HRP20200368T1 - Hibridni imunoglobulin koji sadrži nepeptidilnu vezu - Google Patents
Hibridni imunoglobulin koji sadrži nepeptidilnu vezu Download PDFInfo
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- HRP20200368T1 HRP20200368T1 HRP20200368TT HRP20200368T HRP20200368T1 HR P20200368 T1 HRP20200368 T1 HR P20200368T1 HR P20200368T T HRP20200368T T HR P20200368TT HR P20200368 T HRP20200368 T HR P20200368T HR P20200368 T1 HRP20200368 T1 HR P20200368T1
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- 108060003951 Immunoglobulin Proteins 0.000 title 1
- 102000018358 immunoglobulin Human genes 0.000 title 1
- 125000001151 peptidyl group Chemical group 0.000 title 1
- 150000001413 amino acids Chemical class 0.000 claims 45
- 235000001014 amino acid Nutrition 0.000 claims 43
- -1 poly(lactic acid) Polymers 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 22
- 239000000126 substance Substances 0.000 claims 17
- 108090000765 processed proteins & peptides Proteins 0.000 claims 15
- 229920001184 polypeptide Polymers 0.000 claims 14
- 102000004196 processed proteins & peptides Human genes 0.000 claims 14
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 12
- KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical compound O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims 11
- URYYVOIYTNXXBN-UPHRSURJSA-N cyclooctene Chemical compound C1CCC\C=C/CC1 URYYVOIYTNXXBN-UPHRSURJSA-N 0.000 claims 10
- 239000004913 cyclooctene Substances 0.000 claims 10
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 10
- 235000018417 cysteine Nutrition 0.000 claims 10
- CIISBYKBBMFLEZ-UHFFFAOYSA-N 1,2-oxazolidine Chemical compound C1CNOC1 CIISBYKBBMFLEZ-UHFFFAOYSA-N 0.000 claims 9
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 9
- 150000003852 triazoles Chemical class 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- FDKWRPBBCBCIGA-REOHCLBHSA-N (2r)-2-azaniumyl-3-$l^{1}-selanylpropanoate Chemical compound [Se]C[C@H](N)C(O)=O FDKWRPBBCBCIGA-REOHCLBHSA-N 0.000 claims 7
- BKWQKVJYXODDAC-UHFFFAOYSA-N 1,2-dihydropyridazine Chemical compound N1NC=CC=C1 BKWQKVJYXODDAC-UHFFFAOYSA-N 0.000 claims 7
- FDKWRPBBCBCIGA-UWTATZPHSA-N D-Selenocysteine Natural products [Se]C[C@@H](N)C(O)=O FDKWRPBBCBCIGA-UWTATZPHSA-N 0.000 claims 7
- 125000001721 carboxyacetyl group Chemical group 0.000 claims 7
- WJTCGQSWYFHTAC-UHFFFAOYSA-N cyclooctane Chemical compound C1CCCCCCC1 WJTCGQSWYFHTAC-UHFFFAOYSA-N 0.000 claims 7
- 239000004914 cyclooctane Substances 0.000 claims 7
- ZKZBPNGNEQAJSX-UHFFFAOYSA-N selenocysteine Natural products [SeH]CC(N)C(O)=O ZKZBPNGNEQAJSX-UHFFFAOYSA-N 0.000 claims 7
- 235000016491 selenocysteine Nutrition 0.000 claims 7
- 229940055619 selenocysteine Drugs 0.000 claims 7
- 125000004080 3-carboxypropanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C(O[H])=O 0.000 claims 6
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- 150000005215 alkyl ethers Chemical class 0.000 claims 5
- 150000001412 amines Chemical class 0.000 claims 5
- 150000004676 glycans Chemical class 0.000 claims 5
- 125000003651 hexanedioyl group Chemical group C(CCCCC(=O)*)(=O)* 0.000 claims 5
- 125000001557 phthalyl group Chemical group C(=O)(O)C1=C(C(=O)*)C=CC=C1 0.000 claims 5
- 229920000747 poly(lactic acid) Polymers 0.000 claims 5
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- 229920005862 polyol Polymers 0.000 claims 5
- 150000003077 polyols Chemical class 0.000 claims 5
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- 229960002317 succinimide Drugs 0.000 claims 5
- 229920002554 vinyl polymer Polymers 0.000 claims 5
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical group NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 4
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- 125000004442 acylamino group Chemical group 0.000 claims 4
- 150000001336 alkenes Chemical class 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
