HRP20220720T1 - Analozi egf(a) s masnim kiselinama kao supstituentima - Google Patents
Analozi egf(a) s masnim kiselinama kao supstituentima Download PDFInfo
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- HRP20220720T1 HRP20220720T1 HRP20220720TT HRP20220720T HRP20220720T1 HR P20220720 T1 HRP20220720 T1 HR P20220720T1 HR P20220720T T HRP20220720T T HR P20220720TT HR P20220720 T HRP20220720 T HR P20220720T HR P20220720 T1 HRP20220720 T1 HR P20220720T1
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- gglu
- hooc
- 301leu
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- 125000005313 fatty acid group Chemical group 0.000 title claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 35
- 125000003275 alpha amino acid group Chemical group 0.000 claims 16
- 238000006467 substitution reaction Methods 0.000 claims 16
- 239000000126 substance Substances 0.000 claims 10
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 238000002965 ELISA Methods 0.000 claims 3
- BGGALFIXXQOTPY-NRFANRHFSA-N C1(=C(C2=C(C=C1)N(C(C#N)=C2)C[C@@H](N1CCN(CC1)S(=O)(=O)C)C)C)CN1CCC(CC1)NC1=NC(=NC2=C1C=C(S2)CC(F)(F)F)NC Chemical compound C1(=C(C2=C(C=C1)N(C(C#N)=C2)C[C@@H](N1CCN(CC1)S(=O)(=O)C)C)C)CN1CCC(CC1)NC1=NC(=NC2=C1C=C(S2)CC(F)(F)F)NC BGGALFIXXQOTPY-NRFANRHFSA-N 0.000 claims 2
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- -1 methylsulfonylcarbamoylamino residue Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- FUOSTELFLYZQCW-UHFFFAOYSA-N 1,2-oxazol-3-one Chemical group OC=1C=CON=1 FUOSTELFLYZQCW-UHFFFAOYSA-N 0.000 claims 1
- KQZLRWGGWXJPOS-NLFPWZOASA-N 1-[(1R)-1-(2,4-dichlorophenyl)ethyl]-6-[(4S,5R)-4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-5-methylcyclohexen-1-yl]pyrazolo[3,4-b]pyrazine-3-carbonitrile Chemical compound ClC1=C(C=CC(=C1)Cl)[C@@H](C)N1N=C(C=2C1=NC(=CN=2)C1=CC[C@@H]([C@@H](C1)C)N1[C@@H](CCC1)CO)C#N KQZLRWGGWXJPOS-NLFPWZOASA-N 0.000 claims 1
- PAYROHWFGZADBR-UHFFFAOYSA-N 2-[[4-amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propane-1,3-diol Chemical compound C1=C(I)C(OC)=CC(C(C)C)=C1OC1=CN=C(NC(CO)CO)N=C1N PAYROHWFGZADBR-UHFFFAOYSA-N 0.000 claims 1
- IJRKLHTZAIFUTB-UHFFFAOYSA-N 5-nitro-2-(2-phenylethylamino)benzoic acid Chemical compound OC(=O)C1=CC([N+]([O-])=O)=CC=C1NCCC1=CC=CC=C1 IJRKLHTZAIFUTB-UHFFFAOYSA-N 0.000 claims 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 claims 1
- LIMFPAAAIVQRRD-BCGVJQADSA-N N-[2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl]-8-[(2R,3S)-2-methyl-3-(methylsulfonylmethyl)azetidin-1-yl]-5-propan-2-ylisoquinolin-3-amine Chemical compound F[C@H]1CN(CC[C@H]1OC)C1=NC=CC(=N1)NC=1N=CC2=C(C=CC(=C2C=1)C(C)C)N1[C@@H]([C@H](C1)CS(=O)(=O)C)C LIMFPAAAIVQRRD-BCGVJQADSA-N 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 229940125877 compound 31 Drugs 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/177—Receptors; Cell surface antigens; Cell surface determinants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/475—Growth factors; Growth regulators
- C07K14/485—Epidermal growth factor [EGF], i.e. urogastrone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
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- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Immunology (AREA)
- Toxicology (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Cell Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
Claims (23)
1. Derivat EGF(A) koji sadrži analog peptida EGF(A) koji sadrži 301Leu i supstituent koji sadrži najmanje jednu masnokiselinsku skupinu, naznačen time što analog peptida EGF(A) ima 1-8 aminokiselinskih zamjena u usporedbi s domenom EGF(A), aminokiseline 293-332 u LDL-R, definirane s SEQ ID NO:1, te što derivat ima Ki ispod 5 nM kada se mjeri u testu ELISA s kompeticijom na vezanje na PCSK9-LDL-R, kao što je opisano u Odjeljku D1.1 Opisa izuma.
