HRP20191160T1 - Tfpi inhibitori i postupci upotrebe - Google Patents

Tfpi inhibitori i postupci upotrebe Download PDF

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HRP20191160T1
HRP20191160T1 HRP20191160TT HRP20191160T HRP20191160T1 HR P20191160 T1 HRP20191160 T1 HR P20191160T1 HR P20191160T T HRP20191160T T HR P20191160TT HR P20191160 T HRP20191160 T HR P20191160T HR P20191160 T1 HRP20191160 T1 HR P20191160T1
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amino acid
group
acid selected
peptide
aib
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Michael Dockal
Rudolf Hartmann
Friedrich Scheiflinger
Frank Osterkamp
Thomas Polakowski
Ulrich Reineke
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Baxalta GmbH
Baxalta Incorporated
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81—Protease inhibitors
    • C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
    • C07K14/8114—Kunitz type inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
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    • G01—MEASURING; TESTING
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    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/86—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving blood coagulating time or factors, or their receptors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • G01—MEASURING; TESTING
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    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/81—Protease inhibitors
    • G01N2333/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • G01N2333/811—Serine protease (E.C. 3.4.21) inhibitors
    • G01N2333/8114—Kunitz type inhibitors
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/20—Screening for compounds of potential therapeutic value cell-free systems

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Claims (14)

1. TFPI-vezujući peptidni kompleks koji obuhvaća prvi peptid i drugi peptid, pri čemu (a) prvi peptid obuhvaća strukturu formule (XIII): pri čemu X6001 je aminokiselina izabrana iz grupe koja obuhvaća F, L, M, Y, 1Ni, Thi, Bta, Dopa, Bhf, C, D, G, H, I, K, N, Nmf, Q, R, T, V, i W; pri čemu X6002 je aminokiselina izabrana iz grupe koja obuhvaća Q, G, i K; pri čemu X6003 je aminokiselina izabrana iz grupe koja obuhvaća C, D, E, M, Q, R, S, T, Ede(O), Cmc, A, Aib, Bhs, F, G, H, I, K, L, N, P, V, W i Y; pri čemu X6004 je aminokiselina izabrana iz grupe koja obuhvaća Aib, E, G, I, K, L, M, P, R, W, Y, A, Bhk, C, D, F, H, k, N, Nmk, Q, S, T i V; pri čemu X6005 je aminokiselina izabrana iz grupe koja obuhvaća a, A, Aib, C, D, d, E, G, H, K, k, M, N, Nmg, p, Q, R, NpropilG, aze, pip, tic, oic, hyp, nma, Ncg, Abg, Apg, thz, dtc, Bal, F, L, S, T, V, W i Y; pri čemu X6006 je aminokiselina izabrana iz grupe koja obuhvaća A, C, C(NEM), D, E, G, H, K, M, N, Q, R, S, V, Cit, C(Acm), Nle, I, Ede(O), Cmc, Ecl, Eea, Eec, Eef, Nif, Eew, Aib, Btq, F, L, T, W i Y; pri čemu X6007 je aminokiselina izabrana iz grupe koja obuhvaća I, V, T, Chg, Phg, Tie, A, F, G, K, L, Nmv, P, Q, S, W i Y; pri čemu X6008 je aminokiselina izabrana iz grupe koja obuhvaća F, H, 1Ni, 2Ni, Pmy, Y, i W; pri čemu X6009 je aminokiselina izabrana iz grupe koja obuhvaća Aib, V, Chg, Phg, Abu, Cpg, Tie, L-2-amino-4,4,4-trifluorobutanska kiselina, A, f, I, K, S, T i V; pri čemu X6010 je aminokiselina izabrana iz grupe koja obuhvaća A, C, D, d, E, F, H, K, M, N, P, Q, R, S, T, V, W, Y, Nmd, C(NEM), Aib, G, I, L i Nmf; pri čemu X6011 je aminokiselina izabrana iz grupe koja obuhvaća A, a, G, p, Sar, c, hcy, Aib, C, K, i Nmg; pri čemu X6012 je aminokiselina izabrana iz grupe koja obuhvaća Y, Tym, Pty, Dopa i Pmy; pri čemu X6013 je aminokiselina izabrana iz grupe koja obuhvaća Aib, C, F, 1Ni, Thi, Bta, A, E, G, H, K, L, M, Q, R, W i Y; pri čemu X6014 je aminokiselina izabrana iz grupe koja obuhvaća A, Aib, C, C(NEM), D, E, K, L, M, N, Q, R, T, V, Hcy, Bhe, F, G, H, I, P, S, W i Y; pri čemu X6015 je