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- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 229920001282 polysaccharide Polymers 0.000 claims 4
- 239000005017 polysaccharide Substances 0.000 claims 4
- 235000018102 proteins Nutrition 0.000 claims 4
- 102000004169 proteins and genes Human genes 0.000 claims 4
- 108090000623 proteins and genes Proteins 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 3
- 102000004127 Cytokines Human genes 0.000 claims 3
- 108090000695 Cytokines Proteins 0.000 claims 3
- 102400000326 Glucagon-like peptide 2 Human genes 0.000 claims 3
- 101800000221 Glucagon-like peptide 2 Proteins 0.000 claims 3
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 3
- 239000004472 Lysine Substances 0.000 claims 3
- 125000004423 acyloxy group Chemical group 0.000 claims 3
- 150000001924 cycloalkanes Chemical class 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
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- TWSALRJGPBVBQU-PKQQPRCHSA-N glucagon-like peptide 2 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(O)=O)[C@@H](C)CC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=CC=C1 TWSALRJGPBVBQU-PKQQPRCHSA-N 0.000 claims 3
- 239000000833 heterodimer Substances 0.000 claims 3
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- 150000003335 secondary amines Chemical class 0.000 claims 3
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- 101800001890 Atrial natriuretic peptide Proteins 0.000 claims 2
- 108010022152 Corticotropin-Releasing Hormone Proteins 0.000 claims 2
- 102000012289 Corticotropin-Releasing Hormone Human genes 0.000 claims 2
- 239000000055 Corticotropin-Releasing Hormone Substances 0.000 claims 2
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- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 2
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 2
- NDAUXUAQIAJITI-UHFFFAOYSA-N albuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- NSQLIUXCMFBZME-MPVJKSABSA-N carperitide Chemical compound C([C@H]1C(=O)NCC(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(O)=O)=O)[C@@H](C)CC)C1=CC=CC=C1 NSQLIUXCMFBZME-MPVJKSABSA-N 0.000 claims 2
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- 229940041967 corticotropin-releasing hormone Drugs 0.000 claims 2
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- BWPIARFWQZKAIA-UHFFFAOYSA-N protriptyline Chemical compound C1=CC2=CC=CC=C2C(CCCNC)C2=CC=CC=C21 BWPIARFWQZKAIA-UHFFFAOYSA-N 0.000 claims 1
- 229960003908 pseudoephedrine Drugs 0.000 claims 1
- KWGRBVOPPLSCSI-WCBMZHEXSA-N pseudoephedrine Chemical compound CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WCBMZHEXSA-N 0.000 claims 1
- 239000003368 psychostimulant agent Substances 0.000 claims 1
- RUOKEQAAGRXIBM-GFCCVEGCSA-N rasagiline Chemical compound C1=CC=C2[C@H](NCC#C)CCC2=C1 RUOKEQAAGRXIBM-GFCCVEGCSA-N 0.000 claims 1
- CBQGYUDMJHNJBX-RTBURBONSA-N reboxetine Chemical compound CCOC1=CC=CC=C1O[C@H](C=1C=CC=CC=1)[C@@H]1OCCNC1 CBQGYUDMJHNJBX-RTBURBONSA-N 0.000 claims 1
- 229960003770 reboxetine Drugs 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 229960002720 reproterol Drugs 0.000 claims 1
- WVLAAKXASPCBGT-UHFFFAOYSA-N reproterol Chemical compound C1=2C(=O)N(C)C(=O)N(C)C=2N=CN1CCCNCC(O)C1=CC(O)=CC(O)=C1 WVLAAKXASPCBGT-UHFFFAOYSA-N 0.000 claims 1
- 230000000241 respiratory effect Effects 0.000 claims 1
- 229960001457 rimiterol Drugs 0.000 claims 1
- IYMMESGOJVNCKV-SKDRFNHKSA-N rimiterol Chemical compound C([C@@H]1[C@@H](O)C=2C=C(O)C(O)=CC=2)CCCN1 IYMMESGOJVNCKV-SKDRFNHKSA-N 0.000 claims 1
- 229960001634 ritodrine Drugs 0.000 claims 1
- IOVGROKTTNBUGK-SJCJKPOMSA-N ritodrine Chemical compound N([C@@H](C)[C@H](O)C=1C=CC(O)=CC=1)CCC1=CC=C(O)C=C1 IOVGROKTTNBUGK-SJCJKPOMSA-N 0.000 claims 1
- NEMGRZFTLSKBAP-LBPRGKRZSA-N safinamide Chemical compound C1=CC(CN[C@@H](C)C(N)=O)=CC=C1OCC1=CC=CC(F)=C1 NEMGRZFTLSKBAP-LBPRGKRZSA-N 0.000 claims 1