2. Derivat EGF(A) u skladu s patentnim zahtjevom 1, naznačen time što navedeni supstituent sadrži karboksilnokiselinski, sulfonskokiselinski, tetrazolni ostatak, methilsulfonilkarbamoilamino ostatak ili 3-hidroksiizoksazolni ostatak i 8-20 uzastopnih skupina -CH2-.
3. Derivat EGF(A) u skladu s patentnim zahtjevom 1, naznačen time što navedeni supstituent ima Formulu I:
Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10- [I]
gdje
Z1 se bira između:
Kemijske formule 1: HOOC-(CH2)n-CO-*,
Kemijske formule 2: tetrazolil-(CH2)n-CO-*,
Kemijske formule 3: HOOC-(C6H4)-O-(CH2)m-CO-*,
Kemijske formule 4: HOS(O)2-(CH2)n-CO-*,
Kemijske formule 5: MeS(O)2NH(CO)N-(CH2)n-CO-* i
Kemijske formule 6: 3-HO-izoksazol-(CH2)n-CO-*
gdje
n je cijeli broj u rasponu od 8-20,
m je cijeli broj u rasponu od 8-11,
skupina -COOH u Kemijskoj formuli 3 može biti vezana na položaju 2, 3 ili 4 u fenilnom prstenu, simbol * označuje mjesto vezanja na dušiku u Z2 ili, ako je Z2 veza, na dušiku u susjednom elementu Z;
Z2 se bira između
Kemijske formule 7: *-NH-SO2-(CH2)3-CO-*,
Kemijske formule 8: *-NH-CH2-(C6H10)-CO-* i
veza;
Z3 se bira između:
γGlu, Glu i veze;
Z4, Z5, Z6, Z7, Z8, Z9 se, međusobno neovisno, bira između:
Glu, γGlu, Gly, Ser, Ala, Thr, Ado, Aeep, Aeeep, TtdSuc i veze;
Z10 se bira između:
Kemijske formule 14: *-NH-CH2-(C6H4)-CH2-* i veze.
4. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što derivat EGF(A) sadrži jedan ili dva supstituenta koje se bira iz skupine koju čine:
HOOC-(CH2)18-CO-gGlu-2xADO-
HOOC-(CH2)18-CO-NH-CH2-(C6H10)-CO-gGlu-2xADO-
HOOC-(CH2)16-CO-gGlu-2xADO-
HOOC-(CH2)16-CO-gGlu-2xADO-NH-CH2-(C6H4)-CH2-
HOOC-(CH2)16-CO-gGlu-
HOOC-(CH2)16-CO-NH-CH2-(C6H10)-CO-gGlu-2xADO-
HOOC-(CH2)14-CO-gGlu-2xADO-
HOOC-(CH2)14-CO-gGlu-
HOOC-(CH2)14-CO-gGlu-2xADO-
HOOC-(CH2)12-CO-gGlu-2xADO-
4-HOOC-(C6H4)-O-(CH2)10-CO-gGlu-2xADO-
4-HOOC-(C6H4)-O-(CH2)10-CO-gGlu-3xADO-
4-HOOC-(C6H4)-O-(CH2)10-CO-gGlu-
4-HOOC-(C6H4)-O-(CH2)10-CO-2xgGlu-
4-HOOC-(C6H4)-O-(CH2)10-CO-gGlu-3xGly-
4-HOOC-(C6H4)-O-(CH2)10-CO-2xgGlu-2xADO-
4-HOOC-(C6H4)-O-(CH2)10-CO-gGlu-TtdSuc-
4-HOOC-(C6H4)-O-(CH2)9-CO-
4-HOOC-(C6H4)-O-(CH2)10-CO-gGlu-4xADO-
4-HOOC-(C6H4)-O-(CH2)10-CO-NH-CH2-(C6H10)-CO-gGlu-2xADO-
4-HOOC-(C6H4)-O-(CH2)9-CO-gGlu-2xADO-
3-HOOC-(C6H4)-O-(CH2)9-CO-gGlu-2xADO-
3-HO-izoksazol-(CH2)12-CO-gGlu-2xADO-
