HRP20211342T1 - Analozi kompstatina sa produženim trajanjem djelovanja i njihovi sastavi i postupci - Google Patents
Analozi kompstatina sa produženim trajanjem djelovanja i njihovi sastavi i postupci Download PDFInfo
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- HRP20211342T1 HRP20211342T1 HRP20211342TT HRP20211342T HRP20211342T1 HR P20211342 T1 HRP20211342 T1 HR P20211342T1 HR P20211342T T HRP20211342T T HR P20211342TT HR P20211342 T HRP20211342 T HR P20211342T HR P20211342 T1 HRP20211342 T1 HR P20211342T1
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- Prior art keywords
- compstatin analog
- composition
- lys
- residue
- aeeac
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- RDTRHBCZFDCUPW-KWICJJCGSA-N 2-[(4r,7s,10s,13s,19s,22s,25s,28s,31s,34r)-4-[[(2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-34-[[(2s,3s)-2-amino-3-methylpentanoyl]amino]-25-(3-amino-3-oxopropyl)-7-[3-(diaminomethylideneamino)propyl]-10,13-bis(1h-imidazol-5-ylmethyl)-19-(1h-indol Chemical class C([C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CSSC[C@@H](C(N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)NCC(=O)N[C@@H](CC=2NC=NC=2)C(=O)N1)C(C)C)C(C)C)=O)NC(=O)[C@@H](N)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)C1=CN=CN1 RDTRHBCZFDCUPW-KWICJJCGSA-N 0.000 title claims 18
- 239000000203 mixture Substances 0.000 title claims 13
- 206010064930 age-related macular degeneration Diseases 0.000 claims 4
- 230000001588 bifunctional effect Effects 0.000 claims 3
- 208000008069 Geographic Atrophy Diseases 0.000 claims 2
- 208000000733 Paroxysmal Hemoglobinuria Diseases 0.000 claims 2
- 102100036050 Phosphatidylinositol N-acetylglucosaminyltransferase subunit A Human genes 0.000 claims 2
- 230000000295 complement effect Effects 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 201000003045 paroxysmal nocturnal hemoglobinuria Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000007475 hemolytic anemia Diseases 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000008795 neuromyelitis optica Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 210000000278 spinal cord Anatomy 0.000 claims 1
- 238000007920 subcutaneous administration Methods 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
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/005—Enzyme inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/10—Peptides having 12 to 20 amino acids
-
- 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
- A61K47/54—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 organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- 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
- A61K47/54—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 organic compound
- A61K47/55—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 organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- 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
- A61K47/56—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
- C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
- C07K14/472—Complement proteins, e.g. anaphylatoxin, C3a, C5a
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Claims (12)
1. Analog kompstatina sadrži:
linearni PEG ostatak koji ima molekularnu masu od 40 kD i spregnut je za svaki od dva ostatka analoga kompstatina;
gdje:
i) svaki ostatak analoga kompstatina je ostatak CA28-AEEAc-Lys ;
ii) linearni PEG ostatak je spregnut za bočni lanac Lys svakog ostatka CA28-AEEAc-Lys preko amidne veze; i
iii) svaki ostatak CA28-AEEAc-Lys je Ac-He-Cys*-Val-(1Me)Trp-Gln-Asp-Trp-Gly-Ala-His-Arg-Cys*-Thr-[NH-CH2CH2OCH2CH2OCH2-C(=O)]-Lys-NH2 (SEQ ID NO: 51); gdje Cys* grupe su spojene disulfidnom vezom.
2. Analog kompstatina dobiven spregnućem dva ostatka CA28-AEEAc-Lys za bifunkcionalni linearni ostatak PEG-a koji ima molekularnu masu od 40 kDa; gdje:
i) bifunkcionalni linearni PEG ostatak je spregnut za bočni lanac Lys svakog ostatka CA28-AEEAc-Lys preko amidne veze; i
ii) svaki ostatak CA28-AEEAc-Lys je Ac-Ile-Cys*-Val-(1Me)Trp-Gln-Asp-Trp-Gly-Ala-His-Arg-Cys*-Thr-[NH-CH2CH2OCH2CH2OCH2-C(=O)]-Lys-NH2 (SEQ ID NO: 51); gdje Cys* grupe su spojene disulfidnom vezom.
3. Analog kompstatina prema zahtjevu 2, gdje spomenuti bifunkcionalni linearni PEG ostatak ima Formulu IVa:
[image]
4. Sastav koji sadrži analog kompstatina prema bilo kojem od zahtjeva 1 do 3, i farmaceutski prihvatljiv nositelj.
5. Analog kompstatina prema bilo kojem od zahtjeva 1 do 3, ili sastav prema zahtjevu 4, za upotrebu kao lijek.
6. Analog kompstatina prema bilo kojem od zahtjeva 1 do 3, ili sastav prema zahtjevu 4, za upotrebu u smanjivanju osjetljivosti stanice ili organa na oštećenje ovisno o komplementima.
