HRP20231550T1 - Blok kopolimer koji sadrži hidrofilni prvi blok, hidrofobni drugi blok i funkcionalnu grupu sposobnu da se specifično vezuje za tiol - Google Patents
Blok kopolimer koji sadrži hidrofilni prvi blok, hidrofobni drugi blok i funkcionalnu grupu sposobnu da se specifično vezuje za tiol Download PDFInfo
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- HRP20231550T1 HRP20231550T1 HRP20231550TT HRP20231550T HRP20231550T1 HR P20231550 T1 HRP20231550 T1 HR P20231550T1 HR P20231550T T HRP20231550T T HR P20231550TT HR P20231550 T HRP20231550 T HR P20231550T HR P20231550 T1 HRP20231550 T1 HR P20231550T1
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- 229920001400 block copolymer Polymers 0.000 title claims 11
- 125000000524 functional group Chemical group 0.000 title claims 7
- 230000002209 hydrophobic effect Effects 0.000 title claims 3
- 125000003396 thiol group Chemical class [H]S* 0.000 title 1
- 125000002947 alkylene group Chemical group 0.000 claims 7
- 125000004450 alkenylene group Chemical group 0.000 claims 6
- 125000004419 alkynylene group Chemical group 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
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- 206010028980 Neoplasm Diseases 0.000 claims 4
- -1 anti-diabetics Substances 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
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Classifications
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- A61K9/513—Organic macromolecular compounds; Dendrimers
- A61K9/5146—Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
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- 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
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- 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
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- A61P35/00—Antineoplastic agents
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- C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
- C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
- C08G65/32—Polymers modified by chemical after-treatment
- C08G65/321—Polymers modified by chemical after-treatment with inorganic compounds
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- C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
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- C08G81/00—Macromolecular compounds obtained by interreacting polymers in the absence of monomers, e.g. block polymers
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Claims (8)
1. Blok kopolimer koji sadrži:
hidrofilni prvi blok;
hidrofobni drugi blok; i
funkcionalnu skupinu sposobnu da se specifično vezuje za tiol,
pri čemu hidrofobni drugi blok uključuje, u svom glavnom lancu, jedinicu koja se razlaže u uvjetima pH 4,5 do 7, uključuje, u svom glavnom ili bočnom lancu, jedinicu koja postaje katjonska u uvjetima pH 4,5 do 7, ili uključuje obje jedinice,
pri čemu je blok kopolimer predstavljen Formulom 5 i uključuje funkcionalnu skupinu sposobnu da se specifično vezuje za tiol:
[image]
u formuli,
A1 i A3 su svaki nezavisno izabrani od C1 do C5 linearne ili razgranate alkilen skupine; C2 do C5 linearne ili razgranate alkenilen skupine; i C2 do C5 linearne ili razgranate alkinilen skupine,
A2 je izabran od C1 do C10 linearne ili razgranate alkilen skupine; C2 do C10 linearne ili razgranate alkenilen skupine; i C2 do C10 linearne ili razgranate alkinilen skupine,
B1 i B3 su svaki nezavisno izabrani od C1 do C10 linearne ili razgranate alkilen skupine; C2 do C10 linearne ili razgranate alkenilen skupine; i C2 do C10 linearne ili razgranate alkinilen skupine,
B2 i B4 su svaki nezavisno izabrani od vodika; C1 do C10 linearne ili razgranate alkil skupine; C2 do C10 linearne ili razgranate alkenil skupine; C2 do C10 linearne ili razgranate alkinil skupine; C1 do C10 linearne ili razgranate alkilen skupine; C2 do C10 linearne ili razgranate alkenilen skupine; i C2 do C10 linearne ili razgranate alkinilen skupine,