HOS(O)2-(CH2)15-CO-gGlu-2xADO-NH-CH2-(C6H4)-CH2-
HOS(O)2-(CH2)13-CO-gGlu-2xADO-
tetrazolil-(CH2)15-CO-NH-SO2-(CH2)3-CO-ADO-ADO-NH-CH2-(C6H4)-CH2-
tetrazolil-(CH2)12-CO-gGlu-2xADO-
tetrazolil-(CH2)15-CO-gGlu-2xADO- i
MeS(O)2NH(CO)NH-(CH2)12-CO-gGlu-2xADO-.
5. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži jedan, dva, tri, četiri ili svi pet od sljedećih aminokiselinskih ostataka (divljeg tipa): 295Asn, 296Glu, 298Leu, 302Gly i 310Asp.
6. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži ostatak divljeg tipa 310Asp.
7. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži ostatak divljeg tipa 295Asn.
8. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži 299Asp (D) ili 299Ala (A).
9. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži 307Ile (I).
10. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži 309Arg (R).
11. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži zamjenu 312Lys aminokiselinom koju se bira iz skupine koju čine: 312Glu, 312Asp, 312Gln i 312Arg.
12. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži najmanje dvije aminokiselinske zamjene koje identificira bilo koja od skupina:
i. 301Leu i 309Arg
ii. 301Leu, 309Arg, 312Glu
iii. 301Leu, 307Ile i 309Arg
iv. 301Leu, 307Ile, 309Arg i 312Glu
v. 301Leu, 309Arg i 321Glu
vi. 301Leu, 309Arg, 321Glu i 312Glu
vii. 301Leu, 307Ile, 309Arg i 299Ala
viii. 301Leu, 307Ile, 309Arg, 299Ala i 312Glu
ix. 301Leu i 309Arg i najmanje jedna zamjena Lys
x. 301Leu, 309Arg, 312Glu i najmanje jedna zamjena Lys
xi. 301Leu, 307Ile i 309Arg i najmanje jedna zamjena Lys
xii. 301Leu, 307Ile, 309Arg i 312Glu i najmanje jedna zamjena Lys
xiii. 301Leu, 309Arg i 321Glu i najmanje jedna zamjena Lys
xiv. 301Leu, 309Arg, 321Glu i 312Glu i najmanje jedna zamjena Lys
xv. 301Leu, 307Ile, 309Arg i 299Ala i najmanje jedna zamjena Lys i
xvi. 301Leu, 307Ile, 309Arg, 299Ala i 312Glu i najmanje jedna zamjena Lys.
13. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je najmanje jedan supstituent vezan na ostatak Lys u analogu peptida EGF(A) kojeg se bira iz skupine koju čine: 292Lys, 293Lys, 294Lys, 296Lys, 299Lys, 300Lys, 303Lys, 305Lys, 306Lys, 309Lys, 311Lys, 312Lys, 313Lys, 314Lys, 315Lys, 316Lys, 318Lys, 320Lys, 321Lys, 322Lys, 323Lys, 324Lys, 325Lys, 326Lys, 327Lys, 328Lys, 329Lys, 330Lys, 332Lys i 333Lys.
14. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što analog peptida EGF(A) sadrži najmanje jedan ostatak Lys kojeg se bira iz skupine koju čine: 313Lys, 324Lys, 328Lys i 333Lys.
15. Derivat EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što su jedan ili dva supstituenta vezani na ostatak Lys u analogu peptida EGF(A).
16. Derivat EGF(A) u skladu s patentnim zahtjevom 1, naznačen time što se derivat EGF(A) bira iz skupine derivata EGF(A) koju čine: Egzemplarni spojevi 1-44, 46-47, 51-55, 57, 60-64, 66-69, 71-102 i 106-159 opisani u odjeljku C.1 i tablici 4 u Opisu izuma.
17. Derivat EGF(A), naznačen time što ga se bira iz skupine koju čine:
i. Egzemplarni spoj 31
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO: 32,
ii. Egzemplarni spoj 95,
[image]
,
gdje aminokiselinski slijed the peptidna okosnica je SEQ ID NO: 76,
iii. Egzemplarni spoj 128
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO: 32,
iv. Egzemplarni spoj 133,
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO: 98,
v. Egzemplarni spoj 143,
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO: 98,
vi. Egzemplarni spoj 144,
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO:98,
vii. Egzemplarni spoj 150,
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO:78,
viii. Egzemplarni spoj 151,
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO:104,
ix. Egzemplarni spoj 152
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO:72, te
x. Egzemplarni spoj 153
[image]
,
gdje je aminokiselinski slijed peptidne okosnice SEQ ID NO:105.
18. Derivat EGF(A) N{α}(N{ε328}-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboksi-4-(15-karboksipentadekanoilamino)butanoil]amino]etoksi]etoksi]acetil]amino]etoksi]etoksi]acetil]-[Leu301,Arg309,Glu312,Glu321,Lys328]-LDL-R-(293-332)-peptidil)-N{ε}[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboksi-4-(15-karboksipentadekanoilamino)butanoil]amino]etoksi]etoksi]acetil]amino]etoksi]etoksi]acetil]Lys (Egzemplarni spoj 151),
[image]
,
naznačen time što je aminokiselinski slijed peptidne okosnice SEQ ID NO:104.
19. Analog peptida EGF(A) koji ima 1-8 aminokiselinskih zamjena u usporedbi s domenom EGF(A), aminokiseline 293-332 u LDL-R, definiran s SEQ ID NO 1, naznačen time što analog peptida EGF(A) sadrži 301Leu, 310Asp i aminokiselinsku zamjenu 312Lys, te što analog ima Ki ispod 5 nM kada se mjeri u testu ELISA s kompeticijom na vezanje na PCSK9-LDL-R, kao što je opisano u Odjeljku D1.1 Opisa izuma.
20. Analog peptida EGF(A) koji ima 1-8 aminokiselinskih zamjena u usporedbi s domenom EGF(A), aminokiseline 293-332 u LDL-R, definiran s SEQ ID NO 1, naznačen time što analog peptida EGF(A) sadrži 301Leu i 310Asp, što peptid nema zamjenu 299Asp u Glu, Val ili His, te što analog ima Ki ispod 5 nM kada se mjeri u testu ELISA s kompeticijom na vezanje na PCSK9-LDL-R, kao što je opisano u Odjeljku D1.1 Opisa izuma.
21. Analog peptida EGF(A) u skladu s patentnim zahtjevom 19 ili 20, naznačen time što analog peptida EGF(A) sadrži ostatke Cys: 297Cys, 304Cys, 308Cys, 317Cys, 319Cys i 331Cys.
22. Analog peptida EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva 19-21, naznačen time što analog peptida EGF(A) je definiran kao analog peptida EGF(A) u skladu s bilo kojim od patentnih zahtjeva 5-12.