- 229950002652 safinamide Drugs 0.000 claims 1
- 229960004017 salmeterol Drugs 0.000 claims 1
- HKFMQJUJWSFOLY-OAQYLSRUSA-N sarizotan Chemical compound C1=CC(F)=CC=C1C1=CN=CC(CNC[C@@H]2OC3=CC=CC=C3CC2)=C1 HKFMQJUJWSFOLY-OAQYLSRUSA-N 0.000 claims 1
- 229950007903 sarizotan Drugs 0.000 claims 1
- 229960002101 secretin Drugs 0.000 claims 1
- OWMZNFCDEHGFEP-NFBCVYDUSA-N secretin human Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(N)=O)[C@@H](C)O)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)C1=CC=CC=C1 OWMZNFCDEHGFEP-NFBCVYDUSA-N 0.000 claims 1
- 229960002073 sertraline Drugs 0.000 claims 1
- VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 claims 1
- 229960004953 silodosin Drugs 0.000 claims 1
- PNCPYILNMDWPEY-QGZVFWFLSA-N silodosin Chemical compound N([C@@H](CC=1C=C(C=2N(CCCO)CCC=2C=1)C(N)=O)C)CCOC1=CC=CC=C1OCC(F)(F)F PNCPYILNMDWPEY-QGZVFWFLSA-N 0.000 claims 1
- 229960002370 sotalol Drugs 0.000 claims 1
- ZBMZVLHSJCTVON-UHFFFAOYSA-N sotalol Chemical compound CC(C)NCC(O)C1=CC=C(NS(C)(=O)=O)C=C1 ZBMZVLHSJCTVON-UHFFFAOYSA-N 0.000 claims 1
- 229950010289 soterenol Drugs 0.000 claims 1
- 229960004954 sparfloxacin Drugs 0.000 claims 1
- DZZWHBIBMUVIIW-DTORHVGOSA-N sparfloxacin Chemical compound C1[C@@H](C)N[C@@H](C)CN1C1=C(F)C(N)=C2C(=O)C(C(O)=O)=CN(C3CC3)C2=C1F DZZWHBIBMUVIIW-DTORHVGOSA-N 0.000 claims 1
- 229960002909 spirapril Drugs 0.000 claims 1
- HRWCVUIFMSZDJS-SZMVWBNQSA-N spirapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2(C1)SCCS2)C(O)=O)CC1=CC=CC=C1 HRWCVUIFMSZDJS-SZMVWBNQSA-N 0.000 claims 1
- 108700035424 spirapril Proteins 0.000 claims 1
- PAQZZCOZHPGCFW-UHFFFAOYSA-N sulfinalol Chemical compound C1=CC(OC)=CC=C1CCC(C)NCC(O)C1=CC=C(O)C(S(C)=O)=C1 PAQZZCOZHPGCFW-UHFFFAOYSA-N 0.000 claims 1
- 229950005165 sulfinalol Drugs 0.000 claims 1
- 229960002613 tamsulosin Drugs 0.000 claims 1
- MKTAGSRKQIGEBH-SSDOTTSWSA-N tebanicline Chemical compound C1=NC(Cl)=CC=C1OC[C@@H]1NCC1 MKTAGSRKQIGEBH-SSDOTTSWSA-N 0.000 claims 1
- 229950005834 tebanicline Drugs 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 229960005138 tianeptine Drugs 0.000 claims 1
- COKMIXFXJJXBQG-NRFANRHFSA-N tirofiban Chemical compound C1=CC(C[C@H](NS(=O)(=O)CCCC)C(O)=O)=CC=C1OCCCCC1CCNCC1 COKMIXFXJJXBQG-NRFANRHFSA-N 0.000 claims 1
- 229960003425 tirofiban Drugs 0.000 claims 1
- 229960005204 tretoquinol Drugs 0.000 claims 1
- RGVPOXRFEPSFGH-AWEZNQCLSA-N tretoquinol Chemical compound COC1=C(OC)C(OC)=CC(C[C@H]2C3=CC(O)=C(O)C=C3CCN2)=C1 RGVPOXRFEPSFGH-AWEZNQCLSA-N 0.000 claims 1
- 229960001177 trimetazidine Drugs 0.000 claims 1
- 229960001341 troxipide Drugs 0.000 claims 1
- JQSHBVHOMNKWFT-DTORHVGOSA-N varenicline Chemical compound C12=CC3=NC=CN=C3C=C2[C@H]2C[C@@H]1CNC2 JQSHBVHOMNKWFT-DTORHVGOSA-N 0.000 claims 1
- 229960004751 varenicline Drugs 0.000 claims 1
- SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 claims 1
- 229960001254 vildagliptin Drugs 0.000 claims 1
- 229960001255 viloxazine Drugs 0.000 claims 1
- 229960004928 xamoterol Drugs 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
- A61K47/6855—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6875—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody being a hybrid immunoglobulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/24—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
- C07K16/241—Tumor Necrosis Factors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/46—Hybrid immunoglobulins
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
- C07K2317/21—Immunoglobulins specific features characterized by taxonomic origin from primates, e.g. man
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
- C07K2317/52—Constant or Fc region; Isotype
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
- C07K2317/55—Fab or Fab'
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