pri čemu B1 i B2 mogu biti povezani jedan sa drugim da bi formirali C3 do C20 aliciklični ili aromatični prsten, i
B3 i B4 mogu biti povezani jedan sa drugim da bi formirali C3 do C20 aliciklični ili aromatični prsten,
D1 i D4 su svaki nezavisno C1 ili C2 alkilen skupina,
D2, D3, D5 i D6 su svaki nezavisno izabrani od vodika; halogena; hidroksilne skupine; i metil skupine,
L1 i L2 su povezivači, i
p, q i r su svaki nezavisno ceo broj od 1 do 100, opcionalno pri čemu (p + r)/q je (1:10) do (10:1) opcionalno pri čemu je L1 predstavljen Formulom 4, a L2 je predstavljen Formulom 6:
[image]
[image]
u formulama,
B1 i B3 su svaki nezavisno izabrani od C1 do C10 linearne ili razgranate alkilen skupine; C2 do C10 linearne ili razgranate alkenilen skupine; i C2 do C10 linearne ili razgranate alkinilen skupine,
B2 i B4 su svaki nezavisno izabrani od vodika; halogena; C1 do C10 linearne ili razgranate alkil skupine; C2 do C10 linearne ili razgranate alkenil skupine; C2 do C10 linearne ili razgranate alkinil skupine; C1 do C10 linearne ili razgranate alkilen skupine; C2 do C10 linearne ili razgranate alkenilen skupine; i C2 do C10 linearne ili razgranate alkinilen skupine, i
E1 i E2 su svaki nezavisno jedinica izvedena iz funkcionalne skupine sposobne da reagira sa aminom,
pri čemu B1 i B2 mogu biti povezani jedan sa drugim da bi formirali C3 do C20 aliciklični ili aromatični prsten, i
B3 i B4 mogu biti povezani jedan sa drugim da bi formirali C3 do C20 aliciklični ili aromatični prsten.
2. Blok kopolimer prema patentnom zahtjevu 1, pri čemu funkcionalna skupina sposobna da se specifično vezuje za tiol je sadržana u količini od 0,01 do 5% po masi, na osnovu ukupne mase blok kopolimera.
3. Blok kopolimer prema bilo kojem od prethodnih patentnih zahtjeva, pri čemu funkcionalna skupina sposobna da se specifično vezuje za tiol je izabrana od disulfidne skupine, maleimidne skupine, alkenil skupine, alkinil skupine i njihovih kombinacija, pri čemu opcionalno funkcionalna skupina sposobna da se specifično vezuje za tiol je povezana, direktno ili preko povezivača, za glavni lanac, bočni lanac ili kraj blok kopolimera, ili njihovu kombinaciju.
4. Blok kopolimer prema bilo kojem od prethodnih patentnih zahtjeva, pri čemu je blok kopolimer predstavljen Formulom 7:
[image]
[image]
pri čemu u formuli,
p i r su svaki nezavisno cijeli broj od 5 do 100, a q je cijeli broj od 1 do 60.
5. Nanočestica, koja sadrži blok kopolimer prema bilo kojem od prethodnih patentnih zahtjeva.
6. Vehikulum za isporuku lijeka, koji sadrži:
nanočesticu prema patentnom zahtjevu 5; i
lijek,
pri čemu je opcionalno lijek izabran od agensa protiv raka, antiproliferativnih ili kemoterapijskih lijekova, analgetskih agensa, antiinflamatornih agensa, antiparazitskih agensa, antiaritmičnih agensa, antibakterijskih agensa, antivirusnih agensa, antikoagulansa, antidepresiva, antidijabetika, antiepileptičkih agensa, antifungalnih agensa, agensa protiv gihta, antihipertenziva, antimalarika, antimigrenika, antimuskarinskih agensa, antineoplastičnih agensa, agensa protiv erektilne disfunkcije, imunosupresiva, antiprotozoika, anti-tiroidnih agensa, agensa protiv anksioznosti, sedativa, hipnotika, neuroleptika, β-blokatora, kardiotoničnih agensa, kortikosteroida, diuretika, agensa protiv Parkinsonove bolesti, gastrointestinalnih agensa, antagonista histaminskih receptora, keratolitičkih agensa, modulatora lipida, lijekova za anginu pektoris, inhibitora Cox-2, inhibitora leukotriena, makrolida, mišićnih relaksanasa, nutrijenata, narkotičkih analgetika, inhibitora proteaze, spolnih hormona, stimulanasa, mišićnih relaksanasa, antiosmotskih agensa, lijekova protiv gojaznosti, kognitivnih pojačivača, lijekova za urinarnu inkontinenciju, lijekova za benigne promjene prostate, esencijalnih masnih kiselina, neesencijalnih masnih kiselina i njihovih kombinacija.
