DK2598526T3 - Kimæriske il-1-receptortype-i-agonister og -antagonister - Google Patents

Kimæriske il-1-receptortype-i-agonister og -antagonister Download PDF

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DK2598526T3
DK2598526T3 DK11749612.5T DK11749612T DK2598526T3 DK 2598526 T3 DK2598526 T3 DK 2598526T3 DK 11749612 T DK11749612 T DK 11749612T DK 2598526 T3 DK2598526 T3 DK 2598526T3
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Thomas M Barnes
Jinzhao Hou
Bracken M King
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Eleven Biotherapeutics Inc
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    • 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
    • C07K14/52—Cytokines; Lymphokines; Interferons
    • C07K14/54—Interleukins [IL]
    • C07K14/545—IL-1
    • 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
    • A61K38/19—Cytokines; Lymphokines; Interferons
    • A61K38/20—Interleukins [IL]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Claims (30)

1. Isoleret protein, der omfatter et kimærisk interleukin-1 - (IL-1) familiecytokindomæne, hvor cytokindomænet har en aminosyresekvens, der er mindst 90 % identisk med en sekvens udvalgt fra en hvilken som helst af SEQ ID NO: 17 (P01), SEQ ID NO: 18 (P02), SEQ ID NO: 19 (P03), SEQ ID NO: 20 (P04) og SEQ ID NO: 21 (P05); og hvor det isolerede protein binder til IL-1-receptor-1 (IL-1 RI) og antagoniserer IL-1 Rl-receptorsignaleringsaktivitet.
2. Isoleret protein ifølge krav 1, hvor cytokindomænet har en aminosyresekvens, der er mindst 95 % identisk med en sekvens udvalgt fra en hvilken som helst af SEQ ID NO: 17 (P01), SEQ ID NO: 18 (P02), SEQ ID NO: 19 (P03), SEQ ID NO: 20 (P04) og SEQ ID NO: 21 (P05).
3. Isoleret protein ifølge krav 2, hvor cytokindomænet har en aminosyresekvens udvalgt fra en hvilken som helst af SEQ ID NO: 17 (P01), SEQ ID NO: 18 (P02), SEQ ID NO: 19 (P03), SEQ ID NO: 20 (P04) og SEQ ID NO: 21 (P05).
4. Isoleret protein ifølge krav 1, hvor cytokindomænet har en aminosyresekvens, der er mindst 90 % eller 95 % identisk med en sekvens udvalgt fra en hvilken som helst af SEQ ID NO: 19 (P03), SEQ ID NO: 20 (P04) og SEQ ID NO: 21 (P05), og hvor cytokindomænet har en større termostabilitet end human IL-Ιβ og human IL-1 Ra i en fysiologisk buffer.
5. Isoleret protein ifølge krav 4, hvor cytokindomænet omfatter følgende restpar: (i) E39 og K64; (ii) R9 og Q149, og (iii) S152 og K40.
6. Isoleret protein ifølge krav 5, hvor cytokindomænet har en aminosyresekvens udvalgt fra en hvilken som helst af SEQ ID NO: 19 (P03), SEQ ID NO: 20 (P04) og SEQ ID NO: 21 (P05).
7. Isoleret protein ifølge et hvilket som helst af kravene 4 til 6, hvor cytokindomænet har en Tm, der er mindst 2 °C højere end Tm for human IL-Ιβ og human IL-1Ra ved en koncentration på ca. 0,5 mg/ml.
8. Isoleret protein ifølge et hvilket som helst af kravene 4 til 7, hvor cytokindomænet har en Tm mellem 5-12 °C højere end Tm for human IL-Ιβ og human IL-1 Raved en koncentration på ca. 0,5 mg/ml.
9. Isoleret protein ifølge et hvilket som helst af kravene 1 til 8, hvor cytokindomænet har en aminosyresekvens, der er mindst 91,92, 93, 94, 95, 96, 97, 98, 99 %, eller 100 % identisk med sekvensen ifølge SEQ ID NO: 21 (P05).
10. Isoleret protein ifølge krav 9, hvor proteinet har sekvensen ifølge SEQ ID NO: 21 (P05).
11. Isoleret protein ifølge et hvilket som helst af kravene 1 til 10, hvor proteinet omfatter færre end 15, 12, 11, 10, 9, 8, 7, 6, 5, 4, 3 eller 2 substitutioner.
12. Isoleret protein ifølge et hvilket som helst af kravene 1 til 11, hvor cytokindomænet binder til IL-1-receptor-1 med en Kd på mindre end 100 nM.
13. Isoleret protein, der omfatter et kimærisk interleukin-1 - (IL-1) familiecytokindomæne, hvor cytokindomænet har en aminosyresekvens, der er mindst 90 % identisk med sekvensen ifølge SEQ ID NO: 23 (P06) eller SEQ ID NO: 24 (P07), og hvor det isolerede protein binder til IL-1-receptor-1 (IL-1 RI) og agoniserer IL-1 Rl-receptorsignalleringsaktivitet.
14. Isoleret protein ifølge krav 13, hvor cytokindomænet har en aminosyresekvens, der er mindst 95 % identisk med sekvensen ifølge SEQ ID NO: 23 (P06) eller SEQ ID NO: 24 (P07).
15. Isoleret protein ifølge krav 14, hvor cytokindomænet har aminosyresekvensen ifølge SEQ ID NO: 23 (P06) eller SEQ ID NO: 24 (P07).
16. Isoleret protein ifølge et hvilket som helst af kravene 13 til 15, hvor proteinet omfatter færre end 15, 12, 11, 10, 9, 8, 7, 6, 5, 4, 3 eller 2 substitutioner.
17. Farmaceutisk sammensætning, der omfatter et protein ifølge et hvilket som helst af kravene 1 til 12.
18. Farmaceutisk sammensætning ifølge krav 17, hvor den farmaceutiske sammensætning er en topisk farmaceutisk sammensætning.
19. Farmaceutisk sammensætning ifølge krav 17, hvor den farmaceutiske sammensætning er en oftalmisk farmaceutisk sammensætning.
20. Farmaceutisk sammensætning ifølge et hvilket som helst af kravene 17 til 19, hvor den farmaceutiske sammensætning er vandig og omfatter proteinet ved en koncentration på mellem 0,001 - 5 %.
21. Farmaceutisk sammensætning, der omfatter et protein ifølge et hvilket som helst af kravene 13 til 16.
22. Farmaceutisk sammensætning ifølge krav 21, hvor den farmaceutiske sammensætning er en topisk farmaceutisk sammensætning.
23. Farmaceutisk sammensætning ifølge krav 21, hvor den farmaceutiske sammensætning er en oftalmisk farmaceutisk sammensætning.
24. Farmaceutisk sammensætning ifølge et hvilket som helst af kravene 21 til 23, hvor den farmaceutiske sammensætning er vandig og omfatter proteinet ved en koncentration på mellem 0,001 - 5 %.
25. Farmaceutisk sammensætning ifølge et hvilket som helst af kravene 17 til 20 til anvendelse som et lægemiddel.
26. Farmaceutisk sammensætning ifølge et hvilket som helst af kravene 17 til 20 til anvendelse i behandling af tørre øjne-sygdom eller -forstyrrelse, allergisk conjunctivitis eller reumatoid artritis hos et individ.
27. Isoleret nukleinsyre, der omfatter en sekvens, der koder for proteinet ifølge et hvilket som helst af kravene 1 til 16.
28. Isoleret nukleinsyrevektor, der omfatter nukleinsyren ifølge krav 27, hvor sekvensen er operativt forbundet med en transskriptionsstyringssekvens.
29. Rekombinant værtscelle, der omfatter en rekombinant nukleinsyre, der koder for proteinet ifølge et hvilket som helst af kravene 1 til 16.
30. Rekombinant værtscelle ifølge krav 29, hvor værtscellen er en E. co//-værtscelle.
DK11749612.5T 2010-07-29 2011-07-29 Kimæriske il-1-receptortype-i-agonister og -antagonister DK2598526T3 (da)

