X N-L(D)r; a je 0,1, 2, 3, 4, 5, 6, 7 ali 8; a'je 0,1, 2, 3, 4, 5, 6, 7 ali 8; in a+a’ < 10.
- 5. Proces po katerem koli od zahtevkov 1-4, kjer ima omenjeni linker-konjugat formulo (17):pri čemer R1, L, D in r, so kot je definirano v zahtevku 4; Y je O, S ali NR2, kjer je R2, kot je definirano v zahtevku 4; R3 je neodvisno izbran iz skupine, ki jo sestavljajo vodik, halogen, C1-C24 alkilne skupine, C6-C24 (hetero)aril skupine, C7-C24 alkil(hetero)aril skupine in C7-C24 (hetero)arilalkil skupine; R4 je izbran iz skupine, ki jo sestavljajo vodik, Y-L(D)r, -(CH2)n-Y-L(D)r, halogen, C1-C24 alkilne skupine, C6-C24 (hetero)aril skupine, C7-C24 alkil(hetero)aril skupine in C7-C24 (hetero)arilalkil skupine, alkil skupine, ki so po izbiri prekinjene z enim od večih heteroatomov, izbranih iz skupine, ki jo sestavljajo O, N in S, kjer so alkilne skupine, (hetero)arilne skupine, alkil(hetero)aril skupine in (hetero)arilalkilne skupine neodvisno po izbiri substituirane; in n je 1, 2, 3, 4, 5, 6, 7, 8, 9 ali 10, ali kjer ima omenjeni linker-konjugat formulo (15) ali formulo (19):kjer so L, D in r, kot je definirano v zahtevku 4.
- 6. Protitelo-konjugat po formuli (20) ali (20b):pri čemer L, D, X, R1, a, a', r in q so, kot je definirano v zahtevku 5; b je 0 ali 1; p je 0 ali 1; Q je -N(H)C(0)CH2- ali -CH2-; x je 1, 2, 3 ali 4; y je 1-20; in kjer je AB protitelo, S je sladkor ali derivat sladkorja, GlcNAc je N-acetilglukozamin in Fuc je fukoza.
- 7. Protitelo-konjugat po zahtevku 8, kjer je protitelo-konjugat s formulo (21):kjer so AB, L, D, S, Q, x, y, b, p, R1 in GlcNAc, kot je definirano v zahtevku 6, in kjer so R3, R4, Y, n in r, kot je definirano v zahtevku 4 ali kjer je protitelo konjugat s formulo (15b) ali s formulo (22):kjer so AB, L, D, S, x, y, b, p, Q in GlcNAc, kot so definirani v zahtevku 6:
- 8. Protitelo-konjugat po katerem koli od zahtevkov 6 - 7, kjer je omenjena molekula (D) izbrana iz skupine, ki jo sestavljajo snov, ki je biološko in/ali farmacevtsko aktivna, reporter molekula, azid in (hetero)cikloalkinil skupina.
- 9. Protitelo-konjugat, ki ga lahko dobimo s postopkom po katerem koli od zahtevkov 1-5.
- 10. Protitelo-konjugat po katerem koli od zahtevkov 6 - 9 za uporabo kot zdravilo.
- 11. Protitelo-konjugat po katerem koli od zahtevkov 6 - 9 za uporabo pri zdravljenju raka, prednostno raka dojke, bolj prednostno HER2 pozitiven rak dojke.
- 12. Proces za pripravo protitelo-zdravilo konjugata, ki obsega korake: (i) kontaktiranje protitelesa, ki vsebuje jedrni N-acetilglukozamin (GlcNAc) substituent s spojino s formulo S(A)x-P v prisotnosti katalizatorja, kjer je omenjeni jedrni N-acetilglukozaminski substituent po izbiri fukoziliran, kjer navedeni katalizator obsega mutantno katalitsko domeno iz galaktoziltransferaze, pri čemer je S(A)X derivat sladkorja, ki obsega x funkcionalne skupine A, kjer je A neodvisno izbran iz skupine ki sestoji iz azido skupine, keto skupine in alkinilne skupine in je x 1, 2, 3 ali 4, kjer je P izbran iz skupine, ki jo sestavljajo uridin difosfat (UDP), gvanozin difosfat (GDP) in citidin difosfat (CDP), da dobimo modificirano protitelo, kjer je modificirano protitelo definirano kot protitelo, ki obsega GlcNAc-S(A)x substituent, vezan na protitelo preko C1 N-acetilglukozamina omenjenega substituenta GlcNAc-S(A)x, in kjer je navedeno modificirano protitelo po formuli (4):pri čemer sta S(A)X in x, kot je definirano zgoraj; AB predstavlja protitelo; GlcNAc je N-acetilglukozamin; Fuc je fukoza; b je 0 ali 1; in y je 1 do 20; in (ii) reagiranje omenjenega modificiranega protitelesa s linker- konjugatom, kjer: (a) kadar je navedeno modificirano protitelo azid modificirano protitelo, omenjeni linker- konjugat obsega(hetero)cikloalkinil skupino ali alkinilno skupino in eno ali več molekul, ki nas zanimajo; ali (b) kadar je navedeno modificirano protitelo keto modificirano protitelo, omenjeni linker-konjugat obsega primarno aminsko skupino, aminooksi skupino ali hidrazinilno skupino in eno ali več molekul, ki nas zanimajo; ali (c) kadar je navedeno modificirano protitelo alkin-modificirano protitelo, omenjeni linker-konjugat obsega azido skupino in eno ali več molekul, ki nas zanimajo, kjer je molekula, ki nas zanima (D) konjugirana s protitelesom prek linkerja (L); kjer je omenjena molekula, ki nas zanima snov, ki je biološko in/ali farmacevtsko aktivna.
- 13. Protitelo-zdravilo konjugat, ki ga lahko dobimo s postopkom po zahtevku 12.
- 14. Proces za pripravo modificiranega protitelesa, pri čemer postopek obsega: (a) deglikozilacijo glikana protitelesa, ki ima jedrni N-acetilglukozamin, v prisotnosti endoglikozidaze, da dobimo protitelo, ki obsega jedrni N-acetilglukozamin substituent, pri čemer je omenjeni jedrni N-acetilglukozamin substituent po izbiri fukoziliran, pri čemer je omenjeni jedrni N-acetilglukozamin substituent vezan preko N-glikozidne vezi z atomom amidnega dušika v stranski verigi asparaginske aminokisline protitelesa in kjer je omenjena endoglikozidaza Endo S, Endo S49, Endo F ali njihova kombinacija; sledi (b) kontaktiranje omenjenega protitelesa s spojino s formulo S(A)X-P v prisotnosti katalizatorja, pri čemer omenjeni katalizator obsega mutantno katalitično domeno iz galaktoziltransferaze, pri čemer je S(A)X derivat sladkorja ki obsega x funkcionalne skupine A, kjer je A neodvisno izbran iz skupine, ki jo sestavljajo azido skupina, keto skupina in alkinilna skupina in je x 1, 2, 3 ali 4, kjer je P izbran iz skupine, ki jo sestavljajo ofuridin difosfat (UDP), gvanozin difosfat (GDP) in citidin difosfat (CDP), kjer je modificirano protitelo definirano kot protitelo, ki obsega GlcNAc-S(A)x substituent, vezan na protitelo preko C1 N-acetilglukozamina omenjenega GlcNAc-S(A)x substituenta.
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