aminokiselina izabrana iz grupe koja obuhvaća R, (omega-metil)-R, D, E i K; pri čemu X6016 je aminokiselina izabrana iz grupe koja obuhvaća L, Hcy, Hle i Aml; pri čemu X6017 je aminokiselina izabrana iz grupe koja obuhvaća A, a, Aib, C, c, Cha, Dab, Eag, Eew, H, Har, Hci, Hle, I, K, L, M, Nle, Nva, Opa, Orn, R, S, Deg, Ebc, Eca, Egz, Aic, Apc, Egt, (omega-metil)-R, Bhr, Cit, D, Dap, E, F, G, N, Q, T, V, W i Y; pri čemu X6018 je aminokiselina izabrana iz grupe koja obuhvaća A, Aib, Hcy, hcy, C, c, L, Nle, M, N, R, Bal, D, E, F, G, H, I, K, Q, S, T, V, W i Y; pri čemu X6019 je aminokiselina izabrana iz grupe koja obuhvaća K, R, Har, Bhk i V; i pri čemu X6020 je aminokiselina izabrana iz grupe koja obuhvaća K, L, Hcy, Aml, Aib, Bhl, C, F, G, H, I, Nml, Q, R, S, T, V, W i Y i (b) drugi peptid koji obuhvaća strukturu formule (XIV): pri čemu X7001 je ili prisutna ili odsutna, gdje u slučaju kada je X7001 prisutna je aminokiselina izabrana iz grupe koja obuhvaća A, C, C(NEM), D, E, F, G, H, I, K, L, P, R, S, T, V i W; pri čemu X7002 je ili prisutna ili odsutna, gdje u slučaju kada je X7002 prisutna je aminokiselina izabrana iz grupe koja obuhvaća A, C, C(NEM), D, E, F, G, H, I, K, L, M, P, Q, R, S, T, V, W i Y; pri čemu X7003 je aminokiselina izabrana iz grupe koja obuhvaća A, F, I, K, L, R, S, T, V, W i Y; pri čemu X7004 je aminokiselina izabrana iz grupe koja obuhvaća A, D, E, F, G, I, K, L, R, S, T, V i W; pri čemu X7005 je R ili W; pri čemu X7006 je aminokiselina izabrana iz grupe koja obuhvaća F, H, I, K, L, R, V i W; pri čemu X7007 je aminokiselina izabrana iz grupe koja obuhvaća Orn, homoK, C, Hcy, Dap i K, poželjno izabrana iz grupe koja obuhvaća C i Hcy; pri čemu X7008 je aminokiselina izabrana iz grupe koja obuhvaća A, G, R, S i T; pri čemu X7009 je aminokiselina izabrana iz grupe koja obuhvaća a, A, I, K, L, M, m, Moo, Nle, p, R, Sem i V; pri čemu X7010 je aminokiselina izabrana iz grupe koja obuhvaća A, G, I, K, L, P, R, S, T i V; pri čemu X7011 je aminokiselina izabrana iz grupe koja obuhvaća D, E, G, S i T; pri čemu X7012 je aminokiselina izabrana iz grupe koja obuhvaća A, a, D, d, E, e, F, f, G, l, K, k, L, l, M, m, Moo, Nle, nle, P, p, R, r, S, s, Sem, T, t, V, v, W i w; pri čemu X7013 je aminokiselina izabrana iz grupe koja obuhvaća A, C, C(NEM), Con, Con(Meox), D, d, E, e, Eag, F, G, I, K, L, N, R, S, s, T, V i W; pri čemu X7014 je aminokiselina izabrana iz grupe koja obuhvaća A, D, E, F, G, I, K, L, M, R, S, T, V i W; pri čemu X7015 je aminokiselina izabrana iz grupe koja obuhvaća A, D, E, F, G, I, K, L, M, Nle, R, S, T, V i W; pri čemu X7016 je aminokiselina izabrana iz grupe koja obuhvaća A, D, E, F, I, K, L, M, Moo, Nle, R, S, Sem, T, V, W i Y; pri čemu X7017 je aminokiselina izabrana iz grupe koja obuhvaća A, D, E, F, G, I, K, L, R, S, T, V, W i Y; pri čemu X7018 je aminokiselina izabrana iz grupe koja obuhvaća C i D, poželjno C; pri čemu X7019 je aminokiselina izabrana iz grupe koja obuhvaća A, F, I, L, S, T, V i W; pri čemu X7020 je aminokiselina izabrana iz grupe koja obuhvaća F i W; pri čemu X7021 je aminokiselina izabrana iz grupe koja obuhvaća I, L i V; pri čemu X7022 je aminokiselina izabrana iz grupe koja obuhvaća A, D, E, F, G, I, K, L, P, R, S, T, V i W; pri čemu X7023 je ili prisutna ili odsutna, gdje u slučaju kada je X7023 prisutna je aminokiselina izabrana iz grupe koja obuhvaća A, C, C(NEM), Con, Con(Meox), D, E, Eag, F, G, I, K, L, R, S, T, V, W i Y; pri čemu peptid obuhvaća kao cikličnu strukturu koja se dobija vezivanjem između X7007 i X7018; pri čemu C-kraj prvog peptida je povezan sa N-krajem drugog peptida preko grupe za povezivanje; pri čemu prvi peptid obuhvaća sekvencu aminokiselina najmanje 80%, najmanje 85%, najmanje 90%, najmanje 95%, ili 100% identičnu sa SEQ ID NO: 178 ili SEQ ID NO: 4261; i pri čemu drugi peptid obuhvaća sekvencu aminokiselina najmanje 80%, najmanje 85%, najmanje 90%, najmanje 95%, ili 100% identičnu sa SEQ ID NO: 1044.