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US36879910P 2010-07-29 2010-07-29
US201161436178P 2011-01-25 2011-01-25
US201161436184P 2011-01-25 2011-01-25
US201161493967P 2011-06-06 2011-06-06
US201161493966P 2011-06-06 2011-06-06
PCT/US2011/045995 WO2012016203A1 (en) 2010-07-29 2011-07-29 Chimeric il-1 receptor type i agonists and antagonists

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EP (3) EP4219538A3 (da)
JP (1) JP6030554B2 (da)
KR (1) KR102080704B1 (da)
CN (2) CN103221422B (da)
AU (3) AU2011283669A1 (da)
BR (1) BR112013003646B1 (da)
CA (1) CA2806438C (da)
DK (1) DK2598526T3 (da)
ES (2) ES2952394T3 (da)
HK (1) HK1246327A1 (da)
HR (2) HRP20230776T1 (da)
HU (2) HUE063115T2 (da)
IL (2) IL224435B (da)
LT (1) LT2598526T (da)
MX (1) MX360097B (da)
NZ (1) NZ605928A (da)
PL (2) PL3470421T3 (da)
RU (2) RU2013108836A (da)
SG (1) SG187231A1 (da)
SI (1) SI2598526T1 (da)
WO (1) WO2012016203A1 (da)
ZA (1) ZA201505145B (da)

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