- C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding
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- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicinal Preparation (AREA)
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Claims (16)
1. Spoj naznačen time, da ima strukturu:
A — B - - - - - Z
gdje je A biološki aktivna struktura spoja;
gdje je Z proteinska komponenta spoja, koja proteinska komponenta sadrži jedan ili više polipeptida, kod čega barem jedan od jednog ili više polipeptida obuhvaća aminokiseline u slijedu koje (i) koje su identične s odsječkom aminokiselina u slijedu prisutnih u lancu Fc domene antitijela; (ii) koje se vežu na Fc receptor; i (iii) imaju na svom N-terminusu cistein ili selenocistein; gdje je B kemijska struktura koja veže A i Z;
u čemu crtkana linija između B i Z predstavlja peptidilnu vezu između N-terminalnog cisteina ili selenocisteina polipeptida od Z i aminokiselinskog ostatka ili organskog kiselinskog ostatka od B; i u čemu puna linija između A i B predstavlja nepeptidilnu vezu koja sadrži strukturu:
[image]
u čemu Xa jest kemijska struktura koja sadrži ciklooktan kondenziran na dihidropiridazin; u čemu Ra predstavlja organsku strukturu koja se veže na jedno od A ili B, a Rb predstavlja organsku strukturu koja se veže na drugo od A ili B.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da je Ra vezan na ciklooktan, a Rb je vezan na dihidropiridazin.
3. Spoj prema patentnom zahtjevu 1 ili 2, naznačen time, da Xaima strukturu:
[image]
u čemu Rajest H, alkil ili aril;
ili njihov tautomer.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 - 3, naznačen time, da puna linija između A i B predstavlja nepeptidilnu vezu koja obuhvaća strukturu:
[image]
u čemu Rc jest H, alkil ili aril;
ili njihov tautomer.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 - 4,naznačen time, da su Ra i Rb nezavisno jedan od drugoga, organska struktura koja sadrži ili se sastoji od lanca od 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 ili više jedinica, gdje je svaka jedinica nezavisno izabrana iz skupine koja se sastoji od [PEG(y)]z, polialkilenglikola, polioksialkiliranog poliola, polivinilalkohola, polivinilalkiletera, poli(mliječne kiseline), poli(mliječne-glikolne kiseline), polisaharida, razgrananog ostatka C1-C10 alkila, C3-C10cikloalkana, C2-C10 alkena, C5-C10 cikloalkena, amina, sumpora, kisika, sukcinimida, maleimida, glicerola, triazola, izoksazolidina, C2-C5acila, C2-C5 acilamino, C2-C5aciloksi, sukcinila, malonila, glutarila, ftalila, adipoila, aminokiseline, arilne skupine, heteroarilne skupine, karbamata, kemijske strukture koja sadrži ciklooktan kondenziran na dihidropiridazin, kemijske strukture koja sadrži ciklookten kondenziran na triazol, kemijske strukture koja sadrži ciklookten kondenziran na izoksazolidin, dibenzociklooktena, dibenzoazaciklooktena,
[image]
[image]
i
[image]
i u čemu X1 jest CH ili N, X2 jest CH2ili karbonilna skupina, a R5 jest arilna ili alkilna skupina;
kod čega [PEG(y)] z jest:
[image]
u čemu Y=1-100, a Z=1-10.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 - 5, naznačen time, da Ra ili Rb
i) jest privješen na A preko veze ugljik-dušik ili veze ugljik–sumpor;
ii) jest privješen na A preko veze ugljik-dušik;
iii) jest privješen na A preko veze ugljik-dušik, u čemu veza ugljik-dušik jest amidna veza;
iv) jest privješen na A preko biološki labilne veze;
v) jest privješen na A preko amidne veze između C-terminus aminokiseline od A i amino skupine u B;
vi) jest privješen na A preko amidne veze između C-terminus aminokiseline od A i amino skupine u B, u čemu terminus aminokiseline jest cistein;
vii) jest privješen na A preko veze ugljik-sumpor;
viii) jest privješen na A preko veze ugljik-sumpor stvorene između Ra ili Rbi slobodnog tiola;
ix) sadrži razgranani ostatak; ili
x) jest pričvršćen na više od jednog A preko razgrananog ostatka.