2. Peptidni kompleks prema zahtjevu 1, pri čemu X6001 je aminokiselina izabrana iz grupe koja obuhvaća 1Ni, Bta, Dopa, F, L, Y i M; pri čemu X6002 je Q; pri čemu X6003 je aminokiselina izabrana iz grupe koja obuhvaća D, E, S, M, Q, R, T i C; pri čemu X6004 je aminokiselina izabrana iz grupe koja obuhvaća K, Aib, L, P, R, E, G, I, Y, M i W; pri čemu X6005 je aminokiselina izabrana iz grupe koja obuhvaća p, Nmg, NpropilG, aze, pip, tic, oic, hyp, a, Aib, D, d, G, H, K, k, N, Q, R, A, E, C i M; pri čemu X6006 je aminokiselina izabrana iz grupe koja obuhvaća C, E, K, R, S, V, C(Acm), Nle, C(NEM), I, Cit, A, D, G, H, Q i M; pri čemu X6007 je aminokiselina izabrana iz grupe koja obuhvaća Tle, V i I; pri čemu X6008 je aminokiselina izabrana iz grupe koja obuhvaća H, 1Ni, 2Ni, Pmy, F i Y; pri čemu X6009 je V, Abu ili Tle; pri čemu X6010 je aminokiselina izabrana iz grupe koja obuhvaća D, P, C, T, A, E, K, M, N, Q, R, F, H, S, V, W i Y; pri čemu X6011 je G, a, c, hcy ili Sar; pri čemu X6012 je Y; pri čemu X6013 je aminokiselina izabrana iz grupe koja obuhvaća F, 1Ni, Bta i C; pri čemu X6014 je aminokiselina izabrana iz grupe koja obuhvaća Aib, C, E, Hcy, A, D, K, L, M, N, Q, R, T, V i Aib; pri čemu X6015 je R; pri čemu X6016 je aminokiselina izabrana iz grupe koja obuhvaća L, Aml, Hle i Hcy; pri čemu X6017 je aminokiselina izabrana iz grupe koja obuhvaća A, Aib, C, c, Aic, Eca, Deg, Cha, Dab, Dap, Eag, Eew, H, Har, Hci, Hle, K, Nle, Nva, Opa, Orn, R, I, L, S i M; pri čemu X6018 je aminokiselina izabrana iz grupe koja obuhvaća A, Aib, C, c, L, Hcy, N, M i R; pri čemu X6019 je K; i pri čemu X6020 je aminokiselina izabrana iz grupe koja obuhvaća L, Aml, Hcy i K.
3. Peptidni kompleks prema zahtjevu 1 ili zahtjevu 2, pri čemu prvi peptid i/ili drugi peptid dalje obuhvaća N-terminalnu aminokiselinu(e) i/ili ostatke koji su vezani za X6001 i/ili X7001 i izabrane iz grupe koja obuhvaća FAM-Ttds, PE, Palm, 2-fenil acetil, 3-fenil propionil, 2-(naft-2-il) acetil, heksanoil, 2-metil propionil, 3-metil butanoil, 2-naftilsulfonil, 1-naftilsulfonil, acetil, Con, Con(Meox), AOA, Oxme-AOA, Meox-Lev, levulinsku kiselinu (Lev), i pentansku kiselinu (Pyn).
4. Peptidni kompleks prema bilo kojem od zahtjeva 1-3, pri čemu prvi peptid i/ili drugi peptid dalje obuhvaća X6021 koji je vezan sa X6020 ili X7024 koji je vezan sa X7023, redom, pri čemu X6021 i/ili X7024 obuhvaća C-terminalnu aminokiselinu(e) i/ili ostatke izabrane iz grupe koja obuhvaća Hly, K, Orn, Dab, Dap, Eag, Hcy, Pen, C, c, C(NEM), Con, Con(Meox), K(Ttds-maleimidopropionil(EtSH)), K(Tdts-maleimid), K(AOA), K(Myr), K(Ttds-Myr), K(Ttds-Palm), K(Ttds-Ac), K(Ttds-yGlu-Myr), K(AlbuTag), K(4PBSA), Cea, i amid.
