HRP20210707T1 - Prolinom blokirani označeni peptidi i njihova uporaba - Google Patents
Prolinom blokirani označeni peptidi i njihova uporaba Download PDFInfo
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- HRP20210707T1 HRP20210707T1 HRP20210707TT HRP20210707T HRP20210707T1 HR P20210707 T1 HRP20210707 T1 HR P20210707T1 HR P20210707T T HRP20210707T T HR P20210707TT HR P20210707 T HRP20210707 T HR P20210707T HR P20210707 T1 HRP20210707 T1 HR P20210707T1
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- 102000004196 processed proteins & peptides Human genes 0.000 title claims 24
- 108090000765 processed proteins & peptides Proteins 0.000 title claims 24
- 229920001184 polypeptide Polymers 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 8
- 125000001931 aliphatic group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000002252 acyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000006239 protecting group Chemical group 0.000 claims 3
- 150000001413 amino acids Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000002462 isocyano group Chemical group *[N+]#[C-] 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 239000011347 resin Chemical group 0.000 claims 2
- 229920005989 resin Chemical group 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 150000001371 alpha-amino acids Chemical class 0.000 claims 1
- 235000008206 alpha-amino acids Nutrition 0.000 claims 1
- 235000001014 amino acid Nutrition 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004474 heteroalkylene group Chemical group 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
- C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
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- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
- C07K1/113—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure
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- Diabetes (AREA)
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- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
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Claims (14)
1. Polipeptid naznačen time što polipeptid ima formulu (I) ili (II):
[image]
ili
[image]
ili njegova sol ili stereoizomer;
pri čemu:
svaka instanca K, L, M, L1, i L2 je, neovisno, nesupstituirani C1-6 alkilen;
Ra je vodik; supstituirani ili nesupstituirani alifatski; supstituirani ili nesupstituirani heteroalifatski; supstituirani ili nesupstituirani aril; supstituirani ili nesupstituirani heteroaril; supstituirani ili nesupstituirani acil; smola; amino zaštitna skupina; oznaka kojoj je opcionalno pridružen linker , pri čemu je linker skupina koja se sastoji od jedne ili više kombinacija supstituiranog ili nesupstituiranog alkilena; supstituiranog ili nesupstituiranog alkenilena; supstituiranog ili nesupstituiranog alkinilena; supstituiranog ili nesupstituiranog heteroalkilena; supstituiranog ili nesupstituiranog heteroalkenilena; supstituiranog ili nesupstituiranog karbociklena; supstituiranog ili nesupstituiranog heterociklena; supstituirani ili nesupstituirani arilena; ili supstituirani ili nesupstituirani heteroarilen;
Rb je -RB, -ORB, -N(RB)2, ili -SRB, pri čemu svaka instanca RB je, neovisno, vodik; supstituirani ili nesupstituirani alifatski; supstituirani ili nesupstituirani heteroalifatski; supstituirani ili nesupstituirani aril; supstituirani ili nesupstituirani heteroaril; supstituirani ili nesupstituirani acil; smola; prikladna hidroksilna, amio ili tiol zaštitna skupina; ili dvije RB skupine zajedno koje formiraju 5- do 6-člani heterociklični ili heteroaromatski prsten;
svaka instanca RKL, RLL, i RLM je, neovisno, vodik; supstituirani ili nesupstituirani alifatski; supstituirani ili nesupstituirani heteroalifatski; supstituirani ili nesupstituirani aril; supstituirani ili nesupstituirani heteroaril; supstituirani ili nesupstituirani acil; supstituirani ili nesupstituirani hidroksil; supstituirani ili nesupstituirani tiol; supstituirani ili nesupstituirani amino; azido; cijano; izocijano; halo; ili nitro;
svaka instanca Rd je, neovisno, vodik; supstituirani ili nesupstituirani alifatski; supstituirani ili nesupstituirani heteroalifatski; supstituirani ili nesupstituirani aril; supstituirani ili nesupstituirani heteroaril; supstituirani ili nesupstituirani acil; ili Rd je amino zaštitna skupina;
svaka instanca Re je, neovisno, prikladni bočni lanac aminokiselina; vodik; supstituirani ili nesupstituirani alifatski; supstituirani ili nesupstituirani heteroalifatski; supstituirani ili nesupstituirani aril; supstituirani ili nesupstituirani heteroaril; supstituirani ili nesupstituirani acil; supstituirani ili nesupstituirani hidroksil; supstituirani ili nesupstituirani tiol; supstituirani ili nesupstituirani amino; cijano; izocijano; halo; ili nitro;
svaka instanca G je, neovisno, prirodna ili neprirodna aminokiselina ili skupina formule:
[image]
[image]
[image]
[image]
ili
[image]
.