7. Spoj prema bilo kojem od patentnih zahtjeva 1 - 6, naznačen time, da A
i) sadrži strukturu spoja koji je lijek, odobren za liječenje pacijenta pogođenog bolešću;
ii) sadrži strukturu organskog spoja koji ima molekulsku masu manju od 1000 daltona, DNA aptamer, RNA aptamer, oligonukleotid, ili protein koji je biološki aktivan;
iii) sadrži primarni ili sekundarni amin;
iv) jest vezan na B preko primarnog ili sekundarnog amina;
v) jest aripiprazol ili oseltamivir;
vi sadrži sekundarni amin;
vii) jest respiratorni lijek, antiasmatik, analgetik, antidepresiv, antianginozni lijek, antiaritmik, antihipertenziv, antidijabetik, antihistaminik, antiinfektiv, antibiotik, antiinflamatorni agens, antiparkinsonik, antipsihotik, antipiretik, antiulkusni agens, lijek za poremećaj pozornosti s hiperaktivnošću (ADHD), stimulans središnjeg živčanog sustava, dekongestiv, ili psihostimulans;
viii) jest alprenolol, acebutolol, amidefrin, amineptin, amosulalol, amoksapin, amfetaminil, atenolol, atomoksetin, balofloksacin, bametan, befunolol, benazepril, benfluoreks, benzoktamin, betahistin, betaksolol, bevantolol, bifemelan, bisoprolol, brinzolamid, bufeniod, butetamin, kamilofin, karazolol, kartikain, karvedilol, kefalin, ciprofloksacin, klozapin, clobenzorex, klorprenalin, ciklopentamin, delapril, demeksiptilin, denopamin, dezipramin, desloratadin, dicklofenak, dimetofrin, dioksadrol, dobutamin, dopeksamin, doripenem, dorzolamid, droprenilamin, duloksetin, eltoprazin, enalapril, enoksacin, epinefhrin, ertapenem, esaprazol, esmolol, etoksadrol, fasudil, fendilin, fenetilin, fenfluramin, fenoldopam, fenoterol, fenproporeks, flecamid, fluoksetin, formoterol, frovatriptan, gaboksadol, garenoksacin, gatifloksacin, grepafloksacin, heksoprenalin, imidapril, indalpin, indecainid, indeloksazin hidroklorid, izokssuprin, isproniclin, labetalol, landiolol, lapatinib, levofacetoperan, lizinopril, lomefloksacin, lotrafiban, maprotilin, mecamilamin, meflokine, mepindolol, meropenem, metapramin, metaproterenol, metoksifenamin, dekstrorotari metilfenidat, metifenidat, metipranolol, metoprolol, mitoksantron, mivazerol, moeksipril, moprolol, moksifloksacin, nebivolol, nifenalol, nipradilol, norfloksacin, nortriptilin, nilidrin, olanzapin, oksamnikin, oksprenolol, oksifedrin, paroksetin, perheksilin, fenmetrazin, fenilefrin, fenilpropilmetilamin, foledrin, picilorex, pimetilin, pindolol, pipemidična kiselina, piridokain, praktolol, pradofloksacin, pramipeksol, pramiverin, prenalterol, prenilamin, prilocaln, prokaterol, pronetalol, propafenon, propranolol, propilheksedrin, protokilol, protriptilin, pseudoefedrin, reboksetin, rasagilin, (r)-rasagilin, repinotan, reproterol, rimiterol, ritodrin, safinamid, salbutamol/albuterol, salmeterol, sarizotan, sertralin, silodosin, sotalol, soterenol, sparfloksacin, spirapril, sulfinalol, sinefrin, tamsulozin, tebaniclin, tianeptin, tirofiban, tretokuinol, trimetazidin, troksipid, vareniklin, vildagliptin, viloksazin, vikuidil ili ksamoterol;
ix) sadrži protein koji je biološki aktivan;
x) sadrži sekretorni protein;
xi) sadrži izvanstaničnu domenu proteina
xii) je biološki aktivan tako da ima ciljnovezujuću aktivnost;
xiii) jest nezavisno preklapajući protein ili njegov dio;
xiv) jest glikosilirani protein;
xv) sadrži unutarlančane disulfidne veze;
xvi) veže citokin;
xvii) veže se na citokin, kada citokin jest TNFα;
xviii) sadrži atrijski natriuretski peptid (ANP), kalcitonin, kortikotropin oslobađajući hormon (CRH), endotelin, eksenatid, želučani inhibicijski peptid (GIP), glukagonu sličan peptid-1 (GLP-1), glukagonu sličan peptid-2 (GLP-2), analog od GLP-1 ili GLP-2, glukagon vazoaktivni intestinalni peptid (GVIP), grelin, peptid YY
ili sekretin, ili njegov dio;
xix) sadrži barem jedan odsječak aminokiselina u slijedu u sekvenci HGEGTFTSDVSSYLEEQAAKEFIAWLVKGRG;
xx) sadrži barem jedan odsječak aminokiselina u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u teškom lancu od Fab ili od Fab’ od antitijela;