23. Analog peptida EGF(A) u skladu s bilo kojim od prethodnih patentnih zahtjeva 19-22, naznačen time što EGF(A) dodatno sadrži najmanje jednu zamjenu Lys koju se bira iz skupine koju čine: 292Lys, 293Lys, 294Lys, 296Lys, 299Lys, 300Lys, 303Lys, 305Lys, 306Lys, 309Lys, 311Lys, 313Lys, 314Lys, 315Lys, 316Lys, 318Lys, 320Lys, 321Lys, 322Lys, 323Lys, 324Lys, 325Lys, 326Lys, 327Lys, 328Lys, 329Lys, 330Lys, 332Lys i 333Lys.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2016070791 | 2016-01-13 | ||
| CN2016076580 | 2016-03-17 | ||
| EP16195965 | 2016-10-27 | ||
| PCT/EP2017/050668 WO2017121850A1 (en) | 2016-01-13 | 2017-01-13 | Egf(a) analogues with fatty acid substituents |
| EP17701078.2A EP3402811B1 (en) | 2016-01-13 | 2017-01-13 | Egf(a) analogues with fatty acid substituents |
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| Publication Number | Publication Date |
|---|---|
| HRP20220720T1 true HRP20220720T1 (hr) | 2022-09-30 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20220720TT HRP20220720T1 (hr) | 2016-01-13 | 2017-01-13 | Analozi egf(a) s masnim kiselinama kao supstituentima |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US10822385B2 (hr) |
| EP (1) | EP3402811B1 (hr) |
| JP (2) | JP6797926B2 (hr) |
| KR (1) | KR102417487B1 (hr) |
| CN (1) | CN108473550B (hr) |
| AU (1) | AU2017207862B2 (hr) |
| BR (1) | BR112018013820A2 (hr) |
| CA (1) | CA3010756A1 (hr) |
| CL (1) | CL2018001868A1 (hr) |
| CO (1) | CO2018007440A2 (hr) |
| DK (1) | DK3402811T3 (hr) |
| ES (1) | ES2916998T3 (hr) |
| HR (1) | HRP20220720T1 (hr) |
| HU (1) | HUE058647T2 (hr) |
| IL (1) | IL260043A (hr) |
| LT (1) | LT3402811T (hr) |
| MX (1) | MX2018008681A (hr) |
| MY (1) | MY195199A (hr) |
| PE (1) | PE20181376A1 (hr) |
| PH (1) | PH12018501502A1 (hr) |
| PL (1) | PL3402811T3 (hr) |
| RS (1) | RS63298B1 (hr) |
| RU (1) | RU2747877C2 (hr) |
| SA (1) | SA518391996B1 (hr) |
| SI (1) | SI3402811T1 (hr) |
| WO (1) | WO2017121850A1 (hr) |
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| KR20180098369A (ko) | 2016-01-13 | 2018-09-03 | 그뤼넨탈 게엠베하 | 3-((헤테로-)아릴)-알킬-8-아미노-2-옥소-1,3-디아자-스피로-[4.5]-데칸 유도체 |
| TWI640514B (zh) | 2016-01-13 | 2018-11-11 | 歌林達有限公司 | ３－（羧甲基）－８－胺基－２－側氧基－１，３－二氮－螺－［４．５］－癸烷衍生物 |
| RS60855B1 (sr) | 2016-01-13 | 2020-10-30 | Gruenenthal Gmbh | Derivati 8-amino-2-okso-1,3-diaza-spiro-[4.5]-dekana |
| EA037598B1 (ru) | 2016-01-13 | 2021-04-20 | Грюненталь Гмбх | Производные 3-((гетеро-)арил)-8-амино-2-оксо-1,3-диазаспиро[4,5]декана |
| LT3402811T (lt) | 2016-01-13 | 2022-06-10 | Novo Nordisk A/S | Egf(a) analogai su riebalų rūgščių pakaitais |
| BR112020001286A2 (pt) | 2017-07-19 | 2020-07-28 | Novo Nordisk A/S | composto, e, método de tratamento da diabetes, sobrepeso e/ou doenças cardiovasculares |
| MA49617A (fr) * | 2017-07-19 | 2020-05-27 | Novo Nordisk As | Analogues d'egf(a), préparation, formulations et utilisations associées |