7. Analog kompstatina prema bilo kojem od zahtjeva 1 do 3, ili sastav prema zahtjevu 4, za upotrebu u liječenju poremećaja posredovanog komplementom.
8. Analog kompstatina prema bilo kojem od zahtjeva 1 do 3, ili sastav prema zahtjevu 4, za upotrebu u liječenju ili prevenciji starosne makularne degeneracije (AMD) ili geografske atrofije (GA) kod subjekta kojem je to potrebno.
9. Analog kompstatina za upotrebu ili sastav za upotrebu prema zahtjevu 8, gdje spomenuta upotreba obuhvaća davanje spomenutog analoga kompstatina ili spomenutog sastava u oko spomenutog subjekta.
10. Analog kompstatina za upotrebu ili sastav za upotrebu prema zahtjevu 9, gdje spomenuta upotreba obuhvaća davanje spomenutog analoga kompstatina ili spomenutog sastava intravitrealnim davanjem.
11. Analog kompstatina prema bilo kojem od zahtjeva 1 do 3, ili sastav prema zahtjevu 4, za upotrebu u liječenju odbacivanja transplanta; ishemijskog/reperfuzijskog oštećenja; hemolitičke anemije, autoimune bolesti; neuropatskog bola; membranoproliferativnog glomerulitisa; neuromijelitisa optika; oštećenja leđne moždine; astme, paroksizmalne nokturalne hemoglobinurije (PNH), ili kronične opstruktivne bolesti pluća (COPD).
12. Analog kompstatina za upotrebu ili sastav za upotrebu prema bilo kojem od zahtjeva 5 do 7 ili 11, gdje spomenuta upotreba obuhvaća davanje spomenutog analoga kompstatina ili sastava subkutanoznim ili intravenskim davanjem.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261727094P | 2012-11-15 | 2012-11-15 | |
EP19205426.0A EP3660033B9 (en) | 2012-11-15 | 2013-11-15 | Long-acting compstatin analogs and related compositions and methods |
Publications (2)
Publication Number | Publication Date |
---|---|
HRP20211342T1 true HRP20211342T1 (hr) | 2021-11-26 |
HRP20211342T2 HRP20211342T2 (hr) | 2022-08-19 |
Family
ID=50731833
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20211342TT HRP20211342T2 (hr) | 2012-11-15 | 2013-11-15 | Analozi kompstatina sa produženim trajanjem djelovanja i njihovi sastavi i postupci |
Country Status (24)
Country | Link |
---|---|
US (4) | US10035822B2 (hr) |
EP (3) | EP2920201B1 (hr) |
JP (4) | JP2016505527A (hr) |
CN (2) | CN105051057B (hr) |
AU (4) | AU2013344462B2 (hr) |
BR (1) | BR112015011244B1 (hr) |
CA (1) | CA2891673A1 (hr) |
CY (1) | CY1124474T1 (hr) |
DK (2) | DK2920201T3 (hr) |
ES (2) | ES2780674T3 (hr) |
FR (1) | FR22C1025I2 (hr) |
HK (2) | HK1215445A1 (hr) |
HR (1) | HRP20211342T2 (hr) |
HU (2) | HUE055564T2 (hr) |
IL (2) | IL238852A0 (hr) |
LT (2) | LT3660033T (hr) |
MX (2) | MX366404B (hr) |
NO (1) | NO2022017I1 (hr) |
PL (2) | PL2920201T3 (hr) |
PT (2) | PT3660033T (hr) |
RS (1) | RS62243B9 (hr) |
RU (1) | RU2705215C2 (hr) |
SI (1) | SI3660033T1 (hr) |
WO (1) | WO2014078731A2 (hr) |
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EP4105224A1 (en) | 2011-05-11 | 2022-12-21 | Apellis Pharmaceuticals, Inc. | Long-acting compstatin analogs and uses thereof |
PT3660033T (pt) | 2012-11-15 | 2021-07-06 | Apellis Pharmaceuticals Inc | Análogos de compstatina de longa ação e composições e métodos relacionados |
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WO2020069024A1 (en) | 2018-09-25 | 2020-04-02 | Achillion Pharmaceuticals, Inc. | Morphic forms of complement factor d inhibitors |
WO2020109343A1 (en) | 2018-11-29 | 2020-06-04 | F. Hoffmann-La Roche Ag | Combination therapy for treatment of macular degeneration |
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