xxi) sadrži barem jedan odsječak aminokiselina u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u laganom lancu od Fab ili od Fab’ od antitijela;
xxii) sadrži barem jedan Fab ili Fab’ od antitijela, ili dio od barem jednog Fab ili Fab’;
xxiii) adrži Fab-1 ili Fab’1, ili njihov dio od antitijela;
xxiv) sadrži Fab-2 ili Fab’2, ili njihov dio od antitijela;
xxv) sadrži dvije ruke od Fab ili Fab’ od antitijela;
xxvi) sadrži barem jedan odsječak aminokiselina u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u jednolančanom antitijelu; ili
xxvii) sadrži barem jedan odsječak aminokiselina u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u TNFα receptoru.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 - 7,naznačen time, da Ra ili Rb
i) jest organska struktura koja sadrži [PEG(y)]z skupinu;
ii) jest organska struktura koja sadrži polialkilenglikol, polioksialkilirani poliol, polivinilalkohol, polivinilalkileter, poli(mliječnu kiselinu), poli(mliječnu-glikolnu kiselinu) ili polisaharidnu skupinu;
iii) jest organska struktura koja sadrži C1-C4 alkilnu skupinu;
iv jest organska struktura koja sadrži sukcinimid;
v) jest organska struktura koja sadrži amin;
vi) jest organska struktura koja sadrži sukcinil, malonil, glutaril, ftalil ili adipoil;
vii) jest organska struktura koja sadrži malonil;
viii) jest organska struktura koja sadrži aminokiselinu;
ix) jest organska struktura koja sadrži cistein;
x) jest organska struktura koja sadrži lizin;
xi) jest organska struktura koja se sastoji od lanca od tri jedinice, izabrane iz skupine koja se sastoji od [PEG(y)]z, polialkilenglikola, polioksialkiliranog poliola, polivinilalkohola, polivinilalkiletera, poli(mliječne kiseline), poli(mliječne-glikolne kiseline), polisaharida, razgrananog ostatka, C1-C10alkila, C3-C10 cikloalkana, C2-C10 alkena, C5-C10 cikloalkena, amina, sumpora, kisika, sukcinimida, maleimida, glicerola, triazola, izoksazolidina, C2-C5 acila, C2-C5 acilamino, C2-C5 aciloksi, sukcinila, malonila, glutarila, ftalila, adipoila, aminokiseline, arilne skupine, heteroarilne skupine, karbamata, kemijske strukture koja sadrži ciklooktan kondenziran na dihidropiridazin, kemijske strukture koja sadrži ciklookten kondenziran na triazol, kemijske strukture koja sadrži ciklookten kondenziran na izoksazolidin, dibenzociklooktena, dibenzoazaciklooktena,
[image]
[image]
[image]
i
[image]
xii) jest organska struktura koja se sastoji od lanca od četiri jedinice odabrane iz skupine koja se sastoji od [PEG(y)]z, polialkilenglikola, polioksialkiliranog poliola, polivinilalkohola, polivinilalkiletera, poli(mliječne kiseline), poli(mliječne-glikolne kiseline), polisaharida, razgrananog ostatka, C1-C10 alkila, C3-C10 cikloalkana, C2-C10 alkena, C5-C10 cikloalkena, amina, sumpora, kisika, sukcinimida, maleimida, glicerola, triazola, izoksazolidina, C2-C5 acila, C2-C5 acilamino, C2-C5 aciloksi, sukcinila, malonila, glutarila, ftalila, adipoila, aminokiseline, arilne skupine, heteroarilne skupine, karbamata, kemijske strukture koja sadrži ciklooktan kondenziran na dihidropiridazin, kemijske strukture koja sadrži ciklookten kondenziran na triazol, kemijske strukture koja sadrži ciklookten kondenziran na izoksazolidin, dibenzociklooktena, dibenzoazaciklooktena,
[image]
[image]
i
[image]
xiii) jest organska struktura koja se sastoji od lanca od pet jedinica izabranih iz skupine koja se sastoji od [PEG(y)]z, polialkilenglikola, polioksialkiliranog poliola, polivinilalkohola, polivinilalkiletera, poli(mliječne kiseline), poli(mliječne-glikolne kiseline), polisaharida, razgrananog ostatka, C1- C10 alkila, C3- C10 cikloalkana, C2- C10 alkena, C5- C10 cikloalkena, amina, sumpora, kisika, sukcinimida, maleimida, glicerola, triazola, izoksazolidina, C2- C5 acila, C2- C5 acilamino, C2- C5 aciloksi, sukcinila, malonila, glutarila, ftalila, adipoila, aminokiseline, arilne skupine, heteroarilne skupine, karbamata, kemijske strukture koja sadrži ciklooktan kondenziran na dihidropiridazin, kemijske strukture koja sadrži ciklookten kondenziran na triazol, kemijske strukture koja sadrži ciklookten kondenziran na izoksazolidin, dibenzociklooktena, dibenzoazaciklooktena,