| US11358994B2 (en) * | 2017-07-27 | 2022-06-14 | Saint Louis University | Fatty acid modified human epidermal growth factor |
| WO2020070276A1 (en) | 2018-10-05 | 2020-04-09 | Novo Nordisk A/S | Bifunctional compounds comprising insulin peptides and egf(a) peptides |
| JP2022527448A (ja) | 2019-03-22 | 2022-06-02 | スリーエム イノベイティブ プロパティズ カンパニー | 監視システムを有する落下防止システム |
| CN110357969B (zh) * | 2019-05-27 | 2022-03-08 | 北京志道生物科技有限公司 | 一种GLP1-EGFa异源二聚体蛋白、功能及方法 |
| CN114222581A (zh) | 2019-08-07 | 2022-03-22 | 诺和诺德股份有限公司 | 包含egf(a)衍生物和n-(8-(2-羟基苯甲酰基)氨基)辛酸的盐的固体组合物 |
| CA3154596A1 (en) | 2019-11-07 | 2021-05-14 | Simon Bjerregaard | Solid compositions comprising a pcsk9 inhibitor and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid |
| WO2023012263A1 (en) | 2021-08-04 | 2023-02-09 | Novo Nordisk A/S | Solid oral peptide formulations |
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| JP2009510999A (ja) | 2005-07-29 | 2009-03-19 | エーエムプロテイン コーポレイション | キメラ治療剤 |
| JP5721432B2 (ja) * | 2007-08-15 | 2015-05-20 | ノボ・ノルデイスク・エー／エス | アミノ酸含有アルキレングリコール反復単位を含むアシル部を有するインスリン |
| WO2009131740A2 (en) * | 2008-04-23 | 2009-10-29 | Amgen Inc. | Neutralizing proprotein convertase subtilisin kexin type 9 (pcsk9) variants and uses thereof |
| WO2009143633A1 (en) | 2008-05-30 | 2009-12-03 | Institut De Recherches Cliniques De Montreal | Pcsk9 inhibitors and methods of use thereof |
| TWI516501B (zh) * | 2008-09-12 | 2016-01-11 | 禮納特神經系統科學公司 | Ｐｃｓｋ９拮抗劑類 |
| CN101993485B (zh) | 2009-08-20 | 2013-04-17 | 重庆富进生物医药有限公司 | 促胰岛素分泌肽类似物同源二聚体及其用途 |
| US8939592B2 (en) | 2010-08-02 | 2015-01-27 | Nec Corporation | Polarizer and light-emitting device |
| CN102153652A (zh) | 2010-12-10 | 2011-08-17 | 浙江大学 | 一种融合蛋白的表达方法及用途 |
| EP2675470A1 (en) * | 2011-02-15 | 2013-12-25 | Novo Nordisk A/S | Long-acting il-1 receptor antagonists |
| CA2837658A1 (en) * | 2011-06-20 | 2012-12-27 | Genentech, Inc. | Pcsk9-binding polypeptides and methods of use |
| IN2014CN02448A (hr) * | 2011-09-23 | 2015-06-19 | Novo Nordisk As | |
| TW201315742A (zh) | 2011-09-26 | 2013-04-16 | Novartis Ag | 治療代謝病症之雙功能蛋白質 |
| JP2015502971A (ja) * | 2011-12-21 | 2015-01-29 | ノヴォ ノルディスク アー／エス | Ｎ末端修飾インスリン誘導体 |
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| AR092076A1 (es) | 2012-08-22 | 2015-03-18 | Lilly Co Eli | Proteinas homodimericas |
| KR20150043505A (ko) | 2012-09-07 | 2015-04-22 | 사노피 | 대사 증후군의 치료용 융합 단백질 |
| MX362275B (es) * | 2013-04-18 | 2019-01-10 | Novo Nordisk As | Co-agonista de peptido similar a glucagon tipo 1 (glp-1) receptor de glucagon de larga duracion, estables para uso medico. |
| US10323076B2 (en) | 2013-10-03 | 2019-06-18 | Modernatx, Inc. | Polynucleotides encoding low density lipoprotein receptor |
| CA2935285A1 (en) | 2014-02-21 | 2015-08-27 | Medimmune, Llc | Anti-pcsk9-glp-1 fusions and methods for use |