7. Modificirana stanica, koja sadrži:
vehikulum za isporuku lijeka prema patentnom zahtjevu 6; i
imunsku stanicu pri čemu je opcionalno imunska stanica izabrana od T stanica, stanica prirodnih ubojica, dendritskih stanica (DC), makrofaga, mikroglijalnih stanica i njihovih kombinacija.
8. Farmaceutska kompozicija za primjenu u prevenciji ili liječenju raka ili infekcije, koja sadrži:
blok kopolimer prema bilo kojem od patentnih zahtjeva 1 do 4, nanočesticu prema patentnom zahtjevu 5 ili vehikulum za isporuku lijeka prema patentnom zahtjevu 6; i
bilo koje od lijeka i imunske stanice,
pri čemu je opcionalno rak izabran od raka debelog crijeva, raka pluća, raka pluća ne-malih stanica, raka kostiju, raka gušterače, raka kože, raka glave, cervikalnog raka, melanoma kože, intraokularnog melanoma, raka materice, raka jajnika, raka rektuma, raka želuca, perianalnog raka, raka dojke, karcinoma jajovoda, karcinoma endometrijuma, karcinoma grlića materice, vaginalnog karcinoma, karcinoma vulve, Hodgkinove bolesti, raka jednjaka, raka tankog crijeva, raka endokrinih žlijezda, raka tiroidne žlijezde, raka paratiroidne žlijezde, raka nadbubrežne žlijezde, sarkoma mekih tkiva, raka uretre, raka penisa, raka prostate, kronične leukemije, akutne leukemije, limfocitnog limfoma, raka mjehura, raka bubrega, raka uretera, karcinoma bubrežnih stanica, karcinoma bubrežne karlice, i tumora centralnog nervnog sistema (CNS).
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20180163379 | 2018-12-17 | ||
| PCT/KR2019/017899 WO2020130580A1 (ko) | 2018-12-17 | 2019-12-17 | 친수성 제1 블록, 소수성 제2 블록, 및 티올과 특이적으로 결합할 수 있는 작용기를 포함하는 블록 공중합체 |
| EP19900252.8A EP3900704B1 (en) | 2018-12-17 | 2019-12-17 | Block copolymer comprising hydrophilic first block, hydrophobic second block, and functional group capable of specifically binding to thiol |
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| HRP20231550T1 true HRP20231550T1 (hr) | 2024-05-10 |
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| US (1) | US20210346308A1 (hr) |
| EP (1) | EP3900704B1 (hr) |
| JP (2) | JP7265000B2 (hr) |
| KR (1) | KR102354882B1 (hr) |
| CN (2) | CN117159491A (hr) |
| AU (1) | AU2019407590B2 (hr) |
| CA (2) | CA3112314C (hr) |
| DK (1) | DK3900704T3 (hr) |
| ES (1) | ES2966163T3 (hr) |
| FI (1) | FI3900704T3 (hr) |
| HR (1) | HRP20231550T1 (hr) |
| HU (1) | HUE065015T2 (hr) |
| PL (1) | PL3900704T3 (hr) |
| PT (1) | PT3900704T (hr) |
| RS (1) | RS64992B1 (hr) |
| SI (1) | SI3900704T1 (hr) |
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| US5929177A (en) * | 1995-08-10 | 1999-07-27 | Kazunori Kataoka | Block polymer having functional groups at both ends |
| KR100574341B1 (ko) * | 2003-11-18 | 2006-04-26 | 학교법인 성균관대학 | 썰폰아마이드 이용 ｐＨ 민감성 블록공중합체의 제조 방법및 그에 의한 블록공중합체와 마이셀 |
| KR100732013B1 (ko) | 2005-03-18 | 2007-06-25 | 성균관대학교산학협력단 | ｐＨ 민감성 블록 공중합체 및 이를 이용한 고분자 마이셀 |