[image]
[image]
i
[image]
xiv) sadrži [PEG(y)]z iz skupine vezane na lizin;
xv) sadrži C1-C4 acilnu skupinu vezanu na sukcinimidnu skupinu;
xvi) sadrži lizin vezan na C1-C4 acil;
xvii) sadrži [PEG(y)]z skupine koja je vezana na glutaril;
xviii) je organska struktura koja se sastoji od lanca od tri, četiri ili pet jedinica izabranih iz skupine koja se sastoji od [PEG(y)]z, C2-C5 acila, sukcinila, malonila, glutarila, aminokiseline, kemijske strukture koja sadrži ciklooktan kondenziran na dihidropiridazin, kemijske strukture koja sadrži ciklookten kondenziran na triazol, kemijske strukture koja sadrži ciklookten kondenziran na izoksazolidin, dibenzociklooktena, dibenzoazaciklooktena,
[image]
[image]
i
[image]
u čemu X1 jest CH ili N, X2 je CH2 ili karbonilna skupina, a R5je arilna ili alkilna skupina; u čemu [PEG(y)]z jest:
[image]
u čemu y = 1-100, a z = 1-10;
xix) je veza;
xx) jest cistein:
xxi) ima linearnu strukturu; ili
xxii) ima razgnananu strukturu;
xxiii) ima strukturu:
[image]
xxiv) jest:
[image]
u čemu n jest 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 1-30, 1-40 ili 1-50;
xxv) jest:
[image]
u čemu n jest 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 1-30, 1-40 ili 1-50, x jest 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 019, 20, 1-30, 1-40, ili 1-50; a z jest 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 1-30, 1-40, ili 1-50;
xxvi) jest:
[image]
u čemu x jest 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 1-30, 1-40 ili 1-50, a z jest 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 1-30, 1-40 ili 1-50; ili
xxvii) jest:
[image]
u čemu n jest 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 1-30, 1-40 ili 1-50.
9. Spoj prema bilo kojem od patentnih zahtjeva 1 - 8,naznačen time, da Z sadrži jedan C, u čemu C jest prvi polipeptid, koji prvi polipeptid sadrži aminokiseline u slijedu koje (i) su identične s odsječkom aminokiselina u slijedu prisutnih u lancu Fc domene antitijela; (ii) vežu se na Fc receptor; i (iii) imaju na njihovom N-terminusu sekvencu izabranu iz skupine koja se sastoji od cisteina, selenocisteina, CP, CPXCP (gdje X = P, R, ili S), CDKTHTCPPCP, CVECPPCP, CCVECPPCP i CDTPPPCPRCP.
10. Spoj prema patentnom zahtjevu 9, naznačen time, da C
i) sadrži aminokiseline u slijedu koje (i) su identične odsječku aminokiselina u slijedu prisutnih u lancu Fc domene antitijela; (ii) vežu se na Fc receptor; i (iii) imaju na svojem N-terminusu sekvencu koja sadrži cistein koji se prirodno pojavljuje, odabran iz skupine
koja se sastoji od CP, CPXCP (gdje X = P, R,ili S), CDKTHTCPPCP, CVECPPCP, CCVECPPCP i CDTPPPCPRCP;
ii) jest polipeptidna komponenta spoja, koja polipeptidna komponenta sadrži aminokiseline u slijedu koje (i) su identične s odsječkom aminokiselina u slijedu prisutnih u lancu Fc domene antitijela; (ii) vežu se na Fc receptor; i (iii) imaju na svojem N-terminusu sekvencu koja sadrži cistein ili selenocistein koji se prirodno ne pojavljuje;
(iii) sadrži aminokiseline u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u lancu Fc domene antitijela izabranih iz skupine koja se sastoji od IgG, IgM, IgA, IgD, i IgE;
iv) sadrži aminokiseline u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u lancu Fc6 domene antitijela;
v) sadrži amino kiseline u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u lancu antitijela različitom od lanca Fc domene antitijela;
vi) aminokiseline u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u teškom lancu od Fab ili Fab’ antitijela; ili
vii) sadrži aminokiseline u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u laganom lancu od Fab ili Fab’ antitijela.
