RU2018129760A - Фармацевтический препарат, содержащий полимерное производное на основе камптотецина - Google Patents
Фармацевтический препарат, содержащий полимерное производное на основе камптотецина Download PDFInfo
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- RU2018129760A RU2018129760A RU2018129760A RU2018129760A RU2018129760A RU 2018129760 A RU2018129760 A RU 2018129760A RU 2018129760 A RU2018129760 A RU 2018129760A RU 2018129760 A RU2018129760 A RU 2018129760A RU 2018129760 A RU2018129760 A RU 2018129760A
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- hydrogen atom
- polyglutamic acid
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- 239000000825 pharmaceutical preparation Substances 0.000 title claims 4
- 229940127557 pharmaceutical product Drugs 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 108010020346 Polyglutamic Acid Proteins 0.000 claims 4
- 229920002643 polyglutamic acid Polymers 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 229920001400 block copolymer Polymers 0.000 claims 3
- 125000000291 glutamic acid group Chemical group N[C@@H](CCC(O)=O)C(=O)* 0.000 claims 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical class C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 2
- 125000006823 (C1-C6) acyl group Chemical group 0.000 claims 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 125000001302 tertiary amino group Chemical group 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- 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
- A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/74—Synthetic polymeric materials
- A61K31/785—Polymers containing nitrogen
- A61K31/787—Polymers containing nitrogen containing heterocyclic rings having nitrogen as a ring hetero atom
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- 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
- 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
-
- 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
- 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
- A61K47/02—Inorganic 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (17)
1. Фармацевтический препарат, содержащий:
блок-сополимер полиэтиленгликолевого сегмента и сегмента полиглутаминовой кислоты, соединенных вместе, при этом указанный сегмент полиглутаминовой кислоты содержит звено глутаминовой кислоты, содержащее связанное с ним производное камптотецина; и
одну или более добавок, выбранных из группы, состоящей из аргинина, гистидина и хлорида натрия,
при этом указанный блок-сополимер представляет собой блок-сополимер, представленный общей формулой (1):
где
R1 представляет собой атом водорода или необязательно замещенную (С1-С6) алкильную группу;
А представляет собой (С1-С6) алкиленовую группу;
R2 представляет собой любую группу, выбранную из группы, состоящей из атома водорода, необязательно замещенной (С1-С6) ацильной группы и необязательно замещенной (С1-С6) алкоксикарбонильной группы;
R3 представляет собой водородную группу и/или -N(R6)CONH(R7);
R6 и R7, которые могут быть одинаковыми или разными, каждый представляют собой (С1-С8) алкильную группу, которая может содержать третичную аминогруппу;
R4 представляет собой любую группу, выбранную из группы, состоящей из атома водорода, необязательно замещенной (С1-С6) алкильной группы и необязательно замещенной силильной группы;
R5 представляет собой атом водорода или необязательно замещенную (С1-С6) алкильную группу;
t представляет собой целое число от 45 до 450;
d и е каждый представляют собой целое число; d+е представляет собой целое число от 6 до 60; доля d относительно d+е составляет от 1% до 100%; доля е составляет от 0% до 99%; и
сегмент полиглутаминовой кислоты имеет структуру сегмента полиглутаминовой кислоты, в которой звенья глутаминовой кислоты, содержащие связанное с ними производное камптотецина, и звенья глутаминовой кислоты, содержащие связанную с ними R3 группу, каждое независимо расположены произвольным образом.
