EA200301295A1 - Полипептид, его конъюгат с доксорубицином и фармацевтическая композиция на его основе - Google Patents
Полипептид, его конъюгат с доксорубицином и фармацевтическая композиция на его основеInfo
- Publication number
- EA200301295A1 EA200301295A1 EA200301295A EA200301295A EA200301295A1 EA 200301295 A1 EA200301295 A1 EA 200301295A1 EA 200301295 A EA200301295 A EA 200301295A EA 200301295 A EA200301295 A EA 200301295A EA 200301295 A1 EA200301295 A1 EA 200301295A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- conjugate
- polypeptide
- inventive
- pharmaceutical composition
- growth factor
- Prior art date
Links
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 title abstract 4
- 229920001184 polypeptide Polymers 0.000 title abstract 3
- 102000004196 processed proteins & peptides Human genes 0.000 title abstract 3
- 108090000765 processed proteins & peptides Proteins 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229960004679 doxorubicin Drugs 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 abstract 3
- 102400001368 Epidermal growth factor Human genes 0.000 abstract 2
- 101800003838 Epidermal growth factor Proteins 0.000 abstract 2
- 239000002246 antineoplastic agent Substances 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 229940116977 epidermal growth factor Drugs 0.000 abstract 2
- 210000004881 tumor cell Anatomy 0.000 abstract 2
- VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 abstract 2
- 238000005903 acid hydrolysis reaction Methods 0.000 abstract 1
- 235000001014 amino acid Nutrition 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000012634 fragment Substances 0.000 abstract 1
- 238000010253 intravenous injection Methods 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
-
- 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
- A61K47/62—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 a protein, peptide or polyamino acid
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
- A61K47/642—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent the peptide or protein in the drug conjugate being a cytokine, e.g. IL2, chemokine, growth factors or interferons being the inactive part of the conjugate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07K14/475—Growth factors; Growth regulators
- C07K14/485—Epidermal growth factor [EGF], i.e. urogastrone
-
- 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
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Biophysics (AREA)
- Gastroenterology & Hepatology (AREA)
- Genetics & Genomics (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Abstract
Предложен полипептид, являющийся аналогом фрагмента эпидермального фактора роста с 21 по 31 аминокислоту, способный эффективно связываться с рецептором эпидермального фактора роста, в качестве вектора для направленной доставки противоопухолевых препаратов в опухолевые клетки. Предложен также конъюгат полипептида с доксорубицином, обладающий избирательным действием в отношении раковых опухолей и способный значительно снижать резистентность опухолевых клеток к противовопухолевым препаратам, в котором конъюгированные части соединены неустойчивой к гидролизу химической связью. Фармацевтическая композиция содержит эффективное количество конъюгата и носитель, пригодный для внутривенного введения. Изобретение может быть использовано в медицине для лечения онкологических больных.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
RU2001134536/14A RU2196604C1 (ru) | 2001-12-21 | 2001-12-21 | Полипептид, являющийся аналогом рецепторсвязывающего фрагмента эпидермального фактора роста с 21-й по 31-ю аминокислоту, его конъюгат с доксорубицином и фармацевтическая композиция на его основе |
PCT/RU2002/000544 WO2003053457A1 (fr) | 2001-12-21 | 2002-12-20 | Polypeptide, son conjugue avec doxorubicine et composition pharmaceutique sur cette base |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200301295A1 true EA200301295A1 (ru) | 2004-10-28 |
EA005865B1 EA005865B1 (ru) | 2005-06-30 |
Family
ID=20254793
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200301295A EA005865B1 (ru) | 2001-12-21 | 2002-12-20 | Аналог фрагмента эпидермального фактора роста, его конъюгат с доксорубицином и фармацевтическая композиция на основе конъюгата |
Country Status (13)
Country | Link |
---|---|
US (1) | US7368431B2 (ru) |
EP (1) | EP1466614B1 (ru) |
JP (1) | JP2005513108A (ru) |
CN (1) | CN1281270C (ru) |
AT (1) | ATE411051T1 (ru) |
AU (1) | AU2002362210B9 (ru) |
CA (1) | CA2451993A1 (ru) |
DE (1) | DE50212918D1 (ru) |
EA (1) | EA005865B1 (ru) |