11. Spoj prema patentnom zahtjevu 9 ili 10, naznačen time, da Z nadalje sadrži drugi polipeptid, koji drugi polileptid sadrži aminokiseline u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u lancu antitijela različitom od lanca Fc domene antitijela.
12. Spoj prema patentnom zahtjevu 11, naznačen time, da drugi polipeptid sadrži
i) aminokiseline u slijedu koje su identične s odsječkom amino kiselina u slijedu prisutnih u teškom lancu od Fab ili Fab’ antitijela; ili
ii) aminokiseline u slijedu koje su identične s odsječkom aminokiselina u slijedu prisutnih u laganom lancu od Fab ili Fab’ antitijela.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 - 12, naznačen time, da Z
i) sadrži antitijelo ili njegov dio;
ii) sadrži barem jedan Fab ili Fab’ antitijela, ili dio od barem jednog Fab ili Fab’;
iii) sadrži Fab-1 ili Fab’1, ili njihov dio od antitijela;
iv) sadrži Fab-2 ili Fab’2, ili njihov dio od antitijela;
v) sadrži dvije ruke od Fab ili Fab’ antitijela;
vi) sadrži barem jedan odsječak aminokiselina u slijedu, koje su identične s jednim odsječkom aminokiselina u slijedu prisutnih u jedinom lancu antitijela; ili
vii) sadrži drugi polipeptid, a B je vezan na Z preko peptidilne veze između N-terminus cisteina ili selenocisteina drugog polipeptida od Z i aminokiselinskog ostatka ili organskog kiselinskog ostatka od B.
14. Spoj prema bilo kojem od patentnih zahtjeva 9 – 13, naznačen time, da C-terminus od C
i) sadrži odsječak aminokiselina u slijedu prisutnih u lancu Fc domene od antitijela koje je modificirano; ili
ii) jest cistein, selenocistein, homocistein, ili homoselenosistein, ili derivat cisteina, selenocisteina, homocisteina, ili homoselenosisteina.
15. Homodimer ili heterodimer, naznačen time, da
sadrži spoj prema bilo kojem od patentnih zahtjeva 1-14.
16. Homodimer ili heterodimer prema patentnom zahtjevu 15,naznačen time, da se svaki spoj homodimera ili heterodimera
i) može vezati na drugi preko barem jedne disulfidne veze;
ii) može vezati na drugi preko barem jedne disulfidne veze između C ili drugog polipeptida svakog spoja;
iii) je vezan na drugi preko barem jedne disulfidne veze;
iv) je vezan na drugi barem jednom disulfidnom vezom između C ili drugog polipeptida svakog spoja.
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CA2906175C (en) | 2013-03-15 | 2022-12-13 | Daniel J. Capon | Hybrid immunoglobulin containing non-peptidyl linkage |
SG11201607579TA (en) * | 2014-03-14 | 2016-10-28 | Daniel J Capon | Hybrid immunoglobulin containing non-peptidyl linkage |
ES2607639B1 (es) | 2015-09-30 | 2018-02-28 | Urquima, S.A | Sal de ácido maleico de un intermedio de silodosina |
CN105527433A (zh) * | 2015-12-18 | 2016-04-27 | 南京邮电大学 | 一种检测肿瘤标志物的荧光方法 |
CA3013829A1 (en) * | 2016-02-09 | 2017-08-17 | Alexander Krantz | Site-selective functionalization of proteins using traceless affinity labels |
WO2017191817A1 (ja) | 2016-05-02 | 2017-11-09 | 味の素株式会社 | アジド基含有Fcタンパク質 |
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ES2919779T3 (es) | 2017-06-20 | 2022-07-28 | Imbria Pharmaceuticals Inc | Derivado de 1-[(2,3,4-trimetoxifenil)metil]-piperazina, composiciones del mismo y métodos para aumentar la eficiencia del metabolismo cardíaco |
CA3081543A1 (en) * | 2017-11-03 | 2019-05-09 | Fluidigm Canada Inc. | Reagents and methods for elemental imaging mass spectrometry of biological samples |
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US11530184B2 (en) | 2020-06-30 | 2022-12-20 | Imbria Pharmaceuticals, Inc. | Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate |
US11780811B2 (en) | 2020-06-30 | 2023-10-10 | Imbria Pharmaceuticals, Inc. | Methods of synthesizing 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate |
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