pri čemu:
n je 1, 2, ili 3; i
svaka instanca R1 i R2 je neovisno vodik; supstituirani ili nesupstituirani alifatski; supstituirani ili nesupstituirani heteroalifatski; supstituirani ili nesupstituirani aril; supstituirani ili nesupstituirani heteroaril; supstituirani ili nesupstituirani acil; supstituirani ili nesupstituirani hidroksil; supstituirani ili nesupstituirani tiol; supstituirani ili nesupstituirani amino; ili halo, ili R1 i R2 su spojeni u karbociklički ili heterociklički prsten;
svaka instanca R3 i R4 je, neovisno, vodik; supstituirani ili nesupstituirani alifatski; supstituirani ili nesupstituirani heteroalifatski; hidroksilna zaštitna skupina kada je vezana na atom kisika, ili amino zaštitna skupina kada su vezani za atom dušika ili dva R3 skupine povezane na atom dušika spojene su u heterociklički prsten;
svaka instanca XAA je, neovisno, prirodna ili neprirodna α-amino kiselina;
y je, neovisno, 1 do 8;
s je 0, 1, ili 2;
j je, neovisno, integer između 1 do 10;
p je, neovisno, integer između 1 do 2;
svaka instanca q je neovisno 0, 1, ili 2;
v je, neovisno, integer između 0 do 1;
svaka instanca t, w, i z je, neovisno, integer između 0 i 100; i
[image]
odgovara jednostrukoj, dvostrukoj ili trostrukoj vezi.
2. Polipeptid iz zahtjeva 1, pri čemu polipeptid jepolipeptid je izabran iz skupine koja se sastoji od formula:
[image]
[image]
[image]
[image]
[image]
i njegove soli i stereoizomeri.
3. Polipeptid iz zahtjeva 1, pri čemu polipeptid je:
[image]
ili njegova sol.
4. Polipeptid iz zahtjeva 1, pri čemu polipeptid je:
[image]
ili njegova sol.
5. Polipeptid iz zahtjeva 1, pri čemu polipeptid je:
[image]
ili njegova sol.
6. Polipeptid iz zahtjeva 1, pri čemu polipeptid je:
[image]
ili njegova sol.
7. Polipeptid iz zahtjeva 1, pri čemu polipeptid ima formulu (II):
[image]
ili njegova sol ili stereoizomer.
8. Polipeptid iz zahtjeva 1, pri čemu polipeptid ima formulu (I):
[image]
ili njegova sol ili stereoizomer.
9. Polipetid iz bilo kojeg od zahtjeva 1 do 8, pri čemu y je 2.
10. Polipetid iz bilo kojeg od zahtjeva 1 do 8, pri čemu y je 3.
11. Polipetid iz bilo kojeg od zahtjeva 1 do 8, pri čemu y je 4.
12. Polipetid iz bilo kojeg od zahtjeva 1 do 8, pri čemu y je 5.
13. Polipetid iz bilo kojeg od zahtjeva 1 do 8, pri čemu y je 6.
14. Polipetid iz bilo kojeg od zahtjeva 1 do 8, pri čemu v je 0.
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US201261705950P | 2012-09-26 | 2012-09-26 | |
US201361789157P | 2013-03-15 | 2013-03-15 | |
PCT/US2013/062004 WO2014052647A2 (en) | 2012-09-26 | 2013-09-26 | Proline-locked stapled peptides and uses thereof |
EP13777368.5A EP2920197B1 (en) | 2012-09-26 | 2013-09-26 | Proline-locked stapled peptides and uses thereof |
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HRP20210707T1 true HRP20210707T1 (hr) | 2021-09-17 |
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HRP20210707TT HRP20210707T1 (hr) | 2012-09-26 | 2021-05-06 | Prolinom blokirani označeni peptidi i njihova uporaba |
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US (4) | US9617309B2 (hr) |
EP (2) | EP2920197B1 (hr) |
JP (3) | JP6506166B2 (hr) |
CA (2) | CA3113959A1 (hr) |
CY (1) | CY1125259T1 (hr) |
DK (1) | DK2920197T3 (hr) |
ES (1) | ES2874525T3 (hr) |
HK (1) | HK1213269A1 (hr) |
HR (1) | HRP20210707T1 (hr) |
HU (1) | HUE054444T2 (hr) |
IL (4) | IL237967B (hr) |
LT (1) | LT2920197T (hr) |
PL (1) | PL2920197T3 (hr) |
PT (1) | PT2920197T (hr) |
RS (1) | RS61957B1 (hr) |
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2021
- 2021-05-06 HR HRP20210707TT patent/HRP20210707T1/hr unknown
- 2021-05-12 IL IL283139A patent/IL283139A/en unknown
- 2021-06-08 CY CY20211100497T patent/CY1125259T1/el unknown
- 2021-09-06 JP JP2021144616A patent/JP7448966B2/ja active Active
-
2022
- 2022-02-25 US US17/681,248 patent/US20220177522A1/en not_active Abandoned
-
2023
- 2023-08-21 US US18/453,118 patent/US20240124525A1/en active Pending
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