2. Фармацевтический препарат по п. 1, отличающийся тем, что указанный фармацевтический препарат представляет собой лиофилизированный препарат.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2016-038943 | 2016-03-01 | ||
| JP2016038943 | 2016-03-01 | ||
| PCT/JP2017/006192 WO2017150256A1 (ja) | 2016-03-01 | 2017-02-20 | カンプトテシン類高分子誘導体を含有する医薬製剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2018129760A true RU2018129760A (ru) | 2020-04-01 |
| RU2018129760A3 RU2018129760A3 (ru) | 2020-04-01 |
Family
ID=59743985
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018129760A RU2018129760A (ru) | 2016-03-01 | 2017-02-20 | Фармацевтический препарат, содержащий полимерное производное на основе камптотецина |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20190046653A1 (ru) |
| EP (1) | EP3424513A4 (ru) |
| JP (1) | JP6797182B2 (ru) |
| KR (1) | KR20180114027A (ru) |
| CN (1) | CN108697806A (ru) |
| AU (1) | AU2017226131A1 (ru) |
| CA (1) | CA3015459A1 (ru) |
| RU (1) | RU2018129760A (ru) |
| TW (1) | TW201731510A (ru) |
| WO (1) | WO2017150256A1 (ru) |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20030023697A (ko) | 2000-07-13 | 2003-03-19 | 다이이찌 세이야꾸 가부시기가이샤 | Dds 화합물을 함유하는 의약 조성물 |
| TW200306314A (en) * | 2002-04-16 | 2003-11-16 | Tanabe Seiyaku Co | Liquid preparation comprising camptothecin derivative and pharmaceutical composition producible by lyophilizing the preparation |
| CN1309763C (zh) * | 2002-10-31 | 2007-04-11 | 日本化药株式会社 | 喜树碱的高分子衍生物 |
| US20060029551A1 (en) * | 2004-08-05 | 2006-02-09 | Kui Liu | Stable particle formulations of erythropoietin receptor agonists |
| EP2042195A1 (en) | 2006-07-19 | 2009-04-01 | Nippon Kayaku Kabushiki Kaisha | Polymer conjugate of combretastatin |
| WO2008041610A1 (fr) | 2006-10-03 | 2008-04-10 | Nippon Kayaku Kabushiki Kaisha | Mélange d'un dérivé de résorcinol avec un polymère |
| WO2008056596A1 (fr) | 2006-11-06 | 2008-05-15 | Nippon Kayaku Kabushiki Kaisha | Dérivé polymère d'un antagoniste métabolique d'acide nucléique |
| CN101156854A (zh) * | 2007-09-19 | 2008-04-09 | 哈尔滨峰源高科技开发有限公司 | 喜树碱类药物缓释微胶囊的制备方法 |
| US20110293515A1 (en) * | 2009-01-13 | 2011-12-01 | The Uab Research Foundation | Heterofunctional segment-poly (ethylene glycol) polymers as delivery vehicles |
| US9855261B2 (en) * | 2012-11-08 | 2018-01-02 | Nippon Kayaku Kabushiki Kaisha | Polymeric compound having camptothecin compound and anti-cancer effect enhancer bound thereto, and use of same |
| WO2015125640A1 (ja) * | 2014-02-19 | 2015-08-27 | 日本化薬株式会社 | カンプトテシン誘導体とhsp90阻害剤の結合した高分子化合物及びその用途 |
| WO2015125641A1 (ja) * | 2014-02-19 | 2015-08-27 | 日本化薬株式会社 | 高分子化カンプトテシン誘導体及び高分子化hsp90阻害剤誘導体を含む医薬組成物 |
| CA2969196C (en) * | 2014-12-26 | 2021-04-13 | Nippon Kayaku Kabushiki Kaisha | Pharmaceutical preparation of camptothecin-containing polymer derivative |
| EP3263107B1 (en) * | 2015-02-23 | 2020-11-11 | Nippon Kayaku Kabushiki Kaisha | Block copolymer conjugate of physiologically active substance |
| WO2017038607A1 (ja) * | 2015-09-03 | 2017-03-09 | 日本化薬株式会社 | カンプトテシン類高分子誘導体を含有する医薬組成物 |
-
2017
- 2017-02-20 AU AU2017226131A patent/AU2017226131A1/en not_active Abandoned
- 2017-02-20 CA CA3015459A patent/CA3015459A1/en not_active Abandoned
- 2017-02-20 KR KR1020187022546A patent/KR20180114027A/ko not_active Withdrawn
- 2017-02-20 RU RU2018129760A patent/RU2018129760A/ru unknown
- 2017-02-20 CN CN201780013411.6A patent/CN108697806A/zh active Pending
- 2017-02-20 US US16/078,303 patent/US20190046653A1/en not_active Abandoned
- 2017-02-20 EP EP17759722.6A patent/EP3424513A4/en not_active Withdrawn
- 2017-02-20 JP JP2018503048A patent/JP6797182B2/ja not_active Expired - Fee Related
- 2017-02-20 WO PCT/JP2017/006192 patent/WO2017150256A1/ja not_active Ceased
- 2017-02-23 TW TW106106163A patent/TW201731510A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP6797182B2 (ja) | 2020-12-09 |
| RU2018129760A3 (ru) | 2020-04-01 |
| WO2017150256A1 (ja) | 2017-09-08 |
| AU2017226131A1 (en) | 2018-10-04 |
| KR20180114027A (ko) | 2018-10-17 |
| CA3015459A1 (en) | 2017-09-08 |
| TW201731510A (zh) | 2017-09-16 |
| EP3424513A4 (en) | 2019-10-23 |
| EP3424513A1 (en) | 2019-01-09 |
| JPWO2017150256A1 (ja) | 2018-12-27 |
| US20190046653A1 (en) | 2019-02-14 |
| CN108697806A (zh) | 2018-10-23 |
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