| KR100665672B1 (ko) | 2005-04-13 | 2007-01-09 | 성균관대학교산학협력단 | 새로운 온도 및 ｐＨ 민감성 블록 공중합체 및 이를 이용한고분자 하이드로겔 |
| WO2008105773A2 (en) * | 2006-03-31 | 2008-09-04 | Massachusetts Institute Of Technology | System for targeted delivery of therapeutic agents |
| WO2008124639A2 (en) | 2007-04-04 | 2008-10-16 | Massachusetts Institute Of Technology | Poly (amino acid) targeting moieties |
| KR20080095130A (ko) * | 2007-04-23 | 2008-10-28 | 한국과학기술연구원 | ｐＨ 민감성 블록공중합체를 이용한 약물전달체 제조 및응용 |
| KR100838809B1 (ko) | 2007-05-03 | 2008-06-17 | 성균관대학교산학협력단 | 겔강도가 우수한 온도 및 피에치 민감성 블록 공중합체 및이의 제조방법과 이를 이용한 약물전달체 |
| KR100941774B1 (ko) * | 2007-09-06 | 2010-02-11 | 성균관대학교산학협력단 | 인체안전성이 우수한 온도 및 피에치 민감성 블록공중합체및 이의 제조방법과 이를 이용한 약물전달체 |
| KR101586866B1 (ko) * | 2010-04-14 | 2016-01-21 | 가톨릭대학교 산학협력단 | 약물 전달을 위한 ｐＨ-민감성 나노입자 및 이의 제조방법 |
| WO2012040513A1 (en) * | 2010-09-22 | 2012-03-29 | The Board Of Regents Of The University Of Texas System | Compositions and methods for the delivery of beta lapachone |
| KR101386176B1 (ko) * | 2010-11-12 | 2014-04-18 | 성균관대학교산학협력단 | 피에이치 민감성 폴리머좀 및 이의 제조방법 |
| US9511152B2 (en) * | 2012-04-05 | 2016-12-06 | The Board Of Regents Of The University Of Texas System | Multicolored pH-activatable fluorescence nanoplatform |
| CN103316354A (zh) * | 2013-05-27 | 2013-09-25 | 上海纳米技术及应用国家工程研究中心有限公司 | 肿瘤靶向多肽-聚乙二醇-聚乳酸复合物及制备方法和应用 |
| KR101554703B1 (ko) * | 2014-02-21 | 2015-09-23 | 전북대학교산학협력단 | 벤조일옥시신남알데히드-폴리에틸렌글리콜 결합 마이셀에 아연 프로토포르피린을 담지한 pH 감응형 항암 전구약물 및 이의 제조방법 |
| CN107848957B (zh) * | 2015-07-22 | 2021-05-11 | 华上生技医药股份有限公司 | 递送治疗药物的ph-敏感性的连接物 |
| KR102023058B1 (ko) * | 2016-03-25 | 2019-09-19 | 사회복지법인 삼성생명공익재단 | 이중 이온 pH-민감성 공중합체를 이용한 허혈성 뇌질환 치료용 약물 전달체 |
| EP3530291A1 (en) * | 2018-02-27 | 2019-08-28 | Universite De Geneve | Bi-functionalizable amphiphilic diblock copolymers, conjugates and uses thereof |
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| AU2019407590A1 (en) | 2021-04-08 |
| PL3900704T3 (pl) | 2024-03-18 |
| EP3900704A4 (en) | 2022-02-09 |
| TWI726540B (zh) | 2021-05-01 |
| ES2966163T3 (es) | 2024-04-18 |
| RS64992B1 (sr) | 2024-01-31 |
| CN112955127B (zh) | 2024-02-27 |
| JP7265000B2 (ja) | 2023-04-25 |
| CN112955127A (zh) | 2021-06-11 |
| EP3900704A1 (en) | 2021-10-27 |
| KR20200074899A (ko) | 2020-06-25 |
| AU2019407590B2 (en) | 2022-08-04 |
| HUE065015T2 (hu) | 2024-04-28 |
| PT3900704T (pt) | 2023-11-27 |
| CA3206647A1 (en) | 2020-06-25 |
| WO2020130580A1 (ko) | 2020-06-25 |
| CN117159491A (zh) | 2023-12-05 |
| JP2023109749A (ja) | 2023-08-08 |
| EP3900704B1 (en) | 2023-11-01 |
| FI3900704T3 (fi) | 2023-11-30 |
| SI3900704T1 (sl) | 2024-01-31 |
| TW202039003A (zh) | 2020-11-01 |
| US20210346308A1 (en) | 2021-11-11 |
| KR102354882B1 (ko) | 2022-01-25 |
| DK3900704T3 (da) | 2023-12-04 |
| CA3112314C (en) | 2023-09-19 |
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