5. Peptidni kompleks prema bilo kojem od zahtjeva 1-4, pri čemu X7001 je aminokiselina izabrana iz grupe koja obuhvaća A, D, F, G, H, K, L i S; pri čemu X7002 je aminokiselina izabrana iz grupe koja obuhvaća H, F, M i R; pri čemu X7003 je aminokiselina izabrana iz grupe koja obuhvaća F i Y; pri čemu X7004 je K; pri čemu X7005 je W; pri čemu X7006 je aminokiselina izabrana iz grupe koja obuhvaća F i H; pri čemu X7007 je C; pri čemu X7008 je aminokiselina izabrana iz grupe koja obuhvaća A, G i S; pri čemu X7009 je aminokiselina izabrana iz grupe koja obuhvaća M, Sem i V; pri čemu X7010 je aminokiselina izabrana iz grupe koja obuhvaća K, P i R; pri čemu X7011 je D; pri čemu X7012 je aminokiselina izabrana iz grupe koja obuhvaća F, L, I, M i Sem; pri čemu X7013 je aminokiselina izabrana iz grupe koja obuhvaća D, G, K i S; pri čemu X7014 je G; pri čemu X7015 je aminokiselina izabrana iz grupe koja obuhvaća I i T; pri čemu X7016 je aminokiselina izabrana iz grupe koja obuhvaća D, F, M, Sem i Y; pri čemu X7017 je aminokiselina izabrana iz grupe koja obuhvaća S i T; pri čemu X7018 je C; pri čemu X7019 je aminokiselina izabrana iz grupe koja obuhvaća A i V; pri čemu X7020 je W; pri čemu X7021 je V; pri čemu X7022 je aminokiselina izabrana iz grupe koja obuhvaća F, L, K, R, P i W; pri čemu X7023 je ili prisutna ili odsutna, gdje u slučaju kada je X7023 prisutna je aminokiselina izabrana iz grupe koja obuhvaća A, D, F, M, S i Y; i pri čemu peptid obuhvaća kao cikličnu strukturu koja se dobija vezivanjem između X7007 i X7018.
6. Peptidni kompleks prema bilo kom od zahtjeva 1-5 pri čemu je ostatak grupe za povezivanje dužine 1-100 Å, dužine 5-50 Å, ili dužine 10-30 Å.
7. Peptidni kompleks prema zahtjevu 6, pri čemu ostatak grupe za povezivanje obuhvaća strukturu Z1-20, pri čemu Z je aminokiselina, hidroksi kiselina, etilen glikol, propilen glikol, ili bilo koja kombinacija od gore navedenog.
8. Peptidni kompleks prema zahtjevu 7, pri čemu Z je G, s, S, a, A, Bal, Gaba, Ahx, Ttds, ili bilo koja kombinacija od gore navedenog.
9. Peptidni kompleks prema zahtjevu 1 koji obuhvaća sekvencu aminokiselina koja je predstavljena u SEQ ID NO: 4260.
10. Peptidni kompleks prema zahtjevu 1, pri čemu drugi peptid obuhvaća sekvencu aminokiselina koja je predstavljena u SEQ ID NO: 1334.
11. Peptidni kompleks prema bilo kojem od zahtjeva 1-10, pri čemu je peptidni kompleks konjugiran sa ostatkom polietilen glikola (PEG), albuminom iz humanog seruma (HSA), ili HSA-vezujućim područjem, antitijelom ili njegovim fragmentom, hidroksietil škrobom, prolin-alanin-serin multimerom (PASilacija), C12-C18 masnom kiselinom, ili polisijalinskom kiselinom.
12. Peptidni kompleks prema bilo kojem od zahtjeva 1-11 za upotrebu u postupku za liječenje subjekta.
13. Peptidni kompleks prema zahtjevu 12, pri čemu postupak je za liječenje poremećaja koagulacije krvi.
14. Farmaceutski sastav koji obuhvaća peptidni kompleks prema bilo kojem od zahtjeva 1 do 11 i farmaceutski prihvatljivi nosač, i opcionalno dalje obuhvaća dodatno farmaceutski efikasno sredstvo.
HRP20191160TT 2012-03-21 2019-06-26 Tfpi inhibitori i postupci upotrebe HRP20191160T1 (hr)

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US201261613865P 2012-03-21 2012-03-21
EP13703505.1A EP2827883B1 (en) 2012-03-21 2013-01-31 Tfpi inhibitors and methods of use
PCT/US2013/024167 WO2013141965A1 (en) 2012-03-21 2013-01-31 Tfpi inhibitors and methods of use

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