HK (1) | HK1076601A1 (ru) |
NZ (1) | NZ533849A (ru) |
RU (1) | RU2196604C1 (ru) |
WO (1) | WO2003053457A1 (ru) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100824396B1 (ko) * | 2006-10-10 | 2008-04-22 | (주)케어젠 | 상피세포 성장인자의 활성을 가지는 펩타이드 및 그의 용도 |
WO2009059450A1 (en) * | 2007-11-05 | 2009-05-14 | Shanghai Jiaotong University | Peptide ligand directed drug delivery |
CN101274100B (zh) * | 2008-02-20 | 2010-11-24 | 中山大学 | 一种阿霉素-二肽复合物的制备方法和应用 |
DE102008050347B4 (de) * | 2008-10-02 | 2011-01-20 | Siemens Aktiengesellschaft | Verfahren, Magnetresonanzanlage und Datenträger zur Bestimmung eines Nierenfunktionsparameters |
CN102905762B (zh) | 2010-04-29 | 2017-02-15 | 陶氏环球技术有限责任公司 | 用于诱导饱腹感的方法和组合物 |
CN110386962A (zh) * | 2019-07-04 | 2019-10-29 | 苏州强耀生物科技有限公司 | 一种阿霉素偶联靶向多肽的合成方法 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL69719A0 (en) * | 1983-09-14 | 1983-12-30 | Yeda Res & Dev | Synthetic peptides with egf like activity |
CA1275922C (en) | 1985-11-28 | 1990-11-06 | Harunobu Amagase | Treatment of cancer |
IN165717B (ru) | 1986-08-07 | 1989-12-23 | Battelle Memorial Institute | |
FI102355B (fi) | 1988-02-11 | 1998-11-30 | Squibb Bristol Myers Co | Menetelmä yhdistävän välikappaleen omaavien antrasykliini-immunokonjug aattien valmistamiseksi |
DE4002888A1 (de) * | 1990-02-01 | 1991-08-08 | Behringwerke Ag | Anthracyclin-glycosyl-prodrugs, verfahren zu ihrer herstellung und ihre verwendung in kombination mit funktionalisierten tumorspezifischen enzymkonjugaten |
US5137877B1 (en) | 1990-05-14 | 1996-01-30 | Bristol Myers Squibb Co | Bifunctional linking compounds conjugates and methods for their production |
US5183805A (en) | 1990-08-13 | 1993-02-02 | Board Of Regents, The University Of Texas System | Bioactive egf peptides for promotion of tissue regeneration and cancer therapy |
GB9026491D0 (en) * | 1990-12-05 | 1991-01-23 | Erba Carlo Spa | Anthracycline-conjugates |
US5776458A (en) | 1990-12-05 | 1998-07-07 | Pharmacia & Upjohn S.P.A. | Anthracycline-conjugates |
US5622929A (en) | 1992-01-23 | 1997-04-22 | Bristol-Myers Squibb Company | Thioether conjugates |
US5505931A (en) | 1993-03-04 | 1996-04-09 | The Dow Chemical Company | Acid cleavable compounds, their preparation and use as bifunctional acid-labile crosslinking agents |
US5393737A (en) | 1992-08-20 | 1995-02-28 | Health Research, Inc. | Cytotoxic drug conjugates for treatment of neoplastic diseases |
GB9500660D0 (en) * | 1995-01-13 | 1995-03-08 | Secr Defence | Growth factor anologs |
ATE234635T1 (de) * | 1995-12-22 | 2003-04-15 | Bristol Myers Squibb Co | Verzweigte hydrazongruppen enthaltende kuppler |
-
2001
- 2001-12-21 RU RU2001134536/14A patent/RU2196604C1/ru not_active IP Right Cessation
-
2002
- 2002-12-20 EP EP02796999A patent/EP1466614B1/de not_active Expired - Lifetime
- 2002-12-20 NZ NZ533849A patent/NZ533849A/en unknown
- 2002-12-20 JP JP2003554214A patent/JP2005513108A/ja not_active Ceased
- 2002-12-20 EA EA200301295A patent/EA005865B1/ru not_active IP Right Cessation
- 2002-12-20 DE DE50212918T patent/DE50212918D1/de not_active Expired - Fee Related
- 2002-12-20 AU AU2002362210A patent/AU2002362210B9/en not_active Ceased
- 2002-12-20 CA CA002451993A patent/CA2451993A1/en not_active Abandoned
- 2002-12-20 AT AT02796999T patent/ATE411051T1/de not_active IP Right Cessation
- 2002-12-20 CN CNB028256557A patent/CN1281270C/zh not_active Expired - Fee Related
- 2002-12-20 WO PCT/RU2002/000544 patent/WO2003053457A1/ru active Application Filing
-
2004
- 2004-06-21 US US10/872,827 patent/US7368431B2/en not_active Expired - Fee Related
-
2005
- 2005-09-29 HK HK05108573A patent/HK1076601A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
EP1466614A4 (de) | 2006-05-24 |
US20050070465A1 (en) | 2005-03-31 |
AU2002362210A1 (en) | 2003-07-09 |
CA2451993A1 (en) | 2003-07-03 |
JP2005513108A (ja) | 2005-05-12 |
RU2196604C1 (ru) | 2003-01-20 |
CN1606450A (zh) | 2005-04-13 |
EA005865B1 (ru) | 2005-06-30 |
DE50212918D1 (de) | 2008-11-27 |
AU2002362210B2 (en) | 2008-04-03 |
AU2002362210B9 (en) | 2008-08-21 |
AU2002362210B8 (en) | 2008-04-24 |
ATE411051T1 (de) | 2008-10-15 |
NZ533849A (en) | 2006-09-29 |
EP1466614B1 (de) | 2008-10-15 |
EP1466614A1 (de) | 2004-10-13 |
WO2003053457A1 (fr) | 2003-07-03 |
WO2003053457A8 (fr) | 2004-09-16 |
CN1281270C (zh) | 2006-10-25 |
US7368431B2 (en) | 2008-05-06 |
HK1076601A1 (en) | 2006-01-20 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): KZ KG TJ TM |
|
PC4A | Registration of transfer of a eurasian patent by assignment | ||
MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY MD RU |