| CN106536547A (zh) * | 2014-06-04 | 2017-03-22 | 诺和诺德股份有限公司 | 用于医疗用途的glp‑1/胰高血糖素受体共激动剂 |
| CN104558198A (zh) | 2014-07-25 | 2015-04-29 | 成都贝爱特生物科技有限公司 | GLP-1类似物和amylin类似物的融合蛋白制备及其用途 |
| US20180207223A1 (en) * | 2015-03-19 | 2018-07-26 | Institut De Cardiologie De Montreal | Pcsk9 inhibitory polypolypeptides and methods of use |
| CN105367884A (zh) | 2015-11-02 | 2016-03-02 | 陈薇 | 一种绝缘耐火抗辐射的屏蔽电缆材料及其制备方法 |
| LT3402811T (lt) | 2016-01-13 | 2022-06-10 | Novo Nordisk A/S | Egf(a) analogai su riebalų rūgščių pakaitais |
| MA49617A (fr) | 2017-07-19 | 2020-05-27 | Novo Nordisk As | Analogues d'egf(a), préparation, formulations et utilisations associées |
| BR112020001286A2 (pt) | 2017-07-19 | 2020-07-28 | Novo Nordisk A/S | composto, e, método de tratamento da diabetes, sobrepeso e/ou doenças cardiovasculares |
-
2017
- 2017-01-13 LT LTEPPCT/EP2017/050668T patent/LT3402811T/lt unknown
- 2017-01-13 PL PL17701078T patent/PL3402811T3/pl unknown
- 2017-01-13 CA CA3010756A patent/CA3010756A1/en not_active Withdrawn
- 2017-01-13 WO PCT/EP2017/050668 patent/WO2017121850A1/en active Application Filing
- 2017-01-13 EP EP17701078.2A patent/EP3402811B1/en active Active
- 2017-01-13 DK DK17701078.2T patent/DK3402811T3/da active
- 2017-01-13 AU AU2017207862A patent/AU2017207862B2/en not_active Ceased
- 2017-01-13 MY MYPI2018702319A patent/MY195199A/en unknown
- 2017-01-13 PE PE2018001257A patent/PE20181376A1/es unknown
- 2017-01-13 ES ES17701078T patent/ES2916998T3/es active Active
- 2017-01-13 BR BR112018013820-7A patent/BR112018013820A2/pt not_active Application Discontinuation
- 2017-01-13 RU RU2018127882A patent/RU2747877C2/ru active
- 2017-01-13 JP JP2018536444A patent/JP6797926B2/ja active Active
- 2017-01-13 US US16/069,932 patent/US10822385B2/en active Active
- 2017-01-13 RS RS20220538A patent/RS63298B1/sr unknown
- 2017-01-13 CN CN201780006783.6A patent/CN108473550B/zh active Active
- 2017-01-13 MX MX2018008681A patent/MX2018008681A/es unknown
- 2017-01-13 KR KR1020187022105A patent/KR102417487B1/ko active IP Right Grant
- 2017-01-13 HR HRP20220720TT patent/HRP20220720T1/hr unknown
- 2017-01-13 SI SI201731149T patent/SI3402811T1/sl unknown
- 2017-01-13 HU HUE17701078A patent/HUE058647T2/hu unknown
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2018
- 2018-06-14 IL IL260043A patent/IL260043A/en unknown
- 2018-07-09 CL CL2018001868A patent/CL2018001868A1/es unknown
- 2018-07-10 SA SA518391996A patent/SA518391996B1/ar unknown
- 2018-07-12 PH PH12018501502A patent/PH12018501502A1/en unknown
- 2018-07-16 CO CONC2018/0007440A patent/CO2018007440A2/es unknown
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2020
- 2020-09-17 US US17/024,264 patent/US20200407409A1/en not_active Abandoned
- 2020-11-17 JP JP2020190846A patent/JP2021035989A/ja not_active Withdrawn
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